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1.
Electron. j. biotechnol ; 51: 17-27, May. 2021. tab, ilus, graf
Article in English | LILACS | ID: biblio-1343317

ABSTRACT

BACKGROUND: In order to produce an effective callus in Echinacea purpurea L.; determination of the explant type and growth regulators that best respond to callus induction and the optimization of the culture conditions to increase the amount of caffeic acid derivatives (CADs) in the obtained callus. CADs contents of callus cultures of E. purpurea were evaluated by establishing an effective callus induction system in vitro. RESULTS: Various medium containing different growth regulators were tested using leaf, petiole, cotyledon and root as the explants. The best callus development was achieved in MS medium with 1.0 mg l 1 2,4- D + 2.0 mg l 1 BAP in leaf, 1.0 mg l 1 NAA + 0.5 mg l 1 TDZ in petiole, 2.0 mg l 1 NAA + 1.0 mg l 1 TDZ in cotyledon and 0.5 mg l 1 NAA + 0.5 mg l 1 BAP in roots. Upon optimisation of callus growth, each type of explant was cultured for 4, 6, 8 and 10 weeks in medium for the analyses of caftaric acid, chlorogenic acid, caffeic acid and chicoric acid contents. The highest amounts of caftaric acid (4.11 mg/g) and chicoric acid (57.89 mg/g) were found from petiole explants and chlorogenic acid (8.83 mg/g) from root explants at the end of the 10-week culture time. CONCLUSIONS: As a result of the present study, the production of caffeic acid derivatives was performed by providing the optimization of E. purpurea L. callus cultures. Effective and repeatable protocols established in this study may offer help for further studies investigating the production of caffeic acid derivatives in vitro.


Subject(s)
Caffeic Acids , Echinacea , Plant Growth Regulators , Time Factors , In Vitro Techniques , Cells, Cultured , Plant Roots/growth & development , Plant Leaves/growth & development , Cotyledon/growth & development , Culture Techniques
2.
Braz. arch. biol. technol ; 64: e21190530, 2021. tab, graf
Article in English | LILACS | ID: biblio-1153299

ABSTRACT

HIGHLIGHTS The phenolic composition, antioxidant activity and cytotoxic potential of the extracts of C. solstitialis and U. picroides were investigated. Caffeic acid was found as the most abundant phenolic compound in the extracts. Both species showed promising antioxidant activity towards different assays. The highest cytotoxic potential was observed in the extract of C. solstitialis.


Abstract It is known that some genera of the Asteraceae family are commonly used in Turkish folk medicine. Several studies have investigated the biological effects of different extracts of Centaurea and Urospermum species, but studies involving the phenolic composition of C. solstitialis and U. picroides extracts are very limited. This study aimed to investigate the phenolic composition and antioxidant activity of C. solstitialis and U. picroides and evaluate their possible cytotoxic effect. RP-HPLC analysis was used to elucidate the phenolic profiles of the ethanolic extracts of flowering parts of C. solstitialis and U. picroides.The both ethanolic extracts were assessed for their antioxidant properties using DPPH, FRAP, phosphomolybdenum and metal chelating assays. Furthermore, the effect of the extracts on cell viability was evaluated against MCF-7 and PC-3 cancer cells and HEK293 cell line using the MTT assay. The most abundant phenolic compound in both extracts was determined to be caffeic acid, and the amount of this compound was 24078.03 and 14329.59 µg g-1 in the extracts of C. solstitialis and U. picroides, respectively. The antioxidant activity of the extracts was found similar. Compared with U. picroides extract, C. solstitialis extract had higher potential on the inhibition of cell viability. The IC50 value of C. solstitialis on MCF cells was found as 58.53 µg mL-1. These data suggest that the extracts of C. solstitialis and U. picroides may be considered as novel and alternative natural antioxidant and anticancer sources.


Subject(s)
Humans , Asteraceae/chemistry , Cytotoxins/pharmacology , Centaurea/chemistry , Phenolic Compounds/analysis , Antioxidants/pharmacology , Phenols/pharmacology , Plants, Medicinal , Turkey , Caffeic Acids/pharmacology , Plant Extracts/pharmacology , Chromatography, High Pressure Liquid , HEK293 Cells
3.
Article in Chinese | WPRIM | ID: wpr-879188

ABSTRACT

The metabolites of salvianolic acid A and salvianolic acid B in rats were analyzed and compared by ultra-high-perfor-mance liquid chromatography with linear ion trap-orbitrap mass spectrometry(UHPLC-LTQ-Orbitrap MS). After the rats were administrated by gavage, plasma at different time points and urine within 24 hours were collected to be treated by solid phase extraction(SPE), then they were gradient eluted by Acquity UPLC BEH C_(18) column(2.1 mm×100 mm, 1.7 μm) and 0.1% formic acid solution(A)-acetonitrile(B) mobile phase system, and finally all biological samples of rats were analyzed under negative ion scanning mode. By obtaining the accurate relative molecular mass and multi-level mass spectrometry information of metabolites, combined with the characteristic cleavage law of the reference standard and literature reports, a total of 30 metabolites, including salvianolic acid A and B, were identified. Among them, there were 24 metabolites derived from salvianolic acid A, with the main metabolic pathways including ester bond cleavage, dehydroxylation, decarboxylation, hydrogenation, methylation, hydroxylation, sulfonation, glucuronidation, and their multiple reactions. There were 15 metabolites of salvianolic acid B, and the main biotransformation pathways were five-membered ring cracking, ester bond cleavage, decarboxylation, dehydroxylation, hydrogenation, methylation, sulfonation, glucuronidation, and their compound reactions. In this study, the cross-metabolic profile of salvianolic acid A and B was elucidated completely, which would provide reference for further studies on the basis of pharmacodynamic substances and the exploration of pharmacological mechanism.


