Ellagic acid: A potent glyoxalase-I inhibitor with a unique scaffold.
In this study, a set of structurally diverse polyphenolic natural compounds were investigated as potential GLO-I inhibitors. Ellagic acid was found, computationally and experimentally, to be the most potent GLO-I inhibitor among the tested compounds which showed an IC50 of 0.71 mmol L-1. Its binding to the GLO-I active site seemed to be mainly driven by ionic interaction via its ionized hydroxyl groups with the central Zn ion and Lys156, along with other numerous hydrogen bonding and hydrophobic interactions. Due to its unique and rigid skeleton, it can be utilized to search for other novel and potent GLO-I inhibitors via ...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Al-Shar'i NA, Al-Balas QA, Hassan MA, El-Elimat TM, Aljabal GA, Almaaytah AM Tags: Acta Pharm Source Type: research

In silico data mining of large-scale databases for the virtual screening of human interleukin-2 inhibitors.
This study was carried out to set up an effective virtual screening (VS) pipeline for IL-2. Four docking/scoring approaches (FRED, MOE, GOLD and Surflex-Dock) were compared in the re-docking process to test their performance in producing correct binding modes of IL-2 inhibitors. Surflex-Dock and FRED were the best in predicting the native pose in its top-ranking position. Shapegauss and CGO scoring functions identified the known inhibitors of IL-2 in top 1, 5 and 10 % of library and differentiated binders from non-binders efficiently with average AUC of> 0.9 and> 0.7, resp. The applied docking protocol served as a ba...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Halim SA, Zaheer-Ul-Haq , Khan A, Al-Rawahi A, Al-Harrasi A Tags: Acta Pharm Source Type: research

In vitro antioxidant and antityrosinase activities of Manilkara kauki.
This study investigated the total phenolic and flavonoid contents, and antioxidant and antityrosinase activities in different parts of M. kauki (fruits, leaves, seeds, stem barks and woods) and in fractions of stem barks. The total phenolic and flavonoid contents of the methanol and aqueous crude extracts of different parts of M. kauki ranged from 10.87 to 176.56 mg GAE (gallic acid equivalents) per gram of crude extract and 14.33 to 821.67 mg QE (quercetin equivalents) per gram of crude extract, resp. Leaves and stem barks exhibited higher total phenolic and flavonoid contents and antioxidant and anti-tyrosinase activitie...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Srisupap S, Chaicharoenpong C Tags: Acta Pharm Source Type: research

A cost-effective and sensitive TLC-densitometric identification of meloxicam.
Abstract The influence of different chromatographic conditions and the process of spot visualization on determining the limit of detection as well as quantification (LOD and LOQ) of meloxicam by TLC-densitometric technique was estimated. Of all chromatographic conditions tested, the lowest limiting values, thus the best sensitivity, in the NP-TLC system was achieved on silica gel 60F254 and neutral aluminum oxide plates developed with the mobile phase consisting of ethyl acetate/toluene/n-butylamine (2:2:1, V/V/V). In the case of the RP-TLC method, a mixture of methanol/water (8:2, V/V) enabled densitometric detec...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Parys W, Pyka-Pająk A, Dołowy M Tags: Acta Pharm Source Type: research

Investigation of design space for freeze-drying injectable ibuprofen using response surface methodology.
This study explores the use of a statistical model to build a design space for freeze-drying two formulations with ibuprofen. A 2 × 3 factorial experimental design was used to evaluate independent variables (filling volume and annealing time) and responses as residual moisture content, specific surface area and reconstitution time. A statistical model and response surface plots were generated to define the interactions among the selected variables. The models constructed for both formulations suggest that 1 mL of filled volume and no annealing should be used to achieve optimal residual moisture content, specific surf...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Preskar M, Videc D, Vrečer F, Gašperlin M Tags: Acta Pharm Source Type: research

Protective effects of olive oil phenolics oleuropein and hydroxytyrosol against hydrogen peroxide-induced DNA damage in human peripheral lymphocytes.
This study investigates antioxidant capacity and protective effects of phenolic compounds oleuropein (OLP) and hydroxytyrosol (HT), present in olive oil and olive leaves, against H2O2-induced DNA damage in human peripheral lymphocytes. Antioxidant potency was determined using the measurement of radical-scavenging activity (ABTS∙+ assay), ferric reducing power (FRAP assay) and cupric reducing antioxidant capacity (CUPRAC assay). Both substances were found to be potent antioxidant agents due to their free radical-scavenging activities. Antigenotoxic effects of oleuropein and hydroxytyrosol against H2O2-induced damage in hu...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Zorić N, Kopjar N, Rodriguez JV, Tomić S, Kosalec I Tags: Acta Pharm Source Type: research

