中国红豆杉中一个新的紫杉烷二萜

从中国红豆杉(Taxus chinensis)枝叶中分离得到4个紫杉烷二萜,通过波谱分析分别确定为：1β-羟基-2α,7β-二去乙酰基巴卡亭I(1),1β-羟基巴卡亭I(2),2α,5α,7β,9α,10β,13α-六乙酰氧基紫杉-4(20),11-二烯(3)和2-去乙酰氧基-5-去肉桂酰taxinine J(4)其中化合物1为新化合物。     

利用云南红豆杉悬浮细胞生产紫杉醇和紫杉烷类化合物

云南红豆杉(Taxus yunnanensis Cheng et L. K. Fu)的一株紫杉醇高产细胞系经过8年多的继代培养,仍保持较稳定的紫杉烷类化合物的生物合成能力.从此株紫杉醇高产细胞系的悬浮培养物中分离到8个紫杉烷类化合物,经核磁共振光谱和质谱数据分析,它们的化学结构分别是2,5,10-三乙酰氧基-14-丙酰氧基紫杉二烯(1)、 2,5,10-三乙酰氧基-14-(2′-甲基丙酰氧基)紫杉二烯(2)、 2,5,10,14-四乙酰氧基紫杉二烯(3)、 2,5,10-三乙酰氧基-14-(2′-甲基-3′-羟基丁酰氧基)紫杉二烯及其差向异构体(4和5)、巴卡亭Ⅳ(6)、巴卡亭Ⅲ (7)和紫杉醇(8).化合物3、 5-7为首次从云南红豆杉细胞培养物中分离到.定性分析表明,云南红豆杉细胞悬浮培养液中的化学成分与培养细胞中的相似.另外,此株紫杉醇高产细胞系的紫杉醇含量可高达0.3%,可用来进行大规模培养.     

利用云南红豆杉悬浮细胞生产紫杉醇和紫杉烷类化合物(英文)

云南红豆杉 (TaxusyunnanensisChengetL .K .Fu)的一株紫杉醇高产细胞系经过 8年多的继代培养 ,仍保持较稳定的紫杉烷类化合物的生物合成能力。从此株紫杉醇高产细胞系的悬浮培养物中分离到 8个紫杉烷类化合物 ,经核磁共振光谱和质谱数据分析 ,它们的化学结构分别是 2 ,5 ,10_三乙酰氧基_14_丙酰氧基紫杉二烯 (1)、2 ,5 ,10_三乙酰氧基_14_(2′_甲基丙酰氧基 )紫杉二烯 (2 )、2 ,5 ,10 ,14_四乙酰氧基紫杉二烯 (3)、2 ,5 ,10_三乙酰氧基_14_(2′_甲基_3′_羟基丁酰氧基 )紫杉二烯及其差向异构体 (4和 5 )、巴卡亭Ⅳ (6 )、巴卡亭Ⅲ (7)和紫杉醇 (8)。化合物 3、5 - 7为首次从云南红豆杉细胞培养物中分离到。定性分析表明 ,云南红豆杉细胞悬浮培养液中的化学成分与培养细胞中的相似。另外 ,此株紫杉醇高产细胞系的紫杉醇含量可高达 0 .3% ,可用来进行大规模培养     

美丽红豆杉种子化学成分的研究(Ⅰ)

从美丽红豆杉种子中分离得到1个甾醇和9个紫杉烷类化合物,鉴定为β-谷甾醇(1),5α-cinnamoyloxy-9α％,10β,13α-triacetoxy-taxa-4(20),11-diene(2),taxinine(3),taxinine J(4),taxinine B(5),taxinineE(6),10-deacetyltaxinine(7),taxuspinew(8),decinnarnoyltaxinineE(9)和紫杉醇(10)。除化合物2、3、4以外,其它均为首次从该植物种子中获得。     

