Eliza Matuszewska, Agnieszka Klupczyńska-Gabryszak, Szymon Plewa, Natalia Rzetecka, Kacper Packi, H. Mohd, B. Michniak-Kohn, J. Matysiak
Honeybee venom (HBV) is a product of natural origin with an extremely complex composition. It exhibits several beneficial pharmacological properties, for example anti-inflammatory, antimicrobial, antidiabetic, anti-arthritic, and anti-tumour activities. On the other hand, HBV contains highly allergenic components, including melittin, which makes up more than 50% of its dry weight. Despite many studies conducted, HBV's components and mechanism of action are not yet fully known and understood. Therefore, to enhance the safety of its therapeutical applications, it is essential to establish HBV's composition and biological properties. Many analytical techniques and methods have been reported as potentially useful for the determination of new HBV constituents. Studies focus mainly on the analyses of the HBV proteome and metabolome. Also, properties of its components when applied to the skin, as well as its allergenicity, are being studied. Currently, the most commonly used methods for HBV analysis include high-performance liquid chromatography and mass spectrometry. Choosing the correct and most applicable method for HBV analysis is of great importance in order to obtain in-depth results crucial for the understanding of its mechanism of biological action. The diversity of chemical compounds in HBV also entails an appropriate sample preparation at the pre-analytical stage. In order to summarise the latest knowledge on techniques for the analysis of complex natural products, on the example of HBV, this review paper discusses the modern analytical tools of HBV characterisation, focusing on metabolomic and proteomic studies, topical applications, investigation of venom allergies, and the prospects for future research.
{"title":"Application of modern analytical techniques in the analysis of complex matrices of natural origin on the example of honeybee venom","authors":"Eliza Matuszewska, Agnieszka Klupczyńska-Gabryszak, Szymon Plewa, Natalia Rzetecka, Kacper Packi, H. Mohd, B. Michniak-Kohn, J. Matysiak","doi":"10.32383/appdr/161914","DOIUrl":"https://doi.org/10.32383/appdr/161914","url":null,"abstract":"Honeybee venom (HBV) is a product of natural origin with an extremely complex composition. It exhibits several beneficial pharmacological properties, for example anti-inflammatory, antimicrobial, antidiabetic, anti-arthritic, and anti-tumour activities. On the other hand, HBV contains highly allergenic components, including melittin, which makes up more than 50% of its dry weight. Despite many studies conducted, HBV's components and mechanism of action are not yet fully known and understood. Therefore, to enhance the safety of its therapeutical applications, it is essential to establish HBV's composition and biological properties. Many analytical techniques and methods have been reported as potentially useful for the determination of new HBV constituents. Studies focus mainly on the analyses of the HBV proteome and metabolome. Also, properties of its components when applied to the skin, as well as its allergenicity, are being studied. Currently, the most commonly used methods for HBV analysis include high-performance liquid chromatography and mass spectrometry. Choosing the correct and most applicable method for HBV analysis is of great importance in order to obtain in-depth results crucial for the understanding of its mechanism of biological action. The diversity of chemical compounds in HBV also entails an appropriate sample preparation at the pre-analytical stage. In order to summarise the latest knowledge on techniques for the analysis of complex natural products, on the example of HBV, this review paper discusses the modern analytical tools of HBV characterisation, focusing on metabolomic and proteomic studies, topical applications, investigation of venom allergies, and the prospects for future research.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47995438","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}
Karina Sommerfeld-Klatta, Magdalena Łukasik-Głębocka, E. Krawczak, Anna Stodolska, B. Zielińska-Psuja
Quetiapine (QT) belongs to the second generation of antipsychotics. It is mostly used to treat depression, bipolar disorder, and schizophrenia. During biotransformation via myeloperoxidase (MPO) QT is oxidized to quinoneimine and a reactive radical, which may contribute to the development of oxidative stress during intoxication. The coexisting inflammation may also significantly contribute to the disturbances in the course of QT poisoning. In this study, twenty-one patients poisoned with quetiapine were examined. The study aimed to assess the correlation between blood QT concentration and selected oxidative stress as well as inflammation biomarkers, such as MPO and C-reactive protein (CRP) levels in the serum of poisoned patients. The obtained results were related to the values of the control group consisting of 21 healthy people, untreated and not poisoned with the drug. In patients with a toxic QT concentration in the blood (3.15 ± 2.11 μg/mL), the activity of MPO and CRP serum level were significantly higher in comparison to the control group. The mean level of CRP in the study group was 76.74 mg/L, while in the control group only 1.86 mg/L. The increase in MPO activity and CRP blood level in patients after QT overdose may confirm the hypothesis of oxidative disorders arising during its biotransformation and concomitant inflammation. Statistically significant relationships between selected biomarkers and blood QT concentration, the patient's clinical condition and the type of therapy were demonstrated.
