Pub Date : 2023-11-02DOI: 10.14233/ajomc.2023.ajomc-p27954
Sharmil Thangavel, Ezhilarasi Krishnamoorthy, Shyam Sundar Jaganathan, Abirami M. Padmanaban, Shila Samuel
The aim of the study was to identify effective biomarkers of changes in bone mineral density (BMD) at different stages of rheumatoid arthritis patients from South Indian population, using disease activity score in 28 joints (DAS28) which is being used as a measurement for assessing disease activity in patients with rheumatoid arthritis. The study was carried out in 92 rheumatoid arthritis patients. Serum level of tartrateresistant acid phosphatase-5b (TRAP-5b) and cathepsin K was measured using ELISA. Serum rheumatoid factor (RF) and C-reactive protein (CRP) was recorded by the attending rheumatologists. The C-reactive protein (CRP) was quantified using a latex immunoturbidimetric method. The rheumatoid arthritis (RA) was measured by turbidimetric immunoassay method. The bone mineral density (BMD) T-score was calculated according to WHO guidelines. Reverse transcription PCR (RT-PCR) was used to determine the expression of cathepsin K. The rheumatoid arthritis (RA) patients were categorized into three groups based on the DAS28 score as inactive (DAS ≤ 3.2), moderately active (DAS > 3.2 ≤ 5.1) and very active (DAS > 5.1) at the time of admission. Out of 92 patients, 16 (17.4%) patients had inactive disease condition, 42 (45.6%) patients had moderately active disease condition and 34 (37%) patients had very active disease condition. The mean BMD was significantly lower in very active (0.28 ± 0.04; p < 0.001) as compared with moderately active (0.71 ± 0.13; p < 0.001) and inactive (1.21 ± 0.14). TRAP5b and cathepsin K showed significant increases in very active group (p < 0.001) as compared with moderately active (p < 0.001) and inactive groups. In conclusion, The biomarker TRAP-5b and cathepsin K identified in this study may become a new and highly specific biomarker for rheumatoid arthritis
{"title":"Association of Cathepsin K and Tartrate- Resistant Acid Phosphatase-5b in Different Stages of Rheumatoid Arthritis Patients in South Indian Population","authors":"Sharmil Thangavel, Ezhilarasi Krishnamoorthy, Shyam Sundar Jaganathan, Abirami M. Padmanaban, Shila Samuel","doi":"10.14233/ajomc.2023.ajomc-p27954","DOIUrl":"https://doi.org/10.14233/ajomc.2023.ajomc-p27954","url":null,"abstract":"The aim of the study was to identify effective biomarkers of changes in bone mineral density (BMD) at different stages of rheumatoid arthritis patients from South Indian population, using disease activity score in 28 joints (DAS28) which is being used as a measurement for assessing disease activity in patients with rheumatoid arthritis. The study was carried out in 92 rheumatoid arthritis patients. Serum level of tartrateresistant acid phosphatase-5b (TRAP-5b) and cathepsin K was measured using ELISA. Serum rheumatoid factor (RF) and C-reactive protein (CRP) was recorded by the attending rheumatologists. The C-reactive protein (CRP) was quantified using a latex immunoturbidimetric method. The rheumatoid arthritis (RA) was measured by turbidimetric immunoassay method. The bone mineral density (BMD) T-score was calculated according to WHO guidelines. Reverse transcription PCR (RT-PCR) was used to determine the expression of cathepsin K. The rheumatoid arthritis (RA) patients were categorized into three groups based on the DAS28 score as inactive (DAS ≤ 3.2), moderately active (DAS > 3.2 ≤ 5.1) and very active (DAS > 5.1) at the time of admission. Out of 92 patients, 16 (17.4%) patients had inactive disease condition, 42 (45.6%) patients had moderately active disease condition and 34 (37%) patients had very active disease condition. The mean BMD was significantly lower in very active (0.28 ± 0.04; p < 0.001) as compared with moderately active (0.71 ± 0.13; p < 0.001) and inactive (1.21 ± 0.14). TRAP5b and cathepsin K showed significant increases in very active group (p < 0.001) as compared with moderately active (p < 0.001) and inactive groups. In conclusion, The biomarker TRAP-5b and cathepsin K identified in this study may become a new and highly specific biomarker for rheumatoid arthritis","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"4 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135975082","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 : 2023-11-02DOI: 10.14233/ajomc.2023.ajomc-p27959
Narayan G. Bhat, Percal Lopez
A convenient, novel synthesis of (E)-1-phenyl-1-alkenes based on (Z)-1-bromo-1-alkenylboronate esters will be developed. α-Bromo-(Z)-1-alkenylboronate esters readily available from literature procedures will undergo a reaction with phenyllithium in tetrahydrofuran to provide the corresponding “ate” complexes. These “ate” complexes will then undergo intramolecular nucleophilic substitution reactions to provide the corresponding (E)-1-alkenylboronate esters containing a phenyl moiety which upon protonolysis with acetic acid will afford the corresponding (E)-1-phenyl-1-alkenes. All (E)-1-phenyl-1-alkenes were characterized by PMR and CMR spectral data successfully.
