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Thirty-one phenolic constituents were isolated and purified from the 95% ethanol extract of Sanguisorbae Radix by using various chromatographic techniques, including macroporous resin, silica gel, ODS, Sephadex LH-20 and semi-preparative HPLC. Their structures were elucidated by physicochemical properties, spectroscopic data (MS and NMR) and electronic circular dichroism (ECD) spectra, and identified as 3-methoxyl-2S,3S-epoxyflavanone (1a), 3-methoxyl-2R,3R-epoxyflavanone (1b), longifoin B (2), longifoin C (3), eriodictyol (4), naringenin (5), liquiritigenin (6), 5,3ʹ-dihydroxy-7,4ʹ-dimethoxyflavanone (7), naringenin-7-O-β-D-glucopyranoside (8), dihydroquercetin (9), dihydrokaempferol (10), (-)-garbanzol (11), (2R,3R)-4-methoxyl-distylin (12), kaempferol (13), quercetin (14), α,4,2′,4′-tetrahydroxydihydrochalcone (15), phloretin (16), (+)-catechin (17), ethyl (+)-cyanidan-3-ol-8-carboxylate (18), phyllocoumarin (19), methyl 3-methoxy-4,5-dihydroxybenzoate (20), 4,5-dimethoxy-3-hydroxybenzoic acid methyl ester (21), 3,4′-di-O-methylellagic acid (22), 3,4,3′-O-trimethylellagic acid (23), 3,3ʹ,4ʹ-O-trimethylellagic acid-4-O-β-D-xyloside (24), (3R)-thunberginol C (25), resveratrol (26), 1-hydroxypinoresinol (27), (7S,8S)-3-methoxy-3′,7-epoxy-8,4′-oxyneoligna-4,9,9′-triol (28), emodin-8-O-β-D-glucoside (29), phloracetophenone (30) and 4-(4′-hydroxyphenyl)-butan-2-one (31). Among them, compound 1a and 1b is a pair of new flavonoid enantiomers, compounds 2 and 3 are a pair of new epimers, while compounds 4, 5, 6, 9, 10, 13, 16 and 26 were obtained from S. officinalis for the first time, compounds 7, 8, 27, 30 and 31 were isolated for the first time from the S. officinalis genus, and compounds 11, 12, 15, 18, 19, 25, 28 and 29 were isolated for the first time from the Rosaceae. The antioxidant activities of compounds 1-24 were evaluated by activating the Nrf2 transcriptional pathway, which were measured by the dual-luciferase reporter gene assay in 293T cells. Compounds 4, 6-10, 12, 14, 17, 19, 20 and 22-24 showed significant Nrf2 agonistic effect compared with the control group at 25 μmol·L-1, which provided reference for the research of their antioxidant activity.
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Ubiquitination, a diverse post-translational modification, is carried out by enzymes including E1-activating enzymes, E2-conjugating enzymes, E3 ligases, and deubiquitinating enzymes (DUBs). Ubiquitin itself possesses 7 lysine residues and N-terminal methionine, allowing for the formation of polyubiquitin chains with different lengths and linkages. These chains exhibit various topologies that can be recognized by proteins containing ubiquitin-binding domain, thereby transmitting distinct cellular signals. To unravel the physiological mechanisms associated with ubiquitin, numerous ubiquitin probes have been developed. This review provides an overview of recent advancements in the field of ubiquitin probes, focusing on activity-based and affinity-based probes. Activity-based probes are designed to covalently bind to DUBs, E1s, or E3s, enabling the identification and characterization of these enzymes. Affinity-based probes, on the other hand, selectively bind to ubiquitin-binding domains, facilitating the identification of proteins that interact with ubiquitin. Moreover, this review comprehensively discusses the synthetic methodologies employed for the acquisition of ubiquitin probes. These includes meticulous discussions on the synthesis of individual monomeric modules, the establishment of isopeptide linkages, as well as the incorporation of reactive functional groups. Additionally, the review explores the emerging area of cell-penetrating ubiquitin probes and highlights their latest applications in living cells. These probes incorporate cell-penetrating peptides to enable their internalization into cells, allowing for direct visualization and manipulation of ubiquitin-modified proteins within their native environment. Overall, this review offers insights into the design, synthesis, and applications of ubiquitin probes, highlighting their significance in elucidating ubiquitin-mediated cellular processes.
