Inhibition of Aromatase by Hops, Licorice Species, and their bioactive compounds in Postmenopausal Breast Tissue
biorxiv(2022)
Abstract
Breast cancer risk continues to rise post menopause. Endocrine therapies are employed to prevent postmenopausal breast cancer in high-risk women. However, their adverse effects have reduced acceptability and overall success in cancer preventionatural products such as hops ( Humulus lupulus ) and pharmacopoeial licorice ( Glycyrrhiza ) species, which are used for managing menopausal symptoms, have demonstrated estrogenic and chemopreventive properties. Their beneficial effects on aromatase activity and expression as important factors in postmenopausal breast carcinogenesis are understudied. The presented data show that Gycyrrhiza inflata (GI) has the highest aromatase inhibition potency among these plants. Moreover, phytoestrogens such as 8-prenylnaringenin from hops as well as liquiritigenin and 8-prenylapigenin from licorice are shown to be potent bioactives, in line with computational docking studies. 8-Prenylnaringenin, GI extract, liquiritigenin, and licochalcone A all suppress aromatase expression in postmenopausal women’s breast tissue. Collectively, these data suggest that these natural products may have breast cancer prevention potential for high-risk postmenopausal women.
### Competing Interest Statement
The authors have declared no competing interest.
* AKR1C3
: Aldoketoreductase 1C3
AI
: Aromatase inhibitor
CYP
: Cytochrome P450
E2
: 17β-Estradiol
ER+
: Estrogen receptor positive
E1
: Estrone
Ex/Em
: Excitation/Emission
GG
: Glycyrrhiza glabra
GI
: Glycyrrhiza inflata
GU
: Glycyrrhiza uralensis
G6PDH
: Glucose-6-phosphate dehydrogenase
GST
: Glutathione-S-transferase
HBSS
: Hank’s balanced salt solution
HFC
: 7-Hydroxy-4-trifluoromethyl coumarin
IRB
: Institutional Review Board
IDT
: Integrated DNA Technologies
LigC
: Isoliquiritigenin
IX
: Isoxanthohumol
LicA
: Licochalcone A
LigF
: Liquiritigenin
MFC
: 7-methoxy-4-trifluoromethyl coumarin
NADPH
: Nicotineamide adenine dinucleotide phosphate
NQO1
: NADPH:quinone oxidoreductase 1
6-PN
: 6-prenylnaringenin
8-PA
: 8-prenylapigenin
8-PN
: 8-prenylnaringenin
PII
: Promoter II
PI.3
: promoter I.3
PI.4
: Promoter I.4
SERM
: Selective estrogen receptor modulators
XH
: Xanthohumol
MoreTranslated text
Key words
aromatase,bioactive compounds,licorice species
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