南海疏枝刺柳珊瑚中甾醇类化合物的研究

本文对采自海南三亚海域的疏枝刺柳珊瑚(Echinogorgia pseudossapo)化学成分进行研究,分离到11个甾醇类化合物。经波谱数据分析,分别鉴定为cholest-5-en-3β-ol(1),24-methylene-cholest-4-ene-3β,6β-diol(2),24-norcholesta-22-en-3β-ol(3),acanthovagasteroid A(4),calicoferol E(5),calicoferol F(6),6-hydroxy-cholest-4-ene-3-one(7),echinoflorasterol(8),echissaposterol(9),24-methylcholest-5-en-3β,7α-diol(10)和24-methylcholest-5,22(E)-dien-3β,7α-diol(11)。除化合物8外,其余化合物均首次从该种海洋动物中分离得到。     

中国广西红树林植物海漆的化学成分研究

用硅胶柱层析和凝胶柱层析对红树林植物海漆(Excoecaria agallochaL.)的乙酸乙酯提取物进行分离纯化,从中分离得到9个化合物;通过波谱学数据它们分别鉴定为kayadiol(1)、8(14),15-isopimaradiene-7α,18-diol(2)5、,11-epoxy-9-hydroxy-7-megastigmen-3-one(3)、annuionone E(4)、28,30-dihydroxy-lup-20(29)-ene-3-one(5)、mes-sagenic acid G(6)、3,β24-dihydroxy-12-oleanen-28-oic acid(7)s、yringaresinol(8)、ethyl gallate(9)。这些化合物均为首次从该植物中分离得到。     

木奶果茎叶的化学成分研究

采用常压柱色谱和重结晶相结合的分离方法,从木奶果的茎叶提取物的乙酸乙酯部分中分离得到8个化合物,通过波谱方法及与已知样品对照的手段鉴定它们为(2S,3S,4R)-2-[(2R)-2-hydroxytetracosanoyl-amino]-1,3,4-octadecanetriol(1),Aralia cerebroside(2),(24S)-24-ethylcholesta-3β,5α,6β-triol(3),Stigmast-4-en-6β-ol-3-one(4),7-oxo-β-sitosterol(5),7α-methoxy-sigmast-5-en-3β-ol(6),β-sitosterol(7),daucosterol(8)。化合物1-6为首次从该种植物中发现的。     

苦竹内生真菌Fusarium sp. S13的化学成分研究(英文)

从苦竹内生真菌Fusarium sp.S13的发酵液提取物中分离得到8个化合物,通过波谱技术分别鉴定为:cerevisterol(1),(22E,24S)-24-methyl-5α-cholesta-7,22-diene-3β,5α,6β,9α-tetraol(2),ergosterol peroxide(3),3β,5α,9α-trihydroxy-6β-methoxyergosta-7,22-dien(4),ergosta-7,22-dien-6β-methoxy-3β,5α-diol(5),ergosta-4,6,8(14),22-tetraen-3-one(6),25-hydroxy-ergosta-4,6,8(14),22-tetraen-3-one(7),ergosta-7,22-dien-3β,6β-diol(8)。海虾致死实验结果显示化合物1-8均显示出不同程度的毒性。     

草珊瑚化学成分的研究

采用硅胶、SephadexLH-20、MCI等方法从草珊瑚(Sarcandra glabra)全草乙酸乙酯萃取部位分离得到10个化合物,经波谱学方法鉴定为Chlorajapolide C(1),Shizukanolide H(2),Chloranthalactone E(3),Istanbulin B(4),Istanbulin A(5),4-Hydroxy-4,7-dimethyl-1-tetralone(6),4α,7α-Epoxyguaiane-10α,11-diol(7),(+)-Hydroxydihydroneocurueol(8),3β-Hydroxystigmast-5-en-7-one(9),3β-Hydroxystigmast-5,22-dien-7-one(10)。其中6~10这5个化合物均为首次从该科植物中得到,1、2为首次从该植物中得到。     

