ali asadipour
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Background
Assessing the utilization of intravenous immunoglobulin (IVIG) is crucial due to its high cost and limited availability. IVIG preparations are utilized in various disorders. This study aimed to investigate the prescribing and consumption patterns of IVIG at Kerman Afzalipour Hospital and to propose strategies for reducing drug expenditures.
Materials and MethodsOver one year, physician orders and patient charts of individuals treated with IVIG were reviewed to collect data. Descriptive statistics were employed for data analysis using SPSS software.
ResultsDuring the study period, 62 IVIG administrations were documented at the hospital, with 54.1% involving female patients. Of these, 51.4% were prescribed for labeled indications, while 48.6% were for off-label indications. No contraindications were observed, although precaution was warranted in 9.6% of cases, which was not consistently addressed, and laboratory parameters were not evaluated in any case.
ConclusionThis study reveals that IVIG infusions for off-label indications were nearly as frequent as those for labeled indications.
Keywords: Drug Use Evaluation, Drug Utilization, Intravenous Immunoglobulin, Indications -
IntroductionDistal polyneuropathy is a common complication of diabetes mellitus with a considerable negative impact on the quality of life. The aim of this study was to evaluate the effect of dry cupping on distal polyneuropathy in diabetic patients.MethodsThis controlled clinical trial was performed on 34 patients with diabetic polyneuropathy (DPN) for eight weeks. The non-invasive dry and fixed cupping therapy was performed on the sole of the right foot in the patients three times a week for 10 min, and the left foot of the same patient was considered as a control. The severity of diabetic neuropathy was measured using the modified Toronto Clinical Neuropathy Score (mTCNS), and the symptom and sensory test scores were determined.Results20 patients (40 feet) completed the study. There was a significant difference between the control foot and the treated foot in terms of the mTCNS after four and eight weeks (p-values = 0.004 and 0.001, respectively), in terms of the sensory test scores after four and eight weeks (p-values = 0.007 and 0.005, respectively), and in terms of the symptom scores after eight weeks (p-value = 0.002).ConclusionFor the first time, this study demonstrated that cupping therapy might be effective as a complementary treatment in alleviating the symptoms of DPN, although understanding the underlying mechanism requires further investigation.Keywords: Diabetes, Neuropathy, Dry cupping, Persian medicine
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مجله علمی دانشگاه علوم پزشکی کردستان، سال بیست و هفتم شماره 3 (پیاپی 120، امرداد و شهریور 1401)، صص 23 -35زمینه و هدف
شیمی درمانی یکی از رایج ترین راه های قابل دسترس برای درمان سرطان است. مقاومت دارویی یکی از موانع موفقیت در شیمی درمانی سرطان است؛ بنابراین تحقیق در این زمینه برای کشف داروهای جدید ضروری است. هوموایزوفلاونوییدها ترکیبات طبیعی شناخته ای هستند که دارای فعالیت های فارماکولوژیک وسیعی هستند؛ بنابراین سنتز و ارزیابی سمیت سلولی هوموایزوفلاونوییدهای حاوی مورفولینواتوکسی همراه با شبیه سازی داکینگ مولکولی مورد توجه قرار گرفت.
مواد و روش هادو 7-مورفولینواتوکسی هوموایزوفلاونویید در طی سه مرحله سنتز شدند. مرحله اول شامل یک واکنش SN2 بود که 7-هیدروکسی کرمانون با مورفولینواتیل کلرید هیدروکلرید در محیط بازی و تحت شرایط رفلاکس واکنش داد تا حد واسط 3 به دست آید، در مرحله دوم تراکم آلدولی حد واسط اخیر با آلدهید های مناسب در مجاورت HCl گازی در حلال اتانول صورت گرفت و درنهایت خنثی سازی با سود 5 درصد انجام شد. ساختار محصولات با روش های 13CNMR, 1HNMR و IR تایید و سپس سمیت سلولی ترکیبات بر روی رده های سلولیHT-29 و 3T3 ارزیابی شد. برای بررسی طرز اتصال ترکیبات با پروتیین توبولین، شبیه سازی داکینگ با استفاده از MOE انجام شد.
