Careya arborea Roxb. (Family: Lecythidaceae) is commonly called as Slow match tree and is an important medicinal plant. Its different parts viz. bark, leaves and seeds have been reported to show many pharmacological activities. High-performance thin-layer chromatography (HPTLC) is a simple, fast and precise technique for the detection of phytochemicals present in the plant. Therefore, the objective of the present study was to characterize the phytochemical profile for various secondary metabolites using HPTLC for C. arborea bark, leaves and seeds extracts, which revealed the confirmation of these phytochemicals. The present study suggested that the bark contains all the classes of compounds tested namely alkaloids, anthracene derivatives, arbutin derivatives, bitter compounds, cardiac glycosides, coumarin derivatives, essential oils, flavonoids, lignans, pungent-tasting principles, saponins, triterpenes and valepotriates. Whereas, alkaloids are not detected in leaves, and alkaloids and arbutin derivatives are not detected in seeds.

No abstract

A series of novel diketoquinoline acid derivatives as potential anti-HIV-1 Integrase inhibitors were docked, synthesized and characterized by IR, NMR , CHN and MS spectral analysis. Many compounds were identified and docked in integrase pocket. The target diketoquinolines were prepared from substituted oxoquinoline-3-carboxylate. In vitro biological evaluation revealed that some of the titled compounds exhibited moderate to good anti-HIV-1 Integrase inhibitory activity in comparison with the reference drugs i.e. raltegravir and nevirapine. The cytotoxicity of most of testing compounds on C8166 were very low, the CC50 value of them were higher than 200 μM, except the few compounds. Compounds 1-5 showed weak anti-HIV-1 activity, its therapeutic index was 457, 531, 583, 869 and 909 respectively. As a positive control drug, Nevirapine has the best anti-HIV-1 activity (EC50 = 0.015-0.016 μM) in vitro and the CC50 of was higher than 200 μM, its therapeutic index was higher 12418.50. In integrase assay compound 6 and 7 showed EC50 value 0.08 μM as compared with standard drug raltegravir.

Proton pump inhibitors [PPI] are acid activated pro drugs which convert in to sulfenic acid and then in to tetracycline sulfenamide in the acidic pH of parietal cell canaliculi. They block H+K+ATPase proton pumps and reduce gastric acid secretion. They are used to treat acid peptic disorders and NSAID induced gastric mucosal injury. Activity of PPI against Helicobactor pylori [H.pylori] is proved undisputably. Lansoprazole is the most effective PPI against H.pylori due to its unique chemical structure.PPI inhibit urease activity of H. pylori. They affect respiration and energy metabolism of these organisms as result of decreased ATP synthesis. Structural similarity of benzimidazole PPI with imidazole like metronidazole and tinidazole may contribute for their antibacterial property. Omeprazole and lansoprazole have been found to have anti fungal activity by inhibition of fungal H+K+ATPase-vacuolar ATPase which are essential for fungal survival and to carry out essential physiological functions, the inhibition of which leads to fungicidal action. Recently anti tubercular action of lansoprazole was highlighted which is attributed to its intra mycobacterial sulfoxide reduction to lansoprazole sulfide. This acts on mycobacterial cytochrome bc1 complex and inhibits ATP synthesis and compromises energy metabolism threatening its survival. Cytochrome bc1 of plasmodium also forms a drug target for lansoprazole. Thus, lansoprazole can emerge as a potential drug to treat MDR tuberculosis and malaria. Antiviral action of lansoprazole was noted against rhinovirus. Gram positive and negative organisms other than H.pylori were found to be inhibited by omeprazole in vitro. But this is not supported by in vivo studies.

A series of novel imidazopyridine derivatives as proton pump inhibitors was designed with compounds of CID data base and explored considering AZD0865 as standard. Many compounds were identified and docked in proton pump ATPase pocket (PDB ID: 4ux2). Molecular docking studies revealed that many compounds showed good proton pump ATPase inhibitory activity. The docking poses revealed the interaction of ligands with amino acid. The standard drug AZD0865 had docking score of -7.112302 and displayed interactions with Asn138 and Asp137. A series of novel imidazopyridine derivatives as proton pump inhibitors were docked, synthesized and characterized by IR, NMR, CHN and MS spectral analysis. The target imidazopyridines were prepared from substituted 2-aminonicotinic acid and 2-bromo-1-substituted ethanone. in vitro Studies explained that few compounds exhibited moderate to good proton pump ATPase inhibitory activity in comparison with the reference drugs i.e. AZD0865. Compounds 11 and 12 shown higher activities with the IC50 4.3. Compounds 1, 4, 6, 7, 8, 10 and 13 showed weak anti-ulcer activity with its IC50 5.2, 5.8, 5.5, 5.1, 4.9, 4.6 and 5.9 and positive control AZD0865 shown IC50 2.0.