1 Department of Food Sciences of Federal University of Lavras-UFLA , Lavras-MG, Brazil .
J Med Food. 2014 Jun;17(6):686-93. doi: 10.1089/jmf.2013.0122. Epub 2014 Jan 29.
In the present study, the pharmacological effects of 2,8-dihydroxy-1,6-dimethoxyxanthone from the bark of Haploclathra paniculata were investigated in mice using in vivo inflammation and nociception models. Acetic acid-induced writhing, paw licking induced by formalin, hot plate, and carrageenan-induced paw edema tests were used to investigate the anti-inflammatory and antinociceptive activities of the xanthone compound. Xanthone, at both doses, inhibited abdominal writhing and the formalin test. At a dose of 20 mg/kg, the time of reaction to the hot plate increased, and significant effects were observed after 30, 60 and 90 min of treatment. At doses of 10 and 20 mg/kg p.o., the 2,8-dihydroxy-1,6-dimethoxyxanthone significantly reduced paw edema at 3 h after the stimulus. The tests also showed no acute toxicity of the xanthone compound in mice. 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging ability was also studied and confirmed the antioxidant activity of the xanthone. To propose the mechanism of action of anti-inflammatory activity of the xanthone, a molecular docking was performed using the isoenzymes cyclooxygenase 1 and 2 and the results indicate that the molecule is capable of inhibiting both the enzymes. Therefore, it can be concluded that 2,8-dihydroxy-1,6-dimethoxyxanthone from H. paniculata demonstrates analgesic, anti-inflammatory, and antioxidant activities.
在本研究中,采用体内炎症和疼痛模型研究了来自聚伞花树皮的 2,8-二羟基-1,6-二甲氧基酮的药理作用。醋酸诱导扭体、福尔马林诱导的爪舔、热板和角叉菜胶诱导的爪肿胀试验用于研究该酮化合物的抗炎和镇痛活性。酮在两个剂量下均抑制腹部扭曲和福尔马林试验。在 20mg/kg 剂量下,对热板的反应时间增加,并且在治疗后 30、60 和 90 分钟观察到明显的效果。在 10 和 20mg/kg 口服剂量下,2,8-二羟基-1,6-二甲氧基酮可显著减少刺激后 3 小时的爪肿胀。试验还表明该酮化合物在小鼠中无急性毒性。还研究了 2,2-二苯基-1-苦基肼基(DPPH)自由基清除能力,并证实了酮的抗氧化活性。为了提出酮抗炎活性的作用机制,使用同工酶环加氧酶 1 和 2 进行了分子对接,结果表明该分子能够抑制两种酶。因此,可以得出结论,来自 H. paniculata 的 2,8-二羟基-1,6-二甲氧基酮具有镇痛、抗炎和抗氧化活性。