Subject(s)
Animals , Benzofurans , Caffeic Acids , Chromatography, High Pressure Liquid , Lactates , Mass Spectrometry , Rats , Technology
4.
Article in Chinese | WPRIM | ID: wpr-878915

ABSTRACT

Caffeic acid and its oligomers are the main water-soluble active constituents of the traditional Chinese medicine(TCM) Arnebiae Radix. These compounds possess multiple biological activities such as antimicrobial, antioxidant, cardiovascular protective, liver protective, anti-liver fibrosis, antiviral and anticancer activities. The phenylpropanoid pathway in plants is responsible for the biosynthesis of caffeic acid and its oligomers. Glycosylation can change phenylpropanoid solubility, stability and toxic potential, as well as influencing compartmentalization and biological activity. In view of the important role played by de-glycosylation in the regulation of phenylpropanoid homeostasis, the biosynthesis of caffeic acid and its oligomers are supposed to be under the control of relative UDP-glycosyltransferases(UGTs). Through the data mining of Arnebia euchroma transcriptome, we cloned 15 full-length putative UGT genes. After recombinant expression using the prokaryotic system, the crude enzyme solution of the putative UGTs was examined for the glycosylation activities towards caffeic acid and rosmarinic acid in vitro. AeUGT_01, AeUGT_02, AeUGT_03, AeUGT_04 and AeUGT_10 were able to glycosylate caffeic acid and/or rosmarinic acid resulting in different mono-and/or di-glycosylated products in the UPLC-MS analyses. The characterized UGTs were distantly related to each other and divided into different clades of the phylogenetic tree. Based on the observation that each characterized UGT exhibited substrate or catalytic similarity with the members in their own clade, we supposed the glycosylation abilities towards caffeic acid and/or rosmarinic acid were evolved independently in different clades. The identification of caffeic acid and rosmarinic acid UGTs from A. euchroma could lead to deeper understanding of the caffeic acid oligomers biosynthesis and its regulation. Furthermore, these UGTs might be used for regiospecific glycosylation of caffeic acid and rosmarinic acid to produce bioactive compounds for potential therapeutic applications.


Subject(s)
Boraginaceae/genetics , Caffeic Acids , Chromatography, Liquid , Cinnamates , Cloning, Molecular , Depsides , Glycosyltransferases/genetics , Phylogeny , Tandem Mass Spectrometry
5.
Electron. j. biotechnol ; 47: 17-28, sept. 2020. ilus, graf
Article in English | LILACS | ID: biblio-1253006

ABSTRACT

BACKGROUND: Cichoric acid (CA) is extracted from Echinacea purpurea. It is well known and widely used for its immunological function. However, the effect of CA on peripheral blood mononuclear cells (PBMCs) from yaks is still unclear. This study investigated the potential influences of CA on the proliferation, cytokine induction, and apoptosis of PBMCs from Datong yak in vivo, and aimed to provide a basis for exploring the pharmacological activities of CA on yaks. RESULTS: In this study, CA promoted PBMCs proliferation by combining concanavalin A (Con A) and exhibited a dose-dependent effect as demonstrated by a Cell Counting Kit-8. The concentration of 60 µg/ml CA was the best and promoted the transformation from the G0/G1 phase to the S and G2/M phases with Con A. Furthermore, 60 µg/ml CA significantly increased IL-2, IL-6, and IFN-γ levels and PCNA, CDK4 and Bcl-2 expression levels, but it significantly inhibited the TP53, Bax, and Caspase-3 expression levels. Transcriptome analysis revealed a total of 6807 differentially expressed genes (DEGs) between the CA treatment and control groups. Of these genes, 3788 were significantly upregulated and 3019 were downregulated. Gene Ontology and pathway analysis revealed that DEGs were enriched in cell proliferation and immune function signaling pathways. The expression level of some transcription factors (BTB, Ras, RRM_1, and zf-C2H2) and genes (CCNF, CCND1, and CDK4) related to PBMCs proliferation in yaks were significantly promoted after CA treatment. By contrast, anti-proliferation-associated genes (TP53 and CDKN1A) were inhibited. CONCLUSIONS: In summary, CA could regulate the immune function of yaks by promoting proliferation and inhibiting inflammation and apoptosis of PBMCs.


