Hesperidin, as a flavonone, is recognized as promising anti-inflammatory, antioxidant, and anticancer agent. Its poor bioavailability is crucial bottleneck for therapeutic efficacy. To enhance the stability and bioactive potentials, hesperidin-PLGA-Poloxamer 407 was successfully prepared to minimize or overcome problems associated with hesperidin absorption. The characteristics of nanohesperidin were testing by in vitro dissolution study, XRD, FTIR, PSA and SEM. Antioxidant effects of nanohesperidin were studied. The structure-activity relationship analysis with antioxidant pharmacophore has been performed by using density functional theory method and quantum chemical calculations. The structural properties were investigated using Becke three-parameter hybrid exchange and the Lee-Yang-Parr correction functional methods. Nanohesperidin was found to decrease the H 2 O 2 activity-induced DNA instability. Blood compatibility on human erythrocytes was confirmed by haemolytic and in vitro toxicity assessments. The in vitro anticancer activity of nanohesperidin towards MCF-7 cells using various parameters was carried out. The nanohesperidin was found to exert cell growth arrest, activated DNA fragmentation and induced apoptotic cell death through caspase-3 and p53-dependent pathways. These findings showed that nanohesperidin play an important role in its anticancer effects, suggesting might be used for clinical trials and can represent driving formulation for novel chemotherapeutic agents.
Levan is an industrially important, functional biopolymer with considerable applications in the food and pharmaceutical fields owing to its safety and biocompatibility. Here, levan-type exopolysaccharide produced by Pantoea agglomerans ZMR7 was purified by cold ethanol precipitation and characterized using TLC, FTIR, 1 H, and 13 C NMR spectroscopy. The maximum production of levan (28.4 g/l) was achieved when sucrose and ammonium chloride were used as carbon and nitrogen sources, respectively, at 35°C and an initial pH of 8.0. Some biomedical applications of levan like antitumor, antiparasitic, and antioxidant activities were investigated in vitro. The results revealed the ability of levan at different concentrations to decrease the viability of rhabdomyosarcoma and breast cancer cells compared with untreated cancer cells. Levan appeared also to have high antiparasitic activity against the promastigote of Leishmania tropica. Furthermore, levan had strong DPPH radical scavenging (antioxidant) activity. These findings suggest that levan produced by P. agglomerans ZMR7 can serve as a natural biopolymer candidate for the pharmaceutical and medical fields.
Back ground: Cyproterone acetate (CPA) is a steroidal anti-androgen inhibits the testosterone and DHT action it is used as a medicine for prostate cancer by association with the androgen receptors located on the surface of prostate cells, thus preventing the association of testosterone with receptors.
Objective: Investigation of the anticancer activities of Cyproterone acetate against cancer cell lines testicular (Tera-1), macrophage (RAW 264.7) in comparison to non- tumorigenic fetal hepatic cell line (WRL-68).
Material and method: The cytotoxic effect of CPA was investigated according to selected parameters including: MTT assay as assay of cell function to determined cell viability, high content screening (HCS) technique for the apoptosis of cell. Only the most cytotoxic concentration of CPA and the most sensitive cells as assayed by MTT was selected to complete the other test: (HCS). (MTT) assay was carried out at the Centre of Biotechnology Research’s, Al- NahrainUniversityBaghdad,Iraq . The HCS assay was performed at the Centre for Natural Product Research and Drug Discovery, Department of Pharmacology,Faculty of Medicine, University of Malaya, KualaLumpur, Malaysia
Results: The most significant cytotoxic effect of Cyproterone acetate towards 2 cancer cell lines was obtained when its concentration was 1.25mg/mL. The Tera-1 Cells were more sensitive to Cyproterone acetate compared with RAW264.7 and WRL-68. cells. There was a significant decrease in valid cell count, nuclear intensity and mitochondrial membrane potential (MMP) when CPA (400 μg/mL)was used compared with doxorubicin (20 μg/mL) as a standard. Also, there was a significant increase in membrane permeability and cytochrome C releasing when CPA (400μg/ml) was used compared with positive control.
Conclusion: CPA showed cytotoxic effects against the Tera-1 and RAW264.7 cancer cell lines while the WRL-68. Cells was not affected as determined in-vitro by the MTT assay. The HCStechnique also showed toxic effect towards Tera-1.
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