Publications by authors named "Aida Iraji"

43 Publications

Comparing the effects of Elaegnus Angustifolia, Hypericum Perforatum and Psidium Guajava extracts on metabolic activity of dental pulp-derived mesenchymal stem cells.

Cell Tissue Bank 2021 Apr 11. Epub 2021 Apr 11.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Dental pulp derived-mesenchymal stem cells (DP-MSCs) is considered a suitable are candidate for tissue engineering techniques and osseous reconstruction. Based on the hypothesis that Hypericum perforatum, Elaeagnus Angustifolia and Psidium guajava extracts can be used in cell-based bone tissue engineering due to meagre cytotoxicity response in the cell culture medium, their effects on the viability and metabolic activity of DP-MSCs were investigated and compared with each extract. DP-MSCs were extracted from human dental pulp, characterized by flow cytometry, and differentiated into Osteogenic and adipogenic lineages which were then cultured in different concentrations of E. Angustifolia, H. perforatum and P. guajava extracts at different time intervals followed by MTT assay evaluation. The dental pulp mesenchymal stem cells were evaluated for their plastic adherence ability, fibroblast-like and spindle morphology. According to flow cytometry data, isolated cells from DP-MSCs expressed MSCs markers. A comparison of herbal extracts' concentrations revealed that 500 μg/ml was toxic to dental pulp stem cells, a guide to the toxic dose for DP-MSCs. The P.guajava bore low toxicity and increased dental pulp stem cell viability in comparison to the other two herbal extracts. The hydro-alcoholic extracts of E. Angustifolia, H. perforatum, and P. guajava were efficient in DP-MSCs viability, and therefore were concluded to be useful in maintaining structural and functional cell viability. It was also concluded that the co-culture of stem cells with herbal elements could stimulate endogenous factors to enhance the proliferation and viability of MSCs.
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http://dx.doi.org/10.1007/s10561-021-09923-xDOI Listing
April 2021

Synthesis, in vitro evaluation, and molecular docking studies of novel hydrazineylideneindolinone linked to phenoxymethyl-1,2,3-triazole derivatives as potential α-glucosidase inhibitors.

Bioorg Chem 2021 Mar 29;111:104869. Epub 2021 Mar 29.

Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran; Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran. Electronic address:

In this work, a novel series of hydrazineylideneindolinone linked to phenoxymethyl-1,2,3-triazole derivatives were designed, synthesized, and evaluated for their anti-α-glucosidase activity due to an urgent need to develop effective anti-diabetic agents. Among tested 15 compounds, 8 derivatives (9a, 9b, 9c, 9d, 9e, 9f, 9h, and 9o) demonstrated superior potency compared to that of positive control, acarbose. Particularly, compound 9d possessed the best anti-α-glucosidase activity with around a 46-fold improvement in the inhibitory activity. Additionally, 9d showed a competitive type of inhibition in the kinetic study and the molecular docking study demonstrated that it well occupied the binding pocket of the catalytic center through desired interactions with residues, correlating to the experimental results.
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http://dx.doi.org/10.1016/j.bioorg.2021.104869DOI Listing
March 2021

aromatic water: A traditional drink with considerable anti- activity.

Curr Med Mycol 2020 Sep;6(3):1-8

Department of Pharmacognosy, Shiraz University of Medical Sciences, Shiraz, Iran.

Background And Purpose: Aromatic waters (AWs) are therapeutic distillates, which harbor both essential oil and water-soluble components of a plant. Due to the dispersion of the light amount of essence through the AWs, they have their specific pleasant smell, taste, and medicinal properties. In Iranian traditional medicine, AW is used to treat gastrointestinal disorders. The present study was conducted to determine the chemical composition of the essential oil extracted from AW and its antifungal activities against species.

Materials And Methods: The composition of the essential oil extracted from AW was analyzed by gas chromatography-mass spectrometry. In addition, the evaluation of the antifungal activity of AW against species was performed using broth microdilution methods as recommended by the Clinical Laboratory Standard Institute. Moreover, the biofilm formation inhibition, antioxidant properties, and experimental activity of AW were determined in an animal model.

Results: According to the results, thymol (78.08%) was the major compound of EO, followed by carvacrol (8.20%) and carvotanacetone (6.50%). Furthermore, AW exhibited antifungal activities against the examined fungi and inhibited the biofilm formation of C. albicans at a concentration of up to 0.25 V/V. Histopathological analyses revealed that colonization declined in the mice following the administration of AW in a therapeutic trial.

Conclusion: It seems that the presence of phenolic monoterpenes in AW has resulted in antifungal effects. Pleasant odor and antioxidant properties are extra bonuses to the antimicrobial effects of this plant. Based on the findings, AW might have the potential to be used in the management of alimentary candidiasis or oral hygienic products.
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http://dx.doi.org/10.18502/cmm.6.3.3979DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8018821PMC
September 2020

The natural-based optimization of kojic acid conjugated to different thio-quinazolinones as potential anti-melanogenesis agents with tyrosinase inhibitory activity.

Bioorg Med Chem 2021 Apr 27;36:116044. Epub 2021 Jan 27.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran; Department of Medicinal Chemistry, Faculty of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

Melanin pigment and melanogenesis are a two-edged sword. Melanin has a radioprotection role while melanogenesis has undesirable effects. Targeting the melanogenesis pathway, a series of kojyl thioether conjugated to different quinazolinone derivatives were designed, synthesized, and evaluated for their inhibitory activity against mushroom tyrosinase. All the synthesized compounds were screened for their anti-tyrosinase activity and all derivatives displayed better potency than kojic acid as the positive control. In this regard, 5j and 5h as the most active compounds showed an IC value of 0.46 and 0.50 µM, respectively. In kinetic evaluation against tyrosinase, 5j depicted an uncompetitive inhibition pattern. Designed compounds also exhibited mild antioxidant capacity. Moreover, 5j and 5h achieved good potency against the B16F10 cell line to reduce the melanin content, whilst showing limited toxicity against malignant cells. The proposed binding mode of new inhibitors evaluated through molecular docking was consistent with the results of structure-activity relationship analysis.
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http://dx.doi.org/10.1016/j.bmc.2021.116044DOI Listing
April 2021

Allium hooshidaryae (Alliaceae); Chemical compositions, biological and ethnomedicine uses.

