Abstract: In this work, total phenols, flavonoids, tannins, anthocyanins, the antioxidant capacity (by the DPPH and FRAP method) were determined in the juice and pomice of cornelian cherry from the area of Montenegro. Also, content of microelements and macroelements in the juice, pomice and fruit of cornelian cherry were investigated. In the studied cornelian cherry samples, the content of phenols ranged from 159.57 to 244.93 mg GAE/100 g, flavonoids from 71.74 to 165.5 mg QE/100 g, tannins from 0.33 to 0.81 %, total anthocyanins 0.057-0.310 %. HPLC analysis identified anthocyanins: delphinidin-3-O-glucoside, cyanidin-3-O-galactoside, cyanidin-3-O-glucoside, pelargonin-3-O-glucoside and its derivative. The most abundant essential microelement in the studied cornelian cherry samples was Fe (23.44-37.69 mg/kg), followed by Zn (3.14-6.25 mg/kg), Cu (1.50-1.80 mg/kg) and Mn (0.58-0.78 mg/kg). The most abundant essential macroelement in the examined samples was K (2427.8-3276.2 mg/kg), followed by Ca (361.5-475.7), Mg (95.41-146.5 mg/kg) and Na (8.347-16.59 mg/kg). Pb, Cd and Ni were not detected in the tested samples. A high degree of correlation was obtained between the content of total flavonoids and antioxidant value measured by the FRAP method (R = 0.96), as well as between the content of total anthocyanins and antioxidant activity measured by the DPPH method (R = 0.89). Of individual anthocyanins, high correlation values were shown by cyanidin-3-O-galactoside (R = 0.96), cyanidin-3-O-glucoside (R = 0.95) and pelargonin-3-O-glucoside (R = 0.94) with antioxidant activity measured by the DPPH method.
摘要:本研究采用DPPH法和FRAP法测定了黑山地区山药樱桃汁和果渣中总酚、总黄酮、单宁、花青素和抗氧化能力。并对山茱萸果汁、果渣和果实中微量元素和大量元素的含量进行了研究。山茱萸中酚类含量为159.57 ~ 244.93 mg QE/100 g，黄酮类含量为71.74 ~ 165.5 mg QE/100 g，单宁含量为0.33 ~ 0.81%，总花青素含量为0.057 ~ 0.310%。HPLC分析鉴定花青素:飞燕草苷-3- o -葡萄糖苷、花青素-3- o -半乳糖苷、花青素-3- o -葡萄糖苷、天竺葵苷-3- o -葡萄糖苷及其衍生物。山茱萸样品中必需微量元素含量最高的是铁(23.44 ~ 37.69 mg/kg)，其次是锌(3.14 ~ 6.25 mg/kg)、铜(1.50 ~ 1.80 mg/kg)和锰(0.58 ~ 0.78 mg/kg)。微量元素含量最高的是K (2427.8 ~ 3276.2 mg/kg)，其次是Ca (361.5 ~ 475.7 mg/kg)、mg (95.41 ~ 146.5 mg/kg)和Na (8.347 ~ 16.59 mg/kg)。样品中未检出铅、镉和镍。FRAP法测定的总黄酮含量与抗氧化值呈高度相关(R = 0.96)， DPPH法测定的总花青素含量与抗氧化活性呈高度相关(R = 0.89)。单种花青素中，花青素-3- o -半乳糖苷(R = 0.96)、花青素-3- o -葡萄糖苷(R = 0.95)和天竺葵-3- o -葡萄糖苷(R = 0.94)与DPPH法测定的抗氧化活性具有较高的相关性。
{"title":"ANTIOXIDANT POTENTIAL OF CORNELIAN CHERRY (Cornus mas L.) FROM MONTENEGRO","authors":"Nada Blagojevic, Mara Kandic, Vesna Vukasinovic Pesic, Snezana Brasanac Vukanovic, Vanja Tadic, Dragica Bojovic","doi":"10.32383/appdr/169374","DOIUrl":"https://doi.org/10.32383/appdr/169374","url":null,"abstract":"Abstract: In this work, total phenols, flavonoids, tannins, anthocyanins, the antioxidant capacity (by the DPPH and FRAP method) were determined in the juice and pomice of cornelian cherry from the area of Montenegro. Also, content of microelements and macroelements in the juice, pomice and fruit of cornelian cherry were investigated. In the studied cornelian cherry samples, the content of phenols ranged from 159.57 to 244.93 mg GAE/100 