Publications by authors named "Mahnaz Khanavi"

77 Publications

Phytocatalytic and cytotoxic activity of the purified laccase from bled resin of Pistacia atlantica Desf.

Int J Biol Macromol 2021 Apr 3;176:394-403. Epub 2021 Feb 3.

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

This study reports an efficient and fast procedure for the purification of laccase (PaL) obtained from the resin of Pistacia atlantica Desf. It was purified by one-step affinity chromatography and showed the specific activity of 393 U/mg with 81.9-fold purification. The molecular weight of PaL was estimated to be approximately 60 kDa using gel electrophoresis SDS-PAGE. Moreover, it depicted diphenolase activity and high affinity towards 2,6-dimethoxy phenol (K = 10.01 ± 0.5 mM) and syringaldazine (K = 6.57 ± 0.2 mM) comparing with plant-origin polyphenol oxidases reported in the literature. It should be noted that PaL possessed optimal activity at pH 7.5 and 45 °C. It also remained stable under different conditions of pH (6.5-8.0), temperature (25-45 °C), and when it was exposed to several metal ions. The MTT and flow cytometry assays demonstrated that the enzyme treatment significantly affected growth of HeLa, HepG2, and MDA-MB-231 cells with LC values of 4.83 ± 0.02, 61 ± 0.31, and 26.83 ± 0.11 μM after 72 h, respectively. NOVELTY STATEMENT: This is the first attempt to isolate and characterize a new oxidoreductase from the resin of Pistacia atlantica Desf., native species of Iran, to recruit it in cytotoxicity researches. In the purification process by an efficient affinity column (SBA-NH-GA), the enzyme was eluted promptly with a satisfied yield. The purified laccase exerted higher affinity to diphenolic compounds and pH-thermal stability compared to other plant-derived polyphenol oxidases. The purified enzyme was found to show anti-oxidant capacity and significantly inhibited the growth of cancerous cells in vitro. PaL showed more cytotoxic activity towards HeLa and MDA-MB-231 cells by induction of apoptosis. The cytotoxic activity of the laccase was measured by flow cytometry.
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http://dx.doi.org/10.1016/j.ijbiomac.2021.01.212DOI Listing
April 2021

Phytochemical constituents and biological activities of Salvia macrosiphon Boiss.

BMC Chem 2021 Jan 19;15(1). Epub 2021 Jan 19.

Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

Salvia macrosiphon Boiss. is an aromatic perennial herb belonging to the family Lamiaceae. Phytochemical studies and biological activities of this plant have been rarely documented in the literature. The current study aimed to investigate antibacterial and cytotoxic activity of different fractions of aerial parts of S. macrosiphon. Also, we tried to isolate and identify cytotoxic compounds from the plant. In this respect, the hydroalcoholic extract of the corresponding parts of the plant was fractionated into four fractions. Then, antibacterial and cytotoxic activity of each fraction were examined. It was found that the chloroform fraction had a good antibacterial activity against gram-positive and gram-negative bacteria. The most potent cytotoxicity was also obtained by the n-hexane fraction comparing with etoposide as the reference drug which was selected for the study and characterization of secondary metabolites. Accordingly, 13-epi manoyl oxide (1), 6α-hydroxy-13-epimanoyl oxide (2), 5-hydroxy-7,4'-dimethoxyflavone (3), and β-sitosterol (4) were isolated and evaluated for their cytotoxic activity. Among them, compound 1 revealed significant cytotoxicity against A549, MCF-7, and MDA-MB-231. It merits mentioning that it showed high selectivity index ratio regarding the low cytotoxic effects on Human Dermal Fibroblast which can be considered as a promising anticancer candidate.
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http://dx.doi.org/10.1186/s13065-020-00728-9DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7814726PMC
January 2021

Polyurethane/carboxymethylcellulose nanofibers containing Malva sylvestris extract for healing diabetic wounds: Preparation, characterization, in vitro and in vivo studies.

Mater Sci Eng C Mater Biol Appl 2020 Sep 1;114:111039. Epub 2020 May 1.

Department of Pharmacognosy, Faculty of Pharmacy and Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran; Faculty of Land and Food Systems, University of British Columbia, Vancouver, BC, Canada. Electronic address:

In this study, new polyurethane (PU)-based nanofibers wound dressings containing Malva sylvestris extract were prepared and their effect on diabetic wound healing process was evaluated. Different amounts of carboxymethyl cellulose (CMC) were used to improve the absorption ability of wound exudates. The result showed that the usage of 20% w/w CMC in the polymer blend; and producing of nanofibers with an average diameter of 386.5 nm, led to the gradual release of the herbal compound in 85 h and bead-free morphology. Due to the antibacterial activity of wound dressing and wound healing process, the amount of 15% w/w herbal extract was selected as the optimum. For this sample, the fluid absorption was 412.31%. The extract loaded wound dressing samples showed satisfactory effects on Staphylococcus aureus and Escherichia coli bacteria. In vivo wound-healing and histological performance observations indicated that the use of the herbal extract in wound dressing improved wound healing significantly. On day 14, the average healing rate for gauze bandage, PU/CMC, and different amounts of 5, 10, 15 and 20% w/w extract containing wound dressings was 32.1 ± 0.2%, 51.4 ± 0.4%, 71 ± 0.14%, 87.64 ± 1.02%, 95.05 ± 0.24% and 95.11 ± 0.2%, respectively. Compared to the control groups, treatments with extract loaded wound dressings were effective in lowering acute and chronic inflammations. In diabetic rat wounds, collagen deposition and neovascularization were higher in wounds treated with an herbal extract containing wound dressing compared to the wounds treated with a gauze bandage and PU/CMC treated wounds. It can be suggested that this product may be considered as a good dual anti-inflammatory-antimicrobial wound dressing candidate for improving the diabetic wound healing.
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http://dx.doi.org/10.1016/j.msec.2020.111039DOI Listing
September 2020

Phytochemical investigation and anticholinesterase activity of ethyl acetate fraction of Houtt. seeds.

