College of Pharmacy, Guiyang University of Chinese Medicine, Guiyang, People's Republic of China.
Experiment Center, Guiyang University of Chinese Medicine, 50, Nanming District, Guiyang, 550002, Guizhou Province, People's Republic of China.
Mol Divers. 2020 Feb;24(1):21-30. doi: 10.1007/s11030-019-09928-5. Epub 2019 Feb 22.
The dried rhizome of Musa basjoo Sieb. et Zucc. is Rhizoma Musae. It has been used to treat diabetes in Miao medicine in China. Lupenone was isolated from Rhizoma Musae and has good anti-diabetic activity. Its mechanism of action is unclear. Diabetes is a chronic low-level systemic inflammatory disease, and lupenone has anti-inflammatory activity, but the underlying mechanism is not fully elucidated. In this study, we aimed to construct the drug-target biologic network and predict the anti-inflammatory mechanism of lupenone. The network-based pharmacologic analysis platform was used to identify the target proteins related to inflammation. Furthermore, the effects of lupenone on acute, subacute and diabetic pancreatic inflammation were evaluated. The "component-target-disease" network was constructed using Cytoscape. Lupenone could regulate transcription factor p65, NF-kappa-B inhibitor alpha, transcription factor AP-1, NF-kappa-B essential modulator, nuclear factor NF-kappa-B p105 subunit, epidermal growth factor receptor, hypoxia-inducible factor 1-alpha and other proteins related to the PI3K-Akt, Toll-like receptor and NF-kappa B signaling pathways. In addition, lupenone significantly decreased acute and subacute inflammation in mice as well as the IL-1β and IFN-γ levels in the pancreas of diabetic rats. The above results provide strong support for studying the molecular mechanism of lupenone in the treatment of diabetes from the perspective of anti-inflammation.
芭蕉科芭蕉属植物芭蕉的干燥根茎为中药芭蕉根。在我国苗医中,芭蕉根被用于治疗糖尿病。从芭蕉根中分离得到的双氢美洲花椒酮具有良好的降血糖活性。但其作用机制尚不清楚。糖尿病是一种慢性低度系统性炎症性疾病,而双氢美洲花椒酮具有抗炎活性,但作用机制尚未完全阐明。本研究旨在构建药物-靶标生物网络,预测双氢美洲花椒酮的抗炎作用机制。采用基于网络的药理分析平台鉴定与炎症相关的靶蛋白。此外,还评估了双氢美洲花椒酮对急性、亚急性和糖尿病胰腺炎症的作用。采用 Cytoscape 构建“成分-靶标-疾病”网络。双氢美洲花椒酮可调节转录因子 p65、核因子κB 抑制物α、转录因子 AP-1、核因子κB 必需调节因子、核因子 NF-κB p105 亚基、表皮生长因子受体、缺氧诱导因子 1α等与 PI3K-Akt、Toll 样受体和 NF-κB 信号通路相关的蛋白。此外,双氢美洲花椒酮可显著降低急性和亚急性炎症小鼠以及糖尿病大鼠胰腺中 IL-1β 和 IFN-γ 的水平。上述结果为从抗炎角度研究双氢美洲花椒酮治疗糖尿病的分子机制提供了有力支持。