M. Mączyński, A. Regiec, Paulina Płoszaj, Miroslawa Kacaniova, A. Piwowar
Searching for new compounds with specific biological activity in relation to various bacterial strains due to the increasing number of bacterial infections and the frequently developing antimicrobial resistance (AMR) is a significant problem in healthcare. Based on previous promising research related to the activity of isoxazole-4-carbohydrazide derivatives, we currently examined different substituted isoxazole-4-carbohydrazide derivatives in vitro against a panel of bacterial strains. In this work we evaluated antibacterial activity of 30 derivatives, previously described as mildly antimycobacterial, in 10 bacterial strains (5 Gram-negative (G-) and Gram-postive (G+) bacterias). Based on minimum inhibitory concentration (MIC), the mainly MIC50 and MIC90 values, the tested derivatives generally have shown rather weak and mild antibacterial activity. The most active compounds were 3d and 4d, both with methyl substituent in benzene ring. More detailed examination should be continued but this research increased the library of isoxazole derivatives with broad biological activity.
{"title":"EVALUATION OF ANTIBACTERIAL ACTIVITY 5-AMINO-3-METHYLISOXAZOLE-4-CARBOHYDRAZIDE AND \u00005-AMINOISOXAZOLE[5,4-d]PYRIMIDIN-4-ONE DERIVATIVES","authors":"M. Mączyński, A. Regiec, Paulina Płoszaj, Miroslawa Kacaniova, A. Piwowar","doi":"10.32383/appdr/162790","DOIUrl":"https://doi.org/10.32383/appdr/162790","url":null,"abstract":"Searching for new compounds with specific biological activity in relation to various bacterial strains due to the increasing number of bacterial infections and the frequently developing antimicrobial resistance (AMR) is a significant problem in healthcare. Based on previous promising research related to the activity of isoxazole-4-carbohydrazide derivatives, we currently examined different substituted isoxazole-4-carbohydrazide derivatives in vitro against a panel of bacterial strains. In this work we evaluated antibacterial activity of 30 derivatives, previously described as mildly antimycobacterial, in 10 bacterial strains (5 Gram-negative (G-) and Gram-postive (G+) bacterias). Based on minimum inhibitory concentration (MIC), the mainly MIC50 and MIC90 values, the tested derivatives generally have shown rather weak and mild antibacterial activity. The most active compounds were 3d and 4d, both with methyl substituent in benzene ring. More detailed examination should be continued but this research increased the library of isoxazole derivatives with broad biological activity.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42472572","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}
O. Pınarbaşlı, Tolga Ozbay, G. Gurbetoğlu, Nagehan Sarraçoğlu, A. Doganay
The goal of the current study was to develop a precise, sensitive and validated reverse phase HPLC method for determination of fesoterodine fumarate (FST). The current investigation was performed for a stability indicating method in order to obtain both assay and impurity profiles of FST. All the experiment was done on HPLC Shimadzu Prominence 20A having stainless steel ACE5 C18 column with a particle size of 5µm and a dimension of 4.6 mm X 150 mm. The mobile phase was in gradient mode with mobile phase A (0.03M ammonium acetate buffer : acetonitrile : methanol (55:30:15 v/v) pH 3.8) and mobile phase B (water) . The flow rate was 1.2 mL/min and the wavelength 208 nm was selected for detection. This method was validated for linearity and range, accuracy, precision and robustness in accordance with ICH requirements. The retention time of fesoterodine was found as 11.0 min. The main degradation product 5-hydroxymethyltolterodine (5-HMT; active metabolite of FST) and the other process impurities; aldehyde, benzylated hydroxy, tolterodine ester, diester impurities were detected easily at the retention times 3.8, 13.5, 16.7, 21.5, 37.1 minutes, respectively. It was observed that the retention times of the main peak and its impurities were not affected and the selectivity of the method was proved under the applied stress conditions. With this developed method, FST and its impurities can easily be detected. It is also stable, simple, accurate, and completely validated RP-HPLC technique for the analysis of FST and related impurities that meets with ICH standards.
