Synthesis and antiproliferative potency of 1,3,4-thiadiazole and 1,3-thiazolidine-4-one based new binary heterocyclic molecules: cell-based anticancer studies.

Herein, we report the synthesis and anticancer properties of 21 new 1,3,4-thiadiazole-2-yl-imino-thiazolidine-4-one containing binary heterocyclic molecules. Cytotoxicity of the synthesized molecules was evaluated on various cancer cell lines (MCF-7, PC3, 4T1, MDA-MB-231, and MOC2) and normal human embryonic cell lines (HEK-293) MTT assay. The cytotoxicity data of developed compounds was compared with the reference anticancer molecule BG45, a selective inhibitor of the HDAC3 enzyme.

Significance of TRAIL/Apo-2 ligand and its death receptors in apoptosis and necroptosis signalling: Implications for cancer-targeted therapeutics.

The human immune defensesystem routinely expresses the tumour necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL), which is the most prevalent element for antitumor immunity. TRAIL associates with its death receptors (DRs), DR4 (TRAIL-R1), and DR5 (TRAIL-R2), in cancer cells to initiate the intracellular apoptosis cascade. Accordingly, numerous academic institutions and pharmaceutical companies havetried to exploreTRAIL's capacity to kill tumourcells by producing recombinant versions of it (rhTRAIL) or TRAIL receptor agonists (TRAs) [monoclonal antibody (mAb), synthetic and natural compounds, etc.

Synthetic GPR40/FFAR1 agonists: An exhaustive survey on the most recent chemical classes and their structure-activity relationships.

Free fatty acid receptor 1 (FFAR1 or GPR40) is a potential target for treating type 2 diabetes mellitus (T2DM) and related disorders that have been extensively researched for many years. GPR40/FFAR1 is a promising anti-diabetic target because it can activate insulin, promoting glucose metabolism. It controls T2DM by regulating glucose levels in the body through two separate mechanisms: glucose-stimulated insulin secretion and incretin production.

Therapeutic advancements in targeting BCL-2 family proteins by epigenetic regulators, natural, and synthetic agents in cancer.

Cancer is amongst the deadliest and most disruptive disorders, having a much higher death rate than other diseases worldwide. Human cancer rates continue to rise, thereby posing the most significant concerns for medical health professionals. In the last two decades, researchers have gone past several milestones in tackling cancer while gaining insight into the role of apoptosis in cancer or targeting various biomarker tools for prognosis and diagnosis.

Preparation of seaweed polysaccharide based hydrophobic composite membranes for the separation of oil/water emulsion and protein.

Agarose is a seaweed-based polysaccharide and is widely used for the separation of nucleic acids in molecular biology. Cross-linked agarose beads are also used as solid-phase matrices in size exclusion chromatography for the separation of proteins. To find the application of agarose for the separation of oil/water emulsion and protein, herein hydrophobic derivative of the seaweed biopolymer [M (1.

Synthetic and computational efforts towards the development of peptidomimetics and small-molecule SARS-CoV 3CLpro inhibitors.

Severe Acute Respiratory Syndrome (SARS) is a severe febrile respiratory disease caused by the beta genus of human coronavirus, known as SARS-CoV. Last year, 2019-n-CoV (COVID-19) was a global threat for everyone caused by the outbreak of SARS-CoV-2. 3CLpro, chymotrypsin-like protease, is a major cysteine protease that substantially contributes throughout the viral life cycle of SARS-CoV and SARS-CoV-2.

Understanding stem cells and its pivotal role in regenerative medicine.

Stem cells (SCs) are clonogenic cells that develop into the specialized cells which later responsible for making up various types of tissue in the human body. SCs are not only the appropriate source of information for cell division, molecular and cellular processes, and tissue homeostasis but also one of the major putative biological aids to diagnose and cure various degenerative diseases. This study emphasises on various research outputs that occurred in the past two decades.

Osteoarthritis: Prognosis and emerging therapeutic approach for disease management.