یافته هادو مشتق مورفولینواتوکسی هوموایزوفلاونویید با راندمان تولید متوسط تا خوب تهیه شد. ارزیابی سمیت سلولی این ترکیبات، فعالیت رضایت بخشی را حاصل کرد. نتایج شبیه سازی داکینگ مولکولی، انرژی اتصال قابل قبولی از واکنش بین لیگاندها با جایگاه اتصال پروتیین توبولین را نشان داد: (E)-7-(2-مورفولینواتوکسی)-3-(4-متوکسی بنزیلیدن)کرومان-4-اون برابر با 6838/7- و (E)-7-(2-مورفولینواتوکسی)-3-(3 و4 و5-تری متوکسی بنزیلیدن)کرومان-4-اون،7/3727- کیلوکالری برمول انرژی آزاد کردند.
نتیجه گیرینتایج نشان داد که ترکیب (E)-7-(2-مورفولینواتوکسی)-3-(4-متوکسی بنزیلیدن)کرومان-4-اون سمیت سلولی بیشتری نسبت به ترکیب (E)-7-(2-مورفولینواتوکسی)-3-(3 و4 و 5-تری متوکسی بنزیلیدن)کرومان-4-اون در مقابل رده های سلولی 29-HT و 3T3 دارد. نتایج مطالعات کامپیوتری، نتایج به دست آمده از آزمایش های برون تنی را تایید کرد و سه برهمکنش بین لیگاند (E)-7-(2-مورفولینواتوکسی)-3-(4-متوکسی بنزیلیدن)کرومان-4-اون و اسیدهای آمینه 179αThr، 145αThr و 224αTyr در جایگاه فعال توبولین نشان داد.
کلید واژگان: داکینگ مولکولی, سیتوتوکسیک, هوموایزوفلاونوئیدBackground and AimChemotherapy is one of the most common methods available for the treatment of cancer. Resistance to anticancer drugs can result in failures in chemotherapy of cancers. Therefore, investigation is necessary for the discovery of new drugs. Homoisoflavonoids are well-known natural products that possess a wide range of pharmacological activities. Hence, synthesis and assessment of cytotoxicity of homoisoflavonoids containing morpholinoethoxy moiety and their molecular docking simulation were taken into consideration.
Materials and MethodsTwo 7-morpholinoethoxyhomoisoflavonoids synthesized via three steps including SN2 reaction of 7-hydroxychromanine with morpholino ethyl chloride hydrochloride in the basic media under reflux condition to produce intermediate 3. The second step included aldol condensation of the intermediate with suitable aldehydes in the presence of gaseous HCl in ethanol, and finally neutralization with NaOH 5%. The structures of the products were confirmed using IR, 13CNMR, and 1HNMR techniques. Cytotoxic effects of final products on HT-29 and 3T3 cell lines were assessed. To evaluate the binding mode of compounds with tubulin protein, docking simulation was performed by using MOE.
ResultsTwo morpholinoethoxy homoisiflavonoids were prepared with moderate to good production yield. Cytotoxic evaluation of these compounds showed satisfactory results. The results of molecular docking simulation showed an acceptable binding energy of the interaction between the ligands with the tubulin protein binding site: (E)-7-(2-morpholinoethoxy)-3-(3,4,5-trimethoxybenzylidene) chroman-4-one= -7.3727 Kcal/mol and (E)-3-(4-methoxybenzylidene)-7-(2-morpholinoethoxy) chroman-4-one released -7.6838 Kcal/mol per mole of energy.
ConclusionThe results showed that compound (E)-3-(4-methoxybenzylidene)-7-(2-morpholinoethoxy) chroman-4-one has higher cytotoxicity than (E)-7-(2-morpholinoethoxy)-3-(3,4,5-trimethoxybenzylidene) chroman-4-one against HT-29 and 3T3 cell lines. The in-silico results confirmed the results obtained from in vitro experiments and showed three interactions between ligand (E)-3-(4-methoxybenzylidene)-7-(2-morpholinoethoxy)chroman-4-one and αThr179, αThr145, and αTyr224 amino acids in tubulin active site.
