文冠木化学成分的研究

目的研究文冠木Xanthoceras sorbifolia Bunge的化学成分。方法文冠木70%乙醇提取物采用硅胶、Sephadex LH-20、HP-20型大孔吸附树脂、MCI进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。结果从中分离得到17个化合物,分别鉴定为山柰酚(1)、槲皮素(2)、杨梅素(3)、柚皮素(4)、圣草酚(5)、二氢山柰酚(6)、二氢槲皮素(7)、二氢杨梅素(8)、5, 7, 3′, 4′, 5′-五羟基二氢黄酮(9)、(9S, 10R, 11E, 13R)-9, 10, 13-trihydroxyoctadec-11-enoic-acid(10)、原儿茶酸(11)、七叶内酯(12)、表没食子儿茶素(13)、表儿茶素(14)、epicatechin-5-O-β-D-glucopyranaoside(15)、β-谷甾醇(16)、胡萝卜苷(17)。结论化合物1、4～6、9～12、15均为首次从该植物中分离得到。     

文冠果果柄的化学成分研究

目的 研究文冠果果柄的化学成分,寻找新的药用部位.方法 采用大孔树脂、硅胶柱色谱分离化学成分,通过理化性质及波谱分析等方法进行结构鉴定.结果 从文冠果果柄70%乙醇提取物中分离鉴定了6个化合物,分别为21-当归酰基-24-羟基-R1-barrigenol(21-angeloyl-24-hydroxy-R1-barrigenol,Ⅰ)、23-羟基白桦脂酸(23-hy-droxybetulinic acid,Ⅱ)、23-羟基白桦脂酸-3-咖啡酸酯(3β,23-dihydroxy-lup-20(29)en-28-oic acid-3-caffeate,Ⅲ)、22,23-二氢-a-菠甾酮(22,23-dehydroxy-a-chondrillasterone,Ⅳ)、3-oxotirucalla-7,24-dien-21-oic(Ⅴ),a-菠菜甾醇-3-O-β-D-吡喃葡萄糖苷(spinasterol-3-O-β-D-gIucopyranoside,Ⅵ).结论 化合物Ⅰ为-新天然产物,Ⅱ～Ⅳ.     

文冠果叶化学成分的研究

目的:本试验对文冠果叶化学成分进行研究,为了扩展药用部位及寻求新药源.方法:利用硅胶和Sephadex LH-20等柱色谱分离化合物,通过其理化性质和UV、IR、1H-NMR、13C-NMR等方法进行结构鉴定.结果:分别从文冠果叶的正丁醇相和乙酸乙酯相萃取物中分离得到3种黄酮类化合物和2种香豆素类化合物,并鉴定为:杨梅树皮苷(1)、槲皮素-3-O-鼠李糖苷(2)、芦丁(3)、7-羟基香豆素(4)、秦皮素(5).结论:化合物(2)是首次从文冠果植物中分离得到的,化合物(3)、(4)、(5)是首次从文冠果叶中分离得到.     

Inhibitory effects of Sudanese plant extracts on HIV-1 replication and HIV-1 protease

Forty-eight methanol and aqueous extracts from Sudanese plants were screened for their inhibitory activity on viral replication. Nineteen extracts showed inhibitory effects on HIV-induced cytopathic effects (CPE) on MT-4 cells. The extracts were further screened against HIV-1 protease (PR) using an HPLC assay method. Of the tested extracts, the methanol extracts of Acacia nilotica (bark and pods), Euphorbia granulata (leaves), Maytenus senegalensis (stem-bark) and aqueous extracts of A. nilotica (pods) and M. senegalensis (stem-bark) showed considerable inhibitory effects against HIV-1 PR. Inhibitory principles were isolated from M. senegalensis and their activities were also discussed.     

文冠木化学成分研究

目的:系统研究文冠木化学成分,为进一步阐明其抗炎活性成分提供依据.方法:采用硅胶柱、Sephadex LH-20、MCI柱等方法分离文冠木的化学成分,通过LC-MS-MS、1H-NMR、13C-NMR、CD等波谱数据进行结构鉴定.结果:共分得9个黄酮类化合物,分别为(2R,3R)-双氢杨梅树皮素(Ⅰ)、杨梅树皮素(Ⅱ)、槲皮素(Ⅲ)、儿茶精(Ⅳ)、没食子儿茶精(Ⅴ)、(2R,3R)-3,3′,5,5′,7-五羟基二氢黄酮(Ⅵ)、(2S)-3′,4′,5,5′,7-五羟基二氢黄酮(Ⅶ)、(-)表没食子儿茶精(Ⅷ)、proanthocyanidin A2(Ⅸ).结论:化合物Ⅰ、Ⅳ、Ⅵ、Ⅶ为首次从本属植物中分离得到.     

