2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research最新文献

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Pharmacognostic and Physico-chemical Investigation of Barleria cristata Linn. (Leaf) for Quality Control Assessment 冠芽孢杆菌的生药学和理化研究。(Leaf)用于质量控制评估
Bhuwan Chandra Joshi, Neha Panthri, Nondita Prasad, Jaswinder Kaur Virk
{"title":"Pharmacognostic and Physico-chemical Investigation of Barleria cristata Linn. (Leaf) for Quality Control Assessment","authors":"Bhuwan Chandra Joshi, Neha Panthri, Nondita Prasad, Jaswinder Kaur Virk","doi":"10.18502/pbr.v7i3.7700","DOIUrl":"https://doi.org/10.18502/pbr.v7i3.7700","url":null,"abstract":"Background: Barleria cristata Linn. belongs to the family Acanthaceae and is commonly known as Raktajhinti and VajraDanti. It is widely distributed in countries, such as India, Nepal, Bangladesh, Pakistan, and Asian tropical regions. This plant has been observed to bear multifarious ethnomedical uses in treating lung disorders, inflammatory conditions, toothache, anemia, and snakebite. A wide range of major chemical constituents, such as triterpenes, phenolic compounds, flavonoids, and glycosides are reported to be present in this plant. The plant exhibited diverse pharmacological actions, such as anti-inflammatory, antibacterial, antifungal, and antioxidant activities. The literature revealed insufficient information concerning the standardization of Barleria cristata Linn. \u0000Objectives: The present study aimed to explore the pharmacognostic and phytochemical characteristics of Barleria cristata Linn. (leaf).  \u0000Methods: The present study addressed quality control parameters, including loss on drying, ash values, extractive values, pharmacognostic parameters (e.g. macroscopic & microscopic characters and powder microscopy) as per the World Health Organization (WHO) guidelines.  \u0000Results: Biochemical analysis revealed total ash (16.11±0.38), acid insoluble ash (1.50±0.18), water-soluble ash (11.10±0.23), alcohol-soluble extractive (19.34±0.79), and water-soluble extractive (25.06±0.17), respectively. The transverse section of the leaf revealed the presence of the epidermis, covering trichomes, vascular bundle, and so on. The other parameters such as phytochemical investigation, fluorescence analysis, and thin-layer chromatography were also performed to explore the crucial values of these examinations.  \u0000Conclusion: The obtained data would be useful in the future for preparing a monograph for the authentication and standardization of this crude drug.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"29 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88024049","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 3
In vivo Toxicity Evaluation of Ethanolic Extract From Two Mangrove Plants 两种红树林植物乙醇提取物的体内毒性评价
A. Aunjum, R. Biswas, Abdullah Al Munna, M. Billah, E. Islam, K.M. Didarul Islam
{"title":"In vivo Toxicity Evaluation of Ethanolic Extract From Two Mangrove Plants","authors":"A. Aunjum, R. Biswas, Abdullah Al Munna, M. Billah, E. Islam, K.M. Didarul Islam","doi":"10.18502/pbr.v7i3.7702","DOIUrl":"https://doi.org/10.18502/pbr.v7i3.7702","url":null,"abstract":"Background: Mangrove plants, often possessing a unique collection of metabolites, have extensively been used for the primary healthcare of coastal residents. \u0000Objectives: To determine the safety level and enrich the scientific data, the present study aimed to investigate the toxicity of Avicennia officinalis and Excoecaria agallocha.  \u0000Methods: Ethanolic leaf and stem extracts were evaluated for cytotoxicity by brine shrimp lethality assay. The obtained extracts were administered to Swiss albino in a single dose (200, 400, 800, 1600, & 3200 mg/kg body weight) by oral-gavage for acute toxicity assay. Furthermore, systematic observation was performed by close monitoring for any toxic manifestations and mortality after dosing for the first 4 h, at 24 h and twice daily for 6 days. Evaluating the adverse effects were estimated by comparing the test groups with the controls. After sacrificing all group animals, relative organ weight was measured and histopathological analysis was conducted.  \u0000Results: Having Lethal Concentration (LC50) of 44.66 µg/mL, E. agallocha leaf was found with the highest toxicity against brine shrimp nauplii. The toxicological study data demonstrated no death and noticeable change in behavioral patterns in the test mice groups, compared with the control group. Moreover, no significant (P>0.05) differences were found in body weight and relative organ weights, compared to the controls. The histological structures of the liver in the treated mice displayed regular tissue configurations similar to the control group. \u0000Conclusion: In this study, the mice model exhibited no harmful effects; thus, the reported results indicated that the ethanolic extracts of leaf and stem of these two mangrove plants are safe for therapeutic use. Further long-term toxicological impact of the extracts should be determined for well-founded confirmation.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"39 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89862877","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","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 Aloysia citriodora Hydroalcoholic Extract on Ethanol-induced Hepatotoxicity in Male Wistar Rats 苦瓜水醇提取物对乙醇致雄性Wistar大鼠肝毒性的影响
E. Habibi, Fereshteh Beigom Talebpour Amiri, Mehdi Mokhatari, F. Shaki
{"title":"Effects of Aloysia citriodora Hydroalcoholic Extract on Ethanol-induced Hepatotoxicity in Male Wistar Rats","authors":"E. Habibi, Fereshteh Beigom Talebpour Amiri, Mehdi Mokhatari, F. Shaki","doi":"10.18502/pbr.v7i3.7698","DOIUrl":"https://doi.org/10.18502/pbr.v7i3.7698","url":null,"abstract":"Background: Chronic ethanol consumption presents toxic effects on liver tissue by inducing oxidative stress and inflammation. The antioxidant and anti-inflammatory properties of lemon verbena were established.  \u0000Objectives: The present study aimed to evaluate the protective effects of the hydroalcoholic extract of Aloysia citriodora (A. citriodora) on ethanol-induced hepatotoxicity in male rats by evaluating inflammatory and oxidative stress factors.  \u0000Methods: The study animals were randomly divided into 7 groups, (6/group) including control, extract alone (400mg/kg), ethanol 10 mg/kg, vitamin C 500 mg/kg + ethanol 10 mg/kg, and the fifth, sixth and seventh groups respectively received an intraperitoneal injection of 100, 200, and 400 mg/kg of A. citriodora extract plus ethanol once a day for 6 weeks. Oxidative stress parameters, such as glutathione content, lipid peroxidation, protein carbonyl, and reactive oxygen species were measured. Furthermore, inflammation parameters (nitric oxide) and liver damage were evaluated by determining the levels of liver enzymes including alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and histopathological examinations. \u0000Results: In the liver tissue of the ethanol-receiving group, a significant increase (P<0.001) was observed in ALT, AST, and ALP levels and pathological changes, compared to the control group. There was also a significant increase in the levels of oxidative stress and inflammatory factors. Interestingly, A. citriodora extract could inhibit ethanol-induced liver damage by suppressing oxidative stress and inflammation. \u0000Conclusion: A. citriodora extract significantly attenuated inflammation and oxidative stress caused by ethanol. Therefore, it can be suggested as a beneficial supplement for treating ethanol-induced hepatotoxicity.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82533327","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Clinical Characteristics of Intravenous Pantoprazole Consumption in Cardiac Intensive Care Unit 心脏重症监护病房静脉注射泮托拉唑的临床特点
G. Eslami, Elahe Karimpour Razkenar, Yahya Sharifi, A. Soleimani, E. Salehifar, Parastoo Karimi Aliabadi
