Iranian Journal of Pharmaceutical Research : IJPR最新文献

{"title":"3-Hydroxypyrimidine-2, 4-dione Derivatives as HIV Reverse Transcriptase-Associated RNase H Inhibitors: QSAR Analysis and Molecular Docking Studies.","authors":"Azar Mostoufi,&nbsp;Narges Chamkouri,&nbsp;Samaneh Kordrostami,&nbsp;Elham Alghasibabaahmadi,&nbsp;Ayyub Mojaddami","doi":"10.22037/ijpr.2020.1101004","DOIUrl":"https://doi.org/10.22037/ijpr.2020.1101004","url":null,"abstract":"<p><p>AIDS, as a lethal disease, is caused by infection with the HIV virus that affects millions of people. Three essential enzymes should be encoded for replication of HIV virus: protease, integrase and reverse transcriptase (RT). RT has two different activities including DNA polymerase and ribonuclease H (RNase H). However, all of the marketed RT inhibitors target only the DNA polymerase activity. Therefore, ribonuclease H activity may serve as a new target for drug discovery. In the present study, a series of 3-Hydroxypyrimidine-2, 4-dione derivatives as potent RT-associated RNase H inhibitors were applied to QSAR analysis. Two methods including multiple linear regressions (MLR) and partial least squared based on genetic algorithm (GA-PLS) were utilized to find the relationship between the structural feathers and inhibitory activities of these compounds. The best multiple linear regression equation was generated by GA-PLS method. A combination of 2D autocorrelations, topological, atom-centered, and geometrical descriptors were selected by GA-PLS as they had more effects on the inhibitory activity. Then, the molecular docking studies were carried out. The results showed that the important amino acids inside the active site of the enzyme responsible for essential interactions were Gln475, Asp549, Tyr501, Ser515, Trp534, Asp493, Tyr472, and Gln480 which took part in hydrogen bond formation. Furthermore, docking energy was plotted against pIC₅₀ predicted by GA-PLS method. The result showed that there is a good correlation with R²=0.71. Consequently, these findings suggest that the better method, GA-PLS, could be applied to design new compounds and predict their inhibitory activity.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"84-97"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462486/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38375673","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis of Flower-like Nickel Hydroxide Nanosheets and Application in Electrochemical Determination of Famotidine.","authors":"Rezvan Dehdari Vais,&nbsp;Hossein Yadegari,&nbsp;Hossein Heli","doi":"10.22037/ijpr.2019.14257.12245","DOIUrl":"https://doi.org/10.22037/ijpr.2019.14257.12245","url":null,"abstract":"<p><p>An electrochemical sensor was designed and fabricated for electrocatalytic oxidation and determination of famotidine in pharmaceutical forms. The electrochemical oxidation process and its kinetics were investigated using cyclic voltammetry, steady-state polarization measurements, and chronoamperometry techniques, and also the analytical measurements were performed by amperometry. Upon addition of the drug into the solution, cyclic voltammograms of the fabricated sensor exhibited an increased anodic peak current associated with a decrease in the corresponding cathodic current. These results suggested an electrocatalytic EC' oxidation mechanism for famotidine on the oxyhydroxide species immobilized on the electrode surface. Accordingly, a mechanism involving generation of Ni³⁺ active sites and their subsequent consumption by the drug was proposed. Moreover, the corresponding rate law under the control of charge transfer was developed and kinetic parameters were derived. A sensitive and time-saving amperometric procedure was also developed for the analysis of famotidine with a detection limit of 5.91 mmol L^-1. Using the developed amperometric procedure, famotidine was successfully analyzed in the presence of ibuprofen. The developed sensor in this study displayed enhanced sensitivity and selectivity, compared to some other reported methods.