World Academy of Science, Engineering and Technology

Authors: Lamzira Ebralidze, Aleksandre Tsertsvadze, Dali Berashvili, Aliosha Bakuridze

Abstract:

Nowadays, there is an increasing demand for biologically active substances from vegetable, animal, and mineral resources. In terms of the use of natural compounds, pharmaceutical, cosmetic, and nutrition industry has big interest. The biggest drawback of conventional extraction methods is the need to use a large volume of organic extragents. The removal of the organic solvent is a multi-stage process. And their absolute removal cannot be achieved, and they still appear in the final product as impurities. A large amount of waste containing organic solvent damages not only human health but also has the harmful effects of the environment. Accordingly, researchers are focused on improving the extraction methods, which aims to minimize the use of organic solvents and energy sources, using alternate solvents and renewable raw materials. In this context, green extraction principles were formed. Green Extraction is a need of today’s environment. Green Extraction is the concept, and it totally corresponds to the challenges of the 21st century. The extraction of biologically active compounds based on green extraction principles is vital from the view of preservation and maintaining biodiversity. Novel technologies of green extraction are known, such as "cold methods" because during the extraction process, the temperature is relatively lower, and it doesn’t have a negative impact on the stability of plant compounds. Novel technologies provide great opportunities to reduce or replace the use of organic toxic solvents, the efficiency of the process, enhance excretion yield, and improve the quality of the final product. The objective of the research is the development of green technologies of flavonoids containing preparations. Methodology: At the first stage of the research, flavonoids containing preparations (Tincture Herba Leonuri, flamine, rutine) were prepared based on conventional extraction methods: maceration, bismaceration, percolation, repercolation. At the same time, the same preparations were prepared based on green technologies, microwave-assisted, UV extraction methods. Product quality characteristics were evaluated by pharmacopeia methods. At the next stage of the research technological - economic characteristics and cost efficiency of products prepared based on conventional and novel technologies were determined. For the extraction of flavonoids, water is used as extragent. Surface-active substances are used as co-solvent in order to reduce surface tension, which significantly increases the solubility of polyphenols in water. Different concentrations of water-glycerol mixture, cyclodextrin, ionic solvent were used for the extraction process. In vitro antioxidant activity will be studied by the spectrophotometric method, using DPPH (2,2-diphenyl-1- picrylhydrazyl) as an antioxidant assay. The advantage of green extraction methods is also the possibility of obtaining higher yield in case of low temperature, limitation extraction process of undesirable compounds. That is especially important for the extraction of thermosensitive compounds and maintaining their stability.

Keywords: extraction, green technologies, natural resources, flavonoids

Procedia PDF Downloads 105

Authors: Al. Tsertsvadze. L. Ebralidze, I. Matchutadze. D. Berashvili, A. Bakuridze

Abstract:

Peatlands are landscape elements, they are formed over a very long period by physical, chemical, biologic, and geologic processes. In the moderate zone of Caucasus, the Kolkheti lowlands are distinguished by the diversity of relictual plants, a high degree of endemism, orographic, climate, landscape, and other characteristics of high levels of biodiversity. The unique properties of the Kolkheti region lead to the formation of special, so-called, endemic peat peloids. The composition and properties of peloids strongly depend on peat-forming plants. Peat is considered a unique complex of raw materials, which can be used in different fields of the industry: agriculture, metallurgy, energy, biotechnology, chemical industry, health care. They are formed in permanent wetland areas. As a result of decay, higher plants remain in the anaerobic area, with the participation of microorganisms. Peat mass absorbs soil and groundwater. Peloids are predominantly rich with humic substances, which are characterized by high biological activity. Humic acids stimulate enzymatic activity, regenerative processes, and have anti-inflammatory activity. Objects of the research were Kolkheti peat peloids (Ispani, Anaklia, Churia, Chirukhi, Peranga) possessing different formation phases. Due to specific physical and chemical properties of research objects, the aim of the research was to develop analytical methods in order to study the chemical composition of the objects. The research was held using modern instrumental methods of analysis: Ultraviolet-visible spectroscopy and Infrared spectroscopy, Scanning Electron Microscopy, Centrifuge, dry oven, Ultraturax, pH meter, fluorescence spectrometer, Gas chromatography-mass spectrometry (GC-MS/MS), Gas chromatography. Based on the research ration between organic and inorganic substances, the spectrum of micro and macro elements, also the content of minerals was determined. The content of organic nitrogen was determined using the Kjeldahl method. The total composition of amino acids was studied by a spectrophotometric method using standard solutions of glutamic and aspartic acids. Fatty acid was determined using GC (Gas chromatography). Based on the obtained results, we can conclude that the method is valid to identify fatty acids in the research objects. The content of organic substances in the research objects was held using GC-MS. Using modern instrumental methods of analysis, the chemical composition of research objects was studied. Each research object is predominantly reached with a broad spectrum of organic (fatty acids, amino acids, carbocyclic and heterocyclic compounds, organic acids and their esters, steroids) and inorganic (micro and macro elements, minerals) substances. Modified methods used in the presented research may be utilized for the evaluation of cosmetological balneological and pharmaceutical means prepared on the base of Kolkheti's Sphagnum Peat Peloids.

Keywords: modern analytical methods, natural resources, peat, chemistry

Procedia PDF Downloads 104

Authors: Ismail Celik, Gulgun Ayhan Kilcigil, Berna Guven, Zumra Kara, Arzu Onay-Besikci

Abstract:

Epidermal Growth Factor Receptor is the cell-surface receptor of the ErbB (erythroblastic leukemia viral oncogene homologue receptors) family of tyrosine kinases. It plays a vital role in regulating the proliferation and differentiation of cells. However, a variety of mechanisms, such as EGFR expression, mutation, and ligand-dependent receptor dimerization, are associated with the development of various activated EGFR tumors. EGFR is highly expressed in most solid tumors, including breast, head and neck cancer, non-small cell lung cancer (NSCLC), renal, ovarian, and colon cancers. Thus, specific EGFR inhibition plays one of the key roles in cancer treatment. The compounds used in the treatment as tyrosine kinase inhibitors are known to contain the benzimidazole isosterium indole, pazopanib, and axitinibin indazole rings. In addition, benzimidazoles have been shown to exhibit protein kinase inhibitory activity in addition to their different biological activities.Based on these data, it was planned and synthesized of some oxadiazole bearing benzimidazole derivatives [N-cyclohexyl-5-((2-phenyl/substitutedphenyl-1H-benzo[d]imidazole-1-yl) methyl)-1,3,4-oxadiazole-2-amine]. EGFR kinase inhibitory efficiency of the synthesized compounds was determined by comparing them with a known kinase inhibitor erlotinib in vitro, and two of the compounds bearing phenyl (19a) and 3,4-dibenzyloxyphenyl (21a) ring exhibited significant activities.

