盾叶薯蓣总皂苷及苷元衍生物的抗炎镇痛活性研究  

Anti-inflammatory and Analgesic Effects of Saponins from D.zingiberensis C.H.Wright and Diosgenin Derivative on Mice

作　　者：马茂华[1] 吴晓华[1] 何杨[1] 黄文[1] 

机构地区：[1]四川大学华西医院生物治疗国家重点实验室纳米技术与膜生物学研究所,成都610041

出　　处：《四川大学学报（医学版）》2011年第4期494-497,共4页Journal of Sichuan University(Medical Sciences)

基　　金：国家"十二五"支撑项目(2011BAJ07B04);四川省科技支撑项目(2008S20024)资助

摘　　要：目的研究盾叶薯蓣总皂苷及合成的薯蓣皂苷元衍生物对小鼠抗炎镇痛的作用。方法先将阿司匹林酰氯化,再与薯蓣皂苷元反应,制得具有孪药性质的薯蓣皂苷元衍生物3β-2-乙酰氧基苯甲酰薯蓣皂苷元酯(ABDE),并采用核磁共振氢谱(1H-NMR)和质谱(ESI-MS)进行结构分析确证。在二甲苯所致小鼠耳廓肿胀和醋酸所致小鼠扭体反应的实验中,观察薯蓣总皂苷及新合成的ABDE的抗炎和镇痛作用。结果薯蓣总皂苷126mg/kg和252 mg/kg对小鼠耳廓肿胀抑制率分别是7.92%和14.51%,对扭体反应的抑制率分别是15.42%和26.17%;合成ABDE总收率约为43.5%,是未见文献报道的新化合物;初步生物活性筛选在浓度为21.9、43.8、87.6 mg/kg的3个梯度下,对小鼠耳廓肿胀抑制率分别是18.03%、25.51%、33.48%,对应的阿司匹林单体组的抑制率为13.47%、21.55%、28.20%;醋酸所致小鼠腹腔疼痛抑制率分别是34.87%、41.54%、50.77%,对应的阿司匹林单体组的抑制率为31.80%、49.23%、53.85%.结论薯蓣总皂苷具有抗炎症和镇痛作用;新化合物ABDE结构经1H-NMR和ESI-MS得到确证;ABDE的低中高剂量各组抗炎镇痛作用强度与阿司匹林各对应组相近。Objective To determine the potential anti-inflammatory and analgesic activities of saponins from D.zingiberensis C.H.Wright and diosgenin derivative on xylene-induced acute ear edema in mice.Methods 3β-2-acetoxy-benzoyl-diosgenin ester（ABDE） was synthesized by acylation of aspirin through two-step of reaction.The analgesic activities of ABDE and saponins were investigated through acetic acid-induced writhing response of the mice.The anti-inflammatory effects of saponins and ABDE were observed on the xylene-induced swelling ears of the mice.Results The structure of ABDE was confirmed by 1H-NMR and ESI-MS.ABDE had significantly higher anti-inflammatory and analgesic activities than the comparison drug.The saponins demonstrated 7.92% and 14.51% anti-inflammatory activities at the dose of 126 mg/kg and 252 mg/kg,respectively,and 15.38% and 26.15% analgesic activities at the dose of 126 mg/kg and 252 mg/kg,respectively.Conclusion The saponins of D.zingiberensis C.H.Wright possess acute nonspecific anti-inflammatory and analgesic effects.The anti-inflammatory and analgesic effects of ABDE are equivalent to aspirin.

关 键 词：薯蓣皂苷 薯蓣皂苷元 阿司匹林 酯化 抗炎镇痛活性 

分 类 号：R285.5[医药卫生—中药学]