谢晶曦, 王琳, 刘春雪, 张德勇. 草药矮地茶止咳成分的化学结构及合成J. 药学学报, 1981, 16(6): 425-428.
引用本文: 谢晶曦, 王琳, 刘春雪, 张德勇. 草药矮地茶止咳成分的化学结构及合成J. 药学学报, 1981, 16(6): 425-428.
Xie Jingxi, Wang Lin, Liu Chunxue , Zhang Deyong, . THE IDENTIFICATION AND TOTAL SYNTHESIS OF AICHASU, AN ANTITUSSIVE AGENTJ. Acta Pharmaceutica Sinica, 1981, 16(6): 425-428.
Citation: Xie Jingxi, Wang Lin, Liu Chunxue , Zhang Deyong, . THE IDENTIFICATION AND TOTAL SYNTHESIS OF AICHASU, AN ANTITUSSIVE AGENTJ. Acta Pharmaceutica Sinica, 1981, 16(6): 425-428.

草药矮地茶止咳成分的化学结构及合成

THE IDENTIFICATION AND TOTAL SYNTHESIS OF AICHASU, AN ANTITUSSIVE AGENT

  • 摘要: 矮茶素(Ⅰ)是草药“矮地茶”的有效成分,临床用于治疗慢性气管炎有较好的止咳作用,经光谱等物理常数测定以及化学降解,确定它与虎耳草科等植物中的bergenin是同一物质。在矮茶素(Ⅰ)的全合成中分到一副产物:3β-葡萄糖-4-甲氧基-苯甲酸甲酯(Ⅵ-1),动物初筛也有止咳作用。

     

    Abstract: Aichasu (Ⅰ) was isolated from the Chinese herb Ardisia japonica. It shows antitussive activity in mice (cough induced by ammonium hydroxide spray), and has been used clinically for the treatment of chronic bronchitis with beneficial effect. Through spectroscopic analyses (UV, IR, NMR, MS) and the determination of physico-chemical constant as well as periodate degradation, aichasu (Ⅰ)was identified as bergenin formerly isolated from the root of Bergenia crossefolia.Aichasu (Ⅰ)was synthesized by the reaction of methyl 4-O-methylgallate with acetobromoglucose in the presence of sodium methoxide in methanol. A by-product was separated from the reaction mixture and determinted to be methyl 3-β-glucosyl-4-methoxy-5-hydroxybenzoate (Ⅵ-1).

     

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