Scientia Pharmaceutica[JOURNAL]
Sun
200 papers
Anticancer Activity Evaluation of New Thieno[2,3-]pyrimidin-4(3)-ones and Thieno[3,2-]pyrimidin-4(3)-one Derivatives.
Shyyka O, Pokhodylo N, Finiuk N … +3 more , Matiychuk V, Stoika R, Obushak M
Sci Pharm · 2018 Jul · PMID 30012942 · Full text
Anticancer screening of several novel thienopyrimidines has been performed. The thienopyrimidine derivatives were synthesized from available starting materials according to the convenient synthetic procedures using a one...
Anticancer screening of several novel thienopyrimidines has been performed. The thienopyrimidine derivatives were synthesized from available starting materials according to the convenient synthetic procedures using a one-pot solvent-free reaction which gave a wide access to thienopyrimidine-derivative production. The synthesized compounds were preselected via molecular docking to be tested for their anticancer activity in NCI 60 cell lines. It was observed that some compounds showed remarkable anticancer activity. It was found that the most active compound among thieno[2,3-]pyrimidine-4(3)-ones is 2-(benzylamino)-5,6-dimethylthieno[2,3-]pyrimidin-4(3)-one, which possesses cytotoxic activity on almost all cancer cell lines with mean growth 51.01%, where the most sensitive was the melanoma cell line MDA-MB-435 with GP (Growth Percent) = -31.02%. The patterns of structure⁻activity that are important for further optimization of the structure and the creation of more selective and active anticancer agents were proposed.
Antidepressant-Like Effect of CHAM (Verbenaceae) Essential Oil and Its Major Compound Thymol in Mice.
Parente MSR, Custódio FR, Cardoso NA … +7 more , Lima MJA, Melo TS, Linhares MI, Siqueira RMP, Nascimento AÁD, Catunda Júnior FEA, Melo CTV
Sci Pharm · 2018 Jun · PMID 29954101 · Full text
Depression is a common disease affecting more than 300 million people worldwide. Since has shown central nervous system effects in previous works, we aimed to investigate the effect of essential oil and its major compo...
Depression is a common disease affecting more than 300 million people worldwide. Since has shown central nervous system effects in previous works, we aimed to investigate the effect of essential oil and its major compound, thymol on a corticosterone-induced depression model in mice. Male mice (20⁻25 g) received corticosterone (20 mg/kg, subcutaneously), once a day for 22 days. From the 16th day on, mice were grouped to receive either corticosterone or essential oil (100 and 200 mg/kg), or thymol (25 and 50 mg/kg) or fluoxetine (35 mg/kg) by gavage. The forced swimming test, tail suspension, open field, elevated plus maze and sucrose preference tests were performed from the 19th to 22nd day. Data were analyzed by ANOVA followed by the Student-Newman-Keuls as a post hoc test and the results were considered significant when < 0.05. It was shown that essential oil, thymol and fluoxetine decreased the immobility time in the tail suspension and forced swimming tests and none of these altered locomotor activity in the open field test. However, the drugs increased the amount of grooming. In the elevated plus maze, all drugs increased the number of entries and the time of permanence in the open arms. In the sucrose preference test, the essential oil, thymol and fluoxetine reversed anhedonia. These results suggest that the thymol and essential oil have an antidepressant-like effect, similar to fluoxetine. However, future studies should be encouraged to enhance understanding of the effects of essential oil and thymol for the treatment of depression.
Thiopyrano[2,3-]Thiazoles as New Efficient Scaffolds in Medicinal Chemistry.
Kryshchyshyn A, Roman O, Lozynskyi A … +1 more , Lesyk R
Sci Pharm · 2018 Jun · PMID 29903979 · Full text
This review presents the up to date development of fused thiopyranothiazoles that comprise one of the thiazolidine derivatives classes. Thiazolidine and thiazolidinone-related compounds belong to the widely studied heter...
This review presents the up to date development of fused thiopyranothiazoles that comprise one of the thiazolidine derivatives classes. Thiazolidine and thiazolidinone-related compounds belong to the widely studied heterocycles from a medicinal chemistry perspective. From the chemical point of view, they are perfect heterodienes to undergo -Diels⁻Alder reaction with a variety of dienophiles, yielding regio- and diastereoselectively thiopyranothiazole scaffolds. The annealing of thiazole and thiopyran cycles in condensed heterosystem is a precondition for the “centers conservative” creation of the ligand-target binding complex and can promote a potential selectivity to biotargets. The review covers possible therapeutic applications of thiopyrano[2,3-]thiazoles, such as anti-inflammatory, antibacterial, anticancer as well as aniparasitic activities. Thus, thiopyrano[2,3-]thiazoles may be used as powerful tools in the development of biologically active agents and drug-like molecules.
