中甸前胡的化学成分研究

从伞形科植物中甸前胡(Peucedonum sp.)根中分离鉴定了1个新的香豆素化合物,命名为中旬前胡素(d-laserpitin) (1),经各项光谱测定,其结构确定为3′(S)—羟基—4′(S)—当归酰氧基—二氢邪蒿素。另外,还分离鉴定了silinidin(2),蝉翼素(Pteryxin(3),佛手柑内酯(bergapten(4),ammijin (5)等4个已知香豆素化合物和β—谷甾醇(β—sitosterol)。     

细裂前胡的香豆素成分

细裂前胡Peucedanum macilentum Franch。(伞形科)是云南西部应用的前胡地方品种,从其根的乙醇提取物中经硅胶柱层析得到6个化合物,分别鉴定为香豆素类化合物:伞形花内酯(umbelliferone)(1),佛手柑内酯(bergapten)(2),laserpitin(3),异白花前胡丁素(anomalin)(4);其它化合物:阿魏酸(ferulic acid)(5),β-谷甾醇(β-sitosterol)。     

广西蜘蛛抱蛋中一种甾体皂甙定性定量研究

为了进一步开发和利用广西甾体药源植物奠定基础 ,对广西蜘蛛抱蛋 (Aspidistra retusa K.Y.Langet.S.Z.Huang)块茎甾体皂甙化合物进行了提取分离。在分离得化合物中含量最高的甾体皂甙化合物 4经鉴定为 :偏诺甾体四糖皂甙 ,即 pennogenin-3-β-O-β-D-glucopyranosyl[-α-L-rhamno-pyranosyl(1 -2 ) ]-α-L-rham-no-pyanosyl(1 -4 ) -α-L-rhamnopyranosyl(1 -4 )。该化合物为首次从蜘蛛抱蛋属植物中分离得到。经 HPLC测定其在广西蜘蛛抱蛋中的含量为 1 .5 95 %。     

旱前胡的化学成分

从云南产早前胡(Ligusticum daucoides Franch.)(伞形科)根的脂溶性部分分离了11个化合物,分别为香豆素化合物:columbianadin,isoedultin,archangelicin,旱前胡甲素(daucoidin A),旱前胡乙素(dsucoidin B),佛手柑内酯(bergapten),非香豆素化合物:falcarindiol(7),阿魏酸(ferulic acid),蜡酸(cerotic acid),β-谷甾醇(β-sitosterol),胡萝卜甙(daucosterol)。其中,化合物4和5是新的香豆素化合物,经化学方法及光谱测定,证明其结构为:4是3′去乙酰基isoedultin,即:2′(S)-(1″,1″-二甲基,1″-当归酰氧基)-3′(R)-羟基-角型二氢呋喃香豆素[2′(S)-(1″,1″-dimethvl,1″-angelovloxv)—3′(R)-hydroxy angular dihydrofuranocoumarin];5是2′-(1″-甲基,1″-羟基,1″-当归酰氧亚甲基)-角型二氢呋喃香豆素[2′-(1″-methyl,1″-hydroXy,1″-angeloyloxy-methylene)angular dihydrofuranocoumarin]。     

芽前胡的化学成分

从成都产芽前胡Peucedanum turgeniifolium Wolff.中分离鉴定了12个化合物,分别为香豆素化合物佛手柑内酯(bergapten)(1),异欧芹属乙素(isoimperatorin)(2),(±)diisovaleryl-cis-khellactone(3),(±)dihydrosamidin(4),(±)peuformosin(5),(±)cis-khellactone(6),8-(2’,3’-二羟基,3’-甲基-丁基)-伞形花内酯[8-(2’3’-dihydroxy,3’-methyl-butyl)-umbelliferone](7),(±)selinidin(8),turgeniifolin A(9)以及非香豆素化合物硬脂酸(stearic acid),β-谷甾醇(β-sitosterol),甘露醇(d-mannitol)。     

驼绒藜化学成分研究

从驼绒藜(Ceratoides latens)乙醇提取物中分离得到9个化合物,经波谱分析将它们分别鉴定为香草酸(vanilic acid)(1),乙酰香子兰酮(acetovanillon)(2),三达右松脂-15-烯-8β,12β-二醇(sandaracopimar-15-en-8β,12β-diol)(3),5,7,3’,4’-四甲基槲皮素(5,7,3’,4’-tetramethyl quercitin)(4),小麦黄酮(tricin)(5),丁香亭3-O-β-D-葡萄糖苷(syringetin-3-O-β-D-glycopyranoside)(6),β-谷甾醇(β-sitosterol)(7),胡萝卜苷(daucosterol)(8)和豆甾醇(stigmasterol)(9)。这些化合物均为首次从该植物中分离得到。     

