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1.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 352-363, 2022.
Article in English | WPRIM | ID: wpr-929266

ABSTRACT

Currently, chemoresistance seriously attenuates the curative outcome of liver cancer. The purpose of our work was to investigate the influence of 6-shogaol on the inhibition of 5-fluorouracil (5-FU) in liver cancer. The cell viability of cancer cells was determined by MTT assay. Liver cancer cell apoptosis and the cell cycle were examined utilizing flow cytometry. Moreover, qRT-PCR and western blotting was used to analyse the mRNA and protein expression levels, respectively. Immunohistochemistry assays were used to examine multidrug resistance protein 1 (MRP1) expression in tumour tissues. In liver cancer cells, we found that 6-shogaol-5-FU combination treatment inhibited cell viability, facilitated G0/G1 cell cycle arrest, and accelerated apoptosis compared with 6-shogaol or 5-FU treatment alone. In cancer cells cotreated with 6-shogaol and 5-FU, AKT/mTOR pathway- and cell cycle-related protein expression levels were inhibited, and MRP1 expression was downregulated. AKT activation or MRP1 increase reversed the influence of combination treatment on liver cancer cell viability, apoptosis and cell cycle arrest. The inhibition of AKT activation to the anticancer effect of 6-shogaol-5-FU could be reversed by MRP1 silencing. Moreover, our results showed that 6-shogaol-5-FU combination treatment notably inhibited tumour growth in vivo. In summary, our data demonstrated that 6-shogaol contributed to the curative outcome of 5-FU in liver cancer by inhibiting the AKT/mTOR/MRP1 signalling pathway.


Subject(s)
Humans , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Apoptosis , Catechols , Cell Cycle , Cell Cycle Checkpoints , Cell Line, Tumor , Cell Proliferation , Drug Resistance, Neoplasm , Fluorouracil/pharmacology , Liver Neoplasms/genetics , Multidrug Resistance-Associated Proteins , Proto-Oncogene Proteins c-akt/metabolism , TOR Serine-Threonine Kinases/metabolism
2.
China Journal of Chinese Materia Medica ; (24): 1642-1649, 2022.
Article in Chinese | WPRIM | ID: wpr-928094

ABSTRACT

This study investigated the effects and mechanisms of 6-gingerol on adipose tissue insulin resistance in naturally aging rats with glycolipid metabolism disorders. Twenty-seven aging male SD rats were randomly divided into a model group(aged, n=9) and two groups treated with 6-gingerol at 0.05 mg·kg~(-1)(G-L, n=9) and 0.2 mg·kg~(-1)(G-H, n=9). Six young rats were randomly assigned to a normal control group(NC). Rats were treated for seven weeks by gavage. Non-esterified fatty acid(NEFA) and insulin content was determined by enzyme-linked immunosorbent assay(ELISA), and adipose tissue insulin resistance index(Adipo-IR) was calculated. HE staining was used to observe the size of adipocytes in epididymal white adipose tissue(eWAT). The gene and protein expression levels of adiponectin receptor 1(AdipoR1), AMP-activated protein kinase α(AMPKα), phosphorylated AMPK(p-AMPKα~(Thr172)), peroxisome proliferator-activated receptor-γ coactivator-1α(PGC-1α), phosphatidylinositol 3-kinase(PI3 K), protein kinase B(Akt), phosphorylated Akt(p-Akt~(Ser473)), tumor necrosis factor-α(TNF-α), c-Jun N-terminal kinase 1/2(JNK1/2), phosphorylated JNK1/2(p-JNK~(Thr183/Tyr185)), interleukin-1β(IL-1β), and interleukin-6(IL-6) in adiponectin(APN), insulin, and inflammatory factor signaling pathways were detected by Western blot and real-time RCR, respectively. The results showed that 6-gingerol at a high dose could significantly decrease the fasting plasma content of NEFA and insulin and reduce Adipo-IR. Additionally, 6-gingerol at a high dose significantly increased the protein and mRNA expression of APN, AdipoR1, PGC-1α, and PI3 K in eWAT, elevated the relative expression of p-AMPK~(Thr172) and p-Akt~(Ser 473), reduced the protein and mRNA expression of TNF-α, IL-1, and IL-6 in eWAT, and decreased the relative expression of p-JNK1 and p-JNK2. This study reveals that 6-gingerol can improve insulin sensitivity of adipose tissues in aging rats with glycolipid metabolism disorders, and this effect is presumedly achieved by enhancing the PI3 K/Akt signaling pathway, inhibiting adipose tissue inflammation, increasing APN synthesis, enhancing AdipoR1 expression, and activating its downstream AMPK/PGC-1α signaling pathway.


