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Optimization of Carotenoid Production by Rhodosporidium babjevae and Evaluation of Antifungal and Dyeing Activity 巴氏红孢子虫产类胡萝卜素的优化及其抑菌和染色活性评价
Pub Date : 2022-11-03 DOI: 10.2174/2212796817666221103100531
M. Madani, Nastaran Salimi, P. Shakib
The aim of this study was to evaluate the antifungal, dyeing activity and optimization of carotenoid production by Rhodosporidium babjevae.Rhodosporidium red yeast is one of the natural alternative sources of carotenoids. Carotenoids are produced by a wide variety of bacteria, algae, fungi, and plants. These pigments serve a vital function as antioxidant protectors and have lately caught a lot of attention because of their positive impact on human healthIn this experimental-laboratory study, Rhodosporidium was isolated from different environmental sources in Isfahan. After carotenoid extraction based on the Davis method from Rhodosporidium, cell biomass, and the total amount of carotenoids were measured, and the carotenoid light absorption spectrum was determined. To optimize carotenoid production, one-factor and Taguchi methods evaluated incubation time factors, pH, nitrogen, and carbon source. Then, yeast carotenoid antifungal activity, minimum inhibitory concentration (MIC),and minimum fungicidal concentration (MFC) were determined. The stability of dye against washing, rubbing, and light was investigated to evaluate the carotenoid dyeing activity.In this experimental-laboratory study, Rhodosporidiums were isolated from different environmental sources in Isfahan. After carotenoid extraction according to Davis method from Rhodosporidiums, cell biomass, total amount of carotenoids was measured, and carotenoid light absorption spectrum was determined. To optimize carotenoid production, incubation time factors, pH, nitrogen and carbon source were evaluated by one-factor and Taguchi methods. Then, yeast carotenoid antifungal activity, minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) were determined. The stability of the dye against washing, rubbing and light was investigated to evaluate the carotenoid dyeing activity obtained.The optimum condition for carotenoid production was 96 hours of incubation, 2 g L-1 peptone, pH 5.5, and 30 g L-1 glucose. The optimal conditions of Taguchi were performed, and production of 11.67 mg L-1 was obtained. The carotenoid pigment isolated from Rhodosporidium babjevae showed no anti-candida properties but has antifungal activity against A. flavus and A. niger. Woolen fabric had washing fastness of 2 and cotton fabric had a washing fastness of 3. The staining grade on woolen and cotton fabrics was 4. The grade of color fastness of woolen and cotton fabrics against dry rubbing was 5, while the grade of color fastness against wet rubbing was 2 and 4, respectively.The optimum condition for carotenoids production was 96 hours’ time of incubation, 2g/l peptone, pH 5.5, and 30 g/l glucose. The optimal conditions of Taguchi were performed and a production of 11.67 μg / L was obtained. The carotenoid pigment isolated from Rhodosporidium babjevae showed no anti-candida properties. The color fastness was 4 for wool and 2 for cotton. The degree of washing stability was 2 for