Synthesis and Cytotoxicity Evaluation of Novel Asymmetrical Mono-Carbonyl Analogs of Curcumin (AMACs) against Vero, HeLa, and MCF7 Cell Lines.
Wiji Prasetyaningrum P, Bahtiar A, Hayun H
Sci Pharm · 2018 Jun · PMID 29880783 · Full text
A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synth...
A series of novel asymmetrical mono-carbonyl analogs of curcumin (AMACs) were synthesized and evaluated for cytotoxic activity using BSLT and MTT assay against Vero, HeLa, and MCF7 cell lines. The structures of the synthesized compounds were confirmed by FTIR, ¹H-NMR, C-NMR, and mass spectral data. The results of the cytotoxicity evaluation showed that the synthesized compounds exhibited moderate to very high toxic activity in BSLT (LC value 29.80⁻1704.23 µM); most of the compound exhibited cytotoxic activity against HeLa cell lines, which is comparable to the activity of cisplatin (IC value 40.65⁻95.55 µM), and most of the compound tested against MCF7 cell lines exhibited moderate to very high cytotoxic activity (IC value 7.86⁻35.88 µM). However, the selectivity index (SI) of the compounds was low (.
Influence of Ispaghula and Zein Coating on Ibuprofen-Loaded Alginate Beads Prepared by Vibration Technology: Physicochemical Characterization and Release Studies.
Lyn Heng JJ, Teng JH, Saravanan M … +1 more , Pushpamalar J
Sci Pharm · 2018 Jun · PMID 29874858 · Full text
The purpose behind the work was to fabricate alginate beads with better drug loading and extended drug release. Ispaghula was used to enhance the drug loading while zein was employed to extend the drug release. Ibuprofen...
The purpose behind the work was to fabricate alginate beads with better drug loading and extended drug release. Ispaghula was used to enhance the drug loading while zein was employed to extend the drug release. Ibuprofen was employed as a model drug in this study. Ibuprofen-loaded alginate beads with and without ispaghula were prepared using vibration technology and coated with zein. The beads prepared with alginate alone were shown to have loading and entrapment efficiencies of 35% and 70% , respectively. Addition of ispaghula in alginate showed a significant increase ( < 0.05) in the drug loading (42% ) and entrapment efficiency (84% ). Fourier-transform infrared spectroscopy confirmed the presence of ispaghula and zein coating in the alginate beads as well as the ibuprofen loading. Scanning electron microscopy revealed better spherical geometry in the beads with ispaghula. The surface morphology of the uncoated beads was rough due to crystalline and surface drug. The zein coating has produced a smoother surface and particle adhesion. Differential scanning calorimetry has shown a reduction in drug crystallinity. Alginate beads extended the drug release for 4 h and the presence of zein extended the release for 6 h.
Cocrystal of Ibuprofen⁻Nicotinamide: Solid-State Characterization and In Vivo Analgesic Activity Evaluation.
Yuliandra Y, Zaini E, Syofyan S … +4 more , Pratiwi W, Putri LN, Pratiwi YS, Arifin H
Sci Pharm · 2018 Jun · PMID 29867030 · Full text
Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The...
Ibuprofen is classified as a BCS class II drug which has low solubility and high permeability. We conducted the formation of the cocrystalline phase of ibuprofen with coformer nicotinamide to increase its solubility. The purpose of this study was to characterize the solid state of cocrystalline phase of ibuprofen-nicotinamide, determine the solubility, and evaluate its in vivo analgesic activity. The cocrystal of ibuprofen-nicotinamide was prepared by a slow evaporation method. The solid-state characterization was conducted by powder X-ray diffraction (PXRD) analysis, differential thermal analysis (DTA), and scanning electron microscopy (SEM). To investigate the in vivo analgesic activity, 28 male Swiss-Webster mice were injected with acetic acid 0.5% following oral administration of intact ibuprofen, physical mixture, and its cocrystalline phase with nicotinamide (equivalent to 26 mg/kg ibuprofen). The number of writhes was counted, and pain inhibition was calculated. All data were analyzed with one-way ANOVA followed by Duncan's Multiple Range Test (95% confidence interval). The results revealed that a new cocrystalline phase was successfully formed. The solubility testing showed that the cocrystal formation enhanced the solubility significantly as compared with the physical mixture and intact ibuprofen. A significant increase in the analgesic activity of cocrystal ibuprofen-nicotinamide was also confirmed.
