Farzad Kobarfard
Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Iran. | Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
[ 1 ] - Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors
Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...
[ 2 ] - Clopidogrel Resistance and its Impact on Clinical Outcome of Iranian Patients Undergoing Percutaneous Coronary Intervention
The aim of current study was evaluating the frequency of clopidogrel resistance and its impact on clinical outcome of patients in Iranian patients. Patients undergoing percutaneous coronary intervention in Imam Hussein Medical center, Tehran, Iran, who received standard dosage of clopidogrel (Plavix®, Sanofi, France, 600 mg loading dose and 75 mg/day afterward) were recruited. Platelet aggregat...
[ 3 ] - The Effects of House Cooking Process on Residue Concentrations of 41 Multi-Class Pesticides in Rice
In current study, the effects of Iranian rice cooking method (Kateh) on residue levels of 41 pesticides were investigated. The pesticides were selected according to Iranian National Standards Organization (INSO) regulations and covered 18 permitted and 23 banned pesticides belonging to different chemical classes such as organophosphate, triazole, and carbamate. A 250 g portion of rice sample wa...
[ 4 ] - Exposure Assessment for Some Pesticides through Rice Consumption in Iran Using a Multiresidue Analysis by GC-MS
In communities which consume rice as main food, importance of risk assessment forcontaminants is always taken into consideration by health authorities. The present study isan attempt for monitoring of 56 pesticides from different chemical groups in rice samplescollected from local markets in Tehran and estimation of daily intake of interested pesticidesthrough this monitoring. A valid method ba...
[ 5 ] - RP-HPLC method development and validation for determination of eptifibatide acetate in bulk drug substance and pharmaceutical dosage forms
A new, rapid, economical and isocratic reverse phase high performance liquid chromatography (RP-HPLC) method was developed for the determination of eptifibatide acetate, a small synthetic antiplatelet peptide, in bulk drug substance and pharmaceutical dosage forms. The developed method was validated as per of ICH guidelines. The chromatographic separation was achieved isocratically on C18 colum...
[ 6 ] - Development of an analytical method for dibutyl phthalate determination using Surrogate analyte approach
Dibutyl phthalate (DBP) is a phthalic acid ester and is widely used in polymeric products to make them more flexible. DBP is found in almost every plastic material and is believed to be persistent in the environment. Various analytical methods have been used to measure DBP in different matrices. Considering the ubiquitous nature of DBP, the most important challenge in DBP analyses is the contam...
[ 7 ] - A Multi Residue GC-MS Method for Determination of 12 Pesticides in Cucumber
Cucumber is one of the main vegetables in Iranian food basket. A wide range of pesticides are used for crops protection during the cultivation of vegetables such as cucumber due to heavy pest infestation. Analysis of pesticide residues in food and other environmental commodities have become essential requirement for consumers, producers, and food quality control authorities. This study was aime...
[ 8 ] - Simultaneous Chloramphenicol and Florfenicol Determination by A Validated DLLME-HPLC-UV Method in Pasteurized Milk
The antibiotic residues in milk are a well-known serious problem and pose several health hazards to consumers. We have described a simple, rapid, and inexpensive DLLME-HPLC/UV technique for the extraction of chloramphenicol and florfenicol residues in milk samples. Under the optimum conditions, linearity of the method was observed over the range 0.02-0.85 µg/L with correlation coefficients > 0....
[ 9 ] - Validation of an Analytical Method for Determination of Benzo[a]pyrene Bread using QuEChERS Method by GC-MS
A fast and simple modified QuEChERS (quick, easy, cheap, rugged and safe) extraction method based on spiked calibration curves and direct sample introduction was developed for determination of benzo[a]pyrene (BaP) in bread by gas chromatography-mass spectrometry single quadrupole selected ion monitoring (GC/MS-SQ-SIM). Sample preparation includes extraction of BaP into acetone followed by clean...
[ 10 ] - Simultaneous Determination of 13 Priority Polycyclic Aromatic Hydrocarbons in Tehran’s Tap Water and Water for Injection Samples Using Dispersive Liquid-Liquid Micro Extraction Method and Gas Chromatography-Mass Spectrometry
Abstract Polycyclic aromatic hydrocarbons (PAHs) are classified as persistent and carcinogenic organic pollutants. PAHs contamination has been reported in water. Many of relevant regulatory bodies such as EU and EPA have regulated the limit levels for PAHs in drinking water. In this study, 13 priority polycyclic aromatic hydrocarbons (PAHs) were determined in tap water samples of Tehran and wat...
[ 11 ] - Triterpene Constituents of Euphorbia Erythradenia Bioss. and their Anti-HIV Activity
Phytochemical investigation of the aerial parts of Euphorbia erythradenia Bioss. (Euphorbiaceae), one of Iranian endemic Euphorbias, with particular attention to triterpene constituents, using methanol solvent extraction was carried out. Five known triterpenes, including four cycloartanes and oleanolic acid, were isolated for the first time and identified using NMR and Mass techniques. Anti HIV...
[ 12 ] - Synthesis and Antibacterial Activity of Novel Hydroxy Semicarbazone Derivatives
A series of hydroxysemicarbazone derivatives of substituted diaryl ketones and acetophenones were synthesized and their structures were confirmed by analytical and spectroscopic methods including elemental analysis, infrared and nuclear magnetic resonance spectroscopy. The derivatives were prepared by a condensation reaction between N-hydroxysemicarbazide and substituted diaryl ketones or aceto...
[ 13 ] - Determination of Benzo[a]pyrene in Traditional, Industrial and Semiindustrial Breads Using a Modified QuEChERS Extraction, Dispersive SPE and GC-MS and Estimation of its Dietary Intake.
