C. Schön, R. Wacker, M. Rothe, B. Lipowicz, A. Iphöfer
In case of exocrine pancreatic insufficiency (EPI), the replacement of digestive enzymes with, for example porcine pancreatin or fungal rizoenzymes, is unavoidable under certain conditions. Current guidelines indicate that preparations from porcine pancreas have more advantageous physicochemical properties compared to those from fungi, especially at high bile salt concentrations, and that the latter can, therefore, only be used clinically to a limited extent. Since rizoenzymes are increasingly used in clinical practice, the present in vitro study investigated efficiency of enzymatic activity of rizoenzymes in comparison to pancreatin under various physiological and partly extreme environmental conditions. The lipolytic properties of two typical preparations containing digestive enzymes from porcine pancreatin and rizoenzymes were compared (same dosage of activity units) at different pH values (pH 3–9), with the addition of different bile salt concentrations (0–15 mmol/L sodium taurocholate). Lipolytic activity was measured by quantifying the fatty acids released from olive oil substrate by liquid chromatography–tandem mass spectrometry after enzymatic digestion. For both enzyme preparations, the lipolytic activity maximum was reached at pH 7 with comparable fatty acid conversion rates (57% pancreatin, 58% rizoenzymes). However, in contrast to pancreatin, rizoenzymes were already active for certain fatty acids from pH 3 to 4. At a bile salt concentration up to 10 mmol/L taurocholate, there was an increase in activity of both enzyme preparations (rizoenzymes 69% vs. pancreatin 58% enzymatic conversion). Only at rather unphysiological concentration of 15 mmol/L during EPI, there was a slight decrease in activity (to 56%) for the rizoenzymes. Rizoenzymes are an alternative therapeutic option for EPI. Relevant differences between rizoenzymes and pancreatin with regard to lipolytic activity under different physicochemical conditions could not be demonstrated in this study, whereas a potential advantage in favor of rizoenzymes activity at already low pH values was observed.
{"title":"Characterisation of the lipolytic enzymatic activities of fungal rizoenzymes from Rhizopus oryzae in comparison to pancreatin from pigs","authors":"C. Schön, R. Wacker, M. Rothe, B. Lipowicz, A. Iphöfer","doi":"10.2478/afpuc-2024-0009","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0009","url":null,"abstract":"\u0000 \u0000 \u0000 In case of exocrine pancreatic insufficiency (EPI), the replacement of digestive enzymes with, for example porcine pancreatin or fungal rizoenzymes, is unavoidable under certain conditions. Current guidelines indicate that preparations from porcine pancreas have more advantageous physicochemical properties compared to those from fungi, especially at high bile salt concentrations, and that the latter can, therefore, only be used clinically to a limited extent. Since rizoenzymes are increasingly used in clinical practice, the present in vitro study investigated efficiency of enzymatic activity of rizoenzymes in comparison to pancreatin under various physiological and partly extreme environmental conditions.\u0000 \u0000 \u0000 \u0000 The lipolytic properties of two typical preparations containing digestive enzymes from porcine pancreatin and rizoenzymes were compared (same dosage of activity units) at different pH values (pH 3–9), with the addition of different bile salt concentrations (0–15 mmol/L sodium taurocholate). Lipolytic activity was measured by quantifying the fatty acids released from olive oil substrate by liquid chromatography–tandem mass spectrometry after enzymatic digestion.\u0000 \u0000 \u0000 \u0000 For both enzyme preparations, the lipolytic activity maximum was reached at pH 7 with comparable fatty acid conversion rates (57% pancreatin, 58% rizoenzymes). However, in contrast to pancreatin, rizoenzymes were already active for certain fatty acids from pH 3 to 4. At a bile salt concentration up to 10 mmol/L taurocholate, there was an increase in activity of both enzyme preparations (rizoenzymes 69% vs. pancreatin 58% enzymatic conversion). Only at rather unphysiological concentration of 15 mmol/L during EPI, there was a slight decrease in activity (to 56%) for the rizoenzymes.\u0000 \u0000 \u0000 \u0000 Rizoenzymes are an alternative therapeutic option for EPI. Relevant differences between rizoenzymes and pancreatin with regard to lipolytic activity under different physicochemical conditions could not be demonstrated in this study, whereas a potential advantage in favor of rizoenzymes activity at already low pH values was observed.\u0000","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-08-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141921013","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}
E. Sulastri, Y. Yusriadi, M. Ma’rifa, M. Mulyani, N. Aanisah
Abstract Background White-water yam (Dioscorea alata L.) is one of the potential sources of starch; however, it is not yet available for commercial purposes. Besides, native white-water yam starch (WS) presents limited functionality due to poor flowability, mechanical properties and instability at high temperature and acidic conditions. Therefore, this study aims to modify the starch to improve its characteristics and make it useful as an excipient for the preparation of the tablets. Materials and methods The modification of WS was achieved by physical and chemical treatments, specifically pre-gelatinization and phosphorylation, respectively. Pre-gelatinization WS involves heating, meanwhile phosphorylation WS is obtained by treating WS with sodium tripolyphosphate. Results The results showed that the powder of the modified WS has good characteristics which improved the flowability of the powder mixture as a granule