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The study aims to investigate the anti-hepatic fibrosis and anti-inflammatory activities of palbinone, and to explore the internal regulatory mechanism, so as to lay an active foundation for its development as an anti-non-alcoholic steatohepatitis (NASH) candidate. First, sulforhodamine B (SRB) method was used to detect the effect of palbinone on the proliferation of human hepatic stellate cells LX-2 and rat hepatic stellate cells HSC-T6. Following, in the in vitro hepatic fibrosis cell model that activated by transforming growth factor beta 1 (TGF-β1), quantitative real-time PCR (qRT-PCR) and Western blot were used to detect the inhibitory effect of different concentrations of palbinone on the transcription level and protein expression level of hepatic fibrosis markers. And the regulating mechanism of palbinone on fibrosis-related genes was analyzed at the same time. In addition, in the inflammatory cell model that induced by lipopolysaccharide (LPS) and nigericin, ELISA was used to detect the effect of palbinone on the released interleukin-1β (IL-1β) level. At the same time, Western blot was used to detect the effect of palbinone on the related proteins of inflammatory pathway. The results showed that palbinone could significantly inhibit the proliferation activity of LX-2 and HSC-T6, and their half maximal inhibitory concentration (IC50) values were (375.11 ± 55.45) and (260.27 ± 36.81) nmol·L-1, respectively. In addition, palbinone showed a dose-dependent inhibitory effect on the expression levels of TGF-β1-induced fibrosis-related genes, including collagen type Ⅰ α 1 (COL1A1), TGF-β1, α-smooth muscle actin (α-SMA) and tissue inhibitor of metalloproteinase 1 (TIMP1). Mechanism study showed that palbinone may decrease the expression level of Yes-associated protein (YAP), thereby weakening its activation effect on the downstream fibrosis pathway. In addition, palbinone also exerted an anti-inflammatory effect by inhibiting the activity of nuclear factor kappa-B (NF-κB) signaling pathway and reducing inflammatory factors cysteinyl aspartate specific proteinase-1 (caspase-1) and IL-1β release. In conclusion, palbinone can not only inhibit the proliferation and activation of hepatic stellate cells by inhibiting the expression of YAP, but also inhibit the expression and release of inflammatory factors at the same time. All these studies provide theoretical support for the development of palbinone as an anti-nonalcoholic steatohepatitis drug.
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A new siderophore chelate (1) and 8 known compounds were identified from the liquid co-cultures of the marine-derived Streptomyces sp. IMB18-531 and Cladosporium sp. IMB19-099 by a combination of chromatography methods, including C18 reversed-phase medium pressure chromatography, gel column chromatography and HPLC. Their structures were determined by spectroscopic analysis and chemical methods as aluminioxamine E (1), desferrioxamine E (2), ferrioxamine E (3), terragine E (4), capsimicin (5), cyclo(L-prolinyl-L-tyrosine) (6), anthranilic acid (7), (Z)-14-methylpentadec-9-enoic acid (8), and (Z)-hexadec-8-enoic acid (9). Compound 2 showed inhibitory activities against the expression of liver fibrosis related genes COL1A1, MMP2, and TIMP2. Compounds 5, 8, and 9 displayed antibacterial activities against methicillin-resistant Staphylococcus aureus, S. epidermidis and Bacillus subtilis, with MICs of 16-64 μg·mL-1. Compound 5 showed cytotoxicities against human pancreatic cancer MIA Paca-2 and human colon cancer HT-29 cell lines with IC50 of 2.9 and 6.3 μmol·L-1, respectively.
