浙江七叶树种子中三萜皂苷成分的分离和鉴定*

目的:研究浙江七叶树Aesculus chinensis Bunge var.chekiangensis(Huet Fang)Fang种子中的化学成分。方法:采用大孔吸附树脂柱色谱、高效液相色谱等方法进行分离和纯化,根据化合物的谱学数据鉴定其结构。结果:从浙江七叶树种子的70%乙醇提取物中分离得到3个三萜皂苷类化合物,分别鉴定为七叶树皂苷(escins)IVe和IVh及七叶树皂苷(aesculuside)A。结论:这3个化合物皆为首次从浙江七叶树种子中分离得到。     

七叶树皂苷和熊果酸类化合物对HIV—1蛋白酶活性抑制作用的初步研究*

目的:探讨七叶树皂苷和熊果酸及其衍生物对HIV-1蛋白酶活性的抑制作用,探讨构效关系。方法:采用体外实验法,将待测化合物、HIV-1蛋白酶基质与HIV-1蛋白酶在37℃共温育,根据HIV-1蛋白酶对其基质的水解强度计算待测化合物对HIV-1蛋白酶活性的抑制作用。结果:七叶树总皂苷、七叶树皂苷-Ia和七叶树皂苷-Ib混合物、异七叶树皂苷-Ia和异七叶树皂苷-Ib混合物、七叶树皂苷-Ia、全乙酰化七叶树皂苷-Ia、七叶树皂苷-Ib、熊果酸和乙酰熊果酸在100μmol.L-1浓度对HIV-1蛋白酶活性的抑制率分别为86%,89.9%,50.8%,100%,74.6%,89.3%,100%和100%。七叶树皂苷-Ia、全乙酰化七叶树皂苷-Ia、七叶树皂苷-Ib、熊果酸和乙酰熊果酸对HIV-1蛋白酶活性抑制作用的IC50分别为35,35,50,8和13μmol.L-1。阳性对照药乙酰胃酶抑素在本实验条件下的IC50为0.30μmo.lL-1。在100μmol.L-1浓度,七叶树皂苷-IVc,-IVd,-IVe,-IVf,异七叶树皂苷-Ia,-Ib,-IIa,-IIb,原七叶树皂苷元,21β-O-巴豆酰基原七叶树皂苷元,21β-O-当归酰基原七叶树皂苷元,2α-羟基熊果酸和委陵菜酸对HIV-1蛋白酶活性的抑制率<50%。结论:七叶树总皂苷、七叶树皂苷-Ia和七叶树皂苷-Ib混合物、异七叶树皂苷-Ia和异七叶树皂苷-Ib混合物、七叶树皂苷-Ia、全乙酰化七叶树皂苷-Ia、七叶树皂苷-Ib、熊果酸和乙酰熊果酸对HIV-1蛋白酶活性有抑制作用,最强者为七叶树皂苷-Ia、熊果酸和乙酰熊果酸。     

酸枣仁皂苷E的结构鉴定酸枣仁皂苷E的结构鉴定

目的研究酸枣仁(Ziziphus jujuba Mill var. spinosa)的化学成分。方法用各种色谱方法分离酸枣仁的化学成分,用波谱(IR,UV,MS,NMR)方法鉴定结构。结果从酸枣的干燥种子中分离得到7个化合物,分别鉴定为酸枣仁皂苷E(1,jujuboside E),酸枣仁皂苷B(2,jujuboside B)及酸枣仁皂苷A(3,jujuboside A),白桦酯酸(4,betulic acid),硬脂酸(5,stearic acid),蔗糖(6,sucrose)和肌苷(7,inosine)。结论化合物1为新化合物,5,6和7为首次从酸枣仁中获得。     