本研究的目的是评价巴氏红孢子虫的抑菌活性、染色活性和优化类胡萝卜素的生产工艺。红红酵母是类胡萝卜素的天然替代来源之一。类胡萝卜素由各种各样的细菌、藻类、真菌和植物产生。这些色素作为抗氧化保护剂具有重要的功能,最近因其对人体健康的积极影响而引起了广泛的关注。在这项实验实验室研究中,从伊斯法罕不同的环境来源中分离出红孢子虫。采用Davis法提取红孢子虫类胡萝卜素后,测定细胞生物量和类胡萝卜素总量,测定类胡萝卜素光吸收光谱。为了优化类胡萝卜素的生产,单因素法和田口法评估了培养时间、pH、氮和碳源。然后测定酵母类胡萝卜素抗真菌活性、最小抑菌浓度(MIC)和最小杀真菌浓度(MFC)。考察了染料对洗涤、摩擦和光照的稳定性,评价了类胡萝卜素的染色活性。在本实验-实验室研究中,从伊斯法罕不同的环境源中分离出红孢子菌。采用Davis法提取红孢子草类胡萝卜素后,测定细胞生物量、类胡萝卜素总量,测定类胡萝卜素光吸收光谱。为了优化类胡萝卜素的产量,采用单因素法和田口法对培养时间、pH、氮和碳源进行了评价。测定酵母类胡萝卜素抗真菌活性、最小抑菌浓度(MIC)和最小杀真菌浓度(MFC)。考察了染料对洗涤、摩擦和光照的稳定性,评价了所获得的类胡萝卜素染色活性。类胡萝卜素的最佳生产条件为培养96小时,2 g L-1蛋白胨,pH 5.5, 30 g L-1葡萄糖。对田口发酵条件进行了优化,得到了11.67 mg L-1的产率。从巴氏红孢子虫中分离得到的类胡萝卜素对假丝酵母菌无抑制作用,但对黄霉和黑霉有抑制作用。羊毛织物的洗涤牢度为2,棉织物的洗涤牢度为3。羊毛和棉织物的染色等级为4级。毛、棉织物的干摩擦色牢度为5级,湿摩擦色牢度为2级,湿摩擦色牢度为4级。产类胡萝卜素的最佳条件为:培养96 h,蛋白胨2g/l, pH 5.5,葡萄糖30 g/l。对田口菌的最佳发酵条件进行了优化,其产率为11.67 μg / L。从巴氏红孢子虫中分离得到的类胡萝卜素无抗念珠菌活性。羊毛的色牢度为4,棉的色牢度为2。羊毛织物的洗涤稳定度为2,棉织物的洗涤稳定度为3。毛、棉织物的染色程度均为4。毛、棉织物的干摩擦色稳度为5,毛、棉织物的湿摩擦色稳度为2、4。研究结果表明,巴氏红孢子虫类胡萝卜素是一种较理想的染色剂,具有抗菌性能,可用于工业生产。希望将其用于类胡萝卜素的商业化生产。
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引用次数: 0
Modulation of Lignin and its Implications in Salt, Drought and Temperature Stress Tolerance 木质素的调控及其对盐、干旱和温度胁迫的影响
Pub Date : 2022-08-20 DOI: 10.2174/2212796816666220820110616
K. P B, S. B., Prashant Singam, Sahitya G, Tulya Rupasri V, Rajasheker G, Prashanth Suravajhala
Lignins are phenylpropanoid polymers with complex composition and structures and crucial components in plant cell walls. Lignins are biosynthesized from oxidative polymerization of 4-hydroxycinnamyl alcohols, but differ in the degree of methoxylation.This review makes an endeavour to identify the gaps in our understanding of lignin modulation and gain insights into their relevance to abiotic stress tolerance.Critical review of the recent literature to understand the regulation of lignin, the major biopolymer involved in multitude of functions.Lignin contributes to the growth of tissues, organs that give mechanical protection or lodging resistance and also responses to multiple biotic and abiotic stresses. The quantity and quality of accumulation of lignin is dependent on the type of plant species and abiotic stress. In this review, we briefly discuss about the biosynthesis, modulation of lignin by diverse transcription factors and its role in salt, drought and temperature stress tolerance.We need to explore many areas to gain comprehensive knowledge about the secondary cell wall deposition of monolignols, and their transport, leading to lignin accumulation which imparts biotic and abiotic stress tolerance to plants.
木质素是一种结构复杂的苯丙类聚合物,是植物细胞壁的重要组成部分。木质素是由4-羟基肉桂醇氧化聚合合成的,但其甲氧基化程度不同。这篇综述努力确定我们对木质素调节的理解差距,并深入了解它们与非生物胁迫耐受性的相关性。批判性地回顾了最近的文献,以了解木质素的调节,主要的生物聚合物参与了许多功能。木质素有助于组织、器官的生长,提供机械保护或抗倒伏,也对多种生物和非生物胁迫作出反应。木质素积累的数量和质量取决于植物种类的类型和非生物胁迫。本文就木质素的生物合成、多种转录因子对木质素的调控及其在耐盐、干旱和温度胁迫中的作用作一综述。我们需要探索许多领域来全面了解单脂醇的次生细胞壁沉积及其运输,从而导致木质素的积累,从而赋予植物生物和非生物抗逆性。
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引用次数: 0
The Effect of Substituents and Functional Groups on Enhancing the Antioxidant Activity of Benzoin Derivatives 取代基和官能团对苯甲酸甲酰衍生物抗氧化活性的影响
Pub Date : 2022-05-17 DOI: 10.2174/2212796816666220517103230
B. Thanuja, K. Kripa, T. Bhavadharani, C. Kanagam
2-phenyl hydrazine-1-hydroxy, 1-[2-chlorophenyl] -2-4’-methoxyphenyl] ethane and 2-oxime-1-hydroxy, 1-[2-chlorophenyl] -2-4’-methoxyphenyl] ethane derivatives of benzoin have been synthesized from 2’chloro-4-methoxy benzoin by addition reaction. Structural elucidation of the synthesized compounds was done by FT-IR, FT-NMR studies. The presence of electron-withdrawing and electron-donating groups enhanced the antioxidant activity which was analyzed by 2,2-diphenyl-1-picrylhydrazyl assay, 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) scavenging assay, hydrogen peroxide radical scavenging assay, Ferric