桐花树化学成分的研究

目的 研究桐花树的化学成分.方法 采用硅胶柱色谱法分离纯化,薄层色谱及波谱法鉴定结构.结果 从桐花树茎皮的乙醇提取物分离得9个化合物,结构鉴定为α-菠甾醇(Ⅰ)、豆甾醇(Ⅱ)、齐墩果酸(Ⅲ)、原报春花素A(Ⅳ)、没食子酸甲酯(Ⅴ、化合物Ⅵ可能为α-菠甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅵ)和△5,22豆甾醇-3-O-β-D-吡喃葡萄糖苷(Ⅵb)的混合物、正三十四烷醇(Ⅶ)、正三十二烷醇(Ⅷ)、没食子酸(Ⅸ).结论 化合物Ⅴ、Ⅵ、Ⅶ、Ⅷ为首次从桐花树茎皮中分离得到.     

沙戟化学成分研究

目的 研究新疆产沙戟全草的化学成分.方法 反复硅胶柱色谱,薄层色谱,凝胶柱色谱,波谱分析技术和理化常数对照.结果 分离得到8个化合物,分别鉴定为木犀草素(Ⅰ),阿曼托黄素(Ⅱ),短叶苏木酚(Ⅲ),短叶苏木酚酸乙酯(Ⅳ),7-O-(6″-反式-对桂皮酰基)-β-D-半乳糖芹菜素苷(Ⅴ),木犀草素-7-O-β-D-芦丁糖苷(Ⅵ),没食子酸(Ⅶ)和没食子酸乙酯(Ⅷ).结论 上述化合物均首次从沙戟属中分离得到.     

翻白草抗菌活性成份的研究

首次从翻白草中分离出九个单体化合物,其中七种经理化性质和光谱数据鉴定为富马酸(Fumaric acid)Ⅰ,没食子酸(Gallic acid)Ⅱ,槲皮素(Quercetin)Ⅲ,原儿茶酸(Protocatechuic acid)Ⅳ,柚皮素(Naringenin)V,山柰素(Kaempferol)Ⅵ和间苯二酸(m-Phthalic acid)Ⅷ。以上七种均系首次从翻白草中分离出的已知化合物,其中结晶Ⅰ、Ⅴ和Ⅷ均系首次从委陵菜属植物中分离得到。抑菌实验表明:结晶Ⅰ、Ⅱ、Ⅲ、Ⅳ、Ⅴ、Ⅶ和Ⅷ对福氏和志贺氏痢疾杆菌均具有不同程度的抑制作用。其中尤以Ⅱ和Ⅲ的抑菌活性最强,最低抑茵浓度分别为59和37ppm/ml。此外Ⅱ与Ⅲ,Ⅳ,Ⅴ之间都呈明显的协同作用。     

穿山甲化学成分的研究

自中药穿山甲(Manis pentadactyla Linnaeus)中分离得到七个化合物(Ⅰ～Ⅶ),分别鉴定为硬脂酸(Ⅰ)、胆甾醇(Ⅱ)、二十三酰丁胺(Ⅲ)、碳原子数为26和29的二个脂肪族酰胺(Ⅳ～Ⅴ)、L-丝-L-酪环二肽[cyclo-(L-seryl-L-tyrosyl)](Ⅵ)和D-丝-L-酪环二肽[cyclo-(D-seryl-L-tyrosyl)](Ⅶ),其中Ⅵ和Ⅶ为非对映立体异构体(diastereoisomers),系首次从天然物中得到,化合物Ⅶ为一新的化合物。化合物Ⅵ和Ⅶ的分子结构均经X-衍射方法得到证明。穿山甲含18种微量元素,其水溶液含16种游离氨基酸。分析比较炮制前后的穿山甲化学成分,表明两者基本相同。     

毛脉酸模内生真菌RGT-S11菌丝体化学成分研究

研究毛脉酸模(Rumex gmelini Turcz.)内生真菌RGT-S11菌丝中的化学成分。运用溶剂萃取、硅胶柱色谱、ODS反相柱色谱、Sephadex LH-20柱色谱、制备液相等方法进行分离纯化,根据理化性质、NMR数据鉴定化合物的结构。结果:分离得到7个单体化合物:苯甲酸(Ⅰ),棕榈酸(Ⅱ),麦角甾-5,7,22-三烯-3β-醇(Ⅲ),油酸(Ⅳ),腺苷(Ⅴ),鸟苷(Ⅵ),没食子酸(Ⅶ)。以上化合物均为首次从内生真菌RGT-S11菌丝中分离得到。     

