Pub Date : 2023-09-30DOI: 10.2174/0115734072270060230921093431
Sonia Singh, Manas Kumar Jha
A Proprotein convertase subtilisin/kexin type-9 is considered a zymogen, extensively found in the liver. PCSK9 is found in circulation in the plasma, where it attaches to low-density lipoprotein (LDL) receptors on the cell surface, is internalized, and subsequently directs the receptors to be degraded by lysosomes. Investigations of naturally or organically found PCSK9 gene variations, which generated high levels of plasma LDL cholesterol deviations and varied atherosclerosis proportion factors, released floods of pharmaceutical along with biological and live sciences research into the world. Significant advances in our understanding of the physiological control of PCSK9 led quickly to the development of biological inhibitors of PCSK9 that are now available for purchase. These inhibitors decreased LDL cholesterol levels with other improved cardiovascular outcomes. The current manuscript will show the rapid development of PCSK9, beginning with its discovery as a novel gene and progressing through its use as a therapeutic target, followed by its testing on animals and humans and, eventually, its use in outcome trials and clinical applications.
{"title":"Review on PCSK9: A Pertinent Therapeutic Target in Cardiovascular Disease","authors":"Sonia Singh, Manas Kumar Jha","doi":"10.2174/0115734072270060230921093431","DOIUrl":"https://doi.org/10.2174/0115734072270060230921093431","url":null,"abstract":"A Proprotein convertase subtilisin/kexin type-9 is considered a zymogen, extensively found in the liver. PCSK9 is found in circulation in the plasma, where it attaches to low-density lipoprotein (LDL) receptors on the cell surface, is internalized, and subsequently directs the receptors to be degraded by lysosomes. Investigations of naturally or organically found PCSK9 gene variations, which generated high levels of plasma LDL cholesterol deviations and varied atherosclerosis proportion factors, released floods of pharmaceutical along with biological and live sciences research into the world. Significant advances in our understanding of the physiological control of PCSK9 led quickly to the development of biological inhibitors of PCSK9 that are now available for purchase. These inhibitors decreased LDL cholesterol levels with other improved cardiovascular outcomes. The current manuscript will show the rapid development of PCSK9, beginning with its discovery as a novel gene and progressing through its use as a therapeutic target, followed by its testing on animals and humans and, eventually, its use in outcome trials and clinical applications.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"45 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135037773","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: Bioactive peptides derived from soybeans have recently been identified as having potential health benefits for preventing and curing cancer and cardiovascular disorders. This narrative review focuses on the potential role of these peptides in such conditions and the possible mechanisms by which they may act. Soybean-derived bioactive peptides have been found to possess antitumor, antioxidant, anti-inflammatory, and cholesterol-lowering effects. Animal and in vitro studies have demonstrated that these peptides can modulate multiple signaling pathways, including those involved in the regulation of apoptosis, angiogenesis, and cell proliferation. Furthermore, they may protect against oxidative stress and lipid accumulation, which are associated with cancer and cardiovascular diseases. Also, soybean peptides have been shown to stop enzymes from breaking down cancer-causing chemicals and reduce the production of pro-inflammatory cytokines, which are linked to a higher risk of heart disease. The potential of soybean-derived peptides as a therapeutic tool in cancer and cardiovascular diseases is promising. However, further studies are needed to elucidate their mechanisms of action and assess their safety and efficacy in clinical settings.
