Combinatorial Chemistry & High Throughput Screening - Volume 25, Issue 11, 2022

Infection by the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) provokes acute inflammation due to extensive replication of the virus in the epithelial cells of the upper and lower respiratory system. The mammalian target of rapamycin (mTOR) is a l signalling protein with critical functions in cell growth, metabolism, and proliferation. It is known for its regulatory functions in protein synthesis and angiogenes Read More

Background: L-tryptophan is an essential amino acid necessary for the human body to function. Its degradation occurs through two metabolic pathways. Approximately 95 % of the Ltryptophan available in the body is converted via the kynurenine pathway, while the remainder is degraded via the serotonin pathway. Properly maintained balance between the concentrations of individual small molecular metabolites is extrem Read More

The advancement of computing and technology has invaded all the dimensions of science. Artificial intelligence (AI) is one core branch of Computer Science, which has percolated to all the arenas of science and technology, from core engineering to medicines. Thus, AI has found its way for application in the field of medicinal chemistry and heath care. The conventional methods of drug design have been replaced by comput Read More

The entire world has been in a battle against the COVID-19 pandemic since its first appearance in December 2019. Thus researchers are desperately working to find an effective and safe therapeutic agent for its treatment. The multifunctional coronavirus enzyme papain-like protease (PLpro) is a potential target for drug discovery to combat the ongoing pandemic responsible for cleavage of the polypeptide, deISGylatio Read More

Background: Malaria is responsible for social and economic burden in most lowincome malaria-affected countries. Thus, newer antimalarials are needed to tackle morbidities and mortalities associated with the drug-resistant malarial strains. Haemoglobin digestion inside the food vacuole of malarial parasite would lead to producing redox-active and toxic-free heme. The detoxification process adopted by Plasmodium sp. woul Read More

Background: Short-chain fatty acids exert anti-cancer effects on tumor cells. Objective: We aimed to reveal the signaling network altered by butyrate in Gastric Cancer (GC) using small RNA sequencing (sRNA-seq). Methods: The effects of butyrate on the biological behavior of NCI-N87 and KATO III cells in vitro were assessed by functional assays and half-maximal inhibitory concentrations (IC50) of butyrate in KATO III cells w Read More

Aims and Objectives: A high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for determining hypaphorine, a potential agent for treating osteoclast- based bone loss, was developed and validated in rat plasma. Materials and Methods: Plasma samples were pretreated by the protein precipitation. Chromatographic separation was performed using an Inertsil ODS-3 column (50 mm × 4.6 mm, Read More

Background: Gastric cancer (GC), one of the common clinical malignant tumors of the digestive system, is the fourth most commonly diagnosed cancer and the second lethal cancer worldwide and has the characteristics of high metastasis, fatality, and recurrence rate. This research was conducted to investigate the role and mechanism of miR-4295 in gastric cancer. Methods: The expression capacity of miR-4295 was det Read More

Aim & Objectives: The Gochnatia decora (Kurz) A. L. Cabrera is a rare woody plant belonging to the family of Asteraceae. The bark of this plant is used as a Chinese folk medicine to treat cough and pneumonia. However, the effective substance related to its efficacy remains unknown. This study aims to evaluate the potential anti-inflammatory activities of the chemicals isolated from this plant using a model of LPS-induced Read More

Background: Osteoarthritis (OA) is a degenerative joint disease with an increasing incidence associated with increased life expectancy. The application of traditional Chinese medicine in the treatment of OA has become a research hotspot. Objective: This study investigated the effects of XGS externally applied to osteoarthritic joints and analyze its effect on pain in monosodium iodoacetate (MIA)-induced OA rats. This stud Read More

Background: The occurrence of oxidative stress is an important hallmark of tumorigenesis and the development of cancers, including head and neck squamous cell carcinoma (HNSCC). The purpose of this study was to identify a robust oxidative stress-related prognostic model in HNSCC. Methods: Oxidative stress genes related to the prognosis of HNSCC were identified through multiple bioinformatics methods. Results: Th Read More

Background: Phencyclidine (PCP, I) and its substituted analogs are significant and broadly abused psychotomimetic drugs that affect the central nervous system. They possess many pharmacological properties due to the presence of specific receptors in the brain. Aims and Objective: Methyl group, despite strong electron-donating and characters of dipole moments, was placed on various positions of phenyl and amine moieti Read More

Aims and Objective: In this study, an attempt was made to synthesize, characterize, and develop many applications of functionalized rare metal oxide nanoparticles. Herein, a new strategy for drug delivery is developed to functionalize magnetite nanoparticles to improve their performances in the delivery of celecoxib. Materials and Methods: Magnetite Fe3O4@SiO2 nanoparticles are synthesized by the sol-gel method. The su Read More