Pregnenediones

Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Guggulsterone is the active ingredient in gugulipid, an organic extract of the Commiphora mukul plant. Gugulipid has been used for nearly 3000 years in Ayurvedic medicine, mainly as a treatment for arthritis. Herbal practitioners currently use gugulipid therapy in conditions as diverse as rheumatism, coronary artery disease, arthritis, hyperlipidemia, acne, and obesity. The active ingredient in gugulipid is guggulsterone, a plant sterol compound recently identified as a pregnane X receptor (PXR; NR1I2) ligand.

Author(s): 
Ding, Xunshan
Staudinger, Jeff L.
Publication Title: 
Molecular Cancer Therapeutics

The present study was undertaken to gain insights into the molecular mechanism of cell death (apoptosis) by guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, using PC-3 human prostate cancer cells as a model. The viability of PC-3 cells, but not a normal prostate epithelial cell line (PrEC), was reduced significantly on treatment with guggulsterone in a concentration-dependent manner.

Author(s): 
Singh, Shivendra V.
Zeng, Yan
Xiao, Dong
Vogel, Victor G.
Nelson, Joel B.
Dhir, Rajiv
Tripathi, Yamini B.
Publication Title: 
Cancer Research

Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, causes apoptosis in cancer cells but the sequence of events leading to cell death is poorly understood. We now show that guggulsterone-induced cell death in human prostate cancer cells is caused by reactive oxygen intermediate (ROI)-dependent activation of c-Jun NH(2)-terminal kinase (JNK).

Author(s): 
Singh, Shivendra V.
Choi, Sunga
Zeng, Yan
Hahm, Eun-Ryeong
Xiao, Dong
Publication Title: 
Molecular Cancer Therapeutics

Our previous studies have shown that z-guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. We now report a novel response to z-guggulsterone involving the inhibition of angiogenesis in vitro and in vivo. The z-guggulsterone treatment inhibited capillary-like tube formation (in vitro neovascularization) by human umbilical vein endothelial cells (HUVEC) and migration by HUVEC and DU145 human prostate cancer cells in a concentration- and time-dependent manner.

Author(s): 
Xiao, Dong
Singh, Shivendra V.
Publication Title: 
Carcinogenesis

Guggulsterone (GUG), a resin of the Commiphora mukul tree, has been used in ayurvedic medicine for centuries to treat a variety of ailments. Recent studies have suggested that GUG may also possess anticancer effects. In the present study, we show that GUG possesses antitumor-promoting effects in SENCAR mouse skin tumorigenesis model. We first determined the effect of topical application of GUG to mice against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced conventional markers and other novel markers of skin tumor promotion.

Author(s): 
Sarfaraz, Sami
Siddiqui, Imtiaz A.
Syed, Deeba N.
Afaq, Farrukh
Mukhtar, Hasan
Publication Title: 
BMC complementary and alternative medicine

BACKGROUND: z-Guggulsterone (z-Gug) and Gugulipid (GL) have been used to treat a variety of ailments. We now report their anti-cancer effect and mechanism against human breast cancer. METHODS: Using the human estrogen receptor-positive (MCF-7) and triple-negative (MDA-MB-231) breast cancer cells as well as the normal human mammary epithelial cell line (HMEC), we evaluated the anti-breast-cancer efficacy and apoptosis inducing activity of GL. We determined the cellular and molecular mechanism of GL-inhibited breast cancer cell growth.

Author(s): 
Jiang, Guoqin
Xiao, Xiao
Zeng, Yan
Nagabhushanam, Kalyanam
Majeed, Muhammed
Xiao, Dong
Publication Title: 
Journal of Chromatography. B, Biomedical Sciences and Applications

Simultaneous separation of E- and Z-guggulsterone, which is the main ingredient of 'Guggulip', an ayurvedic drug, was accomplished by HPLC on a C18 column using methanol, acetonitrile, buffer and tetrahydrofuran as a mobile phase. The compounds were monitored at 248 nm on a photodiode array detector. The assay method was used for the simultaneous determination of stereoisomers (E and Z) of guggulsterone in spiked serum and dosed (50 mg/kg, p.o.) rats. The recoveries of E- and Z-isomers from serum samples were always greater than 90%.

Author(s): 
Verma, N.
Singh, S. K.
Gupta, R. C.
Publication Title: 
Molecular Endocrinology (Baltimore, Md.)

Ayurveda, the ancient Indian system of health care and medicine, has a well-organized materia medica in which plants form a dominant part. A key illustration of the exploitation of this knowledge toward the development of a modern drug is the isolation and characterization of two antihyperlipidemic compounds, Z-, and E-guggulsterone from the tree Commiphora mukul, the exudate of which has been traditionally used for mitigating lipid disorders.

Author(s): 
Wu, Jun
Xia, Chunsheng
Meier, Jannika
Li, Suzhen
Hu, Xiao
Lala, Deepak S.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

Guggulsterone is the active ingredient in gugulipid, an organic extract of the Commiphora mukul plant. Gugulipid has been used for nearly 3000 years in Ayurvedic medicine, mainly as a treatment for arthritis. Herbal practitioners currently use gugulipid therapy in conditions as diverse as rheumatism, coronary artery disease, arthritis, hyperlipidemia, acne, and obesity. The active ingredient in gugulipid is guggulsterone, a plant sterol compound recently identified as a pregnane X receptor (PXR; NR1I2) ligand.

Author(s): 
Ding, Xunshan
Staudinger, Jeff L.
Publication Title: 
Molecular Cancer Therapeutics

The present study was undertaken to gain insights into the molecular mechanism of cell death (apoptosis) by guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, using PC-3 human prostate cancer cells as a model. The viability of PC-3 cells, but not a normal prostate epithelial cell line (PrEC), was reduced significantly on treatment with guggulsterone in a concentration-dependent manner.

Author(s): 
Singh, Shivendra V.
Zeng, Yan
Xiao, Dong
Vogel, Victor G.
Nelson, Joel B.
Dhir, Rajiv
Tripathi, Yamini B.

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