g, flavonoids from 71.74 to 165.5 mg QE/100 g, tannins from 0.33 to 0.81 %, total anthocyanins 0.057-0.310 %. HPLC analysis identified anthocyanins: delphinidin-3-O-glucoside, cyanidin-3-O-galactoside, cyanidin-3-O-glucoside, pelargonin-3-O-glucoside and its derivative. The most abundant essential microelement in the studied cornelian cherry samples was Fe (23.44-37.69 mg/kg), followed by Zn (3.14-6.25 mg/kg), Cu (1.50-1.80 mg/kg) and Mn (0.58-0.78 mg/kg). The most abundant essential macroelement in the examined samples was K (2427.8-3276.2 mg/kg), followed by Ca (361.5-475.7), Mg (95.41-146.5 mg/kg) and Na (8.347-16.59 mg/kg). Pb, Cd and Ni were not detected in the tested samples. A high degree of correlation was obtained between the content of total flavonoids and antioxidant value measured by the FRAP method (R = 0.96), as well as between the content of total anthocyanins and antioxidant activity measured by the DPPH method (R = 0.89). Of individual anthocyanins, high correlation values were shown by cyanidin-3-O-galactoside (R = 0.96), cyanidin-3-O-glucoside (R = 0.95) and pelargonin-3-O-glucoside (R = 0.94) with antioxidant activity measured by the DPPH method.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253819","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 Michalina Brzóska, Nazar Michał Smereczański, Joanna Rogalska
The destructive impact of cadmium (Cd) on the oxidative/antioxidative status of the kidney, as well as the possible beneficial effect of co-administration of a 0.1% aqueous extract from Aronia melanocarpa L. berries (AM), were studied in a rat model of low-level and moderate general population exposure to this heavy metal (1 and 5 mg Cd/kg feed, respectively, for up to 24 months). Total antioxidative status (TAS) of the kidney and the main indices of the enzymatic (superoxide dismutase, catalase, glutathione reductase, and glutathione peroxidase) and non-enzymatic (reduced glutathione and thioredoxin) antioxidative barrier were assessed. The total oxidative status (TOS) and concentrations of hydrogen peroxide, xanthine oxidase, myeloperoxidase, and oxidized glutathione were measured as markers of oxidative status. The oxidative stress index (OSI) was calculated (TOS/TAS) to estimate the intensity of oxidative stress in the kidney. The exposure to Cd, dose- and duration-dependently, weakened the enzymatic and non-enzymatic antioxidative potential of the kidney leading to a decrease in its TAS, as well as enhanced oxidative status of this organ resulting in the development of oxidative stress. The administration of AM during the low-level and moderate intoxication with Cd significantly protected from this xenobiotic-induced disruption of the oxidative/antioxidative balance and development of oxidative stress in the kidney. In summary, even low-level long-term exposure to Cd may result in the occurrence of oxidative stress in the kidney, whereas supplementation with chokeberry products may improve the oxidative/antioxidative balance preventing oxidative stress in this organ.
