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1.
Article in Chinese | WPRIM | ID: wpr-879017

ABSTRACT

Chemical constituents of water extracts of Asplenium ruprechtii were investigated. Five 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 aspleniumside G(1), trans-p-coumaric acid(2), trans-p-coumaric acid 4-O-β-D-glucoside(3), cis-p-coumaric acid 4-O-β-D-glucoside(4), and(E)-ferulic acid-4-O-β-D-glucoside(5). Among them, compound 1 is a new 9,19-cycloartane glycoside.


Subject(s)
Chromatography, High Pressure Liquid , Glucosides , Glycosides , Triterpenes
2.
Article in Chinese | WPRIM | ID: wpr-878990

ABSTRACT

Gastrodiae Rhizoma-Uncariae Ramulus cum Uncis is the most frequently used herbal pair in the treatment of Parkinson's disease(PD). Gastrodin and isorhynchophylline are important components of Gastrodiae Rhizoma-Uncariae Ramulus cum Uncis herb pair with anti-Parkinson mechanism. This study aimed to investigate the effect of gastrodin combined with isorhynchophylline on 1-methyl-4-phenylpyridinium(MPP~+)-induced apoptosis of PC12 cells and their antioxidant mechanism. The leakage of lactate dehydrogenase(LDH) from cells to media was analyzed by spectrophotometry. Apoptotic cells were labeled with Annexin V-fluorescein isothiocyanate(FITC) and propidium iodide(PI) and analyzed by flow cytometry. The cell cycle was analyzed using propidium iodide(PI) staining. Lipid peroxidation(LPO) level was analyzed by spectrophotometry. The mRNA expression of caspase-3 was examined by Real-time RT-PCR. The protein expressions of heme oxygenase 1(HO-1) and NADPH: quinoneoxidore-ductase 1(NQO-1) were determined by Western blot. Gastrodin combined with isorhynchophylline reduced the percentage of Annexin V-positive cells and cell cycle arrest in MPP~+-induced PC12 cells. Gastrodin combined with isorhynchophylline down-regulated the mRNA expression of caspase-3, up-regulated the protein expressions of HO-1 and NQO-1, and reduced LPO content in MPP~+-induced PC12 cells. PD98059, LY294002 or LiCl could partially reverse these changes pretreated with gastrodin combined with isorhynchophylline, suggesting that gastrodin combined with isorhynchophylline inhibited MPP~+-induced apoptosis of PC12 cells and oxidative stress through ERK1/2 and PI3 K/GSK-3β signal pathways. Our experiments showed that gastrodin combined with isorhynchophylline could down-re-gulate the mRNA expression of caspase-3 and up-regulate the protein expressions of HO-1 and NQO-1, so as to reduce oxidative stress and inhibit apoptosis.


Subject(s)
1-Methyl-4-phenylpyridinium/toxicity , Animals , Antioxidants , Apoptosis , Benzyl Alcohols , Cell Survival , Glucosides , Glycogen Synthase Kinase 3 beta , Oxindoles , PC12 Cells , Rats
3.
Article in Chinese | WPRIM | ID: wpr-878962

ABSTRACT

This study is to provide the basis of establishing a quality evaluation system, based on the differences in appearance and internal components of Astragali Radix from different sources. The diameter of 18 batches of Astragali Radix, the content of alcohol(water) extract and 7 kinds of flavonoids were determined. The peak area ratio of flavonoid aglycon to aglycone was calculated. PCA and CA were carried out by synthesizing various indexes. The results of PCA and CA showed that Astragali Radix was obviously clustered into three types. Alcohol extract, formononetin/formosan glycosides,(pilose isoflavones+astragalus flavonoid A)/pilose isoflavone glucoside are the most significant differences in the variable importance projection index(VIP) of Astragali Radix. Combining the diameter, alcohol(water) extract, flavonoid aglycon to aglycone peak area ratio can provide an analysis method for the establishment of the grade evaluation system of Astragali Radix.