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Objective To investigate the effect of calcification on the ultrasound-guided radiofrequency ablation(RFA)of papillary thyroid carcinoma(PTC).Methods We retrospectively analyzed the preoperative and follow-up data of 164 patients(182 nodules)with PTC treated by percutaneous ultrasound-guided RFA in the First Medical Center of Chinese PLA General Hospital from January 1,2018 to December 31,2021.The tumor status 12 months after RFA was taken as the endpoint event.The univariate Logistic regression analysis was employed to predict the influencing factors of incomplete ablation.The factors were then included in the multivariate Logistic regression analysis for prediction of the independent risk factors of incomplete ablation.Results The maximum nodule diameter(OR=1.16,95%CI=1.04-1.29,P=0.009)and calcification ratio >2/3(OR=19.27,95%CI=4.02-92.28,P<0.001)were the factors influencing the disappearance of lesion 12 months after RFA.Conclusions PTC with calcification can be treated with ultrasound-guided RFA.In the case of calcification ratio ≤ 2/3,this therapy demonstrates the effect equivalent to that of no calcification.
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Humanos , Cáncer Papilar Tiroideo/cirugía , Estudios Retrospectivos , Recurrencia Local de Neoplasia , Ablación por Radiofrecuencia/métodos , Calcinosis , Neoplasias de la Tiroides/patología , Ultrasonografía IntervencionalRESUMEN
The differences in dryness between raw Aurantii Fructus Immaturus(AFI) and bran-fried products were investigated based on a slow-transit constipation(STC) model. Seventy healthy SPF-grade rats were randomly divided into a blank group(K), a positive drug group(Y), a model group(M), low-and high-dose raw AFI groups(SD and SG), and low-and high-dose bran-fried AFI groups(FD and FG). During the experiment, it was found that compared with the K group, the groups with drug treatment had little effect on the daily body weight of the STC rats. The first defecation time of black stool in the M group was significantly higher than that in the K group, and the 24-hour fecal output significantly decreased starting from the 13th day, indicating successful modeling. The SG group showed a significant increase in the first defecation time, fecal water content, urine output, and water intake than other groups with drug treatment. The FG group had the highest fecal output than other groups with drug treatment. The FD group had the highest salivary secretion than other groups with drug treatment. The levels of cAMP/cGMP, VIP, 5-HT, AQP1, and AQP5 were measured in each group with drug treatment, and the expression of c-Kit and SCF mRNA in gastric antrum tissue and AQP3 mRNA in the kidney and colon were detected by RT-PCR. The results showed that the SD and SG groups had a more significant impact on AQP1, AQP5, and other water channel indexes in STC rats than the FD and FG groups. The FD and FG groups had a more significant impact on c-Kit, SCF, VIP, 5-HT, and other gastrointestinal motility indicators than the SD and SG groups. This study, through in vitro biological observations, immunological detection, and gene expression analysis, found that raw AFI had strong dryness property, while bran-fried AFI could alleviate its dryness property.
