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Current Drug Discovery Technologies

Subhamay Panda, Leena Kumari
Snake bite envenoming cause high rates of morbidity and mortality and is one of the serious health related concern all over the globe. Around 3200 species of snakes have been discovered till date. Amid these species, about 1300 species of snakes are venomous. On account of its severity, World Health Organization (WHO) recently included snake bite envenoming in the list of neglected tropical diseases. Immunotherapy has partially solved the issues related to snake bite envenomation. However, it is associated with numerous adverse effects, due to which alternative treatment strategies are required for the treatment of snake bite...
July 17, 2018: Current Drug Discovery Technologies
Ruchi Sharma, Rekha Rao, Sunil Kumar, Sheefali Mahant, Sarita Khatkar
Mosquito borne diseases such as malaria, filariasis, chikunguniya, yellow fever, dengue and Japanese encephalitis are the major cause of remarkable morbidity and mortality in livestock and humans worldwide. Since ancient times, aromatic plants are used for their medicinal value. Essential oils derived from these plants may be used as effective alternatives/adjuvents in pharmaceuticals, biomedical, cosmetic, food, veterinary and agriculture applications. These oils have also gained popularity and interest for prevention and treatment of various disorders...
July 17, 2018: Current Drug Discovery Technologies
Murugaboopathi Gurusamy, Jainul Fathima
Dengue Fever is a major threatening global health issue caused by a mosquito-borne pathogen. Even though some anti-viral drugs are now available to reduce the disease severity. Still, there is a need for better drug compound to combat with dengue fever. The NS2B/NS3 protease is a major therapeutic drug target for Insilco drug discovery. Previously, we have performed a pharmacophore feature based virtual screening studies, which has led to the identification of ZINC92615064 compound as a potent NS2B/NS3 protease inhibitor and demonstrated its potential to act as anti-dengue drug-like compound using computational approaches...
July 9, 2018: Current Drug Discovery Technologies
Elham Parsa, Roshanak Mokaberinejad, Mahmood Khodadoost, Armin Zareiyan, Morteza Mojahedi, Farideh Yaghmaei, Parisa Jafari, Fatemeh Hakimi
The increasing prevalence of obesity is one of the problems of today's society. Man needs food to continue living, activities, and even the metabolism of food and appetite plays an important role in receiving foods, Appetite and weight reducing synthetic drugs are recommended for some patients with high prices and significant side effects, and limited effectiveness in the treatment of obesity. Given the epidemic of obesity and the lack of satisfaction with synthetic drugs these days, people are more likely to use herbal medicines...
July 3, 2018: Current Drug Discovery Technologies
Tielle Moraes de Almeida, Gilsane Lino von Poser, Liz Girardi Muller, Paula Reis Pereira, Eduardo Cassel, Rubem M F Vargas, Nilson Junior da Silva Nunes, David Driemeier, Eliane Dallegrave, Stella de Faria Valle
Species of Valeriana show sedative, hypnotic, anxiolytic, antidepressant and anti-inflammatory properties, which are associated with valepotriates. However, data about toxicity and safety of these compounds are still limited. The aim of this study was to investigate the toxicity of a valepotriate-enriched fraction (VAL) from Valeriana glechomifolia Meyer based on the Organization for Economic Cooperation and Development (OECD) guidelines 423 and 407. In the acute study, CF1 mice were treated with a single dose of VAL (2000 mg/kg, p...
June 29, 2018: Current Drug Discovery Technologies
Shrayanee Das, Saif Hameed, Zeeshan Fatima
Tuberculosis (TB) caused by Mycobacterium tuberculosis (MTB), still remains a deadly disease worldwide. With prolonged usage of anti-TB drugs, the current therapeutic regimes are becoming ineffective, particularly due to emergence of drug resistance in MTB. Under such compelling circumstances, it is pertinent to look for new drug targets. The cell wall envelope of MTB is composed of unique lipids that are frequently targeted for anti-TB therapy. This is evident from the fact that most of the commonly used front line drugs (Isoniazid and Ethambutol) acts on lipid machinery of MTB...
June 4, 2018: Current Drug Discovery Technologies
Darja Kanduc
Anti-ovarian cancer vaccines based on minimal immune determinants uniquely expressed in ovarian cancer biomarkers and absent in the human proteome appear to promise a high level of sensitivity and specificity for early ovarian cancer immunodiagnostics, immunoprevention, and immunotherapy. In this context, the present study analyses three ovarian cancer biomarkers - namely sperm surface protein Sp17, WAP four-disulfide core domain protein 2, and müllerian-inhibiting substance - and describes a methodology for constructing ovarian cancer biomarker-derived oligopeptide constructs that might be useful for developing new diagnostic and immunotherapeutic approaches...