A fast and simple modified QuEChERS extraction method was developed for determination of Benzo[a]pyrene (BaP) in 137 traditional (Sangak), semi-industrial (Sangak) and industrial bread samples using spiked calibration curves by GC/MS. Sample preparation includes extraction of BaP into acetone followed by cleanup with dispersive solid phase extraction. The limit of detection and limit of quantif...
[ 14 ] - Validation of an Analytical Method for Determination of 13 priority polycyclic aromatic hydrocarbons in mineral water using dispersive liquid-liquid microextraction and GC-MS
Dispersive liquid liquid microextraction (DLLME) combined with gas chromatography–mass spectrometry (GC–MS) was used for the extraction and determination of 13 polycyclic aromatic hydrocarbons (PAHs) in mineral water samples. In this procedure, the suitable combination of extraction solvent (500 µL chloroform) and disperser solvent (1000 µL acetone) were quickly injected into the water sample (...
[ 15 ] - FTIR Biospectroscopy Investigation on Cisplatin Cytotoxicity in Three Pairs of Sensitive and Resistant Cell Line
Fourier Transformed Infrared Spectroscopy (FTIR) has extensively been used for biological applications. Cisplatin is one the most useful antineoplastic chemotherapy drugs for a variety of different human cancers. One of the clinical problems in its application, which would consequently affect the therapeutic outcome of its application, is the occurrence of resistance to this agent. In this proj...
[ 16 ] - Evaluation of anti-platelet aggregation effect of some Allium species
Epidemiologic studies show that the cardiovascular diseases are associated with multiple factors such as raised serum total cholesterol, increased LDL, increased platelet aggregation, hypertension and smoking. In-vitro studies have confirmed the ability of some plants of Allium species to reduce these parameters. Therefore, we evaluated anti-platelet aggregation effect of some Allium species (A...
[ 17 ] - Development and Validation of a Micellar Capillary Electrophoresis Method for Determination of IFNβ-1b in Lyophilized Formulation of a Biosimilar Product
Human interferons (IFNs) are key cytokines secreted by immune system. They have several effects such as antiviral and anti tumors activity, activating immune cells and healing of multiple sclerosis. The type IFNs present in humans are α, β and Υ. IFN β is a polypeptide, normally produced by fibroblasts and seems to be more species-specific than IFN . Structural properties of I FNs are importan...
[ 18 ] - Synthesis and Antiplatelet Aggregation Activity Evaluation of some 2-Aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine Derivatives
A series of novel 2-aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine derivatives have been synthesized and their anti platelet aggregation activities were assessed against ADP and arachidonic acid- induced platelet aggregation in human plasma using light transmission aggregometry. None of the compounds showed satisfactory activity against the aggregation induced by ADP. However, satisfac...
[ 19 ] - Evaluation of Emerging Fusarium mycotoxins beauvericin, Enniatins, Fusaproliferin and Moniliformin in Domestic Rice in Iran
The occurrence of emerging Fusarium mycotoxins beauvericin (BEA), enniatins (ENNs) (A, A1, B, B1), Fusaproliferin and moniliformin was evaluated by a liquid chromatography/electrospray ionization-tandem mass spectrometric (LC/ESI-MS/MS) technique in 65 domestic rice samples produced in Gilan and Mazandaran Provinces in IR Iran. The results showed that 46% of the samples were contaminated with a...
[ 20 ] - Synthesis and Antimycobacterial Activity of some Triazole Derivatives–New Route to Functionalized Triazolopyridazines
A series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. The 4-amino-1,2,4-triazole-5-thione analogues (Ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. Reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivat...
[ 21 ] - Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxy phenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic h...
[ 22 ] - Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent
Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly, a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors. [6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenedia...
[ 23 ] - Method development for simultaneous determination of 41 pesticides in rice using LC-MS/MS technique and its application for the analysis of 60 rice samples collected from Tehran market
For the first time, a multi-residue methodfor simultaneous determination of 41LC-amenable pesticides in rice, belonging to different chemical classes has been developed in Iran by LC-MS/MS. The pesticides were analyzed simultaneously in a single run using positive electrospray ionization with multiple reaction monitoring (MRM) after extraction with slightly modified QuEChERS method. The calibra...
[ 24 ] - Phytochemical investigations on chemical constituents of Achillea tenuifolia Lam.
Achillea tenuifolia Lam (Asteraceae) afforded a methanolic extract from which after fractionation in solvents with different polarities two known flavones 3’, 5- dihydroxy- 4’, 6, 7- trimethoxy flavone (eupatorine, compound 3), 5- hydroxy- 3’, 4’, 6, 7- tetramethoxyflavone (compound 4), besides stearic acid (compound 1 ), lupeol (compound 2), daucosterol (β- sitosterol 3-O- β- D- glucopyranosid...
[ 25 ] - Synthesis of N-arylmethyl Substituted Indole Derivatives as New Antiplatelet Aggregation Agents
A number of N-arylmethyl substituted indole derivatives have been synthesized and their effectiveness against ADP and arachidonic acid induced platelet aggregation in human plasma was determined. The desired compounds were synthesized by reacting the appropriate aniline derivative with isatin (or substituted isatin) to form the corresponding imine structures. The so formed compound was then act...
[ 26 ] - Development and Validation of a Reversed-phase HPLC Method for Assay of the Decapeptide Cetrorelix Acetate in Bulk and Pharmaceutical Dosage Forms
A gradient reversed-phase high performance liquid chromatography (HPLC) method was developed for the assay of cetrorelix acetate, a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment. The HPLC method, which is used to determine cetrorelix in bulk and pharmaceutical dosage forms, was validated per ICH guidelines. The chromatograph...
[ 27 ] - Synthesis and Evaluation of New Fluorinated Anti-Tubercular Compounds
Treatment of tuberculosis (TB) and the discovery of effective new anti tubercular drugs is one of the most urgent priorities in health organizations all around the world. In the present study, fluorinated analogs of some of the most important anti-TB agents such as p-aminosalicylic acid (PAS), thiacetazone and pyrazinamide were synthesized and tested against TB. The fluorinated analog of thiace...
