1. Flavonoids regulate tumor-associated macrophages – From structure-activity relationship to clinical potential (Review).
- Author
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Sun, Qi, Liu, Qi, Zhou, Xintong, Wang, Xiaomin, Li, Huayao, Zhang, Wenfeng, Yuan, Hailian, and Sun, Changgang
- Subjects
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STRUCTURE-activity relationships , *FLAVONOIDS , *MACROPHAGES , *TUMOR microenvironment , *CHEMICAL structure , *ANTINEOPLASTIC agents - Abstract
In recent years, the strategy for tumor therapy has changed from focusing on the direct killing effect of different types of therapeutic agents on cancer cells to the new mainstream of multi-mode and -pathway combined interventions in the microenvironment of the developing tumor. Flavonoids, with unique tricyclic structures, have diverse and extensive immunomodulatory and anti-cancer activities in the tumor microenvironment (TME). Tumor-associated macrophages (TAMs) are the most abundant immunosuppressive cells in the TME. The regulation of macrophages to fight cancer is a promising immunotherapeutic strategy. This study covers the most comprehensive cognition of flavonoids in regulating TAMs so far. Far more than a simple list of studies, we try to dig out evidence of crosstalk at the molecular level between flavonoids and TAMs from literature, in order to discuss the most relevant chemical structure and its possible relationship with the multimodal pharmacological activity, as well as systematically build a structure-activity relationship between flavonoids and TAMs. Additionally, we point out the advantages of the macro-control of flavonoids in the TME and discuss the potential clinical implications as well as areas for future research of flavonoids in regulating TAMs. These results will provide hopeful directions for the research of antitumor drugs, while providing new ideas for the pharmaceutical industry to develop more effective forms of flavonoids. [Display omitted] • The most comprehensive cognition of flavonoids in regulating TAMs so far. • Flavonoids regulate macrophage recruitment, reprogramming, and activity. • Chemical structure determining the activity and efficacy between flavonoids and TAMs. • The multi-target effect of flavonoids makes them affect the TME. [ABSTRACT FROM AUTHOR]
- Published
- 2022
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