Keywords: benzimidazole, EGFR kinase inhibitory, oxadiazole, synthesis

Procedia PDF Downloads 107

Authors: Sabah El-Sawalhi, Elie Fayad, Roula M. Abdel-Massih

Abstract:

Ilex paraguariensis (Yerba Mate) is a medium to large tree commonly consumed by South Americans. Its leaves and stems are associated with different biological activities. The purpose of this study was to evaluate the antibacterial activity of Yerba Mate against Gram-positive and Gram-negative bacterial strains and its action against some resistant bacteria with different resistance profiles. Yerba Mate aqueous extracts were prepared at 70°C for 2 hrs, and the microdilution method was used to determine the minimum inhibitory concentration (MIC). Gram-positive bacteria exhibited a stronger antibacterial activity (MIC ranged between 0.468 mg/mL and 15 mg/mL) than Gram-negative bacteria. Yerba Mate was also extracted with acetone: water (1:1) and then further sub-fractionated with hexane, chloroform, and ethyl acetate. MIC values against Staphylococcus aureus ranged from 0.78 to 2.5 mg/ml for the chloroform fraction, from 1.56 to 3.75 mg/ml for the ethyl acetate fraction, and 0.78 to 1.87 mg/ml for the water fraction. The water fraction also exhibited antibacterial activity against Salmonella species (MIC ranged from 1.56 mg/ml to 3.12 mg/ml). The water fraction exhibited the highest antibacterial activity among all the fractions obtained. More studies are needed to determine the molecule or molecules responsible for this activity.

Keywords: antibacterial activity, bacterial resistance, minimum inhibitory concentration, yerba mate

Procedia PDF Downloads 109

Authors: Arojojoye Oluwatosin Adetola, Nwaechefu Olajumoke Olufunlayo, Ademola Adetokunbo Oyagbemi, Jeremiah Moyinoluwalogo Afolabi, Asaolu Racheal Oluwabukola

Abstract:

The effects of man’s activities on the environment include depletion of natural resources alongside pollution of water bodies. Petroleum exploration in the Niger Delta region of Nigeria has compromised the aquatic environment with grave consequences on the entire ecosystem. In this study, we assessed the environmental safety of Araromi River, located in an oil-producing area in Ondo State, in the Niger Delta region of Nigeria by determining the levels of heavy metals (copper, cadmium, chromium, nickel, lead) and some biomarkers of oxidative stress (malondialdehyde, glutathione-S-transferase, glutathione peroxidase, catalase, superoxide dismutase, myeloperoxidase and reduced glutathione) in Clarias gariepinus (350-400g) from the river using standard methods. Clarias gariepinus from a clean fish farm in the same geographical location as the reference site (Ilesannmi fishery) was used as a control. Water samples from both sites were also analysed for some physicochemical parameters, heavy metals, and bacterial contamination. Our findings show a significant increase in malondialdehyde level (index of lipid peroxidation) as well as alterations in antioxidant status in the organs of Clarias gariepinus from Araromi River compared with control. A significant increase in bacterial contaminants, heavy metal pollutants, and particulate matter deposits were also observed in the water sample from Araromi River compared with control. In conclusion, high levels of indicators of environmental pollution observed in the water sample from Araromi River coupled with induction of oxidative stress in Clarias gariepinus from the river show that Araromi River is polluted; therefore, consumption of fishes and other aquatic organisms from the river may be unsafe for the people in that community.

Keywords: Araromi River, Clarias gariepinus, environmental pollution, heavy metals, oxidative stress

Procedia PDF Downloads 133

Authors: Prosper Kudzanai Mushauri

Abstract:

In issues of anomalous experiences commonly referred to as madness or mental illness, attempts have been made to deal with it so that people manage to live their lives in a more functional way. It is in this stance that psychiatry has sort of portraying itself as seeking to ameliorate perturbations which individuals live with via nosological systems and use of medicine to anomalous experiences. It is from this hegemony that has led to the untold harm which people living with madness have endured from antique to contemporary life. The paper reflects via a literature review on the history of psychiatry and argues that it is akin to contemporary psychiatry to be involved in iatrogenic acts. As antique psychiatry meddled with gory issues of inhumanity, deceit and mass murders which some of those the contemporary psychiatry has not weaned itself from such diabolical acts. The objective of the paper is to suggest to psychiatry that it has not comported to the mores of psychological ethics. In doing this, the paper hopes that psychiatry will reflect and reform its curricular and praxis so that it comports to ethical standards in psychological science in ameliorating anomalous experiences.

Keywords: nosology, psychiatry, madness, diagnosis, eugenics

Procedia PDF Downloads 133

Authors: Taiwo O. Margaret, Olaoluwa O. Olaoluwa

Abstract:

Moraceae family has immense phytochemical constituents and significant pharmacological properties, hence have great medicinal values. The aim of this study was to screen and quantify phytochemicals as well as the antioxidant activities of the leaf and stem bark extracts and fractions (crude ethanol extracts, n-hexane, ethyl acetate and aqueous ethanol fractions) of Ficus sagittifolia. Leaf and stem bark of F. sagittifolia were extracted by maceration method using ethanol to give ethanol crude extract. The ethanol crude extract was partitioned by n-hexane and ethyl-acetate to give their respective fractions. All the extracts were screened for their phytochemicals using standard methods. The total phenolic, flavonoid, tannin, saponin contents and antioxidant activity were determined by spectrophotometric method while the alkaloid content was evaluated by titrimetric method. The amount of total phenolic in extracts and fractions were estimated in comparison to gallic acid, whereas total flavonoids, tannins and saponins were estimated corresponding to quercetin, tannic acid and saponin respectively. 2, 2-diphenylpicryl hydrazyl radical (DPPH)* and phosphomolybdate methods were used to evaluate the antioxidant activities of leaf and stem bark of F. sagittifolia. Phytochemical screening revealed the presence of flavonoids, saponins, terpenoids/steroids, alkaloids for both extracts of leaf and stem bark of F. sagittifolia. The phenolic content of F. sagittifolia was most abundant in leaf ethanol crude extract as 3.53 ± 0.03 mg/g equivalent of gallic acid. Total flavonoids and tannins content were highest in stem bark aqueous ethanol fraction of F. sagittifolia estimated as 3.41 ± 0.08 mg/g equivalent of quercetin and 1.52 ± 0.05 mg/g equivalent of tannic acid respectively. The hexane leaf fraction of F. sagittifolia had the utmost saponin and alkaloid content as 5.10 ± 0.48 mg/g equivalent of saponins and 0.171 ± 0.39 g of alkaloids. Leaf aqueous ethanol fraction of F. sagittifolia showed high antioxidant activity (IC₅₀ value of 63.092 µg/mL) and stem ethanol crude extract (227.43 ± 0.78 mg/g equivalent of ascorbic acid) for DPPH and phosphomolybdate method respectively and the least active was found to be the stem hexane fraction using both methods (313.32 µg/mL; 16.21 ± 1.30 mg/g equivalent of ascorbic acid). The presence of these phytochemicals in the leaf and stem bark of F. sagittifolia are responsible for their therapeutic importance as well as the ability to scavenge free radicals in living systems.

