宽叶秦岭藤根部的化学成分

通过正相和反相硅胶柱层析从宽叶秦岭藤根部乙醇提取物中分离纯化得到19个化合物,经波谱分析并结合化学方法鉴定了其结构,其中4个为新化合物,它们分别是3,5-二羟基二十烷酸羽扇豆醇酯(3),2-羟甲基-5-甲氧基苯基-O-β-D-吡喃葡萄糖甙(11),Δ5-孕甾烯-3β,20(S)-二醇-20-O-β-D-吡喃葡萄糖基(1→6)-β-D-吡喃葡萄糖甙(18,秦岭藤甙C)和Δ5-孕甾烯-3β,20(S)-二醇-3-O-β-D-吡喃葡萄糖基-20-O-β-D-吡喃葡萄糖基(1→6)-β-D-吡喃葡萄糖甙(19,秦岭藤甙D).     

海洋真菌赤褐炭团菌FS521的次级代谢产物研究（英文）

从海洋真菌赤褐炭团菌(Hypoxylon rubiginosum) FS521中分离纯化得到17个聚酮类化合物,分别鉴定为4-乙酰氧基-8-甲氧基-3,4-二氢萘-1(2H)-酮(1)、4,8-二甲氧基-1-萘酚(2)、1'-羟基-4',8,8'-三甲氧基[2,2']联萘-1,4-二酮(3)、3,6-dimethyl-atromentin (4)、4-羟基-8-甲氧基-3,4-二氢萘-1(2H)-酮(5)、regiolone (6)、methylsclerone (7)、5-methylmellein(8)、3,5-二甲基-8-甲氧基-3,4-二羟基异香豆素(9)、9-甲氧基萘(10)、1,8-二甲氧基萘(11)、8-甲氧基-1-萘醇(12)、7-甲氧基-3-甲基异苯并呋喃(13)、3-甲基-4-羟基苯乙酸(14)、nodulisporipyrone A (15)、nodulisporipyrone B (16)、3,4-二甲氧基-乙酰苯乙醇(17).其中化合物1为新化合物,化合物2和3为新天然产物,新化合物的结构通过HRESIMS, 1D NMR和2DNMR等光谱技术确定.此外,对分离所得的化合物1～4进行了体外细胞毒活性测试,结果表明化合物3对SF-268、MCF-7、Hep G-2、A549有较强的细胞毒活性,其IC_(50)值分别为1.85、3.21、2.53、5.09mmol·L~(-1).     

海南染木树叶中的蒽醌成分研究

从海南染木树叶乙醇提取物的乙酸乙酯萃取部位分离得到9个蒽醌类化合物,采用高分辨质谱、一维和二维核磁共振等现代波谱技术,鉴定上述化合物的结构分别为:7-羟基-1,2-二甲氧基-6-甲基-9,10-蒽醌(1),1-羟基-3,6-二甲氧基-9,10-蒽醌(2),10,10'-二蒽酮(3),9,10-蒽醌(4),甲基异茜草素(5),虎刺醇(6),2-羟基-3-甲基-9,10-蒽醌(7),3-羟基-1,2-二甲氧基-9,10-蒽醌(8)和3-羟基-1-甲氧基-2-甲酯基-9,10-蒽醌(9).其中化合物1和2为新天然产物,且化合物1的波谱数据迄今未见任何报道.除化合物9外,其余化合物均为首次从该属植物中分离得到.抗菌活性测试显示,化合物2和9对多种菌株具有很好的抑制作用,尤其是金黄色葡萄球菌,最小抑菌浓度(MIC)值均达到0.078μg/mL;化合物1和6对枯草芽孢杆菌、金黄色葡萄球菌显示出与阳性对照环丙沙星相当或者更强的抑制活性.     

全叶马兰中两个新的黄酮类化合物

利用多种色谱分离方法对全叶马兰(Kalimeris integrifolia)的化学成分进行研究,从其地上部分的乙醇提取物中分离得到两个化合物,应用HR-ESIMS,1D和2D NMR,IR,UV等多种波谱技术确定了化合物的化学结构,经鉴定分别为5,8-二羟基-2-(3-羟基-4,5-二甲氧苯基)-6,7-二甲氧基-4H-色烯-4-酮(1)和5-羟基-6,7-二甲氧基-2-(4'-甲氧基苯基)-4-氧代-4H-色烯-8-(2'-甲基丁酸酯)(2).化合物1和2为两个新的黄酮类化合物.     

