Pub Date : 2020-07-06DOI: 10.19080/omcij.2019.09.555770
M. Sanhoury
A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.
{"title":"Synthesis, In vitro Antibacterial and Antifungal Activities of Trifluoroalkyl-N, N’-Disubstituted Thioureas","authors":"M. Sanhoury","doi":"10.19080/omcij.2019.09.555770","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555770","url":null,"abstract":"A series of N-(4-trifluoromethylphenyl) thiourea derivatives of biological interest has been prepared by the condensation of various isothiocyanates with primary 4-trifluorophenylamine under uncatalyzed conditions. The chemical structures of all the reported compounds were confirmed by FT-IR, multinuclear NMR (1H, 13C, 19F) and HRMS spectrometry. Some of these compounds were screened for their in vitro antibacterial activity against ten pathogenic strains representing different types of gram-positive and gram-negative bacteria, two pathogenic fungi ( Penicilluim sp, Aspergillus flavus ) and two yeasts ( Candida albicans and Candida glabrata ). More than four of the synthesized compounds showed promising inhibition activities against the tested strains ATCC 19436 with reference to standard vancomycin. Best antimicrobial activity was founded for the 3-pyridylthiourea derivative against Enterococcus faecuim ATCC 25923 with CMI= 3.9 mg/mL. The results indicated also that all the new screened compounds have promising antifungal activity comparable to the activity observed for the reference compounds.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"32 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-07-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73367219","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 : 2020-06-25DOI: 10.19080/omcij.2019.09.555769
R. Zibaseresht
A sample of cayenne pepper ,Capsicum annuum –(Family Solanaceae) was collected from a region in Hamadan, west Iran and extracted from EtOH. GC-MS analysis showed at least 8 compounds out of which 7 compounds were isolated and characterized using 1 H NMR analysis. Cytotoxic effects of the 7 isolated and characterized compounds along with the extract were evaluated against Caco-2 cell lines using MTT assay. The IC 50 values for ethyl palmitate (1), linolelaidic acid ethyl ester (2), ethyl stearate (3), ethyl iso-allocholate (4), 2-(((2-ethylhexyl)oxy)carbonyl) benzoic acid (5), capsaicin (6), dihydrocapsaicin (7) and the extract mixture were determined in μ M (111, 112, 118, 40, 130, 91, 115, and 110, respectively). The data indicated higher cytotoxic effects of (4) and (6) suggested as potential compounds against Caco-2 cell lines.
{"title":"Chemical Constituents of an Iranian Grown Capsicum annuum and their Cytotoxic Activities Evaluation","authors":"R. Zibaseresht","doi":"10.19080/omcij.2019.09.555769","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555769","url":null,"abstract":"A sample of cayenne pepper ,Capsicum annuum –(Family Solanaceae) was collected from a region in Hamadan, west Iran and extracted from EtOH. GC-MS analysis showed at least 8 compounds out of which 7 compounds were isolated and characterized using 1 H NMR analysis. Cytotoxic effects of the 7 isolated and characterized compounds along with the extract were evaluated against Caco-2 cell lines using MTT assay. The IC 50 values for ethyl palmitate (1), linolelaidic acid ethyl ester (2), ethyl stearate (3), ethyl iso-allocholate (4), 2-(((2-ethylhexyl)oxy)carbonyl) benzoic acid (5), capsaicin (6), dihydrocapsaicin (7) and the extract mixture were determined in μ M (111, 112, 118, 40, 130, 91, 115, and 110, respectively). The data indicated higher cytotoxic effects of (4) and (6) suggested as potential compounds against Caco-2 cell lines.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76198931","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 : 2020-06-24DOI: 10.19080/omcij.2019.09.555768
Kane S N
