Nicotine promotes epithelial to mesenchymal transition and gemcitabine resistance via hENT1/RRM1 signalling in pancreatic cancer and chemosensitizing effects of Embelin-a naturally occurring benzoquinone.

Pancreatic cancer is lethal due to poor prognosis with 5-year survival rate lesser than 5 %. Gemcitabine is currently used to treat pancreatic cancer and development of chemoresistance is a major obstacle to overcome pancreatic cancer. Nicotine is a known inducer of drug resistance in pancreatic tumor micro-environment.

Tetrahydrobenzothiophene derivatives ameliorate Mia PaCa-2 cell progression and induces apoptosis via inhibiting EGFR2 tyrosine kinase signal.

A series of new thiophene analogues with acarbonitrile-basedmoiety were designed and synthesized via structural optimization. The conjugates were assessed for their in-vitro cytotoxic activity against a human pancreatic cancer cell line (Mia PaCa-2) and among them compound 5b showed IC value of 13.37 ± 2.

Artabotrys odoratissimus Bark Extract Restores Ethanol Induced Redox Imbalance and Toxicity in Hepatocytes and In Vivo Model.

Alcohol-induced oxidative stress is a key player in the development of liver diseases, and herbal alternatives are important means of ameliorating the hepatotoxic effects. The study aimed to evaluate the hepatoprotective potentiality of Artabotrys odoratissimus, an important medicinal shrub from the family Annonaceae. The phenolic compounds from bark ethanol extract (BEE) were detected using RP-HPLC.

Potential role of embelin in the prevention of Freund's adjuvant induced inflammation and ROS.

Inflammation is a complex biological response involving immune cells to an infection creating injury to the normal tissues. The anti-inflammatory efficacy of embelin, a benzoquinone from the plant , was screened for antioxidant and anti-inflammatory activity in carrageenan and Freund's adjuvant-induced inflammation models. Embelin exhibited significant dose-dependent antioxidant potential.

Evaluation of drug candidature: In silico ADMET, binding interactions with CDK7 and normal cell line studies of potentially anti-breast cancer enamidines.

We have recently explored novel class of potentially anti-breast cancer active enamidines in which four molecules 4a-c and 4h showed higher anticancer activity compared to standard drug doxorubicin. As a part of extension of this work, we have further evaluated in silico cheminformatic studies on bioactivity prediction of synthesized series of enamidines using mole information. The normal cell line study of four lead compounds 4a-c and 4h against African green monkey kidney vero strain further revealed that the compounds complemented good selectivity in inhibition of cancer cells.

Novel Furan Coupled Quinoline Diamide Hybrid Scaffolds as Potent Antitubercular Agents: Design, Synthesis and Molecular Modelling.

Background: A novel series of 2-[(2-{[2-(furan-2-yl) quinolin-4-yl] carbonyl} hydrazinyl) carbonyl] benzoic acid, -4-oxobut-2-enoic acid and -4-oxobutanoic acids were synthesized and screened for in vitro antitubercular activity.

Objectives: In the present investigation, we describe the synthesis and biological screening of furan C-2 quinoline coupled diamides for antitubercular activity.

Methods: The mycobacterium tuberculai testing was carried out by MABA method and molecular docking studies were done by open-source molecular docking program, Autovina, using Pyrx 0.

Cytotoxic, DNA Cleavage and Pharmacokinetic Parameter Study of Substituted Novel Furan C-2 Quinoline Coupled 1, 2, 4-Triazole and Its Analogs.

Background: Furan, quinoline and triazoles are known for their wide spectrum biologically active molecules. A series of novel furan C-2 quinoline and 1, 2, 4-triazole (FQT) coupled hybrids were designed and synthesized to evaluate for their DNA cleavage and cytotoxic studies.

Objectives: In this work we describe the synthesis and biological evaluation of furan C-2 quinoline coupled triazoles exposed for cytotoxic and DNA cleavage study.

Analgesic, Antibacterial and Antiviral Activities of 2-(5-Alkyl-1,3,4-oxadiazol-2-yl)-3H-benzo[f]chromen-3-ones.

A novel series of 2-(5-alkyl-1,3,4-oxadiazol-2-yl)-3H-benzo[f]chromen-3-ones (4a-e) have been evaluated for analgesic, antibacterial and antiviral activities. Analgesic activity was carried out using acetic acid-induced writhing method in Swiss albino male mice. The antibacterial activity was performed against Gram-positive and Gram-negative clinical strains by agar well diffusion method.

Microwave assisted rapid synthesis and biological evaluation of stable copper nanoparticles using T. arjuna bark extract.

Terminalia arjuna (T. arjuna) bark extract is used to reduce Cu(2+)→Cu(0) under microwave irradiation. The formation of copper nanoparticles (CuNPs) is monitored by recording the UV-Vis absorption spectra for surface plasmon resonance (SPR) peak, ~535 nm.

Synthesis and DNA cleavage studies of novel quinoline oxime esters.

New 2-chloro-3-formyl quinoline oxime esters were synthesized by the reaction of 2-chloro-3-formyl quinoline oximes with various benzoyl chlorides in the presence of triethyl amine and dichloromethane at 0°C. The DNA photo cleavage studies of some new oxime esters were investigated by neutral agarose gel electrophoresis at different concentrations (40μM and 80μM). Analysis of the cleavage products in agarose gel indicated that few of quinoline oxime esters (3d-i) converted into supercoiled pUC19 plasmid DNA to its nicked or linear form.

Effect of ethanol extract of Rivea hypocrateriformis on the estrous cycle of the rat.

The ethanol extract of Rivea hypocrateriformis was administered orally at the dose levels of 200 and 400 mg/kg body weight to adult albino rats and resulted in an irregular estrous cycle with shortened estrus and metestrus, and with lengthened proestrus in non-dose dependent manner. Significant decreases in number of graffian follicles and corpora lutea and significant increases in number of atretic follicles in treated rats during experimental period indicated the antiovulatory effect of the extract. Increases in the weight of the uterus, its thickness and diameter indicated the uterotrophic effect of the extract.

Antiimplantation and pregnancy interruption efficacy of Rivea hypocrateriformis in the rat.

Petroleum ether, chloroform, ethanol and distilled water extracts of the aerial parts of the plant Rivea hypocrateriformis (Convolvulaceae) were tested for antiimplantation and pregnancy interruption properties in female albino rats. Among these, the ethanol extract was found to be most effective in causing significant antiimplantation and interruption of early pregnancy. The antifertility activity of ethanol extract was reversible on exogenous administration of hydroxy progesterone.