Pub Date : 2024-08-09DOI: 10.3390/scipharm92030043
Aline Rocha Vieira, Aline Furtado Oliveira, Fabiana Vieira Lima Solino Pessoa, Beatriz Nogueira Messias de Miranda, A. Baby
Different reaction control methods for producing nano/microstructures of poly(butyl cyanoacrylate) (PBCA) have been studied, focusing on pH and monomer-to-initiator ratios. However, these methods often require multiple steps and reagents. In the synthesis of PBCA microparticles using three versions of micromixers designed with HH geometry and varying numbers of channels (4, 10, and 15), different synthesis formulations were investigated by varying monomer concentrations. PBCA microparticles synthesized with 19.2% (w/w) n-butyl cyanoacrylate (n-BCA) monomer, a residence time of 0.06 s, a flow rate of 78 mL·min−1, and a phase ratio of 45/55 (W/O), exhibited an average diameter of 642.2 nm as determined by dynamic light scattering (DLS) analysis. In contrast, PBCA microparticles synthesized with 5.0% (w/w) n-BCA monomer, the same residence time of 0.06 s, a flow rate of 39 mL·min−1, and a phase ratio of 20/80 (W/O), exhibited an average diameter of 74.73 µm according to laser diffraction particle size analysis. Polymer formation was confirmed by Fourier-transform infrared (FTIR) spectroscopy in both formulation and process conditions. These results indicate that the parameters for the production of microparticles with different monomer concentrations in the microfluidic system with HH geometry and 15 channels can be optimized for potential applications in cosmetics and pharmaceutical ingredients.
{"title":"Advances in the Production of PBCA Microparticles Using a Micromixer with HH-Geometry in a Microfluidic System","authors":"Aline Rocha Vieira, Aline Furtado Oliveira, Fabiana Vieira Lima Solino Pessoa, Beatriz Nogueira Messias de Miranda, A. Baby","doi":"10.3390/scipharm92030043","DOIUrl":"https://doi.org/10.3390/scipharm92030043","url":null,"abstract":"Different reaction control methods for producing nano/microstructures of poly(butyl cyanoacrylate) (PBCA) have been studied, focusing on pH and monomer-to-initiator ratios. However, these methods often require multiple steps and reagents. In the synthesis of PBCA microparticles using three versions of micromixers designed with HH geometry and varying numbers of channels (4, 10, and 15), different synthesis formulations were investigated by varying monomer concentrations. PBCA microparticles synthesized with 19.2% (w/w) n-butyl cyanoacrylate (n-BCA) monomer, a residence time of 0.06 s, a flow rate of 78 mL·min−1, and a phase ratio of 45/55 (W/O), exhibited an average diameter of 642.2 nm as determined by dynamic light scattering (DLS) analysis. In contrast, PBCA microparticles synthesized with 5.0% (w/w) n-BCA monomer, the same residence time of 0.06 s, a flow rate of 39 mL·min−1, and a phase ratio of 20/80 (W/O), exhibited an average diameter of 74.73 µm according to laser diffraction particle size analysis. Polymer formation was confirmed by Fourier-transform infrared (FTIR) spectroscopy in both formulation and process conditions. These results indicate that the parameters for the production of microparticles with different monomer concentrations in the microfluidic system with HH geometry and 15 channels can be optimized for potential applications in cosmetics and pharmaceutical ingredients.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.3,"publicationDate":"2024-08-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141922447","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-08-08DOI: 10.3390/scipharm92030042
Evgenia Panou, K. Graikou, N. Tsafantakis, Fanourios-Nikolaos Sakellarakis, I. Chinou
Helianthemum nummularium (HN) and Helianthemum oelanticum subsp. incanum (HO) are plant species, among Cistaceae, that are highly distributed in the Mediterranean region. In the current study, extracts of the aerial parts from both species have been analyzed phytochemically. The non-polar extract analysis resulted in the identification of 15 compounds in each species, mainly terpene and fatty acid derivatives, through GC–MS. The methanolic extract analysis, conducted through UHPLC–MS/MS, led to the identification of 39 metabolites in HN and 29 in HO, respectively, the majority of which were phenolics. Among the identified compounds, several have also been isolated and structurally determined (from HN: rutin, linoleic acid, gallic acid, and isoquercetin, and from HO: quercetin-3-O-(2″-O-galloyl)-galactopyranoside, methyl gallate, catechin-3-O-glucopyranoside, and astragalin, while hyperoside, and cis- and trans-tiliroside have been determined in both species). Furthermore, the methanolic extracts of HN and HO displayed a high total phenolic content (177.2 mg GA/g extract and 150.6 mg GA/g extract, respectively) and considerable free-radical scavenging activity against the DPPH radical (94.6% and 94.0% DPPH inhibition, respectively). Antimicrobial testing showed stronger inhibition of HN against Gram (+) bacterial strains (MIC values 0.07–0.15 mg/mL), while both extracts exhibited low tyrosinase-inhibitory activity. Considering the lack of studies conducted on the chemistry and biological activities of the genus Helianthemum, the chemical characterization of extracts could contribute to new sources of bioactive metabolites to be explored and exploited for further potential applications such as food and/ or the cosmetic industry.