We report synthesis condition, and thermal treatment assisted tuning of structural, magnetic properties, and bandgap of Ni nano ferrite. Experimental techniques of x-ray diffraction ‘XRD,’ vibration sample magnetometry, Ultraviolet-visible (UV-Vis) diffuse reflectance measurements, Scanning Electron Microscopy ‘SEM,’ Energy Dispersive spectroscopy ‘EDS’ measurements, were used to study the synthesized samples. XRD verify the formation of nano spinel ferrite phase (grain diameter: 38.3-39.2nm), and incorporation of Ni, Fe in spinel lattice, with lattice parameter (0.8345-0.8352nm), which also shows the presence of α -Fe 2 O 3 phase. Results reveal that synthesis condition, and thermal treatment show: a) SEM images with non-homogeneous particle size dispersion, particle agglomeration, while EDS confirms the presence of all elements in studied NiFe 2 O 4 samples, b) non-equilibrium cation distribution, modification of inversion parameter, oxygen parameter, c) strengthening of A-O-B, A-O-A and weakening of B-O-B interaction super-exchange interactions, d) fine-tuning of bandgap (1.39 eV-1.68 eV), and depends on structural properties, e) observed magnetic properties are a collective effect of non-equilibrium cationic distribution; modification of A-O-B, A-O-A, B-O-B super-exchange interactions, and surface spin-canting. Prospective applications based on synthesized nano ferrites are also discussed. Thus, in this work we report, sol-gel auto-combustion synthesis of NiFe 2 O 4 : by varying synthesis conditions (via microwave-assisted sol-gel synthesis, conventional sol-gel synthesis in dry gel form), and post-preparation thermal annealing, to tune structural, magnetic properties and bandgap energy. Prepared samples are studied by x-ray diffraction ‘XRD,’ vibration sample magnetometry, Ultraviolet-visible (UV-Vis) diffuse reflectance measurements, Scanning Electron Microscopy SEM,’ Energy Dispersive spectroscopy ‘EDS’ measurements.
本文报道了镍纳米铁氧体的合成条件，以及热处理对镍纳米铁氧体结构、磁性能和带隙的影响。采用x射线衍射(XRD)、振动样品磁强计、紫外-可见(UV-Vis)漫反射测量、扫描电镜(SEM)、能谱(EDS)测量等实验技术对合成样品进行了研究。XRD验证了纳米尖晶石铁素体相(晶粒直径38.3 ~ 39.2nm)的形成，Ni、Fe在尖晶石晶格中掺入，晶格参数为0.8345 ~ 0.8352nm，同时α - fe2o3相的存在。结果表明，合成条件和热处理表明:a) SEM图像具有非均匀的粒度分散和颗粒团聚，而EDS证实了所研究的NiFe 2o4样品中所有元素的存在;b)非平衡阳离子分布，反演参数，氧参数的修改;c) a -O- b, a -O- a相互作用的增强和b -O- b相互作用超交换相互作用的减弱;d)带隙的微调(1.39 eV-1.68 eV)，并取决于结构性质。E)观察到的磁性是一种非平衡阳离子分布的集体效应;A-O-B、A-O-A、B-O-B超交换作用的修饰和表面自旋倾斜。并讨论了基于合成纳米铁氧体的应用前景。因此，在这项工作中，我们报告了nife2o4的溶胶-凝胶自燃烧合成:通过不同的合成条件(通过微波辅助的溶胶-凝胶合成，传统的干凝胶形式的溶胶-凝胶合成)，以及制备后的热退火，来调整结构，磁性能和带隙能量。通过x射线衍射(XRD)、振动样品磁强计、紫外可见(UV-Vis)漫反射测量、扫描电子显微镜(SEM)、能量色散光谱(EDS)测量对制备的样品进行了研究。
{"title":"Synthesis Condition and Treatment Assisted Tuning of Structural, Magnetic Properties and Bandgap of Ni Nano Ferrite","authors":"Kane S N","doi":"10.19080/omcij.2019.09.555768","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555768","url":null,"abstract":"We report synthesis condition, and thermal treatment assisted tuning of structural, magnetic properties, and bandgap of Ni nano ferrite. Experimental techniques of x-ray diffraction ‘XRD,’ vibration sample magnetometry, Ultraviolet-visible (UV-Vis) diffuse reflectance measurements, Scanning Electron Microscopy ‘SEM,’ Energy Dispersive spectroscopy ‘EDS’ measurements, were used to study the synthesized samples. XRD verify the formation of nano spinel ferrite phase (grain diameter: 38.3-39.2nm), and incorporation of Ni, Fe in spinel lattice, with lattice parameter (0.8345-0.8352nm), which also shows the presence of α -Fe 2 O 3 phase. Results reveal that synthesis condition, and thermal treatment show: a) SEM images with non-homogeneous particle size dispersion, particle agglomeration, while EDS confirms the presence of all elements in studied NiFe 2 O 4 samples, b) non-equilibrium cation distribution, modification of inversion parameter, oxygen parameter, c) strengthening of A-O-B, A-O-A and weakening of B-O-B interaction super-exchange interactions, d) fine-tuning of bandgap (1.39 eV-1.68 eV), and depends on structural properties, e) observed magnetic properties are a collective effect of non-equilibrium cationic distribution; modification of A-O-B, A-O-A, B-O-B super-exchange interactions, and surface spin-canting. Prospective applications based on synthesized nano ferrites are also discussed. Thus, in this work we report, sol-gel auto-combustion synthesis of NiFe 2 O 4 : by varying synthesis conditions (via microwave-assisted sol-gel synthesis, conventional sol-gel synthesis in dry gel form), and post-preparation thermal annealing, to tune structural, magnetic properties and bandgap energy. Prepared samples are studied by x-ray diffraction ‘XRD,’ vibration sample magnetometry, Ultraviolet-visible (UV-Vis) diffuse reflectance measurements, Scanning Electron Microscopy SEM,’ Energy Dispersive spectroscopy ‘EDS’ measurements.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"4 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73063303","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 : 2020-06-04DOI: 10.19080/omcij.2019.09.555767
