Pub Date : 2019-06-13DOI: 10.11648/J.JDDMC.20190501.11
I. Chetoui, S. Bejaoui, C. Fouzai, Wafa Trabelsi, S. Nechi, E. Chelbi, Mohamed Ghalghaf, M. Cafsi, N. Soudani
Lead is non-essential toxic metal used in the industrial process causes severe risk to aquatic organisms. This study aimed (aims) to evaluate the effect of Pb on oxidative stress in gills of Mactra corallina. During the experiment, bivalves were randomly divided into four groups, control served as control and D1, D2 and D3 groups were exposed to Pb graded doses (1mg/L, 2.5mg/L and 5mg/L) during 5 days, respectively. Pb accumulation was significantly increased in all treated gills with doses dependent manner. The exposure of M. corallina to PbCl2 promoted oxidative stress in gills with an increase in malondialdehyde (MDA) and in metallothionein (MTs) levels. Moreover, a decline in glutathione (GSH), non-protein–SH (NPSH) and ascorbic acid (Vit C) levels were detected in all treated groups. Thus, alterations of enzymatic antioxidants systems were confirmed by a significant increase of catalase (CAT) and decreases of glutathione peroxidase (GPx) and superoxide dismutase (SOD) activities in doses dependent manner. The cholinergic function was confirmed by a significant decrease of acetylcholinesterase (AChE) activity in the highest exposure dose. The impairment of the gill function was confirmed by the histological study.
{"title":"Effect of Lead Graded Doses in Mactra Corallina Gills: Antioxidants Status, Cholinergic Function and Histopathological Studies","authors":"I. Chetoui, S. Bejaoui, C. Fouzai, Wafa Trabelsi, S. Nechi, E. Chelbi, Mohamed Ghalghaf, M. Cafsi, N. Soudani","doi":"10.11648/J.JDDMC.20190501.11","DOIUrl":"https://doi.org/10.11648/J.JDDMC.20190501.11","url":null,"abstract":"Lead is non-essential toxic metal used in the industrial process causes severe risk to aquatic organisms. This study aimed (aims) to evaluate the effect of Pb on oxidative stress in gills of Mactra corallina. During the experiment, bivalves were randomly divided into four groups, control served as control and D1, D2 and D3 groups were exposed to Pb graded doses (1mg/L, 2.5mg/L and 5mg/L) during 5 days, respectively. Pb accumulation was significantly increased in all treated gills with doses dependent manner. The exposure of M. corallina to PbCl2 promoted oxidative stress in gills with an increase in malondialdehyde (MDA) and in metallothionein (MTs) levels. Moreover, a decline in glutathione (GSH), non-protein–SH (NPSH) and ascorbic acid (Vit C) levels were detected in all treated groups. Thus, alterations of enzymatic antioxidants systems were confirmed by a significant increase of catalase (CAT) and decreases of glutathione peroxidase (GPx) and superoxide dismutase (SOD) activities in doses dependent manner. The cholinergic function was confirmed by a significant decrease of acetylcholinesterase (AChE) activity in the highest exposure dose. The impairment of the gill function was confirmed by the histological study.","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89570014","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}
{"title":"Lipophilic Ligand Efficiency as a Useful Metric in Hit and Lead Optimization","authors":"Irannejad H","doi":"10.16966/2578-9589.112","DOIUrl":"https://doi.org/10.16966/2578-9589.112","url":null,"abstract":"","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"18 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73868689","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}
{"title":"Molecular Docking, Drug-likeness Studies and ADMET Prediction of Quinoline Imines for Antimalarial Activity","authors":"K. J, C. D., R. M.","doi":"10.16966/2578-9589.113","DOIUrl":"https://doi.org/10.16966/2578-9589.113","url":null,"abstract":"","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"25 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76333991","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}