based on density, porosity, compressibility index and swelling power determination. The WS granules were found to display the oval or irregular (polygonal) shape with the amylose content 11.92±0.61% for unmodified WS, 10.41±0.90% for pre-gelatinized WS and 12.61±1.75% for phosphorylated WS. Furthermore, the granule was formulated as an excipient in tablet preparations, and the formulas were compressed after wet granulation. The mechanical properties of the tablets were assessed using uniformity of mass and size, hardness, friability and disintegration time. WS modification affects the hardness of tablets when used as a binder. Phosphorylated WS is recommended to be used as a binder in wet granulation formulations because it produces tablets with a longer disintegration time, which means better binding ability. However, the utilization of modified WS with both pre-gelatinization and phosphorylation leads to tablets with low brittleness compared to others with unmodified binder with the disintegration time still met the requirement of fast disintegrating tablet (<15 minutes). Conclusion All the physical properties studied indicated that the modified WS is a promising pharmaceutical excipient in tablets.
{"title":"Physicochemical properties of tablet dosage form based on pre-gelatinized- and phosphorylated-modified starches from white-water yam (Dioscorea alata L.)","authors":"E. Sulastri, Y. Yusriadi, M. Ma’rifa, M. Mulyani, N. Aanisah","doi":"10.2478/afpuc-2024-0007","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0007","url":null,"abstract":"Abstract Background White-water yam (Dioscorea alata L.) is one of the potential sources of starch; however, it is not yet available for commercial purposes. Besides, native white-water yam starch (WS) presents limited functionality due to poor flowability, mechanical properties and instability at high temperature and acidic conditions. Therefore, this study aims to modify the starch to improve its characteristics and make it useful as an excipient for the preparation of the tablets. Materials and methods The modification of WS was achieved by physical and chemical treatments, specifically pre-gelatinization and phosphorylation, respectively. Pre-gelatinization WS involves heating, meanwhile phosphorylation WS is obtained by treating WS with sodium tripolyphosphate. Results The results showed that the powder of the modified WS has good characteristics which improved the flowability of the powder mixture as a granule based on density, porosity, compressibility index and swelling power determination. The WS granules were found to display the oval or irregular (polygonal) shape with the amylose content 11.92±0.61% for unmodified WS, 10.41±0.90% for pre-gelatinized WS and 12.61±1.75% for phosphorylated WS. Furthermore, the granule was formulated as an excipient in tablet preparations, and the formulas were compressed after wet granulation. The mechanical properties of the tablets were assessed using uniformity of mass and size, hardness, friability and disintegration time. WS modification affects the hardness of tablets when used as a binder. Phosphorylated WS is recommended to be used as a binder in wet granulation formulations because it produces tablets with a longer disintegration time, which means better binding ability. However, the utilization of modified WS with both pre-gelatinization and phosphorylation leads to tablets with low brittleness compared to others with unmodified binder with the disintegration time still met the requirement of fast disintegrating tablet (<15 minutes). Conclusion All the physical properties studied indicated that the modified WS is a promising pharmaceutical excipient in tablets.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-06-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141370256","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}
Abstract Objective The objective of the present investigation is to improve the solubility of valsartan and prepare immediate release tablets. Materials and methods To increase the solubility and bioavailability of valsartan, a low-soluble antihypertensive drug, immediate release dosage forms were formulated by a direct compression method using a solid dispersion technique with three different carriers (β-cyclodextrin, polyvinyl pyrrolidone K30 and poloxamer 188) at three different ratios (1:3, 1:4 and 1:5). Nine physical mixtures (PM1–PM9) were prepared and various physical parameters were characterised in in vitro release studies. Results Out of the prepared physical mixtures, PM8 showed the best results, with 94.2% of the drug dissolving within 30 min. Formulation PM8 solid dispersion further used for the preparation of valsartan immediate release tablets by using sodium starch glycolate superdisintegrant, at different concentrations (3%, 4% and 5%; i.e., IF1, IF2 and IF3 formulations, respectively). The optimised formulation showed friability and disintegration values of 0.456±0.9 and 6.2±0.4 min. Among the three immediate release formulations, IF2, which contains 4% sodium starch glycolate, demonstrated an 84.46% drug release in 30 min and a 99.69% drug release in 1 hr, indicating increased drug solubility. When compared with a valsartan pure drug, the solubility of the solid dispersion increased by 135.06-fold. Discussion and conclusion The results show that the optimised IF2 formulation demonstrated enhanced drug solubility by 135.06-fold, using a solid dispersion technique with poloxamer 188. This can be explained by the conversion of crystalline to an amorphous form of drug, leading to a reduction in the contact angle between the drug and the gastric medium. It can be concluded that poloxamer 188 is a suitable carrier and that use of a physical mixture technique is an applicable method to improve the solubility of valsartan.