Khalid M Wahdan
A derivative of thiourea ligand N-(2-chlorophenyl)-N’-Benzoyl thiourea (CBT) in equimolar ratio 1:1and its transition metal complexes Co II , Ni II , Cu II and Zn II were synthesized by microwave (green chemistry). The structure of ligand and its complexes have been characterized by using elemental analysis, mass Spectroscopy, FT-IR, UV-Vis,1HNMR and 13CNMR. The geometry of the proposed structures of the chelates based on their electronic spectra, electron spin resonance (ESR) and magnetic susceptibility. The stability of complexes was studied by TGA analysis (Thermal studies). The free derivative thiourea ligand (CBT) and its complexes were Studied for antibacterial and antifungal activity. Also the anticancer activity of ligand and its complexes were studied against breast cell cancer (MCF-7). It was noticed that the Ni II complex showed the highest cytotoxic activity (IC 50 =122) more than the free CBT ligand.
{"title":"Synthesis, Characterization, Biological and Antitumor Activity of Co(II) , Ni (II) , Cu(II) and Zn (II) Complexes of N-(2-Chlorophenyl)-N’-Benzoyl Thiourea","authors":"Khalid M Wahdan","doi":"10.19080/omcij.2019.09.555767","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555767","url":null,"abstract":"A derivative of thiourea ligand N-(2-chlorophenyl)-N’-Benzoyl thiourea (CBT) in equimolar ratio 1:1and its transition metal complexes Co II , Ni II , Cu II and Zn II were synthesized by microwave (green chemistry). The structure of ligand and its complexes have been characterized by using elemental analysis, mass Spectroscopy, FT-IR, UV-Vis,1HNMR and 13CNMR. The geometry of the proposed structures of the chelates based on their electronic spectra, electron spin resonance (ESR) and magnetic susceptibility. The stability of complexes was studied by TGA analysis (Thermal studies). The free derivative thiourea ligand (CBT) and its complexes were Studied for antibacterial and antifungal activity. Also the anticancer activity of ligand and its complexes were studied against breast cell cancer (MCF-7). It was noticed that the Ni II complex showed the highest cytotoxic activity (IC 50 =122) more than the free CBT ligand.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73244046","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 : 2020-05-27DOI: 10.19080/omcij.2019.09.555766
Clement Osei Akoto
Ficus sur (Moraceae), is a plant that has found use in traditional African medicine in the treatment of sickle cell disease, epilepsy, pain and inflammations. The present study was aimed at investigating hexane and methanol stem-bark extracts of Ficus sur for their phytoconstituents, anti-inflammatory, antimicrobial and antioxidant activities. Phytochemical screenings were performed using standard protocols. In-vitro anti-inflammatory activities were assessed using egg albumin denaturation method. In-vitro antimicrobial (agar and broth dilution method) and antioxidant [total antioxidant capacity (TAC), DPPH and H 2 O 2 scavenging] assays were carried out on the extracts. Thin layer chromatography was employed in the separation of the components of both extracts. The phytochemical investigation revealed the presence of secondary metabolites such as anthraquinones, terpenoids, flavonoids, steroids, saponins, phenols and tannins. The extracts showed anti-inflammatory activity comparable to that of diclofenac sodium. The extracts showed antimicrobial activity against test organisms with MICs ranging from 2.5- 40 mg/ mL. The IC 50 values for methanol and hexane extracts in the DPPH and H 2 O 2 assays were 89.95 ± 0.30 and 350.70 ± 0.72 μg/mL and 708.51 ± 0.28 and 682.76 ± 0.20 μg/mL, respectively. The TAC (gAAE/100 g) for methanol and hexane extracts were 23.560 ± 0.014 and 17.863 ± 0.037 g, respectively. The results suggest that the stem bark of Ficus sur could be exploited as potential therapeutic candidate for the treatment of bacterial infections, inflammations and diseases associated with oxidative-stress.
