27-Hydroxycholesterol

27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Signaling Pathways >> Metabolic Enzyme/Protease >> LXR

Research Areas >> Cancer

Natural Products >> Others

Human Endogenous Metabolite

27-Hydroxycholesterol is an endogenous selective estrogen receptor modulator that displays significant partial agonist activity in a variety of cellular models of estrogen receptor action. It positively regulates both gene transcription and cell proliferation in cellular models of breast cancer[1]. 27-Hydroxycholesterol, through estrogen receptor activation, triggers deleterious effect in prostate cancer cell lines. 27-Hydroxycholesterol significantly increases cell proliferation of LNCaP and PC3 cells and this effect can be attenuated by estrogen receptor inhibitors[2]. 27-Hydroxycholesterol is an oxysterol produced from cholesterol by the monooxygenase CYP27A1, which regulates intracellular cholesterol homeostasis. 27-Hydroxycholesterol also acts as an endogenous selective estrogen receptor modulator capable of increasing breast cancer growth and metastasis. 27-Hydroxycholesterol levels can be modulated by statins or direct inhibition of CYP27A1, thereby attenuating its pro-tumorigenic activities[3]. 27-hydroxylation of cholesterol is an important pathway for LXR activation in response to cholesterol overload[4].

Stock solutions of 27-Hydroxycholesterol are prepared in 100% ethanol and stored at −80°C. 27-Hydroxycholesterol stock solution is dissolved in appropriate volumes of media to prepare the working solutions of 1 μM.

Proliferation assays are conducted on black 96 well plates using a commercial kit which quantifies cell number using DNA content and membrane integrity. LNCaP and PC3 cells are treated with 1 µM 27-Hydroxycholesterol for 48 hours[2].

[1]. DuSell CD, et al. 27-hydroxycholesterol is an endogenous selective estrogen receptor modulator. Mol Endocrinol. 2008 Jan;22(1):65-77.

[2]. Raza S, et al. The cholesterol metabolite 27-hydroxycholesterol stimulates cell proliferation via ERβ in prostate cancer cells. Cancer Cell Int. 2017 May 11;17:52.

[3]. Kimbung S, et al. Impact of 27-hydroxylase (CYP27A1) and 27-hydroxycholesterol in breast cancer. Endocr Relat Cancer. 2017 Jul;24(7):339-349.

[4]. Fu X, et al. 27-hydroxycholesterol is an endogenous ligand for liver X receptor in cholesterol-loaded cells. J Biol Chem. 2001 Oct 19;276(42):38378-87.

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