np7b00284_si_001.pdf (268 kB)
DESIGNER Extracts as Tools to Balance Estrogenic and Chemopreventive Activities of Botanicals for Women’s Health
journal contribution
posted on 2017-08-16, 13:21 authored by Birgit
M. Dietz, Shao-Nong Chen, René F.
Ramos Alvarenga, Huali Dong, Dejan Nikolić, Martin Biendl, Richard B. van Breemen, Judy L. Bolton, Guido F. PauliBotanical 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.
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Keywords
NADestrogenicityNQO 1 inductionestrogenicchemopreventive propertiesmenopausal symptom managementbioactive compoundsadsorbent-free countercurrent separation8- PN levelsuniform standardization requirementsBotanicalXH concentrationscytotoxicbalance 8- PNDESIGNER8- PNchemopreventive constituent xanthohumolXH levelsHumulus lupulus extractspostmenopausal
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