Keywords: Moraceae, Ficus sagittifolia, phytochemicals, antioxidant

Procedia PDF Downloads 186

Authors: Pankaj Prashar, Bimlesh Kumar, Ankita Sood, Anamika Gautam

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Pharmacovigilance (PV) is a rapidly growing discipline in pharmaceutical industries as an integral part of clinical research and drug development over the past few decades. PV carries a breadth of scope from drug manufacturing to its regulation with safer utilization. The fundamental steps of PV not only includes data collection and verification, coding of drugs with adverse drug reactions, causality assessment and timely reporting to the authorities but also monitoring drug manufacturing, safety issues, product quality and conduction of due diligence. Standardization of adverse event information, collaboration of multiple departments in different companies, preparation of documents in accordance to both governmental as well as non-governmental organizations (FDA, EMA, GVP, ICH) are the advancements in discipline of PV. De-harmonization, lack of predictive drug safety models, improper funding by government, non-reporting, and non-acceptability of ADRs by developing countries and reports directly from patients to the monitoring centres respectively are the major road backs of PV. Mandatory pharmacovigilance reporting, frequent inspections, funding by government, educating and training medical students, pharmacists and nurses in this segment can bring about empowerment in PV. This area needs to be addressed with a sense of urgency for the safe utilization of pharmaceuticals.

Keywords: pharmacovigilance, regulatory, adverse event, drug safety

Procedia PDF Downloads 83

Authors: Nadia H. Mohammed, Anmar Al-Taie, Fadia H. Al-Sultany

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Although breast cancer prevalence continues to increase, mortality has been decreasing as a result of early detection and improvement in adjuvant systemic therapy. Nevertheless, this disease required further efforts to understand and identify the associated potential risk factors that could play a role in the prevalence of this malignancy among Iraqi women. The objective of this study was to assess the perception of certain predictive risk factors on the prevalence of breast cancer types among a sample of Iraqi women diagnosed with breast cancer. This was a retrospective observational study carried out at National Cancer Research Center in College of Medicine, Baghdad University from November 2017 to January 2018. Data of 100 patients with breast cancer whose biopsies examined in the National Cancer Research Center were included in this study. Data were collected to structure a detailed assessment regarding the patients’ demographic, medical and cancer records. The majority of study participants (94%) suffered from ductal breast cancer with mean age 49.57 years. Among those women, 48.9% were obese with body mass index (BMI) 35 kg/m². 68.1% of them had positive family history of breast cancer and 66% had low parity. 40.4% had stage II ductal breast cancer followed by 25.5% with stage III. It was found that 59.6% and 68.1% had positive oestrogen receptor sensitivity and positive human epidermal growth factor (HER2/neu) receptor sensitivity respectively. In regard to the impact of prediction of certain variables on the incidence of ductal breast cancer, positive family history of breast cancer (P < 0.0001), low parity (P< 0.0001), stage I and II breast cancer (P = 0.02) and positive HER2/neu status (P < 0.0001) were significant predictive factors among the study participants. The results from this study provide relevant evidence for a significant positive and potential association between certain risk factors and the prevalence of breast cancer among Iraqi women.

Keywords: Ductal Breast Cancer, Hormone Sensitivity, Iraq, Risk Factors

Procedia PDF Downloads 107

Authors: Zahraa Albasry, Hadeel D. Najim, Anmar Al-Taie

Abstract:

Background: Hypertension is considered as one of the most important causes of cardiovascular complications and one of the leading causes of worldwide mortality. Identifying the potential risk factors associated with this medical health problem plays an important role in minimizing its incidence and related complications. The objective of this study is to explore the prevalence of receptor sensitivity regarding assess and understand the perception of specific predictive confounding factors on the prevalence of hypertension (HT) among a sample of Iraqi population in Baghdad, Iraq. Materials and Methods: A randomized cross sectional study was carried out on 100 adult subjects during their visit to the outpatient clinic at a certain sector of Baghdad Province, Iraq. Demographic, clinical and health records alongside specific screening and laboratory tests of the participants were collected and analyzed to detect the potential of confounding factors on the prevalence of HT. Results: 63% of the study participants suffered from HT, most of them were female patients (P < 0.005). Patients aged between 41-50 years old significantly suffered from HT than other age groups (63.5%, P < 0.001). 88.9% of the participants were obese (P < 0.001) and 47.6% had diabetes with HT. Positive family history and sedentary lifestyle were significantly higher among all hypertensive groups (P < 0.05). High salt and fatty food intake was significantly found among patients suffered from isolated systolic hypertension (ISHT) (P < 0.05). A significant positive correlation between packed cell volume (PCV) and systolic blood pressure (SBP) (r = 0.353, P = 0.048) found among normotensive participants. Among hypertensive patients, a positive significant correlation found between triglycerides (TG) and both SBP (r = 0.484, P = 0.031) and diastolic blood pressure (DBP) (r = 0.463, P = 0.040), while low density lipoprotein-cholesterol (LDL-c) showed a positive significant correlation with DBP (r = 0.443, P = 0.021). Conclusion: The prevalence of HT among Iraqi populations is of major concern. Further consideration is required to detect the impact of potential risk factors and to minimize blood pressure (BP) elevation and reduce the risk of other cardiovascular complications later in life.

Keywords: Correlation, Hypertension, Iraq, Risk factors

Procedia PDF Downloads 106

Authors: Pimpak Phumat, Sakornrat Khongkhunthian, Thomas Rades, Anette Müllertz, Siriporn Okonogi

Abstract:

Self-nanoemulsifying drug delivery systems (SNEDDS) containing 4-allylpyrocatechol (AP) extracted from Piper betle were developed to enhance water solubility of AP by using modeling and design (MODDE) program. The amount of AP in each SNEDDS formulation was determined by using high-performance liquid chromatography. The formulation consisted of 20% Miglyol®812N, 40 % Kolliphor®RH40, 30 % Maisine®35-1 and 10 % ethanol was found to be the best SNEDDS that provided the highest loading capacity of AP. (141.48±15.64 mg/g SNEDDS). The system also showed miscibility with water. The particle shape and size of the AP-SNEDDS after dispersing in water was investigated by using a transmission electron microscope and photon correlation spectrophotometer, respectively. The results showed that they were a spherical shape, having a particle size of 34.27 ± 1.14 nm with a narrow size distribution of 0.17 ± 0.04. The particles showed negative zeta potential with a value of -21.66 ± 2.09 mV. Antibacterial activity of AP-SNEDDS containing 1.5 mg/mL of AP was investigated against Streptococcus intermedius. The effect of this system on S. intermedius cells was observed by a scanning electron microscope (SEM). The results from SEM revealed that the bacterial cells were obviously destroyed. Killing kinetic study of AP-SNEDDS was carried out. It was found that the killing rate of AP-SNEDDS against S. intermedius was dose-dependent and the bacterial reduction was 79.86 ± 0.45 % within 30 min. In comparison with chlorhexidine (CHX), AP-SNEDDS showed similar antibacterial effects against S. intermedius. It is concluded that SNEDDS is a potential system for enhancing water solubility of AP. The antibacterial study reveals that AP-SNEDDS can be a promising system to treat bacterial infection caused by S. intermedius.

