Publications by authors named "Bagher Amirheidari"

10 Publications

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In silico and in vitro inhibitory potential of an organometallic Cu (II) complex on Leishmania major stages.

Ann Parasitol 2021 ;67(1):45-54

Leishmaniasis Research Center, Kerman University of Medical Sciences, Kerman, Iran.

Leishmaniosis results in a serious complication, principally in the tropical and subtropical areas. Metalcored complexes, like meglumine antimoniate (MA) have proven antileishmanial activity. Similarly, in this research, we investigated the effects of Cu (II) dimethoxy bipyridine (CuDMOBP) against Leishmania major stages in silico and in vitro. Molecular docking analysis was carried out on the complex and a protozoan metacaspase. The complex's antipromastigote and its cytotoxicity towards macrophages were assayed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method to calculate relative Inhibitory Concentration 50% (IC50), Cytotoxic Concentration 50% (CC50), and Selectivity Index (SI). Expression of TNF-α and IL-10 in intracellular amastigotes and induction of apoptosis was also investigated using quantitative real-time PCR. The complex interacted effectively with four amino acid residues including lysine (Lys171), histidine (His193), arginine (Arg44 and Arg243) of the targeted metacaspase. This indicates a potential affinity between the target macromolecule and the complex. MTT results showed significant in vitro inhibitory effects against promastigotes. Reduction in cellular expression of IL-10 and TNF-α was also significant, p<0.05 and p<0.005, respectively. CuDMOBP showed powerful in vitro anti-leishmanial activity and could be introduced as a new leishmanicidal candidate.
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http://dx.doi.org/10.17420/ap6701.311DOI Listing
May 2021

Optimization of immobilization of lipase on multiwalled carbon nanotubes functionalized with glycyrrhizin and Tween 80.

3 Biotech 2021 Jun 10;11(6):260. Epub 2021 May 10.

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

In the present study, multiwalled carbon nanotubes (MWCNTs) were functionalized with glycyrrhizin and Tween 80 and applied for immobilization of lipase (L). Characterization of f-MWCNTs was performed through Fourier-transform infrared spectroscopy, thermal gravimetric, field emission scanning electron microscopy, and energy-dispersive X-ray spectroscopy analysis. The optimum specific activity of immobilized L (studied by Plackett-Burman statistical design) occurred at 0.3 mg/mL of f-MWCNTs, 25 mM of phosphate buffer (pH 6.0), 15 min sonication time, 8 U/mL of enzyme concentration, and 24 h immobilization time at 4 °C in the absence of glutaraldehyde. In these conditions, the specific activity was 16.57 ± 0.71 U/mg, which was very close to the predicted amount (16.62 ± 0.64 U/mg). The results of thermal and pH stability showed that the stability of immobilized L was higher than that of the free L. The activity of immobilized L on f-MWCNTs held 93% after being incubated for 60 min at 70 °C. Moreover, the immobilized L on f-MWCNTs retained about 65% of its initial activity after 30 days of storage at 25 °C. In addition, about 50% of initial activity of immobilized L retained after 10 cycles of uses. Therefore, f-MWCNTs could be introduced as suitable support for enzymes immobilization.
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http://dx.doi.org/10.1007/s13205-021-02813-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8110682PMC
June 2021

Socialization During the COVID-19 Pandemic: The Role of Social and Scientific Networks During Social Distancing.

Adv Exp Med Biol 2021 ;1318:911-921

Herbal and Traditional Medicines Research Center, Kerman University of Medical Sciences, Kerman, Iran.

In the COVID-19 era, while we are encouraged to be physically far away from each other, social and scientific networking is needed more than ever. The dire consequences of social distancing can be diminished by social networking. Social media, a quintessential component of social networking, facilitates the dissemination of reliable information and fighting against misinformation by health authorities. Distance learning, telemedicine, and telehealth are among the most prominent applications of networking during this pandemic. Additionally, the COVID-19 pandemic highlights the importance of collaborative scientific efforts. In this chapter, we summarize the advantages of harnessing both social and scientific networking in minimizing the harms of this pandemic. We also discuss the extra collaborative measures we can take in our fight against COVID-19, particularly in the scientific field.
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http://dx.doi.org/10.1007/978-3-030-63761-3_51DOI Listing
May 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

Design, synthesis, biological evaluation, and molecular dynamics of novel cholinesterase inhibitors as anti-Alzheimer's agents.

