curcumin and chrysin

Certain industrial chemicals and food contaminants have been demonstrated to possess neurotoxic activity and have been suspected to cause brain-related disorders in humans. Acrylamide (ACR), a confirmed neurotoxicant, can be found in trace amount in commonly consumed human aliments as a result of food processing or cooking. This discovery aroused a great concern in the public, and increasing efforts are continuously geared towards the resolution of this serious threat. The broad chemical diversity of plants may offer the resources for novel antidotes against neurotoxicants. With the goal of attenuating neurotoxicity of ACR, several plants extracts or derivatives have been employed. This review presents the plants and their derivatives that have been shown most active against ACR-induced neurotoxicity, with a focus on their origin, pharmacological activity, and antidote effects.

Topics: Acorus; Acrylamide; Acyclic Monoterpenes; Curcuma; Disulfides; Flavonoids; Humans; Monoterpenes; Neuroprotective Agents; Neurotoxicity Syndromes; Panax; Phytochemicals; Phytotherapy; Rosmarinus; Rutin; Soy Foods; Sulfinic Acids; Zingiber officinale

Mitochondrial dysfunction may lead to cardiomyocyte death in trastuzumab (TZM)-induced cardiotoxicity. Accordingly, this study was designed to evaluate the mitochondrial protective effects of curcumin, chrysin and thymoquinone alone in TZM-induced cardiotoxicity in the rats. Forty-eight male adult Wistar rats were divided into eight groups: control group (normal saline), TZM group (2.5 mg/kg I.P. injection, daily), TZM + curcumin group (10 mg/kg, I.P. injection, daily), TZM + chrysin (10 mg/kg, I.P. injection, daily), TZM + thymoquinone (0.5 mg/kg, I.P. injection, daily), curcumin group (10 mg/kg, I.P. injection, daily), chrysin group (10 mg/kg, I.P. injection, daily) and thymoquinone group (10 mg/kg, I.P. injection, daily). Blood and tissue were collected on day 11 and used for assessment of creatine phosphokinase, lactate dehydrogenase (LDH), troponin, malondialdehyde (MDA) amount, glutathione levels and mitochondrial toxicity parameters. TZM increased mitochondrial impairments (reactive oxygen species formation, mitochondrial swelling, mitochondrial membrane potential collapse and decline in succinate dehydrogenase activity) and histopathological alterations (hypertrophy, enlarged cell, disarrangement, myocytes degeneration, infiltration of fat in some areas, hemorrhage and focal vascular thrombosis) in rat heart. As well as TZM produced a significant increase in the level of CK, LDH, troponin, MDA, glutathione disulfide. In most experiments, the co-injection of curcumin, chrysin and thymoquinone with TZM restored the level of CK, LDH, troponin, MDA, GSH, mitochondrial impairments and histopathological alterations. The study revealed the cardioprotective effects of curcumin, chrysin and thymoquinone against TZM-induced cardiotoxicity which could be attributed to their antioxidant and mitochondrial protection activities.

Topics: Animals; Antioxidants; Benzoquinones; Cardiotoxicity; Curcumin; Doxorubicin; Flavonoids; Glutathione; Male; Mitochondria; Oxidative Stress; Rats; Rats, Wistar; Trastuzumab; Troponin

Cancer, which is defined as abnormal cell growth, is one of the biggest public health problems in the world. Natural compounds, such as polyphenols, are used as chemo- preventive and chemotherapeutic agents in different types of cancer owing to their antioxidant, antineoplastic, and cytotoxic properties. To improve their bioavailability and releasing behavior, hydrogel systems with high drug loadingg, stability and hydrophilic nature have been designed.. We conducted the present study to investigate the anticancer effects of curcumin and chrysin loaded in the alginate-chitosan hydrogel on breast cancer (T47D) and lung cancer (A549).. The curcumin-chrysin-loaded alginate-chitosan hydrogels were prepared through the ionic gelation mechanism utilizing CaCl2. The prepared hydrogels were studied by using the Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). The MTT and DAPI staining assays were employed for cytotoxicity and apoptosis studies of curcumin-chrysin- loaded alginate-chitosan hydrogels. The effects of the curcumin-chrysin-loaded alginate-chitosan hydrogels on the cell cycle of cell lines T47D and A549 were also evaluated using the propidium iodide staining.. The curcumin-chrysin-loaded alginate-chitosan hydrogels could significantly (p<0.05) reduce the viability and induce apoptosis. Morover G2/M causes arrest of the cell cycle in both A549 and T47D cell lines.. The alginate-chitosan hydrogels could work best as an enhanced anticancer drug delivery system.