{"title":"Participation of quetiapine in oxidative stress and inflammation status in the treatment of drug overdose","authors":"Karina Sommerfeld-Klatta, Magdalena Łukasik-Głębocka, E. Krawczak, Anna Stodolska, B. Zielińska-Psuja","doi":"10.32383/appdr/165999","DOIUrl":"https://doi.org/10.32383/appdr/165999","url":null,"abstract":"Quetiapine (QT) belongs to the second generation of antipsychotics. It is mostly used to treat depression, bipolar disorder, and schizophrenia. During biotransformation via myeloperoxidase (MPO) QT is oxidized to quinoneimine and a reactive radical, which may contribute to the development of oxidative stress during intoxication. The coexisting inflammation may also significantly contribute to the disturbances in the course of QT poisoning. In this study, twenty-one patients poisoned with quetiapine were examined. The study aimed to assess the correlation between blood QT concentration and selected oxidative stress as well as inflammation biomarkers, such as MPO and C-reactive protein (CRP) levels in the serum of poisoned patients. The obtained results were related to the values of the control group consisting of 21 healthy people, untreated and not poisoned with the drug. In patients with a toxic QT concentration in the blood (3.15 ± 2.11 μg/mL), the activity of MPO and CRP serum level were significantly higher in comparison to the control group. The mean level of CRP in the study group was 76.74 mg/L, while in the control group only 1.86 mg/L. The increase in MPO activity and CRP blood level in patients after QT overdose may confirm the hypothesis of oxidative disorders arising during its biotransformation and concomitant inflammation. Statistically significant relationships between selected biomarkers and blood QT concentration, the patient's clinical condition and the type of therapy were demonstrated.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42134306","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}
Furosemide and torasemide (loop diuretics) are used to treat hypertension or pulmonary edema. They are often administered in the parenteral route. In critically ill patients, there is a problem of a limited number of venous accesses, which complicates the polytherapy. Drugs of unknown compatibility must be administered separately, and the problem increases in patients receiving parenteral nutrition. Lipid emulsions have been introduced into clinical practice as a high-calorie, non-glucose source of energy for parenteral administration, but they can also be used as lipophilic drug carriers. In this paper, the parenteral nutrition admixture (PNA) Nutriflex Lipid special was used as a drug carrier for furosemide and torasemide. For this purpose, drug stability tests (HPLC method) were carried out in various light and temperature conditions, imitating clinical conditions, and the parameters of the lipid emulsion (pH, zeta potential, the size of the emulsion droplets and polpolydispersity) were tested. Furosemide and torasemide added to Nutriflex Lipid special did not cause significant changes in the physicochemical properties of PNA. Changes in pH and MDD were within acceptable limits. Both drugs when added to Nutriflex Lipid special were degraded, dependent on the storage conditions and the chemical structure.
