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1.
Bioorg Chem ; 118: 105487, 2022 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-34798455

RESUMO

Two series of pyrazoline compounds were designed and synthesized as antiproliferative agents by VEGFR pathway inhibition. All synthesized compounds were screened by the National Cancer Institute (NCI), Bethesda, USA for anticancer activity against 60 human cancer cell lines. Compound 3f exhibited the highest anticancer activity on the ovarian cell line (OVCAR-4) with IC50 = 0.29 µM and on the breast cell line (MDA-MB-468) with IC50 = 0.35 µM. It also exhibited the highest selectivity index (SI = 74). Compound 3f caused cell cycle arrest in OVCAR-4 cell line at the S phase which consequently inhibited cell proliferation and induced apoptosis. Moreover, 3f showed potent down-regulation of VEGF and p-VEGFR-2. Docking studies showed that compound 3f interacts in a similar pattern to axitinib on the VEGFR-2 receptor. The same compound was also able to fit into the gorge of STAT3 binding site, the transcription factor for VEGF, which explains the VEGF down-regulation.

2.
J Microbiol Biotechnol ; 31(8): 1079-1087, 2021 Aug 28.
Artigo em Inglês | MEDLINE | ID: mdl-34226400

RESUMO

Gentisic acid (GA), a benzoic acid derivative present in various food ingredients, has been shown to have diverse pharmaceutical activities such as anti-carcinogenic, antioxidant, and hepatoprotective effects. In this study, we used a co-culture system to investigate the mechanisms of the anti-inflammatory and anti-adipogenic effects of GA on macrophages and adipocytes, respectively, as well as its effect on obesity-related chronic inflammation. We found that GA effectively suppressed lipopolysaccharide-stimulated inflammatory responses by controlling the production of nitric oxide and pro-inflammatory cytokines and modulating inflammation-related protein pathways. GA treatment also inhibited lipid accumulation in adipocytes by modulating the expression of major adipogenic transcription factors and their upstream protein pathways. Furthermore, in the macrophage-adipocyte co-culture system, GA decreased the production of obesity-related cytokines. These results indicate that GA possesses effective anti-inflammatory and anti-adipogenic activities and may be used in developing treatments for the management of obesity-related chronic inflammatory diseases.

3.
Food Chem ; 361: 129866, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34091399

RESUMO

This study investigated the in vitro bioactivities of extracts obtained from viscera, spines, shells, and gonads of Stomopneustes variolaris using subcritical water extraction (SWE) at 110 °C, 150 °C, 190 °C, and 230 °C and Soxhlet extraction. The highest amounts of phenolics (22.68 ± 0.05 mg GAE/g), flavonoids (27.11 ± 0.10 mg RE/g), and proteins (40.25 ± 0.84 mg BSA/g) were recorded from gonads at 230 °C, whereas maximum sugar content (23.38 ± 1.30 mg glucose/g) was in viscera at 150 °C. Gonads at 230 °C exhibited the highest DPPH activity (78.68 ± 0.18%), whereas viscera at 150 °C exhibited the highest ABTS+ (98.92 ± 1.27%) and protein denaturation inhibition activity (37.13 ± 9.94%). Viscera at 110 °C claimed the highest amylase inhibition (42.46 ± 0.83%), and spines at 150 °C had the highest anticancer activity (IC50 = 767.47 µg/mL). SWE achieved superior results in bioactive compound recovery and detected higher levels of bioactivities (p < 0.05). Results suggest processing sea urchin extracts via SWE has potential application to the food and pharmaceutical industries.


Assuntos
Produtos Biológicos/farmacologia , Fracionamento Químico/métodos , Ouriços-do-Mar/química , Animais , Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Produtos Biológicos/isolamento & purificação , Avaliação Pré-Clínica de Medicamentos , Flavonoides/análise , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Química Verde , Células HeLa , Humanos , Hipoglicemiantes/isolamento & purificação , Hipoglicemiantes/farmacologia , Fenóis/análise , Fenóis/isolamento & purificação , Fenóis/farmacologia , Água/química
4.
Mitochondrial DNA B Resour ; 6(3): 1007-1008, 2021 Mar 18.
Artigo em Inglês | MEDLINE | ID: mdl-33796718

RESUMO

Halocynthia aurantium (Stolidobranchia: Pyuridae) is a species of tunicate of commercial value that is commonly found in the northern Pacific Ocean and in the Bering Sea. Here, we determined the complete mitogenome of sea peach H. aurantium using 150 PE high-throughput sequencing. The assembled mitogenome is 14,979 bp in length (overall A + T contents 56.2%), and contains 13 protein-coding genes, 21 transfer RNAs, two ribosomal RNAs. Phylogenetic analysis of the mitogenome sequence of H. aurantium fully resolved it in a clade with H. roretzi. These data and results will be useful for future studies on the evolution of the Halocynthia and the Pyuridae.