J Ethnopharmacol 2021 Feb 12;274:113918. Epub 2021 Feb 12.

Department of Biology, Faculty of Science, Shahid Bahonar University of Kerman, Kerman, Iran.

Ethnopharmacological Relevance: Allium hooshidaryae (sect. Pseudoprason) is a wild plant in northwestern Iran. The plant is traditionally used, besides as spice, also for its medicinal properties.

Aim Of The Study: Due to the shortcoming evidence in scientific research and the importance of this plant in folk medicine, this study aims to assess the chemical compositions and biological activities, which have no longer reported to date.

Materials And Methods: The bulbs of A. hooshidaryae were collected from West Azerbaijan, Iran. The plant essential oil was obtained by hydrodistillation using Clevenger-type apparatus according to the European pharmacopeia. The plant hydromethanolic extract was obtained using maceration method. The volatile oil compositions of A. hooshidaryae bulbs were evaluated by use of combined gas chromatography/flame ionization detector (GC/FID) and gas chromatography/mass spectrometry (GC/MS) techniques. Furthermore, different biological activities of the yielded essential oil and hydromethanolic extract were in vitro evaluated. The antibacterial and antifungal activities were assessed using disc diffusion assay, tube dilution assay, minimal inhibitory concentration (MIC), minimal bactericidal concentration (MBC), and minimal fungicidal concentration (MFC). The cytotoxic activities were assayed by reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) toward two human cancerous cell lines (MOLT-4 and MCF-7). Antioxidant activity was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay.

Results: GC/FID and GC/MS analyses allowed detecting 62 components in the A. hooshidaryae essential oil representing the 91.87% of the total oil. The volatile compounds were identified by comparison of the relative retention indices (RRI), mass spectra with those in NIST08/NIH and Wiley (257 and 7 L) libraries and co-elution with authentic samples where available. Surprisingly, the most abundant compound was obtained as menthol (19.0%) followed by carvacrol (10.1%), menthone (6.4%), methyl (methylthiomethyl) disulfide (4.2%), dimethyl disulfide (3.8%), and thymol (3.8%). Contrary to the other Allium species enriched by sulfur compounds, just three compounds accounting for 10.7% of the total oil were obtained as the sulfur-sulfur bond containing components (Dimethyl disulfide, Methyl (methylthio) methyl disulfide, Bis-methylthiomethyl disulfide). The hydromethanolic extract of A. hooshidaryae showed higher anti-radical (IC of 9.81 μg/mL) and cytotoxic (for MOLT-4 and MCF-7, IC were 76.3 and 128.6 μg/mL, respectively) activities rather than that of the obtained essential oil (IC of 39.9 μg/mL; IC of 109.2 μg/mL, and IC of 297.5 μg/mL). While, the essential oil exhibited the anti-Staphylococcus aurous and anti-Escherichia coli activities approximately the same as Chloramphenicol (positive control). The MIC values were 31.25 and 62.5 μg/mL and the disk inhibition zone values were 23 and 21 mm, respectively. In addition, Candida albicans had moderate sensitivity (MFC of 62.5 μg/mL) for the essential oil.

Conclusions: The hydromethanolic extract of A. hooshidaryae shows the potency to be used for food protection in addition to further cytotoxic investigations. Associated with antimicrobial abilities of both A. hooshidaryae products, the compatible results was observed with the traditional claim having being not investigated to date. These findings will facilitate the development of A. hooshidaryae for further deep investigations.
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http://dx.doi.org/10.1016/j.jep.2021.113918DOI Listing
February 2021

Core-shell chitosan/PVA-based nanofibrous scaffolds loaded with Satureja mutica or Oliveria decumbens essential oils as enhanced antimicrobial wound dressing.

Int J Pharm 2021 Mar 26;597:120288. Epub 2021 Jan 26.

Department of Chemical Engineering, School of Chemical and Petroleum Engineering, Shiraz University, Shiraz, Iran. Electronic address:

Wounds are prone to bacterial infections, which cause a delayed healing process. Regarding the emergence of bacterial resistance to common antibiotics, using natural antimicrobial agents can be beneficial. Chitosan is a biological polymer, which has shown partial antioxidant and antimicrobial activities. In this study, core-shell nanofibrous scaffolds composed of chitosan (CS)/polyvinyl alcohol (PVA) as the core and polyvinylpyrrolidone (PVP)/ maltodextrin (MD) as the shell were developed. Satureja mutica (S. mutica) or Oliveria decumbens (O. decumbens) essential oil (EO) was encapsulated into the core of the produced scaffolds. The broth microdilution analysis showed significant antimicrobial activity of the EOs. The SEM analysis indicated that the unloaded and loaded core-shell scaffolds with S. mutica or O. decumbens EO had a uniform, beadless structure with fiber mean diameters of 210 ± 50, 250 ± 45, and 225 ± 46 nm, respectively. The CS/PVA-PVP/MD and CS/PVA/EO-PVP/MD scaffolds indicated suitable mechanical properties. The addition of the studied EOs enhanced the antioxidant activity of the scaffolds. The antimicrobial test of produced scaffolds showed that loading of 10% S. mutica or O. decumbens EO could broaden the microbicidal activity of the CS/PVA-PVP/MD scaffolds. These results revealed that the CS/PVA/EO-PVP/MD nanofibrous scaffolds are promising candidates for wound dressing.
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http://dx.doi.org/10.1016/j.ijpharm.2021.120288DOI Listing
March 2021

The Antioxidant and Anti-Inflammatory Effects of Extract on TNBS-Induced Ulcerative Colitis in Rats.

Evid Based Complement Alternat Med 2021 7;2021:3075973. Epub 2021 Jan 7.

Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran.

Objectives: Ulcerative colitis is a common subtype of persistent inflammatory bowel disease with high morbidity consequences. Despite unknown definite pathogenesis, multiple anti-inflammatory medications are used for its treatment. Traditionally, (QB), mostly available in the Middle East, has been used for gastrointestinal disorders. Other beneficial effects associated with QB include reduction of oxidative stress, inflammations, homeostatic instability, and improvement in clinical conditions.

