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盐酸双(3-芳基-3-氧代丙基)甲胺在大鼠体内的抗炎活性

Anti-inflammatory activity of bis(3-aryl-3-oxo-propyl)methylamine hydrochloride in rat.

作者信息

Suleyman Halis, Gul Halise Inci, Gul Mustafa, Alkan Mustafa, Gocer Fatma

机构信息

Department of Pharmacology, Faculty of Medicine, Ataturk University, Erzurum, Turkey.

出版信息

Biol Pharm Bull. 2007 Jan;30(1):63-7. doi: 10.1248/bpb.30.63.

Abstract

In this study the effects of compound B1, bis(3-aryl-3-oxo-propyl)methylamine hydrochloride, and an anti-inflammatory drug, indomethacin, were tested by carrageenan-induced paw edema and cotton pellet granuloma tests, for effects on acute and chronic phases of inflammation, respectively. Their effects on vascular permeability were also determined by hyaluronidase-induced capillary permeability test. Anti-inflammatory activity of B1 was compared with indomethacin. B1 decreased the carrageenan-induced paw edema by 49%, 35%, and 47% at 50, 100, and 200 mg kg(-1) doses, respectively, while this decrease was 82% by indomethacin at 20 mg kg(-1) dose. Antiproliferative effects in cotton pellet test of B1 at 50 mg kg(-1) and indomethacin at 20 mg kg(-1) doses were 44% and 43%, respectively. Indomethacin but not B1 inhibited the hyaluronidase-induced increase in capillary permeability. Our results suggest that B1 inhibits both acute and chronic phases of inflammation probably by an effect not mediated by prevention of increased capillary permeability. Especially, its anti-inflammatory activity against chronic phase of inflammation was comparable with that of indomethacin. Further detailed studies are needed to clarify the mechanism(s) of action responsible for the anti-inflammatory activity of B1.

摘要

在本研究中,通过角叉菜胶诱导的爪肿胀试验和棉球肉芽肿试验,分别测试了化合物B1(双(3-芳基-3-氧代丙基)甲胺盐酸盐)和一种抗炎药物吲哚美辛对炎症急性期和慢性期的影响。还通过透明质酸酶诱导的毛细血管通透性试验测定了它们对血管通透性的影响。将B1的抗炎活性与吲哚美辛进行了比较。B1在50、100和200mg kg(-1)剂量下,分别使角叉菜胶诱导的爪肿胀降低了49%、35%和47%,而吲哚美辛在20mg kg(-1)剂量下使肿胀降低了82%。B1在50mg kg(-1)剂量和吲哚美辛在20mg kg(-1)剂量下对棉球试验中的抗增殖作用分别为44%和43%。吲哚美辛而非B1抑制了透明质酸酶诱导毛细血管通透性的增加。我们的数据表明,B1可能通过一种不依赖于防止毛细血管通透性增加介导的作用来抑制炎症的急性期和慢性期。特别是,其对炎症慢性期的抗炎活性与吲哚美辛相当。需要进一步详细研究来阐明负责B1抗炎活性的作用机制。

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