Sevim Küçük, M. Has, Fatih Göger, Filiz Özdemir, Z. Incesu
The Verbascum genus includes many species used in folk medicine or the treatment of various diseases. In this study, the cytotoxic, antioxidant activity, and LC/MS-MS profiles of three Verbascum species, which are endemic in Eskişehir and its surroundings, were investigated. The cytotoxic effects of methanol extract of V.detersile, V. eskisehirensis, and V.gypsicola species on the cervical (HeLa) and ovarian cancer (SKOV-3) cells were investigated using a colorimetric assay. The results indicated that cytotoxic effect was not observed after treatment of SKOV-3 cells with Verbascum. On the other hand, the cytotoxic activity of V. detersile was found to be 0.1910 mg/dL and 1.057 mg/dL for HeLa cells after 24 or 48 hours incubation with V.detersile, respectively. The antioxidant activity was determined as 1,1-diphenyl-2-picrylhydrazyl (DPPH•) radical scavenging activity, trolox equivalent antioxidant capacity (TEAC assay), and also the total phenolic content of the samples was found. Total phenols were estimated as Gallic acid equivalents (GAE), expressed as mg Gallic acid/in 1g extract previously described by Singletton. LC/MS profiles separation and detection of phytochemicals of the extract were performed on a Shimadzu UPLC system consisting of a vacuum degasser, an autosampler (SIL20A Shimadzu Autosampler), a binary pump (LC20AD Shimadzu), an oven (CTO20A Shimadzu Column Oven) and DAD dedector (SPD M20A Shimadzu DAD Detector). In terms of antioxidant activity, V. gypsicola was found to have the least antioxidant activity among the three extracts, which is also correlated with the total amount of phenolic content in its content. In this way, it differs from other species. V. detersile exhibits a different chemical profile from the other two species with the iridoid catalpol derivatives it contains. Apigenin pentoside is the only flavonoid molecule detected in V. detersille.
马鞭草属包括许多用于民间医药或治疗各种疾病的物种。本研究调查了埃斯基谢希尔及其周边地区特有的三种马鞭草的细胞毒性、抗氧化活性和 LC/MS-MS 图谱。 采用比色法研究了 V.detersile、V.eskisehirensis 和 V.gypsicola 的甲醇提取物对宫颈癌(HeLa)和卵巢癌(SKOV-3)细胞的细胞毒性作用。结果表明,用马鞭草处理 SKOV-3 细胞后,未观察到细胞毒性作用。另一方面,V.detersile 对 HeLa 细胞的细胞毒性活性分别为 0.1910 mg/dL 和 1.057 mg/dL。抗氧化活性以 1,1-二苯基-2-苦基肼(DPPH-)自由基清除活性、trolox 当量抗氧化能力(TEAC 法)来测定,同时还测定了样品中的总酚含量。根据 Singletton 的描述,总酚以没食子酸当量(GAE)估算,以没食子酸毫克/1 克提取物表示。采用岛津 UPLC 系统对提取物中的植物化学物质进行 LC/MS 图谱分离和检测,该系统由真空脱气机、自动进样器(SIL20A 岛津自动进样器)、二元泵(LC20AD 岛津)、烤箱(CTO20A 岛津柱烤箱)和 DAD 检测器(SPD M20A 岛津 DAD 检测器)组成。在抗氧化活性方面,发现 V. gypsicola 的抗氧化活性在三种提取物中最低,这也与它所含的酚类物质的总量有关。因此,它与其他物种有所不同。V. detersile 所含的鸢尾梓醇衍生物显示出与其他两个物种不同的化学特征。芹菜素戊苷是在 V. detersille 中检测到的唯一黄酮类分子。
{"title":"Determination of cytotoxic, antioxidant activities and LC/MS-MS profiles of three endemic Verbascum L. species","authors":"Sevim Küçük, M. Has, Fatih Göger, Filiz Özdemir, Z. Incesu","doi":"10.55971/ejls.1364354","DOIUrl":"https://doi.org/10.55971/ejls.1364354","url":null,"abstract":"The Verbascum genus includes many species used in folk medicine or the treatment of various diseases. In this study, the cytotoxic, antioxidant activity, and LC/MS-MS profiles of three Verbascum species, which are endemic in Eskişehir and its surroundings, were investigated. The cytotoxic effects of methanol extract of