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Showing papers on "Galangin published in 2015"


Journal ArticleDOI
TL;DR: Results reveal that phenolic compounds and antioxidant properties of propolis extracts were significantly dependent on the concentration of ethanol/water solvents, and these compounds seem to verify that Beijing propolis may be poplar-type propolis.
Abstract: Propolis is a natural substance known to be beneficial for human health and used as a folk medicine in many parts of the world. In this study, phenolic profiles and antioxidant properties of Beijing propolis extracted by different ethanol/water solvents were analyzed. Our results reveal that phenolic compounds and antioxidant properties of propolis extracts were significantly dependent on the concentration of ethanol/water solvents. Totally, 29 phenolic compounds were identified: 12 phenolic acids, 13 flavonoids, and 4 phenolic acid esters. In particular, 75 wt.% ethanol/water solvent may be the best for the highest extraction yield and the strongest antioxidant properties. Caffeic acid, benzyl caffeate, phenethyl caffeate, 5-methoxy pinobanksin, pinobanksin, pinocembrin, pinobanksin-3-O-acetate, chrysin, and galangin were the characteristic compounds of Beijing propolis, and these compounds seem to verify that Beijing propolis may be poplar-type propolis. In addition, the presence of high level of pinobanksin-3-O-acetate in Chinese propolis may be a novel finding, representing one-third of all phenolics.

194 citations


Journal ArticleDOI
TL;DR: Data suggest that galangin and myricetin might serve as potential anti-angiogenic agents in the prevention of ovarian cancers dependent on new blood vessel networks.

93 citations


Journal ArticleDOI
TL;DR: Galangin might function as an anti-ischemic stroke drug by improving the microenvironment of NVUs by protecting the Wnt/β-catenin pathway coupled with HIF-1α and vascular endothelial growth factor (VEGF).
Abstract: Microenvironmental regulation has become a promising strategy for complex disease treatment. The neurovascular unit (NVU), as the key structural basis to maintain an optimal brain microenvironment, has emerged as a new paradigm to understand the pathology of stroke. In this study, we investigated the effects of galangin, a natural flavonoid isolated from the rhizome of Alpina officinarum Hance, on NVU microenvironment improvement and associated signal pathways in rats impaired by middle cerebral artery occlusion (MCAO). Galangin ameliorated neurological scores, cerebral infarct volume and cerebral edema and reduced the concentration of Evans blue (EB) in brain tissue. NVU ultrastructural changes were also improved by galangin. RT-PCR and western blot revealed that galangin protected NVUs through the Wnt/β-catenin pathway coupled with HIF-1α and vascular endothelial growth factor (VEGF). VEGF and β-catenin could be the key nodes of these two coupled pathways. In conclusion, Galangin might function as an anti-ischemic stroke drug by improving the microenvironment of NVUs.

80 citations


Journal ArticleDOI
TL;DR: DLD-1 assays identified strong anti-proliferative activity associated with these components as well as chrysin, galangin and CAPE and a number of lesser known or lower concentration compounds including benzyl ferulate, benzyl isoferulate, pinostrobin, 5-phenylpenta-2,4-dienoic acid and tectochrysin.

