Anticancer potential of 3-(arylideneamino)-2-phenylquinazoline-4(3H)-one derivatives.

Different quinazoline derivatives have showed wide spectrum of pharmacological activities. Some 3-(arylideneamino)-phenylquinazoline-4(3H)-ones have been reported to possess antimicrobial activity. The present study has been undertaken to evaluate the anticancer effect of these quinazolinone derivatives. The quinazolinone derivatives were synthesized as reported earlier. Compounds containing NO(2), OH, OCH(3), or OH and OCH(3) as substituent(s) on the arylideneamino group were named as P(3a), P(3b), P(3c), and P(3d) respectively. Out of these, P(3a) and P(3d) showed better cytotoxic activity than P(3b) and P(3c) on a panel of six cancer cell lines of different origin, namely, B16F10, MiaPaCa-2, HCT116, HeLa, MCF7, and HepG2, though the effect was higher in B16F10, HCT116, and MCF7 cells. P(3a) and P(3d) induced death of B16F10 and HCT116 cells was associated with characteristic apoptotic changes like cell shrinkage, nuclear condensation, DNA fragmentation, and annexin V binding. Also, cell cycle arrest at G1 phase, alteration of caspase-3, caspase-9, Bcl-2 and PARP levels, loss of mitochondrial membrane potential, and enhanced level of cytosolic cytochrome c were observed in treated B16F10 cells. Treatment with multiple doses of P(3a) significantly increased the survival rate of B16F10 tumor bearing BALB/c mice by suppressing the volume of tumor while decreasing microvascular density and mitotic index of the tumor cells.

In situ synthesis and antibacterial activity of copper nanoparticle loaded natural montmorillonite clay based on contact inhibition and ion release.

Copper nanoparticle based clay composite has been synthesized by in situ reduction of a copper ammonium complex ion and characterized by different analytical instruments. The copper nanoparticles were both intercalated and adsorbed on the surface with diameters of <5nm (for intercalated) and 25-30nm (for adsorbed). The composite showed good stability for over 3 months in air. Excellent antimicrobial activity of the composite was observed on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Enterococcus faecalis with mortality rates >90% after 12h. Cellular membrane damage permeated by direct attachment of the composite and indirect damage caused by released copper ion are the primary sources of antibacterial action. Cytotoxicity measurements showed minimal adverse effect on the two human cell lines beyond the M.B.C. value for the microorganisms studied. In the present form the clay composite shows good promise for use in therapeutic applications.