V.detersile, V. eskisehirensis, and V.gypsicola species on the cervical (HeLa) and ovarian cancer (SKOV-3) cells were investigated using a colorimetric assay. The results indicated that cytotoxic effect was not observed after treatment of SKOV-3 cells with Verbascum. On the other hand, the cytotoxic activity of V. detersile was found to be 0.1910 mg/dL and 1.057 mg/dL for HeLa cells after 24 or 48 hours incubation with V.detersile, respectively. The antioxidant activity was determined as 1,1-diphenyl-2-picrylhydrazyl (DPPH•) radical scavenging activity, trolox equivalent antioxidant capacity (TEAC assay), and also the total phenolic content of the samples was found. Total phenols were estimated as Gallic acid equivalents (GAE), expressed as mg Gallic acid/in 1g extract previously described by Singletton. LC/MS profiles separation and detection of phytochemicals of the extract were performed on a Shimadzu UPLC system consisting of a vacuum degasser, an autosampler (SIL20A Shimadzu Autosampler), a binary pump (LC20AD Shimadzu), an oven (CTO20A Shimadzu Column Oven) and DAD dedector (SPD M20A Shimadzu DAD Detector). In terms of antioxidant activity, V. gypsicola was found to have the least antioxidant activity among the three extracts, which is also correlated with the total amount of phenolic content in its content. In this way, it differs from other species. V. detersile exhibits a different chemical profile from the other two species with the iridoid catalpol derivatives it contains. Apigenin pentoside is the only flavonoid molecule detected in V. detersille.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"77 4","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139146514","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}
Saniye Özcan, Abeer Elriş, Serkan Levent, N. O. Can
In 2015, the Food and Drug Administration granted approval for the use of lumacaftor 200 mg and ivacaftor 125 mg in the treatment of cystic fibrosis patients who possess the F508del mutation, namely those who are 12 years of age or older. Since its approval, the medicine has been implemented in clinical settings, although the presence of numerous disputes, with the aim of mitigating disease symptoms and enhancing the overall quality of life. Given the existing gaps in the literature regarding the analysis of the amalgamation of these two active substances, a straightforward and practical HPLC approach has been devised in adherence to the guidelines outlined in the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) Q2(R1) document. To accomplish this objective, the process of separation was successfully carried out using a monolithic silica stationary phase (Chromolith High Resolution RP-18e, 100 mm × 4.6 mm i.d., Merck KGaA, Darmstadt, Germany). The separation process was conducted using a gradient mode. The initial composition of the mobile phase consisted of acetonitrile and a phosphate buffer solution with a concentration of 0.030 M and a pH of 3.5. The flow rate was recorded as 1.0 mL/min, and avanafil was used as an internal standard. The improved and verified approach has demonstrated successful application in bulk and pharmaceutical formulation evaluations when utilizing the ivacaftor/lumacaftor combination.