Osteoarthritis (OA), a disorder of joints, is prevalent in older age. The contemporary cure for OA is aimed to confer symptomatic relief, consisting of temporary pain and swelling relief. In this paper, we discuss various modalities responsible for the onset of OA and associated with its severity.

Isolation of cytotoxic monomeric protein and morin derivatives from (Lam.) Gandhi.

(Lam.) Gandhi (family- Cucurbitaceae), is used both in the Indian traditional system and folk medicine to treat several pathophysiological conditions and complex diseases including cancer. The screening of the phytochemicals of this plant (aerial parts) was performed to evaluate their cytotoxic effect against an cancer model utilising acute promyelocytic leukaemia HL60 cell line.

Analgesic and Anti-Inflammatory Activities of Quercetin-3-methoxy-4'-glucosyl-7-glucoside Isolated from Indian Medicinal Plant .

(family: Cucurbitaceae), commonly known as kudari, is used in the Indian traditional medicine to treat various inflammation-associated diseases, such as asthma, arthritis and pain. However, the anti-inflammatory active components of this plant have not been identified yet. The aim of this study was to investigate the potential analgesic and anti-inflammatory activities of a compound, quercetin-3-methoxy-4'-glucosyl-7-glucoside, isolated from .

Betulinic Acid, the first lupane-type triterpenoid isolated via bioactivity-guided fractionation, and identified by spectroscopic analysis from leaves of -: its potential biological activities assays.

Betulinic acid was first time isolated via bioactivity-guided fractionation from ethyl acetate extract of - leaves. Its structure was established by FTIR, H and C- nuclear magnetic resonance and high-resolution mass spectrometry. It had shown excellent inhibition of anti-inflammatory properties with IC of 10.

l-Cysteine-Conjugated Ruthenium Hydrous Oxide Nanomaterials with Anticancer Active Application.

Bioactive nanomaterials, namely: ruthenium hydrous oxide (or ruthenium oxy-hydroxide), RuO(OH) and also a surface-conjugated novel material of the same within the template of an amino acid molecule, l-cysteine, have been studied. These compounds have been prepared through a simple wet chemical route, under physiological conditions, such that they could be suitably used in anticancer applications. Several physical methods were used for the nanomaterial characterization, e.

A Novel Tetraenoic Fatty Acid Isolated from Amaranthus spinosus Inhibits Proliferation and Induces Apoptosis of Human Liver Cancer Cells.

Amaranthus spinosus Linn. (Family: Amaranthaceae) has been shown to be useful in preventing and mitigating adverse pathophysiological conditions and complex diseases. However, only limited information is available on the anticancer potential of this plant.

Evaluation of in vitro antioxidant, anticancer and in vivo antitumour activity of Termitomyces clypeatus MTCC 5091.

Context: Termitomyces clypeatus (Lyophyllaceae) is a filamentous edible mushroom, having ethnomedicinal uses. However, information about the antioxidant, anticancer and antitumour properties of this mushroom remains to be elucidated.

Objective: The study examines the in vitro antioxidant, anticancer and in vivo antitumour activity of T.

Antibacterial activity of a novel fatty acid (14E, 18E, 22E, 26E)-methyl nonacosa-14, 18, 22, 26 tetraenoate isolated from Amaranthus spinosus.

Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as ''spiny pigweed'', is used in both Indian traditional system and folk medicine for treatment of infectious diseases for a long time in several traditional herbal medicinal preparations. A novel fatty acid [(14E, 18E, 22E, 26E)-methyl nonacosa-14, 18, 22, 26 tetraenoate] is the major metabolite present.

Microtubule-targeting agents augment the toxicity of DNA-damaging agents by disrupting intracellular trafficking of DNA repair proteins.

The paradigm that microtubule-targeting agents (MTAs) cause cell death via mitotic arrest applies to rapidly dividing cells but cannot explain MTA activity in slowly growing human cancers. Many preferred cancer regimens combine a MTA with a DNA-damaging agent (DDA). We hypothesized that MTAs synergize with DDAs by interfering with trafficking of DNA repair proteins on interphase microtubules.