[ 28 ] - Simultaneous Determination of 17 Pesticide Residues in Rice by GC/MS using a Direct Sample Introduction Procedure and Spiked Calibration Curves
A reliable, rapid and accurate method based on spiked calibration curves and direct sample introduction was developed for determination of 17 pesticide residues in rice by gas chromatography-mass spectrometry single quadrupole selected ion monitoring GC/MS-SQ-SIM. Sample preparation is based on extraction with acetonitrile without clean up. The use of spiked calibration curves for constructing...
[ 29 ] - Synthesis and Antimycobacterial Activity of Symmetric Thiocarbohydrazone Derivatives against Mycobacterium bovis BCG
In this work, we reported the synthesis and evaluation of antimycobacterial and antifungalactivity of a series of thiocarbohydrazone derivatives which are thiacetazone congeners. Thetarget compounds were synthesized in superior yields by reacting thiocarbohydrazide withdifferent aromatic aldehydes and methyl ketones. Compounds 8, 19 and 25 were found to bethe most potent derivatives, exhibiting...
[ 30 ] - Development of a Simple RP-HPLC-UV Method for Determination of Azithromycin in Bulk and Pharmaceutical Dosage forms as an Alternative to the USP Method
The present study was designed to develop a simple, validated liquid chromatographic method for the analysis of azithromycin in bulk and pharmaceutical dosage forms using ultraviolet detector. The best stationary phase was determined as C18 column, 5 µm, 250 mm × 4.6 mm. Mobile phase was optimized to obtain a fast and selective separation of the drug. Flow rate was 1.5 mL/min, Wavelength was se...
[ 31 ] - Resistance to Clopidogrel among Iranian Patients Undergoing Angioplasty Intervention
To study the resistance to standard dosage of clopidogrel among Iranian patients following percutaneous coronary intervention measured by platelet aggregation test.Patients undergoing percutaneous coronary intervention in Imam Hussein Medical center, Tehran, Iran, who were under treatment with aspirin, but had no history of clopidogrel usage, entered the study. Patients received standard dosage...
[ 32 ] - Partial Fractionation of Venoms from Two Iranian Vipers, Echis carinatus and Cerastes persicus Fieldi and Evaluation of Their Antiplatelet Activity
Platelet aggregation inhibitory effect and anticoagulant properties of fractions separated from the venoms of Cerastes persicus fieldi and Echis carinatus were investigated. The partial fractionation was performed on a Sephadex G-100 column. Two fractions separated from Cerastes persicus fieldi showed anti platelet aggregation activity on ADP (200 µM)-induced platelet aggregation (ca 80% inhibi...
[ 33 ] - Synthesis and Cytotoxic Evaluation of Novel 3-Substituted Derivatives of 2-Indolinone
The assessment of the degree or rate of cellular proliferation and cell viability is critical for the assessment of the effects of drugs on both normal and malignant cell populations. In the present study, a few novel 3-substituted derivatives of 2-indolinones were synthesized by condensation of substituted oxindole or isatin derivatives with appropriate aldehydes or primary aromatic amine...
[ 34 ] - Evaluation of the Effect of PEGylated Single-Walled Carbon Nanotubes on Viability and Proliferation of Jurkat Cells
Among the numerous nanosized drug delivery systems currently under investigation, carbon nanotubes (CNTs), regardless of being single or multiple-walled, offer several advantages and are considered as promising candidates for drug targeting. Despite the valuable potentials of CNTs in drug delivery, their toxicity still remains an important issue. After the PEGylation of single-walled CNTs ...
[ 35 ] - A Rapid, Simple, Liquid Chromatographic-Electrospray Ionization, Ion Trap Mass Spectrometry Method for the Determination of Finasteride in Human Plasma and its Application to Pharmacokinetic Study
A fast, accurate, sensitive, selective and reliable method using reversed-phase high performance liquid chromatography coupled to electrospray ionization ion trap mass spectrometry was developed and validated for the determination of finasteride in human plasma. After protein precipitation with perchloric acid, satisfactory separation was achieved on a Zorbax Eclipse® C8 analytical column u...
[ 36 ] - A Simple Electrochemical Method for the Rapid Estimation of Antioxidant Potentials of Some Selected Medicinal Plants
Clinical and Epidemiological studies have shown that a diet rich in fruits and vegetables is associated with a decreased risk of cardiovascular diseases, cancers and other related disorders. These beneficial health effects have been attributed in part to the presence of antioxidants in dietary plants. Therefore screening for antioxidant properties of plant extracts has been one of the inte...
[ 37 ] - Application of Narrow-Bore HPLC Columns in Rapid Determination of Sildenafil Citrate in Its Pharmaceutical Dosage Forms
A special type of silica-based columns has been recently introduced into the market which is called narrow-bore columns. They have lower internal volume than the standard high-performance liquid chromatography (HPLC) columns and thus reduce the solvent consumption by almost 80%. A simple, accurate and environmentally friendly reversed phase- HPLC (RP-HPLC method) which could be used in ...
[ 38 ] - The Effect and Persistency of 1% Aluminum Chloride Hexahydrate Iontophoresis in the Treatment of Primary Palmar Hyperhidrosis
Topical solutions containing aluminum chloride are known to be the first line of therapy for hyperhidrosis. Palmar hyperhidrosis however, is less responsive to aluminum chloride therapy and successful treatment may require 6-8 h application of high concentrations up to 30% that commonly leads to skin irritation. The purpose of this study is to investigate the effect of 30 min iontophoretic appl...
