Search results for: anti-cancer drug yielding plants

Authors: Inna Kornienko, Svetlana Guryeva, Natalia Danilova, Elena Petersen

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Drug toxicity often goes undetected until clinical trials, the most expensive and dangerous phase of drug development. Both human cell culture and animal studies have limitations that cannot be overcome by improvements in drug testing protocols. Tissue engineering is an emerging alternative approach to creating models of human malignant tumors for experimental oncology, personalized medicine, and drug discovery studies. This new generation of bioengineered tumors provides an opportunity to control and explore the role of every component of the model system including cell populations, supportive scaffolds, and signaling molecules. An area that could greatly benefit from these models is cancer research. Recent advances in tissue engineering demonstrated that decellularized tissue is an excellent scaffold for tissue engineering. Decellularization of donor organs such as heart, liver, and lung can provide an acellular, naturally occurring three-dimensional biologic scaffold material that can then be seeded with selected cell populations. Preliminary studies in animal models have provided encouraging results for the proof of concept. Decellularized Organs preserve organ microenvironment, which is critical for cancer metastasis. Utilizing 3D tumor models results greater proximity of cell culture morphological characteristics in a model to its in vivo counterpart, allows more accurate simulation of the processes within a functioning tumor and its pathogenesis. 3D models allow study of migration processes and cell proliferation with higher reliability as well. Moreover, cancer cells in a 3D model bear closer resemblance to living conditions in terms of gene expression, cell surface receptor expression, and signaling. 2D cell monolayers do not provide the geometrical and mechanical cues of tissues in vivo and are, therefore, not suitable to accurately predict the responses of living organisms. 3D models can provide several levels of complexity from simple monocultures of cancer cell lines in liquid environment comprised of oxygen and nutrient gradients and cell-cell interaction to more advanced models, which include co-culturing with other cell types, such as endothelial and immune cells. Following this reasoning, spheroids cultivated from one or multiple patient-derived cell lines can be utilized to seed the matrix rather than monolayer cells. This approach furthers the progress towards personalized medicine. As an initial step to create a new ex vivo tissue engineered model of a cancer tumor, optimized protocols have been designed to obtain organ-specific acellular matrices and evaluate their potential as tissue engineered scaffolds for cultures of normal and tumor cells. Decellularized biomatrix was prepared from animals’ kidneys, urethra, lungs, heart, and liver by two decellularization methods: perfusion in a bioreactor system and immersion-agitation on an orbital shaker with the use of various detergents (SDS, Triton X-100) in different concentrations and freezing. Acellular scaffolds and tissue engineered constructs have been characterized and compared using morphological methods. Models using decellularized matrix have certain advantages, such as maintaining native extracellular matrix properties and biomimetic microenvironment for cancer cells; compatibility with multiple cell types for cell culture and drug screening; utilization to culture patient-derived cells in vitro to evaluate different anticancer therapeutics for developing personalized medicines.

Keywords: 3D models, decellularization, drug discovery, drug toxicity, scaffolds, spheroids, tissue engineering

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Authors: Anela Lupuwana

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The main objective of this paper is to develop an ethnobotanical survey that documents medicinal plants used to treat diarrhea among infants in the Eastern Cape province of South Africa. In South Africa’s pluralistic healthcare system, medicinal plants are an integral part of healing and treating an array of diseases. This is also the case in rural areas of South Africa, where healthcare facilities are hard to access. There is a lack of literature on the use of medicinal plants to cure ailments common to children, and this paper fills this gap. A total of 18 participants were interviewed using semi-structured interviews. A purposive approach was used to sample the study cohorts. A total of 28 medicinal plants representing 19 different families were recorded, with the family Asteraceae (11%) having the most medicinal plants. The remaining plants (82%) were distributed equally among the following families: Rubiaceae, Canellaceae, Aloaceae, Rutaceae, Thymeleaceae, Myrinaceae, Olinaceae, Iradeceae, Zingiberaceae, Capparaceae, Aizoaceae, Fabaceae, Geraniaceae, Cornaceae, Monimiaceae, Talinaceae, Chrysobalanaceae, and Icacinaceae. Oral administration was the most common mode of administration, with 82% of plants taken orally. Healing was proven to be holistic; it was more than just treating physical ailments as such; infants were protected from evil spirits that made them vulnerable to illnesses. There was also evidence of the assimilation of Dutch medicine and animal products into traditional healing methods. In order to mitigate the prevalence of disease and illness in South Africa, I recommend that diversity in healing practices should be acknowledged and appreciated.

Keywords: infants, traditional healers, primary care givers, traditional medicine

Procedia PDF Downloads 67

Authors: Ragaa T. Darwish, Maha A. Demellawy, Haidy M. Megahed, Doreen N. Younan, Wael S. Kholeif

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The testing of drug abuse is authentic in order to affirm the misuse of drugs. Several analytical approaches have been developed for the detection of drugs of abuse in pharmaceutical and common biological samples, but few methodologies have been created to identify them from fingerprints. Liquid Chromatography-Mass Spectrometry (LC-MS) plays a major role in this field. The current study aimed at assessing the possibility of detection of some drugs of abuse (tramadol, clonazepam, and phenobarbital) from fingerprints using LC-MS in drug abusers. The aim was extended in order to assess the possibility of detection of the above-mentioned drugs in fingerprints of drug handlers till three days of handling the drugs. The study was conducted on randomly selected adult individuals who were either drug abusers seeking treatment at centers of drug dependence in Alexandria, Egypt or normal volunteers who were asked to handle the different studied drugs (drug handlers). An informed consent was obtained from all individuals. Participants were classified into 3 groups; control group that consisted of 50 normal individuals (neither abusing nor handling drugs), drug abuser group that consisted of 30 individuals who abused tramadol, clonazepam or phenobarbital (10 individuals for each drug) and drug handler group that consisted of 50 individuals who were touching either the powder of drugs of abuse: tramadol, clonazepam or phenobarbital (10 individuals for each drug) or the powder of the control substances which were of similar appearance (white powder) and that might be used in the adulteration of drugs of abuse: acetyl salicylic acid and acetaminophen (10 individuals for each drug). Samples were taken from the handler individuals for three consecutive days for the same individual. The diagnosis of drug abusers was based on the current Diagnostic and Statistical Manual of Mental disorders (DSM-V) and urine screening tests using immunoassay technique. Preliminary drug screening tests of urine samples were also done for drug handlers and the control groups to indicate the presence or absence of the studied drugs of abuse. Fingerprints of all participants were then taken on a filter paper previously soaked with methanol to be analyzed by LC-MS using SCIEX Triple Quad or QTRAP 5500 System. The concentration of drugs in each sample was calculated using the regression equations between concentration in ng/ml and peak area of each reference standard. All fingerprint samples from drug abusers showed positive results with LC-MS for the tested drugs, while all samples from the control individuals showed negative results. A significant difference was noted between the concentration of the drugs and the duration of abuse. Tramadol, clonazepam, and phenobarbital were also successfully detected from fingerprints of drug handlers till 3 days of handling the drugs. The mean concentration of the chosen drugs of abuse among the handlers group decreased when the days of samples intake increased.

