Piracicaba Dental School, Department of Physiological Sciences, University of Campinas, 901 Limeira Ave., 13414-903 Piracicaba, SP, Brazil.
University of Florida College of Dentistry, Department of Oral Biology, 1395 Center Drive, 32610 Gainesville, Florida, United States.
Eur J Med Chem. 2018 Jun 10;153:49-55. doi: 10.1016/j.ejmech.2017.06.050. Epub 2017 Jun 27.
Anti-Inflammatory drugs have been routinely used in the management of acute and chronic inflammatory conditions. Nevertheless, their undesirable side and adverse effects have encouraged the development of more selective, tolerable and efficacious drugs able to modulate the inflammatory process through distinct mechanisms than those of drugs currently available in the market, for instance, inhibition of leukocyte recruitment (chemotaxis, rolling, adhesion and transmigration). Natural products, including Brazilian propolis, have been considered a rich source of anti-inflammatory molecules due to a very complex phytochemical diversity. Brazil has at least thirteen distinct types of propolis and many bioactive compounds have been isolated therefrom, such as apigenin, artepillin C, vestitol, neovestitol, among others. These molecules were proven to play a significant immunomodulatory role through (i) inhibition of inflammatory cytokines (e.g. TNF-α) and chemokines (CXCL1/KC and CXCL2/MIP2); (ii) inhibition of IκBα, ERK1/2, JNK and p38MAPK phosphorylation; (iii) inhibition of NF-κB activation; and (iv) inhibition of neutrophil adhesion and transmigration (ICAM-1, VCAM-1 and E-selectin expression). In this review, we shed light on the new advances in the research of compounds isolated from Brazilian propolis from Apis mellifera bees as potentially novel anti-inflammatory drugs. The compilation of data and insights presented herein may open further avenues for the pharmacological management of oral and systemic inflammatory conditions. Further research should focus on clinical and acute/chronic toxicological validation of the most promising compounds described in this review.
抗炎药物已被常规用于治疗急性和慢性炎症性疾病。然而，其不理想的副作用和不良反应促使人们开发出更具选择性、耐受性和疗效的药物，这些药物能够通过与现有市场上药物不同的机制来调节炎症过程，例如抑制白细胞募集（趋化、滚动、黏附和迁移）。天然产物，包括巴西蜂胶，由于其非常复杂的植物化学成分多样性，被认为是抗炎分子的丰富来源。巴西至少有 13 种不同类型的蜂胶，从中分离出许多生物活性化合物，如芹菜素、artepillin C、vestitol、neovestitol 等。这些分子已被证明通过以下方式发挥重要的免疫调节作用：（i）抑制炎症细胞因子（如 TNF-α 和趋化因子（CXCL1/KC 和 CXCL2/MIP2）；（ii）抑制 IκBα、ERK1/2、JNK 和 p38MAPK 磷酸化；（iii）抑制 NF-κB 激活；和（iv）抑制中性粒细胞黏附和迁移（ICAM-1、VCAM-1 和 E-选择素表达）。在这篇综述中，我们介绍了从巴西蜂胶中分离得到的化合物作为潜在新型抗炎药物的研究新进展。本文呈现的数据和见解可能为口腔和全身性炎症性疾病的药理学治疗开辟新的途径。进一步的研究应集中在对本文所述最有前途的化合物进行临床和急性/慢性毒理学验证上。
