大花哥纳香化学成分研究

从大花哥纳香（ＧｏｎｉｏｔｈａｌａｍｕｓｇｒｉｆｉｔｈｉＨｏｋｆ．ｅｔＴｈｏｍｓ）的茎枝分得１２个化合物,经光谱（ＩＲ,ＭＳ,ＮＭＲ,２ＤＮＭＲ）分析,鉴定其中７个为苯乙烯内酯：ｇｏｎｉｏｔｈａｌａｍｉｎ（１）、９ｄｅｏｘｙｇｏｎｉｏｐｙｐｙｒｏｎｅ（２）、ａｌｔｈｏｌａｃｔｏｎｅ（３）、ｇｏｎｉｏｄｉｏｌ（４）、ｇｏｎｉｏｔｈａｒｖｅｎｓｉｎ（５）、ｇｏｎｉｏｆｕｆｕｒｏｎｅ（６）和８ａｃｅｔｙｌｇｏｎｉｏｔｒｉｏｌ（７）。另５个化合物鉴定为番荔枝内酰胺（ｓｑｕａｍｏｌｏｎｅ,８）、乔松素（ｐｉｎｏｃｅｍｂｒｉｎ,９）、琥珀酸（ｓｕｃｃｉｎｉｃａｃｉｄ,１０）、β谷甾醇（βｓｉｔｏｓｔｅｒｏｌ,１１）和豆甾醇（ｓｔｉｇｍａｓｔｅｒｏｌ,１２）。化合物１～３和５～１０均为首次从该植物分得。     

乌约活性组分LEF的化学成分及抗风湿作用

从乌药（Ｌｉｎｄｅｒａ ａｇｇｒｗｅｇａｔａ（Ｓｉｍｓ）Ｋｏｓｔｅｒｍ）根的镇痛、抗火活性组分（ＬＥＦ）中分离得到６个缩合鞣质烃化合物,鉴定出其中４个,分别为表儿茶素（１）－ｅｐｉｃａｔｅｃｈｉｎ、表榈儿茶素（－）－ｅｐｉｇａｌｌｏｃａｔｅｃｈｉｎ、ｐｒｏｃｙａｎｉｄｉｎＢ－２及ｔｒｉｍｅｒｉｃ ｐｒｏａｎｔｈｏｃｙａｎｉｄｉｎ（ｃｉｎｎａｍｔａｎｎｉｎｓ Ｂ１）,另得到一个黄酮苷,鉴定为橙皮甙ｈ     

云衫针层孔菌化学成分的研究

从云衫针层孔菌Ｐｈｅｌｌｉｎｕｓ ｙａｍａｎｏｉ（Ｔａｍｚ．）ｓｈａｗ分离得到１２个化合物,借助光谱分析鉴定为：８,１１,１３－ａｂｉｅｔａｄｉｅｎ－１８－ｏｉｃ ａｃｉｄ（１）,１,２－ｂｅｎｚｅｎｅｄｉ－ｃａｒｂｏｘｙｌｉｃ ａｃｉｄｂｉｓ（２－ｅｔｈｙｌ－ｈｅｘｙｌ）ｅｓｔｅｒ（２）,ｅｒｇｏｓｔｅｒｏｌ ｐｅｒｏｘｉｄｅ（３）,ｅｒｇｏｓｔａ ７,２２（Ｅ）－ｉｄｅｎ－３－ｏｌ（４）,ｅｒｇｏｓｔａ ７,２２（Ｚ）－ｄｉｅｎ－３－ｏｌ（５）,ｏｃｔａｄｅｃａｎｏｉｃ ａｃｉｄ－１,３－ｐｒｏｐａｎｅｄｉｙｌ ｅｓｔｅｒ（６）,ｏｃｔａｄｅｃａｎｏｉｃ ａｃｉｄ（７）,８（１９）,１４－ｌａｂｄａｄｉｅｎ－１３－ｏｌ（８）,ｅｒｇｏｓｔａ－４,６,８（１４）,２２－ｔｅｔｒａｅｎ－３－ｏｎｅ（９）,化合     

