In vitro Cytotoxic Effect of Indole Alkaloids from The Roots of Kopsia singapurensis ridl. Against The Human Promyelocytic leukemia (HL-60) and The Human Cervical Cancer (HeLa) Cells

Abdul Manaf, Ali and Kartini, Ahmad and Ulil, Amna (2015) In vitro Cytotoxic Effect of Indole Alkaloids from The Roots of Kopsia singapurensis ridl. Against The Human Promyelocytic leukemia (HL-60) and The Human Cervical Cancer (HeLa) Cells. International Journal of Pharmaceutical Sciences Review and Research, 31 (2). pp. 89-95. ISSN 0976 –044X [P]

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Abstract

Six indole alkaloids; kopsamine N(4)-oxide 1, kopsifine 2, rhazinicine 3, aspidodasycarpine 4, kopsamine 5 and akuammidine 6, were isolated from the roots of Kopsia singapurensis Ridl. (Apocynaceae). Compound 2 is first time isolated from the roots of K. singapurensis Ridl. Those compounds were screened for in vitro cytotoxic activity against human cervical cancer (HeLa), human promyelocytic leukemia (HL-60), and the normal mouse fibroblast (NIH/3T3) cell lines by using the MTT assay. Based on comparison with vincristine (control), kopsifine 2 showed very strong cytotoxic effects against HL-60 cells, while, kopsamine 5 exhibited a moderate cytotoxic activity effects against HL-60 cells with CD50 values of 0.9 μg/mL and 6.9 μg/mL, respectively. Akuammidine 6 and rhazinicine 3 exhibited significant cytotoxicity effects against HeLa cells with the CD50 values 2.8 μg/mL and 2.9 μg/mL, respectively. However, aspidodasycarpine 4 showed a moderate cytotoxicity effects against HeLa cells with the CD50 value of 7.5 μg/mL, and kopsamine N(4)-oxide 1 was inactive against all these cancer cells. Although kopsifine 2, rhazinicine 3, and aspidodasycarpine 4 showed high cytotoxic effects against HL-60 and HeLa cell lines, but they also showed cytotoxic on normal cell (NIH/3T3) with CD50 values of 20.7, 20.8, and 6.4 μg/mL, respectively. Therefore, these three alkaloids are not suggested as cytotoxic agents for these cancer cells. This is the first cytotoxicity report on HL-60, HeLa and NIH/3T3 cell lines for these compounds.

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