The use of Hericium erinaceus and Trametes versicolor extracts in supportive treatment in oncology.
Abstract Substances available in nature with potential therapeutic effects are the subject of research that raises tremendous hopes for new challenges in medicine. Fungi are the most common organisms in the ecosystem and the most interesting in this respect. This review discusses two species of edible fungi, used for centuries in Eastern natural medicine, with the best-documented effect - Hericium erinaceus (He) and Trametes versicolor (Tv). The results of in vivo and in vitro studies conducted on mice and human cell lines demonstrate immunomodulatory, potentially, anticancer, anti-inflammatory and neuroregenerati...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Winder M, Bulska-Będkowska W, Chudek J Tags: Acta Pharm Source Type: research

Improved 11 α-hydroxycanrenone production by modification of cytochrome P450 monooxygenase gene in Aspergillus ochraceus.
Improved 11α-hydroxycanrenone production by modification of cytochrome P450 monooxygenase gene in Aspergillus ochraceus. Acta Pharm. 2021 Mar 01;71(1):99-114 Authors: Li Q, Shi L, Liu Y, Guan S, Zhang S, Cai B, Rong S Abstract Eplerenone is a drug that protects the cardiovascular system. 11α-Hydroxycanrenone is a key intermediate in eplerenone synthesis. We found that although the cytochrome P450 (CYP) enzyme system in Aspergillus ochraceus strain MF018 could catalyse the conversion of canrenone to 11α-hydroxycanrenone, its biocatalytic efficiency is low. To improve the efficiency of...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Li Q, Shi L, Liu Y, Guan S, Zhang S, Cai B, Rong S Tags: Acta Pharm Source Type: research

The controversies of parabens - an overview nowadays.
Abstract Effects of paraben toxicity, i.e., endocrine-disruption properties, are in the focus of researchers for decades, but still - they are a hot subject of debate. Parabens are aliphatic esters of p-hydroxybenzoic acid, which are widely used as antimicrobial agents for the preservation of cosmetics, pharmaceuticals and foods. Mostly used parabens are methyl-, ethyl-, propyl- and butylparaben. Although the toxicity of parabens is reported in animals and in in vitro studies, it cannot be taken for granted when discussing hazards for human health due to an unrealistic exposure -safety profile. Many studies have d...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Petric Z, Ružić J, Žuntar I Tags: Acta Pharm Source Type: research

An analytical "quality by design" approach in RP-HPLC method development and validation for reliable and rapid estimation of irinotecan in an injectable formulation.
The objective of the present study was to develop a robust, simple, economical and sensitive HPLC-UV method using the "quality-by-design" approach for the estimation of irinotecan (IRI) in marketed formulations. RP-HPLC method was developed by applying Box-Behnken design with Hyper-Clone (Phenomenex®) C18 column (250 × 4.6 mm id, particle size 5 µm, ODS 130 Å) as a stationary phase. Acetonitrile and 20 mmol L-1 potassium phosphate buffer (pH 2.5) containing 0.1 % triethylamine in a ratio of 45:55 % (V/V) was used as a mobile phase. The sample was injected in a volume of 20 µL into the ...
Source: Acta Pharmaceutica - July 24, 2020 Category: Drugs & Pharmacology Authors: Bhaskaran NA, Kumar L, Reddy MS, Pai GK Tags: Acta Pharm Source Type: research

Process analytical technology tools for process control of roller compaction in solid pharmaceuticals manufacturing.
This article presents an overview of using process analytical technology in monitoring the roller compaction process. In the past two decades, near-infrared spectroscopy, near-infrared spectroscopy coupled with chemical imaging, microwave resonance technology, thermal effusivity and various particle imaging techniques have been used for developing at-, off-, on- and in-line models for predicting critical quality attributes of ribbons and subsequent granules and tablets. The common goal of all these methods is improved process understanding and process control, and thus improved production of high-quality products. This art...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Vovko AD, Vrečer F Tags: Acta Pharm Source Type: research

Piperazine derivatives as dangerous abused compounds.
Abstract Piperazine derivatives are a group of compounds with a psychostimulant effect. They are an alternative to illegal drugs. They are being searched for recreational use due to their psychoactive and hallucinogenic effects. The high popularity of these compounds can be noticed all over the world due to easy purchase, lack of legal regulations and incorrect assessment of the safety of use. The recreational use of piperazine derivatives can often result in chronic and acute health problems and additionally with unpredictable remote effects. It is also common to take mixtures of psychoactive compounds. This hind...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Welz A, Koba M Tags: Acta Pharm Source Type: research

Anthelmintic activity of praziquantel and Spilanthes acmella extract on an intestinal cestode parasite.
Abstract Spilanthes acmella Murr., popularised as toothache plant, is a well-known culinary and medicinal plant for different purposes, but its use as an anthelmintic is apparently exclusive to the Mizo people of India and Myanmar. A chloroform extract of Spilanthes acmella Murr. was analysed in a single quadrupole GC-MS system, from which it was found that the major compound was an alkylamide, N-isobutyl-(2E,4Z,8Z,10E)-dodecatetraenamide. A comparative study was performed on the anthelmintic activity of the plant extract and praziquantel (PZQ) against an intestinal cestode, Raillietina echinobothrida. In terms of...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Lalthanpuii PB, Zokimi Z, Lalchhandama K Tags: Acta Pharm Source Type: research

