Publications by authors named "Alieh Ameri"

22 Publications

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A review on function and side effects of systemic corticosteroids used in high-grade COVID-19 to prevent cytokine storms.

EXCLI J 2021 15;20:339-365. Epub 2021 Feb 15.

Department of Medicinal Chemistry, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

In December 2019, a cluster of pneumonia caused by a novel coronavirus (2019-nCoV), officially known as severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), emerged in Wuhan, Hubei province, China. Cytokine storm is an uncontrolled systemic inflammatory response resulting from the release of large amounts of pro-inflammatory cytokines and chemokines that occurs at phase 3 of viral infection. Such emergence led to the development of many clinical trials to discover efficient drugs and therapeutic protocols to fight with this single-stranded RNA virus. Corticosteroids suppress inflammation of the lungs during the cytokine storm, weaken immune responses, and inhibit the elimination of pathogen. For this reason, in COVID-19 corticosteroid therapy, systemic inhibition of inflammation is observed with a wide range of side effects. The present review discusses the effectiveness of the corticosteroid application in COVID-19 infection and the related side effects of these agents. In summary, a number of corticosteroids, including and especially methylprednisolone and dexamethasone, have demonstrated remarkable efficacy, particularly for COVID-19 patients who underwent mechanical ventilation.
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http://dx.doi.org/10.17179/excli2020-3196DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7975631PMC
February 2021

Bioactive anti-oxidative polycaprolactone/gelatin electrospun nanofibers containing selenium nanoparticles/vitamin E for wound dressing applications.

J Biomater Appl 2021 Mar 15:8853282211001359. Epub 2021 Mar 15.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

In this study, polycaprolactone/gelatin (PCL/GEL) electrospun nanofibers containing biogenic selenium nanoparticles (Se NPs) and Se NPs/vitamin E (VE) with average diameters of 397.8 nm and 279.5 nm, respectively (as determined by SEM inspection) were prepared and their effect on wound healing was evaluated using in-vivo studies. The energy dispersive X-ray (EDX) mapping, TEM micrograph, and FTIR spectra of the prepared nanofibers strongly demonstrated well entrapment of Se NPs and VE into scaffolds. An amount of 57% Se NPs and 43% VE were gradually released from PCL/GEL/Se NPs/VE scaffold after 4 days immersion in PBS solution (pH 7.4). The both PCL/GEL/Se NPs and PCL/GEL/Se NPs/VE scaffolds supported 3T3 cell proliferation and attachment as confirmed by MTT assay and SEM imaging. Complete re-epithelialization, low level of edema and inflammatory cells in coordination with high level of oriented collagens demonstrated the wound healing activity of PCL/GEL/Se NPs/VE. Besides, significant antioxidant efficacy of PCL/GEL/Se NPs and PCL/GEL/Se NPs/VE scaffolds was demonstrated according to GSH and MDA assays. To sum up, the prepared PCL/GEL/Se NPs/VE scaffold in the present study represented suitable healing effect on animal model which candidate it for further studies.
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http://dx.doi.org/10.1177/08853282211001359DOI Listing
March 2021

Mono- and bis-pyrazolophthalazines: Design, synthesis, cytotoxic activity, DNA/HSA binding and molecular docking studies.

Bioorg Med Chem 2021 01 24;30:115944. Epub 2020 Dec 24.

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Biomaterials Group, Pharmaceutical Sciences Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran 1417614411, Iran. Electronic address:

In an attempt to find new potent cytotoxic compounds, several mono- and bis-pyrazolophthalazines 4a-m and 6a-h were synthesized through an efficient, one-pot, three- and pseudo five-component synthetic approach. All derivatives were evaluated for their in vitro cytotoxic activities against four human cancer cell lines of A549, HepG2, MCF-7, and HT29. Compound 4e showed low toxicity against normal cell lines (MRC-5 and MCF 10A, IC > 200 µM) and excellent cytotoxic activity against A549 cell line with IC value of 1.25 ± 0.19 µM, which was 1.8 times more potent than doxorubicin (IC = 2.31 ± 0.13 µM). In addition, compound 6c exhibited remarkable cytotoxic activity against A549 and MCF-7 cell lines (IC = 1.35 ± 0.12 and 0.49 ± 0.01 µM, respectively), more than two-fold higher than that of doxorubicin. The binding properties of the best active mono- and bis-pyrazolophthalazine (4e and 6c) with HSA and DNA were fully evaluated by various techniques including UV-Vis absorption, circular dichroism (CD), Zeta potential and dynamic light scattering analyses indicating interaction of the compounds with the secondary structure of HSA and significant change of DNA conformation, presumably via a groove binding mechanism. Additionally, molecular docking and site-selective binding studies confirmed the fundamental interaction of compounds 4e and 6c with base pairs of DNA. Compounds 4e and 6c showed promising features to be considered as potential lead structures for further studies in cancer therapy.
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http://dx.doi.org/10.1016/j.bmc.2020.115944DOI Listing
January 2021