{"title":"Clinical Characteristics of Intravenous Pantoprazole Consumption in Cardiac Intensive Care Unit","authors":"G. Eslami, Elahe Karimpour Razkenar, Yahya Sharifi, A. Soleimani, E. Salehifar, Parastoo Karimi Aliabadi","doi":"10.18502/pbr.v7i3.7699","DOIUrl":"https://doi.org/10.18502/pbr.v7i3.7699","url":null,"abstract":"Background: Proton Pump Inhibitors (PPIs) are the most common medicine for the treatment and prophylaxis of acid peptic conditions. The inappropriate use of the PPIs, mainly the intravenous form of pantoprazole may lead to excessive cost and unexpected adverse effects.  \u0000Objectives: The present study aimed to evaluate the use of intravenous pantoprazole in the International Heart Center in the north of Iran. \u0000Methods: The current retrospective study was performed on 215 patients hospitalized in Fatemeh Zahra Hospital in Sari City, Iran. Patients’ demographics, the type and doses of pantoprazole, and other relevant clinical data were recorded from their documentation. The appropriate use of pantoprazole was evaluated according to recommendations provided by Medscape 2020, and UpToDate 2020. \u0000Results: Prescribing PPI was appropriate for 53.5% of the examined patients; however, the majority of intravenous prescription cases were inappropriate (76.7%). Oral PPIs could have been used in 93.5% of the cases; however, they received the parenteral form of pantoprazole. The main cause of pantoprazole prescription in the explored hospital was stress ulcer prophylaxis, with the median 4/18 days used, which internal specialists in most of the cases (45.6%) prescribed. \u0000Conclusion: In the current study, administrating intravenous pantoprazole was inappropriate in most of the cases. As a result of this improper administration, the extensive cost is exposed to the healthcare system, i.e., likely to be unsafe for patients. Accordingly, risk and indication evaluation for the prescription of pantoprazole should be a priority in each patient. Finally, it seems necessary to determine a protocol for PPI prescription per hospital for the rational use of drugs. ","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"38 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91301736","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Involvement of Epigenetics in the Pathogenesis, Testing and Management of Coronavirus Disease 2019 (COVID-19) Pandemic: A Narrative Review 表观遗传学参与冠状病毒病2019 (COVID-19)大流行的发病机制、检测和管理:述评
T. Yahaya, E. Oladele, A. Muhammed, Abdulhakeem Haruna, Usman U. Liman
{"title":"Involvement of Epigenetics in the Pathogenesis, Testing and Management of Coronavirus Disease 2019 (COVID-19) Pandemic: A Narrative Review","authors":"T. Yahaya, E. Oladele, A. Muhammed, Abdulhakeem Haruna, Usman U. Liman","doi":"10.18502/pbr.v7i3.7697","DOIUrl":"https://doi.org/10.18502/pbr.v7i3.7697","url":null,"abstract":"Background: There is an intense search for the Coronavirus Disease 19 (COVID-19) cure, to stem the spread and burden of the disease worldwide. Studies revealed that epigenetic modifications impact the pathogenesis of some COVID-19 cases, which can be used as therapeutic targets.  \u0000Objectives: This review articulated the role of epigenetics in the pathogenesis and management of COVID-19. \u0000Methods: Relevant articles published between January 2000 and November 2020 were retrieved from reputable academic databases, including PubMed, SpringerLink, Scopus, and Google Scholar. \u0000Results: Epigenetic modifications in the COVID-19’s pathogen, called the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) and host’s cells may influence susceptibility or resistance to the disease. Notably, abnormal Deoxyribonucleic Acid (DNA) methylation and histone modification involving immune regulatory genes and molecules, such as cytokines and interferon-regulated genes may compromise immune function and enhance the host’s susceptibility and disease severity. The hypomethylation of SARS-CoV-2’s receptor, called the Angiotensin-Converting Enzyme 2 (ACE2), causing its overexpression, can also enhance SARS-CoV-2’s infectivity. Moreover, SARS-CoV-2 can hijack the host’s MicroRNA (miRNA) using its miRNA and compromise the immune function, increasing its infectivity. Fortunately, epigenetic changes are reversible; thus, a therapy that targets the epigenetic changes in the affected case may reverse COVID-19.  \u0000Conclusion: Modifications in the SARS-CoV-2 or host epigenome promote the pathogenesis and severity of COVID-19. Epigenetic changes are reversible, so healthcare providers are advised to formulate therapeutic procedures that target the causal mechanisms in the affected individual.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"12 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81845507","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Enhancing the Rational Use of Albumin and Intra-venous Pantoprazole in Hospitals by Implementing Pharmaceutical Guidelines in Hospitals: A Quasi-experimental study 实施《医院用药指南》促进白蛋白和静脉注射泮托拉唑在医院的合理使用:一项准实验研究