Nat Prod Res 2020 Jul 8:1-7. Epub 2020 Jul 8.

Faculty of Pharmacy, Medicinal Plants Research Center, Tehran University of Medical Sciences, Tehran, Iran.

In this work, -hexane, chloroform, and ethyl acetate fractions of the methanol extract of Houtt. seeds were evaluated against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) Ellman's method. It was found that all fractions depicted no anti-AChE activity, however, they were active toward BChE with IC values of 361.8, 215.0, and 145.8 µg/mL, respectively comparing with donepezil as the reference drug (IC = 1.97 µg/mL). The ethyl acetate fraction which also showed high neuroprotectivity and metal chelating ability was selected for the phytochemical analysis. Our results confirmed the presence of trimyristin and 5,7-diacetyl chrysin (reported for the first time in ) in the corresponding fraction.
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http://dx.doi.org/10.1080/14786419.2020.1788555DOI Listing
July 2020

Bioactive compounds with possible inhibitory activity of Angiotensin-Converting Enzyme-II; a gate to manage and prevent COVID-19.

Med Hypotheses 2020 10 16;143:109841. Epub 2020 May 16.

Medicinal Plants Processing Research Center, Shiraz University of Medical Sciences, Shiraz, Iran; Epilepsy Research Center, Shiraz University of Medical Sciences, Shiraz, Iran; Department of Phytopharmaceuticals (Traditional Pharmacy), School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran. Electronic address:

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http://dx.doi.org/10.1016/j.mehy.2020.109841DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7229719PMC
October 2020

Efficacy of Extractions of Iranian Native Plants against Main Malaria Vector, in Iran for Making Appropriate Formulation for Disease Control.

J Arthropod Borne Dis 2019 Dec 31;13(4):344-352. Epub 2019 Dec 31.

Department of Medical Entomology and Vector Control, School of Public Health, Tehran University of Medical Sciences, Tehran, Iran.

Background: Malaria is the main vector-borne disease worldwide. There are several reports of insecticide resistant in malaria vectors worldwide due to using different insecticides. The aim of this study was to evaluate different native plant extortions against main malaria vector, in Iran for choosing the appropriate plant for formulation and use for vector control.

Methods: The larvae of were reared in insectary, extraction of plants were carried out at department of Pharmacology. The standard WHO method for biological tests was used for calculation of LC and LC. Probit regration lines were plotted for calculation of LC and LC.

Results: In this study several plants including: , , , , , , , , , , , , , , , were used. Results showed that and , had the lowest and highest LC respectively.

Conclusion: Results indicated that and had the lowest and highest LC respectively. Several other plant extract also showed significant mortality. The formulation of these plants should be prepared and evaluate at the field condition against malaria vectors.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7188767PMC
December 2019

Trachyspermum ammi (L.) Sprague, superb essential oil and its major components on peptic ulcers: in vivo combined in silico studies.

Daru 2019 Jun 19;27(1):317-327. Epub 2019 Jun 19.

Department of Toxicology and Pharmacology, Tehran University of Medical Sciences, Tehran, Iran.

Background: Trachyspermum ammi (L.) Sprague is used for treating gastrointestinal disorders. Several studies indicated gastric antiulcer activity of T. ammi extract, yet the effect of its essential oil has not been studied on.

Objectives: The present study evaluates chemical composition of T. ammi essential oil and anti-peptic ulcer effect of the essential oil as well as its three major components in ethanol induced-gastric ulcers in rats.

Methods: Primarily chemical composition of the essential oil was analyzed by gas chromatography-mass spectrometry (GC/MS). Rats received the essential oil (500, 250, 125, 62.5, 31.25 mg/kg), thymol (30, 100 mg/kg), para-cymene (100, 150 mg/kg) and gamma-terpinene (100, 150 mg/kg) using gavage tube along with ethanol 80%. Finally, dissected stomachs were assessed both macroscopically and microscopically to evaluate anti-ulcerative effect of the essential oil and the pure compounds. Moreover, molecular docking was utilized to explore the interactive behavior of the main components with active site residues of H/K ATPase.

Results: Analysis of the essential oil indicated that para-cymene (37.18%), gamma-terpinene (35.36%) and thymol (20.51%) are the main components. Administration of different doses of the essential oil noticeably diminished the number of peptic ulcers in a dose-dependent manner. Among the main components, thymol was more potent than para-cymene and gamma-terpinene. Administration of the essential oil (500 mg/kg) and thymol (100 mg/kg) observed maximum inhibition percentage (98.58% and 79.37%, respectively). Molecular docking study provides the evidence of thymol ability to inhibit H/K ATPase.

Conclusions: The findings revealed that T. ammi essential oil can be applied to treat gastric ulcer as a natural agent. Graphical abstract.
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http://dx.doi.org/10.1007/s40199-019-00279-yDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6593012PMC
June 2019

, a Bioactive Essential Oil: Chemical Composition and Biological Activities.