本研究的目的是建立一种精确、灵敏、有效的反相高效液相色谱法测定富马酸非索特罗定(FST)的方法。目前的研究是为了获得FST的测定和杂质谱而进行的稳定性指示方法。所有实验均采用高效液相色谱法(HPLC)进行，柱柱为不锈钢ACE5 C18，粒径为5µm，尺寸为4.6 mm X 150 mm。流动相为梯度模式，流动相为A (0.03M醋酸铵缓冲液:乙腈:甲醇(55:30:15 v/v) pH 3.8)，流动相为B(水)。流速为1.2 mL/min，检测波长为208 nm。该方法的线性度、范围、准确度、精密度和鲁棒性均符合ICH要求。fesoterodine的停留时间为11.0 min。主要降解产物5-羟甲基托特罗定(5-HMT;FST活性代谢物)等工艺杂质;醛、苯基化羟基、托特罗定酯、二酯杂质在保留时间分别为3.8、13.5、16.7、21.5、37.1 min时易检出。结果表明，在施加应力条件下，该方法的选择性不受主峰及其杂质的保留时间的影响。该方法可以很容易地检测到FST及其杂质。该方法是一种稳定、简便、准确、经过完全验证的反相高效液相色谱技术，可用于FST及相关杂质的分析，符合ICH标准。
{"title":"Validated stability-indicating RP-HPLC assay method for fesoterodine fumarate in pharmaceutical products","authors":"O. Pınarbaşlı, Tolga Ozbay, G. Gurbetoğlu, Nagehan Sarraçoğlu, A. Doganay","doi":"10.32383/appdr/163015","DOIUrl":"https://doi.org/10.32383/appdr/163015","url":null,"abstract":"The goal of the current study was to develop a precise, sensitive and validated reverse phase HPLC method for determination of fesoterodine fumarate (FST). The current investigation was performed for a stability indicating method in order to obtain both assay and impurity profiles of FST. All the experiment was done on HPLC Shimadzu Prominence 20A having stainless steel ACE5 C18 column with a particle size of 5µm and a dimension of 4.6 mm X 150 mm. The mobile phase was in gradient mode with mobile phase A (0.03M ammonium acetate buffer : acetonitrile : methanol (55:30:15 v/v) pH 3.8) and mobile phase B (water) . The flow rate was 1.2 mL/min and the wavelength 208 nm was selected for detection. This method was validated for linearity and range, accuracy, precision and robustness in accordance with ICH requirements. The retention time of fesoterodine was found as 11.0 min. The main degradation product 5-hydroxymethyltolterodine (5-HMT; active metabolite of FST) and the other process impurities; aldehyde, benzylated hydroxy, tolterodine ester, diester impurities were detected easily at the retention times 3.8, 13.5, 16.7, 21.5, 37.1 minutes, respectively. It was observed that the retention times of the main peak and its impurities were not affected and the selectivity of the method was proved under the applied stress conditions. With this developed method, FST and its impurities can easily be detected. It is also stable, simple, accurate, and completely validated RP-HPLC technique for the analysis of FST and related impurities that meets with ICH standards.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47432535","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}
Katarzyna Giedzicz, Marcin Dytkowski, Justyna Rentflejsz, M. Świętek, Aleksandra Wojszel, Z. Wojszel
Antiarrhythmic drugs are used more and more often, which is related to the aging of the population and the growing number of arrhythmias, especially atrial fibrillation (AF). One of the drugs used in AF is propafenone, considered a relatively safe drug in people without heart disease. Nevertheless, it can cause severe damage to the liver if one ignores the subtle symptoms that indicate an incipient problem. We present the case of an 82-year-old woman diagnosed with paroxysmal AF who developed acute liver injury during treatment with propafenone. On the fifth day of her hospitalization, we observed nausea and vomiting after introducing regular treatment with propafenone. Similar symptoms occurred before hospitalization when propafenone was taken ad hoc in the event of an AF attack. They were treated as dyspeptics in a patient who underwent cholecystectomy. Laboratory tests showed high serum alanine transaminase, gamma-glutamyltranspeptidase, C-reactive protein, total bilirubin, and a slight increase in aspartate transaminase. Infection with hepatic viruses, alcohol abuse, other drugs toxicity, and intrahepatic cholangitis due to cholelithiasis were excluded as a cause of liver damage. With the discontinuation of propafenone, the patient's clinical condition and laboratory test results improved. Similar cases published in the literature are discussed in the paper. It also draws attention to the need to report adverse drug reactions to the appropriate authorities and discusses the reasons for under-reporting in Poland.
