Assessment of in vitro biological activities of Terminalia arjuna Roxb. bark extract and Arjunarishta in inflammatory bowel disease and colorectal cancer

306-313Alternative or complementary therapies for several inflammatory disorders have gained considerable acceptability and popularity in recent years. The Arjuna tree, Terminalia arjuna Roxb. (Combretaceae) holds antidiarrheal and antioxidant potential useful in management of inflammatory gastro intestinal ailments. Here, we evaluated the possible effect of T. arjuna hydroalcoholic extract (TAHA) and traditional Ayurvedic formulation Arjunarishta (AA) for the treatment of inflammatory bowel disease (IBD) and colorectal cancer. The phytochemical profile of test materials was confirmed via investigation of total phenolic and flavanoid content and standardized by HPLC-PDA method. In vitro antioxidant activity was carried out using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing ability of plasma (FRAP) assay. Antimicrobial potential was tested against clinical isolates of IBD patients (HM95, HM233, HM251, HM615). Cytotoxicity was determined against human colorectal adenocarcinoma cells (Caco2, COLO.205), whereas, cytocompatibility against normal rat intestinal epithelial (IEC-6) and mouse fibroblast cells (L929). Additionally, in vitro oxidative cell damage stress was estimated by lipid peroxidation biomarker. TAHA displayed higher antioxidant capacity as compared to AA formulation. Different sensitivities were observed against different study cell lines in dose dependant manner. Similarly, significant (P <0.05) enhanced malondialdehyde (MDA) concentrations in test materials and 5-FU treated colorectal adenocarcinoma cells was detected as compared to control cells. TAHA and AA exhibited antimicrobial activity against IBD associated clinical isolates. These findings provide biological evidence for therapeutic application of TAHA and AA in IBD and colorectal cancer treatment

Catalytic transesterification of beta-ketoesters with zeolite H-FER under solvent free conditions

Zeolite H-FER catalyzes the transesterification of ??-ketoesters with variety of alcohols under solvent-less condition in excellent yields. The catalyst can be reused without any loss of activity. ?? ARKAT

The Alkaloid Ageladine A, Originally Isolated from Marine Sponges, Used for pH-Sensitive Imaging of Transparent Marine Animals

The brominated pyrrole-imidazole Ageladine A was used for live imaging of the jellyfish (jellies) Nausithoe werneri, the sea anemone Metridium senile and the flatworm Macrostomum lignano. The fluorescence properties of Ageladine A allow for estimation of pH values in tissue and organs in living animals. The results showed that Nausithoe werneri had the most acidic areas in the tentacles and close to the mouth (pH 4–6.5), Metridium senile harbours aggregates of high acidity in the tentacles (pH 5) and in Macrostomum lignano, the rhabdoids, the gonads and areas close to the mouth were the most acidic with values down to pH 5

Synthesis of spirocyclic azacycles from the cyclization of furan tethered N-acyliminium ions

The protic and Lewis acid promoted cyclization reactions of tethered furan-4,5-dihydroxypiperid-2-ones, furan-4,5-diacetoxypiperid-2-ones and furan-3,4-diacetoxypyrrolid-2-ones, via their corresponding N-acyliminium ion intermediates, have been studied. In the case of the furan-4,5-dihydroxypiperid-2-one 2a and its diacetate derivative 2b, macrocyclic products were formed from an initial intermolecular reaction between 2a or 2b, via the nucleophilic C5 furan carbon, and their corresponding N-acyliminium ion intermediates. When the furan C5 position of 2b was blocked by substitution with bromine then TFA or Sc(OTf)3 catalysed cyclization reactions gave a spirotricyclic product (a 5-6-6-tricycle) in a highly diastereoselective manner. Cyclization of the analogous C5-Br-furan-pyrrolidone 29 with TFA resulted in a related spirotricyclic (a 5-6-5 tricycle) product. Attempts to prepare an analogous azepine system, a 5-7-5 tricycle, were not successful. Cyclization reactions of the C5-PhS-furan- or C5-phenylsulfonyl-pyrrolidone analogues of 29 with TFA were also not successful

One Pot Synthesis of Ageladine A, Analogues and their Biological Screening

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Synthesis of Ageladine A, analogues and their biological activities

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