秃杉中萜类和酚类化学成分

从秃杉(Taiwania flousiana Gaussen)的根皮中分离鉴定了6个三萜类化合物、1个二萜类化合物、1个倍半萜类化合物和9个酚类化合物,其中两个为新化合物,分别鉴定为 (24S)-3b-methoxy-5a-lanost-9(11)-ene-7b, 24,25-triol(1) 和senecrassidiol-9-O-b-D-glucopyranoside (8),化合物1命名为taiwaniatriol。通过波谱学方法确定了这些化合物的结构。     

广东紫珠中的萜类化合物及其抗炎活性

对岭南药材广东紫珠(Callicarpa kwangtungensis)地上部分进行化学成分研究,得到11个萜类化合物,分别鉴定为sambucunlin A(1)、2α-羟基羽扇豆醇(2)、swinhoeic acid(3)、3β-羟基-乌苏烷-11-烯-13β,28-内酯(4)、蔷薇酸(5)、2α,3β,6β,18β,23-pentahydroxy-olean-12-en-28-oic acid(6)、rel-5-(3S,8S-dihydroxy-1R,5S-dimethyl-7-oxa-6-oxobicyclo-oct-8-yl)-3-methyl-2Z,4E-pentadienoic acid(7)、salvionoside B(8)、齐墩果酸(9)、白桦脂酸(10)和α-香树脂醇(11)。其中,化合物1～4和6～8为首次从该属植物中分离得到。在化学成分分离基础上,进一步选择脂多糖(LPS)诱导的RAW 264.7小鼠巨噬细胞炎症模型进行萜类化合物抗炎活性测试。结果表明:化合物3和9具有显著的抗炎活性,对比结构发现,三萜类化合物(3～6、9和11)抗炎活性优于倍半萜类化合物(7和...     

麻疯树种子二萜类化学成分的研究

为深入了解麻疯树种子的化学成分,有必要对其具有生物活性的二萜类成分进行研究。该研究利用正相硅胶、ODS、制备液相等色谱分离方法,从麻疯树种子的乙醇提取物中共分离得到了6个二萜类化合物,并采用荧光偏振技术对化合物进行蛋白激酶C (PKC)抑制活性的测定。结果表明:根据化合物的理化性质、MS和NMR,并参考相关文献,这6个二萜类化合物分别鉴定为3β-acetoxy-12-methoxy-13-methylpodocarpa-8,11,13-trien-7-one (1)、4-epi-dehydroabietic acid (2)、3β-hydroxy-19-O-acetyl-pimara-8 (9),15-dien-7-one (3)、Jatrophodione A (4)、14-O-acetyl-5,6-epoxy-(14E)-jatrogrossidentadion (5)、2-Hydroxy jatrophone (6)。其中,化合物2、3、6均为首次从该植物中分离得到,且化合物2对PKCβ具有一定的抑制作用。     

大瑶山甜茶正丁醇部位化学成分研究

目的:研究大瑶山甜茶正丁醇部位中的二萜类化学成分,为探索其活性物质奠定基础。方法:采用95%乙醇提取药材,提取液回收至无醇味后溶于水中,依次用石油醚、乙酸乙酯和正丁醇萃取,减压干燥后获得相应萃取物,综合运用各种色谱技术对正丁醇萃取物进行分离纯化,获取二萜类化合物,通过NMR对得到的化合物进行结构鉴定。结果:从大瑶山甜茶中分离得到10个二萜类化合物,分别鉴定为7β, 17-dihydroxy-16β-ent-kauran-19-oic acid 19-O-β-D-glucopyranoside ester (1), 7β, 17-dihydroxy-entkaur-15-en-19-oic acid 19-O-β-D-glucopyranoside ester (2), 13-[(O-β-D-glucopyranosyl)oxy]ent-kaur-16-en-19-oic acid 2-O-β-Dglucopyranosyl-β-D-glucopyranosyl ester (3), 12-α-[(2-O-β-D-glucopyranosyl-β-Dglucopyranosyl)oxy]ent-kaur-16-en-19-oic acidβ-Dglucopyranosyl ester (4), glaucocalyxin G (5),β-D-glucopyranosyl 17-hydroxy-ent-kauran-19-oate-16-O-β-D-glucopyranoside (6),cussoracosides E (7), 17-O-β-D-glucopyranosyl-16α-ent-kauran-19-oic acid (8),cussovantoside A (9),cussovantoside C (10)。结论:化合物1-10首次从大瑶山甜茶中分离得到。     

