目前处于临床研究的抗肿瘤活性海洋天然产物

人们从海洋生物中分离出数万种包括萜类、甾类、多肽、聚醚类、大环内酯类、生物碱类等具有活性的化合物,目前有近二十种抗肿瘤活性化合物正处于临床研究。     

Marine microbial natural products in antifouling coatings

Ecological problems associated with current antifouling technologies have increased interest in the natural strategies that marine organisms use to keep their surfaces clean and free from fouling. Bacteria isolated from living surfaces in the marine environment have been shown to produce chemicals that are potential antifoulants. Active compounds from the cells and culture supernatant of two bacterial strains, FS‐55 and NudMB50–11, isolated from surface of the seaweed, Fucus serratus, and the nudibranch, Archidoris pseudoargus, respectively, were extracted using solid phase extraction. The extracts were combined with acrylic base paint resin and assayed for antifouling activity by measuring their ability to inhibit the growth of fouling bacteria. These formulations were found to be active against fouling bacteria isolated from marine surfaces. The formulation of antifouling paints that incorporate marine microbial natural products is reported here for the first time. This is a significant advance towards the production of an environmentally friendly antifouling paint that utilises a sustainable supply of natural biodegradable compounds.     

海洋生理活性物质的研究及发展趋势

本文概述海洋生理活性物质特有的特异结构和药理作用,对研究治疗心脑血管疾病、癌症和艾滋病等方面的意义及发展前景。阐述我国近年来从海洋生物活性物质中发现如三丙酮胺、喹啉酮、柳珊瑚酸及其衍生物等观种显著生理活性新化合物及１６种海洋生理活性物质;８种已投入市场的海洋药物及保健品。提出对海洋生理活性物质研制成新药的可行途径及应采取的决策和有效措施;提出应用如基因工程、细胞工程、发酵工程和酶学工程等生物技术来研制、生产出纯度高、质量高、成本低的海洋药物资源物质。海洋生物技术领域的迅速发展,对海洋生物活性物质的研究及开发海洋药物具有广阔的应用前景。     

Free Marine Natural Products Databases for Biotechnology and Bioengineering

Marine organisms and micro‐organisms are a source of natural compounds with unique chemical features. These chemical properties are useful for the discovery of new functions and applications of marine natural products (MNPs). To extensively exploit the potential implementations of MNPs, they are gathered in chemical databases that allow their study and screening for applications of biotechnological interest. However, the classification of MNPs is currently poor in generic chemical databases. The present availability of free‐access‐focused MNP databases is scarce and the molecular diversity of these databases is still very low when compared to the paid‐access ones. In this review paper, the current scenario of free‐access MNP databases is presented as well as the hindrances involved in their development, mainly compound dereplication. Examples and opportunities for using freely accessible MNP databases in several important areas of biotechnology are also assessed. The scope of this paper is, as well, to notify the latent potential of these information sources for the discovery and development of new MNPs in biotechnology, and push future efforts to develop a public domain MNP database freely available for the scientific community.     

Marine Natural Products: The Important Resource of Biological Insecticide

Due to the unique environmental conditions and vast territory, marine habitat breeds more abundant biological resources than terrestrial environment. Massive marine biological species provide valuable resources for obtaining a large number of natural products with diverse structure and excellent activity. In recent years, new breakthroughs have been made in the application of marine natural products in drug development. In addition, the use of marine natural products to develop insecticides and other pesticide products has also been widely concerned. Targeting marine plants, animals, and microorganisms, we have collected information on marine natural products with insecticidal activity for nearly decade, including alkaloids, terpenes, flavonoids and phenols fatty acids, peptides, and proteins, et al. In addition, some active crude extracts are also included. This review describes the insecticidal activities of marine natural products and their broad applications for future research in agriculture and health.     

