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Planta Med 1999; 65(4): 311-315
DOI: 10.1055/s-1999-13992
Original Paper

Georg Thieme Verlag Stuttgart · New York

Cytotoxic Activity of Indole Alkaloids from Alstonia macrophylla

Niwat  Keawpradub1,3 , E.  Eno-Amooquaye2 , P. J. Burke2 , P. J. Houghton1
  • 1Pharmacognosy Research Laboratories, Department of Pharmacy, King's College London, Manresa Road, London, U.K.
  • 2VGV;Department of Medical Oncology, Charing Cross Hospital, London, U.K.
  • 3Permanent address: Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Thailand
Further Information

Publication History

August 28, 1998

December 6, 1998

Publication Date:
31 December 1999 (online)

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Abstract:

Thirteen indole alkaloids isolated from the root bark of Alstonia macrophylla and a semisynthetic bisindole O-acetylmacralstonine have been assessed for cytotoxic activity against two human lung cancer cell lines, MOR-P (adenocarcinoma) and COR-L23 (large cell carcinoma), using the SRB assay. Pronounced cytotoxic activity was exhibited by the bisindoles on both cell lines. This suggests that, in comparison with the corresponding monomeric indoles, at least part of both the ring systems present in the bisindoles is essential for cytotoxic activity. The potent alkaloids were further tested against a human normal cell line (breast fibroblasts) and other human cancer cell lines including StMl1 1a (melanoma), Caki-2 (renal cell carcinoma), MCF7 (breast adenocarcinoma), and LS174T (colon adenocarcinoma). The bisindoles O-acetylmacralstonine, villalstonine and macrocarpamine were found to possess pronounced activity against cancer cell lines with IC50 values in the range of 2 - 10 μM, with no discernible cell-type selectivity. However, O -acetylmacralstonine displayed discernibly less toxicity against the normal breast fibroblasts.

Key words:

Alstonia macrophylla - Apocynaceae - indole alkaloids - human cancer cell lines - breast fibroblasts - cytotoxicity -