四合木茎叶石油醚提取物化学成分分析

利用GC-MS法对四合木茎叶的石油醚提取物进行了成分鉴定。鉴定出40种化合物,包括烷烃类化合物8种、羧酸类化合物11种、酯类化合物9种、萜类化合物2种、甾体类化合物2种、醇类化合物4种,占样品总量的80.5%。其中相对含量最高的3种成分依次为油酸(15.33%)、β-谷甾醇(9.12%)和十八碳二烯酸甲酯(7.24%)。β-谷甾醇可能是四合木具有抗虫性的主要成分。     

鞭打绣球中的一个新单萜苷

从鞭打绣球(Hemiphragma heterophyllum Wall.)全草中分离到1个新单萜苷和7个已知化合物.通过波谱数据分析,新单萜苷的结构鉴定为(4S)-α-萜烯醇-8-O-β-D-比喃木糖-(1→6)-β-D-比喃葡萄糖苷,已知化合物分别鉴定为globularin(2)、(2S 3S,4R,9E)-1,3,4-trihydroxy-2-[(2'R)-hydroxy-tetracosanoylamino]-9-octadecene(3)、β-香树素(4)、齐墩果酸(5)、肉桂酸(6)、β-谷甾醇(7)和胡萝卜甙(8).除化合物2外,其余化合物均为首次从鞭打绣球中分离得到.     

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。     

离舌橐吾中艾里莫酚烷型倍半萜类化学成分的研究

为分析菊科橐吾属植物离舌橐吾Ligularia veitchiana(Hemsl.)Greenm中艾里莫酚烷型倍半萜类的化学成分,并对其进行抗肿瘤活性研究,实验综合运用硅胶柱色谱、反相硅胶柱色谱以及制备型高效液相等色谱方法,从其根茎的95%乙醇提取物的乙酸乙酯部位中分离得到了13个艾里莫酚烷型倍半萜类化合物,根据化合物的理化性质及其波谱学数据鉴定为:eremophilenolide(1),eremophila-7(11),9-dien-8-one(2),eremophil-6-en-11-ol(3),8-oxo-eremophil-6-en-11-one(4),(6α,8α)-6-hydroxyeremophil-7(11)-en-12,8-olide(5),8β-hydroxyeremophil-7(11)-en-12,8α-olide(6),6β-hydroxy-8α-methoxyeremophil-7(11)-12,8β-olide(7),2α-hydroxyeremophil-11-en-9-one(8),6β-methoxy-8β-hydroxyeremophil-7(11)-en-12,8α-olide(9),6β-hydroxyeremophil-7(11)-en-12,8β-olide(10),6β-hydroxy-8β-methoxyeremophil-7(11)-12,8α-olide(11), 6β,8β-dihydroxyeremophil-7(11)-en-12,8α-olide(12)和6β,8α-dihydroxyeremophil-7(11)-en-12,8β-olide(13)。其中,化合物5和10、7和11～13为三对非对映异构体。除化合物3和5外,所有化合物均为首次从该植物中分离得到。运用MTT法对所有化合物进行体外抗肿瘤细胞活性的筛选,结果表明其对胃癌细胞HGC-27和宫颈癌细胞Caski均未显示细胞毒作用。     

柯拉斯那沉香的化学成分研究

对柬埔寨野生柯拉斯那(Aquilaria crassna)沉香的化学成分和生物活性进行研究。实验采用多种柱色谱法对该沉香进行分离纯化;通过现代波普技术结合化合物理化性质对所得单体化合物进行结构鉴定,从柬埔寨野生柯拉斯那沉香共分离出12个化合物,分别鉴定为7α-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(1)、7β-H-9(10)-ene-11,12-epoxy-8-oxoeremophilane(2)、neopetasane (eremophila-9,11-dien-8-one)(3)、jinkoh-eremol(4)、(rel)-4β,5β,7β-eremophil-9-en-12,8β-olide(5)、诺卡酮(6)、11-hydroxy-valenc-1(10)-en-2-one(7)、(7S, 9S, 10S)-(+)-9-hydroxy-selina-4,11-dien-14-al(8)、5-羟基-2-[2-(4-甲氧基苯)乙烯基]色酮(9)、5-羟基-6甲氧基-2-(2-苯乙基)色酮(10)、6-甲氧基-2-(2-苯乙基)色酮(11)、5-羟基-6甲氧基-2-[2-(4-甲氧基苯)乙基]色酮(12)。其中化合物1～8为倍半萜类化合物,化合物9为2-(2-苯乙烯基)色酮类化合物,化合物10～12为2-(2-苯乙基)色酮类化合物。且化合物2～11均是首次从柯拉斯那沉香分离。采用Ellman比色法对单体化合物进行乙酰胆碱酯酶抑制活性的测定,活性测定结果表明化合物1～3和12具有乙酰胆碱酯酶抑制活性。     

