远志属两种植物的（口山）酮类成分研究
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摘要
远志(Radix Polygalae)为常用中药，来源于远志科远志属的多种植物，始载于《神农本草经》，被列为上品。具有安神益智，祛痰，消肿之功效。用于心肾不交引起的失眠多梦，健忘惊悸，神志恍惚，咳痰不爽，疮疡肿毒，乳房肿痛等。(口山)酮类化合物是远志属中含量比较丰富的一类成分，为了探讨其化学成分和药理活性之间的联系，为远志属植物的开发利用提供科学依据，并为其质量控制奠定基础，我们对远志属的两种植物：尾叶远志(Polygala caudata Rehd.et Wils.)和黄花倒水莲(P.fallax Hemsl.)中的(口山)酮类成分进行了化学成分及药理活性研究，并对远志属植物的分析方法作了初步的探讨。
采用多种色谱技术进行分离纯化，从尾叶远志根的乙醇提取物中分离得到27种成分，综合运用各种波谱学技术(包括IR、UV、ElMS、HREIMS、ESI-MS、TOF-MS、~1H NMR、~(13)C NMR、DEPT、~1H-~1H COSY、HMQC、HMBC和NOESY)，鉴定了25个化合物，其中6个为新化合物，7个为首次从远志属植物中分离，3个为首次从尾叶远志中分离。新化合物包括5个简单(口山)酮和1个(口山)酮苷，分别为：尾叶远志(口山)酮Ⅰ(2-羟基-1，6，7-三甲氧基(口山)酮，PC-X-01)，尾叶远志(口山)酮Ⅱ(1，4-二甲氧基-2，3-亚甲二氧基咄酮，PC-X-02)，尾叶远志(口山)酮Ⅲ(7-羟基-1，2-二甲氧(口山)酮，PC-X-03)，尾叶远志(口山)酮Ⅳ(1，3-二羟基-2，4-二甲氧基(口山)酮，PC-X-04)，尾叶远志(口山)酮Ⅴ(1，2，3，6-四甲氧基(口山)酮，PC-X-05)，尾叶远志苷B(1-甲氧基-7-羟基(口山)酮-2-O-β-D-吡喃葡萄糖苷，PC-X-17)。已知化合物鉴定为：1，3，7-三羟基(口山)酮(PC-X-06)，2，7-二羟基-1-甲氧基(口山)酮(PC-X-07)，优(口山)酮(1，7-二羟基(口山)酮，PC-X-08)，1-甲氧基-2，3-亚甲二氧基(口山)酮(PC-X-09)，7-羟基-1-甲氧基(口山)酮(PC-X-10)，3-羟基-1，2，4-三甲氧基(口山)酮(PC-X-11)，1，3，6-三甲氧基(口山)酮
Radix Polygalae, the root of Polygala tenuifolia Wild, or P. sibirica L. (Polygalaceae), is a well-known traditional Chinese medicine (TCM), which was used as a sedative, expectorant, and resuscitating agent. Other plants of Polygala genus were also widely used in folk of southern China. Previous chemical research demonstrated that plants of genus Polygala mainly contained xanthones, sapoins and oligosaccharides. In order to determinate the relationship between the chemical constituents and bioactivities, as well as develop a method for the quality control of Polygala L, the roots of P. caudata Rehd. et Wils. and P. fallax Hemsl. were subjected to phytochemical and pharmacological studies, the analytical methods based on HPLC and TLC technology were also established.
Twenty-seven compounds were isolated from the ethanol extracts of the roots of P. caudata by various column chromatographies. On the basis of spectral analysis (including IR, UV, EIMS, HREIMS, ESI-MS, TOF-MS, ~1H NMR, ~(13)C NMR, DEPT, ~1H-~1H COSY, HMQC, HMBC and NOESY), twenty-five structures of them were elucidated, of which six were new, seven were isolated from Polygala L. for the first time and three were first isolated from this plant. The structures of new compounds are elucidated as follows: Polycaudxanthone 1 (2-hydroxy-1, 6, 7-trimethoxyxanthone, PC-X-01), Polycaudxanthone II (1, 4-dimethoxy-2, 3-methyllenedioxyxanthone, PC-
采用多种色谱技术进行分离纯化，从尾叶远志根的乙醇提取物中分离得到27种成分，综合运用各种波谱学技术(包括IR、UV、ElMS、HREIMS、ESI-MS、TOF-MS、~1H NMR、~(13)C NMR、DEPT、~1H-~1H COSY、HMQC、HMBC和NOESY)，鉴定了25个化合物，其中6个为新化合物，7个为首次从远志属植物中分离，3个为首次从尾叶远志中分离。新化合物包括5个简单(口山)酮和1个(口山)酮苷，分别为：尾叶远志(口山)酮Ⅰ(2-羟基-1，6，7-三甲氧基(口山)酮，PC-X-01)，尾叶远志(口山)酮Ⅱ(1，4-二甲氧基-2，3-亚甲二氧基咄酮，PC-X-02)，尾叶远志(口山)酮Ⅲ(7-羟基-1，2-二甲氧(口山)酮，PC-X-03)，尾叶远志(口山)酮Ⅳ(1，3-二羟基-2，4-二甲氧基(口山)酮，PC-X-04)，尾叶远志(口山)酮Ⅴ(1，2，3，6-四甲氧基(口山)酮，PC-X-05)，尾叶远志苷B(1-甲氧基-7-羟基(口山)酮-2-O-β-D-吡喃葡萄糖苷，PC-X-17)。已知化合物鉴定为：1，3，7-三羟基(口山)酮(PC-X-06)，2，7-二羟基-1-甲氧基(口山)酮(PC-X-07)，优(口山)酮(1，7-二羟基(口山)酮，PC-X-08)，1-甲氧基-2，3-亚甲二氧基(口山)酮(PC-X-09)，7-羟基-1-甲氧基(口山)酮(PC-X-10)，3-羟基-1，2，4-三甲氧基(口山)酮(PC-X-11)，1，3，6-三甲氧基(口山)酮
Radix Polygalae, the root of Polygala tenuifolia Wild, or P. sibirica L. (Polygalaceae), is a well-known traditional Chinese medicine (TCM), which was used as a sedative, expectorant, and resuscitating agent. Other plants of Polygala genus were also widely used in folk of southern China. Previous chemical research demonstrated that plants of genus Polygala mainly contained xanthones, sapoins and oligosaccharides. In order to determinate the relationship between the chemical constituents and bioactivities, as well as develop a method for the quality control of Polygala L, the roots of P. caudata Rehd. et Wils. and P. fallax Hemsl. were subjected to phytochemical and pharmacological studies, the analytical methods based on HPLC and TLC technology were also established.
Twenty-seven compounds were isolated from the ethanol extracts of the roots of P. caudata by various column chromatographies. On the basis of spectral analysis (including IR, UV, EIMS, HREIMS, ESI-MS, TOF-MS, ~1H NMR, ~(13)C NMR, DEPT, ~1H-~1H COSY, HMQC, HMBC and NOESY), twenty-five structures of them were elucidated, of which six were new, seven were isolated from Polygala L. for the first time and three were first isolated from this plant. The structures of new compounds are elucidated as follows: Polycaudxanthone 1 (2-hydroxy-1, 6, 7-trimethoxyxanthone, PC-X-01), Polycaudxanthone II (1, 4-dimethoxy-2, 3-methyllenedioxyxanthone, PC-
引文
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