Computational insights into human UCP1 activators through molecular docking, MM-GBSA, and molecular dynamics simulation studies.

The prevalence of obesity is rapidly increasing worldwide. Brown adipose tissue activates uncoupling protein 1 (UCP1) to generate heat through bypassing ATP synthesis, offering a potential target for obesity treatment. Targeting UCP1 activation to induce thermogenesis through small molecules presents a promising approach for obesity management.

Recent innovations in topical delivery for management of rheumatoid arthritis: A focus on combination drug delivery.

Rheumatoid arthritis (RA) is an immune-mediated disease that necessitates a thorough understanding of its intricate pathophysiological mechanism for precise and effective therapeutic targeting. The European League Against Rheumatism (EULAR) has established guidelines for RA treatment, endorsing monotherapy or combination therapy with corticosteroids and synthetic disease-modifying antirheumatic drugs (sDMARDs). This review delves into clinical trials and research outcomes related to combination drug delivery, with an emphasis on the role of natural products in combination with synthetic drugs.

Discovery of thiazolidinedione-based pancreatic lipase inhibitors as anti-obesity agents: synthesis, studies and pharmacological investigations.

A series of new 2,5-disubstituted arylidene derivatives of thiazolidinedione () designed using molecular hybridization approach were synthesized, structurally characterized, and explored for their anti-obesity potential inhibition of Pancreatic Lipase (PL). Compound presented the most potent PL inhibitory activity with IC = 2.71 ± 0.

Synthesis, molecular modelling and pharmacological evaluation of novel indole-thiazolidinedione based hybrid analogues as potential pancreatic lipase inhibitors.

A series of novel indole-thiazolidinedione hybrid analogues ( to ) were synthesised, characterised and evaluated for their potential Pancreatic Lipase (PL) inhibition. Amongst the screened analogues, was found to be the most active PL inhibitor with an IC of 2.67 µM.

Pancreatic lipase and its related proteins: where are we now?

Obesity is a disease of epidemic proportions, with a worrisome upward trend. The high consumption of lipids, a major energy source, leads to obesity because of their high calorific value. Pancreatic lipase (PTL), produced by pancreatic acinar cells, hydrolyzes 50-70% of triacylglycerol (TAG) from food.

Long-term antitrypanosomal effect of quinapyramine sulphate-loaded oil-based nanosuspension in T. evansi-infected mouse model.

The goal of the present work consisted of the formulation development and evaluation of quinapyramine sulphate (QS)-loaded long-acting oil-based nanosuspension for improved antitrypanosomal effect. QS was transformed into a hydrophobic ionic complex using anionic sodium cholate (Na.C).

SET7, a lysine-specific methyl transferase: An intriguing epigenetic target to combat diabetic nephropathy.

Diabetic nephropathy (DN) is a dreadful complication of diabetes that affects ∼50% of diabetics and is a leading cause of end-stage renal disease (ESRD). Studies have linked aberrant expression of lysine methyltransferases (KMTs) to the onset and progression of DN. SET7 is a KMT that methylates specific lysine residues of the histone and nonhistone proteins.

Design, Synthesis, Molecular Modelling and in Vitro Evaluation of Indolyl Ketohydrazide-Hydrazone Analogs as Potential Pancreatic Lipase Inhibitors.

Inhibition of Pancreatic lipase (PL) is considered to be a promising target for the management of obesity, owing to its crucial role in the digestion of dietary triglycerides. A series of 31 indolyl ketohydrazide-hydrazone analogs (5 aa-cm) were designed, synthesized and evaluated for their PL inhibitory potential. The analogs were designed using molecular modelling studies.

Chromone Containing Hybrid Analogs: Synthesis and Applications in Medicinal Chemistry.

The use of privileged scaffolds has proven beneficial for generating novel bioactive scaffolds in drug discovery program. Chromone is one such privileged scaffold that has been exploited for designing pharmacologically active analogs. The molecular hybridization technique combines the pharmacophoric features of two or more bioactive compounds to avail a better pharmacological activity in the resultant hybrid analogs.

Topical Nanotherapeutics for Treating MRSA-Associated Skin and Soft Tissue Infection (SSTIs).

The emergence of methicillin-resistant Staphylococcus aureus (MRSA) imposes a major challenge for the treatment of infectious diseases with existing antibiotics. MRSA associated with superficial skin and soft tissue infections (SSTIs) is one of them, affecting the skin's superficial layers, and it includes impetigo, folliculitis, cellulitis, furuncles, abscesses, surgical site infections, etc. The efficient care of superficial SSTIs caused by MRSA necessitates local administration of antibiotics, because oral antibiotics does not produce the required concentration at the local site.

PCB-77 biodegradation potential of biosurfactant producing bacterial isolates recovered from contaminated soil.

Polychlorinated biphenyls (PCBs) are persistent organic pollutants widely distributed in the environment and possess deleterious health effects. The main objective of the study was to obtain bacterial isolates from PCB-contaminated soil for enhanced biodegradation of PCB-77. Selective enrichment resulted in the isolation of 33 strains of PCB-contaminated soil nearby Bhilai steel plant, Chhattisgarh, India.

Metagenomic analysis for taxonomic and functional potential of Polyaromatic hydrocarbons (PAHs) and Polychlorinated biphenyl (PCB) degrading bacterial communities in steel industrial soil.

