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1.
Ecotoxicol Environ Saf ; 205: 111376, 2020 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-32961488

RESUMO

Deoxynivalenol (DON) is extensively detected in many kinds of foods and feeds to harm human and animal health. This research aims to investigate the effect of chlorogenic acid (CGA) on alleviating inflammation and apoptosis of swine jejunal epithelial cells (IPEC-J2) triggered by DON. The results demonstrated that cell viability was decreased when DON concentrations increased or incubation time expanded. The pretreatment with CGA (40 µg/mL) for 1 h increased cell viability, decreased lactate dehydrogenase (LDH) release and apoptosis in cells triggered by DON at 0.5 µg/mL for 6 h, compared with the DON alone-treated cells. Moreover, the mRNA abundances of IL-8, IL-6, TNF-α, COX-2, caspase-3, Bax and ASCT2 genes, and protein expressions of COX-2, Bax and ASCT2 were significantly down-regulated; while the mRNA abundances of ZO-1, claudin-1, occludin, PePT1 and GLUT2 genes, and protein expressions of ZO-1, claudin-1 and PePT1 were significantly up-regulated in the CGA + DON group, compared with the DON alone group. This study indicated that CGA pretreatment alleviated cytotoxicity, inflammation and apoptosis in DON-triggered IPEC-J2 cells, and protected intestinal cell integrity from DON damages.


Assuntos
Ácido Clorogênico/farmacologia , Substâncias Protetoras/farmacologia , Tricotecenos/toxicidade , Animais , Apoptose/efeitos dos fármacos , Caspase 3 , Contagem de Células , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Ácido Clorogênico/metabolismo , Células Epiteliais/efeitos dos fármacos , Inflamação/metabolismo , Intestinos/efeitos dos fármacos , Ocludina/genética , Suínos
2.
Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi ; 36(8): 693-698, 2020 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-32958125

RESUMO

Objective To investigate the effects of isochlorogenic acid A on the proliferation, migration, invasion and apoptosis of MH7A cells. Methods Following by the induction of 20 µg/L TNF-α in vitro, different concentrations of isochlorogenic acid A (0, 0.04, 0.09, 0.13, 0.16, 0.20 µg/µL) were added into MH7A cells. The proliferation of MH7A cells was detected by CCK-8 assay, and the invasion and migration were observed by TranswellTM assay. The levels of cellular caspase-3, ROS and MMP3 in the MH7A cells were detected by corresponding kits. BAX and Bcl2 expression of MH7A cells were tested by immunofluorescence cytochemistry. Results The proliferation, invasion and migration activity were enhanced significantly and the apoptotic activity was reduced in MH7A cells induced by 20 µg/L TNF-α. Compared with TNF-α in vitro induction, isochlorogenic acid A significantly inhibited the proliferation, invasion, migration and MMP3 secretion of MH7A cells, increased ROS release and promoted MH7A apoptosis. Conclusion Isochlorogenic acid A can inhibit proliferation, invasion, migration and promoted apoptosis of MH7A cells.


Assuntos
Apoptose , Ácido Clorogênico/análogos & derivados , Fator de Necrose Tumoral alfa , Apoptose/efeitos dos fármacos , Linhagem Celular , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Ácido Clorogênico/farmacologia , Humanos , Fator de Necrose Tumoral alfa/imunologia
3.
Biochem Biophys Res Commun ; 530(1): 4-9, 2020 09 10.
Artigo em Inglês | MEDLINE | ID: mdl-32828312

RESUMO

COVID-19 has become one of the worst epidemic in the world, currently already more than four million people have been infected, which probably co-exist with human beings, and has a significant impact on the global economy and political order. In the process of fighting against the epidemic in China, the clinical value of a variety of herbal medicines has been recognized and written into the clinical application guide. However, their effective molecular mechanism and potential targets are still not clear. Pathology and pharmacology research will gradually attract attention in the post-epidemic outbreak term. Here, we constructed a COVID-19 protein microarray of potential therapy targets, which contains the main drug targets to the SARS-CoV-2 virus and the anti-virus, anti-inflammatory cellar targets of the host. Series of quality controls test has been carried out, which showed that it could be applied for drug target screening of bio-active natural products. The establishment of this microarray will provide a useful tool for the study of the molecular pharmacology of natural products.


