首页> 外文期刊>The Journal of Antibiotics: An International Journal >N-acetyl-3,4-dihydroxy-L-phenylalanine, a second identified bioactive metabolite produced by Streptomyces sp. 8812
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N-acetyl-3,4-dihydroxy-L-phenylalanine, a second identified bioactive metabolite produced by Streptomyces sp. 8812

机译:N-乙酰基-3,4-二羟基-L-苯丙氨酸,由链霉菌属第二种鉴定出的生物活性代谢产物。 8812

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The emergence of multi-drug-resistant bacteria and the lack of new antibiotics in the antibiotic drug development pipeline is a major health concern. Therefore, there is a constant need to search for novel antibacterial compounds. Streptomyces species are the richest source of bioactive metabolites, including antibacterial compounds.In this paper, we report the isolation of a second bioactive metabolite, N-acetvl-3,4-dihydroxy-L-phenylalanine, named JS-2 (Figure 1), from the supernatant of a Streptomyces sp. 8812 culture. In the course of our screening program for antimicrobial compounds from actinomycetal metabolites for specific inhibitors of DD-peptidases (EC 3.4.16.4), we used exocellular DD-carboxypeptidase/transpeptidase (DD-peptidase) 64-575 II from Saccharopolyspora erythraea 64-575 II. JS-2 exhibited slight inhibitory properties on the DD-peptidases 64-575 II and R39 from Actinomadura R39 (formerly Streptomyces R39). It showed antimicrobial activity against Bordetella bronchiseptica (B. bronchiseptica), Staphylococcus epidermidis (S. epidermidis) and S. aureus (methicillin-resistant (MRSA) or vancomycin resistant (VRSA).Streptomyces sp. 8812 fermentation culture was conducted as reported previously. Isolation and purification of JS-2 was performed, guided by DD-peptidase 64-575 II assay. Purification steps were done as follows: anion exchange resin IRA-400 (AcO~-), Backerbond SPE (PolarPlus C_18 column, J.T. Baker, Phillipsburg, NJ, USA) and HPLC (Atlantis, dC18, Waters, Milford, MA, USA) (Supplementary Figure IS; Supplementary Purification of JS-2).
机译:抗生素药物开发过程中出现了多药耐药细菌和缺乏新抗生素,这是一个主要的健康问题。因此,一直需要寻找新型的抗菌化合物。链霉菌是包括抗菌化合物在内的生物活性代谢产物的最丰富来源。本文报道了第二种生物活性代谢产物N-acetvl-3,4-dihydroxy-L-phenylalanine JS-2的分离(图1)。 ,来自链霉菌属种的上清液。 8812文化。在我们针对放线菌代谢物的DD肽酶特异性抑制剂的筛选程序(EC 3.4.16.4)的筛选程序中,我们使用了来自红糖酵母(Saccharopolyspora erythraea 64-575)的细胞外DD-羧肽酶/转肽酶(DD-肽酶)64-575 II。二。 JS-2对来自Actinomadura R39(以前是链霉菌R39)的DD肽酶64-575 II和R39表现出轻微的抑制作用。它显示了对支气管芽孢杆菌(B. bronchiseptica),表皮葡萄球菌(S. epidermidis)和金黄色葡萄球菌(Micillillin抗性(MRSA)或万古霉素抗性(VRSA))的抗菌活性。链霉菌(Streptomyces sp。)8812的发酵培养如前所述。在DD-肽酶64-575 II分析的指导下进行JS-2的分离纯化,纯化步骤如下:阴离子交换树脂IRA-400(AcO〜-),Backerbond SPE(PolarPlus C_18色谱柱,JT Baker, HPLC(美国新泽西州菲利普斯堡)和HPLC(美国马萨诸塞州米尔福德,Waters,Atlantis,dC18)(补充图IS; JS-2的补充纯化)。

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