Arch Pharm (Weinheim) 2019 Jul 28;352(7):e1800352. Epub 2019 May 28.

Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutics Research Center, Kerman University of Medical Sciences, Kerman, Iran.

A series of novel chroman-4-one derivatives were designed and synthesized successfully with good to excellent yield (3a-l). In addition, the obtained products were evaluated for their cholinesterase (ChE) inhibitory activities. The results show that among the various synthesized compounds, analogs bearing the piperidinyl ethoxy side chain with 4-hydroxybenzylidene on the 3-positions of chroman-4-one (3l) showed the most potent activity with respect to acetylcholinesterase (anti-AChE activity; IC  = 1.18 μM). In addition, the structure-activity relationship was studied and the results revealed that the electron-donating groups on the aryl ring of the 3-benzylidene fragment (3k, 3l) resulted in the designed compounds to be more potent ChE inhibitors in comparison with those having electron-withdrawing groups (3h). In this category, the strongest ChE inhibition was found for the compound containing piperidine as cyclic amine, and a hydroxyl group (for AChE, compound 3l) and fluoro group (for butyrylcholinesterase (BuChE, compound 3i) on the para-position of the aryl ring of the benzylidene group. The molecular docking and dynamics studies of the most potent compounds (3i and 3l against BuChE and AChE, respectively) demonstrated remarkable interactions with the binding pockets of the ChE enzymes and confirmed the results obtained through in vitro experiments.
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http://dx.doi.org/10.1002/ardp.201800352DOI Listing
July 2019

Tris-chelated complexes of nickel(II) with bipyridine derivatives: DNA binding and cleavage, BSA binding, molecular docking, and cytotoxicity.

J Biomol Struct Dyn 2019 09 5;37(15):3887-3904. Epub 2019 Feb 5.

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

Two nickel(II) complexes with substituted bipyridine ligand of the type [Ni(NN)](ClO), where NN is 4,4'-dimethyl-2,2'-bipyridine (dimethylbpy) () and 4,4'-dimethoxy-2,2'-bipyridine (dimethoxybpy) (), have been synthesized, characterized, and their interaction with DNA and bovine serum albumin (BSA) studied by different physical methods. X-ray crystal structure of shows a six-coordinate complex in a distorted octahedral geometry. DNA-binding studies of and reveal that both complexes sit in DNA groove and then interact with neighboring nucleotides differently; undergoes a partial intercalation. This is supported by molecular-docking studies, where hydrophobic interactions are apparent between and DNA as compared to hydrogen bonding, hydrophobic, and interactions between and DNA minor groove. Moreover, the two complexes exhibit oxidative cleavage of supercoiled plasmid DNA in the presence of hydrogen peroxide as an activator in the order of >. In terms of interaction with BSA, the results of spectroscopic methods and molecular docking show that binds with BSA only via hydrophobic contacts while interacts through hydrophobic and hydrogen bonding. It has been extensively demonstrated that the nature of the methyl- and methoxy-groups in ligands is a strong determinant of the bioactivity of nickel(II) complexes. This may justify the above differences in biomolecular interactions. In addition, the cytotoxicity of the complexes on human carcinoma cells lines (MCF-7, HT-29, and U-87) has been examined by MTT assay. According to our observations, and display cytotoxicity activity against selected cell lines. Communicated by Ramaswamy H. Sarma.
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http://dx.doi.org/10.1080/07391102.2018.1534700DOI Listing
September 2019

Mancozeb induces testicular dysfunction through oxidative stress and apoptosis: Protective role of N-acetylcysteine antioxidant.

Toxicol Ind Health 2018 Nov 23;34(11):798-811. Epub 2018 Jul 23.