Lipase@zeolitic imidazolate framework ZIF-90: A highly stable and recyclable biocatalyst for the synthesis of fruity banana flavour.

Int J Biol Macromol 2021 Jan 6;166:1301-1311. Epub 2020 Nov 6.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box 14155-6451, Tehran 1417614411, Iran. Electronic address:

A zeolitic imidazolate framework (ZIF-90) has been synthesized through solvothermal method. The structure was characterized by means of FT-IR spectroscopy, X-ray diffraction, thermogravimetric analysis (TGA), and scanning electron microscopy (SEM)/energy dispersive X-ray spectroscopy (EDS). The synthesized ZIF-90 was applied as a support for immobilization of porcine pancreatic lipase (PPL). The immobilized enzyme (PPL@ZIF-90) exhibited immobilization yield and efficiency of 66 ± 1.8% and 89 ± 1.4%, respectively. The pH and thermal stability of PPL was improved after immobilization and the initial activity was retained at about 57% after 20 days of storage at 4 °C for PPL@ZIF-90. Moreover, about 57% of the original activity was remained following 10 cycles of application. In Michaelis-Menten kinetic studies, K value for PPL@ZIF-90 was lower, while, the V was higher than free PPL. Moreover, optimized conditions to produce fruity banana flavour upon esterification of butyric acid were investigated. The optimum esterification yield was 73.79 ± 1.31% in the presence of 245 mg PPL@ZIF-90, alcohol/acid ratio of 2.78 and 39 h reaction time. PPL@ZIF-90 showed 39% relative esterification yield after six cycles of reuse. The results suggested that PPL@ZIF-90 can be used as a potential effective biocatalyst for synthesis of isoamyl butyrate.
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http://dx.doi.org/10.1016/j.ijbiomac.2020.11.011DOI Listing
January 2021

Optimization of immobilization conditions of Bacillus atrophaeus FSHM2 lipase on maleic copolymer coated amine-modified graphene oxide nanosheets and its application for valeric acid esterification.

Int J Biol Macromol 2020 Nov 16;162:1790-1806. Epub 2020 Aug 16.

Pharmaceutical Sciences and Cosmetic Products Research Center, Kerman University of Medical Sciences, Kerman, Iran; Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran. Electronic address:

The thermoalkalophilic lipase from Bacillus atrophaeus (BaL) was immobilized onto amine-functionalized graphene oxide nanosheets coated with the poly (maleic anhydride-alt-1-octadecene) copolymer (GO-NH-PMAO) and activated with glutaraldehyde as spacer arm through interfacial activation and subsequent multipoint covalent attachment. Experimental design method was applied for optimization of immobilization conditions including GO-NH-PMAO concentration, buffer concentration, pH, sonication time, enzyme concentration, glutaraldehyde concentration, time, and temperature. The optimum specific activity of the immobilized BaL (105.95 ± 2.37 U/mg) reached at 5 mg/mL for GO-NH-PMAO, 25 mM of buffer, pH 6.0, 60 min sonication time, 100 mM glutaraldehyde, 60 U/mL of enzyme, and 4 h of immobilization time at 25 °C, which was very close to the predicted amount (106.08 ± 1.42 U/mg). Maximum immobilization yield (81.35%) and efficiency (277.63%) were determined in optimal immobilization conditions. The obtained results clearly indicated that the immobilized BaL exhibited better stability at extreme temperature and pH than the free BaL. At temperature of 90 °C and pH 11, more than 90% of the initial activity of the immobilized BaL was retained. Furthermore, the immobilized BaL retained about 90% of its initial activity after 10 days of storage and 6 cycles of application. The esterification studies showed that maximum bioconversion of valeric acid to pentyl valerate using the free BaL (34.5%) and the immobilized BaL (96.3%) occurred in the xylene medium after 48 h of incubation at 60 °C. Therefore, the BaL immobilized on GO-NH-PMAO was introduced as an effective biocatalyst to synthesize green apple flavour ester.
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http://dx.doi.org/10.1016/j.ijbiomac.2020.08.101DOI Listing
November 2020

Immobilization of Thermoalkalophilic Lipase from Bacillus atrophaeus FSHM2 on Amine-Modified Graphene Oxide Nanostructures: Statistical Optimization and Its Application for Pentyl Valerate Synthesis.

