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1.
In isoprenaline (ISO)-induced myocardial infarcted rats, garlic oil (GO) and its main ingredient, diallyl disulfide (DADS), were examined for cardioprotective effects when used with carvedilol (CAR). GO, DADS and CAR were given to rats in their respective groups, either alone or together, with the addition of isoprenaline (3 mg/kg/day, subcutaneously) during the last 10 days of treatment. At the end of 14 days of treatment, blood samples were collected, the hearts were excised under anesthesia and weighed. Heart tissue homogenate was used to measure superoxide dismutase (SOD), catalase (CAT), and thiobarbituric acid reactive substances (TBARS). Furthermore, the serum activities of cardiac markers, including lactate dehydrogenase, creatine kinase, and cardiac troponin, were checked. Moreover, inflammatory markers including tumor necrosis factor alpha, interleukin one beta, interleukin six, and kappa bp65 subunit were assessed. Rats that received GO, DADS, and CAR exhibited a significant increase in the cardiac antioxidant enzyme activities with a simultaneous decrease in serum cardiac markers enzymes and inflammatory markers. The TBARS were significantly reduced in rats that received treatment. The addition of carvedilol to GO or DADS significantly elevated antioxidant activities and decreased the release of cardiac enzymes into blood circulation. Both DADS and GOl were almost similar in efficacy, indicating the potential role of DADS in garlic oil-mediated cardioprotection. Combining GO or DADS with CAR increased CAR’s cardioprotective impact and protected rats from developing ISO-induced myocardial infarction.  相似文献   

2.
The quality of garlic and garlic products is usually related to their alliin content and allicin release potential. Until now no analytical method was able to quantify simultaneously allicin, its direct precursor alliin (S-allyl-L-cysteine sulfoxide), SAC (S-allyl-L-cysteine) as well as various dipeptides that apparently serve as storage compounds in garlic. It is well known that all these intermediates are involved in the allicin biosynthetic pathway. A simple and rapid HPLC method suitable for routine analysis was developed using eluents containing an ion-pairing reagent. Particularly, heptanesulfonate as ion-pairing reagent guarantees a sufficient separation between alliin and the more retained dipeptides at very low pH. Allicin was eluted after 18 min on a 150 x 3 mm column. Synthetic reference compounds were characterized by the same chromatographic method using a diode-array UV detector and an ion trap mass spectrometer (electrospray ionization) in the multiple MS mode. In routine analysis of garlic bulbs, powders and other products, the diode-array detector is sufficient for a relevant quantification. Our method has been used in studies to improve the quality of garlic and its derived products.  相似文献   

3.
目的探究轮状病毒性肠炎引起心肌损害的临床表现。方法选择急性肠炎患儿95例,将其分为RV抗原阳性组、RV抗原阴性组,观察两组心肌酶谱情况。结果 RV抗原阳性组53例,CK(165.2±80.1)U/L、CK-MB(72.5±30.2)U/L、LDH(314.5±90.2)U/L、α-HBDH(235.2±71.2)U/L,RV抗原阴性组42例,CK(110±61.1)U/L、CK-MB(21.5±4.5)U/L、LDH(214±54.2)U/L、α-HBDH(154.2±50.2)U/L,组间差异具有统计学意义(P0.05)。结论RV抗原阳性组腹泻患儿心肌酶谱各项指标显著上升,存在心肌损害。  相似文献   

4.
Aim of the present work was to investigate the effect of methyl-β-cyclodextrin (MβCD) on the solubility and dissolution rate of carvedilol (CAR), a drug used orally for the treatment of hypertension. Phase solubility studies showed an AL-type diagram indicating the formation of inclusion complex in 1:1 molar ratio. Solid binary systems of the drug with MβCD were prepared by various methods. Physicochemical characterizations were performed using Fourier Transformation Infrared Spectroscopy, Differential Scanning Calorimetry and powder X-Ray Diffractometry. It could be concluded that CAR can form inclusion complex with MβCD. The dissolution profiles of inclusion complexes were determined and compared with those of CAR alone and the physical mixture. The dissolution rate of CAR was increased by MβCD inclusion complexation remarkably.  相似文献   

