Iranian Journal of Pharmaceutical Research最新文献

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Synthesis and Biological Evaluation of New Nitroimidazole Derivatives as Anti-Helicobacter pylori Agents Against Metronidazole-Resistant Strains 新型硝基咪唑衍生物抗甲硝唑耐药幽门螺杆菌的合成及生物学评价
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-10-14 DOI: 10.5812/ijpr-137969
Zahra Bayati, Salimeh Amidi, Mahnaz Shahabimehr, Masoud Alebouyeh, Arash Mahboubi, Sayyed Abbas Tabatabai
{"title":"Synthesis and Biological Evaluation of New Nitroimidazole Derivatives as Anti-Helicobacter pylori Agents Against Metronidazole-Resistant Strains","authors":"Zahra Bayati, Salimeh Amidi, Mahnaz Shahabimehr, Masoud Alebouyeh, Arash Mahboubi, Sayyed Abbas Tabatabai","doi":"10.5812/ijpr-137969","DOIUrl":"https://doi.org/10.5812/ijpr-137969","url":null,"abstract":": Since several Helicobacter pylori strains have become resistant to metronidazole, new nitroimidazole derivatives based on metronidazole were designed and synthesized with different substituents on imidazole nitrogen. The activity of the synthesized compounds was evaluated against 20 clinically isolated metronidazole-resistant H. pylori strains. Some synthesized compounds were effective against those metronidazole-resistant H. pylori strains. Three compounds exhibited the most potent inhibitory activities (MIC50 = 8 µg/mL and MIC90 = 16 µg/mL).","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"42 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135803365","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Froriepia subpinnata Leaf Extract-Induced Apoptosis in the MCF-7 Breast Cancer Cell Line by Increasing Intracellular Oxidative Stress 山楂叶提取物通过增加细胞内氧化应激诱导MCF-7乳腺癌细胞凋亡
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-10-14 DOI: 10.5812/ijpr-136643
Hanieh Rostamabadi, Mohammas Rasoul Samandari Bahraseman, Keyvan Esmaeilzadeh-Salestani
{"title":"Froriepia subpinnata Leaf Extract-Induced Apoptosis in the MCF-7 Breast Cancer Cell Line by Increasing Intracellular Oxidative Stress","authors":"Hanieh Rostamabadi, Mohammas Rasoul Samandari Bahraseman, Keyvan Esmaeilzadeh-Salestani","doi":"10.5812/ijpr-136643","DOIUrl":"https://doi.org/10.5812/ijpr-136643","url":null,"abstract":"Background: Froriepia subpinnata (F. subpinnata) is one of the plants used in the diet of Iranian people. Previous studies have investigated the antioxidant and antibacterial effects of this plant extract, but no study has been conducted on its anticancer properties. Objectives: In this study, we investigated the effect of F. subpinnata extract on MCF-7 breast cancer cells. Methods: The inhibitory effect of F. subpinnata leaf extract was determined on the growth of cancer cells by the MTT test. The ROS (reactive oxygen species) test was used to investigate the impact of the extract on intracellular oxidative stress. Flow cytometry and real-time PCR tests were used to investigate the apoptosis-related molecular processes. The GC-MS analysis was performed to determine the most abundant components. Results: The GC-MS analysis showed that phytol, mono-ethylhexyl phthalate (MEHP), cinnamaldehyde, and neophytadiene constituted 60% of the extracted content. The MTT assay demonstrated that F. subpinnata leaf extract caused 50% lethality at a 400 μg/mL dose in MCF7 cells. The F. subpinnata extract at low doses decreased the ROS level for 24 hours in MCF-7, but by increasing the concentration, the ROS levels increased. At the IC50 dose (inhibitory concentration (IC) associated with 50% impact), the ROS level increased 3.5 times compared to the control group. Examining the effect of N-acetyl cysteine (NAC) showed that this antioxidant agent could prevent the lethal impact of the extract and eliminate the ROS increase in MCF7 cells. Flow cytometry and real-time PCR results showed that the extract specifically induced apoptosis through the internal apoptosis pathway in this cancer cell line. Conclusions: The F. subpinnata extract induced apoptosis by increasing ROS in MCF-7 cancer cells and can be considered for further studies.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135803849","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Evaluation of the Relationship Between Serum miR-200b-3p and miR-214-3p Expression Levels with Soluble ACE2 and TMPRSS2 in COVID-19 Patients 评估COVID-19患者血清miR-200b-3p和miR-214-3p表达水平与可溶性ACE2和TMPRSS2的关系