Appl Biochem Biotechnol 2020 Jun 10;191(2):579-604. Epub 2019 Dec 10.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

Synthesis of (3-aminopropyl) triethoxysilane (APTES)-functionalized graphene oxide (GO) nanosheets, statistical optimization of conditions for immobilization of Bacillus atrophaeus lipase (BaL) on as-synthesized support, and application of the immobilized BaL for esterification of valeric acid were carried out in this investigation. The optimum specific activity of the immobilized BaL (81.60 ± 0.28 U mg) was achieved at 3 mg mL of GO-NH, 50 mM of phosphate buffer, pH 7.0, 60 min sonication time, 100 mM glutaraldehyde, 25 U mL of enzyme, and 8 h immobilization time at 4 °C. The immobilized BaL retained about 90% of its initial activity after 10 days of storage. Moreover, about 70% of the initial activity of the immobilized BaL was retained after 10 cycles of application. The results of esterification studies exhibited that maximum pentyl valerate synthesis using the free BaL (34.5%) and the immobilized BaL (92.7%) occurred in the organic solvent medium (xylene) after 48 h of incubation at 60 °C.
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http://dx.doi.org/10.1007/s12010-019-03180-1DOI Listing
June 2020

Antioxidant, cytotoxic and hyperalgesia-suppressing activity of a native Shilajit obtained from Bahr Aseman mountains.

Pak J Pharm Sci 2019 Sep;32(5):2167-2173

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

Shilajit, a blackish-brown exudation obtained from steep rocks of different mountains, has been longly used as a therapeutic agent in traditional medicine. The present study was designed to evaluate the antioxidant, cytotoxic and hyperalgesia-suppressing activity of the aqueous and DMSO extracts of a native Shilajit. The antioxidant and cytotoxic effects of Shilajit extracts was determined using DPPH scavenging activity and MTT assay methods, respectively. In order to examine the hyperalgesia-suppressing activity of the Shilajit aqueous extract the STZ-induced diabetic animals were subjected to oral administration of the extract (50, 100 and 200 mg/kg daily) for six weeks followed by evaluating the behavioral examination (hot plate and tail flick tests) compared to those of diabetic control (Sham) and vehicle groups. The obtained results of antioxidant evaluation of Shilajit represented scavenging activity of 50% at concentration of 2500 μg/mL and 6000 μg/mL in the case of aqueous and DMSO extracts, respectively. Cytotoxic study of water extract of Shilajit revealed IC50 of 727.5±1.9 μg/mL and 1103±3.2 μg/mL on cell lines of MCF-7 (breast cancer) and A549 (lung cancer), respectively. Thermal pain response examination of diabetic rats treated with aqueous extract of Shilajit (100 mg/kg and 200 mg/kg) for six weeks reduced hyperalgesia compared to vehicle and Sham groups. To sum up, considering the moderate antioxidant and hyperalgesia-suppressing activity of this native Shilajit make it as a suitable candidate for further investigation after isolation and characterization of the active compounds.
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September 2019

LabSafety, the Pharmaceutical Laboratory Android Application, for Improving the Knowledge of Pharmacy Students.

Biochem Mol Biol Educ 2020 01 28;48(1):44-53. Epub 2019 Oct 28.

Modeling in Health Research Center, Institute for Futures Studies in Health, Kerman University of Medical Sciences, Kerman, Iran.

Currently, traditional paper methods may not effectively be used in education due to lack of access, outdated content, and poor graphics. Education through mobile-based applications is one of the alternative solutions. The objective of this study was to develop and evaluate LabSafety educational application and its effect on promoting the knowledge of pharmacy students. In this interventional study, the LabSafety application was first developed and evaluated for educating students about the safety measures in laboratories. Then, all pharmacy students from Kerman University of Medical Sciences (n = 316) were selected and randomly enrolled into one of three groups using simple random sampling: control (n = 106), traditional (n = 105), and application (n = 105) groups. To assess students' knowledge before and after the intervention, two valid and reliable (Cronbach's Alpha = 0.94 and 0.93, respectively) questionnaires were used. The results of the study showed no significant differences among the mean scores of the participants' knowledge before intervention (p = 0.82). After the intervention, the mean scores of the application group were 5.52 higher than the scores of the traditional group and 7.3 higher than the scores of the control group (p < 0.0001). Age had no significant effect on the posttest scores of the participants (p = 0.52). As a result, the use of this educational application can effectively increase the knowledge of all age groups of pharmacy students regarding safety measures in pharmaceutical laboratories. The mobile-based applications with online and offline access, interactive features, and user-friendly interfaces are more engaging and they can be used complementary to traditional training methods. © 2019 International Union of Biochemistry and Molecular Biology, 48(1):44-53, 2020.
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http://dx.doi.org/10.1002/bmb.21311DOI Listing
January 2020

