VIKTORIIA PROPISNOVA, TETIANA ZHULAI, Edmund Grześkowiak, Danuta Szkutnik-Fiedler
Sore throat is a common symptom that accompanies infectious and non-infectious diseases. World standards of sore throat treatment mainly regulate approaches to the diagnosis of the streptococcal nature of sore throat and the use of antibacterial therapy in a positive case. However, the predominant cause of sore throat is viruses and symptomatic treatment can be used. The study presents a brief overview of modern medical standards for sore throat, defining the role of a pharmacist and the experience of certain countries in involving him in the diagnosing and treating process. An analysis of the content of the Ukrainian Pharmacist’s protocol “Symptomatic treatment of sore throat” and the dynamics of its changes was carried out. Pharmacist’s Protocol elaborated in Ukraine successfully combines the algorithm of the primary pre-medical assessment of the patient’s condition with information and advisory support when dispensing over-the-counter medicines for responsible self-treatment of sore throat. However, certain improvements in the list of recommended medicines may be appropriate.
{"title":"Sore throat: diagnosis and treatment world standards and approaches to pharmaceutical care in Ukraine","authors":"VIKTORIIA PROPISNOVA, TETIANA ZHULAI, Edmund Grześkowiak, Danuta Szkutnik-Fiedler","doi":"10.32383/appdr/170318","DOIUrl":"https://doi.org/10.32383/appdr/170318","url":null,"abstract":"Sore throat is a common symptom that accompanies infectious and non-infectious diseases. World standards of sore throat treatment mainly regulate approaches to the diagnosis of the streptococcal nature of sore throat and the use of antibacterial therapy in a positive case. However, the predominant cause of sore throat is viruses and symptomatic treatment can be used. The study presents a brief overview of modern medical standards for sore throat, defining the role of a pharmacist and the experience of certain countries in involving him in the diagnosing and treating process. An analysis of the content of the Ukrainian Pharmacist’s protocol “Symptomatic treatment of sore throat” and the dynamics of its changes was carried out. Pharmacist’s Protocol elaborated in Ukraine successfully combines the algorithm of the primary pre-medical assessment of the patient’s condition with information and advisory support when dispensing over-the-counter medicines for responsible self-treatment of sore throat. However, certain improvements in the list of recommended medicines may be appropriate.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135366742","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}
MAGED Almezgagi, MUHAMMAD SHOAIB TAHER, YU ZHANG, Mohammed Gamah, Xiang Gao, QINFANG ZHU, HUAN ZHANG, WEI ZHANG
Ulcerative colitis (UC) is a prevalent disorder characterized by oxidative stress and the release of pro-inflammatory cytokines that disturb the colonic mucosa. Currently, available medicines for UC remain unsatisfactory. Diacerein (DIAC) has exhibited anti-oxidant and anti-inflammatory properties in wide inflammatory disorders. However, the limited understanding of DIAC's role in bowel inflammation has necessitated the investigation of its efficacy in dextran sodium sulfate (DSS)-induced UC in Balb/c mice in this study. Fifty mice were equally divided into five groups. Except for the control, all groups were given DSS for seven days to induce the colitis model. The model was treated with 25 and 50mg/kg/day of DIAC and 00mg/kg/day of 5-aminosalicylic acid (5-ASA) for ten days. Several clinical, molecular and biochemical parameters were evaluated. Following the exposure to DSS, there was a significant upregulation in the pro-inflammatory cytokines (IL-1β, IL-6, IL-17 and TNF-α) and oxidative stress index (MDA). Meanwhile, the concentration of anti-oxidative stress indices (SOD, GPx and CAT) and the levels of IL-10, mucin-1 and 2 and tight junction proteins (TJs) ZO-1 and occludin were markedly suppressed. The colon length and body weight were reduced while DAI and myeloperoxidase (MPO) were elevated. Conversely, DIAC 50mg and 5-ASA significantly reversed the altered pro-inflammatory cytokines, oxidative stress and MPO. Moreover, they significantly restored body weight, colon length, DAI, TJs, mucin-1 and 2 and IL-10. No significant results were found with DIAC 25mg. In conclusion, DIAC exhibited therapeutic effectiveness against colitis. This research may provide hope for testing its effectiveness against UC in humans