5.
J Xray Sci Technol ; 29(3): 383-395, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33749628

RESUMO

This study analyzes the response of increasing radiation dose to the pork tenderloin tissue. Considering its significant cell structure, pork tenderloin tissue samples are selected for the experimental objects to measure their electrical impedance characteristics. This study proposes and investigates an effective approach to characterize the variation of the internal change of the components of pork tenderloin tissues caused by radiation. Changes in the pork tenderloin tissues are that the gap of the myotome is more far apart with increase of radiation dose because of the destroyed Myofibrils under the damage. With the increase of radiation dose, the impedance value of the pork tenderloin tissue decreases. Each of mean differences in the impedance values before and after irradiation dose under 1 Gy, 2 Gy and 4 Gy show 0.55±0.03, 1.09±0.14 and 1.97±0.14, respectively. However, the mean difference substantially increases to 13.08±0.16 at irradiation dose of 10 Gy. Thus, the cell membrane shows the most severe rupture at a radiation dose of 10 Gy. Changes in the microstructure of the irradiated pork tenderloin tissue samples are also checked and validated by a transmission electron microscope.


Assuntos
Impedância Elétrica , Relação Dose-Resposta à Radiação
6.
Bioorg Chem ; 107: 104630, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33476864

RESUMO

Exaggerated inflammatory responses may cause serious and debilitating diseases such as acute lung injury and rheumatoid arthritis. Two series of chalcone derivatives were prepared as anti-inflammatory agents. Methoxylated phenyl-based chalcones 2a-l and coumarin-based chalcones 3a-f were synthesized and compared for their inhibition of COX-2 enzyme and nitric oxide production suppression. Methoxylated phenyl-based chalcones showed better inhibition to COX-2 enzyme and nitric oxide suppression than the coumarin-based chalcones. Among the 18 synthesized chalcone derivatives, compound 2f exhibited the highest anti-inflammatory activity by inhibition of nitric oxide concentration in LPS-induced RAW264.7 macrophages (IC50 = 11.2 µM). The tested compound 2f showed suppression of iNOS and COX-2 enzymes. Moreover, compound 2f decreases in the expression of NF-κB and phosphorylated IκB in LPS-stimulated macrophages. Finally, docking studies suggested the inhibition of IKKß as a mechanism of action and highlighted the importance of 2f hydrophobic interactions.


Assuntos
Anti-Inflamatórios/farmacologia , Chalconas/química , Cumarínicos/química , Regulação para Baixo/efeitos dos fármacos , Desenho de Fármacos , Óxido Nítrico/metabolismo , Animais , Anti-Inflamatórios/síntese química , Anti-Inflamatórios/metabolismo , Sítios de Ligação , Domínio Catalítico , Sobrevivência Celular/efeitos dos fármacos , Chalconas/metabolismo , Chalconas/farmacologia , Ciclo-Oxigenase 2/química , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/síntese química , Inibidores de Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Lipopolissacarídeos/farmacologia , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Simulação de Acoplamento Molecular , NF-kappa B/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Óxido Nítrico Sintase Tipo II/metabolismo , Células RAW 264.7
7.
J Immunol Res ; 2020: 1731457, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33299895

RESUMO

Tumor microenvironment components dictate the growth and progression of various cancers. Tumor-associated macrophages are the most predominant cells in TME and play a major role in cancer invasiveness. Gastric cancer is one of the most common cancers in Asia, and recently, various cases of resistance to fluorouracil treatment have been reported. In this study, we investigated the role of alternatively activated macrophages in the resistance of AGS gastric cancer cells to fluorouracil. THP-1 cells were polarized using recombinant human IL-4, then were cocultured with AGS cells treated with fluorouracil. Cell viability, Western blot, immunofluorescence, and cell invasion were performed for this investigation. Our results demonstrated that polarized macrophages initiated the survival of treated AGS cells and induced the resistance in AGS by upregulating the expression of integrin ß3, focal adhesion protein (FAK), and cofilin proteins. These results reveal that integrin ß3, focal adhesion protein (FAK), and cofilin proteins are potential targets for the improvement of fluorouracil efficacy in gastric cancer treatment.