{"title":"Stability of furosemide and torasemide in parenteral nutrition admixture","authors":"Szymon Tomczak, A. Jelińska, Jan Kościński","doi":"10.32383/appdr/168629","DOIUrl":"https://doi.org/10.32383/appdr/168629","url":null,"abstract":"Furosemide and torasemide (loop diuretics) are used to treat hypertension or pulmonary edema. They are often administered in the parenteral route. In critically ill patients, there is a problem of a limited number of venous accesses, which complicates the polytherapy. Drugs of unknown compatibility must be administered separately, and the problem increases in patients receiving parenteral nutrition. Lipid emulsions have been introduced into clinical practice as a high-calorie, non-glucose source of energy for parenteral administration, but they can also be used as lipophilic drug carriers. In this paper, the parenteral nutrition admixture (PNA) Nutriflex Lipid special was used as a drug carrier for furosemide and torasemide. For this purpose, drug stability tests (HPLC method) were carried out in various light and temperature conditions, imitating clinical conditions, and the parameters of the lipid emulsion (pH, zeta potential, the size of the emulsion droplets and polpolydispersity) were tested. Furosemide and torasemide added to Nutriflex Lipid special did not cause significant changes in the physicochemical properties of PNA. Changes in pH and MDD were within acceptable limits. Both drugs when added to Nutriflex Lipid special were degraded, dependent on the storage conditions and the chemical structure.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44823042","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}
Danuta Szkutnik-Fiedler, Filip Kwiatkowski, Monika Chomej, D. Kołodziej, M. Michalak, E. Grześkowiak, E. Szałek
Most hospitalized patients with COVID-19 require complex pharmacotherapy due to underlying diseases, and polypharmacy may significantly increase the risk of drug-drug interactions (DDIs) and, in consequence, trigger adverse effects. The aim of this study was to assess the risk of potential DDIs during hospitalization in COVID-19 patients. A retrospective analysis of pharmacotherapy in 75 patients (age, Mean±SD, 63.6±14.9) with a proven diagnosis of SARS-CoV-2 infection was conducted. The analysis included drugs administered to treat comorbidities and the COVID-19 treatment. 524 moderate and 112 major interaction cases were revealed in the analyzed COVID-19 patients, and 84% of the patients were exposed to at least one major DDI. Drugs that caused the most frequently observed DDIs include macrolides, low molecular weight heparins, glucocorticosteroids, quinolones, and antihypertensive drugs. Most COVID-19 patients have comorbidities requiring polypharmacy, which increases the risk of DDIs. Therefore, additional monitoring should be considered due to potential adverse effects, drug conversion, and deprescription.
{"title":"Potential drug-drug interactions in hospitalized patients with COVID-19.","authors":"Danuta Szkutnik-Fiedler, Filip Kwiatkowski, Monika Chomej, D. Kołodziej, M. Michalak, E. Grześkowiak, E. Szałek","doi":"10.32383/appdr/162213","DOIUrl":"https://doi.org/10.32383/appdr/162213","url":null,"abstract":"Most hospitalized patients with COVID-19 require complex pharmacotherapy due to underlying diseases, and polypharmacy may significantly increase the risk of drug-drug interactions (DDIs) and, in consequence, trigger adverse effects. The aim of this study was to assess the risk of potential DDIs during hospitalization in COVID-19 patients. A retrospective analysis of pharmacotherapy in 75 patients (age, Mean±SD, 63.6±14.9) with a proven diagnosis of SARS-CoV-2 infection was conducted. The analysis included drugs administered to treat comorbidities and the COVID-19 treatment. 524 moderate and 112 major interaction cases were revealed in the analyzed COVID-19 patients, and 84% of the patients were exposed to at least one major DDI. Drugs that caused the most frequently observed DDIs include macrolides, low molecular weight heparins, glucocorticosteroids, quinolones, and antihypertensive drugs. Most COVID-19 patients have comorbidities requiring polypharmacy, which increases the risk of DDIs. Therefore, additional monitoring should be considered due to potential adverse effects, drug conversion, and deprescription.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41694629","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}
K. Dettlaff, K. Dominiak, Marta Klimaszewska, A. Gostyńska
Intravenous ibuprofen (IBF) is indicated for short-term acute moderate pain and fever management. Limited data concerning the compatibility of intravenous IBF and other parenteral medications makes it inconvenient to use in polypharmacy-required patients. The simultaneous administration of two incompatible drugs is a health- or even life-threatening medical error. This study was performed to evaluate the physical compatibility of two intravenous IBF doses (600 mg/100 mL, 400 mg/100 mL) during Y-site administration with common parenteral medications. Eight infusion fluids, seven ready-to-use solutions for infusion, and thirty concentrates or powders for solutions for infusion were examined. All these drugs, if relevant, were reconstituted and diluted following the manufacturer's instructions to achieve concentrations found most commonly in clinical practice. Samples were prepared by mixing IBFs and selected drug product solutions at the 1:1 volume ratio. All samples underwent visual inspection and determination of pH and turbidity before combining with IBF and in time points (0, 30, 60, and 120 minutes) after simulated Y-site administration with IBF. In the case of propofol, which is an emulsion for infusion, lipid droplet size, zeta potential, and polydispersity index were also determined. The incompatibilities were observed for IBF combinations with amiodarone, ciprofloxacin, clemastine, gentamicin, vinpocetine, and calcium chloride.
