Glycopentalone, a novel compound from Glycosmis pentaphylla (Retz.) Correa with potent anti-hepatocellular carcinoma activity.

ETHNOPHARMACOLOGICAL RELEVANCE: Glycosmis pentaphylla (Retz.) Correa is used in Indian traditional medicine against various liver ailments, including cancer. AIM OF THE STUDY: Isolation and characterization of the most active anti-hepatocellular carcinoma (HCC) compound from the alcohol extract of G. pentaphylla. MATERIALS AND METHODS: Different chromatographic (HPLC, TLC and column chromatography) and methods like IR, LCMS and NMR were used for the isolation and structural identification of the active anti-HCC compound from G. pentaphylla. Cytotoxic and apoptosis inducing effect of the active compound were assessed in Hep3 B, RAW264.7 and HEK293 cell lines by MTT assay, morphological studies, Hoechst staining and Annexin V FITC assay. RESULTS: The most active compound was isolated as yellow needle shaped crystals. The structure of the compound was identified by IR, LCMS and NMR methods. The structural details show that the isolated compound is a novel chemical and have structural similarity with chalcone. MTT assay, physiological and FACS analysis proved the anti-HCC efficacy of the isolated compound in vitro. CONCLUSION: The study confirmed that the most active anti-HCC compound present in the alcohol extract of G. pentaphylla is a chalcone derivative. This compound showed specific cytotoxicity against Hep3 B with minor cytotoxicity against non HCC cell lines, RAW264.7 and HEK293. The present study, therefore, supports the folklore knowledge for the utility of G. pentaphylla and provides a scientific basis for their traditional usage against liver cancer.