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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
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
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