Subject(s)
Animals , Cattle , Succinates/pharmacology , Caffeic Acids/pharmacology , Leukocytes, Mononuclear/drug effects , Echinacea/chemistry , Cell Proliferation/drug effects , Transcription Factors , Enzyme-Linked Immunosorbent Assay , Leukocytes, Mononuclear/cytology , Blotting, Western , Cytokines , Apoptosis/drug effects , Concanavalin A/pharmacology , Real-Time Polymerase Chain Reaction , RNA-Seq
6.
Int. j. morphol ; 38(1): 135-139, Feb. 2020. graf
Article in Spanish | LILACS | ID: biblio-1056411

ABSTRACT

La angiogénesis es el proceso por el cual se forman nuevos vasos sanguíneos a partir de otros ya existentes. Para que esto se lleve a cabo de forma correcta debe existir un balance entre los factores proangiogénicos y los factores antiangiogénicos dentro del microambiente tisular. Por otra parte, la existencia de productos químicos naturales como los polifenoles, que son capaces de adquirirse en la dieta, inducen a estos factores a intervenir en el proceso de angiogénesis. Se administraron los polifenoles en filtros de metilcelulosa sobre la membrana alantocoriónica de huevos White Leghorn, manteniendo el posterior desarrollo normal del feto. Se utilizaron 15 fetos de pollo fijados en formalina tamponada, a los cuales se extrajo el corazón. El procesamiento de las muestras de corazón se realizó a través de técnicas histológicas, histoquímicas e inmunohistoquímica. Finalmente se evaluó la presencia del VEGF y la capacidad de formar vasos sanguíneos bajo el tratamiento con los polifenoles. La inmunorreactividad fue cuantificada mediante Image J®. Los resultados indican que Ácido cafeico y Pinocembrina disminuyen la densidad microvascular y la expresión de VEGF en corazones de fetos de pollo tratados con estos polifenoles. Tanto el Ácido Cafeico como la Pinocembrina cumplen un rol inhibitorio en el proceso de angiogénesis fisiológica en corazón de pollo, pudiendo modular las vías de señalización mediadas por los VEGFR o modulando la disponibilidad de VEGF. Estos polifenoles podrían utilizarse para el estudio de otros tejidos asociados a angiogénesis patológica.


Angiogenesis is the process by which new blood vessels are formed from other existing ones. A balance between proangiogenic factors and anti-angiogenic factors within the microenvironment must exist for the process to be carried out correctly. Similarly, the existence of natural chemicals such as polyphenols, which are capable of being acquired in the diet, induce these factors in the angiogenic process. Polyphenols were administered in the methylcellulose filters on the of chorioallantoic membrane of White Leghorn eggs, maintaining the normal posterior development of the fetus. 15 chicken fetuses were fixed in buffered formalin, obtaining the hearts to histological processing, performing histological, histochemical and immunohistochemical techniques. VEGF levels and the ability of the blood vessels growing under the stimulation of the polyphenols were evaluated. Immunoreactivity was quantified by Image J. The results indicate that caffeic acid and pinocembrin decreased microvascular density and VEGF expression in hearts stimulated with these polyphenols. Both the caffeic and pinocembrin acids play an inhibitory role in the physiological angiogenesis process in the chicken heart, which decrease the microvascular density and could act by modulating the signaling pathways mediated by the VEGFR or by modulating the availability of VEGF. The use of these polyphenols could be useful in studies of other tissues associated with pathological angiogenesis.


Subject(s)
Animals , Caffeic Acids/pharmacology , Neovascularization, Physiologic/drug effects , Chick Embryo , Polyphenols/pharmacology
7.
Electron. j. biotechnol ; 38: 19-26, Mar. 2019. ilus, tab
Article in English | LILACS | ID: biblio-1051542

ABSTRACT

Caffeic acid (CA; 3,4-dihydroxycinnamic acid) is an aromatic compound obtained by the phenylpropanoid pathway. This natural product has antioxidant, antitumor, antiviral, and anti-inflammatory activities. It is also a precursor of CA phenethyl ester (CAPE), a compound with potential as an antidiabetic and liver-protective agent. CA can be found at low concentrations in plant tissues, and hence, its purification is difficult and expensive. Knowledge regarding the pathways, enzymes, and genes involved in CA biosynthesis has paved the way for enabling the design and construction of microbial strains with the capacity of synthesizing this metabolite. In this review, metabolic engineering strategies for the generation of Escherichia coli strains for the biotechnological production of CA are presented and discussed.


Subject(s)
Caffeic Acids/metabolism , Escherichia coli/metabolism , Metabolic Engineering/methods , Biological Products , Biotechnology , Coumaric Acids
8.
Acta cir. bras ; 34(2): e201900204, 2019. tab, graf
Article in English | LILACS | ID: biblio-989051

ABSTRACT

Abstract Purpose: To investigate the protective effects of salvianolic acid A (SAA) on renal damage in rats with chronic renal failure (CRF). Methods: The five-sixth nephrectomy model of CRF was successfully established in group CRF (10 rats) and group CRF+SAA (10 rats). Ten rats were selected as sham-operated group (group S), in which only the capsules of both kidneys were removed. The rats in group CRF+SAA were intragastrically administrated with 10 mg/kg SAA for 8 weeks. The blood urine nitrogen (BUN), urine creatinine (Ucr), creatinine clearance rate (Ccr), and serum uperoxide dismutase (SOD) and malondialdehyde (MDA) were tested. The expressions of transforming growth factor-β1 (TGF-β1), bone morphogenetic protein 7 (BMP-7) and Smad6 protein in renal tissue were determined. Results: After treatment, compared with group CRF, in group CRF+SAA the BUN, Scr, serum MDA and kidney/body weight ratio were decreased, the Ccr and serum SOD were increased, the TGF-β1 protein expression level in renal tissue was decreased, and the BMP-7 and Smad6 protein levels were increased (all P < 0.05). Conclusion: SAA can alleviate the renal damage in CRF rats through anti-oxidant stress, down-regulation of TGF-β1 signaling pathway and up-regulation of BMP-7/Smad6 signaling pathway.