Keywords: SNEDDS, 4-allylpyrocathecol, solubility, antibacterial activity, Streptococcus intermedius

Procedia PDF Downloads 90

Authors: Siriporn Okonogi, Pimpak Phumat, Sakornrat Khongkhunthian

Abstract:

Piper betle has been extensively reported for various pharmacological effects including antimicrobial activity. 4-Allylpyrocatechol (AC) is a principle active compound found in P. betle. However, AC has a problem of solubility in water. The aims of the present study were to prepare AC loaded polymeric micelles for enhancing its water solubility and to evaluate its anti-biofilm activity against oral phathogenic bacteria. AC was loaded in polymeric micelles (PM) of Pluronic F127 by using thin film hydration method to obtain AC loaded PM (PMAC). The results revealed that AC in the form of PMAC possessed high water solubility. PMAC particles were characterized using a transmission electron microscope and photon correlation spectroscopy. Determination of entrapment efficiency (EE) and loading capacity (LC) of PMAC was done by using high-performance liquid chromatography. The highest EE (86.33 ± 14.27 %) and LC (19.25 ± 3.18 %) of PMAC were found when the weight ratio of polymer to AC was 4 to 1. At this ratio, the particles showed spherical in shape with the size of 38.83 ± 1.36 nm and polydispersity index of 0.28 ± 0.10. Zeta potential of the particles is negative with the value of 16.43 ± 0.55 mV. Crystal violet assay and confocal microscopy were applied to evaluate the effects of PMAC on Streptococcus mutans biofilms using chlorhexidine (CHX) as a positive control. PMAC contained 1.5 mg/mL AC could potentially inhibit (102.01 ± 9.18%) and significantly eradicate (85.05 ± 2.03 %) these biofilms (p < 0.05). Comparison with CHX, PMAC showed slightly similar biofilm inhibition but significantly stronger biofilm eradication (p < 0.05) than CHX. It is concluded that PMAC can enhance water solubility and anti-biofilm activity of AC.

Keywords: pluronic, polymeric micelles, solubility, 4-allylpyrocathecol, Streptococcus mutans, anti-biofilm

Procedia PDF Downloads 107

Authors: N. Zandi, M. Sitarz, J. Jastrzebski, M. Vagheian, J. Choinski, A. Stolarz, A. Trzcinska

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¹³⁵La with the half-life of 19.5 h can be considered as a good candidate for Auger therapy. ¹³⁵La decays almost 100% by electron capture to the stable ¹³⁵Ba. In this study, all important possible reactions leading to ¹³⁵La production are investigated in details, and the corresponding theoretical yield for each reaction using the Monte-Carlo method (MCNPX code) are presented. Among them, the best reaction based on the cost-effectiveness and production yield regarding Poland facilities equipped with medical cyclotron has been selected. ¹³⁵La is produced using 16.5 MeV proton beam of general electric PET trace cyclotron through the ¹³⁵Ba(p,n)¹³⁵La reaction. Moreover, for a consistent facilitating comparison between the theoretical calculations and the experimental measurements, the beam current and also the proton beam energy is measured experimentally. Then, the obtained proton energy is considered as the entrance energy for the theoretical calculations. The production yield finally is measured and compared with the results obtained using the MCNPX code. The results show the experimental measurement and the theoretical calculations are in good agreement.

Keywords: efficient ¹³⁵La production, proton cyclotron energy measurement, MCNPX code, theoretical and experimental production yield

Procedia PDF Downloads 108

Authors: Iman A. A. Kassem, Ayman A. Farghaly, Zeinab M. Hassan, Farouk R. Melek, Neveen S. Ghaly

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Lipidium sativum L, an annual herb that grows to 50 cm, is known as an important member of family Brassicaceae. Besides its nutritional value, the seeds were widely used in folk medicine for treatment of cough, asthma, and headache. It was also reported to possess hypocholesterolemic, anti-inflammatory, antidiarrheal, antimicrobial and anticancer activities. In this study, the genoprotective properties of L. sativum seed methanolic extract (LSME) were evaluated in vivo. Three groups of mice were given LSME for five consecutive days at the three dose levels 25, 50 and 100 mg/kg b.wt. The three groups were then injected intraperitoneally with cyclophosphamide at a dose of 20 mg/kg b.wt. to induce DNA damage. A group received only cyclophosphamide (20 mg/kg b.wt.) served as control. LSME significantly inhibited the DNA aberrations in mice caused by cyclophosphamide in a dose-dependent manner in the two groups that received LSME at 50 and 100 mg/kg b.wt. dose levels. The chromosomal aberrations' inhibitory indices were calculated as 18 and 31 in mice bone marrow cells and 27 and 48 in mice spermatocytes, respectively. Phytochemical examination carried out by us revealed that flavonoids were the main chemical constituents of LSME. The major flavonoids kaempferol, kaempferol-3-O-rhamnoside, kaempferol-3-O-glucoside, quercetin, and quercetin-3-O-glucoside were isolated and characterized. It was concluded that the genoprotective effect of LSME might be attributed to the presence of flavonoids which are well-known for their antioxidant properties.

Keywords: cyclophosphamide, flavonoids, genoprotective effect, Lepidium sativum

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Authors: Manjunatha Bangeppagari, Lee Sang Joon

Abstract:

Recently, graphene-related nanomaterials are receiving fast-increasing attention with augmented applications in various fields. Especially, graphene-related materials have been widely applied to the biomedical field in the past years. In the present study, we evaluated the adverse effects of pristine graphene (pG) in zebrafish (Danio rerio) embryos in various aspects, such as mortality rate, heart rate, hatching rate, cardiotoxicity, cardiovascular defect, cardiac looping, apoptosis, and globin expression. For various trace concentrations of pG (1, 5, 10, 15, 20, 25, 30, 35, 40, 45, and 50 μg/L), early life-stage parameters were observed at 24, 48, 72, and 96 hpf. As a result, pG induces significant developmental defects including yolk sac edema, pericardial edema, embryonic mortality, delayed hatching, heartbeat, several morphological defects, pericardial toxicity, and bradycardia. Moreover, the exposure to pG was found to be a potential risk factor to the cardiovascular system of zebrafish embryos. However, further study on their properties which vary according to production methods and surface functionalization is essentially required. In addition, the possible risks of pG flakes to aquatic animals, and public health should be evaluated before releasing them to the surrounding environment.

Keywords: apoptosis, cardiovascular toxicity, globin expression, pristine graphene, zebrafish embryos

Procedia PDF Downloads 109

Authors: Bassant M. M. Ibrahim, Doha H. Abou Baker, Ahmed Abd Elghafour

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Excessive exposure to heavy metals contributes to the occurrence of deleterious health problems that affect vital organs like the brain, liver, kidneys, and heart. The use of natural products that have antioxidant capabilities may contribute to the protection of these organs. In the present study, the essential oil of summer savory (Satureja hortensis) was used to evaluate its protective effects against lead acetate induced damaging effect on rats’ vital organs, due to its high contents of carvacrol, y-terpinene, and p-cymene. Forty female Wister Albino rats were classified into five equal groups, the 1st served as normal group, the 2nd served as positive control group was given lead acetate (60 mg/kg) intra-peritoneal (IP), the third to fifth groups were treated with calcium disodium (EDTA) as chelating agent and summer savory essential oil in doses of (50 and 100mg/kg) respectively. All treatments were given IP concomitant with lead acetate for ten successive days. At the end of the experiment duration electrocardiogram (ECG), an open field test for the evaluation of psychological state, rotarod test as for the evaluation of locomotor coordination ability as well as anti-inflammatory and oxidative stress biomarkers in serum and histopathology of vital organs were performed. The investigations in this study show that the protective effect of high dose of summer savory essential oil is more than the low dose and that the essential oil of summer savory is a promising agent that can contribute to the protection of vital organs against the hazardous damaging effects of lead acetate.

