糖化驱动的生物活性切换:比较的药理学和转化前景的奥洛辛和贝卡莱因
Huan Wang1, Yuan Liu1, Yi-Xuan Song1
1School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu, 611137, China.
概括
奥洛辛和白卡莱因显示出治疗前景,但面临生物可用性和毒性挑战. 先进的输送系统和安全性研究对于其临床使用至关重要.
科学领域:
- 药理学 药理学是指药理学的学科.
- 自然产品 化学 化学
- 药物开发 药物开发
背景情况:
- 奥洛辛和白卡莱因是具有抗癌,抗炎,代谢和心脏保护性能的黄类药物.
- 这些化合物的临床转化受到生物可用性差和毒理学数据不足的限制,特别是对于奥洛辛.
研究的目的:
- 为了比较奥洛辛和拜卡莱因的分子机制,药理动力学和依赖于糖化酶的活性.
- 评估新的生产和交付策略,以克服翻译障碍.
主要方法:
- 在2025年5月之前,使用Web of Science和PubMed进行了全面的文献搜索.
- 研究是根据阐明化合物活性,机制或比较的原始数据进行选择的,不包括缺乏特定或验证数据的研究.
- 包括的研究被分为体外或体内研究.
主要成果:
- 这两种化合物都以情境依赖的方式调节PI3K/AKT,NF-κB和ER应激通路.
- 奥洛辛的糖化改善了溶解性,但降低了透性,影响了分布和稳定性;贝卡莱因经历了广泛的葡萄糖化,具有良好的安全性.
- 微生物生物合成,纳米配方和协同组合等新兴策略可以提高产量,ADME特性和治疗指数.
结论:
- 奥素和白素具有显著的治疗潜力,但临床应用受到生物可用性和毒性担忧的阻碍,特别是对于奥素.
- 未来的研究应该专注于先进的药物输送系统,全面的安全评估,并探索协同作用和免疫调节作用.
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