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-10-11 DOI: 10.5812/ijpr-137832
Faezeh Mortazavi, Mohsen Soltanshahi, Gholamhossein Tamaddon
{"title":"Evaluation of the Relationship Between Serum miR-200b-3p and miR-214-3p Expression Levels with Soluble ACE2 and TMPRSS2 in COVID-19 Patients","authors":"Faezeh Mortazavi, Mohsen Soltanshahi, Gholamhossein Tamaddon","doi":"10.5812/ijpr-137832","DOIUrl":"https://doi.org/10.5812/ijpr-137832","url":null,"abstract":"Background: The emergence and rapid global spread of the coronavirus disease 2019 (COVID-19) has presented a significant global health challenge. Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infects human host cells through the interaction of angiotensin-converting enzyme 2 (ACE2) and transmembrane serine protease 2 (TMPRSS2), which serve as main regulators for viral entry. Specifically, ACE2 and TMPRSS2 genes are influenced by two microRNAs: miR-200b-3p and miR-214-3p, respectively. The objective of this study was to explore the association between the serum levels of miR-200b-3p and miR-214-3p and the presence of circulating ACE2 and TMPRSS2 in severe and non-severe cases of COVID-19. Objectives: This study sought to examine the potential utility of microRNAs as biomarkers for assessing disease severity and progression. Additionally, the study aimed to elucidate the interplay between microRNAs and the ACE2 and TMPRSS2 proteins, which play crucial roles in facilitating SARS-CoV-2 viral entry and infection. Methods: This practical-foundational study involved the collection of samples from 61 hospitalized patients with confirmed COVID-19 and 31 healthy individuals. Subsequently, the enzyme-linked immunosorbent assay (ELISA) technique was utilized to measure the concentrations of ACE2 and TMPRSS2 in the blood samples. Additionally, the expression levels of serum miR-200b-3p and miR-214-3p were analyzed using real-time polymerase chain reaction (PCR). The statistical analysis of the data was conducted using GraphPad Prism software (version 8.02) and SPSS software (version 19.0), ensuring the accurate interpretation of results. Results: The findings revealed significant increases in the peripheral blood concentrations of ACE2 and TMPRSS2 in patients with non-severe COVID-19, compared to healthy individuals (P < 0.001 and P < 0.01, respectively). Similarly, patients with severe COVID-19 exhibited higher serum levels of ACE2 and TMPRSS2 than healthy subjects (P < 0.0001). Additionally, the serum levels of miR-200b-3p and miR-214-3p were decreased in both non-severe and severe COVID-19 patients, compared to healthy individuals (P < 0.01 and P < 0.0001, respectively). Moreover, a decrease in the serum levels of both miR-200b-3p and miR-214-3p was observed in patients with severe COVID-19, compared to those with non-severe cases (P < 0.001). Furthermore, this study identified a negative correlation between miR-200b-3p and ACE2 serum levels and between miR-214-3p and TMPRSS2 peripheral blood levels. Conclusions: The above-mentioned findings suggest that miR-200b-3p and miR-214-3p might be potential biomarkers for disease severity and prognosis in COVID-19 patients.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"630 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136062849","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Integration of Machine Learning and Structural Analysis for Predicting Peptide Antibiofilm Effects: Advancements in Drug Discovery for Biofilm-Related Infections 整合机器学习和结构分析预测肽抗生物膜效应:生物膜相关感染药物发现的进展
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-09-30 DOI: 10.5812/ijpr-138704
Fatemeh Ebrahimi Tarki, Mahboobeh Zarrabi, Ahya Abdiali, Mahkame Sharbatdar