Assuntos
Fatores de Despolimerização de Actina/genética , Resistencia a Medicamentos Antineoplásicos , Fluoruracila/farmacologia , Proteína-Tirosina Quinases de Adesão Focal/genética , Integrina beta3/genética , Macrófagos/imunologia , Macrófagos/metabolismo , Fatores de Despolimerização de Actina/metabolismo , Linhagem Celular Tumoral , Movimento Celular , Polaridade Celular , Resistencia a Medicamentos Antineoplásicos/genética , Resistencia a Medicamentos Antineoplásicos/imunologia , Proteína-Tirosina Quinases de Adesão Focal/metabolismo , Humanos , Integrina beta3/metabolismo , Ativação de Macrófagos/imunologia , NF-kappa B/metabolismo , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Neoplasias Gástricas/etiologia , Neoplasias Gástricas/metabolismo , Neoplasias Gástricas/patologia
8.
Nutr Cancer ; : 1-13, 2020 Dec 26.
Artigo em Inglês | MEDLINE | ID: mdl-33356601

RESUMO

Cancer is one of the leading causes of death and one of the most important public health problems in the world. And every year, millions of new cancers and hundreds of thousands of cancer-related deaths are reported worldwide. In recent decades, a number of biologically active polysaccharides and polysaccharide-protein complexes have been isolated from plants, lichen, algae, yeast, fungi and mushroom, and due to their antitumor and immunomodulatory properties, these compounds have received considerable attention. Overall, the two key mechanisms by which polysaccharides act on tumor cells are direct action (inhibition of cancer cell growth and induction of programmed cell death/apoptosis) and indirect action (stimulation of immunity). Immunosuppressive effects are recognizable in both cancer patients and tumor bearing animals, suggesting that the immune system plays an important role in the immune surveillance of cancer cells. Thus, enhancement of the host immune response has been evaluated as a possible way of inhibiting tumor growth without damaging the host. In addition to their therapeutic and prophylactic properties, the polysaccharides are effective and less toxic than chemotherapy. The anticancer activity and immunomodulatory effects of most polysaccharides have shown the promising and real potential for the benefits of human health.

9.
Liver Cancer ; 9(2): 182-192, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32399432

RESUMO

Background/Aim: Uniform treatment of hepatocellular carcinoma (HCC) with molecular targeted drugs (e.g., sorafenib) results in a poor overall tumor response when tumor subtyping is absent. Patient stratification based on actionable gene expression is a method that can potentially improve the effectiveness of these drugs. Here we aimed to identify the clinical application of actionable genes in predicting response to sorafenib. Methods: Through quantitative real-time reverse transcription PCR, we analyzed the expression levels of seven actionable genes (VEGFR2, PDGFRB, c-KIT, c-RAF, EGFR, mTOR, and FGFR1) in tumors versus noncancerous tissues from 220 HCC patients treated with sorafenib. Our analysis found that 9 responders did not have unique clinical features compared to nonresponders. A receiver operating characteristic curve evaluated the predictive performance of the treatment benefit score (TBS) calculated from the actionable genes. Results: The responders had significantly higher TBS values than the nonresponders. With an area under the curve of 0.779, a TBS combining mTOR with VEGFR2, c-KIT, and c-RAF was the most significant predictor of response to sorafenib. When used alone, sorafenib had a 0.7-3% response rate among HCC patients, but when stratifying the patients with actionable genes, the tumor response rate rose to 15.6%. Furthermore, actionable gene expression is significantly correlated with tumor response. Conclusions: Our findings on patient stratification based on actionable molecular subtyping potentially provide a therapeutic strategy for improving sorafenib's effectiveness in treating HCC.