5.
In this study, the newly synthesized compound (Succ-5) was analyzed through spectral methods, seen for potential receptor targets via molecular docking, and pre-clinically evaluated for therapeutic effects and safety profile using biochemical and histopathological techniques. The biochemical analysis included assessment of cardiac biomarkers, hepatic enzymes, and lipid profiles, while histopathology included evaluation of cardiac and liver tissues. The toxic dose was determined pre-clinically, followed by dividing albino rats into five treatment groups (each having n = 6). The control group received oral saline for eight days. The 5-FU (5-Fluorouracil) group received oral saline for 8 days and 5-FU (150 mg/kg I.P.) on day 5. The atenolol group was administered with atenolol (20 mg/kg) for 8 days and 5-FU (150 mg/kg I.P.) on day 5. Two groups of rats were administered with the test compound (Succ-5) at doses of 5 mg/kg I.P and 10 mg/kg I.P (for 8-days), followed by 5-FU (150 mg/kg I.P.) on day 5. Elevated serum levels of CK-MB (creatinine kinase myocardial band), cTnI (troponin I), LDH (lactate dehydrogenase), lipid profile, and selected liver enzymes including ALP (alkaline phosphatase), ALT (alanine transaminase), AST (aspartate aminotransferase), BT (bilirubin total) and BD (direct bilirubin) were associated with 5-FU toxicity. After administration of the test compound at the mentioned doses, these biomarkers significantly decreased. Likewise, histological examination revealed 5-FU damaged the heart and hepatic tissues, which were also considerably recovered following administration of the test compound. Immunohistochemistry of heart tissue also revealed the low expression of COX-2 and TNF-α in Succ-5 treated groups compared to toxic group. Dose-response evaluation showed that a dose of 10 mg/kg provided better results than 5 mg/kg. The analysis of binding energy values computed via docking simulations showed that Succ-5 interacts with the human beta2-adrenergic G protein-coupled receptor with a slightly stronger affinity than calcium channel T-type. In conclusion, the histological and biochemical findings revealed that the test compound had significant cardioprotective, hepatoprotective, and lipolytic effects in the 5-FU-induced toxicity.  相似文献   

6.
建立了测定卡维地洛(CAR)新的电化学方法.结合紫外、红外光谱分析,研究了CAR与牛血清白蛋白(BSA)的相互作用.实验发现,在pH4.0Britton-Robinson(B-R)缓冲溶液中,CAR在碳糊电极上产生3个不可逆的氧化峰.以0.92V处的氧化峰为研究对象,结果发现峰电流Ipa,1与CAR浓度在2.45×10-5~1.19×10-3mol/L范围呈良好的线性关系,CAR的检出限为5.6×10-6mol/L.当BSA加入CAR溶液后,CAR峰电流降低,氧化峰电流的降低值△Ipa,1与BSA的浓度在2.92×10-7~1.09×10-5mol/L范围内呈良好线性关系,BSA的检出限为4.1×10-8mol/L.电化学结果表明,CAR与BSA之间形成1∶1的结合物,结合常数为3.14×106L/mol.紫外光谱表明CAR的加入使BSA的吸收峰发生红移且有增色效应.红外光谱表明CAR与BSA分子中氨基酸残基的硫及氮原子形成键合作用.  相似文献   

7.
In the present study, we assessed whether nootkatone (NKT), a sesquiterpene in edible plants, can provide protection against dyslipidemia, intramyocardial lipid accumulation, and altered lipid metabolism in a rat model of myocardial infarction (MI) induced by subcutaneous injections of isoproterenol (ISO, 85 mg/kg) on days 9 and 10. The rats were pre- and co-treated with NKT (10 mg/kg, p.o.) administered daily for 11 days. A significant reduction in the activities of myocardial creatine kinase and lactate dehydrogenase, as well as non-enzymatic antioxidants, and alterations in lipids and lipoproteins, along with a rise in plasma lipid peroxidation and intramyocardial lipid accumulation, were observed in ISO-treated rats. ISO administration induced alterations in the activities of enzymes/expressions that played a significant role in altering lipid metabolism. However, NKT treatment favorably modulated all biochemical and molecular parameters altered by ISO and showed protective effects against oxidative stress, dyslipidemia, and altered lipid metabolism, attributed to its free-radical-scavenging and antihyperlipidemic activities in rats with ISO-induced MI. Additionally, NKT decreased the accumulation of lipids in the myocardium as evidenced from Oil red O staining. Furthermore, the in vitro observations demonstrate the potent antioxidant property of NKT. The present study findings are suggestive of the protective effects of NKT on dyslipidemia and the underlying mechanisms. Based on our findings, it can be suggested that NKT or plants rich in NKT can be promising for use as a phytopharmaceutical or nutraceutical in protecting the heart and correcting lipid abnormalities and dyslipidemia, which are risk factors for ischemic heart diseases.  相似文献   

