Cooperative Redox Reactions Encoded by Two Gene Clusters Enable Intermolecular Cycloaddition Cascade for the Formation of Meroaspochalasins

P Pengkun Li (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) J Jie Meng (Hefei National Research Center for Physical Sciences at the Microscale and Synergetic Innovation Center of Quantum Information & Quantum Physics, New Cornerstone Science Laboratory) X Xiaotian Zhang X Xiaopeng Zhang (Institute for Materials Chemistry and Engineering and IRCCS, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan) Y Yonghao Ye Y Yunpeng Zhao X Xuenian Huang (Shandong Provincial Key Laboratory of Synthetic Biology, Key Laboratory of Biofuels Qingdao Institute of Bioenergy and Bioprocess Technology, Chinese Academy of Sciences Qingdao 266101 China) Z Ziou Zha (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) Z Zhenhua Guan (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) S Suitian Lai (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) Z Zhe Chen (Gladstone Institutes, San Francisco, CA, USA.) Z Zengwei Luo (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) J Jianping Wang (Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering) C Chunmei Chen J Junjun Liu (Techshake Biotechnology Co., Ltd., Xi’an, Shaanxi, China.) L Lianghu Gu (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) Y Yuhui Sun S Shuming Li H Hucheng Zhu (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) Y Ying Ye Y Yuan Zhou (State Key Laboratory of Cognitive Science and Mental Health, Institute of Psychology, Chinese Academy of Sciences) Y Yonghui Zhang

Abstract

Abstract Meroaspochalasins (mAPOs) are a group of intricate heteromers comprising two distinct subunits, dienophile aspochalasin, and diene isobenzofuran, of which the biosynthetic mechanism is of great interest yet unrevealed. In this study, two independent biosynthetic gene clusters (BGCs), flas and epi , being responsible for the biosynthesis of aspochalasin B ( 7 ) and pre‐diene hemiacetal 21 (or 26 ), respectively, were identified in the filamentous fungus Aspergillus flavipes . In vivo and in vitro studies proved that a flavin adenine dinucleotide (FAD)‐dependent oxidase FlasF in the flas cluster catalyzes the crucial oxidation to generate diverse aspochalasin monomers, particularly the dienophile 7 . Interactive reduction catalyzed by the short‐chain alcohol dehydrogenase/reductase (SDR) FlasG and endogenous NADPH further increases the complexity of this anabolic network. The cytochrome P450 enzyme EpiC and SDR enzyme EpiD in the epi cluster collaboratively catalyze the formation of pre‐diene 21 (or 26 ), which can spontaneously dehydrate to yield a diene, leading to the nonenzymatic cascade of [4 π + 2 π ] Diels–Alder and formal [5 π + 2π] cycloaddition reaction to generate mAPO dimers and trimer progressively. Moreover, the FAD‐dependent oxidase EpiG catalyzes the hydroxylation at the C3 position of the diene as a critical step in the formation of mAPO trimers.

Article Details

Volume / Issue Vol. 64, Issue 22
Published May 26, 2025
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (22)

P

Pengkun Li

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

J

Jie Meng

Hefei National Research Center for Physical Sciences at the Microscale and Synergetic Innovation Center of Quantum Information & Quantum Physics, New Cornerstone Science Laboratory

X

Xiaotian Zhang

X

Xiaopeng Zhang

Institute for Materials Chemistry and Engineering and IRCCS, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan

Y

Yonghao Ye

Y

Yunpeng Zhao

X

Xuenian Huang

Shandong Provincial Key Laboratory of Synthetic Biology, Key Laboratory of Biofuels Qingdao Institute of Bioenergy and Bioprocess Technology, Chinese Academy of Sciences Qingdao 266101 China

Z

Ziou Zha

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

Z

Zhenhua Guan

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

S

Suitian Lai

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

Z

Zhe Chen

Gladstone Institutes, San Francisco, CA, USA.

Z

Zengwei Luo

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

J

Jianping Wang

Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering

C

Chunmei Chen

J

Junjun Liu

Techshake Biotechnology Co., Ltd., Xi’an, Shaanxi, China.

L

Lianghu Gu

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

Y

Yuhui Sun

S

Shuming Li

H

Hucheng Zhu

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

Y

Ying Ye

Y

Yuan Zhou

State Key Laboratory of Cognitive Science and Mental Health, Institute of Psychology, Chinese Academy of Sciences

Y

Yonghui Zhang