HPLC method development for fampridine using Analytical Quality by Design approach.
;cs-Deák B, Székely-Szentmiklósi B Abstract Offering a systematic and multivariate analysis of the analytical procedure, development and validation of HPLC methods using Quality by Design approach are in the limelight of current research trends. A new, experimental design-aided HPLC method for fampridine was developed and preliminarily validated according to current in-force international guidelines for linearity, accuracy, robustness and precision. The method offers a high throughput sample analysis, with an elution time of 2.9 minutes, and signal detection without excipient interference perf...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Kovács B, Boda F, Fülöp I, Székely-Szentmiklósi I, Kelemen ÉK, Kovács-Deák B, Székely-Szentmiklósi B Tags: Acta Pharm Source Type: research

Antitumor effect of a pyrazolone-based-complex [Cu(PMPP-SAL)(EtOH)] against murine melanoma B16 cell in vitro and in vivo.
In this study, the antitumor effect of [Cu(PMPP-SAL)(EtOH)] (PMPP-SAL = N-(1-phenyl-3-methyl-4-propenylidene-5-pyrazolone)- salicylidene hydrazide anion) in murine melanoma B16 cells in vitro and in vivo was investigated. The results showed that [Cu(PMPP-SAL)(EtOH)] inhibited the survival of B16 cells in vitro, and the IC50 value was superior to cisplatin (DDP) (p
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Abula A, Zhao J, Xu G, Li Y, Sun S Tags: Acta Pharm Source Type: research

Modulatory effects of perindopril on cisplatin-induced nephrotoxicity in mice: Implication of inflammatory cytokines and caspase-3 mediated apoptosis.
In conclusion, perindopril may be safely used with cisplatin in mice since it ameliorated cisplatin-induced histopathological changes, inflammation and apoptosis without affecting renal biomarkers or oxidative stress. PMID: 32412432 [PubMed - as supplied by publisher] (Source: Acta Pharmaceutica)
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Aljuhani N, Ismail RS, El-Awady MS, Hassan MH Tags: Acta Pharm Source Type: research

Probing the release of the chronobiotic hormone melatonin from hybrid calcium alginate hydrogel beads.
Abstract A variety of commonly used hydrogels were utilized in the preparation of calcium alginate beads, which incorporate the chronobiotic hormone melatonin (MLT). The in vitro release of the hormone in aqueous media at pH 1.2 and 6.8 was probed in the conjunction with the swelling of the beads and their thermal degradation properties. It has been found that the release of MLT from the beads was reversibly proportional to the extent of their expansion, which depends on the molecular mass/viscosity of the biopolymers present in the beads; the higher the molecular mass/viscosity of the hydrogels the greater the be...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Vlachou M, Siamidi A, Goula E, Georgas P, Pippa N, Karalis V, Sentoukas T, Pispas S Tags: Acta Pharm Source Type: research

Synthesis and evaluation of bisulfate/mesylate-conjugated chlortetracycline with high solubility and bioavailability.
Abstract The aim of this work is to improve the solubility and bioavailability of chlortetracycline and the function of the immune response. Chlortetracycline bisulfate and chlortetracycline mesylate were successfully synthesized and characterized with several techniques, including spectroscopy, chromatography and mass spectrometry, which demonstrated that the C4-dimethylamino group of chlortetracycline can accept a proton from sulfuric acid and methanesulfonic acid to form the corresponding salts. In addition, chlortetracycline bisulfate and chlortetracycline mesylate were more soluble in water than chlortetracyc...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Liu D, Chen P, Yang X, Wang J Tags: Acta Pharm Source Type: research

Exploring the potential effect and mechanisms of protocatechuic acid on human hair follicle melanocytes.
This study aims to evaluate the effect of protocatechuic acid (PCA) on human hair follicle melanocytes (HFM). Normal primary HFM were isolated and cultured till logarithmic period of second passage, then treated with different concentrations of PCA (0.1-200 μmol L-1) to study the cell proliferation, melanin contents, tyrosinase activity and protein and mRNA expression of melanogenic genes (tyrosinase-related protein 1 (TRP-1), tyrosinase-related protein 2 (TRP-2), and microphthalmia-associated transcription factor (MITF)) in the cultured HFM. In addition, we have also measured the contents of superoxide dismutase (SOD) ...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Li B, Tan J, Zou B, Liu X, Yu Y Tags: Acta Pharm Source Type: research

Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents.
Kaplancikli ZA Abstract The synthesis of new N-(5-substituted-1,3,4-thiadiazol-2-yl)-2-[(5-(substituted amino)-1,3,4-thiadiazol-2-yl)thio]acetamide derivatives and investigation of their anticancer activities were the aims of this work. All the new compounds' structures were elucidated by elemental analyses, IR, 1H NMR, 13C NMR and MS spectral data. Anticancer activity studies of the compounds were evaluated against MCF-7 and A549 tumor cell lines. In addition, with the purpose of determining the selectivity of cytotoxic activities, the most active compound was screened against a noncancer NIH3T3 cell line (mouse...
Source: Acta Pharmaceutica - May 17, 2020 Category: Drugs & Pharmacology Authors: Çevik UA, Osmaniye D, Levent S, Sağlik BN, Çavuşoğlu BK, Karaduman AB, Özkay Y, Kaplancikli ZA Tags: Acta Pharm Source Type: research

Simultaneous spectrofluorometric analysis of tablets containing hydrochlorothiazide combined with timolol maleate or amiloride hydrochloride.
Abstract Green and sensitive spectrofluorometric methods have been developed and validated for the determination of timolol maleate (TML)/hydrochlorothiazide (HCT) and amiloride hydrochloride (AMH)/hydrochlorothiazide in tablets. The proposed spectrofluorometric procedures were found to be linear in the range of 4-12, 5-35 and 0.025-0.2 mg L-1 for HCT, TML and AMH, resp. The excitation and emission wavelengths for HCT, TML and AMH at room temperature were 270 and 375, 295 and 435, 330 and 415 nm, resp. The methods were validated with respect to ICH guidelines. The AMH showed higher sensitivity with lower values of...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Wedian F, Lataifeh A, Mohammed MS Tags: Acta Pharm Source Type: research

2-Amino-1,3,4-thiadiazoles as prospective agents in trypanosomiasis and other parasitoses.
Abstract Parasitic diseases are a serious public health problem affecting hundreds of millions of people worldwide. African trypanosomiasis, American trypanosomiasis, leishmaniasis, malaria and toxoplasmosis are the main parasitic infections caused by protozoan parasites with over one million deaths each year. Due to old medications and drug resistance worldwide, there is an urgent need for new antiparasitic drugs. 1,3,4-Thiadiazoles have been widely studied for medical applications. The chemical, physical and pharmacokinetic properties recommend 1,3,4-thiadiazole ring as a target in drug development. Many scienti...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Serban G Tags: Acta Pharm Source Type: research

Anticonvulsant valproic acid and other short-chain fatty acids as novel anticancer therapeutics: Possibilities and challenges.
Abstract Results from numerous pre-clinical studies suggest that a well known anticonvulsant drug valproic acid (VPA) and other short-chain fatty acids (SCFAs) cause significant inhibition of cancer cell proliferation by modulating multiple signaling pathways. First of all, they act as histone deacetylase (HDAC) inhibitors (HDIs), being involved in the epigenetic regulation of gene expression. Afterward, VPA is shown to induce apoptosis and cell differentiation, as well as regulate Notch signaling. Moreover, it up-regulates the expression of certain G protein-coupled receptors (GPCRs), which are involved in variou...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Lipska K, Gumieniczek A, Filip AA Tags: Acta Pharm Source Type: research

Stability study of thymoquinone, carvacrol and thymol using HPLC-UV and LC-ESI-MS.
Abstract The aim of this study was to investigate the stability of three major antioxidants of Nigella sativa: thymoquinone (TQ), carvacrol (CR) and thymol (THY), under different stress conditions using HPLC and LC-MS/MS. Forced degradation for each compound was performed under different conditions, including oxidation, hydrolysis, photolysis and thermal decomposition. The results showed that both CR and THY were stable under the studied conditions, whereas TQ was not affected by acidic, basic and oxidative forced conditions but the effect of light and heat was significant. The degradation products of TQ were furt...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Soliman RM, Abdel Salam RA, Eid BG, Khayyat A, Neamatallah T, Mesbah MK, Hadad GM Tags: Acta Pharm Source Type: research

Preparation, characterization, and in vivo pharmacokinetics of thermosensitive in situ nasal gel of donepezil hydrochloride.
Abstract Donepezil hydrochloride thermosensitive in situ gel for nasal delivery was prepared by using Poloxamer 407 and Poloxamer 188 as thermoreversible polymers, hydroxypropyl-β-cyclodextrin and ethylparaben as permeation enhancer and preservative, respectively. The gelation temperature and time, pH value of the gel formulation were found to meet the requirements for nasal administration. The in vitro erosion and in vitro release tests exhibited obvious drug sustained release behavior. Meantime, main pharmacokinetic parameters such as tmax, cmax and AUC in plasma as well as in brain were significantly diffe...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Gu F, Fan H, Cong Z, Li S, Wang Y, Wu C Tags: Acta Pharm Source Type: research

