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水杨醛 2-氯苯甲酰腙(H(2)LASSBio-466)、水杨醛 4-氯苯甲酰腙(H(2)LASSBio-1064)及其锌(II)配合物的镇痛和抗炎活性。

Analgesic and anti-inflammatory activities of salicylaldehyde 2-chlorobenzoyl hydrazone (H(2)LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H(2)LASSBio-1064) and their zinc(II) complexes.

机构信息

LaFI Laboratório de Farmacologia e Imunidade, Instituto de Ciências Biológicas e da Saúde, Universidade Federal de Alagoas, Maceió, AL, Brazil.

出版信息

Molecules. 2011 Aug 15;16(8):6902-15. doi: 10.3390/molecules16086902.

Abstract

Salicylaldehyde 2-chlorobenzoyl hydrazone (H(2)LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H(2)LASSBio-1064) and their complexes Zn(LASSBio-466)H(2)O (1) and Zn(HLASSBio-1064)Cl (2) were evaluated in animal models of peripheral and central nociception, and acute inflammation. All studied compounds significantly inhibited acetic acid-induced writhing response. Upon coordination the anti-nociceptive activity was favored in the complex 1. H(2)LASSBio-466 inhibited only the first phase of the formalin test, while 1 was active in the second phase, like indomethacin, indicating its ability to inhibit nociception associated with the inflammatory response. Hence coordination to zinc(II) altered the pharmacological profile of H(2)LASSBio-466. H(2)LASSBio-1064 inhibited both phases but this effect was not improved by coordination. The studied compounds did not increase the latency of response in the hot plate model, indicating their lack of central anti-nociceptive activity. All compounds showed levels of inhibition of zymosan-induced peritonitis comparable or superior to indomethacin, indicating an expressive anti-inflammatory profile.

摘要

水杨醛 2-氯苯甲酰腙(H(2)LASSBio-466)、水杨醛 4-氯苯甲酰腙(H(2)LASSBio-1064)及其配合物[Zn(LASSBio-466)H(2)O](2)(1)和[Zn(HLASSBio-1064)Cl](2)(2)在周围和中枢痛觉模型以及急性炎症的动物模型中进行了评价。所有研究的化合物均显著抑制乙酸诱导的扭体反应。配位后,配合物 1 的抗伤害活性得到了增强。H(2)LASSBio-466 仅抑制福尔马林试验的第一阶段,而 1 与吲哚美辛一样,在第二阶段活跃,表明其抑制与炎症反应相关的伤害感受的能力。因此,与锌(II)配位改变了 H(2)LASSBio-466 的药理特性。H(2)LASSBio-1064 抑制了两个阶段,但这种效果没有通过配位得到改善。研究的化合物在热板模型中没有增加反应潜伏期,表明它们缺乏中枢抗伤害活性。所有化合物对酵母聚糖诱导的腹膜炎的抑制水平与吲哚美辛相当或优于吲哚美辛,表明具有明显的抗炎特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb23/6264688/af5f67ad5474/molecules-16-06902-g001.jpg

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