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在接受葛根素治疗的大鼠模型中,子宫内膜异位症植入物通过降低雌二醇水平而消退。

Endometriotic implants regress in rat models treated with puerarin by decreasing estradiol level.

机构信息

Department of Chinese Traditional Medicine Gynecology, Changhai Hospital, Second Military Medical University, 168 Changhai Road, Shanghai, People's Republic of China.

出版信息

Reprod Sci. 2011 Sep;18(9):886-91. doi: 10.1177/1933719111398500. Epub 2011 Jun 14.

Abstract

Phytoestrogens, which have a weak estrogenic effect, bind to estrogen receptors (ERs), thereby competing with estradiol, have an antiestrogenic effect on women of reproductive age with high estrogenic level. Herein, we examined the ability of the phytoestrogen Puerarin to treat endometriosis in rat models of endometriosis. In total, 75 adult, mature female Sprague-Dawley rats in which endometriotic implants were successfully induced by transplanting autologous endometrial tissue to ectopic sites were used in this study. Oral gavage of Puerarin (at doses of 600, 200, or 60 mg/kg per day) or Danazol (80 mg/kg per day) started 4 weeks after implantation. Control model rats received vehicle alone. After administration for 4 weeks, the weight of the ectopic implants, estradiol concentration, as well as ER-α and Aromatase P450 (P450arom) expression in different groups of rat tissues were evaluated after treatment. The endometriotic tissue weight and serum estrogen levels were significantly lower in high, medium, low dose of Puerarin and Danazol treatment groups than that in control group (P < .05 or P < .01). Low-dose Puerarin inhibited P450arom expression and significantly reduced estrogen levels in endometriotic tissue (P < .01). Three doses of Puerarin had no adverse effects on liver, kidney, and ovary, whereas high-dose Puerarin administration caused thinner bone trabecula with distortion and breakage and Danazol administration caused mild or moderate hepatic cell damage. These data demonstrate that Puerarin was able to effectively suppress the growth and development of ectopic endometrium in the rat endometriosis model, even at low doses, suggesting it may be an effective treatment for endometriosis.

摘要

植物雌激素具有较弱的雌激素作用,与雌激素受体(ERs)结合,从而与处于高雌激素水平的生育期妇女的雌二醇竞争,具有抗雌激素作用。在此,我们研究了植物雌激素葛根素治疗子宫内膜异位症大鼠模型的能力。在这项研究中,总共使用了 75 只成年、成熟的雌性 Sprague-Dawley 大鼠,这些大鼠通过将自体子宫内膜组织移植到异位部位成功诱导了子宫内膜异位症。葛根素(600、200 或 60mg/kg/天)或达那唑(80mg/kg/天)的口服灌胃在移植后 4 周开始。对照模型大鼠单独给予载体。给药 4 周后,评价不同组别大鼠组织异位植入物的重量、雌二醇浓度以及 ER-α 和芳香化酶 P450(P450arom)的表达。与对照组相比,高、中、低剂量葛根素和达那唑治疗组的异位组织重量和血清雌激素水平均显著降低(P <.05 或 P <.01)。低剂量葛根素抑制 P450arom 的表达,显著降低异位组织中的雌激素水平(P <.01)。三剂量葛根素对肝脏、肾脏和卵巢没有不良影响,而高剂量葛根素给药导致骨小梁变薄、变形和断裂,达那唑给药导致轻度或中度肝实质细胞损伤。这些数据表明,葛根素能够有效抑制大鼠子宫内膜异位症模型中异位子宫内膜的生长和发育,即使在低剂量下,也可能是一种有效的子宫内膜异位症治疗方法。

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