长春花悬浮细胞培养体系对脱氢表雄酮的生物转化

利用长春花(Catharanthus roseus(L.)G.Don)悬浮细胞培养体系对脱氢表雄酮进行了生物转化,通过柱层析及制备薄层层析进行分离纯化,并利用核磁共振氢谱、碳谱以及ESI等仪器分析手段进行了化合物的结构鉴定,分离到1 3个转化产物,并对其中的9个进行了结构鉴定,它们分别是:androst-4-ene-3,17-dione(Ⅰ)、6α-hydroxyandrost-4-ene-3,17-dione(Ⅱ)、6α,17β-dihydroxyandrost-4-en-3-one(Ⅲ)、6β-hydroxyandrost-4-ene-3,17-dione(Ⅳ)、17β-hydroxyandrost-4-en-3-one(Ⅴ)、15α,17β-dihydroxyandrost-4-en-3-one(Ⅵ),15β,17β-dihydroxyandrost-4-en-3-one(Ⅶ)、14α-hydroxyandrost-4-ene-3,17-dione(Ⅷ)和17β-hydroxyandrost-4-ene-3,16-dione(Ⅸ).所鉴定的9个化合物均为首次通过生物转化的方法从长春花悬浮细胞培养体系中分离得到.     

高山蓍中的萜类成分及其降糖活性研究CSCD

研究高山蓍Achillea alpina L.全草中萜类成分及其降糖活性。采用ODS、Sephadex LH-20柱色谱和pre-HPLC等方法分离纯化,采用NMR、MS等波谱技术鉴定化合物的结构。从高山蓍的二氯甲烷部位中分离纯化得到13个单体化合物,分别是[3S-[3α,3aα,4α(Z),6α,6aα,9α,9aα,9bβ]],2-butenoic acid,2-methyl-2,3,3a,4,5,6,6a,9,9a,9b-decahydro-6,6a,9-trihydroxy-3,6,9-trimethyl-2-oxoazuleno[4,5-b]furan-4-yl ester(1)、10β-hydroxyisodauc-6-en-14-al(2)、isodauc-6-ene-10β,14-diol(3)、aphanamol II(4)、ent-4(15)-eudesmene-1β,6α-diol(5)、12-羟基-α-香附酮(6)、1β-羟基-α-香附酮(7)、(E)-3,7,11-trimethyl-1,6,10-dodecatriene-3,5-diol(8)、2,6,10-trimethyl-3,6,11-dodecatriene-2,8,10-triol(9)、黑麦草内酯(10)、8-hydroxyphellandral(11)、(3R,6R,7E)-3-hydroxy-4,7-megastigmadien-9-one(12)、saniculamoid D(13)。化合物1~4、6、8和10~13为首次从该属植物中分离得到,化合物5、7和9为首次从植物高山蓍中分离得到。将化合物1~13在棕榈酸诱导的HepG2胰岛素抵抗细胞模型上进行细胞耗糖量的活性筛选,结果显示化合物5、9和10(50μmol/L)具有良好的逆转胰岛素抵抗活性。     

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。     

云南割舌树的化学成分

从云南割舌树（Walsura yunnanensis C.Y.Wu.)树皮的乙醇提取物中分离鉴定了12个化合物,它们分别是walsurol(1),tocopherol(2),sitoindoside Ⅰ（3）,3β-stigmast-5-en-3-yl-β-D-xylopyranoside(4),stigmast-4-en-6β-ol-3-one(5),7-oxositosterol(6),3β-hydroxy-5α,8α-epidioxyergosta-6,22-diene(7),(-)epicatechin(8),3,5-dihydroxy-4-methoxylphenylethanol(9),间三甲氧基苯,（β－谷甾醇和胡萝卜甙,新化合物1命名为割舌醇（walsurol)。     

Biotransformation of dehydroepiandrosterone with Macrophomina phaseolina and β-glucuronidase inhibitory activity of transformed products

The biotransformation of dehydroepiandrosterone (1) with Macrophomina phaseolina was investigated. A total of eight metabolites were obtained which were characterized as androstane-3,17-dione (2), androst-4-ene-3,17-dione (3), androst-4-ene-17β-ol-3-one (4), androst-4,6-diene-17β-ol-3-one (5), androst-5-ene-3β,17β-diol (6), androst-4-ene-3β-ol-6,17-dione (7), androst-4-ene-3β,7β,17β-triol (8), and androst-5-ene-3β,7α,17β-triol (9). All the transformed products were screened for enzyme inhibition, among which four were found to inhibit the β-glucuronidase enzyme, while none inhibited the α-chymotrypsin enzyme.     