Subject(s)
Astragalus Plant , Drugs, Chinese Herbal , Glucosides , Glycosides , Plant Roots
4.
Article in Chinese | WPRIM | ID: wpr-878922

ABSTRACT

Polygonum multiflorum is a traditional Chinese herbal medicine and has many biological activities such as hair-blacking, anti-atherosclerosis, anti-inflammatory and anti-aging. However, the liver injury induced by P. multiflorum has aroused wide attention in recent years. 2,3,5,4'-tetrahydroxystibane-2-O-β-D-glucoside(TSG) is a main component of P. multiflorum, but the role of TSG in inducing liver injury is unclear. The aim of present study was to evaluate TSG's potential liver injury and effects on bile acid homeostasis and phospholipids efflux. C57 BL/6 J mice received intraperitoneal administration of 400 mg·kg~(-1) of TSG daily for 15 days, and then biochemical indexes of liver injury and changes of phospholipid content were detected. The changes of bile acid compositions were detected by LC-MS/MS. The results showed TSG 400 mg·kg~(-1) significantly increased the content of serum total bile acid(TBA) and alkaline phosphatase(ALP). Elevated free bile acid levels were observed in TSG-treated groups, including β-muricholic acid(β-MCA), ursodeoxycholic acid(UDCA), hyodeoxycholic acid(HDCA), chenodeoxycholic acid(CDCA), deoxcholic acid(DCA) in serum and β-MCA, CDCA in liver. TSG inhibited the protein expression of farnesoid X receptor(FXR) and down stream bile salt export pump(BSEP), which may result in the accumulation of bile acid. TSG also inhibited the expression of 25-hydroxycholesterol-7 alpha-hydroxylase(CYP7 B1), which may disturb the alternative pathway for bile acid synthesis. In addition, intraperitoneal injection of TSG 400 mg·kg~(-1) significantly decreased the content of phospholipids in bile. The research showed that TSG significantly inhibited the expression of multidrug resistance protein 2(MDR2) and destroyed the regular distribution of MDR2 on the bile duct membrane of liver. In vitro results showed that the IC_(50) of TSG on HepG2 cells was about 1 500 μmol·L~(-1) and TSG at 500 μmol·L~(-1)(for 24 h) could destroy the distribution of MDR2 on the bile duct membrane of liver. In conclusion, TSG induced liver injury by disrupting bile acid homeostasis and phospholipids efflux.


Subject(s)
Animals , Bile Acids and Salts , Chromatography, Liquid , Glucosides , Homeostasis , Liver , Mice , Phospholipids , Tandem Mass Spectrometry
5.
Chinese Journal of Biotechnology ; (12): 580-592, 2021.
Article in Chinese | WPRIM | ID: wpr-878583

ABSTRACT

A novel β-glucosidase BglD2 with glucose and ethanol tolerant properties was screened and cloned from the deep-sea bacterium Bacillus sp. D1. The application potential of BglD2 toward polydatin-hydrolyzing was also evaluated. BglD2 exhibited the maximal β-glucosidase activity at 45 °C and pH 6.5. BglD2 maintained approximately 50% of its origin activity after incubation at 30 °C and pH 6.5 for 20 h. BglD2 could hydrolyze a variety of substrates containing β (1→3), β (1→4), and β (1→6) bonds. The activity of β-glucosidase was enhanced to 2.0 fold and 2.3 fold by 100 mmol/L glucose and 150 mmol/L xylose, respectively. BglD2 possessed ethanol-stimulated and -tolerant properties. At 30 °C, the activity of BglD2 enhanced to 1.2 fold in the presence of 10% ethanol and even remained 60% in 25% ethanol. BglD2 could hydrolyze polydatin to produce resveratrol. At 35 °C, BglD2 hydrolyzed 86% polydatin after incubation for 2 h. Thus, BglD2 possessed glucose and ethanol tolerant properties and can be used as the potential candidate of catalyst for the production of resveratrol from polydatin.


