Novel drugs are desperately needed in order to combat a significant challenge due to chemo-therapeutic resistance and bad prognosis. This research aimed to assess the anticancer activity of a newly synthesized ciprofloxacin Mannich base (CMB) on ovarian cancer (OVCAR-3) and lung cancer (A-549) cell lines and to investigate probable involved molecular mechanisms. The cytotoxic and pro-apoptotic impact of CMB on both cell lines was investigated using MTT assay, Annexin V assay, and cell cycle analysis, as well as caspase-3 activation. Western blotting was carried out to evaluate downstream targets of the MAPK pathway, while qRT PCR was used to evaluate the gene expression pattern of the p53/Bax/Bcl2 pathway. CMB treatment showed significantly reduced cell proliferation in both OVCAR-3 and A-549 cells with half maximum inhibitory concentration (IC50) = 11.60 and 16.22 µg/mL, respectively. CMB also induced apoptosis, S phase cell cycle arrest, and up-regulated expression of p53, p21, and Bax while down-regulated Bcl2 expression. CMB also halted cell proliferation by deactivating the MAPK pathway. In conclusion, CMB may be regarded as a potential antiproliferative agent for lung and ovarian cancers due to anti-proliferative and pro-apoptotic actions via inhibition of the MAPK pathway and p53/Bax/Bcl2.
Cancer is the most-deadly disease having the most formidable afflictions in the world. Numerous anticancer drugs are available commercially, but the development of acquired drug resistance and the severe side effects of these clinically utilised anticancer drugs pose significant obstacles to the effective chemotherapy. Consequently, the rational design of novel medications with minimal adverse effects is advised. Due to their excellent pharmacological and pharmacokinetic characteristics, fluoroquinolone derivatives are of utmost interest to scientists. They display a number of positive traits, such as increased bioavailability, superior tissue penetration, and a relatively low prevalence of negative effects. The emphasis of the field of research is currently shifting towards these chemicals' anticancer properties because of their potential to intervene in mutagenesis and carcinogenesis. This study outlines current developments in the creation of new fluoroquinolones as prospective cytotoxic and anticancer medicines as well as their potential mechanisms of action for future research. Additionally, this review aims to concentrate on the numerous forthcoming characteristics of fluoroquinolones and offers a fresh perspective on their potential applications in the treatment of cancer.
18 July 2019 in Journal of advanced Biomedical and Pharmaceutical Sciences
Background/Aims: Liver fibrosis presents a worldwide problem. There is an increasing interest in the studying of natural compounds with free radicals scavenging capacity to protect against liver fibrosis. This study investigated the actions of resveratrol and curcumin as two natural polyphenols against CCl4-induced liver fibrosis. Materials and Methods: Animals were divided into four groups: Normal control group; CCl4 only group; Res group (resveratrol + CCl4); Cur group (curcumin + CCl4). Serum ALT and AST were evaluated. Assessment of liver MDA, GSH and catalase was performed. Caspase-3 expression was evaluated by western blotting. Levels of TGF-β1 and TGF-β2 mRNA were determined using qRT-PCR. In addition, liver histopathological sections were examined. Results: We found that serum ALT and AST were elevated by CCl4, however, they were significantly reduced by resveratrol and curcumin. Furthermore, CCl4 induced oxidative stress, stimulated fibrosis and apoptosis. Resveratrol and curcumin significantly attenuated the state of oxidative stress, fibrosis and apoptosis. Conclusion: We conclude that resveratrol and curcumin are natural polyphenols that can protect against liver fibrosis not only via antioxidant, but also via anti-fibrotic and anti-apoptotic potentials.