{"title":"Physical compatibility of ibuprofen and selected parenteral drugs during simulated y-site administration","authors":"K. Dettlaff, K. Dominiak, Marta Klimaszewska, A. Gostyńska","doi":"10.32383/appdr/167804","DOIUrl":"https://doi.org/10.32383/appdr/167804","url":null,"abstract":"Intravenous ibuprofen (IBF) is indicated for short-term acute moderate pain and fever management. Limited data concerning the compatibility of intravenous IBF and other parenteral medications makes it inconvenient to use in polypharmacy-required patients. The simultaneous administration of two incompatible drugs is a health- or even life-threatening medical error. \u0000This study was performed to evaluate the physical compatibility of two intravenous IBF doses (600 mg/100 mL, 400 mg/100 mL) during Y-site administration with common parenteral medications. Eight infusion fluids, seven ready-to-use solutions for infusion, and thirty concentrates or powders for solutions for infusion were examined. All these drugs, if relevant, were reconstituted and diluted following the manufacturer's instructions to achieve concentrations found most commonly in clinical practice. Samples were prepared by mixing IBFs and selected drug product solutions at the 1:1 volume ratio. All samples underwent visual inspection and determination of pH and turbidity before combining with IBF and in time points (0, 30, 60, and 120 minutes) after simulated Y-site administration with IBF. In the case of propofol, which is an emulsion for infusion, lipid droplet size, zeta potential, and polydispersity index were also determined. The incompatibilities were observed for IBF combinations with amiodarone, ciprofloxacin, clemastine, gentamicin, vinpocetine, and calcium chloride.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.4,"publicationDate":"2023-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49190576","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}
Photodynamic therapy (PDT) has emerged as a non-invasive modality where photosensitizer (PS) plays an indispensable role for treating tumors. This study proposes a novel Zein nanoparticle (ZP) encapsulating Zinc phthalocyanine (ZnPc) that targets tumor through intravenous delivery. The ZPs were prepared by phase separation process. Modification of ZPs were realized through encapsulation of polydopamine (PDA) and hyaluronic acid (HA) in order to maintain photothermal, pH-responsive, and tumor-targeting properties. The physiochemical properties, in vitro release, and in vitro evaluation of photothermal and photodynamic effects were studied. The biosafety was analyzed through cytotoxicity assay using human lung cancer cell line A549 as model. The excellent biosafety and significant anti-tumor effect demonstrated that the novel ZPs can be potential candidates for the alternative treatment of cancer.