Keywords: brain, heart, kidneys, lead acetate, liver, protective, summer savory

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Authors: Parul Grover, K. A. Suri, Raj Kumar, Gulshan Bansal

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Background: Nyctanthes arbortristis Linn is traditionally used as anticancer herb in Indian system of medicine, but its introduction into modern system of medicine is still awaited due to lack of systematic scientific studies. Objective: The objective of the present study was to isolate and characterize anticancer phytoconstituents from N. arbortristis L. leaves based on bioactivity guided fractionation. Method: Different extracts of the leaves of the plant were prepared by Soxhlet extractor. Each extract was evaluated for anticancer activity against HL-60 cell lines. Chloroform and HA extract showed potent anticancer activity and hence were selected for fractionation. Fraction C1 from chloroform extract was found to be most potent amongst all when tested against three cell lines (HL-60, A-549, and HCT-116) and thus was selected for further fractionation and a pure compound CP-01 was isolated. RP-HPLC method has been developed for quantification of isolated compound by using Kinetex C-18 column with gradient elution at 0.7 mL/min using mobile phase containing potassium dihydrogen phosphate (0.01 M, pH 3.0) with acetonitrile. The wavelength of maximum absorption (λₘₐₓ) selected was 210 nm. Results: The structure of potent anticancer CP-01 was determined on the basis spectroscopic methods like IR, 1H-NMR, ¹³C-NMR and Mass Spectrometry and it was characterized as 1,1,2-tris(2’,4’-di-tert-butylbenzene)-4,4-dimethyl-pent-1-ene. The content of CP-01 was found to be 0.88 %w/w of chloroform extract and 0.08 %w/w of N.arbortristis leaves. Conclusion: The study supports the traditional use of N. arbortristis as anticancer herb & the identified compound CP-01 can serve as an excellent lead to develop potent and safe anticancer drugs.

Keywords: anticancer, HL-60 cell lines, Nyctanthes arbor-tristis, RP-HPLC

Procedia PDF Downloads 106

Authors: Tatjana Kadifkova Panovska, Svetlana Kulevanova, Blagica Jovanova

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Biological systems possess the ability to neutralize the excess of reactive oxygen species (ROS) and to protect cells from destructive alterations. However, many pathological conditions (cardiovascular diseases, autoimmune disorders, cancer) are associated with inflammatory processes that generate an excessive amount of reactive oxygen species (ROS) that shift the balance between endogenous antioxidant systems and free oxygen radicals in favor of the latter, leading to oxidative stress. Therefore, an additional source of natural compounds with antioxidant properties that will reduce the amount of ROS in cells is much needed despite their broad utilization; many plant species remain largely unexplored. Therefore, the purpose of the present study is to investigate the antioxidant activity of twenty-five selected medicinal and aromatic plant species. The antioxidant activity of the ethanol extracts was evaluated with in vitro assays: 2,2’-diphenyl-1-pycryl-hydrazyl (DPPH), ferric reducing antioxidant power (FRAP), non-site-specific- (NSSOH) and site-specific hydroxyl radical-2-deoxy-D-ribose degradation (SSOH) assays. The Folin-Ciocalteu method and AlCl3 method were performed to determine total phenolic content (TPC) and total flavonoid content (TFC). All examined plant extracts manifested antioxidant activity to a different extent. Cinnamomum verum J.Presl bark and Ocimum basilicum L. Herba demonstrated strong radical scavenging activity and reducing power with the DPPH and FRAP assay, respectively. Additionally, significant hydroxyl scavenging potential and metal chelating properties were observed using the NSSOH and SSOH assays. Furthermore, significant variations were determined in the total polyphenolic content (TPC) and total flavonoid content (TFC), with Cinnamomum verum and Ocimum basilicum showing the highest amount of total polyphenols. The considerably strong radical scavenging activity, hydroxyl scavenging potential and reducing power for the species mentioned above suggest of a presence of highly bioactive phytochemical compounds, predominantly polyphenols. Since flavonoids are the most abundant group of polyphenols that possess a large number of available reactive OH groups in their structure, it is considered that they are the main contributors to the radical scavenging properties of the examined plant extracts. This observation is supported by the positive correlation between the radical scavenging activity and the total polyphenolic and flavonoid content obtained in the current research. The observations from the current research nominate Cinnamomum verum bark and Ocimum basilicum herba as potential sources of bioactive compounds that could be utilized as antioxidative additives in the food and pharmaceutical industries. Moreover, the present study will help the researchers as basic data for future research in exploiting the hidden potential of these important plants that have not been explored so far.

Keywords: ethanol extracts, radical scavenging activity, reducing power, total polyphenols.

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Authors: Yuliya Y. Gavrichenko

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Background and Aims: The increasing bacterial resistance to almost all the available antibiotics has encouraged scientists to search for alternative sources of antibacterial agents. Nowadays, it is known that many plant secondary metabolites have diverse biological activity. These compounds can be potentially active against human bacterial and viral infections. Extended research has been carried out to explore the use of the luminescent bacterial test as a rapid, accurate and inexpensive method to assess the antibacterial properties and to predict the biological activity spectra for plant origin substances. Method: Botanical material of fifteen species was collected from their natural and cultural habitats on the Crimean peninsula. The aqueous extracts of following plants were tested: Robinia pseudoacacia L., Sideritis comosa, Cotinus coggygria Scop., Thymus serpyllum L., Juglans regia L., Securigera varia L., Achillea millefolium L., Phlomis taurica, Corylus avellana L., Sambucus nigra L., Helichrysum arenarium L., Glycyrrhiza glabra L., Elytrigia repens L., Echium vulgare L., Conium maculatum L. The test was carried out using luminous strains of marine bacteria Photobacterium leiognathi, which was isolated from the Sea of Azov as well as four Escherichia coli MG1655 recombinant strains harbouring Vibrio fischeri luxCDABE genes. Results: The bactericidal capacity of plant extracts showed significant differences in the study. Cotinus coggygria, Phlomis taurica, Juglans regia L. proved to be the most toxic to P. leiognathi. (EC50 = 0.33 g dried plant/l). Glycyrrhiza glabra L., Robinia pseudoacacia L., Sideritis comosa and Helichrysum arenarium L. had moderate inhibitory effects (EC50 = 3.3 g dried plant/l). The rest of the aqueous extracts have decreased the luminescence of no more than 50% at the lowest concentration (16.5 g dried plant/l). Antibacterial activity of herbal extracts against constitutively luminescent E. coli MG1655 (pXen7-lux) strain was observed at approximately the same level as for P. leiognathi. Cotinus coggygria and Conium maculatum L. extracts have increased light emission in the mutant E. coli MG1655 (pFabA-lux) strain which is associated with cell membranes damage. Sideritis comosa, Phlomis taurica, Juglans regia induced SOS response in E. coli (pColD-lux) strain. Glycyrrhiza glabra L. induced protein damage response in E. coli MG1655 (pIbpA-lux) strain. Conclusion: The received results have shown that the plants’ extracts had nonspecific antimicrobial effects against both E. coli (pXen7-lux) and P. leiognathi biosensors. Mutagenic, cytotoxic and protein damage effects have been observed. In general, the bioluminescent inhibition test result correlated with the traditional use of screened plants. It leads to the following conclusion that whole-cell luminescent biosensors could be the indicator of overall plants antibacterial capacity. The results of the investigation have shown a possibility of bioluminescent method in medicine and pharmacy as an approach to research the antibacterial properties of medicinal plants.