Iran J Pharm Res 2019 ;18(1):412-421

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

is an aromatic plant traditionally used for treatment of infections and gastrointestinal diseases. In the present study, the volatile oil of the plant was obtained by hydrodistillation and analyzed by GC-MS. In addition, antibacterial and anti- activities of this essential oil were determined using disc diffusion and agar dilution methods, respectively. Insecticidal activity was assessed through topical and fumigation application of the essential oil to cabbage looper larvae. Acetylcholinesterase (AChE) inhibition by the essential oil was examined using Ellman's method. Furthermore, its cytotoxic potential against three different cancer cell lines was assessed using the MTT assay. The phenolic monoterpenoids, thymol (38.79%), and carvacrol (36.30%) were identified as major constituents of the essential oil. We observed significant antibacterial activity of the essential oil against (MIC=20.4 µg /mL) as well as other tested bacteria, except for . essential oil showed significant toxicity to cabbage looper larvae with LD value of 52.1 µg /larva following topical and fumigant administration. essential oil was considerably inhibitory to acetylcholinesterase activity (IC50 = 0.117 µg/mL). Cytotoxic assay of the volatile oil resulted in IC50 = 0.065, 0.104, and 0.141 μg/mL for MCF-7, T47D and MDA- MB-231 cell lines, respectively. According to our data, this species with high concentrations of thymol and carvacrol could be considered as a natural source for pharmaceutical products.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6487399PMC
January 2019

Novel tacrine-coumarin hybrids linked to 1,2,3-triazole as anti-Alzheimer's compounds: In vitro and in vivo biological evaluation and docking study.

Bioorg Chem 2019 03 28;83:303-316. Epub 2018 Oct 28.

Department of Medicinal Chemistry, 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:

A new series of tacrine-coumarin hybrids linked to 1,2,3-triazole were designed, synthesized, and tested as potent dual binding site cholinesterase inhibitors (ChEIs) for the treatment of Alzheimer's disease (AD). Among them, compound 8e was the most potent anti-AChE derivative (IC = 27 nM) and compound 8m displayed the best anti-BChE activity (IC = 6 nM) much more active than tacrine and donepezil as the reference drugs. Compound 8e was also evaluated for its BACE1 inhibitory activity and neuroprotectivity against PC12 cells exposed to Aβ which indicated low activity. Finally, in vivo studies by Morris water maze task showed that compound 8e significantly reversed scopolamine-induced memory deficit in rats.
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http://dx.doi.org/10.1016/j.bioorg.2018.10.056DOI Listing
March 2019

Antioxidant and Larvicidal Activity of Areal Parts of against Malaria Vector .

J Arthropod Borne Dis 2018 Jun 13;12(2):119-126. Epub 2018 Jun 13.

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

Background: is a perennial plant which is native in all parts of Iran, Turkey, and Azerbaijan. In this study, the total phenol content, antioxidant and larvicidal activities of total extract and different fractions of this plant were evaluated.

Methods: The aerial parts of were collected from Boli village, Illam Province, western Iran in Apr 2013. The total phenol content of total extract and different fractions were evaluated by Folin-Ciocalteu method. Moreover, antioxidant activity was tested by DPPH and FRAPS assays. Larvicidal activity was investigated according to standard method described by WHO.

Results: Ethyl acetate fraction (EF) had the highest content of total phenol (75.9±0.06mg Gallic acid equivalent/g dry extract). Furthermore, among the tested extract, methanol-water fraction (MWF), total methanol extract (TME) and water fraction (WF) showed the highest antioxidant activity in the DPPH assay (IC= 226.8, 283.66 and 299.4 μg.ml, respectively). In FRAP assay MWF and WF and TME had the highest antioxidant activities (664.4±0.002, 565.3±0.003, 519.5±0.003mmol FeII/g dry extract, respectively). Ethyl acetate fraction had maximum larvicidal activity (LC 49.1ppm) followed by TME (LC 64.26ppm) and hexane fraction (HF) (LC 89.69).

Conclusion: collected from west of Iran illustrated considerable antioxidant and larvicidal effects and further in vitro and in vivo experimental models for investigation would be required.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6091803PMC
June 2018

Larvicidal Activity of Essential Oil and Extract against Malaria Vector, .

J Arthropod Borne Dis 2018 Mar 18;12(1):85-93. Epub 2018 Mar 18.

Department of Pharmacognosy, School of Pharmacy and Persian Medicine and Pharmacy Research Centre, Tehran University of Medical Sciences, Tehran, Iran.

Background: Malaria, a mosquito-transmitted disease, is still a major human health problem all over the world. Larviciding is a component of comprehensive control program to overcome the disease. Negative aspects of synthetic insecticides application, such as environmental safety concerns, have favored use of natural insecticides.

Methods: Larvicidal activity of essential oil, extracts and fractions of a wild grown and a cultivated type of fruits against malaria vector was assessed according to the method described by WHO.

Results: showed remarkable potency against larvae. LC values for essential oil, total extract, petroleum ether fraction and methanol fraction were 27.4284, 64.9933, 85.9933 and 255.7486ppm for wild type, and 21.3823, 63.2580, 62.7814 and 152.6357ppm for cultivated one.