Keywords: drugs of abuse, fingerprints, liquid chromatography–mass spectrometry, tramadol

Procedia PDF Downloads 108

Authors: Delband Yekta Moazami

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Background: For proper care and treatment of HIV patients and drug users, the medical staff and physicians must have a correct and positive attitude and knowledge towards such patients. We aimed to assess the attitudes in a sample of health care workers (HCW) working in different hospitals and clinics and medical students in Georgia towards HIV infected people and drug users in Tbilisi. Method: We conducted a cross-sectional study to assess attitudes of health care workers towards people living with HIV and drug users in hospitals and clinics in Tbilisi. The study was carried out from 1st of May 2020 till 30th of September 2020. Data were collected using a self-administered structured online questionnaire. With this tool we evaluated four facets of attitudes: Discrimination, Acceptance of HIV/AIDS patients, Acceptance of drug users and Fear. All data were imported and analyzed with the software SPSS 22 for windows. Results: In total data was collected from168 respondents, that among them 107 (65%) were women and majority of the participants were medical doctors. Women had more acceptance attitudes rather than men towards drug abusers. We found significant differences regarding expressing negative attitudes among HCW who were more than 50 years old comparing with other age groups in all four aspects. Medical doctors expressed more acceptances towards people with HIV and drug users comparing two other groups. Also our study revealed that the group with working experience 21 years and more, showed more discriminatory attitudes comparing other groups. Conclusion: Based on our study findings, there are significant differences regarding respondent’s attitudes based on gender, medical specialty and working experience in health care system. People struggling with HIV and drug use need nonjudgmental and positive behaviors from health care workers and physicians in order to help them for harm reduction and receiving appropriate treatment.

Keywords: hiv, addiction, attitudes, healthcare workers

Procedia PDF Downloads 71

Authors: Samah Lakehal, A. Meliani, F. Z. Benrebiha, C. Chaouia

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In the last few years, due to the misuse of antibiotics and an increasing incidence of immunodeficiency-related diseases, the development of microbial drug resistance has become more and more of a pressing problem. Recently, natural products from medicinal plants represent a fertile ground for the development of novel antibacterial agents. Plants essential oils have come more into the focus of phytomedicine. The present study describes antimicrobial activity of Rosmarinus officinalis L. essential oil known medicinally for its powerful antibacterial properties. The essential oil of rosemary obtained by hydrodistillation (using Clevenger type apparatus) growing in Algeria (Djelfa city of south Algeria) was investigated by GC-MS. The essential oil yield of the study was 1.4 %. The major components were found to be camphor, camphene, 1,8-cineole. The essential oil has been tested for antimicrobial activity against eight bacteria (Gram-negative and Gram-positive), and three fungi including Candida albicans. Inhibition of growth was tested by the agar diffusion method based on the determination of the diameter of inhibition. The oil was found to have significant antibacterial activity and therefore can be used as a natural antimicrobial agent for the treatment of several infectious diseases caused by those germs, which have developed resistance to antibiotics.

Keywords: antimicrobial activity, Rosmarinus officinalis L., essential oils, GC/MS, camphor

Procedia PDF Downloads 384

Authors: Gesti Prastiti, Maylina Adani, Yuyun darma A. N., M. Khilmi F., Yunita Wahyu Pratiwi

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Combination therapy may allow interaction on two drugs or more that can give adverse effects on patients. Simvastatin is a drug of antihyperlipidemia it can interact with drugs which work on cytochrome P450 CYP3A4 because it can interfere the performance of simvastatin. Flavonoid found in plants can inhibit the cytochrome P450 CYP3A4 if taken with simvastatin and can increase simvastatin levels in the body and increases the potential side effects of simvastatin such as myopati and rhabdomyolysis. Green tea leaves and mint are herbal medicine which has the effect of antihiperlipidemia. This study aims to determine the potential interaction of simvastatin with herbal drinks (green tea leaves and mint). This research method are experimental post-test only control design. Test subjects were divided into 5 groups: normal group, negative control group, simvastatin group, a combination of green tea group and the combination group mint leaves. The study was conducted over 32 days and total cholesterol levels were analyzed by enzymatic colorimetric test method. Results of this study is the obtainment of average value of total cholesterol in each group, the normal group (65.92 mg/dL), the negative control group the average total cholesterol test in the normal group was (69.86 mg/dL), simvastatin group (58.96 mg/dL), the combination of green tea group (58.96 mg/dL), and the combination of mint leaves (63.68 mg/dL). The conclusion is between simvastatin combination therapy with herbal drinks have the potential for pharmacodynamic interactions with a synergistic effect, antagonist, and a powerful additive, so the combination therapy are no more effective than a single administration of simvastatin therapy.

