Chemotherapeutic dihydromyricetin with remarkable anti-tumor activity and biosafety for muscle invasive bladder cancer.

Plant-derived drugs (PDD) with remarkable anti-tumor activity and biosafety are highly desirable for clinical tumor chemotherapy. In this work, dihydromyricetin (DHM), a natural PDD extracted from ratten tea, was screened out to be a potential chemotherapeutic drug for muscle invasive bladder cancer (MIBC). The results of <i>in vitro</i> assays confirmed that DHM could effectively inhibit the proliferation, survival and migration of MIBC cells, and promote apoptosis (<i>P</i> < 0.05). M1 macrophage polarization was also observed after DHM chemotherapy. The hub genes in cell cycle and apoptosis signaling pathways were differential expressed, and the epithelial-mesenchymal transition (EMT) in MIBC cells was also reversed by DHM treatment. The <i>in vivo</i> effectiveness and biosafety evaluations of DHM chemotherapy were performed using a xenograft bearing mice model. The results revealed that DHM intravenous chemotherapy with a dose of 20 mg/kg for 7 times could significantly suppress the <i>in vivo</i> tumorigenesis of MIBC (<i>P</i> < 0.05), while triggered no obvious drug side effects. In conclusion, this work provided a PPD with remarkable <i>in vitro</i> and <i>in vivo</i> anti-tumor activity and biosafety, which could serve as a promising alternative for the application of MIBC chemotherapy.