两种天然异戊烯基黄烷酮的全合成

以3-甲氧基甲氧基苯甲醛和2,4,6-三甲氧基-3-异戊烯基苯乙酮为原料,经烷基化和缩合反应合成了新化合物——2’-羟基-4-甲氧基-3,4’,6’-三甲氧甲氧基-3’-异戊烯基査尓酮(6);6经环合反应合成了新化合物——(±)-5,7,3’-三甲氧甲氧基-4’-甲氧基-8-异戊烯基黄烷酮(7);7经脱保护和环合反应实现了天然产物(±)-5,7,3’-三羟基-4’-甲氧基-8-异戊烯基-黄烷酮(1,总收率11.6%)和(±)-5,3’-二羟基-7,8-(2,2-二甲基吡喃)-4’-甲氧基黄烷酮(2,总收率10.5%)的全合成,其中1为新化合物,其结构经1H NMR,IR和MS表征。     

由2′,4′-二氢-6′-甲氧基-3′,5′-二甲基查耳酮合成新黄酮

在DMSO/I2的氧化作用下,由2′,4′-二氢-6′-甲氧基-3′,5′-二甲基查耳酮可合成一种全新结构的黄酮:7-羟基-5-甲氧基-6,8-二甲基黄酮(产率91%),而在HCl/MeOH作用下则得到了两种黄烷酮:7-羟基-5-甲氧基-6,8-二甲基黄烷酮(产率70%)和5,7-二羟基-6,8-二甲基黄烷酮(产率20%)。     

由2',4'-二氢-6'-甲氧基-3',5'-二甲基查耳酮合成新黄酮

在DMSO/ I2的氧化作用下,由2',4'-二氢-6'-甲氧基-3',5'-二甲基查耳酮可合成一种全新结构的黄酮:7-羟基-5-甲氧基-6,8-二甲基黄酮(产率91%),而在HCl/MeOH作用下则得到了两种黄烷酮:7-羟基-5-甲氧基-6,8-二甲基黄烷酮 (产率70%) 和 5,7-二羟基-6,8-二甲基黄烷酮 (产率20%).     

白芍中一种内生真菌Penicillium mariae-crucis的次生代谢产物研究

综合运用多种现代色谱学分离方法对白芍中内生真菌Penicilliummariae-crucis的次生代谢产物进行了研究,从其发酵液的乙酸乙酯萃取部位中分离得到了10个化合物,采用多种现代波谱技术确定了这些化合物的化学结构,分别鉴定为:penicmariae-crucis A (1)、penicmariae-crucis B (2)、penicmariae-crucis C (3)、penicmariae-crucis D (4)、(E)-2-甲基己-3-烯二酸(5)、2-乙酰基-3-羟基-5-甲氧基苯乙酸(6)、2-乙酰基-3-羟基-5-甲氧基苯乙酸甲酯(7)、2-乙酰基-3,5-二羟基苯乙酸甲酯(8)、β-谷甾醇(9)、过氧化麦角甾醇(10);其中化合物1～4为新化合物,化合物5为新天然产物,所有化合物均为首次从内生真菌P. mariae-crucis中分离得到.     

2-苯甲酰基嘧啶类化合物的合成与生物活性

2-嘧啶氧基-N-芳基苄胺类化合物结构经过两次骨架结构优化后得到2-苯甲酰基嘧啶类化合物二次先导结构.在二次先导结构基础上,共设计并合成了36个化合物,所有化合物结构经1H NMR、13C NMR、HRMS确认,并进行了室内杀菌活性筛选,对各部位取代基进行了逐次优化.结果表明2-苯甲酰基嘧啶类化合物中R1取代基以2位卤素或烷基取代的苯环或杂环活性最好;中间苯环6位引入氟原子活性保持;嘧啶环4,6位甲氧基取代活性较好,5位甲基取代活性大大降低;羰基被还原为羟基后活性消失.其中2,3-二氯-N-[2-(4,6-二甲氧基嘧啶-2-甲酰基)苯氧基]-N-甲基苯甲酰胺(4AHl)、2,5-二氯-N-[2-(4,6-二甲氧基嘧啶-2-甲酰基)苯氧基]-N-甲基苯甲酰胺(4AHn)及N-[2-(4,6-二甲氧基嘧啶-2-甲酰基)-3-氟苯氧基]-N,2-二甲基苯甲酰胺(4AFd)对黄瓜白粉病的杀菌活性与对照样苯菌酮相当.     

川西獐牙菜中两个新的链状单萜类化合物

利用多种色谱分离方法对川西獐牙菜的化学成分进行研究,从其全草的乙醇提取物中分离得到四个化合物,应用HR-ESIMS,1D和2D NMR,IR,UV等多种现代波谱技术确定了这些化合物的化学结构,经鉴定分别为(S,2E,6E)-2,6-二甲基-4,8-二羟基辛烷-2,6-二烯酸(1),(S,2E,6E)-2,6-二甲基-4-羟基-8-甲酰氧基辛烷-2,6-二烯酸(2),swerimilegenins B和C(3和4).化合物1和2为两个新的链状单萜类化合物,分别命名为川西獐牙菜酸C和D,化合物3和4是两个不常见的C_9骨架的环烯醚萜,为首次从该植物中分离得到.     

