A wide array of therapeutic effects has been exhibited by compounds isolated from natural sources. “Bio-actives of endophytic origin” is a recently explored area that came into recognition over the last 2 decades. Literature search on the secondary metabolites of endophytes have shown several pharmacologically active compounds especially anti-inflammatory compounds, which have been reviewed in the present paper. The article is structured based on the chemical classification of secondary metabolites. The compounds were identified to possess activity against a total of 16 anti-inflammatory targets. The most common targets involved were NO, TNF-α, and inhibition of total ROS. Further, the article gives a detailed insight into the compounds, their endophytic source, and anti-inflammatory target as well as potency. The contents of the article cover all the scientific reports published until Feb. 2019. Thus 118 compounds and 6 extracts have been reported to be obtained from endophytic sources showing anti-inflammatory activities. Amongst these, herbarin, periconianone A, and periconianone B were identified as the most potent compounds in terms of their IC50 values against NO inhibition.