Materials And Methods: This experimental study was designed to assess the possible therapeutic effects of QB on UC and compare its effects with those of sulfasalazine. Of the 70 Wistar rats clustered in seven groups, ten received only alcohols and sixty were confirmed to be suffering from trinitrobenzene sulfonic acid- (TNBS-) induced colitis. Four groups received different dosages of QB extract via oral and rectal routes, one received sulfasalazine, and the other remaining two groups received nothing. The effects of QB were evaluated by assessing macroscopic and histologic scoring, measuring inflammatory mediators, and determining oxidative stress markers.

Results: Comparing to the untreated TNBS-induced control groups, QB-treated groups showed a dose- and route-dependent improvement comparable with sulfasalazine. Treating rats with QB reduced the microscopic and macroscopic damage, decreased TNF-, IL-6, NO, MPO activity, and MDA content, increased superoxide dismutase (SOD) activity, and reduced body weight loss.

Conclusions: Our data recommended the anti-inflammatory and antioxidant effects of QB extract in a dose-dependent manner.
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http://dx.doi.org/10.1155/2021/3075973DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7808820PMC
January 2021

The possible effect of microRNA-155 (miR-155) and BACE1 inhibitors in the memory of patients with down syndrome and Alzheimer's disease: Design, synthesis, virtual screening, molecular modeling and biological evaluations.

J Biomol Struct Dyn 2021 Jan 22:1-13. Epub 2021 Jan 22.

The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran.

MiR-155 plays main roles in several physiological and pathological mechanisms, such as Down syndrome (DS), immunity and inflammation and potential anti-AD therapeutic target. The miR-155 is one of the overexpressed miRNAs in DS patients that contribute directly and indirectly to the onset or progression of the DS. Since the miR-155 can simultaneously reduce the translation of several genes at post-transcriptional levels, targeting the miR-155 might set the stage for the treatment of DS. One of the rational strategies in providing therapeutic interventions in this respect is to design and develop novel small molecules inhibiting the miR-155 function or biogenesis or maturation. In the present study, we aim to introduce small molecule compounds with the potential to inhibit the generation of the selectively miR-155 processing by employing computational drug design approaches, as well as in vitro studies. We designed and synthesized a novel series of imidazo[1,2-a]pyridines derivatives as new nonpeptic candidates for the treatment of DS with AD. The designed compounds were investigated for their BACE1 and miR-155 binder inhibitory potential in vitro and in cell. In addition, we present a systematic computational approach that includes 3 D modeling, docking-based virtual screening, and molecular dynamics simulation to identify Small - molecule inhibitors of pre-miR-155 maturation. To confirm the inhibitory potential of compound 8k on miR-155 maturation, qRT- PCR was performed. All our results confirm that compound 8k, in addition to being a good inhibitor of BACE1, can also be a good inhibitor of miR-155. Communicated by Ramaswamy H. Sarma.
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http://dx.doi.org/10.1080/07391102.2021.1873861DOI Listing
January 2021

Effects of Calendula Officinalis and Hypericum Perforatum on Antioxidant, Anti-Inflammatory, and Histopathology Indices of Induced Periodontitis in Male Rats.

J Dent (Shiraz) 2020 Dec;21(4):314-321

Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran.

Statement Of The Problem: Periodontitis is one of the most common bacterial infections of the oral cavity. It is important to find adjunctive methods for chemical treatment of periodontitis with less complications and proven therapeutic properties.

Purpose: The aim of this study was to compare the effects of and on antioxidant, anti-inflammatory and histopathologic indices of induced periodontitis in male rats.

Materials And Method: In this experimental animal study, forty adult male Sprague-Dawley rats were randomly divided into 4 groups (n=10) and then experimental periodontitis was induced by 3-0 nylon non-absorbable ligature. Each group was treated for 10 days as follows: 1) hydroalcoholic extract, 1000 mg/kg/daily, orally; 2) hydroalcoholic extract, 1000 mg/kg/daily, orally; 3) a mix of the two plants, 1000 mg/kg/ daily, orally, 4) normal saline solution. At the end of study, blood sample were obtained via cardiocentesis, the rats were euthanized, and their maxillae were removed. The samples were analyzed for histopathological scores and total antioxidant capacity and IL-1β were measured.

Results: Mixed hydroalchoholic extract of and decreased IL-1β (4.3020±0.63), and increased the antioxidant parameter in comparison to the control group (3.1192±0.43) (< 0.001). There were significant histopathological differences between the treatment groups and the control group.

Conclusion: Mixed hydroalchoholic extract of and might be considered as an adjunctive treatment for periodontitis.
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http://dx.doi.org/10.30476/DENTJODS.2020.83660.1056DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7737925PMC
December 2020

Design, synthesis, in vitro and in silico studies of novel Schiff base derivatives of 2-hydroxy-4-methoxybenzamide as tyrosinase inhibitors.

Drug Dev Res 2020 Dec 19. Epub 2020 Dec 19.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Due to the fact that tyrosinase is responsible for biosynthesis and regulation of melanins and browning food products, tyrosinase inhibitors can be favorable agents in cosmetics and medicinal industries. A series of novel 2-hydroxy-4-methoxybenzohydrazide were designed, synthesized, and their new application as tyrosinase inhibitors was also disclosed. Based on in vitro tyrosinase inhibitory assay, 4d as the strongest inhibitor of tyrosinase with an IC value of 7.57 μM showed approximately 2.5-fold better inhibition than kojic acid as positive control followed by two compounds 4b (IC = 8.19 ± 0.25 μM) and 4j (IC = 8.92 ± 0.016) which displayed preferable tyrosinase inhibitory activity. Detailed investigations on the mechanism of action of the 4d reported mix type of inhibition. More importantly, molecular modeling assessments proposed the ability of 4d for potential interaction with Cu (metal)-His (residue) within tyrosinase active site. Overall, 4d is a promising candidate for the development of anti-tyrosinase agents.
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http://dx.doi.org/10.1002/ddr.21771DOI Listing
December 2020

Novel N-benzylpiperidine derivatives of 5-arylisoxazole-3-carboxamides as anti-Alzheimer's agents.

Arch Pharm (Weinheim) 2021 Mar 23;354(3):e2000258. Epub 2020 Nov 23.

Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran.