Subject(s)
Enzyme Stability , Glucose , Glucosides/pharmacology , Hydrogen-Ion Concentration , Stilbenes/pharmacology , Substrate Specificity , Temperature , Xylose , beta-Glucosidase/genetics
6.
Chinese Medical Journal ; (24): 1317-1323, 2021.
Article in English | WPRIM | ID: wpr-878102

ABSTRACT

BACKGROUND@#Recent cardiovascular outcome trials (CVOTs) changed the therapeutic strategy of guidelines for type 2 diabetes. We compared the characteristics of patients from real-world hospital settings with those of participants in recent pragmatic randomized trials.@*METHODS@#This electronic medical record (EMR)-based retrospective observational study investigated the data of patients with diabetes from inpatient and outpatient settings in West China Hospital of Sichuan University from January 1, 2011, to June 30, 2019. We identified patients meeting the inclusion criteria of a pragmatic randomized trial (EMPA-REG OUTCOME) based on EMRs and compared their baseline characteristics with those of the trial participants. The cutoff for the clinical significance of each characteristic was set as its minimal clinically important difference based on expert consultation.@*RESULTS@#We included 48,257 inpatients and 36,857 outpatients with diabetes and found that 8389 (17.4%) inpatients and 2646 (7.2%) outpatients met the inclusion criteria for the EMPA-REG OUTCOME trial. Compared with the trial population, the real-world inpatients meeting the eligibility criteria of the EMPA-REG OUTCOME had similar age, blood pressure, and lipid profiles but comprised of fewer males, metformin users, anti-hypertensive drug users, and aspirin users, and had a lower body mass index. The group of outpatients meeting the eligibility criteria had fewer males, similar age, fewer metformin users, fewer insulin users, fewer anti-hypertensive drug users, and fewer aspirin users compared with the trial population.@*CONCLUSIONS@#The trial population in EMPA-REG OUTCOME represents only a small portion of patients with diabetes from the inpatient and outpatient departments of a Chinese tertiary medical center. Evidence localization in different clinical settings and validation are essential to enabling extrapolation of the results from CVOTs in patients with diabetes to Chinese clinical practice.


Subject(s)
Benzhydryl Compounds , Canagliflozin , Cardiovascular Diseases , China , Diabetes Mellitus, Type 2/drug therapy , Glucosides , Humans , Male , Sodium-Glucose Transporter 2 Inhibitors , Tertiary Care Centers
7.
Article in Chinese | WPRIM | ID: wpr-879808

ABSTRACT

OBJECTIVE@#To study the clinical effect and mechanism of total glucosides of paeony (TGP) in the adjuvant therapy for children with Henoch-Schönlein purpura nephritis (HSPN).@*METHODS@#Sixty-four HSPN children with moderate proteinuria were divided into a TGP treatment group (@*RESULTS@#Compared with the healthy children before treatment, the children with HSPN had higher proportion of Tfh cells and expression levels of IL-21 and IL-4 (@*CONCLUSIONS@#TGP has a marked clinical effect in the treatment of HSPN and can reduce the inflammatory response of the kidney and exert a protective effect on the kidney by inhibiting the proliferation of Tfh cells and downregulating the expression of IL-21 and IL-4 in plasma.


Subject(s)
Child , Glucosides/therapeutic use , Humans , Nephritis , Paeonia , Prospective Studies , Purpura, Schoenlein-Henoch/drug therapy
8.
Article in Chinese | WPRIM | ID: wpr-828397

ABSTRACT

Eleven compounds were isolated and purified from Sorghum vulgare root extract, through column chromatography over silica gel, MCI gel, and preparative HPLC. Their structures were established by MS, 1 D NMR and 2 D NMR data as sorgholide A(1), β-sitosterol(2), stigmastero(3), daucosterol(4), 4-methoxycinnamic acid(5), taxiphyllin(6), chlorogenic acid(7), p-hydroxybenzaldehyde(8), succini acid(9), trans-p-hydroxycinnamic acid(10), obtusalin(11). Compounds 4,5 and 9-11 were reported from this species for the first time, and compound 1 is the first 24 ring dimeric double lactonol glycoside formed by reverse polymerization of p-hydroxyphenylacetate glucoside, named sorgholide A.


