Iranian Journal of Pharmaceutical Research : IJPR最新文献

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A Comprehensive Review of the Role of Complementary and Dietary Medicines in Eradicating Helicobacter pylori. 补充和膳食药物在根除幽门螺杆菌中的作用的综合综述。
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-06-18 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-127030
Saeed Abdi, Sara Ataei, Maede Abroon, Pantea Majma Sanaye, Mohammad Abbasinazari, Amir Farrokhian
{"title":"A Comprehensive Review of the Role of Complementary and Dietary Medicines in Eradicating <i>Helicobacter pylori</i>.","authors":"Saeed Abdi,&nbsp;Sara Ataei,&nbsp;Maede Abroon,&nbsp;Pantea Majma Sanaye,&nbsp;Mohammad Abbasinazari,&nbsp;Amir Farrokhian","doi":"10.5812/ijpr-127030","DOIUrl":"https://doi.org/10.5812/ijpr-127030","url":null,"abstract":"<p><p>Antibiotic-resistant <i>Helicobacter pylori</i> isolates have become a global concern. The standard triple or quadruple therapies have recently become the most effective protocol for eradicating <i>H. pylori</i> in the gastrointestinal tract. There is evidence regarding the impact of different complementary or dietary supplements on <i>H. pylori</i> eradication. This review article intended to search electronic bibliographic databases for any clinical studies that evaluated the use of any herbal or dietary supplements to eradicate <i>H. pylori</i> up to June 2021. A total of 20 human studies met our criteria and were reviewed. Although some herbal medicines have shown their efficacy and safety in eradicating <i>H. pylori</i> in different clinical trials, more randomized blind, placebo-controlled human trials with a large sample size must be performed to extend our knowledge.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e127030"},"PeriodicalIF":1.6,"publicationDate":"2022-06-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/51/c4/ijpr-21-1-127030.PMC9420233.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40348992","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}
引用次数: 0
Evaluation of Crocin Effect on Contrast-Induced Nephropathy Following Coronary Angiography or Angioplasty: A Randomized Controlled Trial. 评价藏红花素对冠脉造影或血管成形术后造影剂肾病的疗效:一项随机对照试验。
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-06-14 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-126920
Lida Shojaei, Shima Esfandiary, Mohammad Rouzbahani, Fatemeh Heydarpour, Mostafa Bahremand, Reza Heidary Moghadam, Ghazal Mahmoudi, Farzaneh Korani, Farshid Raissi, Foroud Shahbazi
{"title":"Evaluation of Crocin Effect on Contrast-Induced Nephropathy Following Coronary Angiography or Angioplasty: A Randomized Controlled Trial.","authors":"Lida Shojaei,&nbsp;Shima Esfandiary,&nbsp;Mohammad Rouzbahani,&nbsp;Fatemeh Heydarpour,&nbsp;Mostafa Bahremand,&nbsp;Reza Heidary Moghadam,&nbsp;Ghazal Mahmoudi,&nbsp;Farzaneh Korani,&nbsp;Farshid Raissi,&nbsp;Foroud Shahbazi","doi":"10.5812/ijpr-126920","DOIUrl":"https://doi.org/10.5812/ijpr-126920","url":null,"abstract":"<p><p>Contrast-induced nephropathy (CIN) is the third cause of hospital-acquired acute kidney injury. The CIN prophylactic strategies adopted to date, although not highly efficient, are mostly based on antioxidant activity and hydration therapy. This study was designed and conducted to evaluate crocin's efficacy in the prevention of CIN in chronic kidney disease (CKD) patients undergoing coronary angiography/angioplasty. In this randomized clinical trial, a total of 110 eligible CKD stage 3 patients requiring contrast agent administration for coronary angiography/angioplasty were enrolled and randomly assigned to either crocin (n = 57) or control (n = 53) group. The patients in both groups received standard hydration therapy; nevertheless, in the crocin group, the patients were also orally administered three consecutive oral doses of 30 mg crocin tablets 1 day before up to 1 day after contrast media (CM) exposure. The primary endpoint was CIN incidence defined as an increase in serum creatinine (SrCr) level by ≥ 0.3 mg/dL or any change in urinary neutrophil gelatinase-associated lipocalin (NGAL) from the baseline within 48 hours of CM exposure. During 4 months, 130 patients were recruited. The mean age of the patients was 65.62 ± 9.05 years, and the majority of them were male (64.54%). The SrCr in the crocin group did not significantly increase within 48 hours of angiography/angioplasty. The changes in the urinary NGAL level were not significant in both groups. The CIN incidence was significantly lower in the crocin group than in the control group (1.75% and 13.2%; P = 0.028). Crocin administration plays an important nephron-protective role in the prevention of CIN.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e126920"},"PeriodicalIF":1.6,"publicationDate":"2022-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/76/d6/ijpr-21-1-126920.PMC9420216.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40347215","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}
