Search results for: high-throughput drug screening
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 3109

Search results for: high-throughput drug screening

1579 Wireless Sensor Network to Help Low Incomes Farmers to Face Drought Impacts

Authors: Fantazi Walid, Ezzedine Tahar, Bargaoui Zoubeida

Abstract:

This research presents the main ideas to implement an intelligent system composed by communicating wireless sensors measuring environmental data linked to drought indicators (such as air temperature, soil moisture , etc...). On the other hand, the setting up of a spatio temporal database communicating with a Web mapping application for a monitoring in real time in activity 24:00 /day, 7 days/week is proposed to allow the screening of the drought parameters time evolution and their extraction. Thus this system helps detecting surfaces touched by the phenomenon of drought. Spatio-temporal conceptual models seek to answer the users who need to manage soil water content for irrigating or fertilizing or other activities pursuing crop yield augmentation. Effectively, spatio-temporal conceptual models enable users to obtain a diagram of readable and easy data to apprehend. Based on socio-economic information, it helps identifying people impacted by the phenomena with the corresponding severity especially that this information is accessible by farmers and stakeholders themselves. The study will be applied in Siliana watershed Northern Tunisia.

Keywords: WSN, database spatio-temporal, GIS, web mapping, indicator of drought

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1578 Ultrasound Markers in Evaluation of Hernias

Authors: Aniruddha Kulkarni

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In very few cases of external hernias we require imaging modalities as on most occasions clinical examination tests are good enough. Ultrasound will help in chronic abdominal or groin pain, equivocal clinical results & complicated hernias. Ultrasound is useful in assessment of cause of raised intrabdominal pressure. In certain cases will comment about etiology, complications and chronicicty of lesion. Screening of rest of abdominal organs too is important advantage being real time modality. Cost effectiveness, no radiation allows modality be used repeatedly in indicated cases. Sonography is better accepted by patients too as it is cost effective. Best advanced tissue harmonic equipment and increasing expertise making it popular. Ultrasound can define surgical anatomy, rent size, contents, etiological /recurrence factors in great detail and with authority hence accidental findings in a planned surgical procedure can be easily avoided. Clinical dynamic valselva and reducibility test can better documented by real time ultrasound study. In case of recurrence, Sonography will help in assessing the hernia details better as being dynamic real time investigation. Ultrasound signs in case of internal hernias are well comparable with CT findings.

Keywords: laparoscopic repair, Hernia, CT findings, chronic pain

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1577 Hepatoprotective Effect of Mycophenolate Mofetil against Tacrolimus Exposure in Rat

Authors: Ferjani Hanen, El Arem Amira, Boussema Ayed Imen, Bacha Hassen

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Tacrolimus (TAC), a calcineurin inhibitor, is clinically used as an immunosuppressive agent in the transplant recipient, but its use associated-hepatotoxicity. Mycophenolate mofetil (MMF), an anti-metabolite, is a potent immunosuppressive drug. MMF is not hepatotoxic and is the most common adjunctive immunosuppressant for TAC. The effects of TAC and MMF combination in the liver is still not well understood. This work aimed to investigate their combined effect against in liver in rats Wistar after 24 h. The oral median lethal doses (LD50) of TAC and MMF alone were evaluated in rats are 240 mg/kg and 500 mg/kg respectively. Oral administration of the MMF at 50 mg/kg to male Wistar intoxicated with TAC at 60 mg/kg, demonstrated a significant protective effect by lowering the levels of hepatic markers enzymes (AST, ALT) in the serum rat. MMF attenuated oxidative stress by restoring the activities of SOD, CAT and by reducing the malondialdehyde (MDA) and protein carbonyl levels liver. This study provided evidence that MMF protects rat liver from TAC-induced injury and suggests a most combination use for organ transplantation.

Keywords: tacrolimus, mycophenolate mofetil, combination, liver, rat

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1576 Discovering Traditional Plants Used by Indigenous People in the Tropical Rainforest of Malaysia for the Treatment of Malaria

Authors: Izdihar Ismail, Alona C. Linatoc, Maryati Mohamed

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The tropical rainforest of Malaysia is known for its rich biological diversity and high endemicity. The potential for these forests to hold the cure for many diseases and illnesses is high and much is yet to be discovered. This study explores the richness of the tropical rainforest of Endau-Rompin National Park in Johor, Malaysia in search of plants traditionally used by the indigenous people in the treatment of malaria and malaria-like symptoms. Seven species of plants were evaluated and tested for antiplasmodial activities. Different plant parts were subjected to methanolic and aqueous extractions. A total of 24 extracts were evaluated by histidine-rich protein II (HRP2) assay against K1 strain of Plasmodium falciparum chloroquine-resistant. Ten extracts showed significant inhibition of the growth of P. falciparum. Phytochemical screening of the same extracts revealed the presence of alkaloids, flavonoids, terpenoids and anthraquinones. This study affirms that tropical rainforests may still hold undiscovered cures for many diseases and illnesses that have inflicted millions of people worldwide. The species studied herein have not known to have been studied elsewhere before.

Keywords: Endau-Rompin, malaria, Malaysia, tropical rainforest, traditional knowledge

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1575 In vitro and invivo Antioxidant Studies of Grewia crenata Leaves Extract in Albino Rats

Authors: A. N.Ukwuani, A. K. Abdulfatah

Abstract:

G. crenata is used locally for the treatment of fractured bones, wound healing and inflammatory conditions. In vitro and in vivo antioxidant activity of hydromethanolic extracts of the leaves of G. crenata were assessed. The phytochemical analysis shows the presence of phenols, flavonoids, saponins, cardiac glycosides and tannins. An in vitro quantitative analysis of phenols, flavonoids and tannins respectively were (164±1.20, 199±0.88 and 88.67±0.88 mg/100g FW). In vivo studies of hydromethanolic extract demonstrated a dose dependent increase in hepatic superoxide dismutase (1.14±0.14, 2.13±0.11, 2.55±0.11 U/mg Protein) with improvement in hepatic glutathione (6.98±0.42, 8.91±0.37, 11.07±0.46 µM/mg Protein) and Catalase (4.47±0.05, 6.24±0.02, 7.17±0.04 U/mg Protein) and Total protein (6.18±0.08, 6.69±0.18, 7.27±0.16 mg/ml) respectively at 100-300mg/kg body weight Grewia crenata leaves when compared to the control and standard drug. It can be concluded from the present findings of that G. crenata leaves possess antioxidant potential.