Topics: Alginates; Antineoplastic Agents; Breast Neoplasms; Cell Line; Chitosan; Curcumin; Drug Carriers; Female; Flavonoids; Humans; Hydrogels; Lung

In this study, we explored whether co-nanoencapsulated Curcumin (Cur) and Chrysin (Chr), natural herbal compounds with antitumor activities, regulate miR-132 and miR-502c and their downstream targets, leading to the synergistic growth inhibition in MDA-MB-231 breast cancer cells. For this purpose, Cur and Chr were co-encapsulated into PLGA-PEG nanoparticles (NPs) and characterized through DLS, FTIR and FE-SEM. MTT assay and cell cycle arrest analysis revealed that CurChr-loaded NPs had a considerable synergistic cytotoxicity against MDA-MB-231 cells with more cell accumulation in G2/M phase compared to the other groups. In addition, highest percentage of cell apoptosis was acquired in cells treated with CurChr-loaded NPs according to apoptosis analysis. Real-time PCR findings revealed that co-encapsulated form of Cur and Chr than free combination could further upregulate miR-132 and miR-502c expression (

Topics: Antineoplastic Agents, Phytogenic; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Curcumin; Drug Delivery Systems; Drug Liberation; Flavonoids; Gene Expression Regulation, Neoplastic; Humans; MicroRNAs; Nanoparticles; Polyethylene Glycols; Polyglactin 910; Spectroscopy, Fourier Transform Infrared; Up-Regulation

The aim of the present study was to produce chrysin-curcumin-loaded PCL-PEG nanofibres by an electrospinning technique and to evaluate the biological activity of the chrysin-curcumin-loaded PCL-PEG fibres for wound healing and its related genes using in vivo methods.. The electrospinning method was carried out for the preparation of the chrysin, curcumin and chrysin-curcumin-loaded PCL-PEG nanofibres with different concentrations. FTIR and SEM were performed to characterize the chemical structures and morphology of the nanofibres. In vitro drug release, as well as in vivo wound-healing studies were investigated in male rats. The expressions of genes related to the wound-healing process were also evaluated by real-time PCR.. Our study showed that the chrysin-curcumin-loaded nanofibres have anti-inflammatory properties in several stages of the wound-healing process by affecting the IL-6, MMP-2, TIMP-1, TIMP-2 and iNOS gene expression. Our results demonstrated that the effect of the chrysin-loaded nanofibre, the curcumin-loaded nanofibre and the chrysin-curcumin-loaded nanofibre in the wound-healing process is dose dependent and in accordance with the obtained results in that it might affect the inflammation phase more than the other stages of the wound-healing process.. We have introduced chrysin-curcumin-loaded PCL-PEG nanofibres as a novel compound for shortening the duration of the wound-healing process.

Topics: Animals; Curcumin; Drug Carriers; Drug Liberation; Flavonoids; Gene Expression Regulation, Enzymologic; Interleukin-6; Male; Matrix Metalloproteinase 2; Nanofibers; Nitric Oxide Synthase Type II; Polyesters; Polyethylene Glycols; Rats; Tissue Inhibitor of Metalloproteinase-1; Tissue Inhibitor of Metalloproteinase-2; Wound Healing