Keywords: hyperlipidemia, simvastatin, herbal drinks, green tea leaves, mint leaves, drug interactions

Procedia PDF Downloads 386

Authors: Rizwan Alam, Ikhtiar Khan, Aqib Iqbal

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Plants are naturally exposed to a wide variety of environmental stresses. The stresses may be biotic or/and abiotic. These environmental stresses have adverse effects on photosynthesis, water relation and nutrients uptake of plants. Fertilization of plants with exogenous minerals can enhance the drought tolerance in plants. In this experiment, canola (Brassica napus) was treated with solutions of calcium nitrate in different concentrations before the imposition of drought stress for 10 days. It was observed that drought stress decreased the tissue-K, Ca and K/Ca ratio of canola seedlings. The tissue-carbon and nitrogen contents were also depressed by the drought stress. Application of calcium nitrate, however, could alleviate the adverse effects of drought stress by showing a positive effect on all the aforementioned parameters.

Keywords: Brassica napus, calcium, carbon, potassium

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Authors: M. Abd El Hamid Ezzat

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Two field trials were conducted to study the effect of plant densities i.e., 190, 222, 266, 330 and 440 10³ plants ha⁻¹ on morphological characters, physiological and yield attributes of two faba bean types viz. determinate (FLIP-87 -117 strain) and indeterminate (c.v. Giza-461). The results showed that the indeterminate plants significantly surpassed the determinate plants in plant height at 75 and 90 days from sowing, number of leaves at all growth stages and dry matter accumulation at 45 and 90 days from sowing. Determinate plants possessed greater number of side branches than that of the indeterminate plants, but it was only significant at 90 days from sowing. Greater number of flowers were produced by the indeterminate plants than that of the determinate plants at 75 and 90 days from sowing, and although shedding was obvious in both types, it was greater in the determinate plants as compared with the indeterminate one at 90 days from sowing. Increasing plant density resulted in reductions in number of leaves, branches flowers and dry matter accumulation per plant of both faba bean types. However, plant height criteria took a reversible magnitude. Moreover, under all rates of plant densities the indeterminate type plants surpassed the determinate plants in all growth characters studied except for number of branches per plant at 90 days from sowing. The indeterminate plant leaves significantly contained greater concentrations of photosynthetic pigments i.e., chl. a, b and carotenoids than those found in the determinate plant leaves. Also, the data showed significant reduction in photosynthetic pigments concentration as planting density increases. Light extinction coefficient (K) values reached their maximum level at 60 days from sowing, then it declined sharply at 75 days from sowing. The data showed that the illumination inside the determinate faba bean canopies was better than the indeterminate plants. (K) values tended to increase as planting density increases, meanwhile, significant interactions were reported between faba bean type as planting density on (K) at all growth stages. Both of determinate and indeterminate faba bean plant leaves reached their maximum expansion at 75 days from sowing reflecting the highest LAI values, then their declined in the subsequent growth stage. The indeterminate faba bean plants significantly surpassed the determinate plants in LAI up to 75 days from sowing. Growth analysis showed that NAR, RGR and CGR reached their maximum rates at (60-75 days growth stage). Faba bean types did not differ significantly in NAR at the early growth stage. The indeterminate plants were able to grow faster with significant CGR values than the determinate plants. The indeterminate faba bean plants surpassed the determinate ones in number of seeds/pod and per plant, 100-seed weight, seed yield per plant and per hectare at all rates of plant density. Seed yield increased with increasing plant densities of both types. The highest seed yield was attained for both types 440 103 plants ha⁻¹.

Keywords: determinate, indeterminate faba bean, Physiological attributes, yield attributes

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Authors: Özgür Emi̇nağaoğlu, Hayal Akyildirim Beğen, Şevval Sali̇oğlu, Emrah Yüksel

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This study was carried out in order to determine the scientific name, common name, local names, location, botanical characteristics, used parts, intended use, local usage patterns, usage in the literature of plant species used for medicinal and aromatic purposes in Ardanuç (Artvin, Türkiye) between 2020-2023 years. The research area is located in the A9 square according to Davis’s grid system and is phytogeographically located in the colchic subsection of the Euxine part of the Euro-Siberian flora area of the Holarctic region. As a result of the studies, it has been determined that 167 plant species belonging to 79 families are used for medicinal and aromatic purposes. The families that contain the most taxa in the research area are, respectively, Rosaceae (19 taxa), Asterecaeae (15 taxa), and Lamiaceae (14 taxa). It has been determined that the medicinal, aromatic plants of the Ardanuç region are mostly used in the treatment of diseases (59%), and the plants are mostly used in the treatment of diabetes (37%). It was determined that the most applied method in the internal use of plants was decoction (48%). As a result of the research, the most commonly used plants in different diseases are Sambucus nigra, Plantago lanceolata, Satureja hortensis, Hypericum perforatum, Juniperus communis. These plants are used in the treatment of many diseases, such as colds, cancer, anemia and diabetes.

Keywords: Ardanuç, Artvin, Medicinal and Aromatic plant, Türkiye

Procedia PDF Downloads 65

Authors: Lyudmila V. Ignatova, Yelena V. Brazhnikova, Togzhan D. Mukasheva, Ramza Zh. Berzhanova, Anel A. Omirbekova

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Endophytic microorganisms are presented in plants of different families growing in the foothills and piedmont plains of Trans-Ili Alatau. It was found that the maximum number of endophytic micromycetes is typical to the Fabaceae family. The number of microscopic fungi in the roots reached (145.9±5.9)×103 CFU/g of plant tissue; yeasts - (79.8±3.5)×102 CFU/g of plant tissue. Basically, endophytic microscopic fungi are typical for underground parts of plants. In contrast, yeasts more infected aboveground parts of plants. Small amount of micromycetes is typical to inflorescence and fruits. Antagonistic activity of selected micromycetes against Fusarium graminearum, Cladosporium sp., Phytophtora infestans and Botrytis cinerea phytopathogens was detected. Strains with a broad, narrow and limited range of action were identified. For further investigations Rh2 and T7 strains were selected, they are characterized by a broad spectrum of fungicidal activity and they formed the large inhibition zones against phytopathogens. Active antagonists are attributed to the Rhodotorula mucilaginosa and Beauveria bassiana species.

