中国大戟属植物中二萜成分的化学及生物活性

大约有80种大戟属植物广泛分布于我国,并在民间用来治疗皮肤病、水肿、结核或作为泻药和利尿剂使用.本文综述了近20年来中国产大戟属植物中14个骨架类型共150多个二萜类成分的化学研究,包括最近报道的4个具有新骨架的二萜和2个二聚体.中国产大戟属植物中的一些二萜类成分具有抗肿瘤、抗病毒、促进神经生长因子增长、皮肤刺激、致癌以及镇痛安神的活性.本文还就大戟属中二萜类成分可能的生源代谢途径提出了假设,并对该属未来的研究进行了展望.     

具有生物活性的有机锗化合的研究新进展

综述了近年来发展的具有各种生物活性的六类有机锗化合物的合成及生物活性，即倍半锗和介吗川类有机化合的，锗氧杂，锗氮杂及锗硫杂环酮类化合物，呋喃，噻唑，咪唑、嘧啶取代锗烷及其类似物，烷锗醇，熔锗醚和烷锗酮类化合物，卟啉锗类经合物，其它具有生物活性的有机锗化合物这六类有机锗化合物，并对该领域的研究前景作了展望。     

积雪草酸生物活性的研究进展

积雪草酸属于五环三萜类化合物,是中药积雪草的重要组分,具有广泛的生物活性,如治疗皮肤创伤和慢性溃疡、肝保护、抗抑郁、防治心脑血管疾病、抗阿尔茨海默病等。近年来,关于积雪草酸的药理活性、临床应用及结构修饰等方面的报道越来越多。本文就积雪草酸的药理活性及构效关系等的研究进展进行综述,为今后对积雪草酸的进一步研究提供参考。     

一类新型双有机锗化合物及其生物活性

概要介绍了一类新型双β－羧乙基锗氢氧化物合成，结构及理化性质，重点报道了它们对体外Ｏ２＾－和ＯＨ．自由基的清除活性和抑制人肝癌细胞的作用。     

含氟吡啶羧酸酯类化合物的合成及生物活性

为了寻找具有生物活性的新化合物,以氟乙酸甲酯、氰乙酰胺和甲酸乙酯为起始原料,经环合、氯化、水解、酰氯化等反应合成了含氟吡啶酰氯中间体,再与醇类和酚类反应合成了一系列含氟吡啶羧酸酯类化合物,总收率约38%。其结构经1HNMR、13CNMR、IR、MS及元素分析测试技术确证。初步杀虫抑菌活性测试表明,部分化合物1e、1i、1j和1k在500mg/L浓度下,对淡色库蚊的杀死率在61.9%～100%之间,但对几种受试植物病菌的抑制活性很差。化合物1k活性最好,在500mg/L时对粘虫(armyworm)和淡色库蚊(culex mosquito)的杀死率均为100%。初步构效关系分析表明,芳杂环酚的该类化合物有较好的活性,而脂肪醇的该类化合物无活性。     

硒氰酸酯合成方法及硒氰酸酯化合物生物活性研究进展

硒元素作为生物体的必需微量元素,在人类的生长及发育过程中发挥着极其重要的生理作用。有机硒化合物在抗氧化、抗炎、抗肿瘤等方面展现出卓越的生物活性,对有机硒化合物的开发应用研究是目前化学、生命科学、临床医学等研究领域的一个研究热点。硒氰酸盐是有机硒中的一类含硒化合物,近年来,很多学者开发了不少在有机化合物中直接引入硒氰基官能团的新方法,并合成了许多新型有机硒氰基化合物,这些化合物显示出不同的生物活性,引起人们对硒氰基官能团的极大兴趣。本文主要综述了硒氰酸酯化合物的合成方法研究及非甾体硒氰基化合物和甾体硒氰基化合物的研究进展,并初步探讨有机硒的发展及应用前景,希望为具有不同生物活性的新型有机硒分子的设计合成提供有用参考。     

