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酒石酸依格列净对控制炎性疼痛的作用。

The Effect of Evogliptin Tartrate on Controlling Inflammatory Pain.

作者信息

Cho Pyung Goo, Jang Jun Ho, Ko Sukjin, Shin Dong Ah, Chung Seungsoo, Chang Min Cheol

机构信息

Department of Neurosurgery, Ajou University Medical Center, Suwon-si 16499, Republic of Korea.

BnH Research Co., Ltd., Goyang-si 10594, Gyeonggi-do, Republic of Korea.

出版信息

Biomedicines. 2023 Nov 7;11(11):2990. doi: 10.3390/biomedicines11112990.

Abstract

: Evogliptin tartrate inhibits dipeptidyl peptidase-4 (DPP-4), boosting glucagon-like peptide 1 (GLP-1) secretion and improving insulin release and glucose tolerance, while also exerting anti-inflammatory effects. We investigated its anti-inflammatory and analgesic effects. : Forty male Sprague Dawley rats were divided into (N = 10 in each): (1) naïve, (2) complete Freund's adjuvant (CFA) inflammation + evogliptin tartrate (once for 10 mg/kg) (CFAE), (3) CFA + vehicle (same volume with normal saline with evogliptin tartrate/once) (CFAV), and (4) CFA + indomethacin (5 mg/mL/kg/1 time) (CFAI) groups. CFA was injected subcutaneously into rat plantar regions, and medications (evogliptin tartrate, vehicle, and indomethacin) were administered orally for 5 days. Post treatment, blood from the heart and plantar inflammatory tissue were collected to assess inflammatory cytokines. Evogliptin tartrate effects on controlling inflammation and pain were evaluated by measuring rat plantar paw thickness, paw withdrawal threshold, dorsal root ganglion (DRG) resting membrane potential, DRG action potential firing, and cytokine (TNF-α and IL-1β) levels. : Compared with the naïve group, plantar paw thickness, cytokine (TNF-α and IL-1β) levels, DRG resting membrane potential, and DRG action potential firing increased, whereas the paw withdrawal threshold decreased in all CFA groups. However, CFAE and CFAI rats showed recovery. The degree of CFAE recovery resembled that observed in the CFAI group. : Evogliptin tartrate mirrored the anti-inflammatory pain relief of indomethacin. We aim to broaden its use as an anti-inflammatory drug or pain relief drug.

摘要

酒石酸依格列净抑制二肽基肽酶-4(DPP-4),促进胰高血糖素样肽-1(GLP-1)分泌,改善胰岛素释放和葡萄糖耐量,同时还具有抗炎作用。我们研究了其抗炎和镇痛作用。:将40只雄性Sprague Dawley大鼠分为(每组N = 10):(1)未处理组,(2)完全弗氏佐剂(CFA)炎症+酒石酸依格列净(一次,10 mg/kg)(CFAE)组,(3)CFA+赋形剂(与含酒石酸依格列净的生理盐水等体积/一次)(CFAV)组,和(4)CFA+吲哚美辛(5 mg/mL/kg/1次)(CFAI)组。将CFA皮下注射到大鼠足底区域,口服给药(酒石酸依格列净、赋形剂和吲哚美辛)5天。治疗后,采集心脏血液和足底炎症组织以评估炎性细胞因子。通过测量大鼠足底爪厚度、爪退缩阈值、背根神经节(DRG)静息膜电位、DRG动作电位发放以及细胞因子(TNF-α和IL-1β)水平来评估酒石酸依格列净对控制炎症和疼痛的作用。:与未处理组相比,所有CFA组的足底爪厚度、细胞因子(TNF-α和IL-1β)水平、DRG静息膜电位和DRG动作电位发放均增加,而爪退缩阈值降低。然而,CFAE组和CFAI组大鼠显示恢复。CFAE组的恢复程度与CFAI组相似。:酒石酸依格列净与吲哚美辛的抗炎止痛作用相似。我们旨在扩大其作为抗炎药或镇痛药的用途。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/506d/10669149/dac3be0bc4c2/biomedicines-11-02990-g001.jpg

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