Iranian Journal of Pharmaceutical Research : IJPR最新文献_第4页

Piperine Increases Pentagamavunon-1 Anti-cancer Activity on 4T1 Breast Cancer Through Mitotic Catastrophe Mechanism and Senescence with Sharing Targeting on Mitotic Regulatory Proteins. 胡椒碱通过有丝分裂突变机制和共享靶向有丝分裂调节蛋白的衰老，增加Pentagamavunon-1对4T1乳腺癌的抗癌活性。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-02-04 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr.123820

Endah Endah, Febri Wulandari, Yurananda Putri, Riris Istighfari Jenie, Edy Meiyanto

{"title":"Piperine Increases Pentagamavunon-1 Anti-cancer Activity on 4T1 Breast Cancer Through Mitotic Catastrophe Mechanism and Senescence with Sharing Targeting on Mitotic Regulatory Proteins.","authors":"Endah Endah, Febri Wulandari, Yurananda Putri, Riris Istighfari Jenie, Edy Meiyanto","doi":"10.5812/ijpr.123820","DOIUrl":"https://doi.org/10.5812/ijpr.123820","url":null,"abstract":"Pentagamavunon-1 performs more potent anti-cancer effects than curcumin against various cancer cells, but it remains to be optimized. Piperine shows the activity as an enhancer of a therapeutic agent. This study expects to achieve higher effectiveness of PGV-1 on 4T1 breast cancer cells through co-treatment with piperine with exploring the effect of cytotoxicity, mitotic catastrophe, cellular senescence, and target proteins of PGV-1 and piperine on the regulation of mitosis in TNBC cells (4T1). The assays emphasize MTT assay, May Grünwald-Giemsa staining, SA-β-galactosidase assay, and bioinformatics analysis, respectively, to elicit the respected activities. The results revealed that PGV-1 performed a cytotoxic effect with an IC50 value of 9 µM while piperine showed a lower cytotoxic effect with an IC50 value of 800 µM on 4T1 cells 24 h treatment. However, the combination treatment of both showed a synergistic cytotoxic enhancement effect with an average CI value < 1. Furthermore, the combination of PGV-1 and piperine induced mitotic catastrophe and senescence better than the single treatment. Treatment of 1 µM of PGV-1 and 400 µM of piperine increased the percentage of senescent cells by 33%. Bioinformatics analysis revealed that PGV-1 and piperine target proteins play a role in mitotic regulation, namely CDK1, KIF11, AURKA, AURKB, and PLK1, to contribute to mitotic catastrophe. Therefore, piperine increases the effectiveness of PGV-1 to suppress 4T1 cells growth synergistically that may occur through mitotic catastrophe and senescence targeting on mitotic regulatory proteins.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e123820"},"PeriodicalIF":1.6,"publicationDate":"2022-02-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/d2/ff/ijpr-21-1-123820.PMC9191230.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40404786","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: 6

Review on Approved and Inprogress COVID-19 Vaccines. 已批准和正在研发的COVID-19疫苗综述。

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-01-24 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr.124228

Amir Farnudian-Habibi, Mobina Mirjani, Vahideh Montazer, Shima Aliebrahimi, Iman Katouzian, Saeed Abdolhosseini, Ali Rahmani, Hossein Keyvani, Seyed Nasser Ostad, Mazda Rad-Malekshahi

{"title":"Review on Approved and Inprogress COVID-19 Vaccines.","authors":"Amir Farnudian-Habibi, Mobina Mirjani, Vahideh Montazer, Shima Aliebrahimi, Iman Katouzian, Saeed Abdolhosseini, Ali Rahmani, Hossein Keyvani, Seyed Nasser Ostad, Mazda Rad-Malekshahi","doi":"10.5812/ijpr.124228","DOIUrl":"10.5812/ijpr.124228","url":null,"abstract":"The last generation of Coronavirus named COVID-19 is responsible for the recent worldwide outbreak. Concerning the widespread and quick predominance, there is a critical requirement for designing appropriate vaccines to surmount this grave problem. Correspondingly, in this revision, COVID-19 vaccines (which are being developed until March 29th, 2021) are classified into specific and non-specific categories. Specific vaccines comprise genetic-based vaccines (mRNA, DNA), vector-based, protein/recombinant protein vaccines, inactivated viruses, live-attenuated vaccines, and novel strategies including microneedle arrays (MNAs), and nanoparticles vaccines. Moreover, specific vaccines such as BCG, MRR, and a few other vaccines are considered Non-specific. What is more, according to the significance of Bioinformatic sciences in the cutting-edge vaccine design and rapid outbreak of COVID-19, herein, Bioinformatic principles including reverse vaccinology, epitopes prediction/selection and, their further applications in the design of vaccines are discussed. Last but not least, safety, challenges, advantages, and future prospects of COVID-19 vaccines are highlighted.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e124228"},"PeriodicalIF":0.0,"publicationDate":"2022-01-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/b7/cb/ijpr-21-1-124228.PMC9420219.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40347213","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

