Cyanidin and delphinidin are the main phenolic antioxidants in the grape (Vitis vinifera). The aim of this study was to investigate the in vitro and in vivo inhibitory effects of delphinidin and cyanidin chloride in the free and liposomal forms on the albumin glycation reaction. Delphinidin and cyanidin chlorides were encapsulated in the liposomes using an extrusion method. The rate of albumin glycation was evaluated using the ELISA method. Finally, in vivo anti-glycation of delphinidin and cyanidin chloride in the free and liposomal forms in diabetic mice was investigated. The encapsulation efficacies of delphinidin and cyanidin chloride in the liposomes were 89.05 % ± 0.18 and 85.00 % ± 0.15, respectively. In vitro treatment with 100 mg/mL delphinidin and cyanidin chloride in free forms could reduce the rate of albumin glycation to 30.50 ± 3.46 and 46.00 ± 2.50 %, respectively. Under identical conditions, the delphinidin and cyanidin chloride-loaded liposomes could reduce the rate of albumin glycation to 8.50 ± 2.10 and 14.60 ± 3.60 %, respectively. In vivo testing showed that anti-glycation activity of delphinidin and cyanidin in loaded forms was higher than in free forms. The daily administration of 100 mg/kg delphinidin chloride-loaded liposomes to diabetic mice at eight weeks could decrease the rate of albumin and HbA1c glycation to 46.35 ± 1.20 and 3.60 ± 0.25 %, respectively. Moreover, under identical conditions, the loaded liposomes with cyanidin chloride could decrease the rate of albumin and HbA1c glycation to 55.56 ± 1.32 and 4.95 ± 0.20 %, respectively. The findings showed that delphinidin and cyanidin chloride, in particular in the liposomal forms, could be used for treatment of diabetes mellitus complications.
BackgroundArtemisinin is the major sesquiterpene lactones in sweet wormwood (Artemisia annua L.), and its combination with transferrin exhibits versatile anti-cancer activities. Their non-selective targeting for cancer cells, however, limits their application. The aim of this study was to prepare the artemisinin and transferrin-loaded magnetic nanoliposomes in thermosensitive and non-thermosensitive forms and evaluate their antiproliferative activity against MCF-7 and MDA-MB-231 cells for better tumor-targeted therapy.MethodsArtemisinin and transferrin-loaded magnetic nanoliposomes was prepared by extrusion method using various concentrations of lipids. These formulations were characterized for particle size, zeta potential, polydispersity index and shape morphology. The artemisinin and transferrin-loading efficiencies were determined using HPLC. The content of magnetic iron oxide in the nanoliposomes was analysed by spectrophotometry. The in vitro release of artemisinin, transferrin and magnetic iron oxide from vesicles was assessed by keeping of the nanoliposomes at 37°C for 12 h. The in vitro cytotoxicity of prepared nanoliposomes was investigated against MCF-7 and MDA-MB-231 cells using MTT assay.ResultsThe entrapment efficiencies of artemisinin, transferrin and magnetic iron oxide in the non-thermosensitive nanoliposomes were 89.11% ± 0.23, 85.09% ± 0.31 and 78.10% ± 0.24, respectively. Moreover, the thermosensitive formulation showed a suitable condition for thermal drug release at 42°C and exhibited high antiproliferative activity against MCF-7 and MDA-MB-231 cells in the presence of a magnetic field.ConclusionsOur results showed that the thermosensitive artemisinin and transferrin-loaded magnetic nanoliposomes would be an effective choice for tumor-targeted therapy, due to its suitable stability and high effectiveness.
Background/Aim: Staphylococcusaureus remains a common cause of burn wound infection. Different studies have shown that the entrapment of plant-derived material such as epigallocatechin gallate (EGCG) in liposomes could increase their anti-S. aureus activity. The objectives of this study were to prepare EGCG-loaded nanoliposomes with variable surface charges and to evaluate their efficacy in vitro and in vivo against methicillin-resistant S. aureus (MRSA). Study Design/Methods: EGCG-loaded nanoliposomes with positive, negative and neutral surface charges were prepared by extrusion method. Minimum inhibitory concentrations (MICs) of EGCG nanoliposomal forms against MRSA were determined by broth dilution method. The killing rates of the free and nanoliposomal forms of EGCG were analyzed. Ultimately, the in vivo therapeutic efficacy of the nanoliposomes in burned mouse skin infected by MRSA was investigated. Results: The MICs of the free, cationic, neutral and anionic nanoliposomal forms of EGCG against MRSA were 128, 16, 32 and 256 mg/l, respectively. The killing rates of the EGCG-loaded cationic nanoliposomes were higher than those of the other formulations. Treatment with the EGCG-loaded nanoliposomes with positive, neutral and negative surface charges resulted in almost 100, 70 and 30% survival rates, respectively. Conclusion: The data suggested that the cationic EGCG-loaded nanoliposomes would be a good choice for the treatment of MRSA infections due to its high effectiveness.