Subject(s)
Animals , Male , Rats , Adipose Tissue , Aging , Catechols , Fatty Alcohols , Insulin Resistance , Rats, Sprague-Dawley
3.
Biol. Res ; 54: 35-35, 2021. ilus, graf
Article in English | LILACS | ID: biblio-1505820

ABSTRACT

BACKGROUND: Urushiols are pro-electrophilic haptens that cause severe contact dermatitis mediated by CD8+ effector T-cells and downregulated by CD4+ T-cells. However, the molecular mechanism by which urushiols stimulate innate immunity in the initial stages of this allergic reaction is poorly understood. Here we explore the sub-cellular mechanisms by which urushiols initiate the allergic response. RESULTS: Electron microscopy observations of mouse ears exposed to litreol (3-n-pentadecyl-10-enyl-catechol]) showed keratinocytes containing swollen mitochondria with round electron-dense inclusion bodies in the matrix. Biochemical analyses of sub-mitochondrial fractions revealed an inhibitory effect of urushiols on electron flow through the mitochondrial respiratory chain, which requires both the aliphatic and catecholic moieties of these allergens. Moreover, urushiols extracted from poison ivy/oak (mixtures of 3-n-pentadecyl-8,11,13 enyl/3-n-heptadecyl-8,11 enyl catechol) exerted a higher inhibitory effect on mitochondrial respiration than did pentadecyl catechol or litreol, indicating that the higher number of unsaturations in the aliphatic chain, stronger the allergenicity of urushiols. Furthermore, the analysis of radioactive proteins isolated from mitochondria incubated with 3H-litreol, indicated that this urushiol was bound to cytochrome c1. According to the proximity of cytochromes c1 and b, functional evidence indicated the site of electron flow inhibition was within complex III, in between cytochromes bL (cyt b566) and bH (cyt b562). CONCLUSION: Our data provide functional and molecular evidence indicating that the interruption of the mitochondrial electron transport chain constitutes an important mechanism by which urushiols initiates the allergic response. Thus, mitochondria may constitute a source of cellular targets for generating neoantigens involved in the T-cell mediated allergy induced by urushiols.


Subject(s)
Animals , Mice , Allergens , Cytochromes b , Catechols , Cytochromes c1 , Cytochromes c , Electron Transport , Mitochondria
4.
J. appl. oral sci ; 29: e20210209, 2021. graf
Article in English | LILACS | ID: biblio-1340103

ABSTRACT

Abstract Objective Oral squamous cell carcinoma (OSCC) is one of the common type of cancer that leads to death; and is becoming a global concern. Due to the lack of efficient chemotherapeutic agents for patients with oral cancer, the prognosis remains poor. 6-shogaol, a bioactive compound of ginger, has a broad spectrum of bioactivities and has been widely used to relieve many diseases. However, its effects on human oral cancer have not yet been fully evaluated. In our study, we investigated the anticancer effects of 6-shogaol on the proliferation, migration, invasion, apoptosis, and underlying mechanisms within human OSCC cell lines. Methodology We investigated the effect of 6-shogaol on the growth of OSCC cells by cell viability and soft agar colony formation assay. Migration and invasion assays were conducted to confirm the effect 6-shogaol on OSCC cell metastasis. Apoptosis was detected by flow cytometry and the underlying mechanism on the antigrowth effect of 6-shogaol in OSCC cells was assessed using western blotting. Results In our results, 6-shogaol not only suppressed proliferation and anchorage-independent cell growth in OSCC cells, but also induced apoptosis by regulating the apoptosis-associated factors such as p53, Bax, Bcl-2, and cleaved caspase-3. Migration and invasion of OSCC cells were inhibited following the regulation of E-cadherin and N-cadherin by 6-shogaol. Additionally, 6-shogaol treatment significantly inhibited the PI3K/AKT signaling pathway. Conclusion Therefore, our results may provide critical evidence that 6-shogaol can be a potential new therapeutic candidate for oral cancer.


Subject(s)
Humans , Mouth Neoplasms/metabolism , Catechols/pharmacology , Squamous Cell Carcinoma of Head and Neck/metabolism , Signal Transduction , Cell Movement , Apoptosis , Phosphatidylinositol 3-Kinases/metabolism , Cell Line, Tumor , Cell Proliferation , Proto-Oncogene Proteins c-akt/metabolism
5.
Braz. arch. biol. technol ; 62: e19180360, 2019. tab, graf
Article in English | LILACS | ID: biblio-1055421

ABSTRACT

Abstract Catecholase (EC 1.10.3.1), an oxidoreductase enzyme is a key member of polyphenol oxidase family which catalyze the degradation of catechol. This enzyme possesses vast applications in diverse areas and is found in bacteria, fungi, mushrooms, higher plants, arthropods, amphibians and mammals. Catechol, a phenolic compound, is used as a starting material in the synthesis of various industrial compounds such as inhibitors, antioxidants, pesticides etc. The release of this phenolic compound in the environment causes toxicity to both flora and fauna. In the present studies, emphasis has been laid on isolation, screening and characterization of catechol degrading bacterium coupled with synthesis of catecholase enzyme. Further, the selected isolated strain was phenotypically characterized and was found to be member of genus Pseudomonas. Among all the isolates, BSC-6 was found as best isolate with maximum extracellular catecholase activity of 152.32 IU/L obtained after scale up studies. The herein synthesized bacterial catecholase may be employed for wide applications particularly in bioremediation of phenol enriched polluted sites.