Assuntos
Antivirais/farmacologia , Betacoronavirus/efeitos dos fármacos , Infecções por Coronavirus/tratamento farmacológico , Medicamentos de Ervas Chinesas/farmacologia , Pneumonia Viral/tratamento farmacológico , Proteínas/metabolismo , Proteínas Virais/metabolismo , Betacoronavirus/metabolismo , Produtos Biológicos/farmacologia , Ácido Clorogênico/farmacologia , Infecções por Coronavirus/metabolismo , Diterpenos/farmacologia , Descoberta de Drogas , Glucosídeos/farmacologia , Células HEK293 , Humanos , Simulação de Acoplamento Molecular , Terapia de Alvo Molecular , Pandemias , Pneumonia Viral/metabolismo , Análise Serial de Proteínas , Estilbenos/farmacologia
4.
Food Chem ; 333: 127528, 2020 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-32682231

RESUMO

Endogenous lipase and lipoxygenase play important roles in accelerating lipid oxidation. Polyphenols are a series of commonly used chemicals for preserving fish and seafood products, due to their positive inhibitory effects on lipid oxidation. However, the mechanism involved is still unknown. The inhibitory effects of chlorogenic acid (CGA) on lipase and lipoxygenase were investigated and explored with multi- spectroscopic and molecular docking approaches. Results showed that CGA could inhibit the activities of lipase and lipoxygenase with concentration increased in a highly dose-dependent manner. CGA quenched intrinsic fluorescence intensities of enzymes by static quenching and binding with CGA which led to changes in 3D structures of enzymes. Results of the molecular docking confirmed binding modes, binding sites and major interaction forces between CGA and enzymes, which reduced the corresponding activity. Thus, this study could provide basic mechanisms of the inhibitory effects of polyphenols on lipid oxidation during food preservation.


Assuntos
Ácido Clorogênico/metabolismo , Ácido Clorogênico/farmacologia , Metabolismo dos Lipídeos/efeitos dos fármacos , Inibidores de Lipoxigenase/metabolismo , Inibidores de Lipoxigenase/farmacologia , Simulação de Acoplamento Molecular , Animais , Sítios de Ligação , Conservação de Alimentos , Lipase/antagonistas & inibidores , Lipase/química , Lipase/metabolismo , Lipoxigenase/química , Lipoxigenase/metabolismo , Oxirredução/efeitos dos fármacos , Polifenóis/farmacologia , Espectrometria de Fluorescência
5.
Sci Rep ; 10(1): 8876, 2020 06 01.
Artigo em Inglês | MEDLINE | ID: mdl-32483369

RESUMO

Present study was designed to compared the total flavonoids and polyphenols contents and antibacterial activity of hawthorn extracts with different polarities as well as the underlying antibacterial mechanisms. The results showed that among all hawthorn extracts, methanol and ethanol extracts (ME and EE) exhibited high levels of total flavonoids and polyphenols contents, followed by acetone, ethyl acetate, trichloromethane and petroleum ether extracts. ME exhibited the strongest antibacterial activity against tested bacteria, especially Staphylococcus aureus with a 1.25 µg/mL of the minimum inhibitory concentration (MIC) and minimum bactericide concentration (MBC). Further analysis revealed that the main phenolic compounds from ME were epicatechin (281.6 mg/100 g DW), procyanidin B2 (243.5 mg/100 g DW), chlorogenic acid (84.2 mg/100 g DW) and quercetin (78.4 mg/100 g DW). The action mechanism of ME against S. aureus could be ascribed to ME damaging cell wall and cell membrane integrity, inhibiting intracellular enzyme activity, increasing reactive oxygen species (ROS), also changing expression of associated genes and then inducing apoptosis of S. aureus. In addition, the antimicrobial activity of ME against S. aureus has also been demonstrated to be efficient in the food matrix (whole milk).


Assuntos
Antibacterianos/química , Crataegus/química , Extratos Vegetais/química , Antibacterianos/farmacologia , Catequina/farmacologia , Parede Celular/efeitos dos fármacos , Parede Celular/fisiologia , Ácido Clorogênico/farmacologia , Cromatografia Líquida de Alta Pressão , Crataegus/metabolismo , Flavonoides/química , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Potenciais da Membrana/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Fenóis/química , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio/metabolismo
6.
Phytomedicine ; 71: 153225, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32464299

