2. Academic Validation
  3. Catenulopyrizomicins, new anti-Hepatitis B virus compounds, from the rare actinomycete Catenuloplanes sp. MM782L-181F7

Catenulopyrizomicins, new anti-Hepatitis B virus compounds, from the rare actinomycete Catenuloplanes sp. MM782L-181F7

  • J Antibiot (Tokyo). 2023 Nov 27. doi: 10.1038/s41429-023-00681-4.
Manabu Yamasaki 1,  Ryuichi Sawa 2,  Hideyuki Muramatsu 2,  Yui Yamamoto 2,  Maya Umekita 2,  Yumiko Kubota 2,  Yumi Kanegae 3,  Masayuki Igarashi 2
Affiliations

Affiliations

  • 1 Institute of Microbial Chemistry (BIKAKEN), Shinagawa-ku, Tokyo, Japan. [email protected].
  • 2 Institute of Microbial Chemistry (BIKAKEN), Shinagawa-ku, Tokyo, Japan.
  • 3 Core Research Facilities of Basic Science, Research Center for Medical Science, The Jikei University School of Medicine, Minato-ku, Tokyo, Japan.
PMID: 38008738 DOI: 10.1038/s41429-023-00681-4
Abstract

Hepatitis B virus (HBV) causes chronic hepatitis in humans, and current Antiviral therapies rarely treat viral infections. To improve the treatment efficacy, novel therapeutic agents, especially those with different mechanisms of action, need to be developed for use in combination with the current antivirals. Here, we isolated new anti-HBV compounds, named catenulopyrizomicins A-C, from the fermentation broth of rare actinomycete Catenuloplanes sp. MM782L-181F7. Structural analysis revealed that these compounds contained a structure that is composed of thiazolyl pyridine moiety. The catenulopyrizomicins reduced the amount of intracellular viral DNA in HepG2.2.15 cells with EC50 values ranging from 1.94 to 2.63 µM with small but notable selectivity. Mechanistic studies indicated that catenulopyrizomicin promotes the release of immature virion particles that fail to be enveloped through alterations in membrane permeability.

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