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1.
During 2001--2002, research on the pharmacology of marine chemicals continued to be global in nature involving investigators from Argentina, Australia, Brazil, Canada, China, Denmark, France, Germany, India, Indonesia, Israel, Italy, Japan, Mexico, Netherlands, New Zealand, Pakistan, the Philippines, Russia, Singapore, Slovenia, South Africa, South Korea, Spain, Sweden, Switzerland, Thailand, United Kingdom, and the United States. This current article, a sequel to the authors' 1998, 1999 and 2000 marine pharmacology reviews, classifies 106 marine chemicals derived from a diverse group of marine animals, algae, fungi and bacteria, on the basis of peer-reviewed preclinical pharmacology. Anthelmintic, antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antiprotozoal, antituberculosis or antiviral activities were reported for 56 marine chemicals. An additional 19 marine compounds were shown to have significant effects on the cardiovascular, immune and nervous system as well as to possess anti-inflammatory and antidiabetic effects. Finally, 31 marine compounds were reported to act on a variety of molecular targets and thus may potentially contribute to several pharmacological classes. Thus, during 2001--2002 pharmacological research with marine chemicals continued to contribute potentially novel chemical leads for the ongoing global search for therapeutic agents for the treatment of multiple disease categories.  相似文献   

2.
The current marine pharmacology review that covers the peer-reviewed literature during 2003 and 2004 is a sequel to the authors' 1998-2002 reviews, and highlights the preclinical pharmacology of 166 marine chemicals derived from a diverse group of marine animals, algae, fungi and bacteria. Anthelmintic, antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antiprotozoal, antituberculosis or antiviral activities were reported for 67 marine chemicals. Additionally 45 marine compounds were shown to have significant effects on the cardiovascular, immune and nervous system as well as possessing anti-inflammatory effects. Finally, 54 marine compounds were reported to act on a variety of molecular targets and thus may potentially contribute to several pharmacological classes. Thus, during 2003-2004, research on the pharmacology of marine natural products which involved investigators from Argentina, Australia, Brazil, Belgium, Canada, China, France, Germany, India, Indonesia, Israel, Italy, Japan, Mexico, Morocco, the Netherlands, New Zealand, Norway, Panama, the Philippines, Portugal, Russia, Slovenia, South Korea, Spain, Thailand, Turkey, United Kingdom, and the United States, contributed numerous chemical leads for the continued global search for novel therapeutic agents with broad spectrum activity.  相似文献   

3.
During 2000 research on the pharmacology of marine chemicals involved investigators from Australia, Brazil, Canada, Egypt, France, Germany, India, Indonesia, Israel, Italy, Japan, the Netherlands, New Zealand, Phillipines, Singapore, Slovenia, South Korea, Spain, Sweden, Switzerland, United Kingdom, and the United States. This current review, a sequel to the authors 1998 and 1999 reviews, classifies 68 peer-reviewed articles on the basis of the reported preclinical pharmacologic properties of marine chemicals derived from a diverse group of marine animals, algae, fungi, and bacteria. Antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antituberculosis, or antiviral activity was reported for 35 marine chemicals. An additional 20 marine compounds were shown to have significant effects on the cardiovascular and nervous system, and to possess anti-inflammatory or immunosuppressant properties. Finally, 23 marine compounds were reported to act on a variety of molecular targets and thus could potentially contribute to several pharmacologic classes. Thus, as in 1998 and 1999, during 2000 pharmacologic research with marine chemicals continued to contribute potentially novel chemical leads to the ongoing global search for therapeutic agents in the treatment of multiple disease categories.  相似文献   

4.

Background

The review presents the 2005–2006 peer-reviewed marine pharmacology literature, and follows a similar format to the authors' 1998–2004 reviews. The preclinical pharmacology of chemically characterized marine compounds isolated from marine animals, algae, fungi and bacteria is systematically presented.