Cytotoxic acylated triterpene saponins from the husks of Xanthoceras sorbifolia

Four new oleanane-type triterpene saponins, xanifolia-Y0 (1), xanifolia-Y2 (2), xanifolia-Y3 (3), and xanifolia-Y7 (4), were isolated from the husks of Xanthoceras sorbifolia along with two known analogues, xanifolia-Y8 (5) and xanifolia-Y10 (6). The structures of 1-4 were determined by spectroscopic data interpretation and chemical degradation. Compounds 1-6 were evaluated for their cell-growth inhibition activity toward human ovarian cancer cells (OVCAR3) by a MTT assay, and the IC50 values ranged from 4 to 13 microM. On the basis of the results obtained, it is concluded that a C-3 trisaccharide with a galactose and acylation with an angeloyl group at both C-21 and C-22 are important for cell inhibition activity for this class of compounds.     

不同产地蒙药文冠木中表儿茶素的含量比较

目的对不同产地蒙药文冠木中表儿茶素的含量进行比较研究,建立文冠木中表儿茶素的含量测定方法与质量评价标准。方法流动相为乙腈-0.04%磷酸(13:87);检测波长为280nm;流速1ml·min-1;柱温28℃。结果表儿茶素在0.411~8.22μg范围内与峰面积呈良好线性关系(r=0.9999),平均回收率为100.93%,RSD=1.17%,不同产地文冠木中表儿茶素含量在0.445~2.215%之间,其中以内蒙古鄂尔多斯产含量最高,以购置于安徽亳州(产地:安徽)产含量最低。结论该方法精密度、重复性、稳定性良好,方法准确、可靠,可为蒙药文冠木药材质量控制与质量评价提供实验依据。     

文冠果种皮的化学成分研究

目的研究文冠果Xanthoceras sorbifolia Bunge种皮的化学成分,为文冠果综合开发利用打下科学基础。方法采用多种分离技术对文冠果种皮甲醇提取物的醋酸乙酯部位分离纯化,根据其理化性质和光谱数据进行结构鉴定。结果从文冠果种皮中分离鉴定了7个化合物:(1)十九烷酸、(2)二十一烷酸、(3)豆甾醇、(4)豆甾醇乙酸酯、(5)豆甾-7-烯-3β-醇、(6)二十四烷酸、(7)胡萝卜苷。结论化合物1~4为首次从本属植物中分得,5~7为首次从文冠果种皮中得到。     

文冠果种仁粕中的一个新香豆素

Objective: To study the coumarin from the seeds oil leavings of Xanthoceras sorbifolia.Methods: The chemical constituents were isolated and purified by combination of silica gel, macroporous resin, Sephadex LH-20, and ODS column chromatography. Their structures were elucidated by spectral and chemical methods. The cytotoxicity of the new compound against 10 selected human cancer cell lines was assayed.Results: Five comarins were isolated and identified as fraxetin-7-O-β-D-[6'-(3"–hydroxyl–3"-methylglutaryl)] glucopyranoside(1), fraxoside(2), fraxetin(3), scopoline(4), and esculetin(5), respectively.Conclusion: Compound 1 is a new compound. Unfortunately, this compound exhibited no cytotoxicity with tested cell lines.     

文冠果果壳提取物对学习记忆障碍的改善作用

目的研究文冠果果壳乙醇提取物、总皂苷及ST-n-2对学习记忆障碍的影响,并初步探讨其作用机制。方法采用跳台法观察东莨菪碱和亚硝酸钠所致学习记忆障碍小鼠的学习记忆能力,八臂放射状迷路法观察( )-MK-801致学习记忆障碍大鼠的学习记忆能力。结果文冠果果壳乙醇提取物、总皂苷及ST-n-2均显著改善东莨菪碱所致的记忆获得障碍和亚硝酸钠所致的记忆巩固障碍,文冠果果壳乙醇提取物显著改善( )-MK-801所致的工作记忆和参照记忆障碍。结论文冠果果壳乙醇提取物、总皂苷及ST-n-2对学习记忆障碍均有显著改善作用,其作用机制可能与增强中枢胆碱能神经系统及谷氨酸能神经系统功能、抗脑组织耗氧损伤有关;总皂苷是文冠果果壳改善记忆障碍的有效部位,ST-n-2是其主要有效成分之一。     

