Pub Date : 2022-09-05DOI: 10.1080/2314808X.2022.2109298
Fatima A. M. El-Deeb, Y. Mahmoud, N. H. Hassan
ABSTRACT Hepatocellular carcinoma (HCC) is the fourth cause of cancer mortality worldwide. Metformin is an antidiabetic drug that showed a prophylactic effect in the early stages of some cancers. This study aimed to reevaluate the anticarcinogenic effect of metformin in a cancer model not associated with diabetes. Also, to evaluate the effect of pharmacological antidiabetic dose of metformin (used in cancer studies) at the early stages of HCC versus the sub-pharmacological dose. HCC was induced by a single i.p injection of diethylnitrosamine followed by 16 biweekly i.p injections of carbon-tetrachloride. Metformin was i.p injected (25 or 250 mg/kg) post HCC induction for four weeks. The low dose of metformin suppressed HCC by reducing liver biomarkers levels, and the number and size of hepatic nodules. Also, metformin (25 mg/kg) downstaged HCC via activating Bax and suppressing Bcl-2, VEGF, and PCNA. Mice treated with metformin (250 mg/kg) exhibited lactic acidosis, death, and insignificant differences in nodules’ number and size and immunohistochemical markers compared to the HCC group. This study concluded that the pharmacological dose of metformin cannot be used at advanced stages of HCC, while the sub-pharmacological dose of metformin showed a promising anticarcinogenic effect in chemically-induced HCC model not associated with diabetes. .
{"title":"Re-evaluation of the anticarcinogenic effect of metformin in a chemically-induced hepatocellular carcinoma model not associated with diabetes","authors":"Fatima A. M. El-Deeb, Y. Mahmoud, N. H. Hassan","doi":"10.1080/2314808X.2022.2109298","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2109298","url":null,"abstract":"ABSTRACT Hepatocellular carcinoma (HCC) is the fourth cause of cancer mortality worldwide. Metformin is an antidiabetic drug that showed a prophylactic effect in the early stages of some cancers. This study aimed to reevaluate the anticarcinogenic effect of metformin in a cancer model not associated with diabetes. Also, to evaluate the effect of pharmacological antidiabetic dose of metformin (used in cancer studies) at the early stages of HCC versus the sub-pharmacological dose. HCC was induced by a single i.p injection of diethylnitrosamine followed by 16 biweekly i.p injections of carbon-tetrachloride. Metformin was i.p injected (25 or 250 mg/kg) post HCC induction for four weeks. The low dose of metformin suppressed HCC by reducing liver biomarkers levels, and the number and size of hepatic nodules. Also, metformin (25 mg/kg) downstaged HCC via activating Bax and suppressing Bcl-2, VEGF, and PCNA. Mice treated with metformin (250 mg/kg) exhibited lactic acidosis, death, and insignificant differences in nodules’ number and size and immunohistochemical markers compared to the HCC group. This study concluded that the pharmacological dose of metformin cannot be used at advanced stages of HCC, while the sub-pharmacological dose of metformin showed a promising anticarcinogenic effect in chemically-induced HCC model not associated with diabetes. .","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"35 1","pages":"560 - 576"},"PeriodicalIF":0.0,"publicationDate":"2022-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84449915","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 : 2022-09-05DOI: 10.1080/2314808X.2022.2106693
Norhan H. Mohamed, Hassan Elsayad, Y. Elsherbini, M. Abdraboh
ABSTRACT Diabetes mellitus is characterized by structural abnormalities, oxidative stress and neuroinflammation. This study aimed to determine the antioxidative therapeutic effects of peanut supplementation in improving brain damage resulted from streptozotocin (STZ)-induced diabetes. Forty male Wistar albino rats (Rattus novergicus) were categorized into four groups: control, peanut-supplemented, diabetic, diabetic and peanut-supplemented. The brain was dissected and subjected to biochemical analyses which indicated the role of diabetes in downregulating the expression of superoxide dismutase (SOD), dopamine (DA), serotonin (5-HT), adenosine triphosphate (ATP) and upregulating the levels of malondialdehyde (MDA), tumor necrosis factor-α (TNF-α), 5-lipoxygenase (5-lOX), 8-hydroxy-deoxy guanosine (8-OHdG), Amyloid-β, α-amylase and tau protein expression levels. peanut treatment enhanced the diabetic-dependent brain histopathological features in the cerebrum