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药用植物委陵菜和糙苏生物活性成分的研究
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摘要
中药委陵菜(Potentilla chinensis B)为蔷薇科(Rosaceae)委陵菜属(Potentila)植物委陵菜的全草,广泛分布于我国大部分地区,为常用中草药。委陵菜性寒,味苦,具有清热解毒,凉血止痢的作用。常用于治疗赤痢腹痛、久痢不止、痔疮出血、疮痈肿毒等。本文对委陵菜全草的乙醇提取物进行有机化学成分研究,采用多种现代分离技术(包括硅胶柱色谱,快速层析柱色谱,凝胶柱色谱和制备HPLC)对委陵菜进行研究,对其中具有抗糖尿病作用的有效部位进行了追踪,并对抗糖尿病作用进行了研究。从委陵菜乙醇提取物中分离得到25个单体化合物,通过1H-NMR,13C-NMR,2D-NMR,高分辨质谱等波谱解析方法鉴定了这些化合物的结构。其中黄酮类化合物20具有较强抗糖尿病作用,化合物1, 3~23为首次从该植物中分离得到的化合物。
     糙苏(Phlomis umbrosa Turcz)为唇型科(Labiatae)糙苏属(Phlomis)植物,为土家族民间常用药物。糙苏全草入药,能散风、解毒,主治感冒、慢性支气管炎;根能清热消肿,主治疮痈肿毒、跌打损伤;在鄂西土家族民间糙苏根作为抗风湿药物被广泛应用。文献报道从糙苏中分离得到的化合物主要为环烯醚萜苷类和苯乙醇苷类。为寻找具有良好生物活性的化学单体,本文对糙苏根的石油醚、乙酸乙酯和正丁醇提取部位进行有机化学成分研究。从糙苏中分离得到50个化学单体,通过各种有机波谱解析方法鉴定了其中40个化合物的结构,其中化合物26~37, 45~47, 54是未见文献报道的新化合物,化合物40~44, 48~51, 62~65为首次从本植物中分离得到的化合物。
     本文对委陵菜和糙苏中分离得到的部分单体化合物进行了抗肿瘤细胞活性试验,结果表明一些单体化合物对肿瘤细株具有一定的抑制作用,部分化合物表现出较强的作用,有必要进行进一步的研究。
Potentilla chinensis Bge (Rosaceae) is widely distributed in most place of China. As a folk medicine, it has been used to reduce swelling and staunch bleeding, and has anti-inflammatory and detoxification properties. Our previous study showed that the extracts from P. chinensis revealed significant anti-diabietic activities. In order to search the anti-diabietic constituents from natural source, we began to study the chemical constituents from P. chinensis. By repeated column chromatography, including Silica gel, Sephadex LH-20, Toyopearl HW-40C and preparative HPLC, 25 compounds were separated from the EtOH extract of P. chinensis. Their structures were identified by means of 1H-NMR, 13C-NMR, 2D-NMR spectra. Compounds 1, 3~23 were isolated from this plant for the first time. Compound 20 revealed significant anti-diabietic activity.
     Phlomis umbrosa (Turcz) has been used for headache, arthralgia, chronic bronchitis and stomachalgia in traditional Chinese medicine. Previous studies on this plant led to the isolation of iridoids and phenylethanoids. To find new substance make effective use of this plant, phytochemistry studies were carrying out on the EtOH extract of this plant. By repeated column chromatography, including Silica gel, Toyopearl HW-40C and preparative HPLC, fifty compounds were isolated from the EtOH extract of P. umbrosa, the structures of 40 compounds were elucidated by means of 1H-NMR, 13C-NMR, 2D-NMR spectra and X-ray. Among them, compounds 26~37, 45~47, 54 were new compounds, compounds 40~44, 48~51, 62~65 were separated from the plant for the first time.
     The anti-tumor bioactivities on the compounds were screened by cytotoxity effect with Hela and L929 cell line. Some compounds revealed significant inhibitory effect on Hela and L929 cell line.
引文
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