{"title":"Preparation and characterization of pH-responsive Zein-ZnPc-PDA/HA nanoparticles intended for tumor therapy","authors":"Huixiang Lu, Ming Yang, Xueying Tian, Xianhui He, Yujun Lu, Qian-rong Peng","doi":"10.32383/appdr/163050","DOIUrl":"https://doi.org/10.32383/appdr/163050","url":null,"abstract":"Photodynamic therapy (PDT) has emerged as a non-invasive modality where photosensitizer (PS) plays an indispensable role for treating tumors. This study proposes a novel Zein nanoparticle (ZP) encapsulating Zinc phthalocyanine (ZnPc) that targets tumor through intravenous delivery. The ZPs were prepared by phase separation process. Modification of ZPs were realized through encapsulation of polydopamine (PDA) and hyaluronic acid (HA) in order to maintain photothermal, pH-responsive, and tumor-targeting properties. The physiochemical properties, in vitro release, and in vitro evaluation of photothermal and photodynamic effects were studied. The biosafety was analyzed through cytotoxicity assay using human lung cancer cell line A549 as model. The excellent biosafety and significant anti-tumor effect demonstrated that the novel ZPs can be potential candidates for the alternative treatment of cancer.","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":"45510470","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}
K. El-Sharkawy, H. Alhazmi, A. Najmi, M. Albratty, A. Khalid, R. Hassani, S. Javed
In continuation of our reserach for synthesizing heterocyclic derivatives with a broad range of biological activities, the current research was performed to synthesize 3β-hydroxypregn-5-ene-20-one derivatives of coumarin, isoxazole, pyrazole, pyridine and pyrimidine and screen for antitumor activity. Synthesis of amino-thiopephen derivatives (1a-1b) was performed through reaction of 3β-hydroxypregn-5-ene-20-one with ethyl cyanoacetate or malononitrile and sulphur. 3β-Hydroxypregn-5-ene-20-one was reacted with ethyl cyanoacetate in the presence of hydrazine, urea or thiourea to obtain aminopyrazole (3), aminopyrimidine (4a-4b) derivatives, respectively. The amino-thiophene derivatives (1a-1b) further reacted with either phenylisothiocyanate or benzoylisothiocyanate to form fused thienopyrimidine derivatives (5a-5d). The products 1a and 1b were also treated with ethyl cyanoacetate to afford cyanoacetamidothiophene derivatives (6a-6b) which were converted to fused thienopyridone derivatives (7a-7b) through cyclization reaction. The compounds 6a and 6b were allowed to react with different carbonyl compounds including salicyaldehyde, cyclopentanone-sulphur mixture, acetylacetone and malonaldehyde to prepare coumarin (8a-8b), cyclopentylthiophene (9a-9b) and 2-pyridinone (10a-10d) derivatives respectively. Furthermore, the reactions of hydroxylamine hydrochloride and benzoylacetonitrile with the compounds 6a-6b separately afforded new aminoisoxazole (12a-12b) and phenylpyridone (14a-14b) derivatives, respectively. The structures of new products were established through IR, 1H NMR, 13C NMR spectroscopic and mass spectrometric analysis. The synthesized compounds (1a-1b to 14a-14b) displayed in-vitro antitumor activity against human cell-lines, including MCF-7 (breast adenocarcinoma), SF-268 (CNS cancer) and NCI-H460 (non-small lung cancer cell). The results suggested that all the screened products exhibited cell growth inhibitory activity in a dose-dependents manner. However, the compound 12a showed highest level of inhibition against all three cell-lines.