Subject(s)
Cardiac Glycosides , Glucosides , Glycosides , Phenols , Sorghum
9.
Article in Chinese | WPRIM | ID: wpr-828376

ABSTRACT

The components of traditional Chinese medicine(TCMCs) are the basic unit of raw materials for Chinese medicines, and their physical and chemical properties directly affect the choice of dosage forms and the optimization of prescriptions. However, most of TCMCs are multi-component complex systems, and the characterization of their overall properties is still in the exploration stage. On the basis of biological activity, the representative components are determined, and then the individual characteristics are fitted with the weight coefficient of efficacy contribution rate, which may provide reference for characterizing the overall properties of TCMCs. In this study, with the pharmacological effects of isoproterenol(ISO)-induced myocardial ischemia in rats as the indicators, the pharmacodynamic contribution rates of three representative components of chishao terpene glucoside components(CSTGCs) were evaluated by the normalization weighting method. The contribution rates of paeoniflorin, paeoniflorin and benzoylpaeoniflorin were 54.87%, 32.46% and 12.67%, respectively. The oil-water partition coefficients of paeoniflorin, albiflorin, benzoylpaeoniflorin in water and buffer solutions with different pH values were measured, and the oil-water partition coefficients of CSTGCs were characterized by the weight of their pharmacodynamics contribution rate. The results showed that the apparent oil-water partition coefficient(log P) of CSTGCs in the phosphate buffer system such as n-octanol-water(pH 2.0, 2.5, 5.0, 5.8, 6.8) were 0.18-0.22, indicating that CSTGCs have common absorption and low permeability, providing basis for the preparation of CSTGCs.


Subject(s)
Animals , Coronary Artery Disease , Glucosides , Medicine, Chinese Traditional , Myocardial Ischemia , Rats , Terpenes , Water
10.
Article in Chinese | WPRIM | ID: wpr-828069

ABSTRACT

A new lignan glucoside,(+)-fragransin A_2-4-O-β-D-glucopyranoside(1), has been isolated from the dry root of Paeonia lactiflora by column chromatography on silica gel, Sephadex LH-20, and MCI-gel resin, as well as preparative RP-HPLC. The structure of the new compound was elucidated by spectroscopic data analysis(MS, UV, IR, CD, 1 D and 2 D NMR) and chemical method. Compound 1 showed moderate inhibition against lipopolysaccharide induced nitric oxide production in RAW264.7 macrophages, with an IC_(50) value of 21.3 μmol·L~(-1).


Subject(s)
Chromatography, High Pressure Liquid , Glucosides , Lignans , Paeonia , Plant Extracts
11.
Article in Chinese | WPRIM | ID: wpr-828062

ABSTRACT

In this study, we aimed to establish a rat liver micro-tissue evaluation system to evaluate the hepatotoxicity of the main monomers in Polygonum multiflorum. Rat primary hepatocytes were isolated and purified by two-step in situ perfusion method to prepare hepatic parenchymal cells. The ultra-low adsorption plate and the inverted model were used to establish an in vitro hepatotoxicity evaluation system. After the system was established, the main monomer components(monanthone with emodin type, rhein, emodin, emodin-8-O-β-D-glucopyranoside, physcion) of P. multiflorum were selected for in vitro hepatotoxicity evaluation. This study showed that the primary cells of the liver can form liver micro-tissues in the low adsorption plate method and the mold perfusion method, with good liver structure and function, which can be used to evaluate the hepatotoxicity of the drug to be tested after long-term administration. The five monomers to be tested in P. multiflorum can significantly affect the proliferation of primary liver micro-tissues in rats in a dose-and time-dependent manner. The hepatotoxic effects were as follows: monanthone with emodin type > rhein > emodin > emodin-8-O-β-D-glucopyranoside > physcion. The results suggested that the emodin-type monoterpene and rhein might be the potential hepatotoxic components, while the metabolites of emodin-8-O-β-D-glucoside and emodin methyl ether showed more toxic risks. The rat primary hepatocyte micro-tissue model system established in this experiment could be used to achieve long-term drug administration in vitro, which was consistent with the clinical features of liver injury caused by long-term use of P. multiflorum. The experimental results provided important information and reference on the clinical application and toxic component of P. multiflorum.


