Macrophages M2 polarization have been taken as an anti-inflammatory progression during
inflammation. Natural plant-derived products, with potential therapeutic and preventive activities
against inflammatory diseases, have received increasing attention in recent years because of their whole
regulative effects and specific pharmacological activities. However, the molecular mechanisms about
how different kinds of natural compounds regulate macrophages polarization still unclear. Therefore, in
the current review, we summarized the detailed research progress on the active compounds derived
from herbal plants with regulating effects on macrophages, especially M2 polarization. These
natural occurring compounds including flavonoids, terpenoids, glycosides, lignans, coumarins, alkaloids,
polyphenols and quinones. In addition, we extensively discussed the cellular mechanisms underlying
the M2 polarization for each compound, which could provide potential therapeutic strategies
aiming macrophages M2 polarization.