卵叶娃儿藤中的抗癌活性生物碱

从卵叶娃儿藤(Tylophora ovata (Lindl.) Hook. ex Steud.)根中分离得到 4个菲骈吲哚里西丁类生物碱,分别为tylophoridicine A (1)、娃儿藤宁(2)、氧甲基娃儿藤定(3)和娃儿藤定(4).经波谱分析并结合化学方法鉴定,其结构分别为:(13aR)-6-羟基-3,7-二甲氧基菲骈吲哚里西丁、 (13aS ,14R)-14-羟基-3,6,7-三甲氧基-菲骈吲哚里西丁、(13aS, 14S)-14-羟基-3,6,7-三甲氧基-菲骈吲哚里西丁和(13 aS,14S)-6,14-二羟基-3,7-二甲氧基-菲骈吲哚里西丁.化合物1为新化合物,化合物2-4为首次从该植物得到的化合物.经药理筛选,化合物1、3和4显示很强的抗癌活性.     

海南石斛化学成分研究

为了解海南石斛(Dendrobium hainanense Rolfe)的化学成分,采用色谱技术从海南石斛茎叶中分离得到14个化合物,经波谱分析分别鉴定为:2,6-二甲氧基对苯醌(1)、(+)-dehydrovomifoliol(2)、blumenol A(3)、2,7-二羟基-3,4-二甲氧基-9,10-二氢菲(4)、2,7-二羟基-3,4-二甲氧基菲(5)、3,7-二羟基-2,4-二甲氧基菲(6)、3-羟基-2,4,7-三甲氧基-9,10-二氢菲(7)、3-羟基-2,4,7-三甲氧基菲(8)、3,4,7-三羟基-2-甲氧基菲(9)、3,7-二羟基-2,4-二甲氧基-9,10-二氢菲(10)、(+)-lyoniresinol(11)、丁香脂素(12)、denchrysan A(13)和nobilone(14)。这些化合物均为首次从海南石斛中分离得到。活性测试结果表明化合物4~6、8~9、11和14对乙酰胆碱酯酶有抑制活性。     

黄药子的化学成分研究

综合利用各种色谱方法对黄药子的乙醇提取物进行分离,从中共得到23个化合物。通过波谱分析结合文献数据比对,将它们的结构分别鉴定为:2,7-二羟基-3,4-二甲氧基菲(1)、7-羟基-2,3,4-三甲氧基菲(2)、3,7-二羟基-2,4-二甲氧基-9,10-二氢菲(3)、3-羟基-2,4,7-三甲氧基-9,10-二氢菲(4)、2-羟基-3,4,7-三甲氧基-9,10-二氢菲(5)、7-羟基-2,3,4-三甲氧基-9,10-二氢菲(6)、7-羟基-2,4-二甲氧基-9,10-二氢菲(7)、2-羟基-4,7-二甲氧基-9,10-二氢菲(8)、2,7-二羟基-3,4-二甲氧基-9,10-二氢菲(9)、2'-羟基-3,4,5-三甲氧基联苄(10)、2',3-二羟基-4,5-二甲氧基联苄(11)、3-羟基-4,5-二甲氧基联苄(12)、3,5-二羟基-4-甲氧基联苄(13)、pteryxin(14)、praeruptorin A(15)、山柰酚(16)、7,3',4'-三羟基-3,5-二甲氧基黄酮(17)、黄独乙素(18)、diosbulbin G(19)、3-羟基-β-突厥酮(20)、(6S,9S)-吐叶醇(21)、(6S,9R)-吐叶醇(22)和blumenol B(23)。其中,化合物4~8、10、12~15、20~23共14个化合物均为首次从该植物中分离得到。     