{"title":"The Potential Role of Soybean Bioactive Peptides in the Prevention and Cure of Carcinoma and Cardiovascular Disorder","authors":"Kuldeep Singh, Jeetendra Kumar Gupta, Shivendra Kumar, Talever Singh","doi":"10.2174/1573407219666230907115809","DOIUrl":"https://doi.org/10.2174/1573407219666230907115809","url":null,"abstract":"Abstract: Bioactive peptides derived from soybeans have recently been identified as having potential health benefits for preventing and curing cancer and cardiovascular disorders. This narrative review focuses on the potential role of these peptides in such conditions and the possible mechanisms by which they may act. Soybean-derived bioactive peptides have been found to possess antitumor, antioxidant, anti-inflammatory, and cholesterol-lowering effects. Animal and in vitro studies have demonstrated that these peptides can modulate multiple signaling pathways, including those involved in the regulation of apoptosis, angiogenesis, and cell proliferation. Furthermore, they may protect against oxidative stress and lipid accumulation, which are associated with cancer and cardiovascular diseases. Also, soybean peptides have been shown to stop enzymes from breaking down cancer-causing chemicals and reduce the production of pro-inflammatory cytokines, which are linked to a higher risk of heart disease. The potential of soybean-derived peptides as a therapeutic tool in cancer and cardiovascular diseases is promising. However, further studies are needed to elucidate their mechanisms of action and assess their safety and efficacy in clinical settings.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"155 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135096562","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-31DOI: 10.2174/1573407219666230831091213
Leonid A. Yakovishin, Sergey V. Bukharov, Vasily M. Babaev, Elena V. Nikitina, Elena S. Bulatova
Aims: The study aimed to search of new molecular complexes of licorice saponin with fluoroquinolone antibiotics and to explore their pharmaceutical potential. Background: Molecular complexation of triterpene glycosides with pharmaceutical substances reduces side effects and therapeutic doses, increases bioavailability and stability, and expands the spectrum of biological activity of drugs. Glycyrrhizic acid is the major triterpene glycoside of licorice. Molecular complexes of monoammonium salt of glycyrrhizic acid (glycyram, GC) with fluoroquinolone antibiotics have not been described. Objectives: This study is devoted to the preparation and analysis of molecular complexes of GC with fluoroquinolones, and investigation of their antimicrobial activity. Methods: Complexation was studied via FT-IR spectroscopy, UV-Vis spectroscopy and mass spectrometry methods. Results: Molecular complexes of GC with fluoroquinolone antibiotics, along with their benzylated derivatives, were obtained for the first time. Conclusion: The complexes composition was defined as 1:1. Intermolecular hydrogen bonds are formed during complexation. In addition, stability constants of 105 М–1 order were calculated. Some complexes are comparable in antimicrobial activity with individual antibiotics ciprofloxacin (CP) and moxifloxacin (Moc) or surpass them in relation to a number of bacteria. These molecular complexes could be potential low-dose drugs with antimicrobial activity.
{"title":"New Molecular Complexes of Glycyrrhizic Acid Monoammonium Salt (Glycyram) with Fluoroquinolone Antibiotics","authors":"Leonid A. Yakovishin, Sergey V. Bukharov, Vasily M. Babaev, Elena V. Nikitina, Elena S. Bulatova","doi":"10.2174/1573407219666230831091213","DOIUrl":"https://doi.org/10.2174/1573407219666230831091213","url":null,"abstract":"Aims: The study aimed to search of new molecular complexes of licorice saponin with fluoroquinolone antibiotics and to explore their pharmaceutical potential. Background: Molecular complexation of triterpene glycosides with pharmaceutical substances reduces side effects and therapeutic doses, increases bioavailability and stability, and expands the spectrum of biological activity of drugs. Glycyrrhizic acid is the major triterpene glycoside of licorice. Molecular complexes of monoammonium salt of glycyrrhizic acid (glycyram, GC) with fluoroquinolone antibiotics have not been described. Objectives: This study is devoted to the preparation and analysis of molecular complexes of GC with fluoroquinolones, and investigation of their antimicrobial activity. Methods: Complexation was studied via FT-IR spectroscopy, UV-Vis spectroscopy and mass spectrometry methods. Results: Molecular complexes of GC with fluoroquinolone antibiotics, along with their benzylated derivatives, were obtained for the first time. Conclusion: The complexes composition was defined as 1:1. Intermolecular hydrogen bonds are formed during complexation. In addition, stability constants of 105 М–1 order were calculated. Some complexes are comparable in antimicrobial activity with individual antibiotics ciprofloxacin (CP) and moxifloxacin (Moc) or surpass them in relation to a number of bacteria. These molecular complexes could be potential low-dose drugs with antimicrobial activity.","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"27 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-08-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135944220","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-25DOI: 10.2174/1573407219666230825103621