{"title":"Development and Characterisation of Valsartan Immediate Release Dosage Form Using Solubility Enhancement Technique","authors":"R. Saripilli, P. Teella, K. Nataraj","doi":"10.2478/afpuc-2024-0005","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0005","url":null,"abstract":"Abstract Objective The objective of the present investigation is to improve the solubility of valsartan and prepare immediate release tablets. Materials and methods To increase the solubility and bioavailability of valsartan, a low-soluble antihypertensive drug, immediate release dosage forms were formulated by a direct compression method using a solid dispersion technique with three different carriers (β-cyclodextrin, polyvinyl pyrrolidone K30 and poloxamer 188) at three different ratios (1:3, 1:4 and 1:5). Nine physical mixtures (PM1–PM9) were prepared and various physical parameters were characterised in in vitro release studies. Results Out of the prepared physical mixtures, PM8 showed the best results, with 94.2% of the drug dissolving within 30 min. Formulation PM8 solid dispersion further used for the preparation of valsartan immediate release tablets by using sodium starch glycolate superdisintegrant, at different concentrations (3%, 4% and 5%; i.e., IF1, IF2 and IF3 formulations, respectively). The optimised formulation showed friability and disintegration values of 0.456±0.9 and 6.2±0.4 min. Among the three immediate release formulations, IF2, which contains 4% sodium starch glycolate, demonstrated an 84.46% drug release in 30 min and a 99.69% drug release in 1 hr, indicating increased drug solubility. When compared with a valsartan pure drug, the solubility of the solid dispersion increased by 135.06-fold. Discussion and conclusion The results show that the optimised IF2 formulation demonstrated enhanced drug solubility by 135.06-fold, using a solid dispersion technique with poloxamer 188. This can be explained by the conversion of crystalline to an amorphous form of drug, leading to a reduction in the contact angle between the drug and the gastric medium. It can be concluded that poloxamer 188 is a suitable carrier and that use of a physical mixture technique is an applicable method to improve the solubility of valsartan.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141371288","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}
O. Maslov, M. Komisarenko, S. Ponomarenko, S. Kolisnyk, T. Osolodchenko, M. Golik
Abstract Aim To determine the content of phenolcarboxylic acids using gas chromatography–mass spectrometer (GC–MS) in the obtained extract, conduct a study of the antimicrobial, antifungal, and antioxidant activities of Rubus idaeus shoot lipophilic extract. Material/methods The quantification of phenolcarboxylic was accomplished through GC–MS, antioxidant activity was assessed by potentiometric method, antimicrobial and antifungal activities were determined by well method. Results The 8 compounds were identified by the GC–MS method. The vanillic acid (2.59 ± 0.08 mg/100 g), benzoic acid (1.51±0.08 mg/100 g), and ferulic acid (0.79±0.04 mg/100 g) dominated in the obtained lipophilic R. idaeus shoot extract. Bacillus subtilis (17.00 ± 0.50 mm) was the most sensitive to lipophilic extract, whereas Proteus vulgaris was the most resistant to the lipophilic extract. Moreover, Candida albicans was medium sensitive to lipophilic extract (13.50 ± 0.50 mm). The antioxidant activity was 1.00 mmol-equiv./mdry res; according to Maslov's antioxidant level classification it has low level. Conclusions The lipophilic extract from R. idaeus shoots contains various phenolcarboxylic acids, including vanillic acid, benzoic acid, ferulic acid, p-hydroxybenzoic acid, syringic acid, gentisic acid, salicylic acid, and phenylacetic acid, with the highest concentrations observed for vanillic, benzoic, and ferulic acids. This study highlights the antimicrobial and antifungal properties of the R. idaeus shoot lipophilic extract. However, the obtained lipophilic extract showed a relatively low level of antioxidant activity. Consequently, the derivatives of phenolcarboxylic acids play a substantial role in the antimicrobial and antifungal effects, whereas their contribution to antioxidant activity appears to be limited.