Subject(s)
Animals , Chemical and Drug Induced Liver Injury , Emodin , Fallopia multiflora , Glucosides , Plant Extracts , Polygonum , Rats
12.
Article in Chinese | WPRIM | ID: wpr-827933

ABSTRACT

Two new phenylpropanoid amide glycosides and ten analogues were isolated from the CH_2Cl_2 layer of 95% ethanol extract of the whole plants of Corydalis racemosa by using various chromatographic techniques, including silica gel, Sephadex LH-20, ODS column chromatographies, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, MS, NMR, and IR spectroscopic data as N-cis-sinapoyltyramine-4'-O-β-glucoside(1), N-cis-sinapoyl-3-methoxytyramine-4'-O-β-glucoside(2), N-cis-sinapoyltyramine(3), N-cis-feruloyltyramine(4), N-trans-cinnamoyltyramine(5), N-trans-feruloylphenethylamine(6), N-trans-p-methoxycinnamoyl-3-hydoxyoctopamine(7), N-cis-feruloyl-3-methoxytyramine(8), N-trans-feruloyltyramine(9), N-trans-feruloyl-3-methoxytyramine(10), N-trans-sinapoyltyramine(11), and N-trans-p-coumaroyltyramine(12). Compounds 1 and 2 are new compounds. Compounds 3-7 are obtained from the plants of Papaveraceae for the first time, and compounds 8-12 are firstly isolated from C. racemosa.


Subject(s)
Amides , Chromatography, High Pressure Liquid , Corydalis , Glucosides , Glycosides
13.
Braz. j. med. biol. res ; 53(12): e10109, 2020. graf
Article in English | LILACS, ColecionaSUS | ID: biblio-1132504

ABSTRACT

Psoriasis is a chronic inflammatory skin disorder in humans, and the inflammatory reaction plays an important role in development and onset of psoriasis. 4'-O-β-D-glucosyl-5-O-methylvisamminol (4GMV) is one of the major active chromones isolated from Saposhnikoviae divaricata (Turcz.) Schischk, which has been reported to exhibit excellent anti-inflammatory activities. However, the possible therapeutic effect on psoriasis and underlying mechanism has not been reported. Thus, the aim of this study was to investigate the protective effect of 4GMV on the imiquimod (IMQ)-induced psoriasis-like lesions in BALB/c mice and the anti-inflammatory effect on the lipopolysaccharide (LPS)-induced inflammation in RAW264.7 macrophages. The results demonstrated that 4GMV decreased IMQ-induced keratinocyte proliferation and inflammatory cell infiltration. Moreover, 4GMV treatment significantly inhibited the production of NO, PEG 2, and cytokines such as interleukin (IL)-1β, IL-6, interferon (IFN)-γ, and IL-22 in LPS-stimulated RAW264.7 macrophages. 4GMV also suppressed the LPS-upregulated protein expressions of iNOS and COX-2 in a dose-dependent manner. Furthermore, qRT-PCR analysis showed that 4GMV down-regulated the mRNA level of IL-1β and IL-6 expression. Further studies by western blot indicated that 4GMV inhibited the activation of upstream mediator NF-κB by suppressing the expression of TLR4 and the phosphorylation of IκBα and p65. The phosphorylation of JNK, p38, and ERK were also markedly reversed by 4GMV in LPS-treated RAW264.7 macrophages. Taken together, these results demonstrated that 4GMV showed a protective effect in IMQ-induced psoriasis-like mice and inhibited inflammation through the NF-κB and MAPK signaling pathways, indicating that 4GMV might be a potential therapeutic drug for psoriasis.


Subject(s)
Animals , Rabbits , Psoriasis/chemically induced , Psoriasis/drug therapy , Dermatitis , Lipopolysaccharides , Cytokines , NF-kappa B , Chromones , MAP Kinase Signaling System , Imiquimod , Glucosides , Inflammation , Mice, Inbred BALB C
14.
Article in Chinese | WPRIM | ID: wpr-880776

ABSTRACT

OBJECTIVE@#To investigate the protective effect of arctiin with anti-inflammatory bioactivity against triptolide-induced nephrotoxicity in rats and explore the underlying mechanism.@*METHODS@#Forty SD rats were divided into 4 groups for gastric lavage of normal saline, arctiin (500 mg/kg), triptolide (500 μg/kg), or both arctiin (500 mg/kg) and triptolide (500 μg/kg). Blood samples were collected for analysis of biochemical renal parameters, and the renal tissues were harvested for determining the kidney index and for pathological evaluation with HE staining. In the @*RESULTS@#In SD rats, arctiin significantly antagonized triptolide-induced elevation of BUN, Scr and kidney index (@*CONCLUSIONS@#Arctiin can protect the kidney from triptolide-induced damages in rats possibly through the anti-inflammatory pathway.


