摘要
穿心莲内酯的原型在生物体内的药代动力学分布主要集中于血流丰富的组织器官,对其结构进行修饰得到的衍生物可以加速体内分布或增加其在某些组织器官中的分布。穿心莲内酯可通过抑制NO的产生和环氧合酶的表达,抑制黏附分子及细胞因子产生,阻断NF-κB通路、MAPK通路、PI3K/AKT通路等起到抗炎的作用。目前,关于穿心莲内酯及其衍生物的体内分布与抗炎机制已有广泛研究,进一步阐明其构效关系和作用靶点,以期发现新的靶点和高效抗炎药物的研发,值得深入的研究。
The pharmacokinetic distribution of andrographolide in organisms is mainly concentrated in blood-rich tissues, and its derivatives can accelerate or increase its distribution in other tissues and organs. Andrographolide can inhibit the production of NO and the expression of cyclooxygenase, which inhibit the production of adhesion molecules and cytokine. As a result, NF-κB pathway, MAPK pathway and PI3K/AKT pathway can be block. At present, the in vivo distribution and anti-inflammatory mechanism of andrographolide and its derivatives have been extensively studied. It is beneficial to discover new targets and develop efficient anti-inflammatory drugs that clarifying andrographolide and its derivatives＇ structure-activity relationship and the targets, so further research need to be studied.
作者
张琦
崔庆新
ZHANG Qi, CUI Qingxin(College of Pharmacy, Nankai University, Tianjin 300353, Chin)
出处
《生命的化学》
CAS
CSCD
2018年第1期8-14,共7页
Chemistry of Life
基金
国家自然科学基金项目(81503214)
关键词
穿心莲内酯
体内分布
抗炎机制
andrographolidei in vivo distribution
anti-inflammatory mechanism
