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Current Drug Discovery Technologies

Kushal Shah, Briann Fischetti, Agnes Cha, David R Taft
BACKGROUND: Lamivudine is a nucleoside reverse transcriptase inhibitor used to treat HIV and hepatitis B. It is primarily cleared by the kidney with renal secretion mediated by OCT2 and MATE. OBJECTIVE: To use PBPK modeling to assess the impact of renal impairment on lamivudine pharmacokinetics using the Simcyp® Simulator. METHODS: The model incorporated the Simcyp® Mechanistic Kidney Model option to predict renal disposition. The model was initially verified using the Simcyp® Healthy Volunteer population...
February 14, 2019: Current Drug Discovery Technologies
Nadia Arif, Andleeb Subhani, Waqar Hussain, Nouman Rasool
BACKGROUND: Alzheimer's disease (AD) has become the most common age-dependent disease of dementia. The trademark pathologies of AD are the presence of amyloid aggregates in neurofibrils. Recently phytochemicals being considered as potential inhibitors against various neurodegenerative, anti-fungal, antibacterial and antiviral diseases in human beings. OBJECTIVE: This study targets the inhibition of BACE-1 by phytochemicals using in silico drug discovery analysis...
February 14, 2019: Current Drug Discovery Technologies
Veneta Simon, K V Sreerag, R Sasikumar, S K Kanthlal
BACKGROUND: Although antibiotic-induced hepatotoxicity is recoverable with mild impairment, and few of them were reported to cause morbidity. Hence, an adjuvant is essential in reducing such incidences. OBJECTIVE: The aim of this study to evaluate the protective effect of ascorbic acid on antibiotic induced liver toxicity using liver slices. METHOD: Fresh liver slices collected from leghorn chicken were incubated with different concentrations of sulfamethoxazole tetracycline and clavulanic acid along with ascorbic acid (200μg/ml) for 2 hours...
February 4, 2019: Current Drug Discovery Technologies
Bhoj Raj Singh, Dharmendra Kumar Sinha, O R Vinodh Kumar, Prasanna Vadhana, Monika Bhardwaj, Archana Saraf, Sakshi Dubey, Abhijit M Pawde, Ujjwal Kumar De, Vinod Kumar Gupta
BACKGROUND AND OBJECTIVES: Multiple-Drug-Resistance (MDR) among bacteria is imminent problem and alternative therapies are seen as future abode. Agarwood Oil (AO) is described to possess antimicrobial activity besides many other medicinal utilities. This paper discusses antimicrobial activity of AO on MDR and non-MDR strains of microbes of 69 genera isolated from clinical and non-clinical samples. METHODS AND RESULTS: In this study sensitivity of microbes was determined for conventional antimicrobials and AO using disc diffusion assay followed by determination of minimum inhibitory concentration (MIC) using agar well dilution assay...
January 25, 2019: Current Drug Discovery Technologies
Marco Bonesi, Mariarosaria Leporini, Maria C Tenuta, Rosa Tundis
Natural compounds have always played a key role in drug discovery. Anthocyanins are secondary metabolites belonging to the flavonoids family responsible for the purple, blue, and red colour of many vegetables and fruits. These phytochemicals have attracted the interest of researchers for their important implications in human health and for their use as natural colorants. Many in vitro and in vivo studies demonstrated the potential effects of anthocyanins and anthocyanins-rich foods in the prevention and/or treatment of diabetes, cancer, and cardiovascular and neurodegenerative diseases...
January 25, 2019: Current Drug Discovery Technologies
Khadije Saket, Jalil Tavakol Afshari, Ehsan Saburi, Mahdi Yousefi, Roshanak Salari
From ancient times, medicinal plants have been usually utilized to treat many disorders, but today, interest in these herbs is again aroused, because of their fewer side effects and low-cost. In traditional medicine, for many diseases, various medicinal herbs have been suggested so far. Drimia maritime, also named squill, is an important medicinal plant for the treatment of many diseases, especially respiratory diseases. In the current evidence-based study, we conducted a review of the general characteristics, ingredients, administration form, and side effects of squill in traditional medicine...
January 25, 2019: Current Drug Discovery Technologies
Vaishali M Patil, Preeti Anand, Monika Bhardwaj, Neeraj Masand
The research work aims to investigate Schiff bases of Cinnamaldehyde as biologically potent analogs. In the past decade CADD has emerged as a rational approach in drug development so with the help molecular docking approach we planned to perform virtual screening of the designed data set of Schiff bases. This will be helpful to put some light on the drug receptor interactions required for anti-inflammatory activity. For carrying out virtual screening of the developed Schiff base data set, AutoDock 4.0 was used...