{"title":"Highly Novel Diastereoselective Synthesis of (E)-1-Aryl-1-alkenes","authors":"Narayan G. Bhat, Percal Lopez","doi":"10.14233/ajomc.2023.ajomc-p27959","DOIUrl":"https://doi.org/10.14233/ajomc.2023.ajomc-p27959","url":null,"abstract":"A convenient, novel synthesis of (E)-1-phenyl-1-alkenes based on (Z)-1-bromo-1-alkenylboronate esters will be developed. α-Bromo-(Z)-1-alkenylboronate esters readily available from literature procedures will undergo a reaction with phenyllithium in tetrahydrofuran to provide the corresponding “ate” complexes. These “ate” complexes will then undergo intramolecular nucleophilic substitution reactions to provide the corresponding (E)-1-alkenylboronate esters containing a phenyl moiety which upon protonolysis with acetic acid will afford the corresponding (E)-1-phenyl-1-alkenes. All (E)-1-phenyl-1-alkenes were characterized by PMR and CMR spectral data successfully.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"3 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135975087","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 : 2023-11-02DOI: 10.14233/ajomc.2023.ajomc-p27957
Narayan G. Bhat
The stereo-defined synthesis of 1,4-dienes based on in situ generated stereo-defined alkenylcopper reagents is presented. The hydroboration of alkynes with dibromoborane-methyl sulfide complex followed by treatment with trimethylene glycol provides stable (E)-1-alkenylboronate esters. These boronate esters readily undergo “ate” complexes with a hindered base such as potassium-tert.-butoxide. The transmetalation of the alkenyl group from boron to copper via the “ate” complexes retains the original stereochemistry defined from the starting alkenylboronate esters. The effect of representative bases on stereodefined alkenylboronate esters and subsequent reaction of these boronate esters in the transmetalation reaction with copper(I) bromidemethyl sulfide is investigated. The resulting stereo-defined alkenyl copper species generated in situ readily couple with allylic bromide to give the corresponding 1,4-dienes with retention of stereochemistry. Since (Z)-1-alkenylboronate esters are easily accessible, both cisand trans-isomeric 1,4-dienes are synthesized.
{"title":"Alkenylcopper Reagents Prepared from Stereodefined Alkenylboronate Esters. Reaction with Allylic Halides as a Convenient Route to Stereodefined 1,4-Dienes","authors":"Narayan G. Bhat","doi":"10.14233/ajomc.2023.ajomc-p27957","DOIUrl":"https://doi.org/10.14233/ajomc.2023.ajomc-p27957","url":null,"abstract":"The stereo-defined synthesis of 1,4-dienes based on in situ generated stereo-defined alkenylcopper reagents is presented. The hydroboration of alkynes with dibromoborane-methyl sulfide complex followed by treatment with trimethylene glycol provides stable (E)-1-alkenylboronate esters. These boronate esters readily undergo “ate” complexes with a hindered base such as potassium-tert.-butoxide. The transmetalation of the alkenyl group from boron to copper via the “ate” complexes retains the original stereochemistry defined from the starting alkenylboronate esters. The effect of representative bases on stereodefined alkenylboronate esters and subsequent reaction of these boronate esters in the transmetalation reaction with copper(I) bromidemethyl sulfide is investigated. The resulting stereo-defined alkenyl copper species generated in situ readily couple with allylic bromide to give the corresponding 1,4-dienes with retention of stereochemistry. Since (Z)-1-alkenylboronate esters are easily accessible, both cisand trans-isomeric 1,4-dienes are synthesized.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"106 2","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135974937","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p351
P. Sandhya, K. S. Femina, A. Pradeep
The biologically active pyrazole clubbed imino naphthyl derivatives have been designed and synthesized from 1-phenyl-3-methoxy phenyl-1H-pyrazol-4-carboxaldehyde and substituted naphthyl amines via acid catalyzed condensation reaction. All the synthesized compounds were well characterized by different spectroscopic and mass spectral techniques. The in vitro antibacterial, antifungal and antituberculosis studies were carried out. The molecular docking study was also done with the software Arguslab 4.0.1. The studied compounds showed moderate to good biological activities both experimentally and theoretically. Geometry optimization, DNA binding interaction and FMO analysis were also investigated with the help of Gaussian 16 package at B3LYP/6-31G(d,p) level.