引用次数: 0
Monitoring of Infant Formula and Baby Food for the Pat and NOS Terminator of Genetically Modified Maize and Soybean by Real-time PCR in Iran. 实时荧光定量PCR检测伊朗婴幼儿配方奶粉和婴儿食品中转基因玉米和大豆的Pat和NOS终结者
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-06-14 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-126921
Ramin Beheshti Zadeh, Shila Safaeian, Elham Moslemi, Rezvan Mosavi Nadushen, Kasra Esfahani
{"title":"Monitoring of Infant Formula and Baby Food for the Pat and NOS Terminator of Genetically Modified Maize and Soybean by Real-time PCR in Iran.","authors":"Ramin Beheshti Zadeh,&nbsp;Shila Safaeian,&nbsp;Elham Moslemi,&nbsp;Rezvan Mosavi Nadushen,&nbsp;Kasra Esfahani","doi":"10.5812/ijpr-126921","DOIUrl":"https://doi.org/10.5812/ijpr-126921","url":null,"abstract":"<p><strong>Background: </strong>Soybean and maize are the most cultivated genetically modified (GM) plants. Because of the increase in the imports of GM products to Iran, infant formula and baby food, which is consumed by babies during their first month of life, can also contain soybean and maize. It has become fundamental to screen these types of products.</p><p><strong>Objectives: </strong>The present study aimed to investigate the GM corn and soybean in baby food and infant formula using real-time polymerase chain reaction (PCR).</p><p><strong>Methods: </strong>A total of 60 baby food and infant formulas were collected randomly from the local drugstores in Tehran. Genomic DNA was extracted from all samples, then by real-time PCR detection, tested Pat/NOS. Internal control genes zein and lectin were used for maize and soybean, respectively.</p><p><strong>Results: </strong>Results showed that 5% of infant formulas and 5% of baby food, two Iranian and one imported baby food, and two imported and one Iranian infant formula were positive for pat. However, NOS was detected in none of the samples. The results showed positive results for the presence of the pat gene in the products without an appropriate label.</p><p><strong>Conclusions: </strong>This article provides evidence of GM maize and soybean presence in baby food and infant formula in Iran.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e126921"},"PeriodicalIF":1.6,"publicationDate":"2022-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/72/e7/ijpr-21-1-126921.PMC9420218.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40350131","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}
引用次数: 1
A Neglected Challenge in the Analysis of Active Pharmaceutical Substances with Aldehyde Functional Group in Aqueous Matrices. 水溶液中含有醛官能团的原料药分析中一个被忽视的挑战。
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-24 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-127036
Azadeh Nasiri, Shaya Mokhtari, Bahram Daraei, Hassan Yazdanpanah, Mehrdad Faizi, Farzad Kobarfard
{"title":"A Neglected Challenge in the Analysis of Active Pharmaceutical Substances with Aldehyde Functional Group in Aqueous Matrices.","authors":"Azadeh Nasiri,&nbsp;Shaya Mokhtari,&nbsp;Bahram Daraei,&nbsp;Hassan Yazdanpanah,&nbsp;Mehrdad Faizi,&nbsp;Farzad Kobarfard","doi":"10.5812/ijpr-127036","DOIUrl":"https://doi.org/10.5812/ijpr-127036","url":null,"abstract":"<p><p>Aldehydes are compounds that are widely used and popular in organic synthesis due to their high reactivity. This advantage is a disadvantage in medicinal chemistry. Due to the ability of aldehydes to participate in nucleophilic reactions (especially in aqueous biological media) and access to nucleophiles such as amino acids and nucleic acids, drugs with aldehyde functional groups are always used with caution and carefully quantified in biological fluids. Our experience in working on biologically active aldehydes indicates the transformation of these groups of compounds in aqueous or alcoholic solution and thus the failure of analytical methods for their accurate monitoring in such media. Both mass spectrometry and Proton nuclear magnetic resonance spectroscopic findings indicate the reaction of spiramycin with water molecules in an aqueous solution, resulting in the conversion of spiramycin to a new molecule with 18 mass unit difference and thus, the residue amount which is measured and reported based on a mass spectrometries method does not show the correct amount of spiramycin in these samples.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e127036"},"PeriodicalIF":1.6,"publicationDate":"2022-05-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/8a/85/ijpr-21-1-127036.PMC9420214.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40348996","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}
