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Dihydro-α-Pyrone Antibiotics from a Soil-Derived Fungus Talaromyces sp. G23

文献类型：期刊论文

作者Wang, Zi-Peng1,3; Cheng, Si-Jie3; Li, Ying3; Fang, Chu-Hong3; Liu, Xiang-Yu3; Wang, Xiao-Ning1; Guan, Dong-Liang3; Yue, Jian-Min2,3; Yu, Jin-Hai3
刊名JOURNAL OF NATURAL PRODUCTS
出版日期2026-01-23
卷号89期号:1页码:294-303
ISSN号0163-3864
DOI10.1021/acs.jnatprod.5c01455
英文摘要Nine novel dihydro-alpha-pyrone derivatives, talaromypyrones A-I (1-9), were isolated from the soil-derived fungus Talaromyces sp. G23. These compounds share a conserved 3 ' R-configuration within the 4-hydroxy-5,6-dihydro-2-pyrone core but display notable variations in their flanking polyketide chains. Talaromypyrones A-H (1-8) demonstrate potent antibacterial activity against Gram-positive bacteria, including drug-resistant strains, while exhibiting excellent safety profile by showing no cytotoxicity toward normal human LO2 cells. However, they exhibit no activity against Gram-negative bacteria (likely due to their inability to penetrate the outer membrane) and fungi. Such antimicrobial profile, combined with the structural similarity to the alpha-pyrone antibiotic myxopyronin, suggests a potential target in the switch region of bacterial RNA polymerase (RNAP). Molecular docking studies revealed that talaromypyrone E (5) binds to the same site of RNAP as myxopyronin and forms additional hydrogen bonds between the 4-hydroxy-5,6-dihydro-2-pyrone core and the RNAP residues. Furthermore, talaromypyrones A (1) and D (4) demonstrate moderate anti-inflammatory activity, positioning 4-hydroxy-5,6-dihydro-2-pyrone core as a promising building block for the development of dual-function agents capable of concurrently addressing both conventional and drug-resistant bacterial infections while alleviating associated inflammatory responses.
WOS关键词SERRATIA-PLYMUTHICA ; NATURAL-PRODUCTS ; MOLECULAR-BASIS ; EFFLUX PUMPS ; RESISTANCE
资助项目Key Technology Research and Development Program of Shandong Province[2024CXPT029] ; Shandong Laboratory Program[SYS202205]
WOS研究方向Plant Sciences ; Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001659210300001
出版者AMER CHEMICAL SOC
源URL[http://119.78.100.183/handle/2S10ELR8/322602]  
专题国家级研究中心_原创新药研究全国重点实验室
通讯作者Yue, Jian-Min; Yu, Jin-Hai
作者单位1.Shandong Univ, Cheeloo Coll Med, Sch Pharmaceut Sci, Key Lab Chem Biol,Minist Edu, Jinan 250012, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China
推荐引用方式
GB/T 7714		 Wang, Zi-Peng,Cheng, Si-Jie,Li, Ying,et al. Dihydro-α-Pyrone Antibiotics from a Soil-Derived Fungus Talaromyces sp. G23[J]. JOURNAL OF NATURAL PRODUCTS,2026,89(1):294-303.
APA Wang, Zi-Peng.,Cheng, Si-Jie.,Li, Ying.,Fang, Chu-Hong.,Liu, Xiang-Yu.,...&Yu, Jin-Hai.(2026).Dihydro-α-Pyrone Antibiotics from a Soil-Derived Fungus Talaromyces sp. G23.JOURNAL OF NATURAL PRODUCTS,89(1),294-303.
MLA Wang, Zi-Peng,et al."Dihydro-α-Pyrone Antibiotics from a Soil-Derived Fungus Talaromyces sp. G23".JOURNAL OF NATURAL PRODUCTS 89.1(2026):294-303.

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来源：上海药物研究所

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