8.
The application of the laser Raman spectroscopic(LRS) technique for the analysis of liver tissues from rats with myocardial ischemia induced by isoproterenol(ISO) was described.Animal model of myocardial ischemia was established for rats induced by ISO.Rats were randomly divided into four groups as normal group and myocardial ischemia groups.We observed the successful myocardial ischemia model via serum enzymes levels and hematoxylin-eosin(HE) staining,and detected the liver tissue of the rats from normal g...  相似文献   

9.
Several sampling techniques based on steam distillation (SD), simultaneous distillation and solvent extraction (SDE), solid-phase trapping solvent extraction (SPTE), and headspace solid-phase microextraction (HS-SPME) have been compared for the determination of Korean garlic flavor components by gas chromatography–mass spectrometry (GC–MS). Diallyl disulfide (57.88%), allyl sulfide (23.59%), and diallyl trisulfide (11.40%) were found to be the predominant flavor components of garlic samples extracted by SDE whereas these components were at levels of 89.77%, 2.43%, and 3.89% when the same sample was extracted by SD, 97.77%, 0.17%, and 0.10% by SPTE, and 97.85%, 0.01%, and 0.01% by HS-SPME using the 50/30-m divinyl benzene/carboxen/polydimethylsiloxane (DVB/CAR/PDMS) fiber. Thermal degradation of components such as allyl methyl sulfide, dimethyl disulfide, and thiirane were observed for SDE and SD but not for SPTE or HS-SPME. HS-SPME had several advantages compared with SD, SDE, and SPTE—rapid solvent-free extraction, no apparent thermal degradation, less laborious manipulation, and less sample requirement. Five different fiber coatings were evaluated to select a suitable fiber for HS-SPME of garlic flavor components. DVB/CAR/PDMS was most efficient among the five types of fiber investigated.  相似文献   

10.
The present work explores suspicious consequence of low molecular weight glycosaminoglycan (LMW-GAG) on oxidative stress and cellular abnormalities in isoproterenol (ISO)-induced myocardial infarction in an experimental model. Group-III male Wistar rats (140 ± 10 g) were administrated by ISO (85 mg ISO/ml subcutaneously (SC) injected at the last two days of a 2–week period). Group-IV rats were treated LMW-GAG plus ISO (300 μg/day per rat SC for 1 week followed by 85 mg/kg ISO on the end last two days of the 2 - weeks). Untreated control (Group-I) and LMW-GAG drug control (Group-II) were also included. Serum and tissue lactate dehydrogenase, aminotransferases, and creatine kinase activities were increased in ISO group, which were normalized by LMW-GAG pretreatment rats. Antioxidant enzymes – superoxide dismutase (SOD), catalase and glutathione peroxidase (GPx) activities and non-enzymatic enzyme reduced glutathione (GSH) were decreased in the ISO induced rats, and this was increased by LMW-GAG pretreatment. Increased level of thiobarbituric acid reactive substances (TBARS) in plasma and the heart of ISO treated rats; pre s.c. injected with LMW-GAG to ISO-induced rats decreased the levels of TBARS. Histological examination revealed that the ISO-induced deleterious changes in the heart tissues were offset by LMW-GAG treatment. LMW-GAG affords considerable protection to the tissues challenged by cardiotoxicity, evidenced by its correction and restoration of serum and tissue indices of injury, to normalcy.  相似文献   