The complex pathophysiology of Alzheimer's disease (AD) has prompted researchers to develop multitarget-directed molecules to find an effective therapy against the disease. In this context, a novel series of N-(1-benzylpiperidin-4-yl)-5-arylisoxazole-3-carboxamide derivatives were designed, synthesized, and evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). In vitro biological evaluation demonstrated that compound 4e was the best AChE (IC  = 16.07 μM) and BuChE inhibitor (IC  = 15.16 μM). A kinetic study of 4e was also conducted, which presented a mixed-type inhibition for both enzymes. Molecular docking studies revealed that compound 4e fitted well into the active sites of AChE and BuChE, forming stable and strong interactions with key residues Glu199, Trp84, Asp72, Tyr121, and Phe288 in AChE and His438, Trp82, Ala328, Tyr332, Phe329, Thr120, and Pro285 in BuChE. Besides, the inhibition of BACE1 by 4e and the biometal chelation activity of 4e were measured. The neuroprotective assessment revealed that 4e exhibited 23.2% protection at 50 µM toward amyloid-beta-induced PC12 neuronal cells. Overall, this study exhibited that compound 4e was a promising compound targeting multiple factors associated with AD.
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http://dx.doi.org/10.1002/ardp.202000258DOI Listing
March 2021

Poly(3-Hydroxybutyrate)-Multiwalled Carbon Nanotubes Electrospun Scaffolds Modified with Curcumin.

Polymers (Basel) 2020 Nov 4;12(11). Epub 2020 Nov 4.

Department of Polymer and Biomaterials Science, Faculty of Chemical Technology and Engineering, West Pomeranian University of Technology, Szczecin, Al. Piastow 45, 71-311 Szczecin, Poland.

Appropriate selection of suitable materials and methods is essential for scaffolds fabrication in tissue engineering. The major challenge is to mimic the structure and functions of the extracellular matrix (ECM) of the native tissues. In this study, an optimized 3D structure containing poly(3-hydroxybutyrate) (P3HB), multiwalled carbon nanotubes (MCNTs) and curcumin (CUR) was created by electrospinning a novel biomimetic scaffold. CUR, a natural anti-inflammatory compound, has been selected as a bioactive component to increase the biocompatibility and reduce the potential inflammatory reaction of electrospun scaffolds. The presence of CUR in electrospun scaffolds was confirmed by H NMR and Fourier-transform infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) revealed highly interconnected porosity of the obtained 3D structures. Addition of up to 20 wt% CUR has enhanced mechanical properties of the scaffolds. CUR has also promoted in vitro bioactivity and hydrolytic degradation of the electrospun nanofibers. The developed P3HB-MCNT composite scaffolds containing 20 wt% of CUR revealed excellent in vitro cytocompatibility using mesenchymal stem cells and in vivo biocompatibility in rat animal model study. Importantly, the reduced inflammatory reaction in the rat model after 8 weeks of implantation has also been observed for scaffolds modified with CUR. Overall, newly developed P3HB-MCNTs-CUR electrospun scaffolds have demonstrated their high potential for tissue engineering applications.
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http://dx.doi.org/10.3390/polym12112588DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7694206PMC
November 2020

Design and synthesis of multi-target directed 1,2,3-triazole-dimethylaminoacryloyl-chromenone derivatives with potential use in Alzheimer's disease.

BMC Chem 2020 Dec 27;14(1):64. Epub 2020 Oct 27.

Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran.

To discover multifunctional agents for the treatment of Alzheimer's disease (AD), a new series of 1,2,3-triazole-chromenone derivatives were designed and synthesized based on the multi target-directed ligands approach. The in vitro biological activities included acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibition as well as anti-Aβ aggregation, neuroprotective effects, and metal-chelating properties. The results indicated a highly selective BuChE inhibitory activity with an IC value of 21.71 μM for compound as the most potent compound. Besides, compound could inhibit self-induced Aβ aggregation and AChE-induced Aβ aggregation with 32.6% and 29.4% inhibition values, respectively. The Lineweaver-Burk plot and molecular modeling study showed that compound targeted both the catalytic active site (CAS) and peripheral anionic site (PAS) of BuChE. It should be noted that compound was able to chelate biometals. Thus, the designed scaffold could be considered as multifunctional agents in AD drug discovery developments.
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http://dx.doi.org/10.1186/s13065-020-00715-0DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7592376PMC
December 2020

Effect of flaxseed oil on biochemical parameters, hormonal indexes and stereological changes in ovariectomized rats.

Vet Med Sci 2021 Mar 25;7(2):521-533. Epub 2020 Oct 25.

Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran.

The ovariectomized rat is a widely used preclinical model for studying postmenopausal and its complications. In this study, the therapeutic effect of flaxseed oil on the ovariectomized adult rats was investigated. Our results showed that biochemical parameters including calcium, oestrogen and progesterone levels increase 8 weeks after ovariectomy in rats. Also, the amount of alkaline phosphatase decreased significantly after 8 weeks compared with the OVX rat. The healing potential of flaxseed oil was proven by successfully recovering the affected tissue and preventing the unpleasant symptoms of ovariectomized rats. The biological effects of flaxseed oil may be due to high amounts of fatty acids, phytoestrogens and an array of antioxidants. The results suggest that flaxseed oil can mimic the action of oestrogen and can be a potential treatment for hormone replacement therapy (HRT).
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http://dx.doi.org/10.1002/vms3.372DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8025639PMC
March 2021

Effect of hydroalcoholic extract of and resveratrol on ovarian morphology and biochemical parameters in Letrozole-induced polycystic ovary syndrome rat model: An experimental study.

Int J Reprod Biomed 2020 Aug 19;18(8):637-650. Epub 2020 Aug 19.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Background: Resveratrol and () are known to be natural antioxidants and regulators of human metabolism. However, the effects of resveratrol and on the ovarian morphology in polycystic ovary syndrome (PCOS) are not obvious.

Objective: This study aimed to determine the effect of the hydroalcoholic extract of in combination with resveratrol on some biochemical parameters and ovarian morphology in the letrozole-induced PCOS rat.