{"title":"Synthesis, DFT Calculations, DNA Binding and Molecular Docking Studies on Biologically\u0000Active N-((3-(4-Methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl)methylene)naphthyl Derivatives","authors":"P. Sandhya, K. S. Femina, A. Pradeep","doi":"10.14233/ajomc.2021.ajomc-p351","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p351","url":null,"abstract":"The biologically active pyrazole clubbed imino naphthyl derivatives have been designed and synthesized\u0000from 1-phenyl-3-methoxy phenyl-1H-pyrazol-4-carboxaldehyde and substituted naphthyl amines via\u0000acid catalyzed condensation reaction. All the synthesized compounds were well characterized by\u0000different spectroscopic and mass spectral techniques. The in vitro antibacterial, antifungal and\u0000antituberculosis studies were carried out. The molecular docking study was also done with the software\u0000Arguslab 4.0.1. The studied compounds showed moderate to good biological activities both\u0000experimentally and theoretically. Geometry optimization, DNA binding interaction and FMO analysis\u0000were also investigated with the help of Gaussian 16 package at B3LYP/6-31G(d,p) level.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"78 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83941837","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p345
A. Sanjeev, N. Naresh Reddy, M. Kumara Swamy, Rohini Rondla, S. R. Reddy, P. Muralidhar Reddy
Herein, a new tridentate (NNO) Schiff base ligand, (E)-4-[(quinoline-8-ylimino)methyl]benzene-1,2,3- triol derived from the condensation of 8-aminoquinoline with 2,3,4-trihydroxy benzaldehyde is reported. The ligand was complexed with certain metal ions like Co(II) (1), Ni(II) (2), Cu(II) (3), Zn(II) (4) and were characterized by various spectroscopic and analytical techniques such as FT-IR, UV-Vis, 1H NMR, 13C NMR, ESI-Mass, ESR, elemental analysis and magnetic susceptibility. Spectral data revealed octahedral geometry for cobalt(II), nickel(II), copper(II) complexes and tetrahedral geometry for zinc(II) complex. All the metal(II) complexes along with the Schiff base ligand were screened for their anticancer activities. The CT-DNA binding studies revealed high binding propensity for metal complexes with Kb values 1.50 × 104 M-1 for 1; 3.62 × 104 M-1 for 2; 2.53 × 104 M-1 for 3 and 1.8 × 104 M-1 for 4, respectively. Anticancer studies against A549 & MCF-7 demonstrated excellent antiproliferative activity with IC50 values in the range 17.62-48.82 μM. A standard drug cisplatin was employed to compare the activity of metal complexes. The complexes exhibited remarkable antitumour activity due to their high binding ability with DNA. It is interesting to observe that the complexes did not produce any cytotoxicity towards the normal cell lines.