reducing antioxidant power assay methods. The effect of functional groups and substituents in the core structure was studied and was compared with its parent compound.In this manuscript, two derivatives of benzoin viz. 2-phenyl hydrazine-1-hydroxy, 1-[2-chlorophenyl] -2-[4’-methoxyphenyl] ethane and 2-oxime-1-hydroxy, 1-[2-chlorophenyl]-2-[4’-methoxyphenyl] ethane (HA) derivatives were synthesized by benzoin condensation and followed by addition reaction to find a potential anti-oxidant agent.Qualitative analyses were determined by FT-IR and FT-NMR studies. Anti-oxidant activities were tested by DPPH assay, ABTS assay, FRAP assay H2O2 methodsFrom the obtained results it is confirmed that the effect of withdrawing and electron releasing groups as a substituent in the core structure of parent compounds enhances the activity of anti-oxidant. The role of substituents is discussed in detail.The results of the biochemical assay reveal that the synthesized compounds serve as good free radical inhibitors and scavengers which inhibit the oxidative reactions, are responsible for cell damage, food spoilage, etc. The promising anti-oxidant activities are because of the effective substituents which play a prominent role in the drug industries.
以2 '氯-4-甲氧基苯甲酸为原料,通过加成反应合成了2-氧-1-羟基,1-[2-氯苯]-2-4 ' -甲氧基苯基]乙烷和2-肟-1-羟基,1-[2-氯苯]-2-4 ' -甲氧基苯基]乙烷衍生物。通过FT-IR、FT-NMR对合成的化合物进行了结构分析。采用2,2-二苯基-1-吡啶肼基、2,2′-氮基-双(3-乙基苯并噻唑-6-磺酸)清除率、过氧化氢自由基清除率、铁还原抗氧化能力测定等方法对吸电子基和供电子基的存在增强了其抗氧化活性。研究了核心结构中官能团和取代基的影响,并与母体化合物进行了比较。本文通过苯甲酸缩合和加成反应合成了2-肟-1-羟基,1-[2-氯苯]-2-[4 ' -甲氧基苯基]乙烷(HA)衍生物,以寻找一种潜在的抗氧化剂。定性分析由傅里叶变换红外光谱和傅里叶变换核磁共振研究确定。采用DPPH法、ABTS法、FRAP法对其抗氧化活性进行了测定,结果表明,在母体化合物的核心结构中,作为取代基的吸出基团和释放电子基团的作用增强了其抗氧化活性。详细讨论了取代基的作用。生化实验结果表明,合成的化合物具有良好的自由基抑制剂和清除剂作用,可抑制细胞损伤、食物变质等氧化反应。有效的取代基在药物工业中发挥着突出的作用,具有良好的抗氧化活性。
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引用次数: 0
Acyclic polyorganochalcogenoethers and their functional activities: Synthesis of sterically encumbered hexakis(alkylchalcogenomethyl)benzenes [(RECH2)6C6] [E=S or Se] and their potential as selective ionophores for Hg2+ ions 无环多有机酒精醚及其功能活性:空间负担六烷基(烷基)基因组乙基苯[(RECH2)6C6] [E=S或Se]的合成及其作为Hg2+离子选择性离子载体的潜力
Pub Date : 2022-05-09 DOI: 10.2174/2212796816666220509145236
N. Prabhu, J. Jyoti, R. Kumari, J. Singh, R. Butcher
An efficient synthesis of hexakis(alkylthio/selenomethyl)benzenes [(RSCH2)6C6 and (RSeCH2)6C6] (1-14) (where, R= nPr, iPr, nBu, iBu, sBu, tBu, nPent, iPent, and 2-Methyl-1-butyl) by the reaction of hexakis(bromomethyl)benzene with alkylthio or alkylseleno (RS-/RSe-) anions are demonstrated.They have been characterized by physicochemical and spectroscopic methods including single crystal X-ray crystallography. The balances between multiple [C(sp3)-H…S] or [C(sp3)-H…Se] intramolecular interactions in these species appear to decide their stability. Preliminary spectroscopic (UV-vis. and fluorescence) data on the behavior of alkylchalcogeno substituted hexa-benzenes in solution revealed their potential as ion-sensing species and function as highly selective ionophores for Ag+ and Hg2+ ions recognition.In situ, (Hg-S) and (Hg-Se) bond formation on interaction with the chosen hexa-species (2 and 10) and Hg2+ cation revealed a unique ‘turn-off’ or ‘turn-on’ emissive behavior and these function act as reporting fluorescent tool for Hg2+ quantification without use of any external fluorophore.The present study describes an efficient and simple route for the synthesis of sterically encumbered poly-alkylthio/seleno benzenes in high purity and good yields.