HIV-1 protease and HIV-1 integrase inhibitory substances from Eclipta prostrata

The bioassay-guided fractionation for anti-HIV-1 integrase activity led to the isolation of six compounds from the whole plant extract of Eclipta prostrata extract. They were identified as 5-hydroxymethyl-(2,2':5',2')-terthienyl tiglate (1), 5-hydroxymethyl-(2,2':5',2')-terthienyl agelate (2), 5-hydroxymethyl-(2,2':5',2')-terthienyl acetate (3), ecliptal (4), orobol (5) and wedelolactone (6). Of these, compound 6 showed the highest activity against HIV-1 integrase (IN) with an IC50 value of 4.0+/-0.2 microm, followed by compound 5 (IC50=8.1+/-0.5 microm), whereas the four terthiophene compounds (1-4) were inactive (IC50>100 microm). Regarding HIV-1 protease (PR) inhibitory activity, compound 1 exhibited appreciable activity against HIV-1 PR with an IC50 of 58.3+/-0.8 microm, followed by compound 4 (IC50=83.3+/-1.6 microm) and compound 3 (IC50=93.7+/-0.8 microm), while compounds 2, 5 and 6 were inactive against HIV-1 PR (IC50>100 microm). This is the first report of anti-HIV-1 IN activities for wedelolactone (6), a coumarin derivative, and orobol (5), an isoflavone derivative. This study supports the use of E. prostrata in AIDS patients, which is in accord with its traditional use by Thai traditional doctors for curing blood related diseases.     

文冠果的化学成分与生物活性研究进展

文冠果为我国特有的珍稀木本油料作物,是绿化、食用、药用和制作生物燃料油的重要木本油料树种,近年来广泛受到学术界关注.其果仁、果皮、枝叶等药用部位富含三萜、黄酮、香豆素、甾醇等化学成分.现代医学研究表明,文冠果具有抗炎、抗肿瘤、抑制HIV蛋白酶、促进NGF介导的神经突触生长、改善学习记忆等药理作用和生物活性.对近年来有关文冠果不同药用部位的化学成分、生物活性、检测方法等方面的研究进展进行了综述.     

文冠果种皮制备木糖工艺及其生物活性初步研究

目的:以文冠果种皮醇提残渣为原料,经稀硫酸高温短时水解、中和、脱色、低温结晶,分离木糖、低聚木寡糖糖浆。方法:在单因素实验的基础上,通过正交试验法研究水解温度(A)、硫酸浓度(B)、料液比(C)、水解时间(D)对木糖得率的影响。结果:文冠果种皮渣水解制备木糖的最佳工艺条件为硫酸浓度1.5 mol·L-1,料液比1∶5,温度90℃,水解时间5 h,该条件下木糖的的产量最高可达文冠果种皮干燥基质量的11%,工艺条件稳定;活性实验研究显示,以文冠果种皮制备的木糖具有良好的促乳酸菌生长作用。结论:文冠果种皮是适合制备木糖的原料,同时有助于提高文冠果产业的经济附加值,具有开发前景。     

文冠果叶多糖超声辅助提取工艺及其药效学初步研究

目的:以文冠果叶为原料,研究超声辅助法对文冠果叶多糖提取得率的影响。在此基础上,对文冠果叶多糖抗癌、抗氧化活性进行初步研究。方法:单因素试验基础上采用正交试验法研究温度、料液比、超声功率对文冠果叶多糖得率的影响,进一步优化超声提取的工艺;四甲基偶氮唑盐比色法(MTT)研究文冠果叶多糖对人肝癌细胞HepG2增殖的抑制作用;抗氧化活性通过DPPH·清除实验检测。结果:文冠果叶多糖的最佳提取工艺为提取温度90℃,料液比为1∶20,超声功率90 W,超声时间30 min,在该条件下文冠果叶多糖的提取率可达17.90%;活性研究显示,在浓度2.5 mg·m L~(-1)时,文冠果叶多糖对人肝癌细胞Hep G2增殖抑制率为20.21%;浓度为0.2 mg·m L~(-1)时,对DPPH·自由基清除率高达90.78%。结论:超声辅助提取文冠果叶多糖与传统的水热提取法相比,提取时间短、收率高;文冠果叶多糖具有一定的抗肝癌活性及良好的抗氧化活性,具有开发为药品及化妆品等相关产品的潜能。     

Inhibitory effects of Korean medicinal plants and camelliatannin H from Camellia japonica on human immunodeficiency virus type 1 protease

To identify substances with anti-human immunodeficiency virus (HIV) activity in traditional medicines, 101 extracts of Korean medicinal plants were screened for their inhibitory effects on HIV type 1 protease (PR). The enzyme activity was determined by HPLC. Of the extracts tested, strong inhibitory effects were observed in the acetone extracts of the pericarp and leaves of Camellia japonica, the water extract of the leaves of Sageretia theezans and the methanol extract of the aerial part of Sophora flavescens. Camelliatannin H from the pericarp of C. japonica, showed a potent inhibitory activity on HIV-1 PR with IC(50) of 0.9 microM.     

Antitubercular constituents from the stem wood of Cinnamomum kotoense

Five new compounds, kotolactone A (1), kotolactone B (2), secokotomolide (3), kotodiol (4), and 2-acetyl-5-dodecylfuran (5), and 36 known compounds have been isolated from the stem wood of Cinnamomum kotoense. The structures of these new compounds were determined by means of spectroscopic analysis. The known butanolides, isoobtusilactone A (6) and lincomolide B (7), showed in vitro antitubercular activities with MIC values of 22.48 and 10.16 microM, respectively, against Mycobacterium tuberculosis 90-221387.