Keywords: endophytic micromycetes, fungicidal activity, prevalence, plants

Procedia PDF Downloads 314

Authors: Vadim Makarov, Stewart T.Cole

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PBTZ169 is novel drug candidate with high efficacy in animals models, and its combination treatment of PBTZ169 with BDQ and pyrazinamide was shown to be more efficacious than the standard treatment for tuberculosis in a mouse model. The target of PBTZ169 is famous DprE1, an essential enzyme in cell wall biosynthesis. The crystal structure of the DprE1-PBTZ169 complex reveals formation of a semimercaptal adduct with Cys387 in the active site and explains the irreversible inactivation of the enzyme. Furthermore, this drug candidate demonstrated during preclinical research ‘drug like’ properties what made it an attractive drug candidate to treat tuberculosis in humans. During first clinical trials several cohorts of the healthy volunteers were treated by the single doses of PBTZ169 as well as two weeks repeated treatment was chosen for two maximal doses. As expected PBTZ169 was well tolerated, and no significant toxicity effects were observed during the trials. The study of the metabolism shown that human metabolism of PBTZ169 is very different from microbial or animals compound transformation. So main pathway of microbial, mice and less rats metabolism connected with reduction processes, but human metabolism mainly connected with oxidation processes. Due to this difference we observed several metabolites of PBTZ169 in humans with antitubercular activity, and now we can conclude that animal antituberculosis activity of PBTZ169 is a result not only activity of the drug itself, but it is a result of the sum activity of the drug and its metabolites. Direct antimicrobial plasma activity was studied, and such activity was observed for 24 hours after human treatment for some doses. This data gets high chance for good efficacy of PBTZ169 in human for treatment TB infection. Second phase of clinical trials was started summer of 2017 and continues to the present day. Available data will be presented.

Keywords: clinical trials, DprE1, PBTZ169, metabolism

Procedia PDF Downloads 156

Authors: A. Hilsana, Vinay U. Rao, M. Sudhakar

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Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with different chemistries, they share a common solubility characteristic that is they are relatively more soluble in alkaline environment and practically insoluble in acidic environment. This work deals with developing a wax matrix drug delivery platform for controlled delivery of three model NSAIDS, Diclofenac sodium (DNa), Mefenamic acid (MA) and Naproxen (NPX) using the melt granulation technique. The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24 hours. Full factorial design of experiments was followed for optimization of the formulation.

Keywords: NSAIDs, controlled delivery, target product profile, melt granulation

Procedia PDF Downloads 326

Authors: So-Ra Lee, Myung-Min Oh

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Generally, plants growing on the earth are under the influence of natural electric fields and may even require exposure of the electric field to survive. Electric signals have been observed within plants and seem to play an important role on various metabolic processes, but their role is not fully understood. In this study, we attempted to explore the response of plants under external electric fields in kale (Brassica oleracea var. acephala). The plants were hydroponically grown for 28 days in a plant factory. Electric currents at 10, 50 and 100 mA were supplied to nutrient solution for 3 weeks. Additionally, some of the plants were cultivated in a Faraday cage to remove the natural electric field. Kale plants exposed to electric fields had higher fresh weight than the control and plants in Faraday cage. Absence of electric field caused a significant decrease in shoot dry weight and root growth. Leaf area also showed a similar response with shoot fresh weight. Supplying weak electric stimulation enhanced nutritional quality including total phenolic content and antioxidant capacity. This work provides basic information on the effects of electric fields on plants and is a meaningful attempt for developing a new economical technology to increase crop productivity and quality by applying an electric field. This work was supported by Korea Institute of Planning and Evaluation for Technology in Food, Agriculture, Forestry and Fisheries (IPET) through Agriculture, Food and Rural Affairs Research Center Support Program, funded by Ministry of Agriculture, Food and Rural Affairs (MAFRA) (717001-07-02-HD240).

Keywords: electroculture, electric signal, faraday cage, electric field

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Authors: Hong Li, Tingxian Li, Xudong Wang, Weibo Yang

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Co-limitation of iron (Fe) deficiency in legume nitrogen fixation process is not well understood. Our objectives were to examine how peanut plants cope with Fe deficiency with the rhizobial inoculants and N-nutrient treatments. The study was conducted in the tropical Hainan Island during 2012-2013. The soil was strongly acidic (pH 4.6±0.7) and deficient in Fe (9.2±2.3 mg/kg). Peanut plants were intercropped with cassava. The inoculants and N treatments were arranged in a split-plot design with three blocks. Peanut root nodulation, stem allantoin, amino acids and plant N derived from fixation (P) reduced with declining soil Fe concentrations. The treatment interactions were significant on relative ureide % and peanut yields (P<0.05). Residual fixed N from peanut plants was beneficial to cassava plants. It was concluded that co-variance of Fe deficiency could influence peanut N fixation efficiency and rhizobia and N inputs could help improving peanut tolerance to Fe deficiency stress.

Keywords: amino acids, plant N derived from N fixation, root nodulation, soil Fe co-variance, stem ureide, peanuts, cassava

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Authors: Mahmoud Ahmed Khater

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This study aimed to improve the deleterious effects of salinity stress in chickpeas using both proline and glycine betaine as osmoregulants. The aim was achieved using foliar spraying with different concentrations of proline (5 mM and 10 mM) and glycinebetaine (10 mM and 20 mM) to chickpea plants grown in pots under salinity stress (3000 mg/l NaCl) at the greenhouse of the National Research Centre, Egypt, during two successive seasons 2021/2022 and 2022/2023. Results indicated that all applied treatments caused significant increases in most of the investigated parameters of chickpea plants irrigated with either tap water or saline solution relative to the corresponding control. It is worth mentioning that proline treatments were more effective than glycine betaine treatments in increasing the salinity tolerance of chickpea plants, reflected in their quality and quantity. Moreover, proline treatment at 5mM was the most pronounced treatment in alleviating the deleterious effect of salinity on chickpea plants.

