T-2四醇和T-2五醇的制备

Synthesis of T 2 tetraol and T 2 pentaol

目的：进一步探讨Ｔ－２毒素与其结构效应的关系，制备Ｔ－２毒素的两个衍生物：Ｔ－２四醇和Ｔ－２五醇。方法：通过Ｔ－２毒素在恒温条件下水解、柱层析纯化得到Ｔ－２四醇；使Ｔ－２毒素经四氢铝锂还原、再经薄层层析纯化得到Ｔ－２五醇。结果：经细胞和动物毒性试验表明，Ｔ－２四醇仍有一定毒性作用，但其作用强度仅为Ｔ－２毒素的１％；当母核中环氧环被打开时，毒素的毒性发生明显的改变。

Objective: To synthesize two derivatives of T 2 toxin, T 2 tetraol and T 2 pentaol, in order to study the structure activity relationship of T 2 toxin. Methods: T 2 tetraol was synthesized by way of hydrolysis of T 2 toxin under constant temperature, and purified by elution on silica gel column, while T 2 pentaol was synthesized by way of reduction of T 2 toxin with LiAlH 4, and purified by thin layer chromatography. Results: Cytotoxicity tests and animal experiments showed that T 2 tetraol has a toxicity of only 1/100 strength as that of T 2 toxin . If the epoxy group of the parent nucleus was opened, its toxicity was greatly reduced further. Conclusion: The epoxy structure is the determinant group of the toxicity of these toxins.