Marine biodiversity as a source of chemical diversity

Total global biodiversity is estimated at between 3 and 500 × 10⁶ species of prokaryote and eukaryote organisms spread across 70 or more phyla. The marine macrofauna alone are estimated between 0.5 and 30 × 10⁶ species and represents a broader range of taxonomic diversity than that found in the terrestrial environment, which has been the traditional source of natural products. With a typical eukaryote possessing 50,000 genes, the global marine macrofauna are the source of 2.5 × 10¹⁰ to 1.5 × 10¹² primary products and an associated extensive range of secondary products. However, only a few thousand novel compounds from marine organisms have been described. These compounds have proven unique in chemical and pharmacological terms but, as yet, no therapeutic agents have resulted. Given a broader drug discovery strategy, and facilitated by technological advances, it is predicted that the characterisation of marine chemical diversity will be accelerated. Strategies for drug discovery from the virtually untapped chemical diversity of marine organisms are discussed. © 1994 Wiley-Less, Inc.     

Evidence for the causal role of endogenous interferon-alpha/beta in the regulation of angiogenesis,tumorigenicity, and metastasis of cutaneous neoplasms

Primary tumor growth and metastasis depend on angiogenesis, which is determined by the balance between proangiogenic and antiangiogenic molecules. Interferon (IFN)-α and -β inhibit angiogenesis through downregulation of interleukin-8, matrix metalloproteinase-9, and basic fibroblast growth factor. To provide evidence for the causal role of IFN-α/β in the induction of neoplasms, their angiogenesis, and hence, progressive growth, we carried out experiments using 129S6 IFN-α/β receptor −/− mice back-crossed to BALB/c nude mice. Subcutaneous angiogenesis was determined following implantation of gelfoam sponges containing 0.4% agarose and several proangiogenic molecules. Tumorigenicity and production of lung metastasis were determined subsequent to subcutaneous and intravenous injections, respectively, of highly metastatic A375SM human melanoma cells. Carcinogenesis was induced by chronic exposure of mice to UVB radiation (5 kJ/m², 3 times/week). Angiogenesis, tumorigenicity, and production of metastasis, as well as development of autochthonous skin tumors, were all accelerated in IFN-α/β receptor −/− mice as compared to control mice. Collectively, the data show that inability to respond to endogenous IFN-α/β (through a mutation in the IFN-α/β receptor) leads to increased susceptibility to carcinogenesis, enhanced angiogenesis, tumorigenicity, and metastasis. This revised version was published online in July 2006 with corrections to the Cover Date.     

Viruses Infecting Marine Brown Algae

Viruses infecting algal hosts possess large double-stranded DNA as genomes. We have recently identified a family of viruses specific for filamentous brown algae. In contrast to the better known Chlorella viruses with their lytic infection cycle, marine brown algal viruses latently occur in their host cells and are induced to multiply in response to a variety of external stimuli such as change in light and temperature. Here, I summarize the known properties of this family of viruses and discuss their taxonomic classification.     

高效液相色谱-电感耦合等离子体质谱法测定海鱼中无机砷

目的建立测定海鱼中无机砷含量的高效液相色谱-电感耦合等离子体质谱法。方法海鱼样品经稀硝酸超声热水浴提取后,AS7阴离子交换色谱柱分离,3.5 mmol/L(NH4)2CO3+1%甲醇与100 mmol/L(NH4)2CO3+1%甲醇流动相梯度洗脱,电感耦合等离子体质谱仪测定,以保留时间定性,外标法定量。结果在1~100μg/L的线性范围,6种砷形态化合物的回归方程均呈良好的线性关系,相关系数均优于0.9996,检出限为0.05~0.25μg/L,定量限为0.17~0.84μg/L,3个浓度加标回收率为88.5%~106.4%,相对标准偏差为2.5%~4.9%。结论本方法满足海鱼中无机砷含量的测定要求,提取快速,稳定,操作简单,检出限低,方法的重现性好,灵敏度高。     

苦参碱的镇痛作用部位及机制研究

目的:研究苦参碱的镇痛作用部位及机制.方法:采用小鼠醋酸扭体法,观察用后扭体反应数,舔小足潜期及组织NO含量的变化.结果:苦参碱侧脑室注射(icv)0.25,0.5nm/kg,ip或iv3.75,7.5,15,30mg/kg均可显著减少小鼠扭体反应数,并呈量效关系;ip与iv同等剂量的苦参碱,对小扭体反应的抑制欧以iv为强,给药后各时段的ip抗扭体半数有数量(ED50)均大于iv抗扭体ED50,ip苦参碱7.5,30mg/kg可显著降低醋酸致痛小鼠脑组织NO含量,进一步研究发现苦碱延长小鼠舔小足潜伏期的作用可被沦钙所拮抗,而被维拉帕米所增强.结论:苦参碱的镇痛作用部位在中枢,其镇痛作用可能与影响Ｃa^2 内流和减少ＮＯ生成有关.     

