共查询到20条相似文献,搜索用时 152 毫秒
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癌症已成为全球头号杀手,迫切需要从自然界寻找更新、更有效的抗肿瘤药物。植物内生真菌是指生活在宿主植物体内,不会对宿主植物组织引起明显病害症状的一类真菌。众多研究表明,植物内生真菌在寻找抗肿瘤药物中起着至关重要的作用。随着植物内生真菌研究的深入,从植物内生真菌中寻找新的抗肿瘤活性成分已成为研究的热点。大量的抗肿瘤活性成分从植物内生真菌中分离出来,并表现出良好的抗肿瘤活性。目前,植物内生真菌抗肿瘤活性代谢产物主要有紫杉醇、喜树碱、长春新碱,鬼臼毒素等等,本文主要对近年来植物内生真菌抗肿瘤活性成分的研究进展进行了综述。 相似文献
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内生菌广泛存在于植物组织中,作为一种新型的微生物资源,具有丰富的物种多样性,也是发掘新型天然活性物质的重要途径之一,有些内生菌还能产生与宿主植物相同或相似的活性成分。因此从植物内生菌中挖掘抗菌尤其抗临床耐药菌、抗肿瘤等天然活性产物不仅为新药的研发提供了新的方向,还能在一定程度上解决传统的天然产物药源——药用植物生长缓慢、资源紧缺等问题。从多个角度概述了近年来国内外报道的植物内生菌次生代谢产物及其来源、生物活性等方面的主要成果和最新进展,以期为植物内生菌活性代谢产物的研究提供参考。 相似文献
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植物内生真菌——一类应用前景广阔的资源微生物 总被引:13,自引:1,他引:12
从内生真菌的基本生物学特征出发,着重对近年来关于植物内生真菌的生物学作用方面的研究情况进行了综述,主要包括内生真菌对植物生长发育及其抗逆性的促进作用、内生真菌与生物防治、内生真菌与抗癌药物的开发等。最后还对内生真菌的实际应用中存在的问题和可能采取的提供进行了总结。 相似文献
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植物内生真菌---类应用前景广阔的资源微生物 总被引:29,自引:0,他引:29
从内生真菌的基本生物学特征出发,着重对近年来关于植物内生真菌的生物学作用方面的研究情况进行了综述,主要包括内生真菌对植物生长发育及其抗逆性的促进作用、内生真菌与生物防治、内生真菌与抗癌药物的开发等.最后还对内生真菌在实际应用中存在的问题和可能采取的措施进行了总结. 相似文献
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Rainforest endophytes and bioactive products 总被引:20,自引:0,他引:20
Strobel GA 《Critical reviews in biotechnology》2002,22(4):315-333
An increase in the number of people in the world having health problems caused by certain cancers, drug-resistant bacteria, parasitic protozoans, and fungi has caused alarm. An intensive search for newer and more effective agents to deal with these problems is now underway. Endophytes are a potential source of novel chemistry and biology to assist in helping solve not only human health, but plant and animal health problems also. Endophytes reside in the tissues between living plant cells. The relationship that they establish with the plant varies from symbiotic to bordering on pathogenic. Of all of the world's plants, it seems that only a few grass species have had their complete complement of endophytes studied. As a result, the opportunity to find new and interesting endophytes among the myriad of plants is great. Sometimes extremely unusual and valuable organic substances are produced by these endophytes. These compounds may contribute to the host-microbe relationship. The initial step in dealing with endophytic microorganisms is their successful isolation from plant materials. Then, the isolation and characterization of bioactive substances from culture filtrates is done using bioassay guided fractionation and spectroscopic methods. Some of the more interesting compounds produced by endophytic microbes with which we have dealt are taxol, cryptocin, cryptocandin, jesterone, oocydin, isopestacin, the pseudomycins and ambuic acid. This review discusses an approach for bio-prospecting the rainforests, not only to harvest their endophytic microorganisms, but to eventually build a better understanding of the importance and value they have to humankind. 相似文献
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Gary A. Strobel 《Critical reviews in biotechnology》2013,33(4):315-333
ABSTRACT:?An increase in the number of people in the world having health problems caused by certain cancers, drug-resistant bacteria, parasitic protozoans, and fungi has caused alarm. An intensive search for newer and more effective agents to deal with these problems is now underway. Endophytes are a potential source of novel chemistry and biology to assist in helping solve not only human health, but plant and animal health problems also. Endophytes reside in the tissues between living plant cells. The relationship that they establish with the plant varies from symbiotic to bordering on pathogenic. Of all of the world's plants, it seems that only a few grass species have had their complete complement of endophytes studied. As a result, the opportunity to find new and interesting endophytes among the myriad of plants is great. Sometimes extremely unusual and valuable organic substances are produced by these endophytes. These compounds may contribute to the host-microbe relationship. The initial step in dealing with endophytic microorganisms is their successful isolation from plant materials. Then, the isolation and characterization of bioactive substances from culture filtrates is done using bioassay guided fractionation and spectroscopic methods. Some of the more interesting compounds produced by endophytic microbes with which we have dealt are taxol, cryptocin, cryptocandin, jesterone, oocydin, isopestacin, the pseudomycins and ambuic acid. This review discusses an approach for bio-prospecting the rainforests, not only to harvest their endophytic microorganisms, but to eventually build a better understanding of the importance and value they have to humankind. 相似文献
