Two new lignans (7 S ,7′ R ,8 S ,8′ R )-3,3′-dimethoxy-7,7′-epoxylignan-4,4′,9-triol 4- O -β-D-glucopyranoside ( 1 ) and 9- O -formylaviculin ( 2 ) together with other thirteen known secondary metabolites were isolated from the leaves of Antidesma hainanensis . Their chemical structures were determined using NMR, electrospray ionization (ESI)-MS, circular dichroism (CD) spectroscopic methods, and as well as by comparison with those reported in the literature. Neuro-inflammatory activity of isolated compounds was evaluated by their inhibition on nitric oxide (NO) production in activated BV2 microglial cells. At concentration of 40 µM, compounds 1 – 3 , 5 , 7 , 8 , 9 , 14 , and 15 exhibited inhibitory effects over 50%, suggesting that they could be potential candidate drugs for the cure of neuro-inflammation. In addition, compounds 1 , 8 , 14 , and 15 significantly inhibited 16.23, 27.76, 21.23, and 29.44% NO production at diluted concentration as low as 2.5 µM.