January 25, 2019: Current Drug Discovery Technologies
Marjan Mahjour, Arash Khoushabi
BACKGROUND: Melasma is a skin pigmentation disorder that remains resistant to available therapies. The exact cause of melasma is unknown. Histamine is an inflammatory factor. Its involvement in pigmentation is obscure. The aim of this study is to introduce an herbal anti -histamine H2 receptor which is effective in these disorders. METHODS: This is a review study by searching the electronic databases and also Persian Medicine books, from 2000 to 2018 by the keywords such as H2 antagonist, H2 blocker and melasma...
January 21, 2019: Current Drug Discovery Technologies
Martin Braddock
The unique nature of microgravity encountered in space provides an opportunity for drug discovery and development that cannot be replicated on Earth. From the production of superior protein crystals to the identification and validation of new drug targets to microarray analyses of transcripts attenuated by microgravity, there are numerous examples which demonstrate the benefit of exploiting the space environment. Moreover, studies conducted on Space Shuttle missions, the International Space Station and other craft have had direct benefit for drug development programmes such as those directed against reducing bone and muscle loss or increasing bone formation...
January 12, 2019: Current Drug Discovery Technologies
Alexander N Orekhov, Andrey V Grechko, Elena B Romanenko, Dongwei Zhang, Dimitry A Chistiakov
Atherosclerosis is a chronic arterial disease characterized by vascular inflammation, accumulation of lipids in the arterial wall, and formation and growth of atherosclerotic plaques followed by ischemia. In subclinical atherosclerosis, cholesterol retention in subendothelial cells leads to induction of local inflammation, generation of foam cells and lesion formation, followed by a chain of other pathogenic events. Atherosclerotic progression can frequently be fatal, since plaque rupture may lead to thrombosis and acute events, such as myocardial infarction, stroke and sudden death...
December 31, 2018: Current Drug Discovery Technologies
Francisco Torrens, Gloria Castellano
BACKGROUND: Some lactones prevent protein Myb-dependent gene expression. OBJECTIVE: The object is to calculate inhibitors of Myb-brought genetic manifestation. METHOD: Linear quantitative structure-potency relations result expanded, among sesquiterpene lactones of a huge macrocycle variety (pseudoguaianolides, guaianolides, eudesmanolides and germacranolides), to establish which part of the molecules constitutes their pharmacophore, and predict their inhibitory potency on Myb-reliant genetic manifestation, which may result helpful as leads for antileukaemia therapies with a new mechanism of action...
December 31, 2018: Current Drug Discovery Technologies
Paraskevi Farmaki, Christos Damaskos, Nikolaos Garmpis, Anna Garmpi, Spyridon Savvanis, Evangelos Diamantis
Cardiovascular disease (CAD) remains the leading cause of morbidity and mortality in the western world. Hypolipidemic drugs have long been used for the primary and secondary prevention of heart disease. However, the high frequency of recurrent events in patients despite on hypolipidemic therapy has increased the need for new more targeted therapeutic approaches. Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors are monoclonal antibodies to the PCSK9 gene and represent a new class of drugs that have been shown to further decrease LDL-C when administered as a monotherapy or in combination with statins...
December 10, 2018: Current Drug Discovery Technologies
Atousa Khalatbari, Mehdi Mahdavi, Fahimeh Jafarnezhad, Sanaz Afraei, Farzaneh Tofighi Zavareh, Zahra Aghazadeh, Afshin Ghaderi, Abbas Mirshafiey
This investigation evaluates the pro-apoptotic and anti-inflammatory effects of β-D-mannuronic acid [M2000] compared to diclofenac, based on gene expression involved in apoptosis and inflammation process [including Bcl2, NFκB, IL-8 and Cd49d] in peripheral blood mononuclear cells [PBMCs] of healthy donors under exvivo conditions. The venous blood of twelve healthy volunteers with aged 25-60 years, were collected in heparinized tubes. The healthy volunteers were selected from no smoking group and without using illicit drugs and suffering from diabetes...