and hippocampus, the immunohistochemical localization indicated significant downregulation at the expression of synaptophysin and caspase 3. Peanut supplementation significantly downregulated the gene expression of BAX, SOD, Myloperoxidase (MPO), Tumor necrosis factor- α (TNF-α), peroxisome proliferator-activated receptors (PPAR-α and PPAR-γ) and upregulated glial fibrillary acidic protein (GFAP) expression. In conclusion, peanut supplementation showed therapeutic potential against brain damage induced by diabetes. Peanut treatment significantly protected the brain from diabetic-related oxidative stress, and increased dopamine and serotonin levels by restoring the redox balance. Graphical Abstract
{"title":"Neuroprotective effect of peanut against oxidative stress in streptozotocin-induced diabetic rats","authors":"Norhan H. Mohamed, Hassan Elsayad, Y. Elsherbini, M. Abdraboh","doi":"10.1080/2314808X.2022.2106693","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2106693","url":null,"abstract":"ABSTRACT Diabetes mellitus is characterized by structural abnormalities, oxidative stress and neuroinflammation. This study aimed to determine the antioxidative therapeutic effects of peanut supplementation in improving brain damage resulted from streptozotocin (STZ)-induced diabetes. Forty male Wistar albino rats (Rattus novergicus) were categorized into four groups: control, peanut-supplemented, diabetic, diabetic and peanut-supplemented. The brain was dissected and subjected to biochemical analyses which indicated the role of diabetes in downregulating the expression of superoxide dismutase (SOD), dopamine (DA), serotonin (5-HT), adenosine triphosphate (ATP) and upregulating the levels of malondialdehyde (MDA), tumor necrosis factor-α (TNF-α), 5-lipoxygenase (5-lOX), 8-hydroxy-deoxy guanosine (8-OHdG), Amyloid-β, α-amylase and tau protein expression levels. peanut treatment enhanced the diabetic-dependent brain histopathological features in the cerebrum and hippocampus, the immunohistochemical localization indicated significant downregulation at the expression of synaptophysin and caspase 3. Peanut supplementation significantly downregulated the gene expression of BAX, SOD, Myloperoxidase (MPO), Tumor necrosis factor- α (TNF-α), peroxisome proliferator-activated receptors (PPAR-α and PPAR-γ) and upregulated glial fibrillary acidic protein (GFAP) expression. In conclusion, peanut supplementation showed therapeutic potential against brain damage induced by diabetes. Peanut treatment significantly protected the brain from diabetic-related oxidative stress, and increased dopamine and serotonin levels by restoring the redox balance. Graphical Abstract","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"27 1","pages":"542 - 559"},"PeriodicalIF":0.0,"publicationDate":"2022-09-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75734615","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 : 2022-08-23DOI: 10.1080/2314808X.2022.2098462
Abubakar Sadiq Wada, S. Julde, S. B. Borodo, M. Ahmad, S. Malami, A. Yaro
ABSTRACT Plants are natural sources of readily available phytochemicals which possesses interesting biological activities. The plant Diodia scandens is a creeping and straggling perennial herb commonly dispersed in tropical Africa, tropical Asia and some parts of Cameroon, Congo and Nigeria. It is used traditionally in the treatment of several disease conditions such as snake bites, rheumatic inflammatory disorders, earache, venereal diseases, hypertension and epilepsy. It is also used as an aphrodisiac and in the treatment of uterine inertia and postpartum hemorrhage. Despite its vast traditional uses, a comprehensive information on the plant is still lacking. In this review, we aimed to provide concise information on reported ethnomedicinal uses, phytochemistry, and pharmacological activities of Diodia scandens to support its traditional usage in exploring its therapeutic potentials. Available information about the plant was retrieved from online databases including PubMed and Google Scholar using the search terms ‘Diodia scandens’, ‘ethnomedicinal uses and Diodia scandens’, ‘phytochemistry and Diodia scandens’ and ‘pharmacological activity and Diodia scandens’. The available literatures supported several ethnobotanical claims on the use of D. scandens in traditional medicine. Other claims not yet scientifically verified should be explored to ascertain the veracity of such claims on its therapeutic potentials.
