A novel gedunin-2-hydroxypropyl-β-cyclodextrin inclusion complex improves anti-nociceptive and anti-inflammatory activities of gedunin in rodents.

Q4 Medicine
Mary Olufunmilayo Ologe
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Abstract

Gedunin is a bioactive compound, obtained from Entandrophragma angolense (EA), which has limited therapeutic usefulness due to poor aqueous solubility and first-pass effects. Cyclodextrins are cyclic oligosaccharides that form complexes with poorly soluble compounds, thus enhancing their pharmacological activity. In this article, we evaluated the pharmacological activities of gedunin-2-hydroxypropyl-β-cyclodextrin complex (GCD) in rodents. The antinociceptive activity of GCD (50, 100, 200 mg/kg) and Gedunin (50mg/kg) was tested in acetic acid-induced writhing and formalin-induced paw licking in mice. The anti-inflammatory activity was investigated in carrageenan-induced paw oedema and air pouch inflammation models in rats. Leucocytes counts, Tumour Necrosis Factor-alpha (TNF-α) level, nitric oxide, malondialdehyde, reduced glutathione, and myeloperoxidase enzyme activities were assessed in the air pouch exudate. The GCD (200mg/kg) significantly decreased writhing response, reduced licking duration and decreased oedema compared with gedunin and control. Exudate volume and leucocyte count were significantly reduced by GCD (200 mg/kg), it decreased myeloperoxidase activity and inhibited TNF-α release. The carrageenan-induced GSH depletion, increased malondialdehyde and nitrite levels were significantly reversed by GCD (200 mg/kg) relative to gedunin and control.  The GCD complex demonstrated significant antinociceptive and anti-inflammatory activities relative to gedunin alone via mechanisms associated with inhibition of oxidative stress and inflammation in rodents.

一种新型的根茎素-2-羟丙基-β-环糊精包合物提高根茎素在啮齿动物体内的抗伤害和抗炎活性。
geduin是一种生物活性化合物,从安哥拉内参(EA)中获得,由于水溶性差和首过效应,其治疗作用有限。环糊精是一种环状低聚糖,与难溶性化合物形成复合物,从而增强其药理活性。在本文中,我们评估了geidin -2-羟丙基-β-环糊精复合物(GCD)在啮齿动物中的药理活性。以乙酸致小鼠扭体和福尔马林致小鼠舔爪为实验对象,观察GCD(50、100、200 mg/kg)和根茎苷(50mg/kg)的抗伤感受活性。采用角叉菜胶致大鼠足跖水肿和气袋炎症模型,观察其抗炎活性。评估白细胞计数、肿瘤坏死因子α (TNF-α)水平、一氧化氮、丙二醛、还原性谷胱甘肽和髓过氧化物酶活性。与根茎素和对照组相比,GCD (200mg/kg)显著降低了小鼠的扭动反应,缩短了舔食时间,减少了水肿。GCD (200 mg/kg)可显著降低白细胞计数、降低骨髓过氧化物酶活性、抑制TNF-α释放。GCD (200 mg/kg)可显著逆转卡拉胶诱导的GSH消耗、丙二醛和亚硝酸盐水平升高。在啮齿类动物中,GCD复合物通过与氧化应激和炎症抑制相关的机制,显示出与单独的根茎苷相比显著的抗伤和抗炎活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Nigerian Journal of Physiological Sciences
Nigerian Journal of Physiological Sciences Medicine-Physiology (medical)
CiteScore
0.80
自引率
0.00%
发文量
23
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