title: Anthraquinone compounds from Morinda officinalis inhibit osteoclastic bone resorption in vitro.
abstract: The root of Morinda officinalis has been claimed to have a protective effect against bone loss in sciatic neurectomized and ovariectomized osteoporotic rats, and this protective effect is supposed to be attributed to anthraquinone compounds in the plant. In the present study, we investigated the effects of three anthraquinones isolated from M. officinalis, including 1, 3, 8-trihydroxy-2-methoxy-anthraquinone (1), 2-hydroxy-1-methoxy-anthraquinone (2) and rubiadin (3) on bone resorption activity in vitro and the mechanism on osteoclasts derived from rat bone marrow cells. Compound 1, 2 and 3 decreased the formation of bone resorption pits, the number of multinucleated osteoclasts, and the activity of tartrate resistant acid phosphates (TRAP) and cathepsin K in the coculture system of osteoblasts and bone marrow cells in the presence of 1, 25-dihydroxyvitamine D(3) and dexamethasone. They also enhanced the apoptosis of osteoclasts induced from bone marrow cells with M-CSF and RANKL. In addition, Compound 1, 2 and 3 improved the ratio of mRNA and protein expression of OPG and RANKL in osteoblasts, interfered with the JNK and NF-κB signal pathway, and reduced the expression of calcitonin receptor (CTR) and carbonic anhydrase/II (CA II) in osteoclasts induced from bone marrow cells with M-CSF and RANKL. These findings indicate that the anthraquinone compounds from M. officinalis are potential inhibitors of bone resorption, and may also serve as evidence to explain the mechanism of the inhibitory effects of some other reported anthraquinones on bone loss.
authors.affiliation: Department of Pharmacogonosy, School of Pharmacy, Second Military Medical University, Shanghai, China.
authors.forename: Leilei
authors.initials: L
authors.lastname: Bao
authors.forename: Luping
authors.initials: L
authors.lastname: Qin
authors.forename: Lei
authors.initials: L
authors.lastname: Liu
authors.forename: Yanbin
authors.initials: Y
authors.lastname: Wu
authors.forename: Ting
authors.initials: T
authors.lastname: Han
authors.forename: Liming
authors.initials: L
authors.lastname: Xue
authors.forename: Qiaoyan
authors.initials: Q
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000880:Anthraquinones / Q000494:pharmacology*; D001483:Base Sequence; D001854:Bone Marrow Cells / Q000187:drug effects; D001862:Bone Resorption / Q000517:prevention & control*; D002454:Cell Differentiation / Q000187:drug effects; D018920:Coculture Techniques; D017931:DNA Primers; D005434:Flow Cytometry; D051550:I-kappa B Kinase / Q000378:metabolism; D048670:MAP Kinase Kinase 4 / Q000378:metabolism; D032066:Morinda / Q000737:chemistry*; D010010:Osteoclasts / Q000187:drug effects*; D053244:Osteoprotegerin / Q000378:metabolism; D016133:Polymerase Chain Reaction; D053245:RANK Ligand / Q000378:metabolism; D051381:Rats
chemical_list: D000880:Anthraquinones; D017931:DNA Primers; D053244:Osteoprotegerin; D053245:RANK Ligand; C506032:Tnfrsf11b protein, rat; D051550:I-kappa B Kinase; D048670:MAP Kinase Kinase 4