{"title":"An Assessment of the Anti-Inflammatory, Antimicrobial, and Antioxidant Activities of Ficus sur Stem-Bark","authors":"Clement Osei Akoto","doi":"10.19080/omcij.2019.09.555766","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555766","url":null,"abstract":"Ficus sur (Moraceae), is a plant that has found use in traditional African medicine in the treatment of sickle cell disease, epilepsy, pain and inflammations. The present study was aimed at investigating hexane and methanol stem-bark extracts of Ficus sur for their phytoconstituents, anti-inflammatory, antimicrobial and antioxidant activities. Phytochemical screenings were performed using standard protocols. In-vitro anti-inflammatory activities were assessed using egg albumin denaturation method. In-vitro antimicrobial (agar and broth dilution method) and antioxidant [total antioxidant capacity (TAC), DPPH and H 2 O 2 scavenging] assays were carried out on the extracts. Thin layer chromatography was employed in the separation of the components of both extracts. The phytochemical investigation revealed the presence of secondary metabolites such as anthraquinones, terpenoids, flavonoids, steroids, saponins, phenols and tannins. The extracts showed anti-inflammatory activity comparable to that of diclofenac sodium. The extracts showed antimicrobial activity against test organisms with MICs ranging from 2.5- 40 mg/ mL. The IC 50 values for methanol and hexane extracts in the DPPH and H 2 O 2 assays were 89.95 ± 0.30 and 350.70 ± 0.72 μg/mL and 708.51 ± 0.28 and 682.76 ± 0.20 μg/mL, respectively. The TAC (gAAE/100 g) for methanol and hexane extracts were 23.560 ± 0.014 and 17.863 ± 0.037 g, respectively. The results suggest that the stem bark of Ficus sur could be exploited as potential therapeutic candidate for the treatment of bacterial infections, inflammations and diseases associated with oxidative-stress.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"113 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79387606","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 : 2020-03-06DOI: 10.19080/omcij.2019.09.555764
Nasser M Abu Ghalwa
A modified bromothymol blue BTB electrode was prepared by spin coating of the BTB indicator on conducting glass substrate, and its use as indicator electrode to potentiometric acid-base titration in aqueous solution at 298 K was developed. The change of the open circuit potential with pH (E-pH) curve is linear with slope of 0.052 V/Dec at 298 K. The standard potential of this electrode, E0, was determined with respect to the SCE as reference electrode. The recovery percentage for potentiometric acid-base titration using G/BTB as indicator electrode was calculated
{"title":"Synthesis of a Novel Sensor Electrode Based on Bromothymol Blue as an Indicator Electrode in Potentiometric Acid-Base Titration in Aqueous Solution","authors":"Nasser M Abu Ghalwa","doi":"10.19080/omcij.2019.09.555764","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555764","url":null,"abstract":"A modified bromothymol blue BTB electrode was prepared by spin coating of the BTB indicator on conducting glass substrate, and its use as indicator electrode to potentiometric acid-base titration in aqueous solution at 298 K was developed. The change of the open circuit potential with pH (E-pH) curve is linear with slope of 0.052 V/Dec at 298 K. The standard potential of this electrode, E0, was determined with respect to the SCE as reference electrode. The recovery percentage for potentiometric acid-base titration using G/BTB as indicator electrode was calculated","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"22 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-03-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76344027","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 : 2020-02-21DOI: 10.19080/omcij.2019.09.555760
Hengguang Li
Pseudo nucleoside or short pseudo aptamer and telomerase have been selected as novel ligands and receptors in our effort to discover new anti-cancer reagents. We proposed that lithocholic acid (LCA) could be able to play the role of a vehicle to transport major therapeutic moiety into cell membrane through oral administration, like cholic acid delivering fatty acids, peptides in gastrointestinal track, but it’s more hydrophobic. Zidovudine or azidothymidine (AZT) was used as targeting head or/and therapeutic reagent aiming reverse transcriptase that plays central role of cancer cell telomere repairing. Telomerase is a reverse transcriptase, the major TERT, or hTERT in humans is a catalytic subunit of the entire enzyme. Even though both LCA and AZT have anticancer activities respectively, the conjugate of LCA-AZT was designed as our initial pseudo short aptamer inhibitor of cancer telomerase to verify our hypothetic concept that pseudo short aptamers targeting cancer telomerase are able to shut down the