Bioactivity-guided discovery of antiviral templichalasins A‒C from the endophytic fungus Aspergillus templicola.
10.1016/S1875-5364(25)60880-6
- Author:
Teng CAI
1
;
Jingzu SUN
2
;
Wenxuan CHEN
3
;
Qiang HE
4
;
Baosong CHEN
2
;
Yulong HE
1
;
Peng ZHANG
1
;
Yanhong WEI
3
;
Hongwei LIU
5
;
Xiaofeng CAI
6
Author Information
1. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China.
2. State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China.
3. Sino-German Biomedical Center, Key Laboratory of Fermentation Engineering (Ministry of Education), Hubei University of Technology, Wuhan 430068, China.
4. Institute of Food Inspection, Xianning Public Inspection and Testing Center of Hubei Province, Xianning 437000, China.
5. State Key Laboratory of Mycology, Institute of Microbiology, Chinese Academy of Sciences, Beijing 100101, China. Electronic address: liuhw@im.ac.cn.
6. Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, China; State Key Laboratory of Dao-di Herbs, National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China. Electronic address: caixiaofeng@hust.edu.cn.
- Publication Type:Journal Article
- Keywords:
Antiviral activity;
Aspergillus templicola;
Aspochalasins;
Structural elucidation
- MeSH:
Antiviral Agents/isolation & purification*;
Aspergillus/chemistry*;
Molecular Structure;
Enterovirus B, Human/drug effects*;
Endophytes/chemistry*;
Cytochalasins/isolation & purification*;
Drug Discovery;
Humans
- From:
Chinese Journal of Natural Medicines (English Ed.)
2025;23(6):754-761
- CountryChina
- Language:English
-
Abstract:
The bioactivity-guided isolation of potentially active natural products has been widely utilized in pharmaceutical discovery. In this study, by screening fungal extracts against coxsackievirus B3 (CVB3), three new aspochalasins, templichalasins A‒C (1‒3), along with six known aspochalasins (4‒9) were isolated from an active extract derived from the endophytic fungus Aspergillus templicola LHWf045. Compound 1 features a unique 5/6/5/7/5 pentacyclic ring system, while compounds 2 and 3 possess unusual 5/6/6/7 tetracyclic skeletons. Their structures were characterized through extensive spectroscopic analyses, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. Additionally, we demonstrated that compound 4 can be readily converted into compounds 1‒3 under mild acidic conditions and proposed a plausible mechanism for this conversion. Bioactivity evaluation of compounds 1‒9 against CVB3 revealed the inhibitory effects of all compounds against the virus. Notably, compound 9 exhibited superior antiviral activity, surpassing the commercial drug ribavirin in selectivity index (SI) value.
