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1.
A new series of 5- or 7-substituted 3-{4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenylimino}-indolin-2-one derivatives were screened for in vitro antioxidant and antimicrobial activities. The results of this study revealed that all synthesized compounds were significantly scavenged DPPH free radicals in a concentration-dependant manner. The IC50 values of all test compounds were found to be between 18.34 and 50.54?µM. All compounds significantly inhibited growth of bacteria and most of the minimum inhibitory concentration values were between 20 and 100?mg?mL?1 indicating potent to moderate antibacterial activity. In conclusion, 3-{4-(5-mercapto-1,3,4-oxadiazole-2-yl)phenylimino)-5 or 7-substituted indolin-2-ones derivatives exhibited moderate antioxidant and antimicrobial activities.  相似文献   

2.
Antimicrobial activity of Red Sea corals   总被引:1,自引:0,他引:1  
Scleractinian corals and alcyonacean soft corals are the two most dominant groups of benthic marine organisms inhabiting the coral reefs of the Gulf of Eilat, northern Red Sea. Antimicrobial assays performed with extracts of six dominant Red Sea stony corals and six dominant soft corals against marine bacteria isolated from the seawater surrounding the corals revealed considerable variability in antimicrobial activity. The results demonstrated that, while the majority (83%) of Red Sea alcyonacean soft corals exhibited appreciable antimicrobial activity against marine bacteria isolated from the seawater surrounding the corals, the stony corals had little or no antimicrobial activity. From the active soft coral species examined, Xenia macrospiculata exhibited the highest and most potent antimicrobial activity. Bioassay-directed fractionation indicated that the antimicrobial activity was due to the presence of a range of compounds of different polarities. One of these antibiotic compounds was isolated and identified as desoxyhavannahine, with a minimum inhibitory concentration (MIC) of 48 μg ml−1 against a marine bacterium. The results of the current study suggest that soft and hard corals have developed different means to combat potential microbial infections. Alcyonacean soft corals use chemical defense through the production of antibiotic compounds to combat microbial attack, whereas stony corals seem to rely on other means.  相似文献   

3.
In the present study, the synthesis of new bis-isatin carbohydrazone derivatives and their antimicrobial and antioxidant activities were investigated. The structures of new compounds were elucidated by Fourier transform infrared, 1H nuclear magnetic resonance and mass spectra. The antimicrobial activity of the compounds was determined by using the two-fold serial dilution technique against various bacterial and fungal species in comparison to standard drugs. All synthesized compounds displayed a broad spectrum of activities with minimum inhibitory concentration values ranging from 6.25 to 100 μg/ml against tested microorganisms. The in vitro antioxidant activity was evaluated using 1,1-diphenyl-2-picryl-hydrazyl and hydrogen peroxide (H2O2), and the total antioxidant capacity by a phosphomolybdenum assay and their ability to chelate ferrous iron. In general, the derivatives were found to exhibit antioxidant activity. Further, the compounds with electron-withdrawing groups at the C5 position demonstrated significant antimicrobial and antioxidant activities.  相似文献   

4.
4-(5-(Methylthio)-1,3,4-thiadiazol-2-ylamino)-2-oxo-2H-chromene-3-carbaldehyde (3) and 4-(5-(ethylthio)-1,3,4-thiadiazol-2-ylamino)-2-oxo-2H-chromene-3-carbaldehyde (4) were prepared. The structures of the newly synthesized compounds were characterized by infrared (IR), nuclear magnetic resonance (NMR) spectral data and elemental analysis. The synthesized compounds were screened in vitro for their antibacterial activities. The synthesized compounds demonstrated moderate antimicrobial activity.  相似文献   