{"title":"Phytochemical Profiling and Biological Activities of Two Helianthemum Species Growing in Greece","authors":"Evgenia Panou, K. Graikou, N. Tsafantakis, Fanourios-Nikolaos Sakellarakis, I. Chinou","doi":"10.3390/scipharm92030042","DOIUrl":"https://doi.org/10.3390/scipharm92030042","url":null,"abstract":"Helianthemum nummularium (HN) and Helianthemum oelanticum subsp. incanum (HO) are plant species, among Cistaceae, that are highly distributed in the Mediterranean region. In the current study, extracts of the aerial parts from both species have been analyzed phytochemically. The non-polar extract analysis resulted in the identification of 15 compounds in each species, mainly terpene and fatty acid derivatives, through GC–MS. The methanolic extract analysis, conducted through UHPLC–MS/MS, led to the identification of 39 metabolites in HN and 29 in HO, respectively, the majority of which were phenolics. Among the identified compounds, several have also been isolated and structurally determined (from HN: rutin, linoleic acid, gallic acid, and isoquercetin, and from HO: quercetin-3-O-(2″-O-galloyl)-galactopyranoside, methyl gallate, catechin-3-O-glucopyranoside, and astragalin, while hyperoside, and cis- and trans-tiliroside have been determined in both species). Furthermore, the methanolic extracts of HN and HO displayed a high total phenolic content (177.2 mg GA/g extract and 150.6 mg GA/g extract, respectively) and considerable free-radical scavenging activity against the DPPH radical (94.6% and 94.0% DPPH inhibition, respectively). Antimicrobial testing showed stronger inhibition of HN against Gram (+) bacterial strains (MIC values 0.07–0.15 mg/mL), while both extracts exhibited low tyrosinase-inhibitory activity. Considering the lack of studies conducted on the chemistry and biological activities of the genus Helianthemum, the chemical characterization of extracts could contribute to new sources of bioactive metabolites to be explored and exploited for further potential applications such as food and/ or the cosmetic industry.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.3,"publicationDate":"2024-08-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141929710","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-17DOI: 10.3390/scipharm92030039
Erick Diaz-Morales, Ana Paola Pacheco-Hermosilla, Daniel Esteban Castro-Mangonez, Nerlys Pajaro-Castro
Objectives: In this retrospective observational study, the aim is to establish how the implementation of the use of antimicrobial stewardship programs at the hospital and intensive care unit level in a Sucre Clinic in Sincelejo has had a significant impact on the improvement of the rational use of antibiotics, due to the alarming situation of increasing antibiotic resistance. Materials and methods: The methodology used was to analyze the Excel database of the Clinic in such a way as to compare the data from 2017, the period prior to the implementation of the antimicrobial stewardship program (ASP), with the subsequent evolution between the years 2018 and 2022, in relation to the institutional records of four antibiotics—ceftriaxone3, ciprofloxacin4, meropenem5, and vancomycin6, measured in defined daily dose (DDD). Results: According to the defined daily dose values obtained for the four antibiotics, a reduction in the defined daily dose was identified in the post-implementation period. On the other hand, considering the DDD reported by the World Health Organization for each of the antibiotics, significant differences were verified in comparison with those obtained in the clinic in the hospitalization and intensive care unit services. Conclusions: In conclusion, in the clinic, a reduction in the defined daily dose was verified in the period after the implementation of the antimicrobial stewardship program compared to the previous period, both in the hospitalization and intensive care unit, as well as having a mild-to-large effect with Cohen’s D.