Conclusion: The results of this study suggest as a valuable source of natural insecticides against malaria vector .
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6046109PMC
March 2018

Bio-guided isolation of subsp. cytotoxic components.

Nat Prod Res 2019 Jun 19;33(11):1687-1690. Epub 2018 Feb 19.

d Department of Biotechnology , Iranian Research Organization for Science and Technology , Tehran , Iran.

subsp was extracted by 80% ethanol. The total extract was then partitioned into four fractions including chloroform, ethyl acetate and methanol. Cytotoxic effect of fractions was examined by MTT assay in K562 (chronic myelogenous leukemia), AGS (gastric adenocarcinoma), MCF-7 (breast adenocarcinoma) and SW742 (colon adenocarcinoma) cell lines. The Chloroform fraction, with the lowest LC against K-562 cell lines, was partitioned into 14 subfractions and subjected to further purification by reversed-phase (C18) silica gel and sephadex LH-20 column chromatography. Three flavonoids including cirsimaritin, cirsilinelol and eupatilin were isolated for the first time from the species and the structures were confirmed by spectroscopic data. The high selectivity index of the purified flavonoids indicates valuable components with potential few side effects for normal cell lines. However, solubility tests for isolated components indicates the need for novel pharmaceutical dosage forms, in the case for using natural flavonoids as chemotherapeutic agents.
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http://dx.doi.org/10.1080/14786419.2018.1428590DOI Listing
June 2019

Design and synthesis of novel coumarin-pyridinium hybrids: In vitro cholinesterase inhibitory activity.

Bioorg Chem 2018 04 31;77:311-319. Epub 2018 Jan 31.

Department of Medicinal Chemistry, 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:

A novel series of coumarin-pyridinium hybrids were synthesized and evaluated as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using Ellman's method. Among synthesized compounds, 1-(3-fluorobenzyl)-4-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium bromide (7l) was found to be the most active compound toward AChE (IC = 10.14 µM), 1-(3-chlorobenzyl)-3-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium bromide (7g) and 1-(2,3-dichlorobenzyl)-3-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium chloride (7h) depicted the best BChE inhibitory activity (ICs = 0.32 and 0.43 µM, respectively). Although most compounds showed moderate to good anti-AChE activity, their anti-BChE activity was more significant and compound 7g was found as the most selective BChE with SI of 101.18. Also, kinetic study of the compounds 7g and 7l displayed a mixed type inhibition for both AChE and BChE. Furthermore, they were evaluated against β-secretase; however, they showed low inhibitory activity.
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http://dx.doi.org/10.1016/j.bioorg.2018.01.013DOI Listing
April 2018

Effect of the methanolic extracts of different parts of on naloxone-induced withdrawal behavior in morphine-dependent mice.

Avicenna J Phytomed 2017 Sep-Oct;7(5):426-435

Department of Toxicology and Pharmacology and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

Objective: a native species in Iran, is used for treatment of several diseases particularly for neurological disorders in Iranian Traditional Medicine. The aim of this study is to investigate the effect of methanolic roots, fruits, and aerial parts extracts of on withdrawal syndrome in morphine-dependent mice.

Materials And Methods: Aerial parts, roots, and fruits of the plant were separately extracted with 80% MeOH. For induction of dependence, morphine (50, 50 and 75 mg/kg) was injected subcutaneously three times daily (10 am, 1 pm and 4 pm) for three days and a last dose of morphine (50 mg/kg) was administrated on the fourth day. Withdrawal syndrome was induced by injection of naloxone (5 mg/kg, intraperitoneal) 2 hr after the final dose of morphine. Different doses of the extracts were administered i.p. 60 minutes before naloxone injection and withdrawal sign was recorded 2 minutes after naloxone injection for a period of 60 minutes.

Results: Pre-treatment of animals with different doses (2.5, 5, 10, 20 mg/kg) of methanolic extract of the aerial parts of caused a significant decrease in naloxone-induced behavior. Intraperitoneal administration of different doses (10, 15, 20, 25 mg/kg) of methanolic extract of the fruit significantly reduced the naloxone-induced withdrawal behavior (p<0.001).

Conclusion: It might be concluded that the extracts of affect morphine withdrawal syndrome possibly via interference with the neurotransmitters in nervous system.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5641417PMC
October 2017

Chemodiversity of Nepeta menthoides Boiss. & Bohse. essential oil from Iran and antimicrobial, acetylcholinesterase inhibitory and cytotoxic properties of 1,8-cineole chemotype.

Nat Prod Res 2018 Nov 15;32(22):2745-2748. Epub 2017 Oct 15.

a Faculty of Pharmacy and Medicinal Plants Research Centre, Department of Pharmacognosy , Tehran University of Medical Sciences , Tehran , Iran.

The essential oil of Nepeta menthoides Boiss. & Bohse., from Iran, was analysed by GC/MS. Two types of multivariate analyses were done based on the chemical composition of the investigated sample in this study and 12 other samples reported in the literature to show the chemodiversity in essential oil composition. Antimicrobial, acetylcholinesterase inhibitory and cytotoxic activities of the essential oil and its major component were assessed. Twenty-one compounds were identified, representing 96.81% of the total oil and the major constituent was 1,8-cineole (70.06%). Multivariate analyses revealed two chemotypes, i.e. nepetalactone and 1,8-cineole. The essential oil of the sample investigated in this study which was a 1,8-cineole chemotype and 1,8-cineole showed moderate antimicrobial activity and significantly inhibited the activity of acetylcholinesterase enzyme. Cytotoxicity evaluation against three breast cancer cell lines showed a potent inhibitory activity. Further investigations are necessary to confirm the variety in several populations of N. menthoides.
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http://dx.doi.org/10.1080/14786419.2017.1378202DOI Listing
November 2018

Chemical Constitute and Larvicidal Activity of Fractions of Plant against Malaria Vector .

