Barbigerone reverses multidrug resistance in breast MCF‐7/ADR cells

Abstract

Development of agents to overcome multidrug resistance (MDR) is one of the important strategies in cancer chemotherapy, and P-glycoprotein (P-gp) correlates with the degree of resistance. As a naturally occurring isoflavone, whether barbigerone (BA) could reverse MDR, is unknown. In this paper, we evaluated effects of BA on reversing P-gp mediated MDR of adriamycin (ADR)-resistant human breast carcinoma (MCF-7/ADR) cells. BA (0.5 μM) treatment showed strong potency to increase ADR cytotoxicity toward MCF-7/ADR cells. It was also demonstrated that BA time- and dose-dependently increased accumulations of ADR and reduced the efflux in MCF-7/ADR cells, pretreatment of these cells with BA might relocalized ADR to the nuclei. Furthermore, the results also revealed that BA did not affect P-gp, but alter P-gp ATPase activity. Intravenous administration of BA significantly increased anticancer efficacy of ADR to MCF-7/ADR xenograft model in nude mice. These results revealed that BA might reverse P-gp mediated MDR through inhibition of ATPase activity, which indicated a novel use of BA as a potent candidate for cancer chemotherapy.

Shenmai injection suppresses multidrug resistance in MCF-7/ADR cells through the MAPK/NF-κB signalling pathway

“…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). P-gp overexpression is the main cause of MDR, which weakens the cytotoxicity by pumping intracellular drugs out (Iakusheva et al 2014).…”

Potential of phytochemicals in breast cancer prevention and therapy

“…Experimentally, a number of phytochemicals have been shown to attenuate angiogenesis, migration, adhesion, invasion, and metastasis and/or to promote apoptosis and autophagy of breast cancer cells. Phytochemicals belong to different chemical categories including polyphenols such as cyanidin‐3‐glucoside, epigallocatechin gallate derivatives, quercetin, myricetin, rutin, the isoflavone barbigerone (Lee et al, ; Iriti et al, ; Shin, Kim, Jung, & Chong, ; Li et al, ; Li et al, ; Ci et al, ; Ma & Ning, ), terpenes/terpenoids such as F1012‐2, sesquiterpene lactones from Inula helenium , tanshinone, alantolactone, lambertianic acid, and esculentoside A (Tian et al, ; Chun, Song, & Kim, ; Liu et al, ; Lin et al, ; Liu et al, ; Lee et al, ), irodoids (Elmaidomy et al, ) carotenoids (El‐Baz, Hussein, Mahmoud, & Abdo, ), oligosaccharides (Rosas‐Ramirez et al, ), vanilloids (Mai, Kang, Nadarajah, Hamzah, & Pichika, ), matrine (Xiao et al, ), and various phytochemicals isolated from the stem bark of Citrus reticulata (Tahsin et al, ). Finally, the issue reports a Korean herbal formula which suppressed the proliferation of human breast cancer cells, induced arrest of the cell cycle at the G0/G1 phase, and caused mitochondrial dysfunction and apoptosis (Lee et al, ).…”