Subject(s)
Animals , Anti-Inflammatory Agents , Diterpenes/toxicity , Epoxy Compounds/toxicity , Furans , Glucosides , Kidney/drug effects , Phenanthrenes/toxicity , Rats , Rats, Sprague-Dawley
16.
Rev. Assoc. Med. Bras. (1992) ; 66(supl.1): s17-s24, 2020. tab, graf
Article in English | LILACS | ID: biblio-1057108

ABSTRACT

SUMMARY Type 2 diabetes mellitus is an important public health problem, with a significant impact on cardiovascular morbidity and mortality and an important risk factor for chronic kidney disease. Various hypoglycemic therapies have proved to be beneficial to clinical outcomes, while others have failed to provide an improvement in cardiovascular and renal failure, only reducing blood glucose levels. Recently, sodium-glucose cotransporter-2 (SGLT2) inhibitors, represented by the empagliflozin, dapagliflozin, and canagliflozin, have been showing satisfactory and strong results in several clinical trials, especially regarding the reduction of cardiovascular mortality, reduction of hospitalization due to heart failure, reduction of albuminuria, and long-term maintenance of the glomerular filtration rate. The benefit from SGLT2 inhibitors stems from its main mechanism of action, which occurs in the proximal tubule of the nephron, causing glycosuria, and a consequent increase in natriuresis. This leads to increased sodium intake by the juxtaglomerular apparatus, activating the tubule glomerular-feedback and, finally, reducing intraglomerular hypertension, a frequent physiopathological condition in kidney disease caused by diabetes. In addition, this class of medication presents an appropriate safety profile, and its most frequently reported complication is an increase in the incidence of genital infections. Thus, these hypoglycemic agents gained space in practical recommendations for the management of type 2 diabetes mellitus and should be part of the initial therapeutic approach to provide, in addition to glycemic control, cardiovascular outcomes, and the renoprotection in the long term.


Subject(s)
Humans , Cardiovascular Diseases/prevention & control , Diabetes Mellitus, Type 2/drug therapy , Sodium-Glucose Transporter 2/pharmacology , Sodium-Glucose Transporter 2 Inhibitors/pharmacology , Hypoglycemic Agents/pharmacology , Kidney Diseases/prevention & control , Benzhydryl Compounds/therapeutic use , Cardiovascular Diseases/etiology , Cardiovascular Diseases/mortality , Diabetes Mellitus, Type 2/complications , Diabetic Nephropathies/etiology , Diabetic Nephropathies/metabolism , Diabetic Nephropathies/prevention & control , Sodium-Glucose Transporter 2/therapeutic use , Canagliflozin/therapeutic use , Sodium-Glucose Transporter 2 Inhibitors/therapeutic use , Glomerular Filtration Rate , Glucose/metabolism , Glucosides/therapeutic use , Hypoglycemic Agents/therapeutic use , Kidney/drug effects , Kidney/physiopathology , Kidney/metabolism , Kidney Diseases/etiology , Kidney Diseases/metabolism
17.
Rev. Assoc. Med. Bras. (1992) ; 65(2): 246-252, Feb. 2019. tab, graf
Article in English | LILACS | ID: biblio-990338

ABSTRACT

SUMMARY Sodium-glucose cotransporter-2 inhibitors (SGLT2i) are drugs that act by maintaining glycosuria. Recent studies have shown promising effects of these in the treatment of type 2 diabetes mellitus (DM2). However, there may be an increased risk of developing urinary tract infections (UTIs) in patients treated with these. Our study aims to analyze the association between the risk of UTI in patients treated with SGLT2i. A systematic review of the literature was carried out by randomized clinical trials, totalizing at the end of the selection 23 articles that were statistically evaluated. The incidence of UTI was generally demonstrated in articles and in different subgroups: patients on SGLT2i monotherapy or on combination therapy; according to specific comorbidities of each sample or according to the drug used. They noticed an increase in the chance of UTI in the SGLT2i groups compared to the control groups on placebo or other oral antidiabetic agents. This increased chance was found predominantly with the use of Dapagliflozin, Canagliflozin, and Tofogliflozin, regardless of the dosing. Lastly, stands out that the dimension of UTI chances for DM2 patients who use SGLT2i remains to be more strictly determined.


