Quercetin, Siamois 1 and siamois 2 induce apoptosis in human breast cancer MDA-MB-435 cells xenograft in vivo

Abstract

We sought to investigate the apoptosis-inducing activities of quercetin, Siamois 1, and Siamois 2 against invasive estrogen-receptor negative MDA-MB 435 cells xenografted in athymic nude mice. This study clearly demonstrated that these compounds exhibited apoptosis-inducing activities in cell culture system. Quercetin (20 microg/mL), Siamois 1 (100 microg/mL), and Siamois 2 (200 microg/mL) can induce apoptotic cell death by 40 +/-5%, 44 +/- 14 %, and 31 +/- 13 %, respectively. Two-fold of IC50 of these compounds were clearly found to induce apoptosis in breast tumor tissue which can be determined by 99mTc-Annexin V scintigraphy and histological staining. This is the first report that the apoptosis-inducing effects of quercetin, Siamois 1 and Siamois 2 on the MDA-MB 435 cell in vitro were effectively extrapolated to the in vivo situation. These compounds might be considered as a simple dietary supplement and with further clinical investigation for their use as a nutrition-based intervention in breast cancer treatment.

Quercetin induces apoptosis in the methotrexate-resistant osteosarcoma cell line U2-OS/MTX300 via mitochondrial dysfunction and dephosphorylation of Akt

“…In vitro studies confirm that quercetin at a range of 10-100 µM inhibits cell viability, likely through cell cycle arrest, and induces apoptosis (8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20). While quercetin has been evaluated in several tumors, very little is known about its effects in MTX-resistant osteosarcoma.…”

“…The bioactivities of quercetin are complex and include antioxidative, antiviral, antibacterial and anti-inflammatory effects (4,6,7). Recently, quercetin was found to possess strong anticancer properties in colon cancer (8)(9)(10)(11), breast cancer (12,13), leukemia (14)(15)(16), hepatocellular carcinoma (17), pancreatic carcinoma (18), salivary adenoid cystic carcinoma (19) and lung cancer (20). Although the anti-tumor effects of quercetin have been examined in several tumors, very little is known about its effects in osteosarcoma cells.…”

Relation between Macroscopic Binding Constant and the Anticancer Efficacy of the Bovine Serum Albumin-Quercetin Complex against Drug-Sensitive and Drug-Resistant Cells

“…Particularly, the rutinoside substitution exhibits 5-fold anticancer activity higher than quercetin. Indeed, it is known that quercetin mediated anticancer action at the mitochondrial level triggering particular various cancer cell types to be suicide the so-called "apoptosis" (Samanta and Bhattacharya, 2010;Choiprasert et al, 2010;Kothan et al, 2004;Dechsupa et al, 2007;Li et al, 2007;Ramanouskaya et al, 2009). The efficacy of apoptosis induction of quercetin depends upon its intracellular target concentration.…”

“…Quercetin and its glycoside derivatives present great interest as potential anticancer and anticarcinogenic molecules are increasingly receiving interests due to their a variety of pharmacological activities including anti-inflammatory (Nijveldt et al, 2001;Wang et al, 2006), cardioprotective (Hirvonen et al, 2001;Knekt et al, 2002;Yochum et al, 1999;Hertog et al, 1997;Rimm et al, 1996;Mink et al, 2007) and cancer apoptosis induction activities (Samanta and Bhattacharya, 2010;Choiprasert et al, 2010;Kothan et al, 2004;Dechsupa et al, 2007;Li et al, 2007;Ramanouskaya et al, 2009). Despite the great interest in these compounds over the recent years, there is little data dealing with the physicochemical properties of molecule.…”

The Anticancer Properties of Dietary Polyphenols and its Relation with Apoptosis

“…Oak-aged red wine [175] Overwelming evidence can be found in the literature on the proapoptotic properties of dietary polyphenols against numerous types of human cancer cell lines, from colon and prostate cancers, to breast adenocarcinoma and leukaemia [176,177]. Among many others apoptosis was reported to be induced by anthocyanidins [166] and epicathechin in hepatoma cell lines; by epigallocatechin-3-gallate (EGCG) [178] and pterocarnin [179] in breast adenocarcinoma MCF-7 cells; by quercetin in oral squamous carcinoma [137], leukaemia [180,181], breast [182,183], lung [184], prostate [185,186] and colon cancer cell lines [187]; by gallotannin in human colon cancer cell lines [188]; by resveratrol in prostate cancer [189]; by genistein in breast [190,191], prostate [192,193], gastrointestinal [194], lung [195], and head and neck cancer cell lines [196,197]; by persimmon extract (Diospyros kaki) and related polyphenols in lymphoid leukaemia cells [198] or by olive oil polyphenol-rich extract in AGS stomach cancer cells [199].…”