RESUMO

BACKGROUND: Impaired bone formation is one of the reasons behind osteoporosis. Alterations in the patterns of mesenchymal stromal cell differentiation towards adipocytes instead of osteoblasts contribute to osteoporosis progression. Natural anti-osteoporotic agents are effective and safe alternatives for osteoporosis treatment. PURPOSE: In this context, 3,5-dicaffeoyl­epi-quinic acid (DCEQA) which is a derivative of chlorogenic acid with reported bioactivities was studied for its osteogenic differentiation enhancing potential in vitro. METHODS: Anti-osteoporotic effects of DCEQA were investigated in human bone marrow-derived mesenchymal stromal cells (hBM-MSCs) which were induced to differentiate into osteoblasts or adipocytes with or without DCEQA treatment. Changes in the osteogenic and adipogenic markers such as ALP activity and lipid accumulation, respectively, were observed along with differentiation-specific activation of mitogen activated protein kinase (MAPK) pathways. RESULTS: At 10 µM concentration, DCEQA increased the proliferation of bone marrow-derived human mesenchymal stromal cells (hBM-MSCs) during osteoblast differentiation. The expression of osteogenic markers ALP, osteocalcin, Runx2, BMP2 and Wnt 10a was upregulated by DCEQA treatment. The ALP activity and extracellular mineralization were also increased. DCEQA elevated the phosphorylation levels of p38 and JNK MAPKs as well as the activation of ß-catenin and Smad1/5. DCEQA suppressed the lipid accumulation and downregulated expression of adipogenic markers PPARγ, C/EBPα and SREBP1c in adipo-induced hBM-MSCs. DCEQA also decreased the phosphorylation of p38 and ERK MAPKs and stimulated the activation of AMPK in hBM-MSC adipocytes. CONCLUSION: DCEQA was suggested to enhance osteoblast differentiation via stimulating Wnt/BMP signaling. The adipocyte differentiation inhibitory effect of DCEQA was suggested to arise from its ability to increase AMPK phosphorylation. Overall, DCEQA was shown to possess osteogenesis enhancing and adipogenesis inhibitory properties which might facilitate its use against osteoporotic conditions.


Assuntos
Adipócitos/citologia , Atriplex/química , Ácido Clorogênico/análogos & derivados , Células-Tronco Mesenquimais/efeitos dos fármacos , Osteoblastos/efeitos dos fármacos , Proteínas Quinases Ativadas por AMP/metabolismo , Adipócitos/efeitos dos fármacos , Células da Medula Óssea , Proteína Morfogenética Óssea 2/metabolismo , Diferenciação Celular/efeitos dos fármacos , Células Cultivadas , Ácido Clorogênico/farmacologia , Subunidade alfa 1 de Fator de Ligação ao Core/metabolismo , Humanos , Células-Tronco Mesenquimais/citologia , Osteoblastos/citologia , Osteoblastos/metabolismo , Osteogênese/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Via de Sinalização Wnt/efeitos dos fármacos , beta Catenina/metabolismo
7.
Ecotoxicol Environ Saf ; 194: 110401, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32143102

RESUMO

Zearalenone (ZEA), a toxic substance produced by Fusarium fungi, accumulated in cereals grain and animal feed, causes injury to humans and animals. ZEA can induce obvious reproductive toxicity with the ovarian granulosa cells (GCs) as the main target. However, the study on exploring the protective compounds against ZEA-induced mouse primary ovarian GCs damage remains less. In the current study, the protective effect of 20 compounds derived from traditional Chinese medicines (TCMs) on the injury of mouse GCs caused by ZEA were evaluated using MTT assay and the cell morphology. Our results showed that chlorogenic acid (250, 500, and 1000 µg/mL) significantly suppress ZEA-induced GCs death. Western blot analysis suggested chlorogenic acid could rescue the up-regulated apoptosis of GCs induced by ZEA via attenuating the protein expression of cleaved caspase-3, the ratio of Bax/Bcl-2 and cleaved-PARP. Our results provide strong evidence that chlorogenic acid warrants further optimization for more potent and safer compounds for against the ZEA lead toxicity to humans and animals.


Assuntos
Apoptose/efeitos dos fármacos , Ácido Clorogênico/farmacologia , Células da Granulosa/efeitos dos fármacos , Zearalenona/toxicidade , Animais , Caspase 3/metabolismo , Células Cultivadas , Relação Dose-Resposta a Droga , Feminino , Células da Granulosa/metabolismo , Células da Granulosa/patologia , Camundongos , Camundongos Endogâmicos , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo
8.
Curr Pharm Biotechnol ; 21(11): 1099-1106, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32188382