Keywords: Molecular docking, cytotoxic activity, Homoisoflavonoids -
In the present study, response surface methodology was employed to investigate the effects of main variables, including the initial MB concentration, hydrogen peroxide dosage, current density, and electrolysis time on the removal efficiency of MB using the electro-Fenton (EF) process. The MB concentration determination byU V-Vis spectrometer. The EF process degrades the MB contaminant molecules by the highly oxidizing species of the •OH. A quadratic regression model was developed to predict the removal of MB, where the R2 value was found to be 0.9970, which indicates the satisfactory accuracy of the proposed model. ANOVA analysis showed a non-significant lack of fit value (0.0840). Moreover, the predicted correlation coefficient values (R2=0.9915) were reasonably in agreement with the adjusted correlation coefficient value (R2=0.9958), demonstrating a highly significant model for MB dye removal. In addition, the obtained results showed 95.8% MB was removed in the optimum removal efficiency, including the initial MB concentration of 20 mg L-1, H2O2 dosage of 400 μL, and the current density of 7.0 mA cm-2, and electrolysis time of 10 min which was agreed with the predicted removal efficiency of 98.3%. Electrical energy consumption was found to be 0.163 kWh m-3. The constant rate value of Kapp at the optimum operating condition was 0.3753 min-1.
Keywords: Electro-Fenton process, UV-Vis spectrometer, Methylene blue, Response surface methodology, Degradation, Kinetic -
In this research, meta-(4-bromobenzyloxy) benzaldehyde thiosemicarbazone (MBBOTSC) as a novel ligand was synthesized from the reaction between meta-(4-bromobenzyloxy) benzaldehyde and thiosemicarbazide under basic condition in water and ethanol as solvents. Ligand has the ability to chelate ions and therefore, it was used to form a complex and extract ions. So, the cadmium ions in water and wastewater samples were separated based on MBBOTSC by ultrasound assisted-dispersive-ionic liquid-liquid microextractionmethod (USA-D-ILLME) before determination by AT-F-AAS.The MBBOTSC ligand was added to the mixture of the ionic liquid/acetone(IL/AC, [OMIM][PF 6 ]) and then injected by syringe to 50 mL of water samples at pH 6-7.The sample was put into the ultrasonic accessory for 5 minutes, after complexation (Ligand-Cd; RS...Cd....RS), the water sample was centrifuged for 3 min for phase separation.Due to complexation and back-extraction of Cd in liquid phase, the amount of Cd ions in the water samples was determined by AT-F-AAS after dilution eluent (0.5 M, HNO 3 ) with DW up to 1 mL.In optimized conditions, the Linear ranges and LOD for 50 mL of water samples were obtained 1-36 μ g L -1 and 0.3 μ g L -1 , respectively (Mean RSD= 1.26%). The validation results were successfully achieved by spiking real samples and using electrothermal atomic absorption spectrometry (ET-AAS)
Keywords: Cadmium, Meta-(4-bromobenzyloxy) benzaldehyde thiosemicarbazone, Ligand, Synthesis, Metal extraction, Ultrasound assisted-dispersive-ionic liquid-liquid microextraction -
Background
The effective responses of both innate and adaptive immunity are crucial in combating novel coronavirus-2 infection. An excessive response may lead to cytokine storm, which is a challenging problem in therapeutic strategies.
MethodsA systematic review was carried out by searching Ovid MEDLINE, PubMed, Google Scholar, and Cochrane library databases from inception, for anti-inflammatory and immunomodulatory drugs against coronavirus disease 2019 (COVID-19).
ResultsThe results of the effectiveness of Hydroxychloroquine are just like a sinusoidal diagram and in a state of ambiguity. Thalidomide was effective in some cases but has not yet been proven. Low-dose Corticosteroids may be effective in the early stages of the illness as a bridge. There is no evidence of benefits or adverse outcomes for the use of non-steroidal anti-inflammatory drugs and Cyclosporine-A. In some critically ill patients, Interleukin-6 (IL-6) and IL-1 blockers and to some extent, Tumor-Necrosis-Factor-α and Janus-Kinase inhibitors are useful. Finally, high-dose intravenous immunoglobulin reversed the deterioration of patients in most trials.