天然产物防除海洋污损生物的研究进展

天然防污剂是当前海洋污损生物防除的研究热点,本文综述了天然防污剂的种类和来源,以及天然防污剂的防除机理,并着重叙述了天然防污涂料配制时应关注的问题。     

Factors Controlling the Year-Round Variability in Carbon Flux Through Bacteria in a Coastal Marine System

Data from several years of monthly samplings are combined with a 1-year detailed study of carbon flux through bacteria at a NW Mediterranean coastal site to delineate the bacterial role in carbon use and to assess whether environmental factors or bacterial assemblage composition affected the in situ rates of bacterial carbon processing. Leucine (Leu) uptake rates [as an estimate of bacterial heterotrophic production (BHP)] showed high interannual variability but, on average, lower values were found in winter (around 50 pM Leu⁻¹ h⁻¹) as compared to summer (around 150 pM Leu⁻¹ h⁻¹). Leu-to-carbon conversion factors ranged from 0.9 to 3.6 kgC mol Leu⁻¹, with generally higher values in winter. Leu uptake was only weakly correlated to temperature, and over a full-year cycle (in 2003), Leu uptake peaked concomitantly with winter chlorophyll a (Chl a) maxima, and in periods of high ectoenzyme activities in spring and summer. This suggests that both low molecular weight dissolved organic matter (DOM) released by phytoplankton, and high molecular weight DOM in periods of low Chl a, can enhance BHP. Bacterial respiration (BR, range 7–48 μg C l⁻¹ d⁻¹) was not correlated to BHP or temperature, but was significantly correlated to DOC concentration. Total bacterial carbon demand (BHP plus BR) was only met by dissolved organic carbon produced by phytoplankton during the winter period. We measured bacterial growth efficiencies by the short-term and the long-term methods and they ranged from 3 to 42%, increasing during the phytoplankton blooms in winter (during the Chl a peaks), and in spring. Changes in bacterioplankton assemblage structure (as depicted by denaturing gradient gel electrophoresis fingerprinting) were not coupled to changes in ecosystem functioning, at least in bacterial carbon use.     

Secondary Metabolites from Marine Micromonospora: Chemistry and Bioactivities

Marine Micromonospora was revealed to be a rather untapped and a rich source of chemically diverse and unique bioactive natural products. This review is aimed to make a comprehensive survey of secondary metabolites that were derived from marine Micromonospora including chemical diversity and biological activities. A total of 116 compounds from 41 marine Micromonospora species have been reported, covering the literatures from 1997 to 2019. These compounds contain several structural classes such as polyketides (PKS), nonribosomal peptides (NRPS), PKS‐NRPS hybrids, terpenes and others, and they present cytotoxic, antibacterial, antiparasitic, chemopreventive or antioxidant activities.     

海洋放线菌HSL-6抗菌物质的发酵优化与性质研究

海洋放线菌HSL-6能产生对金黄色葡萄球菌有强烈抑制作用的活性物质。对其发酵条件和理化性质进行了研究,正交实验证明,其产生抗菌活性物质的最佳条件:发酵培养基pH6.5、培养温度为28℃、振荡频率300r/min、发酵培养基配方为蔗糖2%、黄豆粉1.5%、酵母浸粉0.15%、CaCO30.05%、甘油0.20%;菌龄为36h,接种量为10%,发酵时间为96h;该抗菌活性物质具有较好的热稳定性、pH稳定性,易溶于氯仿,经薄层层析展开后在紫外光下具有发荧光的特点,纸电泳实验证实该物质是一种弱酸性物质。     

具有抑菌活性的海洋细菌的分离与鉴定

分离并筛选具有抑菌活性的海洋细菌对于开发和利用海洋微生物具有重要意义,该研究从6份海泥样品中共分离到78株海洋细菌,以6种细菌作为敏感指示菌,采用覆盖技术对分离菌株进行拮抗试验,17株海洋细菌具有抑菌活性,对其中2株具有较强抑菌活性的海洋细菌进行革兰氏染色,耐盐试验,运动性观察,过氧化氢酶测定,明胶液化试验,硫化氢产生试验,石蕊牛奶试验,糖类发酵,硝酸盐还原等特性分析,依据《伯杰氏细菌鉴定手册》进行分类鉴定,它们分别应归属为气单孢菌属（Aeromonas sp.）和假单孢菌属（Pseudomonas sp.）。     

海洋真菌Penicilliun sp.W02A的生长特性及抑菌作用的研究

丝状真菌Penicilliunsp.W02A分离自双壳贝文蛤(MeretrixmeretrixL. )。对其生长特性及抑菌作用研究的结果表明,W02A菌是兼性海洋真菌,在海水及淡水中均能生长、繁殖,但W02A更适合海水的环境,其最适生长的pH为6. 0,盐质量分数为7%。采用固体发酵法培养W02A,培养物产生的生物活性物质对革兰氏阳性菌有明显的抑菌作用。     