Keywords: Grewia crenata, antioxidant, hydromethanolic extract, in vivo, in vitro

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1574 In silico Analysis of Isoniazid Resistance in Mycobacterium tuberculosis

Authors: A. Nusrath Unissa, Sameer Hassan, Luke Elizabeth Hanna

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Altered drug binding may be an important factor in isoniazid (INH) resistance, rather than major changes in the enzyme’s activity as a catalase or peroxidase (KatG). The identification of structural or functional defects in the mutant KatGs responsible for INH resistance remains as an area to be explored. In this connection, the differences in the binding affinity between wild-type (WT) and mutants of KatG were investigated, through the generation of three mutants of KatG, Ser315Thr [S315T], Ser315Asn [S315N], Ser315Arg [S315R] and a WT [S315]) with the help of software-MODELLER. The mutants were docked with INH using the software-GOLD. The affinity is lower for WT than mutant, suggesting the tight binding of INH with the mutant protein compared to WT type. These models provide the in silico evidence for the binding interaction of KatG with INH and implicate the basis for rationalization of INH resistance in naturally occurring KatG mutant strains of Mycobacterium tuberculosis.

Keywords: Mycobacterium tuberculosis, KatG, INH resistance, mutants, modelling, docking

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1573 Antioxidant Activity of Launaea nudicaulis Growing in Southwest of Algeria

Authors: Abdelkrim Cheriti, Mebarka Belboukhari, Nasser Belboukhari

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Launaea Cass. is a small genus of the family Asteraceae (tribe Lactuceae, subtribe Sonchinae), consisting of 54 species, of which 9 are presented in the flora of Algeria and is mainly distributed in the South Mediterranean, Africa and SW Asia. Plants in the Launaea genus have been used ethnobotanically as bitter stomachic, for treating diarrhea, gastrointestinal tracts, as anti-inflammatory, for skin diseases, treatment of infected wounds, hepatic pains, children fever, as soporific, lactagogue, diuretic and as insecticidal. Antioxidants are vital substances, which possess the ability to protect the body from damages caused by free radical induced oxidative stress. A variety of free radical scavenging antioxidants is found in a number of dietary sources. The main objective of this study focused on the screening of antioxidant activity of Launaea nudicaulis (Asteraceae) extracts. The in vitro antioxidant activity was investigated with DPPH radical scavenging assay. The quantitative evaluation of DPPH scavenging activity showed that n-BuOH and EtOAc extracts are the most active extracts with a percentage of antiradical activity of 89,62% and 71,57% respectively.

Keywords: Launaea, phytochemical, South Algeria, Sahara, endemic specie

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1572 Monitoring the Effect of Doxorubicin Liposomal in VX2 Tumor Using Magnetic Resonance Imaging

Authors: Ren-Jy Ben, Jo-Chi Jao, Chiu-Ya Liao, Ya-Ru Tsai, Lain-Chyr Hwang, Po-Chou Chen

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Cancer is still one of the serious diseases threatening the lives of human beings. How to have an early diagnosis and effective treatment for tumors is a very important issue. The animal carcinoma model can provide a simulation tool for the study of pathogenesis, biological characteristics and therapeutic effects. Recently, drug delivery systems have been rapidly developed to effectively improve the therapeutic effects. Liposome plays an increasingly important role in clinical diagnosis and therapy for delivering a pharmaceutic or contrast agent to the targeted sites. Liposome can be absorbed and excreted by the human body, and is well known that no harm to the human body. This study aimed to compare the therapeutic effects between encapsulated (doxorubicin liposomal, LipoDox) and un-encapsulated (doxorubicin, Dox) anti-tumor drugs using Magnetic Resonance Imaging (MRI). Twenty-four New Zealand rabbits implanted with VX2 carcinoma at left thigh were classified into three groups: control group (untreated), Dox-treated group and LipoDox-treated group, 8 rabbits for each group. MRI scans were performed three days after tumor implantation. A 1.5T GE Signa HDxt whole body MRI scanner with a high resolution knee coil was used in this study. After a 3-plane localizer scan was performed, Three-Dimensional (3D) Fast Spin Echo (FSE) T2-Weighted Images (T2WI) was used for tumor volumetric quantification. And Two-Dimensional (2D) spoiled gradient recalled echo (SPGR) dynamic Contrast-enhanced (DCE) MRI was used for tumor perfusion evaluation. DCE-MRI was designed to acquire four baseline images, followed by contrast agent Gd-DOTA injection through the ear vein of rabbits. Afterwards, a series of 32 images were acquired to observe the signals change over time in the tumor and muscle. The MRI scanning was scheduled on a weekly basis for a period of four weeks to observe the tumor progression longitudinally. The Dox and LipoDox treatments were prescribed 3 times in the first week immediately after VX2 tumor implantation. ImageJ was used to quantitate tumor volume and time course signal enhancement on DCE images. The changes of tumor size showed that the growth of VX2 tumors was effectively inhibited for both LipoDox-treated and Dox-treated groups. Furthermore, the tumor volume of LipoDox-treated group was significantly lower than that of Dox-treated group, which implies that LipoDox has better therapeutic effect than Dox. The signal intensity of LipoDox-treated group is significantly lower than that of the other two groups, which implies that targeted therapeutic drug remained in the tumor tissue. This study provides a radiation-free and non-invasive MRI method for therapeutic monitoring of targeted liposome on an animal tumor model.