N. Sharifi, Vahid Kohpeima Jahromi, R. Raoofi, Mohamad Rahmanian, R. Zahedi
{"title":"Enhancing the Rational Use of Albumin and Intra-venous Pantoprazole in Hospitals by Implementing Pharmaceutical Guidelines in Hospitals: A Quasi-experimental study","authors":"N. Sharifi, Vahid Kohpeima Jahromi, R. Raoofi, Mohamad Rahmanian, R. Zahedi","doi":"10.18502/pbr.v7i3.7701","DOIUrl":"https://doi.org/10.18502/pbr.v7i3.7701","url":null,"abstract":"Background: Irrational use of drugs is a serious global problem, especially in developing countries. Scientific evidence has announced albumin and intravenous pantoprazole as expensive drugs, i.e., relatively irrationally applied in hospitals without following the guidelines.  \u0000Objectives: Considering health cost management policy in Iran, this study aimed to evaluate the effects of implementing pharmaceutical guidelines to rationalize and reduce the use of albumin and intravenous pantoprazole and the related inappropriate costs. \u0000Methods: This quasi-experimental study was conducted from January 2016 to October 2018 in two teaching Hospitals in Jahrom City, Iran. Pharmaceutical guidelines were implemented throughout the physical training as well as a pharmacist-led intervention and supervising. All inpatient prescriptions of the studied medicines were evaluated.  \u0000Results: Before conducting the intervention (June 2016), an average of 357 albumin vials were monthly used; after performing the interventions, 166 and 167 vials were used in 2017 and 2018, respectively. Reduced albumin use rate equaled 48%, i.e., significant (P=0.002). Annual cost-saving was estimated to be 25000 USD. In comparison to the previous year, there were 46% and 70% reductions in the mean number of pantoprazole vials prescribed in 2017 and 2018, respectively (P=0.005).Consuming pantoprazole was measured to be 1457 vials per month in 2017 and 795 in 2018, i.e., significant (P=0.002). Cost-Saving in intravenous pantoprazole was estimated to be 16000 USD in 2017 and 25000 USD in 2018.  \u0000Conclusion: Prescription strategies, such as pharmaceutical guidelines with educational measures, pharmacist-led intervention, monitoring the prescribing drug, and feedback to prescribers can significantly decrease the inappropriate use of expensive drugs and their costs.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-11-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89233011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
A Case of Erythema Multiforme Caused by Sildenafil Plus Tramadol 西地那非加曲马多致多形性红斑1例
A. Ghanbarzamani, E. Salehifar, Kaveh Kazemian
{"title":"A Case of Erythema Multiforme Caused by Sildenafil Plus Tramadol","authors":"A. Ghanbarzamani, E. Salehifar, Kaveh Kazemian","doi":"10.18502/pbr.v7i1.7358","DOIUrl":"https://doi.org/10.18502/pbr.v7i1.7358","url":null,"abstract":"In this report, we present a 29-year-old man who experienced EM five days after using sildenafil and tramadol. Based on clinical examination and history, the diagnosis of EM was made confirmed via skin biopsy, which found intra-epidermal bulla filled by fibrinous exudate, some mononuclear cells, and a few eosinophils. The spongiotic epidermis showed lichenoid interface dermatitis, eosinophilic spongiosis, and necrolysis, consistent with EM diagnosis. Fluocinolone, 0.025% ointment, was prescribed for the patient, and the lesions healed after two weeks of treatment.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74652450","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Safety Assessment of a New Strain of Lactobacillus pentosus (IBRC=11143) As a Candidate Probiotic 一株戊酸乳杆菌(IBRC=11143)作为候选益生菌的安全性评价
Saba Bahrehvar, Shiva Khezri, A. Barzegari, V. Nejati
