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Estrogenic and antiandrogenic activities of methoxyflavans isolated from the fruit of Mauritia Flexuosa (Moriche Palm)
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2020-12-19 , DOI: 10.1111/jfbc.13583 Kenchi Miyasaka 1 , Shogo Takeda 1 , Seikou Nakamura 2 , Hisashi Matsuda 2 , Hiroshi Shimoda 1
Journal of Food Biochemistry ( IF 3.5 ) Pub Date : 2020-12-19 , DOI: 10.1111/jfbc.13583 Kenchi Miyasaka 1 , Shogo Takeda 1 , Seikou Nakamura 2 , Hisashi Matsuda 2 , Hiroshi Shimoda 1
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Moriche palm is consumed as both a fresh fruit and processed food in Peru and Brazil. Although its fruit contains phytoestrogens, the active compounds have not yet been identified. Therefore, we purified moriche palm extract (MPE) and identified compounds exhibiting estrogenic and antiandrogenic activities. Estrogenic activity was assessed by the estrogen‐dependent growth of MCF‐7 cells and increases in uterine weights in mice. Antiandrogenic activity was evaluated by 5α‐reductase inhibitory activity and prostate‐specific antigen (PSA) expression in LNCaP cells. In vivo antiestrogenic activity was also assessed based on testosterone‐induced prostate growth in castrated mice. Four methoxyflavans were isolated from MPE and all, except for 7,4′‐dihydroxy‐5‐methoxyflavan, promoted MCF‐7 cell growth, indicating estrogenic activity. Uterine and ovary weights increased in mice orally administered MPE (400 mg/kg) for 2 weeks. Regarding antiandrogenic activity, among the four methoxyflavans isolated, 6,7,4'‐trihydroxy‐5‐methoxyflavan (1 µg/ml) suppressed the mRNA and protein expression of PSA in LNCaP cells. Furthermore, prostate growth was suppressed in mice orally administered MPE (200 mg/kg) for 2 weeks. All methoxyflavans inhibited 5α‐reductase activity with IC50 less than 10 µg/ml. Collectively, the present results demonstrated that orally administered MPE exhibited estrogenic and antiandrogenic activities. Methoxyflavans, particularly 6,7,4′‐trihydroxy‐5‐methoxyflavan, appear to be the active compounds for these activities.
中文翻译：
从毛里塔尼亚（Mauritia Flexuosa）（Moriche Palm）果实中分离出的甲氧基黄酮的雌激素和抗雄激素活性
在秘鲁和巴西，莫里奇棕榈既可以作为新鲜水果也可以作为加工食品消费。尽管其果实含有植物雌激素，但尚未鉴定出活性化合物。因此，我们纯化了Moriche棕榈提取物（MPE），并鉴定了具有雌激素和抗雄激素活性的化合物。通过MCF-7细胞的雌激素依赖性生长以及小鼠子宫重量的增加来评估雌激素活性。通过LNCaP细胞中的5α-还原酶抑制活性和前列腺特异性抗原（PSA）表达来评估抗雄激素活性。体内还根据cast割小鼠睾丸激素诱导的前列腺生长评估了抗雌激素活性。从MPE中分离出了四个甲氧基黄酮，除7,4'-二羟基-5-甲氧基黄酮外，所有其他均促进MCF-7细胞生长，表明雌激素活性。口服MPE（400 mg / kg）2周的小鼠子宫和卵巢重量增加。关于抗雄激素活性，在分离出的四个甲氧基黄酮中，有6,7,4'-三羟基-5-甲氧基黄酮（1 µg / ml）抑制LNCaP细胞中PSA的mRNA和蛋白表达。此外，口服MPE（200 mg / kg）2周的小鼠前列腺生长受到抑制。所有甲氧基黄酮均通过IC 50抑制5α-还原酶活性低于10 µg / ml。总体而言，本结果表明口服MPE表现出雌激素和抗雄激素活性。甲氧基黄酮，尤其是6,7,4'-三羟基-5-甲氧基黄酮，似乎是这些活性的活性化合物。
更新日期：2021-01-19
中文翻译：
从毛里塔尼亚（Mauritia Flexuosa）（Moriche Palm）果实中分离出的甲氧基黄酮的雌激素和抗雄激素活性
在秘鲁和巴西，莫里奇棕榈既可以作为新鲜水果也可以作为加工食品消费。尽管其果实含有植物雌激素，但尚未鉴定出活性化合物。因此，我们纯化了Moriche棕榈提取物（MPE），并鉴定了具有雌激素和抗雄激素活性的化合物。通过MCF-7细胞的雌激素依赖性生长以及小鼠子宫重量的增加来评估雌激素活性。通过LNCaP细胞中的5α-还原酶抑制活性和前列腺特异性抗原（PSA）表达来评估抗雄激素活性。体内还根据cast割小鼠睾丸激素诱导的前列腺生长评估了抗雌激素活性。从MPE中分离出了四个甲氧基黄酮，除7,4'-二羟基-5-甲氧基黄酮外，所有其他均促进MCF-7细胞生长，表明雌激素活性。口服MPE（400 mg / kg）2周的小鼠子宫和卵巢重量增加。关于抗雄激素活性，在分离出的四个甲氧基黄酮中，有6,7,4'-三羟基-5-甲氧基黄酮（1 µg / ml）抑制LNCaP细胞中PSA的mRNA和蛋白表达。此外，口服MPE（200 mg / kg）2周的小鼠前列腺生长受到抑制。所有甲氧基黄酮均通过IC 50抑制5α-还原酶活性低于10 µg / ml。总体而言，本结果表明口服MPE表现出雌激素和抗雄激素活性。甲氧基黄酮，尤其是6,7,4'-三羟基-5-甲氧基黄酮，似乎是这些活性的活性化合物。
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