Keywords: doxorubicin, dynamic contrast-enhanced MRI, lipodox, magnetic resonance imaging, VX2 tumor model

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1571 Identification and Quantification of Lisinopril from Pure, Formulated and Urine Samples by Micellar Thin Layer Chromatography

Authors: Sudhanshu Sharma

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Lisinopril, 1-[N-{(s)-I-carboxy-3 phenyl propyl}-L-proline dehydrate is a lysine analog of enalaprilat, the active metabolite of enalapril. It is long-acting, non-sulhydryl angiotensin-converting enzyme (ACE) inhibitor that is used for the treatment of hypertension and congestive heart failure in daily dosage 10-80 mg. Pharmacological activity of lisinopril has been proved in various experimental and clinical studies. Owing to its importance and widespread use, efforts have been made towards the development of simple and reliable analytical methods. As per our literature survey, lisinopril in pharmaceutical formulations has been determined by various analytical methodologies like polaragraphy, potentiometry, and spectrophotometry, but most of these analytical methods are not too suitable for the Identification of lisinopril from clinical samples because of the interferences caused by the amino acids and amino groups containing metabolites present in biological samples. This report is an attempt in the direction of developing a simple and reliable method for on plate identification and quantification of lisinopril in pharmaceutical formulations as well as from human urine samples using silica gel H layers developed with a new mobile phase comprising of micellar solutions of N-cetyl-N, N, N-trimethylammonium bromide (CTAB). Micellar solutions have found numerous practical applications in many areas of separation science. Micellar liquid chromatography (MLC) has gained immense popularity and wider applicability due to operational simplicity, cost effectiveness, relatively non-toxicity and enhanced separation efficiency, low aggressiveness. Incorporation of aqueous micellar solutions as mobile phase was pioneered by Armstrong and Terrill as they accentuated the importance of TLC where simultaneous separation of ionic or non-ionic species in a variety of matrices is required. A peculiarity of the micellar mobile phases (MMPs) is that they have no macroscopic analogues, as a result the typical separations can be easily achieved by using MMPs than aqueous organic mobile phases. Previously MMPs were successfully employed in TLC based critical separations of aromatic hydrocarbons, nucleotides, vitamin K1 and K5, o-, m- and p- aminophenol, amino acids, separation of penicillins. The human urine analysis for identification of selected drugs and their metabolites has emerged as an important investigation tool in forensic drug analysis. Among all chromatographic methods available only thin layer chromatography (TLC) enables a simple fast and effective separation of the complex mixtures present in various biological samples and is recommended as an approved testing for forensic drug analysis by federal Law. TLC proved its applicability during successful separation of bio-active amines, carbohydrates, enzymes, porphyrins, and their precursors, alkaloid and drugs from urine samples.

Keywords: lisnopril, surfactant, chromatography, micellar solutions

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1570 The Impact of Inconclusive Results of Thin Layer Chromatography for Marijuana Analysis and It’s Implication on Forensic Laboratory Backlog

Authors: Ana Flavia Belchior De Andrade

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Forensic laboratories all over the world face a great challenge to overcame waiting time and backlog in many different areas. Many aspects contribute to this situation, such as an increase in drug complexity, increment in the number of exams requested and cuts in funding limiting laboratories hiring capacity. Altogether, those facts pose an essential challenge for forensic chemistry laboratories to keep both quality and time of response within an acceptable period. In this paper we will analyze how the backlog affects test results and, in the end, the whole judicial system. In this study data from marijuana samples seized by the Federal District Civil Police in Brazil between the years 2013 and 2017 were tabulated and the results analyzed and discussed. In the last five years, the number of petitioned exams increased from 822 in February 2013 to 1358 in March 2018, representing an increase of 32% in 5 years, a rise of more than 6% per year. Meanwhile, our data shows that the number of performed exams did not grow at the same rate. Product numbers are stationed as using the actual technology scenario and analyses routine the laboratory is running in full capacity. Marijuana detection is the most prevalence exam required, representing almost 70% of all exams. In this study, data from 7,110 (seven thousand one hundred and ten) marijuana samples were analyzed. Regarding waiting time, most of the exams were performed not later than 60 days after receipt (77%). Although some samples waited up to 30 months before being examined (0,65%). When marijuana´s exam is delayed we notice the enlargement of inconclusive results using thin-layer chromatography (TLC). Our data shows that if a marijuana sample is stored for more than 18 months, inconclusive results rise from 2% to 7% and when if storage exceeds 30 months, inconclusive rates increase to 13%. This is probably because Cannabis plants and preparations undergo oxidation under storage resulting in a decrease in the content of Δ9-tetrahydrocannabinol ( Δ9-THC). An inconclusive result triggers other procedures that require at least two more working hours of our analysts (e.g., GC/MS analysis) and the report would be delayed at least one day. Those new procedures increase considerably the running cost of a forensic drug laboratory especially when the backlog is significant as inconclusive results tend to increase with waiting time. Financial aspects are not the only ones to be observed regarding backlog cases; there are also social issues as legal procedures can be delayed and prosecution of serious crimes can be unsuccessful. Delays may slow investigations and endanger public safety by giving criminals more time on the street to re-offend. This situation also implies a considerable cost to society as at some point, if the exam takes a long time to be performed, an inconclusive can turn into a negative result and a criminal can be absolved by flawed expert evidence.

Keywords: backlog, forensic laboratory, quality management, accreditation

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1569 X-Ray Shielding Properties of Bismuth-Borate Glass Doped with Rare-Earth Ions

Authors: Vincent Kheswa

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X-rays are ionizing electromagnetic radiation that is used in various industries such as computed tomography scans, dental X-rays, and screening freight trains. However, they pose health risks to humans if they are not shielded properly. In recent years, many researchers around the globe have been searching for nontoxic best possible glass materials for shielding X-rays. In this work, the x-ray shielding properties of 45Na₂O + 10 Bi₂O₃ + (5 - x)TiO₂+ (x) Nb₂O₅ + 40 P₂O₅, were x = 0, 1, 3, 5 mol%, glass materials were studied. The results revealed that the glass sample with the highest TiO2 content has the highest mass and linear attenuation coefficients and lowest half-value thickness, tenth-value thickness and mean-free path in the 20 to 80 keV energy region. The sample with 3 mol% of Nb₂O₅ has the highest mass and linear attenuation coefficients and the lowest half-value thickness, tenth-value thickness, and mean-free path at 15 keV and photon energies between 80 to 300 keV. It was, therefore, concluded that 45Na₂O + 10 Bi₂O₃ + 5 TiO₂ + 40 P₂O₅ glass is best for shielding x-rays of energies between 20 and 80 keV, while 45Na₂O + 10 Bi₂O₃ + 2 TiO₂ + 3 Nb₂O₅ + 40 P₂O₅ is best for shielding 15 keV x-rays and x-rays of energies between 80 keV and 300 keV.

