来自米勒植物的抗原生动物成分，米勒是一种用于墨西哥传统医学治疗腹泻和痢疾的植物。
Antiprotozoal Constituents from Miller, a Plant Used in Mexican Traditional Medicine for the Treatment of Diarrhea and Dysentery.
作者信息
Calzada Fernando, Correa-Basurto Jose, Barbosa Elizabeth, Mendez-Luna David, Yepez-Mulia Lilian
机构信息
Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades-2 piso CORCE Centro Médico Nacional Siglo XXI, IMSS, Av. Cuauhtemoc 330, Col. Doctores, México, D. F.
Sección de Graduados y Departamento de Bioquímica, Escuela Superior de Medicina, Instituto Politécnico Nacional, Plan de San Luís y DíazMirón, México, D. F.
出版信息
Pharmacogn Mag. 2017 Jan-Mar;13(49):148-152. doi: 10.4103/0973-1296.197636.
BACKGROUND
Miller (Annonaceae) is a medicinal plant frequently recommended in Mexican traditional medicine for the treatment of gastrointestinal disorders such as diarrhea and dysentery.
OBJECTIVE
This work was undertaken to obtain information that support the traditional use of , on pharmacological basis using and computational experiments.
MATERIAL AND METHODS
Bioassay-guided fractionation of the ethanol extract of the leaves of afforded five phenolic compounds: caffeic acid, quercetin, kaempferol, nicotinflorin, and rutin.
RESULTS
The antiprotozoal assay showed that kaempferol was the most potent antiamoebic and antigiardial compound with IC values of 7.9 μg/mL for and 8.7 μg/mL for . Computational molecular docking study showed that kaempferol interacted in a region different than metronidazole in the enzyme pyruvate: ferredoxin oxidoreductase (PFOR).
CONCLUSION
Considering that PFOR is a target of metronidazole; kaempferol may be a lead compound for the development of novel antiprotozoal agent. Also, these findings give support to the use of in the traditional medicine from México for the treatment of diarrhea and dysentery.
SUMMARY
Bioassay-guided fractionation of the ethanol extract of the leaves of afforded five phenolic compounds: caffeic acid, quercetin, kaempferol, nicotinflorin and rutin. The antiprotozoal assay showed that kaempferol was the most potent antiamoebic and antigiardial compound with IC50 values of 7.9 μg/mL for and 8.7 μg/mL for . Computational molecular docking study showed that kaempferol interacted in a region different that metronidazole in the enzyme pyruvate: ferredoxin oxidoreductase. PFOR:Pyruvate:ferredoxin oxidoreductase, , .
背景
番荔枝科的米勒木是一种药用植物，在墨西哥传统医学中常用于治疗腹泻和痢疾等胃肠道疾病。
目的
本研究旨在通过药理学和计算实验获取支持米勒木传统药用的信息。
材料与方法
对米勒木叶乙醇提取物进行生物测定导向分离，得到了五种酚类化合物：咖啡酸、槲皮素、山奈酚、芦丁和芸香苷。
结果
抗寄生虫试验表明，山奈酚是最有效的抗阿米巴和抗贾第虫化合物，对溶组织内阿米巴的IC50值为7.9μg/mL，对贾第虫的IC50值为8.7μg/mL。计算分子对接研究表明，山奈酚在丙酮酸：铁氧还蛋白氧化还原酶（PFOR）中与甲硝唑作用区域不同。
结论
鉴于PFOR是甲硝唑的靶点，山奈酚可能是开发新型抗寄生虫药物的先导化合物。此外，这些发现支持了墨西哥传统医学中使用米勒木治疗腹泻和痢疾的做法。
总结
对米勒木叶乙醇提取物进行生物测定导向分离，得到了五种酚类化合物：咖啡酸、槲皮素、山奈酚、芦丁和芸香苷。抗寄生虫试验表明，山奈酚是最有效的抗阿米巴和抗贾第虫化合物，对溶组织内阿米巴的IC50值为7.9μg/mL，对贾第虫的IC50值为8.7μg/mL。计算分子对接研究表明，山奈酚在丙酮酸：铁氧还蛋白氧化还原酶中与甲硝唑作用区域不同。PFOR：丙酮酸：铁氧还蛋白氧化还原酶，溶组织内阿米巴，贾第虫。
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