{"title":"Protective effect of the extract from Aronia melanocarpa L. berries against cadmium-induced oxidative stress in the kidney: A study in an in vivo experimental model","authors":"Małgorzata Michalina Brzóska, Nazar Michał Smereczański, Joanna Rogalska","doi":"10.32383/appdr/169782","DOIUrl":"https://doi.org/10.32383/appdr/169782","url":null,"abstract":"The destructive impact of cadmium (Cd) on the oxidative/antioxidative status of the kidney, as well as the possible beneficial effect of co-administration of a 0.1% aqueous extract from Aronia melanocarpa L. berries (AM), were studied in a rat model of low-level and moderate general population exposure to this heavy metal (1 and 5 mg Cd/kg feed, respectively, for up to 24 months). Total antioxidative status (TAS) of the kidney and the main indices of the enzymatic (superoxide dismutase, catalase, glutathione reductase, and glutathione peroxidase) and non-enzymatic (reduced glutathione and thioredoxin) antioxidative barrier were assessed. The total oxidative status (TOS) and concentrations of hydrogen peroxide, xanthine oxidase, myeloperoxidase, and oxidized glutathione were measured as markers of oxidative status. The oxidative stress index (OSI) was calculated (TOS/TAS) to estimate the intensity of oxidative stress in the kidney. The exposure to Cd, dose- and duration-dependently, weakened the enzymatic and non-enzymatic antioxidative potential of the kidney leading to a decrease in its TAS, as well as enhanced oxidative status of this organ resulting in the development of oxidative stress. The administration of AM during the low-level and moderate intoxication with Cd significantly protected from this xenobiotic-induced disruption of the oxidative/antioxidative balance and development of oxidative stress in the kidney. In summary, even low-level long-term exposure to Cd may result in the occurrence of oxidative stress in the kidney, whereas supplementation with chokeberry products may improve the oxidative/antioxidative balance preventing oxidative stress in this organ.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253820","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 Cebulska, Katarzyna Malik, Kamila Czarnecka, Paweł Szymański
WHO has identified the increase in myopia as the world's greatest threat to vision health due to its association with vision-threatening complications like myopic macular degeneration, retinal detachment, cataract and open angle glaucoma. Pharmacological treatment with atropine is assessed as one of the best option in op-tical approaches to the control and inhibit of myopia progression. The aim of this study was to develop analytical method for quality control of 0.1 mg/mL atropine ophthalmic solution. UPLC analytical method for simultaneous determination of atropine sulfate monohydrate and its related substances described in Eur. Ph. and for additional impurities was developed. For method development low-dose of atropine formulations with a wide range of pH 4.5-6.6 were tested and the impact of formulation pH on the impurity profile was noted. The ionized form of tropic acid was observed in our studies in all buffered formulations with pH above 5. Additionally two isomers of atropine N-oxide were observed in the tested preparation with pH 6.6 in the presence of an oxidizing agent and were just possible to integrate with our new developed UPLC method. The ionized form of tropic acid was already defined in Berton et al. publication (1) and observed in the buffered formulation with pH 6.0. Our result complement and extend the impurity profile of atropine in wider pH range of atropine ophthalmic solutions.
{"title":"Additional degradants in the impurity profile of atropine low-dose ophthalmic solution","authors":"Ewelina Cebulska, Katarzyna Malik, Kamila Czarnecka, Paweł Szymański","doi":"10.32383/appdr/169907","DOIUrl":"https://doi.org/10.32383/appdr/169907","url":null,"abstract":"WHO has identified the increase in myopia as the world's greatest threat to vision health due to its association with vision-threatening complications like myopic macular degeneration, retinal detachment, cataract and open angle glaucoma. Pharmacological treatment with atropine is assessed as one of the best option in op-tical approaches to the control and inhibit of myopia progression. The aim of this study was to develop analytical method for quality control of 0.1 mg/mL atropine ophthalmic solution. UPLC analytical method for simultaneous determination of atropine sulfate monohydrate and its related substances described in Eur. Ph. and for additional impurities was developed. For method development low-dose of atropine formulations with a wide range of pH 4.5-6.6 were tested and the impact of formulation pH on the impurity profile was noted. The ionized form of tropic acid was observed in our studies in all buffered formulations with pH above 5. Additionally two isomers of atropine N-oxide were observed in the tested preparation with pH 6.6 in the presence of an oxidizing agent and were just possible to integrate with our new developed UPLC method. The ionized form of tropic acid was already defined in Berton et al. publication (1) and observed in the buffered formulation with pH 6.0. Our result complement and extend the impurity profile of atropine in wider pH range of atropine ophthalmic solutions.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":"120 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253821","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 Pokajewicz, Mariia Shanaida, Nataliia Hudz, Liudmyla Svydenko, Oksana Yezerska, Piotr Pawieł Wieczorek, Jacek Lipok
