Chocó(哥伦比亚)治疗2型糖尿病和肥胖症常用药用植物对α-葡萄糖苷酶、α-淀粉酶和胰脂肪酶的体外抑制活性

IF 2.3 Q3 PHARMACOLOGY & PHARMACY
Kevin P. Lévuok-Mena, Oscar J. Patiño-Ladino, Juliet A. Prieto-Rodríguez
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引用次数: 0

摘要

植物性疗法被广泛用于治疗全球约80%人口的疾病,包括哥伦比亚的Chocó部门。本研究旨在鉴定和评价Chocó中对肥胖和糖尿病具有显著治疗价值的植物。评估了这些植物对胰脂肪酶(PL)、α-葡萄糖苷酶(AG)和α-淀粉酶(AA)的抑制作用,并选择了最有希望分离和鉴定生物活性成分的物种。根据其在Chocó种群中的传统使用情况,高山竹、苦瓜、紫荆花、叶神经草和巨叶蜜豆被认为是关键种。其中,巨叶粘菌提取物对AG、AA和PL的IC50值分别为0.99±0.21、5.61±0.82和28.91±2.10 μg/mL,具有较好的消化酶抑制作用。进一步的化学分析分离出三种生物活性化合物:5 ' -去甲氧基cadensin g1、对羟基苯甲酸甲酯2和对羟基苯甲酸丁酯3。化合物1抗AG活性最高(IC50 = 164.30±0.11 μM);化合物2 (IC50 = 28.50±4.07 μM)和化合物3 (IC50 = 10.15±3.42 μM)对PL具有较强的抑制作用。分子配对和酶动力学研究表明,这些生物活性化合物主要是AG的混合抑制剂和PL的非竞争性抑制剂。这些研究结果表明,大叶假单胞菌及其化合物可能是肥胖和2型糖尿病相关消化酶的有效抑制剂。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In Vitro Inhibitory Activities against α-Glucosidase, α-Amylase, and Pancreatic Lipase of Medicinal Plants Commonly Used in Chocó (Colombia) for Type 2 Diabetes and Obesity Treatment
Plant-based therapies are widely utilized for treating diseases in approximately 80% of the global population, including Colombia’s Chocó Department. This study aimed to identify and evaluate plants with significant therapeutic value for obesity and diabetes in Chocó. The inhibitory effects of these plants on pancreatic lipase (PL), α-glucosidase (AG), and α-amylase (AA) were assessed, and the most promising species were selected to isolate and identify bioactive components. Artocarpus altilis, Momordica balsamina, Bauhinia picta, Neurolaena lobata, and Vismia macrophylla emerged as key species based on their traditional usage among the Chocó population. Notably, the extract derived from Vismia macrophylla demonstrated the most encouraging outcomes as a digestive enzyme inhibitor, exhibiting IC50 values of 0.99 ± 0.21 μg/mL, 5.61 ± 0.82 mg/mL, and 28.91 ± 2.10 μg/mL for AG, AA, and PL, respectively. Further chemical analysis led to the isolation of three bioactive compounds: 5′-demethoxycadensin G 1, para-hydroxybenzoic acid methyl ester 2, and para-hydroxybenzoic acid butyl ester 3. Compound 1 displayed the highest activity against AG (IC50 = 164.30 ± 0.11 μM), while compounds 2 (IC50 = 28.50 ± 4.07 μM) and 3 (IC50 = 10.15 ± 3.42 μM) exhibited potent inhibitory effects on PL. Molecular docking and enzymatic kinetics studies indicate that these bioactive compounds primarily act as mixed inhibitors of AG and non-competitive inhibitors of PL. These findings underscore the potential of V. macrophylla and its compounds as effective inhibitors of digestive enzymes associated with obesity and type 2 diabetes.
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来源期刊
Scientia Pharmaceutica
Scientia Pharmaceutica Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
4.60
自引率
4.00%
发文量
67
审稿时长
10 weeks
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