Keywords: cicer arietinum L., osmoprotectant, proline, glycinebetaine salinity tolerance

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Authors: Gajera Lalit, Shah Pranav, Shah Shailesh

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Venlafaxine hydrochloride has a short elimination half-life of 5 ± 2 hr, and absorption window in the upper part of gastrointestinal tract. The conventional tablets need to be administered two to three times a day and possess an oral bioavailability of 45%. The purpose of this study was to formulate gastroretentive effervescent floating tablets of Venlafaxine HCl. Different grades of HPMC namely K15M, K4M, K100M and E15LV were employed as swelling polymers whereas sodium bicarbonate was employed as gas generating agent. The direct compression method was employed for the formulation of tablets. The tablets were evaluated in terms of hardness, friability, weight variation, drug content, water uptake, in-vitro floating behavior and in-vitro drug release study. All the formulations exhibited very short floating lag time of < 1 min and total floating time of 12 hr. Formulation L3 containing 25 mg and 75 mg of HPMC E15 LV and HPMC K15M respectively exhibited complete drug release within 12 hrs.

Keywords: venlafaxine HCl, hydroxyl propyl methylcellulose, floating gastro retentive tablets, in-vitro drug release, non-fickian diffusion

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Authors: Yasmin Begum Mohammed

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Ketorolac tromethamine (KTM) is a non-steroidal anti-inflammatory drug with a potent analgesic and anti-inflammatory activity due to prostaglandin related inhibitory effect of drug. It is a non-selective cyclo-oxygenase inhibitor. The drug is currently used orally and intramuscularly in multiple divided doses, clinically for the management arthritis, cancer pain, post-surgical pain, and in the treatment of migraine pain. KTM has short biological half-life of 4 to 6 hours, which necessitates frequent dosing to retain the action. The frequent occurrence of gastrointestinal bleeding, perforation, peptic ulceration, and renal failure lead to the development of other drug delivery strategies for the appropriate delivery of KTM. The ideal solution would be to target the drug only to the cells or tissues affected by the disease. Drug targeting could be achieved effectively by liposomes that are biocompatible and biodegradable. The aim of the study was to develop a parenteral liposome formulation of KTM with improved efficacy while reducing side effects by targeting the inflammation due to arthritis. PEG-anchored (stealth) and non-PEG-anchored liposomes were prepared by thin film hydration technique followed by extrusion cycle and characterized for in vitro and in vivo. Stealth liposomes (SLs) exhibited increase in percent encapsulation efficiency (94%) and 52% percent of drug retention during release studies in 24 h with good stability for a period of 1 month at -20°C and 4°C. SLs showed about maximum 55% of edema inhibition with significant analgesic effect. SLs produced marked differences over those of non-SL formulations with an increase in area under plasma concentration time curve, t₁/₂, mean residence time, and reduced clearance. 0.3% of the drug was detected in arthritic induced paw with significantly reduced drug localization in liver, spleen, and kidney for SLs when compared to other conventional liposomes. Thus SLs help to increase the therapeutic efficacy of KTM by increasing the targeting potential at the inflammatory region.

Keywords: biodistribution, ketorolac tromethamine, stealth liposomes, thin film hydration technique

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Authors: Ila Shrestha

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Bridim Village Development Committee (VDC) is one of the medicinal plants hot spots of Nepal. It is located on a ridge above the lower Langtang Khola, steep and narrow spot in between 1944 m to 4833 m altitude. The study area is homogeneously inhabited by Tamang communities. An investigation on folk herbal medicine on the basis of traditional uses of medicinal plants was done in 2014. The local traditional healers, elder men and women, traders and teachers, were consulted as key informants for documentation of indigenous knowledge on the medicinal plants. It was found that altogether seventy-one medicinal plant species belonging to sixty genera and thirty-three families were used by local people for twenty-seven diseases. Roots of thirty-four species were the most frequently used plant parts and bigger numbers of species were found to be used in fever of ten species. Most medicines were prepared in the form of juice of forty species. The attempt of the study was to document ethno medicinal practices to treat different diseases in the study area for conservation of indigenous knowledge.

Keywords: Bridim village, ethnomedicine, national park, plants

Procedia PDF Downloads 286

Authors: I. C. Orabueze, A. A. Amudalat, S. A. Adesegun, A. A. Usman

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Dental and associated oral diseases are increasingly affecting a considerable portion of the population and are considered some of the major causes of tooth loss, discomfort, mouth odor and loss of confidence. This study focused on the ethnobotanical survey of medicinal plants used in oral therapy and evaluation of the antimicrobial activities of methanolic extracts of two selected plants from the survey for their efficacy against dental microorganisms. The ethnobotanical survey was carried out in six herbal markets in Lagos State, Nigeria by oral interviewing and information obtained from an old family manually complied herbal medication book. Methanolic extracts of Olax subscorpioidea (stem bark) and Bridelia ferruginea (stem bark) were assayed for their antimicrobial activities against clinical oral isolates (Aspergillus fumigatus, Candida albicans, Streptococcus spp, Staphylococcus aureus, Lactobacillus acidophilus and Pseudomonas aeruginosa). In vitro microbial technique (agar well diffusion method and minimum inhibitory concentration (MIC) assay) were employed for the assay. Chlorhexidine gluconate was used as the reference drug for comparison with the extract results. And the preliminary phytochemical screening of the constituents of the plants were done. The ethnobotanical survey produced plants (28) of diverse family. Different parts of plants (seed, fruit, leaf, root, bark) were mentioned but 60% mentioned were either the stem or the bark. O. subscorpioidea showed considerable antifungal activity with zone of inhibition ranging from 2.650 – 2.000 cm against Aspergillus fumigatus but no such encouraging inhibitory activity was observed in the other assayed organisms. B. ferruginea showed antibacterial sensitivity against Streptococcus spp, Staphylococcus aureus, Lactobacillus acidophilus and Pseudomonas aeruginosa with zone of inhibitions ranging from 3.400 - 2.500, 2.250 - 1.600, 2.700 - 1.950, 2.225 – 1.525 cm respectively. The minimum inhibitory concentration of O. subscorpioidea against Aspergillus fumigatus was 51.2 mg ml-1 while that of B. ferruginea against Streptococcus spp was 0.1mg ml-1 and for Staphylococcus aureus, Lactobacillus acidophilus and Pseudomonas aeruginosa were 25.6 mg ml-1. A phytochemical analysis reveals the presence of alkaloids, saponins, cardiac glycoside, tannins, phenols and terpenoids in both plants, with steroids only in B. ferruginea. No toxicity was observed among mice given the two methanolic extracts (1000 mg Kg-1) after 21 days. The barks of both plants exhibited antimicrobial properties against periodontal diseases causing organisms assayed, thus up-holding their folkloric use in oral disorder management. Further research could be done viewing these extracts as combination therapy, checking for possible synergistic value in toothpaste and oral rinse formulations for reducing oral bacterial flora and fungi load.

