Symposium “Plants in Health and Culture”
O. Jansena, M. Fredericha, M. Titsa, L. Angenota, A. Chariotb, E. Ollivierc, G. Balansardc, V. Akhmedjanova d
a Laboratory of Pharmacognosy, Natural and Synthetic Drugs Research Center, University of Liège, Bât. B36, Av. de l’hôpital, 1, 4000 Liège
b Laboratory of Medical Chemistry, Cellular and Molecular Therapy Center, University of Liège
c Laboratory of Pharmacognosy, Faculty of Pharmacy, University of Aix- Marseille II
d Uzbek Academy of Sciences, Yunusov Institute of the Chemistry of plant substances, Tashkent, Uzbekistan
Screening of fourteen alkaloids from the genus Haplophyllum
for their cytotoxic properties
Apparition of resistance with the conventional anticancer drugs stimulated the search for new anticancer agents especially from natural origin.
The genus Haplophyllum has been used for a long time in folk medicine in Central Asia to treat warts, tumors of testes, lichens, herpes, erysipelas and in some painful syndromes from different origins (Avicenna, Canon Medicinae).
In the framework of INTAS project n°2043 called “Research on antitumoral natural compounds from Uzbek and Georgian plants”, fourteen alkaloids isolated from the Uzbek flora, more precisely from the genus Haplophyllum, were screened for their cytotoxic properties against the two cell lines HeLa (cervix cancer) and HCT-116 (colon cancer) using the tetrazolium salt WST-1.
The five more cytotoxic compounds were three furoquinolins: skimmianine, haplopine and γ-fagarine, and two pyranoquinolones: flindersine and haplamine. They were especially active on the HeLa cell line. The cytotoxic properties of these five compounds were further investigated on five other cell lines: MCF-7, MDAMB-231, SKBR-3, OVCAR-3 and HT-29.
This work of screening finally permitted to select haplamine as the most potent agent on all the tested cell lines.
This alkaloid was tested on a panel of cancer cell lines with good results especially on acute leukemia lines. Furthermore, haplamine seems to be less cytotoxic on non cancer cell line (JOHN fibroblasts line).
So, the in vitro cytotoxic properties of haplamine must be confirmed in vivo on a nude mice model.