黄白红菇的化学成分

从野生真菌黄白红菇Russula ochroleuca(Pers).Fr.子实体中首次分得11个化合物,经光谱法和化学法分别鉴定为2个脑苷脂,1－0－β－D－吡喃葡萄糖基－（2S,3R,4E,8EE,2'R）－2－N－(2'－羟基棕榈酰）－9－甲基－4,8－sphingadienine(cerebrosideB,1)和1－O－β－D－啉喃葡萄糖基－（2S,3R,4E,8E,2'R) -2-N-(2'-羟基十八酰B,I）和－9－甲基－4,8－sphingadienine(cerebrosideD,2);3个麦角甾醇,5α,8α－epidioxy-(22E,24R)-ergosta-6,22-dien-3β-ol3,(22E,24R)-ergosta-7,22-dien-3β-ol4,(24S)－ergosta-7-en-3β-ol5.2个含氮杂环化合物,尿嘧啶（uracil6),腺嘌adenine7),1个含硫化合物,硫代乙酰酐（thioacetic anhydride8),以及乙基－β－D－吡喃呤（adenine7),1个含硫化合物,硫代乙酸酐（thioacetic anhydride8),以及乙基－β－D－吡喃葡萄糖苷（ethy1-β－D－glucopyranosde9),D－阿洛醇（D-allitol10),硬脂酸（stearic acid11),化合物1和2为首次从红菇科真菌获得,8作为天然产物系首次报道。     

俯卧前胡的化学成分

从伞形科植物俯卧前胡(Peucedanum decumbens Maxiam)的根中分离鉴定了13个成分,其中化合物(1)是一个新的二氢呋喃香豆素,经各项光谱测定,确定其结构为:顺式-2′-(1″-甲基,1″-千里光酰氧基-乙基)-3′-羟基-线型二氢呋喃香豆素,命名为俯卧前胡素(decumbensol)。     

泽漆的化学成分研究

采用多种分离材料包括硅胶、Sephadex LH-20和反相RP-18从泽漆的95%乙醇提取物的正丁醇部位分离得到12个化合物,经过波谱学方法分别鉴定为Helioscopin D(1),Isofraxidin(2),Swertiamarin(3),13-Car-boxyblumenol C(4),4,4′-dimethoxy-3′-hydroxy-7,9′,7′9-diepoxyligan-3-O-β-D-glucopyranoside(5),(+)-Syringa-resinol-4′-O-β-D-glucoside(6),2S,3R-2,3-Dihydro-2-(4-hydroxy-3-methoxyphenyl)-3-hydroxymethyl-7-methoxy-benzofuran-5-(trans)propen-1-ol-3-O-β-glucoside(7),Quinquenin L1(8),(6R,9S)-megastigman-3-one-4,7-ene-9-ol-9-O-α-L-arabinofuranosyl-(1→6)-β-D-glucopyranoside(9),2R,3R-2,3-Dihydro-2-(4′-hydroxy-3′-methoxyphenyl)-3-(glucosyloxymethyl)-7-methoxy-benzofuran-5-propanol(dihydrodehydrodiconiferyl-alcohol-β-D-glucoside)(10),Thy-midine(11),和Deoxyuridine(12)。其中化合物1为一个降倍半萜类新化合物,其余化合物从该种中首次分离。     

开口箭根茎中甾体化合物的研究

从开口箭根茎部位共分离得到9个甾体化合物,经波谱数据分析结合文献对照分别鉴定为3-epi-neoruscogenin-3-β-D-glucopyranoside(1),3-epi-ruscogenin-3-β-D-glucopyranoside(2),ranmogenin A(3),convallagenin B(4),3-epi-neoruscogenin(5),tupichigenin E(6),(20S,22R)-spirost-25(27)-ene-1β,2β,3β,4β,5β,7α-hexaol-6-one(7),β-谷甾醇(8)和胡萝卜苷(9)。其中化合物1、2和4为首次从该植物中分离得到。     

Coumarin glucosides from Cruciata taurica

Two new coumarin glycosides (1 and 2) along with two known coumarin glucosides, daphnin (3) and daphnetin glucoside (4) were isolated from the aerial parts of Cruciata taurica. The structures of the new compounds were elucidated by spectral methods and chemical means as 7-O-(6' -acetoxy-beta-D-glucopyranosyl)-8-hydroxycoumarin (1) and 7-O-[6 '-O-(3',4'-dihydroxycinnamoyl)-beta-D-glucopyranosyl]-8-hydroxycoumarin (2). The phylogenetic significance of coumarins in C. taurica was discussed.     

Synthesis of radiolabeled biphenylsulfonamide matrix metalloproteinase inhibitors as new potential PET cancer imaging agents

Novel matrix metalloproteinase (MMP) inhibitor radiotracers, (S)-3-methyl-2-(2',3',4'-methoxybiphenyl-4-sulfonylamino)-butyric acid [(11)C]methyl ester (1a-c), (S)-3-methyl-2-(2',3',4'-fluorobiphenyl-4-sulfonylamino)-butyric acid [(11)C]methyl ester (1d-f), and (S)-3-methyl-2-(4'-nitrobiphenyl-4-sulfonylamino)-butyric acid [(11)C]methyl ester (1g), a series of substituted biphenylsulfonamide derivatives, have been synthesized for evaluation as new potential positron emission tomography (PET) cancer imaging agents.     

