Modulating the microbiome as an approach to anticancer drug development

J Jemma Arakelyan (Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong, SAR 999077, People’s Republic of China) H Ho-Jung Choe (Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong SAR 999077, People’s Republic of China) C Chengnan Wu (Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong SAR 999077, People’s Republic of China) D Daniil A. Rusanov (Department of Chemistry, Drug Discovery Lab, City University of Hong Kong) E Elena E. Bardina (A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences) A Anna A. Kirsanova (Department of Chemistry, Drug Discovery Lab, City University of Hong Kong) Y Yuliya V. Zakalyukina (Department of Soil Science, Lomonosov Moscow State University) N Nikita Y. Shmelev (A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences) A Anton P. Tyurin (Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry) V Vladislav Y. Komarov (A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences) V Vladimir Kushnarev (Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong SAR 999077, People’s Republic of China) N Nikolay S. Karnaukhov (Moscow Clinical Research Center named after A.S. Loginov) G Gerald D’Cruz (Department of Chemistry, Drug Discovery Lab, City University of Hong Kong) E Eugene S. Vasilyev (N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences) E Eunice Dotse (Department of Biomedical Sciences, City University of Hong Kong) K Kwan T. Chow (Department of Biomedical Sciences, City University of Hong Kong) W William C. Cho (Department of Clinical Oncology, Queen Elizabeth Hospital) A Alexey V. Tkachev (N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences) A Artem L. Gushchin (A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences) M Maria V. Babak (Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong, SAR 999077, People’s Republic of China)

Abstract

Recent studies have suggested that the commensal microbiome positively affects cancer prognosis and treatment outcomes. However, only a few strategies for regulating the microbiome composition have been reported. In this study, we identified gold(I) complexes that selectively inhibited nonbeneficial bacterial strains in vitro without affecting commensal Lactobacillus strains. In contrast, clinically used drugs demonstrated comparable effects on both commensal and noncommensal strains. Consistent with the in vitro results, the selected gold(I) complex induced favorable changes in the intratumoral and gastrointestinal microbiomes in vivo. Furthermore, its anticancer efficacy was found to be dependent on the composition of microbiome and correlated with the production of short-chain fatty acid bacterial metabolites. Structure–activity relationship studies have dissected the contribution of each structural component in both the in vivo efficacy and microbiome-modulating properties. Transcriptomic analysis of tumors revealed microbiome-associated gene signaling pathways. These findings provide valuable insights for future research on microbiome-modulating anticancer drugs, presenting potential avenues to optimize cancer treatment outcomes and mitigate side effects such as gastrointestinal dysbiosis. Furthermore, our study provides insights into the involvement of microbiome in the mechanism of action of metal-based chemotherapeutics.

Article Details

Volume / Issue Vol. 122, Issue 44
Published November 04, 2025
ISSN 0027-8424
Publisher National Academy of Sciences

Authors (20)

J

Jemma Arakelyan

Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong, SAR 999077, People’s Republic of China

H

Ho-Jung Choe

Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong SAR 999077, People’s Republic of China

C

Chengnan Wu

Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong SAR 999077, People’s Republic of China

D

Daniil A. Rusanov

Department of Chemistry, Drug Discovery Lab, City University of Hong Kong

E

Elena E. Bardina

A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences

A

Anna A. Kirsanova

Department of Chemistry, Drug Discovery Lab, City University of Hong Kong

Y

Yuliya V. Zakalyukina

Department of Soil Science, Lomonosov Moscow State University

N

Nikita Y. Shmelev

A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences

A

Anton P. Tyurin

Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry

V

Vladislav Y. Komarov

A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences

V

Vladimir Kushnarev

Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong SAR 999077, People’s Republic of China

N

Nikolay S. Karnaukhov

Moscow Clinical Research Center named after A.S. Loginov

G

Gerald D’Cruz

Department of Chemistry, Drug Discovery Lab, City University of Hong Kong

E

Eugene S. Vasilyev

N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences

E

Eunice Dotse

Department of Biomedical Sciences, City University of Hong Kong

K

Kwan T. Chow

Department of Biomedical Sciences, City University of Hong Kong

W

William C. Cho

Department of Clinical Oncology, Queen Elizabeth Hospital

A

Alexey V. Tkachev

N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of Russian Academy of Sciences

A

Artem L. Gushchin

A.V. Nikolaev Institute of Inorganic Chemistry, Siberian Branch of Russian Academy of Sciences

M

Maria V. Babak

Drug Discovery Lab, Department of Chemistry, City University of Hong Kong, 83 Tat Chee Avenue, Hong Kong, SAR 999077, People’s Republic of China