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"120-137"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462516/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38375676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Therapeutic Effect of Carvacrol-loaded Albumin Nanoparticles on Arthritic Rats.","authors":"Nasser Gholijani,&nbsp;Samira-Sadat Abolmaali,&nbsp;Kurosh Kalantar,&nbsp;Mohammad-Hadi Ravanrooy","doi":"10.22037/ijpr.2019.15494.13131","DOIUrl":"https://doi.org/10.22037/ijpr.2019.15494.13131","url":null,"abstract":"<p><p>Rheumatoid arthritis (RA) is one of the most common autoimmune diseases. Carvacrol, an important natural terpenoid product in aromatic plants such as <i>thyme</i>, has shown anti-inflammatory effects in animal models of arthritis. However, its poor water solubility and high volatility have limited its application. In the present study in order to overcome this problem, we encapsulated carvacrol in the bovine serum albumin (BSA) nanoparticles and examined its therapeutic and immunomodulatory effects in adjuvant-induced arthritis (AIA). Carvacrol-loaded BSA nanoparticles were prepared by desolvation method. Nanoparticles had encapsulation efficiency (EE) of 67.7 ± 6.9% and loading capacity (LC) of 26.6 ± 2%. The size of particles was 148 ± 25 nm and they had monomodal distribution. After arthritis induction, the rats were treated intraperitoneally with nanoparticle for every 3 days until day 28. The treatment of the rats with 375 mg/mL carvacrol-loaded BSA nanoparticle significantly decreased clinical severity score (27.5 ± 9.8%, <i>p</i> = 0.008), erythrocyte sedimentation rate (33.4 ± 10%, <i>p</i> = 0.02), nitric oxide production (82.3 ± 2.6%, <i>p</i> = 0.004) and interleukin (IL)-17 gene expression (55.1 ± 8.2%, <i>p</i> = 0.003) compared to the untreated arthritic group. A higher reduction in inflammation severity in arthritic rats treated with carvacrol-loaded BSA in comparison to those treated with carvacrol alone was observed. In conclusion, encapsulation of carvacrol in nanoparticles reduced arthritis signs and release of NO and IL-17 inflammatory cytokine and therefore is suggested to be considered as a good approach for improving the therapeutic applications of carvacrol in RA.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"312-320"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462511/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38376526","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Exogenous Ghrelin Could Not Ameliorate 3,4-methylenedioxymethamphetamine-induced Acute Liver Injury in The Rat: Involved Mechanisms.","authors":"Ravieh Golchoobian,&nbsp;Fatemeh Nabavizadeh,&nbsp;Mehrdad Roghani,&nbsp;Alireza Foroumadi,&nbsp;Maryam Izad,&nbsp;Maryam Bahrami,&nbsp;Hafseh Fanaei","doi":"10.22037/ijpr.2020.1100940","DOIUrl":"https://doi.org/10.22037/ijpr.2020.1100940","url":null,"abstract":"<p><p>MDMA (3,4-methylenedioxymethamphetamine, ecstasy) is often abused by youth as a recreational drug. MDMA abuse is a growing problem in different parts of the world. An important adverse consequence of the drug consumption is hepatotoxicity of different intensities. However, the underlying mechanism of this toxicity has not been completely understood. Ghrelin is a gut hormone with growth hormone stimulatory effect. It expresses in liver, albeit at a much lower level than in stomach, and exerts a hepatoprotective effect. In this study, we investigated hepatotoxicity effect of MDMA alone and its combination with ghrelin as a hepatoprotective agent. MDMA and MDMA+ ghrelin could transiently increase serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) followed by tissue necrosis. However, they could significantly decrease liver tumor necrosis factor-a (TNF-±) in both treatment groups. Unexpectedly, in MDMA treated rats, Bax, Bcl-xl, Bcl-2, Fas, Fas ligand (Fas-L), caspase 8, cytochrome c, caspase 3 gene expression, and DNA fragmentation were nearly unchanged. In addition, apoptosis in MDMA+ ghrelin group was significantly reduced when compared with MDMA treated animals. In all, MDMA could transiently increase serum transaminases and induce tissue necrosis and liver toxicity. Ghrelin, however, could not stop liver enzyme rise and MDMA hepatotoxicity. MDMA hepatotoxicity seems to be mediated via tissue necrosis than apoptotic and inflammatory pathways. Conceivably, ghrelin as an anti-inflammatory and anti-apoptotic agent may not protect hepatocytes against MDMA liver toxicity.