11.
Prostate apoptosis response-4 (Par-4), an anticancer protein that interacts with cell surface receptor GRP78, can selectively suppress proliferation and induce apoptosis of cancer cells. The core domain of Par-4 (aa 137–195), designated as SAC, is sufficient to inhibit tumor growth and metastasis without harming normal tissues and organs. Nevertheless, the anticancer effects of SAC have not been determined in ovarian cancer cells. Here, we developed a novel method for producing native SAC in Escherichia coli using a small ubiquitin-related modifier (SUMO) fusion system. This fusion system not only greatly improved the solubility of target protein but also enhanced the expression level of SUMO-SAC. After purified by Ni-NTA affinity chromatography, SUMO tag was cleaved from SUMO-SAC fusion protein using SUMO protease to obtain recombinant SAC. Furthermore, we simplified the purification process by combining the SUMO-SAC purification and SUMO tag cleavage into one step. Finally, the purity of recombinant SAC reached as high as 95% and the yield was 25 mg/L. Our results demonstrated that recombinant SAC strongly inhibited proliferation and induced apoptosis in ovarian cancer cells SKOV-3. Immunofluorescence analysis and competitive binding reaction showed that recombinant SAC could specifically induce apoptosis of SKOV-3 cells through combination with cell surface receptor, GRP78. Therefore, we have developed an effective strategy for expressing bioactive SAC in prokaryotic cells, which supports the application of SAC in ovarian cancer therapy.  相似文献   

12.
Hypogonadism, associated with low levels of testosterone synthesis, has been implicated in several diseases. Recently, the quest for natural alternatives to prevent and treat hypogonadism has gained increasing research interest. To this end, the present study explored the effect of S-allyl cysteine (SAC), a characteristic organosulfur compound in aged-garlic extract, on testosterone production. SAC was administered at 50 mg/kg body weight intraperitoneally into 7-week-old BALB/c male mice in a single-dose experiment. Plasma levels of testosterone and luteinizing hormone (LH) and testis levels of proteins involved in steroidogenesis were measured by enzymatic immunoassay and Western blot, respectively. In addition, mouse testis-derived I-10 cells were also used to investigate the effect of SAC on steroidogenesis. In the animal experiment, SAC significantly elevated testosterone levels in both the plasma and the testis without changing the LH level in plasma and increased phosphorylated protein kinase A (p-PKA) levels. Similar results were also observed in I-10 cells. The findings demonstrating the increasing effect of SAC on p-PKA and mRNA levels of Cyp11a suggest that SAC increases the testosterone level by activating the PKA pathway and could be a potential target for hypogonadism therapeutics.  相似文献   

13.
The first three valence transitions of the two nitromethane conformers (CH3NO2) are two dark n → π* transitions and a very intense π → π* transition. In this work, these transitions in gas‐phase and solvated in water of both conformers were investigated theoretically. The polarizable continuum model (PCM), two conductor‐like screening (COSMO) models, and the discrete sequential quantum mechanics/molecular mechanics (S‐QM/MM) method were used to describe the solvation effect on the electronic spectra. Time dependent density functional theory (TDDFT), configuration interaction including all single substitutions and perturbed double excitations (CIS(D)), the symmetry‐adapted‐cluster CI (SAC‐CI), the multistate complete active space second order perturbation theory (CASPT2), and the algebraic‐diagrammatic construction (ADC(2)) electronic structure methods were used. Gas‐phase CASPT2, SAC‐CI, and ADC(2) results are in very good agreement with published experimental and theoretical spectra. Among the continuum models, PCM combined either with CASPT2, SAC‐CI, or B3LYP provided good agreement with available experimental data. COSMO combined with ADC(2) described the overall trends of the transition energy shifts. The effect of increasing the number of explicit water molecules in the S‐QM/MM approach was discussed and the formation of hydrogen bonds was clearly established. By including explicitly 24 water molecules corresponding to the complete first solvation shell in the S‐QM/MM approach, the ADC(2) method gives more accurate results as compared to the TDDFT approach and with similar computational demands. The ADC(2) with S‐QM/MM model is, therefore, the best compromise for accurate solvent calculations in a polar environment. © 2015 Wiley Periodicals, Inc.  相似文献   