短茎古当归根的化学成分

从短茎古当归〔Ａｒｃｈａｎｇｅｌｉｃａｂｒｅｖｉｃａｕｌｉｓ（Ｒｕｐｒ．）Ｒｃｈｂ．〕根中分得６个结晶,采用ＩＲ、ＭＳ、ＮＭＲ等方法,鉴定了４个化合物,即甲氧基欧芹素（蛇床子内酯,ｏｓｔｈｏｌ,Ⅰ）、欧前胡素（ｉｍｐｅｒａｔｏｒｉｎ,Ⅱ）、古当归素（ａｒｃｈａｎｇｅｌｉｃｉｎ,Ⅳ）、二十八烷酸（ｏｃｔａｃｏｓａｎｉｃａｃｉｄ,Ⅴ）。结晶Ⅳ和Ⅴ为首次从该植物中分出。古当归素为生物合成中最高阶段产物,是本种的特征性成分     

南川前胡化学成分的研究

从伞形科前胡属南川前胡的根中分离得到７个化合物,通过理化常数和波这方法确定了其结构,分别是ｄｅｌｔｏｉｎ,佛手相内酯（ｂｅｒｇａｒｐｔｅｎ）,丁二酸（ｓｕｃｃｉｎｉｃ ａｃｉｄ）,甘露醇（ｄ－ｍａｎｎｉｔｏｌ）,二十五烷酸（ｐｅｎｔａｃｏｓａｎｏｉｃ ａｃｉｄ）,β－谷甾醇（β－ｓｉｔｏｓｔｅｒｏｌ）和胡萝卜甙（ｄａｕｃｏｓｔｅｒｅｌ）。以上化合物均为从本植物中首次分得。     

匙叶翼首花的化学成分

从药用植物匙叶翼首花（Ｐｔｅｒｏｃｅｐｈａｌｕｓ ｈｏｏｋｅｒｉ）中分离了７个化合物。通过波谱分析及已知物数据对照,分别鉴定为ｓｏｎｇｏｒｏｓｉｄｅＡ⑴,ｌｏｇａｎｉｎ⑵,软脂酸（ｐａｌｍｉｔｉｃ ａｃｉｄ,３）,乌索酸（ｕｒｓｏｌｉｃ ａｃｉｄ,４）,齐墩果酸（ｏｌｅａｎｏｌｉｃ ａｃｉｄ,５）,β－谷甾醇（β－ｓｉｔｏｓｔｅｒｏｌ,６）,β－龙胆二糖（β－ｇｅｎｔｉｏｂｉｏｓｅ,７）,其中２是     

云木香化学成分研究Ⅱ

从丽江产云木香（ＳａｕｓｒｅａｌａｐｐａＣ．Ｂ．Ｃｌａｒｋｅ）根中分离得到的另外７个化合物,它们分别是＿孕甾烯醇酮（ｐｒｅｇｎｅｎｏｌｏｎｅ）（１）,β－谷甾醇（β－ｓｉｔｏｓｔｅｒｏｌ）（２）,葫萝卜甙（ｄａｕｃｏｓｔｅｒｏｌ）（３）,苯丙素甙（ｓｙｒｉｎｇｉｎ）（４）,木质素甙（１－ｈｙｄｒｏｘｙｐｉｎｏｒｅｓｉｎｏｌ－１－β－Ｄ－ｇｌｕｃｏｐｙｒａｎｏｓｉｄｅ）（５）,油酸［（ｚ,ｚ）－９,１２－ｏｃｔａｄｅｃａｄｉｅｎｏｉｃａｃｉｄ］（６）和油酸－１,３－甘油二酯［（ｚ,ｚ）－９,１２－ｏｃｔａｄｅｃａｄｉｅｎｏｉｃａｃｉｄ－２－ｈｙｄｒｏｘｙ－１,３－ｐｒｏｐａｎｅｄｉｎｙｌｅｓｔｅｒ］（７）．它们的结构通过波谱和化学的方法得到鉴定。其中化合物１作为天然产物首次从植物中分离得到,化合物３,４,５和７为首次从该植物中分离得到。     