Gowramma Byran, P. Patel, Preeya Negi, Sowmiya Arun, Kaviarasan Lakshmanan, K. Rajagopal, G. Swaminathan
Nuclear enzyme poly (ADP-ribose) polymerase-1 (PARP-1) controls the cell cycle, DNA repair, transcription, and replication processes. In this study, olaparib and rucaparib have been taken as standard drugs for comparison of results. As per previous research data, 1,3,4-Oxadiazole moiety has multidirectional biological activity and shows high activity against cancer. This study aimed to carry out the in silico ligand-based screening for the identification of hits for PARP1 inhibitors bearing 1,3,4-thiadiazole derivatives using Schrodinger suite 2022-1 and to perform MMGBSA and molecular dynamics simulation for lead molecules. A total of 32 derivatives of 1,3,4-Oxadiazole were designed with four different acids: phenoxy acetic acid, 1-Naphthoxy acetic acid, 2-Naphthoxy acetic acid, and piperonylic acid. Molecular docking (XP) studies were performed between 4ZZZ.pdb and the designed analogues, and the binding affinity values lay in the range of -8.52 to -3.52 kcal/mol. 2D interactions between the protein and the ligand were observed. Based on the binding affinity values and ADMET results, top 10 analogues were selected for performing MM-GBSA.A total of 32 derivatives of 1,3,4-Oxadiazole were designed with four different acids that are Phenoxy acetic acid, 1-Naphthoxy acetic acid, 2-Naphthoxy acetic acid, and Piperonylic acid. Molecular docking (XP) studies were performed between 4ZZZ.pdb and the designed analogues and the binding affinity values lie in the range of -8.52 to -3.52 kcal/mol. 2D interactions between the protein and the ligand are observed. Based on the binding affinity values and ADMET results top 10 analogues were selected for performing MM-GBSA. The dG-bind score of the top compounds varied from -2.30 to -60.67 kcal/mol, and analogue D4 was selected for MD simulation studies for 100ns. Results of Molecular dynamics (MD) studies showed that D4 interacted with amino acid residues, and the ligand-protein interaction stabilized from 58-90ns. The in silico study's findings suggested that the chemicals A1, A3, B1, B2, B3, B4, C1, C6, D1, and D4 might be significantly active against breast cancer with potential therapeutic benefits and are likely to be useful after further development. In conclusion, numerous molecules exhibit a high affinity for PARP-1 when derived from 1,3,4-oxadiazole. The in silico study's findings suggested that the chemicals A1, A3, B1, B2, B3, B4, C1, C6, D1, and D4 might be significantly active against breast cancer with potential therapeutic benefits and are likely to be useful after further development.
{"title":"Anticancer Activity of Novel 1,3,4-oxadiazole Derivatives against PARP-1 Inhibitors: An In-silico Approach","authors":"Gowramma Byran, P. Patel, Preeya Negi, Sowmiya Arun, Kaviarasan Lakshmanan, K. Rajagopal, G. Swaminathan","doi":"10.2174/1573407219666230825103621","DOIUrl":"https://doi.org/10.2174/1573407219666230825103621","url":null,"abstract":"\u0000\u0000Nuclear enzyme poly (ADP-ribose) polymerase-1 (PARP-1) controls the cell cycle, DNA repair, transcription, and replication processes. In this study, olaparib and rucaparib have been taken as standard drugs for comparison of results. As per previous research data, 1,3,4-Oxadiazole moiety has multidirectional biological activity and shows high activity against cancer.\u0000\u0000\u0000\u0000This study aimed to carry out the in silico ligand-based screening for the identification of hits for PARP1 inhibitors bearing 1,3,4-thiadiazole derivatives using Schrodinger suite 2022-1 and to perform MMGBSA and molecular dynamics simulation for lead molecules.\u0000\u0000\u0000\u0000A total of 32 derivatives of 1,3,4-Oxadiazole were designed with four different acids: phenoxy acetic acid, 1-Naphthoxy acetic acid, 2-Naphthoxy acetic acid, and piperonylic acid. Molecular docking (XP) studies were performed between 4ZZZ.pdb and the designed analogues, and the binding affinity values lay in the range of -8.52 to -3.52 kcal/mol. 2D interactions between the protein and the ligand were observed. Based on the binding affinity values and ADMET results, top 10 analogues were selected for performing MM-GBSA.A total of 32 derivatives of 1,3,4-Oxadiazole were designed with four different acids that are Phenoxy acetic acid, 1-Naphthoxy acetic acid, 2-Naphthoxy acetic acid, and Piperonylic acid. Molecular docking (XP) studies were performed between 4ZZZ.pdb and the designed analogues and the binding affinity values lie in the range of -8.52 to -3.52 kcal/mol. 2D interactions between the protein and the ligand are observed. Based on the binding affinity values and ADMET results top 10 analogues were selected for performing MM-GBSA.