Impact of Fermented Foods on Human Cognitive Function-A Review of Outcome of Clinical Trials.
Sivamaruthi BS, Kesika P, Chaiyasut C
Sci Pharm · 2018 May · PMID 29857528 · Full text
Food is an essential need for all living creatures which provides the energy to maintain life and grow further. Fermentation is a process used to preserve and advance the quality of foods, and those foods are known as fe...
Food is an essential need for all living creatures which provides the energy to maintain life and grow further. Fermentation is a process used to preserve and advance the quality of foods, and those foods are known as fermented foods. Some foods offer health benefits to consumers apart from nutrition, and such foods are called as functional foods. Most functional foods are fermented foods, and the fermenting microorganism plays a precious role in the functional property of the food. Cognitive decline is closely associated with the productivity of an individual and the society. Even though cognitive decline is connected to aging, dietary pattern influences memory, anxiety and other social behaviors. Many scientific studies have explained the link between food habits and cognitive functions by in vitro and in vivo models. The present review compiled the clinical data on the impact of fermented foods on human cognitive function.
Synthesis, Crystal Structure, and Biological Activity of Ethyl 4-Methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate Polymorphic Forms.
Ukrainets IV, Burian AA, Baumer VN … +5 more , Shishkina SV, Sidorenko LV, Tugaibei IA, Voloshchuk NI, Bondarenko PS
Sci Pharm · 2018 May · PMID 29848976 · Full text
Continuing the search for new potential analgesics among the derivatives of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid, the possibility of obtaining its esters by the alkylation of the corresponding sodiu...
Continuing the search for new potential analgesics among the derivatives of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid, the possibility of obtaining its esters by the alkylation of the corresponding sodium salt with iodoethane in dimethyl sulfoxide (DMSO) at room temperature was studied. It was found that under such conditions, together with the oxygen atom of the carboxyl group, a heteroatom of nitrogen is also alkylated. Therefore, the product of the reaction studied is a mixture of ethyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate (major) and its 1-ethyl-substituted analog (minor). A simple but very effective method of preparative separation of these compounds was proposed. Moreover, the heterogeneous crystallization from ethanol was revealed to result in a monoclinic polymorphic form of ethyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate, while the homogeneous crystallization results in its orthorhombic form. The molecular and crystal structures of both forms were confirmed by X-ray diffraction analysis, and the phase purity by powder diffraction study. The pharmacological tests carried out on the model of a carrageenan edema showed that the screening dose of 20 mg/kg of 1-ethyl-substituted ester and the orthorhombic form of its analog unsubstituted in position 1 exhibited weak anti-inflammatory and moderate analgesic effects. At the same time, the monoclinic form of ethyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate appeared to be both a powerful analgesic and an anti-inflammatory agent that exceeded Piroxicam and Meloxicam in the same doses by these indicators. A detailed comparative analysis of the molecular and crystal structures of two polymorphic forms of ethyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate was carried out using quantum chemical calculations of the energies of pairwise interactions between molecules. An explanation of the essential differences of their biological properties based on this was offered.
Host-Guest Interactions of Plumbagin with β-Cyclodextrin, Dimethyl-β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin: Semi-Empirical Quantum Mechanical PM6 and PM7 Methods.
Srihakulung O, Maezono R, Toochinda P … +3 more , Kongprawechnon W, Intarapanich A, Lawtrakul AL
Sci Pharm · 2018 May · PMID 29762548 · Full text
Molecular interactions of plumbagin inclusion complexes with β-cyclodextrin (BCD), dimethyl--cyclodextrin (MBCD), and hydroxypropyl-β-cyclodextrin (HPBCD) were investigated by semi-empirical, Parameterization Method 6 an...
