【作者】 胡君一；

【导师】 段宏泉；

【作者基本信息】 天津大学 ， 应用化学， 2006， 博士

【摘要】 青刺尖(Prinsepia utilis Royle),为蔷薇科扁核木属(Prinsepia)植物青刺尖的干燥茎叶,为我国云南的多民族的常用药。其性微寒,味苦。攻一切疮毒痈疽,有脓出头,无脓自消,散结核。本文对青刺尖叶的乙醇提取物进行有机化学成分研究。实验采用多种现代分离技术(包括快速层析法,凝胶色谱法和制备HPLC)对青刺尖乙酸乙酯提取部位进行分离,从青刺尖中分离得到13个化学单体,通过1H-NMR,13C-NMR,2D-NMR,高分辨质谱,单晶衍射等波谱解析方法鉴定了化合物的结构,其中2个为新的化合物,9个化合物为首次分离。落新妇[Astilbe chinensis (Maxim.)Franch. et Sav],为虎耳草科落新妇属植物,该植物根茎入药,具有清热解表,祛痰止咳,敛汗的功效。现代药理研究和临床应用已经证明其具有抗肿瘤、镇痛的药理作用。其化学成分主要为三萜和黄酮类。为寻找具有活性的化学单体,本文对落新妇根的石油醚、乙酸乙酯和正丁醇提取部位进行有机化学成分研究,从落新妇中分离得到25个化学单体,通过各种有机波谱解析方法鉴定了其中19个化合物的结构。其中8个为新的化合物,2个化合物为首次分离。本文对青刺尖乙酸乙酯提取物及部分单体化合物1-11进行了免疫抑制活性试验,结果表明单体化合物3-8具有较强的免疫抑制活性,其强度与地塞米松相当。落新妇抗肿瘤作用试验结果表明,落新妇石油醚提取物和正丁醇层提取物具有较强的抗肿瘤活性(Hela)。我们从落新妇分离并且鉴定的部分单体化合物中,化合物14对Hela细胞和L929细胞具有较高的抑制率,而其他化合物17、22、23、25对Hela细胞只显示一定的生长抑制作用;化合物25、27对L929细胞显示一定的生长抑制作用。更多还原

【Abstract】 Prinsepia utilis Royle has been used in folk medicine to treat various skin diseases, rheumatism, inflammation and leprosy in China and India. Many constituents have been reported, such as hydrocyanic acid and fatty oil. By repeated column chromatography, including Silica gel, Sephadex LH-20, Toyopearl HW-40C and preparative HPLC, two new compounds ((+)-(2R,3S)-2-chloro-3-hydroxy- 3-methyl-γ-butyrolactone (1), (+)-(2S,3S)-2-chloro-3-hydroxy-3-methyl-γ-butyrolac tone (2) and eleven known compounds (3-13) were isolated from the EtOAc extract of P. utilis, Their structures were identified by means of 1H-NMR, 13C-NMR , 2D-NMR spectra and X-ray. Known compounds 3-11 were isolated from this plant for the first time.Astilbe chinensis (Maxim.)Franch. et Sav has been used for headache, arthralgia, chronic bronchitis and stomachalgia in traditional Chinese medicine. Six flavonoids and four triterpenes have been isolated from this plant. Pharmacological studies indicated that the extracts of A. chinensis had antineoplastic and immunopotentiating activities. By repeated column chromatography, including Silica gel, Toyopearl HW-40C and preparative HPLC, twenty-five compounds were isolated from the EtOH extract of A. chinensis, and eight new compounds 15-19, 22-25 and two first isolated compounds 26, 27 were identified by means of 1H-NMR, 13C-NMR , 2D-NMR spectra and X-ray.Compounds 3-6 and 7 showed significant inhibitory effects on lymphocyte transformation, compared with the reference compound (dexamethasone). The P. E. and BuOH extracts of A. chinensis was revealed antitumor activities (Hela). Compound 14 exhibited significant cytotoxic activity to Hela and L929 Cell line in vitro. Compounds 17, 22, 23 and 25 showed positively activity to inhibit on Hela cell growth. Compounds 25 and 27 showed positively activity to inhibit on L929 cell growth.更多还原