Cloning, Expression and Purification of Full-length Recombinant Ecarin and Comparing Its Expression and Function with Its Truncated Form. 全长重组Ecarin的克隆、表达与纯化及其与截断型Ecarin的表达与功能比较。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-01-16 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr.123791

Zohreh Jafari, Mojgan Bandehpour, Shivasadat Gheflat, Nasrin Mohammadi, Bahram Kazemi

{"title":"Cloning, Expression and Purification of Full-length Recombinant Ecarin and Comparing Its Expression and Function with Its Truncated Form.","authors":"Zohreh Jafari, Mojgan Bandehpour, Shivasadat Gheflat, Nasrin Mohammadi, Bahram Kazemi","doi":"10.5812/ijpr.123791","DOIUrl":"https://doi.org/10.5812/ijpr.123791","url":null,"abstract":"Ecarin is a metalloproteinase found in snake venom (SVMP) with an important role in coagulation and control of hemostasis. It can specifically produce active-thrombin from prethrombin-2 and does not differentiate between normal and abnormal prothrombin. It is used in diagnostic tests and to evaluate the treatment process of many diseases. There are many drawbacks associated with separating these compounds from snake venom. Therefore, in this study, full-length recombinant Ecarin (r-Ecarin) was cloned, expressed, and purified in eukaryotic host cells. To determine the most effective form of the enzyme, r-Ecarin was compared with the recombinant truncated form, which has only the metalloprotease domain of the protein (r-Ecamet) in terms of function and expression. Briefly, A DNA construct composed of sequence-encoding Ecarin was designed and cloned into pCAGGS expression vector and, subsequently, expressed in Chinese Hamster Ovary (CHO) cells. To identify the enzymatic activity of expressed protein, a bioactivity assay was performed. Blood coagulation time and expression levels of r-Ecarin and r-Ecamet proteins were compared. Also, a histopathological assessment was carried out on the liver of mice treated with these proteins. Comparison of r-Ecarin and r-Ecamet expression pattern demonstrated that full-length Ecarin expression has at least 2-fold higher expression in eukaryotic cells. Determination of r-Ecarin function proved that this protein is capable of prothrombin cleavage and producing thrombin. Comparison of PT test results between the r-Ecarin and r-Ecamet showed that there is a significant difference in the activity of the two enzymes and the full-length protein coagulates the blood in less time.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e123791"},"PeriodicalIF":1.6,"publicationDate":"2022-01-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/33/d8/ijpr-21-1-123791.PMC9191215.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40407924","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

Preparation and Characterization of Lidocaine-Loaded, Microemulsion-Based Topical Gels. 负载利多卡因微乳化外用凝胶的制备与表征。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2022-01-12 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr.123787

Mahshid Daryab, Mehrdad Faizi, Arash Mahboubi, Reza Aboofazeli

{"title":"Preparation and Characterization of Lidocaine-Loaded, Microemulsion-Based Topical Gels.","authors":"Mahshid Daryab, Mehrdad Faizi, Arash Mahboubi, Reza Aboofazeli","doi":"10.5812/ijpr.123787","DOIUrl":"https://doi.org/10.5812/ijpr.123787","url":null,"abstract":"Microemulsion-based gels (MBGs) were prepared for transdermal delivery of lidocaine and evaluated for their potential for local anesthesia. Lidocaine solubility was measured in various oils, and phase diagrams were constructed to map the concentration range of oil, surfactant, cosurfactant, and water for oil-in-water (o/w) microemulsion (ME) domains, employing the water titration method at different surfactant/cosurfactant weight ratios. Refractive index, electrical conductivity, droplet size, zeta potential, pH, viscosity, and stability of fluid o/w MEs were evaluated. Carbomer® 940 was incorporated into the fluid drug-loaded MEs as a gelling agent. Microemulsion-based gels were characterized for spreadability, pH, viscosity, and in-vitro drug release measurements, and based on the results obtained, the best MBGs were selected and subsequently subjected to ex-vivo rat skin permeation anesthetic effect and irritation studies. Data indicated the formation of nano-sized droplets of MEs ranging from 20 - 52 nm with a polydispersity of less than 0.5. In-vitro release and ex-vivo permeation studies on MBGs showed significantly higher drug release and permeation in comparison to the marketed topical gel. Developed MBG formulations demonstrated greater potential for transdermal delivery of lidocaine and advantage over the commercially available gel product, and therefore, they may be considered as potential vehicles for the topical delivery of lidocaine.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e123787"},"PeriodicalIF":1.6,"publicationDate":"2022-01-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/d9/61/ijpr-21-1-123787.PMC9191217.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40407922","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: 5