川芎嗪的结构修饰及生物活性

介绍了川芎嗪的结构修饰及其衍生物的生物活性、川芎嗪衍生物合成及其在新药开发方面的发展前景。     

有机磷酸酯农药分子的电子结构和生物活性

本文用CNDO/2法计算了有机磷酸脂农药系列分子的电子结构。引入新参数CB值, 即磷原子的净电荷与最弱的酯键X=P-Y的总键级之比, 表征有机磷酸酯分子生物活性电子效应, 讨论了有机磷酸酯分子生物活性与电子结构的关系。     

Four New Lanostane Triterpenoids from Euphorbia humifusa

Four new lanostane triterpenoids, namely (3β)‐3‐hydroxy‐24‐methylenelanost‐8‐ene‐7,11‐dione ( 1 ), (3β)‐3‐hydroxylanosta‐8,24‐diene‐7,11‐dione ( 2 ), (3β,7α)‐3,7‐dihydroxylanosta‐8,24‐dien‐11‐one ( 3 ), and (3β,11β)‐3,11‐dihydroxylanosta‐8,24‐dien‐7‐one ( 4 ) were isolated from Euphorbia humifusa, together with 2 known compounds. The structures of these new compounds were elucidated on the basis of extensive spectroscopic analysis and comparison with the related known compounds.     

Triterpenoids and other Constituents from Euphorbia Humifusa

A novel lupane‐type triterpenoid, 3,4‐seco‐lupa‐4(23), 20(29)‐dien‐24‐hydroxy‐3‐oic acid (1) and a new cycloartane‐type triterpenoid, 23(E)‐cycloart‐23‐en‐25‐ethoxy‐3β‐ol (7), as well as eighteen known compounds, were isolated from the hot ethanol extract of the whole plant of Euphorbia humifusa Willd. The new structures were characterized by means of spectroscopic methods including 1D, 2D NMR and HRESIMS, and the known ones were established on the basis of comparing their NMR data with those of the corresponding compounds in the literature. In addition, cytotoxicity against selected cancer cell human gastric carcinoma (SGC‐7901) of compounds 1,3,4,6 were measured in vitro.     

New Cytotoxic Triterpenoids from the Aerial Parts of Euphorbia sieboldiana

Phytochemical investigation of the EtOH extract of Euphorbia sieboldiana led to the isolation of four new oleanane‐type triterpenoids, (1β,2α,3β,19β)‐1,2,3,19‐tetrahydroxyolean‐12‐en‐28‐oic acid, (1β,3β,19β)‐1,3,19‐trihydroxyolean‐12‐en‐28‐oic acid, (1β,2α,3β,16β,19β)‐1,2,3,16,19‐pentahydroxyolean‐12‐en‐28‐oic acid, and (1β,2α,3β,19β,23)‐1,2,3,19,23‐pentahydroxyolean‐12‐en‐28‐oic acid, along with 16 known compounds. Their structures were established by extensive 1D‐ and 2D‐NMR, as well as other spectral analyses. Biological evaluation of the four new triterpenoids revealed potent cytotoxic activities against HeLa and Hep‐G2 cells.     

我国大戟二萜酯及其生理活性研究新进展

介绍了我国近１０年来从大戟属植物中发现的二萜酯类新化合物及它们的刺激性，抗癌活性和杀菌作用等生理活性的研究，其中包括５种新发现碳骨架的２０个高氧化型二萜多酯类化合物。     

Antimicrobial Triterpenoids and Ingol Diterpenes from Propolis of Semi-Arid Region of Morocco

The chemical composition and antimicrobial activity of propolis from a semi-arid region of Morocco were investigated. Fifteen compounds, including triterpenoids (1, 2, 7–12), macrocyclic diterpenes of ingol type (3–6) and aromatic derivatives (13–15), were isolated by various chromatographic methods. Their structures were elucidated by a combination of spectroscopic and chiroptical methods. Compounds 1 and 3 are new natural compounds, and 2, 4–6, and 9–11 are newly isolated from propolis. Moreover, the full nuclear magnetic resonance (NMR) assignments of three of the known compounds (2, 4 and 5) were reported for the first time. Most of the compounds tested, especially the diterpenes 3, 4, and 6, exhibited very good activity against different strains of bacteria and fungi. Compound 3 showed the strongest activity with minimum inhibitory concentrations (MICs) in the range of 4–64 µg/mL. The combination of isolated triterpenoids and ingol diterpenes was found to be characteristic for Euphorbia spp., and Euphorbia officinarum subsp. echinus could be suggested as a probable and new plant source of propolis.     