71 citations


Journal ArticleDOI
TL;DR: The phenolic composition of the analysed propolis samples confirm their affiliation to the European poplar type propolis and the existence of two subgroups according to botanical origin.
Abstract: Introduction Propolis is a resinous natural substance collected by honeybees from different plant sources. Due to the presence of various phytochemicals, this bee-product exhibits numerous biological activities, including anti-bacterial, anti-viral, anti-inflammatory, anti-oxidant, immunostimulating and anti-tumour effects. As the chemical composition and biological activity of propolis depend on its botanical and geographical origin, searching for new bioactive substances in various types of propolis from unexplored regions is of great importance. Objective The aim of this study is the evaluation of the phenolic profile of poplar propolis samples in order to characterise Serbian propolis, to identify possible new constituents and to specify the phenolic components relevant for differentiation of poplar propolis samples into two subgroups through simultaneous analysis of poplar bud extracts. Methods Ethanolic extracts of propolis and poplar buds were comprehensively analysed using ultrahigh-performance liquid chromatography coupled with hybrid mass spectrometry, which combines the linear trap quadrupole and Orbitrap MS/MS mass analyser together with chemometric methods. Results Extensive fingerprint analysis of Serbian propolis was achieved for the first time. Seventy-five phenolic compounds were detected. Eight of them were identified in propolis for the first time. Pattern-recognition methods applied to the content of ten quantified phenolics verified the existence of two subgroups of propolis, with galangin, chrysin and pinocembrin as the most influential distinguishing factors. Conclusion The phenolic composition of the analysed propolis samples confirm their affiliation to the European poplar type propolis and the existence of two subgroups according to botanical origin.

69 citations


Journal ArticleDOI
TL;DR: Galangin effectively inhibited the TPA-induced invasion and migration of HepG2 cells through a protein kinase C/extracellular signal-regulated kinase (PKC/ERK) pathway, indicating that galangin may have widespread applications in clinical therapy as an anti-metastatic medicament.
Abstract: Galangin (3,5,7-trihydroxyflavone) is a flavonoid compound found in high concentration in lesser galangal. The objective of this study was to investigate the ability of galangin to inhibit 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced the invasion and metastasis of HepG2 liver cancer cells. First, using a cell-matrix adhesion assay, immunofluorescence assay, transwell-chamber invasion/migration assay, and wound healing assay, we observed that galangin exerted an inhibitory effect on TPA-induced cell adhesion, morphology/actin cytoskeleton arrangement, invasion and migration. Furthermore, the results of gelatin zymography and reverse transcriptase polymerase chain reaction (RT-PCR) assays showed that galangin reduced the TPA-induced enzyme activity of matrix metalloproteinase-2 (MMP-2) and matrix metalloproteinase-9 (MMP-9) in HepG2 cells; moreover, the messenger RNA level was downregulated. We also observed through a Western blotting assay that galangin strongly inhibited the TPA-induced protein expressions of protein kinase Cα (PKCα), protein kinase Cδ (PKCδ), phosphorylated extracellular signal-regulated kinase 1/2 (ERK1/2), the phospho-inhibitor of kappaBα (phospho-IκBα), c-Fos, c-Jun, and nuclear factor kappa B (NF-κB). Next, galangin dose-dependently inhibited the binding ability of NF-κB and activator protein 1 (AP-1) to MMP-2/MMP-9 promoters, respectively, resulting in the suppression of MMP-2/MMP-9 enzyme activity. The results revealed that galangin effectively inhibited the TPA-induced invasion and migration of HepG2 cells through a protein kinase C/extracellular signal-regulated kinase (PKC/ERK) pathway. Thus, galangin may have widespread applications in clinical therapy as an anti-metastatic medicament.

69 citations


Journal ArticleDOI
TL;DR: A novel role for galangin is highlighted as a promising anti-remodelling agent in asthma, which likely involves the TGF-β1-ROS-MAPK pathway.
Abstract: Galangin, a natural flavonol, has attracted much attention for its potential anti-inflammatory properties. However, its role in the regulation of airway remodelling in asthma has not been explored. The present study aimed to elucidate the effects of galangin on chronic inflammation and airway remodelling and to investigate the underlying mechanisms both in vivo and in vitro. Ovalbumin (OVA)-sensitised mice were administered with galangin 30 min before challenge. Our results showed that severe inflammatory responses and airway remodelling occurred in OVA-induced mice. Treatment with galangin markedly attenuated the leakage of inflammatory cells into bronchoalveolar lavage fluid (BALF) and decreased the level of OVA-specific IgE in serum. Galangin significantly inhibited goblet cell hyperplasia, collagen deposition and α-SMA expression. Lowered level of TGF-β1 and suppressed expression of VEGF and MMP-9 were observed in BALF or lung tissue, implying that galangin has an optimal anti-remodelling effect in vivo. Consistently, the TGF-β1-induced proliferation of airway smooth muscle cells was reduced by galangin in vitro, which might be due to the alleviation of ROS levels and inhibition of MAPK pathway. Taken together, the present findings highlight a novel role for galangin as a promising anti-remodelling agent in asthma, which likely involves the TGF-β1-ROS-MAPK pathway.

