Chen Jialiang, Li Ping, Ye Shuhong, Li Wei, Li Ming, Ding Yan
School of Food Science and Technology, Dalian Polytechnic University, Dalian, China.
Korean Medicine (KM) Application Center, Korea Institute of Oriental Medicine, Daegu, South Korea.
J Food Biochem. 2022 Dec;46(12):e14492. doi: 10.1111/jfbc.14492. Epub 2022 Nov 17.
Phlorotannins, polyphenolic compounds that exist only in brown algae, have an effect on T2DM. However, the structure of phlorotannins is complex and diverse, and the complex role of therapeutic targets and active compounds has not been revealed. In this study, the potential targets and pharmacological effects of phlorotannins in the treatment of T2DM were identified based on network pharmacology and enzyme activity inhibition experiment. In total, 15 phlorotannins and 53 associated targets were yielded. Among them, SRC, ESR1, AKT1, HSP90AB1, and AR were defined as core targets. 527 GO biological processes items and 101 KEGG pathways were obtained, including EGFR tyrosine kinase inhibitor resistance, thyroid hormone signaling pathway, AGE-RAGE signaling pathway in diabetic complications, and VEGF signaling pathway. Phlorotannins could enable resistance against T2DM by inflammatory, survival, gene transcription, proliferation, apoptosis, and atherosclerosis. Finally, α-glucosidase inhibition assay and molecular docking proved the effect of selected phlorotannins on T2DM. PRACTICAL APPLICATIONS: Phlorotannins are a kind of polyphenol compounds that only exists in brown algae. Its structure is polymerized by aromatic precursors phloroglucinol (1,3,5-trihydroxybenzene). They have aroused great interest due to their excellent and valuable biological activities. However, the structure of phlorotannins is complex and diverse, and the complex role of therapeutic targets and active compounds has not been revealed. In this study, the potential targets and pharmacological effects of phlorotannins in the treatment of T2DM were determined basis on network pharmacology and enzyme activity inhibition experiment. In conclusion, the results showed the value of phlorotannins treating on T2DM. Moreover, this study has great significance for improving the medicinal value of phlorotannins and screening natural products for the treatment of T2DM.
间苯三酚单宁是仅存在于褐藻中的多酚类化合物，对2型糖尿病有影响。然而，间苯三酚单宁的结构复杂多样，其治疗靶点和活性化合物的复杂作用尚未揭示。本研究基于网络药理学和酶活性抑制实验，确定了间苯三酚单宁治疗2型糖尿病的潜在靶点和药理作用。共产生了15种间苯三酚单宁和53个相关靶点。其中，SRC、ESR1、AKT1、HSP90AB1和AR被定义为核心靶点。获得了527个基因本体生物学过程条目和101条京都基因与基因组百科全书通路，包括表皮生长因子受体酪氨酸激酶抑制剂抗性、甲状腺激素信号通路、糖尿病并发症中的晚期糖基化终末产物-受体（AGE-RAGE）信号通路和血管内皮生长因子（VEGF）信号通路。间苯三酚单宁可通过炎症、存活、基因转录、增殖、凋亡和动脉粥样硬化来对抗2型糖尿病。最后，α-葡萄糖苷酶抑制试验和分子对接证明了所选间苯三酚单宁对2型糖尿病的作用。实际应用：间苯三酚单宁是一种仅存在于褐藻中的多酚类化合物。其结构由芳香族前体间苯三酚（1,3,5-三羟基苯）聚合而成。由于其优异且有价值的生物活性，它们引起了极大的兴趣。然而，间苯三酚单宁的结构复杂多样，其治疗靶点和活性化合物的复杂作用尚未揭示。本研究基于网络药理学和酶活性抑制实验，确定了间苯三酚单宁治疗2型糖尿病的潜在靶点和药理作用。总之，结果显示了间苯三酚单宁治疗2型糖尿病的价值。此外，本研究对于提高间苯三酚单宁的药用价值以及筛选治疗2型糖尿病的天然产物具有重要意义。