研究了六烷基(溴乙基)苯与烷基硫代或烷基硒代(RS-/RSe-)阴离子反应合成六烷基(烷基硫代/硒甲基)苯[(RSCH2)6C6和(RSeCH2)6C6](1-14)(其中R= nPr, iPr, nBu, iBu, sBu, tBu, nPent, iPent和2-甲基-1-丁基)。用物理化学和光谱学方法(包括单晶x射线晶体学)对它们进行了表征。多种[C(sp3)-H…S]或[C(sp3)-H…Se]分子内相互作用之间的平衡似乎决定了它们的稳定性。初步光谱(紫外-可见)。烷基硫基取代六苯在溶液中的行为数据揭示了它们作为离子传感物质的潜力,以及作为识别Ag+和Hg2+离子的高选择性离子载体的功能。在原位,(Hg-S)和(Hg-Se)与选定的六种(2和10)和Hg2+阳离子相互作用时形成的键显示出独特的“关闭”或“打开”发射行为,这些功能作为报告Hg2+定量的荧光工具,无需使用任何外部荧光团。本文介绍了一种高效、简便、纯度高、产率好的立体负载型聚烷基硫代/硒代苯的合成方法。
{"title":"Acyclic polyorganochalcogenoethers and their functional activities: Synthesis of sterically encumbered hexakis(alkylchalcogenomethyl)benzenes [(RECH2)6C6] [E=S or Se] and their potential as selective ionophores for Hg2+ ions","authors":"N. Prabhu, J. Jyoti, R. Kumari, J. Singh, R. Butcher","doi":"10.2174/2212796816666220509145236","DOIUrl":"https://doi.org/10.2174/2212796816666220509145236","url":null,"abstract":"\u0000\u0000An efficient synthesis of hexakis(alkylthio/selenomethyl)benzenes [(RSCH2)6C6 and (RSeCH2)6C6] (1-14) (where, R= nPr, iPr, nBu, iBu, sBu, tBu, nPent, iPent, and 2-Methyl-1-butyl) by the reaction of hexakis(bromomethyl)benzene with alkylthio or alkylseleno (RS-/RSe-) anions are demonstrated.\u0000\u0000\u0000\u0000They have been characterized by physicochemical and spectroscopic methods including single crystal X-ray crystallography. The balances between multiple [C(sp3)-H…S] or [C(sp3)-H…Se] intramolecular interactions in these species appear to decide their stability. Preliminary spectroscopic (UV-vis. and fluorescence) data on the behavior of alkylchalcogeno substituted hexa-benzenes in solution revealed their potential as ion-sensing species and function as highly selective ionophores for Ag+ and Hg2+ ions recognition.\u0000\u0000\u0000\u0000In situ, (Hg-S) and (Hg-Se) bond formation on interaction with the chosen hexa-species (2 and 10) and Hg2+ cation revealed a unique ‘turn-off’ or ‘turn-on’ emissive behavior and these function act as reporting fluorescent tool for Hg2+ quantification without use of any external fluorophore.\u0000\u0000\u0000\u0000The present study describes an efficient and simple route for the synthesis of sterically encumbered poly-alkylthio/seleno benzenes in high purity and good yields.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-05-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81782321","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Antibacterial activity of zinc oxide nanoparticle-loaded soft contact lens 纳米氧化锌软性隐形眼镜的抗菌活性研究
Pub Date : 2022-04-19 DOI: 10.2174/2212796816666220419121948
Jactty Chew, T. Tong, Mun Lok Chua, Mohammad Ridwane Munngroo, Yi Xing Yap, M. Misran, L. Gew
Contact lenses that are coated with antibacterial agents may reduce the risk of microbial keratitis; however, to the best of our knowledge, such contact lenses are not available in the market.We determined the ability of zinc oxide nanoparticles (ZnO-NPs)-loaded soft contact lenses to prevent the adhesion of Staphylococcus aureus and Pseudomonas aeruginosa. Commercially acquired sterile silicone hydrogel contact lenses were soaked in ZnO-NPs (˂50 nm) suspensions of various concentrations and the stability of the ZnO-NPs coating on contact lenses over 28 days was monitored using a UV-vis spectrophotometer. The cytotoxicity effects of ZnO-NPs on human corneal epithelial cells were evaluated using a lactate dehydrogenase (LDH) kit.The results showed that the ZnO-NPs coating on contact lenses was optimal starting from day seven onward. In the following assays, optimally ZnO-NP-coated contact