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Endophytes as sources of bioactive products 总被引:56,自引:0,他引:56
Strobel GA 《Microbes and infection / Institut Pasteur》2003,5(6):535-544
An increase in the number of people in the world having health problems caused by various cancers, drug-resistant bacteria, parasitic protozoans, and fungi is a cause for alarm. An intensive search for newer and more effective agents to deal with these disease problems is now under way and endophytes are a novel source of potentially useful medicinal compounds. 相似文献
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Flavonoid compounds in maintenance of prostate health and prevention and treatment of cancer 总被引:4,自引:0,他引:4
Compounds based on a flavonoid (di-phenolic) ring structure are emerging as a potentially important new class of pharmaceutical
compounds with a broad range of biological activities, most prominent of which are their potential role as anticancer agents.
These compounds exert a wide range of upregulating and downregulating effects on signal transduction processes within cells
in both plants and animals. The observation that human communities, which consume large quantities of these compounds (legume-based
vegetarian diets), have a lower incidence of many degenerative diseases and some cancers has led to the speculation that these
compounds, or synthetic analogs, may be of therapeutic value. This article reviews the evidence supporting this hypothesis
and provides some examples of attempts to develop new therapeutics based on dietary isoflavones or novel isoflavonoid structures
in maintaining prostate health and in cancer treatment and management. One of these compounds, phenoxodiol, is now in human
clinical trials and has shown promise in patients with recurrent ovarian cancer where the cancer is refractory or resistant
to standard chemotherapy, and in patients with hormone-refractory prostate cancer. 相似文献
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Hyun Lee Jinhong Ren Russell P. Pesavento Isabel Ojeda Amy J. Rice Haining Lv Youngjin Kwon Michael E. Johnson 《Bioorganic & medicinal chemistry》2019,27(10):1981-1989
The development of new therapeutic agents against the coronavirus causing Middle East Respiratory Syndrome (MERS) is a continuing imperative. The initial MERS-CoV epidemic was contained entirely through public health measures, but episodic cases continue, as there are currently no therapeutic agents effective in the treatment of MERS-CoV, although multiple strategies have been proposed. In this study, we screened 30,000 compounds from three different compound libraries against one of the essential proteases, the papain-like protease (PLpro), using a fluorescence-based enzymatic assay followed by surface plasmon resonance (SPR) direct binding analysis for hit confirmation. Mode of inhibition assays and competition SPR studies revealed two compounds to be competitive inhibitors. To improve upon the inhibitory activity of the best hit compounds, a small fragment library consisting of 352 fragments was screened in the presence of each hit compound, resulting in one fragment that enhanced the IC50 value of the best hit compound by 3-fold. Molecular docking and MM/PBSA binding energy calculations were used to predict potential binding sites, providing insight for design and synthesis of next-generation compounds. 相似文献
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There is increasing concern about the effects of pharmaceutical agents in the environment. The use of synthetic 4-quinolone compounds is rapidly increasing: newer and more complex analogues are being developed by the pharmaceutical industry to meet clinical and veterinary needs. This review aims at stimulating the need to consider the fate of pharmaceuticals in the environment as part of overall drug design and development. Currently, regulatory action is triggered if the predicted environmental concentration exceeds an arbitrarily set value, whereas in some countries, there are no regulations at all. By extension, from a clinical perspective, enviropharmacokinetics and enviropharmacodynamics are proposed to quantify the risk to organisms in the environment in a more realistic fashion that is reflective of concentrations at which hazardous effects are observable on such organisms. Such a new approach integrates our knowledge to address ecosystems and related health problems in a more holistic fashion, thus linking public health, environmental degradation, and ecology. Its success requires more collaboration in research and development of newer antibiotics, with their ultimate fate in the environment being central, to bolster the already existing aspirations of controlling the rapid emergence of resistance. 相似文献