RESUMO Os inibidores do cotransportador de sódio-glicose do tipo 2 (SGLT2i) são medicamentos que atuam mantendo a glicosúria. Estudos recentes têm demonstrado efeitos promissores desses no tratamento de diabetes mellitus tipo 2 (DM2). No entanto, pode haver um risco aumentado de desenvolver infecções do trato urinário (UTI) em pacientes tratados com essa classe de medicação. Nosso estudo tem como objetivo analisar a associação entre o risco de desenvolver UTI em pacientes tratados com SGLT2i. Uma revisão sistemática da literatura foi realizada por ensaios clínicos randomizados, totalizando, ao final da seleção, 23 artigos que foram avaliados estatisticamente. A incidência de UTI foi demonstrada genericamente de acordo com os dados dos artigos e em diferentes subgrupos: pacientes em monoterapia com SGLT2i ou em terapia combinada, de acordo com as comorbidades específicas de cada amostra ou de acordo com a droga utilizada. Verificou-se um aumento na chance de UTI nos grupos SGLT2i em comparação com os grupos de controle em placebo ou outros agentes antidiabéticos orais. Essa chance aumentada foi encontrada predominantemente com uso de Dapagliflozina, Canagliflozina e Tofoglifozina, independentemente da dosagem. Por fim, ressaltou-se que as chances de UTI em pacientes com DM2 em uso de SGLT2i ainda precisam ser mais bem determinadas.


Subject(s)
Humans , Urinary Tract Infections/etiology , Diabetes Mellitus, Type 2/drug therapy , Sodium-Glucose Transporter 2 Inhibitors/adverse effects , Benzhydryl Compounds/adverse effects , Benzhydryl Compounds/therapeutic use , Randomized Controlled Trials as Topic , Risk Factors , Diabetes Mellitus, Type 2/complications , Canagliflozin/adverse effects , Canagliflozin/therapeutic use , Sodium-Glucose Transporter 2 Inhibitors/therapeutic use , Glucosides/adverse effects , Glucosides/therapeutic use
18.
Acta Physiologica Sinica ; (6): 575-580, 2019.
Article in Chinese | WPRIM | ID: wpr-777154

ABSTRACT

The aim of the present study was to investigate the effect of salidroside (Sal) on inflammatory activation induced by lipopolysaccharide (LPS) in the co-culture of rat alveolar macrophages (AM) NR 8383 and type II alveolar epithelial cells (AEC II) RLE-6TN. CCK-8 colorimetric method was used to detect cell proliferation percentage. The enzyme-linked immunosorbent assay (ELISA) was used to determine the content of tumor necrosis factor alpha (TNF-α), macrophage inflammatory protein-2 (MIP-2) and interleukin-10 (IL-10) in the supernatant. Western blot was used to examine the expression levels of phosphorylated AKT (p-AKT) and total AKT protein. The results showed that pretreatment of RLE-6TN cells or co-culture of RLE-6TN and NR 8383 cells with 32 and 128 µg/mL Sal for 1 h, followed by continuous culture for 24 h, significantly increased the cell proliferation (P < 0.05). Compared with control group, 32 and 128 µg/mL Sal pretreatment significantly increased the ratio of p-AKT/AKT in RLE-6TN cells (P < 0.05). Pretreatment of 32 µg/mL Sal not only inhibited the secretion of TNF-α and MIP-2 by NR 8383 cells induced by LPS (P < 0.05), but also enhanced the inhibitory effect of RLE-6TN and NR 8383 cells co-culture on the secretion of TNF-α and MIP-2 by NR 8383 cells induced by LPS (P < 0.05). In addition, 32 µg/mL Sal pretreatment promoted LPS-induced IL-10 secretion by NR 8383 cells (P < 0.05), and enhanced the promoting effect of co-culture of RLE-6TN and NR 8383 cells on the IL-10 secretion by LPS-induced NR 8383 cells (P < 0.05). In conclusion, Sal may directly inhibit LPS-induced inflammatory activation of AM (NR 8383), promote the proliferation of AEC II (RLE-6TN) through PI3K/AKT signaling pathway, and enhance the regulatory effect of AEC II on LPS-induced inflammatory activation of AM.