2015 年,美国食品和药物管理局批准将 lumacaftor 200 毫克和 ivacaftor 125 毫克用于治疗拥有 F508del 突变的囊性纤维化患者,即 12 岁或以上的患者。自获得批准以来,尽管存在诸多争议,但该药物已在临床环境中得到应用,目的是减轻疾病症状和提高整体生活质量。鉴于现有文献中关于这两种活性物质混合物分析的空白,我们根据国际人用药品技术要求协调理事会(ICH)Q2(R1)文件中的指导方针,设计了一种简单实用的高效液相色谱法。为了实现这一目标,使用整体硅胶固定相(Chromolith High Resolution RP-18e,100 mm × 4.6 mm i.d.,Merck KGaA,Darmstadt,Germany)成功地进行了分离。分离过程采用梯度模式。流动相的初始成分为乙腈和浓度为 0.030 M、pH 值为 3.5 的磷酸盐缓冲溶液。流速为 1.0 mL/min,阿伐那非用作内标。经改进和验证的方法已成功应用于伊伐卡夫托/卢马卡夫托复方制剂的散装和药物制剂评估。
{"title":"HPLC method for simultaneous quantification of lumacaftor and ivacaftor bulk and pharmaceutical formulations","authors":"Saniye Özcan, Abeer Elriş, Serkan Levent, N. O. Can","doi":"10.55971/ejls.1367996","DOIUrl":"https://doi.org/10.55971/ejls.1367996","url":null,"abstract":"In 2015, the Food and Drug Administration granted approval for the use of lumacaftor 200 mg and ivacaftor 125 mg in the treatment of cystic fibrosis patients who possess the F508del mutation, namely those who are 12 years of age or older. Since its approval, the medicine has been implemented in clinical settings, although the presence of numerous disputes, with the aim of mitigating disease symptoms and enhancing the overall quality of life. Given the existing gaps in the literature regarding the analysis of the amalgamation of these two active substances, a straightforward and practical HPLC approach has been devised in adherence to the guidelines outlined in the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) Q2(R1) document. To accomplish this objective, the process of separation was successfully carried out using a monolithic silica stationary phase (Chromolith High Resolution RP-18e, 100 mm × 4.6 mm i.d., Merck KGaA, Darmstadt, Germany). The separation process was conducted using a gradient mode. The initial composition of the mobile phase consisted of acetonitrile and a phosphate buffer solution with a concentration of 0.030 M and a pH of 3.5. The flow rate was recorded as 1.0 mL/min, and avanafil was used as an internal standard. The improved and verified approach has demonstrated successful application in bulk and pharmaceutical formulation evaluations when utilizing the ivacaftor/lumacaftor combination.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"95 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139147291","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}
Esma Ocak, Filiz Eğin Kolata, Mine Kürkçüoğlu, Sevim Küçük
Ferulago aucheri Boiss, which belongs to the Apiaceae family, is distributed from Türkiye to the Caucasus. Its chemical composition may vary depending on the region where it grows, climate conditions and topography. Essential oil components were determined using two different techniques (hydrodistilled and headspace-solid phase microextraction HS-SPME) with the species collected from Nallıhan district of Ankara, Türkiye. In the present study, essential oil and headspace volatiles of aerial parts of Ferulago aucheri Boiss. were analyzed by GC-GC/MS. Thirty-five components were characterized, representing 99.6% of the oil by hydrodistilled and thirty components were characterized, representing 98.7% by HS-SPME. In both techniques, the main substances were identified as α-pinene, limonene, and δ-3-carene. In previous studies, it has been observed that the main components are in different amounts, and some studies even have different main components.
{"title":"Volatile components of Ferulago aucheri Boiss. (Apiaceae)","authors":"Esma Ocak, Filiz Eğin Kolata, Mine Kürkçüoğlu, Sevim Küçük","doi":"10.55971/ejls.1366082","DOIUrl":"https://doi.org/10.55971/ejls.1366082","url":null,"abstract":"Ferulago aucheri Boiss, which belongs to the Apiaceae family, is distributed from Türkiye to the Caucasus. Its chemical composition may vary depending on the region where it grows, climate conditions and topography. Essential oil components were determined using two different techniques (hydrodistilled and headspace-solid phase microextraction HS-SPME) with the species collected from Nallıhan district of Ankara, Türkiye. In the present study, essential oil and headspace volatiles of aerial parts of Ferulago aucheri Boiss. were analyzed by GC-GC/MS. Thirty-five components were characterized, representing 99.6% of the oil by hydrodistilled and thirty components were characterized, representing 98.7% by HS-SPME. In both techniques, the main substances were identified as α-pinene, limonene, and δ-3-carene. In previous studies, it has been observed that the main components are in different amounts, and some studies even have different main components.