Antidiabetic Activities and GC-MS Analysis of 4-Methoxychalcone

Leonard D. R. Acho, E. S. Oliveira, Simone B Carneiro, Fernanda Paula A. Melo, Leilane de S. Mendonça, Renyer A. Costa, Rosivaldo S. Borges, M. Machado, Hector Koolen, Igor Rafael dos S. Magalhães, Emersom S. Lima
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Abstract

Diabetes mellitus is a chronic metabolic disease that is mainly characterized by hyperglycemia. Chalcones and their derivatives have demonstrated promising pharmacological potential for the treatment of diabetes. The aim of the study was to evaluate antidiabetic activities and analyze 4-methoxychalcone (MPP) using GC-MS. The compound was characterized using mass spectroscopy, nuclear magnetic resonance and headspace with gas chromatography coupled to mass spectrometry (HS-GC-MS). MPP was evaluated via the inhibition of the alpha-glucosidase enzyme, cell viability and antiglycation and hemolytic activities in vitro. The study of the interaction between the bovine serum albumin protein and MPP was investigated via molecular docking. Oral sucrose tolerance and oral glucose tolerance tests were performed in streptozotocin (STZ)-induced diabetic mice. The HS-GC-MS method was able to accurately detect and characterize the compound, and the interaction between MPP and BSA revealed the remarkable affinity for the two main binding sites of BSA. This was confirmed by the in vitro antiglycation test, since MPP showed activity through both oxidative and non-oxidative stress. MPP significantly attenuated the increase in glycemia after glucose loading in STZ-induced diabetic mice. These results confirm that MPP has antihyperglycemic activity and may be an alternative for the treatment of diabetes mellitus.
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4-Methoxychalcone 的抗糖尿病活性和 GC-MS 分析
糖尿病是一种以高血糖为主要特征的慢性代谢疾病。查耳酮及其衍生物在治疗糖尿病方面具有良好的药理潜力。本研究旨在评估 4-甲氧基查尔酮(MPP)的抗糖尿病活性,并利用气相色谱-质谱法对其进行分析。采用质谱、核磁共振和顶空气相色谱耦合质谱法(HS-GC-MS)对该化合物进行了表征。通过抑制体外α-葡萄糖苷酶、细胞活力、抗糖化和溶血活性对 MPP 进行了评估。通过分子对接研究了牛血清白蛋白与 MPP 之间的相互作用。对链脲佐菌素(STZ)诱导的糖尿病小鼠进行了口服蔗糖耐量和口服葡萄糖耐量试验。HS-GC-MS 方法能够准确地检测和表征该化合物,而 MPP 与 BSA 的相互作用表明,该化合物与 BSA 的两个主要结合位点具有显著的亲和力。体外抗糖化试验证实了这一点,因为 MPP 在氧化和非氧化压力下都显示出活性。在 STZ 诱导的糖尿病小鼠体内,MPP 能明显降低葡萄糖负荷后血糖的升高。这些结果证实,MPP 具有降血糖活性,可作为治疗糖尿病的替代药物。
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