Simultaneous determination of warfarin and 7-hydroxywarfarin in rat plasma by HPLC-FLD.
In this study, high-performance liquid chromatography with fluorescence detection (HPLC-FLD) has been used for the first time, for direct determination of warfarin and its major metabolite, 7-hydroxywarfarin, in rat plasma. The simple and sensitive method was developed using Fortis® reversed-phase diphenyl column (150 × 4.6 mm, 3 μm) and a mobile phase composed of phosphate buffer (25 mmol L-1)/methanol/acetonitrile (70:20:10, V/V/V), adjusted to pH 7.4, at a flow rate of 0.8 mL min-1. The diphenyl chemistry of the stationary phase provided a unique selectivity for separating the structurally related aromatic ...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Zayed A, Babaresh WM, Darweesh RS, El-Elimat T Tags: Acta Pharm Source Type: research

Differential effects of acute and chronic treatment with the flavonoid chrysin on anxiety-like behavior and Fos immunoreactivity in the lateral septal nucleus in rats.
E, Rodríguez-Landa JF Abstract The aim of this study was to compare the effects of acute (a single injection) and chronic (21 consecutive days) treatments with chrysin 2, 4, and 8 μmol kg-1 on anxiety-like behavior and Fos immunoreactivity in the lateral septum nucleus (LSN), a structure that is involved in the regulation of anxiety, in male Wistar rats. These effects were compared with the clinically effective anxiolytic diazepam 7 μmol kg-1. The results showed that acute, but not chronic treatment, with 4 μmol kg-1 chrysin exerted anxiolytic- and anti- depressant-like effects with these effects ...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Germán-Ponciano LJ, Puga-Olguín A, De Jesús Rovirosa-Hernández M, Caba M, Meza E, Rodríguez-Landa JF Tags: Acta Pharm Source Type: research

Curcumin inhibits migration and invasion of non-small cell lung cancer cells through up-regulation of miR-206 and suppression of PI3K/AKT/mTOR signaling pathway.
In conclusion, curcumin inhibited cell invasion and migration in NSCLC by elevating the expression of miR-206 which further suppressed the activation of the PI3K/AKT/mTOR pathway. PMID: 32074070 [PubMed - in process] (Source: Acta Pharmaceutica)
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Wang N, Feng T, Liu X, Liu Q Tags: Acta Pharm Source Type: research

Synthesis, in vitro safety and antioxidant activity of new pyrrole hydrazones.
Abstract Six new N-pyrrolylhydrazide hydrazones were synthesized under micro synthesis conditions, assuring about 59-93 % yield, low harmful emissions and reagent economy. The structures of the new compounds were elucidated by melting points, TLC characteristics, IR, 1H and 13C NMR spectral data followed by MS data. The purity of the obtained compounds was proven by the corresponding elemental analyses. "Lipinski's rule of five" parameters were applied for preliminary evaluation of the pharmacokinetic properties of the target molecules. The initial in vitro safety screening for cytotoxicity (on HepG2 cel...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Tzankova D, Vladimirova S, Aluani D, Yordanov Y, Peikova L, Georgieva M Tags: Acta Pharm Source Type: research

Advanced flow cell design for in vitro release testing of mucoadhesive buccal films.
;ek O Abstract Films for buccal application are a slowly emerging new platform for drug delivery. There remains a lack of analytical techniques for the determination of in vitro active pharmaceutical ingredient release. The aim here was to develop an alternative method to the commonly used United States Pharmacopoeia (USP) 2 method, based on the flow-through cell. This system extends the release time and enables more detailed sample discrimination according to formulation. It could be used as a tool for in vivo prediction of drug release rates from buccal film formulations. The flow cell contains two chambers sepa...
Source: Acta Pharmaceutica - February 21, 2020 Category: Drugs & Pharmacology Authors: Grilc B, Zdovc J, Planinšek O Tags: Acta Pharm Source Type: research

Design, synthesis and molecular docking of novel triazole derivatives as potential CoV helicase inhibitors.
Abstract Middle East respiratory syndrome coronavirus (MERS-CoV) had emerged and spread because of the worldwide travel and inefficient healthcare provided for the infected patients in several countries. Herein we investigated the anti-MERS-CoV activity of newly synthesized sixteen halogenated triazole compounds through the inhibition of helicase activity using the FRET assay. All new compounds underwent justification for their target structures via microanalytical and spectral data. SAR studies were performed. Biological results revealed that the most potent compounds were 4-(cyclopent-1-en-3-ylamino)-5-(2-(4-iod...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Zaher NH, Mostafa MI, Altaher AY Tags: Acta Pharm Source Type: research

Biopharmaceutical classification of desloratadine - not all drugs are classified the easy way.
Abstract The biopharmaceutical classification of drugs was designed as a basis for bio-waivers - a mechanism with the double ethical benefit of delivering new drug formulations to the market with less human testing and lower cost. However, many drugs defy simple classification because in vitro permeability and stability assessment can be challenging as shown in this study for desloratadine. Literature shows that desloratadine is highly soluble, while data on luminal stability and permeability are circumstantial. Combined with borderline bioavailability and not really known fraction of absorbed dose, desloratadine ...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Berginc K, Sibinovska N, Žakelj S, Trontelj J, Legen I Tags: Acta Pharm Source Type: research