\u0000\u0000\u0000\u0000The dG-bind score of the top compounds varied from -2.30 to -60.67 kcal/mol, and analogue D4 was selected for MD simulation studies for 100ns. Results of Molecular dynamics (MD) studies showed that D4 interacted with amino acid residues, and the ligand-protein interaction stabilized from 58-90ns. The in silico study's findings suggested that the chemicals A1, A3, B1, B2, B3, B4, C1, C6, D1, and D4 might be significantly active against breast cancer with potential therapeutic benefits and are likely to be useful after further development.\u0000\u0000\u0000\u0000In conclusion, numerous molecules exhibit a high affinity for PARP-1 when derived from 1,3,4-oxadiazole. The in silico study's findings suggested that the chemicals A1, A3, B1, B2, B3, B4, C1, C6, D1, and D4 might be significantly active against breast cancer with potential therapeutic benefits and are likely to be useful after further development.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47469704","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-25DOI: 10.2174/1573407219666230825141438
Sabah Salahvarzi, F. Nadipour, Zeynab Dadgar
Pyrazolidine 5,3-dione derivatives have a wide range of biological and pharmacological activities and play an important role in the sub-structures of various drugs. They also have inhibitory and antimicrobial properties, anti-tumor, anti-inflammatory, analgesic, anti-tuberculosis, anti-hypertensive, anti-cancer, and anti-Alzheimer. The purpose of the current study was to investigate a number of synthesis methods of pyrazolidine-3,5-dione and 1 phenylpyrazolidine-3,5-dione in the presence and absence of ultrasound bath and their anti-cancer effects on mcf-7 breast cancer cells. In this study, pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione were synthesized using hydrazine, phenylhydrazine, and diethyl malonate by different methods. The advantage of this research compared to other studies is the use of different methods (3 methods and each method were performed in two different conditions, toalling 6 methods) for the synthesis of these two derivatives. The effect of two synthesized derivatives on MCF-7 cell line breast cancer cells was also investigated using MTT (methylthiazole tetrazolium) test. IR, 13CNMR, and HNMR spectroscopy methods have also been used to determine the structure of products. The results of FT-IR and NMR spectrum analysis confirm the synthesized pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione. Based on the results in zero doses (control group) and 10 μM of all Samples after 24 hours, no significant difference in the number of cells was observed. However, the number of cells significantly decreased after treatment with 20 μM dose of both pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione. Also, there was no significant difference in reducing cancer cell proliferation between pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione samples. In addition, treatment of cancer cells with 40 μM of both hydrazine and phenylhydrazine samples after 24 hours caused approximately 50% cell death and reduced the number of cancer cells by approximately half compared to the control group. According to the results of this study, treatment of cancer cells with a dose of 40 μM in both samples of pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione after 24 hours caused cell death in approximately 50% of cells and the number of cancer cells is almost half that of the control group.
{"title":"Investigating the Synthesis Methods of 3,5-Dione Pyrazolidine and 3,5-Dione 1-Phenylpyrazolidine in the Presence and Absence Of Ultrasound Bath and their Anticancer Effects on MCF-7 Breast Cancer Cells","authors":"Sabah Salahvarzi, F. Nadipour, Zeynab Dadgar","doi":"10.2174/1573407219666230825141438","DOIUrl":"https://doi.org/10.2174/1573407219666230825141438","url":null,"abstract":"\u0000\u0000Pyrazolidine 5,3-dione derivatives have a wide range of biological and pharmacological activities and play an important role in the sub-structures of various drugs. They also have inhibitory and antimicrobial properties, anti-tumor, anti-inflammatory, analgesic, anti-tuberculosis, anti-hypertensive, anti-cancer, and anti-Alzheimer. The purpose of the current study was to investigate a number of synthesis methods of pyrazolidine-3,5-dione and 1 phenylpyrazolidine-3,5-dione in the presence and absence of ultrasound bath and their anti-cancer effects on mcf-7 breast cancer cells.\u0000\u0000\u0000\u0000In this study, pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione were synthesized using hydrazine, phenylhydrazine, and diethyl malonate by different methods. The advantage of this research compared to other studies is the use of different methods (3 methods and each method were performed in two different conditions, toalling 6 methods) for the synthesis of these two derivatives. The effect of two synthesized derivatives on MCF-7 cell line breast cancer cells was also investigated using MTT (methylthiazole tetrazolium) test. IR, 13CNMR, and HNMR spectroscopy methods have also been used to determine the structure of products.