chrysin and Stomach-Neoplasms

Gastric cancer is one of the most prevalent cancers in the world. Various therapeutic modalities have been used for its treatment, but all exhibit severe side effects, establishing the need for novel approaches. Chrysin is a phytomedicine compound belonging to the flavonoid group. It is found in honey and many plants. Its antitumor effects have been documented against gastric cancer cell lines in vitro, establishing its effects are mediated via different pathways and the expression of miRNA. In this review, we summarize the available literature on chrysin and its effects on gastric cancer, focusing on the cellular mechanisms it targets.

Topics: Cell Line, Tumor; Flavonoids; Humans; MicroRNAs; Stomach Neoplasms

Despite significant biological effects, the clinical use of chrysin has been restricted because of its poor oral bioavailability.. The purpose of the present research was to investigate the targeting potential of Mannose decorated chrysin (5,7- dihydroxyflavone) loaded solid lipid nanocarrier (MC-SLNs) for gastric cancer.. The Chrysin loaded SLNs (C-SLNs) were developed, optimized, characterized and further mannosylated. The C-SLNs were developed with a high shear homogenizer, optimized with 32 full factorial designs and characterized by Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD) and Scanning Electron Microscope (SEM) and evaluated for particle size/polydispersity index, zeta-potential, entrapment efficiency, % release and haemolytic toxicity. The ex-vivo cytotoxicity study was performed on gastric cancer (ACG) and normal cell lines.. DSC and XRD data predict the chrysin encapsulation in the lipid core and FTIR results confirm the mannosylation of C-SLNs. The optimized C-SLNs exhibited a narrow size distribution with a particle size of 285.65 nm. The % Entrapment Efficiency (%EE) and % controlled release were found to be 74.43% and 64.83%. Once C-SLNs were coated with mannose, profound change was observed in a dependent variable - an increase in the particle size of MC-SLNs (307.1 nm) was observed with 62.87% release and 70.8% entrapment efficiency. Further, the in vitro studies depicted MC- SLNs to be least hemolytic than pure chrysin and C-SLNs. MC-SLNs were most cytotoxic and were preferably taken up ACG tumor cells as evaluated against C-SLNs.. These data suggested that the MC-SLNs demonstrated better biocompatibility and targeting efficiency to treat gastric cancer.

Topics: Cell Line; Drug Carriers; Flavonoids; Humans; Lipids; Nanoparticles; Particle Size; Stomach Neoplasms

Topics: Antineoplastic Agents, Phytogenic; Cell Line, Tumor; Down-Regulation; Flavonoids; Gene Expression Regulation, Neoplastic; Humans; Inhibitory Concentration 50; MicroRNAs; Reverse Transcriptase Polymerase Chain Reaction; Stomach Neoplasms; Time Factors; Up-Regulation

Chrysin, as a flavone, has showed cancer chemopreventive activity. The present study utilized the PLGA-PEG-chrysin to evaluate the expression of miR-9 and Let-7a in human gastric cells. The structure of nanoparticles and encapsulated chrysin was evaluated using

Topics: Cell Line, Tumor; Flavonoids; Gene Expression Regulation, Neoplastic; Humans; MicroRNAs; Nanocapsules; RNA, Neoplasm; Stomach Neoplasms; Up-Regulation

Chrysin were well-documented as having significant biological roles particularly cancer chemo-preventive activity. However, the poor water solubility of chrysin limited their bioavailability and biomedical applications. In this study, we encapsulate the chrysin into PLGA-PEG nanoparticles for local treatment. In regard to the amount of the drug load, IC50 was significant decreased in nanocapsulated chrysin in comparison with free chrysin. This was confirmed through decrease of miR-18a, miR-21, and miR-221 genes expression by real-time PCR. The results demonstrated that PLGA-PEG-chrysin complexes can be more effective than free chrysin. Therefore, PLGA-PEG can be a better nanocarrier for this kind of hydrophobic flavonoid.

Topics: Cell Line, Tumor; Down-Regulation; Drug Carriers; Flavonoids; Gene Expression Regulation, Neoplastic; Humans; Lactic Acid; MicroRNAs; Nanoparticles; Polyethylene Glycols; Polyglycolic Acid; Polylactic Acid-Polyglycolic Acid Copolymer; RNA, Neoplasm; Stomach Neoplasms

Cell invasion is one of crucial reasons for cancer metastasis and malignancy. Recepteur d'origine Nantais (RON) has been reported to play an important role in the cancer cell invasion process. High accumulation and activation of RON has been implicated in gastric adenocarcinoma AGS cells. Chrysin is a naturally occurring phytochemical, a type of flavonoid, which has been reported to suppress tumor metastasis. However, the effects of chrysin on RON expression in gastric cancer are not well studied. In the present study, we examined whether chrysin affects RON expression in gastric cancer, and if so, its underlying mechanism. We examined the effect of chrysin on RON expression and activity, via RT-PCR, promoter study, and western blotting in human gastric cancer AGS cells. Chrysin significantly inhibited endogenous and inducible RON expression in a dose-dependent manner. After demonstrating that Egr-1 and NF-κB are the critically required transcription factors for RON expression, we discovered that chrysin suppressed Egr-1 and NF-κB transcription factor activities. Additionally, the phorbol-12-myristate-13-acetate- (PMA) induced cell invasion was partially abrogated by chrysin and an RON antibody. Our results suggest that chrysin has anticancer effects at least by suppressing RON expression through blocking Egr-1 and NF-κB in gastric cancer AGS cells.

Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Movement; Dose-Response Relationship, Drug; Early Growth Response Protein 1; Flavonoids; Humans; NF-kappa B; Promoter Regions, Genetic; Receptor Protein-Tyrosine Kinases; Stomach Neoplasms

Nano-therapy has the potential to revolutionize cancer therapy. Chrysin, a natural flavonoid, was recently recognized as having important biological roles in chemical defenses and nitrogen fixation, with anti-inflammatory and anti-oxidant effects but the poor water solubility of flavonoids limitstheir bioavailability and biomedical applications.. Chrysin loaded PLGA-PEG-PLGA was assessed for improvement of solubility, drug tolerance and adverse effects and accumulation in a gastric cancer cell line (AGS).. Chrysin loaded PLGA-PEG copolymers were prepared using the double emulsion method (W/O/W). The morphology and size distributions of the prepared PLGA-PEG nanospheres were investigated by 1H NMR, FT-IR and SEM. The in vitro cytotoxicity of pure and nano-chrysin was tested by MTT assay and miR-34a was measured by real-time PCR.. 1H NMR, FT-IR and SEM confirmed the PLGA-PEG structure and chrysin loaded on nanoparticles. The MTT results for different concentrations of chrysin at different times for the treatment of AGS cell line showed IC50 values of 68.2, 56.2 and 42.3 μM and 58.2, 44.2, 36.8 μM after 24, 48, and 72 hours of treatment, respectively for chrysin itslef and chrysin-loaded nanoparticles. The results of real time PCR showed that expression of miR-34a was upregulated to a greater extent via nano chrysin rather than free chrysin.. Our study demonstrates chrysin loaded PLGA-PEG promises a natural and efficient system for anticancer drug delivery to fight gastric cancer.

Topics: Apoptosis; Blotting, Western; Cell Proliferation; Drug Carriers; Drug Delivery Systems; Flavonoids; Humans; MicroRNAs; Nanoparticles; Polyethylene Glycols; Polyglactin 910; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Spectroscopy, Fourier Transform Infrared; Stomach Neoplasms; Tumor Cells, Cultured