Effect of Bavachinin and its derivatives on T cell differentiation

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• 作者：Xi Chen^a ; Yanbing Shen^a ; Qikun Liang^a ; Richard Flavell^c ; Zhangyong Hong^b ; Zhinan Yin^b ; Min Wang^a
• 关键词：Bavachinin ; Biotransform ; GATA-3 ; Th2 ; IL-4
• 刊名：International Immunopharmacology
• 出版年：April, 2014
• 年：2014
• 卷：19
• 期：2
• 页码：399-404
• 全文大小：759 K

文摘

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.