Assessment of polynuclear aromatic hydrocarbons ecotoxicity threshold in marine sediments through in situ input/decay measurements

The ability of decomposers to process variable amounts of xenobiotics in the marine sediment is a useful aggregate indicator of their capacity to prevent their accumulation and eventual ecotoxic effects. Since decomposition processes depend on environmental factors at the sediment which are difficult to mimic in laboratory systems, in situ evaluations in undisturbed sediments are of great interest. A method and its results are presented to evaluate the decomposition rates of PAHs (polynuclear aromatic hydrocarbons) in coastal undisturbed marine sediments at different levels of pollution input. The method is based on the application of pulse chromatography concepts to interpret trap and bed sediment monitoring data obtained at regular time intervals, using models of the water column as an anisotropic carrying medium. The results are for a 14 month data series from moderately polluted sediments near an urban site and at a more distant nearly pristine site on the south Atlantic coast. QSAR (quantitative structure activity relations) indicate that decay rates increase with higher UV absorption and lipidic solubility. At low levels of total PAH input to the sediments (<0.05 g day^–1 g^–1), decomposition mechanisms effectively process these compounds within a few days. At higher input levels (up to 0.12 g day^–1 g^–1), decomposition lags behind the inputs by approximately 25% and PAHs accumulate in the sediment. In situ estimates of the PAH input/decay ratios provide reliable ecosystem indicators of a safe threshold for anthropogenic inputs of PAHs to the marine environment and a basis for receptor-based standards aimed at their regulation.     

海绵动物的生物活性产物及其药理作用

概括来源于海洋海绵动物中新发现的36种生物活性次生代谢产物，阐述其化学成分及药理作用的研究进展。其化学成分具有生物碱、甾醇、萜类、大环内酯、肽类等。经药效评价且有抗菌、抗病毒、抗肿瘤以及心血管活性等药理作用。这些具明显药理作用的生理活性化合物，作为新药先导化合物进行研究开发，具有良好的应用前景。     

褐藻酸性寡糖对帕金森病大鼠纹状体、杏仁核多巴胺释放的影响

采用快速周期伏安法(FCV),在以6-羟基多巴胺(6-OHDA)制备的帕金森病(PD)模型大鼠上检测褐藻酸性寡糖HSH971对纹状体(Str)、杏仁核(Amy)多巴胺(DA)释放的影响。结果显示,腹腔注射HSH971 5mg·kg·d~(-1),7d能明显提高PD大鼠损毁侧Str、Amy的DA释放量,而对其健侧无影响。     

生化过程工程与中药现代化

在生化工程20余年的研究工作基础上。结合中药现代化开展了一些技术、材料与设备的研究开发工作。研究植物细胞、组织、器官大规模培养增殖技术，应用于细胞代谢产物、生物转化和人工育种及发根，实现了工厂化生产，并成功研制多种类型的生物反应器；在原有化学工程提取分离技术的基础上，发展了反应分离耦合、微波辅助提取等新技术，实现了高效浸出，并且节能、节水；此外，又发展了包括反胶团萃取、一步三相萃取青霉素、泡沫分级分离、膜分离、高速逆流色谱分离纯化等新技术。高速逆流色谱技术是一种没有固相载体的液一液多级逆流萃取技术，避免了不可逆吸附，已成功用于多种天然产物的分析和分离，作为研究中药指纹图谱的新方法具有很好的精密度和重现性。高效液相色谱、气相色谱、毛细管电泳、质谱等技术在指纹图谱研究中发挥了重要作用。与此同时，还研制了多种分离介质，并在药物的修饰与包埋方面做了大量工作。另外，在海洋药物研究领域，创造了连续培养连续采收的新流程、新技术．进行了转基因藻的培养。用于生产基因工程产品。     

半叶马尾藻化学成分的研究Ⅰ

 目的：对马尾藻科植物半叶马尾藻［Sargassum hemiphyllum(Turn.) Ag.］藻体的甾醇类成分进行研究。方法：利用真空液相层析、Sephadex LH-20层析和反复硅胶柱层析进行分离，根据甾醇的理化性质和光谱数据鉴定其结构。结果：得到5个甾醇类化合物，分别确定为岩藻甾醇(SPⅠ)、24 氢过氧基 24-乙烯基胆固醇(SPⅡ)，(22E，24S)24-甲基-5α胆甾7，22二烯3β，5，6β三醇(SAⅢ)，saringosterol (SPⅣ)和麦角甾醇过氧化物(ergosterol peroxide) (SAⅥ)。结论：SPⅡ，SAⅢ和SAⅥ为首次从褐藻类中发现。