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Die Pharmazie.
Verlag Dr. W. Saenger,
Die Pharmazie.

Verlag Dr. W. Saenger,

0031-7144

Die Pharmazie./Journal Die Pharmazie.
正式出版
收录年代

    Candidate mechanisms of caffeine improving memory dysfunction

    Alhowail, A.
    6页
    查看更多>>摘要：Caffeine is the most common psycho-stimulant that is broadly known to cause peripheral effects. Caffeine is well known as an adenosine receptor antagonist. Adenosine receptors are present in all areas of the brain, which makes caffeine's effects very prevalent. The main goal of thisreview is to summarize recent studies that are investigating the mechanism of action of acute and chronic caffeine treatment of to alleviate the cognitive deficits and synaptic plasticity. This review discusses the effect of caffeine on the brain functions including learning and memory, andsynaptic plasticity in case of various diseases.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Biomarkers in VSMC phenotypic modulation and vascular remodeling

    Qi, YanDai, FanGu, JingyaYao, Wenjuan...
    4页
    查看更多>>摘要：Vascular smooth muscle cells (VSMCs) are not terminally differentiated and can change their phenotype in response to environmental cues. Phenotype switching of VSMCs to less differentiated forms has led to an underestimation of their role in the development of vascular remodeling andmany vascular diseases in both humans and animal models of this disease. In recent studies, many factors, such as microRNAs, matrix metalloproteinases, integrins, oxidative stress, autophagy, have been shown to play important roles in the mechanisms of VSMC phenotypic switch and vascular remodeling.This review highlights the current knowledge regarding the molecular mechanisms of VSMC phenotypic modulation in vascular remodeling. In this review, we want to provide effective molecular targets and opportunities for the future development of new therapeutics to regulate vascular remodelingdiseases.
      原文链接:
    • NSTL

    Copper(II) complex-loaded castor oil-based nanostructured lipid carriers used against Mycobacterium tuberculosis : Development, characterisation, in vitro and in vivo biological assays

    Oshiro-Junior, J. A.Souza, P. C.Campos, D. L.Pereira-Da-Silva, M. A....
    6页
    查看更多>>摘要：A copper(II) complex-loaded castor oil-based nanostructured lipid carrier was evaluated to enhance the poor water solubility of antimicrobial compounds, improving their biological properties and antimicrobial activity against Mycobacterium tuberculosis. Nanostructured lipid carrierswere composed of the castor oil, polyoxyethylene 40 stearate and caprylic/capric triglyceride, poloxamer 407, cetyltrimethylammonium bromide and three different copper(II) complexes. The systems were ultrasonicated at an amplitude of 8% for 20 min and an ice bath was used throughout the procedure.The blank nanostructured lipid carrier (F5) and nanostructured lipid carriers loaded with copper(II) complex 1, 2 and 3 (F5.1, F5.2 and F5.3, respectively) for 45 days presented values of mean diameter, poly dispersity index and zeta potential ranging from 186 to 199 nm, 0.14 to 0.2 and 24to 30 mV, respectively. Atomic force microscopy indicated that the nanostructured lipid carriers were distributed at the nanoscale, corroborating the mean diameter data. Differential scanning calorimetry determined the melting points of the constituents of the nanostructured lipid carriers.The antimicrobial activity of copper(II) complexloaded F5 against M. tuberculosis H37Rv showed better anti-tuberculosis activity than the free complexes. In vivo biological assays of complex-loaded F5 demonstrated reduced toxicity. Our results suggest that nanostructuredlipid carriers could be a potential nanotechnological strategy to optimise tuberculosis treatment.
      原文链接:
    • NSTL