RESUMO

BACKGROUND: Chlorogenic Acid (CA) has diverse, recognized health effects. OBJECTIVE: This study aimed to explore the effects of CA on fat reduction and the underlying mechanism of these effects. MATERIALS AND METHODS: First, we established a Monosodium Glutamate (MSG)-induced obesity mouse model and subjected the mice to 4 weeks of CA gavage. Then, we established an oleic acidinduced model of human fatty liver in HepG2 cells, and administered a CA intervention to the cells for 48 h. Finally, we used Oil red O staining, biochemical detection kits, RT-PCR and Western blot analysis to evaluate the effects of CA on fat reduction and on related pathways. RESULTS: The CA treatment could reduce fat accumulation in the liver and reduce blood lipid levels. In addition, CA decreased the mRNA and protein levels of peroxisome proliferator-activated receptor gamma, coactivator 1 α (PGC-1α) and Uncoupling Protein 1 (UCP1) in the MSG-induced obesity mouse model and the oleic acid-induced HepG2 cells. CONCLUSION: Based on the above results, we deduced that CA could reduce body weight and fat deposition in vitro and in vivo and that the mechanism may be related to the PGC-1α/UCP-1 pathway. CA can be developed as a drug to lower blood lipids and to treat obesity.


Assuntos
Fármacos Antiobesidade/farmacologia , Ácido Clorogênico/farmacologia , Fígado Gorduroso/tratamento farmacológico , Fígado/efeitos dos fármacos , Obesidade/tratamento farmacológico , Perda de Peso/efeitos dos fármacos , Animais , Fármacos Antiobesidade/uso terapêutico , Ácido Clorogênico/uso terapêutico , Modelos Animais de Doenças , Fígado Gorduroso/metabolismo , Células Hep G2 , Humanos , Metabolismo dos Lipídeos/efeitos dos fármacos , Lipídeos/sangue , Fígado/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Obesidade/metabolismo , Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/metabolismo , Transdução de Sinais/efeitos dos fármacos , Glutamato de Sódio/metabolismo , Proteína Desacopladora 1/metabolismo
9.
Life Sci ; 254: 117590, 2020 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-32220624

RESUMO

AIMS: This study aimed to investigate the therapeutic effect and molecular mechanism of chlorogenic acid (CGA) on cyclophosphamide (CYP)-induced rat interstitial cystitis (IC). MATERIALS AND METHODS: An animal model of IC was established by intraperitoneal injection of CYP in female Sprague-Dawley rats. Eighty rats were randomly assigned to four groups: negative control (NC), NC treated with CGA (NC + CGA), IC, and IC treated with CGA (IC + CGA). Bladder urination function was assessed by analyzing urodynamic parameters. The expression of apoptosis-related proteins and inflammatory biomarkers in bladder specimens was detected using western blot and immunohistochemistry analysis. KEY FINDINGS: Compared with the IC group, bladder urinary function was significantly improved in the IC + CGA group. CGA treatment reduced inflammatory damage in the bladder tissue of IC rats. Caspase3 and Bax expression was higher while Bcl-2 expression was lower in the IC group compared to the IC + CGA group. In addition, there were significant differences between the groups in the expression levels of inflammatory biomarkers in the bladder tissue. Furthermore, CGA could inhibit CYP-induced MAPK/NF-κB phosphorylation in the rat bladder tissue. SIGNIFICANCE: In a CYP-induced rat model of IC, CGA could reduce inflammation and apoptosis, thus partially restoring bladder function, and the MAPK/NF-κB pathway was probably involved in it.


Assuntos
Antineoplásicos Alquilantes/farmacologia , Ácido Clorogênico/farmacologia , Ciclofosfamida/farmacologia , Cistite Intersticial/prevenção & controle , Animais , Feminino , Ratos , Ratos Sprague-Dawley
10.
Adv Pharmacol ; 87: 71-88, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32089239

RESUMO

Chlorogenic acid is a widely distributed natural compound with many important pharmacological effects, which are found in a variety of plants. It is also an important secondary metabolite in plants. As a natural plant extract from a wide range of sources, in vitro and in vivo studies have found that the main pharmacological effects of chlorogenic acid are antioxidant, antiinflammatory, antibacterial, antiviral, hypoglycemic, lipid lowering, anticardiovascular, antimutagenic, anticancer, immunomodulatory, etc. Therefore it may play an important role in promoting human health. For example, it can provide new ideas and new ways for the prevention and treatment of cardiovascular disease, cancer, diabetes, and other chronic diseases, but the specific mechanism of action is unclear. Due to the difficulty of extraction and purification, poor stability, poor solubility, low absolute bioavailability of oral administration, the possibility of allergies caused by injection, and so on, there are difficulties in its medicinal research and development. The further study of chlorogenic acid will provide an important theoretical basis for its rational use.