{"title":"Development of an Advanced Delivery System of CSKSSDYQC Peptide Modified N-Trimethyl Chitosan Nanoparticles for Oral Delivery of Gemcitabine","authors":"C. G, H. Y, W. J","doi":"10.16966/2578-9589.109","DOIUrl":"https://doi.org/10.16966/2578-9589.109","url":null,"abstract":"","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76160880","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 : 2019-01-01DOI: 10.11648/j.jddmc.20190501.12
Tembe Fokunang Estella
{"title":"Investigation of Toxicity and Systemic Exposure of Bioactive Compounds of Aqueous Leaf Extract of Azadirachta indica A. Juss (Meliaceae) on Wistar Rats","authors":"Tembe Fokunang Estella","doi":"10.11648/j.jddmc.20190501.12","DOIUrl":"https://doi.org/10.11648/j.jddmc.20190501.12","url":null,"abstract":"","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"19 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73706247","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 : 2019-01-01DOI: 10.11648/J.JDDMC.20190504.12
E. Owhoeke, M. Jnr., Charles Ikenna Osu
The levels of Polycyclic Aromatic Hydrocarbons (PAHs) in contaminated farmland soil from three oil-producing communities (Oboburu, Obagi, and Ogbogu) in Egi, Niger Delta were assessed for variability, origin and health risks. The result showed that tPAHs of Oboburu were 1344±1685 mg/kg for carcinogenic while BaP (257.3±270.5 mg/kg) had the greatest value. Obagi had 4154±3461 mg/kg for cPAHs with BkF (861.5±543.7 mg/kg) having the greatest amount. Ogbogu was 354.7±360.7 mg/kg for total cPAHs while BgP (104.1±141.8 mg/kg) had highest amount. The dominant PAHs were BbF, BkF, DbA, BaP, IdP and BgP. The principal component analysis (PCA) indicated that the PAHs were majorly of pyrogenic and petrogenic origin. The predicted risk due to PAHs in soil for children showed tPAHs was 1.68E-2, with high risk for BaP (9.05E-3), IdP (5.05E-3), BbF (1.63E-3) and BkF (1.04E-3), while the adults estimation showed tPAHs was 1.13E-2 and high risk were for BaP (2.30E-3), IdP (1.08E-3) and BkF (2.57E-4). These values are more than the limit of the US EPA risk management criterion (10-6 to 10-4) where management decisions should be considered. The trend indicated that their presence in the environment makes it unsafe for the dwellers.
{"title":"Source Tracking and Carcinogenic Risk of Polycyclic Aromatic Hydrocarbons in Contaminated Farmlands from Egi, Niger Delta, Nigeria","authors":"E. Owhoeke, M. Jnr., Charles Ikenna Osu","doi":"10.11648/J.JDDMC.20190504.12","DOIUrl":"https://doi.org/10.11648/J.JDDMC.20190504.12","url":null,"abstract":"The levels of Polycyclic Aromatic Hydrocarbons (PAHs) in contaminated farmland soil from three oil-producing communities (Oboburu, Obagi, and Ogbogu) in Egi, Niger Delta were assessed for variability, origin and health risks. The result showed that tPAHs of Oboburu were 1344±1685 mg/kg for carcinogenic while BaP (257.3±270.5 mg/kg) had the greatest value. Obagi had 4154±3461 mg/kg for cPAHs with BkF (861.5±543.7 mg/kg) having the greatest amount. Ogbogu was 354.7±360.7 mg/kg for total cPAHs while BgP (104.1±141.8 mg/kg) had highest amount. The dominant PAHs were BbF, BkF, DbA, BaP, IdP and BgP. The principal component analysis (PCA) indicated that the PAHs were majorly of pyrogenic and petrogenic origin. The predicted risk due to PAHs in soil for children showed tPAHs was 1.68E-2, with high risk for BaP (9.05E-3), IdP (5.05E-3), BbF (1.63E-3) and BkF (1.04E-3), while the adults estimation showed tPAHs was 1.13E-2 and high risk were for BaP (2.30E-3), IdP (1.08E-3) and BkF (2.57E-4). These values are more than the limit of the US EPA risk management criterion (10-6 to 10-4) where management decisions should be considered. The trend indicated that their presence in the environment makes it unsafe for the dwellers.","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"98 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85765298","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}