\u0000\u0000\u0000\u0000The results of FT-IR and NMR spectrum analysis confirm the synthesized pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione. Based on the results in zero doses (control group) and 10 μM of all Samples after 24 hours, no significant difference in the number of cells was observed. However, the number of cells significantly decreased after treatment with 20 μM dose of both pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione. Also, there was no significant difference in reducing cancer cell proliferation between pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione samples. In addition, treatment of cancer cells with 40 μM of both hydrazine and phenylhydrazine samples after 24 hours caused approximately 50% cell death and reduced the number of cancer cells by approximately half compared to the control group.\u0000\u0000\u0000\u0000According to the results of this study, treatment of cancer cells with a dose of 40 μM in both samples of pyrazolidine-3,5-dione and 1-phenylpyrazolidine-3,5-dione after 24 hours caused cell death in approximately 50% of cells and the number of cancer cells is almost half that of the control group.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49298836","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-16DOI: 10.2174/1573407219666230816091455
V. Goulas, A. Christou, Aristi Alkiviadi
Olive oil is rich in monounsaturated fatty acids and is an essential Mediterranean diet component. Many of its health benefits are associated with the presence of phenolic compounds. Several strategies for the enhancement of the phenolic content and, more specifically, the concentration of hydroxytyrosol derivatives in olive oils have been proposed, as extra virgin olive oil (EVOO) of high phenolic content is preferred by health-conscious consumers. The supplementation of EVOO with hydroxytyrosol derivatives from olive leaf extract was performed with the employment of ultrasound-assisted maceration at different concentration levels (2 g·L-1 oil and 4 g L-1 oil), temperatures (20 and 40 oC), and maceration times (20 and 40 min). The phenolic contents of enriched EVOOs were determined by spectrophotometric and HPLC methods. In addition, the effect of supplementation on the physicochemical parameters of EVOOs, namely acidity and extinction coefficients (K232 and K270), was also studied. The addition of extract slightly increased the acidity values and extinction coefficients of the samples, and at the same time, it significantly improved their phenolic composition. The use of appropriate ultrasound-assisted maceration parameters (addition of olive leaf extract at a concentration level of 2 g L-1 at 20 oC for 20 min) provided EVOO with acceptable values for total acidity (<0.8%), K232 (<2.5), and K270 (<0.22), high contents of total phenolics and flavonoids, and improved hydroxytyrosol derivative contents. The enrichment of EVOO with leaf extract is a promising strategy to enhance its content in hydroxytyrosol derivatives, providing premium EVOOs with respect to their bioactive composition.
橄榄油富含单不饱和脂肪酸，是地中海饮食中必不可少的成分。它的许多健康益处都与酚类化合物的存在有关。由于高酚含量的特级初榨橄榄油（EVOO）是注重健康的消费者的首选，因此已经提出了几种提高橄榄油中酚含量，更具体地说，提高羟基酪醇衍生物浓度的策略。用橄榄叶提取物中的羟基酪醇衍生物补充EVOO是通过在不同浓度水平（2g·L-1油和4g L-1油）、温度（20和40℃）和浸渍时间（20和40min）下使用超声辅助浸渍进行的。采用分光光度法和高效液相色谱法测定了富集EVOO中酚类物质的含量。此外，还研究了添加对EVOO的物理化学参数，即酸度和消光系数（K232和K270）的影响。提取物的加入略微提高了样品的酸度和消光系数，同时显著改善了样品的酚类组成。使用适当的超声辅助浸渍参数（在20℃下以2 g L-1的浓度添加橄榄叶提取物20分钟）为EVOO提供了总酸度（<0.8%）、K232（<2.5）和K270（<0.22）的可接受值，总酚和类黄酮含量高，羟基酪醇衍生物含量提高。用叶提取物富集EVOO是一种很有前途的策略，可以提高其在羟基酪醇衍生物中的含量，为其生物活性成分提供优质的EVOO。
{"title":"Improving Hydroxytyrosol Derivatives Content in Virgin Olive Oil Using Ultrasound-assisted Maceration with Olive Leaf Extract","authors":"V. Goulas, A. Christou, Aristi Alkiviadi","doi":"10.2174/1573407219666230816091455","DOIUrl":"https://doi.org/10.2174/1573407219666230816091455","url":null,"abstract":"\u0000\u0000Olive oil is rich in monounsaturated fatty acids and is an essential Mediterranean diet component. Many of its health benefits are associated with the presence of phenolic compounds. Several strategies for the enhancement of the phenolic content and, more specifically, the concentration of hydroxytyrosol derivatives in olive oils have been proposed, as extra virgin olive oil (EVOO) of high phenolic content is preferred by health-conscious consumers.\u0000\u0000\u0000\u0000The supplementation of EVOO with hydroxytyrosol derivatives from olive leaf extract was performed with the employment of ultrasound-assisted maceration at different concentration levels (2 g·L-1 oil and 4 g L-1 oil), temperatures (20 and 40 oC), and maceration times (20 and 40 min). The phenolic contents of enriched EVOOs were determined by spectrophotometric and HPLC methods. In addition, the effect of supplementation on the physicochemical parameters of EVOOs, namely acidity and extinction coefficients (K232 and K270), was also studied.