Results

Anthelmintic, antibacterial, anticoagulant, antifungal, antimalarial, antiprotozoal, antituberculosis and antiviral activities were reported for 78 marine chemicals. Additionally 47 marine compounds were reported to affect the cardiovascular, immune and nervous system as well as possess anti-inflammatory effects. Finally, 58 marine compounds were shown to bind to a variety of molecular targets, and thus could potentially contribute to several pharmacological classes.

Conclusions

Marine pharmacology research during 2005–2006 was truly global in nature, involving investigators from 32 countries, and the United States, and contributed 183 marine chemical leads to the research pipeline aimed at the discovery of novel therapeutic agents.

General significance

Continued preclinical and clinical research with marine natural products demonstrating a broad spectrum of pharmacological activity will probably result in novel therapeutic agents for the treatment of multiple disease categories.  相似文献   

5.
The peer-reviewed marine pharmacology literature in 2007–8 is covered in this review, which follows a similar format to the previous 1998–2006 reviews of this series. The preclinical pharmacology of structurally characterized marine compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, anticoagulant, antifungal, antimalarial, antiprotozoal, antituberculosis and antiviral activities were reported for 74 marine natural products. Additionally, 59 marine compounds were reported to affect the cardiovascular, immune and nervous systems as well as to possess anti-inflammatory effects. Finally, 65 marine metabolites were shown to bind to a variety of receptors and miscellaneous molecular targets, and thus upon further completion of mechanism of action studies, will contribute to several pharmacological classes. Marine pharmacology research during 2007–8 remained a global enterprise, with researchers from 26 countries, and the United States, contributing to the preclinical pharmacology of 197 marine compounds which are part of the preclinical marine pharmaceuticals pipeline. Sustained preclinical research with marine natural products demonstrating novel pharmacological activities, will probably result in the expansion of the current marine pharmaceutical clinical pipeline, which currently consists of 13 marine natural products, analogs or derivatives targeting a limited number of disease categories.  相似文献   

6.
Organic pollutants exhibiting endocrine disrupting activity (Endocrine Disruptors--EDs) are prevalent over a wide range in the aquatic ecosystems; most EDs are resistant to environmental degradation and are considered ubiquitous contaminants. The actual potency of EDs is low compared to that of natural hormones, but environmental concentrations may still be sufficiently high to produce detrimental biological effects. Most information on the biological effects and mechanisms of action of EDs has been focused on vertebrates. Here we summarize recent progress in studies on selected aspects of endocrine disruption in marine organisms that are still poorly understood and that certainly deserve further research in the near future. This review, divided in four sections, focuses mainly on invertebrates (effects of EDs and mechanisms of action) and presents data on top predators (large pelagic fish and cetaceans), a group of vertebrates that are particularly at risk due to their position in the food chain. The first section deals with basic pathways of steroid biosynthesis and metabolism as a target for endocrine disruption in invertebrates. In the second section, data on the effects and alternative mechanisms of action of estrogenic compounds in mussel immunocytes are presented, addressing to the importance of investigating full range responses to estrogenic chemicals in ecologically relevant invertebrate species. In the third section we review the potential use of vitellogenin (Vtg)-like proteins as a biomarker of endocrine disruption in marine bivalve molluscs, used worldwide as sentinels in marine biomonitoring programmes. Finally, we summarize the results of a recent survey on ED accumulation and effects on marine fish and mammals, utilizing both classical biomarkers of endocrine disruption in vertebrates and non-lethal techniques, such as non-destructive biomarkers, indicating the toxicological risk for top predator species in the Mediterranean. Overall, the reviewed data underline the potential to identify specific types of responses to specific groups of chemicals such as EDs in order to develop suitable biomarkers that could be useful as diagnostic tools for endocrine disruption in marine invertebrates and vertebrates.  相似文献   