Telomerase is known as a global therapeutic target in cancer cells due to its main role in tumorigenesis. Nowadays, it is proposed new treatment methods based on molecular target therapy by bioactive substances such as curcumin and chrysin with fewer side effects than other chemical drugs. But due to their low aqueous solubility and high clearance in the bloodstream it can be used of nanoparticles to increase their half-life and biocompatibility of them. Therefore, the goal of this study was to evaluate the effect of Chrysin-Curcumin on the expression of telomerase gene in SW480 colorectal cancer cell line.. PLGA-PEG nanoparticles synthesized and were confirmed using by the scanning electron microscope (SEM) and FTIR Spectroscopy. After treatment of SW480 cells by curcumin and chrysin loaded nanoparticles, their toxicity to cancer cells, was evaluated by MTT. Then, the inhibition of hTERT gene expression was measured using qRT-PCR method.. The results of MTT test showed nanocapsulated curcumin and chrysin compared with free forms of these compounds have high synergistic effect on sw480 cells. Also, real time-PCR showed significant decrease in hTERT gene expression in SW480 cells that treated with nano-curcumin and nano-chrysin compare to untreated cells.. Nano-encapsulation of curcumin and chrysin enhanced delivery of these compounds to SW480 colorectal cancer cells and therefore it can be conclude that PLGA-PEG nanoparticles promote anticancer effects of curcumin-chrysin by increasing bioavailability and the solubility of these drugs.

Topics: Cell Line, Tumor; Cell Survival; Curcumin; Drug Combinations; Drug Synergism; Flavonoids; Gene Expression Regulation; Humans; Nanoparticles; Polyesters; Polyethylene Glycols; Telomerase

Due to the high rate of drug resistance among malignant melanoma cases, it seems necessary to introduce an efficient pharmaceutical approach to melanoma treatment. For this purpose, Curcumin (Cur) and Chrysin (Chr), two natural anti-cancers, were co-encapsulated in PLGA-PEG nanoparticles (NPs), characterized by DLS, FTIR and FE-SEM and investigated for their effects on MMPs, TIMPs and TERT genes expression in C57B16 mice bearing B16F10 melanoma tumours. The results showed that the expression of MMP-9, MMP-2 and TERT genes were significantly decreased in all treated groups compared to the control. This reduction had the highest amount in CurChr NPs group and then CurChr group for each three genes. Likewise, the expression of TIMP-1 and TIMP-2 genes was significantly increased in all treated groups, compared to the control. Combination groups showed the highest rise in expression of these two genes and the observed increase was greater in nano groups. Moreover, the highest melanoma tumour growth inhibition was detected for CurChr NPs, followed by CurChr = Cur NPs > Cur > Chr NP > Chr. Overall, it is speculated that the nano-combination of Cur and Chr into polymeric NPs with a one-step fabricated co-delivery system may be a promising and convenient approach to improve their efficiency in melanoma cancer therapy.

Topics: Animals; Capsules; Cell Proliferation; Curcumin; Disease Models, Animal; Disease Progression; Drug Carriers; Flavonoids; Gene Expression Regulation, Neoplastic; Male; Matrix Metalloproteinases; Melanoma, Experimental; Mice; Mice, Inbred C57BL; Nanoparticles; Neoplasm Metastasis; Polyethylene Glycols; Polylactic Acid-Polyglycolic Acid Copolymer; Telomerase; Tissue Inhibitor of Metalloproteinases

Central nervous system (CNS) drug delivery is often hampered due to the insidious nature of the blood-brain barrier (BBB). Nose-to-brain delivery via olfactory pathways have become a target of attention for drug delivery due to bypassing of the BBB. The antioxidant properties of phytochemicals make them promising as CNS active agents but possess poor water solubility and limited BBB penetration. The primary aim of this study was the development of mesoporous silica nanoparticles (MSNs) loaded with the poorly water-soluble phytochemicals curcumin and chrysin which could be utilised for nose-to-brain delivery. We formulated spherical MSNP using a templating approach resulting in ∼220nm particles with a high surface porosity. Curcumin and chrysin were successfully loaded into MSNP and confirmed through Fourier transformation infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and HPLC approaches with a loading of 11-14% for curcumin and chrysin. Release was pH dependant with curcumin demonstrating increased chemical stability at a lower pH (5.5) with a release of 53.2%±2.2% over 24h and 9.4±0.6% for chrysin. MSNP were demonstrated to be non-toxic to olfactory neuroblastoma cells OBGF400, with chrysin (100μM) demonstrating a decrease in cell viability to 58.2±8.5% and curcumin an IC

Topics: Administration, Intranasal; Animals; Brain; Cell Line, Tumor; Cell Survival; Curcumin; Drug Delivery Systems; Drug Liberation; Flavonoids; Nanoparticles; Porosity; Silicon Dioxide; Swine

