Cytotoxic and antimalarial constituents of the roots of Eurycoma longifolia
| Autor: | Soefjan Tsauri, J. M. Pezzuto, Kosasih Padmawinata, A. D. Kinghorn, Leonardus B.S. Kardono, C K Angerhofer |
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| Předmět: |
Magnetic Resonance Spectroscopy
Stereochemistry Plasmodium falciparum Pharmaceutical Science Antineoplastic Agents Pharmacognosy Analytical Chemistry Antimalarials Alkaloids Drug Discovery Tumor Cells Cultured Animals Humans Cytotoxic T cell Pharmacology Molecular Structure biology Traditional medicine Leukemia P388 Organic Chemistry Biological activity biology.organism_classification Complementary and alternative medicine Cell culture Quassinoid Molecular Medicine Eurycoma longifolia Drug Screening Assays Antitumor Eurycoma |
| Zdroj: | Scopus-Elsevier |
| Popis: | By bioactivity-directed fractionation, five cytotoxic constituents have been characterized from the roots of Eurycoma longifolia collected in Kalimantan, Indonesia. Four canthin-6-one alkaloids, namely, 9-methoxycanthin-6-one, 9-methoxycanthin-6-one-N-oxide, 9-hydroxycanthin-6-one, and 9-hydroxycanthin-6-one-N-oxide, and one quassinoid, eurycomanone, were found to be cytotoxic principles. Each of these compounds was evaluated against a panel of cell lines comprising a number of human cancer cell types [breast, colon, fibrosarcoma, lung, melanoma, KB, and KB-V1 (a multi-drug resistant cell line derived from KB)] and murine lymphocytic leukemia (P-388). The canthin-6-ones 1-4 were found to be active with all cell lines tested except for the KB-V1 cell line. Eurycomanone was inactive against murine lymphocytic leukemia (P-388) but was significantly active against the human cell lines tested. Two additional isolates, the beta-carboline alkaloids beta-carboline-1-propionic acid and 7-methoxy-beta-carboline-1-propionic acid, were not significantly active with these cultured cells. However, compounds 5 and 7 were found to demonstrate significant antimalarial activity as judged by studies conducted with cultured Plasmodium falciparum strains. The structures of the novel compounds 2-4 and 7 were established by spectral and chemical methods. |
| Databáze: | OpenAIRE |
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