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Ratas , Animales , Serotonina , Estreñimiento/tratamiento farmacológico , Medicamentos Herbarios Chinos , ARN MensajeroRESUMEN
Objective:Phthalates (PAEs) are common environmental endocrine disruptors. In this study, the effects of oxidative stress on liver and nutrient metabolism were determined in male diabetic rats exposed to di-2-ethylhexyl phthalate (DEHP), and the mechanism of DEHP toxicity was explored. Methods:Thirty-two SPF male Wistar rats aged five weeks, weighing 150-170 g, were fed adaptively for one week to establish the model of type 2 diabetes. The model was established by intraperitoneal injection of streptozotocin (STZ) (25 mg/kg) after feeding with high sugar and high fat diet for four weeks. Second STZ injection was given two days later. The model was considered to be established successfully when the random blood glucose level was found to be higher than 16.7 mmol/L in two separate tests. Twenty diabetic rats were then randomly divided into four groups, including control group (corn oil), 100, 300 and 900 mg/kg DEHP groups. The rats were treated with DEHP by gavage (5 mL/kg) once a day for 30 days. They were fed with normal diet during the treatment period. Caudal venous blood was collected on the 1st, 14th, and 28th days to measure the random blood glucose level. The changes of glucose tolerance were determined by oral glucose tolerance test on the 29th day. Fasting blood glucose (FPG) was measured on the next day of the last exposure. After the rats were anesthetized with pentobarbital and killed, the liver was weighed, the liver coefficient was calculated and the liver pathological section was made. Blood was taken from the abdominal aorta. The levels of aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), triacylglycerol (TG) and albumin (ALB) in serum were measured by spectrophotometry, and the levels of insulin, glutathione (GSH), H2O2, malondialdehyde (MDA) and superoxide dismutase (SOD) in fasting serum were measured by radioimmunoassay. Results:There was no significant difference in body weight and random blood glucose in the type 2 diabetic rats exposed to different concentrations of DEHP (all P>0.05). At each time point of the glucose tolerance curve, the blood glucose value of the exposure groups was higher than that of the control group. A "false plateau period" appeared after the blood glucose value reached or exceeded the upper limit at 15 minutes, and the blood glucose level in each group was higher than that of the control group at 120 minutes. The liver organ coefficient of 300 and 900 mg/kg DEHP groups was higher than that of the control group (both P<0.01), and the liver organ coefficient was positively correlated with the exposure concentration of DEHP (r=0.80,P<0.000 1). Under the microscope, the liver cells in diabetic rats were swollen, the cytoplasm was light stained, and there were vacuoles in the cells. The serum ALP level in diabetic rats of 900 mg/kg DEHP group was significantly higher than that in the control group (P<0.01). The serum ALP level was positively correlated with the concentration of DEHP (r=0.75, P<0.01). The serum MDA level in diabetic rats of 300 mg/kg and 900 mg/kg DEHP groups was significantly higher than that of the control group (both P<0.01), and the serum MDA level was positively correlated with the concentration of DEHP (r=0.84, P<0.000 1). The serum SOD level of 900 mg/kg DEHP group was significantly higher than that of control group (P<0.01). Conclusion:DEHP exposure could lead to liver damage, abnormal glycolipid metabolism, and increase the level of oxidative stress and antioxidant level in male diabetic rats, but did not show a significant effect on insulin resistance.
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BACKGROUND@#The past decade has witnessed an ever-increasing momentum of transcatheter aortic valve replacement (TAVR) and a subsequent paradigm shift in the contemporary management of severe aortic stenosis (AS). We conducted a multi-centric TAVR registry based on Chinese patients (the China Aortic valve tRanscatheter Replacement registrY [CARRY]) to delineate the clinical characteristics and outcomes of Chinese patients who underwent TAVR and compare the results between different valve types in different Chinese regions.@*METHODS@#CARRY is an all-comer registry of aortic valve disease patients undergoing TAVR across China and was designed as an observational study that retrospectively included all TAVR patients at each participating site. Seven hospitals in China participated in the CARRY, and 1204 patients from April 2012 to November 2020 were included. Categorical variables were compared using the chi-squared test, and continuous variables were analyzed using a t test or analysis of variance (ANOVA) test. The Kaplan-Meier curve was used to estimate the risk of adverse events during follow-up.@*RESULTS@#The mean age of the patients was 73.8 ± 6.5 years and 57.2% were male. The median Society of Thoracic Surgeon-Predicted Risk of Mortality score was 6.0 (3.7-8.9). Regarding the aortic valve, the proportion of bicuspid aortic valve (BAV) was 48.5%. During the hospital stay, the stroke rate was 0.7%, and the incidence of high-degree atrioventricular block indicating permanent pacemaker implantation was 11.0%. The in-hospital all-cause mortality rate was 2.2%. After 1 year, the overall mortality rate was 4.5%. Compared to patients with tricuspid aortic valve (TAV), those with BAV had similar in-hospital complication rates, but a lower incidence of in-hospital mortality (1.4% vs. 3.3%) and 1 year mortality (2.3% vs. 5.8%).@*CONCLUSIONS@#TAVR candidates in China were younger, higher proportion of BAV, and had lower rates of post-procedural complications and mortality than other international all-comer registries. Given the use of early generation valves in the majority of the population, patients with BAV had similar rates of complications, but lower mortality than those with TAV. These findings further propel the extension of TAVR in low-risk patients.@*TRIAL REGISTRATION@#https://www.chictr.org.cn/ (No. ChiCTR2000038526).