Stigmastane derivatives and isovaleryl sucrose esters from Vernonia guineensis (Asteraceae)

Vernoguinoside, 16beta,22R;21,23S-diepoxy-3beta-O-beta-D-glucopyranosyloxy-21S,24-dihydroxy-5alpha-stigmasta-8,14-dien-28-one (1), a new stigmastane derivative, 16beta,22R;21,23S-diepoxy-21S,24-dihydroxy-5alpha-stigmasta-8,14-diene-3,28-dione (2) and two new sucrose esters, 1',3,3',4',6'-pentakis-O-(3-methylbutanoyl)-beta-D-fructofuranosyl alpha-D-glucopyranoside (3) and 1',2,3',6,6'-pentakis-O-(3-methylbutanoyl)-beta-D-fructofuranosyl alpha-D-glucopyranoside (4), have been isolated from the stem bark of Vernonia guineensis. The structures of the new compounds were determined on the basis of spectroscopic evidence.     

New bisabolane sesquiterpenes and coumarin from Leontopodium longifolium

From the roots of Leontopotium longifolium, three new bisabolane sesquiterpenes, rel-(1S,4R,5S,6R)-4,5-diacetoxy-6-[(R)-1,5-dimethylhexa-3,5-dienyl]-3-methylcyclohex-2-enyl (Z)-2-methylbut-2-enoate (1), rel-(1S,4R,5S,6R)-4,5-diacetoxy-6-[(R)-5-hydroxy-1,5-dimethylhex-3-enyl]-3-methylcyclohex-2-enyl (Z)-2-methylbut-2-enoate (2), rel-(1R,2S,4R,5S)-4-acetoxy-2-[(R)-5-hydroxy-1,5-dimethylhex-3-enyl]-5-methylcyclohexyl (Z)-2-methylbut-2-enoate (3), and a new coumarin, 2,3-dihydro-5-hydroxy-2-(1-methylethenyl)-7H-pyrano[2,3-g][1,4]benzodioxin-7-one (4) together with nine known compounds have been isolated. The structures of these compounds were established by spectroscopic methods. Compounds 1 and 2 exhibited moderate cytotoxic activities against human promyelocytic leukemia (HL-60) cells.     

Localization of the elongation factor Tu binding site on Escherichia coli ribosomes

Fluorescent techniques were used to study binding of peptide elongation factor Tu (EF-Tu) to Escherichia coli ribosomes and to determine the distances of the bound factor to points on the ribosome. Thermus thermophilus EF-Tu was labeled with 3-(4-maleimidylphenyl)-4-methyl-7-(diethyl-amino)coumarin (CPM) without loss of activity. In the presence of Phe-tRNA and a nonhydrolyzable analogue of GTP, 70S ribosomes bind the CPM-EF-Tu [Kb = (3 +/- 1.2) X 10(6) M-1] causing a decrease of CPM fluorescence. Binding of CPM-EF-Tu to 50S subunits was at least 1 order of magnitude lower than with 70S ribosomes, and binding to 30S subunits could not be detected. Reconstituted 70S ribosomes containing either S1 labeled with fluoresceinmaleimide or ribosomal RNAs labeled at their 3' ends with fluorescein thiosemicarbazide were used for energy transfer from CPM-EF-Tu. The distances between CPM-EF-Tu bound to the ribosomes and the 3' ends of 16S RNA, 5S RNA, 23S RNA, and the closest sulfhydryl group of S1 were calculated to be 82, 70, 73, and 62-68 A, respectively.     

Monoterpene coumarins from Ferula ferulago.

Two monoterpene coumarins, designated ferulagol A and B, as well as three known monoterpene coumarins and three sesquiterpene lactones were isolated from the chloroform extract of the roots of Ferula ferulago. The structures of ferulagol A and B were determined to be 7-[(E)-3'-hydroxy-3',7'-dimethyl-4',6'-octadienyloxy]coumarin and 7-[(3'Z,5'E)-7'-hydroxy-3',7'-dimethyl-3',5'-octadienyloxy]coumarin, respectively.     

Improved antibacterial activities of coumarin antibiotics bearing 5',5'-dialkylnoviose: biological activity of RU79115

A new series of coumarin inhibitors of DNA gyrase B bearing a N-propargyloxycarbamate at C-3' of various 5',5'-dialkylnoviose, including RU79115, were synthesised and their antibacterial activities have been delineated. Introduction of dialkyl substituents at 5'5'-position of noviose leads to coumarin analogues with improved in vitro and in vivo antibacterial activity.