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Scientia Pharmaceutica

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https://www.readbyqxmd.com/read/29324660/in-vitro-bioavailability-study-of-an-antiviral-compound-enisamium-iodide
#1
Eleonore Haltner-Ukomadu, Svitlana Gureyeva, Oleksii Burmaka, Andriy Goy, Lutz Mueller, Grygorii Kostyuk, Victor Margitich
An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four different buffers. Apparent intestinal permeability (Papp) of enisamium iodide was assessed using human colon carcinoma (Caco-2) cells at three concentrations. The solubility of enisamium iodide in four buffer solutions from pH 1...
January 11, 2018: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/29267246/4-5-dimethoxy-2-nitrobenzohydrazides-and-1-1-benzylpiperidin-4-yl-ethan-1-ones-as-potential-antioxidant-cholinergic-endowed-small-molecule-leads
#2
Rukhsar Banu, Jason Gerding, Cynthia Franklin, Donald Sikazwe, William Horton, Marianna Török, Julian Davis, Kwan H Cheng, Muziya Nakazwe, Bereket Mochona
The objective of this research is to generate leads for developing our ultimate poly-active molecules with utility in central nervous system (CNS) diseases. Indeed, poly-active molecules capable of mitigating brain free radical damage while enhancing acetylcholine signaling (via cholinesterase inhibition) are still being sought for combating Alzheimer's disease (AD). We differentiate "poly-active" agents from "multi-target" ones by defining them as single molecular entities designed to target only specific contributory synergistic pharmacologies in a disease...
December 21, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/29257120/a-fast-and-validated-reversed-phase-hplc-method-for-simultaneous-determination-of-simvastatin-atorvastatin-telmisartan-and-irbesartan-in-bulk-drugs-and-tablet-formulations
#3
Hassan A Alhazmi, Ahmed M Alnami, Mohammed A A Arishi, Raad K Alameer, Mohammed Al Bratty, Zia Ur Rehman, Sadique A Javed, Ismail A Arbab
The aim of this study was to develop and validate a fast and simple reversed-phase HPLC method for simultaneous determination of four cardiovascular agents-atorvastatin, simvastatin, telmisartan and irbesartan in bulk drugs and tablet oral dosage forms. The chromatographic separation was accomplished by using Symmetry C18 column (75 mm × 4.6 mm; 3.5 μ) with a mobile phase consisting of ammonium acetate buffer (10 mM; pH 4.0) and acetonitrile in a ratio 40:60 v/v. Flow rate was maintained at 1 mL/min up to 3...
December 19, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/29160825/theoretical-investigation-of-the-enantioselective-complexations-between-pfdhfr-and-cycloguanil-derivatives
#4
Suriyawut Kulatee, Pisanu Toochinda, Anotai Suksangpanomrung, Luckhana Lawtrakul
Point mutations in Plasmodium falciparum dihydrofolate reductase (pfDHFR), especially the double mutant variant (A16V + S108T), led to ineffective inhibiting by cycloguanil (Cyc). Cycloguanil derivatives showed good inhibiting properties against wild-type and mutant pfDHFR with an inhibition constant as low as the nanomolar level. However, there have been no reports on the stereochemistry of the compounds, and this is important because the pure enantiomeric form of a chiral drug can exert desirable, as well as non-desirable responses on the body or both...
November 21, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/29156612/leishmanicidal-activity-of-biogenic-fe%C3%A2-o%C3%A2-nanoparticles
#5
Mehrdad Khatami, Hajar Alijani, Iraj Sharifi, Fatemeh Sharifi, Shahram Pourseyedi, Sam Kharazi, Marcos Augusto Lima Nobre, Manouchehr Khatami
Abstract: Due to the multiplicity of useful applications of metal oxide nanoparticles (ONPs) in medicine are growing exponentially, in this study, Fe₃O₄ (iron oxide) nanoparticles (IONPs) were biosynthesized using Rosemary to evaluate the leishmanicidal efficiency of green synthesized IONPs. This is the first report of the leishmanicidal efficiency of green synthesized IONPs against Leishmania major. The resulting biosynthesized IONPs were characterized by ultraviolet-visible spectroscopy (UV-Vis), X-ray diffraction (XRD), transmission electron microscopy (TEM), and Fourier transform infrared spectroscopy (FTIR)...
