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One-step gram-scale synthesis of striasteroid B inspired by its nonenzymatic formation
Shan Cheng1, Chunmei Chen2, Yi Chen3
1Key Laboratory of Marine Drugs, Ministry of Education of China, School of Medicine and Pharmacy, Ocean University of China, Qingdao 266003, China.
Abstract:
Striasteroids A and B are fungus-derived hybrid steroids with novel skeletons and promising biological activities. Our investigation suggests that both compounds are likely generated from ergosterol and pyrone derivatives via a nonenzymatic pathway during silica gel chromatography. Based on this finding, we developed an efficient one-step synthesis enabling gram-scale production of striasteroid B. In vitro activity evaluation showed that striasteroid B exhibited anti-renal fibrosis activity comparable to that of the clinical drug pirfenidone (PFD) at a concentration of 10 μM. In addition, preliminary pharmacokinetic studies indicated that this compound possesses favorable drug-like properties. Taken together, these results suggest that striasteroid B holds potential for further development as an anti-renal fibrosis agent.
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