Antiparasitic activity of alkaloids from plant species of Papua New Guinea and Australia

作者：Fernandez Liza S; Sykes Melissa L; Andrews Katherine T; Avery Vicky M^*

来源：International Journal of Antimicrobial Agents, 2010, 36(3): 275-279.

DOI：10.1016/j.ijantimicag.2010.05.008

• Antimalarial
• Antitrypanosomal
• Alkaloid
• Plant
• Flindersia
• Stage specificity

New drugs are needed to help overcome the increasing problem of drug resistance in parasites that cause diseases such as malaria and trypanosomiasis. In this study, alkaloid compounds isolated from extracts of the plants Flindersia amboinensis, Stephania zippeliana and Voacanga papuana from Papua New Guinea and Flindersia acuminata from Australia were examined for their antiparasitic activity against Plasmodium falciparum strains and Trypanosoma brucei brucei as well as their cytotoxicity against the mammalian cell lines HEK 293 and HeLa. The most active compound, dimethylisoborreverine (DMIB), showed sub-micromolar activity, with 50% inhibitory concentration (IC(50)) values between 20nM and 810nM both against drug-sensitive and drug-resistant P. falciparum strains, along with moderate selectivity against T.b. brucei and mammalian cells. Stage specificity studies revealed that P. falciparum trophozoite-stage parasites were more susceptible to DMIB than ring- or schizont-stage parasites. DMIB-treated tropho-zoites showed changes in food vacuole morphology, with an apparent reduction in haemozoin formation that does not appear to be inhibited via the direct binding of haem. These findings suggest a potential for indole alkaloids from Flindersia spp. as new antiparasitic agents.

• 出版日期2010-9
• 单位河北医科大学