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"343-354"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462488/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38376529","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"<i>In-vitro</i> Study of <i>Hottentotta Schach</i> Crude Venom Anticancer Effects on MCF-7 and Vero Cell Lines.","authors":"Saeed Dezianian,&nbsp;Jamil Zargan,&nbsp;Hamid Reza Goudarzi,&nbsp;Ashkan Haji Noormohamadi,&nbsp;Mohsen Mousavi,&nbsp;Hani Keshavarz Alikhani,&nbsp;Behrooz Johari","doi":"10.22037/ijpr.2020.1100957","DOIUrl":"https://doi.org/10.22037/ijpr.2020.1100957","url":null,"abstract":"<p><p>Scorpion venoms contain potentially useful pharmacological agents. Several studies demonstrate that the venoms of some scorpions induce apoptosis and inhibit the growth of cancer cells; therefore, they have been investigated for isolating anticancer components. In this study, antitumor effects of <i>Hottentotta schach</i> crude venom on MCF-7 (breast cancer cell line) as test group and Vero (African green monkey kidney normal cell line) as control group were analyzed. Cell toxicity was analyzed using MTT and neutral red (NR) uptake assays and apoptosis induction was analyzed using comet assay and caspase-3 activity. Oxidative stress following <i>Hottentotta schach</i> crude venom treatment was analyzed using nitrite oxide (NO) determination assay, reduced glutathione (GSH) and catalase enzyme activity assays. Results showed that crude venom (25-200 μg/mL) induced apoptosis and inhibited the growth of MCF-7 and to a lesser extent in Vero cell lines. Nitrite oxide concentration increased while glutathione concentration and catalase enzyme activity were decreased in MCF-7 cells; however, results in Vero cells were reversed completely. It can be concluded that <i>Hottentotta schach</i> crude venom disturbs the oxidation and reduction potential in cancer cells and ultimately induce apoptosis. So this venom can be used as a good source for isolation and designing new anticancer drugs.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"192-202"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462501/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38472985","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Antidiabetic Properties of Hydroalcoholic Leaf and Stem Extract of <i>Levisticum officinale</i>: An implication for α-amylase Inhibitory Activity of Extract Ingredients through Molecular Docking.","authors":"Nahid Ghaedi,&nbsp;Iran Pouraboli,&nbsp;Nayere Askari","doi":"10.22037/ijpr.2020.15140.12901","DOIUrl":"https://doi.org/10.22037/ijpr.2020.15140.12901","url":null,"abstract":"<p><p><i>Levisticum officinale</i> (Apiaceae) is a favorite food spice. Iranian folk medicine claims that it has a prominent antidyslipidemic property but this is not documented scientifically so far. This study evaluated antidyslipidemic and the other antidiabetic aspects of the stem and leaf hydroalcoholic extract of it (LOE). Regarding oral glucose tolerance test results, LOE (500 mg/kg) administration 30 min before glucose loading significantly decreased the blood glucose level (13%) at 90 min in male rats. Additionally, LOE treatment (500 mg/kg, orally, once a day) for 14 days significantly reduced the serum glucose level (24.97%) and markedly improved the lipid profile and the insulin, creatinine, alanine aminotransferase and aspartate aminotransferase serum levels in diabetic rats. Moreover, LOE effectively amended the impaired antioxidant status and ameliorated lipid peroxidation in the plasma and pancreas and liver tissues of diabetics. Also, 14 days LOE treatment, significantly decreased the renal sodium-glucose cotransporter 2 and facilitated glucose transporter 2 (GLUT₂) mRNA levels and GLUT₂ gene expression in the enterocytes of jejunum tissue in comparison with diabetic untreated rats. HPLC method revealed the presence of chlorogenic acid, rosmarinic acid, caffeic acid, quercetin and luteolin and GC-MS analysis detected bioactive compounds like phthalides, thymol, phytol, hexanoic acid, carene and menthofuran. LOE showed α-amylase (αΑ) inhibitory activity and in silico studies predicted that among extract ingredients luteolin, quercetin, rosmarinic, caffeic, and hexanoic acids have the greatest αΑ inhibition potecy. Thus, current results justify antidyslipidemic value of <i>L. officinale</i> and shed light on more antidiabetic health benefits of it.