抗生素是药物史中治疗感染性疾病的最重要的药物之一。然而,因为人们广泛地使用甚至滥用抗生素,所以在临床中不断出现新的耐药菌,导致现有抗生素的效的英语翻译

抗生素是药物史中治疗感染性疾病的最重要的药物之一。然而,因为人们广泛地

抗生素是药物史中治疗感染性疾病的最重要的药物之一。然而,因为人们广泛地使用甚至滥用抗生素,所以在临床中不断出现新的耐药菌,导致现有抗生素的效力不断丧失。细菌耐药性是世界各国共同关注的健康问题,但是耐药菌的发展速度远远超于抗菌药物的研究速度,因此研发活性高,毒性低,低耐药性的抗菌药物俨然成为研究抗菌药物的重中之重。抗菌肽(Antimicrobial Peptides,AMPs)是多细胞生物体内天然存在的,其主要用来阻挡微生物的感染,被称为免疫功能的第一道关卡。它是一种通常带有亲水性的正电荷和亲脂性的侧链的肽类物质。但抗菌肽存在潜在的体内毒性,较差的药代动力学性质等缺点,这些缺点制约着抗菌肽的进一步发展。研究发现一些小分子抗菌肽模拟物在保持其自身活性的前提下又能克服抗菌肽的缺点,展现出良好的抗菌活性,低细胞毒性和低耐药性,成为抗菌药物研发的一个新热点。和厚朴酚的抗菌活性非常显著,对革兰氏阳性菌(G+)、阴性菌(G-)以及真菌都具有明显的抑制作用。同时也有对抗肿瘤的作用、延缓衰老的疗效、和使胆固醇下降的功能。研究发现,和厚朴酚是具有两个疏水的烯丙基脂肪侧链的结构,它们是发挥抗菌活性的重要基团,因此,我们基于抗菌肽的分子结构特性,以和厚朴酚为结构骨架,在其羟基上引入不同长度的阳离子基团如氨基,构建化合物亲水侧链和亲脂骨架的两亲性的特征,形成与抗菌肽类似的空间结构并对其进行了抗菌活性的研究。实验结果表明,目标化合物3和5对多种革兰氏阳性菌和阴性菌显示出优于对照化合物环丙沙星的抗菌活性。
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源语言: -
目标语言: -
结果 (英语) 1: [复制]
复制成功!
Antibiotics are one of the most important drugs in the history of drugs to treat infectious diseases. However, because of the widespread use and even abuse of antibiotics, new drug-resistant bacteria continue to appear in the clinic, resulting in the continuous loss of the effectiveness of existing antibiotics. Bacterial resistance is a common health concern of all countries in the world, but the development rate of drug-resistant bacteria is far faster than the research speed of antibacterial drugs. Therefore, the development of antibacterial drugs with high activity, low toxicity, and low drug resistance has become a research antibacterial drug. The top priority. Antimicrobial peptides (Antimicrobial Peptides, AMPs) are naturally present in multicellular organisms. They are mainly used to block microbial infections and are called the first level of immune function. It is a peptide substance usually with hydrophilic positive charge and lipophilic side chain. However, antimicrobial peptides have potential shortcomings in vivo toxicity, poor pharmacokinetic properties, etc. These shortcomings restrict the further development of antimicrobial peptides. The study found that some small-molecule antimicrobial peptide mimics can overcome the shortcomings of antimicrobial peptides while maintaining their own activity, exhibit good antimicrobial activity, low cytotoxicity and low drug resistance, which has become a new hotspot in the development of antimicrobial drugs. <br>The antibacterial activity of honokiol is very significant, and it has obvious inhibitory effects on Gram-positive bacteria (G +), negative bacteria (G-) and fungi. It also has anti-tumor effects, anti-aging effects, and cholesterol lowering functions. The study found that Honokiol is a structure with two hydrophobic allyl fatty side chains. They are important groups to exert antibacterial activity. Therefore, based on the molecular structural characteristics of antimicrobial peptides, we use Honokiol as the structure Skeleton, the introduction of cationic groups of different lengths such as amino groups on its hydroxyl group, to construct the amphiphilic characteristics of the hydrophilic side chain and lipophilic skeleton of the compound, to form a spatial structure similar to antibacterial peptides and to study its antibacterial activity. The experimental results showed that the target compounds 3 and 5 showed better antibacterial activity than the control compound ciprofloxacin against a variety of Gram-positive and negative bacteria.
