N its multidrug-resistant (MDR) variant HL-60R and verify its ability to interfere with topoisomerase II activity. MTS assay showed that G. rosmarinifolia EO induced a decrease in tumor cell viability equivalent within the two cell lines; this antitumor effect could rely on the pro-oxidant activity of EO in each cell lines. Furthermore, G. rosmarinifolia EO decreased the activity of Topo II inside the nuclear extracts of HL-60 and HL-60R cells, as inferred from the inability to convert the kinetoplast DNA in to the decatenated form then not inducing linear kDNA. Confirming this result, flow cytometric analysis proved that EO induced a G0 -G1 phase arrest, with cell reduction in the S-phase. Furthermore, the combination of EO with etoposide showed a great potentiation impact in terms of cytotoxicity in each cell lines. Our final results highlight the antitumor activity of EO inside the HL-60 cell line and its MDR variant having a peculiar mechanism as a Topo II modulator.Maltohexaose Technical Information As opposed to etoposide, EO doesn’t lead to stabilization of a covalent Topo II-DNA intermediate but acts as a catalytic inhibitor. These data make G. rosmarinifolia EO a prospective anticancer drug candidate on account of its cytotoxic action, which can be not impacted by multidrug resistance. Keywords and phrases: EOs; napthoquinone; Topo II; multidrug resistance1. Introduction The plant kingdom represents one of several most significant sources of active principles in which several biological activities happen to be recognized. In specific, EOs play critical functions each in plant life, such as protection against plants or vermin, repellent or recall action for pollinating insects and as raw supplies for the synthesis of new drugs [1]. The biological properties of EOs have already been demonstrated within the treatment of many diseases, too as becoming productive in increasing the bioavailability of other drugs. Their in vitro anticancer, anti-bioceptive, antiviral, antiphlogistic and antimicrobial activities are widely documented in the vast literature [2]. EOs are highly fat soluble and are characterized by low toxicity and usually by a multi-target activity, precisely for the reason that they may be composed of various molecules with diverse pharmacological actions. Our prior studies have shown that EOs from plants have antitumor activities in distinct kinds ofCopyright: 2022 by the authors.Capreomycin Cancer Licensee MDPI, Basel, Switzerland.PMID:23357584 This article is an open access post distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( creativecommons.org/licenses/by/ 4.0/).Molecules 2022, 27, 4203. doi.org/10.3390/moleculesmdpi/journal/moleculesMolecules 2022, 27,two oftumors, including HCC, TNBC [7,8] and acute myeloid leukemia (AML) [9], all characterized by low responsiveness to chemotherapeutic drugs. EO extracted from the aerial parts (branches with leaves) of Glandora rosmarinifolia (Ten.) D.C. Thomas (Boraginaceae) has previously shown antitumor and cytotoxic activities involving a pro-oxidant mechanism in HCC and TNBC cell lines [7]. The chemical composition of G. rosmarinifolia EO has been identified [7], and an isomer of hydroxymethyl-naphthoquinone was amongst probably the most abundant compounds (5.3 ). Naphthoquinones are quinones with yet another aromatic ring fused onto them and normally take place as glycosides. Naphthoquinones aren’t widespread but are discovered in various plant households (e.g., Bignoniaceae, Ebenaceaeos, Droseraceae, Juglandaceae, Plumbaginaceae, Boraginaceae, among other people). Interestingly, naphthoquinones.
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