Materials And Methods: Seventy adult female Sprague-Dawley rats aged 10-12 weeks weighing 200 20 gr were randomly divided into seven groups (n = 10/each). Group I): normal; Group II): vehicle; Group III): letrozole-induced PCOS 1 mg/kg letrozole orally, rats receiving 1 cc normal saline orally; Group IV): PCOS + receiving 150 mg/kg metformin orally; Group V): PCOS + receiving 20 mg/kg resveratrol orally; Group VI): PCOS + 3 gr/kg barberry orally; and Group VII): PCOS + receiving 3 gr/kg barberry and 20 mg/kg resveratrol orally. All animals were followed-up for 63 days. The biochemical parameters and histological assessments of ovaries were performed.

Results: Resveratrol alone and/or in combination with treatment in rats led to a significant decrease in low-density lipoprotein, triglyceride, malondialdehyde, and tumor necrosis factor-alpha concentrations (p = 0.02). The groups IV, V, VI, and VII showed a decrease in insulin resistance and an increase in the superoxide dismutase, total antioxidant capacity, and high-density lipoprotein (p = 0.01). No significant difference was observed between the level of serum glucose in the treatment groups. Number of cystic follicles had a significant decrease in barberry, resveratrol, and their combination groups (p 0.001).

Conclusion: Resveratrol, , and their combination as natural products with fewer side effects might be effective as an alternative medicine in treatment of PCOS.
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http://dx.doi.org/10.18502/ijrm.v13i8.7505DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7457158PMC
August 2020

The protective effects of grape seed oil on induced osteoarthritis of the knee in male rat models.

J Orthop Surg Res 2020 Sep 10;15(1):400. Epub 2020 Sep 10.

Center of Nanotechnology in Drug Delivery, Faculty of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.

Background: Osteoarthritis (OA), though being treated via various methods and medicines, is still a major healthcare concern mostly due to the increase in diagnosis of these age-related diseases. The present study aimed at investigating the effects of oral and intra articular injection of grape seed oil on OA in male rat models.

Methods And Materials: Seventy male rats were selected and their anterior cruciate ligament was cut to induce OA. They were divided into 7 groups (n = 10): C1, no treatment; C2, receiving 300 mg/day of Piascledine per os (PO); C3, 1 mg sodium hyaluronate intra-articularly in days 1, 7, 14; C4, 1 mg methyl-prednisolone acetate intra-articularly; E1, avocado and grape seed oil combination (2:1, 300 mg/day) PO; E2, 500 mg/day of grape seed oil PO; E3, 200 mg/day grape seed oil intra-articularly. After 10 weeks, the rats were anesthetized and evaluated radiologically and histopathologically. P value ≤ 0.05 was considered as statistically significant.

Results: All the groups made significant differences with C1 regarding all inspected radiological criteria (P ≤ 0.05). E1 and E3 showed significantly better effects on medial femoral condyle, medial tibial condyle, joint space width, total osteophyte, and OA scores (P ≤ 0.04). Joint surface, matrix, cell distribution, cell population viability, calcification, and subchondral bone in treatment groups had significantly better scores versus C1 (P ≤ 0.04). E1 and E3 had significantly superior results regarding joint surface, cell viability, and calcification (P ≤ 0.04).

Conclusions: Grape seed oil has protective effects, both in injectable form and PO in combination with avocado, on OA in rats. Further clinical trials are necessary.
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http://dx.doi.org/10.1186/s13018-020-01932-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7488061PMC
September 2020

N-Cyclohexylimidazo[1,2-a]pyridine derivatives as multi-target-directed ligands for treatment of Alzheimer's disease.

Bioorg Chem 2020 10 28;103:104146. Epub 2020 Jul 28.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

Alzheimer's disease (AD) is the most common form of dementia. While drugs that target several pathways underlying AD have been proposed, effective treatments remain to be discovered. BACE1, an enzyme associated with AD progression, is a promising target for developing anti-Alzheimer drugs. To find novel multifunctional anti-Alzheimer agents, we designed and synthesized a series of new substituted benzyl-1H-1,2,3-triazol-4-yl-N-cyclohexylimidazo[1,2-a]pyridin-3-amine. The in vitro screening results revealed that most of the compounds exhibited moderate to potent BACE1 and BuChE inhibitory and antioxidant activities. Compounds 7f and 7g, bearing dichloro (2,3-Cl and 3,4-Cl) moieties on the benzyl pendant were selected as the most active compounds in our BACE1 inhibitory assay with respective IC values of about 12 and 8.9 μM. In addition, compounds 7g and 7h (4-bromo derivative) showed the highest BuChE inhibitory activity with IC of 3.2 and 2.5 µM, respectively. Compound 7g also possessed antioxidant activity with an IC value of 10.2 μM and metal chelation potential. Moreover, docking studies were performed to investigate the possible mechanism of inhibition. Taken together, we demonstrate that N-cyclohexylimidazo[1,2-a]pyridine containing triazole motif derivatives deserve further investigation for anti-Alzheimer drug development.
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http://dx.doi.org/10.1016/j.bioorg.2020.104146DOI Listing
October 2020

A Series of Benzylidenes Linked to Hydrazine-1-carbothioamide as Tyrosinase Inhibitors: Synthesis, Biological Evaluation and Structure-Activity Relationship.

Chem Biodivers 2020 Aug 3;17(8):e2000285. Epub 2020 Aug 3.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, 71348, Shiraz, Iran.

Tyrosinase is a type 3 copper enzyme responsible for skin pigmentation disorders, skin cancer, and enzymatic browning of vegetables and fruits. In the present article, 12 small molecules of 2-benzylidenehydrazine-1-carbothioamide were designed, synthesized and evaluated for their anti-tyrosinase activities followed by molecular docking and pharmacophore-based screening. Among synthesized thiosemicarbazone derivatives, one compound, (2E)-2-[(4-nitrophenyl)methylidene]hydrazine-1-carbothioamide, is the strongest inhibitor of mushroom tyrosinase with IC of 0.05 μM which demonstrated a 128-fold increase in potency compared to the positive control. Kinetic studies also revealed mix type inhibition by this compound. Docking studies confirmed the complete fitting of the synthesized compounds into the tyrosinase active site. The results underline the potential of 2-benzylidenehydrazine-1-carbothioamides as potent pharmacophore to extend the tyrosinase inhibition in drug discovery.
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http://dx.doi.org/10.1002/cbdv.202000285DOI Listing
August 2020

Synthesis, biological evaluation and molecular docking analysis of vaniline-benzylidenehydrazine hybrids as potent tyrosinase inhibitors.

