Deuteration enhances the anti-tumor effects and relative anti-inflammatory effects via affecting proliferation and apoptosis

Abstract

Apigenin (AP) is a plant flavonoid with potential biomedical applications. To enhance the anti-tumour effect, AP was deuterated via hydrogen–deuterium exchange under hydrothermal conditions. The anti-tumor effects of deuterated AP (D-AP) were then tested on HCT116 cells and on a murine model of turpentine-induced inflammation. Cell cycle progression and cell proliferation were measured by flow cytometry, and in vivo immuno-inflammation was evaluated by quantitating glucose metabolism using ¹⁸F-fluorodeoxyglucose positron emission tomography. According to the mass spectral results, the efficiency of AP deuteration was 62.96%. For both the two groups of AP and D-AP at 24 h and 48 h, there were an obvious increase on perception of G2 phage. Apigenin showed the ability of blocking in G2 phage to inhibit cellular proliferation. Additionally, D-AP induced early apoptosis in more cells than did AP (12.1% vs. 10.4%). Moreover, D-AP induced a more severe process of anti-inflammation during the early period, resulting in a more effective anti-inflammatory response. Therefore, given the innate ability of D-AP to block cell proliferation and induce early apoptosis, we conclude that deuteration enhances the systemic anti-cancer effect of this flavonoid.

Abstract

Apigenin; Deuteration; Apoptosis; Cell proliferation; Anti-inflammation.