The genus Tilia (Tiliaceae) represents 45 species, of which six species are European. Tilia sp. are simple, cordate or deciduous trees with long, silicate shaped, 5-valve fruits and fragrant flowers. It is used as a medicinal tea in traditional medicine for colds, coughs, and hypertension and as an antioxidant. Within the scope of this research, Tilia platyphyllos Scop. in the culture form from Eskişehir was obtained, and infusions were prepared at different times (including 5 min., 10 min., 15 min., and 30 min., respectively). Headspace-solid-phase microextraction (HS-SPME) combined with gas chromatography-mass spectrometry (GC-MS) was used to examine the volatile components in the infusion extracts. Major volatile compounds of infusion extracts determined as E)-β-ocimene (15.7-45.9%) and limonene (11.7-33.4%), respectively. Also, terpinolene (26.0%) were identified as the main compounds for 30 min infusion. After then, the infusion extracts were lyophilized, and the antioxidant activity of the infusion extracts were performed by DPPH· radical scavenging effect. It was determined that inhibition percentages were relatively high in the concentration range of 10-0.02 mg/mL (5.60-72.45%). Our first research was the chemical composition and biological activity of the time-dependent T. platyphyllos infusions.
{"title":"Volatile compositions of Tilia platyphyllos Scop. infusions by headspace-solid-phase microextraction (HS-SPME), antioxidant activity","authors":"D. Kırcı, Gözde Öztürk, B. Demirci","doi":"10.55971/ejls.1207835","DOIUrl":"https://doi.org/10.55971/ejls.1207835","url":null,"abstract":"The genus Tilia (Tiliaceae) represents 45 species, of which six species are European. Tilia sp. are simple, cordate or deciduous trees with long, silicate shaped, 5-valve fruits and fragrant flowers. It is used as a medicinal tea in traditional medicine for colds, coughs, and hypertension and as an antioxidant.\u0000Within the scope of this research, Tilia platyphyllos Scop. in the culture form from Eskişehir was obtained, and infusions were prepared at different times (including 5 min., 10 min., 15 min., and 30 min., respectively). Headspace-solid-phase microextraction (HS-SPME) combined with gas chromatography-mass spectrometry (GC-MS) was used to examine the volatile components in the infusion extracts. Major volatile compounds of infusion extracts determined as E)-β-ocimene (15.7-45.9%) and limonene (11.7-33.4%), respectively. Also, terpinolene (26.0%) were identified as the main compounds for 30 min infusion. After then, the infusion extracts were lyophilized, and the antioxidant activity of the infusion extracts were performed by DPPH· radical scavenging effect. It was determined that inhibition percentages were relatively high in the concentration range of 10-0.02 mg/mL (5.60-72.45%). \u0000Our first research was the chemical composition and biological activity of the time-dependent T. platyphyllos infusions.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"43 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-02-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"130312362","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}
Three-dimensional printing (3DP) is one of the most extensively researched methods for producing nano/micro scale biomaterials. This method is typically applied layer by layer. The 3DP method has many advantages over traditional manufacturing methods and ensures that personalized drug design is feasible. Individual dose adjustment provides significant benefits, particularly in some disadvantaged patient groups. Individual release characteristics may be required in these patient groups in addition to dose adjustment. 3DP technology also allows for the adjustment of release kinetics. All of these factors were also increasing interest in 3DP technology in the pharmaceutical industry. The goal of this review is to understand the pharmacological significance of 3DP technology as well as the parameters influencing the release profiles in tablets produced by using technique, and to establish a correlation between them. Within the scope of this review, 79 literature research studies were examined, and it was determined that there is limited data to determine whether there is a correlation between release kinetics and 3DP techniques. When the release profiles obtained by considering the polymer type used in these techniques are evaluated, immediate and rapid release was obtained in studies using PVA + PLA polymers and studies using PVP polymer, immediate release in studies using Kollidon® and Kollicoat® derivatives, and controlled, extended and sustained release was observed in studies using PCL polymer.
