| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2540855 | International Immunopharmacology | 2014 | 6 Pages |
•Bavachinin inhibits the production of Th2 cytokines by using 4GET mice CD4 + cells.•Bavachinin inhibits the differentiation of Th2 but does not influence the Th1.•Compound B inhibits the production of IL-4 and inhibits the Th2 differentiation.•Compound B inhibits the Th2 by increasing the Th1 differentiation.
Bavachinin, which can be isolated from the Chinese herb Fructus Psoraleae, has the potential as a potent anti-asthma drug. However, the extremely low water solubility of Bavachinin limits its application. In this study, two new derivatives of Bavachinin, i.e., compounds A and B, whose water solubility is better than that of Bavachinin, were synthesized via biotransformation. A comparative investigation was then performed on the effects of these two new derivatives, along with Bavachinin, on T cell differentiation. The results showed that they have different effects. Bavachinin and compound B inhibited green fluorescent protein (GFP) production from the T cells of IL-4-GFP-enhanced transcript (4GET) mice, whereas compound A did not. The effect was mainly attributed to the inhibition of GATA-3 protein production. Bavachinin and compound B can inhibit the production of GATA-3 mRNA, but they showed different effects on the production of T-bet mRNA. Compound B increased the production of T-bet mRNA, whereas Bavachinin did not. The results will be very useful for optimizing Bavachinin so that potent anti-allergic drugs can be developed.The structure–activity relationship of Th2 was revealed based on the difference between Bavachinin and compound B. This finding can enrich the database of preliminary drug screening from their chemical structures.
