Wang Sa, He Hai-bo, Xiao Shu-zhang, Wang Jun-zhi, Bai Cai-hong, Wei Na, Zou Kun
Hubei Key Laboratory of Natural Products Research and Development, College of Chemistry and Life Science, China Three Gorges University, Yichang, Hubei, China.
Medical College of China Three Gorges University, Yichang, Hubei, China.
Pharmacol Rep. 2014 Aug;66(4):677-85. doi: 10.1016/j.pharep.2014.03.014. Epub 2014 Apr 16.
It is well known that fluorescent labeling has recently become a major research tool in molecular and cellular biology for demonstrating therapeutic mechanisms and metabolic pathways. However, few studies have reported the use of fluorescent labeling of natural products.
We recently explored the boron 2-(2'-pyridyl) imidazole (BOPIM) derivative analogs, which are highly fluorescent, non-aggregated, and nontoxic. In the present study, the natural product oleanolic acid (OA) was functionalized and labeled with BOPIM, thus yielding a highly fluorescent probe, the comparison of cardioprotective effects of labeled and unlabeled OAs with BOPIM on primary neonatal rat cardiomyocytes with hypoxia/reoxygenation (H/R) injury were investigated.
Pretreatment with OA and BOPIM-OA significantly prevented the H/R induced cell death in primary neonatal rat cardiomyocytes. However, BOPIM exhibited no improvements on the H/R injury cardiomyocytes, and which were similar to those of the H/R group. The results of comparison of cardioprotective effects between labeled and unlabeled OAs with BOPIM showed that introducing the BOPIM chromophore did not make a difference with H/R injury cardiomyocytes.
BOPIM chromophore is a suitable probe for investigating the pharmacological mechanisms of natural products.
众所周知,荧光标记最近已成为分子和细胞生物学中用于证明治疗机制和代谢途径的主要研究工具。然而,很少有研究报道天然产物的荧光标记应用。
我们最近探索了硼2-(2'-吡啶基)咪唑(BOPIM)衍生物类似物,它们具有高荧光性、不聚集且无毒。在本研究中,天然产物齐墩果酸(OA)被功能化并用BOPIM标记,从而产生一种高荧光探针,研究了标记和未标记的含BOPIM的OA对原代新生大鼠心肌细胞缺氧/复氧(H/R)损伤的心脏保护作用并进行比较。
用OA和BOPIM-OA预处理可显著预防原代新生大鼠心肌细胞中H/R诱导的细胞死亡。然而,BOPIM对H/R损伤的心肌细胞没有改善作用,且与H/R组相似。含BOPIM的标记和未标记OA之间心脏保护作用的比较结果表明,引入BOPIM发色团对H/R损伤的心肌细胞没有影响。
BOPIM发色团是研究天然产物药理机制的合适探针。