lenses were incubated with S. aureus and P. aeruginosa suspensions (1 x 105 colony forming unit) for 24 hr at 37C, followed by enumeration using the plating method. Our data showed that 100 ppm of ZnO-NPs coating on contact lenses reduced the adhesion of 69.9% and 74.6% of S. aureus and P. aeruginosa significantly (p<0.05), respectively. The confocal laser scanning microscopic analyses were consistent with our bacterial adhesion findings. Low cytotoxicity against human corneal epithelial cells was observed even at the highest concentration of 300 ppm.This study provides insights into the potential role of ZnO-NPs in the development of contact lenses with antibacterial properties.
隐形眼镜涂上抗菌剂可以降低患细菌性角膜炎的风险;然而,据我们所知,这种隐形眼镜在市场上是买不到的。我们测定了氧化锌纳米颗粒(ZnO-NPs)负载的软性隐形眼镜防止金黄色葡萄球菌和铜绿假单胞菌粘附的能力。将市售无菌硅水凝胶隐形眼镜浸泡在不同浓度的ZnO-NPs(小于50 nm)悬浮液中,用紫外-可见分光光度计监测隐形眼镜表面ZnO-NPs涂层28天的稳定性。采用乳酸脱氢酶(LDH)试剂盒评价ZnO-NPs对人角膜上皮细胞的细胞毒性作用。结果表明,从第7天开始,隐形眼镜上的ZnO-NPs涂层是最佳的。在接下来的实验中,将最佳的zno - np包膜隐形眼镜与金黄色葡萄球菌和铜绿假单胞菌悬浮液(1 × 105菌落形成单位)在37℃下孵育24小时,然后用电镀法计数。我们的数据显示,100 ppm的ZnO-NPs涂层对金黄色葡萄球菌和铜绿假单胞菌的粘附性分别有69.9%和74.6%的显著降低(p<0.05)。共聚焦激光扫描显微分析与我们的细菌粘附结果一致。即使在最高浓度为300 ppm时,也观察到对人角膜上皮细胞的低细胞毒性。该研究为ZnO-NPs在抗菌隐形眼镜开发中的潜在作用提供了见解。
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引用次数: 0
Antioxidant Activity of a Selenopeptide Modelling the Thioredoxin Reductase Active Site is Enhanced by NH···Se Hydrogen Bond in the Mixed Selenosulfide Intermediate 模拟硫氧还蛋白还原酶活性位点的硒肽的抗氧化活性在混合硒硫化中间体中被NH···Se氢键增强
Pub Date : 2022-04-15 DOI: 10.2174/2212796816666220415142301
M. Iwaoka, Hajime Oba, Kotoi Matsumura, Shuhei Yamanaka, Shingo Shimodaira, S. Kusano, Tatsuya Asami
Thioredoxin reductase (TrxR), one of the representative selenoenzymes, is an important antioxidant enzyme suppressing oxidative stress in living organisms. At the active site of human TrxR, the presence of a Sec•••His•••Glu catalytic triad was previously suggested. Method. In this study, a short selenopeptide mimicking this plausible triad, i.e., H-CUGHGE-OH (1), was designed, synthesized, and evaluated for the TrxR-like catalytic activity.In this study, a short selenopeptide mimicking this plausible triad, i.e., H-CUGHGE-OH (1), was designed, synthesized, and evaluated for the TrxR-like catalytic activityThe molecular simulation in advance by REMC/SAAP3D predicted the preferential formation of Sec•••His•••Glu hydrogen bonding networks in the aqueous solution. Indeed, a significant antioxidant activity was observed for 1 in the activity assay using NADPH as a reductant and H2O2 as a substrate. Tracking the reaction between 1 and GSH by 77Se NMR revealed a reductive cleavage of the selenosulfide (Se-S) bond to generate the diselenide species. The observation suggested that in the transiently formed mixed Se-S intermediate, the NH•••Se hydrogen bond between the Sec and His residues leads a nucleophilic attack of the second thiol molecule not to the intrinsically more electrophilic Se atom but to the less electrophilic S atom of the Se-S bond. Ab initio calculations for the complex between MeSeSMe and an imidazolium ion at the MP2/6-31++G(d,p) level demonstrated that NH•••Se and NH•••S hydrogen bonds are equally favorable as the interaction modes. Thus, importance of the relative spatial arrangement of the Se-S bond with respect to the imidazole ring was suggested for the exertion of the TrxR-like catalytic activity.The proposed umpolung effect of NH•••Se hydrogen bond on the reactivity of a Se-S bond will be a useful tool for developing efficient TrxR models with high redox catalytic activity.
