Synergistic activity of luteolin and amoxicillin combination against amoxicillin-resistant Escherichia coli and mode of action

Eumkeb, Griangsak; Siriwong, Supatcharee; Thumanu, Kanjana

doi:10.1016/j.jphotobiol.2012.10.006

Cited by 81 publications

(63 citation statements)

References 46 publications

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“…Luteolin, also known as 3',4',5',7'-tetrahydroxyflavone, is a flavonoid compound that has a C6-C3-C6 structure and possesses two benzene rings, an oxygen-containing ring and a 2-3 carbon double bond. This compound has been Luteolin, a novel p90 ribosomal S6 kinase inhibitor, suppresses proliferation and migration in leukemia cells LAN found to possess various beneficial properties, including antioxidant (11), anti-inflammatory (12), anti-bacterial (13) and anti-cancer activities (14)(15)(16)(17). Recently, Reipas et al (18) reported that luteolin is a novel p90 RSK inhibitor that can be considered as a promising candidate agent for the treatment of liver, lung, breast, colon, prostate, gastric and ovarian cancer, as well as melanoma.…”

Section: Introductionmentioning

confidence: 99%

Luteolin, a novel p90 ribosomal S6 kinase inhibitor, suppresses proliferation and migration in leukemia cells

Deng

Jiang

et al. 2017

Oncology Letters

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Abstract. Ribosomal S6 kinases (RSKs) are directly regulated by extracellular signal-regulated kinase (ERK) signaling and are implicated in cell growth, survival, motility and senescence. The present study observed that RSK1 was overexpressed in primary untreated leukemia patient bone marrow samples compared with the expression at the complete remission stage, using reverse transcription-quantitative polymerase chain reaction (RT-qPCR). In addition, a high RSK1 expression (relative expression ≥10) was associated with a significantly shorter overall survival (P=0.038) compared with that in patients with low RSK1 expression (relative expression <10). The current study also investigated the effect of luteolin, a novel p90 ribosomal S6 kinase (RSK) inhibitor extracted from Reseda odorata L., which shows strong biochemical functions including anti-allergy, anti-inflammation and anti-cancer functions, in MOLM-13 and Kasumi-1 leukemic cells. The cell viability, apoptosis and migration ability analysis were assessed by performing a cell counting kit-8 assay, Annexin V-FITC/PI double staining and migration filter assay, respectively. The results indicated that luteolin inhibited the growth of the leukemic cell lines through induction of apoptosis, while the migration ability was also suppressed. Overexpression of RSK1 by plasmid transfection was found to decrease the luteolin-induced apoptosis and migration capabilities. By contrast, knockdown of the RSK1 expression by small interfering RNA appeared to induce the same effect as luteolin on MOLM-13 and Kasumi-1 leukemic cells. In conclusion, these results suggest that luteolin inhibits leukemic cell proliferation and induces apoptosis by inhibition of the RSK1 pathways. IntroductionRibosomal S6 kinases (RSKs) are a family of serine/threonine protein kinases that are directly regulated by extracellular signal-regulated kinase (ERK) signaling. RSK1, a member of the RSK family, was initially identified as an X-linked gene in patients with mental retardation (1-3). Typically, RSK is expressed in the cerebellum during embryogenesis and silenced postnatally. Aberrant RSK signaling is integral for various types of cancer, including breast, colon and renal cancer, as well as melanoma. Li et al (4) observed that the p90 RSK2-cAMP response element-binding protein (CREB) pathway is commonly activated in diverse metastatic human cancer cells. Degen et al (5) also demonstrated this phenomenon, and further observed that overexpression of RSK3 and RSK1 supports cellular proliferation under the PI3K signaling pathway blockade. This occurs through the inhibition of apoptosis and regulation of cellular translation in squamous carcinoma cell through phosphorylation of RSK and eukaryotic translation initiation factor 4B. It is thus reported that RSK1 serves a role in squamous carcinoma cell growth and proliferation. In addition, Cohen et al (6) observed that RSK1 overexpression is associated with sunitinib resistance in renal cell carcinoma cell lines. Elf et al (7) also reported that, altho...

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Section: Introductionmentioning

confidence: 99%

Luteolin, a novel p90 ribosomal S6 kinase inhibitor, suppresses proliferation and migration in leukemia cells

Deng

Jiang

et al. 2017

Oncology Letters

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“…Our previous studies proved the utility of computer-aided virtual screening toward many multidrug-resistant pathogens (Skariyachan et al, 2012). Several herbal substances are known to have vital inhibitory properties against various drug targets of many gastrointestinal pathogens (Eumkeb & Chukrathok 2013;Eumkeb, Siriwong, & Thumanu, 2012;Rúa et al, 2012;Schrader, 2010). The genes responsible for multidrug properties of the mentioned organisms were screened from Entrez Gene database and the protein sequences of these genes were retrieved from Uniprot database.…”

Section: Resultsmentioning

confidence: 99%

“…From our studies, it is evident that these phytoligands have significant binding and inhibitory properties toward kanamycin-resistant protein ( Table 2). Recent studies revealed that these phytoligands have good inhibitory properties toward various MDR pathogens and their probable drug targets (Cushnie & Lamb, 2005;Eumkeb et al, 2012).…”

Section: Resultsmentioning

confidence: 99%

Exploring insights for virulent gene inhibition of multidrug resistantSalmonella typhi,Vibrio cholerae, andStaphylococcus areusby potential phytoligands viain silicoscreening