10.
Int J Biol Macromol ; 157: 484-493, 2020 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-32325075

RESUMO

In this study, pressurized liquid extraction (PLE) of polyphenolic-polysaccharide (PP) from Pseuderanthemum palatiferum (Nees) Radlk. leaves was carried out and compared with a conventional technique using 0.1 M sodium hydroxide. The extracts were purified according to the method reported previously to obtain PP conjugates which were further studied about chemical profiles and anticoagulant activity. Fourier-transform infrared spectroscopy (FTIR), UV-Vis, nuclear magnetic resonance (NMR), gel permeation chromatography (GPC), and spectrophotometry analysis were used to characterize the selected PP conjugates. The results showed that PP conjugates comprised of carbohydrate, phenolic, and protein constituents with the yield ranged from 2.76% to 14.34%. Seven mono sugars containing in all conjugates were determined using high-performance liquid chromatography (HPLC), namely, arabinose, fucose, galactose, glucose, mannose, rhamnose, and xylose. PP conjugates obtained from PLE at 150 °C (PP-PLE5) exhibited better anticoagulant activity than those found at 200 °C and comparable to that of the conventional technique. On gel permeation chromatography, PP-PLE5 showed a broad molecular mass from 6 to 642 kDa. From the obtained results, PLE can be used as a green effective technique for the recovery of PP conjugate from P. palatiferum leaves.


Assuntos
Anticoagulantes/química , Anticoagulantes/farmacologia , Fenóis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polissacarídeos/química , Anticoagulantes/isolamento & purificação , Fracionamento Químico , Cromatografia em Gel , Cromatografia Líquida de Alta Pressão , Química Verde , Extratos Vegetais/isolamento & purificação , Espectroscopia de Infravermelho com Transformada de Fourier
11.
Cancers (Basel) ; 12(4)2020 Mar 26.
Artigo em Inglês | MEDLINE | ID: mdl-32225122

RESUMO

Preoperative chemoradiotherapy (PCRT) and subsequent surgery is the standard multimodal treatment for locally advanced rectal cancer (LARC), albeit PCRT response varies among the individuals. This creates a dire necessity to identify a predictive model to forecast treatment response outcomes and identify patients who would benefit from PCRT. In this study, we performed a gene expression study using formalin-fixed paraffin-embedded (FFPE) tumor biopsy samples from 156 LARC patients (training cohort n = 60; validation cohort n = 96); we identified the nine-gene signature (FGFR3, GNA11, H3F3A, IL12A, IL1R1, IL2RB, NKD1, SGK2, and SPRY2) that distinctively differentiated responders from non-responders in the training cohort (accuracy = 86.9%, specificity = 84.8%, sensitivity = 81.5%) as well as in an independent validation cohort (accuracy = 81.0%, specificity = 79.4%, sensitivity = 82.3%). The signature was independent of all pathological and clinical features and was robust in predicting PCRT response. It is readily applicable to the clinical setting using FFPE samples and Food and Drug Administration (FDA) approved hardware and reagents. Predicting the response to PCRT may aid in tailored therapies for respective responders to PCRT and improve the oncologic outcomes for LARC patients.

12.
Mitochondrial DNA B Resour ; 5(3): 3538-3539, 2020 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-33458232

RESUMO

The complete mitochondrial genome of pitted stingray, Bathytoshia brevicaudata (Myliobatiformes: Dasyatoidea) was investigated by next-generation sequencing. The analyzed mitochondrial genome was 17,640 nucleotides in length and had 59.2% for AT contents. This genome contains 2 ribosomal RNA genes, 13 protein-coding genes, 22 transfer RNA genes. and 1 putative control region. Five protein-coding genes (ATPase6, COII, ND2, ND3, ND4) including incomplete stop codons and four tRNAs have atypical codons. The phylogenetic inference including 13 species of the same family revealed a close relationship with Pteroplatytrygon violacea. This is the first mitochondrial genome report from genus Bathytoshia.

