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Updated: Jun 19, 2026
A Robust Discovery Platform for the Identification of Novel Mediators of Melanoma Metastasis
Published on: March 8, 2022
Antimetastatic activity of MONCPT in preclinical melanoma mice model
Xiao-Chun Yang1, Chong-Xing Tu, Pei-Hua Luo
1Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, People's Republic of China.
Abstract:
Previous study demonstrated that MONCPT, a topoisomerase I inhibitor, exhibited potent anti-proliferation and anti-angiogenesis activity in vitro and in vivo. In this study, we report the efficacy of MONCPT against the development of melanoma metastasis by an intravenous injection of green fluorescent protein-transfected mice melanoma carcinoma (B16F10-GFP) cells in C57BL/6 mice. MONCPT (2.0, 5.0 and 12.5 mg/kg/2 days) markedly decreased B16F10-GFP pulmonary metastases by 12.8%, 53.1% and 76.3%, respectively; whereas higher doses of MONCPT (31.0 mg/kg/2 days) significantly inhibited the tumor growth of B16F10 xenograft model. In the in vitro experiment, MONCPT suppressed the B16F10-GFP cell invasion and migration without affecting cell survival. Further studies demonstrated that MONCPT decreased the secretion of matrix metalloproteinase (MMP)-9 and VEGF, and reduced the protein expression of HIF-1α as well as the phosphorylation level of ERK in B16F10-GFP cells. These in vivo and in vitro results indicate that MONCPT possesses both the potent antimetastatic ability and the tumor growth-inhibition activity, and the dual function promises MONCPT as a potential therapeutic agent for tumor metastasis and tumor growth of melanoma carcinoma.
Insights
MONCPT, a topoisomerase I inhibitor, effectively reduced melanoma metastasis and tumor growth in preclinical models. This compound suppressed cancer cell invasion and migration, showing promise as a dual-action therapeutic agent.
Area of Science:
- Oncology
- Pharmacology
Background:
- MONCPT is a topoisomerase I inhibitor with demonstrated anti-proliferation and anti-angiogenesis effects.
- Melanoma metastasis remains a significant challenge in cancer treatment.
Purpose of the Study:
- To evaluate the efficacy of MONCPT against melanoma metastasis and tumor growth.
- To investigate the underlying mechanisms of MONCPT's action.
Main Methods:
- In vivo studies using B16F10-GFP melanoma cells in C57BL/6 mice to assess metastatic burden and tumor growth.
- In vitro experiments to evaluate the effects of MONCPT on cell invasion, migration, and key molecular targets.
Main Results:
- MONCPT significantly decreased pulmonary metastases in a dose-dependent manner (up to 76.3%).
- Higher doses of MONCPT inhibited B16F10 xenograft tumor growth.
- In vitro, MONCPT suppressed B16F10-GFP cell invasion and migration without impacting cell survival.
- MONCPT reduced MMP-9 and VEGF secretion, HIF-1α expression, and ERK phosphorylation.
Conclusions:
- MONCPT exhibits potent antimetastatic and tumor growth-inhibitory activities against melanoma.
- The dual therapeutic potential of MONCPT warrants further investigation for melanoma treatment.
