Bioactivity-guided Isolation of Cytotoxic Sesquiterpene Lactones of Gochnatia polymorpha ssp. floccosa
Article first published online: 22 DEC 2011
Copyright © 2011 John Wiley & Sons, Ltd.
Volume 26, Issue 7, pages 1053–1056, July 2012
How to Cite
Strapasson, R. L. B., Cervi, A. C., Carvalho, J. E., Ruiz, A. L. T. G., Salvador, M. J. and Stefanello, M. É. A. (2012), Bioactivity-guided Isolation of Cytotoxic Sesquiterpene Lactones of Gochnatia polymorpha ssp. floccosa. Phytother. Res., 26: 1053–1056. doi: 10.1002/ptr.3693
- Issue published online: 5 JUL 2012
- Article first published online: 22 DEC 2011
- Fundação Araucaria. Grant Number: 15288/2008
- Gochnatia polymorpha;
- dimeric guaianolides;
- cytotoxic activity
Phytochemical study of Gochnatia polymorpha (Less) Cabr. ssp. floccosa Cabr. trunk bark, guided by antiproliferative assays on 10 human cancer cell lines and the VERO cell line, yielded six known compounds identified as the triterpene bauerenyl acetate, the guaianolide 11α,13-dihydrozaluzanin C and the dimeric guaianolides 10-desoxygochnatiolide A, gochnatiolide A, 8-hydroxi-10-desoxygochnatiolide A and 8-hydroxigochnatiolide A. Extracts, fractions of extracts and isolated compounds were tested in vitro against a panel of human cancer cell lines, including U251 (glioma, CNS), UACC-62 (melanoma), MCF-7 (breast), NCI-ADR/RES (drug-resistant ovarian), 786.0 (kidney), NCI-H460 (lung, no small cells), PC-3 (prostate), OVCAR-3 (ovarian), HT-29 (colon), K562 (leukemia) and against the VERO no cancer cell line. Bauerenyl acetate was inactive, while 11α,13-dihydrozaluzanin C showed weak activity against UACC62 and the VERO cell line. The most active compounds were 10-desoxygochnatiolide A and gochnatiolide A, which inhibited the growth of kidney, melanoma, ovarian-resistant and glioma cell lines with values of TGI (total growth inhibition) varying 0.21–1.09 µg/mL. This is the first report about cytotoxic activity of dimeric lactones against cell lines. Copyright © 2011 John Wiley & Sons, Ltd.