Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

Abstract

Evaluation of the potential antimutagenic activities of new compounds by Ames assay has been of great interest for the development of novel therapeutics for many diseases including cancer. Ten novel bichalcophenes with in vitro and in vivo broad spectrum activities against various microbial strains were investigated throughout the present study for their cytotoxic, antioxidant, and antimutagenic potential in a Salmonella reverse mutation assay system against sodium azide (NaN3) and benzo[a]pyrene (B[a]P). At nontoxic concentrations, all bichalcophenes alone or in combination with NaN3 (1 μg/plate) or B[a]P (20 μM) with S9 mix were not mutagenic. The bichalcophenes significantly reduced NaN3- and B[a]P-induced mutagenicity under pre-exposure and co-exposure conditions in a concentration-independent manner. However, the antimutagenic activity of bichalcophenes against B[a]P varied depending on the exposure regimen, being more effective under pre-exposure conditions. The antimutagenic activity was correlated with a high antioxidant activity that could promote the DNA repair system. Bichalcophenes are least likely to interfere with the microsomal bioactivation of B[a]P. Monocationic bichalcophenes were superior to the corresponding mononitriles as antimutagenic agents against both mutagens investigated, possibly due to the higher nucleophilic centers they have which could bind and protect the bacterial DNA. Three monocationic compounds were shown to have a strong anticancer activity against the 58 cell line. Based on the results of the present investigation, monocationic compounds (1, 4, and 5B) will be selected for further time consuming and costly chemoprevention studies in animal models.

Antioxidant and antimutagenic potential of Psidium guajava leaf extracts

“…Since both the mutagens and carcinogens may act through the generation of reactive oxygen species, the discovery and exploration of plant extracts/phytocompounds possessing both antioxidant and antimutagenic properties are of great practical and therapeutic significance. It is presumed that medicinal plants those are good in antioxidant activity could also show antimutagenic activity and such natural products could reduce or inhibit the mutagenic potential of mutagens and/or procarcinogens (El-Sayed & Hussin, 2013;Garg et al, 2008). However, antimutagenic and anticarcinogenic activities of bioactive compounds can also act by direct action (e.g.…”

Phenolic profile, antibacterial, antimutagenic and antitumour evaluation of Veronica urticifolia Jacq.

“…Humans are provided with many defences and their failure could lead to DNA damage and consequently to cancer (El-Sayed and Hussin, 2013). Carcinogenesis is generally a slow process and often takes decades from tumor initiation to diagnosis, offering a considerable time frame for chemopreventive approaches.…”

Attenuation of DMBA/croton oil induced mouse skin papilloma byApodytes dimidiatamediated by its antioxidant and antimutagenic potential

“…Various recent reports state that the natural antioxidants may reduce or inhibit the mutagenic potential of mutagens and carcinogens (Cardador-Martínez et al, 2006;El-Sayed & Hussin 2013). Zahin et al (2010) have reported that the anticarcinogenic and antimutagenic activities of medicinal and food plants are executed mainly by scavenging of free radicals.…”