biostudies-literatureDeng LNational Natural Science Foundation of ChinaNational Key Research and Development Program of China1968-1976https://www.ebi.ac.uk/biostudies/studies/S-EPMC8597419biostudies-literatureUnknown12(11)Bergenin, which is isolated from <i>Bergenia</i> 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 <b>7</b> and <b>13</b> showed the strongest inhibition effects on mouse splenocyte proliferation (IC₅₀ = 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 <i>n</i>-hexyl and <i>n</i>-heptyl on the two phenolic hydroxyl groups showed better inhibitory activities. The hydrophobicity of bergenin derivatives, the cRSC medicinal chemistrySynthesis and biological evaluation of bergenin derivatives as new immunosuppressants.PMC85974192018YFA0507602918531222197700481821004Wang MWu YFSong CDeng LLi QYe XSNiu YfalseSynthesis and biological evaluation of bergenin derivatives as new immunosuppressants.Bergenin, which is isolated from <i>Bergenia</i> 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 <b>7</b> and <b>13</b> showed the strongest inhibition effects on mouse splenocyte proliferation (IC₅₀ = 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 <i>n</i>-hexyl and <i>n</i>-heptyl on the two phenolic hydroxyl groups showed better inhibitory activities. The hydrophobicity of bergenin derivatives, the c2021-01-01T00:00:00Z2021 Nov2025-04-22T09:59:44.853Z2025-04-05T23:24:08.777ZS-EPMC85974193482519210.1039/d1md00210d