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Anciano , Anciano de 80 o más Años , Humanos , Masculino , Válvula Aórtica/cirugía , Estenosis de la Válvula Aórtica/cirugía , Sistema de Registros , Estudios Retrospectivos , Factores de Riesgo , Reemplazo de la Válvula Aórtica Transcatéter/efectos adversos , Resultado del TratamientoRESUMEN
The chemical constituents of the flower buds of Buddleja officinalis were investigated in this study. Eight compounds were isolated from the water extract of B. officinalis by column chromatography, and their structures were elucidated on the basis of physicochemical properties and spectral data. These compounds were identified as(Z)-hex-3-en-1-ol-1-O-β-D-glucopyranosyl-(1→2)-[β-D-xylcopyranosyl-(1→6)]-β-D-glucopyranoside(1), ebracteatoside B(2), jasmonic acid-11-O-β-D-glucopyranoside(3), 6-hydroxyluteolin-7-O-β-D-glucopyranoside(4), luteolin-7-O-galacturonide(5), vicenin-2(6), decaffeoylverbascoside(7), and 6-O-(E)-feruloyl-D-glucopyranoside(8). Compound 1 is a new 3-hexenol glycoside. Compounds 2, 3, and 6 were isolated from Buddleja genus for the first time, and compounds 4 and 5 were isolated from this plant for the first time.
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Buddleja , Glicósidos Cardíacos , Glicósidos , Extractos VegetalesRESUMEN
This paper analyzes the problems existing in the current theory of divergent meridian (""), such as the unclear route of divergent meridian, the controversy in the "---" and the lack of in-depth research on the theory of "", clarifies the source and privides insights. The author analyzed the word "" by means of the four proofreading methods combined with philology method to explore the origin of " ". The divergent meridians is the remnant of the original meridians system in the bamboo and silk documents, which was put into the meridians system after being sorted out by doctors. The twelve meridians are combined in two, forming the "" point, which is located in the neck, and has a great influence on the blood circulation of the head and neck. "" point and theory can guide the differentiation of acupuncture and moxibustion, and has an important guiding significance for the treatment of empirical, emergency and head and face diseases.
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The chemical constituents of Cinnamomi Ramulus were investigated in this study. Twenty-two compounds were isolated by silica gel, Sephadex LH-20 gel column chromatographies and preparative HPLC and their structures were identified by various spectral analyses as dihydrorosavin(1), rosavin(2), 1-phenyl-propane-1,2,3-triol(3), patchoulol(4), graphostromane B(5),(+)-lyoniresinol-3 a-O-β-D-glucopyranoside(6),(-)-lyoniresinol-3 a-O-β-D-glucopyranoside(7), cinnacaside(8), subaveniumin A(9), 3-phenyl-2-propenyl-6-O-L-arabinopyranosyl-β-glucopyranoside(10), 2-phenylethyl-β-vicianoside(11), cinnacasol(12), [(2R,3S,4S,5R,6R)-6-(benzyloxy)-3,4,5-trihydroxytetrahydro-2H-pyran-2-yl] methyl hydrogen sulfate(13), coniferyl aldehyde(14),(2R,3R)-5,7-dimethoxy-3',4'-methylenedioxyflavan-3-ol(15), cinnacassin L(16), E-cinnamic alcohol(17),(E)-3-(2-methoxyphenyl)-2-propen-1-ol(18), 2-hydroxyphenylpropanol(19), cinnamomulactone(20),(+)-syringaresinol(21) and cinnamomumolide(22), respectively. Among them, 1 is a new compound and 3-7, 9-11, 13, 15, 18 and 19 were isolated from the plant for the first time.