November 20, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/29064425/hydrogen-sulfide-releasing-2-mercaptoacrylic-acid-based-derivative-possesses-cytoprotective-activity-in-a-small-intestine-of-rats-with-medication-induced-enteropathy
#6
Yulia Sklyarova, Iryna Fomenko, Iryna Lozynska, Andrii Lozynskyi, Roman Lesyk, Alexandr Sklyarov
Small intestinal injury is known to be one of the most commonly appearing pathologies, resulting in the use of medications such as: nonsteroidal anti-inflammatory drugs (NSAIDs), antitumor drugs and angiotensin-converting enzyme (ACE) inhibitors. The principal objective of this study is to evaluate the action of a novel mercaptoacrylic acid derivative able to release H₂S on parameters of NO-synthase system and oxidative stress. Inducing enteropathy, three types of medications were used: indomethacin, an NSAID (35 mg/kg); methotrexate, an antitumor drug (10 mg/kg); and enalapril, an ACE inhibitor (2 mg/kg/day)...
October 24, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28974052/antimycobacterial-activities-of-n-substituted-glycinyl-1h-1-2-3-triazolyl-oxazolidinones-and-analytical-method-development-and-validation-for-a-representative-compound
#7
Naser F Al-Tannak, Oludotun A Phillips
Twelve N-substituted-glycinyl triazolyl oxazolidinone derivatives were screened for antimycobacterial activity against susceptible (Mycobacteriumtuberculosis (Mtb) H37Rv) and resistant (isoniazid (INH)-resistant Mtb (SRI 1369), rifampin (RMP)-resistant Mtb (SRI 1367), and ofloxacin (OFX)-resistant Mtb (SRI 4000)) Mtb strains. Most of the compounds showed moderate to strong antimycobacterial activity against all strains tested, with minimum inhibitory concentration (MIC) value ranges of 0.5-11.5, 0.056-11.6, 0...
October 2, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28930168/a-review-of-the-composition-of-the-essential-oils-and-biological-activities-of-angelica-species
#8
REVIEW
Kandasamy Sowndhararajan, Ponnuvel Deepa, Minju Kim, Se Jin Park, Songmun Kim
A number of Angelica species have been used in traditional systems of medicine to treat many ailments. Especially, essential oils (EOs) from the Angelica species have been used for the treatment of various health problems, including malaria, gynecological diseases, fever, anemia, and arthritis. EOs are complex mixtures of low molecular weight compounds, especially terpenoids and their oxygenated compounds. These components deliver specific fragrance and biological properties to essential oils. In this review, we summarized the chemical composition and biological activities of EOs from different species of Angelica...
September 20, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28927024/in-vitro-activities-of-enantiopure-and-racemic-1-acetoxychavicol-acetate-against-clinical-isolates-of-mycobacterium-tuberculosis
#9
Saradee Warit, Kamolchanok Rukseree, Therdsak Prammananan, Poonpilas Hongmanee, Pamaree Billamas, Sarinya Jaitrong, Angkana Chaiprasert, Birgit U Jaki, Guido F Pauli, Scott G Franzblau, Prasit Palittapongarnpim
In the process of evaluating the effect of several plant extracts against Mycobacterium tuberculosis using the Microplate Alamar Blue Assay (MABA), an extract of Thai herb Alpinia galanga rhizome and its major component, 1'-acetoxychavicol acetate (ACA), exhibited marked anti-tuberculosis activity. The minimal inhibition concentrations (MICs) of the S-enantiomer of ACA (S-ACA) against M. tuberculosis H37Ra ATCC 25177 and H37Rv ATCC 27294 strains were 0.2 µg/mL and 0.7 µg/mL, respectively. More than 95% of 100 drug-sensitive and 50 drug-resistant mycobacterial clinical isolates were inhibited by extracted S-ACA at 1...
