Apigenin inhibits rat neurosteroidogenic 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase

[High_Prob]

Apigenin inhibits rat neurosteroidogenic 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase - PubMed

Apigenin, a common flavonoid, has extensive pharmacological activities. Apigenin inhibits some steroid biosynthetic enzymes, suggesting that it may block neurosteroid synthesis. Neurosteroids play many important roles in neurological functions. The objective of the present study is to...

pubmed.ncbi.nlm.nih.gov

Apigenin inhibits rat neurosteroidogenic 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase​

Abstract​

Apigenin, a common flavonoid, has extensive pharmacological activities. Apigenin inhibits some steroid biosynthetic enzymes, suggesting that it may block neurosteroid synthesis. Neurosteroids play many important roles in neurological functions. The objective of the present study is to investigate effects of apigenin on neurosteroidogenic enzymes, 5α-reductase 1 (SRD5A1), 3α-hydroxysteroid dehydrogenase (AKR1C9), and retinol dehydrogenase 2 (RoDH2), in rats. SRD5A1, AKR1C9, and RoDH2 were expressed in COS-1 cells and the effects of apigenin on these enzymes and modes of action were explored using radiolabeled substrates and thin-layer chromatographic separation coupled with radiometry. Apigenin inhibited SRD5A1, AKR1C9, and RoDH2 activities with IC50values of 100, 0.891 ± 0.065, and >100 μM, respectively. Apigenin competitively inhibited rat AKR1C9 when its substrate 5α-dihydrotestosterone was used and uncompetitively inhibited the enzyme when cofactor NADPH was used. In conclusion, apigenin is a potent inhibitor of rat AKR1C9, thereby controlling the rate of neurosteroid biosynthesis.

 

[PurpleHeart]

There are also studies where apigenin increased neurosteroids through other mechanisms, but my opinion is that humans and other omnivores/frugivores have just adapted to fruit toxins,
Fruits probably produce phytoestrogens to try and make whatever is eating them sterile, in an attempt to survive, but some animals spread the seeds in their feces so the trees that were not as toxic as to kill their predators had a better survival rate due to animals carrying the seeds in their intestines and by defecating they spread the tree, so I think that after a while the trees with the least toxic fruiting bodies where the ones that survived natural selection, I mean everyone loves fruits we adapted to eating them I think consuming them in reasonable amounts is healthy, just don't drink 3 liters of OJ a day and supplement apigenin alongside lol.

 

[lampofred]

that's not necessarily a bad thing. 5ar1 goes up to protect against estrogen/PUFA, so if estrogen is lowered then 5ar1 might go down because it's no longer needed. Apigenin is antiestrogenic so it might be reducing the need for 5ar1.

 

[golder]

Anyone know the important differences between naringenin and apigenin?