硫氧还蛋白还原酶(Thioredoxin reductase, TrxR)是生物体内抑制氧化应激的重要抗氧化酶,是硒酶的代表之一。在人类TrxR的活性位点,存在Sec•••His•••Glu催化三联体。方法。在本研究中,我们设计、合成了一个类似trxr的短硒肽,即H-CUGHGE-OH(1),并对其催化活性进行了评价。在本研究中,我们设计、合成了一个模拟这一貌似合理的三元组合的短硒肽,即H-CUGHGE-OH(1),并对其trxr样催化活性进行了评价。通过REMC/SAAP3D预先进行的分子模拟预测了水溶液中Sec••••His•••Glu氢键网络的优先形成。事实上,在使用NADPH作为还原剂和H2O2作为底物的活性测定中,观察到1具有显著的抗氧化活性。通过77Se核磁共振追踪1与谷胱甘肽之间的反应,发现硫代硒(Se-S)键的还原裂解生成了二硒化物。观察结果表明,在瞬时形成的混合Se-S中间体中,Sec和His残基之间的NH•••Se氢键导致第二个硫醇分子的亲核攻击不是针对本质上亲电性较强的Se原子,而是针对亲电性较弱的Se-S原子。对MeSeSMe与咪唑离子在MP2/6-31++G(d,p)水平上的配合物进行从头计算,结果表明,NH•••Se和NH•••S氢键作为相互作用模式同样有利。因此,Se-S键相对于咪唑环的相对空间排列对于trxr类催化活性的发挥具有重要意义。提出的NH•••Se氢键对Se- s键反应性的影响将为开发具有高氧化还原催化活性的高效TrxR模型提供有用的工具。
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引用次数: 1
L-glutamic acid mitigates carbon tetrachloride-induced acute tissue injury by reducing oxidative stress in a rat model l -谷氨酸通过降低大鼠氧化应激模型减轻四氯化碳诱导的急性组织损伤
Pub Date : 2022-04-08 DOI: 10.2174/2212796816666220408104856
N. Salyha, Y. Salyha
on physiological and biochemical processes in the mammalian organism is very important, despiteThe experimental studies aimed at exploring the ameliorative effects of L-glutamic acid (L-Glu) on CCl4 toxicity in myocardium, lung tissues and blood of male rats.Rats were exposed to CCl4, after that rats were treated with L-Glu. The GSH level and the activities of antioxidant enzymes were studied. In addition to this, the content of lipid peroxidation products was monitored.The obtained results suggest that CCl4 causes oxidative stress in rat tissues, accompanied by an increase in lipid peroxidation products, and a decrease in glutathione peroxidase (GPx), glutathione reductase (GR), glutathione transferase (GST), glucose-6-phosphate dehydrogenase (G6PDH), superoxide dismutase (SOD), catalase (CAT) activities and reduced glutathione (GSH) content. The enzymatic activity in tissues of rats treated with L-Glu was restored. Moreover, the changes, which were observed in the studied parameters showed to be less significant compared to CCl4 treated group.These results suggest that L-Glu inhibits of free radical processes. In summary, this study demonstrates the feasibility of the administration of L-Glu supplementation, which could be used to protect and mitigate the CCl4-induced oxidative stress.
