Post-ingestion conversion of dietary indoles into anticancer agents
식이 인돌의 섭취 후 항암제로 전환
Conversión postingestión de indoles dietéticos en agentes anticancerígenos
Conversion post-ingestion des indoles alimentaires en agents anticancéreux
Превращение диетических индолов в противораковые агенты после приема внутрь
Li Ping Lin ¹ ², Dan Liu 刘丹 ², Jia Cheng Qian ², Liang Wu ², Quan Zhao 赵权 ¹, Ren Xiang Tan 谭仁祥 ¹ ²
¹ State Key Laboratory of Pharmaceutical Biotechnology, Institute of Functional Biomolecules, Nanjing University, Nanjing 210023, China 南京大学 功能生物分子研究所 医药生物技术国家重点实验室
² State Key Laboratory Cultivation Base for TCM Quality and Efficacy, Nanjing University of Chinese Medicine, Nanjing 210023, China 南京中医药大学 中药品质与效能国家重点实验室培育点
National Science Review, 13 August 2021

Human health benefits from consuming cruciferous vegetables that release indole-3-carbinol (I3C), but the in vivo transformation of I3C-related indoles remains underinvestigated. Here we present the post-ingestion conversion of I3C into antitumor agents, 2-(indol-3-ylmethyl)-3,3′-diindolylmethane (LTr1) and 3,3′-diindolylmethane (DIM), by conceptualizing and materializing the reaction flux derailing (RFD) approach as a means of unraveling these stepwise transformations to be non-enzymatic but pH-dependent and gut microbe-sensitive.

In the upper (or acidic) gastrointestine, LTr1 generates through the Michael addition of 3-methyleneindolium (3MI, derived in situ from I3C) to DIM producing from I3C via the formaldehyde-releasing (major) and CO2-liberating (minor) pathways. In the large intestine, 'endogenous' I3C and DIM can form respectively from couplings of formaldehyde with one and two molecules of indole (a tryptophan catabolite). Acid-producing gut bacteria such as Lactobacillus acidophilus facilitate the H+-promotable steps. The work updates the understanding on the merits of I3C consumptions and identifies LTr1 as a drug candidate.
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