New classes of carbazoles as potential multi-functional anti-Alzheimer's agents.

Bioorg Chem 2019 10 29;91:103164. Epub 2019 Jul 29.

The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, 1417614411, Iran. Electronic address:

Multi-Target approach is particularly promising way to drug discovery against Alzheimer's disease. In the present study, we synthesized a series of compounds comprising the carbazole backbone linked to the benzyl piperazine, benzyl piperidine, pyridine, quinoline, or isoquinoline moiety through an aliphatic linker and evaluated as cholinesterase inhibitors. The synthesized compounds showed IC values of 0.11-36.5 µM and 0.02-98.6 µM against acetyl- and butyrylcholinesterase (AChE and BuChE), respectively. The ligand-protein docking simulations and kinetic studies revealed that compound 3s could bind effectively to the peripheral anionic binding site (PAS) and anionic site of the enzyme with mixed-type inhibition. Compound 3s was the most potent compound against AChE and BuChE and showed acceptable inhibition potency for self- and AChE-induced Aβ aggregation. Moreover, compound 3s could significantly protect PC12 cells against HO-induced toxicity. The results suggested that the compounds 3s could be considered as a promising multi-functional agent for further drug discovery development against Alzheimer's disease.
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http://dx.doi.org/10.1016/j.bioorg.2019.103164DOI Listing
October 2019

3-Aryl Coumarin Derivatives Bearing Aminoalkoxy Moiety as Multi-Target-Directed Ligands against Alzheimer's Disease.

Chem Biodivers 2019 May 8;16(5):e1800436. Epub 2019 Apr 8.

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, 14176, Iran.

Two series of novel coumarin derivatives, substituted at 3 and 7 positions with aminoalkoxy groups, are synthesized, characterized, and screened. The effect of amine substituents and the length of cross-linker are investigated in acetyl- and butyrylcholinesterase (AChE and BuChE) inhibition. Target compounds show moderate to potent inhibitory activities against AChE and BuChE. 3-(3,4-Dichlorophenyl)-7-[4-(diethylamino)butoxy]-2H-chromen-2-one (4y) is identified as the most potent compound against AChE (IC =0.27 μm). Kinetic and molecular modeling studies affirmed that compound 4y works in a mixed-type way and interacts simultaneously with the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. In addition, compound 4y blocks β-amyloid (Aβ) self-aggregation with a ratio of 44.11 % at 100 μm and significantly protects PC12 cells from H O -damage in a dose-dependent manner.
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http://dx.doi.org/10.1002/cbdv.201800436DOI Listing
May 2019

Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds.

Eur J Med Chem 2018 May 2;152:600-614. Epub 2018 May 2.

Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. Electronic address:

A novel series of coumarin-lipoic acid conjugates were synthesized via cycloaddition click reaction to find out new multi-target-directed ligands (MTDLs) for treatment of Alzheimer's disease (AD). All of synthesized compounds were screened for neuroprotective and anti-cholinesterase activities. Based on primary screening, two compounds (5 and 11) were subjected to further biological evaluations. In particular, compound 11 which was the most potent AChE inhibitor showed good inhibitory effect on Aβ-aggregation and intracellular ROS (reactive oxygen species) formation, as well as the ability of selective bio-metal chelation and neuroprotection against HO- and Aβ-induced cytotoxicity. In the light of these results, the applied hybridization approach introduced new promising lead compound with desired multifunctional properties, being useful in the treatment of Alzheimer's disease.
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http://dx.doi.org/10.1016/j.ejmech.2018.04.058DOI Listing
May 2018

Hybrid Pharmacophore Design, Molecular Docking, Synthesis, and Biological Evaluation of Novel Aldimine-Type Schiff Base Derivatives as Tubulin Polymerization Inhibitor.