Microwave-assisted Syntheses,Structures and Bioactivities of a-Aminophosphonates Containing Pyrazole and 2-Hydroxybenzyl Units

Using 3-amino-4-cyanopyrazole, salicylaldehyde and dialkylphosphite as materials, a series of a-aminophosphonates containing pyrazole and 2-hydroxybenzyl units were synthesized under microwave irradiation without solvents and catalysts. The structures of the compounds were verified by IR, 1H NMR, J3C NMR and elemental analysis. The crystal structure of diisobutyl {a-[3- （4-cyano-lH-pyrazol）amino）]-N-（2-hydroxylbenzyl）}phosphonate （4d, C19H27N404P） was deter- mined by single-crystal X-ray diffraction. Compound 4d crystallizes in the orthorhombic system, space group Pbcn with a = 17.329（4）, b = 20.091（5）, c = 12.433（3）/k, V = 4328.7（17） A3, M,. = 406.42, Dc = 1.247 g/cm3, Z = 8, F（000） = 1728,μ = 0.158 mm-1, MoKa radiation （2 = 0.71073 A）, the final R = 0.064 and wR = 0.0169 for observed reflections with I 〉 2σ（I）. X-ray diffraction analysis reveals that two planes lie in 4d, and the dihedral angle is 85.76°. Intermolecular O（1）-H（1B）-O（2）, N（1）-H（1）-N（4）, N（3）-H（3）.-.N（2） and N（3）-H（3）...O（1） hydrogen bonds are found in the structure. All the compounds were evaluated for their antiviral and antitumor activities respectively. Among them, 4d and 4e showed moderate anti-TMV activities at 500 gg/mL, and 4e possessed excellent antitumor activity against PC3 cells at 10 gmol/L.     

Nordammarane Triterpenoids from Sanguisorba officinalis

Three new nordammarane triterpenoids, 12β‐O‐acetyl‐3β,22‐dihydroxy‐23,24,25,26,27‐pentanordammarane ( 1 ), 12β,22‐dihydroxy‐3‐oxo‐23,24,25,26,27‐pentanordammarane ( 2 ), and 3β,12β‐dihydroxy‐23,24,25,26,27‐pentanordammarane‐22‐carbaldehyde ( 3 ), were isolated from the EtOH extract of the roots of Sanguisorba officinalis. Structural elucidation of these new triterpenoids on the basis of spectroscopic analyses, including including 1D‐ and 2D‐NMR, and HR‐ESI‐MS, is reported     

A new aryl glycoside from Euphorbia helioscopia L.

A new aryl glycoside,3″-O-galloyl-benzyl-O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside,was isolated from Euphor- bia helioscopia L.,and its structure was elucidated on the basis of various spectroscopic data analysis.     

New coumarin derivative from Euphorbia wallichii

One new coumarin derivative (1) and two known compounds, quercetin (2) and glyceraldehyde (3) have been isolated from the whole plants of Euphorbia wallichii. Their structures were elucidated by means of extensive spectroscopic analysis (NMR and ESI-MS) and by comparison with data reported in the literature. This is the first isolation of dihydrocoumarin (1) from the genus of Euphorbia.     

A new diterpenoid from Euphorbia helioscopia

<正>A new jatrophane-type diterpenoid,7β,14β,15β-triacetoxy-3β-benzoyloxy-9-oxojatropha-5E,11E-diene,named euphornin N was isolated from Euphorbia helioscopia L.The structure and relative stereochemistry of the new compound was elucidated by spectroscopic methods.