Anticancer, anti-inflammatory and analgesic activities of aminoalcohol-based quinoxaline small molecules.

Acta cirurgica brasileira Pub Date : 2024-08-05 eCollection Date: 2024-01-01 DOI:10.1590/acb395124

Jannyely Moreira Neri, Paula Emília Apolônio Siqueira, Ana Luiza Cabral de Sá Leitão Oliveira, Renata Mendonça Araújo, Raimundo Fernandes de Araújo Júnior, Agnes Andrade Martins, Isabelle de Lima Marques, Rafaela Alcindo Silva, Aurigena Antunes de Araújo, Fabrício Gava Menezes

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Abstract

Purpose: Bioactive molecules are relevant to fight cancer and associated conditions. Quinoxaline is a privileged N-heterocycle, notably as anticancer agents. Herein, we report the evaluation of the quinoxaline derivatives DEQX and OAQX as anticancer agents, as well as in function of their anti-inflammatory and analgesic activities.

Methods: Quinoxalines were synthesized and tested as anticancer agents based on cell viability and Annexin V-FITC apoptosis. Anti-inflammatory activity was evaluated from mouse carrageenan peritonitis and levels of interleukin (IL)-1β and tumor necrosis factor (TNF)-alfa for enzyme-linked immunosorbent assay. Hot-plate and acetic acid-induced writing test were employed to investigate analgesia.

Results: Both reduced the Ht-29 cell viability in a dependent-concentration manner (p < 0.001). Total apoptosis was detected for cells treated with 12.5 and 25 µg/mL of both the compounds for 24 and 48 h (all doses, p < 0.0001). DEQX (all doses, p < 0.01) and OAQX (all doses, p < 0.001) acted in leukocyte migration and decreased the IL-1β and TNF-β levels (p < 0.05). DEQX (all doses, p < 0.05) and OAQX (5mg/kg, p < 0.001) showed peripheral analgesic effect.

Conclusions: In-vitro and in-vivo results suggest that these quinoxalines are promising for application in pharmacological area due to their anticancer, anti-inflammatory, and peripheric analgesia.

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基于氨基醇的喹喔啉小分子的抗癌、抗炎和镇痛活性。

目的：生物活性分子对抗击癌症和相关疾病具有重要意义。喹喔啉是一种特殊的 N-杂环，尤其可用作抗癌剂。在此，我们报告了对喹喔啉衍生物 DEQX 和 OAQX 作为抗癌剂及其抗炎和镇痛活性的评估：方法：合成了喹喔啉类化合物，并根据细胞活力和 Annexin V-FITC 细胞凋亡情况对其进行了抗癌测试。根据小鼠卡拉胶腹膜炎和酶联免疫吸附试验中白细胞介素（IL）-1β和肿瘤坏死因子（TNF）-α的水平评估了抗炎活性。采用热板试验和醋酸诱导书写试验研究镇痛效果：结果：二者均以依赖浓度的方式降低了 Ht-29 细胞的活力（p < 0.001）。用 12.5 和 25 µg/mL 的两种化合物处理细胞 24 和 48 小时后，检测到细胞完全凋亡（所有剂量，p < 0.0001）。DEQX（所有剂量，p < 0.01）和 OAQX（所有剂量，p < 0.001）对白细胞迁移有作用，并降低了 IL-1β 和 TNF-β 的水平（p < 0.05）。DEQX（所有剂量，p < 0.05）和 OAQX（5 毫克/千克，p < 0.001）具有外周镇痛作用：体外和体内研究结果表明，这些喹喔啉类化合物具有抗癌、抗炎和外周镇痛作用，有望应用于药理学领域。

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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Acta cirurgica brasileira

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