5.
Extracts of 19 of 24 species of sponge collected from Queensland. Australia, inhibited the growth of test microorganisms in in-vitro assays. A similar result has been obtained by earlier workers for extracts of species of sponge obtained from temperate waters. Some of the extracts, including extracts of Thorecta vasiforis, Arenochalina mirabilis and Acanthella kleutha, showed activity against bacterial strains that was comparable with that exhibited by penicillin G and streptomycin against these strains. Gram-positive bacteria were expecially sensitive to many extracts. Little activity was exhibited by any extract against four species of fungi tested. Some of the extracts were markedly toxic to one or more of the test organisms (a fish, a crustacean and a hydroid) used, but no clear pattern linking toxicity to these organisms with antimicrobial properties of the extracts emerged. In general, there bas a negative correlation between antimicrobial activity and surface-fouling, raising the possibility of using freedom from surface-fouling as an indicator of antimicrobial activity. Four of five encrusting species from the undersides of coral boulders showed antimicrobial activity. This study confirmed the value of using methanol-toluene extracts in field-based screening programmes, but emphasised the need to use additional extracting media such as methylene chloride in order to augment the number of antimicrobial compounds detected. There are indications that antimicrobial activity may be widespread in the order Dictyoceratida, in the order Verongida and in the order Axinellida, but sporadic in other orders of Porifera.  相似文献   

6.
This study is the second of two surveys designed to systematically screen extracts from marine plants for antimicrobial effects against ecologically relevant marine microorganisms, and to compare results on a geographical basis. In the preceding survey, extracts from tropical Atlantic marine algae and seagrasses were screened in growth inhibition assays against the pathogenic fungus Lindra thalassiae, the saprophytic fungus Dendryphiella salina, the saprophytic stramenopiles, Halophytophthora spinosa and Schizochytrium aggregatum, and the pathogenic bacterium Pseudoaltermonas bacteriolytica. In this study, the same assay microorganisms were used to examine the antimicrobial effects of lipophilic and hydrophilic extracts from 54 species of marine algae and two species of seagrasses collected from Indo-Pacific reef habitats. Overall, 95% of all species surveyed in this study yielded extracts that were active against one or more, and 77% yielded extracts that were active against two or more assay microorganisms. Broad-spectrum activity against three or four assay microbes was observed in the extracts from 50 to 21% of all species, respectively. Extracts from the green alga Bryopsis pennata and the red alga Portieria hornemannii inhibited the growth of all assay microorganisms. Given that antimicrobial activity was prevalent among extracts of Indo-Pacific marine plants, it is interesting to note that the inhibitory effects of each extract varied considerably between the assay microorganisms. Overall, H. spinosa and D. salina were the most susceptible while L. thalassiae, S. aggregatum, and P. bacteriolytica were the most resistant to the extracts tested. These results provide good evidence that antimicrobial chemical defenses are widespread among Indo-Pacific marine plants. Further, the activity profiles of plant extracts suggest that antimicrobial secondary metabolites can have pathogen-selective or broad-spectrum effects. To confirm these results, chemical studies will be needed to isolate and characterize the compounds responsible for the observed antimicrobial activities.  相似文献   

7.
The potency of free-living and animal-associated marine bacteria to produce antimicrobial substances has been studied in 491 strains isolated from northern and southern parts of the Pacific Ocean. A total of 26% (126 out of 491) of the strains examined produced antimicrobial compounds against 11 test bacterial strains (TBS) including the fish pathogens Aeromonas hydrophila and Vibrio anquillarum. Antimicrobial substances (AS) produced by marine bacteria were especially active against Staphylococcus epidermidis, Proteus vulgaris, Enterococcus faecalis, and Candida albicans. Twelve strains, isolated from different sources, were chosen as promising candidates, producing a number of AS. Production of AS varied within 24 to 72 h, increasing in a culture medium based on natural sea water with Br-ions, and after attachment to polymeric surfaces. In order to study the influence of adsorption, selected strains with a high potential for antimicrobial production were cultivated on polymeric surfaces with different hydrophobicities and chemical functionalities. These parameters of the surface hydrophobicity (measured by means of water contact angles) and chemical functionality of the surfaces were manipulated using the photo- and thermochemistry of a polymeric system (diazo-naphto-quinone/novolak) commonly used as a photoresistant material in semiconducto-manufacturing. The highest antimicrobial activities occurred on hydrophilic surfaces (standard exposed photoresistant films), whereas the number of attached cells was greater on hydrophobic surfaces, characterized as unexposed resistant films. These results suggest that the chemical nature of induced hydrophilicity may also be a major factor in controlling antimicrobial activity of adsorbed bacteria. Received: 5 March 1997 / Accepted: 24 August 1997  相似文献   

