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Aromatase inhibitors isolated from a flowering tea, snow Chrysanthemum (the capitula of Coreopsis tinctoria Nutt.)
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Journal Article
Aromatase inhibitors isolated from a flowering tea, snow Chrysanthemum (the capitula of Coreopsis tinctoria Nutt.)
2023
Overview
Methanol extract from the capitula of
Coreopsis tinctoria
Nutt. (Asteraceae), which is also known as a flowering tea or blooming tea “Snow
Chrysanthemum
,” was found to inhibit the enzymatic activity of aromatase. A total of 24 known isolates (
1
–
24
) were identified from the extract, including three chalcones (
1
–
3
), an aurone (
4
), five flavanones (
5
–
9
), four flavanols (
10
–
13
), a flavonol (
14
), and two biflavanones (
15
,
16
). Among them, okanin (
1
,
K
i = 1.6 μM), (2
S
)-naringenin (
5
, 0.90 μM), isookanin (
6
, 0.81 μM), (2
S
)-7,3',5'-trihydroxyflavaone (
7
, 0.13 μM), and (2
S
)-5,7,3',5'-tetrahydroxyflavanone (
8
, 0.32 μM) exhibited relatively potent competitive inhibition. Specifically, the isolates
7
and
8
, having a common 3',5'-resorcinol moiety at the B ring in their flavanone skeleton, exhibited potent inhibitory activities compared to those of a clinically applied aminoglutethimide (0.84 μM) and naturally occurring flavone, chrysin (0.23 μM), which is a common non-steroidal aromatase inhibitor. Importantly, the active flavonoid constituents (
1
and
5
–
8
) did not inhibit the activity of 5
α
-reductase enzyme, which normally reacts with the same substrate “testosterone,” thus, these compounds were suggested to be specific to aromatase.
Publisher
Springer Nature Singapore,Springer Nature B.V
Subject