元宝山冷杉化学成分的研究

采用色谱技术对元宝山冷杉的化学成分进行分离,根据波谱学方法确定化合物的结构。结果从元宝山冷杉中分离得到5个单体化合物,分别鉴定为:3α-甲氧基-9β-羊毛甾-7,24-二烯-26,23R-内酯(1)、β-谷甾醇(2)、6-甲基-3,7-二甲氧基山奈酚(3)、3-氧代-羊毛甾(9,11)-烯-24S,25-二醇(4)、豆甾-4-烯-6β-羟基-3-酮(5)。所有这些化合物均为首次从该植物中分离得到。     

Selective oxidation of steroidal allylic alcohols

Pyridinium chlorochromate in CH₂Cl₂ containing pyridine (2%) at 2—3°C has been found to effect the high yield selective oxidation of the hydroxyl function of a number of steroidal allylic alcohols. Under these conditions the oxidation of cholest-4-cn-3β-ol to the corresponding ketone was effected in 92% yield. Only the allylic hydroxyl function of 5α-cholest-8(14)-ene-3β,15α-diol, 5α-cholest-8(14)ene-3β,15β-diol and 5α-cholest-8(14)-ene-3β,7β-diol was oxidized under these conditions to give the corresponding α,β-unsaturated ketones in high yields. 5α-Cholest-8(14)-ene-3β,7α,15α-triol gave 5α-cholest-8(14)-ene-3β,7α-diol-15-one in 82% yield. Attempted oxidations of the 5α-cholestan-3β,15α-diol and 5α-cholest-7-ene-3β,15α-diol, both lacking an allylic hydroxyl function, under these conditions, were unsuccessful. Selective oxidation of the allylic alcohol function of 5α-cholest-8(14)-ene-3β,15β-diol using activated manganese dioxide gave 5α-cholest-8(14)-en-3β-ol-15-one in high yield while oxidation of the corresponding 15α-hydroxy epimer using manganese dioxide was unsuccessful.     

Biotransformation of dehydroepiandrosterone with Macrophomina phaseolina and β-glucuronidase inhibitory activity of transformed products

The biotransformation of dehydroepiandrosterone (1) with Macrophomina phaseolina was investigated. A total of eight metabolites were obtained which were characterized as androstane-3,17-dione (2), androst-4-ene-3,17-dione (3), androst-4-ene-17β-ol-3-one (4), androst-4,6-diene-17β-ol-3-one (5), androst-5-ene-3β,17β-diol (6), androst-4-ene-3β-ol-6,17-dione (7), androst-4-ene-3β,7β,17β?triol (8), and androst-5-ene-3β,7α,17β-triol (9). All the transformed products were screened for enzyme inhibition, among which four were found to inhibit the β-glucuronidase enzyme, while none inhibited the α-chymotrypsin enzyme.     

Sterol metabolism. XXVI. Pyrolysis of some sterol allylic alcohols and hydroperoxides

The thermal decomposition of the allylic alcohols 5α-cholest-6-ene-3β,5-diol, cholest-5-ene-3β,7α-diol, and cholest-5-ene-3β,7β-diol and of the allylic hydroperoxides 3β-hydroxy-5α-cholest-6-ene-5-hydroperoxide, 3β-hydroxycho lest-5-ene-7α-hydroperoxide, and 3β-hydroxycholest-5ene-7β-hydroperoxide to six common major pyrolysis products cholest-5-ene-3β,7α-diol, cholest-5-ene-3β,7β-diol, 3β-hydroxycholest-5-en-7-one, cholesta-3,5-dien-7-one, cholesta-4,6-dien-3-one, and cholesta2,4,6-triene was established.     

