Abstract
Natural compounds isolated from plants are excellent starting points in drug design and have been widely studied as anticancer agents; they hence find use in a considerable proportion of anticancer drugs. The genus Plectranthus (Lamiaceae) comprises a large and widespread group of species with various applications in traditional medicine. Therefore, the aim of the present study was to determine the effectiveness of treatment with four abietane diterpenoids isolated from P. madagascariensis and P. ecklonii, 6,7-dehydroroyleanone, 7β,6β-dihydroxyroyleanone, 7α-acetoxy-6β-hydroxyroyleanone and parvifloron D, in initiating apoptosis in a glioma cell line. The pure compounds were found to exhibit anticancer effects in primary H7PX glioma cells line by inducing apoptosis G2/M cell cycle arrest and double-strand breaks, indicated by increased levels of phosphorylated H2A.X and decreasing mitochondrial membrane potential; they also influenced the expression of pro- and anti-apoptotic genes (Bax, Bcl-2, TP53, or Cas-3). Our findings indicate that these compounds may offer potential as beneficial antitumor drugs but further in vivo studies are needed.
Highlights
Glioblastoma multiforme (GBM) is the most malignant and most common form of primary astrocytoma, accounting for more than 60% of all brain tumors in adults [1]
The primary H7PX glioma cells were treated with the four compounds (6,7-dehydroroyleanone-Deroy, 7β,6β-dihydroxyroyleanone- Diroy, 7α-acetoxy-6β-hydroxyroyleanone-Roy and parvifloron D-Parviforon D (Parv D)) at concentrations of 0–100 μg/mL for 24 h, and the percentage of viable cells was determined by MTT assay
It was found that all tested compounds reduced the viability of human H7PX cells but to different degree: the H7PX cells were most sensitive to Parv D, Roy and Deroy compared to Diroy in the tested range of concentrations (Figure 2A–D)
Summary
Glioblastoma multiforme (GBM) is the most malignant and most common form of primary astrocytoma, accounting for more than 60% of all brain tumors in adults [1]. Despite the development of new therapies, it demonstrates high mortality, with patients expecting a median survival period of approximately 14 to 15 months from diagnosis [2,3]. There is a pressing need to identify new compounds for use in therapy. The plant kingdom is a valuable source of natural compounds with potential anti-cancer activity: many metabolites of plant origin have a broad spectrum of activity and are less toxic to patients than synthetic drugs [4]. One potential source is represented by the plants of the genus Plectranthus [5]. BBrioomaodlecsupleesc2t0r2u0,m10,o1f94activity and are less toxic to patients than synthetic drugs [4]. One pote2notifa1l3 source is represented by the plants of the genus Plectranthus [5]
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