细锥香茶菜化学成分的研究

从细锥香茶菜（Ｒａｂｄｏｓｉａｃｏｅｔｓａ（Ｂｕｃｈ．Ｈａｍ．ｅｘＤ．Ｄｏｎ）Ｈａｒａ）的叶中分离到９个化合物,通过波谱分析阐明其结构,其中１个为新的二萜酸———７α,１２α,１４β三羟基１５酮对映贝壳杉１８羧酸,命名为细锥香茶菜酸（ｃｏｅｔｓａｎｏｉｃａｃｉｄ）。另外８个化合物分别为二氢昆明香茶菜丙素、昆明香茶菜丙素、白柔毛香茶菜甲素、大萼香茶菜丙素、４羟基Δ８,９（Ｚ）鞘氨醇２′羟基正二十（二十一二十六）碳酸酰胺、乌苏酸、２α,３β二羟基乌苏酸和胡萝卜甙。神经酰胺类化合物系首次从该属植物中分离得到。     

水青树和昆栏树茎皮的化学成分

用化学和波谱分析方法从水青树（Ｔｅｔｒａｃｅｎｔｒｏｎ ｓｉｎｅｎｓｅ Ｏｌｉｖ．）茎皮中分离鉴定了５个化合物,分别为丁香甙（ｓｙｒｉｎｇａｎｉｄｅ）、儿茶素（ｃａｔｅｃｈｉｎ）、β－谷甾醇（β－ｓｉｔｏｓｔｅｒｏｌ）、胡萝卜甙（ｄａｕｃｏｓｔｅｒｏｌ）和白桦脂醇（ｂｅｔｕｌｉｎ）,均为从该种植物中首次分得。从昆栏树（Ｔｒｏｃｈｏｄｅｎｄｒｏｎ ａｒａｌｉｏｉｄｅ Ｓｉｅｂ．ｅｔＺｕｃｃ．）茎皮中     

地涌金莲化学成分的研究

从地涌金莲（Ｍｕｓｅｌｌａ ｌａｓｉｏｃａｒｐａ（Ｆｒａｎｃｈ．）Ｃ．Ｙ．Ｗｕ．）新鲜植物中分离得到了５种化合物,经理化常数和ＩＲ,ＥＩ－ＭＷ、＾１Ｈ ＮＭＲ,＾１５ＣＮＭＲ波谱数据分析,分别鉴定为,正二十四烷（ｔｅｔｒａｃｏｓａｎｅ,１）,β－谷甾醇（β－ｓｉｔｏｓｔｅｒｏｌ,２）,硬脂酸（ｓｔｅｒａｒｉｅ ａｃｉｄ,３）２,４－二羟基苯甲酸（２,４－ｄｉｔｈｙｄｒｏｘｙ ｂｅｎｚｏｌｅ ａｃｉ     

Synthesis of a novel class of non-peptide NK-2 receptor ligand, derived from 1-phenyl-3-pyrrol-1-ylindan-2-carboxamides

A series of trans,trans-1-phenyl-3-pyrrol-1-ylindan-2-carboxamide derivatives has been synthesized in eight steps starting from cinnamic acid or 3,3-diphenylpropionic acid. The trans,trans configuration of these carboxamides has been established by X-ray analysis and by NOE experiments in NMR. These new compounds were evaluated for their potential NK-1, NK-2 and NK-3 receptors binding affinity. The N,N-disubstituted carboxamides bound selectively on NK-2 receptors.     

Inhibitors of the enkephalin degrading enzymes. Modulation of activity of hydroxamate containing compounds by modifications of the C-terminal residue

To further characterize the S'2 subsite of both the neutral endopeptidase (EC 3.4.24.11, NEP) and aminopeptidase N (EC 3.4.11.2, APN), two enzymes physiologically involved in enkephalin metabolism, a new series of hydroxamate inhibitors containing a cyclic amino acid as the P'2 component were synthesized. These amino acids differ by the size of the cycle, the relative position of the functional groups, and their absolute configuration. Highly efficient inhibitors of NEP were obtained whatever the modification on the P'2 component, while for APN inhibition, a cyclic beta-amino acid was preferred. The most active inhibitors contained a trans cyclopentyl beta-amino acid and a cis or a trans cyclohexyl beta-amino acid. When injected intracerebroventricularly in mice, these two latter compounds elicited potent antinociceptive responses on both the jump latency and the fore paw lick times.     