Chem Biodivers 2018 Mar 7;15(3):e1700518. Epub 2018 Mar 7.

Department of Medicinal Chemistry, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran.

A series of hybrid aldimine-type Schiff base derivatives including trimethoxyphenyl ring and 1,2,4-triazole-3-thiol/thione were designed as tubulin inhibitors. The molecular docking simulations on tubulin complex (PDB: 1SA0) revealed that derivatives with nitro and/or chloro or dimethylamino substitutes (4-nitro, 2-nitro, 3-nitro, 4-Cl-3-nitro, and 4-Me N) on the aldehyde ring were the best compounds with remarkable binding energies (-9.09, -9.07, -8.63, -8.11, and -8.07 kcal mol , respectively) compared to colchicine (-8.12 kcal mol ). These compounds were also showed remarkable binding energies from -10.66 to -9.79 and -10.12 to -8.95 kcal mol on human (PDB: 1PD8) and Candida albicans (PDB: 3QLS) DHFR, respectively. The obtained results of cytotoxic activities against HT1080, HepG2, HT29, MCF-7, and A549 cancer cell lines indicated that 4-nitro and 2-nitro substituted compounds were the most effective agents by mean IC values of 11.84 ± 1.01 and 19.92 ± 1.36 μm, respectively. 4-Nitro substituted compound (5 μm) and 2-nitro substituted compound (30 μm) were able to strongly inhibit the tubulin polymerization compared to colchicine (5 μm) and 4-nitro substituted compound displayed IC values of 0.16 ± 0.01 μm compared to that of colchicine (0.19 ± 0.01 μm). This compound also showed the lowest MIC values on all tested microbial strains including three Gram-positive, four Gram-negative, and three yeast pathogens.
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http://dx.doi.org/10.1002/cbdv.201700518DOI Listing
March 2018

Probiotic and antioxidant properties of selenium-enriched Lactobacillus brevis LSe isolated from an Iranian traditional dairy product.

J Trace Elem Med Biol 2017 Mar 23;40:1-9. Epub 2016 Nov 23.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran. Electronic address:

The present study was designed to isolate a highly selenium-tolerant lactobacillus strain from an Iranian traditional dairy product named as Spar. Different criteria such as tolerance to the low pH, simulated gastric juice (SGJ), simulated intestinal juice (SIJ) and bile salts tolerance as well as Caco-2 cell adhesion assay were examined to evaluate the probiotic potentials of the selected isolate. Furthermore, the antioxidant properties of the isolate cultivated in medium containing and free of SeO ions were evaluated using DPPH scavenging and reducing power assays. The isolate was identified using conventional identification and 16S rDNA gene sequencing methods as Lactobacillus brevis LSe. The obtained results showed that the isolate was able to tolerate high concentration of sodium selenite (3.16mM). By decreasing the pH of the SGJ from 6 to 3, the survival percent of L. brevis LSe was not significantly changed over the time (p>0.05). In addition, the survival percent of the isolate in the SIJ (pH 6 and pH 8) was not statistically altered after 3h, 6h and 24h of incubation (p>0.05). In the presence of bile salts (0.3% and 0.6%) the survival rate of L. brevis LSe was not significantly decreased (p>0.05).L. brevis LSe also demonstrated the satisfactory ability to adhere to Caco-2 cells which were similar to that of the reference strain L. plantarum. The obtained results of antioxidant evaluation showed that L. brevis LSe containing elemental Se exhibited significantly higher radical scavenging ability (36.5±1.31%) and reducing power (OD, 0.14) than L. brevis LSe cultured in selenite-free medium (p<0.05). To sum up, further investigations should be conducted to merit the probable potential health benefit of Se-enriched L. brevis LSe and its application as Se-containing supplements or fermented foods.
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http://dx.doi.org/10.1016/j.jtemb.2016.11.013DOI Listing
March 2017

Synthesis and structure-activity relationship study of tacrine-based pyrano[2,3-c]pyrazoles targeting AChE/BuChE and 15-LOX.

Eur J Med Chem 2016 Nov 21;123:298-308. Epub 2016 Jul 21.