{"title":"Antimicrobial, Antifungal, Antioxidant Activity and Phytochemical Investigation of Phenolcarboxylic Acids by GC–MS of Raspberry (Rubus idaeus L.) Shoot Lipophilic Extract","authors":"O. Maslov, M. Komisarenko, S. Ponomarenko, S. Kolisnyk, T. Osolodchenko, M. Golik","doi":"10.2478/afpuc-2024-0006","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0006","url":null,"abstract":"Abstract Aim To determine the content of phenolcarboxylic acids using gas chromatography–mass spectrometer (GC–MS) in the obtained extract, conduct a study of the antimicrobial, antifungal, and antioxidant activities of Rubus idaeus shoot lipophilic extract. Material/methods The quantification of phenolcarboxylic was accomplished through GC–MS, antioxidant activity was assessed by potentiometric method, antimicrobial and antifungal activities were determined by well method. Results The 8 compounds were identified by the GC–MS method. The vanillic acid (2.59 ± 0.08 mg/100 g), benzoic acid (1.51±0.08 mg/100 g), and ferulic acid (0.79±0.04 mg/100 g) dominated in the obtained lipophilic R. idaeus shoot extract. Bacillus subtilis (17.00 ± 0.50 mm) was the most sensitive to lipophilic extract, whereas Proteus vulgaris was the most resistant to the lipophilic extract. Moreover, Candida albicans was medium sensitive to lipophilic extract (13.50 ± 0.50 mm). The antioxidant activity was 1.00 mmol-equiv./mdry res; according to Maslov's antioxidant level classification it has low level. Conclusions The lipophilic extract from R. idaeus shoots contains various phenolcarboxylic acids, including vanillic acid, benzoic acid, ferulic acid, p-hydroxybenzoic acid, syringic acid, gentisic acid, salicylic acid, and phenylacetic acid, with the highest concentrations observed for vanillic, benzoic, and ferulic acids. This study highlights the antimicrobial and antifungal properties of the R. idaeus shoot lipophilic extract. However, the obtained lipophilic extract showed a relatively low level of antioxidant activity. Consequently, the derivatives of phenolcarboxylic acids play a substantial role in the antimicrobial and antifungal effects, whereas their contribution to antioxidant activity appears to be limited.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-06-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141373646","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}
The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of olanzapine (OLZ) loaded solid lipid nanoparticles (SLNs) for sustained release. OLZ SLNs were prepared by hot melt emulsification and ultrasonication using Precirol ATO 5 (PRE) as a solid lipid, combination of Kolliphor ELP (KELP) and Tween 80 (T80) as surfactants, after optimising formulation and process variables. The SLN system was subjected to evaluation of particle size, zeta potential, entrapment efficiency (EE), in-vitro drug release and ex-vivo intestinal permeability studies using the chicken intestinal segments (jejunum). Further, these SLNs were converted into stable DANs by adsorbing onto a Neusilin US2 (NUS2) and Avicel CL 611 (ACL) carriers using the granulation-evaporative drying method. The DANs were characterised for redispersion properties, in-vitro drug release, thermal behaviour, crystallinity, and morphology. The SLN and DAN had a particle size of 238.0 nm [0.274 polydispersity index (PdI)] and 302.4 [0.494 PdI] respectively. The zeta potentials of SLN and DAN were found to be −29.3 mV and −26.3 mV, respectively. The SLN had 67% EE, and showed a sustained drug release in various media. The highest permeability of SLNs was observed in ex-vivo permeation model compared to the OLZ suspension, indicating that SLNs have the potential to bypass hepatic metabolism. The adsorption of SLNs onto carriers was confirmed by surface morphology. The DAN had good flow properties and sustained drug release similar to that of SLNs. The X-ray diffraction (XRD) patterns and endothermic peaks confirmed the complete encapsulation of actives in lipid matrices. The encapsulating of OLZ in SLNs and converting it into DAN showed a sustained release and adsorption technique that can be used for improving the stability of NLC dispersion. The DANs can be offered in dosage forms such as filling into sachets, capsules and compressed into tablets.
