Sanon S, Azas N, Gasquet M, Ollivier E, Mahiou V, Barro N, Cuzin-Ouattara N, Traore A S, Esposito F, Balansard G, Timon-David P
Laboratory of Pharmacology and Clinical Biochemistry of CRSBAN, UFR/SVT, University of Ouagadougou, Ouagadougou, Burkina Faso.
Parasitol Res. 2003 Jul;90(4):314-7. doi: 10.1007/s00436-003-0859-9. Epub 2003 Apr 4.
In the course of the search for new antimalarial compounds, a study of plants traditionally used against malaria in Burkina Faso was made. An ethnobotanical study permitted the identification of plants currently used by the traditional healers and herbalists. Two plants among them were selected for further study: Pavetta crassipes (K. Schum) and Acanthospermum hispidum (DC). Alkaloid extracts of these plants were tested in vitro against two reference clones of Plasmodium falciparum: the W2 chloroquine-resistant and the D6 chloroquine-sensitive strains. Significant inhibitory activity was observed with Pavetta crassipes (IC(50)=1.23 microg/ml) and A. hispidum (IC(50)=5.02 microg/ml). Antiplasmodial activity was also evaluated against six Plasmodium falciparum isolates from children between 4 and 10 years old. The IC(50) values for the alkaloid extracts were in the range 25-670 ng/ml. These results indicated that P. falciparum wild strains were more sensitive to the alkaloid extracts than strains maintained in continuous culture. Moreover, the alkaloid extracts exhibit good in vitro antimalarial activity and weak cytotoxicity against three human cell lines (THP1, normal melanocytes, HTB-66). Isolation and structural determination are now necessary in order to precisely determine the active compounds.
在寻找新型抗疟化合物的过程中,对布基纳法索传统上用于治疗疟疾的植物进行了一项研究。一项民族植物学研究使得能够识别传统治疗师和草药师目前使用的植物。从中挑选了两种植物进行进一步研究:厚叶巴夫木(Pavetta crassipes (K. Schum))和刺苞果(Acanthospermum hispidum (DC))。对这两种植物的生物碱提取物针对恶性疟原虫的两个参考克隆进行了体外测试:W2氯喹抗性株和D6氯喹敏感株。观察到厚叶巴夫木有显著的抑制活性(IC(50)=1.23微克/毫升),刺苞果的IC(50)=5.02微克/毫升。还针对4至10岁儿童的六种恶性疟原虫分离株评估了抗疟活性。生物碱提取物的IC(50)值在25 - 670纳克/毫升范围内。这些结果表明,恶性疟原虫野生株比连续培养的株系对生物碱提取物更敏感。此外,生物碱提取物在体外表现出良好的抗疟活性,并且对三种人类细胞系(THP1、正常黑素细胞、HTB - 66)具有较弱的细胞毒性。现在需要进行分离和结构测定以便精确确定活性化合物。