Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), CEP, 90610-000, Porto Alegre, RS, Brazil.
Laboratório de Bioquímica Farmacológica, Centro de Pesquisa Experimental (CPE), Hospital de Clínicas de Porto Alegre (HCPA-UFRGS), CEP, 90035-007, Porto Alegre, RS, Brazil.
J Ethnopharmacol. 2021 Apr 24;270:113610. doi: 10.1016/j.jep.2020.113610. Epub 2020 Nov 24.
Acmella oleracea (L.) R. K. Jansen (Asteraceae), known as jambú in Brazil, is used in traditional medicine as analgesic and for inflammatory conditions, characterized by the presence of N-alkylamides, mainly spilanthol. This bioactive compound is responsible for the above-described pharmacological properties, including sialagogue and anesthetic.
This study aimed to characterize the anti-inflammatory effects of A. oleracea leaves (AOEE-L) and flowers (AOEE-F) extracts, including an isolated alkylamide (spilanthol), using in vitro and in vivo models. The mechanism underlying this effect was also investigated.
Extracts were analyzed by HPLC-ESI-MS/MS in order to characterize the N-alkylamides content. AOEE-L, AOEE-F (25-100 μg/mL) and spilanthol (50-200 μM) were tested in vitro on VSMC after stimulation with hyperglycemic medium (25 mM glucose). Their effects over nitric oxide (NO) generation, chymase inhibition and expression, catalase (CAT), superoxide anion (SOD) radical activity were evaluated. After an acute administration of extracts (10-100 mg/mL) and spilanthol (6.2 mg/mL), the anti-inflammatory effects were evaluated by applying the formalin test in rats. Blood was collected to measure serum aminotransferases activities, NO activity, creatinine and urea.
A number of distinct N-alkylamides were detected and quantified in AOEE-L and AOEE-F. Spilanthol was identified in both extracts and selected for experimental tests. Hyperglycemic stimulation in VSMC promoted the expression of inflammatory parameters, including chymase, NO, CAT and SOD activity and chymase expression, all of them attenuated by the presence of the extracts and spilanthol. The administration of extracts or spilanthol significantly inhibited edema formation, NO production and cell tissue infiltration in the formalin test, without causing kidney and liver toxicity.
Taken together, these results provide evidence for the anti-inflammatory activity of leaves and flowers extracts of jambú associated distinctly with their chemical profile. The effects appear to be associated with the inhibition of chymase activity, suppression of the proinflammatory cytokine NO and antioxidant activities.
Acmella oleracea（L.）R. K. Jansen（菊科），在巴西被称为 jambú，被用于传统医学中作为镇痛药和治疗炎症性疾病，其特征在于存在 N-烷基酰胺，主要是 spilanthol。这种生物活性化合物是负责上述药理学特性的物质，包括唾液分泌和麻醉。
本研究旨在通过体外和体内模型，对 A. oleracea 叶（AOEE-L）和花（AOEE-F）提取物以及分离的烷基酰胺（spilanthol）的抗炎作用进行表征。还研究了这种作用的机制。
通过 HPLC-ESI-MS/MS 分析提取物，以表征 N-烷基酰胺的含量。AOEE-L、AOEE-F（25-100μg/mL）和 spilanthol（50-200μM）在高糖培养基（25mM 葡萄糖）刺激后，在 VSMC 中进行体外测试。评估它们对一氧化氮（NO）生成、糜蛋白酶抑制和表达、过氧化氢酶（CAT）、超氧化物阴离子（SOD）自由基活性的影响。在提取物（10-100mg/mL）和 spilanthol（6.2mg/mL）的急性给药后，通过在大鼠中应用福氏试剂测试评估抗炎作用。收集血液以测量血清氨基转移酶活性、NO 活性、肌酐和尿素。
在 AOEE-L 和 AOEE-F 中检测到并定量了多种不同的 N-烷基酰胺。在两种提取物中都鉴定出 spilanthol，并将其选为实验测试。高糖刺激 VSMC 促进了炎症参数的表达，包括糜蛋白酶、NO、CAT 和 SOD 活性以及糜蛋白酶表达，所有这些都被提取物和 spilanthol 减弱。提取物或 spilanthol 的给药显著抑制了福尔马林测试中的水肿形成、NO 产生和细胞组织浸润，且没有引起肾和肝毒性。
综上所述，这些结果为 jambú 叶和花提取物的抗炎活性提供了证据，这种活性与它们的化学特征明显相关。这些作用似乎与抑制糜蛋白酶活性、抑制促炎细胞因子 NO 和抗氧化活性有关。