cancer cell growth, and cause the cells eventually senescence and mortality. As a consequence, two lung cancer cell lines and two colorectal cancer cell lines were treated by the conjugate, except lung cancer cell H1299, the efficacy of the conjugate was better than the parent compounds apparently. It conformed and proofed also the docking predictions via the molecular computational simulation. The all cancer cells used by a CCK-8 assay appeared apoptosis in the range of 56 μM – 90 μM IC50 after exposure to the LCA-AZT conjugate. The effectiveness of the conjugate was also time dependent, because the telomerase is a kind of reverse transcriptase, the mechanism would be like the inhibition of reverse transcriptase in HIV virus, the inhibition of telomere repairing toward cell death would be time consumable.
{"title":"LCA-AZT Conjugate Anti-Cancer invitro Activity","authors":"Hengguang Li","doi":"10.19080/omcij.2019.09.555760","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555760","url":null,"abstract":"Pseudo nucleoside or short pseudo aptamer and telomerase have been selected as novel ligands and receptors in our effort to discover new anti-cancer reagents. We proposed that lithocholic acid (LCA) could be able to play the role of a vehicle to transport major therapeutic moiety into cell membrane through oral administration, like cholic acid delivering fatty acids, peptides in gastrointestinal track, but it’s more hydrophobic. Zidovudine or azidothymidine (AZT) was used as targeting head or/and therapeutic reagent aiming reverse transcriptase that plays central role of cancer cell telomere repairing. Telomerase is a reverse transcriptase, the major TERT, or hTERT in humans is a catalytic subunit of the entire enzyme. Even though both LCA and AZT have anticancer activities respectively, the conjugate of LCA-AZT was designed as our initial pseudo short aptamer inhibitor of cancer telomerase to verify our hypothetic concept that pseudo short aptamers targeting cancer telomerase are able to shut down the cancer cell growth, and cause the cells eventually senescence and mortality. As a consequence, two lung cancer cell lines and two colorectal cancer cell lines were treated by the conjugate, except lung cancer cell H1299, the efficacy of the conjugate was better than the parent compounds apparently. It conformed and proofed also the docking predictions via the molecular computational simulation. The all cancer cells used by a CCK-8 assay appeared apoptosis in the range of 56 μM – 90 μM IC50 after exposure to the LCA-AZT conjugate. The effectiveness of the conjugate was also time dependent, because the telomerase is a kind of reverse transcriptase, the mechanism would be like the inhibition of reverse transcriptase in HIV virus, the inhibition of telomere repairing toward cell death would be time consumable.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"15 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77112956","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 : 2020-02-20DOI: 10.19080/omcij.2019.09.555763
Anil Kumar Nain
Studies on physicochemical properties of l -arginine/ l -histidine in aqueous solutions of betaine hydrochloride are beneficial in understanding solute-solvent interactions. The densities, ρ , ultrasonic speeds, u and viscosities, η of l -arginine and l -histidine in water and in aqueous-betaine hydrochloride (1 % and 2 % betaine hydrochloride in water, w/w) solvents have been experimentally measured at six temperatures (293.15, 298.15, 303.15, 308.15, 313.15 and 318.15) K and at atmospheric pressure in nine different concentrations. Related molecular and thermodynamic properties like the apparent molar volume, V φ , limiting apparent molar volume, and transfer volume, , were also evaluated in this study using density data. Likewise from the ultrasonic data, different thermo-acoustical parameters, such as apparent molar compressibility, , s K φ , limiting apparent molar compressibility, , s K οφ and transfer compressibility, , , s tr K οφ have been evaluated. The trends in transfer properties have been interpreted in terms of cosphere overlap model. In addition, the rheological data have been used to determine Falkenhagen Coefficient, A , Jones-Dole coefficient, B , free energy of activation of viscous flow per mole of solvent, and solute, #2 , entropies, # S ο ∆ and enthalpies, # H ο ∆ of activation of viscous flow. Hydration number, H n has also been calculated. Different parameters such as nature of solute, solute-solvent interactions, etc., were categorized by using different analytical and physical loom. The results show that the studied drug is a structure maker compound in all systems of this work. The free energy parameters indicate the formation of transition state in the presence of amino acids. The solute co-solute interactions are strongest in the system containing l -arginine.