ConclusionOne strategy behind the treatments for COVID-19 is based on breaking the cytokine storm. Although avoiding the suppression of anti-viral immunity is crucial by choosing the weaker and more selective anti-inflammatories, some strategies are kept for hyper-inflammatory situations. Scheduling of treatment is also important. Although low-dose steroids may be effective in the early stages of the illness, “Tocilizumab” is more effective in severe situations, when the IL-6 level is high and other drugs are ineffective. Therefore, consideration should be given to each patient separately
Keywords: Anti-inflammatory, COVID-19, Immunomodulatory, SARS-CoV-2 -
BackgroundAntibiotics such as ciprofloxacin (CIP) are even more important in bacterial resistance, even at low concentrations. The aim of this research was to synthesize CuFe2O4@methylcellulose (MC) as a new nano-photocatalyst for degradation of CIP from aqueous solution.MethodsThe nano-photocatalyst (CuFe2O4@MC) was characterized by FESEM, energy dispersive spectroscopy (EDS), X-ray diffraction (XRD) and Fourier transform infrared (FTIR), thermogravimetric analysis (TGA), and vibrating sample magnetometer (VSM). Powder XRD and EDS analysis confirmed the formation of pure-phase spinel ferrites. After CuFe2O4@MC characterization, the effective parameters in removal efficiency of CIP such as reaction time, initial antibiotic concentration, pH, photocatalyst loading, and degradation kinetic were investigated and conditions were optimized. Then, CIP degradation experiments were conducted on the real sample in the optimal conditions. The removal of chemical oxygen demand (COD) was determined under optimum conditions.ResultsThe structural characterization of the magnetic nanobiocomposite showed that it is in nanoscale, ferromagnetic property, and thermal stability. The optimal conditions were obtained at pH = 7, irradiation time (90 minutes), photocatalyst loading (0.2 g), and initial concentration of CIP (3 mg/L). The removal efficiency of CIP in the optimal conditions was obtained as 80.74% and 72.87% from the synthetic and real samples, respectively. The removal of COD was obtained as 68.26% in this process. The evaluation of kinetic linear models showed that the photocatalytic degradation process was fitted by pseudo-first order kinetic model and Langmuir-Hinshelwood. CuFe2O4@MC photocatalyst had a good stability and reusability for the fourth runs.ConclusionThe photocatalytic degradation of CIP from aqueous media with CuFe2O4@MC photocatalyst has a high efficiency, which can be used in the treatment of pharmaceutical wastewaters.Keywords: Spinel, Ciprofloxacin, Methylcellulose, Wastewater
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نشریه شیمی کاربردی روز، پیاپی 48 (پاییز 1397)، صص 285 -294در این پژوهش، روشی ساده و موثر برای سنتز مشتقات چند استخلافی 5،1-دی هیدروپیرانو]3،2- [cکرومن با استفاده از واکنش سه جزئی آلدئید های آروماتیک، مالونونیتریل و 3-هیدروکسی کومارین در دمای محیط و در حضور پلی اتیلن گلیکول-400 به عنوان حلال و کاتالیزور واکنش معرفی شده است. روش کار آسان، زمان کوتاه واکنش، بهره وری اتمی بالا، بازده بالا، سازگاری با محیط زیست و سهولت جدا کردن محصولات از پلی اتیلن گلیکول از مهمترین مزایای این روش می باشند. افزون بر آن، محصولات تهیه شده از طریق صاف نمودن ساده و بدون نیاز به ستون و تکنیک های کروماتوگرافی با خلوص بالا بدست آمدند.کلید واژگان: پلی اتیلن گلیکول, 5, 1-دی هیدروپیرانو]3, 2- [cکرومن, واکنش سه جزئی, شرایط بدون کاتالیزورIn this research, a simple and effective method for the synthesis of 1,5-dihydropyrano[2,3-c]chromene multi-substituted derivatives has been introduced, using the three-component reaction of aromatic aldehydes, malononitrile and 3-hydroxycoumarin at room temperature and in the presence of polyethylene glycol (PEG-400) as solvent and reaction catalyst. Easy method, short reaction time, high atom economy, high yields, environmental acceptability and the easy of separating of polyethylene glycol are included as the most important advantages of this method. Moreover, the produced products were obtained through simple filtering and no need to column and technique chromatography with high purity. Moreover, the produced products were obtained through simple filtering and no need to column and technique chromatography with high purity.Keywords: Polyethylene glycol, 1, 5-dihydropyrano[2, 3-c]chromenes, three-component reaction, catalyst-free conditions
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BackgroundAn efficient, promoted tri-component catalytic reaction between barbituric acid (or N,N-dimethyl barbituric acid), 4-hydroxy coumarin, and a wide range of aryl aldehydes using zinc oxide nanowires (ZnO NWs) to obtain some new 4-hydroxychromenylarylmethyl-6-hydroxypyrimidine-2,4-diones is described.MethodThe reactants were successfully condensed via three C-C bond formation by zinc oxide nanowires (ZnO NWs) as an efficient, environmentally safe and recyclable nano catalyst to produce target molecules. In addition, the biological effects of synthesized products by the use of DPPH and acyclovir as positive controls and also Hep-2, vero cell, HSV-1, and adenovirus as four applied cell lines have been evaluated.ResultsThe results showed that synthesized products have anti-oxidant, cytotoxic and anti-viral activities and can offer promising prospect as biologically active agents.ConclusionThis achievement in an efficient and eco-friendly synthesis of novel analogous of hybrid molecules in aqueous media with special biological properties may engross chemists and pharmacologists as well as pharmacists in futureKeywords: Synthesis, Ultrasound assisted, Bio-assay, Anti-oxidant, Cytotoxic, Anti-viral, Nano-catalyst
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ObjectivesThis study aimed at investigating the effect of Iranian traditional remedy prepared from Apium graveolens and Trachyspermum copticom (AT) on the severity and frequency of symptoms in patients with functional dyspepsia (FD).