Subject(s)
Oxidoreductases , Catechols , Polyphenols , Pseudomonas , Biodegradation, Environmental
6.
An. acad. bras. ciênc ; 89(4): 2707-2717, Oct.-Dec. 2017. graf
Article in English | LILACS | ID: biblio-886861

ABSTRACT

ABSTRACT 6-Gingerol is the major active constituent of ginger. In the current study, we aimed to investigate the mechanisms underlying the effects of 6-Gingerol on hair growth. Mice were randomly divided into five groups; after hair depilation (day 0), mice were treated with saline, or different concentrations of 6-Gingerol for 11 days. The histomorphological characteristics of the growing hair follicles were examined after hematoxylin and eosin staining. The results indicated that 6-Gingerol significantly suppressed hair growth compared with that in the control group. And choose the concentration of 6-Gingerol at 1 mg/mL to treated with mice. Moreover, 6-Gingerol (1 mg/mL) significantly reduced hair re-growth ratio, hair follicle number, and hair follicle length, which were associated with increased expression of MMP2 and MMP9. Furthermore, the growth factors, such as EGF, KGF, VEGF, IGF-1 and TGF-β participate in the hair follicle cycle regulation and regulate hair growth. We then measured the concentrations of them using ELISA assays, and the results showed that 6-Gingerol decreased EGF, KGF, VEGF, and IGF-1 concentrations, and increased TGF-β concentration. Thus, this study showed that 6-Gingerol might act as a hair growth suppressive drug via induction of MMP2 and MMP9 expression, which could interfere with the hair cycle.


Subject(s)
Animals , Male , Female , Rabbits , Plant Extracts/pharmacology , Catechols/pharmacology , Hair Follicle/drug effects , Matrix Metalloproteinase 2/biosynthesis , Matrix Metalloproteinase 9/biosynthesis , Fatty Alcohols/pharmacology , Insulin-Like Growth Factor I/biosynthesis , Random Allocation , Enzyme Induction , Transforming Growth Factor beta/biosynthesis , Hair Follicle/pathology , Vascular Endothelial Growth Factor A/biosynthesis , Fibroblast Growth Factor 7/biosynthesis , Mice, Inbred C57BL
7.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 434-440, 2016.
Article in English | WPRIM | ID: wpr-812613

ABSTRACT

TRPA1 channels are non-selective cation channels that could be activated by plant-derived pungent products, including gingerol, a main active constituent of ginger. Ginger could improve the digestive function; however whether ginger improves the digestive function through activating TRPA1 receptor in gastrointestinal tract has not been investigated. In the present study, gingerol was used to stimulate cell lines (RIN14B or STC-1) while depletion of extracellular calcium. TRPA1 inhibitor (rethenium red) and TRPA1 gene silencing via TRPA1-specific siRNA were also used for mechanistic studies. The intracellular calcium and secretion of serotonin or cholecystokinin were measured by fura-2/AM and ELISA. Stimulation of those cells with gingerol increased intracellular calcium levels and the serotonin or cholecystokinin secretion. The gingerol-induced intracellular calcium increase and secretion (serotonin or cholecystokinin) release were completely blocked by ruthenium red, EGTA, and TRPA1-specific siRNA. In summary, our results suggested that gingerol derived from ginger might improve the digestive function through secretion releasing from endocrine cells of the gut by inducing TRPA1-mediated calcium influx.


Subject(s)
Humans , Calcium , Metabolism , Calcium Channels , Genetics , Metabolism , Catechols , Pharmacology , Cell Line , Fatty Alcohols , Pharmacology , Gastrointestinal Tract , Metabolism , Ginger , Chemistry , Nerve Tissue Proteins , Genetics , Metabolism , Plant Extracts , Pharmacology , TRPA1 Cation Channel , Transient Receptor Potential Channels , Genetics , Metabolism
8.
Chinese Journal of Stomatology ; (12): 166-171, 2016.
Article in Chinese | WPRIM | ID: wpr-259423

