Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2,3-triazolylbenzohydrazides.

1H-1,2,3-Triazolylbenzohydrazides (6a-h and 11a-l) were synthesized from 2-chloronicotinaldehydes and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv strain (ATCC-27294). Seven compounds 6b, 6e,f, 11d, 11h, 11j and 11l displayed potent anti-mycobacterial activity (MIC 2.8-6.2 µM). Potent anti-mycobacterial compounds were chosen for cytotoxicity studies by MTT protein assay against normal cell lines (PBMC and Raw 264.7) and shown low cytotoxicity. This is the first Letter assigning anti-mycobacterial activity, cytotoxicity and structure activity relationship for 1H-1,2,3-triazolylbenzohydrazides.

New diterpenoids from Caesalpinia species and their cytotoxic activity.

Chemical investigation on Caesalpinia crista afforded two new diterpenoids, 6beta-cinnamoyloxy-7beta-acetoxyvouacapen-5alpha-ol and 6beta,7beta-dibenzoyloxyvouacapen-5alpha-ol and on Caesalpiniapulcherrima another new diterpenoid, 12-demethyl neocaesalpin F along with several known constituents. The structures of the new compounds were settled from their 1D and 2D NMR spectral data. The cytotoxicity of these compounds was measured on two different cancer cell lines.

In vitro effects of chlorpyrifos on the acetylcholinesterase activity of euryhaline fish, Oreochromis mossambicus.

The in vitro effect of a widely used organophosphorus insecticide, chlorpyrifos (CPP), on the acetylcholinesterase (AChE) activity was studied in vitro. The kinetic constants Km and Vmax and the bimolecular constant k(j) were determined in vitro. The in vitro AChE study indicated that CPP is neurotoxic and that it alters the apparent Km values widely in a concentration-dependent manner, resulting in a competitive type of inhibition. Based on the k(i) values, the sensitivity of AChE in brain is greater than that in gill tissue, at 7.3 x 10(-5) M and 11.92 x 10(-5) M, respectively. The study points to the importance of kinetic studies and the results suggest that in biomonitoring programmes brain AChE activity can be a good diagnostic tool for CPP toxicity.

Multifidone: a novel cytotoxic lathyrane-type diterpene having an unusual six-membered A ring from Jatropha multifida.

Chemical examination of the stems of Jatropha multifida afforded a novel lathyrane-type diterpene, multifidone, having an unusual six-membered A ring. The structure of the compound was determined from detailed analysis of its 1D and 2D NMR spectra and X-ray crystallographic analysis. Its cytotoxicity was measured on four different cancerous cell lines.

Evaluation of cytotoxicity, morphological alterations and oxidative stress in Chinook salmon cells exposed to copper oxide nanoparticles.

The current study is aimed to study cytotoxicity and oxidative stress mediated changes induced by copper oxide nanoparticles (CuO NPs) in Chinook salmon cells (CHSE-214). To this end, a number of biochemical responses are evaluated in CHSE-214 cells which are as follows [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide] MTT, neutral red uptake (NRU), lactate dehydrogenase (LDH), protein carbonyl (PC), lipid peroxidation (LPO), oxidised glutathione (GSSG), reduced glutathione (GSH), glutathione peroxidase (GPx), glutathione sulfo-transferase (GST), superoxide dismutase (SOD), catalase (CAT), 8-Hydroxy-2'-deoxyguanosine (8-OHdG) and reactive oxygen species (ROS), respectively. The 50% inhibition concentration (IC50) of CuO NPs to CHSE-214 cells after 24 h exposure was found to be 19.026 µg ml(-1). Viability of cells was reduced by CuO NPs, and the decrease was dose dependent as revealed by the MTT and NRU assay. CHSE-214 cells exposed to CuO NPs induced morphological changes. Initially, cells started to detach from the surface (12 h), followed by polyhedric, fusiform appearance (19 h) and finally the cells started to shrink. Later, the cells started losing their cellular contents leading to their death only after 24 h. LDH, PC, LPO, GSH, GPx, GST, SOD, CAT, 8-OHdG and ROS responses were seen significantly increased with the increase in the concentration of CuO NPs when compared to their respective controls. However, significant decrease in GSSG was perceptible in CHSE-214 cells exposed to CuO NPs in a dose-dependent manner. Our data demonstrated that CuO NPs induced cytotoxicity in CHSE-214 cells through the mediation of oxidative stress. The current study provides a baseline for the CuO NPs-mediated cytotoxic assessment in CHSE-214 cells for the future studies.

Assessment of cytotoxicity and oxidative stress induced by titanium oxide nanoparticles on Chinook salmon cells.

Titanium oxide nanoparticles (TiO2 NPs) have received wide attention in diverse application, but the potential impact of these nanomaterials on the environment, aquatic life and especially on fish cell lines is lacking. The present study aimed to investigate the cytotoxicity and oxidative stress induced by TiO2 NPs on Chinook salmon cells derived from Oncorhynchus tshawytscha embryos (CHSE-214). The The MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide] and neutral red (NR) assays in CHSE-214 cells exposed to TiO2 NPs revealed concentration-dependent cytotoxic effect in the range of 10 to 60 µg/ml for 24 h. CHSE-214 cells exposed to TiO2 NPs (10-60 µg/ml) exhibited significant decline in superoxide dismutase (SOD), catalase (CAT) glutathione (GSH) content and increased lipid peroxidation (LPO) in a concentration-dependent manner. TiO2 NPs induced cytotoxicity and oxidative stress in CHSE-214 cells which serve as a base line studies for future studies.

Modulation of glutathione and its dependent enzymes in gill cells of Anguilla anguilla exposed to silica coated iron oxide nanoparticles with or without mercury co-exposure under in vitro condition.

The current study aimed to investigate the modulation of glutathione (GSH) and its dependent enzymes (glutathione reductase, GR; glutathione peroxidase, GPx; glutathione sulfotransferase, GST) from 0 to 72 h in the gill cells of Anguilla anguilla under in vitro condition exposed to silica coated iron oxide nanoparticles functionalized with dithiocarbamate (Fe3O4@SiO2/SiDTC, hereafter called 'IONPs'; 100 nm; 2.5 mgL(-1)) with or without mercury (Hg) coexposure. Significantly decreased TGSH content under IONP alone exposure from 0 to 72 h indicated increased utilization of the TGSH in response to IONP stress. Significant increases in the activity of GR, GPx and GST were depicted when exposed to IONP alone. Lipid peroxidation (LPO), a membrane damage trait also significantly increased under IONP alone exposure indicating the efficient role of antioxidant induction abolishing the IONP-mediated enhanced reactive oxygen species. Under Hg exposure, gill cells displayed significantly increased activity of the studied enzymes (GR, GPx and GST) and LPO which was accompanied by significantly decreased TGSH content. Concomitant (IONPs+Hg) exposure displayed a synergistic response to that of individual responses of either IOPN or Hg which was evident by significant increases in GR, GPx, GST and LPO. Overall, our findings revealed a fine tuning among the GSH and its dependent enzyme modulation under IONP, Hg and its concomitant (IONPs+Hg) exposure in A. anguilla gill cells under in vitro condition.