EMERGING TRENDS IN THERAPEUTIC PEPTIDE PHARMACEUTICALS: PROSPECTS AND PERSPECTIVES

Over the last few decades, the inclusions of peptide drugs in the pharmaceutical formulation aspects are more contemporary and recurrent. Since peptide moieties for the treatment of various clinical conditions has been started worthwhile since 1930’s. There has been an increasingly sustainable research work regarding the formulation of therapeutic peptides are in the arena, as probably several entities are already in the clinical investigation, where as few more are in the pipeline for clinical indication. In this current discussion, it has been aimed to unleash the potential of therapeutic bioactive peptides and its future prospects, in the area of pharmaceutical formulation. A plinth of area in regard to the, demand for the development of pharmaceutical formulation of bioactive peptides are still need to be uncovered. And hence only we have discussed deeply about the contemporary prospects of the peptide moieties.     Keywords: Peptide drugs, pharmaceutical formulation, current trends, clinical implications &nbsp

Indian herbal formulation Kaba Sura Kudineer possesses the most powerful ligands to block ACE2-RBD interaction of SARS-CoV-2 infection

Medicinal herbs play an important role in the primary health care system of developing countries and always uphold the importance of ethnomedicinal studies in the drug discovery process. Indian Siddha practitioners urged people to consume a polyherbal formulation named ‘Kaba Sura kudineer (KSK)’ as a prophylactic measure against COVID-19. To validate the presence of anti-COVID 19 agents if any in KSK, virtual screening of 80 phytochemicals was done by blind docking, fixing the RBD-ACE2 complex as the target using PyRx software. The binding energy of the compounds was calculated using Autodock Vina. The SWISSADME server was used to identify the phytochemicals that obey the Lipinski rule and the blood-brain barrier permeability of the compounds. The outcome of the study revealed that phytochemicals such as diosgenin, diosgenone, coumaperine, bisdemethoxycurcumin, tinocordifolin, isovanillinand 1,8-Cineole displayed hydrogen bond interactions with the complex residues in the interacting site (−8.9 to −5.1 kcal/mol) and were found to obey the Lipinski rule as well as possess blood-brain barrier (BBB) permeability. Based on the highest docking score and the more number of interacting residues at the active site herein we suggest diosgenin and bisdemethoxycurcumin as potential inhibitors of SARS-Co-V-2

Studies on Antioxidant and Anti-obesity Activity of Salvia hispanica (Chia) Seeds Extracts

Obesity is a condition in which large amount of fat is stored in adipose tissue. Obesity is the greatest risk for many diseases like coronary heart disease, type 2 diabetes millions associated with insulin resistance, arthritis disorder, hypertension and cancers. Currently, the available drugs for obesity have been associated with number of side effects when compared with allopathic drugs. Salvia hispanica was one of the member of Lamiaceae family, collected to study the antiobesity activity. Extraction of Salvia hispanica using different solvents was done and tested for the presence of phytochemical constituents and the antimicrobial activity was monitored to evaluate the zone of inhibition. Further, antioxidant potential activity such as DPPH, FRAP and H2O2 assay was studied. Percentage of inhibition of Salvia hispanica was calculated and was observed as in capturing the free radicals present in the body. The surface and cross-sectional morphology Salvia hispanica extract nanoparticles was examined by using SEM. High ALA content make chia a perfect as it is associated with lower incidence of Cardiovascular diseases. This metabolic syndrome is mediated by inflammatory pathways. Hence, the in vitro activity of anti-inflammatory assay was performed by inhibition of albumin denaturation and anti-obesity activity was performed by lipase inhibition assay. Thus the result indicates that the seed extracts of Salvia hispanica possess antiobesity activity. Keywords: Salvia hispanica, anti-obesity, cholesterol, Antioxidant, lipase inhibitio

Silibinin-mediated metabolic reprogramming attenuates pancreatic cancer-induced cachexia and tumor growth.