Assuntos
Ácido Clorogênico/farmacologia , Animais , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Ácido Clorogênico/química , Humanos , Hipoglicemiantes/farmacologia , Fatores Imunológicos/farmacologia
11.
Food Chem ; 313: 126078, 2020 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31945699

RESUMO

Effects of Chlorogenic acid-Gelatin (CGA-Gel) combined with partial freezing on quality change of sword prawn (Parapenaeopsis hardwickii) stored at -5 °C were evaluated for 23 days. Changes in sensory score, total viable counts (TVC), and physiochemical indexes including pH, total volatile basic nitrogen (TVB-N), thiobarbituric acid reactive substances (TBARS) and Ca2+-ATPase were examined. All shrimp treated with CGA and CGA-Gel had lower total viable counts compared to control (P < 0.05). The value of TVB-N and TBA of CGA-Gel treated group at day 13 were 18.4 mg N/100 g and 0.175 mg/100 g respectively, both below the proposed safe limits and values of CGA treated group. All the results demonstrated that Chlorogenic acid can inhibit growth of microorganism, lipid oxidation and protein degradation. CGA-Gel treated samples presented better quality preservation effects than CGA treated alone. Therefore, CGA-Gel combined with partial freezing is promising in sword prawn shelf life extension.


Assuntos
Ácido Clorogênico/química , Conservação de Alimentos/métodos , Gelatina/química , Penaeidae/fisiologia , Animais , ATPases Transportadoras de Cálcio/metabolismo , Ácido Clorogênico/farmacologia , Congelamento , Humanos , Concentração de Íons de Hidrogênio , Peroxidação de Lipídeos/efeitos dos fármacos , Proteólise/efeitos dos fármacos
12.
World J Microbiol Biotechnol ; 36(2): 24, 2020 Jan 21.
Artigo em Inglês | MEDLINE | ID: mdl-31965331

RESUMO

The study evaluated the antibacterial activity of chlorogenic acid (CA) against Salmonella Enteritidis S1, a foodborne pathogen in chilled fresh chicken. Its minimum inhibitory concentration for S. Enteritidis S1 was 2 mM. 1 MIC CA treatment reduced the viable count of S. Enteritidis S1 by 3 log cfu/g in chilled fresh chicken. Scanning electron microscopy examination indicated that CA induced the cell envelope damage of S. Enteritidis S1. Following this, 1-N-Phenylnaphthylamine assay and LPS content analysis indicated that CA induced the permeability of outer membrane (OM). Confocal laser scanning microscopy examination further demonstrated that CA acted on the inner membrane (IM). To support this, the release of intracellular protein and ATP after CA treatment was also observed. CA also suppressed the activities of malate dehydrogenase and succinate dehydrogenase, two main metabolic enzymes in TCA cycle and electron transport chain. Thus, damage of intracelluar and outer membranes as well as disruption of cell metabolism resulted in cell death eventually. The finding suggested that CA has the potential to be developed as a preservative to control S. Enteritidis associated foodborne diseases.


Assuntos
Antibacterianos/farmacologia , Ácido Clorogênico/farmacologia , Salmonella enteritidis/efeitos dos fármacos , Animais , Proteínas de Bactérias/antagonistas & inibidores , Membrana Celular/efeitos dos fármacos , Galinhas/microbiologia , Contagem de Colônia Microbiana , Regulação Bacteriana da Expressão Gênica/efeitos dos fármacos , Malato Desidrogenase/antagonistas & inibidores , Testes de Sensibilidade Microbiana , Viabilidade Microbiana/efeitos dos fármacos , Microscopia Eletrônica de Varredura , Salmonella enteritidis/enzimologia , Salmonella enteritidis/crescimento & desenvolvimento , Succinato Desidrogenase/antagonistas & inibidores
13.
Nanotechnology ; 31(18): 185101, 2020 May 01.
Artigo em Inglês | MEDLINE | ID: mdl-31995525

RESUMO

Diseases caused by pathogenic bacilli pose an increasing threat to human health. A common feature of these bacteria is a complete cell wall; therefore, drugs that can penetrate this protective barrier could be used as a novel approach for treating these infections. Here we present a simple method for synthesizing a silica mesoporous material loaded with cadmium selenide (CdSe) and chlorogenic acid. Using UV-visible, fluorescence, and infrared imaging in combination with transmission electron microscopy, it was shown that CdSe and chlorogenic acid could be successfully embedded in the mesopores of silica nanoparticles (CSC NPs), and these NPs presented with a strong fluorescence, uniform size, and good dispersion. Additionally, the results of these analyses indicated that the fluorescence of the CSC NPs was localized within the cells of Escherichia coli and Bacillus subtilis, signifying that these NPs could breach the cell wall and enter the cells of these two bacilli. Additional assessments found that these CSC NPs inhibited the proliferation of the bacteria by disrupting the cell wall, and this was most likely due to the overproduction of reactive oxygen species induced by chlorogenic acid. Importantly, histopathology analysis indicated that the CSC NPs had limited side effects and high biocompatibility.


