一个戊二烯酮化合物的合成及其杀菌抗癌活性

目的:合成戊二烯酮类化合物(1E,4E)-1,5-二(2-羟基苯基)-1 ,4-戊二烯-3-酮,并进行杀菌和抗肿瘤活性测定.方法:水杨醛和丙酮反 应得到目标产物;采用生长速率法和MTT比色法分别测定了该化合物的杀菌抗癌活性.结果:目标物结构经元素分析、红外光谱、核磁共振氢谱确证;该化合物在500 μg/mL浓度下对小麦赤霉病原菌、辣椒枯萎病原菌、苹果腐烂病原菌的抑制率分别为73.0% ±3.3%、70.4%±1.5%、79.2%±2.1%;在5.0ìmol/L下对PC-3细胞的72h的体外抑制率为71 .4%±2.7%.结论:该化合物有较好的杀菌抗癌活性,可以以它为先导进行结构优化,以期设计、合成出高效、选择性好的同类化合物.     

膜荚黄芪中两个新的抗菌异黄烷化合物

膜荚黄芪（Astragalus membranaceus (Fisch.)Bunge）为豆科植物,其根入药,有补气固表、利尿脱毒、敛疮疤生肌、益气补中之功效,主要用于气虚乏力、食少便溏、中气下陷、久泻脱肛、便血崩漏、表虚自汗、气虚     

海绵Hyatella sp．中的含氮化合物

本文报道从中国南海湛江硇洲岛海绵Hyatella sp.分离得到5种含氮化合物,经光谱分析鉴定其结构分别为:环脯氨酰-苏氨酸(1),2-N-(1,3,4-三羟基-17-甲基)十八烷基-2′-羟基-18-甲基二十碳酰胺(2),2-N-(1,3,4-三羟基-17-甲基)十八烷基-2′-羟基-19-甲基二十一碳酰胺(3),2-N-(1,3,4-三羟基-17-甲基)十八烷基-2′-羟基-20-甲基二十二碳酰胺(4)和胸腺嘧啶(5),化合物(1)首次从自然界中发现.     

Three New Cembranoids from a Xisha Soft Coral Sarcophyton sp.

Chemical investigation of the Xisha soft coral Sarcophyton sp. has led to the isolation of eight cembrane-type diterpenoids, including three new compounds, namely sarcophynoids A-C ( 1 – 3 ), and five known analog compounds ( 4 – 8 ). Their structures were clarified based on spectroscopic analysis, and computer-assisted methods including TDDFT-ECD calculation and the quantum mechanical-nuclear magnetic resonance (QM-NMR) method. All the above compounds were tested for their antibacterial activities. Among them, compounds 4 – 7 and 8 exhibited antibacterial activities against S. aureus, B. subtilis, and P. aeruginosa, with MIC of 4–64 μg/mL.     

中国南海豆荚软珊瑚(Lobophytum sp.)中倍半萜化学成分的研究

用硅胶柱层析和凝胶对柱层析对豆荚软珊瑚（Lobophytum sp．）的乙醚提取物进行分离纯化,得到6个倍半萜类似物;根据其化学性质,结合波谱技术（MS,NMR等）,它们分别鉴定为：（＋）-alismol（1）,alismoxide（2）,entspathulenol（3）,（＋）-10α,4β-aromadendranediol（4）,4α,10α-aromadendranediol（5）及aromadendrane-10α, 4β-dilo（6）。这些化合物均系首次从该属珊瑚中分离得到。     

Eimeria clethrionomyis sp. n., Eimeria gallatii sp. n., Eimeria pileata sp. n. and Eimeria marconii sp. n. from the Red-Backed Vole Clethrionomys gapperi Vigors,from Pennsylvania§

SYNOPSIS Four new eimerian species are described from red-backed voles. Clethrionomys gapperi in Pennsylvania. Sporulated oocysts of Eimeria clethrionomyis sp. n. are ellipsoidal, 18.8 (16.5–21.5) × 14.9 (14.0–16.5) with elongate, ovoid sporocysts, 10.6 (9.5–12.0) × 6.1 (5.5–7.0). The oocyst wall is smooth, with 2 layers, and thins, with terminal cap at one or both ends. Polar granules, dark Stieda body and sporocyst residuum are present. The occyst residuum is absent. Sporulated oocysts of Eimeria gallatii sp. n. are ellipsoidal, 27.7 (21–32) × 19.3 (17–24) with ovoid sporocysts, 13.5 (12–15) × 8.8 (8–10). The oocyst wall is smooth, 2-layered, with a micropyle and thin wall at the end opposite the micropyle. Polar granules. Stieda body and sporocyst residuum are present. The oocyst residuum is atypical, of cobwebby material. Sporulated oocysts of Eimeria pileata sp. n. are subspherical to spherical, 25.2 (20.5–29.5) × 22.5(19.5–25.5) with ellipsoidal sporocysts, 13.4(10.5–15.0) × 8.4 (7.5–9.5). The oocyst wall is rough, pitted, striated, 2-layered, with no micropyle. Polar granules, oocyst and sporocyst residuum. Stieda body and stiedal cap are present. Sporulated oocysts of Eimeria marconii sp. n. are ellipsoidal, 13.0 (10.5–15.0) × 10.6 (9.5–12.0) with elongate, ovoid sporocysts, 7.7 (7.0–8.5) × 4.2 (3.0–4.5). The oocyst wall is smooth, single-layered, with no micropyle. Polar granules, dark Stieda body and sporocyst residuum are present. There is no oocyst residuum.     