Colin T Mant, Ziqing Jiang, Lajos Gera, Tim Davis, Robert S Hodges
We designed de novo and synthesized two series of five 26-residue amphipathic α-helical cationic antimicrobial peptides (AMPs) with five or six positively charged residues (D-Lys, L-Dab (2,4-diaminobutyric acid) or L-Dap (2,3-diaminopropionic acid)) on the polar face where all other residues are in the D-conformation. Hemolytic activity against human red blood cells was determined using the most stringent conditions for the hemolysis assay, 18h at 37°C, 1% human erythrocytes and peptide concentrations up to 1000 μg/mL (~380 μM). Antimicrobial activity was determined against 7 Acinetobacter baumannii strains, resistant to polymyxin B and colistin (antibiotics of last resort) to show the effect of positively charged residues in two different locations on the polar face (positions 3, 7, 11, 18, 22 and 26 versus positions 3, 7, 14, 15, 22 and 26). All 10 peptides had two D-Lys residues in the center of the non-polar face as "specificity determinants" at positions 13 and 16 which provide specificity for prokaryotic cells over eukaryotic cells. Specificity determinants also maintain excellent antimicrobial activity in the presence of human sera. This study shows that the location and type of positively charged residue (Dab and Dap) on the polar face are critical to obtain the best therapeutic indices.
{"title":"Design of Novel Amphipathic α-Helical Antimicrobial Peptides with No Toxicity as Therapeutics against the Antibiotic-Resistant Gram-Negative Bacterial Pathogen, <i>Acinetobacter Baumannii</i>.","authors":"Colin T Mant, Ziqing Jiang, Lajos Gera, Tim Davis, Robert S Hodges","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>We designed <i>de novo</i> and synthesized two series of five 26-residue amphipathic α-helical cationic antimicrobial peptides (AMPs) with five or six positively charged residues (D-Lys, L-Dab (2,4-diaminobutyric acid) or L-Dap (2,3-diaminopropionic acid)) on the polar face where all other residues are in the D-conformation. Hemolytic activity against human red blood cells was determined using the most stringent conditions for the hemolysis assay, 18h at 37°C, 1% human erythrocytes and peptide concentrations up to 1000 μg/mL (~380 μM). Antimicrobial activity was determined against 7 <i>Acinetobacter baumannii</i> strains, resistant to polymyxin B and colistin (antibiotics of last resort) to show the effect of positively charged residues in two different locations on the polar face (positions 3, 7, 11, 18, 22 and 26 <i>versus</i> positions 3, 7, 14, 15, 22 and 26). All 10 peptides had two D-Lys residues in the center of the non-polar face as \"specificity determinants\" at positions 13 and 16 which provide specificity for prokaryotic cells over eukaryotic cells. Specificity determinants also maintain excellent antimicrobial activity in the presence of human sera. This study shows that the location and type of positively charged residue (Dab and Dap) on the polar face are critical to obtain the best therapeutic indices.</p>","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"2 2","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8351594/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"39300229","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2017-01-01DOI: 10.11648/j.jddmc.20170303.11
Johnson Olaleye Oladele
{"title":"Hepatoprotective Effect of Aqueous Extract of <i>Telfairia occidentalis</i> on Cadmium Chloride-Induced Oxidative Stress and Hepatotoxicity in Rats","authors":"Johnson Olaleye Oladele","doi":"10.11648/j.jddmc.20170303.11","DOIUrl":"https://doi.org/10.11648/j.jddmc.20170303.11","url":null,"abstract":"","PeriodicalId":16581,"journal":{"name":"Journal of Medicinal Chemistry and Drug Design","volume":"3 1","pages":"32"},"PeriodicalIF":0.0,"publicationDate":"2017-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89641812","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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