A novel antioxidant isobenzofuranone derivative from fungus Cephalosporium sp.AL031

Bioassay-guided fractionation of metabolites from the fungus Cephalosporium sp.AL031 isolated from Sinarundinaria nitida led to the discovery of a new isobenzofuranone derivative, 4,6-dihydroxy-5-methoxy-7-methylphthalide (1), together with three known compounds: 4,5,6-trihydroxy-7-methyl-1,3-dihydroisobenzofuran (2), 4,6-dihydroxy-5-methoxy-7-methyl-1,3-dihydroisobenzofuran (3) and 4,5,6-trihydroxy-7-methylphthalide (4). The structure of the new compound 1 was determined based on MS, 1D and 2D NMR spectral data. Compounds 1-4 showed potent antioxidant activity with EC?? values of 10, 7, 22 and 5 μM by 1,1-diphenyl-2-picryhydrazyl (DPPH) radical-scavenging assay.     

Isolation and structure determination of two new constituents from the fruits of Morinda citrifolia Linn

Studies on the chemical constituents of the fruits of Morinda citrifolia Linn. have led to the isolation of two new compounds, morinaphthalene (=1,3,6,7-tetrahydroxy-2-hydroxymethyl-1,2,3,4-tetrahydronaphthalene, (1); and morindafurone (=5-hydroxy-1,10b-dihydro-6H-anthra [1,9-bc] furan-6-one, (2); as well as two known constituents, 1,8-dihydroxy-6-methoxy-3-methyl-9-anthrone (3) and 2,4-dimethoxy-9-anthrone (4). Their structures were elucidated by spectral analysis including 2D NMR techniques.     

Flavonoids isolated from Draconis Resina

One new chalcone, 4,6-dihydroxy-2-methoxy-3-methyldihydrochalcone (4), together with four known compounds, dammaradienol (1), (-)-5-methoxyflavan-7-ol (2), 5-methoxy-6-methyl-2-phenyl-7H-chromen-7-one (3), and dracorhodin (5), were isolated from Draconis Resina. The structures of these compounds were determined by spectral methods. Among these five compounds, compounds 1, 2, and 3 exhibited cytotoxicity against KB and HepG2 cells.     

Structural determination of flavonoids from Sophora flavescens

Eight flavonoids were isolated from Sophora flavescens. Among them, three prenylflavanones: (2S)-6[2(3-hydroxyisopropyl)-5-methyl-4-hexenyl]-5-methoxy-7,2', 4'-trihydroxyflavanone (1), (2S)-5, 4'-dimethoxy-8-lavandulyl-7, 2'-dihydroxy flavanone (2) and (2S)-8-(5-hydroxy-2-isopropenyl-5-methylhexyl)-7-methoxy-5,2', 4'-trihydroxyflavanone (3) are new compounds. Their chemical structures were determined by spectral methods including 2D NMR.     

One new diphenylmethane glycoside from the leaves of Psidium guajava L

To investigate the chemical constituents of Psidium guajava L, the EtOH/H(2)O extract of the fresh leaves was subjected to various chromatography. One diphenylmethane, one benzophenone, and eight flavonoids were isolated and elucidated as 2,6-dihydroxy-3-formaldehyde-5-methyl-4-O-(6″-O-galloyl-β-D-glucopyranosyl)-diphenylmethane (1), 2,6-dihydroxy-3,5-dimethyl-4-O-(6″-O-galloyl-β-D-glucopyranosyl)-benzophenone (2), kaempferol (3), quercetin (4), quercitrin (5), isoquercitrin (6), guaijaverin (7), avicularin (8), hyperoside (9), reynoutrin (10) by spectroscopic methods, including 1D and 2D NMR and HR-ESI-MS spectrometry as well as by comparison with published data. Compounds 5 and 10 are obtained from P. guajava for the first time, and compound 1 is a new diphenylmethane compound.     