引用次数: 1
Expression Modulation of Immune Checkpoint Molecules by Ibrutinib and Everolimus Through STAT3 in MCF-7 Breast Cancer Cells. 依鲁替尼和依维莫司通过STAT3调控MCF-7乳腺癌细胞中免疫检查点分子的表达
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-21 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-127352
Mohsen Soltanshahi, Saeid Taghiloo, Hossein Asgarian-Omran
{"title":"Expression Modulation of Immune Checkpoint Molecules by Ibrutinib and Everolimus Through STAT3 in MCF-7 Breast Cancer Cells.","authors":"Mohsen Soltanshahi,&nbsp;Saeid Taghiloo,&nbsp;Hossein Asgarian-Omran","doi":"10.5812/ijpr-127352","DOIUrl":"https://doi.org/10.5812/ijpr-127352","url":null,"abstract":"<p><p>Tumor-targeted therapy with small-molecule inhibitors (SMIs) has been demonstrated to be a highly effective therapeutic strategy for various cancers. However, their possible associations with immune evasion mechanisms remain unknown. This study examined the association of inhibitors of the protein kinase B (AKT), mammalian target of rapamycin (mTOR), and Bruton's tyrosine kinase (BTK) signaling pathways with the expression of immune checkpoint ligands programmed death-ligand 1 (PD-L1), CD155, and galectin-9 (Gal-9) in a breast cancer cell line. MCF-7 cells were treated with everolimus, MK-2206, and ibrutinib. An MTT assay was used to determine the optimal dose for all drugs. A real-time polymerase chain reaction was utilized to measure the mRNA expression of PD-L1, CD155, and Gal-9. The western blot technique was also employed to evaluate the protein expression of the phosphorylated signal transducer and activator of transcription 3 (STAT3). The optimal doses of everolimus, MK-2206, and ibrutinib were observed to be 200, 320, and 2000 nM, respectively. The PD-L1 and CD155 mRNA expression was significantly decreased following the treatment with everolimus and ibrutinib, but not with MK-2206. There were no differences in Gal-9 expression between the single-treated and control groups; however, combined treatment with everolimus and ibrutinib increased its mRNA expression. Everolimus and ibrutinib both inhibited constitutive STAT3 phosphorylation in MCF-7, which was more pronounced in combination treatment. The findings regarding the modulation of PD-L1, CD155, and Gal-9 molecules by SMIs emphasize the crosstalk between the expression of these immune checkpoint molecules and AKT/mTOR/BTK signaling pathways through STAT3 as a critical transcription factor.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e127352"},"PeriodicalIF":1.6,"publicationDate":"2022-05-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/fe/8a/ijpr-21-1-127352.PMC9293249.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40534589","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}
引用次数: 1
Surface-Active Ionic Liquid-Assisted Cloud Point Extraction for Pre-Concentration and Determination of Cobalt Ions in Pharmaceutical Preparations. 表面活性离子液体辅助云点萃取法预富集和测定药物制剂中钴离子。
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-17 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-127043
Farzad Bamdad, Zahra Habibi
{"title":"Surface-Active Ionic Liquid-Assisted Cloud Point Extraction for Pre-Concentration and Determination of Cobalt Ions in Pharmaceutical Preparations.","authors":"Farzad Bamdad,&nbsp;Zahra Habibi","doi":"10.5812/ijpr-127043","DOIUrl":"https://doi.org/10.5812/ijpr-127043","url":null,"abstract":"<p><p>Herein we describe an efficient, simple, and precise micelle-mediated microextraction strategy based on the aggregation behavior of surface-active ionic liquids (SAILs) for the preconcentration and determination of cobalt ions in pharmaceutical preparations. Unlike the commonly used hydrophobic ionic liquids in IL-based microextraction methods, a water-soluble surface-active ionic liquid [1-hexadecyl 3-methylimidazolium chloride (C<sub>16</sub>MeImCl)] was used. A modified cloud point extraction (CPE) procedure based on the C<sub>16</sub>MeImCl-Triton X-114 mixed micellar system was proposed as an efficient extracting phase. A comparison of the analytical features of the extraction process with and without SAILs revealed the benefits of the proposed method. Advantages such as a wider linear range, lower detection limit, higher reproducibility, and improved extraction efficiency highlighted the proposed method over the conventional CPE method. These attractive specifications are due to the higher extraction efficiencies achieved in the presence of the SAIL and its favorable effects at the phase separation stage. Various parameters affecting the extraction efficiency were optimized by univariate and multivariate (Box-Behnken design) approaches. The calibration curve was obtained in the optimal experimental conditions with a linear range from 0.01 to 5.5 mg L<sup>-1</sup> of cobalt ion concentration (R = 0.9992) and a detection limit of about 0.005 mg L<sup>-1</sup>. The RSD% for 10 replicate determinations of 1.0 mg L<sup>-1</sup> Co was 0.9%. The proposed method was successfully applied to determine cobalt ions in vitamin B<sub>12</sub> ampoules and tablets.