{"title":"Release kinetics of 3D printed oral solid dosage forms: An overview","authors":"Berna Kaval, Engin Kapkın, M. Kaynak","doi":"10.55971/ejls.1181158","DOIUrl":"https://doi.org/10.55971/ejls.1181158","url":null,"abstract":"Three-dimensional printing (3DP) is one of the most extensively researched methods for producing nano/micro scale biomaterials. This method is typically applied layer by layer. The 3DP method has many advantages over traditional manufacturing methods and ensures that personalized drug design is feasible. Individual dose adjustment provides significant benefits, particularly in some disadvantaged patient groups. Individual release characteristics may be required in these patient groups in addition to dose adjustment. 3DP technology also allows for the adjustment of release kinetics. All of these factors were also increasing interest in 3DP technology in the pharmaceutical industry. The goal of this review is to understand the pharmacological significance of 3DP technology as well as the parameters influencing the release profiles in tablets produced by using technique, and to establish a correlation between them. Within the scope of this review, 79 literature research studies were examined, and it was determined that there is limited data to determine whether there is a correlation between release kinetics and 3DP techniques. When the release profiles obtained by considering the polymer type used in these techniques are evaluated, immediate and rapid release was obtained in studies using PVA + PLA polymers and studies using PVP polymer, immediate release in studies using Kollidon® and Kollicoat® derivatives, and controlled, extended and sustained release was observed in studies using PCL polymer.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"6 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"127813750","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}
Merve Tiltay, Aydan Hüseynli, Gülşen Akalın Çiftçi, İ. Ö. Alatas
Capsaicin is the main component of many hot peppers, exerts anticancer effects on various cancer cells by inducing apoptotic pathways. In addition, the ineffectiveness of this apoptotic effect of capsaicin on healthy cells provides a wide-ranging use of capsaicin. In recent years, many studies have been carried out to determine the safety of capsaicin use in lung cancer, which is a common cancer type worldwide with high mortality rates. In the present study anticancer effects of capsaicin were studied on A549 human lung adenocarcinoma cell line. Also, citotoxicity of this compound was studied on L929 mouse embryonic fibroblast cell line. Various concentration of capsaicin (3.90625-500 μM) effectively decreased cell viability in A549 cell line in a dose-dependent manner. Also, this antiproliferative effect of capsaicin was selective compared to L929 cell line. On the other hand, apoptosis inducing effects of capsaicin were studied by Annexin V-FITC and Caspase 3 assays by using IC50 and IC50/2 concentrations on A549 cell by flow cytometric methods. Our results revealed that the anticancer effects induced by capsaicin on A549 cell line involved apoptosis by inducing Caspase 3 pathway.
{"title":"Capsaicin inhibits proliferation and induces apoptosis in human lung adenocarcinoma A549 cell line","authors":"Merve Tiltay, Aydan Hüseynli, Gülşen Akalın Çiftçi, İ. Ö. Alatas","doi":"10.55971/ejls.1151479","DOIUrl":"https://doi.org/10.55971/ejls.1151479","url":null,"abstract":"Capsaicin is the main component of many hot peppers, exerts anticancer effects on various cancer cells by inducing apoptotic pathways. In addition, the ineffectiveness of this apoptotic effect of capsaicin on healthy cells provides a wide-ranging use of capsaicin. In recent years, many studies have been carried out to determine the safety of capsaicin use in lung cancer, which is a common cancer type worldwide with high mortality rates. In the present study anticancer effects of capsaicin were studied on A549 human lung adenocarcinoma cell line. Also, citotoxicity of this compound was studied on L929 mouse embryonic fibroblast cell line. Various concentration of capsaicin (3.90625-500 μM) effectively decreased cell viability in A549 cell line in a dose-dependent manner. Also, this antiproliferative effect of capsaicin was selective compared to L929 cell line. On the other hand, apoptosis inducing effects of capsaicin were studied by Annexin V-FITC and Caspase 3 assays by using IC50 and IC50/2 concentrations on A549 cell by flow cytometric methods. Our results revealed that the anticancer effects induced by capsaicin on A549 cell line involved apoptosis by inducing Caspase 3 pathway.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"121643992","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}
Astragalus tmoleus Boiss. var. bounacanthus (Boiss.) Chamberlain is a member of the Pterophorus Bunge section of the Fabaceae family and consists of the spiny cushion-forming shrub. In this study, morphological, anatomical and pollen properties of the plant, an endemic species for Turkey, have been investigated in detail. Morphological characters such as the shape of paripinnate leaves, stipules and bracts, the flower number in the inflorescence, the stenonychioid type of standard and the reniform type of seed can be helpful to distinguish A. tmoleus var. bounacanthus. The stem, leaf and rachis characteristics of the plant were examined in anatomical studies. There is a secondary growth in stem anatomy. The number of vascular bundles is 15-18 in a circle. The shape of the transversal section of the rachis is polygonal or almost orbicular. The sclerenchyma tissue is located on the vascular bundles in the rachis. A. tmoleus var. bounacanthus has equifasial leaves. The stomata type is anomocytic and occurs on both leaflet epidermises. The pollen grains of A. tmoleus var. bounacanthus have tricolpate aperture and they are subprolate-shaped. While the pollen exine sculpturing is microreticulate, the seed surface sculpturing is a prominent undulate-ridged pattern formed by irregular cells. Scanning electron microscopy (SEM) is used to determine pollen and seed morphology.
