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.