Satureja montana L. is widely used in traditional medicine and culinary. New varieties of this species are created and grown with different purposes. The essential oil (EsO) samples were obtained from the fresh flowering shoots of four new Ukrainian cultivars of S. montana: 'Krymski smaragd', 'Lunata', '697-1', and 'N3-18'. The EsO of cultivars ''Lunata' and 'Krymski smaragd' were studied in two following harvest years (2019 and 2020). The EsO samples were analyzed using gas chromatography-mass spectrometry (GC-MS). More than 60 components were identified in the studied EsO. Carvacrol was the principal component of all the samples (58.3-87.0% (as GC-MS relative abundances). p-Cymene was the second predominant component (5.0–8.8%) in the EsO of all the cultivars collected in the 2020 year, while cultivars ''Lunata' and 'Krymski smaragd' gathered in 2019 contained it in much fewer amounts (1.7% and 0.5%, respectively). γ-Terpinene was the third main component of EsO of the most studied varieties (0.9% to 6.6%). Only cultivar 'N697-1' contained carvacrol methyl ether at a significant level (11.7%). All the tested samples met the requirements of International Standard Organization (ISO) 79284:1991(E), supposing that the qualitative composition of the S. montana EsO should comprise the following main constituents: γ-terpinene, p-cymene, linalool, terpinen-4-ol, and carvacrol. It can be concluded that we dealt with the carvacrol chemotypes of S. montana. It was also revealed that growth year influenced the EsO composition of 'Krymski smaragd' and 'Lunata' cultivars. Our results afforded to compare the EsO of the S. montana new cultivars
{"title":"GC-MS evaluation of the essential oils from the newly developed cultivars of Satureja montana grown in southern Ukraine","authors":"Katarzyna Pokajewicz, Mariia Shanaida, Nataliia Hudz, Liudmyla Svydenko, Oksana Yezerska, Piotr Pawieł Wieczorek, Jacek Lipok","doi":"10.32383/appdr/169373","DOIUrl":"https://doi.org/10.32383/appdr/169373","url":null,"abstract":"Satureja montana L. is widely used in traditional medicine and culinary. New varieties of this species are created and grown with different purposes. The essential oil (EsO) samples were obtained from the fresh flowering shoots of four new Ukrainian cultivars of S. montana: 'Krymski smaragd', 'Lunata', '697-1', and 'N3-18'. The EsO of cultivars ''Lunata' and 'Krymski smaragd' were studied in two following harvest years (2019 and 2020). The EsO samples were analyzed using gas chromatography-mass spectrometry (GC-MS). More than 60 components were identified in the studied EsO. Carvacrol was the principal component of all the samples (58.3-87.0% (as GC-MS relative abundances). p-Cymene was the second predominant component (5.0–8.8%) in the EsO of all the cultivars collected in the 2020 year, while cultivars ''Lunata' and 'Krymski smaragd' gathered in 2019 contained it in much fewer amounts (1.7% and 0.5%, respectively). γ-Terpinene was the third main component of EsO of the most studied varieties (0.9% to 6.6%). Only cultivar 'N697-1' contained carvacrol methyl ether at a significant level (11.7%). All the tested samples met the requirements of International Standard Organization (ISO) 79284:1991(E), supposing that the qualitative composition of the S. montana EsO should comprise the following main constituents: γ-terpinene, p-cymene, linalool, terpinen-4-ol, and carvacrol. It can be concluded that we dealt with the carvacrol chemotypes of S. montana. It was also revealed that growth year influenced the EsO composition of 'Krymski smaragd' and 'Lunata' cultivars. Our results afforded to compare the EsO of the S. montana new cultivars","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":"34 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253824","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}
Dermocosmetics are products intended for sensitive and problematic skin. They are a good solution for additional care of skin affected by conditions such as atopic dermatitis, acne, psoriasis, or for couperose skin. The compounds of particular importance in the care of atopic skin include ceramides, ectoine, hyaluronic acid, vitamins A and E, as well as natural vegetable oils. The aim of this work was to develop a qualitative and quantitative approach and to investigate the characteristics of formulations such as a face cream, a topical cream, a body lotion, and a cleansing foam, dedicated to patients with atopic dermatitis. The newly developed cosmetic formulations showed good physical and chemical characteristics, typical of this type of product. They were also structurally and microbiologically stable during storage at various temperatures. Dermatological tests did not reveal any irritating or allergenic properties. The best data were obtained for the face cream, namely improvement of skin hydration by 21.88%, reduction of transepidermal water loss by 15.86%, alleviation of erythema by 15.77%, and of skin sensitivity by 17.20%. This work resulted in the preparation of innovative dermocosmetics to be used for atopic skin. The cosmetics have a unique composition and delicate formula, show high biofunctionality, and meet all the requirements for cosmetic products intended for marketing.
