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Synthesis and biological evaluation of bergenin derivatives as new immunosuppressants.
- Source :
-
RSC medicinal chemistry [RSC Med Chem] 2021 Aug 24; Vol. 12 (11), pp. 1968-1976. Date of Electronic Publication: 2021 Aug 24 (Print Publication: 2021). - Publication Year :
- 2021
-
Abstract
- Bergenin, which is isolated from Bergenia species, exhibits various pharmacological properties. In the search for new types of immunosuppressants, a series of bergenin derivatives were designed and synthesized, and their immunosuppressive effects were evaluated by the CCK-8 assay. The experimental data demonstrated that compounds 7 and 13 showed the strongest inhibition effects on mouse splenocyte proliferation (IC <subscript>50</subscript> = 3.52 and 5.39 μM, respectively). Further studies revealed that the inhibitory effect may come from the suppression of both IFN-γ and IL-4 cytokines. Alkylated derivatives of bergenin with n -hexyl and n -heptyl on the two phenolic hydroxyl groups showed better inhibitory activities. The hydrophobicity of bergenin derivatives, the configuration of the 4-OH in bergenin, and the ability to form hydrogen bonds of the substituents on the C -4 position are important to the immunosuppressive activity. This work proved that the modifications of bergenin may represent a new route to the discovery of a new class of immunosuppressive agents.<br />Competing Interests: The authors declare no competing financial interest.<br /> (This journal is © The Royal Society of Chemistry.)
Details
- Language :
- English
- ISSN :
- 2632-8682
- Volume :
- 12
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- RSC medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 34825192
- Full Text :
- https://doi.org/10.1039/d1md00210d