{"title":"Phytochemistry, ethnomedicinal uses and pharmacological activity of Diodia scandens; a review of current scientific literature","authors":"Abubakar Sadiq Wada, S. Julde, S. B. Borodo, M. Ahmad, S. Malami, A. Yaro","doi":"10.1080/2314808X.2022.2098462","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2098462","url":null,"abstract":"ABSTRACT Plants are natural sources of readily available phytochemicals which possesses interesting biological activities. The plant Diodia scandens is a creeping and straggling perennial herb commonly dispersed in tropical Africa, tropical Asia and some parts of Cameroon, Congo and Nigeria. It is used traditionally in the treatment of several disease conditions such as snake bites, rheumatic inflammatory disorders, earache, venereal diseases, hypertension and epilepsy. It is also used as an aphrodisiac and in the treatment of uterine inertia and postpartum hemorrhage. Despite its vast traditional uses, a comprehensive information on the plant is still lacking. In this review, we aimed to provide concise information on reported ethnomedicinal uses, phytochemistry, and pharmacological activities of Diodia scandens to support its traditional usage in exploring its therapeutic potentials. Available information about the plant was retrieved from online databases including PubMed and Google Scholar using the search terms ‘Diodia scandens’, ‘ethnomedicinal uses and Diodia scandens’, ‘phytochemistry and Diodia scandens’ and ‘pharmacological activity and Diodia scandens’. The available literatures supported several ethnobotanical claims on the use of D. scandens in traditional medicine. Other claims not yet scientifically verified should be explored to ascertain the veracity of such claims on its therapeutic potentials.","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"23 1","pages":"533 - 541"},"PeriodicalIF":0.0,"publicationDate":"2022-08-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87370848","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 : 2022-08-11DOI: 10.1080/2314808X.2022.2106097
T. Yahaya, E. Oladele, T. Salisu, E. Orji, Z. Zakari, U. U. Liman, Clement Boniface Gomo, M. Abdullahi
ABSTRACT The block-molding industry provides housing and employment globally. However, cement contains toxic metals, so molders need periodic safety monitoring. This study assessed the safety of 25 block molders and 25 control subjects in Lagos, Nigeria. After obtaining informed consent, structured questionnaires were used to obtain participants’ weight, height, age, and skin texture. Moreover, the participants’ blood samples were analyzed for heavy metals (calcium, silicon, aluminum, iron, chromium, copper, and lead) and hematological parameters (hemoglobin, packed cell volume), red blood, and white blood cells). Also evaluated were biomarkers of oxidative stress damage, namely albumin, glutamate dehydrogenase, kidney injury molecule-1, DNA-8-hydroxyguanosine, carcinoembryonic antigen, malondialdehyde, and total antioxidant capacity . The molders’ skin was dry compared to the control. The molders’ blood plasma metals were higher (p ≤ 0.05) than the control, with the exception of lead, and were over the allowed ranges. Similarly, the molders’ packed cell volume, hemoglobin, and red blood cell levels were lower than usual, while their red blood cell levels were higher. The molders’ biomarkers were outside of the acceptable ranges and were significantly different from the control. The findings show that block molders are at risk of health hazards and should take steps to reduce their cement exposure.