Background:The combination of artemisinin and transferrin exhibits versatile anticancer activities. In previous, we successfully prepared artemisinin and transferrin-loaded magnetic nanoliposomes and evaluated their anti-proliferative activity against MCF-7 and MDA-MB-231 cell lines in vitro. In this study, we investigate the in vivo anti-breast cancer activity of artemisinin and transferrin-loaded magnetic nanoliposome against breast transplanted tumors in BALB/c mice model.Materials and Methods:Artemisinin and transferrin-loaded magnetic nanoliposomes were prepared and characterized for some physiochemical properties. Pieces of tumor tissue from the breast cancer-bearing BALB/c mice were transplanted subcutaneously to the syngeneic female BALB/c mice. In the presence of the external magnet that placed at the breast tumor site, the tissue distribution and tumor-suppressing effects of prepared nanoliposomes on tumor growth was evaluated.Results:The prepared nanoliposomes have fine spherical shape, rough surface, nano-sized diameter and magnetic properties. At 2 h after treatment, the intravenous administration of artemisinin and transferrin-loaded magnetic nanoliposomes followed using the magnetic field approximately produced 10- and 5.5-fold higher levels of artemisinin and transferrin in the tumors, respectively, compared with free artemisinin and transferrin. Moreover, in the presence of an external magnetic field, the prepared nanoliposomes could significantly induce apoptosis in the mice breast cancer cells as well as could reduce tumor volume in tumorized mice at 15 days after treatment.Conclusion:The data suggested that the artemisinin and transferrin-loaded magnetic nanoliposomes would be a good choice for the breast tumor-targeted therapy, due to its high targeting efficiency.
Telomerase has been proposed as a novel and potentially selective target in cancer therapy. Silymarin, which is a standardized mixture of flavonolignans from the medical plant Silybum marianum, has potent effects against various types of cancer cells, but its effect on telomerase activity in the human leukemia cell line K562 has not been investigated. The aim of this study was to examine the mechanism of silymarin-induced apoptosis in K562 cells, with particular emphasis on its effect on telomerase activity. The antiproliferation effect of silymarin on K562 cells was evaluated by the MTT assay. To measure apoptosis, Hoechst 33342 staining and flow cytometry were used. The telomerase activity was determined using the telomeric repeat amplification protocol (TRAP)-ELISA assay. The treatment of the K562 cells with silymarin resulted in a significant inhibition of cell growth and telomerase activity. Also, a positive correlation was found between telomerase inhibition and induction of apoptosis in silymarin-treated K562 cells. These results suggest a novel mechanism in the anticancer activity of silymarin in human leukemia K562 cells and may provide a basis for future development of anti-telomerase therapies.
Purpose: To prepare beta-cryptoxanthin-loaded nanoliposomes and evaluate their anti-proliferative activity in leukemia K562 cell line, compared to free beta-cryptoxanthin. Methods: Beta-cryptoxanthin-loaded nanoliposomes were prepared by extrusion method. Morphological characterization of the nanoliposomes was performed by cryo-transmission electron microscopy (cryo-TEM). The anti-proliferation effect of beta-cryptoxanthin (BC) in free and liposomal forms on K562 cell line was studied using 3-(4, 5-dimethylthiazol-2-yl)-
Pseudomonas aeruginosa remains a common cause of wound infections. Different studies have shown that the entrapment of plant-derived materials in liposomes could increase their antibacterial activity against Pseudomonas aeruginosa. The aim of this study was to prepare cyanidinum chloride-loaded liposomes and evaluate their in vitro and in vivo efficacy against a resistant strain of Pseudomonas aeruginosa ATCC 15692. Cyanidinum chloride-loaded liposomes were prepared by extrusion method. The minimum inhibitory concentrations of cyanidinum chloride in the free and liposomal forms against Pseudomonas aeruginosa ATCC 15?692 were determined in vitro by broth dilution method. The in vitro killing rates for free and liposomal cyanidinum chloride were analyzed. Ultimately, the in vivo therapeutic efficacy of the prepared liposomes in mice skin infected by ATCC 15692 was investigated. The minimum inhibitory concentrations of the free and liposomal forms of cyanidinum chloride against ATCC 15692 were 1.5???10?3 and 7.7???10?4?M, respectively. In vivo treatment with the free and cyanidinum chloride-loaded liposomes resulted in almost 40 and 100?% survival rates, respectively. Our results showed that cyanidinum chloride-loaded liposomes would be a good choice for the treatment of wound infection caused by Pseudomonas aeruginosa because of their high effectiveness.
Background:Lycopene, a plant carotenoid, has potent effects against the various types of cancer cells. To date, the effect of lycopene in the free and encapsulated forms on the telomerase activity in human leukemia cell line K562 have not been investigated. The aim of the present study was to prepare a novel lycopene-loaded nanosphere and compare its anti-telomearse activity in K562 cell line with those of free lycopene.Materials and Methods:The lycopene-loaded nanospheres were prepared by nanoprecipitation method. The lycopene entrapment efficacy was measured by high-performance liquid chromatography (HPLC) method. The anti-proliferation effect of the lycopene in the free and encapsulated forms in the different times (0-72 h) and the different doses (0-100 μg/ml) on K562 cell line was studied using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay. The changes of telomerase activity, following treatment with the lycopene in the free and encapsulated forms, were detected using the telomeric repeat amplification protocol-enzyme-linked immunosorbent assay.Results:The entrapment efficacy of lycopene was 78.5% ± 2. Treatment of the K562 cell line with lycopene, in particular in encapsulated form, resulted in a significant inhibition of the cell growth and increasing of percentage of apoptotic cells. It has also been observed that the telomerase activity in the lycopene-loaded nanospheres-treated cells was significantly inhibited in a dose and time-dependent manner.Conclusion:Our data suggest a novel mechanism in the anti-cancer activity of the lycopene, in particular in encapsulated form, and could be provided a basis for the future development of anti-telomerase therapies.
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