{"title":"Morpho-anatomical and palynological properties of endemic Astragalus tmoleus var. bounacanthus (Fabaceae)","authors":"A. Kaya","doi":"10.55971/ejls.1147134","DOIUrl":"https://doi.org/10.55971/ejls.1147134","url":null,"abstract":"Astragalus tmoleus Boiss. var. bounacanthus (Boiss.) Chamberlain is a member of the Pterophorus Bunge section of the Fabaceae family and consists of the spiny cushion-forming shrub. In this study, morphological, anatomical and pollen properties of the plant, an endemic species for Turkey, have been investigated in detail. Morphological characters such as the shape of paripinnate leaves, stipules and bracts, the flower number in the inflorescence, the stenonychioid type of standard and the reniform type of seed can be helpful to distinguish A. tmoleus var. bounacanthus. The stem, leaf and rachis characteristics of the plant were examined in anatomical studies. There is a secondary growth in stem anatomy. The number of vascular bundles is 15-18 in a circle. The shape of the transversal section of the rachis is polygonal or almost orbicular. The sclerenchyma tissue is located on the vascular bundles in the rachis. A. tmoleus var. bounacanthus has equifasial leaves. The stomata type is anomocytic and occurs on both leaflet epidermises. The pollen grains of A. tmoleus var. bounacanthus have tricolpate aperture and they are subprolate-shaped. While the pollen exine sculpturing is microreticulate, the seed surface sculpturing is a prominent undulate-ridged pattern formed by irregular cells. Scanning electron microscopy (SEM) is used to determine pollen and seed morphology.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"19 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131356111","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}
Zeynep Gülcan, N. Saltan, G. İşcan, M. Kürkçüoǧlu, Y. Köse
Sideritis L. (Lamiaceae) is represented by 45 species in Flora of Turkey. Sideritis lanata L. (Hairy ironwort) is located in the north-west, west, south-west and central Anatolia. Mountain tea (Sideritis plants) is used as a traditional remedy against common cold and gastrointestinal disorders. Its beneficial properties are attributed to its rich bioactive constituents. In this study, the antioxidant activities of the extracts of Sideritis lanata prepared using different solvents (n-hexane, ethyl acetate, and 70% ethanol) from the aerial parts were determined by DPPH· scavenging effect assay. Also; determined of the antimicrobial activity of S. lanata extracts against 4 bacteria and 5 Candida species. Dried aerial parts of Sideritis were subjected to hydrodistillation and the oil obtained was analyzed by using GC and GC/MS. S. lanata extracts prepared with 70% ethanol was found to have a higher DPPH· scavenging activity (IC50= 0.241 mg/mL) than extracts prepared with other solvents. All extracts showed generally weak inhibitory effects (500-8000 μg/mL, MIC) against bacterial strains. Inhibitory doses against the tested Candida species were determined between 125-4000 μg/mL. The 70% ethanol extract of S. lanata inhibited Candida tropicalis (ATCC 750) (MIC: 125 μg/mL).
