PLANTS AS SOURCES OF ANTIMALARIAL-DRUGS .7. ACTIVITY OF SOME SPECIES OF MELIACEAE PLANTS AND THEIR CONSTITUENT LIMONOIDS
PLANTS AS SOURCES OF ANTIMALARIAL-DRUGS .7. ACTIVITY OF SOME SPECIES OF MELIACEAE PLANTS AND THEIR CONSTITUENT LIMONOIDS
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DOI：
10.1002/ptr.2650040108
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发表时间：
1990-02-01
影响因子：
7.2
通讯作者：
PHILLIPSON, JD
中科院分区：
文献类型：
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作者：
BRAY, DH;WARHURST, DC;PHILLIPSON, JD
传统上用作退热药的三种楝科植物（印楝、雪松、番石榴）的粗提取物，以及从楝科植物中提取的 27 种柠檬苦素，评估了它们对恶性疟原虫氯喹耐药 K1 菌株的体外抗疟活性。测试的提取物均未表现出高抗疟原虫活性，并且仅发现五种化合物具有中等活性（IC50值：0.72–3.11 μ/mL）。最活跃的柠檬苦素类药物葛杜宁 (gedunin) 具有较低的体外细胞毒性，但不抑制 P. berghei 在小鼠中进行的 4 天测试（剂量为 90 mg/kg/天，皮下和腹腔注射，未观察到毒性）。楝科植物可能无法仅仅通过直接对抗疟疾寄生虫来发挥其活性，患者声称的有益治疗效果可能是由于最近描述的这些植物的抗炎和免疫调节活性。
Crude extracts of three species of the Meliaceae family used traditionally as febrifuges (Azadirachta indica, Cedrela odorata, Guarea multiflora), together with 27 limonoids extracted from the meliaceous plants were evaluated for theirin vitroantimalarial activity against chloroquine resistant K1 strain ofPlasmodium falciparum. None of the extracts tested showed high antiplasmodial activity and only five compounds were found to be moderately active (IC50values: 0.72–3.11 μ/mL). The most active limonoid, gedunin, of lowin vitrocytotoxicity did not inhibitP. bergheiin a 4 day test in mice (at the dose of 90 mg/kg/day, s.c. and i.p., no toxicity observed). Meliaceous plants may not exert their activity solely via direct action against malaria parasites, and the beneficial therapeutic effects claimed by patients might be due to the antiinnflammatory and immunomodulating activities recently described for these plants.