Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana - Xochimilco, Mexico.
Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana - Xochimilco, Mexico.
Life Sci. 2015 Jan 15;121:70-7. doi: 10.1016/j.lfs.2014.11.015. Epub 2014 Dec 2.
The aim of this study was to evaluate the antinociceptive (acute assays) and anti-inflammatory (chronic assays) effects of kramecyne (KACY), a peroxide isolated from Krameria cytisoides.
The antinociceptive activity of KACY was evaluated using the hot plate, acetic acid and formalin tests. The effects of KACY on heat-induced hemolysis in rat erythrocytes were also evaluated. The in vivo anti-inflammatory assays were performed using the chronic TPA (12-O-tetradecanoylphorbol 13-acetate) method to induce ear edema and carrageenan-kaolin induced arthritis (CKIA). In the CKIA model, the hot plate test was performed, serum samples were obtained for the quantitation of pro-inflammatory (IL-1β, IL-6, IL-12 and TNF-α) and anti-inflammatory (IL-4 and IL-10) cytokines.
KACY possess antinociceptive effects with comparable activity to naproxen (NPX). KACY inhibited hemolysis (EC50 = 180 μg/mL), in comparison to the untreated group and with a higher potency than NPX (EC50 = 263 μg/mL). KACY at 50 mg/kg decreased inflammation by 38% (chronic TPA-induced edema model) and by 26% (CKIA model), in comparison with the vehicle group and with similar activity to the positive controls 8 mg/kg indomethacin (IND) and 1 mg/kg methotrexate (MTX), respectively. In the CKIA model, KACY increased the release of anti-inflammatory (IL-4 and IL-10) cytokines but reduced the production of pro-inflammatory cytokines (IL-1β, IL-6, IL-12 and TNF-α). KACY at 50 and 100 mg/kg showed antinociceptive effects by 27% and 23%, respectively, in mice with mono-arthritis.
KACY might be a good alternative for the treatment of rheumatoid arthritis (RA) due its antinociceptive and anti-inflammatory activities.
本研究旨在评估来源于 Krameria cytisoides 的过氧化物 kramecyne（KACY）的镇痛（急性试验）和抗炎（慢性试验）作用。
使用热板、醋酸和福尔马林试验评估 KACY 的镇痛活性。还评估了 KACY 对大鼠红细胞热诱导溶血的影响。采用慢性 TPA（12-O-十四烷酰佛波醇 13-乙酸酯）法进行体内抗炎试验，以诱导耳肿胀和角叉菜胶-高岭土诱导关节炎（CKIA）。在 CKIA 模型中，进行热板试验，获得血清样本以定量测定促炎（IL-1β、IL-6、IL-12 和 TNF-α）和抗炎（IL-4 和 IL-10）细胞因子。
KACY 具有与萘普生（NPX）相当的镇痛作用。与未处理组相比，KACY 抑制溶血（EC50=180μg/mL），且比 NPX（EC50=263μg/mL）的活性更高。与载体组相比，KACY 以 50mg/kg 剂量给药可使炎症减少 38%（慢性 TPA 诱导的肿胀模型）和 26%（CKIA 模型），与阳性对照物 8mg/kg 吲哚美辛（IND）和 1mg/kg 甲氨蝶呤（MTX）的活性相当。在 CKIA 模型中，KACY 增加了抗炎（IL-4 和 IL-10）细胞因子的释放，但减少了促炎细胞因子（IL-1β、IL-6、IL-12 和 TNF-α）的产生。KACY 以 50 和 100mg/kg 剂量给药时，在单关节炎小鼠中分别表现出 27%和 23%的镇痛作用。
由于 KACY 具有镇痛和抗炎作用，因此它可能是治疗类风湿性关节炎（RA）的一种较好的选择。
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