[ 39 ] - Profiling of Ecstasy Tablets Seized in Iran
In this study 50 samples of ecstasy tablets seized in Iran during the period of 2007 through 2008 were examined and their physical characteristics (appearance, marking, scored/not scored, color, weight, diameter, thickness) were determined. In order to determine the chemical characteristics of these tablets, color tests (Marquis test, Simon’s test, Chen’s test and Gallic acid test), Thin Layer ...
[ 40 ] - Effect of Cooking Process on the Residues of Three Carbamate Pesticides in Rice
A gas chromatography mass spectrometry with spike calibration curve method was used to quantify three carbamate pesticides residue in cooked white rice and to estimate the reduction percentage of the cooking process duration. The selected pesticides are three carbamate pesticides including carbaryl and pirimicarb that their MRL is issued by “The Institute of Standards of Iran” and propoxur whic...
[ 41 ] - Design, Synthesis and Evaluation of Substituted Aryl-2-Nitrovinyl Derivatives as Small Molecules Proteasome Inhibitors
Based on the existing structure activity relationship for proteasome inhibitors, a number of substituted aryl-2-nitrovinyl derivatives have been synthesized as Michael acceptor and their cytotoxicity and proteasome inhibitory effects were evaluated on two cancer cell lines. Compound 2d exhibited IC50 values of 0.71 and 17.79 μM comparable to bortezomib against MCF-7 and PC-3, respectively. The ...
[ 42 ] - Clopidogrel Resistance and its Impact on Clinical Outcome of Iranian Patients Undergoing Percutaneous Coronary Intervention
The aim of current study was evaluating the frequency of clopidogrel resistance and its impact on clinical outcome of patients in Iranian patients. Patients undergoing percutaneous coronary intervention in Imam Hussein Medical center, Tehran, Iran, who received standard dosage of clopidogrel (Plavix®, Sanofi, France, 600 mg loading dose and 75 mg/day afterward) were recruited. Platelet aggregat...
[ 43 ] - The Effects of House Cooking Process on Residue Concentrations of 41 Multi-Class Pesticides in Rice
In current study, the effects of Iranian rice cooking method (Kateh) on residue levels of 41 pesticides were investigated. The pesticides were selected according to Iranian National Standards Organization (INSO) regulations and covered 18 permitted and 23 banned pesticides belonging to different chemical classes such as organophosphate, triazole, and carbamate. A 250 g portion of rice sample wa...
[ 44 ] - Exposure Assessment for Some Pesticides through Rice Consumption in Iran Using a Multiresidue Analysis by GC-MS
In communities which consume rice as main food, importance of risk assessment forcontaminants is always taken into consideration by health authorities. The present study isan attempt for monitoring of 56 pesticides from different chemical groups in rice samplescollected from local markets in Tehran and estimation of daily intake of interested pesticidesthrough this monitoring. A valid method ba...
[ 45 ] - RP-HPLC method development and validation for determination of eptifibatide acetate in bulk drug substance and pharmaceutical dosage forms
A new, rapid, economical and isocratic reverse phase high performance liquid chromatography (RP-HPLC) method was developed for the determination of eptifibatide acetate, a small synthetic antiplatelet peptide, in bulk drug substance and pharmaceutical dosage forms. The developed method was validated as per of ICH guidelines. The chromatographic separation was achieved isocratically on C18 colum...
[ 46 ] - Development of an analytical method for dibutyl phthalate determination using Surrogate analyte approach
Dibutyl phthalate (DBP) is a phthalic acid ester and is widely used in polymeric products to make them more flexible. DBP is found in almost every plastic material and is believed to be persistent in the environment. Various analytical methods have been used to measure DBP in different matrices. Considering the ubiquitous nature of DBP, the most important challenge in DBP analyses is the contam...
[ 47 ] - A Multi Residue GC-MS Method for Determination of 12 Pesticides in Cucumber
Cucumber is one of the main vegetables in Iranian food basket. A wide range of pesticides are used for crops protection during the cultivation of vegetables such as cucumber due to heavy pest infestation. Analysis of pesticide residues in food and other environmental commodities have become essential requirement for consumers, producers, and food quality control authorities. This study was aime...
[ 48 ] - Simultaneous Chloramphenicol and Florfenicol Determination by A Validated DLLME-HPLC-UV Method in Pasteurized Milk
The antibiotic residues in milk are a well-known serious problem and pose several health hazards to consumers. We have described a simple, rapid, and inexpensive DLLME-HPLC/UV technique for the extraction of chloramphenicol and florfenicol residues in milk samples. Under the optimum conditions, linearity of the method was observed over the range 0.02-0.85 µg/L with correlation coefficients > 0....
[ 49 ] - Validation of an Analytical Method for Determination of Benzo[a]pyrene Bread using QuEChERS Method by GC-MS
A fast and simple modified QuEChERS (quick, easy, cheap, rugged and safe) extraction method based on spiked calibration curves and direct sample introduction was developed for determination of benzo[a]pyrene (BaP) in bread by gas chromatography-mass spectrometry single quadrupole selected ion monitoring (GC/MS-SQ-SIM). Sample preparation includes extraction of BaP into acetone followed by clean...
[ 50 ] - Simultaneous Determination of 13 Priority Polycyclic Aromatic Hydrocarbons in Tehran’s Tap Water and Water for Injection Samples Using Dispersive Liquid-Liquid Micro Extraction Method and Gas Chromatography-Mass Spectrometry
Abstract Polycyclic aromatic hydrocarbons (PAHs) are classified as persistent and carcinogenic organic pollutants. PAHs contamination has been reported in water. Many of relevant regulatory bodies such as EU and EPA have regulated the limit levels for PAHs in drinking water. In this study, 13 priority polycyclic aromatic hydrocarbons (PAHs) were determined in tap water samples of Tehran and wat...