大花红景天的化学成分研究

目的研究景天科大花红景天的根和根茎中的化学成分。方法采用柱色谱法分离纯化,通过光谱数据鉴定其结构。结果从大花红景天的根和根茎乙醇提取物的石油醚部位、乙酸乙酯部位和正丁醇部位中分离得到12个化合物,分别鉴定为大花红天素(Ⅰ)、胡萝卜甾醇(Ⅱ)、草质素-7-氧-α-L-吡喃鼠李糖苷(Ⅲ)、阿魏酸二十八烷醇酯(Ⅳ)、酪醇(Ⅴ)、红景天苷(Ⅵ)、没食子酸(Ⅶ)、β-谷甾醇(Ⅷ)、正二十六烷酸(Ⅸ)、正二十六烷醇(Ⅹ)、正十八烷酸(Ⅺ)和十九烷(Ⅻ)。结论化合物Ⅱ、Ⅳ、Ⅸ、Ⅹ、Ⅺ、Ⅻ为首次从该植物中分离得到。     

肿节风化学成分研究

目的研究中药肿节风化学成分,为阐明其抗肿瘤有效成分提供依据。方法利用聚酰胺、Sephadex LH-20,Lipophilic sephadex LH-20柱色谱进行分离,根据化合物的理化性质和光谱数据(IR,UV,1H-NMR,13C-NMR)鉴定其结构。结果从肿节风中分离得到7个化合物,分别鉴定为:迷迭香酸甲酯(Ⅰ),迷迭香酸(Ⅱ),丹参素甲甲酯(Ⅲ),咖啡酸(Ⅳ),3,4-二羟基苯甲酸(Ⅴ),异秦皮啶(Ⅵ),邻苯二甲酸二丁酯(Ⅶ)。结论化合物Ⅰ、Ⅱ、Ⅲ、Ⅳ、Ⅶ为首次从本属植物中得到。     

山荷叶中木脂素成分的研究

从陕西产山荷叶(Diphylleia sinensis Li.)根茎中分得9个木脂素和1个黄酮化合物,通过光谱分析证明化合物Ⅸ为新木脂素,即苦鬼臼素-1-乙基醚(picropodophyllin-1-ethyl ether),其它化合物分别为鬼臼毒素(podophyllotoxin,Ⅰ)、异苦鬼臼酮(isopicropodophyllone,Ⅱ)、去氢鬼臼毒素(dehydropodophyllotoxin,Ⅲ)、山荷叶素(diphyllin,Ⅳ)、苦鬼臼素(picropodophyllin,Ⅴ)、鬼臼酯酮(podophyllotoxone,Ⅵ)、4′-去甲基鬼臼毒素(4′-demethylpodophyllotoxin,Ⅶ)、苦鬼臼素葡萄糖甙(picropodophyllin slucoside,Ⅷ)和山奈酚(kaempferol,Ⅹ)。其中化合物Ⅱ,Ⅵ,Ⅶ和Ⅷ为首次从山荷叶属植物中分得。     

藏药波棱瓜子乙酸乙酯部位化学成分研究

目的:研究藏药波棱瓜子乙酸乙酯部位的化学成分.方法:采用硅胶柱层析法进行分离纯化,根据化合物的理化性质和波谱数据进行结构鉴定.结果:从该部位分离得到了7个单体化合物,其结构分别为豆甾醇(Ⅰ)、波棱内酯B(Ⅱ)、波棱内酯A(Ⅲ)、波棱酮(Ⅳ)、尿嘧啶(Ⅴ) 、herpetotriol(Ⅵ)、菠甾醇葡萄糖苷(Ⅶ).结论:化合物Ⅶ为首次从该植物中分得.     

新疆鼠尾草中酚酸类化学成分的研究

目的 研究新疆鼠尾草的酚酸类化学成分.方法 采用多种柱色谱技术对化合物进行分离纯化,根据理化数据及波谱数据鉴定化合物的结构.结果 从新疆鼠尾草中分离得到7个化合物,分别鉴定为:丹参素(Ⅰ)、丹参素甲酯(Ⅱ)、原儿茶醛(Ⅲ)、原儿茶酸(Ⅳ)、咖啡酸(Ⅴ)、迷迭香酸(Ⅵ)、丹酚酸K(Ⅶ).结论 化合物Ⅰ、Ⅱ、Ⅲ、Ⅳ、Ⅴ为首次从新疆鼠尾草中分离得到.     