{"title":"Toxic metals in cement induced hematological and DNA damage as well as carcinogenesis in occupationally-Exposed block-factory workers in Lagos, Nigeria","authors":"T. Yahaya, E. Oladele, T. Salisu, E. Orji, Z. Zakari, U. U. Liman, Clement Boniface Gomo, M. Abdullahi","doi":"10.1080/2314808X.2022.2106097","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2106097","url":null,"abstract":"ABSTRACT The block-molding industry provides housing and employment globally. However, cement contains toxic metals, so molders need periodic safety monitoring. This study assessed the safety of 25 block molders and 25 control subjects in Lagos, Nigeria. After obtaining informed consent, structured questionnaires were used to obtain participants’ weight, height, age, and skin texture. Moreover, the participants’ blood samples were analyzed for heavy metals (calcium, silicon, aluminum, iron, chromium, copper, and lead) and hematological parameters (hemoglobin, packed cell volume), red blood, and white blood cells). Also evaluated were biomarkers of oxidative stress damage, namely albumin, glutamate dehydrogenase, kidney injury molecule-1, DNA-8-hydroxyguanosine, carcinoembryonic antigen, malondialdehyde, and total antioxidant capacity . The molders’ skin was dry compared to the control. The molders’ blood plasma metals were higher (p ≤ 0.05) than the control, with the exception of lead, and were over the allowed ranges. Similarly, the molders’ packed cell volume, hemoglobin, and red blood cell levels were lower than usual, while their red blood cell levels were higher. The molders’ biomarkers were outside of the acceptable ranges and were significantly different from the control. The findings show that block molders are at risk of health hazards and should take steps to reduce their cement exposure.","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"10 1","pages":"499 - 509"},"PeriodicalIF":0.0,"publicationDate":"2022-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86461116","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 : 2022-08-11DOI: 10.1080/2314808X.2022.2106093
A. Elhalawany, Hosnia A. Afifi, E. Ayad
ABSTRACT This study deals with biology and life table parameters of the predatory mite, Cheyletus malaccensis Oudemans were evaluated on three astigmatid mites as prey (i.e. Acarus siro (Linnaeus), Caloglyphus berlesei (Michael) and Tyrophagus putrescentiae (Schrank)) under laboratory conditions. Three constant temperatures (22, 27 and 32 ± 2°C) and constant relative humidity 80 ± 5% were used. Statistical analysis indicated significant difference between prey types and the three different temperatures. The shortest life cycle was recorded on A. siro (11.60 and 8.0 days) at 32°C, while the longest was on C. berlesei (29.5 and 21.2) at 22°C for females and males, respectively. Longest female longevity was on A. siro (43.6 days) at 22°C and shortest was 20.65 days on T. putrescentiae at 32°C. Highest fecundity was found on A. siro (196.50 eggs/female) at 27°C and lowest one was 69.10 eggs/female on C. berlesei at 22°C. The highest net reproduction rate of increase (R0) was 113.2 ♀/♀/generation at 27°C on A. siro. Obtained results suggested that C. malaccensis could develop and reproduce within a wide range of temperatures and prey types. It can also be used as a biological control agent to reduce the amount of acarid mite pests that infest stored commodities.