ABSTRACT

<p><b>OBJECTIVE</b>To provide a theoretical basis for surface modification of titanium implants, the effects of the stiffness of polyelectrolyte multilayer films on titanium surface on bacterium adhesion was explored.</p><p><b>METHODS</b>Via layer-by-layer technique, catechol functionalized polyelectrolyte multilayer film (cPEM) was constructed on titanium surface by using catechol functionalized hyaluronic acid (cHA) and lipopolysaccharide-amine nanopolymersomes (NP). The stiffness of cPEM was controlled by adjusting the catechol substitution degree of cHA (5%, 10%, 20%, 30%, 40%, 50%, 60%, 70%). Titanium samples covered with cPEM were selected as test group, and the cPEM was constructed with the lowest, medium and highest stiffness. The polished titanium was used as a control. The surface topography of titanium before and after film construction was observed by scanning electron microscopy (SEM). At 1 and 24 h after incubation, the adhesion and clonal formation of Streptococcus mutans (S. mutans) on different titanium surfaces were quantified, and their morphology and survival status were observed by SEM and laser scanning confocal microscope (LSCM).</p><p><b>RESULTS</b>When the catechol grafting ratio was 5%, 30% and 70%, the lowest, medium and highest cPEM stiffness were obtained, and the cPEM stiffness were (10.69±4.54) GPa(cPEM-L), (20.99± 5.81) GPa (cPEM-M) and (32.57±6.93) GPa (cPEM-H) respectively, and the stiffness of polished titanium was (107.12±8.68) GPa (P<0.05). SEM observation showed that after cPEM coating, the titanium surface became smoother. After incubation for 1 and 24 h, the amount of adhesion and clonal formation of S. mutans on cPEM were higher than those on control titanium, and the difference was statistically significant (P<0.05). SEM images showed that for 1 h incubation, softer surfaces were beneficial for S. mutans adhering and agglomerating, while this difference nearly disappeared at 24 h. Observation under LSCM revealed that most of bacteria were alive on titanium disks at 1 h, and their amount decreased with the increase of stiffness. At 24 h, the living/dead bacterium ratios on cPEM-L and control titanium was higher than that on cPEM-M and cPEM-H, and cPEM-L surface was dominated by living bacteria, while stiffer cPEM-M and cPEM-H had more dead bacteria than living bacteria.</p><p><b>CONCLUSIONS</b>Increasing the stiffness of polyelectrolyte films on titanium limits the adhesion of S. mutans. As an independent factor, stiffness influences the bacterium adhesion.</p>


Subject(s)
Bacterial Adhesion , Catechols , Elasticity , Hyaluronic Acid , Lipopolysaccharides , Microscopy, Confocal , Microscopy, Electron, Scanning , Nanoparticles , Polymers , Chemistry , Streptococcus mutans , Physiology , Surface Properties , Time Factors , Titanium , Chemistry
9.
Rev. paul. pediatr ; 33(1): 28-33, Jan-Mar/2015. tab
Article in English | LILACS | ID: lil-744701

ABSTRACT

OBJECTIVE: To develop a homologous human milk supplement for very low-birth weight infant feeding, using an original and simplified methodology, to know the nutritional composition of human milk fortified with this supplement and to evaluate its suitability for feeding these infants. METHODS: For the production and analysis of human milk with the homologous additive, 25 human milk samples of 45mL underwent a lactose removal process, lyophilization and then were diluted in 50mL of human milk. Measurements of lactose, proteins, lipids, energy, sodium, potassium, calcium, phosphorus and osmolality were performed. RESULTS: The composition of the supplemented milk was: lactose 9.22±1.00g/dL; proteins 2.20±0.36g/dL; lipids 2.91±0.57g/dL; calories 71.93±8.69kcal/dL; osmolality 389.6±32.4mOsmol/kgH2O; sodium 2.04±0.45mEq/dL; potassium 1.42±0.15mEq/dL; calcium 43.44±2.98mg/dL; and phosphorus 23.69±1.24mg/dL. CONCLUSIONS: According to the nutritional contents analyzed, except for calcium and phosphorus, human milk with the proposed supplement can meet the nutritional needs of the very low-birth weight preterm infant. .


OBJETIVO: Elaborar com metodologia original e simplificada um aditivo homólogo do leite humano para a alimentação do recém-nascido de muito baixo peso, conhecer a composição nutricional do leite humano fortificado com esse aditivo e avaliar sua adequação para a alimentação desses recém-nascidos. MÉTODOS: Para a produção e análise do leite humano com o aditivo homólogo, 25 amostras de 45 mL de leite humano passaram por processos de retirada de lactose, liofilização e foram diluídas em 50 mL de leite humano. Foram feitas dosagens de lactose, proteínas, lipídios, energia, sódio, potássio, cálcio, fósforo e osmolalidade. RESULTADOS: A composição do leite aditivado foi lactose 9,22 ± 1 g/dL; proteínas 2,20 ± 0,36 g/dL; lípides 2,91 ± 0,57 g/dL; calorias 71,93 ± 8,69 kcal/dL; osmolalidade 389,6 ± 32,4mOsmol/kgH2O; sódio 2,04 ± 0,45mEq/dL; potássio 1,42 ± 0,15mEq/dL; cálcio 43,44 ± 2,98 mg/dL; e fósforo 23,69 ± 1,24 mg/dL. CONCLUSÕES: De acordo com os teores nutricionais analisados, com exceção do cálcio e do fósforo, o leite humano com o aditivo proposto pode atender às necessidades nutricionais do recém-nascido pré-termo de muito baixo peso. .