{"title":"Formulation development, in-vitro and ex-vivo evaluation of dry adsorbed solid lipid nanoparticles: an approach of overcoming olanzapine drawbacks","authors":"R. Hirlekar, Alfiha Momin, S. Bhairy","doi":"10.2478/afpuc-2024-0004","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0004","url":null,"abstract":"\u0000 \u0000 \u0000 The present study was aimed at preparing stable dry adsorbed nanoparticles (DANs) of olanzapine (OLZ) loaded solid lipid nanoparticles (SLNs) for sustained release.\u0000 \u0000 \u0000 \u0000 OLZ SLNs were prepared by hot melt emulsification and ultrasonication using Precirol ATO 5 (PRE) as a solid lipid, combination of Kolliphor ELP (KELP) and Tween 80 (T80) as surfactants, after optimising formulation and process variables. The SLN system was subjected to evaluation of particle size, zeta potential, entrapment efficiency (EE), in-vitro drug release and ex-vivo intestinal permeability studies using the chicken intestinal segments (jejunum). Further, these SLNs were converted into stable DANs by adsorbing onto a Neusilin US2 (NUS2) and Avicel CL 611 (ACL) carriers using the granulation-evaporative drying method. The DANs were characterised for redispersion properties, in-vitro drug release, thermal behaviour, crystallinity, and morphology.\u0000 \u0000 \u0000 \u0000 The SLN and DAN had a particle size of 238.0 nm [0.274 polydispersity index (PdI)] and 302.4 [0.494 PdI] respectively. The zeta potentials of SLN and DAN were found to be −29.3 mV and −26.3 mV, respectively. The SLN had 67% EE, and showed a sustained drug release in various media. The highest permeability of SLNs was observed in ex-vivo permeation model compared to the OLZ suspension, indicating that SLNs have the potential to bypass hepatic metabolism. The adsorption of SLNs onto carriers was confirmed by surface morphology. The DAN had good flow properties and sustained drug release similar to that of SLNs. The X-ray diffraction (XRD) patterns and endothermic peaks confirmed the complete encapsulation of actives in lipid matrices.\u0000 \u0000 \u0000 \u0000 The encapsulating of OLZ in SLNs and converting it into DAN showed a sustained release and adsorption technique that can be used for improving the stability of NLC dispersion. The DANs can be offered in dosage forms such as filling into sachets, capsules and compressed into tablets.\u0000","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140681085","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}
Jana Korcová, Mária Húserková, Lucia Lintnerová, J. Valentová
Metal complexes, which, under physiologic conditions, show redox properties and are able to bind to DNA, are great tools to cleave the DNA chain. This aspect is of great importance for their use as antineoplastic drugs. We synthesized ligands derived from short-chain amino acids and from salicylaldehyde. The prepared ligands of the type of reduced Schiff bases were subsequently used for the preparation of copper(II) complexes. The aim of the study was in vitro testing of copper(II) complexes, where it was confirmed that they are capable of cleaving DNA. Their cytotoxic activity was also confirmed by the resazurin redox method on Saccharomyces cerevisiae based on preserved healthy mitochondrial function.