Keywords: bismuth-titanium-phosphate glass, x-ray shielding, LAC, MAC, radiation shielding

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1568 Firm-Created Social Media Communication and Consumer Brand Perceptions

Authors: Rabail Khalid

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Social media has changed the business communication strategies in the corporate world. Firms are using social media to reach their maximum stakeholders in minimum time at different social media forums. The current study examines the role of firm-created social media communication on consumer brand perceptions and their loyalty to brand. An online survey is conducted through social media forums including Facebook and Twitter to collect data regarding social media communication of a well-reputed clothing company’s brand in Pakistan. A link is sent to 900 customers of that company. Out of 900 questionnaires, 534 were received. So, the response rate is 59.33%. During data screening and entry, 13 questionnaires are rejected due to incomplete answer. Therefore, 521 questionnaires are completed in all respect and seem to be helpful for the study. So, the positive response rate is 57.89%. The empirical results report positive and significant influence of company-generated social media communication on brand trust, brand equity, and brand loyalty. The findings of this study provide important information to the marketing professionals and brand managers to understand consumer behavior through social media communication.

Keywords: firm-created social media communication, brand trust, brand equity, consumer behavior, brand loyalty

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1567 Photochemical Degradation of Ibuprofren in Aqueous Solutions

Authors: Stavros Poulopoulos, Aphrodite Tetorou, Constantine Philippopoulos

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Day after day more pharmaceutical compounds that are not efficiently removed by conventional treatment methods are found in treated wastewaters and drinking waters. Due to their refractory nature, they escape conventional wastewater treatment facilities, and thus advanced oxidation processes have to be utilized to effectively eliminate them. In the present study, the removal of Ibuprofen from aqueous solutions containing the commercial drug Algofren (non-steroidal, anti-inflammatory) using UV irradiation, hydrogen peroxide, titanium dioxide and ferric ions was examined. All experiments were conducted in a batch photoreactor operated for 120 min. The main target was to select the most effective operating conditions for the mineralization of the solutions treated. The combination of Fe(III)/ H₂O₂/UV proved to be very efficient in terms of total organic carbon removal and ibuprofen conversion. For solutions containing 5 mg/L ibuprofen and initial total carbon 51.1 mg/L, complete mineralization was achieved by means of 2.2 ppm Fe(III) and 333 mg/L H₂O₂.

Keywords: pharmaceuticals, photocatalytic, photo-Fenton, TiO₂

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1566 In Silico Modeling of Drugs Milk/Plasma Ratio in Human Breast Milk Using Structures Descriptors

Authors: Navid Kaboudi, Ali Shayanfar

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Introduction: Feeding infants with safe milk from the beginning of their life is an important issue. Drugs which are used by mothers can affect the composition of milk in a way that is not only unsuitable, but also toxic for infants. Consuming permeable drugs during that sensitive period by mother could lead to serious side effects to the infant. Due to the ethical restrictions of drug testing on humans, especially women, during their lactation period, computational approaches based on structural parameters could be useful. The aim of this study is to develop mechanistic models to predict the M/P ratio of drugs during breastfeeding period based on their structural descriptors. Methods: Two hundred and nine different chemicals with their M/P ratio were used in this study. All drugs were categorized into two groups based on their M/P value as Malone classification: 1: Drugs with M/P>1, which are considered as high risk 2: Drugs with M/P>1, which are considered as low risk Thirty eight chemical descriptors were calculated by ACD/labs 6.00 and Data warrior software in order to assess the penetration during breastfeeding period. Later on, four specific models based on the number of hydrogen bond acceptors, polar surface area, total surface area, and number of acidic oxygen were established for the prediction. The mentioned descriptors can predict the penetration with an acceptable accuracy. For the remaining compounds (N= 147, 158, 160, and 174 for models 1 to 4, respectively) of each model binary regression with SPSS 21 was done in order to give us a model to predict the penetration ratio of compounds. Only structural descriptors with p-value<0.1 remained in the final model. Results and discussion: Four different models based on the number of hydrogen bond acceptors, polar surface area, and total surface area were obtained in order to predict the penetration of drugs into human milk during breastfeeding period About 3-4% of milk consists of lipids, and the amount of lipid after parturition increases. Lipid soluble drugs diffuse alongside with fats from plasma to mammary glands. lipophilicity plays a vital role in predicting the penetration class of drugs during lactation period. It was shown in the logistic regression models that compounds with number of hydrogen bond acceptors, PSA and TSA above 5, 90 and 25 respectively, are less permeable to milk because they are less soluble in the amount of fats in milk. The pH of milk is acidic and due to that, basic compounds tend to be concentrated in milk than plasma while acidic compounds may consist lower concentrations in milk than plasma. Conclusion: In this study, we developed four regression-based models to predict the penetration class of drugs during the lactation period. The obtained models can lead to a higher speed in drug development process, saving energy, and costs. Milk/plasma ratio assessment of drugs requires multiple steps of animal testing, which has its own ethical issues. QSAR modeling could help scientist to reduce the amount of animal testing, and our models are also eligible to do that.

Keywords: logistic regression, breastfeeding, descriptors, penetration

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1565 Screening for Antibacterial, Antifungal and Cytotoxic Agents in Three Hard Coral Species from Persian Gulf

Authors: Maryam Ehsanpou, Majid Afkhami, Flora Mohammadizadeh, Amirhoushang Bahri, Rastin Afkhami

Abstract:

Within the frame of a biodiversity and bioactivity study of marine macro organisms from the Persian Gulf, three hard coral species extracts were investigated for cytotoxic, antibacterial and antifungal activities against five human pathogenic microorganisms. All concentrations of extracts from three hard corals showed no antifungal activity towards the tested strains. In antibacterial assays, the hard coral extracts showed significant activity solely against Staphylococcus aureus with MICs ranging from 3 to 9 μg/ml. The highest antibacterial activity was found in the aqueous methanol extract of Porites compressa with an inhibition zone of 22 mm against Staphylococcus aureus at 18 μg/ml extract concentration. Methanol extracts from Porites harrisoi and Porites compressa exhibited only weak cytotoxic activities. It is important for future research to concentrate on finding the mechanisms employed by corals to defend themselves against invasion, the mechanism of infections and the type of chemical compounds in coral extracts that inhibit antibacterial growth or proliferation in underexplored areas such as the Persian Gulf.