本实验旨在探讨l -谷氨酸(L-Glu)对CCl4在雄性大鼠心肌、肺组织和血液中的毒性的改善作用。先给大鼠注射CCl4,再给大鼠注射L-Glu。研究了GSH水平和抗氧化酶活性。除此之外,还监测了脂质过氧化产物的含量。结果表明,CCl4引起大鼠组织氧化应激,脂质过氧化产物增加,谷胱甘肽过氧化物酶(GPx)、谷胱甘肽还原酶(GR)、谷胱甘肽转移酶(GST)、葡萄糖-6-磷酸脱氢酶(G6PDH)、超氧化物歧化酶(SOD)、过氧化氢酶(CAT)活性降低,谷胱甘肽(GSH)含量降低。L-Glu处理后大鼠组织酶活性恢复。此外,与CCl4治疗组相比,在研究参数中观察到的变化不太显著。这些结果表明,L-Glu抑制自由基过程。综上所述,本研究证明了补充L-Glu对ccl4诱导的氧化应激具有保护和减轻作用的可行性。
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引用次数: 0
Efficacy of propyl selenoethers against peroxyl radical induced protein damage: Effect of functional group substitution 丙基硒醚对过氧自由基诱导的蛋白质损伤的影响:官能团取代的影响
Pub Date : 2022-03-30 DOI: 10.2174/2212796816666220330093744
V. V. Gandhi, R. P. Das, B. Singh, A. Kunwar
Proteins are the critical molecules for cellular functionality and are also considered to be highly susceptible for reactive oxygen species (ROS)-induced oxidative damages.The present study was aimed to evaluate some simple water soluble aliphatic organoselenium compounds bearing different functional groups but of similar carbon chain (propyl) length for protective effect against 2,2’-azobis-(2-amidinopropane) dihydrochloride (AAPH)-induced oxidative damage using mitochondria as an in vitro model.The results indicated that APPH (20 mM) treatment of mitochondrial fraction induced protein carbonylation leading to inactivation of redox enzymes and electron transport chain (ETC) and ultimately the mitochondrial dysfunction. On the other hand, treatment with 0.5 mM of monoselenobutyric acid (SeBA) and monoselenopropyl alcohol (SePOH) significantly prevented APPH-induced protein carbonylation in mitochondrial fraction and restored activities of mitochondrial proteins. On contrary, monoselenopropyl amine (SePAm) treatment at identical concentration did not show significant protection to mitochondrial activity from AAPH-induced oxidative damages. Above results are in concurrence to the reported peroxyl radical savaging activities of above molecules.In conclusion, SeBA and SePOH are potential candidate molecules to protect proteins from oxidative damages and therefore can be useful for management of oxidative stress in cellular models.
蛋白质是细胞功能的关键分子,也被认为对活性氧(ROS)诱导的氧化损伤非常敏感。本研究以线粒体为体外模型,研究了几种具有不同官能团但碳链(丙基)长度相似的简单水溶性脂肪族有机硒化合物对2,2 ' -偶氮-(2-氨基丙烷)二盐酸(AAPH)诱导的氧化损伤的保护作用。结果表明,APPH (20 mM)处理线粒体片段诱导蛋白质羰基化,导致氧化还原酶和电子传递链(ETC)失活,最终导致线粒体功能障碍。另一方面,0.5 mM单硒丁酸(SeBA)和单硒丙醇(SePOH)处理可显著阻止apph诱导的线粒体部分蛋白羰基化,恢复线粒体蛋白活性。相反,相同浓度的单硒丙基胺(SePAm)处理对aaph诱导的线粒体氧化损伤没有显著的保护作用。上述结果与报道的上述分子的过氧自由基破坏活性一致。综上所述,SeBA和SePOH是保护蛋白质免受氧化损伤的潜在候选分子,因此可以用于细胞模型中氧化应激的管理。
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引用次数: 0
Ebselen’s potential to inhibit planktonic and biofilm growth of Niesseria mucosa 依布selen抑制奈瑟菌粘膜浮游生物和生物膜生长的潜力
Pub Date : 2022-03-30 DOI: 10.2174/2212796816666220330090107
S. Shaikh, I. Priyadarsini, S. Vavilala
Antibiotic resistance of various bacterial communities remains a global burden in healthcare industry. Biofilm formation is one of the resistance mechanisms acquired by bacterial communities in order to reverse the action of antibiotics. There is an urgent need for the discovery of novel antimicrobials and novel approaches to tackle this problem. However, it is very expensive and challenging to develop new antibiotics. Drug repurposing is an efficient strategy which reduces time and cost associated with drug discovery.In the current study, anti-microbial and antibiofilm potential of an organoselenium clinical molecule Ebselen against Neisseria mucosa has been elucidated.Ebselen Antibacterial studies include Minimum Inhibitory Concentration (MIC), growth-kill, Colony Forming Unit (CFU) assays and intracellular Reactive Oxygen Species (ROS) accumulation studies. Antibiofilm studies include inhibition, eradication and cell surface hydrophobicity assays, quantification of Extracellular Polymeric Substance (EPS) and eDNA and for anti-quorum sensing activity protease and urease enzyme activities were elucidated.Ebselen showed efficient bactericidal activity as indicated by its low MIC values, bacterial growth inhibition over time and its ability to prevent clonal propagation in this bacterium. Increased accumulation of ROS in Ebselen treated cells indicates radical mediated induction of bacterial death. Interestingly, Ebselen inhibited and distorted matured biofilms by degrading the eDNA component of the EPS layer. Ebselen also attenuated quorum-sensing pathway as indicated by decreased urease and protease enzyme activities.Taken together, these results paved the way to repurpose Ebselen as a potential drug target to curb Neisseria mucosa infections.
