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Scientia Pharmaceutica

Igor V Ukrainets, Ganna M Hamza, Anna A Burian, Svitlana V Shishkina, Natali I Voloshchuk, Oxana V Malchenko
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 H -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 H -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 H -2λ⁶,1-benzothiazine...
March 8, 2018: Scientia Pharmaceutica
Chutima Jantarat, Pornpak Sirathanarun, Tatsanee Chuchue, Atthaphon Konpian, Gorawit Sukkua, Prutthicha Wongprasert
The herbal ball has been used as a Thai traditional medicine for relieving many diseases including acne. However, the application process of the herbal ball in practice is complicated and time consuming. The objective of this work was to utilize an herbal ball extract to formulate a gel to reach a more favorable use of the herbal ball for acne treatment. An herbal ball consisting of Andrographis paniculata , Centella asiatica , the Benchalokawichian remedy and the stem bark powder of Hesperethusa crenulata was prepared...
February 28, 2018: Scientia Pharmaceutica
Naser F Al-Tannak
Perindopril arginine and Indapamide hemihydrate in combination were proven to have a synergistic antihypertensive impact when compared with the use of each component alone. Therefore, a new Ultra-High Performance Liquid Chromatography coupled with Ultraviolet detector (UHPLC-UV) method has been developed and subsequently validated for simultaneous determination of the anti-hypertensive combination of Perindopril arginine and Indapamide hemihydrate. The separation of Perindopril arginine and Indapamide hemihydrate was achieved using a BEH C18 (1...
February 22, 2018: Scientia Pharmaceutica
Siska Siska, Abdul Mun Im, Anton Bahtiar, Franciscus D Suyatna
Apium graveolens (celery) is an edible and traditionally medicinal plant that is used worldwide, among others for the treatment of hypertension. Combining celery with antihypertensive drugs can affect the pharmacodynamics and pharmacokinetics of the latter drugs. The aim of the study is to assess the effects of administrating the celery extract on captopril pharmacokinetics. Sprague-Dawley strain rats were divided into two groups ( n = 6). Group I was given captopril (10 mg/kg Body Weight (BW)) orally, while Group II was pretreated with celery extract orally (40 mg/kg BW) an hour before administration of captopril...
February 16, 2018: Scientia Pharmaceutica
Jintawee Kicuntod, Kanyani Sangpheak, Monika Mueller, Peter Wolschann, Helmut Viernstein, Saeko Yanaka, Koichi Kato, Warinthorn Chavasiri, Piamsook Pongsawasdi, Nawee Kungwan, Thanyada Rungrotmongkol
Pinostrobin (PNS) belongs to the flavanone subclass of flavonoids which shows several biological activities such as anti-inflammatory, anti-cancerogenic, anti-viral and anti-oxidative effects. Similar to other flavonoids, PNS has a quite low water solubility. The purpose of this work is to improve the solubility and the biological activities of PNS by forming inclusion complexes with β-cyclodextrin (βCD) and its derivatives, heptakis-(2,6-di-O-methyl)-β-cyclodextrin (2,6-DMβCD) and (2-hydroxypropyl)-β-cyclodextrin (HPβCD)...
January 30, 2018: Scientia Pharmaceutica
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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