SOX7 is involved in polyphyllin D-induced G0/G1 cell cycle arrest through down-regulation of cyclin D1.
Abstract The incidence of mortality of prostate cancer (PCa) has been an uptrend in recent years. Our previous study showed that the sex-determining region Y-box 7 (SOX7) was low-expressed and served as a tumor suppressor in PCa cells. Here, we describe the effects of polyphyllin D (PD) on proliferation and cell cycle modifications of PCa cells, and whether SOX7 participates in this process. PC-3 cells were cultured in complete medium containing PD for 12, 24, and 48 h. MTT assay was used to investigate the cytotoxic effects of PD. Cell cycle progression was analyzed using propidium iodide (PI) staining, and prote...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Zheng B, Wang G, Gao W, Wu Q, Zhu W, Weng G Tags: Acta Pharm Source Type: research

Curcumin-loaded nanostructured lipid carrier induced apoptosis in human HepG2 cells through activation of the DR5/caspase-mediated extrinsic apoptosis pathway.
This study aims to unveil the mechanisms underlying the pro-apoptotic effect of Cur-NLC on HepG2 cells. Evidence indicates that low expression of death receptors (DRs) on cancer cell membranes leads to attenuated apoptosis signaling. This study showed that Cur-NLC significantly increased total expression of DR5 protein while simultaneously upregulated cell membrane expression of DR5. Cur-NLC significantly increased caspase-8 and caspase-3 activities, accompanied by increased apoptosis. Furthermore, enhanced apoptosis was inhibited in the presence of a pan-caspase inhibitor, Z-VAD-FMK. Therefore, Cur-NLC induced activation ...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Wang F, Ye X, Zhai D, Dai W, Wu Y, Chen J, Chen W Tags: Acta Pharm Source Type: research

Maternal education, health profession and cigarette smoking are decisive factors for self-medication in children by parents.
The objective of this first national Montenegrin study was to assess the prevalence of and factors influencing SMCP among schoolchildren. Data were obtained from a national representative sample of 4496 schoolchildren aged 7-13 years (50.4 % boys). Parents/caregivers completed a questionnaire concerning their demographic characteristics, socio-economic and cultural status, as well as the self-medication (SM) of their children. The association between SMCP and parents' socio-economic, demographic or cultural status was assessed by logistic regression analyses. The prevalence rate of SMCP was 24.6 %. Univariate logistic regr...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Duborija-Kovacevic N, Martinovic M, Belojevic G, Lausevic D, Asanin B Tags: Acta Pharm Source Type: research

Application of targeted 2D planar chromatography in the control of ginkgolic acids in some herbal drugs and dietary supplements.
Abstract Two-step targeted 2D planar chromatographic method (2DTLC) was used in the determination of ginkgolic acids in pharmaceuticals and dietary supplements. The choice of the extraction method and the separation technique was guided by the formulation type (capsule, tablet, tincture) with expected low amounts of ginkgolic acids in the analyzed herbal samples. Separation of ginkgolic acids C15:1 and C17:1 on HPTLC RP18 WF254s was preceded by its separation from the sample matrix on TLC Si60 F254s. Mobile phases consisted of acetonitrile/water/formic acid (80:20:1, V/V/V) and n-heptane/ethyl acetate/formic acid ...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Migas P, Romańczuk A, Szumacher M, Krauze-Baranowska M Tags: Acta Pharm Source Type: research

Synthesis of bioactive quinazolin-4(3H)-one derivatives via microwave activation tailored by phase-transfer catalysis.
Abstract A series of nine new 2,3-disubstituted 4(3H)-quinazolin-4-one derivatives was furnished starting from the 2-propyl-4(3H)-quinazo-line-4-one (2). The reinvestigation of the key starting quinazolinone 2 was performed under microwave irradiation (MW) and solvent-free conditions. Combination of MW and phase-transfer catalysis using tetrabutylammonium benzoate (TBAB) as a novel neutral ionic catalyst was used for carrying out N-alkylation and condensation reactions of compound 2 as a simple, efficient and eco-friendly technique. The structure of the synthesized compounds was elucidated using different spectral...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: El-Badry YA, El-Hashash MA, Al-Ali K Tags: Acta Pharm Source Type: research

Potential antidiabetic and antioxidant activities of a heliangolide sesquiterpene lactone isolated from Helianthus annuus L. leaves.
This study evaluated the antioxidant and antidiabetic properties of a heliangolide sesquiterpene lactone isolated from Helianthus annuus L. leaves. The heliangolide sesquiterpene lactone was isolated through a combination of solvent-solvent partitioning, column chromatography, thin layer chromatography and high-performance liquid chromatography techniques. The antioxidant activity of the compound was evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and nitric oxide radical scavenging assays while the antidiabetic effects were investigated in alloxan-induced diabetic rats. The heliangolide derivative at the concentratio...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Onoja SO, Nnadi CO, Udem SC, Anaga AO Tags: Acta Pharm Source Type: research