[ 51 ] - Triterpene Constituents of Euphorbia Erythradenia Bioss. and their Anti-HIV Activity
Phytochemical investigation of the aerial parts of Euphorbia erythradenia Bioss. (Euphorbiaceae), one of Iranian endemic Euphorbias, with particular attention to triterpene constituents, using methanol solvent extraction was carried out. Five known triterpenes, including four cycloartanes and oleanolic acid, were isolated for the first time and identified using NMR and Mass techniques. Anti HIV...
[ 52 ] - Synthesis and Antibacterial Activity of Novel Hydroxy Semicarbazone Derivatives
A series of hydroxysemicarbazone derivatives of substituted diaryl ketones and acetophenones were synthesized and their structures were confirmed by analytical and spectroscopic methods including elemental analysis, infrared and nuclear magnetic resonance spectroscopy. The derivatives were prepared by a condensation reaction between N-hydroxysemicarbazide and substituted diaryl ketones or aceto...
[ 53 ] - Determination of Benzo[a]pyrene in Traditional, Industrial and Semiindustrial Breads Using a Modified QuEChERS Extraction, Dispersive SPE and GC-MS and Estimation of its Dietary Intake.
A fast and simple modified QuEChERS extraction method was developed for determination of Benzo[a]pyrene (BaP) in 137 traditional (Sangak), semi-industrial (Sangak) and industrial bread samples using spiked calibration curves by GC/MS. Sample preparation includes extraction of BaP into acetone followed by cleanup with dispersive solid phase extraction. The limit of detection and limit of quantif...
[ 54 ] - Validation of an Analytical Method for Determination of 13 priority polycyclic aromatic hydrocarbons in mineral water using dispersive liquid-liquid microextraction and GC-MS
Dispersive liquid liquid microextraction (DLLME) combined with gas chromatography–mass spectrometry (GC–MS) was used for the extraction and determination of 13 polycyclic aromatic hydrocarbons (PAHs) in mineral water samples. In this procedure, the suitable combination of extraction solvent (500 µL chloroform) and disperser solvent (1000 µL acetone) were quickly injected into the water sample (...
[ 55 ] - FTIR Biospectroscopy Investigation on Cisplatin Cytotoxicity in Three Pairs of Sensitive and Resistant Cell Line
Fourier Transformed Infrared Spectroscopy (FTIR) has extensively been used for biological applications. Cisplatin is one the most useful antineoplastic chemotherapy drugs for a variety of different human cancers. One of the clinical problems in its application, which would consequently affect the therapeutic outcome of its application, is the occurrence of resistance to this agent. In this proj...
[ 56 ] - Evaluation of anti-platelet aggregation effect of some Allium species
Epidemiologic studies show that the cardiovascular diseases are associated with multiple factors such as raised serum total cholesterol, increased LDL, increased platelet aggregation, hypertension and smoking. In-vitro studies have confirmed the ability of some plants of Allium species to reduce these parameters. Therefore, we evaluated anti-platelet aggregation effect of some Allium species (A...
[ 57 ] - Development and Validation of a Micellar Capillary Electrophoresis Method for Determination of IFNβ-1b in Lyophilized Formulation of a Biosimilar Product
Human interferons (IFNs) are key cytokines secreted by immune system. They have several effects such as antiviral and anti tumors activity, activating immune cells and healing of multiple sclerosis. The type IFNs present in humans are α, β and Υ. IFN β is a polypeptide, normally produced by fibroblasts and seems to be more species-specific than IFN . Structural properties of I FNs are importan...
[ 58 ] - Synthesis and Antiplatelet Aggregation Activity Evaluation of some 2-Aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine Derivatives
A series of novel 2-aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine derivatives have been synthesized and their anti platelet aggregation activities were assessed against ADP and arachidonic acid- induced platelet aggregation in human plasma using light transmission aggregometry. None of the compounds showed satisfactory activity against the aggregation induced by ADP. However, satisfac...
[ 59 ] - Evaluation of Emerging Fusarium mycotoxins beauvericin, Enniatins, Fusaproliferin and Moniliformin in Domestic Rice in Iran
The occurrence of emerging Fusarium mycotoxins beauvericin (BEA), enniatins (ENNs) (A, A1, B, B1), Fusaproliferin and moniliformin was evaluated by a liquid chromatography/electrospray ionization-tandem mass spectrometric (LC/ESI-MS/MS) technique in 65 domestic rice samples produced in Gilan and Mazandaran Provinces in IR Iran. The results showed that 46% of the samples were contaminated with a...
[ 60 ] - Synthesis and Antimycobacterial Activity of some Triazole Derivatives–New Route to Functionalized Triazolopyridazines
A series of cyclic analogues of bioactive thiosemicarbazide derivatives have been synthesized as potential antimycobacterial agents. The 4-amino-1,2,4-triazole-5-thione analogues (Ia-f) were prepared by heating a mixture of thiocarbohydrzide and appropriate carboxylic acids. Reaction of thiocarbohydrazide with γ-ketoesters in the presence of sodium methoxide furnished triazolopyridazine derivat...
[ 61 ] - Design, Synthesis and Cytotoxicity Evaluationof New 1,2-diaryl-4, 5, 6, 7-Tetrahydro-1H-benzo[d] Imidazolesas Tubulin Inhibitors
A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxy phenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic h...
[ 62 ] - Synthesis and Preliminary Evaluation of a New 99mTc Labeled Substance P Analogue as a Potential Tumor Imaging Agent
Neurokinin 1 receptors (NK1R) are overexpressed on several types of important human cancer cells. Substance P (SP) is the most specific endogenous ligand known for NK1Rs. Accordingly, a new SP analogue was synthesized and evaluated for detection of NK1R positive tumors. [6-hydrazinopyridine-3-carboxylic acid (HYNIC)-Tyr8-Met(O)11-SP] was synthesized and radiolabeled with 99mTc using ethylenedia...