正在翻译中..
结果 (英语) 2:[复制]
复制成功!
抗生素是药物史中治疗感染性疾病的最重要的药物之一。然而,因为人们广泛地使用甚至滥用抗生素,所以在临床中不断出现新的耐药菌,导致现有抗生素的效力不断丧失。细菌耐药性是世界各国共同关注的健康问题,但是耐药菌的发展速度远远超于抗菌药物的研究速度,因此研发活性高,毒性低,低耐药性的抗菌药物俨然成为研究抗菌药物的重中之重。抗菌肽(Antimicrobial Peptides,AMPs)是多细胞生物体内天然存在的,其主要用来阻挡微生物的感染,被称为免疫功能的第一道关卡。它是一种通常带有亲水性的正电荷和亲脂性的侧链的肽类物质。但抗菌肽存在潜在的体内毒性,较差的药代动力学性质等缺点,这些缺点制约着抗菌肽的进一步发展。研究发现一些小分子抗菌肽模拟物在保持其自身活性的前提下又能克服抗菌肽的缺点,展现出良好的抗菌活性,低细胞毒性和低耐药性,成为抗菌药物研发的一个新热点。<br>和厚朴酚的抗菌活性非常显著,对革兰氏阳性菌(G+)、阴性菌(G-)以及真菌都具有明显的抑制作用。同时也有对抗肿瘤的作用、延缓衰老的疗效、和使胆固醇下降的功能。研究发现,和厚朴酚是具有两个疏水的烯丙基脂肪侧链的结构,它们是发挥抗菌活性的重要基团,因此,我们基于抗菌肽的分子结构特性,以和厚朴酚为结构骨架,在其羟基上引入不同长度的阳离子基团如氨基,构建化合物亲水侧链和亲脂骨架的两亲性的特征,形成与抗菌肽类似的空间结构并对其进行了抗菌活性的研究。实验结果表明,目标化合物3和5对多种革兰氏阳性菌和阴性菌显示出优于对照化合物环丙沙星的抗菌活性。
正在翻译中..
结果 (英语) 3:[复制]
复制成功!
Antibiotics are one of the most important drugs for the treatment of infectious diseases. However, because of the widespread use and even abuse of antibiotics, new drug-resistant bacteria are emerging in clinical practice, resulting in the loss of the effectiveness of existing antibiotics. Drug resistance of bacteria is a common concern of all countries in the world, but the development speed of drug-resistant bacteria is far faster than the research speed of antibacterial drugs, so the research and development of high activity, low toxicity, low drug resistance of antibacterial drugs has become the top priority. Antimicrobial peptides (AMPS) are naturally existing in multicellular organisms, which are mainly used to block the infection of microorganisms, and are called the first checkpoint of immune function. It is a kind of peptide with hydrophilic positive charge and lipophilic side chain. However, antimicrobial peptides have potential toxicity in vivo and poor pharmacokinetic properties, which restrict the further development of antimicrobial peptides. It has been found that some small molecular antimicrobial peptide analogues can overcome the shortcomings of antimicrobial peptides while maintaining their own activity, showing good antibacterial activity, low cytotoxicity and low resistance, which has become a new hotspot in the research and development of antibacterial drugs.<br>And honokiol have significant antibacterial activity, which can inhibit Gram-positive bacteria (G +, G -) and fungi. At the same time, it has the functions of anti-tumor, anti-aging effect and cholesterol lowering. It is found that honokiol and honokiol are the structures of two hydrophobic allylic fatty side chains, and they are important groups to exert antibacterial activity. Therefore, based on the molecular structural characteristics of antibacterial peptides, we take honokiol and honokiol as the structural framework, and introduce different length of cation groups such as amino groups into their hydroxyl groups, to construct the amphiphilic characteristics of the hydrophilic side chain and lipophilic framework of compounds The antibacterial activity of the peptide was studied. The results showed that the antibacterial activity of target compounds 3 and 5 was better than that of ciprofloxacin.
正在翻译中..
 
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