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Objective: To screen out the potential LDH-A (Lactate dehydrogenase A,a novel potential molecular target for cancer therapy) inhibitors from Spatholobus suberectus[1,2].Methods: A bioassay-guided isolation method was applied.Solvent extraction,liquid-liquid partition,various column chromatography were employed for the isolation of bioactive compounds in S.suberectus,and the LDH-A inhibitory activities of the extracts,fractions together with the compounds isolated were evaluated by standard enzyme kinetic experiments.Results: Fifteen compounds were isolated and identified as Formononetin(1),Medicarpin(2),Liquiritigenin(3),Isoliquiritigenin(4),Stigrnast-4-en-3-one(5),Genistein(6),Vanillvlmethanol(7),Methyl ferulate(8),β-sitosterol(9),Daucosterol(10) ,Dihydrokaempferol(11),DalparvneneB(12),2-methoxy-4-(2,-hydroxylethyl)-phenyl-1-O-β-DGluco-pyranoside(13),3,4-dihydroxy-6-methoxyflavonol(14),7-hydroxy-2,4-dimethoxy flavan(15).Methyl ferulate(8) and DalparvneneB(12) were the first time to be isolated from this herb.Liquiritigenin (3),isoliquiritigenin (4) and 3,4-dihydroxy-6-methoxyflavonol (5)showed remakable and dose-dependent inhibitory activities on LDH-A (Figure 1C & 1D).