J Arthropod Borne Dis 2017 Mar 14;11(1):116-123. Epub 2017 Mar 14.

Department of Medical Entomology and Vector Control, School of Public Health, Tehran University of Medical Sciences, Tehran, Iran.

Backgrand: The genus , belongs to Lamiaceae family, is one of the exclusive subspecies in the flora of Iran. The plants of this genus are used traditionally for treatment of joints pain, gout, jaundice, and as insecticide.

Methods: larvicidal activity of methanol 80% extract and partition fractions of hexane, chloroform, and ethyl acetate obtained from aerial parts of subspecies against malaria vector was evaluated. Phytochemical study of active fraction was analyzed using column chromatography and spectroscopy.

Results: According to the results, among different fractions, hexane fraction has the most larvicidal activity with mortality rate of 100% in concentration of 102 ppm and LC of 95.66ppm. The structure of compound 1, main phytoecdysteroid compound separated from hexane fraction, was determined to be ajugalide-E.

Conclusion: The results suggested that the hexane fraction of subsp could be used as a natural and biodegradable insecticide.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5629293PMC
March 2017

In vitro cholinesterase inhibitory activity of some plants used in Iranian traditional medicine.

Nat Prod Res 2017 Nov 6;31(22):2690-2694. Epub 2017 Mar 6.

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

In this study, in vitro evaluation of cholinesterase inhibitory (ChEI) activity of various plants including betel nuts (Areca catechu L.), clove buds (Syzygium aromaticum L.), aerial parts of dodder (Cuscuta chinensis Lam.), common polypody rhizomes (Polypodium vulgare L.) and turpeth roots (Ipomoea turpethum R. Br.) which were recommended for the treatment of AD symptoms in Iranian Traditional Medicine (ITM) is reported. Among them, aqueous extract of A. catechu L. was found as the most potent anti-AChE (IC = 32.00 μg/mL) and anti-BChE (IC = 48.81 ± 0.1200 μg/mL) agent.
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http://dx.doi.org/10.1080/14786419.2017.1290620DOI Listing
November 2017

Antinociceptive effect of extracts of Jacq. aerial parts.

Avicenna J Phytomed 2017 Jan-Feb;7(1):73-79

Department of Pharmacognosy, Faculty of Pharmacy and Persian Medicine and Pharmacy Research center, Tehran University of Medical Sciences, Tehran, Iran; Faculty of Land and Food Systems, University of British Columbia, B.C., Canada.

Objective: The genus is used for treatment of joint pain, gout, stomach-ache and colic in Iranian Traditional Medicine. Jacq. () is a native species in the flora of Iran. The aim of this study was to evaluate the antinociceptive properties of various extracts of aerial parts of .

Materials And Methods: Antinociceptive activities of total hydroalcoholic extract (THE) and its n-hexane (non-polar) and residual partition (polar) fractions were analyzed using formalin test in mice. Morphine (5 mg/kg) and normal saline were used as positive and negative controls, respectively.

Results: Intraperitoneal administration of THE (50, 100 and 200 mg/kg), non-polar fraction (200 mg/kg) and polar fraction (100 and 200 mg/kg), 30 min before formalin injection, caused significant analgesic activity in acute phase (0-5 min after formalin injection) of formalin test (p<0.05 as compared to control and p>0.05 in comparison with morphine). In chronic phase (15-60 min after formalin injection), non-polar and polar fractions (50, 100 and 200 mg/kg) showed significant analgesic activity (p<0.001 as compared to control and p>0.05 in comparison with morphine).

Conclusion: Different extracts of demonstrated antinociceptive activity that support the traditional usage of genus for the treatment of arthritis, gout and other inflammatory diseases.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5329179PMC
March 2017

New Benzodioxole Compounds from the Root Extract of .

Iran J Pharm Res 2016 ;15(4):901-906

Department of Pharmacognosy, Faculty of Pharmacy and Medicinal Plant Research Center, Tehran University of Medical Sciences, Tehran, Iran.

There are many efforts for identification of natural compounds from dietary or medicinal plants. Young roots and aerial parts of have been used as food additive or salad vegetable in some parts of Iran. In this study, different fractions of the root extract of were subjected for isolation and purification of secondary metabolites. The methanol extract of the roots was fractionated with hexane (HE), chloroform (CL), ethyl acetate (EA) and methanol (ME). Five novel compounds were isolated from HE, CL and EA using different chromatographic techniques and were identified by H-NMR, C-NMR, 2D-NMR and MS spectroscopic methods. Elucidated compounds with benzodioxole structure were characterized for the first time as 5-((propanoyl methyl)amino)-4,7-dimethoxybenzo[][1,3]dioxole (1), 5-(3-ethyloxiran-2-yloxy)-4,7-dimethoxybenzo[][1,3]dioxole (2), 4,7-dimethoxy-5-(propanonyl) benzo[][1,3]dioxole (3), 4-ethoxybenzo[][1,3]dioxol-6-carbaldehyde (4), and 4-(O-β-D-glucopyranosyl)-6-(3-propanyloxiran-2-yloxy)benzo[][1,3]dioxole (5).
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5316270PMC
January 2016

Molecularly Imprinted Polymer of Colocynthin, An Effective Tool for Quality Control of Citrullus colocynthis Extracts.