BMC Chem 2020 Dec 7;14(1):28. Epub 2020 Apr 7.

1Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

In this work, 11 novel compounds based on vaniline and benzylidenehydrazine structure were synthesized with various substituents on phenyl aromatic ring of the molecule and evaluated as tyrosinase inhibitors. These new derivatives showed significant anti-tyrosinase activities, among which demonstrated to be the most potent compound, with IC values of 1.58 µM . The structure-activity relationship study of the novel constructed analogs was fully discussed. Kinetic study of compound showed uncompetitive inhibition towards tyrosinase. Furthermore, the high potency of was supported theoretically by molecular docking evaluations.
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http://dx.doi.org/10.1186/s13065-020-00679-1DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7137441PMC
December 2020

Novel small molecule therapeutic agents for Alzheimer disease: Focusing on BACE1 and multi-target directed ligands.

Bioorg Chem 2020 04 4;97:103649. Epub 2020 Feb 4.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

Alzheimer's Disease (AD) is a progressive neurodegenerative disorder that effects 50 million people worldwide. In this review, AD pathology and the development of novel therapeutic agents targeting AD were fully discussed. In particular, common approaches to prevent Aβ production and/or accumulation in the brain including α-secretase activators, specific γ-secretase modulators and small molecules BACE1 inhibitors were reviewed. Additionally, natural-origin bioactive compounds that provide AD therapeutic advances have been introduced. Considering AD is a multifactorial disease, the therapeutic potential of diverse multi target-directed ligands (MTDLs) that combine the efficacy of cholinesterase (ChE) inhibitors, MAO (monoamine oxidase) inhibitors, BACE1 inhibitors, phosphodiesterase 4D (PDE4D) inhibitors, for the treatment of AD are also reviewed. This article also highlights descriptions on the regulator of serotonin receptor (5-HT), metal chelators, anti-aggregants, antioxidants and neuroprotective agents targeting AD. Finally, current computational methods for evaluating the structure-activity relationships (SAR) and virtual screening (VS) of AD drugs are discussed and evaluated.
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http://dx.doi.org/10.1016/j.bioorg.2020.103649DOI Listing
April 2020

One-pot synthesis of thioxo-tetrahydropyrimidine derivatives as potent β-glucuronidase inhibitor, biological evaluation, molecular docking and molecular dynamics studies.

Bioorg Med Chem 2020 04 6;28(7):115359. Epub 2020 Feb 6.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran; Department of Medicinal Chemistry, Faculty of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

A series of N,N-diethyl phenyl thioxo-tetrahydropyrimidine carboxamide have been synthesized and investigated for their β-glucuronidase inhibitory activities. All molecules exhibited excellent inhibition with IC values ranging from 0.35 to 42.05 µM and found to be even more potent than the standard d-saccharic acid. Structure-activity relationship analysis indicated that the meta-aryl-substituted derivatives significantly influenced β-glucuronidase inhibitory activities while the para-substitution counterpart outperforming moderate potency. The most potent compound in this series was 4g bearing thiophene motif with IC of 0.35 ± 0.09 µM. To verify the SAR, molecular docking and molecular dynamics studies were also performed.
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http://dx.doi.org/10.1016/j.bmc.2020.115359DOI Listing
April 2020

Protection by pure and genistein fortified extra virgin olive oil, canola oil, and rice bran oil against acetic acid-induced ulcerative colitis in rats.

Food Funct 2020 Jan;11(1):860-870

Colorectal Research Center and Department of Pharmacology, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran.

Genistein is a major isoflavone with antioxidant and anti-inflammatory activities and hydrophobic features. To increase its bioavailability, researchers supplemented genistein with dietary oils. The present study aims to compare the effectiveness of genistein supplementation with water solution or oils and find the best possible dietary oil for fortification. A total of 135 male Sprague-Dawley rats were randomly assigned to nine groups, including one control group and eight acetic acid-induced colitis groups. The rats in the intervention groups were treated with 5 ml per kg body weight of oral pure and genistein fortified forms of extra virgin olive oil (EVOO), canola oil (CaO), and rice bran oil (RBO); the Genistein group (G) received 100 mg per kg body weight of genistein in aqueous solution orally. The colitis and control groups did not receive any treatment. The levels of colonic MDA (malondialdehyde), MPO (myeloperoxidase) activity, and IL-1β (interleukin-1β) were evaluated and a stereological analysis of colonic tissues was performed. All of the dietary oils (EVOO, CaO, and RBO) were effective at ameliorating the rats' oxidative and inflammatory status (p < 0.05); however, EVOO (with or without genistein) prescription resulted in slightly better results, especially with regard to the inflammatory profile. Additionally, delivering genistein via an oil vehicle was more efficient at reducing MDA formation, MPO activity, and IL-1β concentration than genistein in aqueous solution. The quantitative analysis of colonic tissue was consistent with the biochemical analysis. Our findings suggest that the oral administration of EVOO, canola oil, and rice bran oil can attenuate the elevated IL-1β levels and oxidative damage in induced colitis. Moreover, genistein fortified oils, especially EVOO, showed more beneficial effects in decreasing these markers in comparison with the pure oils or genistein (aqueous solution).
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http://dx.doi.org/10.1039/c9fo01951kDOI Listing
January 2020

Efficacy of inhaled Lavandula angustifolia Mill. Essential oil on sleep quality, quality of life and metabolic control in patients with diabetes mellitus type II and insomnia.

J Ethnopharmacol 2020 Apr 10;251:112560. Epub 2020 Jan 10.

Endocrine and Metabolism Research Center, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

Ethnopharmacologic Relevance: Lavandula angustifolia Mill (lavender) odor was traditionally used as sleep enhancer. Previous studies have shown interaction between insomnia, quality of life and control of diabetes mellitus (DM). Insomnia is suggested to increase the risk of depression and decrease the quality of life in diabetic patients. The aim of this study was to evaluate the efficacy of inhaled Lavandula angustifolia Mill. as a complementary therapy for insomnia in diabetic patients.

