Zingue Stéphane, Michel Thomas, Nde Chantal Beatrice Magne, Njuh Amstrong Nang, Cisilotto Julia, Ndinteh Derek Tantoh, Clyne Colin, Fernandez Xavier, Creczynski-Pasa Tânia Beatriz, Njamen Dieudonné
Department of Life and Earth Sciences, Higher Teachers' Training College, University of Maroua, P.O. Box 55, Maroua, Cameroon.
Department of Pharmaceutical Sciences, Health Sciences Centre, Federal University of Santa Catarina, CEP, Florianópolis, Santa Catarina, 88040-900, Brazil.
BMC Complement Altern Med. 2017 Aug 2;17(1):383. doi: 10.1186/s12906-017-1895-9.
Ficus umbellata is a medicinal plant previously shown to endow estrogenic properties. Its major component was isolated and characterized as 7-methoxycoumarin (MC). Noteworthy, coumarins and the respective active metabolite 7-hydroxycoumarin analogs have shown aromatase inhibitory activity, which is of particular interest in the treatment of estrogen-dependent cancers. The present work aimed at evaluating the estrogenic/antiestrogenic effects of MC in vitro and in vivo.
To do so, in vitro assays using E-screen and reporter gene were done. In vivo, a 3-day uterotrophic assay followed by a postmenopausal-like rat model to characterize MC as well as F. umbellata aqueous extract in ovariectomized Wistar rats was performed. The investigations focused on histological (vaginal and uterine epithelial height) and morphological (uterine wet weight, vagina stratification and cornification) endpoints, bone mass, biochemical parameters and lipid profile.
MC induced a significant (p < 0.05) MCF-7 cell proliferation at a concentration of 0.1 μM, but did not inhibit the effect induced by estradiol in both E-screen and reporter gene assays. In vivo, MC treatment did not show an uterotrophic effect in both rat models used. However, MC (1 mg/kg) induced a significant increase (p < 0.01) of vaginal epithelial height. No significant change was observed with MC in abdominal fat weight, serum lipid levels and bone weight.
These results suggest that MC has a weak estrogenic activity in vitro and in vivo that accounts only in part to the estrogenicity of the whole plant extract. MC could be beneficial with regard to vagina dryness as it showed a tissue specific effect without exposing the uterus to a potential tumorigenic growth.
伞花榕是一种药用植物，先前已证明其具有雌激素特性。其主要成分被分离并鉴定为7-甲氧基香豆素（MC）。值得注意的是，香豆素及其相应的活性代谢物7-羟基香豆素类似物已显示出芳香酶抑制活性，这在雌激素依赖性癌症的治疗中尤为重要。本研究旨在评估MC在体外和体内的雌激素/抗雌激素作用。
为此，进行了使用E-筛选和报告基因的体外试验。在体内，进行了为期3天的子宫增重试验，随后采用绝经后样大鼠模型，以表征去卵巢Wistar大鼠体内的MC以及伞花榕水提取物。研究重点在于组织学（阴道和子宫上皮高度）和形态学（子宫湿重、阴道分层和角质化）终点、骨量、生化参数和血脂谱。
在浓度为0.1μM时，MC诱导MCF-7细胞显著（p < 0.05）增殖，但在E-筛选和报告基因试验中均未抑制雌二醇诱导的作用。在体内，MC处理在两种使用的大鼠模型中均未显示出子宫增重作用。然而，MC（1mg/kg）诱导阴道上皮高度显著增加（p < 0.01）。MC对腹部脂肪重量、血清脂质水平和骨重量无显著影响。
这些结果表明，MC在体外和体内具有较弱的雌激素活性，这仅部分解释了全植物提取物的雌激素性。MC可能对阴道干燥有益，因为它显示出组织特异性作用，而不会使子宫暴露于潜在的致瘤生长风险。