金属复合物在生理条件下具有氧化还原特性，能够与 DNA 结合，是切割 DNA 链的重要工具。这对于将它们用作抗肿瘤药物非常重要。我们合成了来自短链氨基酸和水杨醛的配体。所制备的还原型希夫碱配体随后被用于制备铜（II）配合物。研究的目的是对铜（II）络合物进行体外测试，结果证实它们能够裂解 DNA。在保留健康线粒体功能的基础上，还用雷沙祖林氧化还原法确认了铜(II)络合物对酿酒酵母的细胞毒性活性。
{"title":"DNA Cleavage and Cytotoxic Activity of Copper(II) Complexes Based on Reduced Schiff Bases Derived From Salicylaldehyde and Amino Acids","authors":"Jana Korcová, Mária Húserková, Lucia Lintnerová, J. Valentová","doi":"10.2478/afpuc-2024-0003","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0003","url":null,"abstract":"\u0000 Metal complexes, which, under physiologic conditions, show redox properties and are able to bind to DNA, are great tools to cleave the DNA chain. This aspect is of great importance for their use as antineoplastic drugs. We synthesized ligands derived from short-chain amino acids and from salicylaldehyde. The prepared ligands of the type of reduced Schiff bases were subsequently used for the preparation of copper(II) complexes. The aim of the study was in vitro testing of copper(II) complexes, where it was confirmed that they are capable of cleaving DNA. Their cytotoxic activity was also confirmed by the resazurin redox method on Saccharomyces cerevisiae based on preserved healthy mitochondrial function.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-03-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140372739","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}
O. Farsa, Veronika Ballayová, Radka Žáčková, P. Zubáč
Aminopeptidase N (APN) is a broad specificity zinc metallopeptidase with many functions that do not always depend on its enzymatic activity. Among others, it is involved in tumor angiogenesis and metastasizing and also serves as a cellular receptor of some coronaviruses. Some APN inhibitors, such as bestatin or tosedostat, were used or tested as anticancer drugs in the past. Within the past two decades, we have prepared several series of potential APN inhibitors. Some of them reached interesting values of inhibitory activity and were also successfully tested for antiproliferation activity in cancer cell lines. We also performed some QSAR studies with APN inhibitors prepared by us and other authors.
{"title":"Aminopeptidase N as a potential drug target","authors":"O. Farsa, Veronika Ballayová, Radka Žáčková, P. Zubáč","doi":"10.2478/afpuc-2024-0002","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0002","url":null,"abstract":"\u0000 Aminopeptidase N (APN) is a broad specificity zinc metallopeptidase with many functions that do not always depend on its enzymatic activity. Among others, it is involved in tumor angiogenesis and metastasizing and also serves as a cellular receptor of some coronaviruses. Some APN inhibitors, such as bestatin or tosedostat, were used or tested as anticancer drugs in the past. Within the past two decades, we have prepared several series of potential APN inhibitors. Some of them reached interesting values of inhibitory activity and were also successfully tested for antiproliferation activity in cancer cell lines. We also performed some QSAR studies with APN inhibitors prepared by us and other authors.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140234060","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}
Mushrooms from the genus Cordyceps are characterized by a wide range of biological effects due to the diverse amount of substances contained in them and are an important source of bioactive compounds. In China, mushrooms of the genus Cordyceps have been used as a medicinal preparation of traditional Chinese medicine for centuries. So far, a considerable number of studies have been conducted that focused on analyzing the effects of Cordyceps, which include their antioxidant, antibacterial, immunomodulatory, antidiabetic, antitumor, and many other effects. The ability of fungi to form complexes with various metals is also interesting. It is believed that polysaccharides are the main component of the extracts involved in the complexation with metals, after which their biological effects are improved and deepened. The work deals with the comparison of the antioxidant and antibacterial effects of Cordyceps extracts with extracts of this mushroom enriched with silver ions. Based on scientific studies, it is assumed that there is a complexation between the chemical compounds of the extracts and silver.
{"title":"Medicinal Mushrooms Cordyceps as a New Source of Bioactive Compounds and Their Complexation With Silver Ions","authors":"A. Uhrinová, Lucia Ungvarská Maľučká","doi":"10.2478/afpuc-2024-0001","DOIUrl":"https://doi.org/10.2478/afpuc-2024-0001","url":null,"abstract":"\u0000 Mushrooms from the genus Cordyceps are characterized by a wide range of biological effects due to the diverse amount of substances contained in them and are an important source of bioactive compounds. In China, mushrooms of the genus Cordyceps have been used as a medicinal preparation of traditional Chinese medicine for centuries. So far, a considerable number of studies have been conducted that focused on analyzing the effects of Cordyceps, which include their antioxidant, antibacterial, immunomodulatory, antidiabetic, antitumor, and many other effects. The ability of fungi to form complexes with various metals is also interesting. It is believed that polysaccharides are the main component of the extracts involved in the complexation with metals, after which their biological effects are improved and deepened. The work deals with the comparison of the antioxidant and antibacterial effects of Cordyceps extracts with extracts of this mushroom enriched with silver ions. Based on scientific studies, it is assumed that there is a complexation between the chemical compounds of the extracts and silver.","PeriodicalId":12070,"journal":{"name":"European Pharmaceutical Journal","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-03-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140232468","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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