Keywords: antimicrobial activities, Bridelia ferruginea, dental disinfection, methanolic extract, Olax subscorpioidea, ethnobotanical survey

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Authors: Nouf A. Aldarmahi, Nesrin I. Tarbiah, Nuha A. Alkhattabi, Huda F. Alshaibi

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Nigella sativa which is known as dark cumin is a well-known example for a widely applicable herbal medicine. Nigella sativa can be effective in a variety of diseases such as hypertension, diabetes, bronchitis, gastrointestinal upset, and cancer. The anticancer effect of Nigella sativa appeared to be mediated by immune-modulatory effect through stimulating human natural killer (NK) cells. This is a type of lymphocytes which is part of the innate immunity, also known as the first line of defense in the body against pathogens. This study investigated the effect of thymoquinone as a major component of Nigella sativa on the molecular cytotoxic pathway of NK cell and the role of thymoquinone therapeutic effect on NK cells. NK cells were cultured with breast tumor cells in different ways and cultured media was collected and the concentration of perforin, granzyme B and interferon-α were measured by ELISA. The cytotoxic effect of NK cells on breast tumor cells was enhanced in the presence of thymoquinone, with increased activity of perforin in NK cells. This improved anticancer effect of thymoquinone on breast cancer cells.

Keywords: breast cancer, cancer cells, natural killer cells, thymoquinone

Procedia PDF Downloads 231

Authors: Farzad Khajavi, Farzaneh Jalilfar, Faranak Jafari, Leila Shokrani

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Formulation of Ranolazine in the form of extended-release tablet in 500 mg dosage form was performed using Eudragit L100-55 as a retarding agent. Drug-release profiles were investigated in comparison with the reference Ranexa extended-release 500 mg tablet. F₂ and f₁ were calculated as 64.16 and 8.53, respectively. According to Peppas equation, the release of drug is controlled by diffusion (n=0.5). The tablets were put into accelerated stability conditions (40 °C, 75% humidity) for 3 and 6 months. The dissolution release profiles and other physical and chemical characteristics of the tablets confirmed the robustness and stability of formulation in this condition.

Keywords: drug release, extended-release tablet, ranolazine, stability

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Authors: Alireza Jalalvand, Maryam Saleh, Somayeh Behjat Khatouni, Zahra Bahri Najafi, Foroozan Fatahinia, Narges Ismailzadeh, Behrokh Farahmand

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Object: In the last two decades, the recent outbreak of Coronavirus (SARS-CoV-2) imposed a global pandemic in the world. Despite the increasing prevalence of the disease, there are no effective drugs to treat it. A suitable and rapid way to afford an effective drug and treat the global pandemic is a computational drug study. This study used molecular docking methods to examine the potential inhibition of over 50 antiviral drugs against three fundamental proteins of SARS-CoV-2. METHODS: Through a literature review, three important proteins (a key protease, RNA-dependent RNA polymerase (RdRp), and spike) were selected as drug targets. Three-dimensional (3D) structures of protease, spike, and RdRP proteins were obtained from the Protein Data Bank. Protein had minimal energy. Over 50 antiviral drugs were considered candidates for protein inhibition and their 3D structures were obtained from drug banks. The Autodock 4.2 software was used to define the molecular docking settings and run the algorithm. RESULTS: Five drugs, including indinavir, lopinavir, saquinavir, nelfinavir, and remdesivir, exhibited the highest inhibitory potency against all three proteins based on the binding energies and drug binding positions deduced from docking and hydrogen-bonding analysis. Conclusions: According to the results, among the drugs mentioned, saquinavir and lopinavir showed the highest inhibitory potency against all three proteins compared to other drugs. It may enter laboratory phase studies as a dual-drug treatment to inhibit SARS-CoV-2.

Keywords: covid-19, drug repositioning, molecular docking, lopinavir, saquinavir

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Authors: Masome Moeni, Roya Abedizadeh, Elham Aram, Hamid Sadeghi-Abandansari, Davood Sabour, Robert Menzel, Ali Hassanpour

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Significant number of studies and preclinical research in formulation of cancer nano-pharmaceutics have led to an improvement in cancer care. Nonetheless, the antineoplastic agents have ‘failed to live up to its promise’ since their clinical performance is moderately low. For almost ninety years, iron oxide nanoparticles (IONPS) have managed to keep its reputation in clinical application due to their low toxicity, versatility and multi-modal capabilities. Drug Administration approved utilization of IONPs for diagnosis of cancer as contrast media in magnetic resonance imaging, as heat mediator in magnetic hyperthermia and for the treatment of iron deficiency. Furthermore, IONPs have high drug-loading capacity, which makes them good candidates as therapeutic agent transporters. There are yet challenges to overcome for successful clinical application of IONPs, including stability of drug and poor delivery, which might lead to (i) drug resistance, (ii) shorter blood circulation time, and (iii) rapid elimination and adverse side effects from the system. In this study, highly stable and super paramagnetic IONPs were prepared for efficient and targeted drug delivery in cancer treatment. The synthesis procedure was briefly involved the production of IONPs via co-precipitation followed by coating with tetraethyl orthosilicate and 3-aminopropylethoxysilane and grafting with folic acid for stability targeted purposes and controlled drug release. Physiochemical and morphological properties of modified IONPs were characterised using different analytical techniques. The resultant IONPs exhibited clusters of 10 nm spherical shape crystals with less than 100 nm size suitable for drug delivery. The functionalized IONP showed mesoporous features, high stability, dispersibility and crystallinity. Subsequently, the functionalized IONPs were successfully loaded with oxaliplatin, a chemotherapeutic agent, for a controlled drug release in an actively targeting cancer cells. FT-IR observations confirmed presence of oxaliplatin functional groups, while ICP-MS results verified the drug loading was ~ 1.3%.

