Obesity is characterized by an adipose tissue mass expansion that presents a risk to health, associated with a chronic increase in circulating inflammatory mediators. Anti-inflammatory agents are an obesity alternative treatment. However, the lack of effective agents indicates the need to assess the mechanisms and identify effective therapeutic targets. The present work identified and described the mechanisms of action of anti-inflammatory agents in adipose tissue in experimental studies. The review was registered in the International Prospective Registry of Systematic Reviews (PROSPERO-CRD42020182897). The articles' selection was according to eligibility criteria (PICOS). The research was performed in PubMed, ScienceDirect, Scopus, Web of Science, VHL, and EMBASE. The methodological quality evaluation was assessed using SYRCLE. Initially, 1511 articles were selected, and at the end of the assessment, 41 were eligible. Among the anti-inflammatory agent classes, eight drugs, 28 natural, and five synthetic compounds were identified. Many of these anti-inflammatory agents act in metabolic pathways that culminate in the inflammatory cytokines expression reduction, decreasing the macrophages infiltration in white and adipose tissue and promoting the polarization process of type M1 to M2 macrophages. Thus, the article clarifies and systematizes these anti-inflammatory agents' mechanisms in adipose tissue, presenting targets relevant to future research on these pathways.