各种细菌群落的抗生素耐药性仍然是全球医疗保健行业的负担。生物膜的形成是细菌群落为逆转抗生素作用而获得的耐药机制之一。迫切需要发现新的抗微生物药物和新的方法来解决这一问题。然而,开发新的抗生素是非常昂贵和具有挑战性的。药物再利用是一种有效的策略,可以减少与药物发现相关的时间和成本。在目前的研究中,有机硒临床分子艾布selen对奈瑟菌粘膜的抗菌和抗膜潜力已经被阐明。抗菌研究包括最低抑菌浓度(MIC)、生长杀伤、菌落形成单位(CFU)测定和细胞内活性氧(ROS)积累研究。抗菌膜的研究包括抑制、清除和细胞表面疏水性测定,胞外聚合物质(EPS)和eDNA的定量测定以及抗群体感应活性、蛋白酶和脲酶活性的测定。Ebselen具有较低的MIC值、长期抑制细菌生长和阻止该细菌克隆繁殖的能力,显示出有效的杀菌活性。在艾布selen处理的细胞中ROS积累增加表明自由基介导的细菌死亡诱导。有趣的是,Ebselen通过降解EPS层的eDNA成分来抑制和扭曲成熟的生物膜。依布selen还通过降低脲酶和蛋白酶活性来减弱群体感应途径。综上所述,这些结果为重新利用Ebselen作为抑制奈瑟菌粘膜感染的潜在药物靶点铺平了道路。
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引用次数: 1
A critical review on recent heterocyclic identified for anti-leishmanial therapy 最近发现的用于抗利什曼病治疗的杂环化合物综述
Pub Date : 2022-03-28 DOI: 10.2174/2212796816666220328130800
S. Rathore, Adarsh Sahu, R. Agrawal, A. G. Patil
Leishmaniasis is a multifaceted disease that is prevalent worldwide. It is an epidemic, seldom abandoned tropical/subtropical disease caused by macrophage infection by compulsive leishmania genus intracellular parasites affecting millions of people across the globe.The demand for effective and safe molecules in the field of leishmaniasis is still an active research area. The lack of widely effective anti-leishmanial drugs, therefore, means a critical need for the production of modern, effective, affordable, and safe drugs for leishmaniasis care. In the recent past, many new pharmacophores have been synthesized and evaluated for their antileishmanial activity.Many important heterocycles had proved to be effective against various leishmanial strains in terms of both safety and efficacy. In this article, we have attempted to review the different pharmacophores discovered in the past few years with the potential anti-leishmanial property.
利什曼病是一种在全世界流行的多方面疾病。这是一种罕见的热带/亚热带流行病,由强迫性利什曼原虫属细胞内寄生虫巨噬细胞感染引起,影响全球数百万人。对利什曼病有效、安全分子的需求仍然是一个活跃的研究领域。因此,缺乏广泛有效的抗利什曼病药物意味着迫切需要生产现代、有效、负担得起和安全的利什曼病治疗药物。近年来,许多新的药效团被合成并被评价为具有抗利什曼原虫的活性。许多重要的杂环化合物已被证明在安全性和有效性方面对各种利什曼原虫菌株有效。本文对近年来发现的具有潜在抗利什曼特性的药效团进行了综述。
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引用次数: 1
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Current Chemical Biology
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