| 摘要: |
| 三峡区域药用植物拐芹的根中富含倍半萜类抗溃疡活性成分没药烷吉酮,为可开发和利用的中草药资源。本文对该化合物进行了提取分离、结构修饰和初步的构效关系研究,从拐芹根茎中提取并分离了没药烷吉酮,通过选择性还原、缩合和加成反应制备了四个没药烷吉酮氨基甲酰腙衍生物。用核磁共振波谱、质谱、红外和元素分析等方法确证了其结构,并测试了其体外对H~+/K~+-ATP酶的抑制活性和细胞毒活性。没药烷吉酮还原衍生物2及4-氯苯基取代的氨基甲酰腙衍生物4d较阳性对照药物奥美拉唑具有更好的体外抗溃疡活性(IC50<24μmol/L)。本文探明了没药烷吉酮衍生物的结构对体外H~+/K~+-ATP酶抑制活性的影响,为消化性溃疡的治疗提供了新型倍半萜类候选药物。 |
| 关键词: 拐芹 倍半萜 没药烷吉酮 结构修饰 H+/K+-ATP酶抑制活性 |
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| Structure modification and H~+/K~+-ATPase inhibitory activity of sesquiterpene bisabolangelone from Angelica polymorpha Maxim |
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YAO Yuan,XIE Tianpeng,CHEN Lei,HUANG Nianyu,WANG Junzhi,ZOU Kun,Hubei Key Laboratory of Natural Products Research,Development,College of Biological,Pharmaceutical Sciences,China Three Gorges University
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Hubei Key Laboratory of Natural Products Research and Development,College of Biological and Pharmaceutical Sciences,China Three Gorges University
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| Abstract: |
| The antiulcer sesquiterpene bisabolangelone is rich in the roots of Angelica polymorpha Maxim in the Three Gorges area.In order to develop and apply the bioactive ingredient in the natural medical plants,bisabolangelone was isolated and its structure was modified.Four hydrazinecarboxamides were prepared through selective reduction,condensation and additional reaction,and their structures were characterized by nuclear magnetic resonance(NMR),electrospray ionization mass spectrometry(ESI-MS),infrared spectroscopy(IR)and elemental analysis.They were also evaluated preliminarily for their in vitro H~+/K~+-ATPase inhibition activity and cytotoxicities.The antiulcer activities of bisabolangelone derivitives could be obviously improved by selective reduction derivative 2 and 4-chlorophenyl substituted hydrazinecarboxamide 4d(IC50<24μmol/L),which were better than commercial omeprazole.The research indicated that the bioactivity of bisabolangelone derivatives might be enhanced by inducting some special atoms,and these results provided a new sesquiterpene-type reference drug for the treatment of gastric ulcer. |
| Key words: Angelica polymorpha Maxim sesquiterpene bisabolangelone structure modification H+/K+-ATPase inhibitory activity |