{"title":"Integration of Machine Learning and Structural Analysis for Predicting Peptide Antibiofilm Effects: Advancements in Drug Discovery for Biofilm-Related Infections","authors":"Fatemeh Ebrahimi Tarki, Mahboobeh Zarrabi, Ahya Abdiali, Mahkame Sharbatdar","doi":"10.5812/ijpr-138704","DOIUrl":"https://doi.org/10.5812/ijpr-138704","url":null,"abstract":"Background: The rise of antibiotic resistance has become a major concern, signaling the end of the golden age of antibiotics. Bacterial biofilms, which exhibit high resistance to antibiotics, significantly contribute to the emergence of antibiotic resistance. Therefore, there is an urgent need to discover new therapeutic agents with specific characteristics to effectively combat biofilm-related infections. Studies have shown the promising potential of peptides as antimicrobial agents. Objectives: This study aimed to establish a cost-effective and streamlined computational method for predicting the antibiofilm effects of peptides. This method can assist in addressing the intricate challenge of designing peptides with strong antibiofilm properties, a task that can be both challenging and costly. Methods: A positive library, consisting of peptide sequences with antibiofilm activity exceeding 50%, was assembled, along with a negative library containing quorum-sensing peptides. For each peptide sequence, feature vectors were calculated, while considering the primary structure, the order of amino acids, their physicochemical properties, and their distributions. Multiple supervised learning algorithms were used to classify peptides with significant antibiofilm effects for subsequent experimental evaluations. Results: The computational approach exhibited high accuracy in predicting the antibiofilm effects of peptides, with accuracy, precision, Matthew's correlation coefficient (MCC), and F1 score of 99%, 99%, 0.97, and 0.99, respectively. The performance level of this computational approach was comparable to that of previous methods. This study introduced a novel approach by combining the feature space with high antibiofilm activity. Conclusions: In this study, a reliable and cost-effective method was developed for predicting the antibiofilm effects of peptides using a computational approach. This approach allows for the identification of peptide sequences with substantial antibiofilm activities for further experimental investigations. Accessible source codes and raw data of this study can be found online (hiABF), providing easy access and enabling future updates.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"20 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136278729","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Designing and Expression of Recombinant Chimeric Spike Protein from SARS-CoV-2 in Escherichia coli and Its Immunogenicity Assessment 重组SARS-CoV-2嵌合刺突蛋白在大肠杆菌中的设计表达及其免疫原性评价
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-09-10 DOI: 10.5812/ijpr-137751
Sahar Karimi, Shahram Nazarian, Fattah Sotoodehnejadnematalahi, Roohollah Dorostkar, Jafar Amani
{"title":"Designing and Expression of Recombinant Chimeric Spike Protein from SARS-CoV-2 in Escherichia coli and Its Immunogenicity Assessment","authors":"Sahar Karimi, Shahram Nazarian, Fattah Sotoodehnejadnematalahi, Roohollah Dorostkar, Jafar Amani","doi":"10.5812/ijpr-137751","DOIUrl":"https://doi.org/10.5812/ijpr-137751","url":null,"abstract":": Since December 2019, the world has been grappling with an ongoing global COVID-19 pandemic. Various virus variants have emerged over the past two years, each posing a greater threat than its predecessors. The recent appearance of the omicron variant (B.1.1.529) has raised significant alarm within the field of epidemiology due to its highly contagious nature and rapid transmission rate. The omicron variant possessed mutations in the key receptor-binding domain (RBD) region, the S region, and these modifications have shown a notable impact on the strain's susceptibility to neutralizing antibodies. Developing safe and efficient vaccines to prevent a future severe acute respiratory outbreak of coronavirus syndrome 2 (SARS-CoV-2) is significant. Viral surface spike proteins are ideal targets for vaccines. This study aimed to find a multi-subunit chimeric vaccine. After conducting bioinformatics analysis, the recombinant spike (RS) protein of SARS-CoV-2 was deliberately designed and subsequently produced using E. coli expression systems. The immunogenicity of RS and neutralizing antibody responses were evaluated on immunized BALB/c mice. There was a significant difference in antibody titers between RS-immunized mice and control groups. The endpoint of the serum antibody titer of mice immunized with our chimeric protein was 2.5 times higher than that of the negative control. The chimeric construct could present multiple antigens simultaneously, influentially affecting immunization. Sera from mice vaccinated by RS could recognize the SARS-CoV-2 virus and neutralize antibodies. Our chimeric peptide could bind to antibodies in the serum of patients infected with different serotypes of the SARS-CoV-2 virus, such as alpha, delta, and omicron variants. The results indicated that the RS protein would be a potential novel antigenic candidate for subunit vaccine development and could be used as a useful alternative to generate diagnostic serological tests for SARS-CoV-2 infection.