Keywords: cancer treatment, chemotherapeutic agent, drug delivery, iron oxide, multi-functional nanoparticle

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Authors: Lynn Louis, Bor Shin Chee, Marion McAfee, Michael Nugent

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This article aims to develop a sustained release formulation of microspheres containing the mTOR inhibitor Everolimus (EVR) using Polyvinyl alcohol (PVA) to enhance the bioavailability of the drug and to overcome poor solubility characteristics of Everolimus. This paper builds on recent work in the manufacture of microspheres using the sessile droplet technique by freezing the polymer-drug solution by suspending the droplets into pre-cooled ethanol vials immersed in liquid nitrogen. The spheres were subjected to 6 freezing cycles and 3 freezing cycles with thawing to obtain proper geometry, prevent aggregation, and achieve physical cross-linking. The prepared microspheres were characterised for surface morphology by SEM, where a 3-D porous structure was observed. The in vitro release studies showed a 62.17% release over 12.5 days, indicating a sustained release due to good encapsulation. This result is comparatively much more than the 49.06% release achieved within 4 hours from the solvent cast Everolimus film as a control with no freeze-thaw cycles performed. The solvent cast films were made in this work for comparison. A prolonged release of Everolimus using a polymer-based drug delivery system is essential to reach optimal therapeutic concentrations in treating SEGA tumours without systemic exposure. These results suggest that the combination of PVA and Everolimus via a rheological synergism enhanced the bioavailability of the hydrophobic drug Everolimus. Physical-chemical characterisation using DSC and FTIR analysis showed compatibility of the drug with the polymer, and the stability of the drug was maintained owing to the high molecular weight of the PVA. The obtained results indicate that the developed PVA/EVR microsphere is highly suitable as a potential drug delivery system with improved bioavailability in treating Subependymal Giant cell astrocytoma (SEGA).

Keywords: drug delivery system, everolimus, freeze-thaw cycles, polyvinyl alcohol

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Authors: Shuye Jiang, Ali Ma, Srinivasan Ramachandran

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Indoor air quality could be improved through traditional air purifiers. However, they may not be environmental products. Here, a bio-based method was employed to improve indoor air quality by increasing negative air ion (NAI) release from ornamental plants. A total of 60 plant species has been screened by evaluating their ability to release NAIs, from which four candidates were selected to further study. All of them are from the Dracaena or fabids clade. These four candidates were then subjected to survey their ability to reduce the concentration of particulate matter with diameter of 2.5 or 10 microns (PM2.5 and PM10) in the growth chamber. High concentrations of PM2.5 and PM10 were artificially generated by burning a stick of incense for 2 minutes in the closed growth chamber (80cm length × 80cm width × 80cm height), in which the PM2.5 and PM10 concentration were generally around 500 µg/m3 and 1500 µg/m3, respectively. Both PM2.5 and PM10 were naturally reduced to 410 and 670, respectively after two hours in case that no plants were placed inside the chamber. Interestingly, these two sizes of particulars were reduced to 170 µg/m3 and 210 µg/m3, respectively after two hours when plants were placed to the chamber. It took 4 hours for the plants to reduce particular concentration to acceptable level at less than 55 µg/m3 for both PM2.5 and PM10, respectively. However, the PM2.5 and PM10 concentration were still above 200 µg/m3 and 300 µg/m3, respectively after 4 hours in the growth chamber without any plants. These results suggest the contribution of plants to the particulate deposition. However, all of these data are preliminary and the results may be updated by further studies. In addition, the roles of plants in absorbing indoor formaldehyde have also been explored and their absorbing ability is being improved by optimizing their growth conditions and treating with various exogenous agents. Thus, our preliminary studies provide an alternative strategy to improve indoor air quality.

Keywords: bio-based method, indoor air, negative air ion, particulate matter

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Authors: Paiwan Buachan, Maneekarn Namsa-Aid, Suchada Jongrungruangchok, Foengchat Jarintanan, Wanlaya Uthaisang-Tanechpongtamb

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Lung cancer or pulmonary carcinoma is the uncontrolled growth of abnormal cells in one or both of the lungs. These abnormal cells can spread to other organs of the body through lymphatic system or bloodstream which is called metastatic stage that leading cause of cancer death. Terrein (C₈H₁₀O₃; MW= 154.06 kDa) is a secondary bioactive fungal metabolite, which was isolated from the Aspergillus terreus. In this study, we investigated the effects of terrein on the inhibition of human lung cancer cell proliferation and metastasis. The A549 human non-small cell lung cancer cell line was used as a model. Terrein significantly inhibited lung cancer cell proliferation measuring by a colorimetric MTT assay (IC₅₀ 0.32 mM) and significantly inhibited metastatic processes including migration, invasion, and adhesion that determined by wound healing assay, transwell assay, and adhesion assay, respectively. These findings indicate that terrein could be a potential therapeutic agent for lung cancer.