{"title":"Evaluation of Diacerein Efficacy on Colitis as Anti-inflammatory and Anti-oxidant and its Role in Enhancing of Colon Barrier in Mice","authors":"MAGED Almezgagi, MUHAMMAD SHOAIB TAHER, YU ZHANG, Mohammed Gamah, Xiang Gao, QINFANG ZHU, HUAN ZHANG, WEI ZHANG","doi":"10.32383/appdr/169261","DOIUrl":"https://doi.org/10.32383/appdr/169261","url":null,"abstract":"Ulcerative colitis (UC) is a prevalent disorder characterized by oxidative stress and the release of pro-inflammatory cytokines that disturb the colonic mucosa. Currently, available medicines for UC remain unsatisfactory. Diacerein (DIAC) has exhibited anti-oxidant and anti-inflammatory properties in wide inflammatory disorders. However, the limited understanding of DIAC's role in bowel inflammation has necessitated the investigation of its efficacy in dextran sodium sulfate (DSS)-induced UC in Balb/c mice in this study. Fifty mice were equally divided into five groups. Except for the control, all groups were given DSS for seven days to induce the colitis model. The model was treated with 25 and 50mg/kg/day of DIAC and 00mg/kg/day of 5-aminosalicylic acid (5-ASA) for ten days. Several clinical, molecular and biochemical parameters were evaluated. Following the exposure to DSS, there was a significant upregulation in the pro-inflammatory cytokines (IL-1β, IL-6, IL-17 and TNF-α) and oxidative stress index (MDA). Meanwhile, the concentration of anti-oxidative stress indices (SOD, GPx and CAT) and the levels of IL-10, mucin-1 and 2 and tight junction proteins (TJs) ZO-1 and occludin were markedly suppressed. The colon length and body weight were reduced while DAI and myeloperoxidase (MPO) were elevated. Conversely, DIAC 50mg and 5-ASA significantly reversed the altered pro-inflammatory cytokines, oxidative stress and MPO. Moreover, they significantly restored body weight, colon length, DAI, TJs, mucin-1 and 2 and IL-10. No significant results were found with DIAC 25mg. In conclusion, DIAC exhibited therapeutic effectiveness against colitis. This research may provide hope for testing its effectiveness against UC in humans","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135412008","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}
Małgorzata Bekier, Aleksandra Uruska, Danuta Szkutnik-Fiedler
There is a rising trend of overweight and obesity among individuals with type 1 diabetes. This is often associated with decreased insulin sensitivity, increased insulin dose requirements and poor glycemic control. Insulin resistance is a state of diminished effect of insulin on target tissues, despite normal or elevated serum insulin levels. Metformin as an adjunct to insulin in treating overweight or also not specific image of insulin resistance (without overweight or hormonal disorders) adults with type 1 diabetes is increasingly used. The main goal of this off-label type 1 diabetes treatment method is to improve insulin signaling leading to a subsequent increase in glucose uptake by skeletal myocytes, inhibition of hepatic gluconeogenesis and, as a result, a reduction in the need for a daily dose of insulin. The use of metformin as an addition to insulin may increase the chance of achieving target glucose control and reduce the anabolic effect of this hormone. Metformin can improve insulin sensitivity, glycemia and modulate cardiovascular disease risk factors or nonalcoholic fatty liver disease. In the vast majority of clinical trials conducted with metformin in type 1 diabetes, the effect of the drug on daily insulin doses, improvement in lipid parameters, and decline in body fat was assessed without correlating pre-specified outcomes with drug plasma concentrations.
