RESUMO
The phytochemical profile of essential oils is influenced by genetic and paragenetic factors. In this research, we studied the essential oils of Lavandula angustifolia and Lavandula x intermedia cultivated in Lebanon. The latter is a cross hybrid between Lavandula angustifolia and Lavandula latifolia and is also known as lavandin and Lavandula hybrida. Specifically, the chemical composition and biological activities (antibacterial, antioxidant, anticancer, and hemolytic) of the essential oils were assessed. GC-MS results showed marked differences in the chemical compositions of the oils. For example, linalool was more abundant in L. x intermedia (44.15%) than in L. angustifolia (32%), while an opposite trend was observed for the percentages of 1,8-cineole (8.6% in L. angustifolia and 4.0% in L. x intermedia). FTIR analysis confirmed the richness of both oils in monoterpenes and sesquiterpenes. In terms of antioxidant activity, L. angustifolia essential oil demonstrated significantly better activity (IC50= 5.24 ± 1.20 mg/mL) compared to L. x intermedia oil in the DPPH radical scavenging assay. MTT cell viability assays revealed that L. angustifolia essential oil was a slightly more potent antiproliferative agent than L. x intermedia oil on human colorectal (HCT-116) and human breast (MCF-7) cancer cells. The antibacterial activity of the essential oils was tested against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Escherichia coli, and Serratia marcescens. Both oils showed good antibacterial activities with MIC values of 0.174 and 0.169 mg/mL for L. angustifolia and L. x intermedia oils, respectively. MBC determinations revealed that the antibacterial activity was bactericidal against all bacteria, except Staphylococcus aureus. Furthermore, both essential oils did not exhibit notable hemolytic activity on red blood cells. Overall, Lebanese L. angustifolia and L. x intermedia essential oils have promising industrial and medicinal values.
RESUMO
Introduction: The anticancer and anti-inflammatory activities of a novel series of eleven pyrimido[1,2-b]pyridazin-2-one analogues substituted at position 7 were assessed in the current study. Methods: The physicochemical characteristics were studied using MolSoft software. The antiproliferative activity was investigated by MTT cell viability assay, and cell cycle analysis elucidated the antiproliferative mechanism of action. Western blot analysis examined the expression levels of key pro-apoptotic (Bax, p53) and pro-survival (Bcl-2) proteins. The anti-inflammatory activity was assessed by measuring the production levels of nitric oxide in RAW264.7 cells, and the expression levels of COX-2 enzyme in LPS-activated THP-1 cells. In addition, the gene expression of various pro-inflammatory cytokines (IL-6, IL-8, IL-1ß, TNF-α) and chemokines (CCL2, CXCL1, CXCL2, CXCL3) was assessed by RT-qPCR. Results: Compound 1 bearing a chlorine substituent displayed the highest cytotoxic activity against HCT-116 and MCF-7 cancer cells where IC50 values of 49.35 ± 2.685 and 69.32 ± 3.186 µM, respectively, were achieved. Compound 1 increased the expression of pro-apoptotic proteins p53 and Bax while reducing the expression of pro-survival protein Bcl-2. Cell cycle analysis revealed that compound 1 arrested cell cycle at the G0/G1 phase. Anti-inflammatory assessments revealed that compound 1 displayed the strongest inhibitory activity on NO production with IC50 of 29.94 ± 2.24 µM, and down-regulated the expression of COX-2. Compound 1 also induced a statistically significant decrease in the gene expression of various cytokines and chemokines. Conclusion: These findings showed that the pyrimidine derivative 1 displayed potent anti-inflammatory and anticancer properties in vitro, and can be selected as a lead compound for further investigation.