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":" 13","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139142326","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 genus Achillea (Asteraceae) is distributed in Europe and the Middle East and has approximately 140 endemic species. There are 40 Achillea sp. in the Turkish flora and 20 of them are endemic. This genus has a widespread area all over the world. Also, it has many different uses in traditionally, such as diarrhea, abdominal pain, hemorrhoids and wound healing. Achillea sp. is also widely used as food. Achillea millefolium L. is known as “Yarrow” and has been used as a wound healer, diuretic, appetite stimulant and menstrual bleeding in Türkiye. The aerial parts of the plant are used in a variety of forms, including infusion, tincture, liquid extract, total extract, bath. It has also been stated that the essential oil of the plant is used in mouth sores and dental health due to its antimicrobial effect. It is also preferred in the treatment of aphtha and wounds in the mouth. Within the scope of this project, essential oil of A. millefolium was obtained from European Pharmacopoeia (9th Edition) quality, supplied from German commercial source, with the Clevenger apparatus for 3 h. The chemical composition of the essential oil obtained was elucidated. A total of 67 components were identified. Chamazulene (6.8%), caryophyllene oxide (5.8%), torilenol (5.6%), (E)-nerolidol (4.3%), borneol (4.0%) were found as major constituents of A. millefolium essential oil. The original value of this study, aim of this study is to conduct a pharmacognosic examination of the European Pharmacopoeia quality A. millefolium, one of the Achillea sp. that is of great importance worldwide due to medicinal proporties, especially herbal tea. With this study, the chemical composition of the volatile components of the A. millefolium was elucidated.
蓍草属(菊科)分布于欧洲和中东地区,约有 140 个特有种。土耳其植物区系中有 40 种 Achillea 属植物,其中 20 种为特有种。该属植物广泛分布于世界各地。此外,它在传统上有许多不同的用途,如腹泻、腹痛、痔疮和伤口愈合。Achillea 还被广泛用作食物。Achillea millefolium L. 被称为 "西洋蓍草",在土耳其被用作伤口愈合剂、利尿剂、促进食欲剂和月经出血剂。该植物的气生部分有多种使用形式,包括浸泡、酊剂、液体提取物、总提取物和浴液。还有人指出,该植物的精油具有抗菌作用,可用于治疗口腔溃疡和牙齿健康。它也是治疗口腔溃疡和伤口的首选。在本项目范围内,使用 Clevenger 仪器对从德国商业渠道获得的欧洲药典(第 9 版)质量的 A. millefolium 精油进行了 3 小时的提取。共鉴定出 67 种成分。发现香茅烯(6.8%)、氧化香叶烯(5.8%)、香叶醇(5.6%)、(E)-nerolidol(4.3%)、龙脑(4.0%)是米勒弗洛里精油的主要成分。这项研究的原始价值、目的是对欧洲药典中的优质 A. millefolium 进行药理检查,A. millefolium 是蓍草属植物之一,因其药用比例,尤其是凉茶,在全世界具有重要意义。通过这项研究,阐明了 A. millefolium 挥发性成分的化学组成。
{"title":"Evaluation of volatile components of Achillea millefolium L. essential oil","authors":"Gözde Öztürk, D. Kırcı, Betül Demirci","doi":"10.55971/ejls.1381369","DOIUrl":"https://doi.org/10.55971/ejls.1381369","url":null,"abstract":"The genus Achillea (Asteraceae) is distributed in Europe and the Middle East and has approximately 140 endemic species. There are 40 Achillea sp. in the Turkish flora and 20 of them are endemic. This genus has a widespread area all over the world. Also, it has many different uses in traditionally, such as diarrhea, abdominal pain, hemorrhoids and wound healing. Achillea sp. is also widely used as food. Achillea millefolium L. is known as “Yarrow” and has been used as a wound healer, diuretic, appetite stimulant and menstrual bleeding in Türkiye. The aerial parts of the plant are used in a variety of forms, including infusion, tincture, liquid extract, total extract, bath. It has also been stated that the essential oil of the plant is used in mouth sores and dental health due to its antimicrobial effect. It is also preferred in the treatment of aphtha and wounds in the mouth. Within the scope of this project, essential oil of A. millefolium was obtained from European Pharmacopoeia (9th Edition) quality, supplied from German commercial source, with the Clevenger apparatus for 3 h. The chemical composition of the essential oil obtained was elucidated. A total of 67 components were identified. Chamazulene (6.8%), caryophyllene oxide (5.8%), torilenol (5.6%), (E)-nerolidol (4.3%), borneol (4.0%) were found as major constituents of A. millefolium essential oil. The original value of this study, aim of this study is to conduct a pharmacognosic examination of the European Pharmacopoeia quality A. millefolium, one of the Achillea sp. that is of great importance worldwide due to medicinal proporties, especially herbal tea. With this study, the chemical composition of the volatile components of the A. millefolium was elucidated.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"58 s205","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139145900","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}
