Antitumor activity of four macrocyclic ellagitannins from Cuphea hyssopifolia.
We evaluated the antitumor activities of four macrocyclic hydrolyzable tannin dimers, cuphiin D1, cuphiin D2, oenothein B and woodfordin C isolated from Cuphea hyssopifolia (Lythraceae). All significantly inhibited the growth of the human carcinoma cell lines KB, HeLa, DU-145, Hep 3B, and the leukemia cell line HL-60, and showed less cytotoxicity than adriamycin against a normal cell line (WISH). All four compounds inhibited the viability of S-180 tumor cells in an in vitro assay and an in vivo S-180 tumor-bearing ICR mice model. Oenothein B demonstrated the greatest cytotoxicity (IC50 = 11.4 microg/ml) against S-180 tumor cells in culture, while cuphiin D1 resulted in the greatest increase in survival on S-180 tumor-bearing mice (%ILS = 84.1%). Our findings suggest that the antitumor effects of these compounds are not only related to their cytotoxicity on carcinoma cell lines, but also depended on a host-mediated mechanism; they may therefore have potential for antitumor applications.
Department of Pharmacognosy, Graduate Institute of Pharmaceutical Sciences, Taipei Medical College, Taiwan.
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D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology / Q000627:therapeutic use*; D001835:Body Weight / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D004353:Drug Evaluation, Preclinical; D006801:Humans; D047348:Hydrolyzable Tannins; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000401:mortality / Q000473:pathology; D015996:Survival Rate; D013634:Tannins / Q000494:pharmacology / Q000627:therapeutic use*; D014407:Tumor Cells, Cultured; D014410:Tumor Stem Cell Assay
D000972:Antineoplastic Agents, Phytogenic; D047348:Hydrolyzable Tannins; D013634:Tannins; C120622:cuphiin D(1); C120623:cuphiin D(2); C080077:oenothein B; C065469:woodfordin C