{"title":"Propafenone-induced liver injury in an elderly patient with paroxysmal atrial fibrillation--a new case report and literature review","authors":"Katarzyna Giedzicz, Marcin Dytkowski, Justyna Rentflejsz, M. Świętek, Aleksandra Wojszel, Z. Wojszel","doi":"10.32383/appdr/162793","DOIUrl":"https://doi.org/10.32383/appdr/162793","url":null,"abstract":"Antiarrhythmic drugs are used more and more often, which is related to the aging of the population and the growing number of arrhythmias, especially atrial fibrillation (AF). One of the drugs used in AF is propafenone, considered a relatively safe drug in people without heart disease. Nevertheless, it can cause severe damage to the liver if one ignores the subtle symptoms that indicate an incipient problem. \u0000We present the case of an 82-year-old woman diagnosed with paroxysmal AF who developed acute liver injury during treatment with propafenone. On the fifth day of her hospitalization, we observed nausea and vomiting after introducing regular treatment with propafenone. Similar symptoms occurred before hospitalization when propafenone was taken ad hoc in the event of an AF attack. They were treated as dyspeptics in a patient who underwent cholecystectomy. Laboratory tests showed high serum alanine transaminase, gamma-glutamyltranspeptidase, C-reactive protein, total bilirubin, and a slight increase in aspartate transaminase. Infection with hepatic viruses, alcohol abuse, other drugs toxicity, and intrahepatic cholangitis due to cholelithiasis were excluded as a cause of liver damage. With the discontinuation of propafenone, the patient's clinical condition and laboratory test results improved. Similar cases published in the literature are discussed in the paper. It also draws attention to the need to report adverse drug reactions to the appropriate authorities and discusses the reasons for under-reporting in Poland.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42367557","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}
Photothermal diagnosis and treatment agents are more and more widely studied in cancer diagnosis and treatment. Copper sulfide nanocomposite is an economical and superior semiconductor material in photothermal diagnosis and treatment agents. At present, there are copper sulfide nanocomposites prepared by different materials and methods, and in-depth research has been done in the applications of cancer diagnosis and treatment, antibacterial, and biosensing. This article reviews the preparation of copper sulfide nanocomposites in recent years and their research progress in cancer diagnosis and treatment, and prospects for the future. It could provide a theoretical basis for the application and development of semiconductor materials in the clinical diagnosis and treatment of tumors.
{"title":"Research progress on preparation and anti-tumor application of copper sulfide nanocomposites: A review","authors":"Yuanjiao Feng, Home Miao, Xue Zeng, W. Zhong","doi":"10.32383/appdr/157410","DOIUrl":"https://doi.org/10.32383/appdr/157410","url":null,"abstract":"Photothermal diagnosis and treatment agents are more and more widely studied in cancer diagnosis and treatment. Copper sulfide nanocomposite is an economical and superior semiconductor material in photothermal diagnosis and treatment agents. At present, there are copper sulfide nanocomposites prepared by different materials and methods, and in-depth research has been done in the applications of cancer diagnosis and treatment, antibacterial, and biosensing. This article reviews the preparation of copper sulfide nanocomposites in recent years and their research progress in cancer diagnosis and treatment, and prospects for the future. It could provide a theoretical basis for the application and development of semiconductor materials in the clinical diagnosis and treatment of tumors.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46312990","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}
B. Oyuntsetseg, Khulan Uranchimeg, D. Munkhbat, Khongorzul Tumurkhuyag, Sukhbold Davaa, E. Yadamsuren, A. Natsagdorj, Uranchimeg Erdenebat
We investigated shampoo-related changes in levels of some trace elements in the scalp hair of females and their impact on scalp skin properties. Sixty healthy women divided into control and experimental group who used regular shampoo and Urtica cannabina (U.cannabina) extract shampoo, respectively. Scalp skin was examined using an electronic skin analyzer, and trichometric analysis was performed with a Folliscope. The collected scalp hair samples were digested and measured using inductively coupled plasma-mass spectrometry (ICP-MS). The average copper (p=0.05), zinc (p=0.0002), and iodine (p=0.0004) levels increased notably, whereas the selenium content decreased slightly (p=0.337) in the experimental group. We found that the average iodine content in scalp hair of Mongolian females was three times lower than the global average. The average increase in trace elements may be considered to be due to the transfer of an element into the human scalp during shampooing. These results indicate that some trace elements in human scalp hair are not only associated with nutritional status and environmental factors, but cosmetic products can also affect the trace element composition. The hair growth, diameter, and density gradually increased and were higher in the experimental group than in the control group. Scalp skin moisture, sebum, and pH values increased in the experimental group, whereas the control group showed no notable difference. Herbal extracts may potentially support scalp hair growth and increase the hair density. This ability can be explained by the trace elements in the herbal extract, which may play a key role in inducing hair growth.