Subject(s)
Animals , Male , Rats , Caffeic Acids/therapeutic use , Smad6 Protein/metabolism , Transforming Growth Factor beta1/metabolism , Bone Morphogenetic Protein 7/metabolism , Kidney Failure, Chronic/drug therapy , Lactates/therapeutic use , Down-Regulation , Up-Regulation , Rats, Sprague-Dawley , Disease Models, Animal , Kidney Failure, Chronic/chemically induced , Kidney Failure, Chronic/metabolism , Kidney Function Tests , Nephrectomy
9.
Article in English | WPRIM | ID: wpr-773974

ABSTRACT

OBJECTIVE@#To investigate the effects of salvianolic acid A (SAA) on cardiomyocyte apoptosis and mitochondrial dysfunction in response to hypoxia/reoxygenation (H/R) injury and to determine whether the Akt signaling pathway might play a role.@*METHODS@#An in vitro model of H/R injury was used to study outcomes on primary cultured neonatal rat cardiomyocytes. The cardiomyocytes were treated with 12.5, 25, 50 μg/mL SAA at the beginning of hypoxia and reoxygenation, respectively. Adenosine triphospate (ATP) and reactive oxygen species (ROS) levels were assayed. Cell apoptosis was evaluated by flow cytometry and the expression of cleaved-caspase 3, Bax and Bcl-2 were detected by Western blotting. The effects of SAA on mitochondrial dysfunction were examined by determining the mitochondrial membrane potential (△Ψm) and mitochondrial permeability transition pore (mPTP), followed by the phosphorylation of Akt (p-Akt) and GSK-3β (p-GSK-3β), which were measured by Western blotting.@*RESULTS@#SAA significantly preserved ATP levels and reduced ROS production. Importantly, SAA markedly reduced the number of apoptotic cells and decreased cleaved-caspase 3 expression levels, while also reducing the ratio of Bax/Bcl-2. Furthermore, SAA prevented the loss of △Ψm and inhibited the activation of mPTP. Western blotting experiments further revealed that SAA significantly increased the expression of p-Akt and p-GSK-3β, and the increase in p-GSK-3β expression was attenuated after inhibition of the Akt signaling pathway with LY294002.@*CONCLUSION@#SAA has a protective effect on cardiomyocyte H/R injury; the underlying mechanism may be related to the preservation of mitochondrial function and the activation of the Akt/GSK-3β signaling pathway.


Subject(s)
Adenosine Triphosphate , Animals , Animals, Newborn , Caffeic Acids , Pharmacology , Cell Hypoxia , Cells, Cultured , Glycogen Synthase Kinase 3 beta , Physiology , Lactates , Pharmacology , Mitochondria, Heart , Physiology , Mitochondrial Membrane Transport Proteins , Myocytes, Cardiac , Proto-Oncogene Proteins c-akt , Physiology , Rats , Rats, Sprague-Dawley , Reactive Oxygen Species , Metabolism , Signal Transduction , Physiology
10.
Article in English | WPRIM | ID: wpr-772276

ABSTRACT

Periodontal disease is associated with chronic oxidative stress and inflammation. Caffeic acid phenethyl ester (CAPE), which is a potent inducer of heme oxygenase 1 (HO1), is a central active component of propolis, and the application of propolis improves periodontal status in diabetic patients. Here, primary murine macrophages were exposed to CAPE. Target gene expression was assessed by whole-genome microarray, RT-PCR and Western blotting. The antioxidative and anti-inflammatory activities of CAPE were examined by exposure of the cells to hydrogen peroxide, saliva and periodontal pathogens. The involvement of HO1 was investigated with the HO1 inhibitor tin protoporphyrin (SnPP) and knockout mice for Nrf2, which is a transcription factor for detoxifying enzymes. CAPE increased HO1 and other heat shock proteins in murine macrophages. A p38 MAPK inhibitor and Nrf2 knockout attenuated CAPE-induced HO1 expression in macrophages. CAPE exerted strong antioxidative activity. Additionally, CAPE reduced the inflammatory response to saliva and periodontal pathogens. Blocking HO1 decreased the antioxidative activity and attenuated the anti-inflammatory activity of CAPE. In conclusion, CAPE exerted its antioxidative effects through the Nrf2-mediated HO1 pathway and its anti-inflammatory effects through NF-κB inhibition. However, preclinical models evaluating the use of CAPE in periodontal inflammation are necessary in future studies.