Molecular interactions of plumbagin inclusion complexes with β-cyclodextrin (BCD), dimethyl--cyclodextrin (MBCD), and hydroxypropyl-β-cyclodextrin (HPBCD) were investigated by semi-empirical, Parameterization Method 6 and 7 (PM6, and PM7) in the aqueous phase using polarizable continuum calculations. The results revealed two different binding modes of the plumbagin molecule inside the BCD cavity with a negative value of the complexation energy. In conformation-I, the hydroxyl phenolic group of plumbagin was placed in the BCD cavity near the narrow-side of the host molecule. In the other model, conformation-II, the methyl quinone group of plumbagin was placed in the cavity of BCD near the narrow-side of the host molecule. The higher the negative value of the complexation energy, the more favorable is the pathway of inclusion-complex formation.
Effect of Massoia ( Becc.) Bark on the Phagocytic Activity of Wistar Rat Macrophages.
Hertiani T, Yuswanto A, Utami Tunjung Pratiwi S … +1 more , Muthma'innah Mashar H
Sci Pharm · 2018 May · PMID 29748470 · Full text
The essential oil of Massoia ( Becc., Lauraceae) bark is a potential immunomodulator in vitro. This study evaluated the potential immunomodulatory effects of Massoia bark infusion on the nonspecific immune response (phag...
The essential oil of Massoia ( Becc., Lauraceae) bark is a potential immunomodulator in vitro. This study evaluated the potential immunomodulatory effects of Massoia bark infusion on the nonspecific immune response (phagocytosis) of Wistar rats. For the in vitro assay, macrophages were treated with the freeze-dried infusion at the concentrations of 2.5, 5, 10, 20, or 40 µg/mL media. For the in vivo assay, two-month-old male Wistar rats were divided into five groups. The baseline group received distilled water at the dose of 1 mL/100 g body weight (BW), with the herbal product containing extract that was administered as the positive control at the dose of 0.54 mL/rat. The treatment groups received the infusion at a dose of 100, 300, or 500 mg/100 g BW. Treatments were given orally every day for 14 days. The ability of macrophage cells to phagocyte latex was determined as phagocytic index (PI), and it was observed under microscopy with 300 macrophages. The in vitro study revealed that the phagocytic activity of the infusion-treated macrophages significantly increased in comparison with that of the control macrophages in a concentration-dependent manner. Among all of the treatment concentrations, the concentration of 40 µg/mL provided the highest activity with a PI value of 70.51 ± 1.11%. The results of the in vivo assay confirmed those of the in vitro assay. The results of the present study indicate that Massoia bark can increase the phagocytic activity of rat macrophage cells.
Quantification of 6-Mercaptopurine and Its Metabolites in Patients with Acute Lympoblastic Leukemia Using Dried Blood Spots and UPLC-MS/MS.
Supandi S, Harahap Y, Harmita H … +1 more , Andalusia R
Sci Pharm · 2018 Apr · PMID 29693618 · Full text
This research aimed to quantitatively bioanalyze 6-mercaptopurine (6-MP), 6-methylmercaptopurine (6-MMP), and 6-thioguanosine-5′-monophosphate (6-TGMP) in dried blood spots (DBS) prepared from a small volume of acu...
This research aimed to quantitatively bioanalyze 6-mercaptopurine (6-MP), 6-methylmercaptopurine (6-MMP), and 6-thioguanosine-5′-monophosphate (6-TGMP) in dried blood spots (DBS) prepared from a small volume of acute lymphoblastic leukemia (ALL) patients. Analytes on the DBS card were extracted using 90% methanol with 5-fluorouracil (5-FU) as an internal standard. Analytical separation was performed on a Waters Acquity UPLC BEH AMIDA column of 1.7 μm (2.1 × 100 mm) with a mobile phase mixture of 0.2% formic acid in water and 0.1% formic acid in acetonitrile-methanol, with gradient elution and a flow rate of 0.2 mL/min. Mass detection of 6-MP, 6-MMP, 6-TGMP, and 5-FU showed / values of 153.09 > 119.09, 167.17 > 126.03, 380.16 > 168.00, and 129.09 > 42.05, respectively. This DBS method had a run time of 5 min and yielded a linear calibration curve over a range of 25.5⁻1020 ng/mL for 6-MP, 6-MMP, and 6-TGMP. Analyte analysis in 22 of 24 ALL patients showed that the measured value of 6-TGMP as an active metabolite was in the range of 29⁻429 pmol/8 × 10⁸ erythrocytes. Five of 22 patients had concentrations in a therapeutic range, which indicates that the treatment is effective, while 17 of 24 patients had concentrations below the therapeutic range, which indicates that a treatment dose adjustment is needed. The measured value of 6-MMP, an inactive metabolite, was in the range of 28⁻499 pmol/8 × 10⁸ erythrocytes, which includes concentrations below the hepatotoxic range. The method employed here can thus be effectively utilized to support therapeutic drug monitoring.
