真菌来源新活性化合物2460A的研究

齐小强  朱凤昌  张 洋  郭连宏  姜 蓉  何琪杨  李 元

真菌来源新活性化合物2460A的研究

齐小强朱凤昌张洋郭连宏姜蓉何琪杨李元

Study of a novel compound 2460A with activities produced by fungus

JI Xiao-Jiang

摘要

摘要:
采用自行构建的以重组白细胞介素6受体 (IL-6R) 为靶位, 基于受体配基竞争结合为基础的高通量筛选模型, 从微生物代谢产物中获得了新结构化合物2460A。本文通过对产生菌核糖体DNA转录间隔区 (rDNA-ITS) 序列测定结果, 确定了该化合物产生菌为哈茨木霉; 研究结果显示, 2460A具有和白细胞介素6 (IL-6) 竞争结合白细胞介素6受体 (IL-6R) 的活性, 因此是具有IL-6R配基活性的微生物产物; MTT法测定结果表明, 2460A对CM126和HT-29肿瘤细胞具有抑制作用, IC₅₀分别为2.17×10⁻⁵ mol?L⁻¹和1.8×10⁻⁵ mol?L⁻¹; 对肿瘤细胞周期影响作用实验结果显示, 2460A对HT-29细胞的S期略有阻滞作用。本化合物体内抗瘤活性等深入研究工作正在进行中。

Abstract:
With IL-6R as target, a new compound 2460A was identified from fungus using HTS screening model. The taxonomics of the produced strain was confirmed to be Trichoderma hazianum rifai after sequencing analysis of rDNA-ITS (internal transcribed spacer). Results showed that this compound has a binding activity on IL-6R competed with IL-6, thus it is a new ligand of IL-6R originating from microbe. With MTT assay, the anti-tumor activities of 2460A were demonstrated on CM126 and HT-29 cell lines separately, the IC₅₀ are 2.17×10⁻⁵ mol?L⁻¹ and 1.8×10⁻⁵ mol?L⁻¹ respectively. The compound affected lightly the HT-29 cell cycle at S phase. Studies for the anti-tumor activity of 2460A in vivo are in progress in our lab.

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