首页> 外文期刊>Open Journal of Medicinal Chemistry >Triphenylmethanol Conjugates of Triptorelin as Anti-Lipid Peroxidation Prodrugs
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Triphenylmethanol Conjugates of Triptorelin as Anti-Lipid Peroxidation Prodrugs

机译:三苯甲醇结合曲普瑞林作为抗脂质过氧化的前药。

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Antioxidants are substances that can prevent or slow damage to cells caused by free radicals, unstable molecules that the body produces as a reaction to environmental and other pressures. Free radicals may play a role in heart disease, cancer and other diseases. If the body cannot process and remove free radicals efficiently, oxidative stress can result. This can harm cells and body function. Free radicals are also known as reactive oxygen species (ROS). In this research, Triptorelin ~(®) (TRP) conjugates of triphenylmethanol derivatives (TPMs) were synthesized to evaluate their in vitro lipid peroxidation potency. Comparative lipid peroxidation assays between TRP-TPMs conjugates and the corresponding TPMs derivatives were measured using thiobarbituric reactive substance (TBARS) in a dose- and time-dependent manner following the Fenton’s pathway. Overall, TBARS decreased between 20% - 30% for the treated samples of synthesized conjugates compared to their respective control physical mixtures. These data suggest that TRP-TPMs derivatives can be used to improve the biological activity of TRP.
机译:抗氧化剂是可以预防或减缓自由基,机体由于对环境和其他压力的反应而产生的不稳定分子而对细胞造成损害的物质。自由基可能在心脏病,癌症和其他疾病中起作用。如果人体无法有效地处理和清除自由基,则会导致氧化应激。这会损害细胞和身体功能。自由基也被称为活性氧(ROS)。在这项研究中,三苯甲醇衍生物(TPM)的曲普瑞林〜(®)(TRP)共轭物被合成以评估其体外脂质过氧化能力。按照Fenton途径,使用硫代巴比妥反应性物质(TBARS)以剂量和时间依赖的方式,对TRP-TPMs缀合物和相应的TPMs衍生物之间的脂质过氧化进行比较。总体而言,与它们各自的对照物理混合物相比,处理后的合成缀合物样品的TBARS降低了20%-30%。这些数据表明,TRP-TPMs衍生物可用于改善TRP的生物活性。

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