杨峻山, 罗淑荣, 沈秀兰, 李源湘. 苦木生物碱的化学研究J. 药学学报, 1979, 14(3): 167-177.
引用本文: 杨峻山, 罗淑荣, 沈秀兰, 李源湘. 苦木生物碱的化学研究J. 药学学报, 1979, 14(3): 167-177.
Yang Junshan, Luo Shurong, Shen Xiulan , Li Yuanxiang, . CHEMICAL INVESTIGATION OF THE ALKALOIDS OF KU-MU PICRASMA QUASSIOIDES (D. DON) BENN.J. Acta Pharmaceutica Sinica, 1979, 14(3): 167-177.
Citation: Yang Junshan, Luo Shurong, Shen Xiulan , Li Yuanxiang, . CHEMICAL INVESTIGATION OF THE ALKALOIDS OF KU-MU PICRASMA QUASSIOIDES (D. DON) BENN.J. Acta Pharmaceutica Sinica, 1979, 14(3): 167-177.

苦木生物碱的化学研究

CHEMICAL INVESTIGATION OF THE ALKALOIDS OF KU-MU PICRASMA QUASSIOIDES (D. DON) BENN.

  • 摘要: 苦木(Picrasma quassioides (D.Don)Benn.)总生物碱的各种制剂在临床上证明是有效的抗菌消炎药物。为了阐明其有效成分,对其生物碱进行了研究,自其茎心的乙醇提取物通过硅胶和氧化铝柱层析以及制备性薄层层析,分离得到七个生物碱,根据光谱分析,物理化学常数的测定和衍生物的制备,其中四种鉴别为已知的生物碱:1-甲氧甲酰-β-咔巴啉(Ⅱ),4.5-二甲氧基铁屎米酮(Ⅳ),铁屎米酮(Ⅴ),4-甲氧基-5-羟基铁屎米酮(Ⅵ)。另外三种为新的天然产物,证明其结构为1-乙氧甲酰-β-咔巴啉(Ⅰ),1-甲酰-β-咔巴啉(Ⅲ)和1-乙烯基-4.8-二甲氧基-β-咔巴啉(Ⅶ)。体外抗菌实验表明碱(Ⅱ),(Ⅳ),(Ⅵ)和(Ⅶ)为有效成分。其他生物碱因量少未进行抗菌实验。

     

    Abstract: Some preparation of the total alkaloids of Ku-Mu (Picrasma quassioides (D. Don) Benn.) was Shown to have antibacterial actiyity in clinical trial. For the exploration of the active principles, the present paper deals with the studies of the alkaloids of this medicinal plant. From an alcohol extract of heartwood of Ku-Mu seven alkaloids were isolated through silica gel and alumina column chromatography as well as preparative thin layer chromatography. Beside the known alkaloids 1-carbomethoxy-β-carboline (Ⅱ), 4,5-dimethoxycanthin-6-one (Ⅳ), canthin-6-one (Ⅴ), and 4-methoxy-5-hydroxycanthin-6-one (Ⅵ), three new alkaloids, named Kumujian A, Kumujian C, and Kumujian C, were ident fied as 1-carboethoxy-β-carbotine (Ⅰ), 1-formyl-β-carboline(Ⅲ) and 1-vinyl-4,8-dimethoxy-β-carboline (Ⅶ), respectively. In virto screening of the above alkaloids demonstrated that 1-carbomethoxy-β-carboline (Ⅱ), 4,5-dimethoxycanthin-6-one (Ⅳ), 4-methoxy-5-hydroxycanthin-6-one (Ⅵ) and 1-vinyl-4,8-dimethoxy-β-carboline (Ⅶ) exhibited inhibition against Staphylococcus aureus and its drug-resistant strains. Tests for the antibacterial activity of three other alkaloids were hampered by scarcity of material.

     

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