Keywords: antibacterial, antifungal, cytotoxic, hard corals, Persian Gulf

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1564 The Influence of Carbamazepine on the Activity of CYP3A4 in Patients with Alcoholism

Authors: Mikhail S. Zastrozhin, Valery V. Smirnov, Dmitry A. Sychev, Ludmila M. Savchenko, Evgeny A. Bryun, Mark O. Nechaev

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Cytochrome P-450 isoenzyme 3A4 takes part in the biotransformation of medical drugs. The activity of CYP isoenzymes depends on genetic (polymorphisms of genes which encoded it) and phenotypic factors (a kind of food, a concomitant drug therapy). The aim of the study was to evaluate a carbamazepine effect on the CYP3A4 activity in patients with alcohol addiction. The study included 25 men with alcohol dependence, who received haloperidol during the exacerbation of the addiction. CYP3A4 activity was assessed by urinary 6-beta-hydroxycortisol/cortisol ratios measured by high performance liquid chromatography with mass spectrometry. The study modeled a graph and an equation of the logarithmic regression, that reflects the dependence of CYP3A4 activity on a dose of carbamazepine: y = 5,5 * 9,1 * 10-5 * x2. The study statistically significant demonstrates the effect of carbamazepine on CYP2D6 isozyme activity in patients with alcohol addiction.

Keywords: CYP3A4, biotransformation, carbamazepine, alcohol abuse

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1563 Functionalized Nanoparticles for Biomedical Applications

Authors: Temesgen Geremew

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Functionalized nanoparticles have emerged as a revolutionary class of materials with immense potential in various biomedical applications. These engineered nanoparticles possess unique properties tailored to interact with biological systems, offering unprecedented opportunities in drug delivery, imaging, diagnostics, and therapy. This research delves into the design, synthesis, and characterization of functionalized nanoparticles for targeted biomedical applications. The primary focus lies on developing nanoparticles with precisely controlled size, surface chemistry, and biocompatibility for specific medical purposes. The research will also explore the crucial interaction of these nanoparticles with biological systems, encompassing cellular uptake, biodistribution, and potential toxicity evaluation. The successful development of functionalized nanoparticles holds the promise to revolutionize various aspects of healthcare. This research aspires to contribute significantly to this advancement by providing valuable insights into the design and application of these versatile materials within the ever-evolving field of biomedicine.

Keywords: nanoparticles, biomedicals, cancer, biocompatibility

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1562 Enhancing Food Quality and Safety Management in Ethiopia's Food Processing Industry: Challenges, Causes, and Solutions

Authors: Tuji Jemal Ahmed

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Food quality and safety challenges are prevalent in Ethiopia's food processing industry, which can have adverse effects on consumers' health and wellbeing. The country is known for its diverse range of agricultural products, which are essential to its economy. However, poor food quality and safety policies and management systems in the food processing industry have led to several health problems, foodborne illnesses, and economic losses. This paper aims to highlight the causes and effects of food safety and quality issues in the food processing industry of Ethiopia and discuss potential solutions to address these issues. One of the main causes of poor food quality and safety in Ethiopia's food processing industry is the lack of adequate regulations and enforcement mechanisms. The absence of comprehensive food safety and quality policies and guidelines has led to substandard practices in the food manufacturing process. Moreover, the lack of monitoring and enforcement of existing regulations has created a conducive environment for unscrupulous businesses to engage in unsafe practices that endanger the public's health. The effects of poor food quality and safety are significant, ranging from the loss of human lives, increased healthcare costs, and loss of consumer confidence in the food processing industry. Foodborne illnesses, such as diarrhea, typhoid fever, and cholera, are prevalent in Ethiopia, and poor food quality and safety practices contribute significantly to their prevalence. Additionally, food recalls due to contamination or mislabeling often result in significant economic losses for businesses in the food processing industry. To address these challenges, the Ethiopian government has begun to take steps to improve food quality and safety in the food processing industry. One of the most notable initiatives is the Ethiopian Food and Drug Administration (EFDA), which was established in 2010 to regulate and monitor the quality and safety of food and drug products in the country. The EFDA has implemented several measures to enhance food safety, such as conducting routine inspections, monitoring the importation of food products, and enforcing strict labeling requirements. Another potential solution to improve food quality and safety in Ethiopia's food processing industry is the implementation of food safety management systems (FSMS). An FSMS is a set of procedures and policies designed to identify, assess, and control food safety hazards throughout the food manufacturing process. Implementing an FSMS can help businesses in the food processing industry identify and address potential hazards before they cause harm to consumers. Additionally, the implementation of an FSMS can help businesses comply with existing food safety regulations and guidelines. In conclusion, improving food quality and safety policies and management systems in Ethiopia's food processing industry is critical to protecting public health and enhancing the country's economy. Addressing the root causes of poor food quality and safety and implementing effective solutions, such as the establishment of regulatory agencies and the implementation of food safety management systems, can help to improve the overall safety and quality of the country's food supply.

Keywords: food quality, food safety, policy, management system, food processing industry

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1561 Development and Characterization of Bio-Tribological, Nano- Multilayer Coatings for Medical Tools Application

Authors: L. Major, J. M. Lackner, M. Dyner, B. Major

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Development of new generation bio- tribological, multilayer coatings, opens an avenue for fabrication of future high- tech functional surfaces. In the presented work, nano- composite, Cr/CrN+[Cr/ a-C:H implanted by metallic nanocrystals] multilayer coatings have been developed for surface protection of medical tools. Thin films were fabricated by a hybrid Pulsed Laser Deposition technique. Complex microstructure analysis of nano- multilayer coatings, subjected to mechanical and biological tests, were performed by means of transmission electron microscopy (TEM). Microstructure characterization revealed the layered arrangement of Cr23C6 nanoparticles in multilayer structure. Influence of deposition conditions on bio- tribological properties of the coatings were studied. The bio-tests were used as a screening tool for the analyzed nano- multilayer coatings before they could be deposited on medical tools. Bio- medical tests were done using fibroblasts. The mechanical properties of the coatings were investigated by means of a ball-on-disc mechanical test. The microhardness was done using Berkovich indenter. The scratch adhesion test was done using Rockwell indenter. From the bio- tribological point of view, the optimal properties had the C106_1 material.

