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Scientia Pharmaceutica

Rubén Vilcacundo, Pilar Méndez, Walter Reyes, Herman Romero, Adelita Pinto, Wilman Carrillo
The aim of this study was to increase the antibacterial spectrum of modified hen egg white lysozyme (HEWL) with thermal and chemical treatments against Gram-negative bacteria. The antibacterial activity of heat-denatured HEWL and chemical denatured HEWL against Gram-negative and Gram-positive bacteria was evaluated in 15 h of incubation tests. HEWL was denatured by heating at pH 6.0 and pH 7.0 and chemical denaturing was carried out for 1.0, 1.5, 2.0, and 4.0 h with DL-Dithiothreitol (DTT). HEWL modified by thermal and chemical treatments was characterized using the sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) electrophoresis method...
October 30, 2018: Scientia Pharmaceutica
Anna Kryshchyshyn, Danylo Kaminskyy, Igor Nektegayev, Philippe Grellier, Roman Lesyk
Recently, thiazolidinone derivatives have been widely studied as antiparasitic agents. Previous investigations showed that fused 4-thiazolidinone derivatives (especially thiopyranothiazoles) retain pharmacological activity of their synthetic precursors-simple 5-ene-4-thiazolidinones. A series of isothiochromeno[4a,4- d ][1,3] thiazoles was investigated in an in vitro assay towards bloodstream forms of Trypanosoma brucei brucei . All compounds inhibited parasite growth at concentrations in the micromolar range...
October 19, 2018: Scientia Pharmaceutica
Tatiana Stupina, Anastasia Balakina, Tatiana Kondrat'eva, Galina Kozub, Natalia Sanina, Alexei Terent'ev
NO donating iron nitrosyl complex with 2-aminothiophenyl ligand ( 2-AmPh complex) was studied for its ability to cause cell death and affect nuclear factor kappa B (NF-κB) signaling. The complex inhibited viability of HeLa cells and induced cell death that was accompanied by loss of mitochondrial membrane potential and characteristic for apoptosis phosphatidylserine externalization. At IC50, 2-AmPh caused decrease in nuclear content of NF-κB p65 polypeptide and mRNA expression of NF-κB target genes encoding interleukin-8 and anti-apoptotic protein BIRC3...
October 11, 2018: Scientia Pharmaceutica
Fadi G Saqallah, Wafaa M Hamed, Wamidh H Talib
Mediterranean-native perennial plant Antirrhinum majus was scrutinized in this study for its antioxidant activity and its total phenolic content in order to test for the plant's wound-healing capability. The traditional uses of this plant to treat gum scurvy, various tumors, ulcers, and hemorrhoids were the main idea behind this study. Leaves and flowers of the A. majus were extracted by maceration. Pilot qualitative phytochemical tests were made to check the presence of various secondary metabolites. Quantitatively, the flowers' macerate indicated superlative results regarding antioxidant activity and total phenolic content...
October 7, 2018: Scientia Pharmaceutica
Mohamed M Salama, Manal M Nomir, Maryan W Fahmi, Amal M El-Gayar, Mamdouh M El-Shishtawy
Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related mortality worldwide. In an attempt to understand some potential mechanisms of persistence and oncogenicity of Hepatitis C virus (HCV)-related HCC, microfibrillar-associated protein 4 (MFAP4), fibrotic indices and oxidative status biomarkers were assessed in the sera of 50 patients with HCV-associated HCC, 25 patients with HCV-related liver cirrhosis and 15 healthy individuals. Serum oxidized Coenzyme Q10 (CoQ10) and malondialdehyde showed significant elevation in HCC patients compared to the control group ( p < 0...
September 30, 2018: Scientia Pharmaceutica
Jürgen Krauß, Franz Bracher
Pharmacokinetic enhancers (boosters) are compounds used in combination with a primary therapeutic agent (drug) and are not used for their direct effects on the disease but because they enhance or restore the activity of the primary agent. Hence, in certain cases, they represent an indispensable escort for enzyme-labile drugs. Pharmacokinetic enhancers can exert their activity on different ways. In the most common case, they inhibit enzymes such as human cytochrome P450 enzymes in the liver or other organs and, thereby, block or reduce undesired metabolism and inactivation of the primary drug...