53 citations


Journal ArticleDOI
TL;DR: It is demonstrated that the antiproliferative effect of Sonoran propolis (SP) is induced through apoptosis in a B-cell lymphoma cancer cell line, M12.C3.F6, which is the first report of bioactivity of pinobanksin and some of its ester derivatives as apoptotic inducers.

51 citations


Journal ArticleDOI
TL;DR: This study reports on the inhibitory and bactericidal properties of 39 South African (SA) propolis samples and three Propolis samples from Brazil.
Abstract: Aims This study reports on the inhibitory and bactericidal properties of 39 South African (SA) propolis samples and three propolis samples from Brazil. Methods and Results Ethanolic extracts of propolis (EEP) were prepared and their antimicrobial activities tested using the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. Some samples displayed substantial antimicrobial activity with MIC and MBC values as low as 6 μg ml−1 against Staphylococcus aureus. The correlation between liquid chromatography-mass spectrometry (LC-MS) chemical data and the antimicrobial activity of propolis extracts was investigated using multivariate data analysis tools. Orthogonal projections to latent structures (OPLS) models were created for the two Gram-positive bacteria (Enterococcus faecalis and S. aureus) and Candida albicans. Using the S-plot function, it was possible to identify the bioactive constituents in propolis as chrysin, pinocembrin, galangin and pinobanksin-3-O-acetate. Conclusion The SA propolis samples tested displayed noteworthy antimicrobial activity, favourably comparable to that of the Brazilian comparator and ‘gold standard’. The observed antimicrobial activity of SA propolis can possibly be attributed to its flavonoid content. Significance and Impact of the Study Based on the good antimicrobial activity observed for SA propolis, this natural resource shows promise and should be considered for development which may contribute to growing the bio-economy in the region.

45 citations


Journal ArticleDOI
TL;DR: The results suggest that novel anti-cancer molecules should have ortho-dihydroxy groups in B-ring and hydroxyl groups at positions 3 and 5 in the A-ring system further enhance the cellular cytotoxicity of the flavonoids.
Abstract: Epidemiological studies have linked dietary consumption of plant polyphenols with lower incidence of various cancers. In particular, flavonoids (present in onion, tomato and other plant sources) induce apoptosis and cytotoxicity in cancer cells. These can therefore be used as lead compounds for the synthesis of novel anticancer drugs with greater bioavailability. In the present study, we examined the chemical basis of cytotoxicity of flavonoids by studying the structure-activity relationship of myricetin (MN), fisetin (FN), quercetin (QN), kaempferol (KL) and galangin (GN). Using single cell alkaline gel electrophoresis (comet assay), we established the relative efficiency of cellular DNA breakage as MN > FN > QN > KL > GN. Also, we determined that the cellular DNA breakage was the result of mobilization of chromatin-bound copper ions and the generation of reactive oxygen species. The relative DNA binding affinity order was further confirmed using molecular docking and thermodynamic studies through the interaction of flavonoids with calf thymus DNA. Our results suggest that novel anti-cancer molecules should have ortho-dihydroxy groups in B-ring and hydroxyl groups at positions 3 and 5 in the A-ring system. Additional hydroxyl groups at other positions further enhance the cellular cytotoxicity of the flavonoids.

