1012339-66-0Relevant articles and documents
Potential anticancer activity of naturally occurring and semisynthetic derivatives of aculeatins A and B from Amomum aculeatum
Chin, Young-Won,Salim, Angela A.,Su, Bao-Ning,Mi, Qiuwen,Chai, Hee-Byung,Riswan, Soedarsono,Kardono, Leonardus B. S.,Ruskandi, Agus,Farnsworth, Norman R.,Swanson, Steven M.,Kinghorn, A. Douglas
, p. 390 - 395 (2008)
Activity-guided fractionation of hexanes- and CHCl3-soluble extracts of Amomum aculeatum leaves, collected in Indonesia, led to the isolation of three new dioxadispiroketal-type (3-5) and two new oxaspiroketal-type (6 and 7) derivatives. Nine semisynthetic derivatives (1a-1h and 2a) of the parent compounds, aculeatins A (1) and B (2), were prepared. All isolates and semisynthetic compounds were tested against a small panel of human cell lines. Of these, aculeatin A (1; ED50 0.2-1.0 μM) was found to be among the most cytotoxic of the compounds tested and was further evaluated in an in vivo hollow fiber assay; it was found to be active against MCF-7 (human breast cancer) cells implanted intraperitoneally at doses of 6.25, 12.5, 25, and 50 mg/kg. However, when 1 was tested using P388 lymphocytic leukemia and human A2780 ovarian carcinoma in vivo models, it was deemed to be inactive at the doses used.