中国红豆杉细胞培养物中两种紫杉烷的分离鉴定

从中国红豆杉细胞培养物中分离得到两个紫杉化合物,它们的结构为1β－ 羟基巴卡亭Ⅰ（1β-hydroxy baccatinⅠ）和云南红豆杉甲素（yunnanxane）。     

利用运动红豆杉悬浮细胞生长紫杉醇和紫杉烷类化合物

云南红豆杉（Taxus yunnanensis Cheng et L.K.Fu）的一些株紫杉醇高产细胞系经过8年多的继代培养,仍保持较稳定的紫杉烷类化合物的生物合成能力。从此株紫杉醇高产细胞系的悬浮培养物中分离到8个紫杉烷类合物。经核磁共振光谱和质谱数据分析,它们的化学结构分别是2,5,10－三乙酰基－14－丙酰氧基紫杉二烯（1）、2,5,10－三酰氧基－14－（2′－甲基丙酰氧基）紫杉二烯（2）,2,5,10,14－四乙酰氧基紫杉二烯（3）、2,5,10－三乙酰氧基－14－（2′－甲基－3′－羟基丁酰氧基）紫杉二烯及其差向异构体（4和5）、巴卡亭Ⅳ（6）、巴卡亭Ⅲ（7）和紫杉醇（8）。化合物3、5－7为首次从云南红豆杉细胞培养物中分离到。定性分析表明,云南红豆杉细胞悬浮培养液中的化学成分与培养细胞中的相似。另外,此株紫杉高产细胞系的紫杉醇含量可达高0．3％,可用来进行大规模培养。     

从南方红豆杉中筛选和鉴定25株产紫杉烷的内生真菌

为从南方红豆杉(Taxus chinensis var.mairei)中分离产紫杉烷的内生真菌,从其幼茎、树皮和叶片中分离纯化了491株内生真菌,经筛选获得25株内生真菌具有产紫杉烷的能力,其中,4株可产紫杉醇、巴卡亭Ⅲ和10-去乙酰巴卡亭Ⅲ,8株能产紫杉醇和巴卡亭Ⅲ,1株能产紫杉醇和10-去乙酰巴卡亭Ⅲ,1株能产巴卡亭Ⅲ和10-去乙酰巴卡亭Ⅲ,6株仅产紫杉醇,5株仅产巴卡亭Ⅲ。根据内生真菌的来源,幼茎中有11株产紫杉烷的内生真菌,叶片中有9株,而树皮中仅有5株。这些菌株的紫杉醇、巴卡亭和10-去乙酰巴卡亭Ⅲ产量分别为0.64~9.87、0.48~3.42和0.20~1.00μg L~(–1)。因此,南方红豆杉中具有紫杉烷类代谢途径的内生真菌来源广,数量多,是研究真菌中紫杉烷类化合物代谢途径的良好材料,也为紫杉烷类抗癌药生产提供了潜在的真菌种源。     

云南红豆杉紫杉烷2α-O-苯甲酰转运酶基因的克隆及定性

通过RACE技术,克隆了云南红豆杉紫杉烷2α-O-苯甲酰转运酶基因(TyTBT),该酶催化2-去苯甲酰-7,13-二乙酰巴卡亭Ⅲ生成7,13-二乙酰巴卡亭Ⅲ,是紫杉醇合成途径中的关键酶之一.TyTBT基因cDNA全长1481 bp,含有1 320 bp的开放读码框,编码440个氨基酸的多肽,分子量为50 050 Da,等电点为6.17.氨基酸序列比对表明TyTBT同植物酰化酶家族的其它成员有较高的相似性,超过67%,同东北红豆杉和曼地亚红豆杉的紫杉烷2α-O-苯甲酰转运酶氨基酸序列的一致性和相似性达到最高,分别为95%和96%.广泛地比对分析证明这种较高的相似性在红豆杉属的其它酶家族中具有普遍性,进化树分析表明同东北红豆杉和曼地亚红豆杉的紫杉烷2α-O-苯甲酰转运酶(TBT)的相似性高于紫杉醇合成途径中的其它酰化酶.     