8.
基于比较分子力场分析(CoMFA)方法建立20种取代苯酚类化合物抑藻活性(pI)的三维定量构效关系(3D-QSAR)。训练集中16个化合物用于建立预测模型,测试集5个化合物(含模板分子)作为模型验证。已建立的Co MFA模型的交叉验证系数(Q2)、非交叉验证系数(R2)分别为0.915、0.963,说明所建模型具有较强的稳定性和良好的预测能力。该模型中立体场、静电场贡献率依次为48.4%、51.6%,表明影响抑藻活性(pI)的主要因素是取代基的电荷分布,其次是取代基的疏水性和空间位阻。  相似文献   

9.
Marine phytoplankton have been shown to use chemical feeding deterrents to reduce or inhibit zooplankton grazing. In order to screen phytoplankton species for feeding deterrent production and to isolate and identify feeding deterrent compounds, a new, rapid, and reliable laboratory bioassay was developed. This bioassay used the laboratory-reared harpacticoid copepod Tigriopus californicus and measured inhibition of feeding by measuring the fecal pellet production rate. The bioassay was capable of detecting deterrent compounds: (1) adsorbed onto ground fish food (a normally palatable food); (2) dissolved in a mixture of seawater and live Thalassiosira pseudonana cells (a species of diatom which had no feeding deterrent activity); and (3) present in live cell cultures. Method (2) was recommended for use in bioassay-guided fractionation (isolation of chemical compounds), as it was reliable, rapid, accurate, and easy to perform with large numbers of samples. The total bioassay time was < 48 h, and data collection required only a microscope. Methanolic cell extracts of several phytoplankton species were screened for feeding deterrent activity. Extracts from the diatom Phaeodactylum tricornutum and the dinoflagellate Gonyaulax grindleyi gave feeding deterrent responses, while extracts from the diatom Thalassiosira pseudonana gave no feeding deterrent responses. Live P. tricornutum cells deterred feeding at densities of 6x105 cells ml-1. This bioassay should provide a valuable tool in screening phytoplankton for feeding deterrent compounds and determining the chemical nature of these compounds.  相似文献   

10.
The activity of the heterotrophic microbial population in the saline Lake Grevelingen (The Netherlands) and the Mediterranean Etang Salses Leucate (France) was determined by measuring the oxygen consumption rate, and the uptake of 14C-labelled glycollate, pyruvate and an amino acid mixture. The maximum uptake rate of the applied organic compounds in Lake Grevelingen was generally less than 10% of the carbon mineralization rate calculated from the oxygen consumption experiments. Only for pyruvate and glycollate higher values were found of about 30 to 40% with one exceptionally high value for pyruvate of 149%. However, these higher percentages were found in winter, when the activity of the heterotrophic microbial population was very low. In Etang Salses Leucate higher maximum uptake rates of the 14C-labelled compounds were found, relating this uptake to the oxygen consumption rate. Yet the maximum uptake rate is still always lower than 35% of the carbon mineralization calculated from the oxygen uptake rate. Taking into account that maximum uptake rates were considered, the results demonstrate that the uptake of 14C-labelled organic compounds represents a serious underestimation of the activity of the bacterial population in situ. The extent of the underestimation depends on the water type. It was concluded that the determination of the heterotrophic activity by measuring oxygen consumption rates offers a better insight into the carbon mineralization process in natural waters than the uptake experiments with 14C-labelled substrates.Communication no. 228 of the Delta Institute for Hydrobiological Research, Yerseke, The Netherlands  相似文献   

11.
The effect of organic arsenic compounds and inorganic As(V) and As(III) on Vibrio fischeri luminescence and butyrylcholinesterase activity were evaluated using Microtox and microcalorimetric analysis. Organic arsenic compounds were arsenocholine (AsC), arsenobetaine (AsB), dimethylarsinic acid (DMA), monomethylarsonic acid (MMA) and the antibiotic 4-hydroxy-3-nitrobenzene arsonic acid (HNAA, Roxarsone(R)). HNAA, As(III) and As(V) were found to inhibit Vibrio fischeri light emission whereas MMA, DMA, AsC and AsB produced only a slight effect. By contrast, only AsC, AsB and As(III) were found to inhibit butyrylcholinesterase activity. Selected article from the 6th European Meeting on Environmental Chemistry, University of Belgrade, Serbia and Montenegro organized by Prof. Dr. Branimir Jovancicevic (www.research.plymouth.ac.uk/ace).  相似文献   