September 18, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28914808/structural-and-dynamics-perspectives-on-the-binding-of-substrate-and-inhibitors-in-mycobacterium-tuberculosis-dhfr
#10
Pimonluck Sittikornpaiboon, Pisanu Toochinda, Luckhana Lawtrakul
Dihydrofolate reductase (DHFR), an essential enzyme in the folate pathway, is a potential target for new anti-tuberculosis drugs. Fifteen crystal structures of Mycobacterium tuberculosis DHFR complexed with NADPH and various inhibitors are available in the RCSB Protein Data Bank, but none of them is a substrate binding structure. Therefore, we performed molecular dynamics simulations on ternary complexes of M. tuberculosis DHFR:NADPH with a substrate (dihydrofolate) and each of three competitive inhibitors the in 2,4-diaminopyrimidine series (P1, P157, and P169), in order to gain insight into the inhibition-mechanism of DHFR in the folate pathway...
September 15, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28841190/alkaloids-from-oxytropis-myriophylla-pall-dc
#11
Keisuke Kojima, Purevsuren S, Narantuya S, Tsetsegmaa S, Jamyansan Ya, Kimio Lsaka, Yukio Ogihara
Five alkaloids were isolated from the epigeal part of Oxytropis myriophylla. Three alkaloids were identified as N-benzoyl-β-phenylethylamine, N-trans-cinnamoyl-β-phenylethylamine, N-cis-cinnamoyl-β-phenylethylamine and the structures of two new alkaloids were elucidated to be N-benzoyl-β-hydroxyphenylethylarnine(2), N-trans-cinnamoyl-β-hydroxy-phenylethylamine(5). The absolu.te structures were established by modified Mosher method.
August 25, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28841172/zytoprotektion-mit-amifostin-ethyol-%C3%A2-in-der-chemotherapie-meta-analyse-zum-pharmakokinetischen-interaktionspotential-mit-zytostatika
#12
Martin Czejka, Johannes Schüller, Heidemarie Kletzl
The cytoprotective agent amifostine (AMI) is capable to protect healthy cells (contrary to tumor cells) due to higher activity of alkaline phosphatase at the membrane site of normal cells. In seven clinical trials the influence of AMI on the pharmacokinetics of different cytostatics was investigated. Preadministration of AMI increased Cmax of doxorubicin (+ 44 %, p < 0.06), epirubicin (+ 31 %, P < 0.08), mitomycin C (+ 41 %, p < 0.01) and docetaxel (+ 31 % and + 17 %, not significant). In contrary, the peak concentration of pirarubicin , the tetrahydropyranyl-prodrug of doxorubicin was decreased (- 50 %, P < 0...
August 25, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28825665/evaluation-of-acute-and-subacute-oral-toxicity-induced-by-ethanolic-extract-of-marsdenia-tenacissima-leaves-in-experimental-rats
#13
Mayur Porwal, Najam Ali Khan, Kamal Kishore Maheshwari
The objective of this study is to evaluate the acute and subacute toxicity of the ethanolic extract of Marsdenia tenacissima (MTE) leaves (family: Asclepiadaceae) in albino rats. The acute toxicity was performed where the limit dose of 5000 mg/kg body weight used. Observations were made and recorded for 24 h, and once daily further for a period of 14 days. The rats were weighed and various observations, like mortality, behavior, injury, or any signs of illness were conducted once daily during the period. For subacute study, four groups of 10 animals (female rats) received 10% Tween 20 in distilled water (control), and 250, 500, and 1000 mg/kg of freshly-prepared extracts, respectively, every 24 h orally for 28 days...
August 21, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28817110/extractive-spectrophotometric-determination-of-nortriptyline-hydrochloride-using-sudan-ii-iv-and-black-b
#14
A S Amin, H M Saleh
A simple spectrophotometric methods has been developed for the determination of nortriptyline hydrochloride in pure and in pharmaceuticalformulations based on the formation of ion-pair complexes with sudun II (SII), sudan (IV) (SIV) and sudan black B (SBB). The selectivity of the method was improved through extraction with chloroform. The optimum conditions for complete extracted colour development were assessed. The absorbance measurements were made at 534, 596 and 649 nm for SII, SIV and SBB complexes, respectively...
August 17, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28813032/diterpenoid-alkaloids-from-consolida-regalis-s-f-gray-subsp-paniculata-host-soo-var-paniculata
#15
Filiz Mericl, Ali H Mericli, Haridutt K Desai, Ayhan Ulubelen, S William Pelletier
Seven diterpenoid alkaloids : delcosine(1), delsoline(2), gigactonine(3), lycoctonine(4), takaosamine(5), atisine(6) and hetisinone(7) have been isolated from the aerial parts of Consolida regalis subsp. paniculata var. paniculata. The presence of compounds 1,2,5,6 and 7 in this plant has not been previously reported.