\u0000\u0000\u0000\u0000The addition of extract slightly increased the acidity values and extinction coefficients of the samples, and at the same time, it significantly improved their phenolic composition. The use of appropriate ultrasound-assisted maceration parameters (addition of olive leaf extract at a concentration level of 2 g L-1 at 20 oC for 20 min) provided EVOO with acceptable values for total acidity (<0.8%), K232 \u0000(<2.5), and K270 (<0.22), high contents of total phenolics and flavonoids, and improved hydroxytyrosol derivative contents.\u0000\u0000\u0000\u0000The enrichment of EVOO with leaf extract is a promising strategy to enhance its content in hydroxytyrosol derivatives, providing premium EVOOs with respect to their bioactive composition.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45783733","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-16DOI: 10.2174/1573407219666230816141715
M. Hajizadeh, Faezeh Esmaeili Ranjbar, A. Abasi, M. Abbasifard, M. Mahmoodi, Mojgan Noroozi-Karimabad
Breast cancer was known as the second most common cause of death in the world, natural sources compound derived from milk thistle called silymarin had already shown anticancer properties. In the present study, silymarin was used to treat MCF7 cells and inhibition of stem cell pluripotency genes, as well as cell proliferation. MCF7 cells were cultured in the presence of RPMI-1640 medium consisting of various silymarin extract concentrations (10, 100, 500, 1000, 2000, 3000, 4000, and 5000 µg/mL) for 24, 48, and 72 hours. The inhibitory effects of the compound on cellular proliferation were assessed via employing MTT assay techniques. Following confirming apoptosis, the fold changes of OCT4, NANOG and P53 expression were determined by quantitative Real-Time PCR. There was a significant difference (p value<0.05) in cell viability when various concentrations of silymarin extract were used for 24, 48, and 72 h in comparison to the control. Real-Time- PCR analysis indicated that the expression of OCT4 and NANOG was downregulated while P53 upregulated in compare to untreated control cells (p value <0.05). According to these findings, the silymarin effects on MCF7 cell line and act via modulating OCT4, NANOG, and P53 pathway mediators. Silymarin may introduce this compound as a promising therapeutic compound against MCF7.
{"title":"Regulatory Effects of the Silymarin on Expression of OCT4, NANOG, and P53 in MCF7 Cell Lines","authors":"M. Hajizadeh, Faezeh Esmaeili Ranjbar, A. Abasi, M. Abbasifard, M. Mahmoodi, Mojgan Noroozi-Karimabad","doi":"10.2174/1573407219666230816141715","DOIUrl":"https://doi.org/10.2174/1573407219666230816141715","url":null,"abstract":"\u0000\u0000Breast cancer was known as the second most common cause of death in the world, natural sources compound derived from milk thistle called silymarin had already shown anticancer properties.\u0000\u0000\u0000\u0000In the present study, silymarin was used to treat MCF7 cells and inhibition of stem cell pluripotency genes, as well as cell proliferation.\u0000\u0000\u0000\u0000MCF7 cells were cultured in the presence of RPMI-1640 medium consisting of various silymarin extract concentrations (10, 100, 500, 1000, 2000, 3000, 4000, and 5000 µg/mL) for 24, 48, and 72 hours. The inhibitory effects of the compound on cellular proliferation were assessed via employing MTT assay techniques. Following confirming apoptosis, the fold changes of OCT4, NANOG and P53 expression were determined by quantitative Real-Time PCR.\u0000\u0000\u0000\u0000There was a significant difference (p value<0.05) in cell viability when various concentrations of silymarin extract were used for 24, 48, and 72 h in comparison to the control. Real-Time- PCR analysis indicated that the expression of OCT4 and NANOG was downregulated while P53 upregulated in compare to untreated control cells (p value <0.05).\u0000\u0000\u0000\u0000According to these findings, the silymarin effects on MCF7 cell line and act via modulating OCT4, NANOG, and P53 pathway mediators. Silymarin may introduce this compound as a promising therapeutic compound against MCF7.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41422275","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-15DOI: 10.2174/1573407219666230815105041
P. Astaraki, Bareza Rezaei, M. Ahadi
Epigenetics deals with the changes in gene expression (no change in the genetic code) concerning certain epigenetic elements in response to the environment. Some of the most common epigenetic examples include DNA methylation, histone modifications, and non-coding RNAs. This field has been extensively applied in forensic studies, particularly to determine types of body fluids, distinguish them from mixed samples, uncovering the biological age of the forensic samples and drug-based studies. Considering recent findings, this review highlights the applications of epigenetics in forensic investigations.