{"title":"Safety Assessment of a New Strain of Lactobacillus pentosus (IBRC=11143) As a Candidate Probiotic","authors":"Saba Bahrehvar, Shiva Khezri, A. Barzegari, V. Nejati","doi":"10.18502/pbr.v7i1.7355","DOIUrl":"https://doi.org/10.18502/pbr.v7i1.7355","url":null,"abstract":"Background: It is believed that the consumption of an adequate amount of live lactic acid bacteria (as probiotic) may improve the health of the host. Many strains of lactic acid bacteria are generally considered to be safe. However, some strains have shown some adverse effects. \u0000Objectives: This study aimed to investigate the safety of a new strain of Lactobacillus pentosus (IBRC=11143) in Wistar rats \u0000Methods:In this experimental study, male and female Wistar rats (n=6) were used. A subacute toxicity study (for 28 days) was conducted by oral administration of Lactobacillus pentosus to the animals. In each sex, one group received saline, and the other two groups received the bacteria at doses of 1×108 and 1×109 Colony-Forming Units (CFU)/rat. \u0000Results: No significant alteration in the liver and kidney tissues was seen. However, in both sexes, there were significant differences in urea and creatinine levels between the control and the experimental groups. Some blood parameters (Lymphocyte, red blood cell, hematocrit, and hemoglobin) also showed significant changes in the groups that received the bacteria. Moreover, a significant increase in alkaline phosphatase level was observed in male rats. \u0000Conclusion: The results indicate that Lactobacillus pentosus (11143) is not entirely safe like other Lactobacillus strains. Therefore, the Lactobacillus pentosus (11143) strain may not be the right choice as a probiotic for human consumption.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81550791","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
Dental Prostheses and Risk of Medication-related Osteonecrosis of the Jaw 牙齿修复和药物相关性颌骨骨坏死的风险
L. D. de Castro, Satiro Watanabe, Luciano Leite de Castro
{"title":"Dental Prostheses and Risk of Medication-related Osteonecrosis of the Jaw","authors":"L. D. de Castro, Satiro Watanabe, Luciano Leite de Castro","doi":"10.18502/pbr.v7i1.7351","DOIUrl":"https://doi.org/10.18502/pbr.v7i1.7351","url":null,"abstract":"The article's abstract is not available.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"83 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78060658","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Pyrazolo[1,2-b]phthalazine-5,10- dione Derivatives: A New Class of α –Glucosidase Inhibitors 吡唑[1,2-b]酞嗪-5,10-二酮衍生物的合成:一类新的α -葡萄糖苷酶抑制剂
Maryam Hosseinpoor Tehrani, S. Mirshokraie, M. Khoobi, M. Amini
{"title":"Synthesis of Pyrazolo[1,2-b]phthalazine-5,10- dione Derivatives: A New Class of α –Glucosidase Inhibitors","authors":"Maryam Hosseinpoor Tehrani, S. Mirshokraie, M. Khoobi, M. Amini","doi":"10.18502/pbr.v7i2.7365","DOIUrl":"https://doi.org/10.18502/pbr.v7i2.7365","url":null,"abstract":"Background: Hyperglycemia is a metabolic disorder that refers to an increase in blood sugar in diabetic patients. α-Glucosidase has been introduced as a membrane-bound enzyme, and it is the main enzyme for carbohydrate digestion in some parts of the intestine. Inhibition of α -glucosidase enzyme activity is a reliable approach to control post-prandial hyperglycemia condition. \u0000Objectives: In this study, a series of Pyrazolo[1,2-b]phthalazine-5,10-dione derivatives 5a–t were synthesized via a multicomponent reaction and evaluated as new inhibitors for α-glucosidase. \u0000Methods: The biological activity of the synthesized compounds was studied using a source of the α-glucosidase enzyme (EC3.2.1.20, Saccharomyces cerevisiae) at 20 U/mg concentration. \u0000Results: Four compounds showed higher α-glucosidase inhibitory activity in comparison to a standard, i.e., Acarbose. Compound 5q displays the most potent α-glucosidase inhibitory activity (IC50 = 155.4 ± 6.0 μM). \u0000Conclusion: In conclusion, some of the synthesized compounds, including heterocyclic core molecules, have shown remarkable activity that could be considered as subjects for the development of new, more efficient inhibitors of the α-glucosidase enzyme.","PeriodicalId":6323,"journal":{"name":"2005 Asian Conference on Sensors and the International Conference on New Techniques in Pharmaceutical and Biomedical Research","volume":"69 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-10-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80370985","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
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