Abstract
Crude extracts of Punica granatum fruit peel, its isolates, and semisynthetic analogs were investigated for their Cathepsin D protease reticence. Hexane extract (HE), chloroform extract (CE), and ethyl acetate extract (EAE) exhibited significant inhibition of Cathepsin D activity. The bioactivity-guided isolation of hexane- and chloroform-soluble fractions yielded piperine and ursolic acid as bioactive constituents. Upon semisynthetic modifications of ursolic acid, two of the analogs (7 and 8) exhibited higher inhibition of Cathepsin D activity: IC50 at 12.87 and 9.40 μM, respectively. P. granatum fruit peel extracts may act as breast cancer chemopreventive agent.
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This study was supported by the Council of Scientific and Industrial Research (CSIR), India. S.L. acknowledges the partial financial support from the Council of Science and Technology, Uttar Pradesh.
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Chaturvedi, A.K., Luqman, S., Dubey, V. et al. Inhibition of Cathepsin D protease activity by Punica granatum fruit peel extracts, isolates, and semisynthetic analogs. Med Chem Res 22, 3953–3958 (2013). https://doi.org/10.1007/s00044-012-0397-z
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DOI: https://doi.org/10.1007/s00044-012-0397-z