{"title":"Implementation of an Antimicrobial Stewardship Program at the Hospital and ICU Level of a Clinic in Sincelejo-Sucre","authors":"Erick Diaz-Morales, Ana Paola Pacheco-Hermosilla, Daniel Esteban Castro-Mangonez, Nerlys Pajaro-Castro","doi":"10.3390/scipharm92030039","DOIUrl":"https://doi.org/10.3390/scipharm92030039","url":null,"abstract":"Objectives: In this retrospective observational study, the aim is to establish how the implementation of the use of antimicrobial stewardship programs at the hospital and intensive care unit level in a Sucre Clinic in Sincelejo has had a significant impact on the improvement of the rational use of antibiotics, due to the alarming situation of increasing antibiotic resistance. Materials and methods: The methodology used was to analyze the Excel database of the Clinic in such a way as to compare the data from 2017, the period prior to the implementation of the antimicrobial stewardship program (ASP), with the subsequent evolution between the years 2018 and 2022, in relation to the institutional records of four antibiotics—ceftriaxone3, ciprofloxacin4, meropenem5, and vancomycin6, measured in defined daily dose (DDD). Results: According to the defined daily dose values obtained for the four antibiotics, a reduction in the defined daily dose was identified in the post-implementation period. On the other hand, considering the DDD reported by the World Health Organization for each of the antibiotics, significant differences were verified in comparison with those obtained in the clinic in the hospitalization and intensive care unit services. Conclusions: In conclusion, in the clinic, a reduction in the defined daily dose was verified in the period after the implementation of the antimicrobial stewardship program compared to the previous period, both in the hospitalization and intensive care unit, as well as having a mild-to-large effect with Cohen’s D.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.3,"publicationDate":"2024-07-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141829393","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-15DOI: 10.3390/scipharm92030038
Serap Ozkaya Gul, Alaaddin Korkut, Esra Aydemir
Background: Depression is a common mood disorder that manifests itself simultaneously with chronic diseases. It is especially common in patients diagnosed with cancer, and when neglected, it reduces the success of cancer treatment. The fact that breast cancer is the most common type of cancer in women shows that the treatment of depression in women with cancer is very important. As a result, cancer patients undergoing chemotherapy in oncology units also use antidepressants simultaneously. It is critical to correctly understand the interactions between drugs used in combination. Method: In this study, doses were prepared for MCF7 and MDAMB-231 cell lines by serial dilution from 1000 ng/mL to 1.95 ng/mL. Cell viability was calculated with the WST-1 kit by applying the prepared doses of capecitabine and sertraline alone. In the sertraline/capecitabine combination study, cell viability was examined in MDAMB-231 and MCF-7 cells by applying doses of 300, 100, 50, 25, 10 ng/mL. Combinations that showed selective cytotoxicity after the combination were analyzed with the CompuSyn program and the combination index (CI<1 = synergism) was calculated. Studies on caspase 3-8-9, DNA fragmentation and mTOR were continued using a combination that showed a synergistic effect. Result: It was determined that compared to drug use alone, the sertraline/capecitabine combination decreased cell viability. There is no significant difference in caspase-3,-8,-9 and DNA fragmentation in cancer cells, but there is a reduction in the level of mTOR. This suggests that the death mechanism may be autophagy. Docking studies with autophagy pathway-related proteins further support our results. It is noteworthy that the AKT1-sertraline complex had the best binding affinity among the target proteins (−9.1 kcal/mol).