{"title":"Impact of temperature and prey type on biology and life-table parameters of Cheyletus malaccensis Oudemans (Acari: Cheyletidae)","authors":"A. Elhalawany, Hosnia A. Afifi, E. Ayad","doi":"10.1080/2314808X.2022.2106093","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2106093","url":null,"abstract":"ABSTRACT This study deals with biology and life table parameters of the predatory mite, Cheyletus malaccensis Oudemans were evaluated on three astigmatid mites as prey (i.e. Acarus siro (Linnaeus), Caloglyphus berlesei (Michael) and Tyrophagus putrescentiae (Schrank)) under laboratory conditions. Three constant temperatures (22, 27 and 32 ± 2°C) and constant relative humidity 80 ± 5% were used. Statistical analysis indicated significant difference between prey types and the three different temperatures. The shortest life cycle was recorded on A. siro (11.60 and 8.0 days) at 32°C, while the longest was on C. berlesei (29.5 and 21.2) at 22°C for females and males, respectively. Longest female longevity was on A. siro (43.6 days) at 22°C and shortest was 20.65 days on T. putrescentiae at 32°C. Highest fecundity was found on A. siro (196.50 eggs/female) at 27°C and lowest one was 69.10 eggs/female on C. berlesei at 22°C. The highest net reproduction rate of increase (R0) was 113.2 ♀/♀/generation at 27°C on A. siro. Obtained results suggested that C. malaccensis could develop and reproduce within a wide range of temperatures and prey types. It can also be used as a biological control agent to reduce the amount of acarid mite pests that infest stored commodities.","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"15 1","pages":"452 - 461"},"PeriodicalIF":0.0,"publicationDate":"2022-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81966473","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 : 2022-08-11DOI: 10.1080/2314808X.2022.2098461
K. Banwo, Samuel Oduola, M. Alao, A. Sanni
ABSTRACT Roselle and Beetroots are essential plants used individually for hepatoprotective abilities. This study investigated the preventive potentials of the combinations of Roselle and beetroots against carbon tetrachloride (CCl4)-induced and Escherichia coli (E. coli)-induced hepatic stress. Total phenolic content (TPC), total flavonoids (TF), 1,1-diphenyl-picrylhydrazin (DPPH) and ferric-reducing antioxidant power (FRAP) were evaluated. Oxidative stress was induced in rats with CCl4 and E. coli. Glutathione (GSH), superoxide dismutase (SOD), malondialdehyde (MDA), catalase (CAT) and histopathology were evaluated in the liver. Roselle had the highest TPC and TF of 274.4 and 1140.9 GAE mg/mL, respectively. Roselle and beetroots inhibited DPPH and FRAP by (95.7% and 73.8%) and (887.6 and 662.6 µmol/L), respectively. In the extract-treated animal groups, a significant increase (P < 0.05) in the GSH, SOD and CAT was observed with a decrease in the MDA and histology indicates preserved hepatocellular architecture. The investigated plant extracts combination therefore exhibited antioxidant activities and hepatic cell protection. The results confirmed the combined functionalities of these plants as protective against oxidative stress induced in the liver, which can be incorporated as a dietary strategy to combat hepatic stress after due clinical trials. . Graphical abstract
{"title":"Hepatoprotective potentials of methanolic extracts of Roselle and beetroots against carbon tetrachloride and Escherichia coli induced stress in Wistar rats","authors":"K. Banwo, Samuel Oduola, M. Alao, A. Sanni","doi":"10.1080/2314808X.2022.2098461","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2098461","url":null,"abstract":"ABSTRACT Roselle and Beetroots are essential plants used individually for hepatoprotective abilities. This study investigated the preventive potentials of the combinations of Roselle and beetroots against carbon tetrachloride (CCl4)-induced and Escherichia coli (E. coli)-induced hepatic stress. Total phenolic content (TPC), total flavonoids (TF), 1,1-diphenyl-picrylhydrazin (DPPH) and ferric-reducing antioxidant power (FRAP) were evaluated. Oxidative stress was induced in rats with CCl4 and E. coli. Glutathione (GSH), superoxide dismutase (SOD), malondialdehyde (MDA), catalase (CAT) and histopathology were evaluated in the liver. Roselle had the highest TPC and TF of 274.4 and 1140.9 GAE mg/mL, respectively. Roselle and beetroots inhibited DPPH and FRAP by (95.7% and 73.8%) and (887.6 and 662.6 µmol/L), respectively. In the extract-treated animal groups, a significant