{"title":"Antimicrobial and antioxidant activities of Sideritis lanata L. extracts","authors":"Zeynep Gülcan, N. Saltan, G. İşcan, M. Kürkçüoǧlu, Y. Köse","doi":"10.55971/ejls.1181461","DOIUrl":"https://doi.org/10.55971/ejls.1181461","url":null,"abstract":"Sideritis L. (Lamiaceae) is represented by 45 species in Flora of Turkey. Sideritis lanata L. (Hairy ironwort) is located in the north-west, west, south-west and central Anatolia. Mountain tea (Sideritis plants) is used as a traditional remedy against common cold and gastrointestinal disorders. Its beneficial properties are attributed to its rich bioactive constituents. In this study, the antioxidant activities of the extracts of Sideritis lanata prepared using different solvents (n-hexane, ethyl acetate, and 70% ethanol) from the aerial parts were determined by DPPH· scavenging effect assay. Also; determined of the antimicrobial activity of S. lanata extracts against 4 bacteria and 5 Candida species. Dried aerial parts of Sideritis were subjected to hydrodistillation and the oil obtained was analyzed by using GC and GC/MS. S. lanata extracts prepared with 70% ethanol was found to have a higher DPPH· scavenging activity (IC50= 0.241 mg/mL) than extracts prepared with other solvents. All extracts showed generally weak inhibitory effects (500-8000 μg/mL, MIC) against bacterial strains. Inhibitory doses against the tested Candida species were determined between 125-4000 μg/mL. The 70% ethanol extract of S. lanata inhibited Candida tropicalis (ATCC 750) (MIC: 125 μg/mL).","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"47 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"126834072","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}
This study was carried out to determine the content of the essential oils of Salvia absconditiflora Greuter & Burdet populations which are naturally found in Mediterranean, Iran-Turan and Euro-Sibirya phytogeographical regions. S. absconditiflora plant samples were collected from eight different provinces (Aksaray, Kahramanmaraş, Karaman, Kayseri, Konya, Niğde, Nevşehir and Yozgat) of Turkey. Essential oils of plant samples were isolated by the hydro-distillation method using a Clevenger- type apparatus and the components were determined by GC-FID and GC- MS analysis. Although the major components of S. absconditiflora were found as α-pinene, camphene, 1,8-cineole, camphor, and borneol in almost all samples β-pinene, β-caryophyllene, bornyl acetate, caryophyllene oxide, β-eudesmol and valeranone were recorded as the other important components in some samples.
{"title":"Geographical impact on essential oil composition of endemic Salvia absconditiflora collected from different parts of Turkey","authors":"A. Kaya, S. Doğu, B. Demirci","doi":"10.55971/ejls.1140861","DOIUrl":"https://doi.org/10.55971/ejls.1140861","url":null,"abstract":"This study was carried out to determine the content of the essential oils of Salvia absconditiflora Greuter & Burdet populations which are naturally found in Mediterranean, Iran-Turan and Euro-Sibirya phytogeographical regions. S. absconditiflora plant samples were collected from eight different provinces (Aksaray, Kahramanmaraş, Karaman, Kayseri, Konya, Niğde, Nevşehir and Yozgat) of Turkey. Essential oils of plant samples were isolated by the hydro-distillation method using a Clevenger- type apparatus and the components were determined by GC-FID and GC- MS analysis. Although the major components of S. absconditiflora were found as α-pinene, camphene, 1,8-cineole, camphor, and borneol in almost all samples β-pinene, β-caryophyllene, bornyl acetate, caryophyllene oxide, β-eudesmol and valeranone were recorded as the other important components in some samples.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-11-10","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"133494665","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}
High density lipoproteins (HDLs) are complex lipid carriers which replace their own structures and functions according to different conditions including healthy or pathological status. HDL has substantial roles in reverse cholesterol transport system for regulation of lipid metabolism. Also HDL has many functions such as antiinflammation, antioxidation, antithrombotic and vasodilator actions. However, these functions may be compromised under pathological conditions. Nowadays, it’s known that the function of HDL is more important than it’s dose for preventing against cardiovascular diseases. This review mostly summarizes available information of HDL structure, metabolism and the real information related to the physicochemical changes of HDLs causing their different functions. Also HDLs, that lost their protective functions have been associated with oxidative stress and systemic inflammation diseases.
