A microporous Co(II)-MOF as a pH-responsive 5-Fu delivery system to induce human hemangioma cells apoptosis and abrogate their growth

Abstract

A microporous metal-organic framework containing Co(II) as nodes with a polar pore surface, {[Co(SDB)(bpdh)0.5]}n (1), was formed via reaction of a –SO2 functionalized organic connector (H2SDB = 4,4′-sulfonyldibenzoic acid) combined with (bpdh = 2,5-bis(3-pyridyl)-3,4-diaza-2,4-hexadiene), N-rich spacer under the solvothermal conditions. The diamond channels of the framework for 1 have a size of 6.1 Å along the b axis of the crystal, and the surface area of BET is 541 m2·g−1. FT-IR spectra demonstrated 5-Fu loading and ultraviolet–visible spectra showed the loading capacity of 5-Fu of 27.36%. Compared with normal tissue of pH = 7.4, the drug release in simulated cancer tissue of pH = 5.7 was gradual, showing a rational pH-responsive drug release. Clone formation experiments and CCK-8 assay confirmed the antitumor activity of 5-Fu@1a against EOMA hemangioma cells. Detection of apoptotic protein level and Annexin V-FITC/PI analysis showed that 5-Fu@1a could induce the apoptosis in caspase-dependent manner. Antitumor ability of the 5-Fu was verified by experimental data in vivo, which is consistent with the experimental data in vitro.