Gugliandolo Enrico, Peritore Alessio Filippo, Impellizzeri Daniela, Cordaro Marika, Siracusa Rosalba, Fusco Roberta, D'Amico Ramona, Paola Rosanna Di, Schievano Carlo, Cuzzocrea Salvatore, Crupi Rosalia
Department of Chemical, Biological, Pharmaceutical and Environmental Science, University of Messina, 98168 Messina, Italy.
Innovative Statistical Research srl, Prato Della Valle 24, I-35123 Padova, Italy.
Animals (Basel). 2020 Oct 8;10(10):1827. doi: 10.3390/ani10101827.
Chronic mixed pain and orthopedic dysfunction are the most frequently associated consequences of canine osteoarthritis (OA). An unmet need remains for safe and effective therapies for OA. Palmitoyl-glucosamine (PGA) and curcumin are safe and naturally occurring compounds whose use is limited by poor bioavailability. Micronization is an established technique to increase bioavailability. The aim of this study was to investigate if the dietary supplementation with PGA co-micronized with curcumin (PGA-Cur, 2:1 ratio by mass) could limit pathologic process in two well-established rat models of inflammation and OA pain, i.e., subplantar carrageenan (CAR) and knee injection of sodium monoiodoacetate (MIA), respectively. In CAR-injected animals, a single dose of PGA-cur significantly reduced paw edema and hyperalgesia, as well as tissue damage and neutrophil infiltration. The repeated administration of PGA-Cur three times per week for 21 days, starting the third day after MIA injection resulted in a significant anti-allodynic effect. Protection against cartilage damage and recovery of locomotor function by 45% were also recorded. Finally, PGA-cur significantly counteracted MIA-induced increase in serum levels of TNF-α, IL-1β, NGF, as well as metalloproteases 1, 3, and 9. All the effects of PGA-Cur were superior compared to the compounds used singly. PGA-Cur emerged as a useful dietary intervention for OA.
慢性混合性疼痛和骨科功能障碍是犬骨关节炎（OA）最常见的相关后果。对于OA的安全有效治疗方法仍存在未满足的需求。棕榈酰葡萄糖胺（PGA）和姜黄素是安全的天然化合物，但其生物利用度差限制了它们的使用。微粉化是一种提高生物利用度的成熟技术。本研究的目的是调查在两种成熟的炎症和OA疼痛大鼠模型中，即分别在足底注射角叉菜胶（CAR）和膝关节注射一碘乙酸钠（MIA），饮食中补充与姜黄素共微粉化的PGA（PGA-Cur，质量比2:1）是否可以限制病理过程。在注射CAR的动物中，单剂量的PGA-姜黄素显著减轻了爪部水肿和痛觉过敏，以及组织损伤和中性粒细胞浸润。在MIA注射后第三天开始，每周三次重复给予PGA-Cur，持续21天，产生了显著的抗痛觉过敏作用。还记录到对软骨损伤的保护作用和运动功能恢复45%。最后，PGA-姜黄素显著抵消了MIA诱导的血清中TNF-α、IL-1β、NGF以及金属蛋白酶1、3和9水平的升高。与单独使用的化合物相比，PGA-Cur的所有作用都更优。PGA-Cur成为一种对OA有用的饮食干预措施。
