生物化学与医药 海洋抗癌药物的开发与目标提取物的发现

Southern Ocean seaweeds: A resource for exploration in food and drugs Aquaculture

Benthic macroalga or seaweed, a wonder plant in the sea, has been attracting the human mind since centuries. Countries of south and south East Asia have put in extensive use of this plant for various purposes such as food, feed, fodder, etc. Development of seaweed in these countries was favored by their ready availability and proximities to centers of human population that were particularly concentrated in coastal areas. In the beginning, those seaweed species that could be used for food were the first to be utilized and later the other species were found to yield industrial, medicinal, pharmaceutical and cosmetic products.

A number of constraints will be required to be adapted if world's seaweed industry is to be developed and stabilized. This is mainly because of uncertainty in supply of raw material and sudden burst in demand that occur in cycles. The seaweed resources have undergone successive periods of over exploitation and neglect. Alternatively, new areas shall have to be explored which could supply rich and high quality seaweeds. The Southern Ocean has immense potential for attracting urgent attention for development and exploitation of seaweed resources.

A number of investigations are underway to assess the uses of Antarctic seaweeds. Recently, an active ingredient from Antarctic seaweed has been identified, which blocks the effects of metalloproteinase, an enzyme that accelerates the skin aging process. A skin care products derived from polar seaweeds has been a latest craze in France and are dedicated to men between 25 and 50 years of age. Antarctic red algae have recently been identified for their chemopersity, containing compounds possessing antibacterial and other inhibitive properties to marine animals. The important fact remains that before we go for actual harvesting it is necessary that we have full details of their ecophysiology and annual cycle of occurrence at particular region and devise a legal framework after extensive debate with experts, for sustainable use of this valuable resource.

Environmental costs of mercury pollution

Science of The Total Environment

Mercury (Hg) has been used for millennia in many applications, primarily in artisanal mining and as an electrode in the chlor–alkali industry. It is anthropogenically emitted as a pollutant from coal fired power plants and naturally emitted, primarily from volcanoes. Its unique chemical characteristics enable global

atmospheric transport and it is deposited after various processes, ultimately ending up in one of its final sinks, such as incorporated into deep sediment or bioaccumulated, primarily in the marine environment. All forms of Hg have been established as toxic, and there have been no noted biological benefits from the metal. Throughout time, there have been notable incidents of Hg intoxication documented, and the negative health effects have been documented to those chronically or acutely exposed. Today, exposure to Hg is largely diet or occupationally dependent, however, many are exposed to Hg from their amalgam fillings. This paper puts a tentative monetary value on Hg polluted food sources in the Arctic, where local, significant pollution sources are limited, and relates this to costs for strategies avoiding Hg pollution and to remediation costs of contaminated sites in Sweden and Japan. The case studies are compiled to help policy makers and the public to evaluate whether the benefits to the global environment from banning Hg and limiting its initial emission outweigh the benefits from its continued use or lack of control of Hg emissions. The cases we studied are relevant for point pollution sources globally and their remediation costs ranged between 2500 and 1.1 million US$ kg? 1Hg isolated from the biosphere. Therefore, regulations discontinuing mercury uses combined with extensive flue gas cleaning for all power plants and waste incinerators is cost effective.

海洋开发与环境安全

Drugs and personal care products as ubiquitous pollutants: occurrence and distribution of clofibric acid, caffeine and DEET in the North Sea

An analytical method is presented, which allows the simultaneous extraction of neutral and acidic compounds from 20-L seawater samples at ambient pH (8.3). It is based on a solid-phase extraction by means of a polystyrene–pinylbenzene sorbent and gas chromatographic-mass spectrometric detection, and provides detection limits in the lower pg/L range. The method was applied to the screening of samples from different North Sea areas for clofibric acid, diclofenac, ibuprofen, ketoprofen, propyphenazone, caffeine and N,N-diethyl-3-toluamide (DEET). Whereas clofibric acid, caffeine and DEET showed to be present throughout the North Sea in concentrations of up to 1.3, 16 and 1.1 ng/L, respectively, propyphenazone could only be detected after further clean-up. Diclofenac and ibuprofen were found in the estuary of the river Elbe (6.2 and 0.6 ng/L, respectively) but in none of the marine samples. Ketoprofen was below the detection limit in all samples.