Curr Drug Discov Technol 2017 ;14(3):169-180

Food and Drug Control Laboratories and Research Center, MOH and ME, P.O. Box 11136-15911, Tehran. Iran.

Background: Different parts of Colocynth, Citrullus colocynthis (L.) Schrad., are used in traditional phytotherapy and homeopathy.

Objective: In our new approach, a molecularly imprinted polymer was synthesized to absorb colocynthin, the major plant marker, and its capability was evaluated using HPLC-UV.

Method: A new method was considered to achieve optimal conditions. FT-infrared, N2 adsorption porosimetry, fluorescent and scanning electron microscopy and thermo gravimetric profile of the polymers were studied. The imprinted polymer was applied as molecularly imprinted solid phase extraction sorbent to enrich colocynthin from colocynth oil extract, a traditional medicine dosage form.

Results: The imprinted polymer showed high capacity and affinity toward colocynthin. Physical assessments demonstrated no major differences between imprinted and nonimprinted polymers. The imprinted polymer was able to absorb colocynthin more efficiently than non-imprinted and control simple solvent extraction from the real sample.

Conclusion: In conclusion, this polymer is capable of being applied as a promising adsorbent for analysis of colocynth traditional medicine products.
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http://dx.doi.org/10.2174/1570163814666170104152226DOI Listing
June 2018

Therapeutic Effect of Ethanolic Extract against Localized Cutaneous Leishmaniasis Caused by (MRHO/IR/75/ER).

Iran J Public Health 2016 Oct;45(10):1340-1347

Dept. of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran; Dept. of Pharmacology and Toxicology, Pharmaceutical Sciences Branch, Islamic Azad University, Tehran, Iran.

Background: We evaluated the effect of the ethanolic extract of on the Iranian strain of (MRHO/IR/75/ER) both in vitro and in vivo conditions.

Methods: The effective dose (ED) of ethanolic extract of were determined using MTT assay on the growth of promastigote forms of in axenic culture media. Then, the ED of on mice peritoneal macrophages was determined using calculation of amastigote forms on mice peritoneal macrophages. For in vivo experiments, the therapeutic effects of various concentrations of on infected BALB/c mice was studied. A total of 75 infected mice were randomly divided into five groups: two groups (10% and 50% of ) as experimental and three as control (ethanol 50%, Glucantime® and no treatment). The efficacy were determined by comparing the diameters of lesions and the microscopically examinations.

Results: The effect of extract (0/625%, 1/25%, 2/5%, 5%, 10%, 20% and 50%) on peritoneal macrophages of Balb/c mice infected with in tissue-culture slides was assessed. extract (10%) removed the amastigotes-infected macrophages significantly after 24 h ( < 0.05). The higher concentrations of ethanolic extract (20%, and 50%) had highly toxic effects on macrophages, resulted in the disintegration of the cytoplasm of macrophages after 48 and 72 h. In concentration 10% of , more than 85% of amastigotes-infected macrophages were damaged without cytotoxicity effects on macrophages. The higher concentrations had toxic effects on cultured macrophages.

Conclusion: ethanolic extract 10% had anti leishmanial effects in both in vivo and in vitro.
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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5149498PMC
October 2016

Synthesis of novel chromenones linked to 1,2,3-triazole ring system: Investigation of biological activities against Alzheimer's disease.

Bioorg Chem 2017 02 24;70:86-93. Epub 2016 Nov 24.

Department of Medicinal Chemistry, 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, novel chromenones linked to 1,2,3-triazole ring system were synthesized and evaluated for their anti-ChE activity. Among them, N-((1-(2-chlorobenzyl)-1H-1,2,3-triazol-5-yl)methyl)-8-methoxy-2-oxo-2H-chromene-3-carboxamide (6m) showed good anti-acetylcholinesterase activity (IC=15.42μM). Also, compound 6m demonstrated neuroprotective effect against HO-induced cell death in PC12 neurons, however, it showed no beta-secretase (BACE1) inhibitory activity. Docking and kinetic studies separately confirmed dual binding activity of compound 6m since it targeted both the catalytic active site (CAS) and the peripheral anionic site (PAS) of AChE.
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http://dx.doi.org/10.1016/j.bioorg.2016.11.011DOI Listing
February 2017

Novel Tacrine-Based Pyrano[3',4':5,6]pyrano[2,3-b]quinolinones: Synthesis and Cholinesterase Inhibitory Activity.

Arch Pharm (Weinheim) 2016 Dec 7;349(12):915-924. Epub 2016 Nov 7.