Material andMethodsIn total, 150 FD patients were included in this randomized double-blind trial, based on the ROME III diagnostic criteria, and they were divided into three intervention groups namely, AT, Placebo and omeprazole. Then, severity and frequency of symptoms during this eight-week trial were measured. Obtained information was analyzed using Chi-square test and repeated measures test.ResultIn general, the severity and frequency of symptoms after the 4th week significantly decreased in the AT group as compared to the omeprazole and placebo groups, and continued to reduce by the end of the eighth week. General reduction of symptom severity and frequency in the omeprazole group was significantly different from the placebo group by the end of the 4th and 8th weeks. With respect to each individual symptom, AT markedly improved symptoms, such as burning, pain, early satiation, fullness, bloating, belching and nausea, as compared to placebo-treated group. Moreover, AT significantly improved symptoms, like vomiting, and nausea, except for pain, as compared to omeprazole-treated subjects.ConclusionAccording to the results, AT, as Iranian traditional remedy, was more effective than omeprazole and placebo in reducing the symptoms in FD patients.Keywords: IranianTraditional medicine, Apium Graveolens, Trachyspermum Copticom, Functional Dyspepsia -
مجله دانشگاه علوم پزشکی سبزوار، سال بیست و سوم شماره 1 (پیاپی 84، فروردین و اردیبهشت 1395)، صص 110 -121زمینه و هدفیکی از بزرگترین صنایع تولیدکننده ی فاضلاب های رنگی، صنعت نساجی است. تخلیه ی این فاضلاب ها به آب های پذیرنده از طریق کاهش انتقال نور، کاهش اکسیژن محلول و افزایش COD زندگی آبزیان را به خطر می اندازد. در این تحقیق کارایی نانو ذرات پراکسید کلسیم در حذف راکتیو قرمز 198 از فاضلاب سنتتیک و فاضلاب کارخانه نساجی یزدباف بررسی گردید.مواد و روش هااین تحقیق یک مطالعه ی تجربی است که در بهار و تابستان 1393 در مرکز تحقیقات مهندسی بهداشت محیط دانشگاه علوم پزشکی کرمان انجام شد. مشخصات نانو ذرات سنتز شده از طریق آزمایش های TEM و XRD تعیین گردید. آزمایش های جذب در سیستم ناپیوسته روی نمونه سنتتیک و واقعی انجام شد. تاثیر پارامترهای pH محلول (3-13)، غلظت اولیه رنگ (10 – 300 mg/L)، زمان تماس (5- 90 دقیقه) و دوز جاذب (5 صدم -6 دهم گرم) بررسی و ایزوترم های جذب تعیین شد. داده ها با استفاده از نرم افزارSPSS نسخه ی 21، EXCEL2007 و ضریب همبستگی پیرسون تحلیل گردید.یافته هاجاذب سنتز شده دارای اشکال کروی یکنواخت با اندازه ی متوسط 25-15 نانومتر بود.pHبهینه در حذف رنگ 3-7، زمان تماس تعادلی 50 دقیقه و مقدار بهینه ی جاذب 4 دهم گرم در 100 میلی لیتر بود. در شرایط بهینه بازده ی حذف رنگ در نمونه ی سنتتیک و واقعی، به ترتیب 58/99 و 18/76 درصد به دست آمد. نتایج حاصل شده بیشترین همبستگی را با مدل ایزوترم لانگمویر نشان داد.