The only FDA approved medication for colorectal cancer (CRC) prevention is celecoxib. Its adverse effects underline the need for safer drugs. Polyphenols like resveratrol are in clinical trials for this purpose. This study aimed at examining effects of resveratrol alone and in combination with curcumin or chrysin on UGT induction in Caco-2 cells. Phytochemical combinations were selected using drug combination analyses of various anti-proliferation ratios of resveratrol+curcumin and resveratrol+chrysin.. Cell proliferation and UGT1A1 induction assays were carried out with individual polyphenols and combinations. Cell viability was determined with AlamarBlue assays. UGT1A1 mRNA was quantified via real time RT-PCR. UGT activity was determined with 4-methylumbelliferone (4MU) glucuronidation.. Cell proliferation IC(50) estimates (± SE) for resveratrol, curcumin and chrysin were 20.8 ± 1.2, 20.1 ± 1.1 and 16.3 ± 1.3μM respectively. Combination of anti-proliferative effects showed additivity for resveratrol+chrysin and resveratrol+curcumin. Resveratrol at its IC(50) mediated a four-fold induction of UGT1A1 mRNA in a concentration independent manner. Chrysin at its IC(50) induced UGT1A1 expression seven-fold while Curcumin at its IC(90) mediated a two-fold induction. The 20 μM:40μ M resveratrol+curcumin and 20 μM :32 μM resveratrol+chrysin combinations mediated the greatest increases in mRNA expression (12 and 22 folds respectively). Significant increase in 4-MU glucuronidation was observed with combinations exhibiting maximal mRNA induction.. Phytochemical combinations can offer greater chemoprevention than single agents. These chemicals might offer safer options than present synthetic therapeutics for CRC prevention.

Topics: Anticarcinogenic Agents; Caco-2 Cells; Cell Proliferation; Cell Survival; Colorectal Neoplasms; Curcumin; Dose-Response Relationship, Drug; Drug Synergism; Drug Therapy, Combination; Enzyme Induction; Flavonoids; Glucuronides; Glucuronosyltransferase; Humans; Inhibitory Concentration 50; Resveratrol; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Stilbenes

The mechanism of membrane interactions of most of the flavonoids in the presence of transition-metal ions is not well-understood. To understand this phenomenon, the present work aims to synthesize a chrysin-copper complex at room temperature and investigate its influence on the electrical characteristics of planar lipid bilayers. The chrysin-copper complex was characterized by various spectroscopic techniques and was found to have a metal/ligand ratio of 1:2 and of cationic nature. Its ability to inhibit 1,1'-diphenyl-2-picrylhydrazyl (DPPH) radicals was not significant at alkaline pH because of the involvement of the 5-hydroxy group in coordination with the copper ion compared to its parent flavonoid, chrysin (p < 0.05). The addition of different concentrations (20-100 μM) of chrysin and the chrysin-copper complex to lipid bilayers decreases the resistance, indicating a strong surface interaction and partial insertion into the bilayer near the lipid-water interface. The dose-dependent reduction in resistance as a result of the chrysin-copper complex is more pronounced in comparison to chrysin, implying that the bulkier and charged chrysin-copper complex displays greater ability to distort the lipid bilayer architecture. These conclusions were further confirmed by curcumin-loaded liposome permeabilization studies, where both chrysin and its Cu(II) complex increased the fluidity in a dose-dependent manner. However, the extent of fluidization by the chrysin-copper complex was nearly twice that of chrysin alone (p < 0.05). The implications of these surface interactions of chrysin and its copper complex on cell membranes were studied using a hypotonic hemolysis assay. Our results demonstrate that, at low concentrations (20 μM), the chrysin-copper complex exhibited twice the protection against hypotonic stress-induced membrane disruption when compared to chrysin. However, this stabilizing effect gradually decreased and became comparable to chrysin at higher concentrations. This biphasic behavior of the chrysin-copper complex could further be explored for therapeutic applications.

Topics: Cell Membrane; Copper; Curcumin; Electrochemistry; Flavonoids; Lipid Bilayers; Models, Molecular; Molecular Conformation; Organometallic Compounds