Objective:Pinellia Tuber,the dried tuber of Pinellia ternata,is widely used in Japanese Kampo medicines and traditional Chinese medicines.The unprocessed Pinellia Tuber is known to cause very strong acrid irritation a...Objective:Pinellia Tuber,the dried tuber of Pinellia ternata,is widely used in Japanese Kampo medicines and traditional Chinese medicines.The unprocessed Pinellia Tuber is known to cause very strong acrid irritation at oral and laryngopharynx mucosa.Recent studies have shown that the sharp needle-like crystals called raphides,that are composed of calcium oxalate and proteins,are the main causative substances of the irritation.Ginger,the rhizome of Zingiber officinale,has been used in the processing to reduce the acridity of Pinellia Tuber since before the sixth century,however,the mechanisms of reducing acridity have not been scientifically proved yet.Methods:We developed the raphides denaturation assay(RDA)to quantify the degree of denaturation in the raphides to cause irritation.By their lipophilic characters,the raphides could be extracted in petroleum ether(PE)layer from powdered Pinellia Tuber suspended in water,and the contents of the raphides in PE layer were measured by the absorbance.By this assay,we conducted the activity-guided fractionation from the boiling water extract of ginger to find the ingredients to denature the raphides.We also conducted the gustatory tests to detect the change of the irritation of the denatured raphides.Results:The treatment of powdered Pinellia Tuber suspension with ginger extract reduced the distribution of raphides in PE layer in RDA in a concentration-dependent manner.The activity-guided fractionation using RDA revealed that oxalic acid was the main active ingredient in ginger extract to denature the raphides of Pinellia Tuber.Oxalic acid reduced the lipophilicity of the raphides in the thermo-,time-,and concentration-dependent manners,and its activity was affected by pH.The treatment of powdered Pinellia Tuber suspension with oxalic acid significantly reduced its acrid irritation in gustatory test in human.Conclusions:We found that oxalic acid is the main active ingredient in ginger to reduce the acrid irritation of Pinellia Tuber.展开更多
目的基于网络药理学探讨葛根-半夏对2型糖尿病(type 2 diabetes mellitus,T2DM)的调控机制。方法2022年8—9月,利用中草药系统药理学平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)、中药分子机制的生物信息学分析工具...目的基于网络药理学探讨葛根-半夏对2型糖尿病(type 2 diabetes mellitus,T2DM)的调控机制。方法2022年8—9月,利用中草药系统药理学平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)、中药分子机制的生物信息学分析工具(Bioinformatics Analysis Tool for Molecular mechANism of Traditional Chinese Medicine,BATMAN-TCM)以及中医药百科全书(The Encyclopedia of Traditional Chinese Medicine,ETCM)数据库筛选葛根-半夏活性成分及成分对应靶点,通过GeneCard、OMIM、TTD数据库收集T2DM疾病相关靶点,药物靶点与疾病靶点取交集,利用STRING数据库分析交集靶点,获取蛋白-蛋白互作(PPI)网络图,通过Cytoscape对结果进行可视化分析,得到核心靶点;交集靶点导入Metascape进行基因本体(gene ontology,GO)和京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEEG)功能富集分析。结果葛根-半夏药物活性成分主要包括芒柄花素、β-谷甾醇、黄芩素、豆甾醇和松柏苷等,包括4个葛根和9个半夏成分,其中β-谷甾醇为两者共有,成分靶点和疾病的交集靶点共93个,核心靶点为JUN、TP53、AKT1、ESR1、RELA、FOS、MAPK14、HIF1A、PPARG、NCOA1等,交集靶点主要涉及脂质和动脉粥样硬化、钙信号通路、PI3K-Akt信号通路、糖尿病并发症中的AGE-RAGE信号通路、雌激素信号通路等信号通路。结论葛根-半夏可以通过调节多个生物过程,激活多通路、多靶点发挥改善2型糖尿病的作用。展开更多
基金the grant from Oriental Medicine Research Foundation in 2020.
文摘Objective:Pinellia Tuber,the dried tuber of Pinellia ternata,is widely used in Japanese Kampo medicines and traditional Chinese medicines.The unprocessed Pinellia Tuber is known to cause very strong acrid irritation at oral and laryngopharynx mucosa.Recent studies have shown that the sharp needle-like crystals called raphides,that are composed of calcium oxalate and proteins,are the main causative substances of the irritation.Ginger,the rhizome of Zingiber officinale,has been used in the processing to reduce the acridity of Pinellia Tuber since before the sixth century,however,the mechanisms of reducing acridity have not been scientifically proved yet.Methods:We developed the raphides denaturation assay(RDA)to quantify the degree of denaturation in the raphides to cause irritation.By their lipophilic characters,the raphides could be extracted in petroleum ether(PE)layer from powdered Pinellia Tuber suspended in water,and the contents of the raphides in PE layer were measured by the absorbance.By this assay,we conducted the activity-guided fractionation from the boiling water extract of ginger to find the ingredients to denature the raphides.We also conducted the gustatory tests to detect the change of the irritation of the denatured raphides.Results:The treatment of powdered Pinellia Tuber suspension with ginger extract reduced the distribution of raphides in PE layer in RDA in a concentration-dependent manner.The activity-guided fractionation using RDA revealed that oxalic acid was the main active ingredient in ginger extract to denature the raphides of Pinellia Tuber.Oxalic acid reduced the lipophilicity of the raphides in the thermo-,time-,and concentration-dependent manners,and its activity was affected by pH.The treatment of powdered Pinellia Tuber suspension with oxalic acid significantly reduced its acrid irritation in gustatory test in human.Conclusions:We found that oxalic acid is the main active ingredient in ginger to reduce the acrid irritation of Pinellia Tuber.
文摘目的基于网络药理学探讨葛根-半夏对2型糖尿病(type 2 diabetes mellitus,T2DM)的调控机制。方法2022年8—9月,利用中草药系统药理学平台(Traditional Chinese Medicine Systems Pharmacology,TCMSP)、中药分子机制的生物信息学分析工具(Bioinformatics Analysis Tool for Molecular mechANism of Traditional Chinese Medicine,BATMAN-TCM)以及中医药百科全书(The Encyclopedia of Traditional Chinese Medicine,ETCM)数据库筛选葛根-半夏活性成分及成分对应靶点,通过GeneCard、OMIM、TTD数据库收集T2DM疾病相关靶点,药物靶点与疾病靶点取交集,利用STRING数据库分析交集靶点,获取蛋白-蛋白互作(PPI)网络图,通过Cytoscape对结果进行可视化分析,得到核心靶点;交集靶点导入Metascape进行基因本体(gene ontology,GO)和京都基因与基因组百科全书(Kyoto Encyclopedia of Genes and Genomes,KEEG)功能富集分析。结果葛根-半夏药物活性成分主要包括芒柄花素、β-谷甾醇、黄芩素、豆甾醇和松柏苷等,包括4个葛根和9个半夏成分,其中β-谷甾醇为两者共有,成分靶点和疾病的交集靶点共93个,核心靶点为JUN、TP53、AKT1、ESR1、RELA、FOS、MAPK14、HIF1A、PPARG、NCOA1等,交集靶点主要涉及脂质和动脉粥样硬化、钙信号通路、PI3K-Akt信号通路、糖尿病并发症中的AGE-RAGE信号通路、雌激素信号通路等信号通路。结论葛根-半夏可以通过调节多个生物过程,激活多通路、多靶点发挥改善2型糖尿病的作用。
