Ethnopharmacological relevance Kalimeris indica is a Miao׳s medicinal plant in Guizhou province of China employing to treat various inflammation-related diseases in clinical. The study aims to determine the active fractions of K. indica for its anti-inflammatory activity and to identify their chemical constituents. Material and methods The dried K. indica herb was extracted with 50% aqueous ethanol and then successively separated with macroporous resin and MCI column chromatography to give five fractions (A–E). The anti-inflammatory effects were determined by measuring the NO and TNF-α production in murine macrophage RAW 264.7 cells after exposure to LPS. The chemical constituents of the anti-inflammatory fractions were analyzed by the method of UHPLC-ESI-Q-TOF/MS or GC–MS. Results Five fractions (A–E) of different polarities were prepared from the 50% ethanol extract. Factions C and E showed significant inhibition of NO and TNF-α production. Six constituents, namely 3,4-dicaffeoylquinic acid ( 1 ), 3,5-dicaffeoylquinic acid ( 2 ), 1,5-dicaffeoylquinic acid ( 3 ), rutin ( 4 ), 1-malonyl-3,5-dicaffeoylquinic acid ( 5 ), and 4,5-dicaffeoylquinic acid ( 6 ) were identified from the active fraction C by UHPLC-ESI-Q-TOF/MS. Four compounds including 13-tetradecenal ( 7 ), ( Z , Z )-9,12-octadecadienoic acid ( 8 ), (3α)-12-oleanen-3-yl acetate ( 9 ), and (+)-3-oxo-urs-12-en-24-oic acid methyl ester ( 10 ) were identified from the active fraction E by GC–MS. Conclusion K. indica possessed pronounced anti-inflammatory effect. Dicaffeoylquinic acids and their dirivatives, rutin, as well as oleanolic and fatty acid derivatives are the major constituents and possibly the anti-inflammatory principles of the active fractions of K. indica . All the compounds were identified in K. indica for the first time. The work provided evidence for further development and utilization of K. indica and formed a basis for the establishment of quality control methods and standards for K. indica and its pharmaceutical preparations. [ABSTRACT FROM AUTHOR]