12.
Studies investigating disease resistance in marine plants have indicated that secondary metabolites may have important defensive functions against harmful marine microorganisms. The goal of this study was to systematically screen extracts from marine plants for antimicrobial effects against marine pathogens and saprophytes. Lipophilic and hydrophilic extracts from species of 49 marine algae and 3 seagrasses collected in the tropical Atlantic were screened for antimicrobial activity against five ecologically relevant marine microorganisms from three separate kingdoms. These assay microbes consisted of the pathogenic fungus Lindra thalassiae, the saprophytic fungus Dendryphiella salina, the saprophytic stramenopiles, Halophytophthora spinosa and Schizochytrium aggregatum, and the pathogenic bacterium Pseudoaltermonas bacteriolytica. Overall, 90% of all species surveyed yielded extracts that were active against one or more, and 77% yielded extracts that were active against two or more assay microorganisms. Broad-spectrum activity against three or four assay microorganisms was observed in the extracts from 48 and 27% of all species, respectively. The green algae Halimeda copiosa and Penicillus capitatus (Chlorophyta) were the only species to yield extracts active against all assay microorganisms. Among all assay microorganisms, both fungi were the most resistant to the extracts tested, with less than 21% of all extracts inhibiting the growth of either L. thalassiae or D. salina. In contrast, over half of all lipophylic extracts were active against the stramenopiles H. spinosa and S. aggregatum, and the bacterium P. bacteriolytica. Growth sensitivity to hydrophilic extracts varied considerably between individual assay microorganisms. While 48% of all hydrophilic extracts were active against H. spinosa, 27% were active against P. bacteriolytica, and only 14% were active against S. aggregatum. Overall, more lipophilic extracts inhibited microbial growth than hydrophilic extracts. The variability observed in the antimicrobial effects of individual extracts against each assay microorganism reflects the importance of choosing appropriate test microbes in assays from which ecologically relevant information is sought. Results from this survey demonstrate that antimicrobial activities are prevalent among extracts from marine algae and seagrasses, suggesting that antimicrobial chemical defenses are widespread among marine plants.  相似文献   

13.
The toxicities of seven chemicals [cadmium (Cd) chloride, potassium dichromate, sodium dodecyl sulfate, potassium chloride (KCl), Triton X-100, zinc (Zn) chloride and copper (Cu) (II) sulfate] were determined using the tropical freshwater cladoceran, Ceriodaphnia rigaudii and the temperate species, Daphnia magna. Data generated was subsequently used to determine the relative sensitivities of both species, using interspecies correlation to compare the 48?h LC50 values for both species. The 48?h LC50 values for C. rigaudii ranged from 0.002?mg?L?1 (potassium dichromate) to 21.1?mg?L?1 (KCl), whereas those for D. magna ranged from 0.3?mg?L?1 for Cu to 418.87?mg?L?1 for KCl. The LC50 values for C. rigaudii were significantly less than that for D. magna for six of the compounds tested. The interspecies correlation also showed a low, positive correlation suggesting that the sensitivities of both species were not similar for the compounds tested. The sensitivity factors for C. rigaudii and D. magna ranged between 0.01 and 12.3. These values further suggested that for six of the compounds tested, C. rigaudii appeared to be more sensitive than D. magna. It is therefore possible that because of these differences in relative sensitivities, toxicity data generated with D. magna may not be appropriate for Trinidad.  相似文献   

14.
Abstract

Fusarubin analogues of Fusarium oxysporum f. sp. ciceris were investigated for antifungal activity in vitro against five soil borne phytopathogenic fungi. 3-O-Methyl-8-O-methyl-fusarubin was inhibitory towards S. sclerotiorum (EC50 0.33?mmol L?1) and Sclerotium rolfsii (EC50 0.38?mmol L?1). A structure–antifungal activity relationship of fusarubin analogues was established from their activity performance. Possible mechanism of action of these compounds was studied using molecular docking and simulations against three target enzymes which revealed receptor ligand binding affinity. Docking of 3-O-methyl-8-O-methyl-fusarubin into the succinate dehydrogenase site revealed formation of salt bridge, hydrogen bond, π–anion, π–alkyl, and Van der Waals interactions.  相似文献   

