735 results match your criteria Acta Pharmaceutica[Journal]

Norcantharidin induces G2/M arrest and apoptosis via activation of ERK and JNK, but not p38 signaling in human renal cell carcinoma ACHN cells.

Acta Pharm 2021 Jun;71(2):267-278

Laboratory of Renal Carcinoma, Ningbo Yinzhou No. 2 Hospital, Ningbo 315100, Zhejiang, P.R. China.

Renal cell carcinoma (RCC) is generally acknowledged as the most resistant primary malignancy unresponsive to conventional radiotherapy and chemotherapy treatments. Norcantharidin (NCTD), a therapeutic compound derived from medicinal plants, has been shown to trigger apoptosis, as well as antimetastatic and antioxidant activities in several tumor cells. However, NCTD's mechanism of antitumor activity in the RCC cell line remains unclear. Read More

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Piperine: Chemical, biological and nanotechnological applications.

Acta Pharm 2021 Jun;71(2):185-213

São Paulo State University (UNESP), School of Pharmaceutical Sciences, Department of Drugs and Medicines, Araraquara, São Paulo, Brazil.

Piperine (PIP) is an alkaloid present in several species of piper, mainly Piper nigrum Linn. and P. longum, among other species. Read More

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Polyethylene oxide matrix tablet swelling evolution: The impact of molecular mass and tablet composition.

Acta Pharm 2021 Jun;71(2):215-243

Department of Pharmaceutical Technology Faculty of Pharmacy, University of Ljubljana, 1000 Ljubljana, Slovenia.

This article describes the designing of matrix tablets composed of polyethylene oxides (PEOs) with relative molecular masses of 1 × 106, 2 × 106, and 4 × 106. Percolation thresholds were determined for all of the selected PEO formulations (18, 16, and 12 %, m/m), taking into consideration excipients and tablet surface area which significantly increased the percolation threshold. Moreover, the robustness of the gel layer in PEO matrix tablets was evaluated by magnetic resonance imaging under various mechanical stresses (no flow, 12 mL min-1, and 64 mL-1 of medium flow). Read More

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Ultraviolet B irradiation-induced keratinocyte senescence and impaired development of 3D epidermal reconstruct.

Acta Pharm 2021 Jun;71(2):293-303

Institute for Pharmacy, Freie Universität Berlin, 14195 Berlin Germany.

Ultraviolet B (UVB) induces morphological and functional changes of the skin. This study investigated the effect of UVB on keratinocyte senescence and the development of reconstructed human epidermis (RHE). Primary normal human keratinocytes (NHK) from juvenile foreskin were irradiated with UVB (30 mJ cm-2) and these effects were compared to NHK that underwent senescence in the late passage. Read More

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A new RP-HPLC method as an auxiliary tool for optimization of sample preparation procedures for tracing of PPCPs of different hydrophilicities.

Acta Pharm 2021 Jun;71(2):305-315

Universidad Autónoma de Nuevo León, Facultad de Medicina, Departamento de Química, Analítica, 64460, Francisco I. Madero s/n, Monterrey, Nuevo León, México.

Recently, pharmaceutical and personal care products (PPCPs) have received considerable attention because of their increasing use. Analysis of PPCPs presents a significant analytical challenge, with high-performance liquid chromatography (HPLC) in reversed-phase mode, as the most widely used analytical technique. To facilitate the optimization of the procedures that are applied in the early stages of sample preparation, a simple and fast HPLC method is proposed in this work for the separation of some PPCPs with a wide range of hydrophilicity. Read More

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Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels.

Acta Pharm 2021 Jun;71(2):317-324

Centro Universitario de Investigaciones Biomédicas, Universidad de Colima, Colima, COL 28045, México.

Terfenadine is a second-generation H1-antihistamine that despite potentially can produce severe side effects it has recently gained attention due to its anticancer properties. Lately, the subfamily 2 of inward rectifier potassium channels (Kir2) has been implicated in the progression of some tumoral processes. Hence, we characterized the effects of terfenadine on Kir2. Read More

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Sitagliptin: a potential drug for the treatment of COVID-19?

Acta Pharm 2021 Jun;71(2):175-184

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, P.O. Box 130, Amman 11733 Jordan.

Recently, an outbreak of a fatal coronavirus, SARS-CoV-2, has emerged from China and is rapidly spreading worldwide. Possible interaction of SARS-CoV-2 with DPP4 peptidase may partly contribute to the viral pathogenesis. An integrative bioinformatics approach starting with mining the biomedical literature for high confidence DPP4-protein/gene associations followed by functional analysis using network analysis and pathway enrichment was adopted. Read More

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Tryptanthrin exerts anti-breast cancer effects both in vitro and in vivo through modulating the inflammatory tumor microenvironment.

