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垂盆草苷的合成*
http://www.100md.com 《药学学报》1999年第1期
垂盆草苷|谷丙转氨酶|全合成
     作者:诸国华 周启霆 白东鲁

    单位:(中国科学院上海药物研究所, 上海 200031)

    关键词:垂盆草苷;谷丙转氨酶;全合成

    药学学报990108.htm SYNTHESIS OF SARMENTOSIN*

    Chu Guohua(Chu GH), Zhou Qiting(Zhou QT) and Bai Donglu(Bai DL)**

    (Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 200031)

    ABSTRACT AIM: The synthesis of sarmentosin. METHODS: Condensation of butane-1,2,4-triol-1,2-acetonide(3) with α-D-glucopyranosyl bromide tetraacetate in the presence of Ag2O and molecular sieves gave the desired β-glucoside 4, which was transformed into sarmentosin via a reaction sequence of 7 steps. RESULTS: The overall yield is 5.8%. CONCLUSION: The first synthesis of sarmentosin(1), a potent natural GPT lowering agent, was achieved.

    KEY WORDS sarmentosin; glutamic-pyruvic transaminase(GPT); total synthesis

    Sarmentosin(1) was isolated in 1978 by Fang et al[1] from the whole herb of Sedum sarmentosum Bunge which belongs to the family Crassulaceae. The herb is widely distributed in China and used for the treatment of hepatitis in folk medicine. Clinical trials showed that the herb had a significant effect in lowering the level of serum glutamic-pyruvic transaminase of the patients suffering from chronic virus hepatitis. Later on, sarmentosin was showen to be responsible for this effect[1,2]. Sarmentosin was also found to have immunomodulating activity[3]. Sarmentosin is a water soluble syrupy substance and its structure was elucidated by chemical and spectral methods as compound 1. ......

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