Extraction and cleanup methods for analysis of phenolic and neutral organohalogens in plasma

A method for the analysis of potential endocrine-disrupting compounds, such as phenolic halogenated compounds (e.g., chlorinated and brominated phenols) and hydroxylated PCBs, in blood plasma is presented. Neutral halogenated compounds, specifically brominated diphenyl ethers and PCBs, are also included in the evaluation. An efficient denaturation and extraction step is described, and three methods for lipid removal are evaluated. The latter includes a nondestructive method based on high-resolution gel permeation chromatography (HR-GPC), a newly developed silica gel/sulfuric acid column, and lipid removal by sulfuric acid treatment. Recoveries, based on gas chromatography with an electron capture detector (GC-ECD), were between 70 and 90% for most of the studied compounds. The recoveries of phenolic compounds were generally slightly lower than those of the neutral compounds. The sulfuric acid treatment and silica gel/sulfuric acid column gave the highest yields for acid stable compounds, although a few target compounds were lost during that treatment and all compounds were recovered with the HR-GPC method.     

血根碱、白屈菜红碱离子对化合物的体外抗菌活性研究

目的通过对血根碱离子对化合物、白屈菜红碱离子对化合物的体外抗菌活性研究,寻找具有潜在开发价值的抗菌药物。方法将血根碱、白屈菜红碱与多种有机酸制备成离子对化合物,采用试管稀释法和琼脂平板扩散法测定最低抑菌浓度(MIC)和最小杀菌浓度(MBC),结合抑菌圈实验,比较制备前后化合物的抗菌效果。结果血根碱与苯甲酸、乳酸、富马酸等有机酸形成离子对化合物之后抗菌活性增强,白屈菜红碱与乙酸、丙酸形成离子对化合物之后抗菌活性增强。结论一些结合小分子有机酸形成的离子对化合物显示出良好的抗菌效果,将生物碱制备为离子对化合物的方法为寻找新的抗菌药物提供了一种思路。     

Nalidixic acid prodrugs: Amides from amino acid ester and nalidixic acid

Amides from amino acid ester and nalidixic acid were synthesized. The solubility characteristics and partition coefficient of the compounds were studied. The hydrolysis of the compounds was studied in the simulated gastric fluid and simulated intestinal fluid. Some compounds showed better antibacterial activity than nalidixic acid.     

全反式维甲酸-正丁酸（丙戊酸）前体药物的设计、合成及抗肿瘤活性研究

目的合成全反式维甲酸（ATRA）的前体药物，增强ATRA对急性早幼粒白血病（APL）细胞的分化诱导作用。方法以乙二醇、对苯二酚、乙醇胺及乙二胺等为连接物，通过酯键和酰胺键将分化诱导剂ATRA与组蛋白去乙酰酶（mAC）抑制剂正丁酸、丙戊酸连接起来，形成前体药物。结果合成了13个ATRA与正丁酸或丙戊酸相连接的前体药物，化合物的结构经^1H-NMR、MS和IR确证。结论考察部分化合物对急性早幼粒细胞白血病细胞株NB4的生长抑制作用和对急性早幼粒白血病（APL）细胞分化诱导作用，初步的药理实验结果表明，ATRA与丙戊酸通过酰胺键连接时，对NB4细胞分化诱导能力显著增加。     

Mechanistic evaluation of modifications of distribution. Pharmacokinetic parameters of model organic anions in presence of a model renal tubular secretion inhibitor in rats.

The effects of DL-tropic acid (VIII) on the distribution pharmacokinetic parameters of the model compounds benzoylformic acid (I), p-methylbenzoylformic acid (II), p-ethylbenzoylformic acid (III), D-(-)-mandelic acid (IV), D-(-)-p-methyl-mandelic acid (V), D-(-)-p-ethylmandelic acid (VI), and D-(-)-p-isopropylmandelic acid (VII) were studied in rats. Since VIII is a competitive inhibitor of renal tubular secretion of I-VII and since all of these compounds (I-VIII) are negligibly bound to plasma proteins and are neither metabolized nor reabsorbed from the renal tubules, they were considered as model compounds. Therefore, changes observed in the values of the distribution pharmacokinetic parameters of I-VII were attributed to the influence of VIII on the transmembrane transport of the compounds between body compartments in rats. The decrease in the apparent volumes of the central compartments for I, IV, and VII, the increase in the apparent volumes of the peripheral compartments for IV-VII, the absence of change in the volumes of the central or peripheral compartments for the other compounds, and the increase in the ratios of the rate constants of the transfer of compounds from one compartment into another for I and IV-VII were explained in terms of the "aqueous pore" mechanism for the transmembrane transport of the anions of the compounds as well as the heteroporosity of the tissue membranes.     

Mechanism of action of retinyl compounds on wound healing IV: effect of desmethylretinoic acid and its vinylogs on granuloma formation.