{"title":"Studies on the formulation and functionality of an innovative line of topical products for atopic skin","authors":"Joanna Matysiak, Natalia Rzetecka, Weronika Klimczak, Bożena Michniak-Kohn, Jan Matysiak, Daria Szymanowska","doi":"10.32383/appdr/170202","DOIUrl":"https://doi.org/10.32383/appdr/170202","url":null,"abstract":"Dermocosmetics are products intended for sensitive and problematic skin. They are a good solution for additional care of skin affected by conditions such as atopic dermatitis, acne, psoriasis, or for couperose skin. The compounds of particular importance in the care of atopic skin include ceramides, ectoine, hyaluronic acid, vitamins A and E, as well as natural vegetable oils. The aim of this work was to develop a qualitative and quantitative approach and to investigate the characteristics of formulations such as a face cream, a topical cream, a body lotion, and a cleansing foam, dedicated to patients with atopic dermatitis. The newly developed cosmetic formulations showed good physical and chemical characteristics, typical of this type of product. They were also structurally and microbiologically stable during storage at various temperatures. Dermatological tests did not reveal any irritating or allergenic properties. The best data were obtained for the face cream, namely improvement of skin hydration by 21.88%, reduction of transepidermal water loss by 15.86%, alleviation of erythema by 15.77%, and of skin sensitivity by 17.20%. This work resulted in the preparation of innovative dermocosmetics to be used for atopic skin. The cosmetics have a unique composition and delicate formula, show high biofunctionality, and meet all the requirements for cosmetic products intended for marketing.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":"4 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-10-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136253822","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 Szałabska-Rąpała, Weronika Borymska, M. Zych, Ilona Kaczmarczyk-Żebrowska
Oxidative stress is the basis of the pathogenesis of diabetes, obesity and their complications. Under its influence, free radicals that have not been neutralized or removed from the cell environment lead to damage to cellular macromolecules - carbohydrates, lipids and proteins. Honokiol and magnolol are neolignans derived from magnolia bark, which may be promising candidates in the fight against oxidative stress-related diseases. The aim of this study was to evaluate the antioxidant potential of structural isomers - honokiol and magnolol - in vitro, taking into account their effect on radicals and the potential possibility of protecting biomolecules against oxidative damage, as well as to analyze their capability to inhibit the activity of enzymes associated with carbohydrate and lipid metabolism. The abilities of neolignans to neutralize ABTS and DPPH radicals and also to prevent the formation of markers of oxidative damage - advanced oxidation protein products and thiobarbituric acid reactive substances were tested. The inhibitory properties of the compounds against the activity of enzymes (α-amylase, α-glucosidase, lipase) were also examined. The conducted analyzes indicate that in vitro honokiol possesses much better antioxidant properties and inhibits enzymes related to carbohydrate metabolism than magnolol. It neutralized model radicals and prevented oxidative damages almost as effectively as the reference compounds, with even better ability to inhibit enzymes involved in carbohydrate metabolism. None of the neolignans significantlly affected the reduction of lipase activity. The effectiveness of honokiol and magnolol as free radical scavengers and α-glucosidase and α-amylase inhibitors requires further confirmation in in vivo models.