{"title":"Epigenetics and Forensics: Brightening the Future","authors":"P. Astaraki, Bareza Rezaei, M. Ahadi","doi":"10.2174/1573407219666230815105041","DOIUrl":"https://doi.org/10.2174/1573407219666230815105041","url":null,"abstract":"\u0000\u0000Epigenetics deals with the changes in gene expression (no change in the genetic code) concerning certain epigenetic elements in response to the environment. Some of the most common epigenetic examples include DNA methylation, histone modifications, and non-coding RNAs. This field has been extensively applied in forensic studies, particularly to determine types of body fluids, distinguish them from mixed samples, uncovering the biological age of the forensic samples and drug-based studies. Considering recent findings, this review highlights the applications of epigenetics in forensic investigations.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46130612","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-15DOI: 10.2174/1573407219666230815105059
A. Mohamed, A. Omar, Basma Soliman, A. Dakrory, M. Al-Hammady
Arsenic is a potent environmental toxin with dangerous effects on human and animal populations. Heteroxenia fuscescens (H. fuscescens) extract exhibits potential health effects. The purpose of this study was to assess the protective effect of H. fuscescens extract against sodium arsenite-induced infertility and toxicity in rats Forty male rats were separated into four groups as follows: control group (2% DMSO, orally), sodium arsenite (10 mg/kg, orally), sodium arsenite + H. fuscescens extract (60 mg/kg in 2% DMSO), and H. fuscescens extract (60 mg/kg in 2% DMSO). GC/MS analysis of H. fuscescens indicates the presence of 10 compounds at retention times of 6.00, 12.53, 19.04, 24.60, 28.56, 35.66, 38.99, 45.29, 48.02, and 52.14. fuscescens extract improves levels of sperm count (53.33 ± 1.52), motility (43.00 ± 1.10), FSH ( 2.17 ± 0.04), LH (2.43 ± 0.06), testosterone (1.87 0.02), and testis weight (0.49 ± 0.01). The antioxidant activity of H. fuscescens extract was reported by a significant decrease in MDA (1.02 ± 0.01) and NO (520.39 ± 14.99) levels, while it significantly increased levels of GSH (1.77 ± 0.07), and CAT (71.38 ± 3.45). Histopathological alterations of the testes, liver, and kidney observed with sodium arsenite have been improved in the treatment group. Heteroxenia fuscescens is beneficial in restoring male sex hormone levels, maintaining a healthy sperm profile, and reducing oxidative stress, all of which lead to an improvement in male rat fertility.
{"title":"Protective Effect of Heteroxenia Fuscescens Extract Against Sodium Arsenite-Induced Infertility in Male Rats","authors":"A. Mohamed, A. Omar, Basma Soliman, A. Dakrory, M. Al-Hammady","doi":"10.2174/1573407219666230815105059","DOIUrl":"https://doi.org/10.2174/1573407219666230815105059","url":null,"abstract":"\u0000\u0000Arsenic is a potent environmental toxin with dangerous effects on human and animal populations. Heteroxenia fuscescens (H. fuscescens) extract exhibits potential health effects.\u0000\u0000\u0000\u0000The purpose of this study was to assess the protective effect of H. fuscescens extract against sodium arsenite-induced infertility and toxicity in rats\u0000\u0000\u0000\u0000Forty male rats were separated into four groups as follows: control group (2% DMSO, orally), sodium arsenite (10 mg/kg, orally), sodium arsenite + H. fuscescens extract (60 mg/kg in 2% DMSO), and H. fuscescens extract (60 mg/kg in 2% DMSO).\u0000\u0000\u0000\u0000GC/MS analysis of H. fuscescens indicates the presence of 10 compounds at retention times of 6.00, 12.53, 19.04, 24.60, 28.56, 35.66, 38.99, 45.29, 48.02, and 52.14. fuscescens extract improves levels of sperm count (53.33 ± 1.52), motility (43.00 ± 1.10), FSH ( 2.17 ± 0.04), LH (2.43 ± 0.06), testosterone (1.87 0.02), and testis weight (0.49 ± 0.01). The antioxidant activity of H. fuscescens extract was reported by a significant decrease in MDA (1.02 ± 0.01) and NO (520.39 ± 14.99) levels, while it significantly increased levels of GSH (1.77 ± 0.07), and CAT (71.38 ± 3.45). Histopathological alterations of the testes, liver, and kidney observed with sodium arsenite have been improved in the treatment group.\u0000\u0000\u0000\u0000Heteroxenia fuscescens is beneficial in restoring male sex hormone levels, maintaining a healthy sperm profile, and reducing oxidative stress, all of which lead to an improvement in male rat fertility.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41558680","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-08-15DOI: 10.2174/1573407219666230815121205