نتیجه گیریبراساس نتایج پراکسید کلسیم جاذب مناسبی در حذف راکتیو قرمز 198 می باشد و با توجه به سنتز آسان، می تواند به عنوان یک روش کاربردی در تصفیه ی فاضلاب های نساجی استفاده شود.کلید واژگان: جذب سطحی, پراکسید کلسیم, کارخانه یزدبافBackground and ObjectivesTextile industry is one of the largest industries producing dying wastewater. Discharge of this wastewater to acceptor waters endangers aquaticslife through reducing light transmission, reducing dissolve oxygen, and increasing COD. This study investigated the efficiency of calcium peroxide nanoparticles in removal of Reactive Red 198 from synthetic wastewater and wastewater of YAZDBAF textile factory.Materials and MethodsThis experimental study was performed in spring and summer of 2014 in Environmental Health Engineering Research Center of Kerman University of Medical Science. Characteristic of synthesized nanoparticles was determined by TEM and XRD. Adsorption experiments in batch system were performed on synthetic sample and real wastewater. The effect of solution pH (3-13), initial concentration of dye (10-300 mg/L), contact time (5-90 min) and adsorbent dosage (0.05-0.6 g) was investigated and adsorption isotherms were determined. Data was analyzed by SPSS version 21, Excel 2007 softwares and Pearson correlation coefficient.ResultsSynthesized adsorbent particles had uniformly spherical shape with approximately diameter of 15-25 nm. The optimum pH for removal of reactive red 198 was 3-7. The equilibrium contact time was 50 minutes and optimum dosage of adsorbent was 0.4 g/100 mL. In these optimum conditions, removal efficiency in synthetic and real sample was 99.58 and 76.18 percent, respectively.ConclusionBased on the results, calcium peroxide is an efficient adsorbent in removing reactive red 198 and, with attention to simplicity of synthesis, it can be used as an applied in treating textile wastewaters.Keywords: adsorption, Calcium peroxide, YAZDBAF factory
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آنچه از پی می آید کوشش و پژوهشی است درباره اعتقاد به اصل و منشاء ملکوتی روح که یکی از موتیف های شاخص و بن مایه های اصلی اندیشه های عرفانی است. در این مختصر گفتار سعی شده است به تبیین سیر روح و نزول آن از عالم اعلی به مرتبه ادنی در دو اثر عرفانی قصیده «عینیه» ابن سینا و مصباح الارواح بردسیری کرمانی پرداخته شود. ابن سینا با دفاع از نظریه دوگانگی روح و تن مانند بسیاری از عرفای اسلامی از پیشگامان، تلاش کرده به صورت تمثیلی و با زبانی نمادین کیفیت هبوط روح را در جسم و عالم ماده به تصویر بکشد. اما بردسیری در مصباح الارواح نه تنها به صعود روح و بازگشتش به عالم بالا معتقد است بلکه در مسیر این بازگشت مراحل تکامل روح را نیز بیان می کند. این مقاله بر آن است تا ضمن بررسی تطبیقی این دو اثر و ذکر وجوه تشابه آنها به نکات جدیدی در مورد سیر مراحل روح بپردازد.