Effects of new generation triptans - frovatriptan and almotriptan - on hemodynamic parameters in intact male and female rats.
Abstract The introduction of the second generation triptans in clinical and experimental practice was a major progress in the pharmacotherapy of migraine. Frovatriptan is a second generation triptan with strong 5-HT1B/1D serotonergic agonism and low 5-HT1A/7 receptor affinity, while almotriptan possesses not only the typical 5-HT1B/1D receptor agonist activity, but shows an affinity to the 5-HT1F receptor. The aim of our study was to assess the impact of frovatriptan and almotriptan on hemodynamics in male and female rats. We used a non-invasive "tail-cuff" method to measure the arterial blood pressure. ...
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Saracheva K, Hrischev P, Vasileva L, Topolov M, Nikolova J, Getova D Tags: Acta Pharm Source Type: research

Proton pump inhibitors enhance chemosensitivity, promote apoptosis, and suppress migration of breast cancer cells.
In conclusion, the addition of PPIs to the treatment regimen of breast cancer appears to be a promising strategy to potentiate the efficacy of chemotherapy and may suppress cancer metastasis. PMID: 31955147 [PubMed - in process] (Source: Acta Pharmaceutica)
Source: Acta Pharmaceutica - January 21, 2020 Category: Drugs & Pharmacology Authors: Ihraiz WG, Ahram M, Bardaweel SK Tags: Acta Pharm Source Type: research

Modified release of furosemide from Eudragits ® and poly(ethylene oxide)-based matrices and dry-coated tablets.
Modified release of furosemide from Eudragits® and poly(ethylene oxide)-based matrices and dry-coated tablets. Acta Pharm. 2020 Mar 01;70(1):49-61 Authors: Vlachou M, Geraniou E, Siamidi A Abstract Modified release of furosemide from tablet formulations is preferred by patients, because of physiological problems, acute diuresis being the most serious, compared to the forms designed for immediate release. With this in view, we aimed at achieving furosemide's longer gastric retention and waste minimization by preparing matrix and compression coated tablets incorporating different grades of Eudragit&...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Vlachou M, Geraniou E, Siamidi A Tags: Acta Pharm Source Type: research

TLC-densitometric analysis of allantoin in Symphytum officinale L. roots.
Abstract A TLC-densitometric method for determination of allantoin in Symphytum officinale root was developed. Densitometric quantification of allantoin was carried out on TLC Si60 plates with butanol-50 % methanol/formic acid, 66.5:33.2:0.3 (V/V/V) as developing solvent, at a wavelength of 190 nm. The method was preliminarily validated in terms of specificity, linearity, precision, limit of detection, limit of quantification, recovery and robustness. The results of TLC quantification were compared with HPLC analysis carried out on a HILIC Luna NH2 100A column, with mobile phase consisting of acetonitrile/water 80...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Kimel K, Zienkiewicz M, Sparzak-Stefanowska B, Krauze-Baranowska M Tags: Acta Pharm Source Type: research

Poly(3-hydroxybutyrate): Promising biomaterial for bone tissue engineering.
ez Ž Abstract Poly(3-hydroxybutyrate) is a natural polymer, produced by different bacteria, with good biocompatibility and biodegradability. Cardiovascular patches, scaffolds in tissue engineering and drug carriers are some of the possible biomedical applications of poly(3-hydroxybutyrate). In the past decade, many researchers examined the different physico-chemical modifications of poly(3-hydroxybutyrate) in order to improve its properties for use in the field of bone tissue engineering. Poly(3-hydroxybutyrate) composites with hydroxyapatite and bioglass are intensively tested with animal and human osteoblasts i...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Dariš B, Knez Ž Tags: Acta Pharm Source Type: research

Branched PLGA derivatives with tailored drug delivery properties.
Abstract Despite several shortcomings such as extreme hydrophobicity, low drug capacity, characteristic triphasic drug release pattern with a high burst effect, poly(lactic-co-glycolic acid derivatives are widely used in drug delivery. Most frequent attempts to improve their properties are blending with other polymers or synthesis of block copolymers. We introduce a new class of branched poly(lactic-co-glycolic acid) derivatives as promising biodegradable carriers for prolonged or targeted drug release systems, employed as thin adhesive films, solid dispersions, in situ forming implants or nanoparticles. A series ...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Snejdrova E, Podzimek S, Martiska J, Holas O, Dittrich M Tags: Acta Pharm Source Type: research