44 citations


Journal ArticleDOI
TL;DR: Preliminary results constituted the first study regarding that naturally occurring product such as flavonols kaempferol and myricetin can be potent inhibitors targeting PriA.
Abstract: Staphylococcus aureus is an important etiological agent responsible for healthcare-associated infections. In this study, the effect of flavonoids on the inhibition of S. aureus PriA (SaPriA), an essential helicase for DNA replication restart, which is critical for bacterial survival, was investigated. Using vanadate-sensitive colorimetric assay, the concentration of phosphate, from ATP hydrolysis by SaPriA, was decreased to 37 and 69%, respectively, in the presence of 35 μM kaempferol and myricetin. The effect of quercetin, galangin, dihydromyricetin, and myricitrin was insignificant. From titration curve, IC50 of kaempferol for SaPriA was determined to be 22 ± 2 μM. Using fluorescence quenching, we identified that kaempferol can bind to SaPriA with K(d) of 9.1 ± 3.2 μM. To our knowledge, these preliminary results constituted the first study regarding that naturally occurring product such as flavonols kaempferol and myricetin can be potent inhibitors targeting PriA.

Journal ArticleDOI
TL;DR: It was determined that galangin, chrysin, and baicalein may slightly repress EGFR-Tyr1068 autophosphorylation after EGF treatment, phosphorylation of downstream transcription factor ELK1 and stimulate EGFP-CAR nuclear translocation in primary human hepatocytes, and this study demonstrates new approach how to test the direct CAR interaction with its ligands.

Journal ArticleDOI
TL;DR: In galangin-pretreated mice with induced CIH, increases in serum levels of several inflammatory cytokines were dramatically attenuated, and chemokines and adhesion molecules like interferon inducible protein-10, macrophage inflammatory protein-1α, and inter-cellular adhesion molecule-1 messenger RNA expressions in liver were decreased.
Abstract: Galangin is an active pharmacological ingredient from propolis and Alpinia officinarum Hance, and has been reported to have anti-inflammatory and antioxidative properties. The present study aims to reveal the effect of galangin on Concanavalin A (ConA)-induced hepatitis (CIH), a well-established animal model of immune-mediated liver injury, and to clarify the related mechanism. C57BL/6 mice were pretreated with galangin followed by ConA challenge. Results indicated that galangin inhibited ConA-induced liver damage. Mice pretreated with galangin showed more reduction of liver damage when compared with control mice pretreated with vehicle solution. In galangin-pretreated mice with induced CIH, increases in serum levels of several inflammatory cytokines, including tumor necrosis factor-α, interferon-γ, and interleukin-12 were dramatically attenuated, and chemokines and adhesion molecules like interferon inducible protein-10, macrophage inflammatory protein-1α, and inter-cellular adhesion molecule-1 messenger RNA expressions in liver were decreased. Moreover, CIH mice pretreated with galangin showed less leukocyte infiltration and T-cell activation in the liver. Further, the mechanism of the anti-inflammatory effects of galangin may be attributed to its modulation of crucial inflammatory signaling pathways, including nuclear factor kappa B and interferon-gamma/signal transducer and activator of transcription 1. Collectively, these findings suggest the preventive and therapeutic potential of galangin in immune-mediated liver injury in vivo.

Journal ArticleDOI
TL;DR: In this article, the structure-antiradical properties relationship of flavonoids (chrysin, galangin, pinocembrin and pinostrobin) and phenolic acid (caffeic acid phenethyl ester) commonly found in propolis extracts (PE) was investigated trough M05-2X functional in conjunction with the 6-31G(d,p) and 6- 31+G (d, p) basis sets, considering the structural properties, and free-radical inhibition mechanism: H-atom transfer (HAT