香薷中的化学成分

从香[Eltholtzia ciliata(Thund.)Hyland]中分出14个化合物,用波谱和化学等方法确定为6-甲基三十三烷(Ⅰ),13-环己基二十六烷(Ⅱ),β-谷甾醇(Ⅲ),棕榈酸(Ⅳ_a),亚油酸(Ⅳ_b),亚麻酸(Ⅳ_c),熊果酸(Ⅴ),5-羟基-6、7-二甲氧基黄酮(Ⅵ),5-羟基-7、8-二甲氧基黄酮(Ⅶ),5、7-二羟基-4′-甲氧基黄酮(Ⅷ),5-羟基-7、4′-二甲氧基双氢黄酮醇(Ⅸ),β-谷甾醇-3-β-D-葡萄糖甙(Ⅹ),5-羟基-6-甲基-7-O-α-D-半乳吡喃糖双氢黄酮甙(Ⅺ),刺槐素-7-O-β-D-葡萄糖甙(Ⅻ)。其中化合物Ⅺ为新化合物,除(Ⅳ_b)和(Ⅳ_c)外,其余为首次从该属植物中得到。     

南方红豆杉紫杉烷13α-羟化酶基因的克隆及序列分析

目的:紫杉烷13α-羟化酶是紫杉醇下游合成途径关键酶之一,负责催化紫杉二烯-5α-醇的C13侧链发生羟基化反应生成紫杉二烯-5α、13α-二醇.该研究从南方红豆杉中克隆出紫杉烷13α-羟化酶基因并对其序列进行生物信息学分析.方法:利用南方红豆杉的总DNA和总RNA为模板,采用PCR和RT-PCR技术克隆出紫杉烷13α-羟化酶基因的DNA序列和cDNA序列,利用swiss-prot、DNAMAN等生物信息学工具对其核酸序列和蛋白序列进行分析.结果:测序结果显示其cDNA序列长度为1 651bp,含有一个1 458bp的开放阅读框,同源性比较分析结果表明,其氨基酸序列与已经报道的蔓地亚红豆杉的紫杉烷13α-羟化酶氨基酸序列的一致性为96%.结论:成功克隆出南方红豆杉紫杉烷13α-羟化酶基因,为利用合成生物学工程技术生产紫杉醇或其前体物质提供了分子基础.     

The Chemical Constituents of Elsholtzia ciliata (Thund.) Hyland

Fourteen compounds have been obtained from the Elsholtzia ciliata (Thund.) Hyland. Their structures were identified by spectral and chemical methods as following: Ⅰ. 6-methyl-tritriacontane, Ⅱ. 13-cyclohexyl-hexoacosane, Ⅲ. β-sitosterol, Ⅳa. palmitic acid, Ⅳb. linoleic acid, Ⅳc. linolenic acid, Ⅴ. ursolic acid, Ⅵ. 5-hydroxy--6, 7-dimethoxyflavone, Ⅶ. 5-hyd-foxy-7, 8-dimethoxyflavone, Ⅷ. 5,7-dihydroxy-4'-methoxyflavone, Ⅸ. 5-hydroxy-7,4'-dime-thoxyflavone, Ⅹ.β-sitosterol-β-D-glucoside, Ⅺ. 5-hydroxy-6-methylflavanone-7-O-α-D-galacopy-ranoside, Ⅻ. acacetin-7-O-β-glucoside. Among all the compounds, Ⅺ is a new compound. Except for Ⅳb and Ⅳc, the other twelve compounds were first found in this plant.     

