Instituto de Ciências Biológicas, Departamento de Bioquímica e Imunologia, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.
Programa de Pós-Graduação em Medicamentos e Assistência Farmacêutica, Departamento de Farmácia Social, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, Minas Gerais, Brazil.
Adv Nutr. 2021 Dec 1;12(6):2232-2243. doi: 10.1093/advances/nmab064.
The search for new antiobesogenic agents is increasing because of the current obesity pandemic. Capsaicin (Caps), an exogenous agonist of the vanilloid receptor of transient potential type 1 (TRPV1), has shown promising results in the treatment of obesity. This scoping review aims to verify the pathways mediating the effects of Caps in obesity and the different methods adopted to identify these pathways. The search was carried out using data from the EMBASE, MEDLINE (PubMed), Web of Science, and SCOPUS databases. Studies considered eligible evaluated the mechanisms of action of Caps in obesity models or cell types involved in obesity. Nine studies were included and 100% (n = 6) of the in vivo studies showed a high risk of bias. Of the 9 studies, 66.6% (n = 6) administered Caps orally in the diet and 55.5% (n = 5) used a concentration of Caps of 0.01% in the diet. In vitro, the most tested concentration was 1 μM (88.9%; n = 8). Capsazepine was the antagonist chosen by 66.6% (n = 6) of the studies. Seven studies (77.8%) linked the antiobesogenic effects of Caps to TRPV1 activation and 3 (33.3%) indicated peroxisome proliferator-activated receptor (PPAR) involvement as an upstream connection to TRPV1, rather than a direct metabolic target of Caps. The main secondary effects of Caps were lower weight gain (33.3%; n = 3) or loss (22.2%; n = 2), greater improvement in lipid profile (33.3%; n = 3), lower white adipocyte adipogenesis (33.3%; n = 3), browning process activation (44.4%; n = 4), and higher brown adipocyte activity (33.3%; n = 3) compared with those of the control treatment. Some studies have shown that PPAR agonists modulate TRPV1 activity, and no study has evaluated the simultaneous antagonism of these 2 receptors. Consequently, further studies are necessary to elucidate the role of each of these signaling molecules in the antiobesogenic effects of Caps.
由于当前的肥胖流行,寻找新的抗肥胖因子的研究正在增加。辣椒素(Caps)是瞬时电位型 1 型香草素受体(TRPV1)的外源性激动剂,在肥胖症的治疗中显示出了有前景的结果。本范围界定综述旨在验证 Caps 在肥胖症中发挥作用的途径,以及用于识别这些途径的不同方法。该检索使用了来自 EMBASE、MEDLINE(PubMed)、Web of Science 和 SCOPUS 数据库的数据进行。符合条件的研究评估了 Caps 在肥胖模型或肥胖相关细胞类型中的作用机制。共纳入了 9 项研究,其中 100%(n=6)的体内研究存在较高的偏倚风险。在这 9 项研究中,有 66.6%(n=6)通过饮食给予 Caps 口服,55.5%(n=5)使用饮食中 0.01%的 Caps 浓度。在体外,测试的最常见浓度为 1μM(88.9%;n=8)。有 66.6%(n=6)的研究选择了辣椒素作为拮抗剂。有 7 项研究(77.8%)将 Caps 的抗肥胖作用与 TRPV1 的激活联系起来,有 3 项研究(33.3%)表明过氧化物酶体增殖物激活受体(PPAR)参与 TRPV1 作为上游连接,而不是 Caps 的直接代谢靶标。Caps 的主要次要作用是体重增加减少(33.3%;n=3)或降低(22.2%;n=2)、改善脂质谱(33.3%;n=3)、降低白色脂肪细胞脂肪生成(33.3%;n=3)、激活棕色脂肪细胞褐色化过程(44.4%;n=4)和提高棕色脂肪细胞活性(33.3%;n=3)与对照组相比。一些研究表明,PPAR 激动剂可调节 TRPV1 的活性,且尚无研究评估这两种受体的同时拮抗作用。因此,需要进一步的研究来阐明这些信号分子在 Caps 的抗肥胖作用中的作用。