{"title":"Synthesis, Characterization and in vitro Anticancer Studies of New Co(II), Ni(II), Cu(II) and\u0000Zn(II) Complexes of (E)-4-((Quinoline-8-ylimino)methyl)benzene-1,2,3-triol Ligand","authors":"A. Sanjeev, N. Naresh Reddy, M. Kumara Swamy, Rohini Rondla, S. R. Reddy, P. Muralidhar Reddy","doi":"10.14233/ajomc.2021.ajomc-p345","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p345","url":null,"abstract":"Herein, a new tridentate (NNO) Schiff base ligand, (E)-4-[(quinoline-8-ylimino)methyl]benzene-1,2,3-\u0000triol derived from the condensation of 8-aminoquinoline with 2,3,4-trihydroxy benzaldehyde is reported.\u0000The ligand was complexed with certain metal ions like Co(II) (1), Ni(II) (2), Cu(II) (3), Zn(II) (4) and\u0000were characterized by various spectroscopic and analytical techniques such as FT-IR, UV-Vis, 1H\u0000NMR, 13C NMR, ESI-Mass, ESR, elemental analysis and magnetic susceptibility. Spectral data revealed\u0000octahedral geometry for cobalt(II), nickel(II), copper(II) complexes and tetrahedral geometry for zinc(II)\u0000complex. All the metal(II) complexes along with the Schiff base ligand were screened for their anticancer\u0000activities. The CT-DNA binding studies revealed high binding propensity for metal complexes with\u0000Kb values 1.50 × 104 M-1 for 1; 3.62 × 104 M-1 for 2; 2.53 × 104 M-1 for 3 and 1.8 × 104 M-1 for 4,\u0000respectively. Anticancer studies against A549 & MCF-7 demonstrated excellent antiproliferative activity\u0000with IC50 values in the range 17.62-48.82 μM. A standard drug cisplatin was employed to compare the\u0000activity of metal complexes. The complexes exhibited remarkable antitumour activity due to their\u0000high binding ability with DNA. It is interesting to observe that the complexes did not produce any\u0000cytotoxicity towards the normal cell lines.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80233929","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p348
Ajay N Ambhore
In present work, one-pot multicomponent reaction (MCR) route for the synthesis of benzylideneiminothiazolyl- pyrazol-3-ol derivatives (5a-p) by reacting ethyl cyanoacetate (1), substituted benzaldehyde (2a-c), thiosemicarbazide (3) and substituted phenacyl bromide (4a-g). This reaction proceeds by using bleaching earth clay (BEC) (pH 12.5) in PEG-400 as a green reaction media. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The pharmacological investigation of the synthesized compounds suggest that most of them showed good antioxidant activity.
{"title":"Eco-friendly Synthesis of Some New Benzylidene-iminothiazolyl-pyrazol-3-ol Derivatives via\u0000One-Pot Multicomponent Reaction and Evaluation of Antioxidant Activities","authors":"Ajay N Ambhore","doi":"10.14233/ajomc.2021.ajomc-p348","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p348","url":null,"abstract":"In present work, one-pot multicomponent reaction (MCR) route for the synthesis of benzylideneiminothiazolyl-\u0000pyrazol-3-ol derivatives (5a-p) by reacting ethyl cyanoacetate (1), substituted\u0000benzaldehyde (2a-c), thiosemicarbazide (3) and substituted phenacyl bromide (4a-g). This reaction\u0000proceeds by using bleaching earth clay (BEC) (pH 12.5) in PEG-400 as a green reaction media. All\u0000the synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The\u0000pharmacological investigation of the synthesized compounds suggest that most of them showed good\u0000antioxidant activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"3 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73975867","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p343
B.R. Chaitanya Kumar, K. Sudhakar Babu, J. Latha
A pyridine derivative 2-((E)-1-(2-hydrazinyl-4-methyl-6-phenyl-pyridine-3-carboyl)ethyl)pyridine-4- carbonitrile (CPHPC) ligand and its 3d-metal(II) complexes has been synthesized (where [M = Co(II), Ni(II) and Cu(II)]. The physico-chemical, analytical data, UV-Vis, FT-IR, 1H NMR and ESR spectrum methods were used to characterize all of the synthesized complexes. Spectral investigations of metal(II) complexes revealed that the metal ion is surrounded by an octahedral geometry. Low conductance values indicated that the metal(II) complexes behave as non-electrolyte. The cytotoxic activity on lung cancer cell lines and hepatic cancer cell lines A549 and HepG2, respectively, with the ligand and their metal complexes were tested with MTT assay. The ligand and its metal complexes were tested for diverse harmful bacterial strains using the agar well diffusion method on Gram-negative bacteria such as Pseudomonas desmolyticum, Escherichia coli and Klebsiella aerogenes, as well as Gram-positive bacteria Staphylococcus aureus.
