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The Conjugated Double Bond of Coniferyl Aldehyde Is Essential for Heat Shock Factor 1 Mediated Cytotoprotection
Journal of Natural Products ( IF 5.1 ) Pub Date : 2017-07-24 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00126 Seul-Ki Choi 1 , Gil-Im Mun 1 , Eun Choi 1 , Seo-Young Kim 1 , Youngjoo Kwon 1 , Younghwa Na 2 , Yun-Sil Lee 1
Journal of Natural Products ( IF 5.1 ) Pub Date : 2017-07-24 00:00:00 , DOI: 10.1021/acs.jnatprod.7b00126 Seul-Ki Choi 1 , Gil-Im Mun 1 , Eun Choi 1 , Seo-Young Kim 1 , Youngjoo Kwon 1 , Younghwa Na 2 , Yun-Sil Lee 1
Affiliation
Coniferyl aldehyde (1) is previously reported as a potent inducer of heat shock factor 1 (HSF1). Here, we further examined the active pharmacophore of 1 for activation of HSF1 using the derivatives coniferyl alcohol (2), 4-hydroxy-3-methoxyphenylpropanal (3), and 4-hydroxy-3-methoxyphenylpropanol (4). Both 1 and 2 resulted in increased survival days after a lethal radiation (IR) dose. The decrease in bone marrow (BM) cellularity and Ki67-positive BM cells by IR was also significantly restored by 1 or 2 in mice. These results suggested that the vinyl moiety of 1 and 2 is necessary for inducing HSF1, which may be useful for developing small molecules for cytoprotection of normal cells against damage by cytotoxic drugs and radiation.
中文翻译:
针叶树醛共轭双键对于热休克因子1介导的细胞保护至关重要
松柏基醛(1)以前被报道为热休克因子1(HSF1)的有效诱导剂。在这里,我们进一步研究的活性药效1使用衍生物松柏醇(HSF1激活2),4-羟基-3- methoxyphenylpropanal(3)和4-羟基-3- methoxyphenylpropanol(4)。既1和2导致增加的存活天数致死辐射(IR)剂量后。在小鼠中,IR引起的骨髓(BM)细胞数量和Ki67阳性BM细胞减少也明显恢复了1或2。这些结果表明1和2的乙烯基部分 诱导HSF1是必需的,HSF1可能用于开发小分子,以保护正常细胞免受细胞毒性药物和放射线的损害。
更新日期:2017-07-24
中文翻译:
针叶树醛共轭双键对于热休克因子1介导的细胞保护至关重要
松柏基醛(1)以前被报道为热休克因子1(HSF1)的有效诱导剂。在这里,我们进一步研究的活性药效1使用衍生物松柏醇(HSF1激活2),4-羟基-3- methoxyphenylpropanal(3)和4-羟基-3- methoxyphenylpropanol(4)。既1和2导致增加的存活天数致死辐射(IR)剂量后。在小鼠中,IR引起的骨髓(BM)细胞数量和Ki67阳性BM细胞减少也明显恢复了1或2。这些结果表明1和2的乙烯基部分 诱导HSF1是必需的,HSF1可能用于开发小分子,以保护正常细胞免受细胞毒性药物和放射线的损害。