Subject(s)
Aldose-Ketose Isomerases/antagonists & inhibitors , Anti-Bacterial Agents/pharmacology , Catechols/pharmacology , Enzyme Inhibitors/pharmacology , Escherichia coli/drug effects , Rhodanine/pharmacology , Aldose-Ketose Isomerases/metabolism , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Catechols/chemistry , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/chemical synthesis , Escherichia coli/enzymology , Escherichia coli/growth & development , Microbial Sensitivity Tests , Molecular Structure , Rhodanine/chemistry , Structure-Activity Relationship
10.
Chinese Journal of Natural Medicines (English Ed.) ; (6): 390-400, 2015.
Article in English | WPRIM | ID: wpr-812530

ABSTRACT

The present study was designed to characterize the chemical constituents of Guge Fengtong Tablet (GGFTT). Based on the chromatographic retention behavior, fragmentation pathways of chemical components and the published literatures, a diagnostic ion filtering strategy with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (HPLC-ESI-Q-TOF/MS) was established to identify the multiple bioactive constituents of GGFTT. The rapid identification of forty-seven components, including 18 phenolic acids, 8 saponins, 14 gingerol-related compounds, and 7 diarylhepatonoids, was accomplished using this newly developed method. The coupling of HPLC-ESI-Q-TOF/MS with the diagnostic ion filtering strategy was useful and efficient for the in-depth structural elucidation of chemical compounds of GGFTT.


Subject(s)
Catechols , Chromatography, High Pressure Liquid , Diarylheptanoids , Drugs, Chinese Herbal , Chemistry , Fatty Alcohols , Hydroxybenzoates , Saponins , Spectrometry, Mass, Electrospray Ionization , Tablets, Enteric-Coated , Chemistry , Tandem Mass Spectrometry
11.
China Journal of Chinese Materia Medica ; (24): 3630-3635, 2015.
Article in Chinese | WPRIM | ID: wpr-320895

ABSTRACT

To explore the antagonistic effect of gingerols against the inflammation induced by lectin from Pinellia ternata. In this study, ELISA method was used to determine the effect of different extracts from gingerols on the release of inflammatory factor TNF-α from macrophages induced by lectin from P. ternata. The fluorescence probe was used to determine the effect of gingerols on the changes in ROS of macrophages induced by lectin from P. ternata. The western-blot method was applied to study the effect of gingerols on the increase in expression of cell receptor interacting protein RIP3 in macrophages induced by lectin from P. ternata. The scanning electron microscope (SEM) was used to study the effect of gingerols on morphological changes in macrophages induced by lectin from P. ternata. According to the results, gingerols can significantly inhibit the release of inflammatory factor from macrophages induced by lectin from P. ternata, ROS overproduction and increase in RIP3 expression. SEM results showed that gingerols can inhibit the cytomorphosis and necrocytosis induced by lectin from P. ternata. Fresh ginger's detoxication may be related to gingerols' effects in inhibiing release of inflammatory factor, ROS overproduction and increase in RIP3 expression caused by macrophages induced by lectin from P. ternata, which are mainly inflammatory development.


Subject(s)
Animals , Male , Mice , Catechols , Pharmacology , Cells, Cultured , Drug Antagonism , Fatty Alcohols , Pharmacology , Ginger , Chemistry , Lectins , Toxicity , Macrophages , Metabolism , Mice, Inbred ICR , Pinellia , Chemistry , Toxicity , Reactive Oxygen Species , Metabolism , Receptor-Interacting Protein Serine-Threonine Kinases , Genetics , Metabolism , Tumor Necrosis Factor-alpha , Genetics , Metabolism
12.
China Journal of Chinese Materia Medica ; (24): 4200-4204, 2015.
Article in Chinese | WPRIM | ID: wpr-279262

ABSTRACT

To establish a new method for simultaneously determining the content of five gingerol compounds in different processing degrees of ginger charcoal and PCA principal component analysis was conducted for analysis. Samples were analyzed on Ultimate TM XB-C18 column (4.6 mm x 250 mm, 5 μm) , with acetonitrile (A) -0.1% phosphoric acid solution (B) as mobile phase for gradient elution. Detection wavelength was set at 280 nm. The flow rate was 0.6 mL x min(-1) and the column temperature was 30 degrees C. The five compounds were separated well and showed good linearity (r ≥ 0.999 7) within the concentration ranges tested. The average value for recoveries was between 98.86% - 101.5% (RSD 1.4% - 2.9%). The contents of five compounds showed difference among different processing degrees of ginger charcoal. Zingiberone had the highest content in the standard carbon, and the content of gingerol was decreased as the deepening of processing degree. Different processing degrees of ginger charcoal were classified into three groups with PCA, and provided scientific basis for establishing the quality standards of ginger charcoal.