The stability and persistence of diflubenzuron in marine sediments studied under laboratory conditions and the dispersion to the sediment under a fish farm following medication

A high performance liquid chromatographic (HPLC) method was developed to determine the concentration of diflubenzuron, a delousing agent used in fish farming, in marine mud and shell sand. The recovery of diflubenzuron from mud was 100.8±1.1% and 105.5±4.3% for shell sand. The limit of quantitation was found to be 0.1 μg g?1. The stability of diflubenzuron was studied under laboratory conditions in marine sediments at different temperatures (4 and 14°C). No degradation of diflubenzuron occurred in the organic rich mud sediment or in the shell sand sediment during the experimental period of 204 days. Increasing the temperature from 4 to 14°C had no effect on the stability. Furthermore, diflubenzuron showed to be persistent in both mud and shell sand sediment since no detectable diffusion from the sediment to the water phase occurred during the experimental period of 204 days. Increasing

the water current in the tanks had no effect on the persistence. Under field conditions, the concentrations of diflubenzuron found in the organic material from sediment traps placed 2 m from the bottom under the cage in a fish farm during medication were high and ranged from 71 to 259 μg g?1. The concentrations of diflubenzuron in the sediment under the fish farm were, however, low, with a maximum concentration of 5.4 μg g?1. The dispersion of diflubenzuron to the sediment was limited to less than 20 m from the edge of the cage in every direction. Fifteen months following the medication, only traces (<0.1 μg g?1) of diflubenzuron were detected in the sediment under the fish farm. Possible explanations for this decrease are resuspension and redistribution of sediment and/or oxic degradation of the drug.

Ready for a comeback of natural products in oncology

Biochemical Pharmacology

Since the late 1990s and the rapid expansion of monoclonal antibodies and synthetic protein kinase inhibitors in oncology, anticancer natural products fell out of fashion with the pharmaceutical industry. But in 2007 with the approval of three new drugs derived from natural products, the emergence of promising antitumor compounds from microorganisms (e.g. alvespimycin, salinosporamide) and the growing importance of new formulations of known natural product-derived drugs (nanoparticle formulations, oral forms), we are witnessing a new wave for natural products in oncology. The recent approval of the microtubule-targeted epothilone derivative ixabepilone (Ixempra?), the DNA-alkylating marine alkaloid trabectedin (Yondelis?) and the inhibitor of mTOR protein kinase temsirolimus (Torisel?) is emblematic of the evolution of the field which combines the long established finding of conventional cytotoxic agents and the emergence of molecularly targeted therapeutics. These three examples also illustrate the increasing importance of microbial sources for the discovery of medically useful natural products. The contribution of innovative biological targets is also highlighted here, with references to proteasome inhibitors and novel approaches such as manipulation of mRNA splicing. Altogether, these observationsplead for the return of natural products in oncology.

Marine natural products targeting phospholipases A2

Phospholipases A2 (PLA2s) form a family of enzymes catalyzing the hydrolysis of membrane phospholipids into arachidonic acid, which is the major precursor of pro-inflammatory eicosanoids. As a result, PLA2s have been considered as potential targets in anti-inflammatory drug discovery.

Marine natural products are a rich source of bioactive compounds, including PLA2 inhibitors. Here, we review the properties of marine PLA2 inhibitors identified since the first discovery of PLA2 inhibitory activity in the marine natural product manoalide in the mid 1980s.

Discovery and development of the anticancer agent salinosporamide A (NPI-0052) Bioorganic & Medicinal Chemistry

The discovery of the anticancer agent salinosporamide A (NPI-0052) resulted from the exploration of new marine environments and a commitment to the potential of the ocean to yield new natural products for drug discovery and development. Driving the success of this process was the linkage of academic research together with the ability and commitment of industry to undertake drug development and provide the resources and expertise to advance the entry of salinosporamide A (NPI-0052) into human clinical trials. This paper offers a chronicle of the important events that facilitated the rapid clinical development of this exciting molecule.

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