Qualisud, University Montpellier, CIRAD, Institut Agro, Avignon Université, University de La Réunion, 34090 Montpellier, France.
Laboratory of Natural Substances and Medicinal Chemistry, Faculty of Sciences, University of Kinshasa, Kinshasa 190 Kinshasa XI, Democratic Republic of the Congo.
Molecules. 2021 Sep 13;26(18):5566. doi: 10.3390/molecules26185566.
Plant bioactive extracts represent a major resource for identifying drugs and adjuvant therapy for type 2 diabetes. To promote early screening of plants' antidiabetic potential, we designed a four in vitro tests strategy to anticipate in vivo bioactivity. Two antidiabetic plants were studied: L. (Oc) leaf extract and R. Br. ex Tedlie (Mu) stem bark extract. Chemical compositions were analyzed by LCMS and HPLC. Antidiabetic properties were measured based on (1) INS-1 cells for insulin secretion, (2) L6 myoblast cells for insulin sensitization (Glut-4 translocation), (3) L6 myoblast cells for protection against hydrogen peroxide (HO) oxidative stress (cell mortality), and (4) liver microsomial fraction for glucose-6-phosphastase activity (G6P). Oc extract increased insulin secretion and insulin sensitivity, whereas it decreased oxidative stress-induced cell mortality and G6P activity. Mu extract decreased insulin secretion and had no effect on insulin sensitivity or G6P activity, but it increased oxidative stress-induced cell mortality. Results were compared with NCRAE, an antidiabetic plant extract used as reference, previously characterized and reported with increased insulin secretion and insulin sensitivity, protection against oxidative stress, and decreased G6P activity. The proposed set of four in vitro tests combined with chemical analysis provided insight into the interest in rapid early screening of plant extract antidiabetic potential to anticipate pharmaco-toxicological in vivo effects.
植物生物活性提取物是发现治疗 2 型糖尿病药物和辅助疗法的主要资源。为了促进对植物抗糖尿病潜力的早期筛选,我们设计了一种四合一的体外测试策略来预测体内生物活性。研究了两种具有抗糖尿病作用的植物:L.(Oc)叶提取物和 R. Br. ex Tedlie(Mu)茎皮提取物。采用 LCMS 和 HPLC 分析化学成分。根据以下四个方面来测量抗糖尿病特性:(1)INS-1 细胞的胰岛素分泌,(2)L6 成肌细胞的胰岛素增敏作用(Glut-4 易位),(3)L6 成肌细胞的抵抗过氧化氢(HO)氧化应激(细胞死亡率),以及(4)肝微粒体部分的葡萄糖-6-磷酸酶活性(G6P)。Oc 提取物可增加胰岛素分泌和胰岛素敏感性,同时降低氧化应激诱导的细胞死亡率和 G6P 活性。Mu 提取物可降低胰岛素分泌,对胰岛素敏感性或 G6P 活性没有影响,但可增加氧化应激诱导的细胞死亡率。结果与 NCRAE 进行了比较,NCRAE 是一种抗糖尿病植物提取物,具有增加胰岛素分泌和胰岛素敏感性、保护氧化应激和降低 G6P 活性的特点,已被先前描述和报道。本研究提出的四合一体外测试组合与化学分析相结合,深入了解了快速早期筛选植物提取物抗糖尿病潜力的兴趣,以预测体内药代毒性作用。