Keywords: antibacterial property, bioluminescence, medicinal plants, whole-cell biosensors

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Authors: Alma Ramić, Mirjana Skočibušić, Renata Odžak, Tomica Hrenar, Ines Primožič

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In an attempt to identify a new class of antimicrobial agents, the antimicrobial potential of Cinchona alkaloid derivatives was evaluated. The bark of the Cinchona trees is the source of a variety of alkaloids, among which the best known are quinine, quinidine, cinchonine and cinchonidine. They are very useful as organocatalysts in stereoselective synthesis. On the other hand, quinine is traditionally used in the treatment of malaria. Furthermore, Cinchona alkaloids possess various analgesic, anti-inflammatory and anti–arrhythmic properties as well. In this work we present the synthesis of twenty quaternary derivatives of pseudo−enantiomeric Cinchona alkaloid derivatives to evaluate their antibacterial activity. Quaternization of quinuclidine moiety was carried out with groups diverse in their size. The structures of compounds were systematically modified to obtain drug-like properties with proper physical and chemical properties and avoiding toxophore. All compounds were prepared in good yields and were characterized by standard analytical spectroscopy methods (1D and 2D NMR, IR, MS). The antibacterial activities of all compounds were evaluated against series of recent clinical isolates of antibiotic susceptible Gram-positive and resistant Gram-negative pathogens by determining their zone of inhibition and minimum inhibitory concentrations. All compounds showed good to strong broad-spectrum activity, equivalent or better in comparison with standard antibiotics used. Furthermore, seven compounds exhibited significant antibacterial efficiency against Gram-negative isolates. To visualize the results, principal component analysis was used as an additional classification tool. Cytotoxicity of compounds with different cell lines in human cell culture was determined. Based on these results, substituted quaternary Cinchona scaffold can be considered as promising new class of antimicrobials and further investigations should be performed. Supported by Croatian Science Foundation, Project No 3775 ADESIRE.

Keywords: antibacterial efficiency, cinchona alkaloids, cytotoxicity, pseudo‐enantiomers

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Authors: Nagasamy Venkatesh Dhandapani

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This work aims at investigating the use of β-Cyclodextrin as a cross linker, in an attempt to formulate nanosponges containing ketoconazole. The nanosponges were prepared by cross-linking method. The excipients used in this study did not alter the physicochemical properties of a drug as revealed by FTIR spectroscopy. Studies on various formulation variables revealed that all the variables are inter-related with the formulation. The ideal batch among the formulation was selected based on the higher entrapment efficiency and drug loading. The in vitro release studies of ketoconazole nanosponges in hydrogel exhibited a sustained release over a period of 24 hours. Mathematical analysis of drug release from the formulation followed non-Fickian diffusion obeying first order kinetics. The anti-fungal activity of the formulation exhibited better zone of inhibition when compared to pure drug (ketoconazole) against Tinea corporis.

Keywords: nanosponges, beta-cyclodextrin, ketoconazole, tinea corporis

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Authors: M. Miljkovic, A. Urakpo, M. Simic-Koumoutsaris

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Benefit-risk assessment (BRA) is a valuable tool that takes place in multiple stages during a medicine's lifecycle, and this assessment can be conducted in a variety of ways. The aim was to summarize current BRA methods used during approval decisions and in post-approval settings and to see possible future directions. Relevant reviews, recommendations, and guidelines published in medical literature and through regulatory agencies over the past five years have been examined. BRA implies the review of two dimensions: the dimension of benefits (determined mainly by the therapeutic efficacy) and the dimension of risks (comprises the safety profile of a drug). Regulators, industry, and academia have developed various approaches, ranging from descriptive textual (qualitative) to decision-analytic (quantitative) models, to facilitate the BRA of medicines during the product lifecycle (from Phase I trials, to authorization procedure, post-marketing surveillance and health technology assessment for inclusion in public formularies). These approaches can be classified into the following categories: stepwise structured approaches (frameworks); measures for benefits and risks that are usually endpoint specific (metrics), simulation techniques and meta-analysis (estimation techniques), and utility survey techniques to elicit stakeholders’ preferences (utilities). All these approaches share the following two common goals: to assist this analysis and to improve the communication of decisions, but each is subject to its own specific strengths and limitations. Before using any method, its utility, complexity, the extent to which it is established, and the ease of results interpretation should be considered. Despite widespread and long-time use, BRA is subject to debate, suffers from a number of limitations, and currently is still under development. The use of formal, systematic structured approaches to BRA for regulatory decision-making and quantitative methods to support BRA during the product lifecycle is a standard practice in medicine that is subject to continuous improvement and modernization, not only in methodology but also in cooperation between organizations.

Keywords: benefit-risk assessment, benefit-risk profile, product lifecycle, quantitative methods, structured approaches

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Authors: Ammar Ali Saleh Jaber, Amer Hayat Khan, Syed Azhar Syed Sulaiman

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Tuberculosis (TB) is considered as a major disease that affects daily activities and impairs health-related quality of life (HRQoL). The impact of TB on HRQoL can affect treatment outcome and may lead to treatment defaulting. Therefore, this study aims to evaluate the HRQoL of TB treatment lost to follow-up during and after treatment in Yemen. For this aim, this prospective study enrolled a total of 399 TB lost to follow-up patients between January 2011 and December 2015. By applying HRQoL criteria, only 136 fill the survey during treatment. Moreover, 96 were traced and fill out the HRQoL survey. All eight HRQol domains were categorized into the physical component score (PCS) and mental component score (MCS), which were calculated using QM scoring software. Results show that all lost to follow-up TB patients reported a score less than 47 for all eight domains, except general health (67.3) during their treatment period. Low scores of 27.9 and 29.8 were reported for emotional role limitation (RE) and mental health (MH), respectively. Moreover, the mental component score (MCS) was found to be only 28.9. The trace lost follow-up shows a significant improvement in all eight domains and a mental component score of 43.1. The low scores of 27.9 and 29.8 for role emotion and mental health, respectively, in addition to the MCS score of 28.9, show that severe emotional condition and reflect the higher depression during treatment period that can result to lost to follow-up. The low MH, RE, and MCS can be used as a clue for predicting future TB treatment lost to follow-up.

Keywords: Yemen, tuberculosis, health-related quality of life, Khat

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Authors: Siamak Shahidi, Nasrin Hashemi-Firouzi, Sara Soleimani-Asl, Alireza Komaki

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Introduction: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by progressive memory and cognitive performance. Recently, an involvement of the serotonergic system and their receptors are suspected in the AD progression. In the present behavioral study, the effects of BIMU (selective 5-HT4 receptor agonist) on cognition and memory in the rat model of AD was investigated. Material and Methods: The animal model of the AD was induced by intracerebroventricular (Icv) injection of amyloid beta (Aβ) in adult male Wistar rats. Animals were divided into experimental groups included control, sham, Aβ, Aβ +BIMU groups. The treatment substances were icv injected (1 μg/μL) for thirty consecutive days. Then, novel object recognition (NOR) and passive avoidance learning (PAL) tests were applied to investigate memory and cognitive performance. Results: Aβ decrease the discrimination index of NOR test. Also, it increases the time spent in the dark compartment during PAL test, as compared with sham and control groups. In addition, compared to Aβ groups, BIMU significantly increased the discrimination index of NOR test and decreased the time spent in the dark compartment of PAL test. Conclusion: These findings suggest that 5-HT4 receptor activation prevents progression of memory and cognitive impairment in a rat model of AD.

