Studies On Chemical Constituents And Anti-osteoporotic Activity Of The Roots Of Ficus Auriculata Lour

The Ficus auriculata lour belongs to Ficus genus of Moraceae. Ficus resourcesis rich in China, mainly distributed in Hainan and Guangdong. It has been used as aChinese folk medicine for the treatment of cancer, pneumonia, tonsillitis, rheumatismand pain. Recording list of south herbal garden plants F. auriculata could alsodispelling wind and ventilating lung as well as BSYJ. It has been used for thetreatment of spermatorrhea and hematemesis. There were no reported about chemicalconstituents and pharmacological activities of F. auriculata except that Shao Taiminghad studied on the chemical constituents of the stems of F. auriculata. Under theguidance of the anti-osteoporotic activity, the roots of F. auriculata lour wereextracted with95%EtOH and then evaluated for its anti-osteoporotic activity. Theresults showed that the EtOAc extracts exhibited significant effects on promoteosteoblast proliferation. So we studied on chemical constituents and anti-osteoporoticactivity of the roots of Ficus auriculata Lour, which will provide a theoretical basisfor the development and utilization of the F. auriculata lour.The roots of F. auriculata lour were extracted at room temperature with95%EtOH, and the residue was successively partitioned with petroleum ether and ethylacetate. Then the fractions were purified by means of silica gel columnchromatography, Sephadex LH-20, preparative thin layer chromatography andrecrystallization etc. The structures were elucidated by spectroscopic methods andcomparison with the literature. Thirty-six compounds (1-36) were isolated from theroots of the F. auriculata, including10new compounds and a new natural product.They were divided into5types of structure, including22isoflavones,6steroids,4macrolides,1coumarin and3benzene derivatives. They were identified asFicaurisoflavone I (1), Ficaurisoflavone II (2), Ficaurisoflavone III (3),Ficaurisoflavone IV (4), Ficaurisoflavone V (5), Ficaurisoflavone VI (6),Ficaurisoflavone VII (7), Ficaurisoflavone VIII (8),5,7,4′-trihydroxy-3′-[7-hydroxyl-3,7-dimethyl-2(E)-octenyl] isoflavone (9), Dihydroalpinumisoflavone(10), Alpinumisoflavone (11), Alpinumisoflavone4′-O-glucopyranoside (12), Myrsininone A (13), derrone (14),5,7,4′,2″-tetrahydroxy-6-(3″-methyl-3″-butenyl) isoflavone (15), Wighteone (16), Lupiwighteone (17),3′-isoprenylgenistein(18), Erycibenins A (19), Ficuisoflavone (20), Hydroxyalpinumisoflavone (21),Orobol (22), Steroid-7,22-dinen-3β,5α,6α-triol (23), α-amyrin (24), Stigmasta-3,6-dione (25),6β–hydroxystigmast-4-en-3-one (26),[24S]–steroid–4–en-3-one (27), Stigmast-4-ene-3,6-dione (28),(6S,8R,11R)-FicaurmacrolideI (29), Des–O-methyllasiodiplodin (30),(6S,8R)-Ficaurmacrolide II (31),(6S,8R,10ξ)-Ficaurmacrolide III (32), Decursinol (33),3,4-dihydroxybenzoic acid (34),1,2,4-benzenetri (35) and3ξ-(1ξ-hydroxyethyl)-7-hydroxyl-1-isobenzofuranone (36). Compounds1-4,6-8,29,31-32were new compounds,compound5was new natural product, Compounds9-10,12,18,22-23,25and33-35were isolated from the Ficus genus for the first time, compounds19,20and24were isolated from F. auriculata Lour for the first time.All extracts and the monomeric compounds were evaluated the anti-osteoporoticactivity. The results showed that EtOAc extracts exhibited significant effects onpromote osteoblast proliferation, compounds7and8,11,22exhibited significanteffects on promote osteoblast proliferation, compounds9,13,16-18,21-22compounds24,27and compound30exhibited strong effects on promote osteoblastproliferation.