{"title":"Combined Effect of Sertraline and Capecitabine on Breast Cancer Cell Lines In Vitro and In Silico Evidence for Synergistic Interaction","authors":"Serap Ozkaya Gul, Alaaddin Korkut, Esra Aydemir","doi":"10.3390/scipharm92030038","DOIUrl":"https://doi.org/10.3390/scipharm92030038","url":null,"abstract":"Background: Depression is a common mood disorder that manifests itself simultaneously with chronic diseases. It is especially common in patients diagnosed with cancer, and when neglected, it reduces the success of cancer treatment. The fact that breast cancer is the most common type of cancer in women shows that the treatment of depression in women with cancer is very important. As a result, cancer patients undergoing chemotherapy in oncology units also use antidepressants simultaneously. It is critical to correctly understand the interactions between drugs used in combination. Method: In this study, doses were prepared for MCF7 and MDAMB-231 cell lines by serial dilution from 1000 ng/mL to 1.95 ng/mL. Cell viability was calculated with the WST-1 kit by applying the prepared doses of capecitabine and sertraline alone. In the sertraline/capecitabine combination study, cell viability was examined in MDAMB-231 and MCF-7 cells by applying doses of 300, 100, 50, 25, 10 ng/mL. Combinations that showed selective cytotoxicity after the combination were analyzed with the CompuSyn program and the combination index (CI<1 = synergism) was calculated. Studies on caspase 3-8-9, DNA fragmentation and mTOR were continued using a combination that showed a synergistic effect. Result: It was determined that compared to drug use alone, the sertraline/capecitabine combination decreased cell viability. There is no significant difference in caspase-3,-8,-9 and DNA fragmentation in cancer cells, but there is a reduction in the level of mTOR. This suggests that the death mechanism may be autophagy. Docking studies with autophagy pathway-related proteins further support our results. It is noteworthy that the AKT1-sertraline complex had the best binding affinity among the target proteins (−9.1 kcal/mol).","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.3,"publicationDate":"2024-07-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141648301","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-07-04DOI: 10.3390/scipharm92030037
S. Dimitrova, S. Dragomanova, G. Kehayova
In recent years, an innovative approach has emerged in the field of toxicology for managing acute intoxications caused by lipophilic substances: intravenous lipid emulsions (ILEs). Through numerous experiments and case reports, the efficacy of lipid emulsions in counteracting toxicities induced by lipophilic agents, including a significant number of antiepileptic (AE) drugs, have become increasingly evident. Data spanning a 10-year period (2010–2020) were analyzed by searching through multiple scientific publication platforms like PubMed, Science Direct, Research Gate, and Springer Link. This study focused on reviewing relevant case reports detailing successful intravenous lipid emulsion (ILE) administration in patients with acute intoxications with antiepileptics, specifically examining the impact of fat emulsions on neurological status, Glasgow Coma Scale (GCS) scores, and corrected QT interval concerning hemodynamic instability. The typical symptoms of antiepileptic toxicity include central nervous system depression, ataxia, and nystagmus. Intravenous lipid emulsion application resulted in an increase in Glasgow Coma Scale scores and enhanced recovery from drug intoxication. This study provides a comprehensive overview of the potential utility of ILE as a component to antidote therapy in cases of acute AE poisoning involving neurotropic drugs. The process involves the engagement of various mechanisms of antitoxic activity.
近年来，毒理学领域出现了一种创新方法来治疗亲脂性物质引起的急性中毒：静脉注射脂质乳剂（ILEs）。通过大量实验和病例报告，脂质乳剂在对抗亲脂性药物（包括大量抗癫痫（AE）药物）引起的中毒方面的功效日益明显。本研究通过搜索 PubMed、Science Direct、Research Gate 和 Springer Link 等多个科学出版物平台，分析了 10 年间（2010-2020 年）的数据。本研究重点回顾了相关病例报告，这些报告详细介绍了抗癫痫药物急性中毒患者成功静脉注射脂质乳剂（ILE）的情况，特别考察了脂质乳剂对神经系统状态、格拉斯哥昏迷量表（GCS）评分以及有关血液动力学不稳定的校正 QT 间期的影响。抗癫痫药物中毒的典型症状包括中枢神经系统抑制、共济失调和眼球震颤。静脉注射脂质乳剂可提高格拉斯哥昏迷量表评分，促进药物中毒的恢复。这项研究全面概述了 ILE 作为解毒剂治疗急性 AE 中毒（涉及神经刺激性药物）病例的潜在作用。这一过程涉及多种解毒机制。
{"title":"Intravenous Lipid Emulsions in Anticonvulsants’ Toxicity","authors":"S. Dimitrova, S. Dragomanova, G. Kehayova","doi":"10.3390/scipharm92030037","DOIUrl":"https://doi.org/10.3390/scipharm92030037","url":null,"abstract":"In recent years, an innovative approach has emerged in the field of toxicology for managing acute intoxications caused by lipophilic substances: intravenous lipid emulsions (ILEs). Through numerous experiments and case reports, the efficacy of lipid emulsions in counteracting toxicities induced by lipophilic agents, including a significant number of antiepileptic (AE) drugs, have become increasingly evident. Data spanning a 10-year period (2010–2020) were analyzed by searching through multiple scientific publication platforms like PubMed, Science Direct, Research Gate, and Springer Link. This study focused on reviewing relevant case reports detailing successful intravenous lipid emulsion (ILE) administration in patients with acute intoxications with antiepileptics, specifically examining the impact of fat emulsions on neurological status, Glasgow Coma Scale (GCS) scores, and corrected QT interval concerning hemodynamic instability. The typical symptoms of antiepileptic toxicity include central nervous system depression, ataxia, and nystagmus. Intravenous lipid emulsion application resulted in an increase in Glasgow Coma Scale scores and enhanced recovery from drug intoxication. This study provides a comprehensive overview of the potential utility of ILE as a component to antidote therapy in cases of acute AE poisoning involving neurotropic drugs. The process involves the engagement of various mechanisms of antitoxic activity.