August 16, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28809815/determination-of-amineptine-and-amprolium-hydrochlorides-through-ion-associates-with-cobalt-ii-thiocyanate
#16
Abou Attia Fekria M
Two new methods for the determination of amineptine (AMN) and amprolium (AMP) have been developed. The methods consist of extractin the ion - pairs between the drug and the inorganic complex [Co (SCN)₄](-2). The optimal experimental conditions of both methods including pH, concentration of Co (II) and tlxocyanate ions, and the organic solvents were studied. The optimum pH was found to be 3.9, nitrobenzene proved to be the most suitable solvent, giving quantitative extraction for the two drugs. The two drugs can be determined in the organic phase spectrophotometrically at 625 nm showing Sandell sensitivities of 0...
August 15, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28758958/evaluation-of-antioxidant-activity-and-growth-control-properties-of-nonoscale-structure-produced-from-aloe-vera-var-littoralis-extract-on-clinical-isolates-of-salmonella
#17
Reza Ranjbar, Mohammad Arjomandzadegan, Hossein Hosseiny
The aim of the study was to examine antibacterial properties of microemulsion structure produced from Aloe vera var. littoralis extract as a new tool of nanoscale drug-like materials. Aloe vera var. littoralis (A. littoralis) extract was prepared by distillation method. A nonocarrier structure in the microemulsion system was prepared from the extract. Serial concentrations were prepared from 8 mg/mL extract and the nonocarrier containing 0.1 mg/mL pure extract and were evaluated by a disk diffusion method for 35 Salmonella clinical isolates...
July 31, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28753970/reversed-phase-uhplc-enantiomeric-separation-of-rasagiline-salts-using-a-chiralpak-%C3%A2-agp-column
#18
Nagarajan Balaji, Sayeeda Sultana
We report the first rapid ultra-high performance liquid chromatographic (UHPLC) enantiomeric reversed-phase separation of rasagiline mesylate and its tartrate salts using a Chiralpak(®) AGP column (50 mm × 2.1 mm, 5 μm) as a stationary phase. This method was developed as an alternative to the usage of previously reported normal-phase chiral LC columns for isomer separation. Our method is based on an isocratic approach using a mixture of ammonium acetate and isopropyl alcohol (90:10, v/v) as the mobile phase (0...
July 19, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28671634/regressions-of-breast-carcinoma-syngraft-following-treatment-with-piperine-in-combination-with-thymoquinone
#19
Wamidh H Talib
Thymoquinone (TQ) and piperine, the active ingredients in cumin (Nigella sativa) and black pepper (Piper longum), respectively, exhibit various bioactivities including anticancer effects. The aim of the present study is to investigate the antineoplastic activity of a combination of TQ and piperine against breast cancer implanted in mice. The antiproliferative effects of TQ, piperine, and a combination of both agents were tested against mouse epithelial breast cancer cell line (EMT6/P) using MTT assay. The isobolographic method was used to calculate the combination index (CI)...
July 3, 2017: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/28653975/development-of-rp-hplc-stability-indicating-method-for-degradation-products-of-linagliptin-in-presence-of-metformin-hcl-by-applying-2-level-factorial-design-and-identification-of-impurity-vii-viii-and-ix-and-synthesis-of-impurity-vii
#20
Sushant B Jadhav, P Sunil Reddy, Kalyanaraman L Narayanan, Popatrao N Bhosale
The novel reverse phase-high performance liquid chromatography (RP-HPLC), stability indicating method was developed for determination of linagliptin (LGP) and its related substances in linagliptin and metformin HCl (MET HCl) tablets by implementing design of experiment to understand the critical method parameters and their relation with critical method attributes; to ensure robustness of the method. The separation of nine specified impurities was achieved with a Zorbax SB-Aq 250 × 4.6 mm, 5 µm column, using gradient elution and a detector wavelength of 225 nm, and validated in accordance with International Conference on Harmonization (ICH) guidelines and found to be accurate, precise, reproducible, robust, and specific...
June 27, 2017: Scientia Pharmaceutica
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