Acta Pharm 2021 Jun;71(2):245-266

School of Pharmacy, Key Laboratory of Optimal, Utilizaiton of Natural Medicine Resources, Guizhou Medical University, Guiyang 550025 Guizhou, China.

Tryptanthrin is an indole quinazoline alkaloid from the indigo-bearing plants, such as Isatis indigotica Fort. Typically, this natural compound shows a variety of pharmacological activities such as antitumor, antibacterial, anti-inflammatory and antioxidant effects. This study was conducted to assess the antitumor activity of tryptanthrin in breast cancer models both in vitro and in vivo, and to explore the important role of the inflammatory tumor microenvironment (TME) in the antitumor effects of tryptanthrin. Read More

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Identification of potential COVID-19 main protease inhibitors using structure-based pharmacophore approach, molecular docking and repurposing studies.

Acta Pharm 2021 Jun;71(2):163-174

Department of Pharmaceutical Sciences, School of Pharmacy, The University of Jordan, Amman, Jordan.

The current outbreak of novel coronavirus (COVID-19) infections urges the need to identify potential therapeutic agents. Therefore, the repurposing of FDA-approved drugs against today's diseases involves the use of de-risked compounds with potentially lower costs and shorter development timelines. In this study, the recently resolved X-ray crystallographic structure of COVID-19 main protease (Mpro) was used to generate a pharmacophore model and to conduct a docking study to capture antiviral drugs as new promising COVID-19 main protease inhibitors. Read More

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Efficacy and safety of the metformin-mazindol anorectic combination in rat.

Acta Pharm 2021 Jun;71(2):279-291

Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, Instituto Politécnico Nacional Plan de San Luis y Díaz Mirón s/n Col. Casco de Santo Tomas, Miguel Hidalgo, 11340, Ciudad de México, México.

The current study investigates the anorectic interaction and safety of the mazindol-metformin combination in rats. Isobologram and interaction index were used to determine anorectic interaction between mazindol and metformin in the sweetened milk model. The safety profile of the mazindol-metformin combination was determined by measuring anxiety, blood pressure, hematic biometry and blood chemistry. Read More

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An analytical "quality by design" approach in RP-HPLC method development and validation for reliable and rapid estimation of irinotecan in an injectable formulation.

Acta Pharm 2021 Mar;71(1):57-79

Department of Pharmaceutics Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal 576104, Udupi Karnataka, India.

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. Read More

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The controversies of parabens - an overview nowadays.

Acta Pharm 2021 Mar;71(1):17-32

Independent Unit of Toxicology University of Zagreb Faculty of Pharmacy and Biochemistry 10 000 Zagreb, Croatia.

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. Read More

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Improved 11α-hydroxycanrenone production by modification of cytochrome P450 monooxygenase gene in Aspergillus ochraceus.

Acta Pharm 2021 Mar;71(1):99-114

Department of Bioengineering Shanghai Institute of Technology Fengxian, Shanghai, 201418, China.

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. Read More

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The use of Hericium erinaceus and Trametes versicolor extracts in supportive treatment in oncology.

Acta Pharm 2021 Mar;71(1):1-16

Department of Internal Medicine and Oncological Chemotherapy, Medical University of Silesia Katowice 40-027, Poland.

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). Read More

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Protective effects of olive oil phenolics oleuropein and hydroxytyrosol against hydrogen peroxide-induced DNA damage in human peripheral lymphocytes.

Acta Pharm 2021 Mar;71(1):131-141

University of Zagreb, Faculty of Pharmacy and Biochemistry Department of Microbiology, 10000 Zagreb, Croatia.

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. Read More

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Investigation of design space for freeze-drying injectable ibuprofen using response surface methodology.

Acta Pharm 2021 Mar;71(1):81-98

University of Ljubljana, Faculty of Pharmacy, SI-1000, Ljubljana, Slovenia.

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. Read More

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A cost-effective and sensitive TLC-densitometric identification of meloxicam.

Acta Pharm 2021 Mar;71(1):143-152

Department of Analytical Chemistry Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia in Katowice, 41-200 Sosnowiec, Poland.

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 detection of meloxicam at the lowest concentration level on RP-8F254 and RP-18F254 plates. Read More

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In vitro antioxidant and antityrosinase activities of Manilkara kauki.

Acta Pharm 2021 Mar;71(1):153-162

Institute of Biotechnology and Genetic Engineering, Chulalongkorn University Bangkok 10330, Thailand.

Manilkara kauki L. Dubard is a tropical plant in the genus Manilkara of family Sapotaceae. This study investigated the total phenolic and flavonoid contents, and antioxidant and antityrosinase activities in different parts of M. Read More

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In silico data mining of large-scale databases for the virtual screening of human interleukin-2 inhibitors.