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.3,"publicationDate":"2024-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141678979","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-07DOI: 10.3390/scipharm92020032
Marilia Amável Gomes Soares, F. Souza-Silva, Carlos Roberto Alves, Leonardo Vazquez, T. S. de Araújo, Carlos Serpa, O. A. Chaves
Cardiovascular diseases (CVDs), especially arterial hypertension, stand as prominent contributors to global mortality. Regrettably, individuals with diabetes encounter a two-fold increase in the risk of mortality associated with CVDs. Hydrochlorothiazide (HCTZ) represents a primary intervention for hypertension, particularly in diabetic patients. Nevertheless, there has not yet been a comprehensive assessment of the biophysical characteristics regarding the impact of glucose levels on its binding affinity with human serum albumin (HSA). Thus, the present work reports the interactive profile of HSA/HCTZ in nonglycemic, normoglycemic (80 mg/dL), and hyperglycemic (320 mg/dL) conditions by time-resolved fluorescence, saturation transfer difference–nuclear magnetic resonance (STD-NMR), and surface plasmon resonance (SPR). There was a moderate ground state association of HSA/HCTZ with subdomain IIA that was affected in the presence of different glucose levels. The hyperglycemic condition decreased the binding affinity of HCTZ to subdomain IIA and increased the possibility of subdomain IB also being considered as a secondary binding site due to cooperativity and/or alterations in the protein’s structure. Overall, the glucose level under hyperglycemic conditions led to the cavities being more likely to receive more ligands, offering insights into the necessity of glucose control in the human bloodstream to not impact the residence time (pharmacokinetic profile) and pharmacotherapeutic potential of HCTZ.
{"title":"Evidence of Hyperglycemic Levels Improving the Binding Capacity between Human Serum Albumin and the Antihypertensive Drug Hydrochlorothiazide","authors":"Marilia Amável Gomes Soares, F. Souza-Silva, Carlos Roberto Alves, Leonardo Vazquez, T. S. de Araújo, Carlos Serpa, O. A. Chaves","doi":"10.3390/scipharm92020032","DOIUrl":"https://doi.org/10.3390/scipharm92020032","url":null,"abstract":"Cardiovascular diseases (CVDs), especially arterial hypertension, stand as prominent contributors to global mortality. Regrettably, individuals with diabetes encounter a two-fold increase in the risk of mortality associated with CVDs. Hydrochlorothiazide (HCTZ) represents a primary intervention for hypertension, particularly in diabetic patients. Nevertheless, there has not yet been a comprehensive assessment of the biophysical characteristics regarding the impact of glucose levels on its binding affinity with human serum albumin (HSA). Thus, the present work reports the interactive profile of HSA/HCTZ in nonglycemic, normoglycemic (80 mg/dL), and hyperglycemic (320 mg/dL) conditions by time-resolved fluorescence, saturation transfer difference–nuclear magnetic resonance (STD-NMR), and surface plasmon resonance (SPR). There was a moderate ground state association of HSA/HCTZ with subdomain IIA that was affected in the presence of different glucose levels. The hyperglycemic condition decreased the binding affinity of HCTZ to subdomain IIA and increased the possibility of subdomain IB also being considered as a secondary binding site due to cooperativity and/or alterations in the protein’s structure. Overall, the glucose level under hyperglycemic conditions led to the cavities being more likely to receive more ligands, offering insights into the necessity of glucose control in the human bloodstream to not impact the residence time (pharmacokinetic profile) and pharmacotherapeutic potential of HCTZ.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141373788","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-05DOI: 10.3390/scipharm92020031
Łukasz Duda, K. Kłosiński, G. Budryn, Andrzej Jaśkiewicz, D. Kołat, Ż. Kałuzińska-Kołat, Zbigniew Pasieka