13.
Int J Mol Med ; 44(6): 2321-2328, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-31661129

RESUMO

Kaempferol­3­O­ß­rutinoside is one of the compounds isolated from tartary buckwheat (Fagopyrum tatricum), and its biological effects have not been studied yet. The present study examined the anti­inflammatory effects of kaempferol­3­O­ß­rutinoside and explore its regulatory mechanisms in lipopolysaccharide (LPS)­induced macrophage RAW264.7 cells. Kaempferol­3­O­ß­rutinoside exhibited no cytotoxic effect in RAW 264.7 macrophage and 293 cell lines up to 300 µM. As the concentration of kaempferol­3­O­ß­rutinoside was increased, the activity of nitric oxide was inhibited in LPS­stimulated RAW264.7 cells. In addition, kaempferol­3­O­ß­rutinoside treatment downregulated the expression of inflammation­related cytokines tumor necrosis factor­α and interleukin­6 in LPS­stimulated RAW264.7 cells. Furthermore, kaempferol­3­O­ß­rutinoside treatment suppressed inflammatory­mediated factors, such as inducible nitric oxide synthase and cyclooxyganse­2. These inflammation­related proteins are known to be regulated by NF­κB and mitogen­activated protein kinase (MAPK) signaling, therefore the effect of kaempferol­3­O­ß­rutinoside on these pathways was investigated. The results demonstrated that kaempferol­3­O­ß­rutinoside decreased the expression of inhibitor of κB (IκB) protein and IκB kinases; as a result, the nuclear translocation and expression of NF­κB was inhibited in LPS­stimulated RAW264.7 cells. Furthermore, kaempferol­3­O­ß­rutinoside inhibited the phosphorylation of p38, extracellular signal­regulated kinase and stress­activated protein kinase in LPS­stimulated RAW264.7 cells. Thus, the present data demonstrated that kaempferol­3­O­ß­rutinoside suppressed inflammation­related gene expression through the NF­κB and MAPK pathways, and suggested that it may be a useful reagent in pharmacological research.


Assuntos
Proliferação de Células/efeitos dos fármacos , Mediadores da Inflamação/farmacologia , Inflamação/tratamento farmacológico , Quempferóis/farmacologia , Animais , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Inflamação/induzido quimicamente , Inflamação/genética , Inflamação/patologia , Lipopolissacarídeos/toxicidade , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , NF-kappa B/genética , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/genética , Fosforilação/efeitos dos fármacos , Células RAW 264.7
14.
Colloids Surf B Biointerfaces ; 183: 110455, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31493630

RESUMO

Green chemistry is beneficial for the production of eco-friendly and stable nanoparticles using biological agents. The present study was performed to explore the potential of the marine bacterium Paracoccus haeundaensis BC74171T for the extracellular synthesis of gold nanoparticles (AuNPs). Cell-free supernatant-mediated AuNPs were characterized by different techniques and analyzed for their antioxidant activity and antiproliferative effect on normal and cancer cells. Visual observations indicated the formation of AuNPs by the development of a ruby red color and were confirmed by a UV-vis absorbance peak at about 535 nm. The synthesized AuNPs were spherical in shape and had an average size of 20.93 ± 3.46 nm, as determined by transmission electron microscopy and a dynamic light scattering particle size analyzer, respectively. From Fourier transform infrared spectroscopy, the interaction of functional groups was determined and the presence of biomaterial on the AuNP surface was confirmed. Concentration-dependent antioxidant activity of AuNPs was observed by the 2,2-diphenyl-1-picrylhydrazyl method. The AuNPs synthesized do not show growth inhibition on HaCaT and HEK293 normal cells, while they show concentration-dependent growth inhibition in the case of A549 and AGS cancer cells. Thereby, this study proves that AuNP synthesis using P. haeundaensis is a facile method and that the AuNPs synthesized are non-toxic to human cells, which indicates that they can be useful in biomedical applications.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Proliferação de Células/efeitos dos fármacos , Ouro/química , Nanopartículas Metálicas/química , Paracoccus/metabolismo , Células A549 , Antibacterianos/química , Antioxidantes/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Espaço Extracelular/metabolismo , Células HEK293 , Humanos , Testes de Sensibilidade Microbiana , Água do Mar/microbiologia
15.
Int J Biol Macromol ; 137: 844-852, 2019 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-31295479

RESUMO

Fucoidan is a sulfated hetero-polysaccharide, found in cell-wall composition of brown algae. Recent studies have reported the role of fucoidan in the induction of Endoplasmic Reticulum (ER) stress-related cell death in cancer cells but the mechanism of action of fucoidan in cervical HeLa cells is not well-known. The purpose of this study was to investigate if fucoidan induces HeLa cells death through ER-stress-related cell death and G1 phase arrest. 200-600 µg/ml concentrations of fucoidan inhibited the proliferation of HeLa cells after 48 h of treatment while investigated normal cell lines (HaCaT: Keratinocytes and HEK-293: embryonic kidney) were not affected. The exposure of HeLa cells to these concentrations of fucoidan induced phosphorylation of ER stress sensors followed by upregulation of Bip/GRP78, CHOP expression which triggered a buildup of malfolded proteins in ER, therefore, initiating unfolded protein response (UPR) mechanism. In addition, intracellular calcium levels were elevated following the treatment suggesting that this contributed to the ER stress-induced apoptosis. Fucoidan treatment caused G1phase arrest by inducting CDKIs and inhibiting CDKs and Cyclins as well as apoptosis by activating the mitochondrial-dependent pathway in HeLa cells. We demonstrated that Fucoidan inhibits HeLa cells proliferation by inducing apoptosis, G1 phase arrest, ER stress, and mitochondrial-mediated apoptosis.


