A series of 5- or 7-substituted 3-{4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenylimino}-indolin-2-one derivatives were synthesized by treating 5-(4-aminophenyl)-1,3,4-oxadiazole-2-thiol with different isatin derivatives. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, (1)H NMR, MS) analyses. All the synthesized derivatives were screened for anticancer activity against HeLa cancer cell lines using MTT assay. All the synthetic compounds produced a dose dependant inhibition of growth of the cells. The IC50 values of all the synthetic test compounds were found between 10.64 and 33.62 μM. The potency (IC50 values) of anticancer activity of compounds VIb-d was comparable with that of known anticancer agent, Cisplatin. Among the synthesized 2-indolinones, compounds VIb-d with halogen atom (electron withdrawing groups) at C5 position showed the most potent activity. These results indicate that C5 substituted derivatives may be useful leads for anticancer drug development in the future.
In this study, we have evaluated the pulmonary toxicity of intratracheally (i.t.) instilled two multi walled carbon nanotubes (MWCNT) in rats. The lungs of rats were instilled with phosphate buffered saline + 1% of Tween 80 or MWCNT or carbonyl iron or quartz particles at a dose of 0.2, 1, and 5 mg/kg b.w. Following exposure, bronchoalveolar lavage (BAL) fluid was collected from the lungs to analyze lactate dehydrogenase (LDH), alkaline phosphatase (ALP), lipid peroxidation products (MDA; malondialdehyde), and total microprotein (MTP) levels at 24 h, one week, one month, and three months post instillation periods. The lungs of particle exposed rats were also collected at the same intervals to evaluate for histopathology. Exposures of MWCNT and quartz particles to rats produced transient dose dependant increase in BAL fluid LDH, ALP, MDA, and MTP values than control at all post exposure periods. Results of lung histopathology revealed that exposure of MWCNT produced a dose dependant focal peribronchiolar lymphoid aggregates, foamy alveolar macrophage accumulation, lymphoplasmocytic infiltration, fibrosis and diffuse alveolar damage. In conclusion, instillation of MWCNT produced a greater pulmonary toxicity in rats and was comparable with that of quartz.
The present study aimed to evaluate the effect of Copper Oxide (CuO) Nanoparticles (NP) on liver following oral exposure in rats. A total of 18 male wister rats were used in the experiments including a control group (6 rats). NP were given to the rats with a doses (5, 50 mg/kg b.w./day) via oral gavage and a control group (received only 200 μl PBS). The treatment was continued for 14 days. The supernatants of rat Liver tissue homogenates were used to analyze for glutathione levels (GSH), Catalase, superoxide dismutase (SOD), the extent of lipid peroxidation products (Malondialdehyde, MDA). Oral administration of NP to rats caused a significant (P < 0.05) dose dependent alterations in antioxidant enzyme activities. Data results clearly showed the significant decrease (p < 0.05) in GSH, Catalase (CAT) and SOD activity, whereas the lipid peroxidation product (MDA) levels were increased (p < 0.05). In conclusion, oral exposure of CuO nanoparticles to rats causes significant toxicity to the liver and it might be due to oxidative stress.
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