a College of Pharmacy , Fujian University of Traditional Chinese Medicine , Fuzhou , PR China.
b College of Chemical and Material Science Engineering , Kaili University , Guizhou , PR China.
Pharm Biol. 2019 Dec;57(1):82-89. doi: 10.1080/13880209.2018.1561730.
Notopterygium incisum Ting ex H. T. Chang (Umbelliferae) (NI) specializes in treatment of upper limb rheumatoid arthritis (RA), but the exact mechanism is unclear. P2Xs are useful targets for inflammatory pain therapy. It led us to hypothesize that NI may preferentially act on particular P2Xs and these receptors may be unevenly distributed in the upper/lower limb.
To investigate P2Xs distribution in the upper/lower limb and NI's targets in upper limb RA.
The SD rats were randomized into 11 groups of 10 animals each. Eight experimental groups were established by the injection of 0.1 mL FCA into the plantar surface of rat paw. Three control groups suffered the same volume of saline. The articular cavities were then taken on the seventh day to detect P2Xs expression. NI (3 g/kg) and prednisone (10 mg/kg) were respectively given by oral gavage once daily for 14 d. The swelling degree and P2Xs were evaluated individually.
In normal rats, the expressions of P2X and P2X in forelimb were markedly higher than that of in hind limb (P < 0.05). After induced by FCA, P2X, P2X, P2X, P2X and P2X were increased significantly (P < 0.01). The biggest difference was P2X. In NI treatment rats, swelling degree of the 7th/14th day in forelimb was 68.24%/38.89%, whereas that of in hind limb was 88.72%/79.92%. P2X mRNA and protein expression was significantly reduced as contrasted with the control group (P < 0.05).
P2X receptor was predominantly expressed in the forelimb RA rat. NI relieved the FCA-induced RA by inhibiting upper limb's P2X receptor.
羌活(伞形科)(NI)专门治疗上肢类风湿关节炎(RA),但其确切机制尚不清楚。P2X 是治疗炎症性疼痛的有用靶点。这使我们假设 NI 可能优先作用于特定的 P2X,这些受体在上肢/下肢的分布可能不均匀。
研究 P2X 在上下肢的分布以及 NI 在治疗上肢 RA 中的靶点。
将 SD 大鼠随机分为 11 组,每组 10 只。将 0.1ml FCA 注射到大鼠足底表面建立 8 个实验组。3 个对照组接受相同体积的生理盐水。第七天取出关节腔,检测 P2X 表达。NI(3g/kg)和泼尼松(10mg/kg)分别每天口服 1 次,共 14 天。单独评估肿胀程度和 P2X。
在正常大鼠中,前肢 P2X 和 P2X 的表达明显高于后肢(P<0.05)。用 FCA 诱导后,P2X、P2X、P2X、P2X 和 P2X 的表达均显著增加(P<0.01)。最大的差异是 P2X。在 NI 治疗大鼠中,前肢第 7 天/第 14 天的肿胀程度分别为 68.24%/38.89%,而后肢的肿胀程度分别为 88.72%/79.92%。与对照组相比,P2X mRNA 和蛋白表达显著降低(P<0.05)。
P2X 受体在上肢 RA 大鼠中主要表达。NI 通过抑制上肢 P2X 受体缓解 FCA 诱导的 RA。