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"15 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136072046","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Cerasome Versus Liposome: A Comparative Pharmacokinetic Analysis Following Intravenous Administration into Rats 脂质体与脂质体:大鼠静脉给药后的比较药代动力学分析
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-09-09 DOI: 10.5812/ijpr-138362
Shima Bahri, Erfan Abdollahizad, Iman Mahlooji, Elham Rezaee, Zahra Abbasian, Simin Dadashzadeh
{"title":"Cerasome Versus Liposome: A Comparative Pharmacokinetic Analysis Following Intravenous Administration into Rats","authors":"Shima Bahri, Erfan Abdollahizad, Iman Mahlooji, Elham Rezaee, Zahra Abbasian, Simin Dadashzadeh","doi":"10.5812/ijpr-138362","DOIUrl":"https://doi.org/10.5812/ijpr-138362","url":null,"abstract":"Background: Cerasomes, due to their external siloxane network, demonstrate markedly higher physicochemical stability and, therefore, easier handling and storage than liposomes. Objectives: The main objective of this study was to compare the pharmacokinetics (PK) of cerasome and liposome following intravenous administration. The PK of PEGylated and non-PEGylated cerasomes was also compared to see whether the presence of a hydrophilic siloxane network on the surface of cerasomes can play the role of polyethylene glycol (PEG) in increasing the blood circulation of these vesicles. Methods: Silver sulfide (Ag2S) quantum dots (Qds)-loaded PEGylated and non-PEGylated cerasomes and PEGylated liposomes were fabricated and thoroughly characterized in terms of particle size, polydispersity index, zeta potential, entrapment efficiency, and in vitro stability. For pharmacokinetic evaluation, the free Qds and the selected formulations were intravenously injected into rats, and blood samples were collected for up to 72 hours. Pharmacokinetic parameters were calculated by the non-compartmental method. Results: Both cerasomal and liposomal carriers significantly improved the PK of Qds. For example, the elimination half-life (t1/2) and the area under the plasma concentration-time curve from time 0 to time infinity (AUC0-∞) for the free Qds were 4.39 h and 8.01 µg/mL*h and for cerasomal and liposomal formulations were 28.82 versus 26.95 h and 73.25 versus 62.02 µg/mL*h, respectively. However, compared to each other, the plasma concentration-time profiles of PEGylated cerasomes and liposomes displayed similar patterns, and the statistical comparison of their pharmacokinetic parameters did not show any significant difference between the two types of carriers. For PEGylated cerasomes, t1/2 and AUC0-∞ values were respectively 1.6 and 3.3 times greater than the classic cerasome, indicating that despite the presence of a hydrophilic siloxane network, the incorporation of PEG is necessary to reduce the clearance of cerasomes. Conclusions: The comparable PK of PEGylated cerasomes and liposomes, along with the higher physicochemical stability of cerasomes, can be considered an important advantage for the clinical application of cerasomes. Additionally, the easy surface functionalizing ability of cerasomes confers a dual advantage over liposomes. The study findings also showed that the presence of a hydrophilic siloxane network on the surface of cerasomes alone is not enough to make them circulate long.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"16 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136107799","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A Mechanistic Study on the Fluidization and Enhancement Effects of Cineole Toward Stratum Corneum Intercellular Lamellar Lipids: A Liquid Crystalline Model Approach 桉叶脑对角质层细胞间层状脂质流化和增强作用的机理研究:液晶模型方法