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López-Vallejo F Castillo R Yépez-Mulia L Medina-Franco JL 《Journal of biomolecular screening》2011,16(8):862-868
Parasitic infections caused by Entamoeba histolytica are still major threats against public health, especially in developing countries. Although current therapies exist, the problems associated with parasite resistance and negative side effects make it imperative to search for new therapeutic agents. A systematic scaffold analysis reported herein of a public database containing 474 antiamoebic compounds reveals that benzimidazole is the most active scaffold reported thus far. To gain insights into the antiamoebic activity of novel compounds, the authors report herein the biological activity of 12 compounds, including benzotriazole and indazole derivatives, scaffolds not previously tested against E. histolytica. Compounds with the benzotriazole and indazole scaffolds showed low micromolar activity (IC(50) = 0.304 and 0.339 μM) and are more active than metronidazole, which is the drug of choice used for the treatment of amebiosis. The novel compounds have similar properties to approved drugs. Compounds with novel scaffolds represent promising starting points of an optimization program against E. histolytica. 相似文献
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Andrei Mocan Gianina Crişan 《Journal of enzyme inhibition and medicinal chemistry》2016,31(6):200-210
AbstractConsiderable interest has been shown in natural sources and their compounds in developing new therapeutically agents for different diseases. In this framework, investigations performed on this topic play a central role for human health and drug development process. Schisandra chinensis (Turcz.) Baill is a medicinal and edible plant showing highly advantageous bioactivity and nutritional value. The main bioactive compounds from its fruits are lignans, derivatives of dibenzocyclooctadiene whereas concerning its leaves, phenolic acids, and flavonoids are dominant. The purpose of this study was to investigate the enzyme inhibitory potential on selected carbohydrate hydrolases, cholinesterases, and tyrosinase of extracts from fruits and leaves of Schisandra in relation with their main bioactive compounds. Furthermore, the interactions between dominant compounds (schisandrol A, schisandrol B, schisandrin B, and cinnamic acid) from extracts and selected enzymes were investigated by molecular modeling and molecular dynamic studies in order to explain at a molecular level our findings. 相似文献
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Mehdi Pordel Shirin Ramezani Maryam Jajarmi Mina Sokhanvar 《Russian Journal of Bioorganic Chemistry》2016,42(1):106-110
Resistance to antimicrobial agents is a concern that exists globally and has a considerable impact on human and animal health, so that the discovery of new antibacterial compounds has become increasingly more important in combating infectious disease. In this paper, imidazo[4,5-a]quinindolines are introduced as new antibacterial agents against Gram-positive and Gram-negative bacteria. These pentacyclic compounds are synthesized by the reaction of N-alkyl-5-nitrobenzimidazoles with 2-(1-alkyl-1H-3-indolyl)acetonitrile under basic conditions in excellent yields. The structures of newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, and mass spectral data. The antibacterial activities of the synthesized compounds were screened against standard strains of two Gram-positive and two Gram-negative bacteria using the broth microdilution method. Most of the compounds studied showed promising activities against both types of bacteria. 相似文献
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Yang Q Li Y Dou D Gan X Mohan S Groutas CS Stevenson LE Lai Z Alliston KR Zhong J Williams TD Groutas WC 《Archives of biochemistry and biophysics》2008,475(2):115-120
A new class of carbamylating agents based on the cyclosulfamide scaffold is reported. These compounds were found to be efficient time-dependent inhibitors of human neutrophil elastase (HNE). Exploitation of the three sites of diversity present in the cyclosulfamide scaffold yielded compounds which inhibited HNE but not proteinase 3 (PR 3) or bovine trypsin. The findings reported herein suggest that the introduction of appropriate recognition elements into the cyclosulfamide scaffold may lead to highly selective agents of potential value in the design of activity-based probes suitable for investigating proteases associated with the pathogenesis of chronic obstructive pulmonary disease. 相似文献