Subject(s)
Catechols , Chemistry , Charcoal , Chemistry , Chemistry, Pharmaceutical , Methods , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Chemistry , Fatty Alcohols , Chemistry , Ginger , Chemistry , Principal Component Analysis , Methods
13.
Biomedical and Environmental Sciences ; (12): 808-819, 2015.
Article in English | WPRIM | ID: wpr-258874

ABSTRACT

Recently, a wide range of food-derived phytochemical compounds and their synthetic derivatives have been proposed for cancer treatment. Unfortunately, data available in related literature focus on the anti-cancer properties of compounds derived from edible plants, while very little is known about those derived from non-edible plants. And thus, the underlying mechanisms of their anti-cancer effects are yet to be elucidated. This review collates the available data on the anti-cancer activities of six phytochemical-derived compounds from edible and non-edible plants, i.e. rottlerin, berbamine, sparstolonin B, sulforaphane, plumbagin and 6-shogaol. These compounds are used as bioactive markers for cytotoxicity against tumors. As such, understanding their mode of action will provide the rationale for the combination strategies of these compounds with other drugs in the battle against cancer.


Subject(s)
Humans , Acetophenones , Pharmacology , Therapeutic Uses , Antineoplastic Agents, Phytogenic , Pharmacology , Therapeutic Uses , Benzopyrans , Pharmacology , Therapeutic Uses , Benzylisoquinolines , Pharmacology , Therapeutic Uses , Catechols , Pharmacology , Therapeutic Uses , Heterocyclic Compounds, 4 or More Rings , Pharmacology , Therapeutic Uses , Isothiocyanates , Pharmacology , Therapeutic Uses , Naphthoquinones , Pharmacology , Therapeutic Uses , Neoplasms , Drug Therapy , Phytotherapy , Plant Extracts , Pharmacology , Therapeutic Uses , Signal Transduction
14.
China Journal of Chinese Materia Medica ; (24): 1630-1634, 2014.
Article in Chinese | WPRIM | ID: wpr-300216

ABSTRACT

Phytochemical investigation on the EtOH extract from the aerial part of Callicarpa kwangtungensis led to the isolation and characterization of 10 caffeoyl phenylethanoid glycosides, 2'-acetylacteoside (1), tubuloside E (2), acteoside (3), tubuloside B (4), isoacteoside (5), alyssonoside (6), 2'-acetylforsythoside B (7), brandioside (8), forsythoside B (9), and poliumoside (10). Compound 4 was isolated from the plants of Verbenaceae,and 6 was obtained from the Callicarpa genus, for the first time, while compounds 1, 2, 5 and 7 were firstly reported from the plant.


Subject(s)
Caffeic Acids , Chemistry , Catechols , Chemistry , Chromatography, High Pressure Liquid , Ethanol , Chemistry , Glucosides , Chemistry , Glycosides , Chemistry , Phenols , Chemistry , Verbenaceae , Chemistry
15.
China Journal of Chinese Materia Medica ; (24): 1704-1708, 2014.
Article in Chinese | WPRIM | ID: wpr-300202

ABSTRACT

To develop a LC-MS/MS method for the determination of protocatechuic acid, protocatechuic aldehyde, salvianolic acid A, salvianolic acid B, cryptotanshinone and tanshinone II(A) in rat plasma and brain. The plasma and brain samples were precipitated with ethyl acetate, then were separated on an Agilent eclipse plus-C18 column (2.1 mm x 50 mm, 3.5 microm) using acetonitrile (consisting of 0.1% formic acid) and water (consisting of 0.1% formic acid) as mobile phase in gradient elution mode. The mass spectrometer was operated under both positive and negative ion mode with the ESI source, and the detection was performed by MRM. The transition of 154.3/153.1 m/z for protocatechuic acid, 137.3/108 m/z for protocatechuic aldehyde, 493.0/295.2 m/z for Salvianolic acid A, 718.0/520.0 m/z for salvianolic acid B, 321.4/152.3 m/z for chloramphenicol, 297.4/254.3 m/z for cryptotanshinone, 295.5/249.3 m/z for tanshinone II(A) and 285.2/154.0 m/z for Diazepam. The calibration curves in the range of 0.625-1 000 microg x L(-1) for protocatechuic acid and protocatechuic aldehyde, 1.25-1 000 microg x L(-1) for salvianolic acid A, 2.5-1 000 microg x L(-1) for salvianolic acid B, 0.15-1 000 microg x L(-1) for cryptotanshinone, 0.625-1 000 microg x L(-1) for tanshinone II(A) are with good linearityin rat plasma and brain. The analysis method is sensitive, simple, and suitable enough to be applied in the pharmacokinetic study of the 6 main components. Animal testing gives the lgBB of the drugs and further studies of the 6 components cross the blood-brain barrier can be carried out.