不同番茄品种挥发物对B型烟粉虱寄主选择行为的影响

采用顶空固相微萃取和气相色谱-质谱法鉴定了6个番茄品种(浙杂809、浙杂203、合作903、凯特一号、黄椭圆和金妃)植株挥发物的成分,并利用Y型嗅觉仪测定了烟粉虱对不同番茄品种植株及其挥发物的嗅觉反应.结果表明:从6个番茄品种中共鉴定出13种化合物,其主要成分为萜类化合物,品种间挥发物的组成成分和各成分所占比例存在差异.(+)-3-蒈烯和β-石竹烯对B型烟粉虱的驱避性较其他萜类强.烟粉虱对含萜类挥发物种类多、比例高的品种(如浙杂809和浙杂203)选择性较弱,而对含萜类挥发物种类少、比例低的品种(如黄椭圆和金妃)选择性较强.     

Two novel C29-5beta-sterols from the stems of Opuntia dillenii

Two novel C29-5beta-sterols, opuntisterol [(24R)-24-ethyl-5beta-cholest-9-ene-6beta,12alpha-diol] (1) and opuntisteroside [(24R)-24-ethyl-6beta-[(beta-d-glucopyranosyl)oxy]-5beta-cholest-9-ene-12alpha-ol] (2), together with nine known compounds, beta-sitosterol (3), taraxerol (4), friedelin (5), methyl linoleate (6), 7-oxositosterol (7), 6beta-hydroxystigmast-4-ene-3-one (8), daucosterol (9), methyl eucomate (10) and eucomic acid (11), were isolated from the stems of Opuntia dillenii collected in Guizhou Province, China. Their structures were elucidated mainly by spectroscopic analysis. The absolute configuration of 1 were deduced from comparative 1H NMR data of the (S)- and (R)-methoxyphenyl acetate derivatives. Compounds 6-8, 10 and 11 were isolated from O. dillenii for the first time.     

Opioid modulation of LH secretion by pig pituitary cells in vitro

The effects of naloxone and beta-endorphin on LH secretion by pig pituitary cells were studied in primary cultures. On Day 4 of culture, cells (10(5) seeded/well) were challenged with 10(-9), 10(-8) or 10(-7) M gonadotrophin-releasing hormone (GnRH), 10(-10), 10(-9), 10(-8) or 10(-7) M-beta-endorphin or 10(-6) M-naloxone individually or in combinations. Secreted LH was measured at 4 h and 24 h after treatment and cellular content of LH was measured after 24 h. Basal LH secretion (control) was 23.5 +/- 7.6 and 36.9 +/- 10.3 ng/well at 4 h and 24 h, respectively. Relative to control at 4 h, 10(-9), 10(-8) or 10(-7) M-GnRH stimulated (P less than 0.05) LH secretion 140%, 210% and 250%, respectively. At 24 h, LH secretion was increased (P less than 0.05) by GnRH compared to control, but the dose-response to GnRH was absent. Naloxone increased (P less than 0.01) LH secretion 166 +/- 13% at 4 h and 141 +/- 13% (P less than 0.06) at 24 h. Secretion of LH after simultaneous addition of 10(-8) M-GnRH plus naloxone was greater (P less than 0.01) than after GnRH alone at 4 h but not at 24 h. beta-Endorphin at 10(-10), 10(-9), 10(-8) or 10(-7) M failed to alter basal LH secretion at 4 h but decreased secretion at 24 h, while cellular LH content was similar to control at 24 h.(ABSTRACT TRUNCATED AT 250 WORDS)     