{"title":"Insulin resistance and iatrogenic hyperinsulinemia in type 1 diabetes - norm or complication? Role of metformin in type 1 diabetes mellitus","authors":"Małgorzata Bekier, Aleksandra Uruska, Danuta Szkutnik-Fiedler","doi":"10.32383/appdr/171429","DOIUrl":"https://doi.org/10.32383/appdr/171429","url":null,"abstract":"There is a rising trend of overweight and obesity among individuals with type 1 diabetes. This is often associated with decreased insulin sensitivity, increased insulin dose requirements and poor glycemic control. Insulin resistance is a state of diminished effect of insulin on target tissues, despite normal or elevated serum insulin levels. Metformin as an adjunct to insulin in treating overweight or also not specific image of insulin resistance (without overweight or hormonal disorders) adults with type 1 diabetes is increasingly used. The main goal of this off-label type 1 diabetes treatment method is to improve insulin signaling leading to a subsequent increase in glucose uptake by skeletal myocytes, inhibition of hepatic gluconeogenesis and, as a result, a reduction in the need for a daily dose of insulin. The use of metformin as an addition to insulin may increase the chance of achieving target glucose control and reduce the anabolic effect of this hormone. Metformin can improve insulin sensitivity, glycemia and modulate cardiovascular disease risk factors or nonalcoholic fatty liver disease. In the vast majority of clinical trials conducted with metformin in type 1 diabetes, the effect of the drug on daily insulin doses, improvement in lipid parameters, and decline in body fat was assessed without correlating pre-specified outcomes with drug plasma concentrations.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135366744","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}
Controlling blood glucose is the primary therapeutic strategy for T2DM. Both saxagliptin and andrographolide possess hypoglycemic effects, which makes the combination easy. This study aimed to evaluate the co-administration of saxagliptin and andrographolide in rats and revealed their combined impact on type 2 diabetes (T2DM). T2DM rat models were established by high-fat diet and the injection of nicotinamide and streptozotocin. The blood glucose and insulin resistance index were monitored after modeling. The pharmacokinetics of saxagliptin was assessed by orally administrating 10 mg/kg saxagliptin. The co-administration was performed with the pre-treatment of 30 or 100 mg/kg andrographolide. In vitro, the metabolic stability of saxagliptin was assessed in rat liver microsomes. The co-administration of saxagliptin with andrographolide induced significant changes in the pharmacokinetics of saxagliptin, behaving as the increasing AUC(0-t), Cmax, t1/2, and the decreasing clearance rate. The effect of andrographolide was enhanced with the growing concentration. Combination with andrographolide enhanced the hypoglycemic effect and alleviated insulin resistance of saxagliptin in T2DM rats. Co-administration of saxagliptin with 100 mg/kg andrographolide induced hypoglycemia. In vitro, andrographolide significantly improved the metabolic stability of saxagliptin and showed a significant inhibitory effect on the activity of CYP3A4. Combining saxagliptin with andrographolide could increase the systemic exposure of saxagliptin via inhibiting CYP3A4 and improve the hypoglycemic effect, but the high concentration of andrographolide is the risk of inducing hypoglycemia.
{"title":"Pharmacokinetic interaction of saxagliptin with andrographolide and their hypoglycemic effect in type 2 diabetes rats","authors":"Suyan Wu, Haifei Pan, Yingying Huang","doi":"10.32383/appdr/170911","DOIUrl":"https://doi.org/10.32383/appdr/170911","url":null,"abstract":"Controlling blood glucose is the primary therapeutic strategy for T2DM. Both saxagliptin and andrographolide possess hypoglycemic effects, which makes the combination easy. This study aimed to evaluate the co-administration of saxagliptin and andrographolide in rats and revealed their combined impact on type 2 diabetes (T2DM). T2DM rat models were established by high-fat diet and the injection of nicotinamide and streptozotocin. The blood glucose and insulin resistance index were monitored after modeling. The pharmacokinetics of saxagliptin was assessed by orally administrating 10 mg/kg saxagliptin. The co-administration was performed with the pre-treatment of 30 or 100 mg/kg andrographolide. In vitro, the metabolic stability of saxagliptin was assessed in rat liver microsomes. The co-administration of saxagliptin with andrographolide induced significant changes in the pharmacokinetics of saxagliptin, behaving as the increasing AUC(0-t), Cmax, t1/2, and the decreasing clearance rate. The effect of andrographolide was enhanced with the growing concentration. Combination with andrographolide enhanced the hypoglycemic effect and alleviated insulin resistance of saxagliptin in T2DM rats. Co-administration of saxagliptin with 100 mg/kg andrographolide induced hypoglycemia. In vitro, andrographolide significantly improved the metabolic stability of saxagliptin and showed a significant inhibitory effect on the activity of CYP3A4. Combining saxagliptin with andrographolide could increase the systemic exposure of saxagliptin via inhibiting CYP3A4 and improve the hypoglycemic effect, but the high concentration of andrographolide is the risk of inducing hypoglycemia.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135412827","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}