{"title":"Design, synthesis and antitumor activity of coumarin, isoxazole, pyrazole, pyridine and pyrimidine compounds: 3β-hydroxypregn-5-ene-20-one derivatives","authors":"K. El-Sharkawy, H. Alhazmi, A. Najmi, M. Albratty, A. Khalid, R. Hassani, S. Javed","doi":"10.32383/appdr/161430","DOIUrl":"https://doi.org/10.32383/appdr/161430","url":null,"abstract":"In continuation of our reserach for synthesizing heterocyclic derivatives with a broad range of biological activities, the current research was performed to synthesize 3β-hydroxypregn-5-ene-20-one derivatives of coumarin, isoxazole, pyrazole, pyridine and pyrimidine and screen for antitumor activity. Synthesis of amino-thiopephen derivatives (1a-1b) was performed through reaction of 3β-hydroxypregn-5-ene-20-one with ethyl cyanoacetate or malononitrile and sulphur. 3β-Hydroxypregn-5-ene-20-one was reacted with ethyl cyanoacetate in the presence of hydrazine, urea or thiourea to obtain aminopyrazole (3), aminopyrimidine (4a-4b) derivatives, respectively. The amino-thiophene derivatives (1a-1b) further reacted with either phenylisothiocyanate or benzoylisothiocyanate to form fused thienopyrimidine derivatives (5a-5d). The products 1a and 1b were also treated with ethyl cyanoacetate to afford cyanoacetamidothiophene derivatives (6a-6b) which were converted to fused thienopyridone derivatives (7a-7b) through cyclization reaction. The compounds 6a and 6b were allowed to react with different carbonyl compounds including salicyaldehyde, cyclopentanone-sulphur mixture, acetylacetone and malonaldehyde to prepare coumarin (8a-8b), cyclopentylthiophene (9a-9b) and 2-pyridinone (10a-10d) derivatives respectively. Furthermore, the reactions of hydroxylamine hydrochloride and benzoylacetonitrile with the compounds 6a-6b separately afforded new aminoisoxazole (12a-12b) and phenylpyridone (14a-14b) derivatives, respectively. The structures of new products were established through IR, 1H NMR, 13C NMR spectroscopic and mass spectrometric analysis. The synthesized compounds (1a-1b to 14a-14b) displayed in-vitro antitumor activity against human cell-lines, including MCF-7 (breast adenocarcinoma), SF-268 (CNS cancer) and NCI-H460 (non-small lung cancer cell). The results suggested that all the screened products exhibited cell growth inhibitory activity in a dose-dependents manner. However, the compound 12a showed highest level of inhibition against all three cell-lines.","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":"69582411","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. Pawlikowska-Pawlęga, J. Kapral-Piotrowska, A. Jarosz-Wilkołazka, B. Chudzik, R. Paduch, J. Jakubowicz-Gil, A. Wawrzyniak, I. Łuszczewska-Sierakowska, A. Sławińska-Brych, B. Zdzisińska, E. Reszczyńska, K. Trebacz, W. Gruszecki
Apigenin, non-toxic and non-mutagenic flavonoid, is an alternative to classical drugs that interact with membranes. Hence, the objects of the study were to examine its effects on liposomes made of egg yolk phosphatidylcholine (EYPC) with the use of 1H NMR, four-electrode BLM and EPR techniques, and determine its activity on lipids and proteins of human cervix carcinoma (HeLa) cells. In addition its protective efficacy against H2O2- induced oxidative shock was investigated. FTIR spectroscopy was applied to study molecular interactions with membrane lipids and proteins of HeLa cells. Microscopic techniques (SEM, light, and fluorescence), flow cytometer analysis, and NR assays were employed to reveal apigenin involvement in apoptosis in different cell conditions. Apigenin affected mainly the region of choline head groups and the hydrophobic core below this area. Simultaneously, the ordering effect was shown. The fingerprint region of lipids in the HeLa cells was found as a target for apigenin. Furthermore, in the amide I and amide II regions, a decrease in β-sheets and an increase in turns, loops, and unordered structures were noted. Apigenin reduced viability of cells and induced apoptosis. SEM observations revealed characteristic changes in morphology of the examined cells. Pretreatment of HeLa cells with apigenin protected them against H2O2-induced oxidative stress by the increase in glutathione content as well as superoxide dismutase and catalase levels. The consequences of molecular changes related to membranes and cancer cells make apigenin a unique and very interesting bio-compound with great significance for medical and biological applications.