Betulin-3,28-diphosphate as a Component of Combination Cytostatic Drugs for the Treatment of Ehrlich Ascites Carcinoma In Vitro and In Vivo Experiments.
Vorobyova O, Deryabina O, Malygina D … +4 more , Plotnikova N, Solovyeva A, Belyaeva K, Melnikova N
Sci Pharm · 2018 Apr · PMID 29690651 · Full text
The activity of betulin-3,28-diphosphate (BDP) in combination with the cytostatics such as 5-fluorouracil (5-FU) and hydrazine sulfate (HS) was demonstrated by using the transplanted Ehrlich ascites carcinoma (EAC) in mi...
The activity of betulin-3,28-diphosphate (BDP) in combination with the cytostatics such as 5-fluorouracil (5-FU) and hydrazine sulfate (HS) was demonstrated by using the transplanted Ehrlich ascites carcinoma (EAC) in mice. The dose-dependent effect of combination drugs BDP + HS and BDP + 5-FU was revealed by in vitro experiments on rats. The synergetic effect of HS and BDP on oxidative stress and energy metabolism was established. The malonic dialdehyde (MDA) level both in plasma and erythrocytes decreased by 87 ± 2%, and the superoxide dismutase (SOD) activity increased by 105 ± 7% in comparison with the control. The combination of BDP + HS promoted the increase of lactate dehydrogenase (LDH) activity in the reverse reaction by 195 ± 21% compared to the control. The combination drug of 5-FU with BDP caused the synergetic decrease of the lipid peroxidation (LPO) intensity estimated by the MDA level decrease up to 14 ± 4% compared to pure compounds. Betulin-3,28-diphosphate in combination with cytostatics for EAC treatment improved the animal health status, as well as decreased the cytostatics dose that can be used in palliative therapy.
Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier.
Sharif Makhmal Zadeh B, Niro H, Rahim F … +1 more , Esfahani G
Sci Pharm · 2018 Apr · PMID 29677103 · Full text
One drawback of traditional forms of medical ocular dosage is drug dilution by tear; moreover, drugs are rapidly drained away from pre-corneal cavity by tear flow and lacrimo-nasal drainage. Prolonging contact time with...
One drawback of traditional forms of medical ocular dosage is drug dilution by tear; moreover, drugs are rapidly drained away from pre-corneal cavity by tear flow and lacrimo-nasal drainage. Prolonging contact time with different strategies and mucoadhesive vehicles will help to continuously deliver drugs to the eyes. For this study, we prepared and evaluated the effects of a nanostructure lipid carrier (NLC) on propranolol hydrochloride as a hydrophilic drug model for rabbit corneal permeation. Propranolol hydrochloride NLC was prepared using cold homogenization. The lipid was melted, then the drug and surfactant were dispersed and stirred into the melted lipid. This fused lipid phase was scattered in aqueous solution containing the cosurfactant at 4 °C and then homogenized. We evaluated particle size, drug loading, drug release, and NLC permeability through rabbit cornea as well as the formula’s effect on the cornea. Our results show that drug loading efficiency depended on the surfactant/lipid ratio (S/L) and the percentages of liquid lipid and Transcutol (Gattefosse, Saint-Priest, France) (as solubilizer). Drug release data were evaluated with the Higuchi model and a significant correlation was shown between the S/L ratio and the amount of drug released after 4 and 48 h. NLC formulations improved propranolol hydrochloride permeation. We conclude that the effect of the NLC formulations was due to mucoadhesive and film forming properties.
Novel Mutations in Gene of Pyrazinamide Resistant Clinical Isolates of .
Kahbazi M, Sarmadian H, Ahmadi A … +4 more , Didgar F, Sadrnia M, Poolad T, Arjomandzadegan M
Sci Pharm · 2018 Apr · PMID 29659533 · Full text
In clinical isolates of (MTB), resistance to pyrazinamide occurs by mutations in any positions of the gene (NC_000962.3) especially in nucleotides 359 and 374. In this study we examined the gene sequence in clinical i...
