Baicalin suppresses lung cancer growth by targeting PDZ-binding kinase/T-LAK cell-originated protein kinase.
Baicalin is the main bioactive component extracted from the traditional Chinese medicine Baical Skullcap Root, and its anti-tumor activity has been studied in previous studies. PDZ-binding kinase/T-LAK cell-originated protein kinase (PBK/TOPK), a serine/threonine protein kinase, is highly expressed in many cancer cells and stimulates the tumorigenic properties, and so, it is a pivotal target for agent to cure cancers. We reported for the first time that baicalin suppressed PBK/TOPK activities by directly binding with PBK/TOPK in vitro and in vivo. Ex vivo studies showed that baicalin suppressed PBK/TOPK activity in JB6 Cl41 cells and H441 lung cancer cells. Moreover, knockdown of PBK/TOPK in H441 cells decreased their sensitivity to baicalin. In vivo study indicated that injection of baicalin in H441 tumor-bearing mice effectively suppressed cancer growth. The PBK/TOPK downstream signaling molecules Histone H3 and ERK2 in tumor tissues were also decreased after baicalin treatment. Taken together, baicalin can inhibit proliferation of lung cancer cells as a PBK/TOPK inhibitor both in vitro and in vivo.
['Diao|Xin|X|', 'Yang|Danfen|D|', 'Chen|Yu|Y|', 'Liu|Wentian|W|0000-0002-6390-9698']
D000072283:A549 Cells D000818:Animals D000970:Antineoplastic Agents D002460:Cell Line D049109:Cell Proliferation D005419:Flavonoids D006801:Humans D008175:Lung Neoplasms D051379:Mice D008819:Mice, Nude D020929:Mitogen-Activated Protein Kinase Kinases D047428:Protein Kinase Inhibitors
Baicalin lung cancer PBK/TOPK inhibitor