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Cromatografía Líquida de Alta Presión , Cinnamomum/química , Medicamentos Herbarios Chinos , Fitoquímicos/análisisRESUMEN
AIM To study the chemical constituents from P.americana L..METHODS The 90% ethanol extract from P.americana was isolated and purified by silica,ODS,Sephadex LH-20,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Sixteen compounds were isolated and identified as L-leucine (1),uracil (2),acetamide (3),valine (4),γ-aminobutyric acid (5),glycerol (6),methyl,2-piperidinecarboxylate (7),pyrazine (8),protocatechuic acid-4-O-β-D-glucopyranoside (9),thymidine (10),cyclo (Pro-Ser) (11),cyclo (Pro-Asn) (12),phenylalanine (13),4-(2-aminoethyl) benzene-1,2-diol (14),inosine (15),tyramine (16).CONCLUSION Compounds 3,7-12,14,16 are all isolated from Periplaneta americana and genus Periplaneta for the first time.
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Diabetes mellitus, a chronic disease, is characterized by high blood glucose that could induce various complications. Procyanidin, a kind of polyphenol compounds existing in many plants, have shown to be effective in preventing and treating type 2 diabetes mellitus as they may lower blood glucose, moderate insulin resistance and protect islet β cells. This review focused on the research advances on the preventive and therapeutic application of procyanidin in promoting glucose absorption, protecting islet β cells, modulating intestinal microbiota and regulating diabetic complications of type 2 diabetes mellitus, which should provide useful reference for subsequent studies.
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Two new sulfated sesquiterpenoids, megastigman-7-ene-3, 5, 6, 9-tetrol-3-O-β-D-6'-sulfonated-glucopyranoside (1) and 3-O-β-D-6'-sulfonated-glucopyranosyl-6-(3-oxo-2-butenylidenyl)-1, 1, 5-trimethylcyclohexan-5-ol (2), along with one known sesquitepenoid compound icariside B1 (3) were isolated from the whole herb of Petasites tricholobus Franch. Their structures were identified by their chemical and spectroscopic characters. All obtained compounds were tested for their cytotoxicity against four cancer cell lines.
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Humanos , Línea Celular Tumoral , Glicósidos , Farmacología , Norisoprenoides , Farmacología , Petasites , Química , Sesquiterpenos , FarmacologíaRESUMEN
Phytochemical investigation of the roots of Scrophularia buergeriana Miq. (Scrophulariaceae), resulted in the isolation of a new iridoid derivative named as buergerinin (1). Its structure was elucidated as rel-(1R, 5R, 6R)-(2-oxa-bicyclo[3.3.0]oct-7-en-6, 7-diyl)dimethoxypropane based mainly on MS and 1D and 2D NMR spectroscopic analyses.
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Iridoides , Química , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Raíces de Plantas , Química , Scrophularia , QuímicaRESUMEN
One new neolignan identified as 2, 3-( trans) -dihydro-2-(4-hydroxy-3-methoxyphenyl) -3-[(beta-D-glucopyranosyloxy) methyl]-7-methoxybenzofuran-5-propenoic acid (1) and five known steroidal glycosides namely torvoside A(2), torvoside C(3), torvoside H(4), solanolactoside A (5), (25S)-6alpha-hydroxy-5alpha-spirostan-3-one-6-0-[alpha-L-rhamnopyranosyl-(1-->3-beta3)-beta-D-D-quinovopyr-anoside] (6) were isolated from the fruits of Solanum torvum. Their structures were elucidated on the basis of 1D, 2D NMR and MS spectroscopic analysis.
