乌罗立A:一个有前途的选择性雌激素受体调节剂和27-基胆固醇减弱剂在乳腺癌中
Ravindran Vini1,2, Vishnu Sunil Jaikumar3, Viji Remadevi1,2
1Cancer Research Program, Rajiv Gandhi Centre for Biotechnology (RGCB), Thiruvananthapuram, India.
Phytotherapy research : PTR
|June 22, 2023
概括
乌罗立A (UA) 对抗乳腺癌中27-胆固醇 (27-HC) 的有害影响. 氨酸表现出抗增殖和雌激素受体调节作用,具有作为安全治疗剂的潜力.
科学领域:
- 生物化学 生物化学
- 分子生物学分子生物学
- 在瘤学瘤学.
背景情况:
- 27-胆固醇 (27-HC) 作为内源性选择性雌激素受体调节器 (SERM),有助于雌激素受体 (ER) 介导的乳腺癌进展.
- 石榴提取物含有丰富的ellagitannins和ellagic酸,被肠道微生物群代谢成urolithins,例如urolithin A (UA) 和urolithin B (UB).
- 乌罗利已经证明了有益的特性,包括抗增殖和雌激素活性,这表明了潜在的治疗应用.
研究的目的:
- 研究乌罗素,特别是UA在对抗和抵消27-HC在乳腺癌细胞中的不良影响方面的潜力.
- 评估UA对乳腺癌细胞增殖,膜潜力和亡的影响.
- 评估UA的雌激素受体α (ERα) 调节活性及其体内有效性和安全性.
主要方法:
- 使用乳腺癌细胞进行体外测试,以评估UA对27-HC诱导的增殖,膜潜力和亡的影响.
- 对雌激素反应元 (ERE) 转录活性和对雌激素反应基因调制的分析.
- 在体内空洞纤维测试以评估UA在降低乳腺癌细胞活力和27-HC诱导的增殖方面的有效性.
- 在体内对UA对子宫增殖和血液生物化学参数的影响的评估.
主要成果:
- 亚氨酸表现出显著的抗增殖能力,减弱了乳腺癌细胞中27-HC诱导的增殖.
- 在乳腺癌细胞中,UA诱导了亡和膜潜力的丧失.
- 通过诱导ERE转录活性和调节雌激素反应基因,UA表现出类似SERM的活性.
- 在体内研究证实了UA能够降低乳腺癌细胞活力并抵消27-HC的影响,而不会对子宫增殖或血液参数产生不良影响.
结论:
- 乌罗立A (UA) 作为一种强大的ERα调节剂和27-HC抗剂,在对抗胆固醇相关的乳腺癌方面表现有前途.
- 氨酸对乳腺癌细胞具有抗增殖和诱导亡的特性.
- 氨酸是安全的,耐受性很好,这表明它作为治疗雌激素依赖性疾病的治疗剂的潜力.
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