{"title":"The change of copper, zinc, iodine, and selenium contents in the scalp hair of healthy females and the efficacy of herbal extract shampoo treatment","authors":"B. Oyuntsetseg, Khulan Uranchimeg, D. Munkhbat, Khongorzul Tumurkhuyag, Sukhbold Davaa, E. Yadamsuren, A. Natsagdorj, Uranchimeg Erdenebat","doi":"10.32383/appdr/161275","DOIUrl":"https://doi.org/10.32383/appdr/161275","url":null,"abstract":"We investigated shampoo-related changes in levels of some trace elements in the scalp hair of females and their impact on scalp skin properties. Sixty healthy women divided into control and experimental group who used regular shampoo and Urtica cannabina (U.cannabina) extract shampoo, respectively. Scalp skin was examined using an electronic skin analyzer, and trichometric analysis was performed with a Folliscope. The collected scalp hair samples were digested and measured using inductively coupled plasma-mass spectrometry (ICP-MS). The average copper (p=0.05), zinc (p=0.0002), and iodine (p=0.0004) levels increased notably, whereas the selenium content decreased slightly (p=0.337) in the experimental group. We found that the average iodine content in scalp hair of Mongolian females was three times lower than the global average. The average increase in trace elements may be considered to be due to the transfer of an element into the human scalp during shampooing. These results indicate that some trace elements in human scalp hair are not only associated with nutritional status and environmental factors, but cosmetic products can also affect the trace element composition. The hair growth, diameter, and density gradually increased and were higher in the experimental group than in the control group. Scalp skin moisture, sebum, and pH values increased in the experimental group, whereas the control group showed no notable difference. Herbal extracts may potentially support scalp hair growth and increase the hair density. This ability can be explained by the trace elements in the herbal extract, which may play a key role in inducing hair growth.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47622324","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}
Abstract: Production of preparations based on natural ingredients has become a priority in the cosmetic and pharmaceutical industries. The novelty of the study was to present a possible method for obtaining pure diacylglycerols (DAG) from natural raw materials like fats (hemp seed oil and mutton tallow). We have determined the optimum water content for enzymatic interesterification to shift the reaction equilibrium towards hydrolysis and obtain the highest DAG formation yield. Then, DAG were separated and purified by column chromatography. Raw fats were characterized by fatty acids composition and their positional distribution using gas chromatography. Triacylglycerols, diacylglycerols, monoacylglycerols and free fatty acid contents were determined using gel permeation chromatography. The main fatty acids found in sn-2 MAG of hemp seed oil was linoleic acid, which was followed by oleic acid. Saturated fatty acids in hemp seed oil’s TAG showed preference for the outer sn-1,3 positions. For mutton tallow, the majority of oleic acid were found at sn-2 position. The optimum water content applied during enzymatic interesterification for DAG formation was estimated to be 2.0 % w/w, using the following conditions: 5 % w/w of catalyst, 200 rpm, 60 °C, 6h. DAG yield was 27 %. Purification of the mutton tallow-based and hemp seed oil-based DAG yielded with 83 % w/w and 82 % w/w, respectively. High purity DAG could be applied as effective emulsifiers in food, cosmetic or pharmaceutical emulsions.
