Ellipticine, its Derivatives: Re-evaluation of Clinical Suitability with the Aid of Drug Delivery Systems

Abstract

Targeted drug delivery systems gave newer dimensions for safer and more effective use of therapeutic drugs, thus helping in circumventing the issues of toxicity and unintended drug accumulation. These ongoing developments in delivery systems can, in turn, bring back drugs that suffered various limitations, Ellipticine (EPT) being a candidate. EPT derivatives witnessed entry into clinical settings but failed to survive in clinics citing various toxic side effects. A large body of preclinical data deliberates the potency of drug delivery systems in increasing the efficiency of EPT/derivatives while decreasing their toxic side effects. Recent developments in drug delivery systems provide a platform to explore EPT and its derivatives as good clinical candidates in treating tumors. The present review deals with delivery mechanisms of EPT/EPT derivatives as antitumor drugs, in vitro and in vivo, and evaluates the suitability of EPT-carriers in clinical settings.

Synthesis, Molecular Docking, and Cytotoxic Evaluation of Fluorinated Podophyllotoxin Derivatives

“…The cytotoxic activities of the 2 products 8a and 8b against epidermoid carcinoma (KB), hepatoma carcinoma (HepG2), non-small lung (A549), and breast (MCF7) cancer cell lines were determined using MTT (3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide) assay. Ellipticine, 35,36 a powerful anticancer agent, was used as a positive control. As described in Table 1, products 8a and 8b exhibited a significant cytotoxic effect on all tested cancer cell lines with half maximal inhibitory concentrations (IC 50 ) ranging from 0.58 to 3.17 µM.…”

Synthesis and biological activity, and molecular modelling studies of potent cytotoxic podophyllotoxin-naphthoquinone compounds

“…48 Toward this, as compounds 5a, 5b exhibited anti-proliferative efficacy on human lung SK-LU-1 cancer cells, their inuence on the cell cycle progression has been assessed by monitoring the distribution of cells in populations based on distinct phases including G0/G1 phase, S phase (Synthesis), and G2/M phase (Gap 2/Mitosis). Ellipticine [49][50][51] and Vincristine, 2 which are anticancer agents currently in clinical use for the treatment of various diseases, were used as positive controls.…”

Bioactivities and Action Mechanisms of Ellipticine Derivatives Reported Prior to 2023

“…Ellipticine is a naturally occurring alkaloid, and several publications have reviewed its isolation, synthesis and biological activity. [6][7][8][9][10] But these publications either did not comprehensively discuss the mechanism or only focus on the ellipticine instead of its' derivative. In this review, the structures, bioactivities, and mechanisms of action of ellipticine as well as its derivatives reported prior to 2023 are reviewed.…”