Abstract
BackgroundBreast cancer-related mortality increases annually. The efficacy of current breast cancer treatments is limited, and they have numerous side effects and permit high recurrence. Patients with estrogen receptor (ER)-negative or triple-negative breast cancer are particularly difficult to treat. Treatment for this type of cancer is lacking, and its prognosis is poor, necessitating the search for alternative treatments.MethodsThis study screened Chinese herb Hibiscus syriacus extracts and identified a novel anti-cancer drug for patients with ER-negative breast cancer. The inhibitory effects on cell viability and migration were evaluated for each compound, and the molecular regulatory effects were evaluated on both mRNA and protein levels.ResultWe found several triterpenoids including betulin (K02) and its derivatives (K03, K04, and K06) from H. syriacus inhibited human triple-negative breast cancer cell viability and migration but revealed smaller cytotoxic effects on normal mammalian epithelial cells. Betulin and its derivatives induced apoptosis by activating apoptosis-related genes. In addition, they activated p21 expression, which induced cell cycle arrest in breast cancer cells. Betulin (K02) and betulinic acid (K06) had stronger inhibitory effects on cell viability and migration than K03 and K04.ConclusionsH. syriacus extracts might inhibit breast cancer cell viability and induce apoptosis by activating p53 family regulated pathways and inhibiting AKT activation. H. syriacus extracts may provide important insight into the development of novel alternative therapies for breast cancer.Electronic supplementary materialThe online version of this article (doi:10.1186/s12906-015-0592-9) contains supplementary material, which is available to authorized users.
Highlights
HISY-F2, HISY-F3, and HISYF4 showed the best effects on both breast cancer cell lines
MDA-MB-231 cells showed a stronger tolerance to drug treatment
The cells treated with those triterpenoids showed a significant increase in the proportion of cells in sub-G1 phase compared to the DMSO control group. These results indicate that betulin and it derivatives induced apoptosis in breast cancer cells (Additional file 1: Figure S2)
Summary
The efficacy of current breast cancer treatments is limited, and they have numerous side effects and permit high recurrence. Patients with estrogen receptor (ER)-negative or triple-negative breast cancer are difficult to treat. Treatment for this type of cancer is lacking, and its prognosis is poor, necessitating the search for alternative treatments. Traditional treatments to alleviate or improve breast cancer and the side effects caused by treatment. The effect of Chinese herbal medicines on cancer has become a hot research topic. EGCG extracted from green tea inhibits the growth of pancreatic cancer cells [4]. Betulin, isolated from H. syriacus [9], is a natural triterpene that has anti-cancer effects, but its mechanism of action remains unclear [10,11]
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