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Scientia Pharmaceutica

Rinrada Chotigarpa, Kannika Na Lampang, Surachai Pikulkaew, Siriporn Okonogi, Kittisak Ajariyakhajorn, Raktham Mektrirat
Staphylococcus aureus and S. epidermidis are the major teat skin bacteria and lead to severe bovine mastitis. Teat antiseptic is an important tool for controlling intramammary infection. The antibacterial activity of lactic acid (LA) against one reference strain of S. aureus ATCC 25923 and two field strains including S. aureus and S. epidermidis was investigated using the broth microdilution method. Its minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were 0.5% for strains belonging to both species...
July 16, 2018: Scientia Pharmaceutica
Olga Shyyka, Nazariy Pokhodylo, Nataliya Finiuk, Vasyl Matiychuk, Rostyslav Stoika, Mykola Obushak
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...
July 16, 2018: Scientia Pharmaceutica
Michele Sanford Rangel Parente, Feliphy Rodrigues Custódio, Nayara Araújo Cardoso, Márcia Jordana Araújo Lima, Tiago Sousa de Melo, Maria Isabel Linhares, Rafaelly Maria Pinheiro Siqueira, Aristides Ávilo do Nascimento, Francisco Eduardo Aragão Catunda Júnior, Carla Thiciane Vasconcelos de Melo
Depression is a common disease affecting more than 300 million people worldwide. Since Lippia sidoides has shown central nervous system effects in previous works, we aimed to investigate the effect of L. sidoides 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 L. sidoides essential oil (100 and 200 mg/kg), or thymol (25 and 50 mg/kg) or fluoxetine (35 mg/kg) by gavage...
June 27, 2018: Scientia Pharmaceutica
Anna Kryshchyshyn, Olexandra Roman, Andrii Lozynskyi, Roman Lesyk
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 hetero -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...
June 14, 2018: Scientia Pharmaceutica
Pekik Wiji Prasetyaningrum, Anton Bahtiar, Hayun Hayun
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, 13 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 (LC50 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 (IC50 value 40...
June 7, 2018: Scientia Pharmaceutica
Jillian Jin Lyn Heng, Jia Hao Teng, Muniyandy Saravanan, Janarthanan Pushpamalar
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% w/w , respectively...
June 5, 2018: Scientia Pharmaceutica
Yori Yuliandra, Erizal Zaini, Syofyan Syofyan, Wenny Pratiwi, Lidiya Novita Putri, Yuti Sahra Pratiwi, Helmi Arifin
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)...
June 4, 2018: Scientia Pharmaceutica
Bhagavathi Sundaram Sivamaruthi, Periyanaina Kesika, Chaiyavat Chaiyasut
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...
May 31, 2018: Scientia Pharmaceutica
Igor V Ukrainets, Anna A Burian, Vyacheslav N Baumer, Svitlana V Shishkina, Lyudmila V Sidorenko, Igor A Tugaibei, Natali I Voloshchuk, Pavlo S Bondarenko
Continuing the search for new potential analgesics among the derivatives of 4-methyl-2,2-dioxo-1 H -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 H -2λ⁶,1-benzothiazine-3-carboxylate (major) and its 1-ethyl-substituted analog (minor)...
May 30, 2018: 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
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