Journal ArticleDOI
TL;DR: In this article, a simple, reliable and fast capillary electrophoresis method was developed and partially validated for simultaneous detection of 20 polyphenolic compounds (presumed to be found in propolis and plant extracts) in less than 27 min.
Abstract: In this work, a simple, reliable and fast capillary electrophoresis method was developed and partially validated for simultaneous detection of 20 polyphenolic compounds (presumed to be found in propolis and plant extracts) in less than 27 min. The best results were obtained using 45 mM tetraborate buffer with 0.9 mM sodium dodecyl sulfate (pH = 9.35) as a background electrolyte. The polyphenolic compound order of elution was the following: resveratrol, pinostrobin, acacetin, chrysin, rutin, naringenin, isoquercitrin, umbelliferone, cinnamic acid, chlorogenic acid, galangin, sinapic acid, syringic acid, ferulic acid, kaempferol, luteolin, coumaric acid, quercetin, rosmarinic acid and caffeic acid. Linearity ranges used for compound quantification were satisfactory, presenting correlation coefficients between 0.997 and 0.999 for all 20 compounds. The method showed good performance characteristics: detection and quantification limits of 0.02 to 1.75 and 0.07 to 5.77 μg mL−1, respectively. The relative standard deviation values for repeatability did not exceed 4.86 % for intra-day assays and 5.07 % for inter-day assays. The recovery assays presented results between 87.4 and 114. 2 % for Origanum sample and between 85.0 and 111.0 % for propolis sample. The results obtained from the analysis of samples are in good correlation with literature data and bring new information about less studied samples such us aqueous Romanian propolis extracts and ethanolic Mentha aquatica extract.

Journal ArticleDOI
TL;DR: The results indicate that galangin and kaempferol suppress PMA-induced MMP-9 expression by blocking activation of NF-κB and AP-1 and these flavonols could be used as chemopreventive agents to lower the risk of diseases involving M MP-9.
Abstract: Matrix metalloproteinase (MMP)-9 degrades type IV collagen in the basement membrane and plays crucial roles in several pathological implications, including tumorigenesis and inflammation. In this study, we analyzed the effect of flavonols on MMP-9 expression in phorbol-12-myristate-13-acetate (PMA)-induced human fibrosarcoma HT-1080 cells. Galangin and kaempferol efficiently decreased MMP-9 secretion, whereas fisetin only weakly decreased its secretion. Galangin and kaempferol did not affect cell viability at concentrations up to 30 μM. Luciferase reporter assays showed that galangin and kaempferol decrease transcription of MMP-9 mRNA. Moreover, galangin and kaempferol strongly reduce IκBα phosphorylation and significantly decrease JNK phosphorylation. These results indicate that galangin and kaempferol suppress PMA-induced MMP-9 expression by blocking activation of NF-κB and AP-1. Therefore, these flavonols could be used as chemopreventive agents to lower the risk of diseases involving MMP-9.

Journal ArticleDOI
H. Zeng1, P. Huang1, Xiaoping Wang1, Jun Wu1, M. Wu1, Jian Huang1 
TL;DR: Zhang et al. as mentioned in this paper investigated whether epigenetic mechanisms, such as histone acetylation and DNA methylation, were involved in galangin-induced transcriptional regulation of BACE1.

Journal ArticleDOI
TL;DR: Systemic exposure to Galangin and its metabolites was different in rat plasma between oral and intravenous administration and further research is needed to characterize the structures of galangin conjugates and to evaluate the biological activities of these metabolites.
Abstract: Background: Galangin (3,5,7-trihydroxyflavone) is present in high concentrations in herbal medicine such as Alpinia officinarum Hance. Galangin shows multifaceted in vitro and in vivo biological activities. The number and position of hydroxyl groups in this molecule play an important role in these biological activities. However, these hydroxyl groups undergo glucuronidation and sulfation in in vitro assay system. However, the systemic exposure to galangin after dosing in animals and/or humans remains largely unknown. Thus it is not clear whether the galangin exists in the body at concentrations high enough for the biological effects. Furthermore, the metabolite identification and the corresponding plasma pharmacokinetics need to be characterized. Results: Two LC-MS/MS methods were developed and validated and successfully applied to analyze the parent drug molecules and aglycones liberated from plasma samples via β-glucuronidase hydrolysis. Our major findings were as follows: (1) The routes of administration showed significant influences on the systemic exposure of galangin and its metabolites. (2) Galangin was preferentially glucuronidated after p.o. dosing but sulfated after i.v. medication. (3) Kaempferol conjugates were detected demonstrating that oxidation reaction occurred; however, both glucuronidation and sulfation were more efficient. (4) Oral bioavailability of free parent galangin was very low. Conclusions: Systemic exposure to galangin and its metabolites was different in rat plasma between oral and intravenous administration. Further research is needed to characterize the structures of galangin conjugates and to evaluate the biological activities of these metabolites.