Methods: In a randomized crossover placebo-controlled clinical trial, 52 patients with type II diabetes mellitus (DM) and insomnia, defined as Pittsburgh Insomnia Rating Scale-20(PIRS-20)>5,were treated with inhaled lavender or placebo for two periods of 4 weeks duration with one week interval as washing period. Sleep quality, quality of life and mood status were assessed by PIRS-20, WHO Quality of Life-BREF(WHOQOL-BREF) Questionnaire and Beck Depression Inventory (BDI) scale respectively, at baseline and end of each period of study. Fasting blood glucose (FBS), calorie intake and physical activity were measured before and after the interventions.

Results: At the end of study, data of 37 patients (all received both lavender and placebo in cross-over design) were analyzed. Based on crossover analysis the first treatment was not effective on the second treatment. Inhaled lavender resulted in a significant better outcome compared to placebo according to mean PIRS-20, WHOQOL-BREF and Beck Depression Inventory scores in both crossover arms. Likewise there was a significant better outcome in PIRS-20 domains for quality and quantity of sleep after Inhaled lavender compared to placebo. No significant improvement was observed in fasting glucose in lavender compared to placebo administration period.

Conclusion: Inhaled lavender can improve sleep quality and quantity, quality of life and mood in diabetic patients suffering from insomnia with no significant effect on metabolic status.
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http://dx.doi.org/10.1016/j.jep.2020.112560DOI Listing
April 2020

Effects of Citrullus colocynthis L. in a rat model of diabetic neuropathy.

J Integr Med 2020 Jan 6;18(1):59-67. Epub 2019 Dec 6.

Endocrine and Metabolism Research Center, Shiraz University of Medical Sciences, Shiraz 73, Iran. Electronic address:

Objective: This study investigated the biochemical, histopathological and physiological effects of Citrullus colocynthis on peripheral neuropathy in rats with streptozotocin (STZ)-induced diabetes.

Methods: Seventy adult male Sprague-Dawley rats were included in the present study. Diabetes was induced in 60 rats, with a single intraperitoneal injection of STZ (65 mg/kg). After 4 weeks, the diabetic rats were assessed for neuropathy. Then, the diabetic rats with neuropathy were randomly divided into 6 groups for a 4-week treatment with gabapentin, oral administration of C. colocynthis fruit pulp powder (100 and 300 mg/kg per day), topical preparations as oil-based solution and ointment, or placebo. Changes in metabolic, physiological, biochemical and histological parameters were considered as treatment outcomes.

Results: Metabolic outcomes (body weight and blood glucose level) were improved in the C. colocynthis-treated groups as compared to placebo. Tail-flick and hot-plate tests also had lower latency in the C. colocynthis-treated groups. Measurement of oxidative stress markers (malondialdehyde, superoxide dismutase and catalase) showed the antioxidant effect of C. colocynthis. Histological evaluation of the sciatic nerve showed that C. colocynthis decreased the number of demyelinated and degenerated nerve fibers. Among the C. colocynthis-treated groups, the one receiving 100 mg/kg power per day orally had the best treatment outcomes.

Conclusion: The present study showed that C. colocynthis fruit, through its antioxidant and hypoglycemic activities, has a positive effect in the treatment of diabetic neuropathy.
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http://dx.doi.org/10.1016/j.joim.2019.12.002DOI Listing
January 2020

Structure-Based Design, Synthesis, Biological Evaluation and Molecular Docking Study of 4-Hydroxy-N'-methylenebenzohydrazide Derivatives Acting as Tyrosinase Inhibitors with Potentiate Anti-Melanogenesis Activities.

Med Chem 2020 ;16(7):892-902

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran

Background: Melanogenesis is a process of melanin synthesis, which is a primary response for the pigmentation of human skin. Tyrosinase is a key enzyme, which catalyzes a ratelimiting step of the melanin formation. Natural products have shown potent inhibitors, but some of these possess toxicity. Numerous synthetic inhibitors have been developed in recent years may lead to the potent anti- tyrosinase agents.

Objective: A number of 4-hydroxy-N'-methylenebenzohydrazide analogues with related structure to chalcone and tyrosine were constructed with various substituents at the benzyl ring of the molecule and evaluate as a tyrosinase inhibitor. In addition, computational analysis and metal chelating potential have been evaluated.

Methods: Design and synthesized compounds were evaluated for activity against mushroom tyrosinase. The metal chelating capacity of the potent compound was examined using the mole ratio method. Molecular docking of the synthesized compounds was carried out into the tyrosine active site.

Results: Novel 4-hydroxy-N'-methylenebenzohydrazide derivatives were synthesized. The two compounds 4c and 4g showed an IC50 near the positive control, led to a drastic inhibition of tyrosinase. Confirming in vitro results were performed via the molecular docking analysis demonstrating hydrogen bound interactions of potent compounds with histatidine-Cu+2 residues with in the active site. Kinetic study of compound 4g showed competitive inhibition towards tyrosinase. Metal chelating assay indicates the mole fraction of 1:2 stoichiometry of the 4g-Cu2+ complex.

Conclusion: The findings in the present study demonstrate that 4-Hydroxy-N'- methylenebenzohydrazide scaffold could be regarded as a bioactive core inhibitor of tyrosinase and can be used as an inspiration for further studies in this area.
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http://dx.doi.org/10.2174/1573406415666190724142951DOI Listing
January 2020

5,6-Diphenyl triazine-thio methyl triazole hybrid as a new Alzheimer's disease modifying agents.

Mol Divers 2020 Aug 20;24(3):641-654. Epub 2019 Jul 20.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

In this study, new derivatives of 5,6-diphenyl triazine-thio methyl triazole hybrid were designed, synthesized and evaluated as multifunctional agents for Alzheimer's disease. Among all synthesized compounds, 4a and 4h showed the best inhibitory activities against BACE1 (40% and 37.5% μM inhibition at 50 µM, respectively). Molecular docking studies showed that compound 4a occupied the entire BACE1 enzyme and the thio triazine fragment deeply penetrates into S2 binding site via two hydrogen bonds with Thr72 and Gln73 amino acids. Different aromatic moieties occupy S'2 pocket via hydrophobic interactions. 6-Phenyl ring also had a potential hydrophobic interaction with S1 pocket. In vitro ChE inhibitory assay demonstrated that most of the derivatives exhibited more selectivity toward BuChE than AChE. 4c as the most potent BuChE inhibitor displayed an IC value of 6.4 µM, and 4b exhibited AChE inhibitory activity with 25.1% inhibition at 50 μM. Further, molecular docking studies revealed that the thiazolidinones moiety plays a key role in the inhibition mechanism by well fitting into the enzyme bounding pocket. Moreover, molecular docking study of 4a, 4b and 4c with ChE active site was also performed.
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http://dx.doi.org/10.1007/s11030-019-09970-3DOI Listing
August 2020

Synthesis of novel sepiolite-iron oxide-manganese dioxide nanocomposite and application for lead(II) removal from aqueous solutions.