Assuntos
Antineoplásicos/farmacologia , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Polissacarídeos/farmacologia , Apoptose/efeitos dos fármacos , Cálcio/metabolismo , Ciclo Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Células HeLa , Homeostase/efeitos dos fármacos , Humanos
16.
Drug Dev Res ; 80(4): 504-512, 2019 06.
Artigo em Inglês | MEDLINE | ID: mdl-30860609

RESUMO

The fungus Chaetomium sp. is a causative agent of infections in humans and is ubiquitous in the natural environment. The secondary metabolites of this genus exhibit many biological activities, including antifungal activity and toxicity in mitochondria. In this study, we isolated cristazine from the fungus C. cristatum, which has the potential to inhibit the growth of human epidermoid carcinoma (A431) cells in a dose- and time-dependent manner. Its inhibitory activity was examined using a cell viability assay and cell death was elucidated by western blot analysis. Cristazine triggered apoptotic cell death via the Type I death receptor pathway including the activation of caspases and other target proteins. However, cristazine did not have any effect on mitochondrial apoptotic proteins such as Bid, cytochrome c, and apoptosis-inducing factor. Cristazine inhibited the cell cycle progression by arresting the G1 /S phase and up-regulating the inhibitory proteins of cyclin-dependent kinases. Thus, cristazine has great potential for inducing apoptosis in A431 cells via both cell cycle arrest and the inhibition of cell growth.


Assuntos
Alcaloides/farmacologia , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Piperazinas/farmacologia , Receptores de Morte Celular/metabolismo , Alcaloides/isolamento & purificação , Antineoplásicos/isolamento & purificação , Carcinoma de Células Escamosas/metabolismo , Carcinoma de Células Escamosas/patologia , Técnicas de Cultura de Células , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Chaetomium/química , Relação Dose-Resposta a Droga , Humanos , Estrutura Molecular , Piperazinas/isolamento & purificação , Neoplasias Cutâneas/metabolismo , Neoplasias Cutâneas/patologia , Fatores de Tempo
17.
Mar Drugs ; 17(2)2019 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-30795639

RESUMO

ß-thymosin is known for having 43 amino acids, being water-soluble, having a light molecular weight and ubiquitous polypeptide. The biological activities of ß-thymosin are diverse and include the promotion of wound healing, reduction of inflammation, differentiation of T cells and inhibition of apoptosis. Our previous studies showed that oyster ß-thymosin originated from the mantle of the Pacific oyster, Crassostrea gigas and had antimicrobial activity. In this study, we investigated the anti-inflammatory effects of oyster ß-thymosin in lipopolysaccharide (LPS)-induced RAW264.7 macrophage cells using human ß-thymosin as a control. Oyster ß-thymosin inhibited the nitric oxide (NO) production as much as human ß-thymosin in LPS-induced RAW264.7 cells. It also showed that oyster ß-thymosin suppressed the expression of prostaglandin E2 (PGE2), inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Moreover, oyster ß-thymosin reduced inflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin-1ß (IL-1ß) and interleukin-6 (IL-6). Oyster ß-thymosin also suppressed the nuclear translocation of phosphorylated nuclear factor-κB (NF-κB) and degradation of inhibitory κB (IκB) in LPS-induced RAW264.7 cells. These results suggest that oyster ß-thymosin, which is derived from the mantle of the Pacific oyster, has as much anti-inflammatory effects as human ß-thymosin. Additionally, oyster ß-thymosin suppressed NO production, PGE2 production and inflammatory cytokines expression via NF-κB in LPS-induced RAW264.7 cells.