Acta Pharm 2021 Mar;71(1):33-56

Natural and Medical Science Research Center, University of Nizwa Birkat-ul-Mouz 616, Nizwa Sultanate of Oman.

Interleukin-2 (IL-2) is involved in the activation and differentiation of T-helper cells. Uncontrolled activated T cells play a key role in the pathophysiology by stimulating inflammation and autoimmune diseases like arthritis, psoriasis and Crohn's disease. T cells activation can be suppressed either by preventing IL-2 production or blocking the IL-2 interaction with its receptor. Read More

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Ellagic acid: A potent glyoxalase-I inhibitor with a unique scaffold.

Acta Pharm 2021 Mar;71(1):115-130

Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, P.O. Box 3030, Irbid 22110, Jordan.

The glyoxalase system, particularly glyoxalase-I (GLO-I), has been approved as a potential target for cancer treatment. 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. Read More

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Synthesis and biological evaluation of novel 1,3,4-thiadiazole derivatives as possible anticancer agents.

Acta Pharm 2020 Dec;70(4):499-513

Department of Pharmaceutical Chemistry, Faculty of Pharmacy Anadolu University, 26470Eskişehir Turkey.

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. Read More

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December 2020

Exploring the potential effect and mechanisms of protocatechuic acid on human hair follicle melanocytes.

Acta Pharm 2020 Dec;70(4):539-549

Department of plastic and aesthetic laser surgery, The people's Hospital of Hunan province, 1st Affiliated Hospital of Hunan Normal University Changsha410005, Hunan,China.

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. Read More

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December 2020

Synthesis and evaluation of bisulfate/mesylate-conjugated chlortetracycline with high solubility and bioavailability.

Acta Pharm 2020 Dec;70(4):483-498

Key Laboratory of Biorheological Science and Technology, Ministry of Education Bioengineering College, Chongqing University, Chongqing, 400044 People's Republic ofChina.

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 chlortetracycline hydrochloride, but the antibacterial activity was not enhanced. Read More

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December 2020

Probing the release of the chronobiotic hormone melatonin from hybrid calcium alginate hydrogel beads.

Acta Pharm 2020 Dec;70(4):527-538

Theoretical and Physical Chemistry Institute, National Hellenic Research Foundation, 11635Athens, Greece.

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. Read More

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December 2020

Modulatory effects of perindopril on cisplatin-induced nephrotoxicity in mice: Implication of inflammatory cytokines and caspase-3 mediated apoptosis.

Acta Pharm 2020 Dec;70(4):515-525

Department of Pharmacology and Toxicology, College of Pharmacy Taibah University, Al-Madinah Al-Munawwarah,Saudi Arabia.

Cisplatin-induced nephrotoxicity limits its anticancer effectiveness, thus this study's aim was to assess the potential modulatory effect of perindopril on cisplatin-induced nephrotoxicity and to elucidate the possible underlying mechanisms. Renal dysfunction was induced in mice by a single injection of cisplatin (10 mg kg-1, i.p. Read More

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December 2020

Antitumor effect of a pyrazolone-based-complex [Cu(PMPP-SAL)(EtOH)] against murine melanoma B16 cell in vitro and in vivo.

Acta Pharm 2020 Dec;70(4):561-575

Xinjiang Key Laboratory of Biological Resources and Genetic Engineering College of Life Science and Technology Xinjiang University, Urumqi830046 PRChina.

Pyrazolone-based derivative metal complexes were reported to have cytotoxicity in some tumor cells. 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 < 0. Read More

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December 2020

HPLC method development for fampridine using Analytical Quality by Design approach.

Acta Pharm 2020 Dec;70(4):465-482

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine, Pharmacy, Science and Technology of Tîrgu Mureș540139,Tîrgu Mureș, Romania.

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. Read More

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December 2020

Anthelmintic activity of praziquantel and Spilanthes acmella extract on an intestinal cestode parasite.

Acta Pharm 2020 Dec;70(4):551-560

Department of Life Sciences, Pachhunga University College Aizawl796001, Mizoram,India.

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. Read More

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December 2020

Piperazine derivatives as dangerous abused compounds.

Acta Pharm 2020 Dec;70(4):423-441

Department of Toxicology Faculty of Pharmacy, Collegium Medicum Nicolaus Copernicus University Bydgoszcz, Poland.

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. Read More

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December 2020

Process analytical technology tools for process control of roller compaction in solid pharmaceuticals manufacturing.

Acta Pharm 2020 Dec;70(4):443-463

Krka, d.d. Novo mesto, 8501 Novo mesto,Slovenia.

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. Read More

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December 2020