Iron and steel industries are the major contributors to persistent organic pollutants (POPs). The microbial community present at such sites has the potential to remediate these contaminants. The present study highlights the metabolic potential of the resident bacterial community of PAHs and PCB contaminated soil nearby Bhilai steel plant, Chhattisgarh (India).

Mechanistically acting anti-obesity compositions/formulations of natural origin: a patent review (2010-2021).

Introduction: Current health trends indicate that the rate of incidence of obesity has risen considerably. According to the World Health Organization (WHO) report 2017, the issue of obesity has grown to an epidemic proportion, with over 4 million people dying every year. Orlistat, a potent pancreatic lipase (PL) inhibitor for long-term treatment of obesity has been recently reported to cause hepatic and renal toxicities.

Synthesis, molecular modelling, and evaluation of conophylline inspired novel benzyloxy substituted indole glyoxylamides as potent pancreatic lipase inhibitors.

Pancreatic lipase is a digestive enzyme involved in the hydrolysis of dietary fats. Orlistat, a potent pancreatic lipase inhibitor, is widely prescribed for long-term obesity treatment. Nevertheless, orlistat is reported for severe adverse effects including hepatotoxicity and pancreatitis.

Design, synthesis and biological evaluation of N-substituted indole-thiazolidinedione analogues as potential pancreatic lipase inhibitors.

Pancreatic Lipase (PL) is a key enzyme responsible for the digestion of 50%-70% of dietary triglycerides, hence its inhibition is considered as a viable approach for the management of obesity. A series of indole-TZD hybrid analogues were synthesized, characterized and evaluated for their PL inhibitory activity. Knoevenagel condensation of various substituted indole-3-carboxaldehyde with substituted thiazolidinediones resulted in the formation of titled analogues.

U.S. FDA Approved Drugs from 2015-June 2020: A Perspective.

In the present work, we report compilation and analysis of 245 drugs, including small and macromolecules approved by the U.S. FDA from 2015 until June 2020.

Preparation and Evaluation of Quinapyramine Sulphate-Docusate Sodium Ionic Complex Loaded Lipidic Nanoparticles and Its Scale Up Using Geometric Similarity Principle.

The objective of the present work is to prepare and evaluate ionically complexed Quinapyramine sulphate (QS) loaded lipid nanoparticles and its scale up using geometric similarity principle. Docusate sodium (DS), at a molar ratio of 1:2 of QS to DS, was used to prepare hydrophobic Quinapyramine sulphate-Docusate sodium (QS-DS) ionic complex. Based on the difference in total solubility parameter and polarity of QS-DS complex and different lipids, precirol was selected as a lipid for the preparation of lipidic nanoparticles.

Recent advances in the pharmacological diversification of quinazoline/quinazolinone hybrids.

Due to the pharmacological activities of quinazoline and quinazolinone scaffolds, it has aroused great interest in medicinal chemists for the development of new drugs or drug candidates. The pharmacological activities of quinazoline and its related scaffolds include anti-cancer, anti-microbial, anti-convulsant, and antihyperlipidaemia. Recently, molecular hybridization technology is used for the development of hybrid analogues with improved potency by combining two or more pharmacophores of bioactive scaffolds.

Impact of quercetin on pharmacokinetics of quetiapine: insights from studies in wistar rats.

Quercetin (QCN) is commonly used in high doses as a dietary supplement for weight loss. Psychotic patients are at greater risk of developing obesity than the general population. The present study was designed to understand the impact of QCN on the exposure of quetiapine (QTE), an anti-psychotic drug with narrow therapeutic index and brain penetrating capability.

Evaluation of biphenyl- and polychlorinated-biphenyl (PCB) degrading sp. MAPN-1 on growth of by pot study.

This study focused on isolation of bacteria with biphenyl/polychlorinated biphenyl (PCB) degrading ability from the rhizosphere of (mulberry plant). Repetitive enrichment of rhizospheric soil samples with biphenyl resulted in the isolation of sp. MAPN-1, identified by 16S rRNA gene sequence analysis.

Design, synthesis, evaluation, and molecular modeling studies of indolyl oxoacetamides as potential pancreatic lipase inhibitors.

A series of indolyl oxoacetamide analogs was synthesized, characterized, and evaluated for their pancreatic lipase inhibitory activity using porcine pancreatic lipase (type II) and 4-nitrophenyl butyrate. Compound 8d exhibited a potent inhibition, with an IC value of 4.53 µM, followed by 8c (IC  = 5.

Rapid and cost-effective LC-MS/MS method for determination of hydroxycitric acid in plasma: Application in the determination of pharmacokinetics in commercial Garcinia preparations.

Garcinia cambogia is one of the most commonly used anti-obesity dietary supplements, and hydroxycitric acid (HCA) is a major constituent in the commercial preparations of Garcinia. High doses of HCA are often consumed without much awareness of its pharmacokinetic and toxicokinetic parameters, and therefore, a complete understanding of its effects is lacking. The first step in understanding these parameters is the availability of a reliable bioanalytical method.

Nanotechnological interventions for treatment of trypanosomiasis in humans and animals.

Trypanosomiasis is a parasitic infection caused by Trypanosoma. It is one of the major causes of deaths in underprivileged, rural areas of Africa, America and Asia. Depending on the parasite species responsible for the disease, it can take two forms namely African trypanosomiasis (sleeping sickness) and American trypanosomiasis (Chagas disease).