牛心朴子须根的化学成分研究

从采自宁夏的萝摩科鹅绒藤属植物牛心朴子 (CynanchumkomaroviiAl.Iljinski.)须根的乙醇提取物中分离鉴定了十个非C2 1 甾体类化合物 :β D 呋喃果糖基 (2→ 1) α D [6 O 芥子酰基 ] 吡喃葡萄糖甙 (1) ,β D (3 O 芥子酰基 ) 呋喃果糖基 (2→ 1) α D [6 O 芥子酰基 ] 吡喃葡萄糖甙 (2 ) ,[6 O β D 吡喃葡萄糖基 (1→ 6 ) β D 吡喃葡萄糖基 1,2 双氧 (4 羟基 3,5 二甲氧基肉桂酰 ) (3) ,7 脱甲氧基娃儿藤碱 (4) ,9 羟基 芳樟醇 3 O β D 吡喃木糖基 (1→ 6 ) β D 吡喃葡萄糖甙 (5 ) ,(2E ,6R) 2 ,6 二甲基 2 ,7 辛二烯 1,6 二醇 (6 ) ,[(+) 丁香素 ](7) ,4′ O demethylepiyangambin(8) ,4′ 羟基 2′ 甲氧基苯乙酮 (9) ,(2S ,3S ,4R ,12E) N [2′ (R) 羟基二十二碳烷基 ] 1,3,4 三羟基 2 酰胺 二十碳烷基 12 烯 (10 )。除化合物 4和 9外 ,其余化合物均为首次从该植物中分离得到。     

大鼠大脑皮层细胞膜色谱法筛选老瓜头镇痛活性成分研究

从老瓜头二氯甲烷、乙酸乙酯萃取层得到4个化合物,分别为新白前酮(1)、邻苯二甲酸二丁酯(2)、华北白前醇(3)、β-谷甾醇(4);正丁醇层得到2个化合物,分别为3-甲氧基-4-羟基苯甲酸(5)、对羟基苯基酸(6);总生物碱中分离到1个化合物,鉴定为7-脱氧基娃儿藤碱(7)。大鼠大脑皮层细胞膜色谱模型上发现乙酸乙酯、正丁醇层在CMC固定相上无保留,二氯甲烷层有弱保留,总生物碱有强保留;化合物1有弱保留,化合物3、7有强保留,保留因子分别为1.5、23.0、20.0。本实验建立的CMC模型可正确反映活性部位、活性成分与细胞膜及膜受体的相互作用,初筛得到3个可能具有镇痛活性的痕量单体化合物,2个为非生物碱,1个为菲骈吲哚里希啶类生物碱,为老瓜头后续研究奠定基础。     

荷叶的化学成分研究

从荷叶(Folium Nelumbinis)的乙醇提取物中分离鉴定出13个化合物,分别为荷叶碱(nuciferine,1),鹅掌楸碱(liriodenine,2),2-羟基-1-甲氧基阿朴啡(2-hydfoxy-1-methoxyaporphine,3),原荷叶碱(pronuciferine,4),去氢莲碱(dehydroroemerine,5),去氢荷叶碱(dehydronuciferine,6),莲碱(roemerine,7),胡萝卜苷(daucosterol,8),β-谷甾醇(β-sitosterol,9),1-二十烷醇(1-icosanol,10),1-十一烷醇(1-undecanol,11),(2R,4S,4aS,8aS)-4,4a-环氧-4,4a-二氢食用西番莲素[(2R,4S,4aS,8aS)-4,4a-epoxy-4,4a-dihydroedulan,12]和邻二羟基苯酚(benzene-1,2-did,13).其中化合物10～13为首次从荷叶中分离得到.     

钩枝藤枝条中抗菌活性成分研究

采用硅胶柱色谱、Sephadex LH-20 凝胶柱色谱、制备高效液相色谱从钩枝藤[Ancistrocladus tectorius (Lour.) Merr.]枝条的乙醇提取物中分离得到10个化合物,根据各化合物的光谱数据和理化性质鉴定其结构为：表丁香脂素 (1)、丁香脂素 (2)、松脂醇 (3)、浙贝素 (4)、4-羟基-3-甲氧基苯乙醇 (5)、ancistrocline (6)、hamatine (7)、ancistrocladine (8)、ancistrotectorine (9)和β-谷甾醇 (10)。化合物1 ~ 5为首次从该属植物中分离得到。用滤纸片琼脂扩散法测定上述化合物的抗菌活性,结果表明,化合物 1、3、4和6对金黄色葡萄球菌有抑制作用。     

湖北旋覆花化学成分的研究(英文)