[ 63 ] - Method development for simultaneous determination of 41 pesticides in rice using LC-MS/MS technique and its application for the analysis of 60 rice samples collected from Tehran market
For the first time, a multi-residue methodfor simultaneous determination of 41LC-amenable pesticides in rice, belonging to different chemical classes has been developed in Iran by LC-MS/MS. The pesticides were analyzed simultaneously in a single run using positive electrospray ionization with multiple reaction monitoring (MRM) after extraction with slightly modified QuEChERS method. The calibra...
[ 64 ] - Phytochemical investigations on chemical constituents of Achillea tenuifolia Lam.
Achillea tenuifolia Lam (Asteraceae) afforded a methanolic extract from which after fractionation in solvents with different polarities two known flavones 3’, 5- dihydroxy- 4’, 6, 7- trimethoxy flavone (eupatorine, compound 3), 5- hydroxy- 3’, 4’, 6, 7- tetramethoxyflavone (compound 4), besides stearic acid (compound 1 ), lupeol (compound 2), daucosterol (β- sitosterol 3-O- β- D- glucopyranosid...
[ 65 ] - Synthesis of N-arylmethyl Substituted Indole Derivatives as New Antiplatelet Aggregation Agents
A number of N-arylmethyl substituted indole derivatives have been synthesized and their effectiveness against ADP and arachidonic acid induced platelet aggregation in human plasma was determined. The desired compounds were synthesized by reacting the appropriate aniline derivative with isatin (or substituted isatin) to form the corresponding imine structures. The so formed compound was then act...
[ 66 ] - Development and Validation of a Reversed-phase HPLC Method for Assay of the Decapeptide Cetrorelix Acetate in Bulk and Pharmaceutical Dosage Forms
A gradient reversed-phase high performance liquid chromatography (HPLC) method was developed for the assay of cetrorelix acetate, a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment. The HPLC method, which is used to determine cetrorelix in bulk and pharmaceutical dosage forms, was validated per ICH guidelines. The chromatograph...
[ 67 ] - Synthesis and Evaluation of New Fluorinated Anti-Tubercular Compounds
Treatment of tuberculosis (TB) and the discovery of effective new anti tubercular drugs is one of the most urgent priorities in health organizations all around the world. In the present study, fluorinated analogs of some of the most important anti-TB agents such as p-aminosalicylic acid (PAS), thiacetazone and pyrazinamide were synthesized and tested against TB. The fluorinated analog of thiace...
[ 68 ] - Simultaneous Determination of 17 Pesticide Residues in Rice by GC/MS using a Direct Sample Introduction Procedure and Spiked Calibration Curves
A reliable, rapid and accurate method based on spiked calibration curves and direct sample introduction was developed for determination of 17 pesticide residues in rice by gas chromatography-mass spectrometry single quadrupole selected ion monitoring GC/MS-SQ-SIM. Sample preparation is based on extraction with acetonitrile without clean up. The use of spiked calibration curves for constructing...
[ 69 ] - Synthesis and Antimycobacterial Activity of Symmetric Thiocarbohydrazone Derivatives against Mycobacterium bovis BCG
In this work, we reported the synthesis and evaluation of antimycobacterial and antifungalactivity of a series of thiocarbohydrazone derivatives which are thiacetazone congeners. Thetarget compounds were synthesized in superior yields by reacting thiocarbohydrazide withdifferent aromatic aldehydes and methyl ketones. Compounds 8, 19 and 25 were found to bethe most potent derivatives, exhibiting...
[ 70 ] - Development of a Simple RP-HPLC-UV Method for Determination of Azithromycin in Bulk and Pharmaceutical Dosage forms as an Alternative to the USP Method
The present study was designed to develop a simple, validated liquid chromatographic method for the analysis of azithromycin in bulk and pharmaceutical dosage forms using ultraviolet detector. The best stationary phase was determined as C18 column, 5 µm, 250 mm × 4.6 mm. Mobile phase was optimized to obtain a fast and selective separation of the drug. Flow rate was 1.5 mL/min, Wavelength was se...
[ 71 ] - Resistance to Clopidogrel among Iranian Patients Undergoing Angioplasty Intervention
To study the resistance to standard dosage of clopidogrel among Iranian patients following percutaneous coronary intervention measured by platelet aggregation test.Patients undergoing percutaneous coronary intervention in Imam Hussein Medical center, Tehran, Iran, who were under treatment with aspirin, but had no history of clopidogrel usage, entered the study. Patients received standard dosage...
[ 72 ] - Partial Fractionation of Venoms from Two Iranian Vipers, Echis carinatus and Cerastes persicus Fieldi and Evaluation of Their Antiplatelet Activity
Platelet aggregation inhibitory effect and anticoagulant properties of fractions separated from the venoms of Cerastes persicus fieldi and Echis carinatus were investigated. The partial fractionation was performed on a Sephadex G-100 column. Two fractions separated from Cerastes persicus fieldi showed anti platelet aggregation activity on ADP (200 µM)-induced platelet aggregation (ca 80% inhibi...
[ 73 ] - Synthesis and Cytotoxic Evaluation of Novel 3-Substituted Derivatives of 2-Indolinone
The assessment of the degree or rate of cellular proliferation and cell viability is critical for the assessment of the effects of drugs on both normal and malignant cell populations. In the present study, a few novel 3-substituted derivatives of 2-indolinones were synthesized by condensation of substituted oxindole or isatin derivatives with appropriate aldehydes or primary aromatic amine...
[ 74 ] - Evaluation of the Effect of PEGylated Single-Walled Carbon Nanotubes on Viability and Proliferation of Jurkat Cells
Among the numerous nanosized drug delivery systems currently under investigation, carbon nanotubes (CNTs), regardless of being single or multiple-walled, offer several advantages and are considered as promising candidates for drug targeting. Despite the valuable potentials of CNTs in drug delivery, their toxicity still remains an important issue. After the PEGylation of single-walled CNTs ...