Development and validation of a UPLC-MS method for determination of atazanavir sulfate by the "analytical quality by design" approach.
Development and validation of a UPLC-MS method for determination of atazanavir sulfate by the "analytical quality by design" approach. Acta Pharm. 2020 Mar 01;70(1):17-33 Authors: Saha C, Gupta NV, Chandan RS Abstract A UPLC-MS method for the estimation of atazanavir sulfate was developed using the "analytical quality by design" approach. The critical chromatographic quality attributes identified were retention time, theoretical plates and peak tailing. The critical method parameters established were percent of organic modifier, flow rate and injection volume. Optimization performe...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Saha C, Gupta NV, Chandan RS Tags: Acta Pharm Source Type: research

Self-microemulsifying drug delivery systems of Moringa oleifera extract for enhanced dissolution of kaempferol and quercetin.
Abstract The aim of the present study was to develop self-microemulsifying drug delivery systems (SMEDDS) of the extract of Moringa oleifera, a herbal medicinal plant. Kaempferol and quercetin, the flavonoids present in the leaf extract of M. oleifera, were chosen as markers for quantification. The optimized formulation of SMEDDS consisted of propylene glycol dicaprylocaprate, polysorbate 80, and polyethylene glycol 400 (PEG 400) in a percentage ratio of 20:60:20 (m/m). SMEDDS emulsified immediately (within 20 s) after dilution in water, resulting in transparent microemulsions with a droplet size of 49 nm. SMEDDS ...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Sermkaew N, Plyduang T Tags: Acta Pharm Source Type: research

Sildenafil alters biogenic amines and increases oxidative damage in brain regions of insulin-hypoglycemic rats.
n HJ, Jiménez FT Abstract The aim of the present study was to determine the effect of sildenafil on dopamine, 5-hydroxyindol acetic acid (5-HIAA) and selected biomarkers of oxidative stress in the brain of hypoglycemic rats. The animals were treated intraperitoneally as follows: group 1 (control), saline solution; group 2, insulin (10 U per rat or 50 U kg-1); group 3, insulin + single dose of sildenafil (50 U kg-1 + 50 mg kg-1); group 4, insulin + three doses of sildenafil every 24 hours (50 U kg-1 + 50 mg kg-1). In groups 2, 3 and 4, insulin was administered every 24 hours for 10 days. Blood glucose was me...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Guzmán DC, Brizuela NO, Herrera MO, Peraza AV, Mejía GB, Olguín HJ, Jiménez FT Tags: Acta Pharm Source Type: research

Beneficial effects of baicalein on a model of allergic rhinitis.
This study assessed the in vivo protective effect of baicalein post-treatment in an ameliorating ovalbumin (OVA)-sensitized AR rat model. Baicalein attenuated histological alterations, aberrant tissue repair and inflammation after OVA-induced AR. Baicalein reduced the frequency of nasal/ear rubs and sneezes in rats, and inhibited generation of several inflammatory cytokines (TNF-α, IL-1β, and IL-6) in both blood and nasal lavage of rats. Infiltrations of eosinophils, lymphocyte, and neutrophils were decreased in baicalein-administered rats. Furthermore, baicalein inhibited the expression of STAT3 phosphorylation...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Liu T, Xu J, Wu Y, Li X, Ding D, Ma D, Yao M, Wei W, Zhang W, Wang S, Yao J, Li X Tags: Acta Pharm Source Type: research

Qualitative and quantitative HPLC-ELSD-ESI-MS analysis of steroidal saponins in fenugreek seed.
aranowska M Abstract Fenugreek seeds are known as a source of various compounds, the most common of which are steroidal saponins. However, despite the growing interest in this plant material as a healing agent, spice and dietary supplement ingredient, the composition of Polish fenugreek seeds remains unknown. Therefore, the steroidal saponin complex in the seeds of T. foenum-graecum cultivated in Poland was qualitatively and quantitatively analyzed by the HPLC-ELSDESI-MS method. Two C-18 columns connected in series were used for the first time in analysis of fenugreek saponins and ELS detector parameters were opti...
Source: Acta Pharmaceutica - November 6, 2019 Category: Drugs & Pharmacology Authors: Król-Kogus B, Głód D, Krauze-Baranowska M Tags: Acta Pharm Source Type: research

Efficacy and safety of local lysozyme treatment in patients with oral mucositis after chemotherapy and radiotherapy.
Abstract This observational clinical study was composed of two substudies: a non-comparative one (n = 166), testing only lysozyme-based compounds (LBCs), and a comparative substudy (n = 275), testing both LBCs and bicarbonate-based local compounds (BBCs) on the healing of oral mucositis during radio- or chemotherapy. The density of ulcerations has decreased significantly after the treatment with lysozyme in both substudies. The density of ulcerations in the radiotherapy group was lower in patients treated with LBCs compared to patients treated with BBCs (p
Source: Acta Pharmaceutica - October 23, 2019 Category: Drugs & Pharmacology Authors: Eminagić D, Lokvančić A, Hasanbegović B, Mekić-Abazović A, Avdičević A, Marijanović I, Janković SM, Kapo B Tags: Acta Pharm Source Type: research