Investigational New Drugs

, Volume 33, Issue 1, pp 1–11 | Cite as

Momordica Charantia lectin exhibits antitumor activity towards hepatocellular carcinoma



Background The incidence and mortality of hepatocellular carcinoma (HCC) remain high worldwide. Drug screening from natural plants is one of the potential therapeutic approaches on HCC. Methods The antitumor effect of momordica charantia lectin (MCL) was examined, using MTT, colony formation, AnnexinV/PI staining, western blot and animal model. Results MCL treatment induced G2/M phase arrest, autophagy, DNA fragmentation, mitochondrial injury, and subsequently cell apoptosis in HCC cells. Activation of caspase and MAPK pathway was involved in MCL-induced apoptosis. In vitro and in vivo studies showed that up-regulation of truncated Bid (tBid) upon MCL treatment. Correlation analysis revealed that Bid expression was reversely associated with the IC50 of MCL. Bid suppression using Bid siRNA, BI-6C9 (Bid inhibitor) and Z-IETD-FMK (caspase 8 inhibitor) dramatically attenuated MCL-induced cell proliferation inhibition, caspase 3 activation, ΔΨm depolarization and apoptosis. In addition, combination of MCL and sorafenib exerted stronger lethal activity towards HCC in vitro and in vivo. Conclusion Our data show that the natural compound MCL manifests antitumor activities towards HCC and therefore suggest MCL as a promising chemotherapeutic agent.


MCL Bid Apoptosis Hepatocellular carcinoma 



Momordica Charantia lectin


hepatocellular carcinoma


truncated Bid


acidic vesicular organelles


Mitogen activated protein kinase



We thank Dr. George Gong Chen from The Chinese University of Hong Kong for his valuable advices on our study. This work was supported by grants from the National Natural Science Foundation of China (No. 81201717) and the China Postdoctoral Science Foundation (No. 2012 M511867).

Conflicts of interest

There are no conflicts of interest.

Supplementary material

10637_2014_156_MOESM1_ESM.doc (680 kb)
ESM 1 (DOC 680 kb)


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Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  1. 1.Department of Pathology, Sun Yat-sen University Cancer CenterGuangzhouChina
  2. 2.Sun Yat-sen University Cancer Center; State Key Laboratory of Oncology in South China; Collaborative Innovation Center for Cancer MedicineGuangzhouChina
  3. 3.Laboratory of Molecular Gerontology, National Institute on AgingBaltimore, MDUSA
  4. 4.Department of Biochemistry and Molecular BiologyGuangdong Medical CollegeZhanjiangChina

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