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-06-22 DOI: 10.5812/ijpr-134731
Leila Karami, Hamid Reza Moghimi
{"title":"A Mechanistic Study on the Fluidization and Enhancement Effects of Cineole Toward Stratum Corneum Intercellular Lamellar Lipids: A Liquid Crystalline Model Approach","authors":"Leila Karami, Hamid Reza Moghimi","doi":"10.5812/ijpr-134731","DOIUrl":"https://doi.org/10.5812/ijpr-134731","url":null,"abstract":"Background: The stratum corneum (SC) serves as the primary barrier for permeation in human skin. Penetration enhancers, such as 1,8-cineole, are utilized to enhance the permeation of drugs. Cineole increases the permeation of chemicals through different mechanisms. However, its mechanism, particularly at high concentrations, has not been well-studied and is the subject of the present investigation. Objectives: In continuation of our previous studies, the present investigation aims to elucidate the mechanism of action and concentration dependency of the effects of 1,8-cineole on the structure, diffusional properties, and partitioning behavior of the SC at high concentrations. This will be achieved through lamellar liquid crystalline models and ex-vivo skin studies. Methods: A lamellar liquid crystalline lipid matrix model in the presence (25 - 90%, w/w) and absence of cineole was prepared from SC lipids and characterized by X-ray diffraction, differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and polarized light microscopy (PLM) studies. Release of the model lipophilic drug (diazepam) from cineole and cineole-treated matrices and the permeation of the drug from cineole and cineole-containing matrices (as a vehicle similar to the stratum corneum lipids) through excised rat skin were studied. Drug assay was performed by HPLC. Results: The PLM, DSC, and X-ray studies showed that the model matrix had a lamellar gel-liquid crystalline structure, and cineole fluidized the structure concentration-dependently and created other mesomorphic textures, such as myelinic figures. Release experiments showed that diffusion coefficients remained almost constant at high cineole concentrations of 40-90%, suggesting similar fluidization states. Skin permeation studies indicated that the diffusion coefficient (estimated from lag-time) increased concentration-dependently and played a role in permeability coefficient (Kp) increments alongside the increased partitioning of the model drug into the skin. Data suggest that high concentrations of cineole at the skin surface might not provide enough cineole in the skin for full fluidization, despite the similarity of the vehicle to SC lipids and even at high concentrations. Conclusions: The enhancement effect of cineole is concentration-dependent and might reach maximum fluidization at certain concentrations, but this maximum might not be easily achievable when cineole is used in formulations as pure or in a vehicle.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"8 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136286497","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A Mechanistic Study on the Fluidization and Enhancement Effects of Cineole Toward Stratum Corneum Intercellular Lamellar Lipids: A Liquid Crystalline Model Approach 桉叶脑对角质层细胞间层状脂质流化和增强作用的机理研究:液晶模型方法
IF 1.6 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-06-22 DOI: 10.5812/ijpharm-134731
L. Karami, H. Moghimi
{"title":"A Mechanistic Study on the Fluidization and Enhancement Effects of Cineole Toward Stratum Corneum Intercellular Lamellar Lipids: A Liquid Crystalline Model Approach","authors":"L. Karami, H. Moghimi","doi":"10.5812/ijpharm-134731","DOIUrl":"https://doi.org/10.5812/ijpharm-134731","url":null,"abstract":"Background: The stratum corneum (SC) serves as the primary barrier for permeation in human skin. Penetration enhancers, such as 1,8-cineole, are utilized to enhance the permeation of drugs. Cineole increases the permeation of chemicals through different mechanisms. However, its mechanism, particularly at high concentrations, has not been well-studied and is the subject of the present investigation. Objectives: In continuation of our previous studies, the present investigation aims to elucidate the mechanism of action and concentration dependency of the effects of 1,8-cineole on the structure, diffusional