Monika Kompała, Julia Kuc, Zbigniew Skotnicki, Agata Jasińska-Balwierz, Nataliia Hudz, Radosław Jerzy Balwierz, Jacek Lipok
An alcohol hangover is a complex set of adverse symptoms that occur after excessive consumption of alcoholic beverages. Hangovers are not solely caused by ethanol, but mainly by its toxic metabolites, such as acetaldehyde and acetic acid. Most of the negative symptoms occur when the concentration of alcohol in the blood decreases after drinking. Given that a large percentage of people consume alcohol and experience negative effects from its consumption, potential supplementation to help eliminate these adverse effects has been proposed. One promising ingredient is ginseng, which has been used in Eastern culture and traditional Chinese medicine for over 2,000 years. The aim of this study was to present the potential of Panax ginseng C.A. Mey. as an aid for the adverse effects of alcohol consumption and its protective effect on liver function. The literature analysis was based on data indexed in medical databases PubMed, Scopus, and Medline since 2010, using keywords such as "Panax ginseng," "hangover," "alcohol consumption," and "metabolism," connected by the logical conjuction “and.” The analysis confirmed the effectiveness of P. ginseng in the treatment and prevention of hangovers. Preparations containing P. ginseng can support ethanol metabolism by inducing enzymes such as alcohol dehydrogenase, aldehyde dehydrogenase, and the cytochrome P450 isoform 2E1 system. An additional advantage of using P. ginseng may be its hepatoprotective effect.
{"title":"Panax ginseng C.A. Mey. as a potential raw material in the treatment of negative effects of alcohol consumption","authors":"Monika Kompała, Julia Kuc, Zbigniew Skotnicki, Agata Jasińska-Balwierz, Nataliia Hudz, Radosław Jerzy Balwierz, Jacek Lipok","doi":"10.32383/appdr/170201","DOIUrl":"https://doi.org/10.32383/appdr/170201","url":null,"abstract":"An alcohol hangover is a complex set of adverse symptoms that occur after excessive consumption of alcoholic beverages. Hangovers are not solely caused by ethanol, but mainly by its toxic metabolites, such as acetaldehyde and acetic acid. Most of the negative symptoms occur when the concentration of alcohol in the blood decreases after drinking. Given that a large percentage of people consume alcohol and experience negative effects from its consumption, potential supplementation to help eliminate these adverse effects has been proposed. One promising ingredient is ginseng, which has been used in Eastern culture and traditional Chinese medicine for over 2,000 years. The aim of this study was to present the potential of Panax ginseng C.A. Mey. as an aid for the adverse effects of alcohol consumption and its protective effect on liver function. The literature analysis was based on data indexed in medical databases PubMed, Scopus, and Medline since 2010, using keywords such as \"Panax ginseng,\" \"hangover,\" \"alcohol consumption,\" and \"metabolism,\" connected by the logical conjuction “and.” The analysis confirmed the effectiveness of P. ginseng in the treatment and prevention of hangovers. Preparations containing P. ginseng can support ethanol metabolism by inducing enzymes such as alcohol dehydrogenase, aldehyde dehydrogenase, and the cytochrome P450 isoform 2E1 system. An additional advantage of using P. ginseng may be its hepatoprotective effect.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136038653","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}
Ewelina Szalek, Boguslawa Musial, Kamila Czarnecka, Paweł Szymański
Vilanterol (VT) and fluticasone furoate (FF) are components recently used in dry powder inhaler (DPI) to be administrated for patients with respiratory diseases, such as asthma or chronic obstructive pulmonary disease (COPD). In the present study, an approach to an analytical procedure development and validation is presented. Next generation impactor (NGI) and high performance liquid chromatography (HPLC) with UV detector were applied to determine two compounds and fine particle dose (FPD) of each active ingredients in DPI. The most satisfying chromatographic separation was obtained on Poroshell SB C18 (100 mm × 4.6 mm, 2.7 µm) column applying gradient elution by phosphonate buffer and acetonitrile. VT and FF were detected on a UV detector at wavelength of 210 nm and 245 nm, respectively. Among various coating agents, 4% polyethylene glycol PEG 200 in acetone (w/v) was selected as the most effective. Although various physicochemical properties of VT and FF, the analytical procedure allows simultaneously determine two compounds at different wavelengths. Limit of quantitative (LOQ) of vilanterol and fluticasone furoate were determined as 0.049 µg/ml and 0.032 µg/ml, respectively, what is desirable to determine of FPD of active ingredients in microdoses in DPI. The analytical procedure was determined as linear and accurate in the range of LOQ – 2.5 µg/ml and LOQ – 10.0 µg/ml of VT and FF, respectively. The coefficient of determination (R2) was found to be 0.9999 and 1.000 for VT and FF, respectively.
