Background: Ethnomedicinally, the family Polygonaceae is famous for the management of cancer. Various species of\nthis family have been reported with anticancer potentials. This study was designed to isolate anticancer compounds\nfrom ethnomedicinally important species Polygonum barbatum.\nMethods: The column chromatography was used for the isolation of compounds from the solvent fraction of P.\nbarbatum. The characterization of isolated compounds was performed by various spectroscopic techniques like UV,\nIR, mass spectrometry and 1D-2D NMR spectroscopy. Keeping in view the ethnomedicinal importance of the family,\ngenus and species of P. barbatum, the isolated compounds (1â??3) were screened for anticancer potentials against oral\ncancer (CAL-27) and lungs cancer (NCI H460) cell lines using MTT assay. Active compound was further investigated for\napoptosis by using morphological changes and flow cytometry analysis. In vivo anti-angiogenic study of the isolated\ncompounds was also carried using chorioallantoic membrane assay. Docking studies were carried out to explore the\nmechanism of anticancer activity.\nResults: Three dihydrobenzofuran derivatives (1â??3) have been isolated from the ethyl acetate fraction of P. barbatum.\nThe structures of isolated compounds were elucidated as methyl (2S,3S)-2-(3,4-dimethoxyphenyl)-4-((E)-3-ethoxy-\n3-oxoprop-1-en-1-yl)-7-methoxy-2,3-dihydrobenzo-furan-3-carboxylate (1), (E)-3-((2S,3S)-2-(3,4-dimethoxyphenyl)-\n7-methoxy-3-(methoxy carbonyl)-2,3-dihydrobenzofuran-4-yl)acrylic acid (2) and (2S,3S)-4-((E)-2-carboxyvinyl)-
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