{"title":"Honokiol and magnolol - comparison of inhibitory activity of enzymes involved in carbohydrate and lipid metabolism and antioxidant properties in in vitro studies","authors":"Katarzyna Szałabska-Rąpała, Weronika Borymska, M. Zych, Ilona Kaczmarczyk-Żebrowska","doi":"10.32383/appdr/168699","DOIUrl":"https://doi.org/10.32383/appdr/168699","url":null,"abstract":"Oxidative stress is the basis of the pathogenesis of diabetes, obesity and their complications. Under its influence, free radicals that have not been neutralized or removed from the cell environment lead to damage to cellular macromolecules - carbohydrates, lipids and proteins. Honokiol and magnolol are neolignans derived from magnolia bark, which may be promising candidates in the fight against oxidative stress-related diseases. The aim of this study was to evaluate the antioxidant potential of structural isomers - honokiol and magnolol - in vitro, taking into account their effect on radicals and the potential possibility of protecting biomolecules against oxidative damage, as well as to analyze their capability to inhibit the activity of enzymes associated with carbohydrate and lipid metabolism. The abilities of neolignans to neutralize ABTS and DPPH radicals and also to prevent the formation of markers of oxidative damage - advanced oxidation protein products and thiobarbituric acid reactive substances were tested. The inhibitory properties of the compounds against the activity of enzymes (α-amylase, α-glucosidase, lipase) were also examined. The conducted analyzes indicate that in vitro honokiol possesses much better antioxidant properties and inhibits enzymes related to carbohydrate metabolism than magnolol. It neutralized model radicals and prevented oxidative damages almost as effectively as the reference compounds, with even better ability to inhibit enzymes involved in carbohydrate metabolism. None of the neolignans significantlly affected the reduction of lipase activity. The effectiveness of honokiol and magnolol as free radical scavengers and α-glucosidase and α-amylase inhibitors requires further confirmation in in vivo models.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45944826","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}
One third of breast cancer patients also suffer from diabetes, which is associated with a 40% higher risk of mortality. Patients undergoing anti-cancer treatment are also exposed to xenoestrogens present in everyday life, which may affect the effectiveness of the therapies used. The purpose of our study was to analyzed the effect of metalloestrogens (Al, Cr[III]) on the effectiveness of aromatase inhibitors (AIs) under high glucose conditions prevailing in the cellular model. On two human breast cancer cell lines—MCF-7 and MCF-7/DOX—a cell viability assay, a flow cytometer analysis of apoptosis, and protein activity of BAX, Bcl-2, and VEGF-A by ELISA were carried out. Results were analyzed using one-way ANOVA, followed post hoc by Tukey’s multiple comparisons tests. High glucose conditions reduced the effectiveness of AIs in both cell lines (decreased cytotoxicity, inhibition of apoptosis, increase in Bcl-2/BAX ratio and angiogenesis), regardless of the combination with metalloestrogens. Hyperglycemia may affect the effectiveness of AIs to a greater extent than metalloestrogens alone - the activity of drugs in the presence of high glucose concentrations was significantly lower, regardless of the combination with metalloestrogens, which indicates the key role of hyperglycemia in attenuating their activity. Therefore controlling hyperglycemia and individualized treatment regimens in cancer patients with diabetes may have important therapeutic implications.
{"title":"High glucose reduces anti-tumor activity of aromatase inhibitors in a hormone-dependent breast cancer cell model","authors":"Kamila Boszkiewicz, Agnieszka Piwowar","doi":"10.32383/appdr/168363","DOIUrl":"https://doi.org/10.32383/appdr/168363","url":null,"abstract":"One third of breast cancer patients also suffer from diabetes, which is associated with a 40% higher risk of mortality. Patients undergoing anti-cancer treatment are also exposed to xenoestrogens present in everyday life, which may affect the effectiveness of the therapies used. The purpose of our study was to analyzed the effect of metalloestrogens (Al, Cr[III]) on the effectiveness of aromatase inhibitors (AIs) under high glucose conditions prevailing in the cellular model. On two human breast cancer cell lines—MCF-7 and MCF-7/DOX—a cell viability assay, a flow cytometer analysis of apoptosis, and protein activity of BAX, Bcl-2, and VEGF-A by ELISA were carried out. Results were analyzed using one-way ANOVA, followed post hoc by Tukey’s multiple comparisons tests. High glucose conditions reduced the effectiveness of AIs in both cell lines (decreased cytotoxicity, inhibition of apoptosis, increase in Bcl-2/BAX ratio and angiogenesis), regardless of the combination with metalloestrogens. Hyperglycemia may affect the effectiveness of AIs to a greater extent than metalloestrogens alone - the activity of drugs in the presence of high glucose concentrations was significantly lower, regardless of the combination with metalloestrogens, which indicates the key role of hyperglycemia in attenuating their activity. Therefore controlling hyperglycemia and individualized treatment regimens in cancer patients with diabetes may have important therapeutic implications.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":"96 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-07-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135154642","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}
Trastuzumab is one of the most commonly used monoclonal antibodies in the treatment of breast cancer. It is effective because it binds to the HER2 receptor and inhibits the signaling pathways for proliferation and metastasis. However, intrinsic or acquired resistance resulting from the various signaling pathways of heterogeneous breast cancer reduces its efficacy. To increase its efficacy, it is combined with different agents in the treatment. In this study, the synergistic effect of the combination of trastuzumab and gambogic acid on the breast cell line MDA-MB -453 was investigated in vitro. At the end of 12-, 24-, 48-, and 72-hour incubation, their antiproliferative effects were determined by XTT method. Combination Index (CI) values of the study were calculated using CompuSyn.exe software. The highest synergistic effect was obtained with 12.5 µg/mL trastuzumab + 1.25 µM gambogic acid (CI-4) at the 72nd hour. The activity of the antioxidant enzyme catalase (CAT) was also measured for the applications. We observed that combination of trastuzumab and gambogic acid decreased CAT activity at 24, 48 and 72nd hours. It was concluded that gambogic acid may be a good candidate for combination with other agents in targeted drug design.
