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国际海洋天然产物研究进展及展望--第10次国际海洋天然产物研讨会简介 总被引:10,自引:2,他引:8
国际海洋天然产物研讨会(InternationalSymposium on Marine Natural Products,简称MaNaPro)是反映国际海洋天然产物研究最新趋势、动态和进展的重要的国际性会议,每3年举行1次。自1975年在英国举行第1届MaNaPro会议以来,至今已举行了10次。每次会议都吸引众多国际一流的专家学者前往展示与交流各自的最新研究成果,同时探讨学科新的研究发展方向,对国际海洋 相似文献
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海洋拟诺卡菌由于其独特的代谢功能,成为海洋放线菌次级代谢产物的重要来源。根据2010-2013年初的海洋放线菌天然产物的统计表明,对拟诺卡菌的研究仅次于链霉菌。本文综述了从2001年的第一个海洋来源的拟诺卡菌天然产物至2018年6月17年间报道的65个海洋拟诺卡菌天然产物的微生物来源、结构及其生物活性。其结构包括吡喃酮类、二酮哌嗪类、多肽类等,其中吡喃酮类化合物是主要类型,占海洋拟诺卡菌天然产物总数的46%;而29%的海洋拟诺卡菌天然产物表现出抑菌、细胞毒、抗炎等生物活性。 相似文献
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从海洋天然产物中发现药物近年来再次引起广泛关注。2004年12月,美国FDA批准了第1个源自海洋生物的止痛药齐考诺肽(ziconotide,Prialt),用于治疗疼痛。2007年10月欧盟了第1个抗癌海洋药物海鞘素(ecteinascidin,Yondelis)。本文将举例说明影响药物发现的因素和要完成一种化合物从海洋到临床试验的飞跃会遇到的各种困难,展望未来,分析海洋药物的乐观前景。 相似文献
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Identification of a Natural Product Antagonist against the Botulinum Neurotoxin Light Chain Protease
Eubanks LM Silhár P Salzameda NT Zakhari JS Xiaochuan F Barbieri JT Shoemaker CB Hixon MS Janda KD 《ACS medicinal chemistry letters》2010,1(6):268-272
Botulinum neurotoxins (BoNTs) are the etiological agents responsible for botulism, a disease characterized by peripheral neuromuscular blockade and a characteristic flaccid paralysis of humans. BoNTs are the most lethal known poisons affecting humans and has been recognized as a potential bioterrorist threat. Current treatments for botulinum poisoning are predominately prophylactic in nature relying on passive immunization with antitoxins. Inhibition of the BoNT light chain metalloprotease (LC) has emerged as a new therapeutic strategy for the treatment of botulism that may provide an effective post-exposure remedy. A high-throughput screening effort against the light chain of BoNT serotype A (LC/A) was conducted with the John Hopkins Clinical Compound Library comprised of over 1,500 existing drugs. Lomofungin, a natural product first isolated in the late 1960's, was identified as an inhibitor of LC/A, displaying classical noncompetitive inhibition kinetics with a K(i) of 6.7 ± 0.7 μM. Inhibitor combination studies reveal that lomofungin binding is nonmutually exclusive (synergistic). The inhibition profile of lomofungin has been delineated by the use of both an active site inhibitor, 2,4-dichlorocinnamic hydroxamate, and a noncompetitive inhibitor d-chicoric acid; the mechanistic implications of these observations are discussed. Lastly, cellular efficacy was investigated using a rat primary cell model which demonstrated that lomofungin can protect against SNAP-25 cleavage, the intracellular protein target of LC/A. 相似文献
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得益于基因测序技术、微生物组学研究和生物信息学分析手段的快速发展,人体微生物天然产物研究近年来取得了长足的进展。随着研究的深入,人们发现人体微生物天然产物往往会参与产生菌与宿主或与其他人体微生物之间的相互作用,可以直接或间接地影响人体健康。相应地,不少人体微生物天然产物展现出良好的成药性或作为疾病诊疗新型标志物的潜力。因此,研究人体微生物天然产物不仅能够拓展活性天然产物的来源,促进药物研发,而且在疾病诊断和改善人体健康方面具有重要的意义。综述了人体微生物天然产物研究常用的 3 类策略,并着重介绍了一些具有代表性的化合物的发现方法及其多样的结构与活性,以期为相关方向的进一步深入研究提供参考。 相似文献
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Apratoxins家族是由海洋蓝藻菌中分离得到的一种次级代谢产物,通过抑制共翻译转运过程表现出强力细胞毒性活性,具有作为抑癌药物的开发潜力。近年来由于Apratoxins家族抑制肿瘤的高效活性,人们对它们的合成以及药理机制已经做了大量研究,本文主要对近年来Apratoxins家族的研究进展做一简要介绍。 相似文献
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海洋特殊的生态系统是天然抗肿瘤活性物质的重要来源之一,许多源于海洋生物的抗肿瘤活性化合物已经进入临床研究阶段。简要介绍海洋天然抗肿瘤活性产物的作用机制,综述新近发现的海洋天然抗肿瘤活性化合物的最新临床研究进展。 相似文献
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《Expert opinion on therapeutic patents》2013,23(9):1207-1222
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Natural products and derivatives thereof are of considerable importance in the discovery of new pharmaceuticals, for example, for the treatment of cancer, diabetes, inflammation diseases, and infection diseases caused by bacteria, fungi, viruses, or parasites. The great biodiversity of marine microorganisms is reflected in their huge chemical diversity, which provides a rich source of biologically active compounds. An increasing interest in marine microorganisms as promising producers of new compounds with potential medical applications has raised increasing interest in the sustainable exploration of marine microbial resources for the discovery of new antibiotics, which is highlighted. The bottlenecks in the development of drugs using the large marine natural product pipeline are also discussed. 相似文献
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