首页|Polyaspers A and B,the First Ergosterol-Polyether Adducts with Unprecedented 6/6/6/5/5/6/6/6/6 Nonacyclic Architecture from Aspergillus sp.TJ507

Polyaspers A and B,the First Ergosterol-Polyether Adducts with Unprecedented 6/6/6/5/5/6/6/6/6 Nonacyclic Architecture from Aspergillus sp.TJ507

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Psoriasis is a chronic immune-mediated inflammatory skin disease and the TNF-α is an important therapeutic target of this disease.In our continuous study of bioactive natural products from fungi,the first ergosterol-polyether adducts,polyaspers A(1)and B(2),along with two known ergosterols,(36,5α,6α,22E)-5,6-epoxy-3-hydroxyergosta-8,22-dien-7-one(3)and calvasterol B(4),were iso-lated from Aspergillus sp.TJ507.Structure elucidation was accomplished by extensive spectroscopic analysis and single-crystal X-ray diffraction tests.Polyaspers A and B possessing an unequalled 6/6/6/5/5/6/6/6/6 nonacyclic system,and their biosynthetic path-ways were proposed to include intermolecular cyclization and Diels-Alder reactions.Activity screen of these isolates showed that 1-3 could improve the cell viability in an actinomycin D/TNF-α induced L929 cells death model,with the EC50 values of 49.85,46.75 and 4.99 μmol/L,respectively,and the activity of 3 was even comparable with that of the positive control SPD304.Further bioactive investigations discovered 3 could suppress the inflammatory response simulated with TNF-α in HaCaT cells.In an imiquimod-induced psoriasis murine model,3 significantly restrained the development of psoriasis symptoms and reduced the expression of IL-17 and IL-23,presenting an anti-psoriatic effect.As such,those ergosterol derivatives,might serve as lead compounds for the development of novel TNF-α inhibitory agents in the clinical treatment of psoriasis.

PsoriasisAspergillus sp.TJ507TNF-αErgosterol-polyether adductsInflammatory skin disease

Hong Hu、Lanqin Li、Zhengyi Shi、Xueqi Lan、Yeting Zhang、Xinye Huang、Xincai Hao、Qun Zhou、Weiguang Sun、Changxing Qi、Yonghui Zhang

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Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation,Tongji Medical College,Huazhong University of Science and Technology,Wuhan,Hubei 430030,China

Hubei Key Laboratory of Wudang Local Chinese Medicine Research,Hubei Engineering Technology Center for Comprehensive Utilization of Medicinal Plants,College of Pharmacy,Hubei University of Medicine,Shiyan,Hubei 442000,China

Institute of Organ Transplantation,Tongji Hospital,Tongji Medical College,Huazhong University of Science and Technology,Key Laboratory of Organ Transplantation,Ministry of Education,NHC Key Laboratory of Organ Transplantation,Key Laboratory of Organ Transplantation,Chinese Academy of Medical Sciences,Wuhan,Hubei 430030,China

国家杰出青年科学基金国家自然科学基金国家自然科学基金国家自然科学基金湖北省自然科学基金Research and Development Program of Hubei ProvinceOpen Foundation of Hubei Key Laboratory of Wudang Local Chinese Medicine Research

817250218200363382173705319728652023AFB7912020BCA058WDCM2023010

2024

10.1002/cjoc.202300649

中国化学(英文版)
中国化学会 上海有机化学研究所

中国化学(英文版)

CSTPCD
影响因子：0.848
ISSN：1001-604X
年,卷(期)：2024.42(7)
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