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E2, 0.17 mg/kg body weight/day); and OVX with BHH10 in graded doses (250, 500, or 750 mg/kg/day). Daily oral administration of BHH10, ALN or E2 started on week 2 after OVX and continued for 12 weeks. Body and uterus weight, serum biochemical bone turnover markers, bone mineral density (BMD), and microarchitectural parameters were assessed. Results: BHH10 inhibited OVX-induced body weight gain, uterus atrophy, and significantly decreased levels of the bone formation markers serum alkaline phosphatase (ALP) and osteocalcin (OCN), and the bone resorption parameter C-telopeptide type 1 collagen (CTX). BHH10 also notably enhanced BMD and bone microstructure in both total femur and femoral neck measurements compared to OVX rats. Conclusions: These results suggested that BHH10 administration improved biochemical markers of bone metabolism, bone biomechanical quality, and bone structural integrity in OVX rats. The potent anti-osteoporosis effect of BHH10 might be mediated by its action of stimulating bone formation and regulating bone resorption with no significant toxicity.