May 24, 2018: Current Drug Discovery Technologies
Ramin Ansari, Mohammad Mehdi Zarshenas, Amir Hossein Dadbakhsh
INTRODUCTION AND BACKGROUND: Linum usitatissimum L., known as common Flax or linseed, from the family Linnaceae, has long been cultivated in different nations due to its applications in medicine and industry. The present study aims to collect nearly all available information about chemical constituents of Flax, as well as pharmacological properties and confirmed clinical usages of it. METHODS: We searched through databases such as Scopus and PubMed for relevant literatures using the keywords: (Linum usitatissimum), (pharmacology) and (phytochemical) from the beginning to 13 Aug 2017...
May 20, 2018: Current Drug Discovery Technologies
Mahsa Taeb, Abdollah Jafarzadeh, Seyed Shahabeddin Mortazavi-Jahromi, Nahid Zainodini, Mohammad Reza Mirzaei, Fahimeh Jafarnezhad-Ansariha, Zahra Aghazadeh, Abbas Mirshafiey
OBJECTIVE: This research aimed to study the anti-aging and anti-inflammatory effects of low and high doses of the β-D-mannuronic (M2000) on gene expression of enzymes involved in oxidative stress (including SOD2, GST, GPX1, CAT, iNOS, and MPO) in peripheral blood mononuclear cells (PBMCs) of healthy donors under in vitro conditions. METHODS: The PBMCs were separated and the RNAs were then extracted and the cDNAs synthesized, and expression levels of the mentioned genes were detected by qRT-PCR...
May 15, 2018: Current Drug Discovery Technologies
Jagdish K Sahu, Arun K Mishra
OBJECTIVE: Ozenoxacin is one of the potent quinolone antibiotics, recently approved by the United States Food and Drug Administration (USFDA) with reported pharmacology to treat the impetigo. The demand for better acting topical formulation is increasing day by day. The present review is an attempt to summarize the facts behind the chemistry and biological applications of Ozenoxacin. Mechanism of action: This novel drug being a quinolone antibiotic compound, acts by inhibiting DNA gyrase A and topoisomerase IV and affects supercoiling, supercoil relaxation, chromosomal condensation, chromosomal decatenation and many others...
May 2, 2018: Current Drug Discovery Technologies
Javad Behravan, Atefeh Razazan, Ghazal Behravan
Breast cancer is the second leading cause of cancer death among women. National cancer institute of the US estimates that one in eight women will be diagnosed with breast cancer during their life time. Considering the devastating effects of the disease and the alarming numbers many scientists and research groups have devoted their research to fight breast cancer. Several recommendations are to be considered as preventing measures which include living a healthy life style, regular physical activity, weight control and, smoking cessation...
May 2, 2018: Current Drug Discovery Technologies
Rasmus N Klitgaard, Anders Lobner-Olesen
BACKGROUND: One of many strategies to overcome antibiotic resistance is the discovery of compounds targeting cellular processes, which have not yet been exploited. METHODS AND MATERIALS: Using various genetic tools, we constructed a novel high throughput, cell based, fluorescence screen for inhibitors of chromosome replication initiation in bacteria. RESULTS: The screen was validated by expression of an intra-cellular cyclic peptide interfering with the initiator protein DnaA and by over-expression of the negative initiation regulator SeqA...
April 22, 2018: Current Drug Discovery Technologies
Kenneth Lundstrom
Epigenetic mechanisms comprising of DNA methylation, histone modifications and gene silencing by RNA interference have been strongly linked to the development and progression of various diseases. These findings have triggered research on epigenetic functions and signal pathways as targets for novel drug discovery. Dietary intake has also presented significant influence on human health and disease development and nutritional modifications have proven important in prevention, but also treatment of disease. Moreover, a strong link between nutrition and epigenetic changes has been established...
April 19, 2018: Current Drug Discovery Technologies
Jacob Peedicayil
The rapid and major advances being made in epigenetics is impacting pharmacology, giving rise to new sub-disciplines in pharmacology, pharmacoepigenetics, the study of the epigenetic basis of variation in response to drugs; and pharmacoepigenomics, the application of pharmacoepigenetics on a genome-wide scale. This article gives an overview of the current state of knowledge of pharmacoepigenetics and pharmacoepigenomics. The article highlights the following areas: epigenetic therapy, the role of epigenetics in pharmacokinetics, the relevance of epigenetics to adverse drug reactions, personalized medicine, drug addiction, and drug resistance, and the use of epigenetic biomarkers in drug therapy...
