KMID : 0606920140220040347
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Biomolecules & Therapeutics 2014 Volume.22 No. 4 p.347 ~ p.354
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Selective Estrogen Receptor Modulation by Larrea nitida on MCF-7 Cell Proliferation and Immature Rat Uterus
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Ahn Hye-Na
Jeong Si-Yeon Bae Gyu-Un Chang Min-Sun Zhang Dongwei Liu Xiyuan Pei Yihua Chin Young-Won Lee Joong-Ku Oh Sei-Ryang Song Yun-Seon
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Abstract
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Larrea nitida is a plant that belongs to the Zygophyllaceae family and is widely used in South America to treat inflammatory diseases, tumors and menstrual pain. However, its pharmacological activity remains unclear. In this study we evaluated the property of selective estrogen receptor modulator (SERM) of Larrea nitida extracts (LNE) as a phytoestrogen that can mimic, modulate or disrupt the actions of endogenous estrogens, depending on the tissue and relative amount of other SERMs. To investigate the property of SERM of LNE, we performed MCF-7 cell proliferation assays, estrogen response element (ERE)-luciferase reporter gene assay, human estrogen receptor (hER) binding assays and in vivo uterotrophic assay. To gain insight into the active principles, we performed a bioassay-guided analysis of LNE employing solvents of various polarities and using classical column chromatography, which yielded 16 fractions (LNs). LNE showed high binding affinities for hER¥á and hER¥â with IC50 values of 1.20 ¡¿10?7 g/ml and 1.00¡¿10?7 g/ml, respectively. LNE induced 17¥â-estradiol (E2)-induced MCF-7 cell proliferation, however, it reduced the proliferation in the presence of E2. Furthermore, LNE had an atrophic effect in the uterus of immature rats through reducing the expression level of progesterone receptor (PR) proteins. LN08 and LN10 had more potent affinities for binding on hER ¥á and ¥â than other fractions. Our results indicate that LNE had higher binding affinities for hER¥â than hER¥á, and showed SERM properties in MCF-7 breast cancer cells and the rat uterus. LNE may be useful for the treatment of estrogen-related conditions, such as female cancers and menopause.
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KEYWORD
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Larrea nitida, Lignan, Phytoestrogen, Estrogen receptor, MCF-7 cell, Uterus
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