DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women’s Health
| Autor: | René F. Ramos Alvarenga, Martin Biendl, Guido F. Pauli, Judy L. Bolton, Shao-Nong Chen, Huali Dong, Dejan Nikolic, Richard B. van Breemen, Birgit M. Dietz |
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| Rok vydání: | 2022 |
| Předmět: |
0301 basic medicine
Humulus lupulus Pharmaceutical Science Phytoestrogens Pharmacology Article Analytical Chemistry 03 medical and health sciences chemistry.chemical_compound Drug Discovery Humans Humulus Uncategorized Flavonoids Propiophenones Postmenopausal women biology Molecular Structure Chemistry Extramural Organic Chemistry Estrogens biology.organism_classification 030104 developmental biology Complementary and alternative medicine Phytochemical Xanthohumol Dietary Supplements Flavanones Molecular Medicine Alkaline phosphatase Women's Health Female |
| Zdroj: | Journal of Natural Products |
| DOI: | 10.25417/uic.19723909 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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