Subject(s)
Animals , Rats , Benzaldehydes , Blood , Pharmacokinetics , Benzofurans , Blood , Pharmacokinetics , Blood-Brain Barrier , Metabolism , Brain , Metabolism , Caffeic Acids , Blood , Pharmacokinetics , Catechols , Blood , Pharmacokinetics , Chromatography, Liquid , Methods , Abietanes , Blood , Pharmacokinetics , Hydroxybenzoates , Blood , Pharmacokinetics , Injections, Intravenous , Lactates , Blood , Pharmacokinetics , Phenanthrenes , Blood , Pharmacokinetics , Plant Preparations , Blood , Pharmacokinetics , Reproducibility of Results , Salvia miltiorrhiza , Chemistry , Tandem Mass Spectrometry , Methods
16.
Braz. j. med. biol. res ; 46(9): 780-788, 19/set. 2013. graf
Article in English | LILACS | ID: lil-686573

ABSTRACT

4-Nerolidylcatechol (4-NC) is found in Pothomorphe umbellata root extracts and is reported to have a topical protective effect against UVB radiation-induced skin damage, toxicity in melanoma cell lines, and antimalarial activity. We report a comparative study of the antioxidant activity of 4-NC and α-tocopherol against lipid peroxidation initiated by two free radical-generating systems: 2,2′-azobis(2-aminopropane) hydrochloride (AAPH) and FeSO4/H2O2, in red blood cell ghost membranes and in egg phosphatidylcholine (PC) vesicles. Lipid peroxidation was monitored by membrane fluidity changes assessed by electron paramagnetic resonance spectroscopy of a spin-labeled lipid and by the formation of thiobarbituric acid-reactive substances. When lipoperoxidation was initiated by the hydroxyl radical in erythrocyte ghost membranes, both 4-NC and α-tocopherol acted in a very efficient manner. However, lower activities were observed when lipoperoxidation was initiated by the peroxyl radical; and, in this case, the protective effect of α-tocopherol was lower than that of 4-NC. In egg PC vesicles, malondialdehyde formation indicated that 4-NC was effective against lipoperoxidation initiated by both AAPH and FeSO4/H2O2, whereas α-tocopherol was less efficient in protecting against lipoperoxidation by AAPH, and behaved as a pro-oxidant for FeSO4/H2O2. The DPPH (2,2-diphenyl-1-picrylhydrazyl) free-radical assay indicated that two free radicals were scavenged per 4-NC molecule, and one free radical was scavenged per α-tocopherol molecule. These data provide new insights into the antioxidant capacity of 4-NC, which may have therapeutic applications for formulations designed to protect the skin from sunlight irradiation.


Subject(s)
Humans , Antioxidants/pharmacology , Catechols/pharmacology , Erythrocyte Membrane/drug effects , Peroxides/analysis , Phospholipids/pharmacology , alpha-Tocopherol/pharmacology , Amidines/administration & dosage , Amidines/pharmacology , Electron Spin Resonance Spectroscopy , Free Radicals/analysis , Lipid Peroxidation/drug effects , Malondialdehyde/analysis , Phosphatidylcholines/pharmacology , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Roots/chemistry
17.
China Journal of Chinese Materia Medica ; (24): 371-375, 2013.
Article in Chinese | WPRIM | ID: wpr-346814

ABSTRACT

<p><b>OBJECTIVE</b>1H-NMR technology was carried out to investigate the chemical difference between 30 batches of Cibotium baronetz decoction pieces and look for new method for quality control of C. baronetz decoction pieces.</p><p><b>METHOD</b>Six hundreds MHz H-NMR spectroscopy and principle component analysis (PCA) were used to discriminate between 30 batches of commercially available cibotium samples based on multi-component metabolite profiles.</p><p><b>RESULT</b>Saccharide is the principle component of C. baronetz decoction pieces, and steroid and triterpene were the discriminately chemical component. Protocatechuic acid, protocatechuic aldehyde, cibotiumbaroside A, cibotiumbaroside B and 4-O-caffeoyl-D-glucoside could be used as the marker for controlling the quality of commercial C. baronetz decoction pieces.</p><p><b>CONCLUSION</b>Pattern-recognition techniques applied to proton nuclear magnetic resonance (1H-NMR) spectra of 80% methanol extraction of C. baronetz could correctly discriminate not only the quality, but also the chemical component for batches of commercial C. baronetz decoction pieces.</p>