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Frutas , Química , Isomerismo , Lignanos , Química , Solanum , QuímicaRESUMEN
To control the quality of Humulus scandens, the quality standard was established in this study. According to the method recorded in the Appendix of Chinese Pharmacopoeia (2010 Edition) , the water and ash inspections were carried out. The component luteoloside and cosmosiin in Humulus scandens were identified and assayed by TLC and HPLC. The results showed a strong characteristics microscopic of Humulus scandens, and trichoromethane-methanol-formic acid (10: 3: 0. 3) as the mobile phase of TLC, the spots at 365 nm with a UV lamp was clear. The 16 batches of samples were analyzed by HPLC with a gradient elution of acetonitrile and phosphate solution (0.2%) at a flow rate of 1.0 mL · min(-1) and detected at 350 nm. The content of luteoloside was 0.015%- 0.651% (average 0.148%); the content of cosmosiin was 0.003%-0.118% (average 0.036%). The linear calibration curve of luteoloside and cosmosiin was acquired in the ranges of 0.011-0.364 g · L(-1) (r = 1.000 0) and 0.003-0.096 g · L(-1) (r = 1.000 0), respectively. The average recovery was 100.5% and 98.5%, respectively. The methods are convenient and reliable, which can be ap- plied for quality assessment of Humulus scandens.
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China , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos , Estándares de Referencia , Humulus , Química , Control de CalidadRESUMEN
To study the chemical constituents of Lysimachia patungensis Hand.-Mazz., silica gel column chromatography, reverse phase ODS column chromatography, MCI and Sephadex LH-20, were used to separate the 95% EtOH extract of the whole plant of Lysimachia patungensis Hand.-Mazz.. The structures of the isolated compounds have been established on the basis of chemical and NMR spectroscopic evidence as well as ESI-MS in some cases. Twelve phenolic compounds were obtained and identified as quercetin-3, 3'-di- O-alpha-L-rhamnoside (1), myricetrin (2), quercitrin (3), rutin (4), 2-hydroxynaringenin-4'-O-glucopyranoside (5), naringenin 7-O-glucopyranoside (6), liquiritin apioside (7), licochalcone B (8), tetrahydroxymethoxy chalcone (9), methyl-p-coumarate (10), 2, 4, 6-trihydroxy acetophenone-2-O-glucopyranoside (11) and vaccihein A (12). Among them, compound 1 is a new compound, and compounds 5, 11 and 12 are isolated from the genus Lysimachia L. for the first time, and the others are isolated from the plant for the first time.