Studies on Chemical Constituents of Fritillaria yuminensis

Six compounds were isolated from the bulbs of Fritillaria yuminensis X. Z. Duan. They were elucidated as 5α, 14α-cevanine-3α-hydroxy-6-one ( Ⅰ ), 5α, 14α-cevanine-3-one-6β-O-β-D-glucoside ( Ⅱ ), imperialine ( Ⅲ ), delavinone ( Ⅳ ), tortifolisine ( Ⅴ ) and adenosine( Ⅵ ) by means of spectral analysis and chemical reaction. They all were firstly isolated from this plant. Among them, compound Ⅰ and Ⅱ, named yubeinine and yubeiside respectively, were new compounds.     

The Glucosides from Swertia mussotii Franch

Swertia mussotii Franch. is a herb used for treatment of liver disease in Qinghai-Tibcran Plateau folk. Further investigation on chemical constituents in aqueous extract of Swertia mussotii Franch. has been reported here. Seven compounds (Ⅰ, Ⅲ–Ⅷ) were achieved except mangiferin (Ⅱ) isolated previously by a chromatograph. They belong in secoiridoids, flavonoids and xanthonoids, respectively. The structures of known compounds were identified as amarogentin(Ⅲ), swertisin(Ⅷ), 8-O-β-D-glucopyranosyl-1, 3, 5-trihydroxyxanthone(Ⅶ) and 8-O-β-D-glucopyranosyl-(1-6)-β-D-glucopyranosyl)-I, 7-dihydroxy-3-methoxyxanthone (Ⅵ). The structures of other three new compounds have been elucidated as 7-O-β-D-xylopy-ranosyl-1, 8-dihydroxy-3-methoxyxanthone (Ⅳ), 7-O-[α-L-rhamnopyranosyl- (1-2)-β-D-xylopyranosyl]-l,8-dihydroxy-3-methoxyxanthone(Ⅰ)and 3-O-β-D-glucopyranosy 1,8-dihydroxy-5-methoxyxanthone (Ⅴ), by means of the chemical and spectral methods. Mangiferin, amarogentin and 7-0- [α-L-rhamnopyranosyl-(1-2)-β-D-xylopyranosyl]-l,8-dihydroxy-3-methoxyxanthone are the principal glucosides in this plant.     

肋果茶中的萜类化学成分研究

从肋果茶(Sladenia celastrifolia)95％乙醇提取物的乙酸乙酯部位中分离得到15个萜类化合物,经波谱学方法分别鉴定为sladeniafolin A(1),grasshopper ketone (2),(3S,5R,6S,7E,9R) -7-megastigmene-3,6,9-triol (3),hedytriol (4),(3S,5R,6R,7E,9R) -3,5,6,9-tetrahydroxy-7-megastigmene(5),1′S*,4′R*-8-(4′-hydroxy-2′,6′,6′-trimethylcyclohex-2-enyl)-6-methyloct-3E,5E,7E-trien -2-one (6),2α,3α,19α,23-tetrahydroxyurs-12-en-28-oic acid (7),2α,3β,19α,23-tetrahydroxyurs-12-en-28-oic acid(8),pomolic acid(9),3-O-acetyl pomolic acid(10),ursaldehyde (11),camarolide (12),3β-hydroxyurs-11-en-13β(28) -olide (13),3β-hydroxy -11α,12α-epoxy-urs-13β,28-olide (14)和28-0-β-D-glucopyranosyl euscaphic acid (15).以上化合物均首次从该植物中分离得到,其中1为新的C9裂环烯醚萜.     

栗柄金粉蕨的黄酮类成分

从栗柄金粉蕨（ Ｏｎｙｃｈｉｕｍ ｌｕｃｉｄｕｍ ） 地上部分的甲醇抽提物中分到１０ 个成分, 经详细的一维、二维核磁数据分析, 它们被鉴定为： 木犀草甙（１） , ３ , ７ － 二甲基槲皮素（２） , 高山甙Ｂ （３） , 金粉蕨素（４） , 栗柄醇（５） , 金粉蕨醇Ｂ（６） , β－ 谷甾醇（７） , 胡萝卜甙（８） ,齐墩果酸（９） 和蔗糖（１０） 。栗柄醇系新成分。１ , ２, ９ 系首次由金粉蕨属分到。     

