Department of Chemical Sciences, University of Naples Federico II, Complesso Universitario Monte S. Angelo, Via Cintia 4, 80126, Naples, Italy.
Chembiochem. 2021 Dec 2;22(23):3263-3269. doi: 10.1002/cbic.202100283. Epub 2021 Jul 30.
Sphaeropsidin A (SphA) is a tetracyclic pimarane diterpene, first isolated as the main phytotoxin produced by Diplodia cupressi the causal agent of a severe canker disease of Italian cypress (Cupressus sempervirens L.). It was also produced, together with several analogues, by different pathogenic Diplodia species and other fungi and showed a broad array of biological activities suggesting its promising application in agriculture and medicine. The anticancer activity of SphA is very potent and cell specific. Recent studies have revealed its unique mode of action. This minireview reports the structures of SphA and its family of natural analogues, their biosynthetic origins, their fungal sources, and biological activities. The preparation of various SphA derivatives is also described as well as the results of structure-activity relationship (SAR) studies and on their potential practical applications.
球海松 A(SphA)是一种四环松烷二萜,最初是作为意大利柏(Cupressus sempervirens L.)严重溃疡病的致病因子 Diplodia cupressi 产生的主要植物毒素被分离出来的。它还与几种类似物一起由不同的致病 Diplodia 物种和其他真菌产生,并显示出广泛的生物活性,这表明它在农业和医学中有很有前途的应用。SphA 的抗癌活性非常强且具有细胞特异性。最近的研究揭示了其独特的作用模式。本综述报告了 SphA 及其天然类似物家族的结构、生物合成起源、真菌来源和生物活性。还描述了各种 SphA 衍生物的制备以及结构-活性关系(SAR)研究及其潜在实际应用的结果。