In clinical isolates of (MTB), resistance to pyrazinamide occurs by mutations in any positions of the gene (NC_000962.3) especially in nucleotides 359 and 374. In this study we examined the gene sequence in clinical isolates of MTB. Genomic DNA of 33 clinical isolates of MTB was extracted by the Chelex100 method. The polymerase chain reactions (PCR) were performed using specific primers for amplification of 744 bp amplicon comprising the coding sequences (CDS) of the gene. PCR products were sequenced by an automated sequencing Bioscience system. Additionally, semi Nested-allele specific (sNASP) and polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP) methods were carried out for verification of probable mutations in nucleotides 359 and 374. Sequencing results showed that from 33 MTB clinical isolates, nine pyrazinamide-resistant isolates have mutations. Furthermore, no mutation was detected in 24 susceptible strains in the entire 561 bp of the gene. Moreover, new mutations of G→A at position 3 of the gene were identified in some of the resistant isolates. Results showed that the sNASP method could detect mutations in nucleotide 359 and 374 of the gene, but the PCR-RFLP method by the SacII enzyme could not detect these mutations. In conclusion, the identification of new mutations in the gene confirmed the probable occurrence of mutations in any nucleotides of the gene sequence in resistant isolates of MTB.
Honey Bee as Alternative Medicine to Treat Eleven Multidrug-Resistant Bacteria Causing Urinary Tract Infection during Pregnancy.
Bouacha M, Ayed H, Grara N
Sci Pharm · 2018 Apr · PMID 29652864 · Full text
Medicinal benefits of honey bee have been recognized in the medical community since ancient times as a remedy for many diseases and infections. This study aimed to investigate the susceptibility of 11 multidrug-resistan...
Medicinal benefits of honey bee have been recognized in the medical community since ancient times as a remedy for many diseases and infections. This study aimed to investigate the susceptibility of 11 multidrug-resistant bacterial strains, isolated from urinary tract infections of pregnant women, to six honey samples collected from different localities in the east of Algeria. The evaluation of the antibacterial activity was performed by the well method followed by the broth dilution method using two-fold dilutions of each honey sample ranging from 2.5 to 80% (w/v). The results obtained in this study revealed that all tested honeys exhibited potent antibacterial activity against the tested strains. The diameters of inhibition ranged from 19.67 to 53.33 mm, with minimum inhibitory concentrations (MICs) ranging from 2.5 to 40% (w/v) and minimum bactericidal concentration (MBCs) varied between 2.5 and 80% (w/v). Gram-positive bacteria were found to be more susceptible than Gram-negative bacteria with diameters ranging from 43.33 to 53.33 mm; MIC and MBC values ranged from 2.5 to 5% (w/v). The strain was found to be less susceptible than other strains with inhibitory diameters ranging from 19.67 to 27.33 mm; MICs ranged from 20 to 40% and MBCs ranged from 20 to 80% (). This contribution has provided a broad overview of the antibacterial activity of Algerian honey and shown that honey bee has great potential for therapeutic use as an alternative therapy for urinary tract infection treatment which is safe and efficient during pregnancy.
Gliadin Peptide Facilitates FITC Dextran Transport across the Non Everted Gut Sac of Rat Small Intestine.
Utami RA, Hakiki A, Asyarie S … +1 more , Retnoningrum DS
Sci Pharm · 2018 Apr · PMID 29642636 · Full text
Superoxide dismutase (SOD) is an antioxidant protein. When administered orally, it has low bioavailability due to its low permeation. In a previous study we fused gliadin peptide P51 (LGQQQPFPPQQPYPQPQPF) and gliadin pep...