宁夏枸杞根和茎的化学成分及抗炎活性研究

研究宁夏枸杞(Lycium barbarum L.)根部和茎部的化学成分。采用硅胶柱、ODS开放柱、Sephadex LH-20葡聚糖凝胶柱及半制备反相高效液相等色谱手段,对宁夏枸杞根和茎部乙醇提取物的石油醚部位及乙酸乙酯部位化学成分进行分离纯化,根据其理化性质以及波谱数据鉴定得到12个化合物,分别为N-[2-(3,4-dihydroxyphenyl)-2-hydroxyethyl]-3-(4-methoxyphenyl)prop-2-enamide(1)、3-(4-hydroxy-3-methoxy phenyl)-N-2-(4-hydroxyphenyl)-2-methoxyethyl]acrylamide(2)、N-trans-coumaroyloctopamine(3)、(E)-2-(4,5-dihydroxy-2-{3-[(4-hydroxyphenethyl)amino]-3-oxopropyl}phenyl)-3-(4-hydroxy-3,5-dimethoxyphenyl)-N-(4-acetamidobutyl)acrylamide(4)、1,2-dihydro-6,8-dimethoxy-7-hydroxy-1-(3,4-dihydroxy-phenyl)-N1,N2-bis[2-(4-hydroxyphenyl)ethyl]-2,3-naphthalene dicarboxamide(5)、(+)-syringaresinol(6)、zhebeiresinol(7)、(±)-eriodictyol(8)、isovanilin(9)、5,5′-dimethoxybiphenyl-2,2′-diol(10)、p-hydroxyphenethyltrans-ferulate(11)、E-ferulic acid hexacosyl ester(12),所有化合物均为首次从该植物中分离得到。此外,采用MTT法和抑制一氧化氮(NO)生成实验,从细胞毒活性和抗炎活性两方面评估了化合物的生物活性。结果表明,化合物2具有显著的抗炎活性,其IC50值(17.00±1.11μmol/L)小于阳性对照药槲皮素的IC50值(17.21±0.50μmol/L)。     

p-coumaric acid esters from Tanacetum longifolium

Two new long chain alkyl p-coumaric acid esters (2-3) along with eicosanyl trans-p-coumarate (1) were isolated from chloroform extract of the roots of Tanacetum longifolium. The structures of new compounds were assigned as 21'-hydroxyheneicosanyl-4-hydroxy-(cis and trans) p-coumarate (2a, 2b) and 27'-hydroxy heptacosanyl-cis-p-coumarate (3) by extensive chromatographic and spectroscopic analysis and by comparison with literature data of known compounds.     

Isolation of chlorogenic acids and their derivatives from Stemona japonica by preparative HPLC and evaluation of their anti-AIV (H5N1) activity in vitro

Two chlorogenic acids and five chlorogenic acid derivatives were simultaneously separated and purified from Stemona japonica by preparative high-performance liquid chromatography. Five of the collected compounds were over 95% pure while the other two compounds were over 90% pure. Their structures were elucidated as 3-O-feruloylquinic acid (1), 4-O-feruloylquinic acid (2), methyl 3-O-feruloylquinate (3), methyl 5-O-caffeyolquinate (4), methyl 4-O-feruloylquinate (5), ethyl 3-O-feruloylquinate (6) and the new compound ethyl 4-O-feruloylquinate (7) by UV, NMR and ESI-MS. All compounds were obtained from Stemona species for the first time, however compounds 6 and 7 are believed to be artefacts from the ethanol extraction. The anti-AIV (H5N1) activities were evaluated by Neutral Red uptake assay. Compounds 3 and 4 exerted moderate inhibitory effect against AIV (H5N1) in vitro.     