从湖北旋覆花(Inula hupehensis)地上部分分离得到19个化合物,经波谱数据分析分别鉴定为9-羟基-百里香酚(1),8,10-去氢-β-羟基-百里香酚(2),2-羟基-4-甲基苯乙酮(3),8,9-双羟基-9-百里香酚(4),10-羟基-8,9-双氧亚异丙基百里香酚(5),8,10-二羟基-9-异丁酰百里香酚(6),8-羟基-9-异丁酰-10-(2-甲基丁酰)百里香酚(7),8,9,10-三羟基百里香酚(8),8-羟基-9,10-二异丁酰百里香酚(9),neoechinulin A(10),3-醛基吲哚(11),3-羟乙酰基吲哚(12),丁香酸(13),4,6-二羟基-2-甲氧基苯乙酮(14),7-甲氧基-8-羟基香豆素(15),6-甲氧基山奈酚(16),(+)-正丁香酯素(17),β-棕榈精(18)和豆甾醇(19)。除了化合物8和9外,其他化合物均为首次从该植物中分离得到。     

老瓜头中的化学成分

从老瓜头(Cynanchum komarovii Al.Iljinski)中分得10种化合物,根据理化常数、光谱分析及化学反应鉴定为7-脱甲氧娃儿藤碱(Ⅰ),表赤杨醇(Ⅱ),β-谷甾醇(Ⅲ),三十烷酸(Ⅳ),蔗糖(Ⅴ),氧化脱氧娃儿藤次碱(Ⅵ),磁麻脂(Ⅶ),牡丹酚(Ⅷ),β-谷甾醇-β-D-葡萄糖甙(Ⅸ)和葡萄糖(Ⅹ)。其中Ⅵ为微量新生物碱。生物试验结果表明,Ⅰ、Ⅵ及反应产物Ⅺ均具有细胞毒作用,后者亦为新化合物。     

尖刀唇石斛化学成分研究

本文对尖刀唇石斛(Dendrobium heterocarpum Lindl.)中的化学成分及其抗炎和抗氧化活性进行研究。实验采用硅胶、Sephadex LH-20凝胶和高效液相色谱等手段进行分离纯化,并用波谱学方法鉴定化合物结构,从尖刀唇石斛的乙酸乙酯萃取部位中分离得到15个化合物,分别鉴定为3,4′-二羟基-5-甲氧基联苄(1)、batatasinⅢ(2)、3-羟基-4′,5-二甲氧基联苄(3)、3-O-methylgigantol(4)、gigantol(5)、3,4-二羟基-4′,5-二甲氧基联苄(6)、moscatilin(7)、dendrocandin A(8)、(S)-3,4,α-三羟基-4′,5-二甲氧基联苄(9)、densiflorol A(10)、dendrocandin I(11)、dendrocandin F(12)、coelonin(13)、红花素(14)、4-羟基-2-甲氧基-3,6-二甲基苯甲酸(15)。化合物1～15均为首次从该种植物中分离得到,其中化合物14为首次从该属植物中分离得到。化合物3、 5、 11具有抑制小鼠RAW264.7巨噬细胞生成一氧化氮的作用;化合物5具有较好的ABTS自由基清除能力,化合物6具有较好的DPPH自由基清除能力。     

Non-glycosidic iridoids from Cymbaria mongolica

Six non-glycosidic iridoids, i.e. (1R,4S,4aS,7S,7aS)-7-hydroxyl-4-hydroxy- methyl-7-methyl-1-methoxyl-1,4,4a,7a-tetrahydrocyclopenta[e]pyran-3-one (1), (1S,4R,4aS,7S,7aS)-7-hydroxyl-4-hydroxymethyl-7-methyl-1-methoxyl-1,4,4a,7a-tetrahydrocyclopenta[e]pyran-3-one (2), (1R,4R,4aS,7S,7aS)-7-hydroxyl-4-hydroxy-methyl-7-methyl-1-methoxyl-1,4,4a,7a-tetrahydrocyclopenta[e]pyran-3-one (3), (1R, 4R, 4aS, 7aS)-4,7-dihydroxymethyl-1-methoxyl-1,4,4a,7a-tetrahydrocyclopenta-6-ene[e]pyran-3-one (4), (1R, 4R, 4aS, 7aS)-4,7-dihydroxymethyl-1-hydroxyl-1,4,4a, 7a-tetrahydrocyclopenta-6-ene[e]pyran-3-one (5), (1R, 4S, 4aS, 7aS)-4,7-dihydroxy-methyl-1-methoxyl-1,4,4a,7a-tetrahydrocyclopenta-6-ene[e]pyran-3-one (6), as well as five known non-glycosidic iridoids mussaenin A (7), gardendiol (8), isoboonein (9), 4-epi-alyxialactone (10) and rehmaglutin D (11) have been isolated from the Chinese medicinal plant Cymbaria mongolica. Their structures were elucidated by spectroscopic methods. These compounds exhibit significant antitumor and antibacterial activity.     