Terpenoids from Marine Organisms: Unique Structures and their Pharmacological Potential

Marine organisms produce a wide array of fascinating terpenoid structures distinguished by characteristic structural features. Certain structural classes, e.g. cembrane, chamigrene, amphilectane skeletons, and unusual functional groups such as isonitrile, isothiocyanate, isocyanate, dichloroimine and halogenated functionalities occur predominantly in marine metabolites. Especially striking is the frequent occurrence of sesterterpenes in marine organisms, and sponges must be considered as one of the prime sources of these C₂₅ terpenoid compounds. In most cases however, these structural features are not strictly unique for marine natural products. The prominent biological activity of marine terpenes is evident in their ecological role in the marine environment, and makes them interesting as potential drugs. Several terpenoid compounds, e.g. eleutherobin, sarcodictyin, contignasterol derivatives, are in preclinical or clinical development. Despite the many structures known and their ecological and pharmacological importance, only a few biosynthetic studies on marine terpenoid compounds have been performed.     

A database of natural products and chemical entities from marine habitat

Marine compound database consists of marine natural products and chemical entities, collected from various literature sources, which are known to possess bioactivity against human diseases. The database is constructed using html code. The 12 categories of 182 compounds are provided with the source, compound name, 2-dimensional structure, bioactivity and clinical trial information. The database is freely available online and can be accessed at http://www.progenebio.in/mcdb/index.htm     

Isolation of Marine Bacteria by In Situ Culture on Media-Supplemented Polyurethane Foam

Polyurethane foam (PUF) supplemented with various agar media was used in situ to trap marine bacteria and it consequently provided a substrate on which they could be cultivated while exposed to natural seawater in the coral reef area. The bacterial population on the PUF blocks was analyzed by denaturing gradient gel electrophoresis (DGGE) of polymerase chain reaction (PCR)-amplified 16S rDNA fragments. Changing the composition of the cultivation medium in the PUF blocks and selecting different sampling sites resulted in different bacteria being detected on the PUF blocks. For example, iron-utilizing (IU) bacteria, siderophore-producing (SP) bacteria, and petroleum-degrading (PD) bacteria were isolated from PUF blocks and it was discovered that IU and SP contained iron and PD contained hydrocarbon. This method opens up the possibility for isolating novel and useful marine bacteria.     

氨基酸生产和海洋生物的氨基酸资源开发

氨基酸在医药、食品、饲料等领域有着极为重要和广泛的用途,世界上氨基酸总需求量以５～１０％递增,市场竞争十分激烈。生物资源提取、化学合成、生物合成和综合法是生产氨基酸的４种技术,目前的发展趋势为生物合成和综合法,特别是将现代生物工程技术应用于氨基酸生产。另外,氨基酸生产领域另一个新的倾向是海洋生物氨基酸资源的开发和应用,尤其是海洋生物所产生的特殊氨基酸、肽及其衍生物的开发,同时,综合利用海产品加工后的废弃物来生产氨基酸也受到重视。     

Indole and aminoimidazole moieties appear as key structural units in antiplasmodial molecules