increase (P < 0.05) in the GSH, SOD and CAT was observed with a decrease in the MDA and histology indicates preserved hepatocellular architecture. The investigated plant extracts combination therefore exhibited antioxidant activities and hepatic cell protection. The results confirmed the combined functionalities of these plants as protective against oxidative stress induced in the liver, which can be incorporated as a dietary strategy to combat hepatic stress after due clinical trials. . Graphical abstract","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"80 1","pages":"423 - 440"},"PeriodicalIF":0.0,"publicationDate":"2022-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84938915","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 : 2022-08-11DOI: 10.1080/2314808X.2022.2108592
Mustapha Abdullahi, A. Uzairu, G. Shallangwa, P. Mamza, M. T. Ibrahim
ABSTRACT Due to the emergence of drug-resistant strains of influenza A virus (IAV) in recent times, the need to search and discover more potent anti-IAV inhibitors is of great interest, especially with the devastating COVID-19 pandemic. The present research applied 2D-QSAR, 3D-QSAR, molecular docking, and ADMET predictions on some novel analogs of 2-((1 H-indol-3-yl)thio)-N-phenyl-acetamide as IAV inhibitors. The 2D-QSAR modeling results revealed GFA-MLR ( =0.8861, q2 = 0.7864) and GFA-ANN ( =0.8980, q2 = 0.8884) models with the most relevant descriptors for predicting the anti-IAV responses of the compounds, which have passed the benchmarks for accepting QSAR models. The 3D-QSAR modeling results suggested CoMFA_SE ( =0.925, q2 = 0.59) and CoMSIA_EAD ( =0.929, q2 = 0.767) models for good and reliable activity predictions. The molecular docking of the compounds with the active site of neuraminidase (NA) receptor theoretically confirms their resilient potency. The compounds mostly formed H-bond and hydrophobic interactions with key residues, such as ARG118, ASP151, GLU119, TRP179, ARG293 and PRO431 that triggered the catalytic reaction for the NA inhibition. However, compounds 16 and 21 were identified as lead compounds in the in-silico search for more potent candidates. The outcome of this study set a course for the in-silico design and search of potential candidates for influenza therapy.
{"title":"2D-QSAR, 3D-QSAR, molecular docking and ADMET prediction studies of some novel 2-((1H-indol-3-yl)thio)-N-phenyl-acetamide derivatives as anti-influenza A virus","authors":"Mustapha Abdullahi, A. Uzairu, G. Shallangwa, P. Mamza, M. T. Ibrahim","doi":"10.1080/2314808X.2022.2108592","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2108592","url":null,"abstract":"ABSTRACT Due to the emergence of drug-resistant strains of influenza A virus (IAV) in recent times, the need to search and discover more potent anti-IAV inhibitors is of great interest, especially with the devastating COVID-19 pandemic. The present research applied 2D-QSAR, 3D-QSAR, molecular docking, and ADMET predictions on some novel analogs of 2-((1 H-indol-3-yl)thio)-N-phenyl-acetamide as IAV inhibitors. The 2D-QSAR modeling results revealed GFA-MLR ( =0.8861, q2 = 0.7864) and GFA-ANN ( =0.8980, q2 = 0.8884) models with the most relevant descriptors for predicting the anti-IAV responses of the compounds, which have passed the benchmarks for accepting QSAR models. The 3D-QSAR modeling results suggested CoMFA_SE ( =0.925, q2 = 0.59) and CoMSIA_EAD ( =0.929, q2 = 0.767) models for good and reliable activity predictions. The molecular docking of the compounds with the active site of neuraminidase (NA) receptor theoretically confirms their resilient potency. The compounds mostly formed H-bond and hydrophobic interactions with key residues, such as ARG118, ASP151, GLU119, TRP179, ARG293 and PRO431 that triggered the catalytic reaction for the NA inhibition. However, compounds 16 and 21 were identified as lead compounds in the in-silico search for more potent candidates. The outcome of this study set a course for the in-silico design and search of potential candidates for influenza therapy.","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"s3-45 1","pages":"510 - 532"},"PeriodicalIF":0.0,"publicationDate":"2022-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90836764","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 : 2022-08-11DOI: 10.1080/2314808X.2022.2106096
G. Nayak, S. Bhuyan, Ruchi Bhuyan, Akankshya Sahu, D. Kar, A. Kuanar