15.
Phosphate depleted Pyrocystis noctiluca (Murray) Schuett 1895 has at least one phosphomonoesterase (EC 3:1:3:1) which is triphasic between 0.1 and 222 mol P. The enzyme has a broad temperature range with maximum activity at 50 °C and a Q10 of 1.4 to 1.5. A break in the Arrhenius plot at 35 °C implies the enzyme is membrane-bound. Cytological staining of whole cells and cell fractionation studies (showing 26 times higher specific activity in the particulate compared with the cytoplasmic fraction) suggest the enzyme is plasmalemma-bound. The enzyme has an absolute metal requirement which would be satisfied by Mg++ but not Mn++, Zn++, Fe++, or Co++ at seawater concentrations. Alkaline phosphatase is a stable enzyme whose activity is not altered by inhibitors of protein synthesis. Orthophosphate inhibition of enzyme activity was largely eliminated in the presence of these inhibitors. Apparently, a protein induced by PO4 3-, rather than PO4 3- itself, inhibits alkaline phosphatase. Cell-free alkaline phosphatase can hydrolyze a variety of phosphate esters and linear polymers of inorganic phosphorus as well as disolved organic phosphorus from tropical oceanic waters. These same hydrolysable organic and inorganic phosphorus compounds support the axenic culture growth of P. noctiluca, suggesting that naturally occurring hydrolysable organic phosphorus compounds may also support the growth of this alga.  相似文献   

16.
依据经济合作与发展组织(OECD)关于定量结构-活性关系(QSAR)模型构建和使用导则,将780个有机化合物,以4:1的比例随机划分为训练集(624个化合物)和验证集(156个化合物),通过多元线性回归(MLR)方法构建了一个包含12个描述符的有机化合物鱼类生物富集因子(BCF)的QSAR模型。QSAR模型的调整决定系数R2ad j=0.809,去一法交叉验证系数Q2LOO=0.803,外部验证系数Q2EXT=0.732,表明模型具有较好的拟合优度、稳健性和预测能力。采用欧几里德距离方法表征模型应用域,通过威廉姆斯图分析模型离群点,并对模型进行机理解释。所构建的模型,可以用于预测应用域内有机化学品的生物富集因子。  相似文献   

17.
Alkaline phosphatase activity (APA) was determined in 44 species of marine macrophytes collected throughout 1991 and 1992 along the southern coast of Spain. Activity varied between 0.83 mol paranitrophenol (pNP) released g-1 dry wt h-1 in Ulva rigida var. gigantea and 238.8 mol pNP g-1 dry wt h-1 in Bangia fuscopurpurea. Using a histochemical method, APA sites were located in five of these species: Corallina elongata Ellis et Soland, Gelidium latifolium (Grev.) Thur. et Born., G. sesquipedale (Clem.) Born. et Thur., Porphyra umbilicalis (L.) Kützing and Zostera noltii Hornem. Enzymatic activity was found in the outer part of the thallus, either on the cell wall or in the cortical cells. In the marine phanerogam Z. noltii activity was also located in the vascular bundle. The results suggest that APA is present in many, if not all, marine macrophytes from southern Spain, and plays a relevant role in the utilization of dissolved organic phosphorus compounds.  相似文献   