14.
Solid dispersion particles of carvedilol (CAR) were prepared with porous silica (Sylysia 350) by the solvent evaporation method in a vacuum evaporator to ensure an effective pore-filling procedure. Two sets were prepared, each with various amounts of CAR in solid dispersions, and with the pore-filling process differing each time. Set A was prepared by a one-step filling method and set B by a multiple-step pore-filling method of CAR into porous silica. The solid dispersions were then characterized using thermal analysis, X-ray diffraction, and nitrogen adsorption experiments. The results showed that the drug release can be significantly improved compared with the dissolution of the drug in its pure crystalline or amorphous state. Drug release from solid dispersion was faster when the drug content in the solid dispersion was low, which enabled the drug to be finely dispersed along the hydrophilic carrier's surface. The results also showed that a multiple-step pore-filling procedure is more effective for drug loading as indicated by the absence of a crystalline drug state, greatly reduced porosity, and improved wettability and physical stability of the amorphous CAR.  相似文献   

15.
The specific aims of this study were to evaluate the inhibition effect on CYP3A of di-n-butyl-di-(4-chlorobenzohydroxamato)tin (IV) (DBDCT), a tin-based complex with high antitumor activity, and the probable mechanism(s) of this action. Adult male SD rats were treated separately with natural saline (NS), lipopolysaccharide (LPS, 5 mg/kg), DBDCT (1.25, 2.5 and 5.0 mg/kg) intraperitoneally for 2 days after induction of CYP3A with dexamethasone (DEX, 100 mg/kg) for 4 days. Western blot analysis and fluorescent quantitation PCR (FQ-PCR) were conducted to determine the changes in expression of CYP3A, PXR, CAR and RXR. The biological accumulation of DBDCT and total Sn were determined by high-performance liquid chromatography (HPLC) and atomic fluorescence spectrometry (AFS). CYP450 content and CYP3A activities were significantly inhibited (p < 0.05) in DBDCT-treated rats compared with the control group, as was the expression of CYP3A (p < 0.05) at both protein and mRNA levels. In DBDCT-treated groups, the expression of PXR protein and mRNA increased, while the expression of CAR decreased. The biological accumulation of DBDCT and Sn in rat livers treated with DBDCT was high. The accumulation of DBDCT and Sn due to the inhibition of CYP3A may be involved in the mechanism of toxicity of DBDCT in rat liver.  相似文献   

16.
Qiao Z  Ma J  Liu H 《Molecules (Basel, Switzerland)》2011,16(12):10002-10012
The present study was undertaken to evaluate the protection potential of ethanol extract of Salvia miltiorrhiza (SMEE) against oxidative injury in the ischemia-reperfusion (I/R) model of rats in vivo. Rats were divided into six groups of 10 rats each. Group I/R model and sham were fed with a standard rat chow, groups SMEE I and SMEE II were fed with a standard rat chow and 400 or 800 mg/kg b.w. ethanol extract for 12 days before the beginning of I/R studies. Positive control group was fed with a standard rat chow and salvianolic acid B (55 mg/kg b.w.) or tanshinone II-A (55 mg/kg b.w.) for 12 days before the beginning of I/R studies. To produce I/R, the left anterior descending artery (LAD) was occluded in anesthetized rats for 15 min, followed by 120 min reperfusion. Infarct sizes were found significantly decreased in SMEE-treated and positive control groups compared to I/R model group. Serum AST, LDH and CK-MB activities were significantly reduced and myocardium Na+-K+ ATPase, Ca2+-Mg2+ ATPase activities and antioxidant enzyme activities (SOD, CAT, GSH-Px) were markedly increased in SMEE-treated and salvianolic acid B or tanshinone II-A positive control groups compared to the I/R model group. Pretreatment of S. miltiorrhiza ethanol extract and salvianolic acid B or tanshinone II-A dose-dependently reduced significantly myocardium MDA level, ROS and NOS activities and enhanced myocardium GSH level in I/R rats compared to I/R rats model. In conclusion, we clearly demonstrated that S. miltiorrhiza ethanol extract pretreatment can decrease oxidative injury in rats subjected to myocardial I/R.  相似文献   