7.
Petroleum (or crude oil) is a complex mixture of hydrocarbons. Annually, millions of tons of crude petroleum oil enter the marine environment from either natural or anthropogenic sources. Hydrocarbon-degrading bacteria (HDB) are able to assimilate and metabolize hydrocarbons present in petroleum. Crude oil pollution constitutes a temporary condition of carbon excess coupled to a limited availability of nitrogen that prompts marine oil-degrading bacteria to accumulate storage compounds. Storage lipid compounds such as polyhydroxyalkanoates (PHAs), triacylglycerols (TAGs), or wax esters (WEs) constitute the main accumulated lipophilic substances by bacteria under such unbalanced growth conditions. The importance of these compounds as end-products or precursors to produce interesting biotechnologically relevant chemicals has already been recognized. In this review, we analyze the occurrence and accumulation of lipid storage in marine hydrocarbonoclastic bacteria. We further discuss briefly the production and export of lipophilic compounds by bacteria belonging to the Alcanivorax genus, which became a model strain of an unusual group of obligate hydrocarbonoclastic bacteria (OHCB) and discuss the possibility to produce neutral lipids using A. borkumensis SK2.  相似文献   

8.
BackgroundMarine algae are rich in some unique biologically active secondary metabolites having diverse pharmacological benefits. Of these, sterols comprise a group of functional lipid compounds that have attracted much attention to natural product scientists.PurposeThis review was aimed to update information on the health effects of algae-derived phytosterols and their molecular interactions in various aspects of human health and diseases and to address some future perspectives that may open up a new dimension of pharmacological potentials of algal sterols.MethodsA literature-based search was carried out to retrieve published research information on the potential health effects of algal phytosterols with their pharmacological mechanisms from accessible online databases, such as Pubmed, Google Scholar, Web of Science, and Scopus, using the key search terms of ‘marine algae sterol’ and ‘health potentials such as antioxidant or anti-inflammatory or anti-Alzheimer's or anti-obesity or cholesterol homeostasis or hepatoprotective, antiproliferative, etc.’ResultsPhytosterols of marine algae, particularly fucosterol, have been investigated for a plethora of health benefits, including anti-diabetes, anti-obesity, anti-Alzheimer's, antiaging, anticancer, and hepatoprotection, among many others, which are attributed to their antioxidant, anti-inflammatory, immunomodulatory and cholesterol-lowering properties, indicating their potentiality as therapeutic leads. These sterols interact with enzymes and various other proteins that are actively participating in different cellular pathways, including antioxidant defense system, apoptosis and cell survival, metabolism, and homeostasis.ConclusionIn this review, we briefly overview the chemistry, pharmacokinetics, and distribution of algal sterols, and provide critical insights into their potential health effects and the underlying pharmacological mechanisms, beyond the well-known cholesterol-lowering paradigm.  相似文献   

9.
By combining the recently reported repelling natural dihydrostilbene scaffold with an oxime moiety found in many marine antifoulants, a library of nine antifouling hybrid compounds was developed and biologically evaluated. The prepared compounds were shown to display a low antifouling effect against marine bacteria but a high potency against the attachment and growth of microalgae down to MIC values of 0.01 μg/mL for the most potent hybrid. The mode of action can be characterized as repelling via a reversible non-toxic biostatic mechanism. Barnacle cyprid larval settlement was also inhibited at low μg/mL concentrations with low levels or no toxicity observed. Several of the prepared compounds performed better than many reported antifouling marine natural products. While several of the prepared compounds are highly active as antifoulants, no apparent synergy is observed by incorporating the oxime functionality into the dihydrostilbene scaffold. This observation is discussed in light of recently reported literature data on related marine natural antifoulants and antifouling hybrids as a potentially general strategy for generation of improved antifoulants.  相似文献   