April 19, 2018: Current Drug Discovery Technologies
Rajalakshmi Rukmangathen, Indira Muzib Yallamalli, Prasanna Raju Yalavarthi
Selegiline hydrochloride, a hydrophilic anti-Parkinson' moiety, undergoes extensive first-pass metabolism and has low bioavailability. A process to obtain of selegiline (SH) loaded chitosan nanoparticles was attempted to circumvent the above problem, through intranasal delivery. SH loaded polymeric nanoparticles were prepared by ionic gelation of chitosan with tripolyphosphate, and stabilized by tween 80/ poloxamer 188. The resulting nanoparticles (NPs) were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, particle size, zeta potential and surface morphology by scanning electron microscopy...
April 18, 2018: Current Drug Discovery Technologies
Anoja Priyadarshani Attanayake, Kamani Ayoma Perera Wijewardana Jayatilaka, Lakmini Kumari Boralugoda Mudduwa, Chitra Pathirana
Effective β-cell regeneration is a recognized therapeutic strategy in the treatment of type 1 diabetes mellitus. Regeneration of β-cells could be achieved via exogenous natural sources as medicinal plant extracts. Medicinal plants selected for the investigation were Spondias pinnata (Linn. f.) Kurz, Coccinia grandis (L.) Voigt and Gmelina arborea Roxb. The objective was to determine the β-cell regenerative potential of these plant extracts in alloxan induced diabetic rats. Alloxan monohydrate was used to induce diabetes (150 mg/kg, ip)...
April 18, 2018: Current Drug Discovery Technologies
Maria M Trush, Vasyl Kovalishyn, Alla D Ocheretniuk, Oleksandr L Kobzar, Maryna V Kachaeva, Volodymyr S Brovarets, Larisa O Metelytsia
This paper describes QSAR studies by using the Online Chemical Modeling Environment, synthesis, in vitro antifungal activity of 1,3-oxazolylphosphonium derivatives and their acetylcholinesterase inhibitory potential. Three classification QSAR models were created using Random Forests (WEKA-RF), k-Nearest Neighbors and Associative Neural Networks methods and different combinations of descriptors. The predictive ability of the models was tested through cross-validation, giving a balanced accuracy BA=80-91%. All compounds demonstrated good antifungal properties and slight inhibition of acetylcholinesterase activity...
April 18, 2018: Current Drug Discovery Technologies
Tapasree Basu, Bipul Kumar, Anil Khushalrao Shendge, Sourav Panja, Heerak Chugh, Hemant K Gautam, Nripendranath Mandal
BACKGROUND: Farsetia hamiltonii Royle, also known as Hiran Chabba grows in desert regions. It is widely used as folk medicine to treat joint pains, diarrhea and diabetes. However, its antioxidant and iron chelation abilities both in vitro and in vivo have not yet been investigated. METHODS: The 70% methanolic extract of F.hamiltonii (FHME) was investigated for its free radical scavenging and iron chelation potential, in vitro. An iron-overload situation was established by intraperitoneal injection of iron-dextran in Swiss albino mice, followed by oral administration of FHME...
April 18, 2018: Current Drug Discovery Technologies
Kirtee Baheti, Mayura Ajay Kale
BACKGROUND: Since last two decades, there has been more focus on the development strategies related to Anti-Alzheimer's drug research. This may be attributed to the fact that most of the Alzheimer's cases are still mostly unknown except for a few cases, where genetic differences have been identified. With the progress of the disease, the symptoms involve intellectual deterioration, memory impairment, abnormal personality and behavioural patterns, confusion, aggression, mood swings, irritability Current therapies available for this disease give only symptomatic relief and do not focus on manipulations of biololecular processes...
April 17, 2018: Current Drug Discovery Technologies
Mohammad Aminianfar, Siavash Parvardeh, Mohsen Soleimani
BACKGROUND: Clostridium botulinum causes botulism, resulting from the ingestion of a botulinal toxin, which is a serious paralytic illness. Due to strong antimicrobial activity of silver nanoparticles' products, the applications of silver nanoparticles in the field of healthcare in particular are being expanded. Therefore, the objective of current study was to assess a therapeutic strategy for the treatment of botulism toxicity using silver nanoparticles. METHODS: A preliminary test was conducted, based on the ranges that produce illness in laboratory animals, to determine absolute lethal dose (LD100) of botulinum toxin type A (BoNT/A) in mice...
April 3, 2018: Current Drug Discovery Technologies
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