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e127043"},"PeriodicalIF":1.6,"publicationDate":"2022-05-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/18/c6/ijpr-21-1-127043.PMC9347226.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40677225","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}
引用次数: 3
Assessment of Different Radioiodine Doses for Post-ablation Therapy of Thyroid Remnants: A Systematic Review. 不同放射性碘剂量对甲状腺残余消融后治疗的评价:一项系统综述。
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-14 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-123825
Mojtaba Ansari, Mostafa Rezaei Tavirani
{"title":"Assessment of Different Radioiodine Doses for Post-ablation Therapy of Thyroid Remnants: A Systematic Review.","authors":"Mojtaba Ansari,&nbsp;Mostafa Rezaei Tavirani","doi":"10.5812/ijpr-123825","DOIUrl":"https://doi.org/10.5812/ijpr-123825","url":null,"abstract":"<p><p>The determination of radioiodine remnant ablation (RRA) dosage in post-operation thyroid residual tissues resection has been largely subject of discussion, yet no concise conclusion is released through systematic review studies. In this study, we conducted a systematic review of comparative experiments to evaluate and compare the efficacy of different prescribed dosages of radioiodine in post-op thyroid residual tissues resection among low, intermediate, and high-risk patients to approve the common method. Using automated searches, studies were collected from PubMed, Google Scholar, Elsevier, Scopus, and UpToDate, all until April 2021. Alongside the aforementioned sources, comparative experiments were added in for further investigation. Overall, 4000 patients with papillary thyroid cancer, differentiated thyroid carcinoma (DTC), metastasized and non-metastasized thyroid cancer took part in twenty-one trials are assessed. We discovered no significant difference in successful thyroid residual tissues excision between low-activity and high-activity radioiodine treatment in people with low and intermediate risk. In these individuals, there was no significant difference between the high therapeutic dose of 3700 MBq and the lesser dose of 1850 MBq for RRA. However, high-dose treatment usually yielded superior results. Low activity RRA causes fewer adverse effects in metastasis-free patients than high-activity 3.7 GBq. There was no significant therapeutic difference regarding treatment efficacy in patients with low and moderate risks. However, in patients with high-risk status, applying a high-dose regimen of RRA produced a significantly better response.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e123825"},"PeriodicalIF":1.6,"publicationDate":"2022-05-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/67/a6/ijpr-21-1-123825.PMC9420215.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40350129","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}
引用次数: 0
Enhancement of Sensitivity to Tamoxifen by Berberine in Breast Cancer Cells by Inhibiting ER-α36 Expression. 小檗碱通过抑制ER-α36表达增强乳腺癌细胞对他莫昔芬的敏感性
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-13 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-126919
Xiaohua Pan, Zhen Song, Yue Cui, Ming Qi, Guojun Wu, Molin Wang
{"title":"Enhancement of Sensitivity to Tamoxifen by Berberine in Breast Cancer Cells by Inhibiting ER-α36 Expression.","authors":"Xiaohua Pan,&nbsp;Zhen Song,&nbsp;Yue Cui,&nbsp;Ming Qi,&nbsp;Guojun Wu,&nbsp;Molin Wang","doi":"10.5812/ijpr-126919","DOIUrl":"https://doi.org/10.5812/ijpr-126919","url":null,"abstract":"<p><p>Berberine, an isoquinoline alkaloid purified from Chinese herbs, was verified to have antitumor effects. It has also been reported that berberine can enhance the anticancer effect of tamoxifen (TAM) in estrogen receptor (ER)-positive breast cancer cells; however, the involved underlying mechanism is still unclear. In the present study, the role of one variant of ER-α, ER-α36, in the TAM sensitizing effect of berberine was explored in TAM-resistant breast cancer cells. This study demonstrated that berberine potently sensitized TAM-resistant breast cancer cells, including TAM-resistant MCF7 and BT-474 cells, to TAM treatment. Additionally, this study showed that berberine could simultaneously suppress ER-α36 expression in TAM-resistant cells. However, when ER-α36 was knocked down in TAM-resistant cells, there was no significant TAM-sensitizing effect by berberine. Therefore, this study indicated that ER-α36 is involved in berberine's TAM-sensitizing effect on ER-positive breast cancer cells, which provided supporting data for the application of berberine in cancer therapy as an adjuvant agent for TAM treatment.