Posted by admin on Nov 30, 2019 in |
A new series of hydroxamic (5a-5j) and carboxylic acid analogs (4a-4j) based on the 1, 3, 4-thiadiazole scaffold was designed and synthesized to explore its potential as new antitumor agents. The chemical structures of the compounds were confirmed based on TLC, IR, 1H NMR, and 13C NMR analysis. Molecular docking studies showed that the target compounds correctly dock into the binding pocket of histone deacetylase inhibitor (PDB Code 1w22 reference compound), while their bioavailability / drug-likeness was predicted to be acceptable. The predicted physicochemical were compared with those of a reference compound. Biological results revealed that the structural modifications proposed significantly affected inhibitory potency as well as selectivity for HDAC inhibitors. Most target compounds were significantly more active specifically 5a, 5b, 5e with IC50 values in the low micromolar or, the most active compounds in the series. Selected compounds were tested on the viability of MDA-MB-231 (breast cancer cell) and K562 (chronic myelogenous leukemia cell), A549 (human lung cancer), PC3 (Prostate cancer cell lines) using MTT...
Read More
Posted by admin on Nov 30, 2019 in |
Type 2 diabetes mellitus poses an important health care problem because of its associated two to threefold increased risk of cardiovascular disease and its high prevalence and incidence worldwide. Dyslipidemia is an independent risk factor for severe morbidity and mortality in terms of cardiovascular risk in type-2 DM patients. Studies have shown an association between metformin and lipid profile changes although results are inconclusive. Thus, this study was done to evaluate the changes in serum lipid profiles in patients who are newly started on metformin. It was a prospective, observational and non-interventional study. 50 newly diagnosed patients of type 2 DM were enrolled and started on metformin. Lipid profile was assessed before starting treatment and then after 12 weeks. Statistical analysis was done using paired t-test. In results serum total cholesterol, triglyceride and VLDL were significantly decreased after 12 weeks of metformin therapy. The apparent change was also observed in serum LDL and HDL, but it was not statistically significant. Thus, it may be speculated that metformin has beneficial...
Read More
Posted by admin on Nov 30, 2019 in |
Propolis is a natural resinous substance with a wide range of biological properties, synthesized by bees from bud exudates of some plants. Bees make use of propolis as a building material and to defend the hive. The chemical composition of propolis varies depending on vegetation and species having plethora of therapeutic activities. To detect compounds present in propolis an efficient, precise, and reliable HPLC method was used for quantification which offers advantages in terms of speed and accuracy. This method allowed eliciting the chromatographic fingerprint by comparing the retention time and molecular weight of commercially available standards that are known to be present in propolis such as p-coumaric acid, ferulic acid, epicatechin, gallic acid, caffeic acid and quercetin in different samples. The bioactive compounds present in varying amount has anti-cancer, anti-proliferative, antioxidant, antimicrobial, anti-inflammatory, cardioprotective and hepato protective properties. The main aim of the study is to analyze the flavonoids in propolis taken from areas surrounded by moderate vegetation of different honeybee species. The interesting results provide a basis...
Read More
Posted by admin on Nov 30, 2019 in |
The present study concerns the development, characterization, and optimization of nanoparticulate oral formulations of Tolbutamide using poly (ԑ-caprolactone) which is a biodegradable polymer. Emulsion Solvent Evaporation technique was used for preparation of drug-loaded polymeric nanoparticles. This research was carried out to improve the therapeutic efficacy of tolbutamide by increasing its bioavailability through size reduction and to achieve the sustained release of drugs by preparing polymeric nanoparticles. The results of FTIR and DSC analysis indicated that there was no significant interaction between drug and excipients. The prepared drug-loaded Poly (ԑ-caprolactone) nanoparticles were characterized for their surface characteristics via morphology, particle size, stability by zeta potential and drug loading efficiency. The prepared nanoparticles were found to in nanosized range with spherical morphology and stable. The free drug particles can be seen on the polymeric surface which attributes to burst effect and immediate onset of action. The sustained release of drugs through polymeric matrix is evident from drug release studies. The prepared polymeric nanoparticles were found to be stable at 5 ±...
Read More
Posted by admin on Nov 30, 2019 in |
Monocarboxylate transporter 11 (MCT11) is a transporter protein encoded by the SLC16A11 gene. MCT11 protein is found to play an important role in many biological activities in different species. MCT11 helps in hepatic lipid metabolism by catalyzing the transport of pyruvate molecules across the membrane. It is also found to be involved in regulation of Diabetes. Therefore, MCT11 protein is taken into consideration for this study. Moreover, a rapid analysis through different protein databases revealed that there is no protein crystal structure available. Therefore, Homology modeling is adopted to generate the model using SWISS-MODEL and validated using PROCHECK. More specifically, this is the first Homology model developed for the MCT11 protein. The sequence analysis studies such as physicochemical properties such as molecular weight (47790.99 Da), Theoretical isoelectric point (8.67), Total number of positively (Asp+Glu) and negatively (Arg+Lys) charged residues (+R/-R) were 19 and 22 respectively. The grand average of hydropathicity (GRAVY) indicating a value of 0.687 was computed. The secondary structure prediction and conserved domain sequence were computed. Finally,...
Read More
