Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, 12 Jichang Road, Guangzhou 510405, China.
College of mechanical engineering, Yangzhou University, 88 South University Ave., Yangzhou 225009, China.
Molecules. 2018 Feb 11;23(2):384. doi: 10.3390/molecules23020384.
As one of the major active ingredients in Radix Scutellariae, wogonin has been shown to be associated with various pharmacological activities on cancer cell growth, apoptosis, and cell invasion and migration. Here, we demonstrated that wogonin may harbor potential anti-metastatic activities in hepatocarcinoma (HCC). The anti-metastasis potential of wogonin and its underlying mechanisms were evaluated by ligand-protein docking approach, surface plasmon resonance assay, and in vitro gelatin zymography studies. Our results showed that wogonin (100 μM, 50 μM) suppressed MHCC97L and PLC/PRF/5 cells migration and invasion in vitro. The docking approach and surface plasmon resonance assay indicated that the potential binding affinity between wogonin and matrix metalloproteinase-9 (MMP-9) may lead to inhibition of MMP-9 activity and further leads to suppression of tumor metastasis. This conclusion was further verified by Western blot results and gelatin zymography analysis. Wogonin might be a potent treatment option for disrupting the tumor metastasis that favors HCC development. The potential active targets from computational screening integrated with biomedical study may help us to explore the molecular mechanism of herbal medicines.
作为黄芩的主要活性成分之一，汉黄芩素已被证明与癌细胞生长、凋亡以及细胞侵袭和迁移的各种药理活性有关。在这里，我们证明汉黄芩素可能在肝癌（HCC）中具有潜在的抗转移活性。通过配体-蛋白对接方法、表面等离子体共振分析和体外明胶酶谱分析评估了汉黄芩素的抗转移潜力及其潜在机制。我们的结果表明，汉黄芩素（100 μM、50 μM）抑制 MHCC97L 和 PLC/PRF/5 细胞的体外迁移和侵袭。对接方法和表面等离子体共振分析表明，汉黄芩素与基质金属蛋白酶-9（MMP-9）之间的潜在结合亲和力可能导致 MMP-9 活性的抑制，进而抑制肿瘤转移。Western blot 结果和明胶酶谱分析进一步验证了这一结论。汉黄芩素可能是一种有效的治疗选择，可以破坏有利于 HCC 发展的肿瘤转移。计算筛选与生物医学研究相结合的潜在活性靶点可能有助于我们探索草药的分子机制。
