Effect of essential oils, such as raspberry ketone and its derivatives, on antiandrogenic activity based on in vitro reporter gene assay.
The effect of essential oils, such as raspberry ketone, on androgen (AR) receptor was investigated using a MDA-kb2 human breast cancer cell line for predicting potential AR activity. Among them, eugenol had the highest AR antagonistic activity with its IC(50) value of 19 microM. Raspberry ketone, which has threefold higher anti-obese activity than that of capsaicin, also had AR antagonist activity with its IC(50) value of 252 microM. Based on these findings, a more precise CoMFA model was proposed as follows: pIC(50) [log (1/IC(50))]=3.77+[CoMFA field terms] (n=39, s=0.249, r(2)=0.834, s(cv)=0.507, q(2)=0.311 (three components).
Ogawa
Yoshihisa
Y
Department of Environmental Bioscience, Meijo University, Nagoya 468-8502, Japan.
Akamatsu
Miki
M
Hotta
Yudai
Y
Hosoda
Akifumi
A
Tamura
Hiroto
H
D000726:Androgen Antagonists / Q000737:chemistry / Q000494:pharmacology*; D059002:Androgen Receptor Antagonists; D002074:Butanones / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D017930:Genes, Reporter; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D009822:Oils, Volatile / Q000737:chemistry / Q000494:pharmacology*; D011485:Protein Binding; D011944:Receptors, Androgen / Q000737:chemistry / Q000378:metabolism*
C410798:AR protein, human; D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D002074:Butanones; D009822:Oils, Volatile; D011944:Receptors, Androgen; C035522:raspberry ketone