7-Chloro-4-phenylsulfonyl quinoline，一种新的抗伤害和消炎分子：一种具有药理活性的喹啉衍生物的结构改进。,Regulatory Toxicology and Pharmacology

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7-Chloro-4-phenylsulfonyl quinoline，一种新的抗伤害和消炎分子：一种具有药理活性的喹啉衍生物的结构改进。
Regulatory Toxicology and Pharmacology ( IF 3.0 ) Pub Date : 2017-08-27 , DOI: 10.1016/j.yrtph.2017.08.014
Mikaela P Pinz ₁ , Angélica S Reis ₁ , Renata Leivas de Oliveira ₁ , Guilherme T Voss ₁ , Ane G Vogt ₁ , Manoela do Sacramento ₂ , Juliano A Roehrs ₂ , Diego Alves ₂ , Cristiane Luchese ₁ , Ethel A Wilhelm ₁

Affiliation

本研究旨在检查7-氯-4-苯基磺酰基喹啉（PSOQ）的抗伤害感受和抗炎作用。在进行乙酸，热板和野外试验之前30分钟，对小鼠进行口服（po）口服PSOQ（0.01-10 mg / kg），美洛昔康（10 mg / kg）预处理。PSOQ减少了乙酸引起的腹部扭动，而美洛昔康没有作用。处理不会改变热板测试的潜伏时间和开放视野测试中的运动/探索活动。为了评估口服PSOQ或美洛昔康（10 mg / kg）后的胃耐受性，在暴露于药物之前将小鼠禁食18 h。四小时后，评估病变的发展。在所评估的剂量和时间，PSOQ和美洛昔康不会诱发溃疡。的确，研究了PSOQ的抗炎和抗水肿特性。为此，在巴豆油施用前30分钟，用PSOQ（0.01-50 mg / kg；口服），美洛昔康（50 mg / kg；口服）对动物进行预处理。PSOQ和美洛昔康（50 mg / kg）减少了巴豆油在耳组织中引起的水肿形成和髓过氧化物酶活性。这些数据加在一起表明PSOQ发挥了急性抗炎和抗伤害感受的作用，表明它可能代表了未来新治疗策略发展的一种选择。

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7-Chloro-4-phenylsulfonyl quinoline, a new antinociceptive and anti-inflammatory molecule: Structural improvement of a quinoline derivate with pharmacological activity.

The present study was designed to examine the antinociceptive and anti-inflammatory effects of 7-chloro-4-phenylsulfonyl quinoline (PSOQ). Mice were orally (p.o) pretreated with PSOQ (0.01-10 mg/kg), meloxicam (10 mg/kg), 30 min prior to the acetic acid, hot-plate and open field tests. PSOQ reduced abdominal writhing induced by acetic acid, while meloxicam presented no effect. The latency time in the hot-plate test and locomotor/exploratory activities in the open field test were not altered by treatments. In order to evaluate the gastric tolerability after oral administration of PSOQ or meloxicam (10 mg/kg), mice were fasted for 18 h prior to drug exposure. Four hours later, the development of lesions was assessed. PSOQ and meloxicam did not induce ulcer at the dose and time evaluated. Indeed, anti-inflammatory and anti-edematogenic properties of PSOQ were investigated. For this, animals were pretreated with PSOQ (0.01-50 mg/kg; p.o.), meloxicam (50 mg/kg; p.o.), 30 min prior to croton oil application. PSOQ and meloxicam (50 mg/kg) diminished the edema formation and myeloperoxidase activity induced by croton oil in the ear tissue. Taken together these data demonstrated that PSOQ exerts acute anti-inflammatory and antinociceptive actions, suggesting that it may represent an alternative in the development of future new therapeutic strategies.

更新日期：2019-11-01

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