Assuntos
Antibacterianos/farmacologia , Ácido Clorogênico/farmacologia , Nanopartículas/química , Espécies Reativas de Oxigênio/metabolismo , Dióxido de Silício/farmacologia , Animais , Bacillus subtilis/efeitos dos fármacos , Bacillus subtilis/ultraestrutura , Compostos de Cádmio/toxicidade , Ácido Clorogênico/toxicidade , Escherichia coli/efeitos dos fármacos , Escherichia coli/ultraestrutura , Masculino , Camundongos Nus , Testes de Sensibilidade Microbiana , Nanopartículas/toxicidade , Nanopartículas/ultraestrutura , Porosidade , Padrões de Referência , Compostos de Selênio/toxicidade
14.
PLoS One ; 15(1): e0222126, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31995555

RESUMO

Most existing cancer treatments involve high-cost chemotherapy and radiotherapy, with major side effects, prompting effort to develop alternative treatment modalities. It was reported that the combination of thermal-cycling hyperthermia (TC-HT) and phenolic compound exhibited a moderate cytotoxic effect against human pancreatic cancer PANC-1 cells. In this study, we investigate the efficacy of triple combination in PANC-1 cancer cells by adopting low-intensity pulsed electric field (LIPEF) to couple with TC-HT and CGA (chlorogenic acid). The study finds that this triple combination can significantly impede the proliferation of PANC-1 cells, with only about 20% viable cells left after 24h, whereas being non-toxic to normal cells. The synergistic activity against the PANC-1 cells was achieved by inducing G2/M phase arrest and apoptosis, which were associated with up-regulation of p53 and coupled with increased expression of downstream proteins p21 and Bax. Further mechanism investigations revealed that the cytotoxic activity could be related to mitochondrial apoptosis, characterized by the reduced level of Bcl-2, mitochondrial dysfunction, and sequential activation of caspase-9 and PARP. Also, we found that the triple treatment led to the increase of intracellular reactive oxygen species (ROS) production. Notably, the triple treatment-induced cytotoxic effects and the elevated expression of p53 and p21 proteins as well as the increased Bax/Bcl-2 ratio, all could be alleviated by the ROS scavenger, N-acetyl-cysteine (NAC). These findings indicate that the combination of CGA, TC-HT, and LIPEF may be a promising modality for cancer treatment, as it can induce p53-dependent cell cycle arrest and apoptosis through accumulation of ROS in PANC-1 cells.


Assuntos
Antineoplásicos/farmacologia , Proliferação de Células/efeitos dos fármacos , Ácido Clorogênico/farmacologia , Neoplasias Pancreáticas/terapia , Apoptose/efeitos dos fármacos , Pontos de Checagem do Ciclo Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Radiação Eletromagnética , Humanos , Hipertermia Induzida/métodos , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Mitocôndrias/efeitos dos fármacos , Neoplasias Pancreáticas/patologia , Espécies Reativas de Oxigênio/metabolismo
15.
J Ethnopharmacol ; 252: 112606, 2020 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-31988013

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Porana sinensis Hemsl. has been widely used to treat joint pain and rheumatoid arthritis in traditional Chinese medicine (TCM). Although evidence exists to support a pharmacological action of P. sinensis for the treatment of gout arthritis (GA), the underlying mechanism of action remains unknown due to it being a multi-component and multi-target agent. AIM OF THE STUDY: To clarify the active compounds and mechanism of P. sinensis against GA. MATERIALS AND METHODS: The present study combined network pharmacology with experiments to clarify the mechanism of P. sinensis against GA. A protein-protein interaction network for gout was constructed to identify the potential drug targets, and molecular docking was subsequently performed to determine whether the protein was a target for the compounds of P. sinensis. KEGG pathway analysis was then conducted to elucidate the pathway involved in the P. sinensis-mediated treatment of gout. A rat model of GA was used to further investigate the mechanism of P. sinensis against GA. RESULTS: The network pharmacology study indicates that coumarins and chlorogenic acids of P. sinensis may serve as additives to GA treatment. P. sinensis played a role in the treatment of GA by regulating the PI3K-Akt, MAPK, NF-kappa B and toll-like receptor pathways and so on. Moreover, experimental validation suggests that P. sinensis extract significantly suppressed the expression of TLR2 and MyD88 mRNA, regulating the release of cytokines (IL-1ß, IL-4 and TGF-ß), lowering lipid peroxidation (MDA) and increasing antioxidant status (SOD). CONCLUSION: The present study clarifies the mechanism of P. sinensis against GA, and provides evidence to support its clinical use.


