College of Pharmacy, Drug Research and Development Center, Daegu Catholic University.
Division of Computational Physics, Institute for Computational Science, Ton Duc Thang University.
Biol Pharm Bull. 2021 Mar 1;44(3):298-304. doi: 10.1248/bpb.b20-00994. Epub 2020 Dec 23.
The white-flowered leaves of Eclipta prostrata L. together with leaves of Scoparia dulcis and Cynodon dactylon are mixedly boiled in water and given to diabetic patients resulting in the significant improvement in the management of diabetes. However, the active constituents from this plant for antidiabetic and anti-obesity properties are remaining unclear. Thus, this study was to discover anti-diabetes and anti-obesity activities through protein tyrosine phosphatases (PTP)1B inhibitory effects. We found that the fatty acids (23, 24) showed potent PTP1B inhibition with IC values of 2.14 and 3.21 µM, respectively. Triterpenoid-glycosides (12-15) also exhibited strong to moderate PTP1B inhibitory effects, with IC values ranging from 10.88 to 53.35 µM. Additionally, active compounds were investigated for their PTP1B inhibitory mechanism and docking analysis. On the other hand, the anti-inflammatory activity from our study revealed that compounds (1-4, 7, 8, 10) displayed the significant inhibition nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Especially, compound 9 showed the potent inhibitory effects in LPS-induced NO production on RAW264.7 cell. Therefore, further Western blot analysis was performed to identify the inhibitory expression including heme oxygenase-1 (HO-1) and inhibitor of kappaB (IκB) phosphorylation.
白花蛇舌草与地胆草和狗尾草的叶片混合在水中煮沸，给糖尿病患者服用，可显著改善糖尿病的治疗效果。然而，这种植物用于抗糖尿病和抗肥胖的活性成分仍不清楚。因此，本研究旨在通过蛋白酪氨酸磷酸酶（PTP）1B 抑制作用来发现抗糖尿病和抗肥胖活性。我们发现，脂肪酸（23,24）对 PTP1B 表现出很强的抑制作用，IC 值分别为 2.14 和 3.21μM。三萜糖苷（12-15）也表现出较强至中等强度的 PTP1B 抑制作用，IC 值范围为 10.88 至 53.35μM。此外，还对活性化合物进行了 PTP1B 抑制机制和对接分析的研究。另一方面，我们的研究表明，化合物（1-4、7、8、10）具有抗炎活性，可显著抑制脂多糖（LPS）刺激的 RAW264.7 细胞中一氧化氮（NO）的产生。特别是化合物 9 对 LPS 诱导的 RAW264.7 细胞中 NO 产生具有很强的抑制作用。因此，进一步进行了 Western blot 分析，以鉴定包括血红素加氧酶-1（HO-1）和κB 抑制蛋白（IκB）磷酸化在内的抑制表达。
