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Scientia Pharmaceutica

Ornin Srihakulung, Ryo Maezono, Pisanu Toochinda, Waree Kongprawechnon, Apichart Intarapanich, And Luckhana Lawtrakul
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...
May 15, 2018: Scientia Pharmaceutica
Triana Hertiani, Agustinus Yuswanto, Sylvia Utami Tunjung Pratiwi, Harlyanti Muthma'innah Mashar
The essential oil of Massoia ( Massoia aromatica 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 Phyllanthus niruri extract that was administered as the positive control at the dose of 0...
May 10, 2018: Scientia Pharmaceutica
Supandi Supandi, Yahdiana Harahap, Harmita Harmita, Rizka Andalusia
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...
April 25, 2018: Scientia Pharmaceutica
Olga Vorobyova, Olga Deryabina, Darina Malygina, Nadezhda Plotnikova, Anna Solovyeva, Kseniya Belyaeva, Nina Melnikova
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...
April 23, 2018: Scientia Pharmaceutica
Behzad Sharif Makhmal Zadeh, Hassan Niro, Fakher Rahim, Golbarg Esfahani
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...
April 20, 2018: Scientia Pharmaceutica
Manijeh Kahbazi, Hossein Sarmadian, Azam Ahmadi, Farshideh Didgar, Maryam Sadrnia, Toktam Poolad, Mohammad Arjomandzadegan
In clinical isolates of Mycobacterium tuberculosis (MTB), resistance to pyrazinamide occurs by mutations in any positions of the pncA gene (NC_000962.3) especially in nucleotides 359 and 374. In this study we examined the pncA 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 pncA gene...
April 16, 2018: Scientia Pharmaceutica
Mabrouka Bouacha, Hayette Ayed, Nedjoud Grara
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 in vitro 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...
April 13, 2018: Scientia Pharmaceutica
Ratna Annisa Utami, Aunillah Hakiki, Sukmadjaja Asyarie, Debbie Soefie Retnoningrum
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 Citrus limon (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...
April 10, 2018: Scientia Pharmaceutica
Igor V Ukrainets, Lyudmila V Sidorenko, Mykola Y Golik, Igor M Chernenok, Lina A Grinevich, Alexandra A Davidenko
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- ij ]quinoline-6-carboxanilides was carried out by amidation of ethyl-7-hydroxy-5-oxo-2,3-dihydro-1 H ,5 H -pyrido[3,2,1- ij ]quinoline-6-carboxylate with aniline, aminophenols and O -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 H ,5 H -pyrido[3,2,1- ij ]quinolin-5-one...
April 9, 2018: Scientia Pharmaceutica
Muamer Dizdar, Danijela Vidic, Franc Požgan, Bogdan Štefane, Milka Maksimović
Phenolic acids and their derivatives found in nature are well-known for their potential biological activity. In this study, two amides derived from trans -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 Electrophorus electricus 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...
April 4, 2018: Scientia Pharmaceutica
Kandhasamy Sowndhararajan, Minju Kim, Ponnuvel Deepa, Se Jin Park, Songmun Kim
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...
March 26, 2018: 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 ( P app ) 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 ( pf DHFR), 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 pf DHFR 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
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