    Design, evaluation and optimization of taste masked clarithromycin powder

    Ntemi, P. V.Walker, R. B.Khamanga, S. M. M.
    7页
    查看更多>>摘要：Clarithromycin (CLA) is an extremely bitter macrolide antibiotic used to treat paediatric and adult infections. The bitter taste affects patient adherence and may compromise therapy. This research developed a taste masked CLA resinate using Indion? 234, a weak acidic cation exchangeresin. The factors affecting formation of the CLA-resin complex were assessed. Design of experiments was used to optimize response while evaluating input variables such as temperature, CLA-resin ratio,stirring time and pH. CLA loading efficiency was determined spectrophotometrically and CLArelease using USP Apparatus II. Differential Scanning Calorimetry (DSC), Scanning Electron Microscop (SEM), Fourier Transform Infrared (FT-IR) Spectroscopy and X-ray Diffraction (XRD) were used to confirm complex formation. A spectrophotometric method was used to assess taste evaluation. Theoptimum CLA-resin ratio, temperature, and stirring time were 1:4, 80 °C, 3 hours, respectively, at pH 8. Characterization techniques revealed that CLA was crystalline and the complex amorphous in nature. FT-IR spectra of resinate revealed the absence of resonance due to the tertiary aminefunctional group that is responsible for the bitter taste of CLA. CLA was stable in simulated salivary fluid and was released within 3 hours in gastric fluid. All CLAresin batches revealed complete taste masking. Taste analysis highlighted the improvement of taste masking properties of theresinate as the CLA to resin ratio, increased.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Pharmacokinetic variations of nimesulide in mongrel dogs according to age

    Guillé, Pérez G.Guillé, Pérez B. E.Espinosa, Rivera L.Juárez-Olguín, H....
    4页
    查看更多>>摘要：The purpose of this research was to investigate the possible variations to the pharmacokinetics of nimesulide by the effect of age using an animal model. An experimental, analytical, prospective and longitudinal study in five dogs, from birth to 730 days of age was carried out. Nimesulideblood levels were measured in different months; concentrations were determined by HPLC-UV. Pharmacokinetic parameters were calculated by using the WinNonlin software. There were statistically significant differences (p <0.05) in most of the pharmacokinetic parameters between study of 6months against the other three studies in different ages. Changes in the pharmacokinetic parameters of nimesulide as a result of age, are determined by the growing and maturation of the animals. Resulting data suggest that nimesulide can be used safely as a long-term analgesic in dogs, but,the dosing regimens in humans should be different when administered at early age.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Transfer of epinastine to infants through human breast milk

    Iwasa, C.Zaima, K.Metori, K.Harikai, N....
    5页
    查看更多>>摘要：The purpose of this study was to develop an analytical method for analyzing epinastine in breast milk and maternal plasma samples to determine the safety of epinastine in breastfed infants. Six nursing mothers took epinastine hydrochloride (20 mg) once a day for 7 days, while a nursingmother took it for 30 days. Breast milk and blood samples were collected 2, 4, and 10 h after administration from the volunteers. A liquid chromatography-mass spectrometry system was used to analyze samples pretreated by liquid-liquid extractions. The concentration of epinastine in human milkwas 10.3–33.5 ng/mL after 2 h, 9.1–63.8 ng/mL after 4 h, and 8.3–28.9 ng/mL after 10 h. The increase achieved 4 h after administration indicates that epinastine was transferred into human breast milk. However, the milk-to-plasma ratio had a wide range (0.82–3.39), whilethe relative infant dose at 4 h was 0.36–2.49%, which is lower than the safety level of transferability (10%). Moreover, the plasma levels of epinastine in two infants were slightly below the quantification limit. Overall, our results suggested that epinastine can safely be used by nursingmothers without affecting their infants.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Metformin administration increases the survival rate of doxorubicin-treated mice

    Alhowail, A.Almogbel, Y.
    3页
    查看更多>>摘要：Background: The chemotherapeutic agent doxorubicin (DOX), an anthracycline broadly used to treat different types of cancers, induces several side effects, including cardiotoxicity, hepatotoxicity, and nephrotoxicity, in a time- and dose-dependent manner. Metformin (MET) is anantidiabetic drug used as a first-line treatment for type-2 diabetes, and is reported to work against various various drug-induced toxicities. This study aimed to investigate whether the administration of MET prophylactically suppresses DOX-induced toxicity, and prolongs the survival followingDOX treatment. Methods: Fifty mice were divided into four groups, and each group received different treatments. The animals in the control group received a single injection of saline. The animals in the DOX group received a single dose of DOX (25 mg/kg). The animals in the MET groupreceived MET on a daily basis. The animals in the DOX+MET group received only a single dose of DOX and daily doses of MET. The animals were observed on a daily basis for determining their body weight and evaluating the survival rate of the four study groups. Results: DOX acceleratedthe mortality rate of the animals in the DOX-treated group. Co-administration of MET and DOX increased the survival rate of the mice. Conclusion: The results of this study demonstrated that the administration of MET can reduce DOX-induced toxicity and increase the survival rate amongchemotherapy-treated mice.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Verapamil enhances the sensitivity of oxaliplatin to tumor cells by influencing the PARP pathway

