Bone-protective and anti-tumor effect of baicalin in osteotropic breast cancer via induction of apoptosis

Purpose: Research suggested that bone is the specific target organ for breast cancer metastasis. The related tumor causes significant morbidity due to a reduction in quality of life and physical function. Increased osteoclast function is implicated in the bone microenvironment during the outgrowth of breast cancer. In the present experimental study, we examined the potential bone-protective effect of baicalin osteotropic breast Cancer and explored the possible mechanism of action.

Methods: In vitro cell viability effect of baicalin was assessed on the breast cancer cell lines (MDA-MB-231 and MCF-7). We also estimated the in vitro osteoclast and bone resorption. Further, baicalin-regulated osteoblastogenesis and osteoclastogenesis were also estimated in vitro. Finally, the role of the baicalin in the expansion of osteolytic bone disease was scrutinized in a breast cancer bone metastases model.

Results: Baicalin significantly (p < 0.001) downregulated the viability of murine and human cancer cell lines and diminished the osteoclastogenesis of osteoclast progenitors via estimation with the help of qRT-PCR. Baicalin showed the downregulation in the mRNA expression of OCN and ALP. Baicalin reduced the TRAP-positive cells in the presence of RANKL. Baicalin considerably upregulated the cytochrome c secretion into the cytoplasm. Baicalin markedly increased the DNA fragmentation, caspase-3, caspase-8, and caspase-9. Baicalin significantly (p < 0.001) reduced the metastatic growth of MDA-MB-231 cells,preserving the bone mass in a bone metastasis model.

Conclusion: Collectively, we can conclude that these results highlight the bone-protective effect of baicalin, which also highlighted the anti-tumor effect; further research is needed into the likely effects on bone health in the bone metastases and osteoporosis populations, such as post-menopausal women with breast cancer.

Keywords: Antiresorptive; Baicalin; Bone; Breast cancer; mTOR inhibition.