{"title":"Enzymatic synthesis and purification of diacylglycerols from mutton tallow and hemp seed oil","authors":"M. Kowalska, M. Woźniak, S. Tavernier","doi":"10.32383/appdr/157008","DOIUrl":"https://doi.org/10.32383/appdr/157008","url":null,"abstract":"Abstract: Production of preparations based on natural ingredients has become a priority in the cosmetic and pharmaceutical industries. The novelty of the study was to present a possible method for obtaining pure diacylglycerols (DAG) from natural raw materials like fats (hemp seed oil and mutton tallow). We have determined the optimum water content for enzymatic interesterification to shift the reaction equilibrium towards hydrolysis and obtain the highest DAG formation yield. Then, DAG were separated and purified by column chromatography. Raw fats were characterized by fatty acids composition and their positional distribution using gas chromatography. Triacylglycerols, diacylglycerols, monoacylglycerols and free fatty acid contents were determined using gel permeation chromatography. The main fatty acids found in sn-2 MAG of hemp seed oil was linoleic acid, which was followed by oleic acid. Saturated fatty acids in hemp seed oil’s TAG showed preference for the outer sn-1,3 positions. For mutton tallow, the majority of oleic acid were found at sn-2 position.\u0000The optimum water content applied during enzymatic interesterification for DAG formation was estimated to be 2.0 % w/w, using the following conditions: 5 % w/w of catalyst, 200 rpm, 60 °C, 6h. DAG yield was 27 %. Purification of the mutton tallow-based and hemp seed oil-based DAG yielded with 83 % w/w and 82 % w/w, respectively. High purity DAG could be applied as effective emulsifiers in food, cosmetic or pharmaceutical emulsions.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"69582400","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}
L. Hassouneh, Salameh Aldajah, M. Najdawi, Z. Abudayeh, Qais Abualassal, Amajad aburmelah, Alaa Sirhan
Old-age-associated pathologies usually coincide with altered sphingolipid metabolism. Changes in the level of sphingomyelin (SM) and ceramide are largely determined by the activation of neutral sphingomyelinase (nSMase) during aging. nSMase is a key enzyme in sphingolipid turnover; it generates ceramide through the hydrolysis of SM. While N—acetylcysteine (NAC) is a powerful antioxidant which has anti-inflammatory properties and it is the precursor of glutathione (GSH). The aim of this study is to determine the impact of NAC on nSMase activity in the age-dependent changes of sphingolipid (SM and ceramide) levels and GSH content in blood serum, gastrocnemius muscle and kidney tissue of 24-month-old rats. It was found that the effect of NAC on the tissue of 24-month-old rats increased SM content; GSH content and decreased the ceramide content. The gastrocnemius muscle and kidney were the most sensitive to the effects of NAC. The results show that GSH inhibit the activity of nSMase. These results emphasize that nSMase. plays a key role in age-associated ceramide accumulation in rat tissues during aging. Furthermore, it was indicated that NAC is an effective modulator of nSMase and has pleiotropic effects that may alter sphingolipid metabolism. The nSMase inhibition enhances the benefits of NAC treatment.
