Total Biocatalytic Synthesis of Capsaicinoids Using Ferulic Acid: A Versatile Two‐Step Strategy for Natural Product Diversification

T Taresh P. Khobragade (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) P Pritam Giri M Mahesh D. Patil (Chemical Engineering and Process Development Division CSIR‐ National Chemical Laboratory Pune 411008 India) S Sangwoo Joo (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) S Sunga Cho (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) Y Yechan Kim (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) R Rohan Ghosh (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) S Sanghun Jeong (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) M Minyeong Maeng (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) M Min‐Ho Song (Department of Biological Environment Kangwon University Chuncheon Campus Chuncheon‐si Republic of Korea) J Jeong‐Min Park (Department of Chemistry Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) E Eun Ho Lee (Department of Chemistry Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) Y Young‐Soo Keum (Department of Crop Science Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) T Taek Jin Kang (Department of Chemical and Biochemical Engineering Dongguk University, Seoul Dongguk University Seoul 04620 Republic of Korea) Y Yong‐Seok Heo (Department of Chemistry Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea) H Hyungdon Yun (Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea)

Abstract

Abstract The wide‐ranging application of capsaicinoids, the active compounds in chili peppers, has driven increasing interest in the development of sustainable production strategies. However, capsaicinoid synthesis remains a challenge. The objective of this pioneering study is to report the total biocatalytic synthesis of structurally diverse capsaicinoids from bio‐based ferulic acids. An X‐ray crystallographic study elucidated the structural basis for the exceptional potential of a novel transaminase from Phaeobacter porticola (PPTA) to transform the highest ever reported concentration of vanillin (100–200 mM) to vanillylamine, with >99% conversion and modest conversion ranging from 48% to 79% for 300 to 500 mM substrate. Using PPTA in tandem with phenolic acid decarboxylase (PAD) and aromatic dioxygenase (ADO) further enabled the direct synthesis of vanillylamine from ferulic acid with >99% conversion. Furthermore, the integration of a multi‐enzymatic cascade with carboxylic acid reductases (CARs) successfully synthesized structurally diverse capsaicinoids via amide bond formation between vanillylamine and free fatty acids, with excellent conversions ranging from 72% to >88%. A 50‐mM enzymatic reaction afforded 95% and 80% conversion of vanillylamine and capsaicin, respectively.

Article Details

Volume / Issue Vol. 64, Issue 49
Published December 01, 2025
ISSN 1433-7851
Publisher Wiley

Journal Info

Angewandte Chemie International Edition

Wiley

ISSN: 1433-7851 Physical Sciences

Authors (16)

T

Taresh P. Khobragade

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

P

Pritam Giri

M

Mahesh D. Patil

Chemical Engineering and Process Development Division CSIR‐ National Chemical Laboratory Pune 411008 India

S

Sangwoo Joo

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

S

Sunga Cho

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

Y

Yechan Kim

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

R

Rohan Ghosh

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

S

Sanghun Jeong

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

M

Minyeong Maeng

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

M

Min‐Ho Song

Department of Biological Environment Kangwon University Chuncheon Campus Chuncheon‐si Republic of Korea

J

Jeong‐Min Park

Department of Chemistry Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

E

Eun Ho Lee

Department of Chemistry Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

Y

Young‐Soo Keum

Department of Crop Science Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

T

Taek Jin Kang

Department of Chemical and Biochemical Engineering Dongguk University, Seoul Dongguk University Seoul 04620 Republic of Korea

Y

Yong‐Seok Heo

Department of Chemistry Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea

H

Hyungdon Yun

Department of Systems Biotechnology Konkuk University 120 Neungdong‐ro, Gwangjin‐gu Seoul 05029 Republic of Korea