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 (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 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.

中文翻译：

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山毛榉素衍生物作为新型免疫抑制剂的合成及生物学评价

Bergenin 是从Bergenia物种中分离出来的，具有多种药理特性。在寻找新型免疫抑制剂的过程中，设计合成了一系列山毛榉素衍生物，并通过CCK-8法评价了它们的免疫抑制作用。实验数据表明，化合物7和13对小鼠脾细胞增殖的抑制作用最强（IC ₅₀分别为 3.52 和 5.39 μM）。进一步的研究表明，抑制作用可能来自对 IFN-γ 和 IL-4 细胞因子的抑制。具有正己基和正己基的山毛榉素的烷基化衍生物-庚基对两个酚羟基表现出较好的抑制活性。bergenin 衍生物的疏水性、bergenin 中 4-OH 的构型以及C -4 位上的取代基形成氢键的能力对免疫抑制活性很重要。这项工作证明了对bergenin的修饰可能代表了发现一类新的免疫抑制剂的新途径。