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

In order to develop effective anti-cholinesterase compounds, a novel series of pyrano[3',4':5,6]pyrano[2,3-b]quinolinones were designed, synthesized, and evaluated in vitro against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All derivatives showed very good AChE inhibitory (AChEI) activity (IC  = 0.37-5.62 μM) compared with rivastigmine (IC  = 11.07 μM). Among them, 11-amino-12-(2,3-dichlorophenyl)-3-methyl-7,8,9,10-tetrahydropyrano[3',4':5,6]pyrano[2,3-b]quinolin-1(12H)-one (6f) displayed the best inhibitory activity. However, most of the synthesized compounds showed no anti-BChE activity and compounds 6b and 6f were found to be only moderate inhibitors. The most potent anti-AChE compound 6f had low and moderate inhibitory activity and neuroprotective effects against beta-secretase (BACE1) and oxidative stress-induced cell death, respectively. Also, kinetic and molecular docking studies of binding interactions elucidated that compound 6f bound to both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of AChE.
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http://dx.doi.org/10.1002/ardp.201600123DOI Listing
December 2016

Novel tacrine-1,2,3-triazole hybrids: In vitro, in vivo biological evaluation and docking study of cholinesterase inhibitors.

Eur J Med Chem 2017 Jan 8;125:1200-1212. Epub 2016 Nov 8.

Department of Medicinal Chemistry, 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:

A new series of tacrine-1,2,3-triazole hybrids were designed, synthesized, and evaluated as potent dual cholinesterase inhibitors. Most of synthesized compounds showed good in vitro inhibitory activities toward both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Among them, 7-chloro-N-((1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)-1,2,3,4-tetrahydroacridin-9-amine (5l) was found to be the most potent anti-AChE derivative (IC = 0.521 μM) and N-((1-(4-methoxybenzyl)-1H-1,2,3-triazol-4-yl)methyl)-1,2,3,4-tetrahydroacridin-9-amine (5j) demonstrated the best anti-BChE activity (IC = 0.055 μM). In vivo studies of compound 5l in Morris water maze task confirmed memory improvement in scopolamine-induced impairment. Also, molecular modeling and kinetic studies showed that compounds 5l and 5j bound simultaneously to the peripheral anionic site (PAS) and catalytic sites (CS) of the AChE and BChE.
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http://dx.doi.org/10.1016/j.ejmech.2016.11.008DOI Listing
January 2017

Cytotoxic Potential of Centaurea bruguierana ssp. belangerana: The MTT Assay.

Acta Med Iran 2016 Sep;54(9):583-589

Department of Pharmacognosy, Medicinal Plants Research Center, Tehran University of Medical Sciences, Tehran, Iran. AND Faculty of Land and Food Systems, University of British Columbia, Vancouver, Canada.

The genus Centaurea with an extensive background in Iranian traditional medicine represents more than 70 species in Iran that some of them are endemic to Iran. A variety of secondary metabolites has been isolated from this genus thus far. Sesquiterpene lactones and flavonoids have been reported as main compounds of C.bruguierana. Methanolic extract and different fractions of the whole fruiting samples of Centaurea bruguierana ssp.belangerana (Asteraceae) were examined for cytotoxicity against various cell lines using MTT cytotoxicity assay in order to identify active fraction(s). The chloroform and ethyl acetate fractions of plant have demonstrated significant cytotoxicity against colon adenocarcinoma and breast ductal carcinoma cell lines, which chloroform fraction, exhibited the most potent in vitro cytotoxic activity against colon adenocarcinoma cell line, and therefore, can be considered as the potential fraction through main compounds of plant against the adenocarcinoma colon cancer cell line. Moreover, only chloroform fraction was moderately active against Swiss embryo fibroblast cell lines while the other fractions were nontoxic. To summarize, the chloroform fraction of C.bruguierana demonstrated better cytotoxic activity against all of the tested cell lines compared with the other fractions; and promisingly in some cases represented moderate to very good cytotoxicity that suggests more investigations about its phytochemical properties.
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September 2016

Burn Wound Healing Activity of Lythrum salicaria L. and Hypericum scabrum L.

Wounds 2016 Sep 29. Epub 2016 Sep 29.

Department of Pharmacognosy, Faculty of Pharmacy and Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran and Faculty of Land and Food Systems, University of British Columbia, Vancouver, Canada.

Objective: Burns are complicated traumatic injuries caused by several physical or chemical factors. Plants with a wide range of secondary metabolites, with valuable properties like antioxidant and anti-inflammatory activities, can be a promising source of wound healing agents.

Materials And Methods: Effects of hydromethanolic extracts of Lythrum salicaria and Hypericum scabrum, individually and in combination, were assessed in second-degree burn wounds in rats in comparison to a white oleaginous base (negative control) and silver sulfadiazine (positive control). Histological assessments as well as total thiol molecules, lipid peroxidation, and total antioxidant power were evaluated in skin tissue samples. Total phenol, flavonoids, and tannins along with the antioxidant and antimicrobial activities of the extracts were also as- sessed.

Results: Total phenol, total flavonoid, and total tannin amounts for L. salicaria and H. scabrum were 331 ± 3.7 and 308.1 ± 5.2 μg gallic acid/mg extract, 5.8 ± 0.4 and 4.3 ± 0.3 μg quercetin/mg extract, and 430 ± 2.33 and 13.4 ± 0.5 μg tannic acid/mg extract, respectively. H. scabrum significantly inhibited S. aureus and L. salicaria moderately suppressed Staphylococcus aureus and Candida albicans growth. Wound contraction percentage with L. salicaria and H. scabrum was 89.5 ± 3.7 and 77.6 ± 4.1, respectively. A well-organized epidermal layer and normal appearance in dermis layer were more observable in the L. salicaria group. Moreover, L. salicaria ointment individually displayed better influence on tissue oxidative stress parameters than H. scabrum and the negative control (P < 0.05).