A vast web of organizations, companies, and teams involved in creating, researching, and producing drugs and associated products makes up the pharmaceutical sector. In this context, the term “supply chain” refers to the network of individuals, processes, information, and resources that transform raw materials and parts into finished goods and services before being supplied to customers. The pharmaceutical supply chain system, then, offers customers medications in the right amount, at the right time, with acceptable quality, and for the lowest feasible cost. Pharmaceutical companies are increasingly contracting out their supply chain activities due to the severe push to keep R&D expenses under control. Instead of being a cost-cutting measure, global supply chain outsourcing can be seen as a strategic competitive weapon that can improve positional advantage, offer production flexibility, and meet the ever-increasing expectations of final consumers. Global supply chain outsourcing is crucial for pharmaceutical firms to enhance performance and profit margins by leveraging core skills and resources beyond other strategies which can lower risk, increase flexibility, improve returns on capital, and improve a company’s ability to respond to the needs of its shareholders and consumers. Even while there is widespread recognition of the alluring advantages of global outsourcing, many of the related concerns are frequently disregarded. In addition to briefly discussing risk assessment methods, the goal of this work is to offer manufacturer-focused insight into supply chain-related outsourcing concerns within the pharmaceutical industry.
{"title":"Pharmaceutical supply chain: The importance of outsourcing","authors":"Özlem Akbal Dağıstan","doi":"10.55971/ejls.1395960","DOIUrl":"https://doi.org/10.55971/ejls.1395960","url":null,"abstract":"A vast web of organizations, companies, and teams involved in creating, researching, and producing drugs and associated products makes up the pharmaceutical sector. In this context, the term “supply chain” refers to the network of individuals, processes, information, and resources that transform raw materials and parts into finished goods and services before being supplied to customers. The pharmaceutical supply chain system, then, offers customers medications in the right amount, at the right time, with acceptable quality, and for the lowest feasible cost. Pharmaceutical companies are increasingly contracting out their supply chain activities due to the severe push to keep R&D expenses under control. Instead of being a cost-cutting measure, global supply chain outsourcing can be seen as a strategic competitive weapon that can improve positional advantage, offer production flexibility, and meet the ever-increasing expectations of final consumers. Global supply chain outsourcing is crucial for pharmaceutical firms to enhance performance and profit margins by leveraging core skills and resources beyond other strategies which can lower risk, increase flexibility, improve returns on capital, and improve a company’s ability to respond to the needs of its shareholders and consumers. Even while there is widespread recognition of the alluring advantages of global outsourcing, many of the related concerns are frequently disregarded. In addition to briefly discussing risk assessment methods, the goal of this work is to offer manufacturer-focused insight into supply chain-related outsourcing concerns within the pharmaceutical industry.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"4 5","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139148234","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}
Abdüllatif Karakaya, Zahra Maryam, Tuğba Erçetin, U. Acar Çevik
In the present research, we synthesized two unique series of thiazole compounds having 5-bromothiophene and 3-methylthiophene (2a-2f) in their structure. After that, spectroscopic methods were used to analyze the chemical compositions of the newly synthesized molecules. Then in vitro evaluation was done to determine acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activity of the synthesized compounds using galantamine as reference standard. The compounds’ antioxidant properties were assessed using DPPH radical scavenging and ferrous ion-chelating techniques. The results of the study showed weak anticholinesterase activity against AChE and BuChE enzymes for all the final compounds. The synthesized analogs also showed significant DPPH radical scavenging activities with IC50 values in the range of 29.16 ± 0.009 to 33.09 ± 0.004 µM (for DDPH) incomparison to standard gallic acid with IC50 = 31.13 ± 0.008 µM (for DDPH). Especially, compound 2c showed the best antioxidant activity with IC50 value of 29.16 ± 0.009 µM.