18.
生物半减期(t1/2)是评价外源化合物在鱼体内蓄积效应的重要参数。实验测定t_(1/2)的速度慢、成本高,难以满足化学品生态风险评价的需求,需要发展替代实验的模型预测方法。本研究搜集了653种化合物t1/2实测值,采用多元线性回归(MLR)和支持向量机(SVM) 2种方法,建立了鱼体logt1/2的定量构效关系(QSAR)预测模型。MLR模型的校正决定系数(R(adj)~2)为0.751,均方根误差(RMSE_(train))为0.587,去一法交叉验证系数(Q_(LOO)~2)为0.735,外部验证系数(Q_(ext)~2)为0.682,这表明模型具有较好的拟合度、稳健性和预测能力。SVM模型具有更好的拟合和预测能力(R_(adj)~2=0.839,RMSE_(train)=0.457,Q_(ext)~2=0.708)。采用Williams法对模型的应用域进行表征。所建模型可用于预测多环芳烃、多氯联苯、多溴联苯醚、有机磷农药、药物等典型化合物,以及其他烷烃、环烷烃、烯烃、醇、醚、酸、酯、酮、含卤素化合物、芳香族化合物、含硫、氮、磷化合物的在鱼体内的logt1/2值。  相似文献   

19.
The aim of this investigation was to examine biochemical differences in the gastropod Rapana venosa (R. venosa) from polluted (RvP) and nonpolluted (RvN) sites of the Black Sea's Bulgarian coast that may serve as bioindicators of environmental quality. Mussels Mytilus galloprovincialis (MMg) were collected from polluted (MMgP) and nonpolluted (MMgN) sites at the same time for comparison. Bioactive compounds and the antioxidant activity of dry matter (DM) methanol extracts from RvP and RvN were determined. Three-dimensional fluorometry (3D-FL) and Fourier transform infrared (FTIR) analyses were used to evaluate polyphenols and proteins. DM methanol extracts from RvP, and to lesser extent RvN, showed high amounts of total phenolics (23.22±2.9 and 15.60±1.8 mg GAE · g?1 DW) and exhibited high levels of antioxidant activity in some radical scavenging assays (μ MTE · g?1 DW): 56.38±5.2 and 33.79±3.3 by 2,2azino-bis (3-ethyl-benzothiazoline-6-sulfonic acid) diamonium salt (ABTS·+); 54.79±5.6 and 33.7±2.6 by cupric reducing antioxidant capacity (CUPRAC); 62.34±6.8 and 30.31±3.9 by the 1diphenyl-2-picrylhydrazyl method (DPPH). A correlation in the above indices was found between R. venosa and M. galloprovincialis, but all results were relatively higher for M. galloprovincialis than for R. venosa. The obtained indices of R. venosa may serve as a bioindicator of environmental ecological quality.  相似文献   

20.
为了探讨马拉硫磷和主要水解产物对圆瘤浮萍的生长抑制作用及可能的氧化损伤机制,采用静态培养法,研究不同浓度的马拉硫磷及其水解产物二甲基二硫代磷酸酯(DMDTP)、二甲基硫代磷酸酯(DMTP)、二甲基磷酸酯(DMP)对圆瘤浮萍生长、叶绿素含量、叶绿体活性、超氧化物歧化酶(SOD)、过氧化物酶(POD)和过氧化氢酶(CAT)活性及丙二醛(MDA)含量的影响。结果表明,暴露7 d后,浓度为100 mg a.i.·L-1处理下的浮萍叶状体生长量与空白对照组无显著性差异;DMDTP、DMTP和DMP对圆瘤浮萍叶状体生长量的半数抑制浓度(7 d-IC50)分别为52.9、45.5和98.0 mg a.i.·L-1。随着试验液中DMDTP、DMTP和DMP浓度的升高,圆瘤浮萍叶绿素含量均明显降低,叶绿体活性则分别表现为诱导-抑制、抑制和抑制效应。在DMDTP、DMTP和DMP胁迫下,脂质过氧化产物丙二醛(MDA)含量明显增加;圆瘤浮萍体内的抗氧化酶系统均受到影响。总体表现为随着DMDTP浓度的增加,SOD活性先降低后升高;DMTP和DMP胁迫下,SOD活性呈现先降后升再降的趋势;POD和CAT活性则随3种水解产物浓度的增加呈现先升后降趋势;这表明抗氧化酶系统对外部胁迫的应答很复杂。马拉硫磷对圆瘤浮萍的毒性较小,其水解产物DMDTP、DMTP和DMP均对圆瘤浮萍的生长产生一定的毒性作用。在实际生产中,应多加关注马拉硫磷水解产物对环境生物的风险评估。  相似文献   

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