10.
11.
Teratogenesis has been a topic of increasing interest and concern in recent years, generating controversy in association with danger to humans and other living things. A veritable host of chemicals is known to be involved, encompassing a wide variety of classes, both organic and inorganic. Contact with these chemicals is virtually unavoidable due to contamination of air, water, ground, food, beverages, and household items, as well as exposure to medicinals. The resulting adverse effects on reproduction are numerous. There is uncertainty regarding the mode of action of these chemicals, although various theories have been advanced, e.g., disruption of the central nervous system (CNS), DNA attack, enzyme inhibition, interference with hormonal action, and insult to membranes, proteins, and mitochondria. This review provides extensive evidence for involvement of oxidative stress (OS) and electron transfer (ET) as a unifying theme. Successful application of the mechanistic approach is made to all of the main classes of toxins, in addition to large numbers of miscellaneous types. We believe it is not coincidental that the vast majority of these substances incorporate ET functionalities (quinone, metal complex, ArNO2, or conjugated iminium) either per se or in metabolites, potentially giving rise to reactive oxygen species (ROS) by redox cycling. Some categories, e.g., peroxides and radiation, appear to generate ROS by non-ET routes. Other mechanisms are briefly addressed; a multifaceted approach to mode of action appears to be the most logical. Our framework should increase understanding and contribute to preventative measures, such as use of antioxidants.  相似文献   

12.
13.
A Standardized Protocol for Assessing Regulators of Pigmentation   总被引:10,自引:0,他引:10  
Varied effects of chemical or biological compounds on mammalian pigmentation have been reported by many groups, but to date, no standardized method has established necessary and/or optimal parameters for testing such agents. A standardized method has been developed to screen compounds with potential effects on pigmentation. The protocol comprises basic parameters to analyze melanogenic effects and allows for further characterization of candidate compounds, providing important insights into their mechanism of action. In this protocol (termed STOPR, for standardized testing of pigmentation regulators), compounds are initially screened using purified tyrosinase and are then tested on melanocytes in culture. After treatment of melanocytes with potentially bioactive compounds, cell proliferation and viability, total melanin accumulated, and melanogenic potential are measured. This protocol is an important first step in characterizing chemical regulation of effects on melanogenesis. When bioactive candidate compounds are identified, testing may proceed for pharmacological or otherwise commercial applications in coculture and/or organ culture models followed by in vivo testing. As an application of this method, results for compounds known to stimulate and/or inhibit melanogenesis (including arbutin, hydroquinone, kojic acid, melanocyte-stimulating hormone, and thymidine dimers) as well as some commercial skin whiteners are reported.  相似文献   

14.

The genus Phoma contains several species ubiquitously present in soil, water, and environment. There are two major groups of Phoma, viz., terrestrial and marine. After 1981 researchers all over the world have focused on marine-derived Phoma for their bioactive compounds. The marine Phoma are very rich sources for novel bioactive secondary metabolites, which could potentially be used as drugs. Recently, a large number of structurally unique metabolites with potential biological and pharmacological activities have been isolated from the marine Phoma species particularly Phoma herbarum, P. sorghina, and P. tropica. These metabolites mainly include diterpenes, enolides, lactones, quinine, phthalate, and anthraquinone. Most of these compounds possess antimicrobial, anticancer, radical scavenging, and cytotoxic properties. The present review has been focused on the general background of Phoma, current approaches used for its identification and their limitations, difference between terrestrial and marine Phoma species. In addition, this review summarizes the novel bioactive compounds derived from marine Phoma and their biological activities.

  相似文献   

15.
Historically, invertebrates have been excellent models for studying endocrine systems and for testing toxic chemicals. Some invertebrate endocrine systems are well suited for testing chemicals and environmental media because of the ease of using certain species, their sensitivity to toxic chemicals, and the broad choice of models from which to choose. Such assays will be useful in identifying endocrine disruptors to protect invertebrate populations and as screening systems for vertebrates. Hormone systems are found in all animal phyla, although the most simple animals may have only rudimentary endocrine systems. Invertebrate endocrine systems use a variety of types of hormones, including steroids, peptides, simple amides, and terpenes. The most well-studied hormone systems are the molting and juvenile hormones in insects, the molting hormones in crustaceans, and several of the neurohormones in molluscs and arthropods. These groups offer several options for assays that may be useful for predicting endocrine disruption in invertebrates. A few invertebrate phyla offer predictive capabilities for understanding vertebrate endocrine-disrupting chemicals. The echinoderms, and to a lesser extent molluscs, have closer evolutionary relationships with the vertebrates than the arthropods and these phyla. The recently identified estrogen receptor structure within the genome of the marine gastropod, Aplysia, indicates that the estrogens, and probably the basic steroid receptor, are quite old evolutionarily. This review of the recent literature confirms the effects of some endocrine-disrupting chemicals on invertebrates--tributyltin on snails, pesticides on insects and crustaceans, and industrial compounds on marine animals.  相似文献   

