Abstract
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 μM. Most of them showed potent inhibition against protein tyrosine phosphatase 1B with IC50 values ranging from 0.33 to 9.84 μM. 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.
Highlights
Diabetes mellitus (DM) is a fast-growing metabolic disease affecting people globally
DM is a metabolic ailment that is categorized by glucose intolerance and deviations of lipid and protein metabolism processes
We examined the activity of the pimarane diterpenes 1–7 on 2-NBDG uptake in the 3T3-L1 adipocytes model
Summary
Diabetes mellitus (DM) is a fast-growing metabolic disease affecting people globally. Searching for PTP1B inhibitors, especially inhibitory agents from natural and medicinal plants, microorganisms, and animals, are the main prospects in both type 2 diabetes treatment and obesity [7,8]. Many chemical and pharmacological research works, and numerous natural compounds that could be used in anti-diabetic treatments through PTP1B inhibitory action have been identified in Chinese and Southeast Asian medicinal plants. In East Asia countries, such as China, Japan, Korea, Thailand, Vietnam, and Indonesia, the traditional medical treatment of diabetes often considers the integrated effects of different medicinal plants. Belongs to the Orthosiphon genus, which is one of the largest genus in the Lamiaceae family This plant is widely distributed in Southeast Asia, Australia, and Africa [13], and is used for the treatment of many diseases in traditional medicines [14]. We report the isolation, structural elucidation, and the 2-NBDG uptake effects along with their PTP1B inhibitory activities of the pimarane diterpenes from O. stamineus
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