The constituents from aerial part of Cayratia albifolia and its anti-RA activities in vitro were studied. The ethanol extract of C. albifolia was isolated and identified by various chromatographic techniques and spectroscopy methods. Twenty compounds were isolated and elucidated as stigmastane-3,6-dione (1),sitostenone (2),β-sitosterol (3),daucosterol (4),betulinic acid (5),resveratrol (6),(E)-resveratrol 3-O-β-glucoside (7) and (Z)-resveratrol 3-O-β-glucoside (8),1H-indole-3-carboxylic acid (9),(3S,5R,6S,7E)-megastigma-7-ene-3,5,6,9-tetrol (10),ethyl β-D-glucopyranoside (11),6,7-dihydroxy-3,7-dimethyl-2-octenoic acid (12),2-deoxy-D-ribono-1,4-lactone (13),3,4-dihydroxybenzoic acid (14),pyrocatechol (15),adiadienedioic acid (16),9,12-linoleic acid-2′,3′-dihyodroxy propyl ester (17),nonadecanoic acid (18),n-hexadecanoic acid (19),and rel-5-(3S,8S-dihydroxy-1R,5S-dimethyl-7-oxa-6-oxobicyclo［3,2,1］oct-8-yl)-3-methyl-2Z,4E-pentadienoic acid (20). Compounds 1-20 were isolated from the plant for the first time,all compounds except 3 and 4 were isolated from this genus for the first time. MTT assay was used to study the anti-proliferation activity of the isolates against RA-FLS cells in vitro,and ELISA assay was used to determine the effects of the isolates on LPS induced production of TNF-α,IL-1β and IL-6 in RAW 264.7 cells. Compounds 1,15,19 and 20 showed anti RA-FLS activities with the IC₅₀ values of 23.07,26.92,23.59 and 19.22 μmol/L,respectively. Compounds 1,15,19 and 20 suppressed the production of TNF-α with IC₅₀ values of 13.58,18.51,13.45 and 9.58 μmol/L,respectively,and compounds 15 and 20 inhibited the production of IL-1β and IL-6 with IC₅₀ values of 13.56,17.30 and 14.42,8.71 μmol/L,respectively.