Posted by admin on Mar 31, 2021 in |
Marfan syndrome (MFS) is a common dominant inherited disorder that affects connective tissue, which is associated with mutation of the gene FBN1. The protein encoded by this gene contributes to the final structure of microfibrils. Single nucleotide polymorphisms (SNPs) of this gene links to variations in gene expression phenotypically among patients. Therefore SNPs would be the main target for identification and analysis, which may help in further diagnosis of such life-threatening disorder. In this study, various computational methods have been used to analyze the genetic variations and identify non-synonymous or amino acid-changing SNPs (nsSNP). It can quicken to evaluate a considerable outcome of a mutation before literally doing the lab work. In total, 475 high-risk nsSNPs have been identified using the NCBI SNPs database. Among these nsSNPs, residues are assigned to predict deleterious or disease-related nsSNP. The conservation of functional amino acid residues and secondary and tertiary structure predictions were also reported using various tools. Swiss-Pdb Viewer allows changing amino acid side chains, causing an artificial mutation to the...
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Posted by admin on Mar 31, 2021 in |
Leucas aspera is the medicinal plant commonly known as ‘Thumbai’ found all over India. It is being used in traditional medicine to treat cough, cold, diarrhea, inflammatory diseases, and paste of the plant that has been used to treat the wound to enhance the wound healing process. The plant is reported to have anti-inflammatory, analgesic, antidiarrheal, antimicrobial, antioxidant, and insecticidal activities. The current study has been taken up to evaluate the aqueous extract of L. aspera leaves (LaLE) for its proteolytic activity and its role in the blood coagulation cascade. The concentration of protein in LaLE was estimated to be 1 mg/ml. The proteolytic activity was determined with a specific activity of 2.40 U/mg/ml. The protein banding profile was analyzed on SDS-PAGE. LaLE hydrolyzed fibrinogen, fibrin, and collagen (I and IV) in a dose-dependent manner. LaLE increased the clotting time in prothrombin time (PT) and recalcification time (RT) by 3.87- and 5.43-folds, respectively, indicating its potentiality as an anticoagulant protease. LaLE inhibited ADP-induced platelet aggregation by 2.38-folds, suggesting its...
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Posted by admin on Mar 31, 2021 in |
The maintenance of an appropriate serum concentration of a drug is important to ensure therapeutic efficacy. Functional alterations of drug transporters may influence the serum concentration of drugs through changes in its pharmacokinetics and pharmacodynamics (PK/PD). In this study, we have focused on the influence of functional alterations in the intestinal P-glycoprotein (P-gp) on the PK of linagliptin (LIN) by the oral route under normal and diabetic conditions before and after pretreatment with resveratrol (RSV) and verapamil (VER) as standard. The interaction between LIN and RSV has been studied using in-vitro noneverted sac study, in-situ Single-Pass Intestinal Perfusion (SPIP) study, and in-vivo oral bioavailability study in rats. Pretreatment with RSV significantly enhanced the intestinal transport, apparent permeability, and effective permeability of LIN in normal and diabetic rats indicating the active role of P-gp in LIN absorption. Pretreatment with RSV significantly altered the Cmax and AUC of LIN in both normal and diabetic rats. But compared to normal rats, diabetic rats show a significant decrease in intestinal transport, and increased...
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Posted by admin on Mar 31, 2021 in |
Objective: In the present work, A Simple, rapid, sensitive, precise, and reproducible, specific UV spectrophotometric method for the determination of Saxagliptin (SAXA) and Dapagliflozin (DAPI) in bulk drug and pharmaceutical dosage form were developed and validated. Methods: A simple double beam UV spectrophotometric method has been developed and validated with different parameters such as linearity, precision, repeatability, the limit of detection (LOD), Limit of Quantification (LOQ), accuracy as per ICH guidelines. Results: UV-visible spectrophotometric method, measurement of absorption at a maximum wavelength in 10 ml methanol and volume make with water solvent system as reference SAXA and DAPI were found to be at 224 nm and 274 nm respectively. The drug obeyed the Beer’s law and showed a good correlation. Beer’s law was obeyed in the concentration range 2-10 µg/ml for Saxagliptin and 4-20 µg/ml for Dapagliflozin, respectively with a correlation coefficient was 0.999. The LOD and LOQ of Saxagliptin were found to be 0.040 μg/ml and 0.01230 μg/ml, Dapagliflozin was found to be 0.1230 μg/ml and 0.5460 μg/ml,...
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Posted by admin on Mar 31, 2021 in |
Tuberculosis is one of the major contagious diseases and a leading cause of death in humans. Current treatment methods suffer from a multitude of problems like long duration of treatment, lack of patient compliance, presence of drug-resistant bacteria, etc. To combat the disease effectively, there is an urgent need for the development of new drugs effective against both drug-sensitive and drug-resistant bacteria. Cynodon dactylon is known to be effective against cough and other lung diseases. The objective of the present study is to identify the component in Cynodon dactylon, which is therapeutically effective against Mycobacterium tuberculosis by in-silico docking analysis using Autodock. Here InhA, the enoyl acyl carrier protein reductase from Mycobacterium tuberculosis was taken as the target protein for docking analysis. Phytochemicals from Cynodon dactylon were selected based on molecular and ADME properties. Among the phytochemicals investigated, luteolin showed a good docking score and better interaction with the target protein and is comparable to the commercially available first-line antitubercular drug, isoniazid. Based on our preliminary analysis of molecular...
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