番荔枝内生真菌Hypoxylon sp.B38的代谢产物研究

从番荔枝内生真菌Hypoxylon sp.B38的固体平板发酵提取物中分离到5个化合物,通过NMR和MS等方法把它们分别被鉴定为Lachnellin D(1)、D ienetriol 9(2)、Lachnellin C(3)、Lachnellin B(4)和Benzo[d][1,3]d ioxol-5-ylm ethanol(5)。     

Osteoclastogenesis Modulatory Steroids from the South China Sea Gorgonian Coral Iciligorgia sp.

A new 9,11‐secosteroid, (22R)‐22‐acetoxy‐3β,6α,11‐trihydroxy‐9,11‐seco‐5α‐cholest‐7‐en‐9‐one, along with twelve known analogues were isolated from the South China Sea gorgonian coral Iciligorgia sp. Their structures were determined by the spectroscopic analysis and comparison with reported data. In an in vitro test of osteoclastic differentiation, three compounds exhibited significant down‐regulating effect whereas two compounds showed significant up‐regulating effect at 0.5 and 1.0 μm . This is the first report of the chemical investigation of the gorgonian Iciligorgia sp. The acetoxy substitution at C‐22 seems to play an important role in the regulating activity.     

海绵Dysideidae sp.中的两个溴代酚类化合物

利用各种层析手段,从海绵Dysideidae sp.的正丁醇部分纯化了两个溴代酚类化合物,通过各种波谱数据鉴定为3,4,5-三溴-2-(2,′4′-二溴-苯氧基)-苯酚(1)和3,4,5,6-四溴-2-(2,′4′-二溴-苯氧基)-苯酚(2)。     

自由生活海洋线虫Chromadorina sp.的生活史研究

线虫种类繁多、分布广泛、数量极丰富,已鉴定的种类有2万多种,据估计其种类约在4万至1千万种之间。秀丽隐杆线虫（Caenorhabditis elegans）因易于培养、生活周期短、细胞结构简单等,被广泛地用作生物学和毒理学研究的模式生物。1990年,Williams等将C．elegans应用于水域、土壤环境的毒理学研究中,Tominaga等提出了以C．elegans为模式生物筛选苯酚类和合成激素毒性和激素活性大小的简便实验系统。[第一段]     

Antitumor Cembrane Diterpenoids from the South China Sea Soft Coral Lobophytum sp.

Two new highly functionalized cembrane diterpenoids named ximaolobophytolides A ( 1 ) and B ( 2 ) as minor components, together with seven related known compounds ( 3 – 9 ), have been isolated and identified from the Ximao soft coral Lobophytum sp. They were characterized by the presence of an α-methylene-γ-lactone moiety. Based on the comprehensive analyses of 1D and 2D NMR spectroscopic data, the absolute configurations of these two new compounds were elucidated by the combination of quantum mechanical (QM)-NMR and time-dependent density functional theory/electronic circular dichroism (TDDFT-ECD) calculation approaches. In the anti-tumor bioassays, compounds 3 – 9 showed moderate to significant inhibitory effects (IC₅₀ values ranging from 29.66 to 0.39 μM) against the proliferations of five tumor cells HEL, A549, H1975, MDA-MB-231, and H1299. It might be worthy to point out that compounds 4 , 7 , and 8 exhibited better anti-tumor activities than that of the positive control Doxorubicin.     

Torulaspora quercuum sp. nov. and Candida pseudohumilis sp. nov., novel yeasts from human and forest habitats

Strains XZ-46A, XZ-105, XZ-129 and XZ-281^T isolated from the oral cavities of healthy Tibetan volunteers were revealed to represent two novel ascomycetous yeast species by molecular taxonomic characterizations. Strain XZ-281^T was most closely related to Candida humilis , but differed from the type strain of the species by eight (1.2%) substitutions in the 26S rRNA gene D1/D2 domain and by >100 (>20%) mismatches in the internal transcribed spacer (ITS) region. Strains XZ-46A, XZ-105 and XZ-129 had identical or similar D1/D2 and ITS sequences with each other and with strain 17YF^T isolated from a leaf of an oak tree ( Quercus sp.). The closest relative of this group was Torulaspora microellipsoides . They differed from the type strain of the species by five (0.9%) substitutions in the D1/D2 domain and >70 (>15%) mismatches in the ITS region. A sexual state was observed in strain 17YF^T, but not in the other four oral strains. An anamorphic name Candida pseudohumilis sp. nov. is proposed for strain XZ-281^T (=AS 2.3956^T=CBS 11404^T) and a teleomorphic name Torulaspora quercuum sp. nov. is proposed for strain 17YF^T (=AS 2.3768^T=CBS 11403^T) and the other three oral strains.