Conclusion: Results of this study clearly confirm the effectiveness of L. salicaria topical ointment as a wound healing agent, possibly due to the considerable polyphenolic content and antioxidant properties.
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September 2016

Medicinal Plants Used in Iranian Traditional Medicine (ITM) as Contraceptive Agents.

Curr Pharm Biotechnol 2016;17(11):974-85

Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical, Sciences, P.O. Box: 14176, Tehran, Iran.

Background: In recent years, rapid population growth and unsafe abortions have emerged as controversial health issues in some countries. Hence, safe and effective contraceptive methods or agents have attracted a great deal of attention and the corresponding market has been widely expanded.

Objective: In this study, we present a review profiting from Iranian Traditional Medicine (ITM) to introduce expedient plants as efficient contraceptive agents.

Methods: Medicinal plants suggested as contraceptive agents were obtained from ITM text books and they were also investigated using search engines to confirm their in vitro and in vivo efficacy.

Results: According to credible Iranian medical literature a wide spectrum of plants possesses contraceptive activity and among them, Ruta graveolens, Ricinus communis, Piper nigrum, and Physalis alkekengi were found to be more efficient.

Conclusion: Complementary and Alternative Medicine (CAM), particularly herbal remedies have received a lot of attention because of their truly healing properties. Focusing on ITM knowledge, there are various comments based on medicinal plants to reduce unsafe abortions leading to better public health in the society.
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http://dx.doi.org/10.2174/1389201017666160808162331DOI Listing
December 2016

Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.

Bioorg Chem 2016 08 2;67:84-94. Epub 2016 Jun 2.

Department of Medicinal Chemistry, 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:

A novel series of acridine-chromenone and quinoline-chromenone hybrids were designed, synthesized, and evaluated as anti-Alzheimer's agents. All synthesized compounds were evaluated as cholinesterases (ChEs) inhibitors and among them, 7-(4-(6-chloro-2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamino)phenoxy)-4-methyl-2H-chromen-2-one (8e) exhibited the most potent anti-acetylcholinesterase (AChE) inhibitory activity (IC50=16.17μM) comparing with rivastigmine (IC50=11.07μM) as the reference drug. Also, compound 8e was assessed for its β-secretase (BACE1) inhibitory and neuroprotective activities which demonstrated satisfactory results. It should be noted that both kinetic study on the inhibition of AChE and molecular modeling revealed that compound 8e interacted simultaneously with both the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE.
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http://dx.doi.org/10.1016/j.bioorg.2016.06.001DOI Listing
August 2016

An Evidence-Based Review on Medicinal Plants Used as Insecticide and Insect Repellent in Traditional Iranian Medicine.

Iran Red Crescent Med J 2016 Feb 13;18(2):e22361. Epub 2016 Feb 13.

Department of Traditional Pharmacy, Faculty of Traditional Medicine, Tehran University of Medical Sciences, Tehran, IR Iran; Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, IR Iran; Department of Pharmacognosy, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, IR Iran.

Context: Insects can be the cause of major ecological problems; they can transmit microbes and parasites that affect humans, and damage food crops, trees, and homes. The total economic cost of insect-related damage and disease is immeasurable. In traditional Iranian medicine (TIM), several medicinal plants have been identified as insecticides or insect repellents, but many of them are still unknown. Therefore, the aim of this study was to review the insecticidal or insect repellent activity of certain medicinal plants described in TIM.

Evidence Acquisition: Information about medicinal plants proposed as insecticides and insect repellents in the TIM was collected from the TIM literature, and searched in modern medical databases to find studies that confirmed their efficacy.

Results: Modern investigations have supported the claims of the insecticidal activity of several plants, including Allium sativum, Artemisia absinthium, Citrullus colocynthis, Laurus nobilis, Mentha pulegium, Myrtus communis, Nerium oleander, Ocimum basilicum, and Origanum majorana. However, in the cases of plants like Iris florentina and Malva sylvestris, there is not enough evidence in modern medicine to prove their effectiveness with regard to their insecticidal and insect repellent activities.

Conclusions: This study confirmed the Iranian traditional medicine claims of the insecticidal and insect repellent activity of certain plants. Further pharmacological and clinical studies are recommended to evaluate the overall efficacy and possible mechanisms underlying these herbs.
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http://dx.doi.org/10.5812/ircmj.22361DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4867175PMC
February 2016

Phytochemical analysis, antimicrobial, antioxidant activities and total phenols of Ferulago carduchorum in two vegetative stages (flower and fruit).

Pak J Pharm Sci 2016 Mar;29(2):623-8

Department of Pharmacognosy, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran / Faculty of Land and Food Systems, University of British Columbia, Vancouver, BC, Canada.

Ferulago carduchorum (Apiaceae family) is an endemic plant of Iran. The crude extract and four fractions of aerial parts of F. carduchorum in two vegetative stages (flower and fruit) were studied for their total phenolic contents, antimicrobial and antioxidant activities using folin-ciocalteu assay, micro dilution method and DPPH assay, respectively. The results indicated that the best antioxidant activity was determined in flower crude extract (IC50=0.44 mg/mL). The flower ethyl acetate fraction (FLE) showed better antimicrobial and antifungal activities than other fractions. So, FLE was selected for phytochemical investigations, resulting in isolation of a flavonoid (hesperetin). Hesperetin showed antimicrobial activity. The results showed that the antimicrobial and antioxidant effects during the flowering are obviously more than the fruit season.
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March 2016