Keywords: Alzheimer disease, cognition, memory, serotonin receptors

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Authors: Tina Naser Torabi

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Prevalence of allergy is affected by different factors according to its base and seasonal weather changes, and it also needs various treatments.Although reasons of allergy existence are not clear but generally, allergens cause reaction between antigen and antibody because of their antigenic traits. In this state, allergens cause immune system to make mistake and identify safe material as threat, therefore function of immune system impaired because of histamine secretion. There are different reasons for allergy, but herbal reasons are on top of the list, although animal causes cannot be ignored. Important point is that allergenic compounds, cause making dedicated antibody, so in general every kind of allergy is different from the other one. Therefore, most of the plants in herbal allergenic category can cause various allergies for human beings, such as respiratory allergies, nutritional allergies, injection allergies, infection allergies, touch allergies, that each of them show different symptoms based on the reason of allergy and also each of them requires different prevention and treatment. Geographical condition is another effective factor in allergy. Seasonal changes, weather condition, herbal coverage variety play important roles in different allergies. It goes without saying that humid climate and herbal coverage variety in different seasons especially spring cause most allergies in human beings in Iran and India that are discussed in this article. These two countries are good choices for allergy prevalence because of their condition, various herbal coverage, human and animal factors. Hay fever is one of the allergies, although the reasons of its prevalence are unknown yet. It is one of the most popular allergies in Iran and India because of geographical, human, animal and herbal factors. Hay fever is on top of the list in these two countries. Significant point about these two countries is that herbal factor is the most important factor in prevalence of hay fever. Variety of herbal coverage especially in spring during herbal pollination is the main reason of hay fever prevalence in these two countries. Based on the research result of Pharmacognosy and Phytochemistry, pollination of some plants in spring is major reason of hay fever prevalence in these countries. If airborne pollens in pollination season enter the human body through air, they will cause allergic reactions in eyes, nasal mucosa, lungs, and respiratory system, and if these particles enter the body of potential person through food, they will cause allergic reactions in mouth, stomach, and other digestive systems. Occasionally, chemical materials produced by human body such as Histamine cause problems like: developing of nasal polyps, nasal blockage, sleep disturbance, risk of asthma developing, blood vasodilation, sneezing, eye tears, itching and swelling of eyes and nasal mucosa, Urticaria, decrease in blood pressure, and rarely trauma, anesthesia, anaphylaxis and finally death. This article is going to study the reasons of hay fever prevalence in Iran and India and presents prevention and treatment Method from Phytochemistry and Pharmocognocy point of view by using local natural products in these two countries.

Keywords: hay fever, India, Iran, natural treatment, phytochemistry

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Authors: Mustafa Malki, Ewan R. Pearson

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Tools utilized by health care practitioners to flag potential adverse drug reactions secondary to drug-drug interactions ignore individual genetic variation, which has the potential to markedly alter the severity of these interactions. To our best knowledge, there have been limited published studies on the impact of genetic variation on drug-drug interactions. Therefore, our aim in this project is the discovery of previously unrecognized, clinically important drug-drug-gene interactions (DDGIs) within the list of most commonly used drug combinations in the UK. The UKBB database was utilized to identify the top most frequently prescribed drug combinations in the UK with at least one route of interaction (over than 200 combinations were identified). We have recognised 37 common and unique interacting genes considering all of our drug combinations. Out of around 600 potential genetic variants found in these 37 genes, 100 variants have met the selection criteria (common variant with minor allele frequency ≥ 5%, independence, and has passed HWE test). The association between these variants and the use of each of our top drug combinations has been tested with a case-control analysis under the log-additive model. As the data is cross-sectional, drug intolerance has been identified from the genotype distribution as presented by the lower percentage of patients carrying the risky allele and on the drug combination compared to those free of these risk factors and vice versa with drug tolerance. In GoDARTs database, the same list of common drug combinations identified by the UKBB was utilized here with the same list of candidate genetic variants but with the addition of 14 new SNPs so that we have a total of 114 variants which have met the selection criteria in GoDARTs. From the list of the top 200 drug combinations, we have selected 28 combinations where the two drugs in each combination are known to be used chronically. For each of our 28 combinations, three drug response phenotypes have been identified (drug stop/switch, dose decrease, or dose increase of any of the two drugs during their interaction). The association between each of the three phenotypes belonging to each of our 28 drug combinations has been tested against our 114 candidate genetic variants. The results show replication of four findings between both databases : (1) Omeprazole +Amitriptyline +rs2246709 (A > G) variant in CYP3A4 gene (p-values and ORs with the UKBB and GoDARTs respectively = 0.048,0.037,0.92,and 0.52 (dose increase phenotype)) (2) Simvastatin + Ranitidine + rs9332197 (T > C) variant in CYP2C9 gene (0.024,0.032,0.81, and 5.75 (drug stop/switch phenotype)) (3) Atorvastatin + Doxazosin + rs9282564 (T > C) variant in ABCB1 gene (0.0015,0.0095,1.58,and 3.14 (drug stop/switch phenotype)) (4) Simvastatin + Nifedipine + rs2257401 (C > G) variant in CYP3A7 gene (0.025,0.019,0.77,and 0.30 (drug stop/switch phenotype)). In addition, some other non-replicated, but interesting, significant findings were detected. Our work also provides a great source of information for researchers interested in DD, DG, or DDG interactions studies as it has highlighted the top common drug combinations in the UK with recognizing 114 significant genetic variants related to drugs' pharmacokinetic.

Keywords: adverse drug reactions, common drug combinations, drug-drug-gene interactions, pharmacogenomics

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Authors: P. H. Mfengwana, S. S. Mashele, L. Verschaeve, R. Anthonissen, I. T. Manduna

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Gunnera perpensa is traditionally used mostly by women for the treatment of different gynaecological related conditions due to its proven uterine contractility effects. The uses of this plant include menstrual pain relief, treatment of infertility and promotion of easy labour. However, even though this plant species has been reported to possess numerous medicinal properties, to author’s best knowledge, its safety has not been investigated. Thus, this study was aimed at investigating the genotoxicity and antigenotoxicity of Gunnera perpensa aqueous, methanol and dichloromethane extracts. The in vitro toxicity of the plant extracts was assessed with the neutral red uptake (NRU) test. Genotoxic and antigenotoxic properties of Gunnera perpensa were investigated using high-throughput assays: bacterial Vitotox test and the alkaline comet assay with and without S9 activation on human C3A cells. Ethyl Methanesulfonate (EMS) and 4-nitroquinoline-oxide (4-NQO) were used as positive controls, respectively. All extracts showed toxicity in a dose-dependent manner; however, that does not mean they were all genotoxic. Methanol extract did show genotoxicity with S9 (metabolism) only at the highest concentration of 500 µg/ml due to increased DNA damage observed, however, no genotoxicity was observed from other concentrations. Therefore, the results show that Gunnera perpensa extracts are genotoxic and not safe for human use.

