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Experimental Study of Hepatocellular Carcinoma Treatment by Shikonin Through Regulating PKM2
Tong Liu1,2,3, Sainan Li2, Liwei Wu2
1Department of Gastroenterology, Putuo People's Hospital, Tongji University School of Medicine, Shanghai 200060, People's Republic of China.
Objective:
Shikonin is a natural product with many activities, including anti-cancer effects. Pyruvate kinase type M2 (PKM2) plays a crucial role in the growth of tumor cells. However, the effect of shikonin on PKM2 in hepatocellular carcinoma (HCC) is unclear.
Methods:
Cell viability, apoptosis level, glucose uptake, and lactate production were detected in HCC cells. Lentivirus-overexpressed and -shRNA of PKM2 were used to verify the key target of shikonin. A xenograft mouse model was used to detect the efficacy of shikonin and its combination with sorafenib in vivo.
Results:
Shikonin inhibited proliferation and glycolysis and induced apoptosis in HCC cells. Either PKM2-overexpressed or PKM2-shRNA alleviated or enhanced this effect. The results of CCK-8 showed that shikonin significantly inhibited cell viability of HCC cells. The levels of glucose uptake and lactate production were dramatically decreased by shikonin-treated. Results of flow cytometry and Western blot showed that the levels of apoptosis of HCC cells were significantly increased in a dose-dependent manner after shikonin treatment. In addition, shikonin enhanced the anti-cancer effect of sorafenib in vitro and in vivo. Our results showed that SK combined with sorafenib markedly inhibits tumor growth in HCC-transplanted nude mice compared to SK or sorafenib alone.
Conclusion:
By inhibiting PKM2, shikonin inhibited proliferation and glycolysis and induced cell apoptosis in HCC cells. The effect of shikonin on tumor cell proliferation, apoptosis and glycolsis will make it promising drug for HCC patients.
Insights
Shikonin, a natural compound, inhibits hepatocellular carcinoma (HCC) cell growth by targeting pyruvate kinase type M2 (PKM2). This natural product shows promise as an anti-cancer drug for HCC treatment.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- Shikonin exhibits anti-cancer properties.
- Pyruvate kinase type M2 (PKM2) is vital for tumor cell proliferation.
- The specific impact of shikonin on PKM2 in hepatocellular carcinoma (HCC) requires elucidation.
Purpose of the Study:
- To investigate the effect of shikonin on PKM2 in HCC.
- To determine shikonin's impact on HCC cell viability, apoptosis, and glycolysis.
- To evaluate shikonin's efficacy alone and in combination with sorafenib in HCC models.
Main Methods:
- Assessed cell viability, apoptosis, glucose uptake, and lactate production in HCC cells.
- Utilized lentivirus-mediated overexpression and shRNA knockdown of PKM2.
- Employed a xenograft mouse model to assess in vivo efficacy.
Main Results:
- Shikonin suppressed HCC cell proliferation and glycolysis while inducing apoptosis.
- PKM2 modulation influenced shikonin's effects.
- Shikonin demonstrated synergistic anti-cancer activity with sorafenib in vitro and in vivo.
Conclusions:
- Shikonin inhibits HCC progression by targeting PKM2, reducing proliferation and glycolysis, and promoting apoptosis.
- Shikonin presents potential as a therapeutic agent for hepatocellular carcinoma.
