DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women’s Health,Journal of Natural Products

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DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women’s Health
Journal of Natural Products ( IF 3.3 ) Pub Date : 2017-08-16 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00284
Birgit M Dietz , Shao-Nong Chen , René F Ramos Alvarenga , Huali Dong , Dejan Nikolić , Martin Biendl ₁ , Richard B van Breemen , Judy L Bolton , Guido F Pauli

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Botanical dietary supplements contain multiple bioactive compounds that target numerous biological pathways. The lack of uniform standardization requirements is one reason that inconsistent clinical effects are reported frequently. The multifaceted biological interactions of active principles can be disentangled by a coupled pharmacological/phytochemical approach using specialized (“knock-out”) extracts. This is demonstrated for hops, a botanical for menopausal symptom management. Employing targeted, adsorbent-free countercurrent separation, Humulus lupulus extracts were designed for pre- and postmenopausal women by containing various amounts of the phytoestrogen 8-prenylnaringenin (8-PN) and the chemopreventive constituent xanthohumol (XH). Analysis of their estrogenic (alkaline phosphatase), chemopreventive (NAD(P)H-quinone oxidoreductase 1 [NQO1]), and cytotoxic bioactivities revealed that the estrogenicity of hops is a function of 8-PN, whereas their NQO1 induction and cytotoxic properties depend on XH levels. Antagonization of the estrogenicity of 8-PN by elevated XH concentrations provided evidence for the interdependence of the biological effects. A designed postmenopausal hop extract was prepared to balance 8-PN and XH levels for both estrogenic and chemopreventive properties. An extract designed for premenopausal women contains reduced 8-PN levels and high XH concentrations to minimize estrogenic while retaining chemopreventive properties. This study demonstrates the feasibility of modulating the concentrations of bioactive compounds in botanical extracts for potentially improved efficacy and safety.

中文翻译：

DESIGNER 提取物作为平衡植物性雌激素和化学预防活性的工具，促进女性健康

植物膳食补充剂含有多种针对多种生物途径的生物活性化合物。缺乏统一的标准化要求是经常报告不一致的临床效果的原因之一。活性成分的多方面生物相互作用可以通过使用专门的（“敲除”）提取物的药理学/植物化学耦合方法来解开。啤酒花（一种治疗更年期症状的植物药）就证明了这一点。采用有针对性的无吸附剂逆流分离，蛇麻草提取物专为绝经前和绝经后女性而设计，含有不同含量的植物雌激素 8-异戊二烯柚皮素 (8-PN) 和化学预防成分黄腐酚 (XH)。对它们的雌激素（碱性磷酸酶）、化学预防（NAD(P)H-醌氧化还原酶 1 [NQO1]）和细胞毒性生物活性的分析表明，啤酒花的雌激素性是 8-PN 的函数，而它们的 NQO1 诱导和细胞毒性特性取决于在 XH 水平上。升高 XH 浓度对 8-PN 雌激素作用的拮抗作用为生物效应的相互依赖性提供了证据。设计了一种绝经后啤酒花提取物，以平衡 8-PN 和 XH 水平，从而实现雌激素和化学预防特性。专为绝经前女性设计的提取物含有降低的 8-PN 水平和高 XH 浓度，可最大限度地减少雌激素，同时保留化学预防特性。这项研究证明了调节植物提取物中生物活性化合物的浓度以潜在提高功效和安全性的可行性。

更新日期：2017-08-16

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