胡芦巴的化学成分研究

从豆科胡芦巴属植物胡芦巴(Trigonella foerum-graecum L.)的干燥成熟种子中分离鉴定了9个化合物:其中5个为螺甾烷型甾体皂苷,分别为三角叶薯蓣皂苷(1a)和盾叶薯蓣皂苷A3(1b)的混合物(1),fenugreek saponin II(2),fenugreek saponin III(3),薯蓣皂苷(4);4个为黄酮类化合物即chrysoeriol-7-O-[6’’(E)-p-coumaroyl]-β-D-glucopyranoside(5),小麦黄素-7-O-β-D-葡萄糖苷(6),牡荆素(7),异荭草素(8)。其中化合物1a、1b、5为首次从葫芦巴属植物中分得。     

中华七叶树种子化学成分及生物活性研究进展

目的对中华七叶树种子的化学成分及生物活性研究进展进行综述。方法结合数据库检索及文献查阅,对其化学成分及生物活性进行系统分析和归纳总结。结果中华七叶树种子主要含有五环三萜皂苷类化合物26个、黄酮苷类化合物10个,具有抗炎消渗、抗肿瘤、抗病毒、抗血管生成和减肥等方面的生物活性。结论七叶皂苷Ⅰa和七叶皂苷Ⅰb,异七叶皂苷Ⅰa和异七叶皂苷Ⅰb是中华七叶树种子中含量最高的4种功效成分,其药理作用显著,临床应用前景广阔。     

桔梗中三萜皂苷的分离与结构鉴定

目的分离、鉴定桔梗[Platycodon grandiflorum(Jacq.)A.DC.]根中的皂苷类化学成分.方法采用乙醇提取、乙酸乙酯萃取、大孔树脂柱色谱、硅胶柱色谱及高效液相色谱等方法进行分离,得到5个化学成分,通过IR、MS、1H-NMR、13C-NMR等光谱法分析,鉴定化合物的结构.结果分离鉴定了5个三萜皂苷类化合物,它们分别为:deapio platycodin D(Ⅰ)、deapio platycodin D3(Ⅱ)、platycoside A (Ⅲ) 、platycoside F(Ⅳ)以及3-O-β-D-glucopyranosyl platycodigenin(Ⅴ).结论化合物Ⅰ～Ⅴ均为已知化合物,化合物Ⅴ是首次从该植物中分得的天然产物,也是首次从桔梗中分离得到的单糖链糖苷.     

七叶皂苷A、B的制备液相色谱法分离和结构确证

目的 建立制备型高效液相对β-七叶皂苷钠原料进行分离纯化制得七叶皂苷A(escin Ia)和七叶皂苷B(escin Ib)的方法.方法 采用制备色谱柱waters HRC18;以乙腈-1%醋酸(28∶72)为流动相;流速为42mL·min-1,检测波长为220nm.结果 用紫外、红外、质谱和核磁共振法确证结构,经分析型HPLC检查,纯度达98.0%以上.结论 该法可靠、准确,适合于七叶皂苷A、B的制备、分离、纯化.     

胡芦巴皂苷VIII的结构鉴定

目的　研究中国产胡芦巴Trigonellafoenum graecumL .种子的化学成分。方法　采用硅胶色谱柱进行分离 ,通过物理、化学和光谱学方法鉴定化合物的结构。结果　分离得到一甾体皂苷 ,命名为胡芦巴皂苷VIII,鉴定其结构为 2 6 O β D 吡喃葡糖基 2 5 (R) 5α 呋甾烷 2 0 ( 2 2 ) 烯 2α ,3 β ,2 6 三醇 3 O β D 吡喃木糖基 ( 1→ 6) β D 吡喃葡糖苷。结论　胡芦巴皂苷VIII为新化合物。     

胡芦巴皂苷Ⅷ的结构鉴定

目的研究中国产胡芦巴Trigonella foenum-graecum L.种子的化学成分.方法采用硅胶色谱柱进行分离,通过物理、化学和光谱学方法鉴定化合物的结构.结果分离得到一甾体皂苷,命名为胡芦巴皂苷VIII,鉴定其结构为26-O-β-D-吡喃葡糖基-25(R)-5α-呋甾烷-20(22)-烯-2α,3β,26-三醇-3-O-β-D-吡喃木糖基(1→6)-β-D-吡喃葡糖苷.结论胡芦巴皂苷VIII为新化合物.     