17.
A fast and an efficient ultrasound‐assisted extraction technique using a lower density extraction solvent than water was developed for the trace‐level determination of tebuconazole in garlic, soil and water samples followed by capillary gas chromatography combined with nitrogen–phosphorous selective detector (GC–NPD). In this approach, ultrasound radiation was applied to accelerate the emulsification of the ethyl acetate in aqueous samples to enhance the extraction efficiency of tebuconazole without requiring extra partitioning or cleaning, and the use of capillary GC–NPD was a more sensitive detection technique for organonitrogen pesticides. The experimental results indicate an excellent linear relationship between peak area and concentration obtained in the range 1–50 μg/kg or μg/L. The limit of detection (S/N, 3 ± 0.5) and limit of quantification (S/N, 7.5 ± 2.5) were obtained in the range 0.2–3 and 1–10 μg/kg or μg/L. Good spiked recoveries were achieved from ranges 95.55–101.26%, 96.28–99.33% and 95.04–105.15% in garlic, Nanivaliyal soil and Par River water, respectively, at levels 5 and 20 μg/kg or μg/L, and the method precision (% RSD) was ≤5%. Our results demonstrate that the proposed technique is a viable alternative for the determination of tebuconazole in complex samples.  相似文献   

18.
This study was aimed at evaluating the preventive role of the ethanolic extract of Lagenaria siceraria (Mol) fruit on membrane-bound enzymes, such as sodium potassium-dependent adenosine triphosphatase (Na(+)/K(+) ATPase), calcium-dependent adenosine triphosphatase (Ca(2+) ATPase) and magnesium-dependent adenosine triphosphatase (Mg(2+) ATPase) on isoproterenol (ISO)-induced myocardial infarction (MI) in rats. Male albino Wistar rats were pretreated with the ethanolic extract of L. siceraria (Mol) fruit (125, 250 and 500?mg?kg(-1) body weight) for a period of 30 days. After the treatment period, ISO (85mg?kg(-1) body weight) was subcutaneously injected into rats at 24-h intervals for 2 days. ISO-induced rats showed a significant (p?相似文献   

19.
10-羟基喜树碱-癸二酸-LDH杂化物的制备及性能   总被引:1,自引:0,他引:1  
采用二次插层法成功制备了10-羟基喜树碱(HCPT)-癸二酸(SC)插层的层状双金属氢氧化物(LDH). 先采用共沉淀法制备SC柱撑LDH杂化物(SC-LDH), 再在乙醇介质中将HCPT插入LDH层间形成HCPT-SC-LDH纳米杂化物. 依据SC和HCPT的分子尺寸和纳米杂化物的通道高度, 推测SC分子在层间可能为双层排列, SC分子两端的羧基同时键合在同一个LDH层片表面上; HCPT分子插入(或溶入)SC分子碳氢链形成的疏水区中. 所制备的纳米杂化物既可稳定HCPT的内酯环, 又可明显提高HCPT的溶解度, 还具有明显的药物缓释效果, 其释放动力学过程符合准二级动力学方程.  相似文献   

20.
A sensitive and selective method for simultaneous determination of carvedilol and dopamine was described. The emission wavelengths of carvedilol and dopamine were at 354 nm and 314 nm with the excitation at 290 nm, respectively. The determination of carvedilol and dopamine by normal fluorometry was difficult because the emission spectra of carvedilol and dopamine were overlapped seriously. The first derivative peaks of carvedilol and dopamine were at 336 nm and 302 nm, respectively. The linear regression equations of the calibration graphs of carvedilol and dopamine were C = 0.000557H-0.00569 and C = 0.00438H-0.0812, with the correlation coefficients were 0.9953 and 0.9988, respectively. The liner range for the determination of carvedilol was 0.002 microg ml(-1) to 0.02 microg ml(-1), and 0.05 microg ml(-1) to 0.6 microg ml(-1) for dopamine. The detection limits were 1 ng ml(-1) for carvedilol and 0.04 microg ml(-1) for dopamine, respectively. The relative standard derivative (RSD) of 4.38% and 4.35% was observed for carvedilol and dopamine, respectively. The recovery of carvedilol was from 95.00% to 106.7% in human serum and from 97.50% to 105.0% in urine sample. The recovery of dopamine was from 100.0% to 102.5% in human serum and from 97.50% to 105.0% in urine sample. This method is simple and can be used for determination of carvedilol and dopamine in human serum and urine sample with satisfactory results.  相似文献   

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