{"title":"Synthesis of thiazole derivatives as cholinesterase inhibitors with antioxidant activity","authors":"Abdüllatif Karakaya, Zahra Maryam, Tuğba Erçetin, U. Acar Çevik","doi":"10.55971/ejls.1374823","DOIUrl":"https://doi.org/10.55971/ejls.1374823","url":null,"abstract":"In the present research, we synthesized two unique series of thiazole compounds having 5-bromothiophene and 3-methylthiophene (2a-2f) in their structure. After that, spectroscopic methods were used to analyze the chemical compositions of the newly synthesized molecules. Then in vitro evaluation was done to determine acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) activity of the synthesized compounds using galantamine as reference standard. The compounds’ antioxidant properties were assessed using DPPH radical scavenging and ferrous ion-chelating techniques. The results of the study showed weak anticholinesterase activity against AChE and BuChE enzymes for all the final compounds. The synthesized analogs also showed significant DPPH radical scavenging activities with IC50 values in the range of 29.16 ± 0.009 to 33.09 ± 0.004 µM (for DDPH) incomparison to standard gallic acid with IC50 = 31.13 ± 0.008 µM (for DDPH). Especially, compound 2c showed the best antioxidant activity with IC50 value of 29.16 ± 0.009 µM.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"102 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139145638","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}
Gülnar Farmanlı, S. Ilgın, B. Ergun, Merve Baysal, A. Karaduman, Özlem Atlı Eklioğlu
Since the liver metabolizes many drugs, including antiepileptics, this organ is the main target of drug-induced damage. There is very little data on hepatotoxicity due to carbamazepine and perampanel metabolized in the liver. The available data are based solely on published case reports. For this reason, this study aims to evaluate the hepatotoxicity of carbamazepine and perampanel, which are frequently used in treating epilepsy and which do not have a detailed investigation, although they are suspected of hepatotoxicity. Hepatotoxicity in the HepG2 cell line, IC50 values were calculated by MTT cytotoxicity test, followed by determination of apoptosis/necrosis, various biochemical analyzes (ALT, AST, urea), which is currently a biomarker for liver injury, and hepatotoxicity by ROS and GSH determination. Both drugs increased liver biomarkers, oxidative stress, and cytotoxicity in HepG2 cells. The investigation found that the drugs triggered liver apoptosis, not necrosis. In conclusion, Perampanel may have hepatotoxicity similar to carbamazepine.