{"title":"Apigenin targets protein and lipids of HeLa cells and exhibits protective efficacy against oxidative stress","authors":"B. Pawlikowska-Pawlęga, J. Kapral-Piotrowska, A. Jarosz-Wilkołazka, B. Chudzik, R. Paduch, J. Jakubowicz-Gil, A. Wawrzyniak, I. Łuszczewska-Sierakowska, A. Sławińska-Brych, B. Zdzisińska, E. Reszczyńska, K. Trebacz, W. Gruszecki","doi":"10.32383/appdr/163049","DOIUrl":"https://doi.org/10.32383/appdr/163049","url":null,"abstract":"Apigenin, non-toxic and non-mutagenic flavonoid, is an alternative to classical drugs that interact with membranes. Hence, the objects of the study were to examine its effects on liposomes made of egg yolk phosphatidylcholine (EYPC) with the use of 1H NMR, four-electrode BLM and EPR techniques, and determine its activity on lipids and proteins of human cervix carcinoma (HeLa) cells. In addition its protective efficacy against H2O2- induced oxidative shock was investigated. FTIR spectroscopy was applied to study molecular interactions with membrane lipids and proteins of HeLa cells. Microscopic techniques (SEM, light, and fluorescence), flow cytometer analysis, and NR assays were employed to reveal apigenin involvement in apoptosis in different cell conditions. Apigenin affected mainly the region of choline head groups and the hydrophobic core below this area. Simultaneously, the ordering effect was shown. The fingerprint region of lipids in the HeLa cells was found as a target for apigenin. Furthermore, in the amide I and amide II regions, a decrease in β-sheets and an increase in turns, loops, and unordered structures were noted. Apigenin reduced viability of cells and induced apoptosis. SEM observations revealed characteristic changes in morphology of the examined cells. Pretreatment of HeLa cells with apigenin protected them against H2O2-induced oxidative stress by the increase in glutathione content as well as superoxide dismutase and catalase levels. The consequences of molecular changes related to membranes and cancer cells make apigenin a unique and very interesting bio-compound with great significance for medical and biological applications.","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":"41708294","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}
We would like to take this opportunity to thank you for the effort and expertise that you contribute to reviewing, without which it would be impossible to maintain the high editorial standards of Acta Poloniae Pharmaceutica – Drug Research.
我们想借此机会感谢您在审稿过程中所付出的努力和专业知识，没有这些，我们就不可能保持Acta Poloniae Pharmaceutica - Drug Research的高编辑标准。
{"title":"Acknowledgement to Reviewers 2022","authors":"Michał Tomczyk","doi":"10.32383/appdr/164727","DOIUrl":"https://doi.org/10.32383/appdr/164727","url":null,"abstract":"We would like to take this opportunity to thank you for the effort and expertise that you contribute to reviewing, without which it would be impossible to maintain the high editorial standards of Acta Poloniae Pharmaceutica – Drug Research.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136375467","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}
Qi Huang, Yingli Zhao, Xing Fang, J. Liu, Quan Xia, Chao Tan, Yao Peng, Jingjing Wu
Mixed micelles (MMs), as a new targeted drug delivery system with high adjustability, have been widely studied in biomedicines. In order to study whether mixtures containing two different molecules have excellent targeted anti-tumor effect, MMs based on D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and triblock copolymer P84 were prepared, and the characterization, cell endocytosis, and exocytosis of P84/TPGS MMs were observed. Paclitaxel (PTX), a classical anti-tumor drug, was selected as a model compound to explore its anti-tumor effect in vivo. The results showed that P84/TPGS MMs had better stability, suitably distributed particle size, good cell endocytosis, and tumor sphere permeability, which could improve the permeability of PTX in the tumor site and effectively inhibit the growth of H22 tumor in mice. In conclusion, P84/TPGS MMs is a potential micelle carrier system of cancer targeting, needing further investigation.
{"title":"Development and optimization of TPGS/P84 mixed polymeric micelles: enhanced stability and anticancer effect of paclitaxel against tumor therapy","authors":"Qi Huang, Yingli Zhao, Xing Fang, J. Liu, Quan Xia, Chao Tan, Yao Peng, Jingjing Wu","doi":"10.32383/appdr/161587","DOIUrl":"https://doi.org/10.32383/appdr/161587","url":null,"abstract":"Mixed micelles (MMs), as a new targeted drug delivery system with high adjustability, have been widely studied in biomedicines. In order to study whether mixtures containing two different molecules have excellent targeted anti-tumor effect, MMs based on D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and triblock copolymer P84 were prepared, and the characterization, cell endocytosis, and exocytosis of P84/TPGS MMs were observed. Paclitaxel (PTX), a classical anti-tumor drug, was selected as a model compound to explore its anti-tumor effect in vivo. The results showed that P84/TPGS MMs had better stability, suitably distributed particle size, good cell endocytosis, and tumor sphere permeability, which could improve the permeability of PTX in the tumor site and effectively inhibit the growth of H22 tumor in mice. In conclusion, P84/TPGS MMs is a potential micelle carrier system of cancer targeting, needing further investigation.","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":"48358978","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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