Boldine: a potential new antiproliferative drug against glioma cell lines

Abstract

Malignant gliomas are the most common and devastating primary tumors of the central nervous system. Currently no efficient treatment is available. This study evaluated the effect and underlying mechanisms of boldine, an aporphine alkaloid of Peumus boldus, on glioma proliferation and cell death. Boldine decreased the cell number of U138-MG, U87-MG and C6 glioma lines at concentrations of 80, 250 and 500 muM. We observed that cell death caused by boldine was cell-type specific and dose-dependent. Exposure to boldine for 24 h did not activate key mediators of apoptosis. However, it induced alterations in the cell cycle suggesting a G(2)/M arrest in U138-MG cells. Boldine had no toxic effect on non-tumor cells when used at the same concentrations as those used on tumor cells. Based on these results, we speculate that boldine may be a promising compound for evaluation as an anti-cancer agent.

Evaluation of cytotoxic and chemotherapeutic properties of boldine in breast cancer using in vitro and in vivo models

“…However, recent studies have found that this compound also possesses antitrypanosomal,15 hepatoprotective,16 and anti-inflammatory properties 17. Although a preliminary cytotoxic effect was reported in bladder carcinoma and glioma cancer cells,18,19 the anticancer mechanism of boldine has yet to be demonstrated. In the present study, we investigated the antitumor activity of boldine in breast adenocarcinoma using in vitro and in vivo models.…”

The Efficacy of a Practical Activity in the Construction of Knowledge of the Concepts of Species and Phenotypic Plasticity Using the Boldo Mirim (<i>Plectranthus neochilus</i> Schltr.)

“…These species are the subject of disciplines such as ethnobotany and pharmacognosis ranging from the history of their cultivation, collection, conservation, commercialization (Silva et al, 2010;Viu et al, 2010;Coradin et al, 2011) to the extraction and identification and dosage of substances with active principles such as essential oils and components such as boldine which may be a novel compound for the development of anticancer strategies and phenolic compounds with anti-oxidant properties (Ascensão, 1998;Rosal, 2008;Gerhardt et al, 2009;Menon et al, 2012).…”

Therapeutic strategies for targeting telomerase in cancer

“…Here, we collect natural telomerase inhibitors reported in the literature and summarize their telomerase inhibition effects, structures, possible mechanisms, and provide references for pharmaceutical chemists searching for suitable lead compounds. Table and Figures and show natural products and chemical structures that target the telomere elongation process …”

“…Boldine ( 48 ) is a natural opioid alkaloid with 1,10‐dimethoxy‐2,9‐dihydroxy aporphine moiety. Boldine exhibits cytotoxic effects against various tumor cell lines (HepG‐2, T24, U138‐MG, U87, and MGC6), and this cytotoxic effect is dose‐and time‐dependent . A decrease in telomerase activity can be observed in these cell lines; however, the specific mechanism behind inhibiting telomere elongation remains unclear.…”