{"title":"Synergistic effects of trastuzumab and gambogic acid on MDA-MB-453 breast cancer cell line","authors":"Abdullah Alpkan, M. Cankaya","doi":"10.32383/appdr/166509","DOIUrl":"https://doi.org/10.32383/appdr/166509","url":null,"abstract":"Trastuzumab is one of the most commonly used monoclonal antibodies in the treatment of breast cancer. It is effective because it binds to the HER2 receptor and inhibits the signaling pathways for proliferation and metastasis. However, intrinsic or acquired resistance resulting from the various signaling pathways of heterogeneous breast cancer reduces its efficacy. To increase its efficacy, it is combined with different agents in the treatment. In this study, the synergistic effect of the combination of trastuzumab and gambogic acid on the breast cell line MDA-MB -453 was investigated in vitro. At the end of 12-, 24-, 48-, and 72-hour incubation, their antiproliferative effects were determined by XTT method. Combination Index (CI) values of the study were calculated using CompuSyn.exe software. The highest synergistic effect was obtained with 12.5 µg/mL trastuzumab + 1.25 µM gambogic acid (CI-4) at the 72nd hour. The activity of the antioxidant enzyme catalase (CAT) was also measured for the applications. We observed that combination of trastuzumab and gambogic acid decreased CAT activity at 24, 48 and 72nd hours. It was concluded that gambogic acid may be a good candidate for combination with other agents in targeted drug design.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48888108","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}
Muscle atrophy is a common complication in diabetes mellitus. Gallic acid (GA) possesses multiple biologic effects in hyperglycemia and muscle functions. However, whether GA can ameliorate muscular dystrophy during diabetes is unknown. Our data demonstrated GA alleviated muscle dysfunction by promoting myocyte area and grip strength. In serum, GA enhanced T-AOC, SOD and CAT levels, and reduced MDA, TNF-α and IL-6 levels. In gastrocnemius, GA restrained protein degradation by mitigating F-box protein 32 (FBXO-32) and tripartite motif-containing 63 (TRIM-63) expressions. The mechanism of GA against diabetes-associated muscle atrophy is closely linked to its regulations on endoplasmic reticulum stress by attenuating DDIT-3 (DNA-damage inducible transcript 3) and heat shock protein 5 (HSPA-5) expressions. Moreover, GA improved mitochondria bioactivity by enhancing nuclear respiratory factor 1 (NRF-1) and PPARG coactivator 1 alpha (PGC-1α) expressions. Lastly, GA suppressed apoptosis by increasing BCL2-associated X protein (BAX) expressions and decreasing BCL2 apoptosis regulator (BCL-2) expressions. In conclusion, GA prevented from diabetic myopathy via its regulations of endoplasmic reticulum stress, mitochondria function and apoptosis. These data suggested GA could be a newer strategy against diabetic muscle atrophy.