Assuntos
Artrite Gotosa/metabolismo , Convolvulaceae , Extratos Vegetais/farmacologia , Animais , Articulação do Tornozelo/efeitos dos fármacos , Articulação do Tornozelo/patologia , Artrite Gotosa/tratamento farmacológico , Artrite Gotosa/genética , Artrite Gotosa/patologia , Ácido Clorogênico/farmacologia , Ácido Clorogênico/uso terapêutico , Cumarínicos/farmacologia , Cumarínicos/uso terapêutico , Citocinas/sangue , Masculino , Simulação de Acoplamento Molecular , Fator 88 de Diferenciação Mieloide/genética , Farmacologia/métodos , Extratos Vegetais/uso terapêutico , Mapas de Interação de Proteínas , Ratos Sprague-Dawley , Receptor 2 Toll-Like/genética
16.
Crit Rev Food Sci Nutr ; 60(5): 760-779, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-30614247

RESUMO

Coffee is reported to be among the most widely consumed beverages in the world and coffee consumption has been associated with reductions in the risk of several chronic diseases. Among its constituents, caffeine represents the most investigated component. The main impact of caffeine on health is associated with the central nervous system, the cardiovascular system, the inflammatory mechanisms, the metabolism of carbohydrates, and the cancer. Current research is devoted to the role of this compound and its analogs or derivatives on neuroinflammation and neurodegenerative disorders, mainly Alzheimer's Disease and Parkinson's Disease. However, coffee is also rich in polyphenols, mainly phenolic acids (chlorogenic acids, caffeic acid, ferulic acid), quinic acid, and quercetin. Many aspects still require greater clarification, including the effect of coffee compounds different from caffeine, on several pathologies. This review aimed to provide a comprehensive overview of the potential benefits of decaffeinated coffee constituents, focusing the attention on neurological processes and pathologies, such as mainly memories disorders, Parkinson's Disease, neurophatic pain disorders, and cerebral ischemia.


Assuntos
Bebidas , Café/química , Doenças Neurodegenerativas , Cafeína , Ácido Clorogênico/análise , Ácido Clorogênico/farmacologia , Humanos
17.
Yakugaku Zasshi ; 140(1): 113-116, 2020 Jan 01.
Artigo em Japonês | MEDLINE | ID: mdl-31611478

RESUMO

Phellodendron amurense is a broad-leaved tree; its outer bark and cork layers are removed and used as a crude medicinal agent known as Phellodendri Cortex. These trees are cultivated for approximately 15 to 20 years, harvested by felling, and processed by separating the outer and inner bark. Conventionally, parts other than the inner bark (i.e., fruit, leaves, and heartwood) remain unused. However, the revenue earned from by-products could contribute to continued cultivation of Phellodendron amurense. Herein, we examined the extraction condition and investigated the content of chlorogenic acid in the leaves of domestic Phellodendron amurense, which possesses antioxidant activity.


Assuntos
Ácido Clorogênico/isolamento & purificação , Phellodendron/química , Folhas de Planta/química , Antioxidantes , Ácido Clorogênico/farmacologia
18.
Biomed Pharmacother ; 121: 109602, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31707349

RESUMO

Esophageal squamous cell carcinoma (ESCC) is one of the most common cancers in China, accompanied by an extremely high mortality rate. Chlorogenic acid (CGA) is a small-molecule compound, that has been shown to have a wide range of biological activities, including antitumor. However, the efficacy and molecular mechanism of CGA on ESCC remains unknown. In this study, we confirmed the inhibition of proliferation by CGA in ESCC cells, as well as the reduction of ESCC xenograft volume by CGA in vivo. In addition, CGA also suppressed both the migration and invasion of ESCC cells in vitro. In a carcinogen-induced murine model of ESCC, hyperplasia of the esophagus was slowed by CGA, while mice suffering from ESCC that were treated with CGA had longer survival times than mice in the control group. The measurement of pluripotency factors (BMI1, SOX2, OCT4 and Nanog) that are related to poor prognosis revealed reduced expression of both BMI1 and SOX2, but not of OCT4 or Nanog, in ESCC cells, in both a dose- and time-dependent manner. Together, our initial findings demonstrate that CGA suppresses ESCC progression, downregulates the expression of BMI1 and SOX2, and provide an anti-tumor candidate for ESCC therapy.