维兰特罗(VT)和糠酸氟替卡松(FF)是最近在干粉吸入器(DPI)中使用的成分，用于哮喘或慢性阻塞性肺疾病(COPD)等呼吸系统疾病患者。在本研究中，提出了一种分析程序开发和验证的方法。采用新一代冲击器(NGI)和高效液相色谱法(HPLC)结合紫外检测器测定了DPI中两种化合物和各有效成分的细颗粒剂量(FPD)。在Poroshell SB C18 (100 mm × 4.6 mm, 2.7µm)柱上，采用磷酸盐缓冲液和乙腈梯度洗脱，获得了最满意的色谱分离效果。VT和FF分别在波长为210 nm和245 nm的紫外检测器上检测。在各种涂层剂中，选择4%聚乙二醇PEG 200在丙酮(w/v)中的效果最好。虽然VT和FF的物理化学性质各不相同，但分析过程允许在不同波长同时测定两种化合物。维兰特罗和糠酸氟替卡松的定量限分别为0.049µg/ml和0.032µg/ml，符合DPI中微量剂量有效成分FPD的测定要求。VT和FF的LOQ分别为- 2.5µg/ml和- 10.0µg/ml，分析方法线性准确。VT和FF的决定系数R2分别为0.9999和1.000。
{"title":"Simultaneously determination of fine particle dose of vilanterol and fluticasone furoate for dry powder inhaler (DPI) by utilizing gradient elution in chromatography system","authors":"Ewelina Szalek, Boguslawa Musial, Kamila Czarnecka, Paweł Szymański","doi":"10.32383/appdr/170317","DOIUrl":"https://doi.org/10.32383/appdr/170317","url":null,"abstract":"Vilanterol (VT) and fluticasone furoate (FF) are components recently used in dry powder inhaler (DPI) to be administrated for patients with respiratory diseases, such as asthma or chronic obstructive pulmonary disease (COPD). In the present study, an approach to an analytical procedure development and validation is presented. Next generation impactor (NGI) and high performance liquid chromatography (HPLC) with UV detector were applied to determine two compounds and fine particle dose (FPD) of each active ingredients in DPI. The most satisfying chromatographic separation was obtained on Poroshell SB C18 (100 mm × 4.6 mm, 2.7 µm) column applying gradient elution by phosphonate buffer and acetonitrile. VT and FF were detected on a UV detector at wavelength of 210 nm and 245 nm, respectively. Among various coating agents, 4% polyethylene glycol PEG 200 in acetone (w/v) was selected as the most effective. Although various physicochemical properties of VT and FF, the analytical procedure allows simultaneously determine two compounds at different wavelengths. Limit of quantitative (LOQ) of vilanterol and fluticasone furoate were determined as 0.049 µg/ml and 0.032 µg/ml, respectively, what is desirable to determine of FPD of active ingredients in microdoses in DPI. The analytical procedure was determined as linear and accurate in the range of LOQ – 2.5 µg/ml and LOQ – 10.0 µg/ml of VT and FF, respectively. The coefficient of determination (R2) was found to be 0.9999 and 1.000 for VT and FF, respectively.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136038837","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 Aim: Recent studies demonstrate that individuals with T2DM more likely to develop AD. While, disturbed glucose or insulin homeostasis, are at the forefront of AD research, not much is known about extra- and intracellular interplay between different forms of Aβ and microenviromental fluctuations of glucose or insulin concentrations in neuronal cells. Methods: We create conditions imitating the coexistence of T2DM with AD and compare the results with state where the neuropathological changes are yet not developed. We have investigated the effect of the physiological (Aβ40) and toxic amyloid form (Aβ25–35) and its co-incubation with glucose or insulin on neuronal proliferation, H2O2, Aβ42, S100B, S100A8 protein concentrations, mature neuronal protrusions and neurogenesis. Results: Aβ40 and Aβ25-35 with hyperglycaemia provoked stronger cytotoxic effect comparing to Aβ alone, while hyperinsulinemia dampen this effect. Opposite results were obtained in H2O2 measurement. Insulin stimulated Aβ42 generation when co-incubated with both Aβ forms. Aβ40 and Aβ25-35 caused similar pattern of extracellular S100B protein influx an concomitant cytosolic efflux. Neuronal protrusions and neurogenesis were initiated by co-incubation of Aβ40 with hyperglycaemia while reduced in Aβ25-35 and hyperglycemia or insulinemia. Significance: Our finding suggest that for understanding the biochemical origins of neuropathological amyloid β progression and potential involvement of metabolic disturbances in this process, it’s crucial to gasp preliminary interactions on cellular level. Our data can lead to hypothesis that S100B protein could be a potential modulator as well as indicator of prodromal neuropathological alterations.