6 Department of Biotechnology, School of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

Mancozeb (MZB) is one of the fungicides used in pest control programs that might affect human health including reproductive system. The aim of this study was to demonstrate the mechanisms through which MZB induces testicular tissue damage and the probable protective effect of N-acetylcysteine (NAC), a modified amino acid, with antioxidant property, against MZB toxicity in an animal model. Male albino mice ( n = 8) were exposed to different doses of MZB (250 and 500 mg/kg/day) by oral gavage without or with NAC (200 mg/kg, twice/week) for 40 days. Sub-chronic MZB dose-dependently decreased sperm motility and count. Exposure to MZB increased lipid peroxidation and protein carbonyl, while it reduced antioxidant enzymes activities, total antioxidant capacity, and glutathione content. The histopathological examination clearly showed deleterious changes in the testicular structure. At the molecular levels, the results of quantitative real time-poly chain reaction (qRT-PCR) showed that MZB upregulated oxidative stress markers inducible nitric oxide synthase (iNOS) and NADPH oxidase 4 (NOX4) and downregulated expression of the glutathione peroxidase 1 (Gpx1) gene as one of the most important antioxidant enzymes. MZB also induced apoptosis dose-dependently in the testes as determined by the terminal dUTP nick-end labeling assay and immunoblotting. NAC administration decreased the mRNA levels of both iNOS and NOX4 with a concomitant increase in Gpx1 expression. It also significantly decreased MZB-induced oxidative stress and apoptosis. Collectively, the present study showed MZB-induced oxidative damage in testes leading to apoptosis. It revealed that antioxidants such as NAC can mitigate oxidant injury induced by the dithiocarbamate pesticides in the reproductive system.
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http://dx.doi.org/10.1177/0748233718778397DOI Listing
November 2018

Production and characterization of monoclonal antibodies against aflatoxin B1.

J Immunoassay Immunochem 2014 ;35(4):335-43

a Department of Clinical Biochemistry, School of Medicine , Mashhad University of Medical Sciences , Mashhad , Iran.

In this article, we embarked on production of mouse monoclonal antibodies against aflatoxin B1 which is the most commonly occurring fungal toxin in food and feed products. After immunization and fusion with myloma cells, two stable clones (A218 and B319) were selected. Isotyping showed that these monoclonal antibodies (mAbs) were IgG2b with kappa light chains. The affinity of A218 and B319 clons were 5×10(11) M(-1) and 6×10(9) M(-1), respectively. Competitive indirect ELISA results indicated these mAbs had complete (100%) cross-reaction with four major types of aflatoxins: B1, B2, G1, and G2. These mAbs could be used for immunoassay measurement of aflatoxins with high affinity and low detection limits.
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http://dx.doi.org/10.1080/15321819.2013.863207DOI Listing
March 2015

Indomethacin-enhanced anticancer effect of arsenic trioxide in A549 cell line: involvement of apoptosis and phospho-ERK and p38 MAPK pathways.

Biomed Res Int 2013 10;2013:237543. Epub 2013 Nov 10.

Neuroscience Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman 7619813159, Iran.

Background: Focusing on novel drug combinations that target different pathways especially apoptosis and MAPK could be a rationale for combination therapy in successful treatment of lung cancer. Concurrent use of cyclooxygenase (COX) inhibitors with arsenic trioxide (ATO) might be a possible treatment option.

Methods: Cytotoxicity of ATO, dexamethasone (Dex), celecoxib (Cel), and Indomethacin (Indo) individually or in combination was determined at 24, 48, and 72 hrs in A549 lung cancer cells. The COX-2 gene and protein expression, MAPK pathway proteins, and caspase-3 activity were studied for the most cytotoxic combinations.

Results: The IC50s of ATO and Indo were 68.7 μmol/L and 396.5 μmol/L, respectively. Treatment of cells with combinations of clinically relevant concentrations of ATO and Indo resulted in greater growth inhibition and apoptosis induction than did either agent alone. Caspase-3 activity was considerably high in the presence of ATO and Indo but showed no difference in single or combination use. Phosphorylation of p38 and ERK1/2 was remarkable in the concurrent presence of both drugs.

Conclusions: Combination therapy with ATO and Indo exerted a very potent in vitro cytotoxic effect against A549 lung cancer cells. Activation of ERK and p38 pathways might be the mechanism of higher cytotoxic effect of ATO-Indo combination.
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http://dx.doi.org/10.1155/2013/237543DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3842073PMC
June 2014