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"231-250"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462500/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38473426","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Bi-heterocycles as Potent Inhibitors of Urease and Less Cytotoxic Agents: 3-({5-((2-Amino-1,3-thiazol-4-yl)methyl)-1,3,4-oxadiazol-2-yl}sulfanyl)-<i>N</i>-(un/substituted-phenyl)propanamides.","authors":"Muhammad Athar Abbasi,&nbsp;Muhammad Shahid Ramzan,&nbsp;Aziz Ur-Rehman,&nbsp;Sabahat Zahra Siddiqui,&nbsp;Mubashir Hassan,&nbsp;Syed Adnan Ali Shah,&nbsp;Muhammad Ashraf,&nbsp;Muhammad Shahid,&nbsp;Sung-Yum Seo","doi":"10.22037/ijpr.2019.13084.11362","DOIUrl":"https://doi.org/10.22037/ijpr.2019.13084.11362","url":null,"abstract":"<p><p>The synthesis of a novel series of bi-heterocyclic propanamides, <b>7a-l</b>, was accomplished by <i>S</i>-substitution of 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol (<b>3</b>). The synthesis was initiated from ethyl 2-(2-amino-1,3-thiazol-4-yl)acetate (<b>1</b>) which was converted to corresponding hydrazide, <b>2</b>, by hydrazine hydrate in methanol. The refluxing of hydrazide, <b>2</b>, with carbon disulfide in basic medium, resulted in 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazol-2-thiol (<b>3</b>). A series of electrophiles, <b>6a-l</b>, was synthesized by stirring un/substituted anilines (<b>4a-l</b>) with 3-bromopropanoyl chloride (<b>5</b>) in a basic aqueous medium. Finally, the targeted compounds, <b>7a-l</b>, were acquired by stirring <b>3</b> with newly synthesized electrophiles, <b>6a-l</b>, in DMF using LiH as a base and an activator. The structures of these bi-heterocyclic propanamides were confirmed through spectroscopic techniques, such as IR, ¹H-NMR, ¹³C-NMR, and EI-MS. These molecules were tested for their urease inhibitory potential, whereby, the whole series exhibited very promising activity against this enzyme. Their cytotoxic behavior was ascertained through hemolysis and it was observed that all these were less cytotoxic agents. The <i>in-silico</i> molecular docking analysis of these molecules was also in full agreement with their <i>in-vitro</i> enzyme inhibition data.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"487-506"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462494/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38373587","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Chemical Composition, Antioxidant, Genotoxique and Antigenotoxic Potentials of <i>Phlomis Bovei</i> De Noé Aerial Parts.","authors":"Nabila Zaabat,&nbsp;Anne-Emmanuelle Hay,&nbsp;Serge Michalet,&nbsp;Inès Skandrani,&nbsp;Leila Chekir-Ghedira,&nbsp;Marie-Geneviève Dijoux-Franca,&nbsp;Salah Akkal","doi":"10.22037/ijpr.2019.15197.12938","DOIUrl":"https://doi.org/10.22037/ijpr.2019.15197.12938","url":null,"abstract":"<p><p>In the present work, chemical investigation of the aerial parts of <i>Phlomis</i> <i>bovei</i> de Noé an endemic species from Algeria, led to the isolation and identification of seven known compounds including five flavones glycosides: Chrysoeriol 7-<i>O</i>-(3''-(<i>E</i> et <i>Z</i>)-<i>p</i>-coumaroyl)-β-glucoside <b>(1)</b>, terniflorin (apigenin-7-<i>O</i>-(6''-<i>E-p</i>-coumaroyl)glucoside) <b>(3)</b>, apigenin-7-<i>O</i>-(6''-(5'''-methoxy-coumaryl) glucoside <b>(4)</b>, apigenin 7-<i>O</i>-(3″-<i>p</i>-coumaryl)<i>glucoside</i> <b>(5)</b>, hispidulin-7-<i>O</i>-glucuronide <b>(6)</b> and two cinnamic acid derivatives: <i>p</i>-coumaric acid methyl ester (<i>E</i> et <i>Z</i>) <b>(2)</b>, chlorogenic acid <b>(7)</b>. Compound <b>4</b> is described for the first time in the species <i>bovei</i> de Noé, the genus <i>Phlomis</i> and the <i>Lamiaceae</i> family. Structures elucidation was performed by comprehensive 1D and 2D NMR analyses, mass spectrometry and by comparison with literature data. Some pure compounds and extracts have been evaluated for their antioxidant activities through different methods: DPPH and ABTS assays as well as CUPRAC assay. Genotoxic and antigenotoxic activities of pure compounds were also evaluated <i>in-vitro</i> on <i>Escherichia coli</i> PQ37 cells by the SOS Chromotest.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"282-291"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462515/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38376524","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"STAT3-mediated Apoptotic-enhancing Function of Sclareol Against Breast Cancer Cells and Cell Sensitization to Cyclophosphamide.","authors":"Havva Afshari,&nbsp;Mitra Nourbakhsh,&nbsp;Niloufar Salehi,&nbsp;Mohammad Mahboubi-Rabbani,&nbsp;Afshin Zarghi,&nbsp;Shokoofe Noori","doi":"10.22037/ijpr.2020.112587.13843","DOIUrl":"https://doi.org/10.22037/ijpr.2020.112587.13843","url":null,"abstract":"<p><p>Sclareol is an organic compound with potential anti-tumor effects against various cancer types. However, its precise molecular mechanism in the suppression of tumor growth has not been fully elucidated. In the present study, the anti-proliferative