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Chalconas , Química , Cinamatos , Química , Estructura Molecular , Fenoles , Química , Plantas Medicinales , Química , Primulaceae , Química , Quercetina , Química , Rutina , QuímicaRESUMEN
<p><b>OBJECTIVES</b>To prove the protective effect of Edaravone to neurons and to study the particular mechanism.</p><p><b>METHODS</b>Neurons were collected from 18-day fetal rat brains and a culture of almost pure neurons was obtained after 14-day culture, then the cells were randomly assigned to one of the three groups: control group, hydrogen peroxide (H₂O₂)-treated group, and Edaravone-treated group. In H₂O₂-treated group, 300 µmol/L H₂O₂ was added to the medium, followed by returning to the normal culture for the presupposition of time. In Edaravone-treated group, 500 µmol/L Edaravone was prophylactically added to the medium for 30 minutes before the insult. Morphology of mitochondria was visualized by transmission electron microscopy. The rate of apoptotic cells was detected by flow cytometry analysis. The relationships between the proteins and the key proteins expressions were observed by immunoprecipitation and immunoblotting.</p><p><b>RESULTS</b>Compared to the Edaravone-treated group, mitochondria in H₂O₂-treated group displayed more vesicular matrix compartments at the same time. Percentage of apoptotic cells in H₂O₂-treated group after 0.5, 2, 6 and 12 h were 14.40% ± 1.23%, 45.50% ± 2.81%, 56.40% ± 3.53%, 62.50% ± 4.23%, which were higher than control group (F = 274.8, P < 0.01). Edaravone-treated group were 0.90% ± 0.07%, 1.10% ± 0.08%, 3.50% ± 1.90%, 12.60% ± 1.10%, which were lower than H₂O₂-treated group (F = 362.7, P < 0.01). After H₂O₂ stimulation for 0.5 h in H₂O₂-treated group, the levels of p-JNK (Thr183/Tyr185) and cytochrome c in cytosol and BAX in heavy membrane were increased significantly at 0.5 h, reaching a peak at 12 h after stimulation, In addition, the expressions of p-BAD, BAX, BAD and 14-3-3 of cytoplasm decreased, however, these changes were inhibited in the Edaravone-treated group.</p><p><b>CONCLUSIONS</b>As a free radical scavenger, the Edaravone could protect neurons by inhibiting the activity of JNK, the disassociation of BAD from 14-3-3 and the translocation of BAX from the cytosol to mitochondria.</p>
Asunto(s)
Animales , Ratas , Proteínas 14-3-3 , Metabolismo , Antipirina , Farmacología , Apoptosis , Células Cultivadas , Depuradores de Radicales Libres , Farmacología , Peróxido de Hidrógeno , Metabolismo , Sistema de Señalización de MAP Quinasas , Mitocondrias , Neuronas , Fármacos Neuroprotectores , Farmacología , Cultivo Primario de Células , Ratas Sprague-Dawley , Proteína X Asociada a bcl-2 , Metabolismo , Proteína Letal Asociada a bcl , MetabolismoRESUMEN
<p><b>OBJECTIVES</b>To evaluate the value of the metastatic to examined lymph nodes (rN) ratio in gastric cancer patients who underwent radical resection.</p><p><b>METHODS</b>In this retrospective study, data were collected from the medical records of 710 patients who underwent radical gastrectomy (R0) for gastric cancer from 1980 to 2006 in the Department of Surgical Oncology at the First Affiliated Hospital of China Medical University. The patients were divided into 2 groups according to the number of examined lymph nodes: Group 1 consisted of 327 patients with <15 examined lymph nodes and Group 2 consisted of 383 patients with ≥15 lymph nodes. rN categories staging and pN categories were divided separately according to the metastatic lymph node ratio and the examined lymph nodes. The prognostic factors were analyzed by univariate (Log-rank) and multivariate (Cox model) analysis methods.</p><p><b>RESULTS</b>The median survival time was 74 months (95% CI:55.6-92.4 months) in Group 1 and 96 months (95% CI:77.8-119.2 months) in Group 2, and the difference was not statistically significant (P>0.05). On multivariate analysis, the N ratio remained as an independent prognostic factor in both Group 1 (P<0.01, RR=1.225, 95% CI:1.102-1.362) and Group 2 (P<0.01, RR=1.421, 95% CI:1.269-1.592). However, pN stage was an independent prognostic factor only in Group 1. When the rN ratio classification was applied, there were no significant differences between each categories (P>0.05). However, the overall survival of patients with pN1 disease in Group 1 was significantly shorter than that in Group 2 according to the pN stage classification (P<0.01).</p><p><b>CONCLUSIONS</b>The metastatic lymph node ratio is an independent prognostic factor of the prognosis of gastric cancer. The staging system based on metastatic lymph node ratio (rN) is more reliable than the system based on the number of metastatic lymph nodes in the prediction of the prognosis of gastric cancer.</p>