首页|Spirohypertones A and B as potent antipsoriatics:Tumor necrosis factor-α inhibitors with unprecedented chemical architectures

Spirohypertones A and B as potent antipsoriatics:Tumor necrosis factor-α inhibitors with unprecedented chemical architectures

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Tumor necrosis factor-α(TNF-α)is a promising target for inflammatory and autoimmune dis-eases.Spirohypertones A(1)and B(2),two unprecedented polycyclic polyprenylated acylphloroglucinols with highly rearranged skeletons,were isolated from Hypericum patulum.The structures of 1 and 2 were confirmed through comprehensive spectroscopic analysis,single-crystal X-ray diffraction and electronic cir-cular dichroism calculations.Importantly,2 showed remarkable TNF-α inhibitory activity,which could pro-tect L929 cells from death induced by co-incubation with TNF-α and actinomycin D.It also demonstrated the ability to suppress the inflammatory response in HaCaT cells stimulated with TNF-α.Notably,in an imiquimod-induced psoriasis murine model,2 restrained symptoms of epidermal hyperplasia associated with psoriasis,presenting anti-inflammatory and antiproliferative effects.This discovery positions 2 as a potent TNF-α inhibitor,providing a promising lead compound for developing an antipsoriatic agent.

Hypericum patulumPolycyclic polyprenylated acylphloroglucinolsTumor necrosis factor-α inhibitory activityPsoriasis

Yulin Duan、Weiguang Sun、Yongqi Li、Zhengyi Shi、Lanqin Li、Yeting Zhang、Kun Huang、Zhiping Zhang、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 430030,China

Department of Pharmacy,Wuhan No.1 Hospital,Wuhan 430022,China

Program for Changjiang Scholars of Ministry of Education of the People's Republic of ChinaNational Natural Science Foundation for Distinguished Young Scholars,ChinaNational Natural Science Foundation of ChinaNational Natural Science Foundation of ChinaNational Natural Science Foundation of ChinaNational Natural Science Foundation of Hubei Province,ChinaNational Natural Science Foundation of Hubei Province,ChinaKnowledge Innovation Project of Wuhan Science and Technology Bureau,ChinaResearch and Development Program of Hubei Province,ChinaOpen Foundation of Hubei Key Laboratory of Wudang Local Chinese Medicine Research,ChinaOpen Research Fund Program of State Key Laboratory of Biocatalysis and Enzyme Engineering,China

T2016088817250218200363332100321323003352023AFB7912023AFB53020230202010205342020BCA058WDCM2023010SKLBEE2023003

2024

10.1016/j.apsb.2024.02.002

药学学报(英文版)

药学学报(英文版)

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ISSN：
年,卷(期)：2024.14(6)
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