کلید واژگان: عرفان اسلامی, عینیه, ابن سینا, مصباح الارواح, بردسیریThe belief that the soul originates from the celestial world and is imprisoned in the material world as a result of neglect is a fundamental belief in mysticism. the sophis try to purify the soul through knowledge and wisdom before it unites with the God in the afterworld. Aviccina focuses on this purification in his Ode (Einieh) and the Persian poet, Bardsiri Kermani, does the same in his long piece of poetry(Mesbah-ol-Arvah) and follows the example of Einieh. makes use of several terms and themes of Islamic mysticism including vesal, Boka, Bareqe and Hejab similarly references are made to light and darkness.This paper comparatively explores the theme in these works.Keywords: Islamic mysticism, Aviccina, Einieh, Bardsiri Kermani, Mesbah, ol, Arvah -
Nitro-containing heteroaromatic derivatives structurally related to nitroimidazole (Metronidazole) are being extensively evaluated against Helicobacter pylori isolates. On the other hand, 1,3,4-thiadiazole derivatives have also demonstrated promising antibacterial potential. In present study, we evaluated anti-H. pylori activity of novel hybrid molecules bearing nitroaryl and 1,3,4-thiadiazole moieties. Anti-H. pylori activity of novel 5-(5-nitroaryl)-1,3,4-thiadiazole derivatives bearing different bulky alkylthio side chains at C-2 position of thiadiazole ring, were assessed against three different metronidazole resistant H. pylori isolates by paper disk diffusion method. Most of the compounds demonstrated moderate to strong inhibitory response especially at 25 μg/disk. The structure-activity relationship study of the compounds demonstrated that introduction of different alkylthio moieties at C-2 position of thiadiazole ring alter the inhibitory activity which is mainly dependent on the type of C-5 attached nitrohetercyclic ring. The promising compound of this scaffold, bearing 1-methyl-5-nitroimidazole moiety at C-5 and α-methylbenzylthio side chain at C-2 position of thiadiazole ring, showed strong inhibitory response against metronidazole resistant H. pylori isolates at 12.5 μg/disk (the inhibition zone diameter at all evaluated concentrations (12.5-100 μg/disk) is > 50 mm). Novel 5-(5-nitroaryl)-1,3,4-thiadiazole scaffold bearing different C-2 attached thio-pendant moieties with promising anti-H. pylori potential were identified. Among different nitroheterocycles, 5-nitrofuran and 5-nitroimidazole moieties were preferable for the substitution at C-5 position of 1,3,4-thiadiazole ring. Introduction of different alkylthio side chains at C-2 position of central ring alter the inhibitory activity which is mainly dependent on the type of C-5 attached nitrohetercyclic ring.Keywords: 1, 3, 4, thiadiazole, anti, Helicobacter pylori activity, Nitroheterocycle
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Centaurea aucheri (DC.) Wagenitz is one of the species of Asteraceae that has not been the subject of many investigations. Different species of this genus have been used in traditional medicine. In this investigation C. aucheri was collected from Khanesorkh of Kerman and the essential oil of the aerial parts of plant was extracted by Clevenger apparatus and analyzed by GC-MS. Identification of the components of oils were based on their retention indices and mass spectra data in comparison with those reported in literatures. The amount of essential oil was 0.16% and 22 substances consisting 80.03% of the composition of the essential oil were identified. The main compounds were caryophyllene oxide (19.44%), β-caryophyllene (14%), Geremacrene-D (13.38%). The essential oil was rich in sesquiterpene oil.
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Abstract: The essential oil from flowering aerial parts of Nepeta depauperata Benth., an endemic Iranian plant, obtained by steam distillation was analyzed by GC/MS. The constituents were identified by their mass spectra and Kovats’ indices. Thirty-three compounds consisting 82.52% of the total components were identified from the oil obtained with a yield of 0.3%v/w. Among them, spathulenol (31.84%), beta caryophyllene (12.93%) and caryophyllene oxide (10.27%) were the major components of the oil
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Analgesic and ulcerogenic effect of methanolic extract of Artemisia dracunculus and histopathological evaluationIn this study, the analgesic effect of Artemisia dracunculus, which has been used in traditional medicine as an analgesic, anti-rheumatic and toothache releiver was studied. For extraction, suxhelet and percolation methods by 80% methanol was used. The extract was then concentrated and the weight of dried extract was determined and dissolved in normal saline to produce desired concentration. The analgesic effect of the extract was determined by the formalin and hot-plate tests. The results of formalin test showed that all doses of the extract have analgesic effect in comparison with control group and the extract at a dose of 800 mg/kg produces the highest analgesic effect. In this respect, there was no significant difference regarding the extracting methods. The results of hot plate showed that the extract at a dose of 800 mg/kg has a significant analgesic effect compared to control group. In addition, the analgesic effect of extract was compared with ASA and morphine by formalin and hot plate tests. The results showed that the analgesic effect of 800 mg/kg of extract was higher than ASA and lower than morphine in some trials. Furthermore, pretreatment of animals with naloxone decreased the analgesic effect of extract. Therefore, it seems that part of analgesic effect of the extract may be attributed to opioid system. At the end of the study, those rats receiving 800 and 1600 mg/kg of the extract and control ones were collected for histopathological evaluation. The results showed that there is only small congestion in liver and kidney after the extract injection. In addition, there was no sign of peptic ulcer in comparison with rats receiving indomethacin.
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