The aim of this review is to discuss the numerous health-promoting properties of Cichorium intybus L. and bring together a range of publications to broaden knowledge and encourage further research and consideration of the plant use as treatment for a range of conditions. A comprehensive search of articles in Polish and English from 1986–2022 years was carried out in PubMed, Google Scholar and ScienceDirect using the keywords chicory, Cichorium intybus L., sesquiterpene lactones and their synonyms. Articles were checked for titles, abstracts, and full-text reviews. The first part of the review article discusses chicory, the countries in which it is found, its life cycle or modern cultivation methods, as well as its many uses, which will be discussed in more detail later in the article. The increased interest in plants as medicines or supplements is also briefly mentioned, as well as some limits that are associated with the medical use of plants. In the Results and Discussion section, there is a discussion of the numerous health-promoting properties of Cichorium intybus L. as a whole plant, with its collection of all the components, and we then examine the structure and the individual constituents of Cichorium intybus L. Among these, this article discusses those that can be utilized for causal applications in medicine, including sesquiterpene lactones and polyphenols, mainly known for their anti-cancer properties, although, in this article, their other health-promoting properties are also discussed. The article also examines inulin, a major component of Cichorium intybus L. The Discussion and the Conclusions sections propose directions for more detailed research and the range of factors that may affect specific results, which may have safety implications when used as supplements or medications.
{"title":"Medicinal Use of Chicory (Cichorium intybus L.)","authors":"Łukasz Duda, K. Kłosiński, G. Budryn, Andrzej Jaśkiewicz, D. Kołat, Ż. Kałuzińska-Kołat, Zbigniew Pasieka","doi":"10.3390/scipharm92020031","DOIUrl":"https://doi.org/10.3390/scipharm92020031","url":null,"abstract":"The aim of this review is to discuss the numerous health-promoting properties of Cichorium intybus L. and bring together a range of publications to broaden knowledge and encourage further research and consideration of the plant use as treatment for a range of conditions. A comprehensive search of articles in Polish and English from 1986–2022 years was carried out in PubMed, Google Scholar and ScienceDirect using the keywords chicory, Cichorium intybus L., sesquiterpene lactones and their synonyms. Articles were checked for titles, abstracts, and full-text reviews. The first part of the review article discusses chicory, the countries in which it is found, its life cycle or modern cultivation methods, as well as its many uses, which will be discussed in more detail later in the article. The increased interest in plants as medicines or supplements is also briefly mentioned, as well as some limits that are associated with the medical use of plants. In the Results and Discussion section, there is a discussion of the numerous health-promoting properties of Cichorium intybus L. as a whole plant, with its collection of all the components, and we then examine the structure and the individual constituents of Cichorium intybus L. Among these, this article discusses those that can be utilized for causal applications in medicine, including sesquiterpene lactones and polyphenols, mainly known for their anti-cancer properties, although, in this article, their other health-promoting properties are also discussed. The article also examines inulin, a major component of Cichorium intybus L. The Discussion and the Conclusions sections propose directions for more detailed research and the range of factors that may affect specific results, which may have safety implications when used as supplements or medications.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141382991","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-06-03DOI: 10.3390/scipharm92020030
Yina Montero-Pérez, J. Olivero-Verbel
Acetaminophen (APAP) is a widely used analgesic, especially for children. Its primary mechanism involves inhibiting cyclooxygenase enzymes and activating the endocannabinoid and TRPV1 systems. Though its toxicity is low, it can harm the liver in a dose-dependent manner. Low APAP doses can also increase pollutant-induced liver damage. Little is known about interactions between APAP and benzo[a]pyrene (B[a]P). This study aimed to assess if co-exposure to non-hepatotoxic doses of B[a]P and APAP causes liver injury in mice, exploring the underlying mechanisms. Female ICR mice received 50 mg/kg B[a]P or a vehicle for three days, followed by 200 mg/kg APAP or a vehicle. Liver injury was assessed through histopathological examination, serum transaminase activity, and gene expression analysis. In the B[a]P/APAP group, several histology changes were observed, including ballooning injury, steatosis, necrosis, inflammation, and apoptosis. Transaminase levels correlated with histopathological scores, and there was an increase in hepatic cytochrome P450 family 1 subfamily a member 1 (Cyp1a1) mRNA levels and a decrease in aryl hydrocarbon receptor (Ahr), cytochrome P450 family 2 subfamily e polypeptide 1 (Cyp2e1), superoxide dismutase 1 (Sod1), peroxisome proliferator activated receptor gamma (Ppar-γ), and caspase 3 (Casp3). This suggests that prior exposure to B[a]P makes mice more susceptible to APAP-induced liver injury, involving changes in gene expression related to metabolism, redox balance, and cell proliferation. Therefore, using therapeutic APAP doses after exposure to B[a]P could lead to liver injury.