Novel 2-(Diphenylmethylidene) Malonic Acid Derivatives as Anti-HIV Agents: Molecular Modeling, Synthesis and Biological Evaluation. 新型2-(二苯基甲基)丙二酸衍生物抗hiv药物:分子模拟、合成和生物学评价。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2021-12-14 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr.123827

Mehrnaz Lotfaliei, Elham Rezaee, Zahra Hajimahdi, Mohammad Mahboubi Rabbani, Rezvan Zabihollahi, Mohammad Reza Aghasadeghi, Sayyed Abbas Tabatabai

{"title":"Novel 2-(Diphenylmethylidene) Malonic Acid Derivatives as Anti-HIV Agents: Molecular Modeling, Synthesis and Biological Evaluation.","authors":"Mehrnaz Lotfaliei, Elham Rezaee, Zahra Hajimahdi, Mohammad Mahboubi Rabbani, Rezvan Zabihollahi, Mohammad Reza Aghasadeghi, Sayyed Abbas Tabatabai","doi":"10.5812/ijpr.123827","DOIUrl":"https://doi.org/10.5812/ijpr.123827","url":null,"abstract":"HIV, the virus that causes AIDS (acquired immunodeficiency syndrome), is one of the world's most severe health and development challenges. In this study, a novel series of 2-(diphenyl methylidene) malonic acid derivatives were designed as triple inhibitors of HIV reverse transcriptase, integrase, and protease. Docking models revealed that the target compounds have appropriate affinities to the active sites of the three HIV key enzymes. The synthesized malonic acid analogs were evaluated for their activities against the HIV virus (NL4-3) in HeLa cells cultures. Among them, compound 3 was the most potent anti-HIV agent with 55.20% inhibition at 10 μM and an EC50 of 8.4 μM. Interestingly, all the synthesized compounds do not show significant cytotoxicity at a concentration of 10 μM. As a result, these compounds may serve as worthy hits for the development of novel anti-HIV-agents.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e123827"},"PeriodicalIF":1.6,"publicationDate":"2021-12-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/bf/ca/ijpr-21-1-123827.PMC9191218.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40407917","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

Effects of Wound Fluid on Breast Cancer-derived Spheroids in a 3D Culture System: A Case Series Study. 三维培养系统中伤口液对乳腺癌源性球体的影响:一个病例系列研究

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2021-07-08 eCollection Date: 2022-12-01 DOI: 10.5812/ijpr.123828

Ali Hojat, Shabnam Jeibouei, Amir Reza Aref, Alireza Kalbasi, Maryam Moghaddam, Farzaneh Mohammadi, Seyed Mohammadreza Javadi, Mohammad Ajoudanian, Kazem Sharifi, Hakimeh Zali, Mohammad Esmaeil Akbari

{"title":"Effects of Wound Fluid on Breast Cancer-derived Spheroids in a 3D Culture System: A Case Series Study.","authors":"Ali Hojat, Shabnam Jeibouei, Amir Reza Aref, Alireza Kalbasi, Maryam Moghaddam, Farzaneh Mohammadi, Seyed Mohammadreza Javadi, Mohammad Ajoudanian, Kazem Sharifi, Hakimeh Zali, Mohammad Esmaeil Akbari","doi":"10.5812/ijpr.123828","DOIUrl":"https://doi.org/10.5812/ijpr.123828","url":null,"abstract":"Surgery is the standard treatment for breast malignancies, although local and distant relapses might occur. Previous studies have shown that surgery-induced wound fluid (WF) contains tumor-initiating and progressing factors; however, these experiments have only been performed on breast cancer cell lines. Since a cancerous tumor includes various components like malignant cells, recruited non-malignant cells and extracellular matrix, those investigations that only focused on cancer cell lines themselves are not adequate to establish WF's effects. We conducted a 3D model study where we mimicked the tumor microenvironment to re-assess previous in-vitro findings. We generated human-derived breast tumor spheroids from 23 patient specimens, dissociated and cultured them in microfluidic devices. The spheroids from each sample were treated with the patients' WF or RPMI medium. The proportion of live and dead cells was assessed using live/dead assays and fluorescent imaging on day 6. In 22 samples, the percentage of live cells was significantly higher in the WF-treated group than in the RPMI-treated group. In one sample, we observed an opposite trend. The results were contrary in one of the samples, and we reported that case with more details. We compared the two groups using the 3D culture environment of human-derived tumor spheroids prepared from different microfluidic devices to mimic the tumor environment heterogeneity. Our findings showed that most patients with breast cancer benefit from surgical wound healing. However, removal of the surgical-induced serum may not be a method of inhibiting the tumor in all patients.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"e123828"},"PeriodicalIF":1.6,"publicationDate":"2021-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://ftp.ncbi.nlm.nih.gov/pub/pmc/oa_pdf/f2/51/ijpr-21-1-123828.PMC9191216.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"40407921","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: 2

