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来自阔叶辛托木茎皮的抗疟4-苯基香豆素。

Antimalarial 4-phenylcoumarins from the stem bark of Hintonia latiflora.

作者信息

Argotte-Ramos Rocío, Ramírez-Avila Guillermo, Rodríguez-Gutiérrez María del Carmen, Ovilla-Muñoz Marbella, Lanz-Mendoza Humberto, Rodríguez Mario H, Gonzalez-Cortazar Manasés, Alvarez Laura

机构信息

Instituto Nacional de Salud Pública, Centro de Investigación sobre Enfermedades Infecciosas, Enfermedades Transmitidas por Vector, Departamento de Entomología Médica, Avenida Universidad 655, Cuernavaca, Morelos, México.

出版信息

J Nat Prod. 2006 Oct;69(10):1442-4. doi: 10.1021/np060233p.

DOI:10.1021/np060233p
PMID:17067158
Abstract

The EtOAc extract of the stem bark of Hintonia latiflora showed the suppression of total parasitemia and the chemosuppression of schizont numbers, when tested in vivo against Plasmodium berghei infection in mice. Bioassay-directed fractionation of the EtOAc extract, using the in vitro 16 h and the in vivo 4-day suppression tests on P. berghei schizont numbers, led to the isolation of the new compound 5-O-beta-D-glucopyranosyl-7,4'-dimethoxy-3'-hydroxy-4-phenylcoumarin (1), along with the known 5-O-beta-D-glucopyranosyl-7-methoxy-3',4'-dihydroxy-4-phenylcoumarin (2). The structure of compound 1 was established on the basis of spectroscopic data interpretation. Compounds 1 and 2 suppressed the development of P. berghei schizonts in vitro with IC50 values of 24.7 and 25.9 microM, respectively. Compound 2 suppressed the development of schizonts at the dose of 40 mg/kg by 70.8% in the in vivo assay.

摘要

阔叶欣托木茎皮的乙酸乙酯提取物在针对小鼠伯氏疟原虫感染进行体内测试时,显示出对总疟原虫血症的抑制作用以及对裂殖体数量的化学抑制作用。使用针对伯氏疟原虫裂殖体数量的体外16小时和体内4天抑制试验,对乙酸乙酯提取物进行生物测定导向的分级分离,得到了新化合物5-O-β-D-吡喃葡萄糖基-7,4'-二甲氧基-3'-羟基-4-苯基香豆素(1),以及已知的5-O-β-D-吡喃葡萄糖基-7-甲氧基-3',4'-二羟基-4-苯基香豆素(2)。化合物1的结构是根据光谱数据解释确定的。化合物1和2在体外抑制伯氏疟原虫裂殖体的发育,IC50值分别为24.7和25.9 microM。在体内试验中,化合物2以40 mg/kg的剂量抑制裂殖体发育70.8%。

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