[ 75 ] - A Rapid, Simple, Liquid Chromatographic-Electrospray Ionization, Ion Trap Mass Spectrometry Method for the Determination of Finasteride in Human Plasma and its Application to Pharmacokinetic Study
A fast, accurate, sensitive, selective and reliable method using reversed-phase high performance liquid chromatography coupled to electrospray ionization ion trap mass spectrometry was developed and validated for the determination of finasteride in human plasma. After protein precipitation with perchloric acid, satisfactory separation was achieved on a Zorbax Eclipse® C8 analytical column u...
[ 76 ] - A Simple Electrochemical Method for the Rapid Estimation of Antioxidant Potentials of Some Selected Medicinal Plants
Clinical and Epidemiological studies have shown that a diet rich in fruits and vegetables is associated with a decreased risk of cardiovascular diseases, cancers and other related disorders. These beneficial health effects have been attributed in part to the presence of antioxidants in dietary plants. Therefore screening for antioxidant properties of plant extracts has been one of the inte...
[ 77 ] - Application of Narrow-Bore HPLC Columns in Rapid Determination of Sildenafil Citrate in Its Pharmaceutical Dosage Forms
A special type of silica-based columns has been recently introduced into the market which is called narrow-bore columns. They have lower internal volume than the standard high-performance liquid chromatography (HPLC) columns and thus reduce the solvent consumption by almost 80%. A simple, accurate and environmentally friendly reversed phase- HPLC (RP-HPLC method) which could be used in ...
[ 78 ] - The Effect and Persistency of 1% Aluminum Chloride Hexahydrate Iontophoresis in the Treatment of Primary Palmar Hyperhidrosis
Topical solutions containing aluminum chloride are known to be the first line of therapy for hyperhidrosis. Palmar hyperhidrosis however, is less responsive to aluminum chloride therapy and successful treatment may require 6-8 h application of high concentrations up to 30% that commonly leads to skin irritation. The purpose of this study is to investigate the effect of 30 min iontophoretic appl...
[ 79 ] - Profiling of Ecstasy Tablets Seized in Iran
In this study 50 samples of ecstasy tablets seized in Iran during the period of 2007 through 2008 were examined and their physical characteristics (appearance, marking, scored/not scored, color, weight, diameter, thickness) were determined. In order to determine the chemical characteristics of these tablets, color tests (Marquis test, Simon’s test, Chen’s test and Gallic acid test), Thin Layer ...
[ 80 ] - Effect of Cooking Process on the Residues of Three Carbamate Pesticides in Rice
A gas chromatography mass spectrometry with spike calibration curve method was used to quantify three carbamate pesticides residue in cooked white rice and to estimate the reduction percentage of the cooking process duration. The selected pesticides are three carbamate pesticides including carbaryl and pirimicarb that their MRL is issued by “The Institute of Standards of Iran” and propoxur whic...
[ 81 ] - Development and Validation of a GC/MS Method for Simultaneous Determination of 7 Monoterpens in Two Commercial Pharmaceutical Dosage Forms
Terpenes are active constituents of many pharmaceutical dosage forms with naturalproducts origin. One of the challenges in developing dosage forms with herbal originis their standardization as pharmaceutical products. GC-Mass is the most decisive andreliable technique to fulfill the requirements in this regard. In the present study, a reliable,rapid, and accurate method was developed for determ...
[ 82 ] - Biosynthesis and characterization of biogenic tellurium nanoparticles by using Penicillium chrysogenum PTCC 5031: A novel approach in gold biotechnology
Production of nanoparticles has been attractive by biological based fabrication as an alternative to physical and chemical approaches due to exceeding need to develop safe, reliable, clean and eco-friendly methods for the preparation of nanoparticle for pharmaceutical and biomedical applications. In the present study, biogenic tellurium nanoparticles (TeNPs) were successfully prepared using pot...
[ 83 ] - Biological Evaluation of the Isolated Compounds from Methanol fraction of Leutea avicennia Mozaff.
Leutea avicenniae Mozaff. belongs to Apiaceae family is an endemic species distributed in the west of Iran. The aim of this study was to investigate the antioxidant activity and acetylcholinestrase (AchE) inhibition of the crude extract, fractions and isolated compounds from methanolic fraction of L. avicenniae. Five compounds were detected from methanol fraction, three phenolic compounds as p-...
[ 84 ] - Development and Validation of a GC/MS Method for Simultaneous Determination of 7 Monoterpens in Two Commercial Pharmaceutical Dosage Forms
Terpenes are active constituents of many pharmaceutical dosage forms with naturalproducts origin. One of the challenges in developing dosage forms with herbal originis their standardization as pharmaceutical products. GC-Mass is the most decisive andreliable technique to fulfill the requirements in this regard. In the present study, a reliable,rapid, and accurate method was developed for determ...
[ 85 ] - Biosynthesis and characterization of biogenic tellurium nanoparticles by using Penicillium chrysogenum PTCC 5031: A novel approach in gold biotechnology
Production of nanoparticles has been attractive by biological based fabrication as an alternative to physical and chemical approaches due to exceeding need to develop safe, reliable, clean and eco-friendly methods for the preparation of nanoparticle for pharmaceutical and biomedical applications. In the present study, biogenic tellurium nanoparticles (TeNPs) were successfully prepared using pot...
[ 86 ] - Biological Evaluation of the Isolated Compounds from Methanol fraction of Leutea avicennia Mozaff.
Leutea avicenniae Mozaff. belongs to Apiaceae family is an endemic species distributed in the west of Iran. The aim of this study was to investigate the antioxidant activity and acetylcholinestrase (AchE) inhibition of the crude extract, fractions and isolated compounds from methanolic fraction of L. avicenniae. Five compounds were detected from methanol fraction, three phenolic compounds as p-...