穿龙薯蓣中甾体皂苷的分离与鉴定

目的 研究穿龙薯蓣Dioscorea ni pponica Makin根茎的化学成分.方法 采用硅胶柱色谱、ODS柱色谱以及制备HPLC等手段进行分离纯化,通过理化性质和波谱学技术进行结构鉴定.结果 从正丁醇层中分离得到5个甾体皂苷类化合物,分别鉴定为纤细皂苷(1)、薯蓣皂苷(2)、伪原薯蓣皂苷(3)、甲基原纤细皂苷(4)、原薯蓣皂苷(5).结论 其中化合物4为首次从穿龙薯蓣中分离得到.     

酸枣仁皂苷D的分离及结构鉴定

目的研究酸枣仁Ziziphus jujuba Mill var. Spinosa (Bunge) Hu ex. H.F.的化学成分。方法用多种色谱方法分离化学成分、鉴定结构。结果从正丁醇部分分离得到5个化合物，其结构分别为：酸枣仁皂苷D(1, jujuboside D)，酸枣仁皂苷A(2, jujuboside A)，5,7,4′-三羟基黄酮醇-3-O-β-D-鼠李糖(1→6)-β-D-葡糖苷(3), 5,4′-二羟基-7-甲氧基黄酮-6-C-6-对香豆酰基-β-D-葡萄糖(1→2)-β-D-葡糖苷(4, 6-coumaroylspinosin)及苯丙氨酸(5)。结论化合物1为新化合物，化合物4作为阻转异构体存在为首次报道，化合物3和5为首次从酸枣仁获得。     

Identification of novel saponins from edible seeds of Japanese horse chestnut (Aesculus turbinata Blume) after treatment with wooden ashes and their nutraceutical activity

Natural seeds of Japanese horse chestnut (Aesculus turbinata Blume) contain large amounts of mixed triterpenoidal saponins called escins. Recent studies have shown that escins have several biological activities including anti-inflammatory action and inhibitory effects on the absorption of ethanol and glucose. For the edible utilization of the seeds, natural seeds are usually treated with wooden ashes to remove harshness. Here, we found the novel compounds derived from escins in the edible seeds after the food processing with wooden ashes. The instrumental analyses revealed the chemical structures of escins and the derivatives. These compounds are identified as four types of deacetylescins Ia, IIa, Ib, and IIb as well as two types of desacylescins I and II. To determine their biological activity, the purified compounds were tested for their potential nutraceutical activity. The oral glucose tolerance test in mice revealed that a single oral administration of the isolated components of deacetylescins at a dose of 100 mg/kg was clearly effective in attenuating the elevation of blood glucose levels. The inhibitory effects of escins and their derivatives were in the order of escins>deacetylescins>desacylescins. Moreover, we found the inhibitory activity of those compounds on pancreatic lipase. Escins were the most potent in inhibiting the enzyme activity, and followed by desacylescins and then deacetylescins. Taken together, our results suggest the potential usefulness of novel saponins including deacetylescins and desacylescins from edible seeds as novel sources for nutraceutical foods with anti-obese effects.     

毛节缬草的解剖构造观察

目的：观察黑龙江省毛节缬草的解剖构造，明确其鉴别特征，为进一步制定缬草的质量标准及开发利用提供科学依据。方法：石蜡切片技术。结果：明确了黑龙江省毛节缬草的根、根茎、茎和叶的显微特征。结论：这些显微特征可作为毛节缬草的鉴别手段。     

The microsomal N-oxidation of phentermine.