研究甜菜碱水溶液中l -精氨酸/ l -组氨酸的理化性质有助于理解溶剂型相互作用。在293.15、298.15、303.15、308.15、313.15和318.15)K 6种温度和9种不同浓度的常压下，测定了l -精氨酸和l -组氨酸在水和盐酸水(1%和2%盐酸甜菜碱，w/w)溶剂中的密度、ρ、超声速度、u和粘度、η。相关的分子和热力学性质，如表观摩尔体积，V φ，极限表观摩尔体积和传动体积，也在本研究中使用密度数据进行了评估。同样，根据超声数据，对不同的热声参数，如表观摩尔压缩率，s K φ，极限表观摩尔压缩率，s K οφ和传递压缩率，s tr K οφ进行了评价。用球圈重叠模型解释了转移性质的变化趋势。此外，利用流变学数据确定了Falkenhagen系数，A, Jones-Dole系数，B，每摩尔溶剂的粘性流动激活自由能，溶质，#2，熵，# S ο∆和粘性流动激活焓，# H ο∆。还计算了水化数H n。利用不同的分析和物理织机对溶质性质、溶质-溶剂相互作用等参数进行了分类。结果表明，所研究的药物在本工作的所有体系中都是结构制造化合物。自由能参数反映了在氨基酸存在下过渡态的形成。在含有l -精氨酸的体系中，溶质-溶质相互作用最强。
{"title":"Insight into Interactions of l-Arginine/l-Histidine with Drug Betaine Hydrochloride in Aqueous Medium at Different Temperatures by using Physicochemical Methods","authors":"Anil Kumar Nain","doi":"10.19080/omcij.2019.09.555763","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555763","url":null,"abstract":"Studies on physicochemical properties of l -arginine/ l -histidine in aqueous solutions of betaine hydrochloride are beneficial in understanding solute-solvent interactions. The densities, ρ , ultrasonic speeds, u and viscosities, η of l -arginine and l -histidine in water and in aqueous-betaine hydrochloride (1 % and 2 % betaine hydrochloride in water, w/w) solvents have been experimentally measured at six temperatures (293.15, 298.15, 303.15, 308.15, 313.15 and 318.15) K and at atmospheric pressure in nine different concentrations. Related molecular and thermodynamic properties like the apparent molar volume, V φ , limiting apparent molar volume, and transfer volume, , were also evaluated in this study using density data. Likewise from the ultrasonic data, different thermo-acoustical parameters, such as apparent molar compressibility, , s K φ , limiting apparent molar compressibility, , s K οφ and transfer compressibility, , , s tr K οφ have been evaluated. The trends in transfer properties have been interpreted in terms of cosphere overlap model. In addition, the rheological data have been used to determine Falkenhagen Coefficient, A , Jones-Dole coefficient, B , free energy of activation of viscous flow per mole of solvent, and solute, #2 , entropies, # S ο ∆ and enthalpies, # H ο ∆ of activation of viscous flow. Hydration number, H n has also been calculated. Different parameters such as nature of solute, solute-solvent interactions, etc., were categorized by using different analytical and physical loom. The results show that the studied drug is a structure maker compound in all systems of this work. The free energy parameters indicate the formation of transition state in the presence of amino acids. The solute co-solute interactions are strongest in the system containing l -arginine.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"16 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84907011","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 : 2020-02-20DOI: 10.19080/omcij.2019.09.555761
Dame Seye
Nine rare earth complexes have been synthesized from reaction carried in common organic solvent between salicylate, maleate, phtalate, phenylsulfonate or phosphate ammonium salt and MCl3 (M = Y, Dy, Pr). All compounds have been structurally characterized by infrared. Structures involving the complex anions have been proposed. The suggested structures are discrete or of double metallic components type. The oxyanions behave towards metallic centres as monodentate, monochelating or monochelating and monodentate ligands. The coordination number at rare earth metal atoms vary from five (5) for Pr and Dy to twelve (12) for Dy. For compounds containing a protonated amine, when the possible hydrogen bonding interactions are considered supramolecular architectures may be