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14176, Iran. Electronic address:

A series of tacrine-based pyrazolo[4',3':5,6]pyrano[2,3-b]quinolines and related compounds were designed and synthesized for targeting AChE, BuChE and 15-LOX enzymes in the field of Alzheimer's disease therapy. Most of compounds showed potent activity against cholinesterases and mild potency toward 15-LOX enzyme. In particular, compounds 29, 32 and 40 displayed inhibition at nano-molar level against AChE and BuChE (IC50s = 0.005-0.08 μM), being more potent than reference drug tacrine. Moreover, compound 32 with IC50 value of 31 μM was the most potent compound against 15-LOX. The cytotoxicity assay on HepG2 cells revealed that compounds 29 and 32 showed no significant cytotoxic activity even at concentration of 50 μM. The cytotoxicity of compounds 29 and 32 was significantly less than that of tacrine at higher concentrations.
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http://dx.doi.org/10.1016/j.ejmech.2016.07.043DOI Listing
November 2016

Novel Aldimine-Type Schiff Bases of 4-Amino-5-[(3,4,5-trimethoxyphenyl)methyl]-1,2,4-triazole-3-thione/thiol: Docking Study, Synthesis, Biological Evaluation, and Anti-Tubulin Activity.

Arch Pharm (Weinheim) 2016 Aug 19;349(8):662-81. Epub 2016 Jun 19.

Department of Medicinal Chemistry, Faculty of Pharmacy, Isfahan University of Medical Sciences, Isfahan, Iran.

The present study was planned to design some novel aldimine-type Schiff bases bearing 3,4,5-trimethoxyphenyl and 1,2,4-triazole-3-thione/thiol as potential tubulin polymerization inhibitors. The obtained results of the molecular docking study using the tubulin complex (PDB code: 1SA0) showed that compounds H-25 and H-26 were well fitted in the colchicine binding site of tubulin with binding energies of -8.68 and -8.40 kcal/mol, respectively, in comparison to the main ligand (-8.20 kcal/mol). In parallel, molecular simulations were also performed on five other 3,4,5-trimethoxyphenyl-containing ligand targets including hsp90, VEGFR2, and human and microbial (Staphylococcus aureus and Candida albicans) dihydrofolate reductase, among which H-17, H-45, H-27, H-02, and H-19 were the most suitable compounds, respectively. Evaluation of the cytotoxic effect of the most efficient compounds of the docking steps (H-25) revealed IC50 values of 12.48 ± 1.10, 4.25 ± 0.22, 3.33 ± 0.31, and 9.71 ± 0.75 µM against the HT1080, HT29, MCF-7, and A549 cell lines, respectively, compared to doxorubicin (12.69 ± 1.23, 6.12 ± 0.47, 3.51 ± 0.32, and 6.40 ± 0.31 µM, respectively). The in vitro tubulin polymerization investigation launched compounds H-25 and H-26 as potent antitubulin agents due to their IC50 values of 0.17 ± 0.01 and 10.93 ± 0.43 µM, respectively.
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http://dx.doi.org/10.1002/ardp.201600021DOI Listing
August 2016

Studies on the laccase-mediated decolorization, kinetic, and microtoxicity of some synthetic azo dyes.

J Environ Health Sci Eng 2016 13;14. Epub 2016 May 13.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, P.O. Box 14155-6451, Tehran, 1417614411 Iran.

Background: Enzymatic elimination of synthetic dyes, one of the most environmentally hazardous chemicals, has gained a great interest during the two last decades. The present study was performed to evaluate the decolorization and detoxification potential of the purified laccase of Paraconiothyrium variabile in both non-assisted and hydroxybenzotriazole-aided form against six azo dyes.

Results: The obtained results showed that Acid Orange 67, Disperse Yellow 79, Basic Yellow 28, Basic Red 18, Direct Yellow 107, and Direct Black 166 were decolorized up to 65.3, 53.3, 46.7, 40.7, 34, and 26.2 %, respectively, after 1 h treatment with laccase (0.5 U/mL). Addition of HBT up to 5 mM enhanced decolorization percent of all the investigated dyes. The results of kinetic study introduced the monoazo dye of Acid Orange 67 as the most suitable substrate for laccase with K m of 0.49 mM and V max of 189 mmol/min/mg. Evaluation the toxic effect of laccase-treated dye sample based on the growth inhibition of standard bacterial strains revealed decrease in toxicity of all applied dyes after treatment by laccase.

Conclusions: Application of the P. variabile laccase as biocatalyst efficiently decreased the toxicity of all studied synthetic azo dyes.
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http://dx.doi.org/10.1186/s40201-016-0248-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4866392PMC
May 2016

Laccase-catalyzed decolorization and detoxification of Acid Blue 92: statistical optimization, microtoxicity, kinetics, and energetics.