{"title":"Acetylcysteine modulates sphingolipid levels by inhibiting neutral sphingomyelinase during aging in rat tissues","authors":"L. Hassouneh, Salameh Aldajah, M. Najdawi, Z. Abudayeh, Qais Abualassal, Amajad aburmelah, Alaa Sirhan","doi":"10.32383/appdr/162546","DOIUrl":"https://doi.org/10.32383/appdr/162546","url":null,"abstract":"Old-age-associated pathologies usually coincide with altered sphingolipid metabolism. Changes in the level of sphingomyelin (SM) and ceramide are largely determined by the activation of neutral sphingomyelinase (nSMase) during aging. nSMase is a key enzyme in sphingolipid turnover; it generates ceramide through the hydrolysis of SM. While N—acetylcysteine (NAC) is a powerful antioxidant which has anti-inflammatory properties and it is the precursor of glutathione (GSH). The aim of this study is to determine the impact of NAC on nSMase activity in the age-dependent changes of sphingolipid (SM and ceramide) levels and GSH content in blood serum, gastrocnemius muscle and kidney tissue of 24-month-old rats. It was found that the effect of NAC on the tissue of 24-month-old rats increased SM content; GSH content and decreased the ceramide content. The gastrocnemius muscle and kidney were the most sensitive to the effects of NAC. The results show that GSH inhibit the activity of nSMase. These results emphasize that nSMase. plays a key role in age-associated ceramide accumulation in rat tissues during aging. Furthermore, it was indicated that NAC is an effective modulator of nSMase and has pleiotropic effects that may alter sphingolipid metabolism. The nSMase inhibition enhances the benefits of NAC treatment.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41286302","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}
Tataringa Gabriela, Tuchilus Cristina, Zbancioc ANA MARIA
Phenols represent an important class of compounds that present high antimicrobial potential. The seventeen selected phenols were tested in vitro for their antimicrobial activity showing different activity to S. aureus ATCC 25923, E. coli ATCC 25922, P. aeruginosa ATCC 27853 and C. albicans ATCC 90028. Most of the phenolic compounds have a good efficacy on S. aureus and C. albicans. 2- and 4-aminophenol have been found to be the most potent antimicrobial agents against S. aureus, with MIC values 0.170 mg/mL and 0.340 mg/mL, respectively. The frontier orbital energy and the global reactivity descriptors (calculated using Spartan 16 software) were discussed for the selected phenols; results revealed that the theoretical calculations of antimicrobial activity were related to the quantum chemical parameters.
{"title":"Antimicrobial prospection and density functional study of some phenolic compounds","authors":"Tataringa Gabriela, Tuchilus Cristina, Zbancioc ANA MARIA","doi":"10.32383/appdr/162792","DOIUrl":"https://doi.org/10.32383/appdr/162792","url":null,"abstract":"Phenols represent an important class of compounds that present high antimicrobial potential. The seventeen selected phenols were tested in vitro for their antimicrobial activity showing different activity to S. aureus ATCC 25923, E. coli ATCC 25922, P. aeruginosa ATCC 27853 and C. albicans ATCC 90028. Most of the phenolic compounds have a good efficacy on S. aureus and C. albicans. 2- and 4-aminophenol have been found to be the most potent antimicrobial agents against S. aureus, with MIC values 0.170 mg/mL and 0.340 mg/mL, respectively. The frontier orbital energy and the global reactivity descriptors (calculated using Spartan 16 software) were discussed for the selected phenols; results revealed that the theoretical calculations of antimicrobial activity were related to the quantum chemical parameters.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43332709","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}
Purpose: To investigate the in vitro skin permeation and transdermal behavior of diclofenac sodium using a new system of microemulsion. Methods: Diclofenac sodium was incorporated into oil-in-water (o/w) and water-in-oil (w/o) microemulsions consisting of a 2:1 ratio of Cremophor RH 40: Span 80 as surfactant phase, ethylhexyl palmitate as oil phase, and a 2:1 ratio of water: isopropanol as aqueous phase. Franz diffusion cell was used to determine the in vitro skin permeation. Morphology of microemulsions were characterized by transmission electron microscopy (TEM). The depth of penetration distribution was visualized by fluorescently labelling, and observing using confocal laser scanning microscopy (CLSM). Results: The o/w type provided an enhanced permeation flux, with more than a 3- fold increase in permeability coefficient across skin as compared with w/o type. The morphology characterization indicated that both o/w and w/o type were nano-sized and spherical in shape. It was observed by CLSM that o/w type significantly facilitated the penetration of sulforhodamine B (SRB) to the deeper layers of the skin (220 μm) than w/o type (150 μm). Conclusion: This study demonstrates that diclofenac sodium microemulsion can be transdermal, and the skin penetration depends on the microstructure and composition of microemulsion.