Silencing of Nucleostemin by siRNA Induces Apoptosis in MCF-7 and MDA-MB-468 Cell Lines. siRNA沉默核干素诱导MCF-7和MDA-MB-468细胞株凋亡

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2020-01-01 DOI: 10.22037/ijpr.2020.1100950

Mahdiyeh Moudi, Ramin Saravani, Saman Sargazi

{"title":"Silencing of Nucleostemin by siRNA Induces Apoptosis in MCF-7 and MDA-MB-468 Cell Lines.","authors":"Mahdiyeh Moudi, Ramin Saravani, Saman Sargazi","doi":"10.22037/ijpr.2020.1100950","DOIUrl":"https://doi.org/10.22037/ijpr.2020.1100950","url":null,"abstract":"One of the most important modulators involved in controlling apoptosis induction and viability of cancerous cells is nucleostemin (NS). Some studies revealed that NS is also needed to maintain the proliferation of embryonic neural stem cells and early embryogenesis. This study was designed to better elucidate the association between NS depletion status and apoptosis induction of both MCF-7 and MDA-MB-468 cell lines. We examined the effects of NS-targeting siRNAs on the expression of NS in MCF-7 and MDA-MB-468 human breast cancer cell lines by the Real-time polymerase chain reaction method. In addition, we investigated the correlation between knockdown of NS and viability rates and apoptosis induction in MCF-7 and MDA-MB-468 cell lines using the MTT assay and annexin V/PI staining, respectively. The NS-targeting siRNAs inhibited the viability of the cells in a dose- and time-dependent manner and induced apoptosis after 48 h in the cells. Thus, consistent with previous articles, this protein can be one of the regulators related to the inhibition of apoptosis and the increased viability of tumor-initiating cells in human breast cancer cell lines as well as other cancers.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"37-45"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462512/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38373751","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

LED Photo-polymerization, a Novel Strategy for Triggered Release Liposomes. LED光聚合:一种触发释放脂质体的新策略。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2020-01-01 DOI: 10.22037/ijpr.2019.112366.13712

Afsoon Akbarzadeh, Pezhman Sasanpour, Hamid R Moghimi

{"title":"LED Photo-polymerization, a Novel Strategy for Triggered Release Liposomes.","authors":"Afsoon Akbarzadeh, Pezhman Sasanpour, Hamid R Moghimi","doi":"10.22037/ijpr.2019.112366.13712","DOIUrl":"https://doi.org/10.22037/ijpr.2019.112366.13712","url":null,"abstract":"LED light is used for many medical and cosmetic applications such as phototherapy and skin rejuvenation. Such physical methods can be combined with drug therapy, such as LED-responsive drug delivery system, the subject of present investigation. To perform this investigation, a nanoliposome composed of DPPC, DSPE-PEG2000, and DC8,9PC, was prepared as LED-sensitive systems. Calcein was loaded in the liposomes as a fluorescent probe for drug release studies. Different LED wavelengths (blue, green and red) were used for triggering release of calcein from nanoliposome. Indoor daylight, darkness, and sunlight were applied as controls. Results showed that liposomes do not release their cargo in darkness, but they released it in response to indoor daylight, sunlight and LEDs, with the blue light showing the highest effect. Results also showed that release of calcein was sensitive to wavelength. Our results reveal potential of LED-sensitive liposomes for medical and cosmetic applications and that such system can be combined with phototherapy. Such concomitant therapies can increase medical/cosmetic effects and decrease adverse reactions to phototherapy.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"260-270"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462490/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38473428","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

