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Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Barbigerone has been reported to have antitumor, antioxidant, and antiplasmodial activity toward Plasmodium falciparum. Its potential anticancer and/or chemopreventive potential is based partly on reports that it causes apoptosis of murine lung-cancer LL/2 cells in laboratory experiments. These in vitro studies showed that it can inhibit the proliferation of LL/2 cells in a time-and concentration-dependent manner, leading to death by apoptosis, thought to be due to enhancement of mitochondrial cytochrome C release along with activation of various caspases. However, it has also been shown to up-regulate the Bcl-2-associated protein Bax, and down-regulate Bcl-2 in LL/2 cells. Based on other experiments, barbigerone has been shown to have differential cytotoxicity toward tumor versus healthy cells, and it can decrease the levels of phosphorylated Akt and phosphorylated p42/44 mitogen-activated protein kinase (p42/44 MAPK) in tumor cells.
Shenmai injection suppresses multidrug resistance in MCF-7/ADR cells through the MAPK/NF-κB signalling pathway
Published in Pharmaceutical Biology, 2020
Lin Yang, Chengda Zhang, Jiaoting Chen, Sheng Zhang, Guixuan Pan, Yanfei Xin, Lin Lin, Zhenqiang You
As a DNA-damaging agent, the nucleus is the target of ADR (Finn et al. 2011). Previous studies reported that P-gp is overexpressed not only on the cell membrane but also on the nuclear membrane (Munteanu et al. 2006; Barot et al. 2013), which may prevent ADR entry into the nucleus to produce its cytotoxic effect and provoke MDR (Li Y et al. 2018). To investigate the effects of SMI on the accumulation of ADR in the nucleus, the nuclear accumulation of ADR was evaluated qualitatively and quantitatively. The results demonstrated that ADR accumulation was enhanced in the nuclei of SIM treated MCF7/ADR cells. Similar results were observed with barbigerone, which reverses MDR (Li X et al. 2018).