A new ester of fatty acid from a methanol extract of the whole plant of Amaranthus spinosus and its α-glucosidase inhibitory activity.

Context: Amaranthus spinosus Linn. (Amaranthaceae), commonly known as "spiny pigweed", is used both in the Indian traditional system and in folk medicine to treat diabetes.

Objective: The present study evaluates the scientific basis of antidiabetic activity of chloroform fraction of methanol extract of A.

Evaluation of Analgesic and Anti-Inflammatory Activity of Chloroform and Methanol Extracts of Centella asiatica Linn.

A variety of active constituents with wide range of pharmacological actions have been reported with Centella asiatica. The present study was undertaken to assess analgesic and anti-inflammatory properties of its leaf extracts. Dried leaves were defatted with petroleum ether and extracted with chloroform and methanol.

Anti-inflammatory effect of O-methylated flavonol 2-(3,4-dihydroxy-phenyl)-3,5-dihydroxy-7-methoxy-chromen-4-one obtained from Cassia sophera Linn in rats.

Ethnopharmacological Relevance: Cassia sophera Linn (Family Caesalpiniaceae), popularly known as kasundi, is used both in the Indian traditional system and folk medicine to treat several inflammatory pathologies such as asthma, arthritis and pains. The aim of the present study was to evaluate the scientific basis of anti-inflammatory activity of Cassia sophera ethanol extracts and of an isolated constituent of Cassia sophera.

Materials And Methods: The anti-inflammatory activity of Cassia sophera was studied using the carrageenan, dextran induced rat paw edema, and cotton pellet induced granuloma in rats.

Is pregnancy safe with extrahepatic portal vein obstruction? An analysis.

Introduction: We aimed to analyse the pregnancy outcome of women with extrahepatic portal vein obstruction.

Methods: This was a retrospective observational analysis conducted at the Institute of Postgraduate Medical Education and Research, Kolkata, India, between January 2007 and September 2009. A total of 41 pregnancies in 24 women were evaluated.

Hypoglycaemic effect of Melothria heterophylla in streptozotocin-induced diabetic rats.

Context: In the Indian traditional system of medicine, Melothria heterophylla (Lour.) Cogn., (Cucurbitaceae) is prescribed for the treatment of diabetes mellitus.

Evaluation of Hepatoprotective Effect of Leaves of Cassia sophera Linn.

In the present study, the hepatoprotective activity of ethanolic extracts of Cassia sophera Linn. leaves was evaluated against carbon-tetrachloride- (CCl(4)-) induced hepatic damage in rats. The extracts at doses of 200 and 400 mg/kg were administered orally once daily.

Isolation and in vivo hepatoprotective activity of Melothria heterophylla (Lour.) Cogn. against chemically induced liver injuries in rats.

Objective: To investigate hepatoprotective activity of ethanol extract of Melothria heterophylla Lour Cogn. (EEMH) against CCl(4)-induced hepatic damage in rats.

Methods: β-sitosterol was isolated by column chromatography and characterized spectroscopically.

Antihyperglycemic activity of bacosine, a triterpene from Bacopa monnieri, in alloxan-induced diabetic rats.

This article describes the antihyperglycemic activity, in vivo antioxidant potential, effect on hemoglobin glycosylation, estimation of liver glycogen content, and in vitro peripheral glucose utilization of bacosine, a triterpene isolated from the ethyl acetate fraction (EAF) of the ethanolic extract of Bacopa monnieri. Bacosine produced a significant decrease in the blood glucose level when compared with the diabetic control rats both in the single administration as well as in the multiple administration study. It was observed that the compound reversed the weight loss of the diabetic rats, returning the values to near normal.

Antihyperglycemic and hypolipidemic effects of Melothria maderaspatana and Coccinia indica in Streptozotocin induced diabetes in rats.

Antihyperglycemic and hypolipidemic effects of ethanol extract of aerial parts of Melothria maderaspatana and Coccinia indica were evaluated in STZ induced diabetes in Sprague-Dawley rats. The rats were concurrently treated with 100 or 200 mg/kg b.w.