College of Pharmacy, Drug Research and Development Center, Daegu Catholic University, Gyeongsan, 38430, Republic of Korea.
Faculty of Medicine and Pharmacy, Thanh Dong University, Hai Duong city, Vietnam.
Arch Pharm Res. 2020 Feb;43(2):204-213. doi: 10.1007/s12272-020-01211-8. Epub 2020 Jan 21.
Kadsura coccinea (Lem.) A. C. Smith has been used as a tonic, decongestant, and digestive agent. The roots are also employed in traditional medicine to treat chronic enteritis, acute gastritis, duodenal ulcers, rheumatic pain in bone, and traumatic injuries. In the present study, we have described the biological evaluation of constituents from the roots of K. coccinea with PTP1B and AChE inhibitory activities for the first time in literature. A new compound (1), kadcoccilactone T, and 24 known ones (2‒25) were isolated and identified using spectroscopic methods. All the isolates were examined for PTP1B and AChE inhibitory activities. Compounds 4 and 8 expressed strong PTP1B inhibition with IC values of 1.57 ± 0.11 and 3.99 ± 1.08 μM, respectively. Apparently, these compounds were further studied for PTP1B enzyme kinetic analysis. The result indicated that compounds 4 and 8 exhibited mixed-type inhibition with the Κ values of 4.97 and 3.26 µM, respectively.
红毛藤（Kadsura coccinea）（Lem.）A. C. Smith 被用作滋补品、解充血剂和消化剂。其根部也被用于传统医学中，用于治疗慢性肠炎、急性胃炎、十二指肠溃疡、骨风湿痛和创伤损伤。在本研究中，我们首次描述了来自红毛藤根部的成分的生物评估，这些成分具有 PTP1B 和 AChE 抑制活性。使用光谱方法分离和鉴定了一种新化合物（1），kadcoccilactone T 和 24 种已知化合物（2-25）。所有分离物均进行了 PTP1B 和 AChE 抑制活性测试。化合物 4 和 8 表现出强烈的 PTP1B 抑制活性，IC 值分别为 1.57 ± 0.11 和 3.99 ± 1.08 μM。显然，这些化合物进一步进行了 PTP1B 酶动力学分析。结果表明，化合物 4 和 8 表现出混合抑制，Κ 值分别为 4.97 和 3.26 μM。