Pancreatic ductal adenocarcinoma (PDAC) is the fourth leading cause of cancer-related deaths in the US. Cancer-associated cachexia is present in up to 80% of PDAC patients and is associated with aggressive disease and poor prognosis. In the present studies we evaluated an anti-cancer natural product silibinin for its effectiveness in targeting pancreatic cancer aggressiveness and the cachectic properties of pancreatic cancer cells and tumors. Our results demonstrate that silibinin inhibits pancreatic cancer cell growth in a dose-dependent manner and reduces glycolytic activity of cancer cells. Our LC-MS/MS based metabolomics data demonstrates that silibinin treatment induces global metabolic reprogramming in pancreatic cancer cells. Silibinin treatment diminishes c-MYC expression, a key regulator of cancer metabolism. Furthermore, we observed reduced STAT3 signaling in silibinin-treated cancer cells. Overexpression of constitutively active STAT3 was sufficient to substantially revert the silibinin-induced downregulation of c-MYC and the metabolic phenotype. Our in vivo investigations demonstrate that silibinin reduces tumor growth and proliferation in an orthotopic mouse model of pancreatic cancer and prevents the loss of body weight and muscle. It also improves physical activity including grip strength and latency to fall in tumor-bearing mice. In conclusion, silibinin-induced metabolic reprogramming diminishes cell growth and cachectic properties of pancreatic cancer cells and animal models

Cost of Dry Eye Treatment in an Asian Clinic Setting

10.1371/journal.pone.0037711PLoS ONE76

Towards quantifying the role of hydrogen bonding within amphiphile self-association and resultant aggregate formation

Herein, we present a series of five tetrabutylammonium (TBA) sulfonate–urea amphiphilic salts. In solution these amphiphilic salts have been shown to form a variety of self-associated species. The proportion and type of which are both solvent and concentration dependent. In DMSO-d6 a variety of NMR experiments provide evidence towards the formation of mainly dimeric over larger aggregate species. Increasing the percentage of water was shown to increase the concentration of the larger aggregates over dimers in solution. A correlation was established between critical micelle concentration (CMC) values obtained in a 1?:?19 EtOH?:?H2O mixture, dimeric self-association constants obtained in a DMSO-d6 – 0.5% H2O and the results of simple semi-empirical PM6 computational modelling methods. This approach begins to quantify the role of hydrogen bonding in amphiphile self-association and the effects it imparts on surfactant properties. This consequently provides preliminary evidence that these properties maybe predicted by simple low level computational modelling techniques

Retrospective evaluation of whole exome and genome mutation calls in 746 cancer samples

Funder: NCI U24CA211006Abstract: The Cancer Genome Atlas (TCGA) and International Cancer Genome Consortium (ICGC) curated consensus somatic mutation calls using whole exome sequencing (WES) and whole genome sequencing (WGS), respectively. Here, as part of the ICGC/TCGA Pan-Cancer Analysis of Whole Genomes (PCAWG) Consortium, which aggregated whole genome sequencing data from 2,658 cancers across 38 tumour types, we compare WES and WGS side-by-side from 746 TCGA samples, finding that ~80% of mutations overlap in covered exonic regions. We estimate that low variant allele fraction (VAF < 15%) and clonal heterogeneity contribute up to 68% of private WGS mutations and 71% of private WES mutations. We observe that ~30% of private WGS mutations trace to mutations identified by a single variant caller in WES consensus efforts. WGS captures both ~50% more variation in exonic regions and un-observed mutations in loci with variable GC-content. Together, our analysis highlights technological divergences between two reproducible somatic variant detection efforts

Indian herbal formulation Kaba Sura Kudineer possesses the most powerful ligands to block ACE2-RBD interaction of SARS-CoV-2 infection

885-890Medicinal herbs play an important role in the primary health care system of developing countries and always uphold the importance of ethnomedicinal studies in the drug discovery process. Indian Siddha practitioners urged people to consume a polyherbal formulation named ‗Kaba Sura kudineer (KSK)‘ as a prophylactic measure against COVID-19. To validate the presence of anti-COVID 19 agents if any in KSK, virtual screening of 80 phytochemicals was done by blind docking, fixing the RBD-ACE2 complex as the target using PyRx software. The binding energy of the compounds was calculated using Autodock Vina. The SWISSADME server was used to identify the phytochemicals that obey the Lipinski rule and the blood-brain barrier permeability of the compounds. The outcome of the study revealed that phytochemicals such as diosgenin, diosgenone, coumaperine, bisdemethoxycurcumin, tinocordifolin, isovanillinand 1,8-Cineole displayed hydrogen bond interactions with the complex residues in the interacting site (−8.9 to −5.1 kcal/mol) and were found to obey the Lipinski rule as well as possess blood-brain barrier (BBB) permeability. Based on the highest docking score and the more number of interacting residues at the active site herein we suggest diosgenin and bisdemethoxycurcumin as potential inhibitors of SARS-Co-V-2