November 9, 2018: Current Drug Discovery Technologies
Ishan I Panchal, Roshani Rajput, Ashish D Patel
CONTEXT: objective: The series of 2-(4-Phenylamino)-N-(5-((4-nitrophenoxy)methyl) -1,3,4-oxadiazol-2-yl)acetamide (5a-5e) and substituted N-(5-(Phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-(phenylamino)acetamide (5f-5i) were designed, synthesized and investigated for Collapsin response mediator protein 1 (CRMP 1) inhibitors as small lung cancer. DESIGN: Design of compounds was done by literature review and molecular docking studies in iGEMDOCK 2.0. METHODS AND MATERIAL: Novel 1, 3, 4 Oxadiazole derivatives were synthesized and characterized by melting point, TLC, IR Spectroscopy, Mass spectroscopy and 1H NMR...
November 5, 2018: Current Drug Discovery Technologies
Fatemeh Forouzanfar, Mohammad Mahdi Vahedi, Azita Aghaei, Hassan Rakhshandeh
BACKGROUND: Insomnia is the most common sleep disorder. The present study was undertaken to evaluate the sedative-hypnotic potential of hydroalcoholic extract (HAE) of Cuscuta epithymum and its fractions. METHOD: HAE and its fractions including: water fraction (WF), ethyl acetate fraction (EAF) and n-hexan fraction (NHF) were i.p administered to male mice and 30 min later pentobarbital (30 mg/kg, i.p.) was injected to induce sleep. Then the latent period and continuous sleeping time were recorded...
November 4, 2018: Current Drug Discovery Technologies
Bhavana B Bhat, N Udupa, D Sreedhar
Herbal medicines have been used by mankind from time immemorial. Moreover, many modern medicines are originated from plant sources. In earlier days, patients were dependent on herbs for treatment and well-being. However, due to advent of industrial revolution and modern science, scenario of treating diseases has changed over a period of time. Majority of patients started preferring allopathy medicines due to their several advantages over herbal medicines. However, due to long term treatment by allopathic medicines for chronic diseases have led to side effects, hence, patients are now drifting back to the traditional medicines...
November 4, 2018: Current Drug Discovery Technologies
Ishan I Panchal, Sandip N Badeliya, Rakesh Patel
mTORC1/ PI3K control multiple anabolic pathways, including protein synthesis, ribosome production, lipogenesis, and nucleotide synthesis, all of which are important for cell and tissue growth.Sapanisertib and Dactolisib inhibit PI3K/AKT/mTOR pathway, an important signalling pathway for many cellular functions such as growth control, metabolism and translation initiation.Dactolisib contain quinolin-3-yl-2,3-dihydroimidazo[4,5-c]quinolin scaffold and Sapanisertib contain benzo[d]oxazol-5-yl-1-ethyl-1H-pyrazolo[3,4-d]pyrimidinnucleous...
November 2, 2018: Current Drug Discovery Technologies
Farnoush Falahat, Sedigheh Ayatiafin, Lida Jarahi, Roshanak Mokaberinejad, Hasan Rakhshandeh, Zohre Feyzabadi, Mandana Tavakkoli
BACKGROUND: The aim of this study was to evaluate the efficacy of the herbal tea based on Foeniculum vulgare, on inducing regular bleeding in women with oligomenorrhea and secondary amenorrhea(oligo/amenorrhea). METHODS: Forty women aged 18- 40 with oligo/amenorrhea were enrolled in this randomized controlled clinical trial and were allocated to two groups equally. The women in the first group were treated by Fomentex (Foeniculum vulgare / Mentha longifolia / Vitex agnus-castus) herbal tea 11...
October 29, 2018: Current Drug Discovery Technologies
Yau Xin Yi, Anand Gaurav
INTRODUCTION: The primary aim of this study is to understand the binding of curcumin and its analogues to different PDE4 subtypes and identification of the role of PDE4 subtype inhibition in the anti-inflammatory property of curcumin. Docking analysis has been used to acquire the above mentioned structural information and this has been further used for designing of curcumin derivatives with better anti-inflammatory activity. MATERIALS AND METHOD: Curcumin and its analogues were subjected to docking using PDE4A, PDE4B, PDE4C and PDE4D as the target...
October 16, 2018: Current Drug Discovery Technologies
Marjan Mahjour, Arash Khoushabi
BACKGROUND: Vitiligo is a pigmentary disorder characterizing by white macules due to loss of melanocytes. Vitiligo affects about 1 to 4% of people around the world. The treatment of vitiligo has a high cost and the long process of treatment in spite of no complete remedy. It has various psychological side-effects such as depression and anxiety affecting the quality of life seriously. Avicenna in his Canon treated these patients over a thousand years ago. This study aimed to introduce some herbal drugs in vitiligo based on the Canon of Avicenna besides the conventional medical treatments...
October 16, 2018: Current Drug Discovery Technologies
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