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Molecules 2014, 19(11), 18690-18704;

The Antiosteoporotic Activity of Central-Icaritin (CIT) on Bone Metabolism of Ovariectomized Rats

Affiliated Hospital on Integration of Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210023, Jiangsu Province, China
Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, 100# Shizi Road, Nanjing 210028, Jiangsu Province, China
Author to whom correspondence should be addressed.
Received: 22 September 2014 / Revised: 23 October 2014 / Accepted: 29 October 2014 / Published: 14 November 2014
(This article belongs to the Collection Bioactive Compounds)
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Central-icaritin (CIT) is a flavonoid aglycone first discovered in our laboratory, which is an isomeric aglycone of icaritin (IT). We wanted to know whether CIT also had anti-osteoporosis activity. In this study, CIT was investigated in an ovariectomized rat (OVX) model. Fifty-six 6-month old female Sprague-Dawley rats were randomly assigned to sham operated group (Sham) and six OVX subgroups (n = 8 each). The OVX rats were then subdivided into six groups treated with vehicle (OVX), icaritin (IT, 40 mg/kg body weight/day), estradiol valerate (EV, 100 μg/kg body weight/day) or CIT (10, 20, and 40 mg/kg body weight/day) for 12 weeks, respectively. Then, the serum biochemical parameters, bone mineral density (BMD), bone biomechanical properties, bone microarchitecture, bone immunohistochemistry and related protein and gene expressions were evaluated. In OVX rats, the increases of body weight, HOP, AKP, and TRACP5b levels, and the decreases of uterus wet weight, femurs weight, BMD, serum OPG/RANKL and OCN were significantly inhibited by CIT treatment. Micro-CT analysis results showed that CIT apparently enhanced trabecular bone compared with the OVX group (p < 0.05). Total femur BMD and biomechanical strength of tibia were significantly improved (p < 0.05) after 12 weeks of CIT administration. In addition, the CIT administration also significantly enhanced the OPG expression, whereas reduced the RANKL expression in femurs according to RT-PCR, western blot assays and immunohistochemical evaluation. CIT had the antiosteoporotic activity, and its antiosteoporotic effects in OVX rats may be stronger than that of IT. View Full-Text
Keywords: central-icaritin (CIT); antiosteoporotic activity; ovariectomized rats central-icaritin (CIT); antiosteoporotic activity; ovariectomized rats

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Jiang, J.; Li, J.; Jia, X. The Antiosteoporotic Activity of Central-Icaritin (CIT) on Bone Metabolism of Ovariectomized Rats. Molecules 2014, 19, 18690-18704.

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