{"title":"High-density lipoprotein: Quality is more important than quantity!","authors":"Ipek Ertorun, G. Çiftçi, Ö. Alataş","doi":"10.55971/ejls.1099595","DOIUrl":"https://doi.org/10.55971/ejls.1099595","url":null,"abstract":"High density lipoproteins (HDLs) are complex lipid carriers which replace their own structures and functions according to different conditions including healthy or pathological status. HDL has substantial roles in reverse cholesterol transport system for regulation of lipid metabolism. Also HDL has many functions such as antiinflammation, antioxidation, antithrombotic and vasodilator actions. However, these functions may be compromised under pathological conditions. Nowadays, it’s known that the function of HDL is more important than it’s dose for preventing against cardiovascular diseases. This review mostly summarizes available information of HDL structure, metabolism and the real information related to the physicochemical changes of HDLs causing their different functions. Also HDLs, that lost their protective functions have been associated with oxidative stress and systemic inflammation diseases.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"49 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114492972","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}
Derya Osmaniye, B. Sağlık, Serkan Levent, Y. Özkay, Z. Kaplancıklı
Monoamine oxidase (MAO) enzymes have an important place in neurodegenerative diseases. While MAO-A inhibitors are used in depression; MAO-B enzyme has an important place in Parkinson's disease. Within the scope of this study, 7 new piperazine-dithiocarbamate derivative compounds were synthesized. Structure determinations of the compounds were performed using 1H-NMR, 13C-NMR and HRMS spectroscopic methods. The MAO inhibitory activities of the compounds were determined by in vitro fluorometric methods. According to the obtained results, compound 2d with IC50=0.108±0.004 µM; compound 2e exhibited inhibitory activity with an IC50=0.074±0.003 µM.
{"title":"Synthesis and characterization of new Piperazine-Dithiocarbamate compounds as potent MAO-A inhibitors","authors":"Derya Osmaniye, B. Sağlık, Serkan Levent, Y. Özkay, Z. Kaplancıklı","doi":"10.55971/ejls.1089254","DOIUrl":"https://doi.org/10.55971/ejls.1089254","url":null,"abstract":"Monoamine oxidase (MAO) enzymes have an important place in neurodegenerative diseases. While MAO-A inhibitors are used in depression; MAO-B enzyme has an important place in Parkinson's disease. Within the scope of this study, 7 new piperazine-dithiocarbamate derivative compounds were synthesized. Structure determinations of the compounds were performed using 1H-NMR, 13C-NMR and HRMS spectroscopic methods. The MAO inhibitory activities of the compounds were determined by in vitro fluorometric methods. According to the obtained results, compound 2d with IC50=0.108±0.004 µM; compound 2e exhibited inhibitory activity with an IC50=0.074±0.003 µM.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"50 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123033889","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}
M. Altıntop, Belgin Sever, H. Temel, Z. Kaplancıklı, A. Özdemir
Inhibition of cyclooxygenases (COXs), by selective and nonselective inhibitors, is a favorable approach for pharmacologic intervention in a variety of disorders such as cancer. For this purpose, a new class of tetrazole-hydrazone hybrids (1-12) was designed. A facile and efficient procedure was applied for the preparation of compounds 1-12, which were tested for their inhibitory activities towards cyclooxygenases (COXs) by means of an in vitro colorimetric method. The most potent and selective COX-1 inhibitors were determined as 2-[(1-methyl-1H-tetrazol-5-yl)thio]-N'-(4-(piperidin-1-yl)benzylidene)acetohydrazide (1) (40.88±2.79%) and 2-[(1-methyl-1H-tetrazol-5-yl)thio]-N'-(4-(morpholin-4-yl)benzylidene)acetohydrazide (2) (39.80±2.78%), whereas the most potent and selective COX-2 inhibitor was found as 2-[(1-phenyl-1H-tetrazol-5-yl)thio]-N'-(4-(pyrrolidin-1-yl)benzylidene)acetohydrazide (10) (42.38±1.16%). In general, 1-methyl-1H-tetrazole moiety resulted in selective COX-1 inhibition, whereas 1-phenyl-1H-tetrazole moiety gave rise to preferential COX-2 inhibition.