J Environ Health Sci Eng 2015 16;13:31. Epub 2015 Apr 16.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, P.O. Box 14155-6451, Tehran, 1417614411 Iran ; Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 1417614411 Iran.

Background: In recent years, enzymatic-assisted removal of hazardous dyes has been considered as an alternative and eco-friendly method compared to those of physicochemical techniques. The present study was designed in order to obtain the optimal condition for laccase-mediated (purified from the ascomycete Paraconiothyrium variabile) decolorization of Acid Blue 92; a monoazo dye, using response surface methodology (RSM). So, a D-optimal design with three variables, including pH, enzyme activity, and dye concentration, was applied to optimize the decolorization process. In addition, the kinetic and energetic parameters of the above mentioned enzymatic removal of Acid Blue 92 was investigated.

Results: Decolorization of Acid Blue 92 was maximally (94.1% ± 2.61) occurred at pH 8.0, laccase activity of 2.5 U/mL, and dye concentration of 75 mg/mL. The obtained results of kinetic and energetic studies introduced the laccase-catalyzed decolorization of Acid Blue 92 as an endothermic reaction (Ea, 39 kJ/mol; ΔS, 131 J/mol K; and ΔH, 40 kJ/mol) with K m and V max values of 0.48 mM and 227 mM/min mg, respectively. Furthermore, the results of microtoxicity study revealed that the toxicity of laccase-treated dye was significantly reduced compared to the untreated dye.

Conclusions: To sum up, the present investigation introduced the Paraconiothyrium variabile laccase as an efficient biocatalyst for decolorization of synthetic dye Acid Blue 92.
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http://dx.doi.org/10.1186/s40201-015-0183-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407540PMC
April 2015

Preparation and evaluation of the effect of Fe3 O4 @piroctone olamine magnetic nanoparticles on matrix metalloproteinase-2: a preliminary in vitro study.

Biotechnol Appl Biochem 2014 Nov-Dec;61(6):676-82

Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman, Iran.

In the present study, Fe3 O4 magnetic nanoparticles were synthesized by the coprecipitation of Fe(2+) and Fe(3+) ions and used as a nanocarrier for the production of piroctone-olamine-loaded Fe3 O4 nanoparticles (Fe3 O4 @PO NPs). The nanocrystalline structure of the prepared iron oxide species was confirmed by the X-ray diffraction spectroscopy method. Particle size distribution analysis showed that the size of Fe3 O4 @PO NPs was in the range of 5-55 nm. The magnetization curve of Fe3 O4 @PO NPs (with saturation magnetization of 28.2 emu/g) confirmed its ferromagnetic property. Loading of PO on the surface of Fe3 O4 NPs qualitatively verified by Fourier transform infrared spectrum obtained from Fe3 O4 @PO NPs. Cytotoxicity studies on the human fibrosarcoma cell line (HT-1080) revealed higher inhibitory effect of Fe3 O4 @PO NPs (50% cell death [IC50 ] of 8.1 µg/mL) as compared with Fe3 O4 NPs (IC50 of 117.1 µg/mL) and PO (IC50 of 71.2 µg/mL) alone. In the case of human normal fibroblast (Hs68), the viability percentage was found to be 75% in the presence of Fe3 O4 @PO NPs (120 µg/mL). Gelatin zymography showed 17.2% and 34.6% inhibition of matrix metalloproteinase-2 (MMP-2) in the presence of Fe3 O4 @PO and PO, respectively, at the same concentration of 40 µg/mL, whereas Fe3 O4 NPs did not inhibit MMP-2 at any concentration.
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http://dx.doi.org/10.1002/bab.1231DOI Listing
August 2015

One-pot, four-component synthesis of novel cytotoxic agents 1-(5-aryl-1,3,4-oxadiazol-2-yl)-1-(1H-pyrrol-2-yl)methanamines.

Eur J Med Chem 2014 May 16;78:151-6. Epub 2014 Mar 16.