{"title":"Comparison of physiological state and conditions imitating the comorbidity of type 2 diabetes with Alzheimer's disease. The impact on: proliferation, H2O2, Aβ42, S100A8, S100B levels, neuronal protrusion and neurogenesis","authors":"Adriana Kubis-Kubiak, Benita Wiatrak, Agnieszka Piwowar","doi":"10.32383/appdr/171296","DOIUrl":"https://doi.org/10.32383/appdr/171296","url":null,"abstract":"Abstract Aim: Recent studies demonstrate that individuals with T2DM more likely to develop AD. While, disturbed glucose or insulin homeostasis, are at the forefront of AD research, not much is known about extra- and intracellular interplay between different forms of Aβ and microenviromental fluctuations of glucose or insulin concentrations in neuronal cells. Methods: We create conditions imitating the coexistence of T2DM with AD and compare the results with state where the neuropathological changes are yet not developed. We have investigated the effect of the physiological (Aβ40) and toxic amyloid form (Aβ25–35) and its co-incubation with glucose or insulin on neuronal proliferation, H2O2, Aβ42, S100B, S100A8 protein concentrations, mature neuronal protrusions and neurogenesis. Results: Aβ40 and Aβ25-35 with hyperglycaemia provoked stronger cytotoxic effect comparing to Aβ alone, while hyperinsulinemia dampen this effect. Opposite results were obtained in H2O2 measurement. Insulin stimulated Aβ42 generation when co-incubated with both Aβ forms. Aβ40 and Aβ25-35 caused similar pattern of extracellular S100B protein influx an concomitant cytosolic efflux. Neuronal protrusions and neurogenesis were initiated by co-incubation of Aβ40 with hyperglycaemia while reduced in Aβ25-35 and hyperglycemia or insulinemia. Significance: Our finding suggest that for understanding the biochemical origins of neuropathological amyloid β progression and potential involvement of metabolic disturbances in this process, it’s crucial to gasp preliminary interactions on cellular level. Our data can lead to hypothesis that S100B protein could be a potential modulator as well as indicator of prodromal neuropathological alterations.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136038838","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}
Both curcumin and naproxen possess the activity of pain relief, which makes it possible to co-administrate these drugs in the same prescription. This study aimed to assess the potential pharmacokinetic interaction of naproxen with curcumin in rats. Sprague-Dawley (SD) rats were orally administrated with naproxen (10 mg/kg body weight) and curcumin (10 or 20 mg/kg, body weight) synchronously or successively with a single administration of naproxen as the control group. The plasma concentration of naproxen was analyzed with liquid chromatography tandem mass spectrometry and the plasma concentration-time curve was established to obtain the pharmacokinetic parameters. In vitro, the metabolic stability of naproxen and the activity of CYP2C9 was assessed in rat liver microsome to reveal the potential mechanism. Both synchronous and successive co-administration of naproxen and curcumin induced increased maximum concentration (Cmax), area under the curve (AUC0-t), half-life (t1/2) and reduced clearance rate (CLF) of naproxen in rats, and the effect of curcumin was enhanced with its increasing concentration. In vitro, curcumin (10 and 20 mg/kg) was found to enhance the metabolic stability of naproxen (half-life from 29.7 ± 1.34 to 41.8 ± 5.07 and 46.9 ± 3.33 min) and significantly inhibited the activity of CYP2C9 with the IC50 of 16.36 μmol/L (P < 0.05). A combination of naproxen and curcumin would induce pharmacokinetic interaction, which increased the systemic exposure of naproxen. The concentration-dependent inhibition of CYP2C9 by curcumin was the potential mechanism underlying the drug-herb interaction.
