Vegetable and Fruit Improvement Center, Department of Horticultural Sciences, Texas A&M University, 1500 Research Parkway, Suite A120, College Station, TX 77845, USA.
Department of Poultry Science, Texas A&M University, College Station, TX 77845, USA.
Bioorg Med Chem. 2019 Jul 15;27(14):3097-3109. doi: 10.1016/j.bmc.2019.05.035. Epub 2019 May 23.
Bitter melon (Momordica charantia) has been used to manage diabetes and related conditions in various parts of the world. In the present study, ten compounds were isolated from acetone and methanol extracts of bitter melon. The chemical structures of compounds were unambiguously elucidated by 1D, 2D NMR, and high-resolution mass spectra. Identified compounds 1-7 exhibited significant inhibition of α-amylase and moderate inhibition of α-glucosidase activities. Momordicoside G and gentisic acid 5-O-β-d-xyloside showed the highest inhibition of α-amylase (70.5%), and α-glucosidase (56.4%), respectively. Furthermore, molecular docking studies of isolated compounds 1-7 were able to bind to the active sites of both enzymes. Additionally, the isolated compounds 1-7 significantly attenuated lipopolysaccharide (LPS)-induced inflammation, downregulating the expression of pro-inflammatory markers NF-κB, INOS, IL-6, IL-1β, TNF-α, and Cox-2 in murine macrophage RAW 264.7 cells. One phenolic derivative, gentisic acid 5-O-β-d-xyloside, was isolated and identified for the first time from bitter melon, and significantly suppressed the expression of Cox-2 and IL-6 compared to the LPS-treated group. α-Amylase and α-glucosidase are targets of anti-diabetes drugs, our findings suggest that compounds purified from bitter melon may have potential to use as functional food ingredients for the prevention of type 2 diabetes and related inflammatory conditions.
苦瓜（Momordica charantia）已被用于世界各地管理糖尿病和相关病症。在本研究中，从苦瓜的丙酮和甲醇提取物中分离出了 10 种化合物。通过 1D、2D NMR 和高分辨率质谱明确了化合物的化学结构。鉴定出的化合物 1-7 对α-淀粉酶具有显著的抑制作用，对α-葡萄糖苷酶也具有中等抑制作用。苦瓜苷 G 和龙胆酸 5-O-β-D-吡喃木糖苷对α-淀粉酶（70.5%）和α-葡萄糖苷酶（56.4%）的抑制作用最强。此外，对分离出的化合物 1-7 的分子对接研究表明，它们能够与两种酶的活性部位结合。此外，分离出的化合物 1-7 可显著减轻脂多糖（LPS）诱导的炎症，下调鼠巨噬细胞 RAW 264.7 细胞中促炎标志物 NF-κB、INOS、IL-6、IL-1β、TNF-α和 Cox-2 的表达。一种酚类衍生物，龙胆酸 5-O-β-D-吡喃木糖苷，首次从苦瓜中分离鉴定，与 LPS 处理组相比，它对 Cox-2 和 IL-6 的表达有显著的抑制作用。α-淀粉酶和α-葡萄糖苷酶是抗糖尿病药物的靶点，我们的研究结果表明，从苦瓜中纯化的化合物可能有潜力作为功能性食品成分，用于预防 2 型糖尿病和相关炎症。