三种毒菌的化学成分研究

本文对三种毒菌的化学成分进行了研究。从光盖伞(Psilocybe spp)分离鉴定了4个化合物,经波谱分析鉴定为:(22E,24R)-麦角甾-7,22-二烯-3β-十八烷酸酯(1)、β-胡萝卜苷(2)、(22E,24R)-5α,6α-环氧麦角甾-8,22-二烯-3β,7α-二醇(3)、色氨酸(4);从假褐云斑鹅膏(Amanita pseudoporphyria)分离鉴定了4个化合物:(22E,24R)-3β-羟基-5α,8α-过氧化麦角甾-6,22-二烯(5)、(22E,24R)-麦角甾-7,22-二烯-3β,5α,6β-三醇(6)、1-O-β-D-吡喃葡萄糖基-(2S,3R,4E,8E,2′R)-2-N-(2′-羟基棕榈酰)-9-甲基-4,8-脱氢鞘氨醇(7)、1-O-β-D-吡喃葡萄糖基-(2S,3R,4E,8E,2′R)-2-N-(2′-羟基十八烷酰)-9-甲基-4,8-脱氢鞘氨醇(8);大青褶伞(Chlorophyllum molybdites)发酵菌丝体分离鉴定了4个化合物:5、6、(22E,24R)-5α,6α-环氧麦角甾-8(14),22-二烯-3β,7α-二醇(9)、(22E,24R)-麦角甾-7,22-二烯-3β-醇(10)。除化合物9外其它化合物均为首次从以上相应毒菌中分离得到。     

一例罕见的复杂易位携带者的染色体绘画研究

本文报道了一例罕见的复杂易位男性携带者,结婚８年,其妻连续７次流产、死胎和出生早夭的畸型儿。用染色体显微切割、ＰＣＲ技术构建的人类７号和８号染色体特异性探针地对其进行了染色体绘画研究,分析确定其核型为：４６,ＸＹ,－７,－８,－９,＋ｄｅｒ（７）、ｔ（７;９）（ｑ２２００;ｐ２４）,＋ｄｅｒ（８）ｉｎｖｉｎｓ（８;７）（ｑ２１００;ｑ３１．２ｑ２２００）,＋ｄｅｒ（９）ｔ（９;７）（ｐ２４;ｑ３１．２）．ｉｓｈｄｅｒ（７）ｔ（７;９）（ｗｃｐ７＋）,ｄｅｒ（８）ｉｎｖｉｎｓ（８;７）（ｗｃｐ７＋,ｗｃｐ８＋）,ｄｅｒ（９）ｔ（９;７）（ｗｃｐ７＋）。染色体绘画技术为研究染色体异常提供了一种有效的分子细胞遗传学技术,本文并对携带者复杂易位的发生机理进行了讨论。     

绿槽枝衣的化学成分

从地衣绿槽枝衣( Sulcaria virens) 中分离得到一个新的亚油酸异丙叉衍生物, 通过波谱学方法包括2D-NMR 确定其化学结构为: 9, 10-O-异丙叉基- (12 Z)-十八碳烯酸(1) 。同时还得到其它12 个已知化合物:( 9 Z, 12 Z )-十八碳二烯酸(2), 扁枝衣二酸(3), ( R ) -松萝酸(4), 枕酸甲酯( 5), 黑茶渍素(6) , virensic acid ( 7), abieslactone (8), 3α-羟基羊毛甾-7, 24-二烯-26, 23 R-内酯(9), 蒲公英赛醇(10 ), 蒲公英赛酮 ( 11 ), (22 E , 24 R )-5α, 8α-过氧麦角甾-6, 22-二烯-3β-醇(12) 和2, 2′-四氢角鲨烯(13)。     

Synthesis and structure-activity investigation of novel vasopressin hypotensive peptide agonists.

