Department of Anatomy and Histology & Embryology, Faculty of Basic Medical Science, Kunming Medical University, Kunming 650500, Yunnan, China.
Key Laboratory of Chemistry in Ethnic Medicine Resource, State Ethnic Affairs Commission & Ministry of Education, School of Ethno-Medicine and Ethno-Pharmacy, Yunnan Minzu University, Kunming 650504, Yunnan, China.
J Agric Food Chem. 2020 Jul 8;68(27):7143-7151. doi: 10.1021/acs.jafc.0c02535. Epub 2020 Jun 24.
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-NH, 785.97 Da) in water extract obtained from shelled 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 identified peptide reduced uric acid levels and renal damage in hyperuricemic mice and showed anti-inflammatory and analgesic activities, indicating the potential of RDP3 as an antigout medicine candidate.
痛风和高尿酸血症会严重影响生活质量；然而，目前现有的药物无法满足所有临床需求。在本研究中，从去壳的 果实的水提取物中鉴定出一种新型肽（即大米衍生肽-3（RDP3），AAAAMAGPK-NH，785.97 Da）。试验表明，RDP3（最小有效浓度 100 μg/kg）既没有表现出血溶作用，也没有表现出急性毒性，并且通过抑制黄嘌呤氧化酶活性和降低尿酸转运蛋白 1 的表达来降低高尿酸血症小鼠的血清尿酸水平。RDP3 还通过降低 NLRP3 炎性体的表达来减轻高尿酸血症小鼠的肾脏损伤。此外，RDP3 减轻了福尔马林诱导的爪疼痛，并减少了单钠尿酸盐晶体诱导的爪肿胀和小鼠的炎症因子。因此，这种新鉴定的肽可降低高尿酸血症小鼠的尿酸水平和肾脏损伤，并具有抗炎和镇痛作用，表明 RDP3 有作为抗痛风药物候选物的潜力。