New linalool derivatives in muscat of alexandria grapes and wines

The CHCl₃ extract of Muscat of Alexandria grapes as well as extracts of wines made from these grapes were found to contain 3,7-dimethyloct-1-en-3,6,7-triol, 3,7-dimethyloct-1-en-3,7-diol, 3,7-dimethylocta-1,7-dien-3,6-diol and 3,7-dimethylocta-1,5-dien-3,7-diol.     

石菖蒲的化学成分研究

运用色谱法从石菖蒲根茎提取物中分离得到18个化合物,经波谱学分析鉴定为:(7S,8R)-4,9’-di-hydroxyl-3,3’-dimethoxyl-7,8-dihydrobenzofuran-1’-propylneolignan(1),(7S,8R)-4,9’-dihydroxyl-3,3’-dimethoxyl-7,8-dihydrobenzofuran-1’-propylneoligan-9-O-β-D-glucopyranoside(2),7’-hydroxylariciresinol-9-acetate(3),5-羟基-3,7,4’-三甲氧基黄酮(4),野漆树苷(5),紫云英苷(6),松属素-3-O-芸香糖苷(7),山奈酚-3-O-芸香糖苷(8),德钦红景天苷(9),isoschaftoside(10),5-羟甲基糠醛(11),反式桂皮酸(12),3,7-dihydroxy-11,15,23-trioxo-lanost-8,16-dien-26-oicacid(13),3,7-dihydroxy-11,15,23-trioxo-lanost-8,16-dien-26-oic acid methyl ester(14),环阿屯醇(15),胡萝卜苷(16),羽扇豆醇(17),(22E,24R)-ergosta-5,7,22-trien-3β-ol(18)。除化合物4、11和16外,其余15个化合物均为首次从该植物中分离得到。     

生姜中一新的抗氧化二苯基环氧庚烷成分

通过活性跟踪、从生姜（Zingiber officinale Roscoe)中分离得到一个新的具抗氧化作用的二苯基环氧庚烷类成分,由其质谱、1D和2D-NMR等光谱数据,鉴定其结构为1,5-环氧-3-羟基-1-（3,4-二羟基-5甲氧基苯基）-7-（3,4二羟基苯基）庚烷（1）。     

Phenolic glycosides from Kaempferia parviflora

Three phenolic glycosides were isolated together with two known flavonol glycosides from the H2O-soluble fraction of rhizomes of Kaempferia parviflora. Their structures were determined to be rel-(5aS,10bS)-5a,10b-dihydro-1,3,5a,9-tetrahydroxy-8-methoxy-6H-benz[b]indeno[1,2-d]furan-6-one 5a-O-[alpha-L-rhamnopyranosyl-(1-->6)-beta-d-glucopyranoside] (1), its rel-5aS,10bR isomer (2), and (2R,3S,4S)-3-O-[alpha-L-rhamnopyranosyl-(1-->6)-beta-d-glucopyranosyl]-3'-O-methyl-ent-epicatechin-(2alpha-->O-->3,4alpha-->4)-(5aS,10bS)-5a,10b-dihydro-1,3,5a,9-tetrahydroxy-8-methoxy-6H-benz[b]indeno[1,2-d]furan-6-one 5a-O-[alpha-L-rhamnopyranosyl-(1-->6)-beta-D-glucopyranoside] (3). The structures were elucidated on the basis of analyses of chemical and spectroscopic evidence.     

Antioxidant and alpha-amylase inhibitory compounds from aerial parts of Varthemia iphionoides Boiss