Iridoid glucosides and a C₁₃-norisoprenoid from Lamiophlomis rotata and their effects on NF-κB activation

Four new iridoid glucosides, 7-dehydroxyzaluzioside (1), 6'-O-syringylphlorigidoside C (2), barlerin-6″-hydroxy-2″,6″-dimethylocta-2″,7″-dienate ester (3), 6β-n-butoxy-7,8-dehydropenstemonoside (4), and a new C(13)-norisoprenoid derivative, 5β,6α-dihydroxy-3β-(β-D-glucoyranosyloxy)-7-megastigmen-9-one (5), together with 16 known iridoid glucosides, were isolated from Lamiophlomis rotata. The structures of these new compounds were elucidated by HRMS, 1D and 2D NMR spectroscopy. A stable nuclear factor kappaB (NF-κB)-luciferase-expressing human embryonic kidney 293 cell line was used in the luciferase assay for monitoring the anti-inflammatory activity of the compounds. It was found that 6β-n-butoxy-7,8-dehydropenstemonoside (4) and two known compounds (8-epi-7-deoxyloganin and 7,8-dehydropenstemonoside) had a significant inhibitory effect on lipopolysaccharide-stimulated NF-κB activation.     

佛司可林类成分的光谱特征(一)

活性二萜佛司可林和异佛司可林已从毛喉鞘蕊花分离得到。本文详细描述了它们的光谱特征(包括一维和二维的核磁共振谱)。     

Study on Chemical Constituents of Gentianopsis barbata var. Stennocalyx H. W. Li ex T.N. Ho

Nine compounds were isolated from Gentianopsis barbata var. stennocalyx H. W. Li ex. T.N.Ho. Their structures are identified as 1-hydroxy4, 7, 8-trimethoxyxanthone (Ⅰ), 1, 7-dihydroxy-3, 8-dimethoxyxanthone (Ⅱ), 1, 7, 8-trihydroxy-3-methoxyxanthone (Ⅲ), 1-O-(β-D- xylopyranosyl-(1→6)-β-D-glucopyranosyl)-3, 7, 8-trimethoxyxanthone (Ⅳ), 1-O-(β-D-xylopy- ranosyl- (1→6)-β-D-glucopyranosyl)-7-hydroxy-3, 8-dimethoxyxanthone (Ⅴ), 1-O-(β-D-xylo- pyranosyl-(1→6)-β-D-glucopyranosyl)-7, 8-dihydroxy-3-methoxyxanthone (Ⅵ), luteolin-7-O- β-D-glucoside (Ⅶ), oleanolic acid (Ⅷ) and ursolic acid (Ⅸ) by means of chemical methods and UV, IR and NMR determinations respectively.     

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。     

The Structure of Tenacigenin A

Tenacigenin A was obtained from crude glucoside of Marsdenia tenacissima (Roxb.) Wight et Arn., a folk antitumor drug in Yunnan, by treatment with acid and base. This compound C21H32O5, mp 255–260℃, belonging to C21-steroidal type, readily yielded a diacetate (Ⅲ) and under forcing condition a triacetate (Ⅳ). Two of the three hydroxyl groups were able to be oxidized to diketone (Ⅵ), which were attached to the six-membered rings. The other two oxygenatoms existed as in the form of epoxy. Tenacigenin A afforded 3β, 12β, 14β-triacetoxy-5α-pregn-7(8), 9(11)-diene- 20-one (Ⅸ), which was hydrogenized with Pt in AcOH to (Ⅹ), by successive treatment with Ac2O and PTS at 100 ℃ for 30hr. Accoring to the above chemical reactions (Fig. 3) and data of IR, UV, NMR (Fig. 1) and MS (Fig. 2), the structure of tenacigenin A has been suggested as (Ⅰ).