阿里红总三萜酸的制备及其抗哮喘作用研究  

Preparation of total triterpene acid and its anti-asthma effect

作　　者：许福春 杜茂波[2] XU Fu-chun;DU Mao-bo(Sinopharm Xingsha Pharmaceuticals(Xiamen)Co.,Ltd.,Xiamen Fujian 361028;Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700)

机构地区：[1]国药控股星鲨制药(厦门)有限公司,福建厦门361028 [2]中国中医科学院中药研究所,北京100700

出　　处：《中南药学》2023年第8期2053-2058,共6页Central South Pharmacy

摘　　要：目的以总三萜酸和3个三萜酸单体作为指标优化阿里红总三萜酸的制备工艺,并对总三萜酸的抗哮喘作用进行研究。方法以总三萜酸含量和转移率为指标,采用Hunter和星点设计-响应面法优化阿里红总三萜酸的大孔树脂富集纯化工艺,确定关键工艺参数,并以3个三萜酸成分含量对制备工艺进行验证。最后采用氯化乙酰胆碱和磷酸组织胺致喘豚鼠的动物模型,评估阿里红总三萜酸对哮喘豚鼠引喘潜伏期和血清中血栓素B_(2)(TXB_(2))和白三烯B_(4)(LTB_(4))含量的影响。结果最优工艺为:乙醇除杂浓度30.0%(23.0%~35.7%),乙醇解析浓度83.0%(72.0%~97.2%)和乙醇解析用量7.5倍(5~10倍);3批总三萜酸中齿孔酸含量依次为7.91%、6.56%、8.91%,去氢齿孔酸含量依次为4.95%、4.56%、6.02%,去氢硫色多孔菌酸含量依次为11.2%、11.0%、12.8%;与模型组相比,阿里红总三萜酸低、中和高剂量组均能显著延长哮喘豚鼠引喘潜伏期,中和高剂量组均可显著降低哮喘豚鼠血清中TXB_(2)和LTB_(4)含量。结论所建立的HPLC分析方法可准确测定阿里红总三萜酸中3个三萜酸的含量,优化的D101型大孔树脂富集纯化阿里红总三萜酸的工艺稳定可行,所得总三萜酸具有较好的抗哮喘活性。Objective To optimize the process parameters of total triterpene acid enrichment from Fomes officinalis Ames based on total triterpene acid and three triterpenoids,and to determine its anti-asthma effect.Methods Total triterpene acid content and transfer rate were used as indexes.Hunter and the central composite design response surface method were combined to optimize the process of total triterpene acid enrichment.The optimum values and acceptable ranges of the key process parameters were determined.The content of three triterpenoids was used to verify the preparation process.The asthma model of guinea pigs was established by acetylcholine chloride and histamine phosphate,which was used to assess the effect of total triterpene acid on the incubation period of asthma,and the amount of TXB_(2)and LTB_(4)in the blood serum.Results The optimum values and acceptable ranges of the three key parameters were:ethanol fraction for impurity removal 30.0%(23.0%~35.7%),ethanol fraction for elution 83.0%(72.0%~97.2%)and ethanol amount for elution 7.5 fold(5~10 fold).Three batches of samples were analyzed,with the contents of eburicoic acid 7.91%,6.56%,and 8.91%,that of dehydroeburicoic acid 4.95%,4.56%,6.02%,and that of dehydrosulphurenic acid 11.2%,11.0%,and 12.8%.The total triterpene acid significant prolonged the incubation period of asthmatic guinea pigs in the three dose groups,and reduced TXB_(2)and LTB_(4)levels in the blood serum in the middle and high dose groups.Conclusion HPLC is suitable for the simultaneous determination of three triterpenoids.The developed enrichment method for total triterpene acid from Fomes officinalis Ames using D101 macroporous resin is stable and feasible.The obtained total triterpene acids have good bioactivity and anti-asthma effect.

关 键 词：阿里红总三萜酸 星点设计-响应面法 设计空间 含量测定 抗哮喘作用 

分 类 号：R284.1[医药卫生—中药学] R285[医药卫生—中医学]