{"title":"Exposure to Benzo(a)pyrene Enhances Acetaminophen-Induced Liver Injury in Mice at Non-Hepatotoxic Doses","authors":"Yina Montero-Pérez, J. Olivero-Verbel","doi":"10.3390/scipharm92020030","DOIUrl":"https://doi.org/10.3390/scipharm92020030","url":null,"abstract":"Acetaminophen (APAP) is a widely used analgesic, especially for children. Its primary mechanism involves inhibiting cyclooxygenase enzymes and activating the endocannabinoid and TRPV1 systems. Though its toxicity is low, it can harm the liver in a dose-dependent manner. Low APAP doses can also increase pollutant-induced liver damage. Little is known about interactions between APAP and benzo[a]pyrene (B[a]P). This study aimed to assess if co-exposure to non-hepatotoxic doses of B[a]P and APAP causes liver injury in mice, exploring the underlying mechanisms. Female ICR mice received 50 mg/kg B[a]P or a vehicle for three days, followed by 200 mg/kg APAP or a vehicle. Liver injury was assessed through histopathological examination, serum transaminase activity, and gene expression analysis. In the B[a]P/APAP group, several histology changes were observed, including ballooning injury, steatosis, necrosis, inflammation, and apoptosis. Transaminase levels correlated with histopathological scores, and there was an increase in hepatic cytochrome P450 family 1 subfamily a member 1 (Cyp1a1) mRNA levels and a decrease in aryl hydrocarbon receptor (Ahr), cytochrome P450 family 2 subfamily e polypeptide 1 (Cyp2e1), superoxide dismutase 1 (Sod1), peroxisome proliferator activated receptor gamma (Ppar-γ), and caspase 3 (Casp3). This suggests that prior exposure to B[a]P makes mice more susceptible to APAP-induced liver injury, involving changes in gene expression related to metabolism, redox balance, and cell proliferation. Therefore, using therapeutic APAP doses after exposure to B[a]P could lead to liver injury.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-06-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141271268","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-22DOI: 10.3390/scipharm92020028
Ekaterina Naumenko, Ivan Guryanov, M. Gomzikova
The incidence of cancer is growing every year and covers all age groups, including the working population, which makes cancer socially significant. Existing methods of treatment, despite the effectiveness of individual compounds in relation to cancer cells, are not perfect due to a number of side effects associated with high doses that physicians are forced to administer when using treatment protocols. A particularly difficult issue is the creation of effective functional containers that would have the properties of targeting certain types of cells. The solution of this problem is currently relevant, which is reflected in the growth of publications on this subject in recent years. The most promising is the use of nanotechnology in the development of bioengineered therapeutics and containers for chemotherapeutic agents. In this review, we tried to assess the trends that exist in this area of research, as well as show the wide using of some commercially available formulations based on the nano-sized vehicles.