ABSTRACT Hard tissue reconstruction of bone has attracted the interest of clinical researchers to overcome the anomalous effect on general well-being. Bone is a supporting skeleton structure that also plays a pivotal role in the normal physiological functioning body. The introduction of bone tissue engineering has been instrumental in overcoming fragmental defined bone to diseases, accidents, or debilitating conditions. For this, various bone grafting materials are used to restore the patency. These various bone grafting options have shown promising results. But the search for ideal grating material continues. However, the available grafting resources may not ensure regeneration. And the grafts like autogenous grafts that provide the capacity, are often, acquired in limited quantity. Its incapacity to fill the defect has led to the requirement of alternative material. Marine sources have shown acceptable clinical outcomes and are rendered safe for use also have a rich calcium phosphate-containing scaffold, over which the new cells are formed owing to its porous and 3D grains. The wide range of available marine sources has been put into clinical trials. The collagen found in the Marine sources has shown comparatively better results than that of the available synthetic alternatives. Graphical abstract
{"title":"Marine sources as an unexplored bone tissue reconstruction material -A review","authors":"G. Nayak, S. Bhuyan, Ruchi Bhuyan, Akankshya Sahu, D. Kar, A. Kuanar","doi":"10.1080/2314808X.2022.2106096","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2106096","url":null,"abstract":"ABSTRACT Hard tissue reconstruction of bone has attracted the interest of clinical researchers to overcome the anomalous effect on general well-being. Bone is a supporting skeleton structure that also plays a pivotal role in the normal physiological functioning body. The introduction of bone tissue engineering has been instrumental in overcoming fragmental defined bone to diseases, accidents, or debilitating conditions. For this, various bone grafting materials are used to restore the patency. These various bone grafting options have shown promising results. But the search for ideal grating material continues. However, the available grafting resources may not ensure regeneration. And the grafts like autogenous grafts that provide the capacity, are often, acquired in limited quantity. Its incapacity to fill the defect has led to the requirement of alternative material. Marine sources have shown acceptable clinical outcomes and are rendered safe for use also have a rich calcium phosphate-containing scaffold, over which the new cells are formed owing to its porous and 3D grains. The wide range of available marine sources has been put into clinical trials. The collagen found in the Marine sources has shown comparatively better results than that of the available synthetic alternatives. Graphical abstract","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"8 1","pages":"477 - 498"},"PeriodicalIF":0.0,"publicationDate":"2022-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87467935","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 : 2022-08-11DOI: 10.1080/2314808X.2022.2099116
Komal Saraswat, Raushan Kumar, S. Rizvi
ABSTRACT Glucosamine, an amino-polysaccharide, has been widely used for alleviating osteoarthritis. . In the present study, attempts have been made to evaluate the potential role of glucosamine, a caloric restriction mimetic (CRM), for erythrocyte membrane transporter protection in D-galactose (D-gal) induced accelerated and natural aging models of rat specifically Ca2+-ATPases (PMCA pump), Na+/K+-ATPases (NKA pump), and the Na+/H+ exchanger (NHE) and redox biomarkers during aging. The study comprised of young (3–4 months old; 150 ± 20 g), naturally aged (above 24 months; 420 ± 20 g) and D-galactose-induced aged (3–4 months old; 150 ± 20 g, administered with D-Gal at 300 mg/kg B.W., subcutaneously) male albino rats of Wistar strain. All the rats were supplemented with Glucosamine hydrochloride (300 mg/kg body weight) for 12 weeks. There was a significant (P < 0.05) decrease in the activity of Ca2+-ATPases, Na+/K+-ATPases and induced NHE activity in D-Gal and naturally old rats. Levels of redox biomarkers such as intracellular Ca2+ ion, protein carbonyl, and lipid hydroperoxides were also found to be increased significantly (P < 0.05). These results were found to be reversed in the rats supplemented with glucosamine. Our findings suggest that glucosamine supplementation improves ion homeostasis by protecting the erythrocyte membrane transporters against age-related alterations.