Keywords: bio- tribological coatings, cell- material interaction, hybrid PLD, tribology

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1560 A Greener Approach towards the Synthesis of an Antimalarial Drug Lumefantrine

Authors: Luphumlo Ncanywa, Paul Watts

Abstract:

Malaria is a disease that kills approximately one million people annually. Children and pregnant women in sub-Saharan Africa lost their lives due to malaria. Malaria continues to be one of the major causes of death, especially in poor countries in Africa. Decrease the burden of malaria and save lives is very essential. There is a major concern about malaria parasites being able to develop resistance towards antimalarial drugs. People are still dying due to lack of medicine affordability in less well-off countries in the world. If more people could receive treatment by reducing the cost of drugs, the number of deaths in Africa could be massively reduced. There is a shortage of pharmaceutical manufacturing capability within many of the countries in Africa. However one has to question how Africa would actually manufacture drugs, active pharmaceutical ingredients or medicines developed within these research programs. It is quite likely that such manufacturing would be outsourced overseas, hence increasing the cost of production and potentially limiting the full benefit of the original research. As a result the last few years has seen major interest in developing more effective and cheaper technology for manufacturing generic pharmaceutical products. Micro-reactor technology (MRT) is an emerging technique that enables those working in research and development to rapidly screen reactions utilizing continuous flow, leading to the identification of reaction conditions that are suitable for usage at a production level. This emerging technique will be used to develop antimalarial drugs. It is this system flexibility that has the potential to reduce both the time was taken and risk associated with transferring reaction methodology from research to production. Using an approach referred to as scale-out or numbering up, a reaction is first optimized within the laboratory using a single micro-reactor, and in order to increase production volume, the number of reactors employed is simply increased. The overall aim of this research project is to develop and optimize synthetic process of antimalarial drugs in the continuous processing. This will provide a step change in pharmaceutical manufacturing technology that will increase the availability and affordability of antimalarial drugs on a worldwide scale, with a particular emphasis on Africa in the first instance. The research will determine the best chemistry and technology to define the lowest cost manufacturing route to pharmaceutical products. We are currently developing a method to synthesize Lumefantrine in continuous flow using batch process as bench mark. Lumefantrine is a dichlorobenzylidine derivative effective for the treatment of various types of malaria. Lumefantrine is an antimalarial drug used with artemether for the treatment of uncomplicated malaria. The results obtained when synthesizing Lumefantrine in a batch process are transferred into a continuous flow process in order to develop an even better and reproducible process. Therefore, development of an appropriate synthetic route for Lumefantrine is significant in pharmaceutical industry. Consequently, if better (and cheaper) manufacturing routes to antimalarial drugs could be developed and implemented where needed, it is far more likely to enable antimalarial drugs to be available to those in need.

Keywords: antimalarial, flow, lumefantrine, synthesis

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1559 Screening, Selection and Optimization of Extracellular Methanol and Ethanol Tolerant Lipase from Acinetobacter sp. K5B4

Authors: Khaled M. Khleifat

Abstract:

An extracellular methanol and ethanol tolerant lipase producing bacterial strain K5b4 was isolated from soil samples contaminated with hydrocarbon residues. It was identified by using morphological and biochemical characteristics and 16srRNA technique as Acinetobacter species. The immobilized lipase from Acinetobacter sp. K5b4 retained more than 98% of its residual activity after incubation with pure methanol and ethanol for 24 hours. The highest hydrolytic activity of the immobilized enzyme was obtained in the presence of 75% (v/v) methanol in the assay solution. In contrary, the enzyme was able to maintain its original activity up to only 25% (v/v) ethanol whereas at elevated concentrations of 50 and 75% (v/v) the enzyme activity was reduced to 10 and 40%, respectively. Maximum lipase activity of 31.5 mU/mL was achieved after 48 hr cultivation when the optimized medium (pH 7.0) that composed of 1.0% (w/v) olive oil, 0.2% (w/v) glycerol, 0.15% (w/v) yeast extract, and 0.05% (w/v) NaCl was inoculated with 0.4% (v/v) seed culture and incubated at 30°C and 150 rpm agitation speed. However, the presence of CaCl2 in the growth media did not show any inhibitory or stimulatory effect on the enzyme production as it compared to the control experiment. Meanwhile, the other mineral salts MgCl2, MnCl2, KCl and CoCl2 were negatively affected the production of lipase enzyme. The inhibition of lipase production from Acinetobacter sp. K5b4 in presence of glucose suggesting that lipase gene expression is prone to catabolic repression.

Keywords: K5B4, methanol and ethanol, acinetobacter, morphological

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1558 Digital Retinal Images: Background and Damaged Areas Segmentation

Authors: Eman A. Gani, Loay E. George, Faisel G. Mohammed, Kamal H. Sager

Abstract:

Digital retinal images are more appropriate for automatic screening of diabetic retinopathy systems. Unfortunately, a significant percentage of these images are poor quality that hinders further analysis due to many factors (such as patient movement, inadequate or non-uniform illumination, acquisition angle and retinal pigmentation). The retinal images of poor quality need to be enhanced before the extraction of features and abnormalities. So, the segmentation of retinal image is essential for this purpose, the segmentation is employed to smooth and strengthen image by separating the background and damaged areas from the overall image thus resulting in retinal image enhancement and less processing time. In this paper, methods for segmenting colored retinal image are proposed to improve the quality of retinal image diagnosis. The methods generate two segmentation masks; i.e., background segmentation mask for extracting the background area and poor quality mask for removing the noisy areas from the retinal image. The standard retinal image databases DIARETDB0, DIARETDB1, STARE, DRIVE and some images obtained from ophthalmologists have been used to test the validation of the proposed segmentation technique. Experimental results indicate the introduced methods are effective and can lead to high segmentation accuracy.

