Department of Pharmacy, University of Naples, Via Domenico Montesano, 49, 80131 Naples, Italy.
Department of Medicine and Surgery, University of Perugia, Piazza L. Severi, 1, 06132 Perugia, Italy.
Mar Drugs. 2023 May 8;21(5):291. doi: 10.3390/md21050291.
The marine environment is considered a vast source in the discovery of structurally unique bioactive secondary metabolites. Among marine invertebrates, the sponge spp. represents an arsenal of novel compounds ranging from peptides, alkaloids, terpenes, macrolides, and sterols. In this review, we summarize the recent reports on sterols isolated from this amazing sponge, describing their structural features and peculiar biological activities. We also discuss the total syntheses of solomonsterols A and B and the medicinal chemistry modifications on theonellasterol and conicasterol, focusing on the effect of chemical transformations on the biological activity of this class of metabolites. The promising compounds identified from spp. possess pronounced biological activity on nuclear receptors or cytotoxicity and result in promising candidates for extended preclinical evaluations. The identification of naturally occurring and semisynthetic marine bioactive sterols reaffirms the utility of examining natural product libraries for the discovery of new therapeutical approach to human diseases.
海洋环境被认为是发现结构独特的生物活性次生代谢产物的巨大来源。在海洋无脊椎动物中， 属海绵代表了一系列新型化合物，包括肽、生物碱、萜类、大环内酯和甾体。在这篇综述中，我们总结了最近从这种神奇的海绵中分离得到的甾体的报道，描述了它们的结构特征和特殊的生物活性。我们还讨论了 solomonsterols A 和 B 的全合成以及 theonellasterol 和 conicasterol 的药物化学修饰，重点关注化学转化对这一类代谢物生物活性的影响。从 属中鉴定出的有前途的化合物对核受体具有明显的生物活性或细胞毒性，为进一步的临床前评估提供了有希望的候选药物。天然存在和半合成海洋生物活性甾体的鉴定证实了检查天然产物文库以发现新的治疗人类疾病方法的实用性。
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