{"title":"Evaluation of in vitro hepatotoxicity of perampanel in comparison with carbamazepine: old versus new","authors":"Gülnar Farmanlı, S. Ilgın, B. Ergun, Merve Baysal, A. Karaduman, Özlem Atlı Eklioğlu","doi":"10.55971/ejls.1324501","DOIUrl":"https://doi.org/10.55971/ejls.1324501","url":null,"abstract":"Since the liver metabolizes many drugs, including antiepileptics, this organ is the main target of drug-induced damage. There is very little data on hepatotoxicity due to carbamazepine and perampanel metabolized in the liver. The available data are based solely on published case reports. For this reason, this study aims to evaluate the hepatotoxicity of carbamazepine and perampanel, which are frequently used in treating epilepsy and which do not have a detailed investigation, although they are suspected of hepatotoxicity. Hepatotoxicity in the HepG2 cell line, IC50 values were calculated by MTT cytotoxicity test, followed by determination of apoptosis/necrosis, various biochemical analyzes (ALT, AST, urea), which is currently a biomarker for liver injury, and hepatotoxicity by ROS and GSH determination. Both drugs increased liver biomarkers, oxidative stress, and cytotoxicity in HepG2 cells. The investigation found that the drugs triggered liver apoptosis, not necrosis. In conclusion, Perampanel may have hepatotoxicity similar to carbamazepine.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"67 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128242995","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}
Depression is the most frequent psychiatric illness among mood disorders, affecting approximately 10% of adults. Especially recurrent and moderate/severe depression can become a serious public health problem by impairing people’s life quality. The monoamine hypothesis is the most widely accepted hypothesis for clarifying the pathophysiology of depression. Depression’s pathogenesis and etiology, however, are still poorly understood. Tricyclic antidepressants, monoamine oxidase inhibitors, selective serotonin or noradrenaline reuptake inhibitors, different atypical antidepressants, and electroconvulsive therapy are currently available therapies for depression. Although these treatment options are effective, a large number of patients do not respond to treatment or do not attain long-term remission. Furthermore, present antidepressants used in clinics have disadvantages such as delayed onset of effects, side effects, and patient compliance problems. Therefore, the discovery of new antidepressant medications is crucial. Animal models are critical in investigating the etiology of depression and developing novel treatments. Hence, in this review, the main mechanisms involved in the etiopathogenesis of depression and the experimental depression models used in preclinical studies have been demonstrated.
{"title":"Etiopathogenesis of depression and experimental depression models used in preclinical studies","authors":"Ümmühan Kandemir","doi":"10.55971/ejls.1327521","DOIUrl":"https://doi.org/10.55971/ejls.1327521","url":null,"abstract":"Depression is the most frequent psychiatric illness among mood disorders, affecting approximately 10% of adults. Especially recurrent and moderate/severe depression can become a serious public health problem by impairing people’s life quality. The monoamine hypothesis is the most widely accepted hypothesis for clarifying the pathophysiology of depression. Depression’s pathogenesis and etiology, however, are still poorly understood. Tricyclic antidepressants, monoamine oxidase inhibitors, selective serotonin or noradrenaline reuptake inhibitors, different atypical antidepressants, and electroconvulsive therapy are currently available therapies for depression. Although these treatment options are effective, a large number of patients do not respond to treatment or do not attain long-term remission. Furthermore, present antidepressants used in clinics have disadvantages such as delayed onset of effects, side effects, and patient compliance problems. Therefore, the discovery of new antidepressant medications is crucial. Animal models are critical in investigating the etiology of depression and developing novel treatments. Hence, in this review, the main mechanisms involved in the etiopathogenesis of depression and the experimental depression models used in preclinical studies have been demonstrated.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"160 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"115747780","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}
Saniye Özcan, Egemen Güvenç Öğüt, Serkan Levent, N. O. Can
Selexipag is a new non-prostanoid prostacyclin receptor agonist used to treat pulmonary arterial hypertension. Selexipag is a long-acting IP receptor agonist with a shorter half-life than all other licensed drugs targeting the prostacyclin pathway, mostly administered intravenously or by subcutaneous infusion or inhalation. In this study, a new high performance liquid chromatography (HPLC) method was developed to analyze Selexipag in bulk and pharmaceutical formulations. The method used a column with Supelco Ascentis® Express (Sigma Aldrich, USA) model phenyl hexyl functional group (100×4.6 mm, ID, 2.7µm). Chromatographic separation was in isocratic elution mode, and the mobile phase mixture was acetonitrile containing 0.1% formic acid: water containing 0.1% formic acid (60:40, v/v) ratio. The method was linear in the concentration range of 15.7-117.6 µg/mL, and the LOD and LOQ were obtained as 2.4 and 3.1 µg/mL, respectively. Various method parameters have been tested according to the ICH Q2(R1) manual, and it is a method with high accuracy and precision. Therefore, the developed method is suitable for selexipag’s bulk and pharmaceutical formulation analysis.