Keywords: retinal images, fundus images, diabetic retinopathy, background segmentation, damaged areas segmentation

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1557 MTT Assay-Guided Isolation of a Cytotoxic Lead from Hedyotis umbellata and Its Mechanism of Action against Non-Small Cell Lung Cancer A549 Cells

Authors: Kirti Hira, A. Sajeli Begum, S. Mahibalan, Poorna Chandra Rao

Abstract:

Introduction: Cancer is one of the leading causes of death worldwide. Although existing therapy effectively kills cancer cells, they do affect normal growing cells leading to many undesirable side effects. Hence there is need to develop effective as well as safe drug molecules to combat cancer, which is possible through phyto-research. The currently available plant-derived blockbuster drugs are the example for this. In view of this, an investigation was done to identify cytotoxic lead molecules from Hedyotis umbellata (Family Rubiaceae), a widely distributed weed in India. Materials and Methods: The methanolic extract of the whole plant of H. umbellata (MHU), prepared through Soxhlet extraction method was further fractionated with diethyl ether and n-butanol, successively. MHU, ether fraction (EMHU) and butanol fraction (BMHU) were lyophilized and were tested for the cytotoxic effect using 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay against non-small cell lung cancer (NSCLC) A549 cell lines. The potentially active EMHU was subjected to chromatographic purification using normal-phase silica columns, in order to isolate the responsible bioactive compounds. The isolated pure compounds were tested for their cytotoxic effect by MTT assay against A549 cells. Compound-3, which was found to be most active, was characterized using IR, 1H- and 13C-NMR and MS analysis. The study was further extended to decipher the mechanism of action of cytotoxicity of compound-3 against A549 cells through various in vitro cellular models. Cell cycle analysis was done using flow cytometry following PI (Propidium Iodide) staining. Protein analysis was done using Western blot technique. Results: Among MHU, EMHU, and BMHU, the non-polar fraction EMHU demonstrated a significant dose-dependent cytotoxic effect with IC50 of 67.7μg/ml. Chromatography of EMHU yielded seven compounds. MTT assay of isolated compounds explored compound-3 as potentially active one, which inhibited the growth of A549 cells with IC50value of 14.2μM. Further, compound-3 was identified as cedrelopsin, a coumarin derivative having molecular weight of 260. Results of in vitro mechanistic studies explained that cedrelopsin induced cell cycle arrest at G2/M phase and down-regulated the expression of G2/M regulatory proteins such as cyclin B1, cdc2, and cdc25C, dose dependently. This is the first report that explores the cytotoxic mechanism of cedrelopsin. Conclusion: Thus a potential small lead molecule, cedrelopsin isolated from H. umbellata, showing antiproliferative effect mediated by G2/M arrest in A549 cells was discovered. The effect of cedrelopsin against other cancer cell lines followed by in vivo studies can be performed in future to develop a new drug candidate.

Keywords: A549, cedrelopsin, G2/M phase, Hedyotis umbellata

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1556 Drug Residues Disposal from Wastewater Using Carbon Nanomaterials

Authors: Stefan Nicolae, Cristina Cirtoaje, Emil Petrescu, Florin-Razvan Duca

Abstract:

In the context of the accelerated expansion of urban agglomerations and the exponential development of industry, a huge amount of water is used, and a crisis of drinking water may occur any time. Classic wastewater treatment removes most pollutants but, for some chemical residues, special methods are needed. Carbon nanotubes and other carbon materials might be used in many cases [1-2], especially for heavy metals removal but also on pharmaceutical products such as paracetamol [3]. Our research has confirmed the better efficiency of nanotubes compared to graphene on paracetamol removal from water, but even better results were obtained on single-walled nanotubes (SWCNTs) and graphene nanoplatelets. This can be due to their better dispersion in water which leads to an increased contact surface, so we propose a filtration system of membranes and carbon materials that can be used for paracetamol removal from wastewater but also for other drugs that affect the aquatic life as well as terrestrial animals and people who use this contaminated water.

Keywords: applied physics, wastewater, nanomaterials, enviromental science

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1555 Secondary Metabolites from Turkish Marine-Derived Fungi Hypocrea nigricans

Authors: H. Heydari, B. Konuklugil, P. Proksch

Abstract:

Marine-derived fungi can produce interesting bioactive secondary metabolites that can be considered the potential for drug development. Turkey is a country of a peninsula surrounded by the Black Sea at the north, the Aegean Sea at the west, and the Mediterranean Sea at the south. Despite the approximately 8400 km of coastline, studies on marine secondary metabolites and their biological activity are limited. In our ongoing search for new natural products with different bioactivities produced by the marine-derived fungi, we have investigated secondary metabolites of Turkish collection of the marine sea slug (Peltodoris atromaculata) associated fungi Hypocrea nigricans collected from Seferihisar in the Egean sea. According to the author’s best knowledge, no study was found on this fungal species in terms of secondary metabolites. Isolated from ethyl acetate extract of the culture of Hypocrea nigricans were (isodihydroauroglaucin,tetrahydroauroglaucin and dihydroauroglaucin. The structures of the compounds were established based on an NMR and MS analysis. Structural elucidation of another isolated secondary metabolite/s continues.

Keywords: Hypocrea nigricans, isolation, marine fungi, secondary metabolites

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1554 Metastatic Invasive Lobular Cancer Presenting as a Cervical Polyp

Authors: Sally Shepherd, Craig Murphy

Abstract:

Introduction: The uterus or cervix are unusual locations as metastatic sites for cancers. It is further unusual for it to be a site of metastasis, whilst the primary malignancy remains occult. Case Report: A 63-year-old female with three months of altered bowel habits underwent a CT scan of the abdomen and pelvis, revealing a bulky uterus and left ovary, nonspecific colonic thickening, and diffuse peritoneal changes. She underwent colposcopy, which revealed a large endocervical polyp that was excised, revealing strongly hormone-positive metastatic invasive lobular breast cancer. She subsequently underwent a PET scan, which showed moderately diffuse activity in the cervix and left adnexa. Breast examination was unremarkable, and screening mammography, ultrasound, and MRI of the breast did not identify any lesions. Her blood tests revealed a Ca 15-3 of 934, CA-125 of 220, and CEA of 27. She was commenced on letrozole and ribociclib with an improvement in her symptoms. Conclusion: It is rare for occult breast cancer to be established and diagnosed by pelvic imaging and biopsy. Suspicion of uterine or cervical metastasis should be heightened in patients with an active or past history of breast cancer.