Noncompetitive Inhibition of Bovine Liver Catalase by Lawsone: Kinetics, Binding Mechanism and in silico Modeling Approaches. Lawsone对牛肝过氧化氢酶的非竞争性抑制:动力学、结合机制和硅模拟方法。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2020-01-01 DOI: 10.22037/ijpr.2019.111600.13255

Simin Khataee, Gholamreza Dehghan, Samaneh Rashtbari, Siavash Dastmalchi, Mehrdad Iranshahi

{"title":"Noncompetitive Inhibition of Bovine Liver Catalase by Lawsone: Kinetics, Binding Mechanism and in silico Modeling Approaches.","authors":"Simin Khataee, Gholamreza Dehghan, Samaneh Rashtbari, Siavash Dastmalchi, Mehrdad Iranshahi","doi":"10.22037/ijpr.2019.111600.13255","DOIUrl":"https://doi.org/10.22037/ijpr.2019.111600.13255","url":null,"abstract":"Lawsone (2-hydroxy-1,4-naphtoquinone; LAW), as a naphthoquinone derivative, is the biologically active component of Henna leaves. In this study, the structural and functional effects of LAW on bovine liver catalase (BLC), has been studied utilizing ultraviolet-visible (UV-vis) absorption, fluorescence, and ATR-FTIR spectroscopic techniques, and molecular docking approach. In-vitro kinetic study showed that by adding gradual concentrations of LAW, catalase activity was significantly decreased through noncompetitive inhibition mechanism. UV-vis and ATR-FTIR spectroscopic results illustrated that additional concentration of LAW lead to significant change in secondary structure of the enzyme.The fluorescence spectroscopic results at different temperatures indicated that LAW quenches the intrinsic fluorescence of BLC by dynamic mechanismand there is just one binding site for LAW on BCL. Changing the micro-environment nearby two aromatic residues (tryptophan (Trp) and tyrosine (Tyr)) were resulted from synchronous fluorescence. The thermodynamic parameters were implied that the hydrophobic bindings have a significant impress in the organization of the LAW-catalase complex. Molecular docking data in agreement with experimental results, confirmed that hydrophobic interactions are dominant. Inhibition of enzyme activity by LAW, showed that along withits helpful effects as ananti-oxidant compounds, the side effects of LAW should not be overlooked.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"383-397"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462507/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38373580","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: 4

Phytochemical Study of Tanacetum Sonbolii Aerial Parts and the Antiprotozoal Activity of its Components. 黄芪地上部分的植物化学研究及其成分的抗原虫活性。

IF 1.6

Iranian Journal of Pharmaceutical Research : IJPR Pub Date : 2020-01-01 DOI: 10.22037/ijpr.2020.1100951

Sahar Mofidi Tabatabaei, Mahdi Moridi Farimani, Samad Nejad-Ebrahimi, Peyman Salehi

{"title":"Phytochemical Study of Tanacetum Sonbolii Aerial Parts and the Antiprotozoal Activity of its Components.","authors":"Sahar Mofidi Tabatabaei, Mahdi Moridi Farimani, Samad Nejad-Ebrahimi, Peyman Salehi","doi":"10.22037/ijpr.2020.1100951","DOIUrl":"https://doi.org/10.22037/ijpr.2020.1100951","url":null,"abstract":"The genus Tanacetum includes some popular endemic species of the flora of Iran, with important medicinal properties. In a project, directed at structurally interesting bioactive metabolites from Iranian endemic species, we studied Tanacetum sonbolii Mozaff. Eight compounds comprising six phenolic and two terpenoidal compounds were isolated from the ethyl acetate extract of the aerial parts of the plant by normal and reverse phase chromatography. Their structures were established mainly by 1D and 2D NMR spectroscopic techniques, including 1H-1H COSY, HSQC and HMBC methods and confirmed by comparing their NMR data with those reported in the literature. The compounds namely: 2,4-dihydroxy-6-methoxyacetophenone (1), apigenin (2), 5-desmethylsinensetin (3), 5-desmethylnobiletin (4), 8-methoxycirsilineol (5), scopoletin (6), ursolic acid (7), and β-sitosterol (8). In-vitro antiprotozoal activity of compounds 1, 3, and 5 were evaluated against Trypanosoma brucei rhodesiense, Trypanosoma cruzi, Leishmania donovani and Plasmodium falciparum parasites and also toxicity against rat myoblast (L6) cells. Compound 5 showed promising activity against T. b. rhodesiense.","PeriodicalId":416671,"journal":{"name":"Iranian Journal of Pharmaceutical Research : IJPR","volume":" ","pages":"77-83"},"PeriodicalIF":1.6,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7462493/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"38375672","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: 2