In vitro cytotoxic potential of newly synthesized furo[3,2-c]pyran-4-one derivatives in cultured human lymphocytes

Abstract

The in vitro cytotoxic potentials of Furo[3,2-c]pyran-4-one derivatives in human lymphocytes were investigated. Blood samples were obtained from six healthy donors, non-smoking volunteers, which were incubated and exposed to increasing concentrations (0.05, 0.1, 0.5, 1 and 2 mg/mL) of Furo[3,2-c] pyran-4-one derivatives which are methyl 2-methoxy-7-(4-methylbenzoyl)-6-(4-methylphenyl)-4-oxo-4H-furo [3,2-c]pyran-3-carboxylate (1a) and methyl 2-methoxy-7-(4-methoxybenzoyl)-6-(4-methoxyphenyl)-4-oxo-4H-furo[3,2-c]pyran-3-carboxylate (1b). Compounds 1a and 1b induced micronucleus, mitotic and replication indexes in human lymphocytes (1 and 2 mg/mL). The increases of micronucleus, mitotic and replication indexes show that compounds at high concentrations may become cytotoxic, genotoxic and carcinogenic.

Eicosapentaenoic acid protects against 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced hepatic toxicity in cultured rat hepatocytes

“…In addition, LMN test was performed for the first time and revealed that TCDD exposure increased the rate of MNHEPs in hepatocytes. MN assay is a reliable test indicated chromosomal damage (Yilmaz et al 2008;Eroglu et al 2011) and MNHEPs production as 8-OH-dG is one of the key pieces of evidence for the possible involvement of antioxidant activity in oxidative DNA damage . ROS can alter vital cell components like polyunsaturated fatty acids, proteins and nucleic acids (Halliwell and Gutteridge 1990) The increased production of reactive oxygen species, lipid peroxidation, and DNA and membrane damage are always associated with TCDD exposure (Shertzer et al 1998;Hung et al 2006).…”

Design, Synthesis and Cytotoxic Activities of Pyrazole‐Perimidine Hybrids

“…In addition, a significant decrease of the two parameters, namely MI and RI, which is indicative of anticarcinogenic and cytotoxic properties. [19] The data can be showed that both compounds possibly induce chromosome aberrations, particularly at high concentrations as the alkylating agent. In addition, the compounds may have contributed to MN formation by leading to centromeric division errors and dysfunction of spindle strands (stimulating aneuploidy) and forming chromosomal fractures (clastogenic).…”

“…Therefore, it is very important to find out whether physical and chemical agents with the potential to have these effects have mutagenic, carcinogenic and teratogenic effects for the human genome. [19] In this study, some hybrid structured perimidine compounds were synthesized and their structures were illuminated by spectroscopic methods (Scheme 1). Genotoxic, mutagenic and carcinogenic / anticarcinogenic effects of two perimidine compounds (5 b and 5 i) were investigated.…”

Efficient Microwave‐Assisted Synthesis, In Vitro Antimicrobial Evaluation of Furo[3,2‐c]pyrones and Furo[3,2‐c]coumarins along with Molecular Docking Studies

“…3-Acetyl-4-hydroxycoumarin (4) was prepared from 4hydroxycoumarin (3) and POCl 3 in acetic acid. [24] α,β-Unsaturated carbonyl compounds of 3-acetyl-4-hydroxycoumarin (5) were synthesized using different aryl aldehydes in the presence of piperdine as a catalyst in methanol solvent. [25] Protocol of this reaction is outlined in Scheme-2.…”

“…They are known to possess interesting biological activities such as, phelligridimer A, a highly oxygenated and unsaturated 26membered macrocyclic metabolite with antioxidant activity [1] and phelligridin H inhibited protein tyrosin phosphatase IB and rat liver microsomal lipid peroxidation were available in fungus P. igniarius, [2] Neo-tanshinlactone isolated from S. miltiorrhiza, showed significant in vitro anti-breast cancer activity. [3] The variety of furo [3,2-c]pyrones and furo [3,2-c]coumarins have attracted the considerable attention of pharmacologist and chemist world over due to wide spectrum of remarkable biological properties e. g. antimicrobial, [4] anticancer, [5][6][7] antiinflammatory, [8] anticoagulant, [9] insect antifeedant, [10] etc. [11][12][13] Few naturally occurring and synthetic molecules possessing furo [3,2-c] Further, there is continuous effort in the development of synthetic methodology for furo [3,2-c]pyrones and furo [3,2-c] coumarins.…”