Keywords: occult breast cancer, cervical metastasis, invasive lobular carcinoma, metastasis

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1553 Naturally Occurring Chemicals in Biopesticides' Resistance Control through Molecular Topology

Authors: Riccardo Zanni, Maria Galvez-Llompart, Ramon Garcia-Domenech, Jorge Galvez

Abstract:

Biopesticides, such as naturally occurring chemicals, pheromones, fungi, bacteria and insect predators are often a winning choice in crop protection because of their environmental friendly profile. They are considered to have lower toxicity than traditional pesticides. After almost a century of pesticides use, resistances to traditional insecticides are wide spread, while those to bioinsecticides have raised less attention, and resistance management is frequently neglected. This seems to be a crucial mistake since resistances have already occurred for many marketed biopesticides. With an eye to the future, we present here a selection of new natural occurring chemicals as potential bioinsecticides. The molecules were selected using a consolidated mathematical paradigm called molecular topology. Several QSAR equations were depicted and subsequently applied for the virtual screening of hundred thousands molecules of natural origin, which resulted in the selection of new potential bioinsecticides. The most innovative aspect of this work does not only reside in the importance of the identification of new molecules overcoming biopesticides’ resistances, but on the possibility to promote shared knowledge in the field of green chemistry through this unique in silico discipline named molecular topology.

Keywords: green chemistry, QSAR, molecular topology, biopesticide

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1552 Biotechnology Approach: A Tool of Enhancement of Sticky Mucilage of Pulicaria Incisa (Medicinal Plant) for Wounds Treatment

Authors: Djamila Chabane, Asma Rouane, Karim Arab

Abstract:

Depending of the chemical substances responsible for the pharmacological effects, a future therapeutic drug might be produced by extraction from whole plants or by callus initiated from some parts. The optimized callus culture protocols now offer the possibility to use cell culture techniques for vegetative propagation and open minds for further studies on secondary metabolites and drug establishment. In Algerian traditional medicine, Pulicaria incisa (Asteraceae) is used in the treatment of daily troubles (stomachache, headhache., cold, sore throat and rheumatic arthralgia). Field findings revealed that many healers use some fresh parts (leaves, flowers) of this plant to treat skin wounds. This study aims to evaluate the healing efficiency of artisanal cream prepared from sticky mucilage isolated from calluses on dermal wounds of animal models. Callus cultures were initiated from reproductive explants (young inflorescences) excised from adult plants and transferred to a MS basal medium supplemented with growth regulators and maintained under dark for for months. Many calluses types were obtained with various color and aspect (friable, compact). Several subcultures of calli were performed to enhance the mucilage accumulation. After extraction, the mucilage extracts were tested on animal models as follows. The wound healing potential was studied by causing dermal wounds (1 cm diameter) at the dorsolumbar part of Rattus norvegicus; different samples of the cream were applied after hair removal on three rats each, including two controls (one treated by Vaseline and one without any treatment), two experimental groups (experimental group 1, treated with a reference ointment "Madecassol® and experimental group 2 treated by callus mucilage cream for a period of seventeen days. The evolution of the healing activity was estimated by calculating the percentage reduction of the area wounds treated by all compounds tested compared to the controls by using AutoCAD software. The percentage of healing effect of the cream prepared from callus mucilage was (99.79%) compared to that of Madecassol® (99.76%). For the treatment time, the significant healing activity was observed after 17 days compared to that of the reference pharmaceutical products without any wound infection. The healing effect of Madecassol® is more effective because it stimulates and regulates the production of collagen, a fibrous matrix essential for wound healing. Mucilage extracts also showed a high capacity to heal the skin without any infection. According to this pharmacological activity, we suggest to use calluses produced by in vitro culture to producing new compounds for the skin care and treatment.

Keywords: calluses, Pulicaria incisa, mucilage, Wounds

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1551 Pattern Of Polymorphism SLC22A1 Gene In Children With Diabetes Mellitus Type 2

Authors: Elly Usman, S. Dante, Diah Purnamasari

Abstract:

Type 2 diabetes mellitus ( T2DM ) is a syndrome characterized by a state of increased blood sugar levels due to chronic disorders of insulin secretion by pancreatic beta cells and insulin action or a combination of both. The organic cation transporter 1, encoded by the SLC22A1 gene, responsible for the uptake of the antihyperglycemic drug, metformin, in the hepatocyte. We assessed whether a genetic variation in the SLC22A1 gene was associated with the glucose - lowering effect of metformin. Method case study research design. Samples are children with type 2 diabetes mellitus who meet the inclusion criteria. The results proportions SLC22A1 gene polymorphisms in children with diabetes mellitus type 2 amounted to 52.04 % at position 400T/C, there is one heterozygous and one at position 595T/C Conclusion The presence of SLC22A1 gene polymorphisms in children with diabetes mellitus type 2.

Keywords: diabetes Mellitus type 2, metformin, organic cation transporter 1, pharmacogenomics

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1550 Hepatitis B Virus Infection Among Egyptian Children Vaccinated during Infancy

Authors: Iman I. Salama, Samia M. Sami, Somaia I. Salama, Zeinab N. Said, Thanaa M. Rabah, Aida M. Abdel-Mohsin

Abstract:

This is a national community-based project to evaluate the effectiveness of HBV vaccination program in prevention of infection. HBV markers were tested in the sera of 3600 vaccinated children. Infected children were followed up for 1 year. Prevalence of HBV infection was 0.39 % (0.28% positive for anti-HBc, 0.03% positive for HBsAg and 0.08% positive for both). One year later, 50% of positive anti-HBc children turned negative with sustained positivity for positive HBsAg cases. HBV infection was significantly higher at age above 9 years (0.6%) compared to 0.2% at age 3-9 years and 0% at younger age (P < 0.05). Logistic analysis revealed that predictors for HBV infection were history of blood transfusion, regular medical injection, and family history of either HBV infection or drug abuse (adjusted odds ratios 6.2, 5.6, 7.6 & 19.1 respectively). HBV vaccination program produced adequate protection. Adherence to infection control measures and safe blood transfusion are recommended.

Keywords: HBV infection, HBV vaccine, children, Egypt

Procedia PDF Downloads 438