title: Ginsenoside Rh2 inhibiting HCT116 colon cancer cell proliferation through blocking PDZ-binding kinase/T-LAK cell-originated protein kinase.
abstract: BACKGROUND
  Ginsenoside Rh2 (GRh2) is the main bioactive component in American ginseng, a commonly used herb, and its antitumor activity had 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 HCT116 colorectal cancer cells.
  
  
  METHODS
  We examined the effect of GRh2 on HCT116 cellsex vivo. Next, we performedin vitrobinding assay andin vitrokinase assay to search for the target of GRh2. Furthermore, we elucidated the underlying molecular mechanisms for the antitumor effect of GRh2ex vivoandin vivo.
  
  
  RESULTS
  The results of ourin vitrostudies indicated that GRh2 can directly bind with PBK/TOPK and GRh2 also can directly inhibit PBK/TOPK activity.Ex vivostudies showed that GRh2 significantly induced cell death in HCT116 colorectal cancer cells. Further mechanistic study demonstrated that these compounds inhibited the phosphorylation levels of the extracellular regulated protein kinases 1/2 (ERK1/2) and (H3) in HCT116 colorectal cancer cells.In vivostudies showed GRh2 inhibited the growth of xenograft tumors of HCT116 cells and inhibited the phosphorylation levels of the extracellular regulated protein kinases 1/2 and histone H3.
  
  
  CONCLUSIONS
  The results indicate that GRh2 exerts promising antitumor effect that is specific to human HCT116 colorectal cancer cells through inhibiting the activity of PBK/TOPK.
authors.affiliation: Department of interventional radiology, Affiliated Hospital of Yan'an University, Shanxi, China.
authors.forename: Jianjun
authors.initials: J
authors.lastname: Yang
authors.affiliation: Department of interventional radiology, Affiliated Hospital of Yan'an University, Shanxi, China.
authors.forename: Donghong
authors.initials: D
authors.lastname: Yuan
authors.affiliation: Department of General Surgery, The Fourth People's Hospital, Shanxi, China.
authors.forename: Tongchao
authors.initials: T
authors.lastname: Xing
authors.affiliation: Department of Anesthesiology, Yanan University Affiliated Hospital, Shanxi, China.
authors.forename: Hongli
authors.initials: H
authors.lastname: Su
authors.affiliation: Department of General Surgery, Yanan University Affiliated Hospital, Shanxi, China.
authors.forename: Shengjun
authors.initials: S
authors.lastname: Zhang
authors.affiliation: Department of Radiology, Central Hospital of Tongchuan Mining Bureau, Shanxi, China.
authors.forename: Jiansheng
authors.initials: J
authors.lastname: Wen
authors.affiliation: Department of Pharmacy, Yanan University Affiliated Hospital, Shanxi, China.
authors.forename: Qiqiang
authors.initials: Q
authors.lastname: Bai
authors.affiliation: Department of Pathogenic microbiology, Medical College of Yan'an University, Shanxi, China.
authors.forename: Dongmei
authors.initials: D
authors.lastname: Dang
keywords: HCT116 colorectal cancer cells; PDZ-binding kinase/T-LAK cell-originated protein kinase; antitumor effect; apoptosis; ginsenoside Rh2