Skariyachan

Jayaprakash

Bharadwaj

et al. 2013

Journal of Biomolecular Structure and Dynamics

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In our recent studies on prevalence of multidrug resistant pathogens in Byramangala reservoir, Karnataka, India, we identified Salmonella typhi, Staphylococcus aureus, and Vibrio cholerae which had acquired multiple drug resistance (MDR) and emerged as superbugs. Hence, there is a pressing demand to identify alternative therapeutic remedies. Our study focused on the screening of herbal leads by structure-based virtual screening. The virulent gene products of these pathogens towards Kanamycin(aph), Trimethoprim(dfrA1), Methicillin (mecI), and Vancomycin (vanH) were identified as the probable drug targets and their 3D structures were predicted by homology modeling. The predicted models showed good stereochemical validity. By extensive literature survey, we selected 58 phytoligands and their drug likeliness and pharmacokinetic properties were computationally predicted. The inhibitory properties of these ligands against drug targets were studied by molecular docking. Our studies revealed that Baicalein from S. baicalensis (baikal skullcap) and Luteolin from Taraxacum officinale (dandelion) were identified as potential inhibitors against aph of S. typhi. Resveratrol from Vitis vinifera (grape vine) and Wogonin from S. baicalensis were identified as potential inhibitors against dfrA1 of S. typhi. Herniarin from Herniaria glabra (rupture worts) and Pyrocide from Daucus carota (Carrot) were identified as the best leads against dfrA1 of V. cholerae. Taraxacin of T. officinale (weber) and Luteolin were identified as potential inhibitors against Mec1. Apigenin from Coffee arabica (coffee) and Luteolin were identified as the best leads against vanH of S. aureus. Our findings pave crucial insights for exploring alternative therapeutics against MDR pathogens.

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“…The ability of isolated α-mangostin from the pericarp of GML to inhibit the activity of β -lactamase type IV isolated from E. cloacae was determined in accordance with the methods of Eumkeb et al and Richards et al [21, 22]. Concisely, benzylpenicillin, a substrate for β-lactamase type IV, was adjusted to concentrations sufficient to hydrolyze 50-60 % substrate within 5 min, β-lactamase at 100 μg/ml was used.…”

Section: Methodsmentioning

confidence: 99%

Synergism and the mechanism of action of the combination of α-mangostin isolated from Garcinia mangostana L. and oxacillin against an oxacillin-resistant Staphylococcus saprophyticus

et al. 2016

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BackgroundGlobally, staphylococci have developed resistance to many antibiotics. New approaches to chemotherapy are needed and one such approach could be to use plant derived actives with conventional antibiotics in a synergestic way. The purpose of this study was to isolate α-mangostin from the mangosteen (Garcinia mangostana L.; GML) and investigate antibacterial activity and mechanisms of action when used singly and when combined with oxacillin against oxacillin-resistant Staphylococcus saprophyticus (ORSS) strains. The isolated α-mangostin was confirmed by HPLC chromatogram and NMR spectroscopy. The minimum inhibitory concentration (MIC), checkerboard and killing curve were determined. The modes of action of these compounds were also investigated by enzyme assay, transmission electron microscopy (TEM), confocal microscopic images, and cytoplasmic membrane (CM) permeabilization studies.ResultsThe MICs of isolated α-mangostin and oxacillin against these strains were 8 and 128 μg/ml, respectively. Checkerboard assays showed the synergistic activity of isolated α-mangostin (2 μg/ml) plus oxacillin (16 μg/ml) at a fractional inhibitory concentration index (FICI) of 0.37. The kill curve assay confirmed that the viability of oxacillin-resistant Staphylococcus saprophyticus DMST 27055 (ORSS-27055) was dramatically reduced after exposure to isolated α-mangostin (2 μg/ml) plus oxacillin (16 μg/ml). Enzyme assays demonstrated that isolated α-mangostin had an inhibitory activity against β-lactamase in a dose-dependent manner. TEM results clearly showed that these ORSS-27055 cells treated with this combination caused peptidoglycan and cytoplasmic membrane damage, irregular cell shapes and average cell areas were significantly larger than the control. Clearly, confocal microscopic images confirmed that this combination caused considerable peptidoglycan damage and DNA leakage. In addition, the CM permeability of ORSS-27055 was also increased by this combination of actives.ConclusionsThese findings provide evidence that isolated α-mangostin alone has not only some activity but also shows the synergistic activity with oxacillin against ORSS-27055. The chromone and isoprenyl structures could play a significant role in its action. This synergistic activity may involve three mechanisms of action. Firstly, potential effects of cytoplasmic membrane disruption and increases permeability. Secondly, inhibit β-lactamase activity. Finally, also damage to the peptidoglycan structure. We proposes the potential to develop a novel adjunct phytopharmaceutical to oxacillin for the treatment of ORSS. Future studies require clinical trials to establish if the synergy reported can be translated to animals and humans.

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Synergistic activity of luteolin and amoxicillin combination against amoxicillin-resistant Escherichia coli and mode of action

Cited by 81 publications

References 46 publications

Luteolin, a novel p90 ribosomal S6 kinase inhibitor, suppresses proliferation and migration in leukemia cells

Luteolin, a novel p90 ribosomal S6 kinase inhibitor, suppresses proliferation and migration in leukemia cells

Exploring insights for virulent gene inhibition of multidrug resistantSalmonella typhi,Vibrio cholerae, andStaphylococcus areusby potential phytoligands viain silicoscreening

Synergism and the mechanism of action of the combination of α-mangostin isolated from Garcinia mangostana L. and oxacillin against an oxacillin-resistant Staphylococcus saprophyticus

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