{"title":"A new HPLC method for selexipag analysis in pharmaceutical formulation and bulk form","authors":"Saniye Özcan, Egemen Güvenç Öğüt, Serkan Levent, N. O. Can","doi":"10.55971/ejls.1320502","DOIUrl":"https://doi.org/10.55971/ejls.1320502","url":null,"abstract":"Selexipag is a new non-prostanoid prostacyclin receptor agonist used to treat pulmonary arterial hypertension. Selexipag is a long-acting IP receptor agonist with a shorter half-life than all other licensed drugs targeting the prostacyclin pathway, mostly administered intravenously or by subcutaneous infusion or inhalation. In this study, a new high performance liquid chromatography (HPLC) method was developed to analyze Selexipag in bulk and pharmaceutical formulations. The method used a column with Supelco Ascentis® Express (Sigma Aldrich, USA) model phenyl hexyl functional group (100×4.6 mm, ID, 2.7µm). Chromatographic separation was in isocratic elution mode, and the mobile phase mixture was acetonitrile containing 0.1% formic acid: water containing 0.1% formic acid (60:40, v/v) ratio. The method was linear in the concentration range of 15.7-117.6 µg/mL, and the LOD and LOQ were obtained as 2.4 and 3.1 µg/mL, respectively. Various method parameters have been tested according to the ICH Q2(R1) manual, and it is a method with high accuracy and precision. Therefore, the developed method is suitable for selexipag’s bulk and pharmaceutical formulation analysis.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"13 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"129313905","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}
Proper nutrition is vital for all patients with an expected lifespan. It is strongly recommended that patients whose oral intake is impaired or suspected to be impaired should be provided nutritional support. Concurrent medication administration during enteral nutrition may result in complications unless necessary precautions are taken. This study presents a case of a 94-year-old male patient with poor general health condition and being treated in a palliative care service. The patient was fed with an enteral feeding tube for seven drugs. There have been two tube occlusions causing the replacement of the tube since the enteral feeding tube was placed.The clinical pharmacist checked how the patient’s drugs were given through a nasogastric tube and how the patient’s relatives administered the drugs. Inappropriate dosage form selections and errors in administration through the nasogastric tube were identified. The interaction and incompatibility of the patient’s medications with the nutritional formula were also investigated. The clinical pharmacist informed the person giving the medicine to the patient about the correct administration of the medicine from the tube. The proper method for administering medications from the tube was ensured accordingly. Following the clinical pharmacist’s training, it was observed that the nasogastric tube was correctly used to administer the drug and the patient being monitored had no tube obstruction in the later phases of the treatment.It may be beneficial for a pharmacist to review drug dosage forms and applications in patients with a feeding tube in order to ensure correct administration and avoid undesired drug interactions.
{"title":"Oral medicine administration errors in a patient with an enteral feeding tube","authors":"Özgenur Geridönmez, Kamer Tecen Yücel, Uygar Olgen","doi":"10.55971/ejls.1316049","DOIUrl":"https://doi.org/10.55971/ejls.1316049","url":null,"abstract":"Proper nutrition is vital for all patients with an expected lifespan. It is strongly recommended that patients whose oral intake is impaired or suspected to be impaired should be provided nutritional support. Concurrent medication administration during enteral nutrition may result in complications unless necessary precautions are taken. This study presents a case of a 94-year-old male patient with poor general health condition and being treated in a palliative care service. The patient was fed with an enteral feeding tube for seven drugs. There have been two tube occlusions causing the replacement of the tube since the enteral feeding tube was placed.The clinical pharmacist checked how the patient’s drugs were given through a nasogastric tube and how the patient’s relatives administered the drugs. Inappropriate dosage form selections and errors in administration through the nasogastric tube were identified. The interaction and incompatibility of the patient’s medications with the nutritional formula were also investigated. The clinical pharmacist informed the person giving the medicine to the patient about the correct administration of the medicine from the tube. The proper method for administering medications from the tube was ensured accordingly. Following the clinical pharmacist’s training, it was observed that the nasogastric tube was correctly used to administer the drug and the patient being monitored had no tube obstruction in the later phases of the treatment.It may be beneficial for a pharmacist to review drug dosage forms and applications in patients with a feeding tube in order to ensure correct administration and avoid undesired drug interactions.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"2 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114137567","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}