Antitumor efficiency of the natural alkaloid berberine complexed with C60 fullerene in Lewis lung carcinoma in vitro and in vivo

Abstract Background Berberine (Ber) is a herbal alkaloid with pharmacological activity in general and high anticancer potency particular. However, due to its low bioavailability, the difficulty reaching target choosing right dose, there need improve approaches of Ber use therapy. In this study, Ber, noncovalently bound carbon nanostructure C 60 fullerene (C ) at various molar ratios components, was explored against Lewis lung carcinoma (LLC). Methods –Ber noncovalent nanocomplexes were synthesized 1:2, 1:1 2:1 ratios. release from studied after prolonged incubation different pH liquid chromatography–mass spectrometry analysis free content. Biological effects -complaxated vitro towards LLC cells phase-contrast fluorescence microscopy, flow cytometry, MTT reduction, caspase wound closure assays. The treatment nanocomplex evaluated vivo LLC-tumored C57Bl mice. mice body weight, tumor size, weight index assessed for four groups, treated saline, 15 mg /kg, 7.5 Ber/kg or -Ber (15 Ber/kg). Results promoted medium acidification. followed by enhanced intracellular uptake as compared Ber. cytotoxicity agents order: < 1:2 nanocomplex. cytotoxic effect confirmed 21.3-fold decrease IC 50 value (0.8 ± 0.3 µM) (17 2 µM). induced 3/7 activation suppressed migration cells. therapeutic mouse model LLC. growth group approximately 50% end experiment, while tumor-bearing no detected. Conclusions This study indicates that complexation natural may be novel strategy carcinoma. Graphical abstract