16.
Rare Actinomycetes from underexplored marine environments are targeted in drug discovery studies due to the Actinomycetes’ potentially huge resource of structurally diverse natural products with unusual biological activity. Of all marine bacteria, 10 % are Actinomycetes, which have proven an outstanding and fascinating resource for new and potent bioactive molecules. Past and present efforts in the isolation of rare Actinomycetes from underexplored diverse natural habitats have resulted in the isolation of about 220 rare Actinomycete genera of which more than 50 taxa have been reported to be the producers of 2,500 bioactive compounds. That amount represents greater than 25 % of the total Actinomycetes metabolites, demonstrating that selective isolation methods are being developed and extensively applied. Due to the high rediscovery rate of known compounds from Actinomycetes, a renewed interest in the development of new antimicrobial agents from rare and novel Actinomycetes is urgently required to combat the increasing number of multidrug-resistant human pathogens. To facilitate that discovery, this review updates all selective isolation media including pretreatment and enrichment methods for the isolation of marine rare Actinomycetes. In addition, this review demonstrates that discovering new compounds with novel scaffolds can be increased by intensive efforts in isolating and screening rare marine genera of Actinomycetes. Between 2007 and mid-2013, 80 new rare Actinomycete species were reported from marine habitats. They belong to 23 rare families, of which three are novel, and 20 novel genera. Of them, the family Micromonosporaceae is dominant as a producer of promising chemical diversity.  相似文献   

17.
Many evaluations estimating safe levels of hydrophobic organic chemicals in sediments do not account for confounding factors such as physical habitat quality or covariance among chemicals. Controlled experiments demonstrating cause and effect can be conducted with spiked sediment toxicity tests, but application of this methodology has been limited in part by concerns about chemical bioavailability and challenges in achieving target concentrations. Relevant literature was reviewed to assess the utility of standardizing sediment equilibration times; hydrophobicity, complex sediment characteristics, and temperature were identified as potentially equally important factors. Disequilibrium appears likely following limited equilibration time but should yield conservative toxicity test results relative to aged field sediments. Nominal and measured concentrations in over 20 published studies were compared to assess spiked chemical recovery (i.e., measured concentration/nominal concentration). Recovery varied substantially among studies and was not readily predictable based on spiking or extraction method, chemical properties, or measured sediment characteristics, although unmeasured differences between sediments appeared to be important. Factors affecting specific studies included chemical adsorption to glassware, biodegradation, and volatilization. Pre- and post-toxicity test analyses are recommended to confirm exposure concentrations. Studies with 2,3,7,8-tetrachloro-dibenzo-p-dioxin (2,3,7,8-TCDD) and hexachlorobenzene (HCB) exemplify the utility of verifying results of field studies using spiked sediment tests. Sediments spiked with these chemicals at concentrations greatly exceeding those in associated field studies caused no adverse effects in test organisms, demonstrating that other chemicals co-occurring in test sediment samples caused toxicity initially attributed to 2,3,7,8-TCDD and HCB in the field studies. Another key application of spiked sediment tests has been the investigation of TOC as the primary factor affecting bioavailability of hydrophobic organic chemicals. A review of LC50s for nine chemicals reported in 12 studies shows that comparable LC50s derived in different sediments generally agree within a factor of five when concentrations are normalized to a constant TOC. Additionally, use of spiked sediment toxicity testing to investigate toxicological interactions among chemicals provides a promising approach to improving the ability to predict sediment toxicity in the field.  相似文献   