Journal ArticleDOI
TL;DR: A combination of flavonols has the potential to modulate sugar metabolism, both uptake into cells as evident from effects on deoxyglucose, and also further cellular glucose metabolism.
Abstract: Scope Insulin-regulated glucose metabolism in cells is critical for proper metabolic functioning, and insulin resistance leads to type 2 diabetes. We performed a human study to assess the availability of structurally related dietary flavonols and tested their ability to affect cellular glucose uptake, metabolism, and glucose transporter gene expression in a liver HepG2 cell model. Methods and results Eight healthy volunteers consumed a meal containing galangin, kaempferol, quercetin, and myricetin. In plasma, myricetin was absent, but the others were present, mostly as conjugates. In HepG2 cells, a combination of galangin, kaempferol, and quercetin (5 μM each) for 12 h increased the acute uptake of [U-14C]-glucose and 2-[U-14C]-deoxyglucose by almost 100 and ∼10%, respectively. All of the combinations increased glucose metabolism, but the effect on transport was less pronounced and mixed. A mixture of all flavonols significantly increased mRNA expression of the main glucose transporter Glut1 in HepG2 cells. Conclusion These results for the first time show the presence of galangin conjugates in human plasma, and allow direct comparison between absorption of flavonols. A combination of flavonols has the potential to modulate sugar metabolism, both uptake into cells as evident from effects on deoxyglucose, and also further cellular glucose metabolism.

Journal ArticleDOI
TL;DR: It is demonstrated that a novel AILI mouse model can be established by single propacetamol injection and compared the protective and therapeutic effects of galangin with a known liver protective extract, silymarin, and the only clinical agent for treating APAP toxicity, N-acetylcysteine, at the same dose in the model mice.
Abstract: Acetaminophen (APAP) overdose causes severe liver and kidney damage. APAP-induced liver injury (AILI) represents the most frequent cause of drug-induced liver failure. APAP is relatively insoluble and can only be taken orally; however, its prodrug, propacetamol, is water soluble and usually injected directly. In this study, we examined the time-dependent effects of AILI after propacetamol injection in mice. After analyses of alanine aminotransferase and aspartate aminotransferase activities and liver histopathology, we demonstrated that a novel AILI mouse model can be established by single propacetamol injection. Furthermore, we compared the protective and therapeutic effects of galangin with a known liver protective extract, silymarin, and the only clinical agent for treating APAP toxicity, N-acetylcysteine (NAC), at the same dose in the model mice. We observed that galangin and silymarin were more effective than NAC for protecting against AILI. However, only NAC greatly improved both the surviv...

Journal ArticleDOI
TL;DR: Looking at the structure-activity relationship of flavonols in hPXR activation may facilitate nutraceutical development efforts in the treatment of PXR-associated intestinal diseases, such as inflammatory bowel disease.