[ 87 ] - Simultaneous Determination of Isoniazid, Pyrazinamide and Rifampin in Human Plasma by High-performance Liquid Chromatography and UV Detection
Therapeutic Drug Monitoring (TDM) of first-line anti-tuberculosis (TB) drugs is a decisive tool, allowing the clinician to successfully treat TB patients. The objective of the study was to develop and optimize a simple, sensitive, and reliable high-performance liquid chromatography (HPLC) method for the simultaneous determination of isoniazid (INH), pyrazinamide (PZA), and rifampin (RIF) levels...
[ 88 ] - Fungus-mediated Extracellular Biosynthesis and Characterization of Zirconium Nanoparticles Using Standard Penicillium Species and Their Preliminary Bactericidal Potential: A Novel Biological Approach to Nanoparticle Synthesis
Biological synthesis of nanoparticles (NPs) has gained extensive attention during recent years by using various biological resources such as plant extracts and microorganisms as reducing and stabilizing agents. The objective of the present study was to biosynthesize zirconium NPs using Penicillium species as a reliable and eco-friendly protocol for the first time. The synthesized NPs w...
[ 89 ] - Simultaneous Determination of Isoniazid, Pyrazinamide and Rifampin in Human Plasma by High-performance Liquid Chromatography and UV Detection
Therapeutic Drug Monitoring (TDM) of first-line anti-tuberculosis (TB) drugs is a decisive tool, allowing the clinician to successfully treat TB patients. The objective of the study was to develop and optimize a simple, sensitive, and reliable high-performance liquid chromatography (HPLC) method for the simultaneous determination of isoniazid (INH), pyrazinamide (PZA), and rifampin (RIF) levels...
[ 90 ] - Fungus-mediated Extracellular Biosynthesis and Characterization of Zirconium Nanoparticles Using Standard Penicillium Species and Their Preliminary Bactericidal Potential: A Novel Biological Approach to Nanoparticle Synthesis
Biological synthesis of nanoparticles (NPs) has gained extensive attention during recent years by using various biological resources such as plant extracts and microorganisms as reducing and stabilizing agents. The objective of the present study was to biosynthesize zirconium NPs using Penicillium species as a reliable and eco-friendly protocol for the first time. The synthesized NPs w...
[ 91 ] - The Photothermal Effect of Targeted Methotrexate-Functionalized Multi-Walled Carbon Nanotubes on MCF7 Cells
Abstract Purpose: our goal is to reduce the release rate of methotrexate (MTX) and increase cell death efficiency. Methods: Carboxylated multi-walled carbon nanotubes (MWCNT-COOH) were functionalized with MTX as a cytotoxic agent, FA as a targeting moiety and polyethylene amine (PEI) as a hydrophilic agent. Ultimately, MWCNT-MTX and MWCNT-MTX-PEI-FA were synthesized. Methotrexate re...
[ 92 ] - The Photothermal Effect of Targeted Methotrexate-Functionalized Multi-Walled Carbon Nanotubes on MCF7 Cells
Abstract Purpose: our goal is to reduce the release rate of methotrexate (MTX) and increase cell death efficiency. Methods: Carboxylated multi-walled carbon nanotubes (MWCNT-COOH) were functionalized with MTX as a cytotoxic agent, FA as a targeting moiety and polyethylene amine (PEI) as a hydrophilic agent. Ultimately, MWCNT-MTX and MWCNT-MTX-PEI-FA were synthesized. Methotrexate re...
[ 93 ] - Validation and application of an analytical method for determination of Persistent Organic Pollutants in Rainbow trout (Onchorhynchus mykiss) collected from Tehran retail markets
Persistent organic pollutants are a wide group of toxic and dangerous compounds. These organic compounds are chemically and physically stable even beams. In this study an analysis method for simultaneous determination of 18 persistent organic pollutants including eleven Organochlorine pesticides (OCPs): HCB, Dieldrin, Methoxychlor, α-, ϒ-Chlordane, α-, β-Endosulfan and o,p’-DDE, p,p’-DDE, o,p’-...
[ 94 ] - Multivesicular liposome (DepoFoam) in human diseases
Drug development is a key point in the research of new therapeutic treatments for increasing maximum drug loading and prolonged drug effect. Encapsulation of drugs into multivesicular liposomes (DepoFoam) is a nanotechnology that allow deliver of the active constituent at a sufficient concentration during the entire treatment period. This guarantees the reduction of drug administration frequenc...
[ 95 ] - Novel Application of Near-infrared Spectroscopy and Chemometrics Approach for Detection of Lime Juice Adulteration
The aim of this study is to investigate the novel application of a handheld near infra-red spectrophotometer coupled with classification methodologies as a screening approach in detection of adulterated lime juices. For this purpose, a miniaturized near infra-red spectrophotometer (Tellspec®) in the spectral range of 900–1700 nm was used. Three diffuse reflectance spectra of 31 pure...
[ 96 ] - Multivesicular liposome (DepoFoam) in human diseases
Drug development is a key point in the research of new therapeutic treatments for increasing maximum drug loading and prolonged drug effect. Encapsulation of drugs into multivesicular liposomes (DepoFoam) is a nanotechnology that allow deliver of the active constituent at a sufficient concentration during the entire treatment period. This guarantees the reduction of drug administration frequenc...
[ 97 ] - Novel Application of Near-infrared Spectroscopy and Chemometrics Approach for Detection of Lime Juice Adulteration
The aim of this study is to investigate the novel application of a handheld near infra-red spectrophotometer coupled with classification methodologies as a screening approach in detection of adulterated lime juices. For this purpose, a miniaturized near infra-red spectrophotometer (Tellspec®) in the spectral range of 900–1700 nm was used. Three diffuse reflectance spectra of 31 pure...