Assuntos
Anti-Inflamatórios/farmacologia , Crassostrea/química , Dinoprostona/biossíntese , Macrófagos/efeitos dos fármacos , Óxido Nítrico/biossíntese , Timosina/farmacologia , Fator de Necrose Tumoral alfa/metabolismo , Animais , Sobrevivência Celular , Células Cultivadas , Ciclo-Oxigenase 2/metabolismo , Dinoprostona/metabolismo , Humanos , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Queratinócitos/efeitos dos fármacos , Lipopolissacarídeos/farmacologia , Macrófagos/metabolismo , Camundongos , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Células RAW 264.7 , Alinhamento de Sequência , Transdução de Sinais/efeitos dos fármacos , Timosina/isolamento & purificação
18.
Int J Mol Med ; 43(4): 1859-1865, 2019 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-30720064

RESUMO

Inhibition of over­activated inflammation has been demonstrated as one of the most efficient strategies for treating inflammatory diseases. In the present study, 6­formyl umbelliferone (6FU) was used to evaluate its anti­inflammatory effects on lipopolysaccharide (LPS)­stimulated RAW 264.7 macrophages. 6FU inhibited chronic inflammatory processes, including increasing nitric oxide levels, and the expression of pro­inflammatory genes and producing cytokines was investigated by a nitrite assay and reverse transcription­polymerase chain reaction, respectively. Nitric oxide and pro­inflammatory cytokines, including tumor necrosis factor­α, interleukin (IL)­1ß and IL­6 were decreased by treatment with 6FU, without cell cytotoxicity in LPS­stimulated RAW 264.7 cells, which was measured by a WST­1 assay. In the western blot analysis, the expression levels of phosphorylated extracellular signal­regulated kinase (ERK)1/2 was downregulated in 6FU­treated cells. Furthermore, in the western blotting and immunofluorescence staining results, translocation activities of ERK1/2 and NF­κB from the cytoplasm to the nucleus were suppressed, which may inhibit translation of numerous proteins associated with pro­inflammation, including inducible nitric oxide synthase and cyclooxygenase­2. Therefore, based on these results, it was suggested that 6FU may be a potential candidate for the development of agents against chronic inflammation.


Assuntos
Anti-Inflamatórios/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , NF-kappa B/metabolismo , Umbeliferonas/farmacologia , Animais , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/metabolismo , Citocinas/genética , Citocinas/metabolismo , Ativação Enzimática/efeitos dos fármacos , Lipopolissacarídeos , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Óxido Nítrico/biossíntese , Óxido Nítrico Sintase Tipo II/metabolismo , Fosforilação/efeitos dos fármacos , Transporte Proteico/efeitos dos fármacos , Células RAW 264.7 , RNA Mensageiro/genética , RNA Mensageiro/metabolismo
19.
Mitochondrial DNA B Resour ; 4(2): 3179-3181, 2019 Sep 24.
Artigo em Inglês | MEDLINE | ID: mdl-33365908

RESUMO

The complete mitochondrial genome of Pseudotolithus elongatus (Perciformes: Sciaenidae) is determined based on NGS technology. The assembled mitogenome is a 16,497 bp in length containing a typical set of the 13 protein-coding genes, 22 tRNAs, 2 rRNA genes, and the 1 putative control region. The overall base composition is A (27.8%), T (25.3%), G (16.1%), and C (30.8%) with an A-T content of 53.1%. The phylogenetic analysis of 36 mitogenomes from the GenBank indicated that P. elongatus is closely related to the Aplodinotus grunniens. This mitogenome information of the P. elongatus would be useful to understand evolutionary and phylogenetic analysis of the family Sciaenidae fishes.

20.
Anim Cells Syst (Seoul) ; 22(5): 341-351, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30460116

RESUMO

In this study, we identified four canonical calmodulin genes in the Pacific abalone, Haliotis discus hannai. Their full-length cDNAs were variable in the 5' and 3' untranslated regions, but highly similar (91-97%) in the coding region. Each of the genes encoded 149 amino acids, with 93-97% similarity among themselves and 94-98% similarity with human CAM I. There were 54 substitutions distributed unevenly throughout the coding regions, found mostly in the third codon position. Gene structure analysis revealed that each of the calmodulin genes comprised five exons and four introns. The intron positions and phases were identical and there were no introns in the fourth exon. The corresponding introns differed in their sequences and sizes. Expression profiles of nine tissues from abalone revealed that the calmodulin genes were transcribed in common in gill and mantle tissue, but differentially in the other tissues. A phylogenetic analysis based on the amino acid sequences revealed that calmodulin C was the most common isoform in Gastropoda and calmodulin was the most diverged isoform. An in silico analysis of the calmodulin genes identified paralogous genes in other Haliotis species, indicating that gene duplication might have occurred in the last common ancestor of Haliotis. Abbreviations: ORF: open reading frame; RACE: random amplification of cDNA end; TSA: transcriptome shotgun assembly; UTR: untranslated region.

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