Florentino Iziara F, Silva Daiany P B, Galdino Pablinny M, Lino Roberta C, Martins José L R, Silva Dayane M, de Paula José R, Tresvenzol Leonice M F, Costa Elson A
Laboratório de Farmacologia de Produtos Naturais e Sintéticos, ICB, UFG, Goiânia, GO, Brazil.
Laboratório de Farmacologia de Produtos Naturais e Sintéticos, ICB, UFG, Goiânia, GO, Brazil.
J Ethnopharmacol. 2016 Jun 20;186:298-304. doi: 10.1016/j.jep.2016.04.010. Epub 2016 Apr 11.
The leaves and stems bark of Memora nodosa (Silva Manso) Miers (Bignoniaceae) are used in Brazilian traditional medicine in the treatment of external ulcers and wounds; its roots are used to treat abdominal pain and scabies.
Our aim was to evaluate the antinociceptive and anti-inflammatory activities of Memora nodosa roots ethanolic extract (EMN) and allantoin, a secondary metabolite isolated from this plant.
The EMN and allantoin antinociceptive activity were evaluated in mice using both chemical and heat-induced pain models such as acetic acid-induced writhing, formalin and tail-flick tests. In the formalin test, a pre-treatment with naloxone was used to verify an involvement of opioid receptor in the antinociceptive effect of EMN and allantoin. Pre-treatment with glibenclemide was used to verity an involvement of ATP-sensitive K(+)channel in the allantoin antinociceptive effect. EMN and allantoin anti-inflammatory activity were assessed by carrageenan-induced paw edema and pleurisy tests.
The treatment with EMN (250, 500 and 1000mg/kg, p.o.) inhibit the acetic acid and formalin (both phases)-induced nociception. However, just at doses 500 and 1000mg/kg increased the latency time in tail-flick test. These results suggest the involvement of both peripheral and central antinociceptive mechanisms. The treatment with allantoin (40, 60 and 80mg/kg p.o.) produced a dose-dependent antinociceptive effect in both phases of formalin-induced nociception test; allantoin (60mg/kg) was not able to increase the latency time in tail flick-test. The pre-treatment with naloxone completely reversed the EMN (1000mg/kg) and allantoin (60mg/kg) effect in the first phase of formalin test; and glibenclamide reversed the allantoin effect. The administration of EMN (250, 500 and 1000mg/kg) and allantoin (60mg/kg) showed significant anti-inflammatory activity in the whole carrageenan-induced paw edema. Furthermore, EMN and allantoin reduced the leukocytes migration and pleural exudate to the pleural cavity.
EMN have significant antinociceptive and anti-inflammatory effects, which appear to be, at least in part, due to the presence of allantoin. However, allantoin is not responsible for the EMN central antinociceptive activity. Allantoin has peripheral antinociceptive activity that involves the opioid receptor and ATP-sensitive K(+)channels. Opioid receptors are also involved in the EMN antinociceptive activity. These findings support the use of Memora nodosa in popular medicine and demonstrate that this plant has therapeutic potential for the development of antinociceptive and anti-inflammatory phytomedicines.
巴西传统医学中,诺多记忆木(Memora nodosa (Silva Manso) Miers,紫葳科)的叶、茎皮用于治疗外部溃疡和伤口;其根用于治疗腹痛和疥疮。
我们的目的是评估诺多记忆木根乙醇提取物(EMN)和从该植物中分离出的次生代谢产物尿囊素的镇痛和抗炎活性。
使用化学和热诱导疼痛模型,如醋酸诱导扭体、福尔马林和甩尾试验,在小鼠中评估EMN和尿囊素的镇痛活性。在福尔马林试验中,用纳洛酮预处理以验证阿片受体是否参与EMN和尿囊素的镇痛作用。用格列本脲预处理以验证ATP敏感性钾通道是否参与尿囊素的镇痛作用。通过角叉菜胶诱导的爪肿胀和胸膜炎试验评估EMN和尿囊素的抗炎活性。
EMN(250、500和1000mg/kg,口服)治疗可抑制醋酸和福尔马林(两个阶段)诱导的伤害感受。然而,仅在500和1000mg/kg剂量下,甩尾试验的潜伏期时间增加。这些结果表明外周和中枢镇痛机制均参与其中。尿囊素(40、60和80mg/kg,口服)治疗在福尔马林诱导的伤害感受试验的两个阶段均产生剂量依赖性镇痛作用;尿囊素(60mg/kg)不能增加甩尾试验的潜伏期时间。在福尔马林试验第一阶段,用纳洛酮预处理可完全逆转EMN(1000mg/kg)和尿囊素(60mg/kg)的作用;格列本脲可逆转尿囊素的作用。EMN(250、500和1000mg/kg)和尿囊素(60mg/kg)给药在整个角叉菜胶诱导的爪肿胀中均显示出显著的抗炎活性。此外,EMN和尿囊素减少了白细胞向胸腔的迁移和胸腔渗出液。
EMN具有显著的镇痛和抗炎作用,这似乎至少部分归因于尿囊素的存在。然而,尿囊素并非EMN中枢镇痛活性的原因。尿囊素具有外周镇痛活性,涉及阿片受体和ATP敏感性钾通道。阿片受体也参与EMN的镇痛活性。这些发现支持了诺多记忆木在民间医学中的应用,并表明该植物具有开发镇痛和抗炎植物药的治疗潜力。