and apoptosis-inducing effects of sclareol with cyclophosphamide were investigated in breast cancer cells and the involvement of the JAK/STAT pathway was evaluated. For this purpose, MCF-7 breast cancer cells were cultured and treated with various concentrations of sclareol to determine its IC₅₀. Cell viability was measured by MTT assay and apoptosis was assessed by flow cytometric analysis of annexin V binding. Gene and protein expression were examined by real-time PCR and Western blotting, respectively. The activity of caspase enzymes was also measured. The results showed that sclareol significantly reduced cell viability and triggered cell death and its co-administration with cyclophosphamide enhanced its anti-cancer properties. Additionally, sclareol up-regulated the expression of p53 and BAX and reduced the expression of Bcl-2. Docking studies indicated an interaction between sclareol and STAT3 which was proved by attenuation of STAT3 phosphorylation after treatment of the cells with sclareol. Sclareol was also capable of suppressing the function of IL-6 in modulating the expression of apoptosis-associated genes. Altogether these data suggest the potential of sclareol as an anti-cancer agent and demonstrate that a combination of sclareol with cyclophosphamide might serve as an effective chemotherapeutic approach resulting in improvements in the treatment of breast cancer.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"398-412"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462487/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38373581","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of Neuroprtective Effects of L-Carnitine and Fat Emulsion in the CVA Patients: A Prospective, Randomized, Double Blind, Clinical Trial.","authors":"Kaveh Kazemian,&nbsp;Shahram Ala,&nbsp;Mojtaba Mojtahedzadeh,&nbsp;Mahmoud Abedini,&nbsp;Abbas Alipour,&nbsp;Saeid Abediankenari,&nbsp;Mohammadreza Rafati,&nbsp;Ali Abaskhanidavanloo,&nbsp;Fatemeh Mohajerani","doi":"10.22037/ijpr.2020.1100952","DOIUrl":"https://doi.org/10.22037/ijpr.2020.1100952","url":null,"abstract":"<p><p>Cerebral infarction presents with neurological deficits caused by the death of neurons in a focal area of the brain. S100B is a biomarker that increases in brain damage. Neuroprotectives can reduce the brain sequels after neurological insult. The purpose of this study was to evaluate the neuroprotective effects of L-carnitine and Fat emulsion (Lipofundin^®) alone and in combination in patients with ischemic stroke. In a prospective, RCT, and double-blind study 100 patients with MCA ischemic cerebrovascular accident who were admitted in the first 24 h of injury entered the study. The patients were randomly assigned into four groups of L-carnitine, fat emulsion, L-carnitine plus fat emulsion and control. Fat emulsion 10%, 500 mL, was infused over 6 to 12 h and 1 gr of L-carnitine (10 mL of solution) was administered orally to patients in addition to common therapies, according to the American Heart Association and American Stroke Association (AHA/ASA) guidelines. The patients in the control group received only the usual treatment according to stroke guidelines. Blood samples before the intervention, then after 24 h, 48 h, and 7 days later were taken and immunoenzymatic colorimetric method was used for quantitative determination of S100B concentration in the patients' serum. In the within group analysis, all of our treatment interventions (except control group) have decreased S100B levels statistically significant (<i>P</i> < 0.05). Moreover, changes in observed levels of S100B before and after intervention were different between the groups and the observed differences were statistically significant (<i>P</i> = 0.01). In the GEE model, it was found that S100B levels in the L-carnitine plus fat emulsion group decreased more than the control group and this decline has been statistically significant [<i>P</i> = 0.02, 20.47 (CI 95%: 6.25-34.41)], but in comparison of L-carnitine and fat emulsion group with control group, did not reached statistical significance (<i>P</i> > 0.05). Based on the results obtained from this study, it seems that L-carnitine with fat emulsion could lead to neuroprotective effects with a significant reduction in the S100B biomarker.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"111-119"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462480/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38375675","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}