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14176, Iran. Electronic address:

A series of N-benzyl-1-(5-aryl-1,3,4-oxadiazol-2-yl)-1-(1H-pyrrol-2-yl)methanamines were synthesized via one-pot reaction of appropriate benzylamine, pyrrole-2-carbaldehyde, (N-isocyanimino)triphenylphosphorane, and a carboxylic acid. The anti-tumor potential of title compounds was tested against several cancer cell lines by using MTT assay. Some tested compounds including 5e, 5p and 5q exhibited comparable or better cytotoxic activity against A549, HT29 or HT1080 cells in comparison to the reference drug doxorubicin. Also, the cytotoxic activity of compounds 5d and 5n against MCF-7 was better than that of doxorubicin. Compound 5n with IC50 value of 4.3 μM was 4-fold more potent than doxorubicin. The structure-activity relationship study revealed that the introduction of halogen atoms on both 5-phenyl ring and N-benzyl part improved the cytotoxic activity against all tested cell lines.
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http://dx.doi.org/10.1016/j.ejmech.2014.03.049DOI Listing
May 2014

Synthetic dye decolorization by three sources of fungal laccase.

Iranian J Environ Health Sci Eng 2012 Dec 15;9(1):27. Epub 2012 Dec 15.

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, P,O, Box 14155-6451, Tehran, 14174, Iran.

Decolorization of six synthetic dyes using three sources of fungal laccase with the origin of Aspergillus oryzae, Trametes versicolor, and Paraconiothyrium variabile was investigated. Among them, the enzyme from P. variabile was the most efficient which decolorized bromophenol blue (100%), commassie brilliant blue (91%), panseu-S (56%), Rimazol brilliant blue R (RBBR; 47%), Congo red (18.5%), and methylene blue (21.3%) after 3 h incubation in presence of hydroxybenzotriazole (HBT; 5 mM) as the laccase mediator. It was also observed that decolorization efficiency of all dyes was enhanced by increasing of HBT concentration from 0.1 mM to 5 mM. Laccase from A. oryzae was able to remove 53% of methylene blue and 26% of RBBR after 30 min incubation in absence of HBT, but the enzyme could not efficiently decolorize other dyes even in presence of 5 mM of HBT. In the case of laccase from T. versicolor, only RBBR was decolorized (93%) in absence of HBT after 3 h incubation.
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http://dx.doi.org/10.1186/1735-2746-9-27DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3564790PMC
December 2012

Antimicrobial activity of Bacillus sp. strain FAS1 isolated from soil.

Pak J Pharm Sci 2011 Jul;24(3):269-75

Faculty of Pharmacy and Pharmaceutical Research Center, Kerman University of Medical Sciences, Kerman, Iran.

During screening for antibiotic producing microorganisms from environmental soil samples, the supernatant of a bacterial isolate was found to have antibacterial and antifungal activity on the standard indicator species. The standard cylinder-plate method was used to determine the inhibitory effect of the crude supernatant of each isolate on 6 bacterial and 3 fungal standard strains by measuring the diameter of inhibition zone. The highest inhibition zone on Aspergillus niger belonged to culture broth of isolate FAS1 by 25 mm, and this isolate was the most efficient microorganism to inhibit standard bacterial and fungal species. Based on morphological and biochemical properties as well as 16S rDNA gene analysis, the selected isolate (isolate FAS(1)) belonged to Bacillus genus. Investigation on the ability of different culture media for antibiotic production led to select Luria-Bertani media for further studies. Treatment of the culture broth of the isolate FAS(1) using typical protease didn't decrease the antimicrobial activity of the supernatant. After extracting of culture broth of the selected isolate by ethyl acetate as an organic solvent, the inhibitory effect was mainly increased. More investigation was done by bioautography method where the ethyl acetate fraction of the broth culture was separated on TLC by chloroform:methanol, 60:40 as mobile phase and R(f) were calculated for inhibition spots.
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July 2011

Bioassay screening of the essential oil and various extracts from 4 spices medicinal plants.

Pak J Pharm Sci 2009 Jul;22(3):317-22

Department of Pharmacognosy, Pharmaceutical Research Center, School of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

Four commonly used spices plants in Iran were evaluated for cytotoxicity effect using Brine Shrimp Lethality (BSL) assay. Essential oils and various extracts of Heracleum persicum, Nigella arvensis, Cinnamomum zeylanicum and Zingiber officinale were assessed by two methods of disk and solution of BSL. Data were processed in probit-analysis program to estimate LC50 values. All of the tested fractions have exhibited more cytotoxicity in the solution method. Essential oils of H. persicum and C. zeylanicum have shown the most cytotoxicity with LC50 values 0.007 and 0.03 microg/ml respectively. None of aqueous extracts showed significant cytotoxicity. The analysis of the essential oil of H. persicum showed the hexyl butyrate and octyl acetate as the main compounds. These results suggest some limitation for using of these spices in diet. Furthermore, these plants could be considered as a source of cytotoxic compounds which might be studied in more details.
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July 2009