From a library of compounds of natural sources, a big series of molecules was chosen by random sampling to evaluate their in vitro antimalarial activity against Plasmodium falciparum and their antifungal activity against Candida sp. From 184 molecules tested, no molecules were active against Candida sp. (MIC > 10 μg/ml) whereas 13 clearly showed high antiplasmodial activity in vitro, with an IC₅₀ less than 1 μg/ml against the chloroquine-resistant strain of P. falciparum FcM29-Cameroon. The molecules with the best antiplasmodial efficacy were 10-hydroxy-ellipticin (IC₅₀: 0.08 μg/ml), tchibangensin (IC₅₀: 0.13 μg/ml), ellipticin hydrochloride (IC₅₀: 0.17 μg/ml), usambarensin (IC₅₀: 0.23 μg/ml), 7S,3S-ochropposinine oxindole (IC₅₀: 0.25 μg/ml), 3,14-dihydro-ellipticin (IC₅₀: 0.25 μg/ml), tetrahydro-4′,5′,6′17-usambarensin 17S (IC₅₀: 0.26 μg/ml), ellipticine (IC₅₀: 0.28 μg/ml), aricin (IC₅₀: 0.3 μg/ml), 10-methoxy-ellipticin (IC₅₀: 0.32 μg/ml), aplysinopsin (IC₅₀: 0.43 μg/ml), descarbomethoxydihydrogambirtannin (IC₅₀: 0.46 μg/ml) and ochrolifuanin A (IC₅₀: 0.47 μg/ml). Among these 13 promising molecules, all except descarbomethoxydihydrogambirtannin, ochrolifuanine A and usambarensine presented here novel biological activities since they had never been described in the literature for their antiplasmodial activity. In spite of the large diversity of the molecules which have been tested, it is interesting to note that the ones active against Plasmodium are all indole derivatives (and one is both indolic and aminoimidazolic). To find new antiplasmodial compounds, ethnopharmacological approaches studying traditional medicine treatments for malaria is largely used but random research produced here an interesting yield (7%) of new antiplasmodial hits and appears therefore complementary to the traditional medicine way.     

海洋放线菌的研究现状及未来展望

【背景】放线菌具有丰富的遗传和功能多样性,其次级代谢产物活性广泛,在临床医疗、农业生产和污染防治等领域都发挥着重要的作用。海洋放线菌由于其特殊的代谢途径,能产生独特的活性天然产物而受到广泛关注。【目的】探究国内外海洋放线菌领域研究的热点和趋势,为后续研究提供参考。【方法】以“marine actinomycetes or marine actinobacteria”为关键词,在Web of Science中检索海洋放线菌领域的文章进行计量分析,使用VOSviewer软件对其关键词、国家、机构、作者、发表时间进行可视化分析。【结果】海洋放线菌领域的文章发表数量总体呈逐年上升趋势,主要集中在微生物学及药学领域,中美两国在论文数量和引用频次上远超其他国家,海洋放线菌领域的研究集中在菌株的分离鉴定、活性天然产物挖掘以及生物信息学等方面。【结论】海洋放线菌在全球范围内愈发受到重视,国内外机构应当加强合作,运用生物信息学技术进一步挖掘活性次级代谢产物,推动海洋放线菌领域进一步发展。     

Screening of Marine Bacteria for the Production of Microbial Repellents Using a Spectrophotometric Chemotaxis Assay

A method for screening marine bacteria for the production of microbial repellents has been developed. The spectrophotometer provided quantitative information on bacterial chemotaxis in response to extracts from other strains of marine bacteria. Aqueous extracts were incorporated into an agar plug at the base of a cuvette, which was overlaid with a suspension of a motile strain. Negative chemotaxis of the motile strain in response to diffusion of repellent compounds from the agar could be measured by a fall in the optical density, allowing the direct screening of supernatants for repellent activity. Three strains producing metabolites with a repellent effect on a motile marine bacterium were identified. Antibiotic activity and the repellent effect of the supernatants were compared, with no significant correlation being found. The screening method will therefore allow the identification of bioactive metabolites that would be overlooked using traditional antibiotic screening strategies. Received March 4, 1998; accepted November 11, 1998.     

Bacterial Biofilm in Seawater: Cell Surface Properties of Early-attached Marine Bacteria

The development of antifouling strategies in seawater requires knowledge of the physico-chemical properties of the cell surfaces of early adherent bacteria. The hydrophilic, electrostatic and the Lewis acid-base cell surface properties of eleven marine bacteria were characterized. Although these bacteria adhered to a hydrophilic support immersed for 3 and 6?h, they presented various physico-chemical properties. Eleven strains possessed a hydrophilic surface and five a hydrophobic surface. Although the majority of the bacteria presented an electron-donating character, some could not generate Lewis acid-base interactions with the support. On the other hand, all strains possessed an isoelectric point ranging from 2.2 to 3.4 and were negatively charged at the pH of seawater. Hydrophilicity was a preponderant property among these bacteria, but other properties should not be ignored. The development of new antifouling paints must take account all the possible interaction levels used by the bacteria to adhere to an immersed surface.