ABSTRACT
The anticancer activity of terretonin N (1) and butyrolactone I (2), obtained from the thermophilic fungus Aspergillus terreus TM8, was intensively studied against prostate adenocarcinoma (PC-3) and ovary adenocarcinoma (SKOV3) human cell lines. According to this study, both compounds showed potent cytotoxicity towards ovarian adenocarcinoma cells (SKOV3) with IC50 1.2 and 0.6 µg/mL, respectively. With respect to metastatic prostate cells (PC-3), the two compounds 1 and 2 showed a significantly promising cytotoxicity effect with IC50 of 7.4 and 4.5 µg/mL, respectively. The tested fungal metabolites showed higher rates of early and late apoptosis with little or no necrotic apoptotic pathway in all treated prostate adenocarcinoma (PC-3) and ovary adenocarcinoma (SKOV3) human cell lines, respectively. The results reported in this study confirmed the promising biological properties of terretonin N (1) and butyrolactone I (2) as anticancer agents via the induction of cellular apoptosis. However, further studies are needed to elucidate the molecular mechanism by which cellular apoptosis is induced in cancer cells.
Subject(s)
4-Butyrolactone/analogs & derivatives , Apoptosis/drug effects , Aspergillus/chemistry , Ovarian Neoplasms/pathology , Prostatic Neoplasms/pathology , Terpenes/pharmacology , 4-Butyrolactone/chemistry , 4-Butyrolactone/pharmacology , Cell Line, Tumor , Cell Nucleus/drug effects , Cell Nucleus/metabolism , Cell Shape/drug effects , Female , Humans , Inhibitory Concentration 50 , Male , Terpenes/chemistryABSTRACT
The current article describes the chiral separation of tioconazole, miconazole, isoconazole, sertaconazole and terconazole, with Lux i-Cellulose 5 and Lux i-Amylose-1 chiral columns under organic polar, normal and reversed mobile phases modes. The mobile phase flow rate was 1 mL/min with 230 nm detection at 25 ± 1 °C temperature. The polar organic mobile phases offered certain advantages for separation such as short analysis time, order of elution, high plate numbers and favorable signal to noise ratio. The values of k, α and Rs were ranged from 0.6 to 7.87, 1.10 to 1.62 and 0.37 to 5.72 in polar organic, 0.15 to 43.86, 1.02 to 2.01 and 0.36 to 8.03 in normal, and 0.34 to 15.99, 1.03 to 1.40 and 0.59 to 4.18 in reversed phases modes, respectively. The reported methods were applied in urine samples and the results were satisfactory. The reported methods were applied to the analysis of urine samples.