The microsomal N-oxidation of phentermine (Ia) to N-hydroxyphentermine (Ib) and to alpha,alpha-dimethyl-alpha-nitroso-beta-phenylethane (Ic was investigated. Maximum activities were obtained with microsomal (9000 g supernatant and microsomes) fractions of rabbit liver in the presence of an NADPH generating system. Incubation of Ia with hepatic washed microsomes from a phenobarbitone pretreated rabbit increased the formation of Ib and decreased that of Ic but the total amount of N-oxidized metabolites (i.e. Ib + Ic) was not affected. The ratio of the metabolically produced Ic to Ib but not the total amount of N-oxygenated metabolites varied greatly depending of the liver microsomal fractions used in the incubation mixtures of Ia; more Ib was produced from Ia using 9000 g supernatant and conversely, more Ic was formed using the washed microsomes of the same liver. The nitroso compound (Ic) was metabolically reduced to Ib and Ib to Ia by the hepatic 9000 g supernatant and soluble fraction; under the same conditions, washed microsomes had only limited reductive properties towards Ic and Ib. N-Hydroxyphentermine (Ib) was not metabolically oxidized to Ic when incubated with washed microsomes from rabbit liver. The use of known carbon-oxidation inhibitors showed that cytochrome P-450 is not involved in the incorporation of oxygen at the nitrogen centre of Ia. The metabolic characteristics and kinetic behavior of the microsomal N-oxidation of Ia supported a recently proposed mechanism explaining the independent formation of Ib and Ic from a common precursor resulting from metabolic N-oxidation of Ia.     

Identification of novel saponins from edible seeds of Japanese horse chestnut (Aesculus turbinata Blume) after treatment with wooden ashes and their nutraceutical activity

Natural seeds of Japanese horse chestnut (Aesculus turbinata Blume) contain large amounts of mixed triterpenoidal saponins called escins. Recent studies have shown that escins have several biological activities including anti-inflammatory action and inhibitory effects on the absorption of ethanol and glucose. For the edible utilization of the seeds, natural seeds are usually treated with wooden ashes to remove harshness. Here, we found the novel compounds derived from escins in the edible seeds after the food processing with wooden ashes. The instrumental analyses revealed the chemical structures of escins and the derivatives. These compounds are identified as four types of deacetylescins Ia, IIa, Ib, and IIb as well as two types of desacylescins I and II. To determine their biological activity, the purified compounds were tested for their potential nutraceutical activity. The oral glucose tolerance test in mice revealed that a single oral administration of the isolated components of deacetylescins at a dose of 100 mg/kg was clearly effective in attenuating the elevation of blood glucose levels. The inhibitory effects of escins and their derivatives were in the order of escins > deacetylescins > desacylescins. Moreover, we found the inhibitory activity of those compounds on pancreatic lipase. Escins were the most potent in inhibiting the enzyme activity, and followed by desacylescins and then deacetylescins. Taken together, our results suggest the potential usefulness of novel saponins including deacetylescins and desacylescins from edible seeds as novel sources for nutraceutical foods with anti-obese effects.     

Three new taxane diterpenoids from seeds of the Chinese yew, Taxus yunnanensis and T. chinensis var. mairei

Three new taxane diterpenoids were isolated from the seeds of the Chinese yew, Taxus yunnanensis Cheng et L. K. Fu and T. chinensis var. mairei Cheng et L. K. Fu. The structures were established as 1beta,10beta-dihydroxy-9alpha,13alpha-diacetoxy-5alpha-(3'-dimethylamino-3'-phenyl)-propionyloxytaxa-4(20),11-diene, 5alpha-hydroxy-9alpha,100,13alpha-triacetoxy-11(15-->1)abeotaxa-4(20),11-di-ene, and 5alpha,13alpha-dihydroxy-9alpha,10beta-diacetoxy-11 (15-->1 )abeo-taxa-4(20),11-diene on the basis of 1D, 2D NMR, and mass spectral analysis.     

藿香正气方超临界萃取物质谱及薄层色谱分析

目的考察SFE-CO2萃取法提取藿香正气方挥发性成分的可行性。方法用TLC和GC-MS检测。结果在与百秋李醇对照品色谱相应的位置上,显相同的紫红色斑点,在与厚朴酚、和厚朴酚对照品色谱相应的位置上,显相同颜色斑点。GC-MS能检测出厚朴酚、和厚朴酚,广藿香醇、广藿香酮成分。结论SFE-CO2萃取法提取藿香正气方中挥发性成分是可行的。