Vegetable and Fruit Improvement Center, Department of Horticultural Sciences, Texas A&M University, 1500 Research Parkway, Suite A120, College Station, TX 77843, USA.
Department of Nutrition, Texas A&M University, College Station, TX 77843, USA.
Molecules. 2021 Feb 16;26(4):1038. doi: 10.3390/molecules26041038.
Diabetes mellitus is a chronic disease and one of the fastest-growing health challenges of the last decades. Studies have shown that chronic low-grade inflammation and activation of the innate immune system are intimately involved in type 2 diabetes pathogenesis. L. fruits are used in traditional medicine to manage diabetes. Herein, we report the purification of a new 23--β-d-allopyranosyl-5β,19-epoxycucurbitane-6,24-diene triterpene (charantoside XV, ) along with 25ξ-isopropenylchole-5(6)-ene-3--β-d-glucopyranoside (), karaviloside VI (), karaviloside VIII (), momordicoside L (), momordicoside A () and kuguaglycoside C () from an Indian cultivar of . At 50 µM compounds, - differentially affected the expression of pro-inflammatory markers , , and , and mitochondrial marker . Compounds tested for the inhibition of α-amylase and α-glucosidase enzymes at 0.87 mM and 1.33 mM, respectively. Compounds showed similar α-amylase inhibitory activity than acarbose (0.13 mM) of control (68.0-76.6%). Karaviloside VIII (56.5%) was the most active compound in the α-glucosidase assay, followed by karaviloside VI (40.3%), while momordicoside L (23.7%), A (33.5%), and charantoside XV (23.9%) were the least active compounds. To better understand the mode of binding of cucurbitane-triterpenes to these enzymes, in silico docking of the isolated compounds was evaluated with α-amylase and α-glucosidase.
糖尿病是一种慢性疾病,也是过去几十年增长最快的健康挑战之一。研究表明,慢性低度炎症和先天免疫系统的激活与 2 型糖尿病的发病机制密切相关。苦瓜在传统医学中用于治疗糖尿病。在此,我们报告了一种新的 23--β-d-吡喃阿拉伯糖基-5β,19-环氧葫芦烷-6,24-二烯三萜(苦瓜甙 XV,)以及 25ξ-异丙烯基胆甾-5(6)-烯-3--β-d-吡喃葡萄糖苷()、苦瓜甙 VI()、苦瓜甙 VIII()、苦瓜甙 L()、苦瓜甙 A()和苦瓜甙 C()从印度栽培的苦瓜中分离得到。在 50µM 化合物时,- 差异地影响了促炎标志物、和的表达,以及线粒体标志物。测试了化合物对α-淀粉酶和α-葡萄糖苷酶的抑制作用,抑制率分别为 0.87mM 和 1.33mM。化合物的α-淀粉酶抑制活性与阿卡波糖(0.13mM)相当(68.0-76.6%)。苦瓜甙 VIII(56.5%)在α-葡萄糖苷酶试验中是最活跃的化合物,其次是苦瓜甙 VI(40.3%),而苦瓜甙 L(23.7%)、A(33.5%)和苦瓜甙 XV(23.9%)则是最不活跃的化合物。为了更好地理解葫芦烷三萜与这些酶的结合方式,对分离得到的化合物进行了α-淀粉酶和α-葡萄糖苷酶的计算机对接。