以水杨酸盐、马来酸盐、邻苯二甲酸盐、苯基磺酸盐或磷酸铵盐与mc3 (M = Y, Dy, Pr)为原料，在常见有机溶剂中合成了9种稀土配合物。所有化合物都用红外光谱进行了结构表征。已经提出了涉及复合阴离子的结构。所建议的结构是离散的或双金属构件型的。氧阴离子对金属中心表现为单齿、单螯合或单螯合和单齿配体。稀土金属原子的配位数从Pr和Dy的5(5)到Dy的12(12)不等。对于含有质子化胺的化合物，当可能的氢键相互作用被认为是超分子结构时
{"title":"New MCl3 (M = Y, Dy, Pr) Salicylato, Maleato, Phtalato, Phenylsufonato and Phosphato Complexes and Adducts: Synthesis and Infrared Study","authors":"Dame Seye","doi":"10.19080/omcij.2019.09.555761","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555761","url":null,"abstract":"Nine rare earth complexes have been synthesized from reaction carried in common organic solvent between salicylate, maleate, phtalate, phenylsulfonate or phosphate ammonium salt and MCl3 (M = Y, Dy, Pr). All compounds have been structurally characterized by infrared. Structures involving the complex anions have been proposed. The suggested structures are discrete or of double metallic components type. The oxyanions behave towards metallic centres as monodentate, monochelating or monochelating and monodentate ligands. The coordination number at rare earth metal atoms vary from five (5) for Pr and Dy to twelve (12) for Dy. For compounds containing a protonated amine, when the possible hydrogen bonding interactions are considered supramolecular architectures may be","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"26 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77738056","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 : 2020-02-18DOI: 10.19080/omcij.2019.09.555759
A. Intisar
Drug resistance among pathogenic bacteria has been a major concern for decades. Diseases caused by them have been the main cause of death in developing countries where this factor contributes around one third of the total number of deaths. With the gradual increase in microbial resistance and the side effects that synthetic medicines may cause, there has always been a need of finding natural medicines that can effectively treat such diseases. Among such potent resources are plant essential oils that have been reported in literature and is a recent topic of extraordinary interest. In this study, antimicrobial potential of essential oils of various plants against two resistant strains: methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Mycobacterium tuberculosis (MDRTB), has been discussed.
{"title":"Essential Oil Activity Against Methicillin-Resistant Staphylococcus aureus and Multidrug-Resistant Mycobacterium tuberculosis: A Mini-Review","authors":"A. Intisar","doi":"10.19080/omcij.2019.09.555759","DOIUrl":"https://doi.org/10.19080/omcij.2019.09.555759","url":null,"abstract":"Drug resistance among pathogenic bacteria has been a major concern for decades. Diseases caused by them have been the main cause of death in developing countries where this factor contributes around one third of the total number of deaths. With the gradual increase in microbial resistance and the side effects that synthetic medicines may cause, there has always been a need of finding natural medicines that can effectively treat such diseases. Among such potent resources are plant essential oils that have been reported in literature and is a recent topic of extraordinary interest. In this study, antimicrobial potential of essential oils of various plants against two resistant strains: methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Mycobacterium tuberculosis (MDRTB), has been discussed.","PeriodicalId":19547,"journal":{"name":"Organic & Medicinal Chemistry International Journal","volume":"116 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-02-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79223164","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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