Guilherme Viviane A, Cunha Vanessa R R, de Paula Eneida, de Araujo Daniele R, Constantino Vera R L
Departamento de Bioquímica e Biologia Tecidual, Instituto de Biologia, Universidade Estadual de Campinas-UNICAMP, Campinas 13083-862, SP, Brazil.
Faculdade de Farmácia, Universidade Adventista de São Paulo-UNASP, Engenheiro Coelho 13448-900, SP, Brazil.
Pharmaceutics. 2022 Apr 25;14(5):934. doi: 10.3390/pharmaceutics14050934.
Coumaric acid (CouH), an antioxidant molecule assimilated by food consumption, was intercalated into layered double hydroxide (LDH) nanocarrier, having zinc and aluminium ions in the layers (LDH-Cou), to evaluate its pharmacological activity through in vitro and in vivo assays in mice. Therefore, the following tests were performed: coumarate delivery in saline solution, fibroblasts’ cell viability using neutral red, peritonitis induced by carrageenan, formalin test, acetic-acid-induced writhing, and tail-flick assay, for the non-intercalated CouH and the intercalated LDH-Cou system. Furthermore, different pharmacological pathways were also investigated to evaluate their possible anti-inflammatory and antinociceptive mechanisms of action, in comparison to traditionally used agents (morphine, naloxone, caffeine, and indomethacin). The LDH-Cou drug delivery system showed more pronounced anti-inflammatory effect than CouH but not more than that evoked by the classic non-steroidal anti-inflammatory drug (NSAID) indomethacin. For the analgesic effect, according to the tail-flick test, the treatment with LDH-Cou expressively increased the analgesia duration (p < 0.001) by approximately 1.7−1.8 times compared to CouH or indomethacin. Thus, the results pointed out that the LDH-Cou system induced in vivo analgesic and anti-inflammatory activities and possibly uses similar mechanisms to that observed for classic NSAIDs, such as indomethacin.
香豆酸（CouH）是一种通过食物摄入而被吸收的抗氧化分子，它被插层到层状双氢氧化物（LDH）纳米载体中，该纳米载体层中含有锌离子和铝离子（LDH-Cou），以通过对小鼠的体外和体内试验来评估其药理活性。因此，进行了以下试验：对未插层的CouH和插层的LDH-Cou体系进行香豆酸盐在盐溶液中的递送、使用中性红检测成纤维细胞的细胞活力、角叉菜胶诱导的腹膜炎、福尔马林试验、乙酸诱导的扭体反应以及甩尾试验。此外，还研究了不同的药理途径，以评估它们可能的抗炎和抗伤害感受作用机制，并与传统使用的药物（吗啡、纳洛酮、咖啡因和吲哚美辛）进行比较。LDH-Cou药物递送系统显示出比CouH更显著的抗炎作用，但不超过经典非甾体抗炎药（NSAID）吲哚美辛所引起的抗炎作用。对于镇痛作用，根据甩尾试验，与CouH或吲哚美辛相比，用LDH-Cou治疗可使镇痛持续时间显著增加（p < 0.001），约为1.7 - 1.8倍。因此，结果表明LDH-Cou体系在体内诱导了镇痛和抗炎活性，并且可能使用了与经典NSAIDs（如吲哚美辛）类似的机制。
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