    Zhang, TengyueYang, GuangshanLiu, YabeiFan, Pingsheng...
    4页
    查看更多>>摘要：PARP is a DNA damage-modifying enzyme present in most eukaryotic cells. In this study, reverse docking showed that verapamil (Vera), which can effectively bind PARP1/2, could significantly inhibit PARP1/2 activity inside and outside the system. Moreover, it could enhance the sensitivityof oxaliplatin to low-expression P-glycoprotein (P-gP) tumor cells and strengthen its apoptosis-inducing effect on tumor cells under the reverse drug resistance concentration of tumor cells. Vera, which can reverse chemotherapy resistance of tumor cells, showed no simple correlations withoxaliplatin drug resistance or P-gP expression and could enhance the anti-tumor effect of platinum chemotherapeutic agents by influencing the PARP pathway.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Downregulation of organic cation transporter 1 and breast cancer resistance protein with the induction of Pregnane X receptor in rat kidney impaired by doxorubicin

    Nagai, K.Fukuno, S.Yamamoto, K.Omotani, S....
    3页
    查看更多>>摘要：Transporters expressed in the kidney play an important role in the excretion of endogenous substances and chemical drugs. The Pregnane X receptor (PXR) has been reported to be involved in regulating the expression of numerous transporters. In the present study, we examined the alterationin expression level of PXR, organic cation transporter 1 (OCT1) and breast cancer resistance protein (BCRP) in renal cell lines of rat origin and the kidney of rats when damaged by doxorubicin (DOX). The expression level of PXR in renal tubular epithelium NRK-52E cells was significantly increasedby DOX at a concentration confirmed to cause cellular damage. The expression levels of OCT1 and BCRP were significantly lower in the DOX-treated cells than in the untreated cells. In model rats with DOX-induced nephrotoxicity, the alterations in renal expression of PXR, OCT1 and BCRP weresimilar to those in NRK-52E cells, although there was a difference in the degree of the changes.
      原文链接:
    • NSTL
    • Govi-Verlag Pharmazeutischer Verlag Gmbh

    Sinomenine can promote the proliferation and differentiation of osteoblasts by regulating the Akt/Runx2 signaling pathway in MC3T3-E1 cells

    Zhang, BoZhang, HaijunLuo, HaoYang, Chao...
    4页
    查看更多>>摘要：This study aimed to explore the effect of sinomenine on the proliferation and differentiation of MC3T3-E1 cells and the related mechanism. Mouse preosteoblastic cell line MC3T3-E1 cells were divided into four groups: control group, treatment of sinomenine with the concentrations of100, 500 or 1000 μM. The proliferation and apoptosis of the cells were determined by MTT assay at 0, 24, 48 and 72 h, and flow cytometry method was used to determine the effect of sinomenine on the apoptosis of MC3T3-E1 cells at 72 h; furthermore, after 72 h, the cell culture supernatantswere collected, and the levels of alkaline phosphatase and osteocalcin were examined by enzyme-linked immunosorbent assay (ELISA); next, cells were collected, and the expression of type I collagen (COL1A1), osteopontin (OPN), protein kinase B (Akt), runt-related transcription factor 2 (Runx2),B-cell lymphoma 2 (Bcl-2) and Bcl-2-associated X protein (Bax) were examined by RT-qPCR and Western Blot methods. It was observed that treatment of 500 and 1000 μM sinomenine has induced significant increase in the proliferation and decrease in the apoptosis of MC3T3-E1 cells; furthermore,sinomenine also lead to increased secretion of osteocalcin and alkaline phosphatase in MC3T3-E1 cells; finally, sinomenine induced marked increase in the expression of type I collagen, osteopontin and also induced the activation of the Akt/Runx2 signaling pathway. To sum up, we observed thatsinomenine may promote the proliferation and differentiation of MC3T3-E1 cells via activating the Akt/Runx2 signaling pathway.
      原文链接:
    • NSTL