Assuntos
Ácido Clorogênico/uso terapêutico , Neoplasias Esofágicas/metabolismo , Carcinoma de Células Escamosas do Esôfago/metabolismo , Inibidores do Crescimento/uso terapêutico , Complexo Repressor Polycomb 1/biossíntese , Proteínas Proto-Oncogênicas/biossíntese , Fatores de Transcrição SOXB1/biossíntese , Animais , Linhagem Celular , Linhagem Celular Tumoral , Ácido Clorogênico/farmacologia , Relação Dose-Resposta a Droga , Regulação para Baixo/efeitos dos fármacos , Regulação para Baixo/fisiologia , Neoplasias Esofágicas/tratamento farmacológico , Neoplasias Esofágicas/genética , Carcinoma de Células Escamosas do Esôfago/tratamento farmacológico , Carcinoma de Células Escamosas do Esôfago/genética , Regulação Neoplásica da Expressão Gênica , Inibidores do Crescimento/farmacologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Endogâmicos NOD , Camundongos SCID , Complexo Repressor Polycomb 1/antagonistas & inibidores , Complexo Repressor Polycomb 1/genética , Proteínas Proto-Oncogênicas/antagonistas & inibidores , Proteínas Proto-Oncogênicas/genética , Fatores de Transcrição SOXB1/antagonistas & inibidores , Fatores de Transcrição SOXB1/genética
19.
J Microencapsul ; 37(1): 52-64, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31714160

RESUMO

Nanoencapsulation by spray drying was performed to protect and preserve antioxidant rich dietary polyphenols from green coffee beans. Nano-encapsulation of green coffee was done using maltodextrin as wall material. The nanoparticles were further characterised by zetasizer, differential scanning colorimetry, X-ray diffraction, In vitro gastric intestinal studies and storage stability. Optimal nanoparticles were obtained at a drying temperature of 125 °C and 2:1 Mwall/Mcore ratio (10% w/w maltodextrin), provided better encapsulation yield (40% w/w) and 70 ± 5% (w/w) encapsulation efficiency with 82.34 nm particle size, -28.8 mV zeta-potential. The In-vitro bioactivity of nanoparticles ensured 80 ± 2% (w/w) of chlorogenic acid availability in a controlled release in the intestine. Storage stability of nanoparticles under varied temperature was remarkably improved compared to non-encapsulated green coffee extract. However, the results indicated that the potential benefits of using maltodextrin coated green coffee nanoparticles for controlled release of Chlorogenic acid and sufficient antioxidative protection during prolonged period.


Assuntos
Antioxidantes/administração & dosagem , Café/química , Preparações de Ação Retardada/química , Polifenóis/administração & dosagem , Polissacarídeos/química , Antioxidantes/química , Antioxidantes/farmacologia , Ácido Clorogênico/administração & dosagem , Ácido Clorogênico/química , Ácido Clorogênico/farmacologia , Composição de Medicamentos , Liberação Controlada de Fármacos , Nanopartículas/química , Nanopartículas/ultraestrutura , Tamanho da Partícula , Polifenóis/química , Polifenóis/farmacologia
20.
Biomed Chromatogr ; 34(3): e4762, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31760665

RESUMO

Glechomae Herba (GH) is derived from the dried aerial part of Glechoma longituba (Nakai) Kupr., which is harvested from spring to autumn. It has the effects of clearing heat and detoxification. The aim of this paper was to study the chemical composition and the anti-complement activity of GH collected in different months. Ultra-high-performance liquid chromatography coupled to quadrupole time-of-flight tandem mass spectrometry based on predicted compounds screening and diagnostic ion filter strategy was developed for identifying the chemical composition of GH collected in different months. A total of 102 compounds-40 chlorogenic acids (CGAs), 32 phenolic acids, and 30 flavonoids-were reasonably identified in GH. Thirty-four CGAs were discovered in GH for the first time. The correlations between chemical compositions and anti-complement activities of GH collected in different months were analyzed. Phenolic acids and flavonoids were found to be negatively correlated with anti-complement activity, and CGAs were positively correlated with anti-complement activity. At the same time, six CGA standards had obvious anti-complement activity. It was demonstrated that different harvest months had a significant impact on the difference in chemical composition and anti-complement activity of GH. And CGAs might play an important role in the anti-complement activity of GH.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Inativadores do Complemento , Lamiaceae/química , Extratos Vegetais , Espectrometria de Massas em Tandem/métodos , China , Ácido Clorogênico/análise , Ácido Clorogênico/farmacologia , Inativadores do Complemento/análise , Inativadores do Complemento/farmacologia , Flavonoides/análise , Flavonoides/farmacologia , Hidroxibenzoatos/análise , Hidroxibenzoatos/farmacologia , Medicina Tradicional Chinesa , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Estações do Ano
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