{"title":"Cytotoxicity and Antibacterial Studies of Newly Synthesized Novel\u0000Heterocylcic Pyridine Derivative and its Metal Complexes","authors":"B.R. Chaitanya Kumar, K. Sudhakar Babu, J. Latha","doi":"10.14233/ajomc.2021.ajomc-p343","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p343","url":null,"abstract":"A pyridine derivative 2-((E)-1-(2-hydrazinyl-4-methyl-6-phenyl-pyridine-3-carboyl)ethyl)pyridine-4-\u0000carbonitrile (CPHPC) ligand and its 3d-metal(II) complexes has been synthesized (where [M = Co(II),\u0000Ni(II) and Cu(II)]. The physico-chemical, analytical data, UV-Vis, FT-IR, 1H NMR and ESR spectrum\u0000methods were used to characterize all of the synthesized complexes. Spectral investigations of metal(II)\u0000complexes revealed that the metal ion is surrounded by an octahedral geometry. Low conductance\u0000values indicated that the metal(II) complexes behave as non-electrolyte. The cytotoxic activity on\u0000lung cancer cell lines and hepatic cancer cell lines A549 and HepG2, respectively, with the ligand and\u0000their metal complexes were tested with MTT assay. The ligand and its metal complexes were tested\u0000for diverse harmful bacterial strains using the agar well diffusion method on Gram-negative bacteria\u0000such as Pseudomonas desmolyticum, Escherichia coli and Klebsiella aerogenes, as well as Gram-positive\u0000bacteria Staphylococcus aureus.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73803111","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p355
M. Kausar, B. Manjunatha, C. Purvika, Mizba Farkana
The present study was carried out to investigate the antibacterial activity of the bioactive phenolic extract from Leucas aspera and Leucas cephalotes. The phenolic compounds were extracted using water: ethanol (1:3, v/v) by hydroethanolic extraction method. The hydroethanolic extracts were subjected to qualitative and FTIR analysis as a confirmatory step for the presence of phenolics. Synthesis of silver nanoparticle from both plants was carried out by acid hydrolysis method and subjected to UV-visible spectrophotometry, SEM, TEM and XRD analysis, for confirmation of tagged bioactive compound to AgNO3. The nanoparticle size distribution ranged between 50-94 nm in L. aspera and 40-67 nm in L. cephalotes. The antibacterial study was carried out using both crude phenolic extract and synthesized nanoparticles and tested against 5 pathogens namely Escherichia coli (ATCC® 8739™), Pseudomonas aeruginosa (ATCC® 25619™), Staphylococcus aureus (ATCC® 6538™), Bacillus subtilis (ATCC® 11774™) and Klebsiella pneumonia (ATCC® 13882™) for their antibacterial activity. From present study, the crude extract of L. cephalotes showed good antibacterial effect against test pathogen species wherein highest inhibition was observed in, P. aeruginosa, followed by B. subtilis and S. aureus with an average zone of inhibition of 23, 14 and 12 mm, E. coli and K. pneumonia measured 9 and 7 mm. The crude extract of L. aspera showed the highest inhibition in P. aeruginosa followed by S. aureus and E. coli with an average zone of inhibition of 12,11 and 10 mm B. subtilis and K. pneumonia measured 8 and 7 mm. Statistical analysis was calculated using One way ANOVA and was found to be statistically significant with p < 0.05.
