Sa Wang1, Hai-bo He2, Shu-zhang Xiao1, Jun-zhi Wang1, Cai-hong Bai1, Na Wei3, Kun Zou4. 1. Hubei Key Laboratory of Natural Products Research and Development, College of Chemistry and Life Science, China Three Gorges University, Yichang, Hubei, China. 2. Medical College of China Three Gorges University, Yichang, Hubei, China. Electronic address: haibohe2001@gmail.com. 3. Medical College of China Three Gorges University, Yichang, Hubei, China. 4. Hubei Key Laboratory of Natural Products Research and Development, College of Chemistry and Life Science, China Three Gorges University, Yichang, Hubei, China. Electronic address: kzou@ctgu.edu.cn.
Abstract
BACKGROUND: 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. METHODS: 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. RESULTS: 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. CONCLUSION: BOPIM chromophore is a suitable probe for investigating the pharmacological mechanisms of natural products.
BACKGROUND: 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. METHODS: 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. RESULTS: 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. CONCLUSION:BOPIM chromophore is a suitable probe for investigating the pharmacological mechanisms of natural products.