选择性和非选择性抑制剂抑制环加氧酶(cox)是多种疾病(如癌症)的药物干预的有利途径。为此，设计了一类新的四唑-腙杂化物(1-12)。采用简便高效的方法制备了化合物1 ~ 12，并用体外比色法测定了化合物1 ~ 12对环氧合酶(cox)的抑制活性。结果表明，COX-1抑制剂2-[(1-甲基- 1h -四氮唑-5-基)硫代]- n '-(4-(1-甲基- 1h -四氮唑-5-基)硫代]- n '-(4-(1-甲基- 1h -四氮唑-5-基)硫代]- n '-(4-(morpholin-4-基)苄基)乙酰肼(2)(39.80±2.78%)，而COX-2抑制剂2-[(1-苯基- 1h -四氮唑-5-基)硫代]- n '-(4-(吡咯烷-1-基)苄基)乙酰肼(10)(42.38±1.16%)。一般来说，1-甲基- 1h -四唑片段导致选择性抑制COX-1，而1-苯基- 1h -四唑片段导致优先抑制COX-2。
{"title":"Design, Synthesis and In vitro COX Inhibitory Profiles of A New Series of Tetrazole-based Hydrazones","authors":"M. Altıntop, Belgin Sever, H. Temel, Z. Kaplancıklı, A. Özdemir","doi":"10.55971/ejls.1095818","DOIUrl":"https://doi.org/10.55971/ejls.1095818","url":null,"abstract":"Inhibition of cyclooxygenases (COXs), by selective and nonselective inhibitors, is a favorable approach for pharmacologic intervention in a variety of disorders such as cancer. For this purpose, a new class of tetrazole-hydrazone hybrids (1-12) was designed. A facile and efficient procedure was applied for the preparation of compounds 1-12, which were tested for their inhibitory activities towards cyclooxygenases (COXs) by means of an in vitro colorimetric method. The most potent and selective COX-1 inhibitors were determined as 2-[(1-methyl-1H-tetrazol-5-yl)thio]-N'-(4-(piperidin-1-yl)benzylidene)acetohydrazide (1) (40.88±2.79%) and 2-[(1-methyl-1H-tetrazol-5-yl)thio]-N'-(4-(morpholin-4-yl)benzylidene)acetohydrazide (2) (39.80±2.78%), whereas the most potent and selective COX-2 inhibitor was found as 2-[(1-phenyl-1H-tetrazol-5-yl)thio]-N'-(4-(pyrrolidin-1-yl)benzylidene)acetohydrazide (10) (42.38±1.16%). In general, 1-methyl-1H-tetrazole moiety resulted in selective COX-1 inhibition, whereas 1-phenyl-1H-tetrazole moiety gave rise to preferential COX-2 inhibition.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"1 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"131216476","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}
M. Kürkçüoǧlu, H. G. Ağalar, B. Temiz, A. Duran, K. Başer
This study was aimed to evaluate the essential oil composition of Chaerophyllum libanoticum fruits and its potential uses in the cosmetic industry. The essential oil was analyzed by Gas Chromatography (GC) and Gas Chromatography-Mass Spectrometry (GC/MS) systems, simultaneously. The yield of essential oil was calculated as 0.22 % (v/w). Major components of the oil were characterized as limonene (26.7%), p-cymene (25.5%), and β-phellandrene (7.0%). In addition, antioxidant and antityrosinase activities of the essential oil were evaluated. The oil exhibited moderate antioxidant activity (TEAC). In the DPPH assay, the oil was tested at 5 mg/mL concentration, and the inhibition ratio was calculated as 31.3 ± 1.1%. At 1 mg/mL of concentration, TEAC (mmol/L) value was determined as 0.027 ± 0.008. As evidence to its skin whitening properties, the oil inhibited the tyrosinase 17.7 ± 1.6 % at 1 mg/mL.
{"title":"Chaerophyllum libanoticum Boiss. Et Kotschy: The fruit essential oil, composition, skin-whitening and antioxidant activities","authors":"M. Kürkçüoǧlu, H. G. Ağalar, B. Temiz, A. Duran, K. Başer","doi":"10.55971/ejls.1095855","DOIUrl":"https://doi.org/10.55971/ejls.1095855","url":null,"abstract":"This study was aimed to evaluate the essential oil composition of Chaerophyllum libanoticum fruits and its potential uses in the cosmetic industry. The essential oil was analyzed by Gas Chromatography (GC) and Gas Chromatography-Mass Spectrometry (GC/MS) systems, simultaneously. The yield of essential oil was calculated as 0.22 % (v/w). Major components of the oil were characterized as limonene (26.7%), p-cymene (25.5%), and β-phellandrene (7.0%). In addition, antioxidant and antityrosinase activities of the essential oil were evaluated. The oil exhibited moderate antioxidant activity (TEAC). In the DPPH assay, the oil was tested at 5 mg/mL concentration, and the inhibition ratio was calculated as 31.3 ± 1.1%. At 1 mg/mL of concentration, TEAC (mmol/L) value was determined as 0.027 ± 0.008. As evidence to its skin whitening properties, the oil inhibited the tyrosinase 17.7 ± 1.6 % at 1 mg/mL.","PeriodicalId":176179,"journal":{"name":"European Journal of Life Sciences","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2022-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"128708437","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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