研究领域：药理学 生物化学 医学

关键字：RDP3 抗痛风肽 水提取物 水稻 高尿酸血症 黄嘌呤氧化酶 尿酸转运蛋白1 NLRP3炎性体 肾损伤 抗炎 镇痛

痛风及高尿酸血症可严重损害患者生活质量；然而目前临床可用药物尚无法完全满足治疗需求。本研究从去壳水稻（Oryza sativa）果实水提物中鉴定出一种新型肽类物质，即水稻源性肽-3（RDP3，序列为AAAAMAGPK-NH₂，分子量785.97 Da）。药理学评价显示，RDP3最低有效剂量为100 μg/kg，未表现出溶血活性及急性毒性；其可通过抑制黄嘌呤氧化酶活性并下调尿酸转运蛋白1（URAT1）表达，显著降低高尿酸血症小鼠血清尿酸水平。此外，RDP3还可通过下调NLRP3炎症小体表达，缓解高尿酸血症小鼠的肾脏损伤。在疼痛与炎症模型中，RDP3亦可显著缓解甲醛诱导的小鼠足爪疼痛，并减轻单钠尿酸盐晶体诱导的小鼠足爪肿胀及炎症因子释放。综上，该新鉴定肽RDP3在高尿酸血症小鼠模型中兼具降尿酸、肾脏保护、抗炎及镇痛作用，展现出作为抗痛风候选药物的潜在价值。Gout and hyperuricemia can seriously affect the quality of life; at present, however, existing medicines are unable to meet all clinical needs. In the current study, a novel peptide (i.e., rice-derived-peptide-3 (RDP3), AAAAMAGPK-NH2, 785.97 Da) in water extract obtained from shelled Oryza sativa fruits was identified. Testing revealed that RDP3 (minimum effective concentration 100 μg/kg) did not show both hemolytic and acute toxicity, and reduced uric acid levels in the serum of hyperuricemic mice by inhibiting xanthine oxidase activity and decreasing urate transporter 1 expression. RDP3 also alleviated renal injury in hyperuricemic mice by decreasing NLRP3 inflammasome expression. Furthermore, RDP3 alleviated formalin-induced paw pain and reduced monosodium urate crystal-induced paw swelling and inflammatory factors in mice. Thus, this newly...