Subject(s)
Animals , Caffeic Acids , Pharmacology , Heme Oxygenase-1 , Genetics , Metabolism , Humans , Inflammation , Drug Therapy , Mice , NF-kappa B , Genetics , Metabolism , Oxidative Stress , Phenylethyl Alcohol , Pharmacology
11.
Int. j. morphol ; 36(1): 97-103, Mar. 2018. tab, graf
Article in English | LILACS | ID: biblio-893194

ABSTRACT

SUMMARY: Head trauma damages the optic nerve visual function and visual acuity.Effects of head trauma on the retina was investigated with biochemical, histological and immunohistochemical respects.The study was conducted on 30 rats with three groups: group 1 was control group (n=10). Second group was head-traumatized group (n=10) and last group was head-traumatized+Caffeic acid phenethyl ester (CAPE, i.p. 20ml/kg/day). Upon head was traumatized, CAPE was applied to trauma+CAPE group and then for the following four days. At the end of 5th day, rats were anesthetized with ketamine hydroxide and then blood samples were taken for biochemical analysis. MDA and GSH-Px values were compared. After blood sample, total eyes of rats were dissected for histopathological and immunohistochemical analysis. In trauma group, degeneration in retinal photoreceptor cells, disintegrity and in inner and outer nuclear layers, hypertrophy in ganglion cells, and hemorrhage in blood vessels were observed. In the group treated with CAPE, lesser degeneration in photoreceptor cells, regular appearances of inner and outer nuclear layers, mild hemorrhage in blood vessels of ganglionic cell layer were observed. The apoptotic changes caused by trauma seen in photoreceptor and ganglionic cells were decreased and cellular organization was preserved due to CAPE treatment. CAPE was thought to induce healing process on traumatic damages.


RESUMEN: El trauma craneal daña la función visual del nervio óptico y la agudeza visual. Se investigaron los efectos del traumatismo craneal en la retina con aspectos bioquímicos, histológicos e inmunohistoquímicos. El estudio se realizó en 30 ratas distribuidas en tres grupos: grupo control (n = 10); grupo con traumatismo craneal (n = 10); grupo con traumatismo craneoencefálico + Éster fenetílico de ácido cafeico (CAPE, i.p. 20 ml / kg / día). Sobre la cabeza traumatizada, se aplicó CAPE a trauma + grupo CAPE durante los siguientes cuatro días. Al final del día 5, las ratas se anestesiaron con hidróxido de ketamina y luego se tomaron muestras de sangre para el análisis bioquímico. Se compararon los valores de MDA y GSH-Px. Después de la muestra de sangre, se disecaron los ojos de las ratas para su análisis histopatológico e inmunohistoquímico. En el grupo de traumatismos, se observó degeneración en las células fotorreceptoras retinianas, desintegridad en capas nucleares internas y externas, hipertrofia en células ganglionares y hemorragia en los vasos sanguíneos. En el grupo tratado con CAPE, se observó una menor degeneración en las células fotorreceptoras, apariciones regulares de capas nucleares internas y externas, hemorragia leve en los vasos sanguíneos de la capa de células ganglionares. Los cambios apoptóticos causados por el trauma visto en el fotorreceptor y las células ganglionares disminuyeron y la organización celular se conservó debido al tratamiento con CAPE. Se concluyó que CAPE induce un proceso de curación en daños traumáticos.


Subject(s)
Animals , Male , Rats , Caffeic Acids/administration & dosage , Phenylethyl Alcohol/administration & dosage , Retinal Diseases/drug therapy , Retina/drug effects , Brain Injuries, Traumatic/pathology , Glutathione Peroxidase/analysis , Immunohistochemistry , Malondialdehyde/analysis , Phenylethyl Alcohol/analogs & derivatives , Rats, Sprague-Dawley , Retinal Diseases/pathology , Retina/pathology
12.
Article in English | WPRIM | ID: wpr-812414

ABSTRACT

Salvianolic acid A (SAA) is a water-soluble component from the root of Salvia Miltiorrhiza Bge, a traditional Chinese medicine, which has been used for the treatment of cerebrovascular diseases for centuries. The present study aimed to determine the brain protective effects of SAA against cerebral ischemia reperfusion injury in rats, and to figure out whether SAA could protect the blood brain barrier (BBB) through matrix metallopeptidase 9 (MMP-9) inhibition. A focal cerebral ischemia reperfusion model was induced by middle cerebral artery occlusion (MCAO) for 1.5-h followed by 24-h reperfusion. SAA was administered intravenously at doses of 5, 10, and 20 mg·kg. SAA significantly reduced the infarct volumes and neurological deficit scores. Immunohistochemical analyses showed that SAA treatments could also improve the morphology of neurons in hippocampus CA1 and CA3 regions and increase the number of neurons. Western blotting analyses showed that SAA downregulated the levels of MMP-9 and upregulated the levels of tissue inhibitor of metalloproteinase 1 (TIMP-1) to attenuate BBB injury. SAA treatment significantly prevented MMP-9-induced degradation of ZO-1, claudin-5 and occludin proteins. SAA also prevented cerebral NF-κB p65 activation and reduced inflammation response. Our results suggested that SAA could be a promising agent to attenuate cerebral ischemia reperfusion injury through MMP-9 inhibition and anti-inflammation activities.


