Abstract

Actinomycetes are well-known as the main producers of bioactive compounds such as antibiotics, anticancers, and immunosuppressants. Screening of natural products from actinomycetes has been an essential part of several drug discovery programs. Finding such novel biologically active metabolites is immensely important because of their beneficial health effects. Recently, the discovery of new compounds has diverted attention to rare actinomycetes, since they are rich sources of natural products. In this study, a collection of rare actinomycetes at Kitasato University has been screened for potential novel compound producers. Among the rare actinomycetes, Saccharopolyspora sp. KR21-0001 isolated from soil on Ōha Island, Okinawa, Japan was selected as a potential producer. The strain was cultured in 20 L of production medium in a jar fermenter and the culture broth was extracted. Further purification revealed the presence of a new compound designated KR21-0001A (1). The structure was elucidated by NMR, and the absolute stereochemistry was determined by advanced Marfey’s method. The results indicated that 1 is a new analog of dihydroxybenzoic acid. 1 has no antimicrobial activity against bacteria and fungi but showed potent antioxidant activity_.

Beilstein J. Org. Chem. 2024, 20, 497–503. doi:10.3762/bjoc.20.44

摘要

众所周知，放线菌是抗生素、抗癌剂和免疫抑制剂等生物活性化合物的主要生产者。从放线菌中筛选天然产物一直是多个药物发现计划的重要组成部分。寻找这种新颖的生物活性代谢物非常重要，因为它们对健康有益。最近，新化合物的发现将注意力转移到稀有放线菌上，因为它们是天然产物的丰富来源。在这项研究中，北里大学的一系列稀有放线菌已被筛选，以寻找潜在的新型化合物生产者。在罕见的放线菌中，糖多孢菌属sp。从日本冲绳大叶岛土壤中分离出来的 KR21-0001 被选为潜在生产者。将菌株在发酵罐中的20L生产培养基中培养，并提取培养液。进一步纯化表明存在一种名为 KR21-0001A 的新化合物 ( 1 )。通过NMR阐明了结构，并通过先进的Marfey方法测定了绝对立体化学。结果表明1是二羟基苯甲酸的新类似物。1对细菌和真菌没有抗菌活性，但显示出有效的抗氧化活性_。

贝尔斯坦 J. 组织。化学。 2024, 20, 497–503。doi:10.3762/bjoc.20.44