{"title":"Investigation of transdermal permeation behavior of diclofenac sodium microemulsion by confocal laser scanning microscopy","authors":"Hui Yang, P. Boonme, T. Amnuaikit","doi":"10.32383/appdr/162214","DOIUrl":"https://doi.org/10.32383/appdr/162214","url":null,"abstract":"Purpose: To investigate the in vitro skin permeation and transdermal behavior of diclofenac sodium using a new system of microemulsion. \u0000Methods: Diclofenac sodium was incorporated into oil-in-water (o/w) and water-in-oil (w/o) microemulsions consisting of a 2:1 ratio of Cremophor RH 40: Span 80 as surfactant phase, ethylhexyl palmitate as oil phase, and a 2:1 ratio of water: isopropanol as aqueous phase. Franz diffusion cell was used to determine the in vitro skin permeation. Morphology of microemulsions were characterized by transmission electron microscopy (TEM). The depth of penetration distribution was visualized by fluorescently labelling, and observing using confocal laser scanning microscopy (CLSM). \u0000Results: The o/w type provided an enhanced permeation flux, with more than a 3- fold increase in permeability coefficient across skin as compared with w/o type. The morphology characterization indicated that both o/w and w/o type were nano-sized and spherical in shape. It was observed by CLSM that o/w type significantly facilitated the penetration of sulforhodamine B (SRB) to the deeper layers of the skin (220 μm) than w/o type (150 μm). \u0000Conclusion: This study demonstrates that diclofenac sodium microemulsion can be transdermal, and the skin penetration depends on the microstructure and composition of microemulsion.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47189488","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}
A. Zakrzeska, P. Kitlas, A. Shlyahtun, Ryszard Jabłoński, M. Tomulewicz, Natalia Szymańska
The purpose of this study was to show the preventive properties of the botulin (Bet) and its combination with cyclodextrin in a model of neurodegenerative disease like Alzheimer's disease (AD) in rats. Betulin was obtained from birch bark using standard methodology. The AD model was induced by administering aluminum chloride AlCl3 (200 mg/kg/day) to animals for 120 days. All animals were divided into 4 groups: the control group (sham operation), the second - the AD model (Alz) without prevention with betulin, the third - the Alz+Bet receiving betulin (100 mg/kg/day, i.g., during the last 50% of the experimental days), and the Alz+Bet Complex receiving betulin in complex with cyclodextrin (100 mg/kg/day, i.g., during the last 50% of the experimental days). We showed that betulin in complex with cyclodextrin improve the spatial memory and lowered levels of the TNF-α, APLP2 and β-amyloid in rats with AlCl3-induced AD. We conclude that betulin has neuroprotective properties which may form the basis for the development of a new pharmaceutical that is effective in both the prevention and treatment of Alzheimer's disease.
{"title":"Protective effect of betulin against aluminium-induced Alzheimer-like neurodegeneration","authors":"A. Zakrzeska, P. Kitlas, A. Shlyahtun, Ryszard Jabłoński, M. Tomulewicz, Natalia Szymańska","doi":"10.32383/appdr/161588","DOIUrl":"https://doi.org/10.32383/appdr/161588","url":null,"abstract":"The purpose of this study was to show the preventive properties of the botulin (Bet) and its combination with cyclodextrin in a model of neurodegenerative disease like Alzheimer's disease (AD) in rats. Betulin was obtained from birch bark using standard methodology. The AD model was induced by administering aluminum chloride AlCl3 (200 mg/kg/day) to animals for 120 days. All animals were divided into 4 groups: the control group (sham operation), the second - the AD model (Alz) without prevention with betulin, the third - the Alz+Bet receiving betulin (100 mg/kg/day, i.g., during the last 50% of the experimental days), and the Alz+Bet Complex receiving betulin in complex with cyclodextrin (100 mg/kg/day, i.g., during the last 50% of the experimental days). We showed that betulin in complex with cyclodextrin improve the spatial memory and lowered levels of the TNF-α, APLP2 and β-amyloid in rats with AlCl3-induced AD. We conclude that betulin has neuroprotective properties which may form the basis for the development of a new pharmaceutical that is effective in both the prevention and treatment of Alzheimer's disease.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-04-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44087892","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}
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