Superoxide dismutase (SOD) is an antioxidant protein. When administered orally, it has low bioavailability due to its low permeation. In a previous study we fused gliadin peptide P51 (LGQQQPFPPQQPYPQPQPF) and gliadin peptide P61 (QQPYPQPQPF) with SOD (SOD_Cl), namely GliSOD_P51 and GliSOD_P61 to increase permeation of SOD_Cl through intestine. In this work, the permeation of fluorescein isothiocyanate (FITC)-Dextran 10 kDa, FD10 and 40 kDa, FD40 as paracellular transport markers across excised rat intestinal wall was investigated with the presence of GliSOD_P51 and GliSOD_P61. A permeability study was performed using non-everted rat intestine by incubating FD10 or FD40 with SOD_Cl, and GliSOD_P61. The presence of SOD_Cl, GliSOD_P51 or GliSOD_P61 inside intestine (apical) and outside intestine (basolateral) was analyzed by protein electrophoresis. The concentration of FD that penetrated to the basolateral solution was analyzed by spectrofluorometry. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) analysis revealed the presence of GliSOD_P51 and GliSOD_P61 but not SOD_Cl in basolateral compartment. The percentage of FD10 but not FD40 and SOD_Cl that penetrated to the basolateral solution significantly increased with the presence of gliadin in GliSOD_P51 and GliSOD_P61. GliSOD_P51 and GliSOD_P61 are able to penetrate the rat intestinal epithelial membrane and the gliadin peptides facilitate FD10 to penetrate the epithelial.
N-Aryl-7-hydroxy-5-oxo-2,3-dihydro-1H,5H-pyrido-[3,2,1-ij]quinoline-6-carboxamides. The Synthesis and Effects on Urinary Output.
Ukrainets IV, Sidorenko LV, Golik MY … +3 more , Chernenok IM, Grinevich LA, Davidenko AA
Sci Pharm · 2018 Apr · PMID 29642551 · Full text
Continuing a targeted search for new leading structures with diuretic action among tricyclic derivatives of hydroxyquinolines, which are of interest as potential inhibitors of aldosterone synthase, the synthesis of a ser...
Continuing a targeted search for new leading structures with diuretic action among tricyclic derivatives of hydroxyquinolines, which are of interest as potential inhibitors of aldosterone synthase, the synthesis of a series of the corresponding pyrido[3,2,1-]quinoline-6-carboxanilides was carried out by amidation of ethyl-7-hydroxy-5-oxo-2,3-dihydro-1,5-pyrido[3,2,1-]quinoline-6-carboxylate with aniline, aminophenols and -alkylsubstituted analogs with high yields and purity. The optimal conditions of this reaction are proposed; they make it possible to prevent partial destruction of the original heterocyclic ester and thereby avoid formation of specific impurities of 7-hydroxy-2,3-dihydro-1,5-pyrido[3,2,1-]quinolin-5-one. To confirm the structure of all substances obtained, elemental analysis, nuclear magnetic resonance (NMR) spectroscopy, and mass spectrometry were used. Moreover, the peculiarities of their ¹H and C-NMR spectra, as well as their mass spectrometric behavior under conditions of electron impact ionization, were discussed. The effect of pyrido[3,2,1-]quinoline-6-carboxanilides on the urinary function of the kidneys was studied in white rats of both genders by the standard method of oral administration at a dose of 10 mg/kg. Testing was conducted in comparison with hydrochlorothiazide, as well as with structurally close pyrrolo[3,2,1-] quinoline-5-carboxanilides studied earlier with the same substituents in the anilide fragments. It was found that addition of one methylene unit to the heterocycle partially hydrogenated and annelated with the quinolone core has a positive impact on biological properties-most of the substances studied exhibit a statistically significant diuretic effect exceeding the activity of not only hydrochlorothiazide, in some cases, but also the action of the structural analogs. The important structural and biological regularities, which are common with pyrroloquinolines and introduced by a chemical modification, were revealed. The importance of the presence in the structure of terminal amide fragments of tricyclic quinoline-3-carboxamides of a 4-methoxy-substituted aromatic ring was particularly marked. The expediency of further study of pyridoquinolines as promising diuretic agents has been shown.
Acetylcholinesterase Inhibition and Antioxidant Activity of --Caffeoyldopamine and --Feruloyldopamine.
Dizdar M, Vidic D, Požgan F … +2 more , Štefane B, Maksimović M
Sci Pharm · 2018 Apr · PMID 29617286 · Full text
Phenolic acids and their derivatives found in nature are well-known for their potential biological activity. In this study, two amides derived from -caffeic/ferulic acid and dopamine were synthesized and characterized by...
