Anti-ulcer constituents of Annona squamosa twigs.

Dinesh K Yadav, Neetu Singh, Kapil Dev, Rolee Sharma, Mahendra Sahai, Gautam Palit, Rakesh Maurya

Division of Medicinal and Process Chemistry, Central Drug Research Institute, CSIR, Lucknow 226001, India.

Fitoterapia 2011 Jun

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Phytochemical investigation of Annona squamosa twigs, resulted in isolation and identification of twelve known (1-12) compounds among them one 1-(4-β-D-glucopyranosyloxyphenyl)-2-(β-D-glucopyranosyloxy)-ethane (11) is synthetically known but first time isolated from natural sources. Their structures were elucidated using 1D and 2D NMR spectroscopic analysis. The isolated compounds (2-8, 11) were evaluated for H(+) K(+)-ATPase activity. Three of these compounds (+)-O-methylarmepavine (2), N-methylcorydaldine (3), isocorydine (6) showed promising anti-secretory activity. Activity of these compounds, comparable to the standard drug omeprazole is novel to our finding. Moreover, there is no information accessible regarding the pharmacological effect of A. squamosa on the gastrointestinal system. This study is the first of its kind to show the significant anti-ulcer effect of A. squamosa. The present study aimed to evaluate the gastroprotective effect of A. squamosa (AS) and to identify its active constituents. Anti-ulcer activity was evaluated against cold restraint (CRU), pyloric ligation (PL), aspirin (ASP), alcohol (AL) induced gastric ulcer and histamine (HA) induced duodenal ulcer model and further confirmed through in vitro assay of H(+) K(+)-ATPase activity and plasma gastrin level. AS and its chloroform and hexane fraction attenuated ulcer formation in CRU, PL, HA model and displayed anti-secretory activity in vivo through reduced free, total acidity and pepsin in PL, confirmed by in vitro inhibition of H(+) K(+)-ATPase activity with corresponding decrease in plasma gastrin level. Cytoprotection of AS was apparent with protection in AL, ASP models and enhanced mucin level in PL. Copyright © 2011 Elsevier B.V. All rights reserved.

Citation

Dinesh K Yadav, Neetu Singh, Kapil Dev, Rolee Sharma, Mahendra Sahai, Gautam Palit, Rakesh Maurya. Anti-ulcer constituents of Annona squamosa twigs. Fitoterapia. 2011 Jun;82(4):666-75