A biologically guided isolation of secondary metabolites from Cousinia alata Schrenk wild plant growing in Akmola region, Kazakhstan, led to the isolation of the bioactive diterpene grindelic acid (1). Six flavonoids were also isolated and identified as retusine (2), pachipodol (3), jaranol (4), penduletin (5), casticin (6), and 5, 7, 3′-trihydroxy-3, 4′-dimethoxyflavone (7). Penduletin (5) showed moderate cytotoxic activity assay. Grindelic acid exhibited promising cytotoxic activity against the Artemia salina nauplii and antibacterial activity against Staphylococcus aureus, Bacillus cereus, and Salmonella enteritidis. The presence of the essential pharmacophoric features of histone deacetylase (HDAC) inhibitors in the structure of grindelic acid encouraged us to run a molecular docking study against the HDAC enzyme to understand its mechanism of action on a molecular level. Grindelic acid showed a binding mode of interaction similar to that of the cocrystallized ligand and exhibited good binding affinity against HDAC with the binding free energy of −18.70 kcal/mol. The structures of isolated compounds were determined by MS, 1D, and 2D NMR spectroscopy methods. Compounds (1–7) were isolated for the first time from Cousinia genus.

No abstract

No abstract

The investigation of the chemical composition, antioxidant and cytotoxic activities of the essential oil of Pulicaria vulgaris wild growing in Akmola region, Kazakhstan was the aim of the study. The essential oil was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry (GC/MS). A total of 49 compounds were identified representing 86.4 % and the major components were patchoulane (37.4), buddledin C (13.9%), T-cadinol (4.7%), trans-sesquisabinene hydrate (4.1%), dyhydro--agarofuran (2.7%), (Z)-α-atlantone (1.8%) and corymbolone (1.2%). Six components were identified as unknown (2.6%). The antioxidant activity was evaluated by using 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and the essential oil demonstrated an average scavenging effect at 0.75 and 1 mg ml-1 concentrations compared with butylhydroxyanisole (BHA). The antiradical activity results of the P. vulgaris essential oil is published for the first time. Cytotoxic activity assay was studied against Artemia salina larvae and it can be concluded that the essential oil has a good lethal toxicity in all tested concentrations (10-1 mg ml-1). The authors attribute this result to the presence of the patchoulane as a major component, which is known for its activity against ovarian cancer cells.