Keywords: antigenotoxicity, comet test, genotoxicity, Gunnera perpensa, vitotox assay

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Authors: Tomilola J. Ajayi

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A category of nanovalves system containing the α-cyclodextrin (α-CD) ring on a stalk tethered to the pores of mesoporous silica nanoparticles (MSN) is theoretically and computationally modelled. This functions to control opening and blocking of the MSN pores for efficient targeted drug release system. Modeling of the nanovalves is based on the interaction between α-CD and the stalk (p-anisidine) in relation to pH variation. Conformational analysis was carried out prior to the formation of the inclusion complex, to find the global minimum of both neutral and protonated stalk. B3LYP/6-311G**(d, p) basis set was employed to attain all theoretically possible conformers of the stalk. Six conformers were taken into considerations, and the dihedral angle (θ) around the reference atom (N17) of the p-anisidine stalk was scanned from 0° to 360° at 5° intervals. The most stable conformer was obtained at a dihedral angle of 85.3° and was fully optimized at B3LYP/6-311G**(d, p) level of theory. The most stable conformer obtained from conformational analysis was used as the starting structure to create the inclusion complexes. 9 complexes were formed by moving the neutral guest into the α-CD cavity along the Z-axis in 1 Å stepwise while keeping the distance between dummy atom and OMe oxygen atom on the stalk restricted. The dummy atom and the carbon atoms on α-CD structure were equally restricted for orientation A (see Scheme 1). The generated structures at each step were optimized with B3LYP/6-311G**(d, p) methods to determine their energy minima. Protonation of the nitrogen atom on the stalk occurs at acidic pH, leading to unsatisfactory host-guest interaction in the nanogate; hence there is dethreading. High required interaction energy and conformational change are theoretically established to drive the release of α-CD at a certain pH. The release was found to occur between pH 5-7 which agreed with reported experimental results. In this study, we applied the theoretical model for the prediction of the experimentally observed pH-responsive nanovalves which enables blocking, and opening of mesoporous silica nanoparticles pores for targeted drug release system. Our results show that two major factors are responsible for the cargo release at acidic pH. The higher interaction energy needed for the complex/nanovalve formation to exist after protonation as well as conformational change upon protonation are driving the release due to slight pH change from 5 to 7.

Keywords: nanovalves, nanogate, mesoporous silica nanoparticles, cargo

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Authors: Hakam Alkhateeb

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Oleuropein, the main constituent of leaves and fruits of the olive tree, has been demonstrated to exert beneficial effects on parameters relevant to the normal homeostatic mechanisms of glucose regulation in rat skeletal muscle. However, the antidiabetic effect of oleuropein, to our knowledge, has not been examined. Therefore, in this study, we examined whether oleuropein ameliorated palmitate-induced insulin resistance in skeletal muscle. To examine this question, insulin resistance was rapidly induced by incubating (12h) soleus muscle with a high concentration of palmitate(2mM). Subsequently, we attempted to restore insulin sensitivity by incubating (12h) muscles with oleuropien (1.5mM), while maintaining high concentrations of palmitate. Palmitate treatment for 12 h reduced insulin-stimulated glucose transport, GLUT4 translocationandAS160 phosphorylation. Oleuropein treatment (12 h) fully restoredinsulin-stimulated glucose transport, GLUT4translocationandAS160 phosphorylation. Inhibition of PI3K phosphorylation with wortmannin (1µM)did not affect the oleuropein-induced improvements in insulin-stimulated glucose transport, GLUT4 translocation, and AS160 phosphorylation. These results suggested that the improvements in these parameters cannot account for activating PI3K pathway. Taken altogether, it appears that oleuropein, through activation of another pathway like activated protein kinase (AMPK), may provide a possible strategy by which they ameliorate palmitate-induced insulin resistance in skeletal muscles.

Keywords: AS160, diabetes, GLUT4, oleuropein

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Authors: Fabio Rodriguez Sanchez, Josef Bruers, Iciar Arteagoitia, Carlos Rodriguez Andres

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Background: Oral implants are a routine treatment to replace lost teeth. Although they have a high rate of success, implant failures do occur. Perioperative antibiotics have been suggested to prevent postoperative infections and dental implant failures, but they remain a controversial treatment among healthy patients. The objective of this study was to determine whether antibiotic prophylaxis is a common treatment in the Netherlands among general dentists, maxillofacial-surgeons, periodontists and implantologists in conjunction with oral implant surgery among healthy patients and to assess the nature of antibiotics prescriptions in order to evaluate whether any consensus has been reached and the current recommendations are being followed. Methodology: Observational cross-sectional study based on a web-survey reported according to the Strengthening the Reporting of Observational studies in Epidemiology (STROBE) guidelines. A validated questionnaire, developed by Deeb et al. (2015), was translated and slightly adjusted to circumstances in the Netherlands. It was used with the explicit permission of the authors. This questionnaire contained both close-ended and some open-ended questions in relation to the following topics: demographics, qualification, antibiotic type, prescription-duration and dosage. An email was sent February 2018 to a sample of 600 general dentists and all 302 oral implantologists, periodontists and maxillofacial surgeons who were recognized by the Dutch Association of Oral Implantology (NVOI) as oral health care providers placing oral implants. The email included a brief introduction about the study objectives and a link to the web questionnaire, which could be filled in anonymously. Overall, 902 questionnaires were sent. However, 29 questionnaires were not correctly received due to an incorrect email address. So a total number of 873 professionals were reached. Collected data were analyzed using SPSS (IBM Corp., released 2012, Armonk, NY). Results: The questionnaire was sent back by a total number of 218 participants (response rate=24.2%), 45 female (20.8%) and 171 male (79.2%). Two respondents were excluded from the study group because they were not currently working as oral health providers. Overall 151 (69.9%) placed oral implants on regular basis. Approximately 79 (52.7%) of these participants prescribed antibiotics only in determined situations, 66 (44.0%) prescribed antibiotics always and 5 dentists (3.3%) did not prescribe antibiotics at all when placing oral implants. Overall, 83 participants who prescribed antibiotics, did so both pre- and postoperatively (58.5%), 12 exclusively postoperative (8.5%), and 47 followed an exclusive preoperative regime (33.1%). A single dose of 2,000 mg amoxicillin orally 1-hour prior treatment was the most prescribed preoperative regimen. The most frequent prescribed postoperative regimen was 500 mg amoxicillin three times daily for 7 days after surgery. On average, oral health professionals prescribed 6,923 mg antibiotics in conjunction with oral implant surgery, varying from 500 to 14,600 mg. Conclusions: Antibiotic prophylaxis in conjunction with oral implant surgery is prescribed in the Netherlands on a rather large scale. Dutch professionals might prescribe antibiotics more cautiously than in other countries and there seems to be a lower range on the different antibiotic types and regimens being prescribed. Anyway, recommendations based on last-published evidence are frequently not being followed.

Keywords: clinical decision making, infection control, antibiotic prophylaxis, dental implants

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