{"title":"Drug Delivery Nano-Platforms for Advanced Cancer Therapy","authors":"Ekaterina Naumenko, Ivan Guryanov, M. Gomzikova","doi":"10.3390/scipharm92020028","DOIUrl":"https://doi.org/10.3390/scipharm92020028","url":null,"abstract":"The incidence of cancer is growing every year and covers all age groups, including the working population, which makes cancer socially significant. Existing methods of treatment, despite the effectiveness of individual compounds in relation to cancer cells, are not perfect due to a number of side effects associated with high doses that physicians are forced to administer when using treatment protocols. A particularly difficult issue is the creation of effective functional containers that would have the properties of targeting certain types of cells. The solution of this problem is currently relevant, which is reflected in the growth of publications on this subject in recent years. The most promising is the use of nanotechnology in the development of bioengineered therapeutics and containers for chemotherapeutic agents. In this review, we tried to assess the trends that exist in this area of research, as well as show the wide using of some commercially available formulations based on the nano-sized vehicles.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-05-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141109439","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-05-20DOI: 10.3390/scipharm92020027
J. Tomović, Aleksandar Kočović, Marijana Anđić, Jovana V Bradic, Nevena Zubić, V. Jakovljević, Miroslav Sovrlić, P. Vasiljević, N. Manojlovic
Lichens, a diverse group of organisms, have a unique structure consisting of fungal filaments and photosynthetic partner cells. This research conducted a comprehensive chemical analysis and evaluation of the anti-inflammatory and antioxidant properties of methanolic and acetone extracts from Umbilicaria crustulosa lichen, along with its isolated metabolites. The process involved separating atranorin and chloratranorin fractions, physodic acid, and gyrophoric acid. Secondary metabolites were identified using chromatographic and spectroscopic data. The total polyphenols content was determined spectrophotometrically. This study examined the antioxidant activity of extracts of the lichen U. crustulosa and the isolated fractions using three methods: DPPH scavenging activity, ABTS scavenging activity, and reducing power. This study also evaluated the acute oral toxicity and the anti-inflammatory activity of the extracts in Wistar albino rats. A higher content of the total phenolic compounds was found in the acetone extract, but antioxidant and anti-inflammatory activities were more prominent in the methanolic extract. The isolated atranorin and chloratranorin fractions and compound physodic acid showed the highest antioxidant activity. No toxic effects were noted in the acute oral toxicity study. This study highlights the potential of the investigated lichen as a valuable source of novel biological agents.
地衣是一种多种多样的生物，具有由真菌菌丝和光合作用伴侣细胞组成的独特结构。这项研究对甲醇和丙酮提取物进行了全面的化学分析，并评估了甲壳鞘氨醇地衣及其分离代谢物的抗炎和抗氧化特性。这一过程包括分离阿曲霉素和氯曲霉素馏分、物理酸和石膏酸。利用色谱和光谱数据对次生代谢物进行了鉴定。总多酚含量采用分光光度法测定。本研究采用三种方法检测了地衣 U. crustulosa 提取物和分离馏分的抗氧化活性：DPPH 清除活性、ABTS 清除活性和还原力。该研究还评估了提取物对 Wistar 白化大鼠的急性口服毒性和抗炎活性。丙酮提取物中总酚类化合物的含量较高，但甲醇提取物的抗氧化和抗炎活性更为突出。分离出的阿曲霉苷和氯曲霉苷馏分以及复合物理酸显示出最高的抗氧化活性。在急性口服毒性研究中未发现任何毒性作用。这项研究凸显了所研究地衣作为新型生物制剂宝贵来源的潜力。
{"title":"Bioactive Components Analysis and Pharmacological Properties of Extracts and Metabolites of Lichen Umbilicaria crustulosa","authors":"J. Tomović, Aleksandar Kočović, Marijana Anđić, Jovana V Bradic, Nevena Zubić, V. Jakovljević, Miroslav Sovrlić, P. Vasiljević, N. Manojlovic","doi":"10.3390/scipharm92020027","DOIUrl":"https://doi.org/10.3390/scipharm92020027","url":null,"abstract":"Lichens, a diverse group of organisms, have a unique structure consisting of fungal filaments and photosynthetic partner cells. This research conducted a comprehensive chemical analysis and evaluation of the anti-inflammatory and antioxidant properties of methanolic and acetone extracts from Umbilicaria crustulosa lichen, along with its isolated metabolites. The process involved separating atranorin and chloratranorin fractions, physodic acid, and gyrophoric acid. Secondary metabolites were identified using chromatographic and spectroscopic data. The total polyphenols content was determined spectrophotometrically. This study examined the antioxidant activity of extracts of the lichen U. crustulosa and the isolated fractions using three methods: DPPH scavenging activity, ABTS scavenging activity, and reducing power. This study also evaluated the acute oral toxicity and the anti-inflammatory activity of the extracts in Wistar albino rats. A higher content of the total phenolic compounds was found in the acetone extract, but antioxidant and anti-inflammatory activities were more prominent in the methanolic extract. The isolated atranorin and chloratranorin fractions and compound physodic acid showed the highest antioxidant activity. No toxic effects were noted in the acute oral toxicity study. This study highlights the potential of the investigated lichen as a valuable source of novel biological agents.","PeriodicalId":21601,"journal":{"name":"Scientia Pharmaceutica","volume":null,"pages":null},"PeriodicalIF":2.5,"publicationDate":"2024-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141122764","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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