September 27, 2018: Scientia Pharmaceutica
Oludotun Adebayo Phillips, Edet Ekpenyong Udo, Roselyn Jennifer D'silva
Bacterial resistance towards the existing class of antibacterial drugs continues to increase, posing a significant threat to the clinical usefulness of these drugs. These increasing and alarming rates of antibacterial resistance development and the decline in the number of new antibacterial drugs' approval continue to serve as a major impetus for research into the discovery and development of new antibacterial agents. We synthesized a series of d -/ l -alaninyl substituted triazolyl oxazolidinone derivatives and evaluated their antibacterial activity against selected standard Gram-positive and Gram-negative bacterial strains...
September 26, 2018: Scientia Pharmaceutica
Amirah Adlia, Ilham Tomagola, Sophi Damayanti, Ardyanto Mulya, Heni Rachmawati
Conjugation of curcumin and gold with green chemistry is an approach to improve the effectiveness of curcumin as anti-fibrosis. In this work, curcumin and gold were conjugated to deliver curcumin to the liver. Curcumin-gold nanoparticles (cAuNPs) were prepared by varying curcumin pH and concentration. The successful of cAuNPs formation were identified by using UV-visible and FTIR spectrophotometers. The particle size and morphology were analyzed using particle size analyzer and cryo-TEM respectively. In vitro antioxidant assay was performed to determine the curcumin activity after conjugation...
September 21, 2018: Scientia Pharmaceutica
Claudia Juliano, Mauro Marchetti, Maria Luisa Pisu, Marianna Usai
The in vitro antibacterial activity of some essential oils from Sardinian flora, both alone and in combination with chitosan, was investigated against a strain of Cutibacterium acnes , a bacterium involved in pathogenesis of acne. The composition of the essential oils was determined by gas chromatography and gas chromatography/mass spectrometry. The results of this investigation demonstrated that some of the oils examined, characterised by different chemical profiles, possessed some activity against C. acnes ...
September 13, 2018: Scientia Pharmaceutica
Chutima Jantarat, Pornpak Sirathanarun, Somruedee Boonmee, Wanida Meechoosin, Husna Wangpittaya
Curcumin is a naturally occurring substance with various pharmacological activities. It has not been developed as a drug because of its low bioavailability due to its low solubility and absorption. Piperine is a natural enhancer that is popularly used to increase the absorption of curcumin in oral applications; however, it has not been applied for transdermal curcumin delivery. This study aims to develop a transdermal curcumin delivery system using piperine as a skin permeation enhancer in the form of composite double-layer membrane; the upper layer consisted of curcumin and the lower layer consisted of piperine...
September 13, 2018: Scientia Pharmaceutica
Marsella Widjaja, Jefri Gan, Joseph Sunder Raj Talpaneni, Raymond Rubianto Tjandrawinata
Eudragit® L100 is a commonly used polymer in a coating layer of modified-release drug formulation to prevent drug release in the stomach. The amount of Eudragit® L100 in the formula determines the dissolution profile of drug at its release medium. Hence, its quantification in reference product will facilitate the formulation of a bioequivalent drug product. Some analytical methods including size-exclusion chromatography (SEC) have been reported for characterization of Eudragit® L100 either as single component or its conjugate with the enzyme, but none for its quantification in drug formulation...
September 12, 2018: Scientia Pharmaceutica
Bhagavathi Sundaram Sivamaruthi, Periyanaina Kesika, Chaiyavat Chaiyasut
Fermented foods are known for several health benefits, and they are generally used among the Asian people. Microorganisms involved in the fermentation process are most responsible for the final quality of the food. Traditional fermented (spontaneous fermentation) foods are a versatile source of bioactive molecules and bioactive microbes. Several reports are available regarding the isolation and characterization of potent strains from traditional fermented foods. A collection of information for easy literature analysis of bioactive microbes derived from Thai fermented food is not yet available...
September 11, 2018: Scientia Pharmaceutica
Nada A Al-Hasawi, Sanaa A Amine, Ladislav Novotny
Cadmium (Cd) is a toxic heavy metal occurring in the environment as an industrial pollutant. The systematic accumulation of Cd in the human body may lead to major health problems. Quercetin (QE) is a natural flavonoid widely distributed in plants and is a part of human diet. Many studies have demonstrated the multiple benefits of QE to humans in protecting cells of our bodies. The aim of this study was to investigate the effect of QE and Cd on the proliferation of astrocytoma 1321N1 cells. Results indicated that the simultaneous exposure of the cells to 200 µM QE and 16 μM Cd significantly reduced cell viability to 6...