Phenolic acids and their derivatives found in nature are well-known for their potential biological activity. In this study, two amides derived from -caffeic/ferulic acid and dopamine were synthesized and characterized by Fourier-transform infrared spectroscopy (FTIR), mass spectrometry, proton and carbon-13 nuclear magnetic resonance spectroscopy. The compounds were tested for the inhibition of acetylcholinesterase (AChE) from and for antioxidant activity by scavenging 2,2-diphenyl-1-pycrylhydrazyl free radical (DPPH) and 2,2′-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) radical cation (ABTS), reducing ferric ions, and ferrous ions chelation. --Feruloyldopamine displayed the highest inhibitory effect on AChE with half-maximal inhibitory concentration () values of 8.52 μM. In addition, an in silico study was done to determine the most favorable AChE cluster with the synthesized compounds. Further, these clusters were investigated for binding positions at the lowest free binding energy. Both synthesized hydroxycinnamates were found to be better antioxidants than the parent acids in in vitro tests applied. --Caffeoyldopamine showed the best antioxidant activity in the three tested methods—against non-biological stable free radicals 5.95 μM for DPPH, 0.24 μM for the ABTS method, and for reducing power (ascorbic acid equivalent 822.45 μmol/mmol)—while for chelation activity against Fe ions --feruloyldopamine had slightly better antioxidant activity ( 3.17 mM).
Application of the P300 Event-Related Potential in the Diagnosis of Epilepsy Disorder: A Review.
Sowndhararajan K, Kim M, Deepa P … +2 more , Park SJ, Kim S
Sci Pharm · 2018 Mar · PMID 29587468 · Full text
Epilepsy is one of the most serious chronical neurological disorders, affecting more than 50 million people worldwide. It can be defined as a spectrum disorder, and patients with epilepsy possess abnormalities in cogniti...
Epilepsy is one of the most serious chronical neurological disorders, affecting more than 50 million people worldwide. It can be defined as a spectrum disorder, and patients with epilepsy possess abnormalities in cognitive functions. A number of factors can cause cognitive dysfunctions in epileptic syndromes, including etiology, the age of onset, type of seizure and severity, duration, and antiepileptic drugs. Event-related potentials (ERPs) are very useful clinical and research instruments to evaluate cognitive function in patients with neuropsychiatry disorders. Event-related potentials directly reflect cortical neuronal activity and provide a particular level of temporal resolution. Among various ERP components, the P300 is the most important component for assessing cognitive processes such as attention, working memory, and concentration. Numerous studies have reported the abnormalities in amplitude or latency of P300 component of ERP in epileptic patients, and these abnormalities are indicative of cognitive dysfunction. Therefore, the purpose of this review is to consolidate the existing literature in connection with the use of P300 in epileptic patients.
4-Methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxylic Acid. Peculiarities of Preparation, Structure, and Biological Properties.
Ukrainets IV, Hamza GM, Burian AA … +3 more , Shishkina SV, Voloshchuk NI, Malchenko OV
Sci Pharm · 2018 Mar · PMID 29518063 · Full text
In order to determine the regularities of the structure-analgesic activity relationship, the peculiarities of obtaining, the spatial structure, and biological properties of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carb...
In order to determine the regularities of the structure-analgesic activity relationship, the peculiarities of obtaining, the spatial structure, and biological properties of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid and some of its derivatives have been studied. Using nuclear magnetic resonance (NMR) spectroscopy and X-ray diffraction analysis, it has been proven that varying the reaction conditions using alkaline hydrolysis of methyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate makes it possible to successfully synthesize a monohydrate of the target acid, its sodium salt, or 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine. The derivatographic study of the thermal stability of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid monohydrate has been carried out; based on this study, the optimal conditions completely eliminating the possibility of unwanted decomposition have been proposed for obtaining its anhydrous form. It has been shown that 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine is easily formed during the decarboxylation of not only 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid, but also its sodium salt, which is capable of losing СО₂ both in rather soft conditions of boiling in an aqueous solution, and in more rigid conditions of dry heating. The NMR spectra of the compounds synthesized are given; their spatial structure is discussed. To study the biological properties of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid and its sodium salt, the experimental model of inflammation caused by subplantar introduction of the carrageenan solution in one of the hind limbs of white rats was used. The anti-inflammatory activity and analgesic effect were assessed by the degree of edema reduction and the ability to affect the pain response compared to the animals of control groups. According to the results of the tests performed, it has been found that after intraperitoneal injection, the substances synthesized demonstrate a moderate anti-inflammatory action and simultaneously increase the pain threshold of the experimental animals very effectively, exceeding Lornoxicam and Diclofenac in a similar dose by their analgesic activity.
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