Liu Naixin, Meng Buliang, Zeng Lin, Yin Saige, Hu Yan, Li Shanshan, Fu Yang, Zhang Xinping, Xie Chun, Shu Longjun, Yang Meifeng, Wang Ying, Yang Xinwang
Department of Anatomy and Histology & Embryology, Faculty of Basic Medical Science, Kunming Medical University, Kunming, Yunnan 650500, China.
Food Funct. 2020 Dec 1;11(12):10542-10553. doi: 10.1039/d0fo01774d. Epub 2020 Nov 13.
As a metabolic disease, gout, which seriously affects the normal life of patients, has become increasingly common in modern society. However, the existing medicines cannot completely meet the clinical needs. In the current study, a novel short peptide (named rice-derived-peptide-2 (RDP2), AAAAGAMPK-NH2, 785.97 Da) was isolated and identified from water extract of shelled Oryza sativa fruits, without toxic side effects but excellent stability. Our results indicated that RDP2 (the minimum effective concentration is 5 μg kg) induced a significant reduction in serum uric acid levels in hyperuricemic mice via suppressing xanthine oxidase activity and urate transporter 1 expression, as well as alleviated renal damage through inhibiting the activation of NLRP3 inflammasome. In addition, RDP2 can also alleviate paw swelling and inflammatory reactions in mice after subcutaneous injection of monosodium urate crystals. As mentioned above, we obtained a novel peptide which could work through all stages of gout, not only reducing uric acid levels and renal damage in hyperuricemic mice, but also alleviating inflammatory responses associated with acute gout attack, and thus provided a new peptide molecular template for the development of anti-gout drugs.
作为一种代谢性疾病，痛风严重影响患者的正常生活，在现代社会中已变得越来越普遍。然而，现有的药物并不能完全满足临床需求。在当前的研究中，从去壳水稻果实的水提取物中分离并鉴定出一种新型短肽（命名为水稻衍生肽-2（RDP2），AAAGAMPK-NH2，785.97 Da），其无毒性副作用但稳定性极佳。我们的结果表明，RDP2（最低有效浓度为5 μg/kg）通过抑制黄嘌呤氧化酶活性和尿酸盐转运蛋白1的表达，显著降低高尿酸血症小鼠的血清尿酸水平，并通过抑制NLRP3炎性小体的激活减轻肾脏损伤。此外，皮下注射尿酸钠晶体后，RDP2还可减轻小鼠足爪肿胀和炎症反应。如上所述，我们获得了一种新型肽，其可作用于痛风的各个阶段，不仅降低高尿酸血症小鼠的尿酸水平和肾脏损伤，还减轻与急性痛风发作相关的炎症反应，从而为抗痛风药物的开发提供了一种新的肽分子模板。
