Hwang Hoseong, Lee Dahae, Son Jong Dai, Baek Jong Gwon, Lee Hyeon-Seong, Park InWha, Kim Dong Hoon, Lee Soon Kwang, Kim Won Kyu, Kwon Hak Cheol, Kang Ki Sung, Kwon Jaeyoung
KIST Gangneung Institute of Natural Products, Korea Institute of Science and Technology, Gangneung 25451, Republic of Korea.
College of Korean Medicine, Gachon University, Seongnam 13120, Republic of Korea.
Bioorg Chem. 2023 May;134:106466. doi: 10.1016/j.bioorg.2023.106466. Epub 2023 Mar 12.
Actinidia polygama has been used as a traditional medicine for treating various diseases. In the present study, 13 compounds, including three new monoterpenoids (1-3), were isolated from the leaves of A. polygama to investigate the bioactive constituents of the plant. The structures were characterized by analyzing spectroscopic and chiroptical data. These compounds were preliminarily screened for their ability to increase insulin secretion levels after glucose stimulation. Of these, 3-O-coumaroylmaslinic acid (4) and jacoumaric acid (5) showed activity. In further biological studies, these compounds exhibited increased glucose-stimulated insulin secretion (GSIS) activity without cytotoxicity in rat INS-1 pancreatic β-cells as well as α-glucosidase inhibitory activity. Furthermore, both compounds increased insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), protein kinase B (Akt), pancreatic and duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) expression. Hence, these compounds may be developed as potential antidiabetic agents.
软枣猕猴桃已被用作治疗各种疾病的传统药物。在本研究中，从软枣猕猴桃叶中分离出13种化合物，包括三种新的单萜类化合物（1-3），以研究该植物的生物活性成分。通过分析光谱和旋光数据对这些化合物的结构进行了表征。对这些化合物在葡萄糖刺激后增加胰岛素分泌水平的能力进行了初步筛选。其中，3-O-香豆酰山楂酸（4）和紫丁香酸（5）表现出活性。在进一步的生物学研究中，这些化合物在大鼠INS-1胰腺β细胞中表现出增加的葡萄糖刺激胰岛素分泌（GSIS）活性且无细胞毒性，以及α-葡萄糖苷酶抑制活性。此外，这两种化合物均增加了胰岛素受体底物-2（IRS-2）、磷脂酰肌醇3激酶（PI3K）、蛋白激酶B（Akt）、胰腺和十二指肠同源盒-1（PDX-1）以及过氧化物酶体增殖物激活受体-γ（PPAR-γ）的表达。因此，这些化合物可能被开发为潜在的抗糖尿病药物。