Subject(s)
Alveolar Epithelial Cells , Metabolism , Animals , Cell Line , Chemokine CXCL2 , Metabolism , Coculture Techniques , Glucosides , Pharmacology , Interleukin-10 , Metabolism , Lipopolysaccharides , Macrophages, Alveolar , Metabolism , Phenols , Pharmacology , Phosphatidylinositol 3-Kinases , Metabolism , Proto-Oncogene Proteins c-akt , Metabolism , Rats , Signal Transduction , Tumor Necrosis Factor-alpha , Metabolism
19.
Neuroscience Bulletin ; (6): 461-470, 2019.
Article in English | WPRIM | ID: wpr-775428

ABSTRACT

Gastrodin is a phenolic glycoside that has been demonstrated to provide neuroprotection in preclinical models of central nervous system disease, but its effect in subarachnoid hemorrhage (SAH) remains unclear. In this study, we showed that intraperitoneal administration of gastrodin (100 mg/kg per day) significantly attenuated the SAH-induced neurological deficit, brain edema, and increased blood-brain barrier permeability in rats. Meanwhile, gastrodin treatment significantly reduced the SAH-induced elevation of glutamate concentration in the cerebrospinal fluid and the intracellular Ca overload. Moreover, gastrodin suppressed the SAH-induced microglial activation, astrocyte activation, and neuronal apoptosis. Mechanistically, gastrodin significantly reduced the oxidative stress and inflammatory response, up-regulated the expression of nuclear factor erythroid 2-related factor 2, heme oxygenase-1, phospho-Akt and B-cell lymphoma 2, and down-regulated the expression of BCL2-associated X protein and cleaved caspase-3. Our results suggested that the administration of gastrodin provides neuroprotection against early brain injury after experimental SAH.


Subject(s)
Animals , Apoptosis , Astrocytes , Metabolism , Benzyl Alcohols , Blood-Brain Barrier , Metabolism , Brain , Metabolism , Brain Edema , Calcium , Metabolism , Glucosides , Glutamic Acid , Metabolism , Male , Microglia , Metabolism , Neurons , Neuroprotective Agents , Oxidative Stress , Rats, Sprague-Dawley , Subarachnoid Hemorrhage , Metabolism
20.
Article in Chinese | WPRIM | ID: wpr-775261

ABSTRACT

OBJECTIVE@#To develop methods of extraction and purification of Cterminal NUDT9 homology domain of human transient receptor potential melastatin 2 (TRPM2) channel.@*METHODS@#After sonication and centrifuge of strain Rosetta (DE3) which was induced by isopropylthio-β-D-galactoside, GST-NUDT9-H was collected after the binding of supernatant with GST beads and eluted with reduced glutathione. Then the elution buffer containing fusion protein was purified by size exclusion chromatography after concentration and centrifuge. Finally, with the cleavage of thrombin and binding with the GST beads, NUDT9-H with high purity in supernatant was collected.@*RESULTS@#The GST-NUDT9-H fusion protein was stabilized with lysis buffer containing 0.5% n-dodecyl -β-d-maltoside (DDM), and wash buffer containing 0.025% DDM in size-exclusion chromatography system, and finally the NUDT9-H with high purity was obtained after cleaved by thrombin (1 U/2 mg fusion protein) for 24 h.@*CONCLUSIONS@#Due to the poor stability of NUDT9-H, it is necessary to add DDM in extraction and purification buffer to stabilize the conformation of NUDT9-H, so as to increase its yields and purity.


Subject(s)
Escherichia coli , Genetics , Glucosides , Chemistry , Humans , Protein Domains , Protein Stability , Pyrophosphatases , Chemistry , Genetics , Recombinant Fusion Proteins , Chemistry , TRPM Cation Channels , Chemistry , Thrombin , Metabolism
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