Biotransformation of progesterone by suspension cultures of Digitalis purpurea cultured cells

It has been shown that the cultured cells of Digitalis purpruea are capable of transforming progesterone (I) to 5α-pregnane-3,20-dione (II), 5α-pregnan-3β-ol-20-one (III), its glucoside (IV), 5α-pregnane-3β,20α-diol (V), its glucoside (VI), 5α-pregnane-3β,20β-diol (VII), its glucoside (VIII), Δ⁴-pregnen-20α-ol-3-one (IX), its glucoside (X), Δ-pregnen-20β-ol-3-one (XI) and its glucoside (XII). 5α-Pregnan-3β-ol-20-one glucoside (IV), 5α-pregnane-3β,20α-diol glucoside (VI), 5α-pregnane-3β,20β-diol glucoside (VIII), Δ⁴-pregnen-20α-ol-3-one glucoside (X) and Δ⁴-pregnen-20β-ol-3-one glucoside (XII) have been found for the first time as new metabolises by plant tissue cultures. A scheme for the biotransformation of progesterone (I) has been proposed, and the reduction and glucosidation activities distinctly have been observed in these cultured cells.     

石山巴豆枝叶的化学成分研究

石山巴豆( Croton euryphyllus)为大戟科( Euphorbiaceae)巴豆属( Croton)植物,主要分布于西南各省的岩溶石山地区,民间用于杀虫和治疗跌打损伤。为了阐明其化学物质基础,该研究采用硅胶柱层析、Sephadex LH-20、HPLC等方法对石山巴豆枝叶醇提物进行分离纯化。结果表明：共分离得到16个化合物,分别鉴定为异毛叶巴豆萜(1), jatrophoidin (2),山藿香定(3),异山藿香素(4),山藿香素(5),赖百当-13-烯-8,15-二醇(6),7-酮基-β-谷甾醇(7),(22E)-5α,8β-表二氧麦角甾-6,22-二烯-3β-醇(8),豆甾烷-4-烯-6β-醇-3-酮(9),齐墩果烷-12-烯-2α,3β-二醇(10),东莨菪内酯(11),催吐萝芙木醇(12), lyratol F (13),罗布麻酚A (14),芹菜素(15),金色酰胺醇酯(16)。所有化合物均为首次从该植物中分离得到,其中化合物8－16为首次从巴豆属中发现。     

龙芽草化学成分研究

从药用植物龙芽草(Agrimonia pilosa Ledeb)全草的95%乙醇提取物中分离得到4个化合物,通过理化性质及波谱学方法分别鉴定为豆甾-5-烯-3β,7β-二醇(1)、豆甾-5-烯-3β7,α-二醇(2)、豆甾-3β6,α-二醇(3)和β-谷甾醇(4)。化合物1～3均为首次从龙芽草中分离得到。     

Measurement of fecal steroids in the black rhinoceros (Diceros bicornis) using group-specific enzyme immunoassays for 20-oxo-pregnanes

The metabolism and excretion of progesterone in different animal species results in several fecal 5-reduced progesterone metabolites (pregnanes), which in recent studies were quantified using progesterone antibodies. To increase the accuracy of fecal 20-oxo-pregnane evaluations in the black rhinoceros, enzyme immunoassays (EIA) using antibodies against 5α-pregnane-3β-ol-20-one 3HS:BSA (5α-20-one EIA) and 5β-pregnane-3α-ol-20-one 3HS:BSA (5β-20-one EIA) were developed. The assays showed high crossreactivities with pregnanes containing a 20-oxo group and are referred to as group-specific; results of these assays were compared with an EIA using an antibody against 6HS-progesterone (4-ene-20-one EIA). Fecal samples of both subspecies of the black rhinoceros (Diceros bicornis michaeli, n = 5, and Diceros bicornis minor, n = 1) during pregnancy were collected 1–3 times/week. HPLC separation showed three major immunoreactive fecal 20-oxo-pregnane peaks; their elution profiles and different crossreactivities in the three EIAs provided strong evidence that these peaks are 5α-pregnane-3, 20-dione, 5α-pregnane-3α-ol-20-one, and 5α-pregnane-3β-ol-20-one. Pregnane values in the pregnant animals continuously increased between months 3–7 and were significantly (P < 0.01) elevated above the levels of nonpregnant animals (0.2 μg/g) by week 11. During months 6–13 concentrations in the 5α-20-one and in the 5β-20-one EIA (5–11 μg/g) were significantly (P < 0.01) higher than in the 4-ene-20-one EIA (1.5–3 μg/g). In conclusion, the immunoreactive fecal 20-oxo-pregnane metabolites in the black rhinoceros are determined more accurately with antibodies against pregnane-20-one-C3 conjugates, as compared with a progesterone antibody. © 1996 Wiley-Liss, Inc.