L. Vivekanandan, Prabha Thangavelu, Jagadeeswaran Murugesan, Hemalatha Selvaraj
Emesis is a complexand distressing protective mechanism that helps to remove toxic substances from the stomach and prevent further ingestion. The emetics and cathartics are predominantly used for accidental and intentional ingestion of poisons or toxins. The availability and usage of emetics in humans are limited because of their side effects. Therefore, to treat poisoned people, we need effective medications. Sapindus emarginatus Vahl., often called soapnut, is a member of the Sapindaceae family. They have historically been used as emetic, antipruritic, laxative, antifertility, and anti-inflammatory medicines. This study aims to assess the gut serotonin level and emetic effect of Sapindus emarginatus hydroethanolic pericarp extract (HESE) by using animal models. Gravimetric analysis was used to determine the HESE's saponin content. The emetic effect of the HESE at a dose of 250, 500, 1000, and 2000 mg/kg was evaluated by copper sulfate-induced emesis in the chick model and cisplatin-induced emesis in the rat-pica model. The serotonin level in rat intestinal mucosa was measured by spectrofluorimetry. HESE was estimated to contain 11.92% saponin. The extract at high doses of 1000 and 2000 mg/kg showed emetic activity evidenced by increased frequency of retching in chick, increased kaolin intake, and anorexia in the rat-pica model. The extract showed a significant increase in serotonin levels in the proximal part of the small intestine in comparison with normal animals. According to the results of the current investigation, which employed various animal models, the HESE demonstrated appreciable emetic activity. The extract at a high dose showed a significant emetic effect due to increased serotonin levels in the gut. The HESE was discovered to be a strong contender for the treatment of poisoned patients. More research are required to validate their adverse effects of frequent usage.
{"title":"Role of Sapindus emarginatus Pericarp Extract in Gut Serotonin Level and its Emetic Activity in Animal Models","authors":"L. Vivekanandan, Prabha Thangavelu, Jagadeeswaran Murugesan, Hemalatha Selvaraj","doi":"10.2174/1573407219666230815121205","DOIUrl":"https://doi.org/10.2174/1573407219666230815121205","url":null,"abstract":"\u0000\u0000Emesis is a complexand distressing protective mechanism that helps to remove toxic substances from the stomach and prevent further ingestion. The emetics and cathartics are predominantly used for accidental and intentional ingestion of poisons or toxins. The availability and usage of emetics in humans are limited because of their side effects. Therefore, to treat poisoned people, we need effective medications. Sapindus emarginatus Vahl., often called soapnut, is a member of the Sapindaceae family. They have historically been used as emetic, antipruritic, laxative, antifertility, and anti-inflammatory medicines.\u0000\u0000\u0000\u0000This study aims to assess the gut serotonin level and emetic effect of Sapindus emarginatus hydroethanolic pericarp extract (HESE) by using animal models.\u0000\u0000\u0000\u0000Gravimetric analysis was used to determine the HESE's saponin content. The emetic effect of the HESE at a dose of 250, 500, 1000, and 2000 mg/kg was evaluated by copper sulfate-induced emesis in the chick model and cisplatin-induced emesis in the rat-pica model. The serotonin level in rat intestinal mucosa was measured by spectrofluorimetry.\u0000\u0000\u0000\u0000HESE was estimated to contain 11.92% saponin. The extract at high doses of 1000 and 2000 mg/kg showed emetic activity evidenced by increased frequency of retching in chick, increased kaolin intake, and anorexia in the rat-pica model. The extract showed a significant increase in serotonin levels in the proximal part of the small intestine in comparison with normal animals.\u0000\u0000\u0000\u0000According to the results of the current investigation, which employed various animal models, the HESE demonstrated appreciable emetic activity. The extract at a high dose showed a significant emetic effect due to increased serotonin levels in the gut. The HESE was discovered to be a strong contender for the treatment of poisoned patients. More research are required to validate their adverse effects of frequent usage.\u0000","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43003641","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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