Environ Sci Pollut Res Int 2019 Jun 10;26(18):18893-18903. Epub 2019 May 10.

Central Research Laboratory, Shiraz University of Medical Sciences, Shiraz, Iran.

In this study, the sepiolite-iron oxide-manganese dioxide (Sep-FeO-MnO) nanocomposite was synthesized and applied as a magnetically separable adsorbent for removal of Pb(II) ions from water in a batch system. The effects of initial Pb(II) concentration, adsorbent dosage, contact time, pH value, and temperature were investigated to optimize the conditions for maximum adsorption. The equilibrium adsorption data were analyzed with the Langmuir, Freundlich, and Temkin models. The adsorption process closely agreed with the Langmuir adsorption isotherm, and the monolayer saturation adsorption value was achieved as 131.58 mg g. The adsorption kinetics follow the pseudo-second-order (PSO) model that illustrated the rate controlling step might be chemisorption. Thermodynamic investigations for the removal process were conducted by determining the values of ∆G°, ∆H°, and ∆S°. The adsorption behavior of Pb(II) on the Sep-FeO-MnO was a spontaneous and endothermic process. Several consecutive adsorption-desorption cycles confirmed that the proposed Sep-FeO-MnO nanocomposite could be reused after successive lead removal. Furthermore, the practical application of the adsorbent was successfully realized by the treatment of real Pb-contaminated water samples.
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http://dx.doi.org/10.1007/s11356-019-05119-9DOI Listing
June 2019

Efficacy of black seed (Nigella sativa L.) on kidney stone dissolution: A randomized, double-blind, placebo-controlled, clinical trial.

Phytother Res 2019 May 14;33(5):1404-1412. Epub 2019 Mar 14.

Pharmaceutical Sciences Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Preclinical studies have shown beneficial effects of black seed (Nigella sativa L.) in the prevention and treatment of renal stones. Hence, we designed a study to evaluate the renal-stone-dissolving efficacy of black seed. Sixty patients with renal stones were randomly enrolled in two arms of a randomized, triple-blind, placebo-controlled, clinical trial. The patients were treated by black seed capsules (500 mg) or placebo two times per day for 10 weeks. Patients were assessed in terms of size of renal stones by using sonography before and after intervention. In the black seed group, 44.4% of patients excreted their stones completely, and the size of the stones remained unchanged and decreased in 3.7% and 51.8% of patients, respectively. In contrast, in the placebo group, 15.3% of the patients excreted their stones completely, 11.5% had reduction in stone size, 15.3% had increase in stone size, and 57.6% had no change in their stone size. The difference in the mean size of renal stones after the study was significant between the two groups (p < 0.05). N. sativa L., as compared with placebo, is demonstrated to have significant positive effects on disappearance or reduction of size of kidney stones.
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http://dx.doi.org/10.1002/ptr.6331DOI Listing
May 2019

Efficacy of Anise (Pimpinella anisum L.) oil for migraine headache: A pilot randomized placebo-controlled clinical trial.

J Ethnopharmacol 2019 May 7;236:155-160. Epub 2019 Mar 7.

Student Research Committee, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

Seyed Hamdollah Mosavat has made substantial contributions in conception, designing, acquisition of data and preformed clinical trial., Amin Moayedfard and Abbas Rahimi Jaberi had contribution in designing and preformed clinical trial. Zahra Sobhani and Maryam Mosaffa-Jahromi designed and prepared drugs of study. Aida Iraji has made drug biochemical assay. Seyed Hamdollah Mosavat had contribution in designing and revised the manuscript critically for important intellectual content and had contribution in designing and analyzing of data. Seyed Hamdollah Mosavat, Amin Moayedfard and Abbas Rahimi Jaberi had contribution in conception and designing and revised the manuscript critically for important intellectual content. All authors read and approved the final manuscript.
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http://dx.doi.org/10.1016/j.jep.2019.01.047DOI Listing
May 2019

Multi-target inhibitors against Alzheimer disease derived from 3-hydrazinyl 1,2,4-triazine scaffold containing pendant phenoxy methyl-1,2,3-triazole: Design, synthesis and biological evaluation.

Bioorg Chem 2019 03 29;84:363-371. Epub 2018 Nov 29.

Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran.

Alzheimer's disease (AD) is a complex neurological disorder with diverse underlying pathological processes. Several lines of evidence suggest that BACE1 is a key enzyme in the pathogenesis of AD and its inhibition is of particular importance in AD treatment. Ten new 3-hydrazinyl-1,2,4-triazines bearing pendant aryl phenoxy methyl-1,2,3-triazole were synthesized as multifunctional ligands against AD. We show that compounds containing Cl and NO groups at the para position of the phenyl ring, namely compounds 7c (IC = 8.55 ± 3.37 µM) and 7d (IC = 11.42 ± 2.01 µM), possess promising BACE1 inhibitory potential. Furthermore, we assessed the neuroprotective activities of 7c and 7d derivatives in PC12 neuronal cell line, which showed moderate protection against amyloid β peptide toxicity. In addition, compound 7d demonstrated metal chelating activity and moderate antioxidant potential (IC = 44.42 ± 7.33 µM). Molecular docking studies of these molecules revealed high-affinity binding to several amino acids of BACE1, which are essential for efficient inhibition. These results demonstrate that 1,2,4-triazine derivatives bearing an aryl phenoxy methyl-1,2,3-triazole have promising properties as therapeutic agents for AD.
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http://dx.doi.org/10.1016/j.bioorg.2018.11.038DOI Listing
March 2019