September 10, 2018: Scientia Pharmaceutica
Elsa Trinovita, Fadlina Chany Saputri, Abdul Mun'im
The presence of gamma-oryzanol in rice bran oil can be 10⁻20-fold higher than tocopherol and tocotrienol. Gamma-oryzanol has various pharmacological properties. The objective of this study was to evaluate the effectiveness of rice bran extract as a gastroprotective in reducing lesions in ethanol-induced acute gastric ulcer models in rat, using the ionic liquid-microwave-assisted extraction (IL-MAE) method. Rice bran extract was obtained using the IL-MAE method with ionic liquid (IL), 1-butyl-3-methylimidazolium tetrafluoroborate [BMIM]BF₄ (concentration 0...
September 7, 2018: Scientia Pharmaceutica
Urip Harahap, Hafiza Mitha Agustya, Dira Ummul Azizah, Syari Widia Alfiah
Picria fel-terrae extract has been investigated for its hepatoprotective activity. This current study was conducted to evaluate the subchronic toxic effect of Picria fel-terrae Lour. leaf extract. The subchronic toxicity of ethanol extract of P. fel-terrae leaf was evaluated by OECD (Organization for Economic Cooperation and Development) guidelines. The extract at doses of 125, 250, 500, 1000 mg/kg body weight (BW) were orally administered to the test animals for 90 days. Signs of toxicity and mortality were observed for 90 days and 118 days...
September 4, 2018: Scientia Pharmaceutica
Warintorn Ruksiriwanich, Jakkapan Sirithunyalug, Chiranan Khantham, Krot Leksomboon, Pensak Jantrawut
This study aimed to encapsulate Celastrus paniculatus seed oil (CPSO) in 2-hydroxypropyl-β-cyclodextrin (HPβCD) cavities and investigate their biological activity, physicochemical stability, and skin penetration by vertical Franz diffusion cells of the CPSO-HPβCD inclusion complex formulations. For biological activity studies-including 2,2-diphenyl-1-picryhydrazyl radical (DPPH) scavenging, metal ion chelating, and inhibition of lipid and tyrosinase inhibition activities-the CPSO-HPβCD inclusion complex exhibited lower inhibition activity than free CPSO...
September 1, 2018: Scientia Pharmaceutica
Md Shahinozzaman, Takahiro Ishii, Ryo Takano, Mohammad A Halim, Md Amzad Hossain, Shinkichi Tawata
Sea cucumbers have long been utilized in foods and Asiatic folk medicines for their nutritive and health benefits. Herein, three sea cucumber species were investigated and Holothuria atra showed the highest cytotoxicity among these. Next, a desulfated saponin, desulfated echinoside B (DEB), was purified from H. atra through bioassay-guided fractionation. LC-ESI-MS (Liquid chromatography-electrospray ionization mass spectrometry) analysis also showed H. atra to be a rich source of saponins. DEB showed cytotoxicity on cancer cells with IC50 values of 0...
August 31, 2018: Scientia Pharmaceutica
Igor V Ukrainets, Mykola Y Golik, Lyudmila V Sidorenko, Valentina I Korniyenko, Lina A Grinevich, Galina Sim, Olga V Kryvanych
In accordance with the principles of "me-too" technique, the preparative method for obtaining has been proposed, and the synthesis of a large series of new N -(arylalkyl)-6-hydroxy-2-methyl-4-oxo-2,4-dihydro-1 H -pyrrolo[3,2,1- ij ]quinoline-5-carboxamides as structurally close analogs of tricyclic pyrrolo- and pyridoquinoline diuretics has been carried out. All target compounds were obtained with high yields and purity by amidation of ethyl ester of the corresponding 2-methyl-pyrroloquinoline-5-carboxylic acid with arylalkylamines in boiling ethanol...
August 29, 2018: Scientia Pharmaceutica
Justyna Żwawiak, Lucjusz Zaprutko
Many interesting applications have been found for nitroimidazoles as therapeutic agents. Among others, some of these compounds can radiosensitize hypoxic tumor cells. The introduction of a second nitroimidazole ring to the molecule can improve the level of its pharmacological effect. The aim of this article is to overview the literature concerning active compounds that contain two nitroimidazole moieties in their structures.
July 25, 2018: 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
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