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从 f. Pilosa Ohwi 中分离的化合物的提取物和合成衍生物对小鼠神经病理性疼痛的影响。

Effect of Extract and Synthesized Derivatives of Isolated Compound from f. Pilosa Ohwi on Neuropathic Pain in Mice.

机构信息

Department of Food Science and Nutrition, Hallym University, 1 Hallymdeahak-gil, Chuncheon 24252, Korea.

R&D Center, Frontbio Inc., 32 Soyanggang-ro, Chuncheon 24232, Gangwon-do, Korea.

出版信息

Molecules. 2021 Mar 15;26(6):1639. doi: 10.3390/molecules26061639.

Abstract

Neuropathic pain is described as the "most terrible of all tortures that a nerve wound may inflict." The aim of the present study was to demonstrate the antinociceptive effect of f. pilosa Ohwi water extract (SCW) and synthesized derivatives of the isolated compound. The antinociceptive effect was tested using the acetic acid-induced writhing and 5% formalin tests. Antinociceptive effects on neuropathic pain were evaluated using the von Frey test with chronic constriction injury (CCI) and surgical nerve injury (SNI) models and tail-flick test with a vincristine-induced pain model. An Ames test was also conducted. 5-hydroxymethylfurfural (5-HMF) was isolated and derivatives were synthesized with various acid groups. Among the plant water extracts, SCW showed significantly effective activity. Additionally, SCW presented antinociceptive effects in the neuropathic pain models. The SCW water fraction resulted in fewer writhes than the other fractions, and isolated 5-HMF was identified as an effective compound. Because 5-HMF revealed a positive response in the Ames test, derivatives were synthesized. Among the synthesized derivations, 5-succinoxymethylfurfural (5-SMF) showed the best effect in the neuropathic pain model. Our data suggest that SCW and the synthesized compound, 5-SMF, possess effective antinociceptive activity against neuropathic pain.

摘要

神经病理性疼痛被描述为“神经损伤可能造成的所有痛苦中最可怕的一种”。本研究旨在展示 f. pilosa Ohwi 水提取物 (SCW) 和分离化合物的合成衍生物的镇痛作用。使用醋酸诱导的扭体和 5%甲醛试验测试镇痛作用。使用慢性缩窄性损伤 (CCI) 和手术神经损伤 (SNI) 模型的冯弗雷测试和长春新碱诱导疼痛模型的尾巴闪烁测试评估对神经病理性疼痛的镇痛作用。还进行了艾姆斯试验。分离出 5-羟甲基糠醛 (5-HMF),并用各种酸基合成衍生物。在植物水提取物中,SCW 表现出显著有效的活性。此外,SCW 在神经病理性疼痛模型中表现出镇痛作用。SCW 水馏分比其他馏分产生的扭体少,分离出的 5-HMF 被鉴定为有效化合物。由于 5-HMF 在艾姆斯试验中呈阳性反应,因此合成了衍生物。在合成的衍生物中,5-琥珀酰亚甲基糠醛 (5-SMF) 在神经病理性疼痛模型中表现出最佳效果。我们的数据表明,SCW 和合成化合物 5-SMF 对神经病理性疼痛具有有效的镇痛作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b5e9/7999106/8ab4c4c9deb9/molecules-26-01639-g001.jpg

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