Abstract：
Opuntia ficus-indica fruit (OFI) is rich in bioactive compounds, which can promote human health. In this work, the purified OFI extract was prepared from OFI and its bioactivities were investigated. Xanthine oxidase (XOD) and α-glucosidase (α-Glu) inhibitors of the purified OFI extract were screened and identified by bio-affinity ultrafiltration combined with UPLC-QTRAP-MS/MS technology. The inhibitory effect of these inhibitors on enzymes were verified, and the potential mechanism of action and binding sites of inhibitors with enzymes were revealed based on molecular docking. The results showed that the total phenolic content of the purified OFI extract was 355.03 mg GAE/g DW, which had excellent antioxidant activity. Additionally, the extract had a certain inhibitory effect on XOD (IC50 = 199.00 ± 0.14 µg/mL) and α-Glu (IC50 = 159.67 ± 0.01 µg/mL). Seven XOD inhibitors and eight α-Glu inhibitors were identified. Furthermore, XOD and α-Glu inhibition experiments in vitro confirmed that inhibitors such as chlorogenic acid, taxifolin, and naringenin had significant inhibitory effects on XOD and α-Glu. The molecular docking results indicated that inhibitors could bind to the corresponding enzymes and had strong binding force. These findings demonstrate that OFI contains potential substances for the treatment of hyperuricemia and hyperglycemia.
摘要：
仙人掌果（OFI）富含生物活性化合物，可以促进人类健康。在这项工作中,从OFI中制备纯化的OFI提取物，并研究其生物活性。采用生物亲和超滤结合UPLC-QTRAP-MS/MS技术对纯化后的OFI提取物的黄嘌呤氧化酶(XOD)和α-葡萄糖苷酶(α-Glu)抑制剂进行筛选和鉴定。验证了这些抑制剂对酶的抑制作用，基于分子对接，揭示了抑制剂与酶的潜在作用机制和结合位点。结果表明，纯化的OFI提取物的总酚含量为355.03mgGAE/gDW，具有优异的抗氧化活性。此外,提取物对XOD(IC50=199.00±0.14µg/mL)和α-Glu(IC50=159.67±0.01µg/mL)有一定的抑制作用。鉴定了7种XOD抑制剂和8种α-Glu抑制剂。此外，体外XOD和α-Glu抑制实验证实绿原酸等抑制剂,taxifolin,柚皮素对XOD和α-Glu有明显的抑制作用。分子对接结果表明，抑制剂可以与相应的酶结合，并具有很强的结合力。这些发现表明OFI含有治疗高尿酸血症和高血糖症的潜在物质。