Subject(s)
Animals , Anti-Inflammatory Agents , Blood-Brain Barrier , Allergy and Immunology , Brain , Brain Ischemia , Drug Therapy , Genetics , Caffeic Acids , Drugs, Chinese Herbal , Humans , Lactates , Male , Matrix Metalloproteinase 9 , Genetics , Metabolism , Rats , Rats, Sprague-Dawley , Reperfusion Injury , Genetics , Allergy and Immunology , Salvia miltiorrhiza , Chemistry , Tissue Inhibitor of Metalloproteinase-1 , Genetics , Metabolism , Transcription Factor RelA , Genetics , Allergy and Immunology
13.
Article in English | WPRIM | ID: wpr-812341

ABSTRACT

Poliumoside is representative of phenylethanoid glycosides, which are widely found in many plants. Poliumoside is also regarded as the main active component of Callicarpa kwangtungensis Chun (CK), though its oral bioavailability in rat is extremely low (0.69%) and its in vivo and in vitro metabolism has not yet been systematically investigated. In the present study, an ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) method was employed to identify the metabolites and investigate the metabolic pathways of poliumoside in rat after oral administration 1.5 g·kg of poliumoside. As a result, a total of 34 metabolites (30 from urine, 17 from plasma, and 4 from bile) and 9 possible metabolic pathways (rearrangment, reduction, hydration, hydrolyzation, dehydration, methylation, hydroxylation, acetylation, and sulfation) were proposed in vivo. The main metabolite, acteoside, was quantified after incubated with rat intestinal bacteria in vitro. In conclusion, the present study systematically explored the metabolites of poliumoside in vivo and in vitro, proposing metabolic pathways that may be significant for further metabolic studies of poliumoside.


Subject(s)
Administration, Oral , Animals , Bacteria , Metabolism , Bile , Chemistry , Caffeic Acids , Blood , Chemistry , Urine , Callicarpa , Chemistry , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Metabolism , Glycosides , Blood , Chemistry , Urine , Intestines , Microbiology , Male , Mass Spectrometry , Methods , Molecular Structure , Plasma , Chemistry , Rats , Rats, Sprague-Dawley , Urine , Chemistry
14.
Article in English | WPRIM | ID: wpr-773624

ABSTRACT

Salvianolic acid A (SAA) is a water-soluble component from the root of Salvia Miltiorrhiza Bge, a traditional Chinese medicine, which has been used for the treatment of cerebrovascular diseases for centuries. The present study aimed to determine the brain protective effects of SAA against cerebral ischemia reperfusion injury in rats, and to figure out whether SAA could protect the blood brain barrier (BBB) through matrix metallopeptidase 9 (MMP-9) inhibition. A focal cerebral ischemia reperfusion model was induced by middle cerebral artery occlusion (MCAO) for 1.5-h followed by 24-h reperfusion. SAA was administered intravenously at doses of 5, 10, and 20 mg·kg. SAA significantly reduced the infarct volumes and neurological deficit scores. Immunohistochemical analyses showed that SAA treatments could also improve the morphology of neurons in hippocampus CA1 and CA3 regions and increase the number of neurons. Western blotting analyses showed that SAA downregulated the levels of MMP-9 and upregulated the levels of tissue inhibitor of metalloproteinase 1 (TIMP-1) to attenuate BBB injury. SAA treatment significantly prevented MMP-9-induced degradation of ZO-1, claudin-5 and occludin proteins. SAA also prevented cerebral NF-κB p65 activation and reduced inflammation response. Our results suggested that SAA could be a promising agent to attenuate cerebral ischemia reperfusion injury through MMP-9 inhibition and anti-inflammation activities.


Subject(s)
Animals , Anti-Inflammatory Agents , Blood-Brain Barrier , Allergy and Immunology , Brain , Brain Ischemia , Drug Therapy , Genetics , Caffeic Acids , Drugs, Chinese Herbal , Humans , Lactates , Male , Matrix Metalloproteinase 9 , Genetics , Metabolism , Rats , Rats, Sprague-Dawley , Reperfusion Injury , Genetics , Allergy and Immunology , Salvia miltiorrhiza , Chemistry , Tissue Inhibitor of Metalloproteinase-1 , Genetics , Metabolism , Transcription Factor RelA , Genetics , Allergy and Immunology
15.
Article in English | WPRIM | ID: wpr-776919

ABSTRACT

Poliumoside is representative of phenylethanoid glycosides, which are widely found in many plants. Poliumoside is also regarded as the main active component of Callicarpa kwangtungensis Chun (CK), though its oral bioavailability in rat is extremely low (0.69%) and its in vivo and in vitro metabolism has not yet been systematically investigated. In the present study, an ultra performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UPLC/Q-TOF-MS) method was employed to identify the metabolites and investigate the metabolic pathways of poliumoside in rat after oral administration 1.5 g·kg of poliumoside. As a result, a total of 34 metabolites (30 from urine, 17 from plasma, and 4 from bile) and 9 possible metabolic pathways (rearrangment, reduction, hydration, hydrolyzation, dehydration, methylation, hydroxylation, acetylation, and sulfation) were proposed in vivo. The main metabolite, acteoside, was quantified after incubated with rat intestinal bacteria in vitro. In conclusion, the present study systematically explored the metabolites of poliumoside in vivo and in vitro, proposing metabolic pathways that may be significant for further metabolic studies of poliumoside.