Various extracts of aerial parts of Varthemia (Varthemia iphionoides Boiss) were investigated for radical-scavenging activity, antioxidative activity, and porcine pancreas alpha-amylase inhibitory activity. The ethanol and water extracts showed a pronounced 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity, with inhibition of about 90% at a concentration of 100 microg/ml, and alpha-amylase inhibitory activity of about 70% at a concentration of 200 microg/ml by the 2-chloro-4-nitrophenyl alpha-maltotrioside (CNP-G3) degradation method. The ethanol extract was purified by column chromatography to give seven 3-methoxyflavones (1-7) and eudesmane sesquiterpene, selina-4,11(13)-dien-3-on-12-oic acid (8). The structures of these compounds were established by NMR, MS, and UV spectroscopy. Of 3-methoxyflavones, 5,7,4'-trihydroxy-3,6-dimethoxyflavone (1), 5,7,4'-trihydroxy-3,3'-dimethoxyflavone (2), and 5,4'-dihydroxy-3,7,3'-trimethoxyflavone (3,7,3'-tri-O-methyl-quercetin) (7) exhibited pronounced radical-scavenging activity. The antioxidative activity in the linoleic acid system was considerable in compounds 1, 2, and 5,4'-dihydroxy-3,6,7-trimethoxyflavone (4). Compounds 1, 2, 4, 5 (5,7,4'-trihydroxy-3-methoxyflavone), and 6 (5,4'-dihydroxy-3,7-dimethoxyflavone) showed markedly high inhibitory activity against porcine pancreas alpha-amylase. Eudesmane sesquiterpene did not show any activity.     

Synthesis of novel pyrrolo[3,4-d]pyrazole-dicarboxylic acids and evaluation of their interaction with glutamate receptors

Chiral pyrazoline amino acids (3aR,4S,6aR)-1a and (3aR,4S,6aR)-1b, and (3aS,6S,6aS)-2a and (3aS,6S,6aS)-2b, which are conformationally constrained analogues of glutamic and homoglutamic acid, respectively, were prepared via a strategy based on the 1,3-dipolar cycloaddition of a nitrile imine to methyl N-Boc-3,4-didehydro-(S)-prolinate. The new 'amino acids' were tested for activity at ionotropic glutamate receptors. Solely the derivative (3aR,4S,6aR)-1a, which is structurally related to the previously described 4,5-dihydroisoxazole analogue (S)-CIP-A, turned out to be a potent and selective agonist for the AMPA receptors. The biological activity is due to the interaction with the orthosteric glutamate binding site.     

Synthesis of methyl dihydrohardwickiate and its C-4 epimer. Structural amendment of natural crolechinic acid

Reduction of the alpha, beta-unsaturated ester moiety of (+)-methyl hardwickiate with magnesium in methanol afforded methyl (4aS,6S,8aS,1R,5R)-5, 6,8a-trimethyl-5-[2'-(3"-oxoyl)-ethyl-perhydro-1-naphthalenyl]- carboxaylate, while reduction with sodium in n-propanol, followed by esterification with diazomethane, furnished its C-4 epimer. After comparison of the 1H- and 13C-NMR data of these compounds with those reported for crolechinic acid isolated from Croton lechleri, a stereochemical revision for the natural product is suggested.     

Pyrrolo[1,4]benzodiazepine antitumor antibiotics: evidence for two forms of tomaymycin bound to DNA

Tomaymycin is an antibiotic belonging to the pyrrolo[1,4]benzodiazepine group of antitumor compounds. Previous studies have shown that tomaymycin and other members of this group, which include anthramycin, sibiromycin, and the neothramycins, bind covalently through N-2 of guanine and lie within the minor groove of DNA. Two fluorescent ground-state species of tomaymycin were observed in protic solvents and on DNA. 1H NMR studies showed that the two fluorescent species in methanol are the 11R,11aS and 11S,11aS diastereomeric 11-methyl ethers of tomaymycin. On the basis of epimerization experiments and exchange of carbon-13 from 13CH3OH into the C-11 methoxy group of the tomaymycin methyl ether, a mechanism is proposed for their interconversion via 10,11-anhydrotomaymycin. Coupling information revealed that the solution conformations of the two diastereomers differ, with the C-5 carbonyl lying closer to the plane of the aromatic ring in the 11R,11aS diastereomer. The fluorescence excitation and emission spectra of the two emitting species in methanol were separated by time-resolved fluorescence spectroscopy and were associated with the diastereomeric forms identified by 1H NMR. Time-resolved fluorescence studies of tomaymycin in protic solvents and on DNA indicated that the absorption spectrum of the longer lifetime component (11R,11aS form) is red-shifted relative to the absorption spectrum of the shorter lifetime component (11S,11aS form), consistent with more extensive conjugation. The two conformational forms of tomaymycin on DNA were tentatively identified as the 11S,11aS and 11R,11aS diastereomeric adducts, which bind in opposite orientations in the minor groove. This proposal is supported by molecular modeling studies using a 6-mer duplex adduct of d(ATGCAT)2.