properties, and partitioning behavior of the SC at high concentrations. This will be achieved through lamellar liquid crystalline models and ex-vivo skin studies. Methods: A lamellar liquid crystalline lipid matrix model in the presence (25 - 90%, w/w) and absence of cineole was prepared from SC lipids and characterized by X-ray diffraction, differential scanning calorimetry (DSC), Thermogravimetric Analysis (TGA), and Polarized Light Microscopy (PLM) studies. The release of the model lipophilic drug (diazepam) from cineole and cineole-treated matrices and the permeation of the drug from cineole and cineole-containing matrices (as a vehicle similar to the stratum corneum lipids) through excised rat skin were studied. A drug assay was performed by HPLC. Results: The PLM, DSC, and X-ray studies showed that the model matrix had a lamellar gel-liquid crystalline structure, and cineole fluidized the structure concentration dependently and created other mesomorphic textures, such as myelinic figures. Release experiments showed that diffusion coefficients remained almost constant at high cineole concentrations of 40-90%, suggesting similar fluidization states. Skin permeation studies indicated that the diffusion coefficient (estimated from lag-time) increased concentration-dependently and played a role in permeability coefficient (Kp) increments alongside the increased partitioning of the model drug into the skin. Data suggest that high concentrations of cineole at the skin surface might not provide enough cineole in the skin for full fluidization, despite the similarity of the vehicle to SC lipids and even at high concentrations. Conclusions: The enhancement effect of cineole is concentration-dependent and might reach maximum fluidization at certain concentrations, but this maximum might not be easily achievable when cineole is used in formulations as pure or in a vehicle.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"1 1","pages":""},"PeriodicalIF":1.6,"publicationDate":"2023-06-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89788613","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effects of Komouni Formulation (Herbal Product of Persian Medicine) With a Low-Calorie Diet on Cardiometabolic Risk Factors in Overweight and Obese Women: A Triple-Blinded Randomized Clinical Trial 低热量饮食对超重和肥胖女性心脏代谢危险因素的影响:一项三盲随机临床试验
4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-06-21 DOI: 10.5812/ijpr-136114
Zahra Aghabeiglooei, Nazli Namazi, Mehrdad Karimi, Samaneh Soleymani, Mohammad Hossein Ayati, Hossein Rezaeizadeh
{"title":"Effects of Komouni Formulation (Herbal Product of Persian Medicine) With a Low-Calorie Diet on Cardiometabolic Risk Factors in Overweight and Obese Women: A Triple-Blinded Randomized Clinical Trial","authors":"Zahra Aghabeiglooei, Nazli Namazi, Mehrdad Karimi, Samaneh Soleymani, Mohammad Hossein Ayati, Hossein Rezaeizadeh","doi":"10.5812/ijpr-136114","DOIUrl":"https://doi.org/10.5812/ijpr-136114","url":null,"abstract":"Background: The prevalence of obesity has almost tripled since 1975, and obesity places a heavy economic burden on healthcare systems. There is a high tendency to use a variety of complementary medicine modalities for weight management among obese patients. Persian Medicine is an ancient medical school practiced for thousands of years in Iran. Found in reliable Iranian traditional resources, Komouni formulation (KF) is a compound medicine that can be effective in the treatment of obesity. It comprises black caraway (Bunium persicum Boiss.), anise (Pimpinella anisum L.), fennel (Foeniculum vulgare Miller), and ajwain (Trachyspemum ammi L.) Objectives: This study aimed to determine the effects of KF on anthropometric indices and metabolic parameters in overweight and obese women. Methods: This triple-blinded randomized controlled clinical trial was performed on 70 overweight or obese women aged 20 - 40 years, with a body mass index (BMI) of 25 - 34.9 kg/m2. The subjects were randomly divided into two groups (each group n = 35) to receive a calorie-restricted diet with 2 g/day (500 mg 30 minutes before breakfast, 1000 mg 30 minutes before lunch, and 500 mg 30 minutes before dinner) KF or placebo for 8 weeks. Anthropometric indices, food intake, and biochemical parameters were measured at baseline