{"title":"Protective effect of gallic acid on muscle atrophy and grip strength in diabetic mice","authors":"Xianchu Liu, Ming-xue Liu","doi":"10.32383/appdr/167031","DOIUrl":"https://doi.org/10.32383/appdr/167031","url":null,"abstract":"Muscle atrophy is a common complication in diabetes mellitus. Gallic acid (GA) possesses multiple biologic effects in hyperglycemia and muscle functions. However, whether GA can ameliorate muscular dystrophy during diabetes is unknown. Our data demonstrated GA alleviated muscle dysfunction by promoting myocyte area and grip strength. In serum, GA enhanced T-AOC, SOD and CAT levels, and reduced MDA, TNF-α and IL-6 levels. In gastrocnemius, GA restrained protein degradation by mitigating F-box protein 32 (FBXO-32) and tripartite motif-containing 63 (TRIM-63) expressions. The mechanism of GA against diabetes-associated muscle atrophy is closely linked to its regulations on endoplasmic reticulum stress by attenuating DDIT-3 (DNA-damage inducible transcript 3) and heat shock protein 5 (HSPA-5) expressions. Moreover, GA improved mitochondria bioactivity by enhancing nuclear respiratory factor 1 (NRF-1) and PPARG coactivator 1 alpha (PGC-1α) expressions. Lastly, GA suppressed apoptosis by increasing BCL2-associated X protein (BAX) expressions and decreasing BCL2 apoptosis regulator (BCL-2) expressions. In conclusion, GA prevented from diabetic myopathy via its regulations of endoplasmic reticulum stress, mitochondria function and apoptosis. These data suggested GA could be a newer strategy against diabetic muscle atrophy.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46839056","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}
Expression of recombinant paraoxonase 1 (PON1) in the human embryonic kidney (HEK293F) cell line was evaluated. Two recombinant human PON1 proteins were investigated: PON1-Fc, which has an Fc-tag on its C-terminal, and His-PON1-Fc, which has an Fc-tag on its C-terminal and histidine on its N-terminal. The influence of high and low-density lipoproteins, copper ions, iron ions, and thiolactone homocysteine, on arylesterase and lactonase activities of PON1 in human serum was examined. Two activities of PON1, arylesterase and lactonase, were measured using earlier elaborated kinetic spectrophotometric method with temperature control at 37°C using the water thermostated cuvette holder. It was demonstrated that the HEK293F expression platform is useful for obtaining recombinant human PON1 protein. Also, addition of high-density lipoprotein increased serum arylesterase and lactonase activity of PON1 to a greater extent than the addition of PON1-Fc or HisPON1-Fc recombinant proteins. In contrast, the addition of high-density lipoprotein to samples containing PON1-Fc or His-PON1-Fc did not increase PON1 activities, while low-density lipoprotein, copper ions, and iron ions, depressed PON1 arylesterase and lactonase activity. Obtained results indicated that it may be advantageous to stimulate PON1 activities rather than supplement with endogenous PON1 protein and HDL, which could be an interesting direction for further study. Furthermore, the work has highlighted some potential research directions for the use of PON1 as a therapeutic molecules. Nevertheless, the study had some limitations and should therefore be treated as a preliminary study.
{"title":"Expression of paraoxonase 1 in HEK293 cells and its effect on lactonase and arylesterase activity in samples containing human serum and/or prooxidant or antioxidant agents - a preliminary study","authors":"A. Bizoń, A. Piwowar","doi":"10.32383/appdr/163453","DOIUrl":"https://doi.org/10.32383/appdr/163453","url":null,"abstract":"Expression of recombinant paraoxonase 1 (PON1) in the human embryonic kidney (HEK293F) cell line was evaluated. Two recombinant human PON1 proteins were investigated: PON1-Fc, which has an Fc-tag on its C-terminal, and His-PON1-Fc, which has an Fc-tag on its C-terminal and histidine on its N-terminal. The influence of high and low-density lipoproteins, copper ions, iron ions, and thiolactone homocysteine, on arylesterase and lactonase activities of PON1 in human serum was examined. Two activities of PON1, arylesterase and lactonase, were measured using earlier elaborated kinetic spectrophotometric method with temperature control at 37°C using the water thermostated cuvette holder. It was demonstrated that the HEK293F expression platform is useful for obtaining recombinant human PON1 protein. Also, addition of high-density lipoprotein increased serum arylesterase and lactonase activity of PON1 to a greater extent than the addition of PON1-Fc or HisPON1-Fc recombinant proteins. In contrast, the addition of high-density lipoprotein to samples containing PON1-Fc or His-PON1-Fc did not increase PON1 activities, while low-density lipoprotein, copper ions, and iron ions, depressed PON1 arylesterase and lactonase activity. Obtained results indicated that it may be advantageous to stimulate PON1 activities rather than supplement with endogenous PON1 protein and HDL, which could be an interesting direction for further study. Furthermore, the work has highlighted some potential research directions for the use of PON1 as a therapeutic molecules. Nevertheless, the study had some limitations and should therefore be treated as a preliminary study.","PeriodicalId":7147,"journal":{"name":"Acta poloniae pharmaceutica","volume":" ","pages":""},"PeriodicalIF":0.4,"publicationDate":"2023-07-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46419207","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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