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e126919"},"PeriodicalIF":1.6,"publicationDate":"2022-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/5c/c1/ijpr-21-1-126919.PMC9420211.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40347214","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}
引用次数: 1
Targeted Synthesis and Study of Anti-tyrosinase Activity of 2-Substituted Tetrahydrobenzo[4,5]Thieno[2,3-d]Pyrimidine-4(3H)-One. 2-取代四氢苯并[4,5]噻吩[2,3-d]嘧啶-4(3H)- 1的靶向合成及抗酪氨酸酶活性研究
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-13 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-126557
Alexey Chiriapkin, Ivan Kodonidi, Dmitry Pozdnyakov
{"title":"Targeted Synthesis and Study of Anti-tyrosinase Activity of 2-Substituted Tetrahydrobenzo[4,5]Thieno[2,3-d]Pyrimidine-4(3H)-One.","authors":"Alexey Chiriapkin,&nbsp;Ivan Kodonidi,&nbsp;Dmitry Pozdnyakov","doi":"10.5812/ijpr-126557","DOIUrl":"https://doi.org/10.5812/ijpr-126557","url":null,"abstract":"<p><strong>Background: </strong>The high prevalence of skin hyperpigmentation makes it necessary to search for remedies that could hinder this process. Among such substances, tyrosinase inhibitors can be distinguished, which may be pyrimidine derivatives.</p><p><strong>Objectives: </strong>This study aimed to investigate new compounds with anti-tyrosinase activity in 2-substituted tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one by an in vitro analysis and investigating their molecular docking.</p><p><strong>Methods: </strong>A molecular docking was performed using AutoDock 4.0 with the 3-dimensional structure of tyrosinase of the fungus Agaricus bisporus from the Protein Data Bank (PDB; rcsb.org) with identification number 2Y9X. A synthesis of 2-substituted tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one was carried out during the heterocyclization reaction of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in glacial acetic acid with the addition of dimethyl sulfoxide. Tyrosinase activity was determined in vitro by the spectrophotometric method.</p><p><strong>Results: </strong>Molecular docking data suggest the feasibility of synthesizing 2-substituted tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one as possible tyrosinase inhibitors. Of particular interest are compounds with hydroxy groups in the radical. Next, pharmacological screening showed that the leading compound is 4g. It is likely that metal-ligand interactions are the main interactions in the active site of tyrosinase because kojic acid, hydroquinone, and lactic acid (reference compounds), as well as compounds with only hydroxy groups in phenyl substituents (4b, 4c, and 4g), have the greatest anti-tyrosinase activity.</p><p><strong>Conclusions: </strong>As a result of molecular docking studies, the feasibility of synthesizing 2-substituted tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one as potential tyrosinase inhibitors was justified. 2-Substituted tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one was obtained using new synthesis conditions. The leading compound is 4g containing a fragment of 2,4-dihydroxybenzene.</p>","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e126557"},"PeriodicalIF":1.6,"publicationDate":"2022-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/66/fa/ijpr-21-1-126557.PMC9420225.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40350132","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}
引用次数: 3
Montmorillonite-Famotidine/Chitosan Bio-nanocomposite Hydrogels as a Mucoadhesive/Gastroretentive Drug Delivery System. 蒙脱石-法莫替丁/壳聚糖生物纳米复合水凝胶作为黏附/胃保留给药系统。
IF 1.6
Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-05-12 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr-127035
Hassan Farhadnejad, Seyed Alireza Mortazavi, Sanaz Jamshidfar, Amir Rakhshani, Hamidreza Motasadizadeh, Yousef Fatahi, Athar Mahdieh, Behzad Darbasizadeh
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引用次数: 5
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