{"title":"CYP2C9 mediates the herb-drug interaction of curcumin with naproxen in rats","authors":"Yongjun Qiu, Sujun Huang, Minfang Zhu","doi":"10.32383/appdr/170203","DOIUrl":"https://doi.org/10.32383/appdr/170203","url":null,"abstract":"Both curcumin and naproxen possess the activity of pain relief, which makes it possible to co-administrate these drugs in the same prescription. This study aimed to assess the potential pharmacokinetic interaction of naproxen with curcumin in rats. Sprague-Dawley (SD) rats were orally administrated with naproxen (10 mg/kg body weight) and curcumin (10 or 20 mg/kg, body weight) synchronously or successively with a single administration of naproxen as the control group. The plasma concentration of naproxen was analyzed with liquid chromatography tandem mass spectrometry and the plasma concentration-time curve was established to obtain the pharmacokinetic parameters. In vitro, the metabolic stability of naproxen and the activity of CYP2C9 was assessed in rat liver microsome to reveal the potential mechanism. Both synchronous and successive co-administration of naproxen and curcumin induced increased maximum concentration (Cmax), area under the curve (AUC0-t), half-life (t1/2) and reduced clearance rate (CLF) of naproxen in rats, and the effect of curcumin was enhanced with its increasing concentration. In vitro, curcumin (10 and 20 mg/kg) was found to enhance the metabolic stability of naproxen (half-life from 29.7 ± 1.34 to 41.8 ± 5.07 and 46.9 ± 3.33 min) and significantly inhibited the activity of CYP2C9 with the IC50 of 16.36 μmol/L (P < 0.05). A combination of naproxen and curcumin would induce pharmacokinetic interaction, which increased the systemic exposure of naproxen. The concentration-dependent inhibition of CYP2C9 by curcumin was the potential mechanism underlying the drug-herb interaction.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136182408","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}
Marek Pająk, Elżbieta Kamysz, Jakub Fichna, Magdalena Woźniczka
The present work describes the protolytic properties of the sialorphin derivative (Pal-Lys- Lys-Gln-His-Asn-Pro-Arg) in an aqueous solution, at constant temperature 25.0 ± 0.1 °C and ionic strength 0.1 M (NaClO4), over the entire pH range. The overall protonation constants of the studied ligand were calculated by the potentiometric method. The logarithm values of the stepwise dissociation constants of the sialorphin derivative were found to be: [LH] = 11.88 ± 0.09, [LH2]+ = 9.96 ± 0.03, [LH3]2+ = 8.71 ± 0.03, [LH4]3+ = 5.49 ± 0.03, [LH5]4+ = 2.82 ± 0.03. The percentage of each species formed in an aqueous solution was estimated from the species distribution curves as a function of pH (82% [LH] at pH 11.0, 68% [LH2]+ at pH 9.3, 95% [LH3]2+ at pH 7.1, 90% [LH4]3+ at pH 4.2, 85% [LH5]4+ at pH 2.0). The five protonation constants indicate that the studied ligand can be very active in forming complexes with different metal ions. In addition, the sialorphin derivative can also be tested as a bioactive material, which warrants its further in vitro and in vivo studies.