The effect of side-chain length of desmethylretinoic acid on granuloma formation induced by implantation of cotton pellets was studied. As in the homologous series of retinoic acid studies, compounds with side chains shorter than retinoic acid were not active while compounds with side chains as long or longer than retinoic acid were active. The compound with a chain two carbons longer than retinoic acid was the most active. The hydroxyproline and hexosamine contents of the granuloma were analyzed. The mechanisms of action of these active compounds on wound healing are discussed.     

Cytotoxic triterpenoids from the fruits of Zizyphus jujuba

The following eleven triterpenoic acids were isolated from the fruits of Zizyphus jujuba (Rhamnaceae): colubrinic acid, alphitolic acid, 3-O-cis-p-coumaroylalphitolic acid (3), 3-O-trans-p-coumaroylalphitolic acid (4), 3-O-cis-p-coumaroylmaslinic acid, 3-O-trans-p-coumaroylmaslinic acid, betulinic acid (7), oleanolic acid, betulonic acid (9), oleanonic acid and zizyberenalic acid. The in vitro cytotoxicities of the triterpenoic acids against K562, B16(F-10), SK-MEL-2, PC-3, LOX-IMVI, and A549 tumor cell lines were investigated by the sulforhodamin B (SRB) method. Among these compounds, the lupane-type triterpenes, such as compounds 3, 4, 7, and 9, showed high cytotoxic activities. In particular, the cytotoxic activities of 3-O-p-coumaroylalphitolic acids (compounds 3 and 4) were better than those of non-coumaroic triterpenenoids (compounds 7 and 9). These results suggest that the coumaroyl moiety at the C-3 position of the lupane-type triterpene may play an important role in enhancing cytotoxic activity.     

中药升麻酚酸类化学成分研究

目的寻找中药升麻(Cimicifuga foetida L.)的有效成分.方法利用硅胶柱及Sephadex LH-20柱进行分离纯化,根据理化性质和各种波谱数据(UV,IR,MS,1D及2D-NMR),辅以化学方法,进行结构鉴定.结果从升麻生药乙醇提取物分离的酚酸性部分获得了8种成分:升麻酸(cimicifugic acid,1),马栗树皮素(esculetin,2),咖啡酸甲酯(caffeic acid methyl ester,3),4-氧-乙酰基咖啡酸(4-O-acetyl-caffeic acid,4),芥子酸(sinapic acid,5),咖啡酸(caffeic acid,6),阿魏酸(ferulic acid,7),异阿魏酸(isoferulic acid,8).结论 1为新的化合物,命名为升麻酸;2～7为首次从该生药中分得.     

板栗总苞中的抗糖尿病活性成分

目的分离鉴定板栗(Castanea mollissima Blume)总苞中抗糖尿病活性化合物。方法采用正-反相硅胶柱色谱和制备型HPLC进行分离,经理化常数测定、核磁共振技术分析等方法鉴定化合物的结构;对分离得到的单体化合物进行醛糖还原酶(aldose reductase,AR)抑制活性实验。结果从活性部位中分离得到9个化合物,分别为山柰酚(kaempferol,1)、没食子酸(gallic acid,2)、3,4-二羟基苯甲酸(3,4-dihydroxy-benzoic acid,3)、鞣花酸(ellagic acid,4)、苯甲基-6-O-β-D-吡喃葡萄糖苷(benzyl-O-β-D-glucopyranoside,5)、没食子酸正丁酯(n-butyl gallate,6)、2,4,6-三羟基苯甲酸(2,4,6-trihydroxy-benzoic acid,7)、没食子酸甲酯(methyl-gallate,8)、豆甾烷-4-烯-3,6-二酮(stig-mast-4-en-3,6-dione,9)。结论化合物5-7为首次从该属植物中分离得到,活性结果显示9个化合物均显示不同程度抑制活性,其中化合物4、5最为显著。     

哈士蟆卵油化学成分研究(Ⅱ)

目的分离鉴定哈士蟆卵油化学成分。方法硅胶、LH 2 0柱色谱分离 ,通过IR、NMR及MS光谱分析法确定结构。结果分得 6个化合物 ,分别鉴定为 (Ⅰ )棕榈酸 α 单甘油酯、(Ⅱ )棕榈酸 α,α′ 甘油二酯、(Ⅲ )油酸 α 单甘油酯、(Ⅳ )硬脂酸、(Ⅴ )棕榈酰胺和 (Ⅵ )棕榈酸乙酯及硬脂酸乙酯。结论 6个化合物均为首次从哈士蟆卵中分离得到。