{"title":"Synthesis of Silver Nanoparticle Using Bioactive Phenolic Compound Extracts of\u0000Leucas aspera and Leucas cephalotes and Evaluation of its Antibacterial Activity","authors":"M. Kausar, B. Manjunatha, C. Purvika, Mizba Farkana","doi":"10.14233/ajomc.2021.ajomc-p355","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p355","url":null,"abstract":"The present study was carried out to investigate the antibacterial activity of the bioactive phenolic extract\u0000from Leucas aspera and Leucas cephalotes. The phenolic compounds were extracted using water:\u0000ethanol (1:3, v/v) by hydroethanolic extraction method. The hydroethanolic extracts were subjected to\u0000qualitative and FTIR analysis as a confirmatory step for the presence of phenolics. Synthesis of silver\u0000nanoparticle from both plants was carried out by acid hydrolysis method and subjected to UV-visible\u0000spectrophotometry, SEM, TEM and XRD analysis, for confirmation of tagged bioactive compound to\u0000AgNO3. The nanoparticle size distribution ranged between 50-94 nm in L. aspera and 40-67 nm in L.\u0000cephalotes. The antibacterial study was carried out using both crude phenolic extract and synthesized\u0000nanoparticles and tested against 5 pathogens namely Escherichia coli (ATCC® 8739™), Pseudomonas\u0000aeruginosa (ATCC® 25619™), Staphylococcus aureus (ATCC® 6538™), Bacillus subtilis (ATCC®\u000011774™) and Klebsiella pneumonia (ATCC® 13882™) for their antibacterial activity. From present\u0000study, the crude extract of L. cephalotes showed good antibacterial effect against test pathogen species\u0000wherein highest inhibition was observed in, P. aeruginosa, followed by B. subtilis and S. aureus with\u0000an average zone of inhibition of 23, 14 and 12 mm, E. coli and K. pneumonia measured 9 and 7 mm.\u0000The crude extract of L. aspera showed the highest inhibition in P. aeruginosa followed by S. aureus\u0000and E. coli with an average zone of inhibition of 12,11 and 10 mm B. subtilis and K. pneumonia\u0000measured 8 and 7 mm. Statistical analysis was calculated using One way ANOVA and was found to be\u0000statistically significant with p < 0.05.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79716419","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p349
S. Prasad, S. L. Khokra, M. Devgun
Molecular docking is the identification of ligand’s correct binding geometry i.e. pose in the binding site and estimation of its binding affinity for rational design of drug molecule. The current study endeavored the high throughput in silico screening of 56 derivatives of dihydropyridazin-3(2H)-one docked with human cytosolic branched chain amino transferase using PyRx-virtual screening tool. Out of 56 compounds, almost all the test compounds showed very good binding affinity score. Gabapentin was used as standard drug which shows binding affinity of -6.2. On the basis of H-bond interactions, compounds 3, 9, 11, 25, 26, 31, 34, 39, 47, 48, 51, 54, 56 were found to be potent outcome for anticonvulsant activity. Compounds 11, 25, 39, 56 showed excellent H-bond interactions with protein active site, Among which compound 11 showed the outstanding interactions with acceptable bond length 2.34, 2.57, 2.62, 3.03 Å.
{"title":"Molecular Docking Studies of Dihydropyridazin-3(2H)-one\u0000Derivatives as Anticonvulsant Agents","authors":"S. Prasad, S. L. Khokra, M. Devgun","doi":"10.14233/ajomc.2021.ajomc-p349","DOIUrl":"https://doi.org/10.14233/ajomc.2021.ajomc-p349","url":null,"abstract":"Molecular docking is the identification of ligand’s correct binding geometry i.e. pose in the binding\u0000site and estimation of its binding affinity for rational design of drug molecule. The current study\u0000endeavored the high throughput in silico screening of 56 derivatives of dihydropyridazin-3(2H)-one\u0000docked with human cytosolic branched chain amino transferase using PyRx-virtual screening tool. Out\u0000of 56 compounds, almost all the test compounds showed very good binding affinity score. Gabapentin\u0000was used as standard drug which shows binding affinity of -6.2. On the basis of H-bond interactions,\u0000compounds 3, 9, 11, 25, 26, 31, 34, 39, 47, 48, 51, 54, 56 were found to be potent outcome for\u0000anticonvulsant activity. Compounds 11, 25, 39, 56 showed excellent H-bond interactions with protein\u0000active site, Among which compound 11 showed the outstanding interactions with acceptable bond\u0000length 2.34, 2.57, 2.62, 3.03 Å.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 6 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82228728","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 : 2021-12-31DOI: 10.14233/ajomc.2021.ajomc-p350
M. Das Sarma
Moringa oleifera Lam. (Moringaceae) is a multifarious beneficial tree and widely cultivated in the tropical and subtropical regions all over the world. All parts of this plants are edible and used as a plentiful source of phytochemicals with high nutritional values. Since antiquity, this plant was recognized as a panacea for the treatment of several ailments in ethnomedicinal system. In last few decades, this fact is further reconfirmed by various scientific research works in which the plant was found to show broad spectrum of biological activities including antioxidant, anti-inammatory, antiurolithic, antimicrobial, anangesic, antidiabetic, antihypertensive, antiproliferative, hepatoprotective, cardioprotective, etc. Different parts of this plant exhibited significant inhibitory activity against a variety of cancer cells at moderate to low concentrations and also possess low toxicity in normal cells. This review mainly focuses a brief overview on the anticancer profile of this wonderful tree.
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