摘要
用巴豆油诱发的小鼠耳炎症模型及小鼠溶血素抗体生成模型作指标,测定从雷公藤中分离的7个环氧二萜内酯化合物的抗炎及免疫抑制活性的半数有效剂量(ED_(50))、治疗指数(TI)和可靠安全系(CSF)。结果表明:雷藤内酯醇(T10)、雷藤氯内酯醇(T4)、雷藤内酯酮(T7)、雷藤内酯二醇(T8)、雷醇内醋(T9)和16-羟基内酪醇(L2)兼有抗炎、免疫抑制活性;而雷藤内酯三醇(T11)仅具抗炎活性。7个合物抗炎作用的TI由大至小依序为:T11(>19)、T10(17)、T9(9.6)、T4(9.0)、T8(7.3)、L2(6.6)、T7(5.9);6个化合物免疫抑制作用的TI依序为:T9(30.7)、T4(16.7)、L2(15.8)、T10(13.7)、T8(8.8)、T7(7.5)。全部化合物的抗炎、免疫抑制作用的CSF都大于1,其中T9、T4、L2免疫抑制作用的CSF分别为7.1、5.1和3.6。这显示雷公藤抗炎免疫有效成份是多元的。这些差别可作为化合物药用评价和选择的依据之一。然而,这些化合物的实用价值还取决于它们在药材中的含量和得率,合成和衍生物制备的难易以及遗传毒性检测的结果。
The half-effective dose(ED50)、 therapeutic index(TI) and certain safety factor(CSF) of 7 diterpene lactone epoxide compounds with antiinflammatory and immunosuppressive action extracted from Tripterygium wilfordii (TW) were assayed using croton oil-induced ear swelling and hemolysin-antibody formation mouse models.The results indicated that triptolide(T10). trpchlorolide(T4)、triptonide(T7)、 tripdiolide(T8), triptolidenol(T9) and 16-hydroxytriptolide(L2) possessed both anti-inflammatory and immunosuppressive activities, while triptriolide(T11) had antiinflammatory activity only. The TI of the antiinflammatory action of 7 compounds were arranged in following order:T11(> 19), T10(17)、 T9(9.6)、T4(9.0)、 T8(7.3)、 L2(6.6)、 T7(5.9)、 while the TI of the immunosuppressive action of 6 compounds were arranged in following order: T9(30.7)、 T4(16.7)、 L2(15.8)、 T10(l3.7)、 T8(8.8)、 T7(7.5). The CSF parameters of both the activities of 7 compounds were all higher than 1. In which, the CSF of the immunosuppressive action of T9?T4 and L2 were 7.1、5.1 and 3.6 respectively. These facts clearly demonstrate that the antiinflammatory and immunosuppressive compounds in TW are pluralistic. These differences among these compounds can be used as one of the bases for the evaluation and selection of these compounds.The above experiments conclude that the practical value of these compounds, however, will also depend on their content and yield rate in the herb, on the degree of difficulty in synthesizing these compounds, and on difficulty involved in the preparation of their derivatives. The future of these compounds will depend on the results of genetic toxicology studies as well.
出处
《中国医学科学院学报》
CAS
CSCD
北大核心
1991年第6期391-397,共7页
Acta Academiae Medicinae Sinicae
基金
国家自然科学基金
关键词
雷公藤
环氧二萜内酯
抗炎
抗生育
Tripterygium wilfordii. diterpene lactone expoxide antiinflammatory immunosuppressive therapeutic index cartain safety factor
