Correlation between Cytotoxic Activities and Reduction Potentials of Heterocyclic Quinones

Abstract

To search for possible anti-tumor agents or anti-tumor promoters among natural or synthetic products, we used cyclic voltammetry to determine the reduction-oxidation potentials of heterocyclic quinones in phosphate buffer at pH 7.2. We determined the growth inhibitory- and cytotoxic activities of 12 heterocyclic quinone anti-tumor agent candidates against a panel of 39 human cancer cell lines (JFCR39). The average concentrations of the heterocyclic quinones required for 50% growth inhibition (GI50) against JFCR39 ranged from 0.045 to 13.2 μM, and the 50% lethal concentration (LC50) against JFCR39 ranged from 0.398 to 77.7 μM. The average values of GI50 or LC50 of the heterocyclic quinones correlated significantly with their reduction potentials. These results suggested that reduction-oxidation potentials could be a useful method for the discovery of novel antitumor agents.

A mode of action study of cationic anthraquinone analogs: a new class of highly potent anticancer agents

“…Caspase-3 is the key player in the digestion of the cellular component, while caspase-7 is responsible for the detachment of apoptotic cells. 29 The redox potentials of CAAs were determined by cyclic voltammetry ( Table 2). The result showed an increase in caspase-3 activity in a concentration and time dependent manner ( Fig.…”

Phytoelectrochemical analysis of Zanthoxylum chiloperone

“…Conventional solution‐phase electrochemistry has been widely applied to characterize pharmacologically active compounds (De Abreu et al ) and correlate activities with electrochemical parameters, formal electrode potentials in particular and estimating antioxidant properties (Yang et al ; Brainina et al ; Koyama et al ), among others (Doménech‐Carbó et al ). VMP studies in this field were confined to those from Komorsky‐Lovrić and Novak (, ) on testing the antioxidant capacity of samples from dry extracts of fruits and vegetables.…”

Antineoplastic activity of a methanolic extract from Kigelia pinnata DC stem bark

“…isopinnatal, kigelinole and isokigelinol, and kigelinone [22,23,27,43], the latter being characterized as cytotoxic agent and identified in other plants used as traditional antineoplastic remedies [16,44]. Moreover, quinone structural fragment is found in some important anticancer drugs, or investigational cytotoxic agents including the anthracycline antibiotics, mitoxanthrone, aloeemodin, lapachol (an identified constituent of K. africana) [21,35,[45][46][47][48] etc.…”