Glucose Uptake Stimulatory and PTP1B Inhibitory Activities of Pimarane Diterpenes from Orthosiphon stamineus Benth
Glucose Uptake Stimulatory and PTP1B Inhibitory Activities of Pimarane Diterpenes from Orthosiphon stamineus Benth
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DOI：
10.3390/biom9120859
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发表时间：
2019-12-01
期刊：
影响因子：
5.5
通讯作者：
Dao Cuong To
中科院分区：
文献类型：
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作者：
Phi Hung Nguyen;Huynh Nhu Tuan;Dao Cuong To
从 Orthosiphon stamineus Benth 中分离得到 7 个海螺烷二萜 (1-7)。通过测定引导的分离。所有分离株在浓度为 5 和 10 μM 时均对 3T3-L1 脂肪细胞具有 2-脱氧-2-((7-硝基-2,1,3-苯并恶二唑-4-基)氨基)-d-葡萄糖摄取作用。其中大多数对蛋白酪氨酸磷酸酶 1B 表现出有效的抑制作用，IC50 值范围为 0.33 至 9.84 μM。研究中，所有抑制类型都暴露了所检查的效力，包括混合竞争性 (1)、非竞争性 (3 和 5)、竞争性 (6) 和非竞争性 (7)。结果表明，O. stamineus 及其吡玛烷二萜可能通过胰岛素信号通路抑制蛋白酪氨酸磷酸酶 1B (PTP1B) 活性发挥降血糖作用。
Seven pimarane diterpenes (1-7) were isolated from Orthosiphon stamineus Benth. by assay-guided isolation. All of the isolates possessed a 2-deoxy-2-((7-nitro-2,1,3-benzoxadiazol-4-yl)amino)-d-glucose uptake effect in 3T3-L1 adipocytes at concentrations of 5 and 10 mu M. Most of them showed potent inhibition against protein tyrosine phosphatase 1B with IC50 values ranging from 0.33 to 9.84 mu M. In the kinetic study, all inhibition types were exposed for the examined potencies, including mixed-competitive (1), non-competitives (3 and 5), competitive (6), and uncompetitive (7). The results suggested that O. stamineus and its pimarane diterpenes might exert the hypoglycemic effect via the insulin signaling pathway targeting inhibition of protein tyrosine phosphatase 1B (PTP1B) activity.