Abstract Title:

Antitumor Effect of Shikonin, a PKM2 Inhibitor, in Cholangiocarcinoma Cell Lines.

Abstract Source:

Anticancer Res. 2020 Sep ;40(9):5115-5124. PMID: 32878800

Abstract Author(s):

Unchalee Thonsri, Wunchana Seubwai, Sakda Waraasawapati, Sopit Wongkham, Thidarat Boonmars, Ubon Cha'on, Chaisiri Wongkham

Article Affiliation:

Unchalee Thonsri


BACKGROUND/AIM: Pyruvate kinase M2 (PKM2) is an enzyme that is predominantly overexpressed in various types of cancer. The role of PKM2 in liver fluke-associated cholangiocarcinoma (CCA) remains unclear. This study aimed to investigate the antitumor activity of shikonin, a PKM2 inhibitor, in CCA cells.

MATERIALS AND METHODS: Immunohistochemistry and immunoblotting were used to determine PKM2 expression in CCA tissues and cells. Antiproliferative effects of shikonin were evaluated using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, colony-formation and trypan blue exclusion assays. The anti-metastatic activity of shikonin was determined using the Boyden chamber assay. Mechanisms by which shikonin inhibited CCA progression were determined.

RESULTS: PKM2 was overexpressed in CCA compared to normal bile duct epithelial cells. Shikonin significantly inhibited growth, and migration of CCA cells while inducing their death. A mechanistic study revealed that antitumor effects of shikonin in CCA cells depended on increased production of reactive oxygen species.

CONCLUSION: Shikonin may be a novel therapeutic agent for patients with CCA.

Study Type : In Vitro Study

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Sayer Ji
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