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自然化合物图书馆查确定了用于治疗酸诱导的肠道功能障碍的托利德

Ji-Qian-Zhu Zhang¹, Xiao-Yu Dai¹, Jing-Jing Mao¹

¹Department of Health Toxicology, Faculty of Naval Medicine, Second Military Medical University, 800 Xiangyin Road, Shanghai 200433, China.

Ecotoxicology and environmental safety

|September 18, 2025

概括

特里普托利德通过减少肠道损伤和抑制内分泌网膜应激作用,防止腹性贝类毒素 (奥卡迪酸) 毒害. 这种天然化合物显示出作为治疗奥卡迪酸毒性的治疗剂的潜力.

科学领域:

毒理学毒理学毒理学
药理学药理学是指药理学的学科.
细胞生物学细胞生物学

背景情况:

酸 (OA) 是一种引起腹的贝类毒素,引起显著的肠道和全身毒性.
目前没有批准的治疗药物针对OA诱导的腹.
高通量选是一种有价值的方法,用于识别潜在的治疗化合物.

研究的目的:

识别天然化合物,可以防止Okadaic酸诱导的亡.
调查三托利德在减轻OA毒性的治疗潜力.

主要方法:

2131种天然化合物的高通量选.
向暴露于OA的小鼠和HUVECs (人类静脉内皮细胞) 施用托利德.
评估肠道透性,粘膜损伤,细胞活力和亡活性.
基于生物素的标签,以识别三胺的活性部位.
RNA测序以分析与内质网膜 (ER) 压力相关的基因表达变化.

主要成果:

特里普托利德被确定为一种保护性化合物,可以防止OA诱导的亡.
在小鼠中,托利降低了肠道透性和粘膜损伤.
三托利德增加了HUVEC活力,并以剂量依赖的方式抑制了亡.
鉴定出三酸的基是必需活性部位.
托利德抑制了OA诱导的ER蛋白合成基因上调,并通过防止p-eIF-2α/eIF-2α比率下降来减轻了ER压力.

结论:

特里普托利德通过抑制ER压力介导的内皮细胞亡来减轻OA诱导的毒性.
ptolide 保持了肠道屏障的完整性,这表明它有可能成为OA中毒的治疗剂.

关键词:

细胞灭亡 (apoptosis) 是一种死亡的过程.细胞内膜网膜应激压力肠道功能障碍肠道功能障碍自然化合物图书馆自然化合物图书馆奥卡迪酸是什么意思? 奥卡迪酸是什么意思三托利化物是什么

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