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(Z)-2-(5-氯-2-氧代吲哚啉-3-亚基)-N-苯基-肼甲硫酰胺在小鼠体内的抗炎和镇痛作用。

Anti-inflammatory and antinociceptive effects of the isatin derivative (Z)-2-(5-chloro-2-oxoindolin-3-ylidene)-N-phenyl-hydrazinecarbothioamide in mice.

机构信息

Programa de Pós-Graduação em Desenvolvimento e Inovação Tecnológica em Medicamentos, Universidade Federal do Rio Grande do Norte, Natal, RN, Brasil.

Programa de Pós-Graduação em Bioquímica, Universidade Federal do Rio Grande do Norte, Natal, RN, Brasil.

出版信息

Braz J Med Biol Res. 2020;53(10):e10204. doi: 10.1590/1414-431X202010204. Epub 2020 Sep 7.

DOI:10.1590/1414-431X202010204
PMID:32901685
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7485313/
Abstract

Several isatin derivatives have shown important biological activities, which have attracted interest from researchers. For this reason, the present study aimed to evaluate the anti-inflammatory and antinociceptive effects of the isatin derivative (Z)-2-(5-chloro-2-oxoindolin-3-ylidene)-N-phenyl-hydrazinecarbothioamide (COPHCT) in mice. Three doses of this compound were tested: 1.0, 2.5, and 5.0 mg/kg. The anti-inflammatory activity was assessed using the carrageenan-induced paw edema model and the zymosan-induced air pouch model. The evaluation of the antinociceptive effect was performed through the formalin test and the acetic acid-induced abdominal writhing test. The paw edema assay demonstrated that all doses of the compound showed a significant reduction of the edema in the second hour evaluated, but a better response was observed in the fourth hour. The zymosan-induced air pouch model indicated that the compound, in all doses, significantly reduced leukocyte migration and total protein concentration levels. In the formalin test, the doses 1.0, 2.5, and 5.0 mg/kg of COPHCT showed activity only in the second phase, with reduction in paw pain time of 73.61, 79.46, and 73.85%, respectively. The number of abdominal writhings decreased with the increasing dose, but only 5.0 mg/kg COPHCT exhibited a significant response, with a reduction of 24.88%. These results demonstrated the ability of this compound to interfere in the anti-inflammatory activity of edema, vascular permeability, and cell migration. In addition, its possible antinociceptive effect may be related to the dose used.

摘要

几种色胺衍生物表现出重要的生物活性,引起了研究人员的兴趣。因此,本研究旨在评估色胺衍生物(Z)-2-(5-氯-2-氧代吲哚啉-3-亚基)-N-苯基-肼甲硫酰胺(COPHCT)在小鼠中的抗炎和镇痛作用。测试了该化合物的三个剂量:1.0、2.5 和 5.0mg/kg。使用角叉菜胶诱导的足肿胀模型和酵母聚糖诱导的气囊模型评估抗炎活性。通过福马林试验和醋酸诱导的腹部扭体试验评估镇痛作用。足肿胀试验表明,化合物的所有剂量在评估的第二小时均显著减少了水肿,但在第四小时观察到更好的反应。酵母聚糖诱导的气囊模型表明,该化合物在所有剂量下均显著降低了白细胞迁移和总蛋白浓度水平。在福马林试验中,COPHCT 的 1.0、2.5 和 5.0mg/kg 剂量仅在第二阶段表现出活性,分别减少了 73.61%、79.46%和 73.85%的足痛时间。随着剂量的增加,腹部扭动的次数减少,但只有 5.0mg/kg 的 COPHCT 表现出显著的反应,减少了 24.88%。这些结果表明该化合物能够干扰水肿、血管通透性和细胞迁移的抗炎活性。此外,其可能的镇痛作用可能与所用剂量有关。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/eb2d5a966966/1414-431X-bjmbr-53-10-e10204-gf006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/06be02401cc8/1414-431X-bjmbr-53-10-e10204-gf001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/7d5df847bab2/1414-431X-bjmbr-53-10-e10204-gf002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/0ac0639f1dc8/1414-431X-bjmbr-53-10-e10204-gf003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/e65f1b96d957/1414-431X-bjmbr-53-10-e10204-gf004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/07e1efaa33fe/1414-431X-bjmbr-53-10-e10204-gf005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/eb2d5a966966/1414-431X-bjmbr-53-10-e10204-gf006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/06be02401cc8/1414-431X-bjmbr-53-10-e10204-gf001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/7d5df847bab2/1414-431X-bjmbr-53-10-e10204-gf002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/0ac0639f1dc8/1414-431X-bjmbr-53-10-e10204-gf003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/e65f1b96d957/1414-431X-bjmbr-53-10-e10204-gf004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/07e1efaa33fe/1414-431X-bjmbr-53-10-e10204-gf005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c27b/7485313/eb2d5a966966/1414-431X-bjmbr-53-10-e10204-gf006.jpg

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