18.
Polychlorinated biphenyls (PCBs), persistent chemicals widely used for industrial purposes, have been banned in most parts of the world for decades. Owing to their bioaccumulative nature, PCBs are still found in high concentrations in marine mammals, particularly those that occupy upper trophic positions. While PCB-related health effects have been well-documented in some mammals, studies among dolphins and whales are limited. We conducted health evaluations of bottlenose dolphins (Tursiops truncatus) near a site on the Georgia, United States coast heavily contaminated by Aroclor 1268, an uncommon PCB mixture primarily comprised of octa- through deca-chlorobiphenyl congeners. A high proportion (26%) of sampled dolphins suffered anaemia, a finding previously reported from primate laboratory studies using high doses of a more common PCB mixture, Aroclor 1254. In addition, the dolphins showed reduced thyroid hormone levels and total thyroxine, free thyroxine and triiodothyronine negatively correlated with PCB concentration measured in blubber (p = 0.039, < 0.001, 0.009, respectively). Similarly, T-lymphocyte proliferation and indices of innate immunity decreased with blubber PCB concentration, suggesting an increased susceptibility to infectious disease. Other persistent contaminants such as DDT which could potentially confound results were similar in the Georgia dolphins when compared with previously sampled reference sites, and therefore probably did not contribute to the observed correlations. Our results clearly demonstrate that dolphins are vulnerable to PCB-related toxic effects, at least partially mediated through the endocrine system. The severity of the effects suggests that the PCB mixture to which the Georgia dolphins were exposed has substantial toxic potential and further studies are warranted to elucidate mechanisms and potential impacts on other top-level predators, including humans, who regularly consume fish from the same marine waters.  相似文献   

19.
The Environmental Protection Department (EPD) of the Hong Kong Special Administrative Region Government (HKSARG) commissioned a consultancy study in 1999 to better understand the potential sources, fates, and existing pollution state of toxic substances in Hong Kong's marine environment. A desk-top survey and assessment was first performed on a comprehensive initial list of 556 toxic substances. A Preliminary Priority Toxic Substances List (PPTSL) of 135 chemicals was established, consisting of heavy metals, inorganic compounds, organo-metallic compounds, and trace organics. A territory-wide baseline field sampling and laboratory analysis exercise was then undertaken during 2001–2002 to determine the level of these PPTSL chemicals in the potential pollution sources (effluent discharges, stormwater discharges, air deposition) and the receiving marine environment (water, sediment, biota). A draft Priority Toxic Substances List (PTSL) was developed, taking into account chemicals detected in the local marine environment and those listed under the Stockholm Convention, the Rotterdam Convention, and the International Maritime Organization's Harmful Antifouling System Convention. The draft PTSL chemicals were subject to ecological and incremental human health risk assessments. Based on the risk assessment results, 17 Chemicals of Potential Concern (COPC) for Hong Kong's marine environment were identified, most of which were heavy metals in the sediment. The study findings suggest that Hong Kong's marine environment is not widely polluted with chemicals present at concentrations of toxicological concern. Although a number of potentially problematic pollutants (COPC) were identified, they are confined to a few “hot spots” and are unlikely to pose a territory-wide risk. Based on the study recommendations, the EPD initiated in 2004 a toxic substances monitoring program to keep the COPC in the marine environment under close surveillance.  相似文献   

20.
Summary

The influence of juvenile hormone (JH)-active chemicals on the settlement and metamorphosis of metatrochophore larvae of the polychaete annelid Capitella sp. I of the Capitella complex has been investigated. These studies demonstrate that JH-active chemicals are able to induce settlement and metamorphosis of Capitella larvae, and that these effects may possibly be mediated by protein kinase C induction. Evidence for the presence of JH-active compounds in marine sediments is also presented, suggesting that these chemicals may serve a natural role as chemical cues for settlement and metamorphosis for Capitella larvae in the marine environment.  相似文献   

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