To investigate the chemical constituents of Clerodendrum yunnanense Hu ex Hand.-Mazz. and their antimalarial activity, isolation, purification, and identification were conducted for acetone extract from the above-ground parts of C. yunnanense by using multiple chromatographic methods and spectroscopic technologies such as nuclear magnetic resonance and mass spectrometry, and their in vitro antimalarial activity was determined with the SYBR Green Ⅰ method. The results show that 11 compounds are identified, namely hispidulin (1), luteolin (2), p-hydroxybenzoic acid (3), p-methoxybenzoic acid (4), p-hydroxy-acetophenone (5), 3, 4-dihydroxybenzoic acid methyl ester (6), 4-hydroxy-3, 5-dimethoxybenzaldehyde (7), cis-p-hydroxy cinnamic acid (8), trans-p-hydroxy cinnamic acid (9), ferulic acid (10), and palmitic acid (11). All the above compounds are isolated from C. yunnanense for the first time. Compounds 1 and 2 show a certain inhibitory activity against the Plasmodium falciparum Welch 3D7 strain, with the half-maximal inhibitory concentrations (IC50) of 7.092 and 16.190 μmol·L^-1, respectively.