Keywords: terrein, lung cancer, anticancer, antimetastatic

Procedia PDF Downloads 156

Authors: H. R. Kelidari, M. Saeedi, J. Akbari, K. Morteza-Semnani, H. Valizadeh

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Spironolactoe (SP) a synthetic steroid diuretic is a poorly water-soluble drug with a low and variable oral bioavailability. Regarding to the good solubility of SP in lipid materials, SP loaded Solid lipid nanoparticles (SP-SLNs) and nanostructured lipid carrier (SP-SLNs) were thus prepared in this work for accelerating dissolution of this drug. The SP loaded NLC with stearic acid (SA) as solid lipid and different Oleic Acid (OA) as liquid lipid content and SLN without OA were prepared by probe ultrasonication method. With increasing the percentage of OA from 0 to 30 wt% in SLN/NLC, the average size and zeta potential of nanoparticles felled down and entrapment efficiency (EE %) rose dramatically. The obtained micrograph particles showed pronounced spherical shape. Differential Scanning Calorimeter (DSC) measurements indicated that the presence of OA reduced the melting temperature and melting enthalpy of solid lipid in NLC structure. The results reflected good long-term stability of the nanoparticles and the measurements show that the particle size remains lower in NLC compare to SLN formulations, 6 months after production. Dissolution of SP-SLN and SP-NLC was about 5.1 and 7.2 times faster than raw drugs in 120 min respectively. These results indicated that the SP loaded NLC containing 70:30 solid lipid to liquid lipid ratio is a suitable carrier of SP with improved drug EE and steady drug release properties.

Keywords: drug release, lipid nanoparticles, spironolactone, stability

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Authors: Daniel Motlhanka, Neo Kerebotswe

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The strong and long history of use of medicinal plants in Botswana to address existing and emerging health threats provides undebatable evidence for their potential as innovative therapeutic tools. The prevalence of emerging health threats, such as COVID-19 and hard-to-treat non-communicable diseases, warrants the scientific community to revisit and exploit ethnopharmacology for its potential as a source of therapeutic tools. Many studies conducted on bioactivity-guided bioassays of ethnobotanical resources have proved a number of health beneficial properties of these plants, such as free radical scavenging, anti-inflammatory, antimicrobial and, most importantly, the capability of medicinal plants to alleviate oxidative stress. In this work, a number of medicinal plants used in Botswana traditional medicine were investigated for both their free radical scavenging capability and total phenolic contents using the Free Radical Scavenging Power (FRSP) and Folin Ciocalteau (FC) method. At 100 micrograms/ml all the studied plants expressed above 90% Scavenging power and expressed total phenolic contents between 5000- 8890 mg/L.GAE. These plants are promising tools for engineering active therapeutic tools against life-threatening diseases of oxidative stress origin.

Keywords: oxidative stress, non-communicable diseases, total phenolics, ethnobotanicals

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Authors: Elisha Didam Markus, Thapelo Maqame

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This paper focuses on studying the effects of magnetism on water and their impact to plant growth. Magnetic fields are known to induce higher rate of biochemical reaction and therefore can be used for growth related reactions in plants. For the purpose of this study, two 2 litres bottles were taken, one with two opposite poles magnets (500 mT) one on top and one at the bottom of the bottle. Another bottle was not altered in any way (used as control). Each bottle contained tap water stored up for 24 hours. Plants planted into different pots were watered using water from these bottles. Four pots with soil and manure equally mixed were used and equal volume of radish berry seeds were planted. Two pots were watered with magnetised water and the other two with normal tap water. The developments of plants were monitored in terms of their lengths for a period of 21 days. After 21 days, the lengths of plants watered with magnetised water were found to be 5.6% longer than those watered with tap water.

Keywords: magnetised water, radish berry, growth percentage, magnetic fields

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Authors: Adebisi Adunola Demehin, Wanlaya Thamnarak, Jaruwan Chatwichien, Chatchakorn Eurtivong, Kiattawee Choowongkomon, Somsak Ruchirawat, Nopporn Thasana

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The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein involved in cellular signalling processes and, its aberrant activity is crucial in the development of many cancers such as lung cancer. Selaginellaceae are fern allies that have long been used in Chinese traditional medicine to treat various cancer types, especially lung cancer. Biflavonoids, the major secondary metabolites in Selaginellaceae, have numerous pharmacological activities, including anti-cancer and anti-inflammatory. For instance, amentoflavone induces a cytotoxic effect in the human NSCLC cell line via the inhibition of PARP-1. However, to the best of our knowledge, there are no studies on biflavonoids as EGFR inhibitors. Thus, this study aims to investigate the EGFR inhibitory activities of biflavonoids isolated from Selaginella siamensis and Selaginella bryopteris. Amentoflavone, tetrahydroamentoflavone, sciadopitysin, robustaflavone, robustaflavone-4-methylether, delicaflavone, and chrysocauloflavone were isolated from the ethyl-acetate extract of the whole plants. The structures were determined using NMR spectroscopy and mass spectrometry. In vitro study was conducted to evaluate their cytotoxicity against A549, HEPG2, and T47D human cancer cell lines using the MTT assay. In addition, a target-based assay was performed to investigate their EGFR inhibitory activity using the kinase inhibition assay. Finally, a molecular docking study was conducted to predict the binding modes of the compounds. Robustaflavone-4-methylether and delicaflavone showed the best cytotoxic activity on all the cell lines with IC50 (µM) values of 18.9 ± 2.1 and 22.7 ± 3.3 on A549, respectively. Of these biflavonoids, delicaflavone showed the most potent EGFR inhibitory activity with an 84% relative inhibition at 0.02 nM using erlotinib as a positive control. Robustaflavone-4-methylether showed a 78% inhibition at 0.15 nM. The docking scores obtained from the molecular docking study correlated with the kinase inhibition assay. Robustaflavone-4-methylether and delicaflavone had a docking score of 72.0 and 86.5, respectively. The inhibitory activity of delicaflavone seemed to be linked with the C2”=C3” and 3-O-4”’ linkage pattern. Thus, this study suggests that the structural features of these compounds could serve as a basis for developing new EGFR-TK inhibitors.

Keywords: anticancer, biflavonoids, EGFR, molecular docking, Selaginellaceae

Procedia PDF Downloads 190