Subject(s)
Administration, Oral , Animals , Bacteria , Metabolism , Bile , Chemistry , Caffeic Acids , Blood , Chemistry , Urine , Callicarpa , Chemistry , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Chemistry , Metabolism , Glycosides , Blood , Chemistry , Urine , Intestines , Microbiology , Male , Mass Spectrometry , Methods , Molecular Structure , Plasma , Chemistry , Rats , Rats, Sprague-Dawley , Urine , Chemistry
16.
An. acad. bras. ciênc ; 89(2): 1095-1109, Apr.-June 2017. tab, graf
Article in English | LILACS | ID: biblio-886704

ABSTRACT

ABSTRACT Hepatic disorders such as steatosis and alcoholic steatohepatitis are common diseases that affect thousands of people around the globe. This study aims to identify the main phenol compounds using a new HPLC-ESI+-MS/MS method, to evaluate some oxidative stress parameters and the hepatoprotective action of green dwarf coconut water, caffeic and ascorbic acids on the liver and serum of rats treated with ethanol. The results showed five polyphenols in the lyophilized coconut water spiked with standards: chlorogenic acid (0.18 µM), caffeic acid (1.1 µM), methyl caffeate (0.03 µM), quercetin (0.08 µM) and ferulic acid (0.02 µM) isomers. In the animals, the activity of the serum γ-glutamyltranspeptidase (γ-GT) was reduced to 1.8 I.U/L in the coconut water group, 3.6 I.U/L in the ascorbic acid group and 2.9 I.U/L in the caffeic acid groups, when compared with the ethanol group (5.1 I.U/L, p<0.05). Still in liver, the DNA analysis demonstrated a decrease of oxidized bases compared to ethanol group of 36.2% and 48.0% for pretreated and post treated coconut water group respectively, 42.5% for the caffeic acid group, and 34.5% for the ascorbic acid group. The ascorbic acid was efficient in inhibiting the thiobarbituric acid reactive substances (TBARS) in the liver by 16.5% in comparison with the ethanol group. These data indicate that the green dwarf coconut water, caffeic and ascorbic acids have antioxidant, hepatoprotective and reduced DNA damage properties, thus decreasing the oxidative stress induced by ethanol metabolism.


Subject(s)
Animals , Male , Ascorbic Acid/pharmacology , DNA Damage/drug effects , Caffeic Acids/pharmacology , Cocos/chemistry , Oxidative Stress/drug effects , Ethanol/pharmacology , Liver/drug effects , Time Factors , Triglycerides/blood , Water/pharmacology , Lipid Peroxidation , Cholesterol/blood , Reproducibility of Results , Thiobarbituric Acid Reactive Substances , Rats, Wistar , Tandem Mass Spectrometry , Liver/metabolism , Antioxidants/pharmacology
17.
An. acad. bras. ciênc ; 89(1): 45-55, Jan,-Mar. 2017. tab, graf
Article in English | LILACS | ID: biblio-886629

ABSTRACT

ABSTRACT Propolis produced by selected bees Apis mellifera were collected from March to June of 2013 and in March of 2015 and analyzed in order to evaluate the influence of climate, colony of origin, and food supplementation of colonies on the content of total phenolic and flavonoid by chromatographic analysis and antioxidant activity by radical scavenging of 2,2-diphenyl-1-picrylhydrazyl hydrate (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) and ferric reducing antioxidant power (FRAP) methods. The Principal Component Analysis (PCA) was carried out with propolis collected in 2013 and two clusters were formed. Propolis produced in the months of March and April showed a higher content of total phenolic compounds (TPC) and antioxidant capacity than those produced in May and June. The results of PCA obtained from samples collected in March of 2013 and 2015 showed two clusters, and propolis collected in 2015 were more bioactive and presented a higher content of TPC. The chromatographic analysis of extracts allowed the identification of phenolic acids p-coumaric, ferulic and caffeic with similar chemical profiles that could be closely related to the botanical origin of propolis. It can be concluded that the season and food supplementation of colonies influenced the chemical composition and the biological activity of samples analysed.


Subject(s)
Animals , Propolis/chemistry , Seasons , Bees/physiology , Dietary Supplements , Hydroxybenzoates/analysis , Antioxidants/analysis , Reference Values , Temperature , Flavonoids/analysis , Caffeic Acids/analysis , Multivariate Analysis , Reproducibility of Results , Chromatography, High Pressure Liquid , Coumaric Acids/analysis , Principal Component Analysis , Indicators and Reagents
18.
Int. j. morphol ; 35(1): 141-147, Mar. 2017. ilus
Article in English | LILACS | ID: biblio-840945

ABSTRACT

The aim of this study was to investigate the effects of caffeic acid phenethyl ester (CAPE) as a prophylactic agent on ischemia/reperfusion (I/R) injury in the rat ovary. A total of 28 Wistar rats were divided into 4 equal groups: (I) sham, (II) ischemia, (III) ischemia + reperfusion, and (IV) IR + CAPE. In groups I and II, ovary torsion was not performed and no drug was administered. In group III, 1 hour of ischemia and 2 hours of reperfusion were performed and no drug was given. Ovarian tissue concentrations of malondialdehyde were significantly higher in the torsion and detorsion groups compared with the sham and Cape groups (P<0.005). The detorsion group showed preantral ovarian follicles and luteal folicules around the blood vessels and positive expression of CD34. In the CAPE group the stromal vascular endothelium with weak expression of CD34 was detected in small areas, and the ovarian follicles and the corpus luteum showed negative expression of CD34. In the study, Biochemical and histopathological results of CAPE treatment was considered to torsion-detorsioned the model showed a protective effect against tissue damage.


