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生物活性弗兰切丁类型的二类化物:分离,合成,抗炎,抗作用,以及分子对接

Yan Xiao¹, Ye Chang², Yu-Yan Liu³

¹School of Life Science and Engineering, Southwest Jiaotong University, Chengdu, Sichuan, PR China.

Bioorganic chemistry

|September 27, 2024

概括

来自Aconitum sinoaxillare的法兰切丁衍生物通过抑制关键信号通路,显示出强大的抗炎作用. 化合物1具有显著的抗炎和止痛特性,具有低毒性,为新药开发提供了潜力.

科学领域:

自然产品化学自然产品化学
药理学药理学是指药理学的学科.
药用化学医学化学

背景情况:

阿科尼图姆 (Aconitum sinoaxillare) 是二甲类类化合物的来源.
弗兰切丁衍生物具有潜在的药理活性.
炎症和疼痛是严重的健康问题,需要新的治疗药物.

研究的目的:

为了分离和合成法兰切丁类型的二类化物.
评估这些化合物的抗炎和止痛作用.
阐明最活跃化合物的作用机制.

主要方法:

从Aconitum sinoaxillare中分离了四种法兰切丁类型的二类化物.
合成了十四种不同的法兰切丁类型.
试验室试验评估对氧化 (NO) 生产,可诱导氧化合成酶 (iNOS) 和循环氧化酶-2 (COX-2) 的抑制作用.
在体外研究以调查TLR4-MyD88/NF-κB/MAPKs信号通路的抑制.
在体内研究以评估小鼠的止痛作用和毒性.
电生理学研究评估对NaV1.7和NaV1.8通道的影响.

主要成果:

化合物1,2,7和16显示出比celecoxib更强大的NO生产抑制.
化合物1表现出对iNOS和COX-2的最强烈抑制.
化合物1的抗炎作用通过抑制TLR4-MyD88/NF-κB/MAPKs通路,减少炎症介质 (NO,ROS,TNF-α,IL-6,IL-1β,iNOS,COX-2) 来进行介导.
化合物1的毒性低 (LD50>20毫克/公斤) 和显著的止痛作用 (ED50 = 2.15 ± 0.07毫克/公斤).
化合物1减少了NaV1.7和NaV1.8通道电流.

结论:

弗兰切丁衍生物具有显著的抗炎和止痛特性.
化合物1是开发新型抗炎和止痛药的有希望的候选物.
这项研究为法兰切丁衍生物的药理活动提供了宝贵的见解.

关键词:

弗朗切蒂尼尼 (Franchetine) 是一种法轮功产品.弗兰切丁的类似物是弗兰切丁.这就是MAPKs.在 NF-κBB 中.的Na (V) 频道.

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