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Selection of antimicrobial frog peptides and temporin-1DRa analogues for treatment of bacterial infections based on their cytotoxicity and differential activity against pathogens.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-05-18 , DOI: 10.1111/cbdd.13569 Rogier A Gaiser 1 , Jaione Ayerra Mangado 1 , Milena Mechkarska 2 , Wendy E Kaman 3 , Peter van Baarlen 1 , J Michael Conlon 2 , Jerry M Wells 1
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-05-18 , DOI: 10.1111/cbdd.13569 Rogier A Gaiser 1 , Jaione Ayerra Mangado 1 , Milena Mechkarska 2 , Wendy E Kaman 3 , Peter van Baarlen 1 , J Michael Conlon 2 , Jerry M Wells 1
Affiliation
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Cationic, amphipathic, α‐helical host‐defense peptides (HDPs) that are naturally secreted by certain species of frogs (Anura) possess potent broad‐spectrum antimicrobial activity and show therapeutic potential as alternatives to treat infections by multidrug‐resistant pathogens. Fourteen amphibian skin peptides and twelve analogues of temporin‐1DRa were studied for their antimicrobial activities against clinically relevant human or animal skin infection‐associated pathogens. For comparison, antimicrobial potencies of frog skin peptides against a range of probiotic lactobacilli were determined. We used the VITEK 2 system to define a profile of antibiotic susceptibility for the bacterial panel. The minimal inhibitory concentration (MIC) values of the naturally occurring temporin‐1DRa, CPF‐AM1, alyteserin‐1c, hymenochirin‐2B, and hymenochirin‐4B for pathogenic bacteria were threefold to ninefold lower than the values for the tested probiotic strains. Similarly, temporin‐1DRa and its [Lys4], [Lys5], and [Aib8] analogues showed fivefold to 6.5‐fold greater potency against the pathogens. In the case of PGLa‐AM1, XT‐7, temporin‐1DRa and its [D‐Lys8] and [Aib13] analogues, no apoptosis or necrosis was detected in human peripheral blood mononuclear cells at concentrations below or above the MIC. Given the differential activity against commensal bacteria and pathogens, some of these peptides are promising candidates for further development into therapeutics for topical treatment of skin infections.
中文翻译：
基于它们的细胞毒性和针对病原体的差异活性，选择用于治疗细菌感染的抗菌蛙肽和temporin-1DRa类似物。
某些种类的青蛙（Anura）自然分泌的阳离子，两亲性，α螺旋宿主防御肽（HDP）具有有效的广谱抗菌活性，并显示出了替代治疗多种药物引起的病原体的治疗潜力。研究了14种两栖动物皮肤肽和temporin-1DRa的12种类似物对与临床相关的人或动物皮肤感染相关病原体的抗菌活性。为了进行比较，确定了青蛙皮肤肽对一系列益生菌乳酸菌的抗菌效力。我们使用VITEK 2系统定义了细菌对抗生素敏感性的概况。天然Temporin-1DRa，CPF-AM1，alyteserin-1c，hymenochirin-2B，和致病菌的hyperochirin-4B比被测益生菌菌株的值低三到九倍。同样，temporin-1DRa及其[Lys4 ]，[Lys 5 ]和[Aib 8 ]类似物显示出对病原体的效力提高了五倍至6.5倍。对于PGLa-AM1，XT-7，temporin-1DRa及其[D-Lys 8 ]和[Aib 13 ]类似物，在低于或高于MIC浓度的人外周血单核细胞中均未检测到凋亡或坏死。考虑到针对共生细菌和病原体的不同活性，这些肽中的某些是有希望的候选物，其可以进一步发展成用于皮肤感染的局部治疗的疗法。
更新日期：2019-05-18
中文翻译：
基于它们的细胞毒性和针对病原体的差异活性，选择用于治疗细菌感染的抗菌蛙肽和temporin-1DRa类似物。
某些种类的青蛙（Anura）自然分泌的阳离子，两亲性，α螺旋宿主防御肽（HDP）具有有效的广谱抗菌活性，并显示出了替代治疗多种药物引起的病原体的治疗潜力。研究了14种两栖动物皮肤肽和temporin-1DRa的12种类似物对与临床相关的人或动物皮肤感染相关病原体的抗菌活性。为了进行比较，确定了青蛙皮肤肽对一系列益生菌乳酸菌的抗菌效力。我们使用VITEK 2系统定义了细菌对抗生素敏感性的概况。天然Temporin-1DRa，CPF-AM1，alyteserin-1c，hymenochirin-2B，和致病菌的hyperochirin-4B比被测益生菌菌株的值低三到九倍。同样，temporin-1DRa及其[Lys4 ]，[Lys 5 ]和[Aib 8 ]类似物显示出对病原体的效力提高了五倍至6.5倍。对于PGLa-AM1，XT-7，temporin-1DRa及其[D-Lys 8 ]和[Aib 13 ]类似物，在低于或高于MIC浓度的人外周血单核细胞中均未检测到凋亡或坏死。考虑到针对共生细菌和病原体的不同活性，这些肽中的某些是有希望的候选物，其可以进一步发展成用于皮肤感染的局部治疗的疗法。
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