and after the intervention. Results: A total of 60 women (intervention = 30; placebo = 30) completed the trial. After the intervention, the KF group experienced a significant reduction in weight (-4.8 vs. -3.2 kg; P = 0.0001), BMI (-1.8 vs. -0.79 kg/m2; P = 0.0001), waist circumference (-5.28 vs. -3.20 cm; P = 0.004), hip circumference (-0.018 vs. -0.008 cm; P = 0.047), fasting blood sugar (-5.6 vs. 0.33; P = 0.025), and low-density lipoprotein (-11.7 vs. 6.7; P = 0.0001), compared to the placebo group. None of the patients in the intervention and placebo groups reported any side effects. Conclusions: Using KF, along with a calorie-restricted diet, can reduce cardiometabolic risk factors in overweight and obese women. However, further studies are needed to elucidate the efficacy of KF as a complementary therapy in obesity.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"104 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135089505","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Effects of Komouni Formulation (Herbal Product of Persian Medicine) With a Low-Calorie Diet on Cardiometabolic Risk Factors in Overweight and Obese Women: A Triple-Blinded Randomized Clinical Trial 低热量饮食对超重和肥胖女性心脏代谢危险因素的影响:一项三盲随机临床试验
IF 1.6 4区 医学
Iranian Journal of Pharmaceutical Research Pub Date : 2023-06-21 DOI: 10.5812/ijpharm-136114
Zahra Aghabeiglooei, N. Namazi, M. Karimi, S. Soleymani, M. Ayati, H. Rezaeizadeh
{"title":"Effects of Komouni Formulation (Herbal Product of Persian Medicine) With a Low-Calorie Diet on Cardiometabolic Risk Factors in Overweight and Obese Women: A Triple-Blinded Randomized Clinical Trial","authors":"Zahra Aghabeiglooei, N. Namazi, M. Karimi, S. Soleymani, M. Ayati, H. Rezaeizadeh","doi":"10.5812/ijpharm-136114","DOIUrl":"https://doi.org/10.5812/ijpharm-136114","url":null,"abstract":"Background: The prevalence of obesity has almost tripled since 1975, and obesity places a heavy economic burden on healthcare systems. There is a high tendency to use a variety of complementary medicine modalities for weight management among obese patients. Persian Medicine is an ancient medical school practiced for thousands of years in Iran. Found in reliable Iranian traditional resources, Komouni formulation (KF) is a compound medicine that can be effective in the treatment of obesity. It comprises black caraway (Bunium persicum Boiss.), anise (Pimpinella anisum L.), fennel (Foeniculum vulgare Miller), and ajwain (Trachyspemum ammi L.) Objectives: This study aimed to determine the effects of KF on anthropometric indices and metabolic parameters in overweight and obese women. Methods: This triple-blinded randomized controlled clinical trial was performed on 70 overweight or obese women aged 20 - 40 years, with a body mass index (BMI) of 25 - 34.9 kg/m2. The subjects were randomly divided into two groups (each group n = 35) to receive a calorie-restricted diet with 2 g/day (500 mg 30 minutes before breakfast, 1000 mg 30 minutes before lunch, and 500 mg 30 minutes before dinner) KF or placebo for 8 weeks. Anthropometric indices, food intake, and biochemical parameters were measured at baseline and after the intervention. Results: A total of 60 women (intervention = 30; placebo = 30) completed the trial. After the intervention, the KF group experienced a significant reduction in weight (-4.8 vs. -3.2 kg; P = 0.0001), BMI (-1.8 vs. -0.79 kg/m2; P = 0.0001), waist circumference (-5.28 vs. -3.20 cm; P = 0.004), hip circumference (-0.018 vs. -0.008 cm; P = 0.047), fasting blood sugar (-5.6 vs. 0.33; P = 0.025), and low-density lipoprotein (-11.7 vs. 6.7; P = 0.0001), compared to the placebo group. None of the patients in the intervention and placebo groups reported any side effects. Conclusions: Using KF, along with a calorie-restricted diet, can reduce cardiometabolic risk factors in overweight and obese women. However, further studies are needed to elucidate the efficacy of KF as a complementary therapy in obesity.","PeriodicalId":14595,"journal":{"name":"Iranian Journal of Pharmaceutical Research","volume":"8 11","pages":""},"PeriodicalIF":1.6,"publicationDate":"2023-06-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72427245","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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