生物活性

• 描述Estradiol Benzoate (β-Estradiol 3-benzoate), a prodrug of estradiol, acts as a steroid sex hormone. Diacerein (50mg/kg/day) was given orally to rats for 4 weeks in the presence or absence of cervical hyperkeratosis induced by intramuscular injection of Estradiol benzoate (60μg/100g) 3 times per week for 4 weeks. Estradiol benzoate succeeded to induce cervical hyperkeratosis which was detected by typical histopathological changes. In addition; there was significant reduction in superoxide dismutase levels and caspase-3 immunoexpression but significant increase in serum total cholesterol, malondialdehyde, total nitrites and interleukin-1b immunoexpression^[2]. Administration of estradiol benzoate 1 week before cabergoline improved induction and synchronization of estrus in dogs^[3]. In comparison with the controls, the mice treated with estradiol benzoate showed significantly decreased testicular indexes, no sperm in the sperm suspension or epididymal tubes, remarkably reduced numbers of spermatogonia, primary spermatocytes and Sertoli cells, down-regulated expression of PCNA and mRNA expressions of CyclinA1, CyclinB1, PCNA and VASA in the seminiferous tubules, but a dose-dependent increase of the p53 level^[4]. Estradiol benzoate protective effect against MPP+ neurotoxicity is related to antioxidant effect of PON2 (paraoxonase-2), pro-inflammatory cytokines and GSHR but not to SOD2, catalase, GPX1 or GPX4^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00650442	Healthy	Phase 1	Completed	-	United States, West Virginia ... more >> Kendle International Inc. Morgantown, West Virginia, United States, 26505 Collapse <<
  NCT02670785	Vulvovaginal Atrophy ... more >> Menopause Dyspareunia Collapse <<	Phase 2	Completed	-	United States, Arizona ... more >> Visions Clinical Research-Tucson Tucson, Arizona, United States, 85712 United States, California Genesis Center for Clinical Research San Diego, California, United States, 92103 United States, Connecticut Coastal Connecticut Research, LLC New London, Connecticut, United States, 06320 United States, Florida Women's Medical Research Group, LLC Clearwater, Florida, United States, 33759 Radiant Research, Inc. Pinellas Park, Florida, United States, 33781 Comprehensive Clinical Trials, LLC West Palm Beach, Florida, United States, 33409 United States, Georgia Fellows Research Alliance, Inc Savannah, Georgia, United States, 31406 United States, Michigan Beyer Research Kalamazoo, Michigan, United States, 49009 United States, Nevada Office of R. Garn Mabey, M.D. Las Vegas, Nevada, United States, 89128 United States, North Carolina Carolina Women's Research and Wellness Center Durham, North Carolina, United States, 27713 Hawthorne Medical Research, Inc. Winston-Salem, North Carolina, United States, 27103 United States, Ohio Rapid Medical Research, Inc. Cleveland, Ohio, United States, 44122 Women's Health Research Columbus, Ohio, United States, 43213 United States, Pennsylvania Clinical Research of Philadelphia, LLC Philadelphia, Pennsylvania, United States, 19114 United States, South Carolina Fellows Research Alliance, Inc Bluffton, South Carolina, United States, 29910 United States, Texas Radiant Research, Inc. Dallas, Texas, United States, 75231 Radiant Research, Inc. San Antonio, Texas, United States, 78229 United States, Virginia Virginia Women's Center Richmond, Virginia, United States, 23233 United States, Washington Seattle Women's Health, Research, Gynecology Seattle, Washington, United States, 98105 North Spokane Women's Clinic Spokane, Washington, United States, 99207 Collapse <<
  NCT03069781	Muscle Atrophy	Early Phase 1	Withdrawn(Lack of funding)	-	Canada, Ontario ... more >> McMaster Univeristy Hamilton, Ontario, Canada Collapse <<

• 更多
• 参考文献

• [1] Matthews J, Celius T, et al. Differential estrogen receptor binding of estrogenic substances: a species comparison. J Steroid Biochem Mol Biol. 2000 Nov 15;74(4):223-34.

  [2] Refaie MMM, El-Hussieny M. Diacerein inhibits Estradiol-benzoate induced cervical hyperkeratosis in female rats. Biomed Pharmacother. 2017 Nov;95:223-229

  [3] Mogheiseh A, Mosavi Ghiri MJ, Bandarian E. The Clinical Follow-Up of Estradiol Benzoate Priming During Induction of Estrus With Cabergoline in Dogs. Top Companion Anim Med. 2017 Mar;32(1):16-19

  [4] Zhang R, Zheng R, Yang LN, Lei XC, Chen W. [Estradiol benzoate induces abnormal proliferation of spermatogenic cells in the testis of infertile male mice]. Zhonghua Nan Ke Xue. 2018 Janurary;24(1):19-26

  [5] Aguirre-Vidal Y, Morales-Montor J, Gómez de León CT, Ostoa-Saloma P, Díaz-Zaragoza M, Montes S, Arteaga-Silva M, Monroy-Noyola A. Protection induced by estradiol benzoate in the MPP+ rat model of Parkinson's disease is associated with the regulation of the inflammatory cytokine profile in the nigro striatum. J Neuroimmunol. 2020 Dec 15;349:577426

• 更多

• Collapse