{"title":"Glucosamine modulates membrane and cellular ionic homeostasis: studies on accelerated senescent and naturally aged rats","authors":"Komal Saraswat, Raushan Kumar, S. Rizvi","doi":"10.1080/2314808X.2022.2099116","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2099116","url":null,"abstract":"ABSTRACT Glucosamine, an amino-polysaccharide, has been widely used for alleviating osteoarthritis. . In the present study, attempts have been made to evaluate the potential role of glucosamine, a caloric restriction mimetic (CRM), for erythrocyte membrane transporter protection in D-galactose (D-gal) induced accelerated and natural aging models of rat specifically Ca2+-ATPases (PMCA pump), Na+/K+-ATPases (NKA pump), and the Na+/H+ exchanger (NHE) and redox biomarkers during aging. The study comprised of young (3–4 months old; 150 ± 20 g), naturally aged (above 24 months; 420 ± 20 g) and D-galactose-induced aged (3–4 months old; 150 ± 20 g, administered with D-Gal at 300 mg/kg B.W., subcutaneously) male albino rats of Wistar strain. All the rats were supplemented with Glucosamine hydrochloride (300 mg/kg body weight) for 12 weeks. There was a significant (P < 0.05) decrease in the activity of Ca2+-ATPases, Na+/K+-ATPases and induced NHE activity in D-Gal and naturally old rats. Levels of redox biomarkers such as intracellular Ca2+ ion, protein carbonyl, and lipid hydroperoxides were also found to be increased significantly (P < 0.05). These results were found to be reversed in the rats supplemented with glucosamine. Our findings suggest that glucosamine supplementation improves ion homeostasis by protecting the erythrocyte membrane transporters against age-related alterations.","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"166 1","pages":"441 - 451"},"PeriodicalIF":0.0,"publicationDate":"2022-08-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85981940","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 : 2022-08-07DOI: 10.1080/2314808X.2022.2104071
A. Ugya, Lin Pohan, Qifeng Wang, K. Meguellati
ABSTRACT From the top-down view, an organism is constituted by an assembly of cells where a network of molecules interacts to create a regulated complex system. Cells are a universe of molecular interactions maintained under non-equilibrium regimes. The complex network of interactions drives life where DNA and epigenetic signals are considered as the memory of a cell. The full understanding of these interactions is the first step toward the design of artificial synthetic pathways controlling a program. In our review, we present some insights into the different methods and designs applicable for the development of synthetic artificial cells. A self-replicative process of these cells, thermodynamic and kinetic features, as well as equilibrium systems of artificial cells, will enable scientists to have an in-depth knowledge of this domain. Furthermore, the cascade of encoded molecular chemical interactions orchestrated by the genetic program DNA, biomolecules, epigenetic signals, and nano-factory modulation will be discussed in terms of their application in the entire set of interactomes within a cell.
{"title":"Design of artificial cells: artificial biochemical systems, their thermodynamics and kinetics properties","authors":"A. Ugya, Lin Pohan, Qifeng Wang, K. Meguellati","doi":"10.1080/2314808X.2022.2104071","DOIUrl":"https://doi.org/10.1080/2314808X.2022.2104071","url":null,"abstract":"ABSTRACT From the top-down view, an organism is constituted by an assembly of cells where a network of molecules interacts to create a regulated complex system. Cells are a universe of molecular interactions maintained under non-equilibrium regimes. The complex network of interactions drives life where DNA and epigenetic signals are considered as the memory of a cell. The full understanding of these interactions is the first step toward the design of artificial synthetic pathways controlling a program. In our review, we present some insights into the different methods and designs applicable for the development of synthetic artificial cells. A self-replicative process of these cells, thermodynamic and kinetic features, as well as equilibrium systems of artificial cells, will enable scientists to have an in-depth knowledge of this domain. Furthermore, the cascade of encoded molecular chemical interactions orchestrated by the genetic program DNA, biomolecules, epigenetic signals, and nano-factory modulation will be discussed in terms of their application in the entire set of interactomes within a cell.","PeriodicalId":11512,"journal":{"name":"Egyptian Journal of Basic and Applied Sciences","volume":"116 1","pages":"393 - 412"},"PeriodicalIF":0.0,"publicationDate":"2022-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91356754","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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