{"title":"The protolytic properties of the sialorphin derivative Pal-Lys-Lys-Gln-His-Asn-Pro-Arg in an aqueous solution","authors":"Marek Pająk, Elżbieta Kamysz, Jakub Fichna, Magdalena Woźniczka","doi":"10.32383/appdr/170103","DOIUrl":"https://doi.org/10.32383/appdr/170103","url":null,"abstract":"The present work describes the protolytic properties of the sialorphin derivative (Pal-Lys- Lys-Gln-His-Asn-Pro-Arg) in an aqueous solution, at constant temperature 25.0 ± 0.1 °C and ionic strength 0.1 M (NaClO4), over the entire pH range. The overall protonation constants of the studied ligand were calculated by the potentiometric method. The logarithm values of the stepwise dissociation constants of the sialorphin derivative were found to be: [LH] = 11.88 ± 0.09, [LH2]+ = 9.96 ± 0.03, [LH3]2+ = 8.71 ± 0.03, [LH4]3+ = 5.49 ± 0.03, [LH5]4+ = 2.82 ± 0.03. The percentage of each species formed in an aqueous solution was estimated from the species distribution curves as a function of pH (82% [LH] at pH 11.0, 68% [LH2]+ at pH 9.3, 95% [LH3]2+ at pH 7.1, 90% [LH4]3+ at pH 4.2, 85% [LH5]4+ at pH 2.0). The five protonation constants indicate that the studied ligand can be very active in forming complexes with different metal ions. In addition, the sialorphin derivative can also be tested as a bioactive material, which warrants its further in vitro and in vivo studies.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253823","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 Jakimiuk, Daniel Augustynowicz, Sylwia Wojtulewicz, Wiktoria Wiśniewska, Jakub Władysław Strawa, Julia Wyszkowska, Michał Tomczyk
Plant extracts remain an infinite source of bioactive chemicals and an inexhaustible resource for discovering new drugs of natural origin. Thus, in this study, we focused on analysing 29 ethanolic extracts (E1-E29) from selected plants of flora of Poland to assess their antioxidant, anti-inflammatory and acetylcholinesterase inhibitory properties in relation to the chemical profiles of phenolic compounds. The results show that the investigated samples differed in terms of their chemical compositions and biological activities. The extract from Cirsium palustre leaves (E13) possesses the highest phenolic and flavonoid contents as well as antiradical activity in the DPPH (2,2-diphenyl-1-picrylhydrazyl) test (415.28 ± 2.22 µM of Trolox equivalent). On the other hand, the most potent anti-inflammatory agents (at 125 µg/mL) were extracts from Odontites vulgaris herbs (E24), with a COX-2 (cyclooxygenase-2) inhibition percentage of 74.54 ± 0.77, and Erigeron acris flower heads (E22), with a 15-sLOX (soybean 15-lipooxygenase) inhibition percentage of 42.45 ± 3.32. All extracts exhibited moderate acetylcholinesterase inhibitory activity. Moreover, to the best of our knowledge, the present study is the first to report phytochemical and pharmacological analyses of extracts from Anthericum ramosum and Lysimachia europaea.
{"title":"In vitro antioxidant, anti-inflammatory activities and acetylcholinesterase inhibition properties of selected plant extracts","authors":"Katarzyna Jakimiuk, Daniel Augustynowicz, Sylwia Wojtulewicz, Wiktoria Wiśniewska, Jakub Władysław Strawa, Julia Wyszkowska, Michał Tomczyk","doi":"10.32383/appdr/171435","DOIUrl":"https://doi.org/10.32383/appdr/171435","url":null,"abstract":"Plant extracts remain an infinite source of bioactive chemicals and an inexhaustible resource for discovering new drugs of natural origin. Thus, in this study, we focused on analysing 29 ethanolic extracts (E1-E29) from selected plants of flora of Poland to assess their antioxidant, anti-inflammatory and acetylcholinesterase inhibitory properties in relation to the chemical profiles of phenolic compounds. The results show that the investigated samples differed in terms of their chemical compositions and biological activities. The extract from Cirsium palustre leaves (E13) possesses the highest phenolic and flavonoid contents as well as antiradical activity in the DPPH (2,2-diphenyl-1-picrylhydrazyl) test (415.28 ± 2.22 µM of Trolox equivalent). On the other hand, the most potent anti-inflammatory agents (at 125 µg/mL) were extracts from Odontites vulgaris herbs (E24), with a COX-2 (cyclooxygenase-2) inhibition percentage of 74.54 ± 0.77, and Erigeron acris flower heads (E22), with a 15-sLOX (soybean 15-lipooxygenase) inhibition percentage of 42.45 ± 3.32. All extracts exhibited moderate acetylcholinesterase inhibitory activity. Moreover, to the best of our knowledge, the present study is the first to report phytochemical and pharmacological analyses of extracts from Anthericum ramosum and Lysimachia europaea.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253818","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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