Iridoids and anthraquinones from the Malaysian medicinal plant,Saprosma scortechinii (Rubiaceae)

A further investigation of the leaves and stems of Saprosma scortechinii afforded 13 compounds, of which 10 are new compounds. These were elucidated as the bis-iridoid glucosides, saprosmosides G (1) and H (2), the iridoid glucoside, 6-O-epi-acetylscandoside (3), and the anthraquinones, 1-methoxy-3-hydroxy-2-carbomethoxy-9,10-anthraquinone (4), 1-methoxy-3-hydroxy-2-carbomethoxy-9,10-anthraquinone 3-O-beta-primeveroside (5), 1,3-dihydroxy-2-carbomethoxy-9,10-anthraquinone 3-O-beta-primeveroside (6), 1,3,6-trihydroxy-2-methoxymethyl-9,10-anthraquinone (7), 1-methoxy-3,6-dihydroxy-2-hydroxymethyl-9,10-anthraquinone (8), 1,3,6-trihydroxy-2-hydroxymethyl-9,10-anthraquinone 3-O-beta-primeveroside (9), and 3,6-dihydroxy-2-hydroxymethyl-9,10-anthraquinone (10). Structure assignments for all compounds were established by means of mass and NMR spectroscopies, chemical methods, and comparison with published data. The new anthraquinones were derivatives of munjistin and lucidin.     

Chemical Constituents from Bletilla ochracea Schltr.

To study the chemical constituents in Bletilla ochracea Schltr.,repeated column chromatographies and preparative TLC were used for the isolation of compounds,and spectroscopic techniques(NMR,IR,UV and MS)were used for their structural identification.Seven compounds,2,7-bis(allyloxy)-5-methoxy-3-methyl-9,10-dihydrophenanthrene(1),gastrodin(2),gastrodigenin(3),β-sitosterol(4),stigmasterol(5),4-hydroxybenzaldehyde(6),and daucosterol(7)were obtained from the roots of B.ochracea Schltr.Compound 1 is structurally illustrated as a novel compound,and the others are isolated from the title plant for the first time.     

New stilbenoids from Pholidota yunnanensis and their inhibitory effects on nitric oxide production

Six new stilbenoids, a (bibenzyldihydrophenanthrene) ether designated phoyunnanin D (1), a bis(dihydrophenanthrene) ether designated phoyunnanin E (2), and four stilbenes designated phoyunbene A-D (3-6), were isolated from the air-dried whole plant of Pholidota yunnanensis ROLFE. The new compounds were identified as 7-[2-(3-hydroxyphenethyl)-4-hydroxy-6-methoxyphenoxy]-4-hydroxy-2-methoxy-9,10-dihydrophenanthrene (1), 1-[(9,10-dihydro-4-hydroxy-2-methoxy-7-phenanthrenyl)oxy]-4,7-dihydroxy-2-methoxy-9,10-dihydrophenanthrene (2), trans-3,3'-dihydroxy-2',4',5-trimethoxystilbene (3), trans-3,4'-dihydroxy-2',3',5-trimethoxystilbene (4), trans-3,3'-dihydroxy-2',5-dimethoxystilbene (5), and trans-3-hydroxy-2',3',5-trimethoxystilbene (6) based on spectroscopic evidence. Furthermore, the inhibitory effects of compounds 1-6 on nitric oxide production in a murine macrophage-like cell line (RAW 264.7) activated by lipopolysaccharide and interferon-gamma were examined.     

Isolation of four new flavonoids from Melicope triphylla

Four new flavonoids, 3,5-dihydroxy-7,8-dimethoxy-3',4'-methylenedioxyflavone (1), 3,5-dihydroxy-7-methoxy-3',4'-methylenedioxyflavone (2), 3,5-dihydroxy-7-isopentenyloxy-8-methoxy-3',4'-methylenedioxyflavone (3) and 5-hydroxy-3-isopentenyloxy-7-methoxy-3',4'-methylenedioxyflavone (4), were isolated from the leaves of Melicope triphylla. In addition, two known flavonoids were detected including 5-hydroxy-3,7-dimethoxy-3',4'-methylenedioxyflavone (5) and 5-hydroxy-7-isopentenyloxy-3,8-dimethoxy-3',4'-methylenedioxyflavone (6). The structures of the new compounds were established by spectroscopic methods.     

Phenanthrenes from Juncus effusus with anxiolytic and sedative activities

Eight phenanthrenes, 7-carboxy-2-hydroxy-1-methyl-5-vinyl-phenanthrene (1); 2,7-dihydroxy-1-methyl-5-aldehyde-9,10-dihydrophenanthrene (2); dehydroeffusol (3); dehydrojuncusol (4); 7-carboxy-2-hydroxy-1-methyl-5-vinyl-9,10-dihydrophenanthrene (5); 8-carboxy-2-hydroxy-1-methyl-5-vinyl-9,10-dihydrophenanthrene (6); effusol (7) and juncusol (8), were isolated from the aerial part of Juncus effusus. Compounds 1 and 2 were identified as new constituents. Compounds 7 and 8 showed anxiolytic and sedative activities.