El objetivo de este trabajo consistió en investigar los efectos del éster fenetílico del ácido cafeico (EFAC) como agente profiláctico en la lesión por isquemia/reperfusión (I / R) en el ovario de rata. Un total de 28 ratas Wistar se dividieron en 4 grupos iguales: (I) control, (II) isquemia, (III) isquemia + reperfusión, y (IV) IR + EFAC. En los grupos I y II, no se realizó torsión ovárica y no se administró ningún fármaco. En el grupo III, se provocó una hora de isquemia, dos horas de reperfusión y no se administró ningún fármaco. Las concentraciones de malondialdehído en los tejidos ováricos fueron significativamente mayores en los grupos de torsión y de destorsión, en comparación con los grupos sham y de EFAC (P <0,005). El grupo de destorsión mostró folículos ováricos preantrales y folículos lúteos alrededor de los vasos sanguíneos y expresión positiva de CD34. En el grupo EFAC el endotelio vascular estromal con expresión débil de CD34 se detectó en áreas pequeñas, y los folículos ováricos y el cuerpo lúteo mostraron expresión negativa de CD34. En el estudio, fueron considerados los resultados bioquímicos e histopatológicos del tratamiento EFAC en relación a la torsión-destorsión, desarrollando un modelo que mostró un efecto protector contra el daño tisular.


Subject(s)
Animals , Female , Rats , Caffeic Acids/pharmacology , Ovary/drug effects , Phenylethyl Alcohol/pharmacology , Reperfusion Injury/drug therapy
19.
Braz. j. med. biol. res ; 49(3): e5003, Mar. 2016. tab, graf
Article in English | LILACS | ID: lil-771936

ABSTRACT

Fractionation of the EtOH extract from aerial parts of Baccharis uncinella C. DC. (Asteraceae) led to isolation of caffeic and ferulic acids, which were identified from spectroscopic and spectrometric evidence. These compounds exhibit antioxidant and anti-inflammatory properties and have been shown to be effective in the prevention/treatment of metabolic syndrome. This study investigated whether the combined treatment of caffeic and ferulic acids exhibits a more significant beneficial effect in a mouse model with metabolic syndrome. The combination treatment with caffeic and ferulic acids was tested for 60 days in C57 mice kept on a high-fat (40%) diet. The data obtained indicated that treatment with caffeic and ferulic acids prevented gain in body weight induced by the high-fat diet and improved hyperglycemia, hypercholesterolemia and hypertriglyceridemia. The expression of a number of metabolically relevant genes was affected in the liver of these animals, showing that caffeic and ferulic acid treatment results in increased cholesterol uptake and reduced hepatic triglyceride synthesis in the liver, which is a likely explanation for the prevention of hepatic steatosis. In conclusion, the combined treatment of caffeic and ferulic acids displayed major positive effects towards prevention of multiple aspects of the metabolic syndrome and liver steatosis in an obese mouse model.


Subject(s)
Animals , Male , Baccharis/chemistry , Caffeic Acids/administration & dosage , Coumaric Acids/administration & dosage , Metabolic Syndrome/prevention & control , Protective Agents/administration & dosage , Caffeic Acids/chemistry , Cholesterol/metabolism , Coumaric Acids/chemistry , Diet, High-Fat/adverse effects , Drug Therapy, Combination/methods , Fatty Liver/metabolism , Fatty Liver/pathology , Metabolic Syndrome/drug therapy , Mice, Inbred C57BL , Models, Animal , Protective Agents/chemistry , Triglycerides/metabolism
20.
Acta Pharmaceutica Sinica ; (12): 100-104, 2016.
Article in English | WPRIM | ID: wpr-320010

ABSTRACT

A new caffeate compound, (E)-erythro-syringylglyceryl caffeate (1), was isolated from the roots and rhizomes of Nardostachys chinensis Batal., together with nine known phenolic compounds, including (+)-licarin A (2), naringenin 4', 7-dimethyl ether (3), pinoresinol-4-O-β-D-glucoside (4), caraphenol A (5), Z-miyabenol C (6), protocatechuic acid (7), caffeic acid (8), gallic acid (9) and vanillic acid (10). Their chemical structures were elucidated on the basis of spectroscopic data and physicochemical properties. Furthermore, this is the first report of compounds 2, 5 and 6 from Nardostachys genus.


Subject(s)
Caffeic Acids , Chemistry , Flavanones , Chemistry , Furans , Chemistry , Glucosides , Chemistry , Hydroxybenzoates , Chemistry , Lignans , Chemistry , Nardostachys , Chemistry , Plant Roots , Chemistry , Rhizome , Chemistry , Vanillic Acid , Chemistry
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