N1,N5,N10-Tris(4-hydroxycinnamoyl)spermidines from Microdesmis keayana roots

Three new N1,N5,N10-tris(4-hydroxycinnamoyl)spermidines were isolated from a methanolic root extract of Microdesmis keayana. They were identified as N5,N10-di(p-coumaroyl)-N1-feruloylspermidine,N5-(p-coumaroyl)-N1,N10-diferuloylspermidine, and N1,N5,N10-triferuloylspermidine, and were named keayanidines A, B, and C (1-3), respectively. Their structures were established by spectral techniques(electrospray mass spectrometry, one- and two-dimensional NMR). A 4',4',4'-trimethylated derivative was prepared by methylation of keayanidine C, and the same compound was synthesized fromspermidine and 3,4-dimethoxycinnamic acid to confirm the spectral attributions of the NMR data of the natural compounds. Radical-scavenging properties of all compounds were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical spectrophotometric assay.     

Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776

Two new streptothricins (1 and 2) and a new streptothricin acid derivative (3), all with the carbamoyl group substituted at C-12 of the gulosamine moiety, together with the known N(β)-acetylstreptothricin D acid (4), have been isolated from the culture broth of Streptomyces sp. I08A 1776. The structures of the new compounds were determined by MS, CD, and 1D and 2D NMR spectroscopic data analysis. The isolated compounds were evaluated for antibacterial and antifungal activities. Streptothricin E (6) showed potent activity against the clinically isolated extensively drug-resistant Mycobacterium tuberculosis with MIC values of 0.25-0.5μg/mL.     

Synthesis and anti-influenza activity of aminoalkyl rupestonates

A series of aminoalkyl rupestonates were designed and synthesized by reacting rupestonic acid with 1,ω-dibromoalkanes, followed by amination. All of the new compounds were bioassayed in vitro to determine their activities against influenza A (H3N2, H1N1) and B viruses. The results showed that compounds 5a-5g, which each contain a 1H-1,2,4-triazolyl moiety, were found to be the most potent set of compounds. Compound 5g was demonstrated to possess the highest inhibitory activity against influenza H3N2 and H1N1, with IC(50) values of 0.97 and 0.42 μM, respectively. Our results also indicated that compounds 2g, 3g, 4g and 5g, which contain ten-CH(2)-unit spacers between the rupestonic acid and amino functional groups, were the most potent inhibitors of influenza H1N1 among the synthesized compounds. Unfortunately, most of the synthesized compounds did not show an obvious activity against influenza B; the only exceptions were compounds 5d and 5f, which had IC(50) values of 17.3 and 3.2 μM, respectively. Compounds 4g and 5g were potent inhibitors of influenza H1N1, and they might be potentially developed as new lead anti-influenza virus compounds. Further studies of the mechanism of action are underway.     

Novel amides modified rupestonic acid derivatives as anti-influenza virus reagents

In spired by the important role of amide groups of anti-influenza drugs oseltamivir, zanamivir and peramivir in bioactivity, a series of novel amides modified rupestonic acid derivatives were designed and synthesized. The absolute configuration of critical intermediate bearing chloride with newly formed stereocenter was confirmed by X-ray crystallographic analysis. And all new compounds were evaluated for their in vitro inhibitory activities against influenza A (H1N1 and H3N2) and influenza B viruses. The bioassay results showed that 5h with 4-fluorbenzylsulfonyl modified to 2 position of methyl rupestonate displayed the highest activity against influenza A (H1N1 and H3N2) viruses, even stronger than reference drugs oseltamivir and ribavirin (RVB), and might be recommended as a lead compound to further develop the new anti-influenza reagent.     

In vitro inhibition of polyphenol oxidase by some new diarylureas

A new series of N,N'-diarylureas (1-9) was synthesized. These compounds were investigated as inhibitors of polyphenol oxidase (PPO) which had been purified from banana by an affinity gel comprised of Sepharose 4B-l-tyrosine-p-amino benzoic acid. K(i) values for (1), (2), (3), (5), (6), (7) and (8) were determined as 0.285, 17.97, 0.187, 0.108, 0.063, 0.044 and 0.047?mM, respectively. Thus (2) was by far the most effective inhibitor. Interestingly, (4) and (9) behaved as an activator of PPO in this study.