Small molecule inhibitor of nicotinamide N-methyltransferase shows anti-proliferative activity in HeLa cells.
Level 5 - mechanism / opinion, no new human data
In vitro laboratory bench research with no human subjects
PubMed 33645410 · doi:10.1080/01443615.2020.1854696
What was done
HeLa epithelial cervical cancer cells were treated in vitro with 0.1-500 μM of the NNMT inhibitor 5-methylquinolinium (5MQ). Cell viability was evaluated using the MTT assay, cellular morphology was assessed for apoptotic features, mRNA expression of TWIST, ZEB1, SERPIN1, SIRT1, and CD16 was measured by qRT-PCR, and protein levels of phospho-Akt and SIRT1 were evaluated by Western blotting. Effects on HEK-293 cells were also examined.
What was found
5MQ significantly inhibited HeLa cell proliferation in a concentration- and time-dependent manner, inducing cell shrinkage, loss of adhesion, and apoptotic bodies, without apparently affecting HEK-293 proliferation. 5MQ treatment resulted in increased ZEB1, SIRT1, and CD16 mRNA levels, decreased TWIST and SERPIN1 mRNA levels, and decreased protein expressions of phospho-Akt and SIRT1. No exact numerical values, effect sizes, IC50 concentrations, or p-values are reported in the abstract.
Why it matters
This study provides preliminary in vitro proof-of-concept that NNMT inhibition via 5MQ can impede cervical cancer cell proliferation and alter oncogenic signaling.
Limits
The study is restricted to in vitro experiments on cell lines, with no in vivo animal models or human clinical data. The abstract lacks all specific quantitative metrics and statistical values.
Cited by
- partial 5-Amino-1MQ inhibits nicotinamide N-methyltransferase (NNMT), which preserves NAD levels.