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Novel Benzoxazoles Containing 4-Amino-Butanamide Moiety Inhibited LPS-Induced Inflammation by Modulating IL-6 or IL-1β mRNA Expression
- Title
- Novel Benzoxazoles Containing 4-Amino-Butanamide Moiety Inhibited LPS-Induced Inflammation by Modulating IL-6 or IL-1β mRNA Expression
- Authors
- Yoo J.; Park J.; Kim D.; Huh Y.; Choo H.-Y.P.; Woo H.A.
- Ewha Authors
- 박혜영; 우현애; 박지영
- SCOPUS Author ID
- 박혜영; 우현애; 박지영
- Issue Date
- 2022
- Journal Title
- International Journal of Molecular Sciences
- ISSN
- 1661-6596
- Citation
- International Journal of Molecular Sciences vol. 23, no. 10
- Keywords
- anti-inflammatory effect; benzoxazole; IL-1β; IL-6; mRNA expression; small molecules; TNF-α
- Publisher
- MDPI
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- LPS induces inflammatory cytokines, including IL-1β, IL-6, and TNF-α, and causes an inflammatory response. The development of small molecules that have suppressive effect on those inflammatory cytokines is a desirable strategy for the treatment of inflammatory diseases. We synthesized 12 novel compounds with 4-amino-N-(4-(benzo[d]oxazol-2-ylamino)phenyl)butanamide moiety and evaluated their biological activities. Among them, 4 compounds (compound 5d, 5c, 5f, 5m and synthetic intermediate 4d) showed potent inhibition activities on IL-1β and IL-6 mRNA expression in vitro. Further, in vivo activity was evaluated with two compounds (5f and 4d) and mRNA levels of IL-1β, IL-6, and TNF-α were significantly decreased without hepatotoxicity. From the in vivo and in vitro test results, we confirmed that our synthesized compounds are effective for suppression of representative inflammatory cytokines. © 2022 by the authors. Licensee MDPI, Basel, Switzerland.
- DOI
- 10.3390/ijms23105331
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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