Subject(s)
Benzaldehydes , Chemistry , Caffeic Acids , Chemistry , Catechols , Chemistry , Drugs, Chinese Herbal , Chemistry , Reference Standards , Ferns , Chemistry , Furans , Chemistry , Glucose , Chemistry , Glucosides , Chemistry , Glycosides , Chemistry , Hydroxybenzoates , Chemistry , Magnetic Resonance Spectroscopy , Methods , Maltose , Chemistry , Quality Control , Steroids , Chemistry , Sucrose , Chemistry , Triterpenes , Chemistry
18.
China Journal of Chinese Materia Medica ; (24): 208-211, 2013.
Article in Chinese | WPRIM | ID: wpr-318691

ABSTRACT

To explore the effects of protocatechuic acid (PCA) and its derivants on angiogenesis of the chick embryo chorioallantoic membrane (CAM) and scavenging DPPH radical in vitro. The protection of benzyl and alkaline hydrolysis of benzyl ester were employed. The structures of PCA-1, PCA-2 and PCA-3, the derivates of PCA, were elucidated by 1H, 13C-NMR and MS data The bioactivity of PCA and its derivants was evaluated on the models of DPPH radical and chick embryo chorioallantoic membrane (CAM), respectively. PCA and PCA-1 showed the best activity of scavenging DPPH radical among all the compounds. In contrast to PCA-2, PCA and PCA-3 displayed inhibition to angiogenesis (P < 0.001). Pyrocatechol hydroxyl is the active site of PCA on scavenging DPPH radical in vitro. PCA with carboxyl and without pyrocatechol hydroxyl seems to show promotion to angiogenesis, but it needs more evidences.


Subject(s)
Animals , Chick Embryo , Angiogenesis Inducing Agents , Chemistry , Biphenyl Compounds , Catechols , Chemistry , Chorioallantoic Membrane , Drugs, Chinese Herbal , Chemistry , Free Radical Scavengers , Chemistry , Hydroxybenzoates , Chemistry , Magnetic Resonance Spectroscopy , Molecular Structure , Picrates
19.
Sudan Journal of Medical Sciences. 2013; 8 (4): 175-179
in English | IMEMR | ID: emr-178093

ABSTRACT

Vanilloid receptors 1 [VR 1], a group of transient receptor potential channels family was cloned in 1997. They were found to be a potential target for treatment of different acute and chronic pain disorder. Recently these receptors were reported to be involved in several pathological conditions. The present study aimed to investigate the potential anticonvulsant activity of five vanilloidal agonists [capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol]. Experimental animal model of pentylenetetrazole [PTZ] induced seizure was used to investigate the potential anticonvulsant activity of capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol. The data obtained showed that, all tested compounds [capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol] possess dose dependant anticonvulsant activity. The five vanilloidal agonists; capsaicin, nonivamide, zingerone, dehydrozingerone and 6-gingerol exhibit anticonvulsant activity and may find clinical application


Subject(s)
Animals, Laboratory , TRPV Cation Channels/agonists , Capsaicin , Guaiacol/analogs & derivatives , Styrenes , Catechols , Fatty Alcohols , Pentylenetetrazole , Rats
20.
Korean Journal of Dermatology ; : 179-184, 2013.
Article in Korean | WPRIM | ID: wpr-208908

ABSTRACT

BACKGROUND: Urushiol is a widely known potent allergen that causes severe contact dermatitis through the epidermis or blood vessels. The role of antigen presenting cells (APC) in allergic contact dermatitis (ACD) is well known, but the role of APC in systemic contact dermatitis (SCD) is not yet fully evaluated. OBJECTIVE: The aim of this study is to observe the changes of APC in thenormal and SCD skin and to discuss their possible roles in the disease process. METHODS: Immunohistochemical differences of the Langerhans cells (LC) and dermal dendritic cells (DDC) were investigated in cases of the normal and SCD skin (Ed note: keep uniformity as above). Immunohistochemical staining with anti-CD1a, S-100 protein, HLA-DR, and factor XIIIa antibodies were performed. The number of CD1a, S-100 protein, and HLA-DR positive cells per mm2 of the epidermis was counted. The number of HLA-DR and Factor XIIIa-positive DDC per mm2 was also evaluated. RESULTS: The LC positive for CD1a and S-100 in the epidermis were slightly higher in SCD, but their difference was not statistically significant. HLA-DR and Factor XIIIa-positive DDC in the dermis weresignificantly increased in the skin of SCD than normal. HLA-DR positive LC in the epidermis was also increased. CONCLUSION: Our results suggest that DDC plays a more important role than that of epidermal LC in urushiol-induced SCD. Increased HLA-DR-positive LC in the epidermis suggests that antigen delivery through the blood also affects the epidermal Langerhans cell beside the dermal dendritic cells.


Subject(s)
Antibodies , Antigen-Presenting Cells , Blood Vessels , Catechols , Dermatitis, Allergic Contact , Dermatitis, Contact , Dermis , Epidermis , Factor XIIIa , HLA-DR Antigens , Lacquer , Langerhans Cells , Rhus , S100 Proteins , Skin
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