Niosomal gel improves dermal delivery of nimbolide: a promising approach for treatment of psoriasis.

Psoriasis is a chronic inflammatory skin disorder characterized by the excessive proliferation of keratinocytes, forming thickened skin plaques due to immune-mediated cytokine responses. Delivering drugs through this barrier to target inflamed tissues remains challenging. Nimbolide (NIM), known for its anti-inflammatory and anticancer properties, shows promise in managing psoriasis.

Peptidyl arginine deiminase-4 inhibitor ameliorates pulmonary fibrosis through positive regulation of developmental endothelial locus-1.

Recurring lung injury, chronic inflammation, aberrant tissue repair and impaired tissue remodelling contribute to the pathogenesis of pulmonary fibrosis (PF). Neutrophil extracellular traps (NETs) are released by activated neutrophils to trap, immobilise and kill invading pathogen and is facilitated by peptidyl arginine deiminase-4 (PAD-4). Dysregulated NETs release and abnormal PAD-4 activation plays a crucial role in activating pro-fibrotic events in PF.

In vivo and in vitro metabolite profiling of nirmatrelvir using LC-Q-ToF-MS/MS along with the in silico approaches for prediction of metabolites and their toxicity.

Nirmatrelvir (NRV), a 3C-like protease or M inhibitor of SARS-CoV-2, is used for the treatment of COVID-19 in adult and paediatric patients. The present study was accomplished to investigate the comprehensive metabolic fate of NRV using in vitro and in vivo models. The in vitro models used for the study were microsomes (human liver microsomes, rat liver microsomes, mouse liver microsomes) and S9 fractions (human liver S9 fractions and rat liver S9 fractions) with the appropriate cofactors, whereas Sprague-Dawley rats were used as the in vivo models.

Exploration of cytotoxic potential and tubulin polymerization inhibition activity of -stilbene-1,2,3-triazole congeners.

To scrutinize -stilbene based molecules with potential anticancer and tubulin polymerization inhibition activity, a new series of -stilbene-1,2,3-triazole congeners was designed and synthesized a click chemistry protocol. The cytotoxicity of these compounds 9a-j and 10a-j was screened against lung, breast, skin and colorectal cancer cell lines. Based on the results of MTT assay, we further evaluated the selectivity index of the most active compound 9j (IC 3.

Design, synthesis and cytotoxicity evaluation of indolo-pyrazoles grafted with thiazolidinone as tubulin polymerization inhibitors.

In the pursuit of potential and effective chemotherapeutic agents, a series of 2-((3-(indol-3-yl)-pyrazol-5-yl)imino)thiazolidin-4-ones was designed and synthesized, conjoining salient pharmacophoric properties for directing prominent cytotoxicity. The cytotoxicity evaluation revealed potent compounds with IC values <10 μM on tested human cancer cell lines. Compound 6c exhibited the highest cytotoxicity with an IC value of 3.

selenocyclization of secondary allylic carboxamides using Woollins' reagent: to 2,5-disubstituted selenazolines.

We report microwave-assisted selenation and cyclization of secondary allylic carboxamides using Woollins' reagent, a serendipitous finding observed during an attempt to synthesize -allylbenzoselenoamide compounds. This resulted in the first reported synthesis of 2-aryl-5-methyl selenazolines. Twenty-one diversified selenazolines and three late-stage-functionalized drug molecules were synthesized in 42-93% and 25-52% yield, respectively, and these were evaluated further for their anti-proliferative activity.

Acetaminophen induced hepatotoxicity: An overview of the promising protective effects of natural products and herbal formulations.

Background: The liver plays an important role in regulating the metabolic processes and is the most frequently targeted organ by toxic chemicals. Acetaminophen (APAP) is a well-known anti-allergic, anti-pyretic, non-steroidal anti-inflammatory drug (NSAID), which upon overdose leads to hepatotoxicity, the major adverse event of this over-the-counter drug.

Purpose: APAP overdose induced acute liver injury is the second most common cause that often requires liver transplantation worldwide, for which N-acetyl cysteine is the only synthetic drug clinically approved as an antidote.

Borneol protects against cerulein-induced oxidative stress and inflammation in acute pancreatitis mice model.

Borneol is a commonly used flavouring substance in traditional Chinese medicine, which possesses several pharmacological activities including analgesic, antiinflammatory, and antioxidant properties. The aim of this study was to investigate the effects of borneol on cerulein-induced acute pancreatitis (AP) model. Swiss albino mice were pretreated with borneol (100 and 300 mg/kg) daily for 7 days, before six consecutive injections of cerulein (50 μg/kg/hr, intraperitoneally).

Piperlongumine attenuates bile duct ligation-induced liver fibrosis in mice via inhibition of TGF-β1/Smad and EMT pathways.

Liver fibrosis (LF) is a progressive liver injury that may result in excessive accumulation of extracellular matrix (ECM). However, transforming growth factor-beta (TGF-β) and epithelial to mesenchymal transition (EMT) play a central role in the progression of LF through the activation of matrix producing hepatic stellate cells (HSCs). Piperlongumine (PL), an alkaloid extracted from Piper longum, has been reported to possess anti-inflammatory and antioxidant activities in various diseases but its hepatoprotective and antifibrotic effects have not been reported yet.