Journal ArticleDOI
TL;DR: Galangin protects human keratinocytes against UVB radiation-induced cellular damage and apoptosis via its antioxidant effects and rescued cells undergoing apoptosis through recovering mitochondrial polarization and down-regulating apoptotic proteins.
Abstract: Most skin damage caused by ultraviolet B (UVB) radiation is owing to the generation of reactive oxygen species. Phytochemicals can act as antioxidants against UVB-induced oxidative stress. This study investigated the protective effects of the flavone galangin against UVB-induced oxidative damage in human keratinocytes. Galangin efficiently scavenged free radicals and reduced UVB-induced damage to cellular macromolecules, such as DNA, lipids, and proteins. Furthermore, galangin rescued cells undergoing apoptosis induced by UVB radiation via recovering mitochondrial polarization and down-regulating apoptotic proteins. These results showed that galangin protects human keratinocytes against UVB radiation-induced cellular damage and apoptosis via its antioxidant effects.

Journal ArticleDOI
31 Mar 2015
TL;DR: In this article, nine samples of propolis from different parts of the UK were extracted and profiled by high resolution LC-MS and features were extracted into 0.02 amu windows.
Abstract: Nine samples of propolis from different parts of the UK were extracted and profiled by high resolution LC-MS. The data were aligned and features were extracted into 0.02 amu windows. The profiles contained thousands of features. In order to establish a platform for comparison of the samples the top 125 features by average peak intensity across the samples, after excluding abundant dimer peaks, were selected for further characterisation by MS 2 . Of the top 125 features around 90% of the peaks could be assigned an identity with some degree of confidence. Only ca 50% of these puta- tively identified compounds had been reported in propolis before. The compounds fell into a few major categories: fla- vonoid esters and possibly some flavonoid ethers, phenyl propanoid esters, glycerol esters, flavonoid glycosides and hy- droxylated fatty acids. Pinobanksin was the most abundant compound by average response across nine samples. The fla- vonoids pinocembrin, pinobanksin, galangin and chrysin showed a relatively low degree of variation across the samples whereas some compounds such as flavonoid esters and glycerol esters were much more variable in their abundance. The role of propolis in preventing infections in the bee hive has yet to be established but the approach taken in this paper pro- vides a potential method for trying to correlate hive health with the composition of the propolis gathered by the hive if suitable metadata were collected.

Journal ArticleDOI
TL;DR: In this paper, the effects of MK571 on the efflux of flavonoid conjugates were investigated, and it was shown that MK571 dose-dependently inhibited the intracellular biosynthesis of all flavonol glucuronides and sulphates by Caco-2 cells.

Journal ArticleDOI
TL;DR: It was showed that EEP reduced melanoma tumour progression/dissemination and extended mice life span, and this complementary therapy to classical treatment may help patients with melanoma, when used under certain conditions for which autophagy is not contraindicated.
Abstract: Melanoma the more dangerous skin cancer and metastatic melanoma still carries poor prognosis. Despite recent therapeutic advances, prolonged survival remains rare and research is still required. Propolis extracts from many countries have attracted a great deal of attention for their biological properties. We have investigated the ability of an ethanolic extract of Algerian Propolis (EEP) to control melanoma tumour growth when given as either preventive or therapeutic to mice bearing B16F1melanoma tumour. EEP given after tumour occurrence increased mice survival (+30%) and reduced tumour growth (–75%), further confirmed by measuring the Mitotic Index (–75%) and Ki-67 (–50%) expression. EEP given before or before and after tumour occurrence also reduced tumour growth, but without prolonging mice life. Isolation of B16F1 melanoma cells from resected tumour showed that preventive and curative EEP treatments reduced invasiveness by 55% and 40%, respectively compared to control. Galangin, one of the most abundant flavonoids in propolis, significantly reduced melanoma cell proliferation and induced autophagy/apoptosis dose dependently. In conclusion, we showed that EEP reduced melanoma tumour progression/dissemination and extended mice life span. This complementary therapy to classical treatment may help patients with melanoma, when used under certain conditions for which autophagy is not contraindicated.