We report the solid phase synthesis and vasodepressor potencies of the novel hypotensive peptide [1(-beta-mercapto-beta,beta-pentamethylene propionic acid)-2-O-ethyl-D-tyrosine, 3-arginine, 4-valine] arginine vasopressin, d(CH2)5[D-Tyr(Et)2, Arg3, Val4]AVP (A), its related Lys3 (B), Tyr-NH(9)2 (C), [Lys3, Tyr-NH(9)2 (D) analogs and in a preliminary structure-activity study of positions 2-4 and 7-9, 24 analogs (1-24) of A-C. Peptides 1-6, 9-14 have the following single substituents at positions 2, 3, 4, 8 and 9 in (A): 1, D-Tyr(Me)2; 2, L-Tyr(Et)2; 3, Orn3; 4, N-Me-Arg3; 5, Glu3; 6, Arg4; 9, D-Arg8; 10, Eda9; 11, Arg-NH(9)2; 12, Ala-NH(9)2; 13, desGly9; 14, desGly-NH(9)2. Peptides 15 and 16 are analogs of B which possess the following single modifications: 15, Arg-NH(9)2; 16, desGly9. Peptides 7 and 8 are analogs of (C) with the following single modification: 7, Gln4; 8, Lys8. Peptides 17-24 are analogs of A possessing the following multiple modifications: 17, [Sar7, Eda9]; 18, [Arg7, Eda9]; 19, [Arg7, Eda9<--Tyr10]; 20, [Arg4, Arg-NH(9)2]; 21, [Ile4, desGly9]; 22, [Arg4, desGly9]l; 23, [Arg7, desGly9]; 24, [Arg7, Lys8, desGly9]. All 24 new peptides were evaluated for agonistic and antagonistic activities in in vivo antidiuretic (V2-receptor), vasopressor (V1a-receptor) and in in vitro (no Mg2+) oxytocic (OT-receptor) assays and like the parent peptides (A-D) (Chan et al. Br. J. Pharmacol. 1998; 125: 803-811) were found to exhibit no or negligible activities in these assays. Vasodepressor potencies were determined in anesthetized male rats with baseline mean arterial blood pressure maintained at 110-120 mmHg. The effective dose (ED), in microg 100 g(-1) i.v., required to produce a vasodepressor response of 5 cm2, area under the vasodepressor response curve (AUC) during the 5-min period following the injection of the test peptide, was determined. Therefore, the EDs measure the relative vasodepressor potencies of the hypotensive peptides. The following ED values were obtained for A-D and for peptides 1-24: A, 4.66; B, 5.75; C, 10.56; D, 11.60; 1, approximately 20; 2, approximately 30; 3, 6.78; 4, non-detectable (ND); 5, ND; 6, approximately 32; 7, ND; 8, 8.67; 9, ND; 10, 2.43; 11, 3.54; 12, 10.57; 13, 4.81; 14, ND; 15, 4.47; 16, 9.78; 17, 5.72; 18, 1.10; 19, 1.05; 20, 10.41; 21, 9.13; 22, approximately 33; 23, 3.01; 24, 1.71. A is clearly the most potent of the four original hypotensive peptides A-D. These data provide insights to which modification of A enhance, retain or abolish hypotensive potencies. Six of the new hypotensive peptides are significantly more potent than A. These are peptides 10, 11, 18, 19, 23 and 24. Peptide 19, a radioiodinatable ligand, is ten times more potent than C or D. The Gln4 modification of C and the N-Me-Arg3, Glu3, D-Arg8 and desGly-NH(9)2 modifications of A abolished hypotensive potency. By contrast, the Eda9, Arg-NH(9)2, [Sar7, Eda9], [Arg7, Eda9<- -Tyr10], [Arg7, desGly9], [Arg7, Lys8, desGly9] modifications of A all led to enhancements of hypotensive potency. This initial structure-activity exploration provides useful clues to the design of (a) more potent vasodepressor peptides and (b) high affinity radioiodinatable ligands for the putative AVP vasodilating receptor. Some of the peptides here may be of value as pharmacological tools for studies on the complex cardiovascular actions of AVP and may lead to the development of a new class of anti-hypertensive agents.     

飞蛾藤中的新C_(30)甾体类化合物(英文)

A novel C30 sterol, (22E, 24ξ)-24-n-propylcholest-7, 22-dien-3β-ol (racemosol, 1), along withscopoletin (2), scopolin (3), umbelliferone (4), methylβ-D-frucopyranoside (5), syringaresinol-4-O-β-D-glucopyranoside (6), quercetin-3-O-β-D-glucopyranoside (7), quercetin-3-O-α-L-rhamnopyranoside (8),eupatilin (9), kaempferol-3-O-β-D-glucopyranoside (10) and (E）-N-2-(2,3-dihydroxyphenyl) ethyl cinnamamide(11), was isolated from the whole plants of Porana racemosa Roxb. Their structures were elucidatedpredominantly by spectral evidence.     

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。     

钮子瓜化学成分研究

从民间药物钮子瓜全草95%乙醇提取物中首次分离得到14个化合物,应用波谱方法及与已知品对照的手段鉴定它们为(2S,3S,4R,10E)2[(2R)2-羟基二十四烷酰氨基]10十八烷-1,3,4-三醇(1)、(2S,3S,4R)2-二十四烷酰胺基十八烷-1,3,4-三醇(2)、胡萝卜苷(3)、swertish(4)、苯甲酸(5)、水杨酸(6)、loliolide(7)、胸腺嘧啶(8)、尿嘧啶(9)、(23Z)-9,19-环阿尔廷-23-烯-3β,25-二醇(10)、(20S,22E,24R)5α,8α-表二氧麦角甾6,22二烯3β醇(11)、十六烷酸1甘油酯(12)、大豆脑苷Ⅰ(13)、(22E,24S)24甲基5α胆甾7,22二烯3β,5α,6β三醇(14)。