Journal ArticleDOI
TL;DR: It is suggested that compounds being tested can modulate TRAil-R1 expression and can enhance TRAIL-mediated apoptosis.
Abstract: Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Receptors (TRAIL-R) are an important factor of apoptosis in cancer cells. There are no data about the effect of flavonols on the receptor expression on a surface of macrophage like cells. In this study, the expression level of TRAIL-R1 on murine RAW264.7 macrophages in the presence of selected flavonols: galangin, kaempferol, kaempferide and quercetin, which differ from their phenyl ring substituents, were studied. The expression of TRAIL-R1 death receptors on non-stimulated and lipopolysaccharide (LPS)-stimulated macrophages was determined using flow cytometry. The results suggested that compounds being tested can modulate TRAIL-R1 expression and can enhance TRAIL-mediated apoptosis.

Journal ArticleDOI
TL;DR: Galangin is able to inhibit Topo I activity and to reduce the unwinding rate of single stranded DNNA in tumor cells, which plays an important role in induction of A549 and H46 cell apoptosis.
Abstract: OBJECTIVE To explore the eff ect of galangin on DNA topoisomerases in lung cancer cells A549 and H46 as well on cell growth. METHODS The inhibitory effect of galangin on the growth of A549 and H46 cells was analyzed by MTT method. The effect of galangin on Topo I activity was detected by the agarose gel electrophoresis method. Furthermore, the interaction between galangin and Topo I was evaluated by fluorescence spectroscopy. Finally, the eff ect of galangin on the Topo I structure was discussed. RESULTS Galangin could induce the apoptosis of A549 and H46 cells (IC50 was 0.221 mmol/L and 0.173 mmol/L, respectively). Agarose gel electrophoresis showed that galangin exerted significant inhibitory effect on Topo I activity. Fluorescence spectrum analysis showed that galangin was able to quench Topo I fluorescence, and hydrophobic interaction was the main driving force. Circular dichroism analysis showed that galangin induced Topo I conformation change and increased the content of α-helix, which prevented the formation of active center and in turn led to the decrease in Topo I activity. Molecular simulation results showed that galangin could bind to the active center of Topo I to form hydrogen bonds with the catalytic site at Arg364 and Asn352. CONCLUSION Galangin is able to inhibit Topo I activity and to reduce the unwinding rate of single stranded DNNA in tumor cells, which plays an important role in induction of A549 and H46 cell apoptosis.

Journal ArticleDOI
TL;DR: A simple, sensitive, and robust analytical method based on ultra-performance liquid chromatography (UPLC) has been developed for the determination of galangin in rat plasma using diazepam as internal standard (IS) and was successfully applied to a pharmacokinetic study involving oral administration of Galangin to rats.

01 Jan 2015
TL;DR: In this article, the HPTLC densitometric technique was selected for quantitative and qualitative determination of galangin in Alpinia galanga and alpinia officinarum respectively.
Abstract: The aim of the work is to develop a simple, rapid, selective and cost effective HPTLC method for the determination of galangin in Alpinia galanga & Alpinia officinarum The HPTLC densitometric technique was therefore, selected for the quantitative and qualitative determination of galangin in Alpinia galanga and Alpinia officinarum respectively There are different analytical methods were used to isolate constituents from Alpinia galanga and Alpinia officinarum Literature survey reveals that no HPTLC method so far is reported for the determination of galangin in Alpinia galangal & Alpinia officinarum The present study describes HPTLC method for the qualitative and quantitative estimation of galangin Both the methods were found to be simple, precise, specific, reproducible, sensitive and accurate and can be used for the quantitation of galangin and routine quality control of raw materials and formulations containing galangin

Patent
29 Apr 2015
TL;DR: The Galangin extract can also be used in a functional food or a food for the purpose of nutrition as mentioned in this paper, and a preparation method and application thereof to treat dysmenorrhea.
Abstract: The invention belongs to the field of natural medicines, and particularly relates to a galangin extract, and a preparation method thereof and application thereof to treat dysmenorrhea. The galangin extract can also be used in a functional food or a food for the purpose of nutrition.