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Die Pharmazie

M Kimura, M Iwai, E Usami, H Teramachi, T Yoshimura
For patients with advanced/recurrent colorectal cancer, the trifluridine/tipiracil combination tablet (TAS 102) and regorafenib are last-line treatments. This study aimed to clarify prognostic factors in patients receiving last-line chemotherapy. Between April 2014 and December 2016, 47 patients received last-line chemotherapy at Ogaki Municipal Hospital, Japan. The primary outcome was overall survival. To determine factors associated with survival, those considered significant in the univariate analysis (p <0...
February 1, 2018: Die Pharmazie
M Todo, S Ueda, S Osaki, I Sugitani, T Takahashi, M Takahashi, H Makabe, T Saeki, Y Itoh
Combination therapy with everolimus and an aromatase inhibitor such as exemestane is an effective treatment option for advanced or recurrent breast cancer. However, the therapy is often limited because of the occurrence of severe adverse events (AEs), including oral mucositis, interstitial lung disease, diarrhea, and rash. Therefore, early management of AEs is extremely important to obtain maximum treatment outcome. We investigated here the effects of comprehensive pharmaceutical care for prevention of severe AEs on patient's quality-of-life (QOL) and continuation of therapy...
February 1, 2018: Die Pharmazie
M Kawami, Y Yamada, O Issarachot, V B Junyaprasert, R Yumoto, M Takano
The extract of Azadirachta indica, commonly known as neem, has found extensive use in traditional medicine for treating various human diseases. In this study, the effect of the 50% ethanol extract of A. indica (AI01) on P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) was examined using MDR cell lines, specifically paclitaxel-resistant HepG2 (PR-HepG2) and doxorubicin (DOX)-resistant (DR) colon-26 cells. 96-h treatment of the two cell lines with AI01 (30 μg/mL) showed no effect on the expression of P-gp mRNA (human MDR1 and mouse mdr1b) and protein, while AI01 increased the accumulation of rhodamine 123, a P-gp substrate, in both PR-HepG2 and DR-colon-26 cells...
February 1, 2018: Die Pharmazie
Fan-Fang Tie, Guang-Xiang Luan, Wen-Na Zhou, Zhen-Hua Wang, Xiao-Bing Shi, Gang Li, Hong-Lun Wang
The dried seeds of Iris lactea Pall. var. chinensis (Fisch.) Koidz, an important traditional Chinese medicine, are regarded to have effects of clearing heat, eliminating dampness and pharyngitis and so on. It has been used in the treatment of jaundice, diarrhea, leucorrhea and carbuncles. Previous phytochemical studies of Iris species showed the presence of flavones, isoflavones, triterpenes and stilbenes. In our previous research, we isolated five known oligostilbenes, vitisin A, vitisin B, vitisin C, vitisin D, and cis-vitisin A were successfully isolated from Iris lactea for the first time...
February 1, 2018: Die Pharmazie
Deqing Sun, Aiying Xue, Xia Xue, Manru Ren, Jing Wu, Rongmei Wang
High mobility group box 1 (HMGB1), a non-histone DNA-binding protein, is massively released into the extracellular space from neuronal cells after ischemic injury, initiates inflammatory response and aggravates brain tissue damage. Acetylpuerarin (AP), an acetylated derivative of puerarin, was reported to protect against cerebrovascular ischemia-reperfusion injury in rats through anti-inflammation. In the present study, we aim to investigate whether AP inhibited HMGB1 release in oxygen-glucose deprivation (OGD)-treated BV2 microglia...
February 1, 2018: Die Pharmazie
Z M Jiang, H B Qiu, S Q Wang, J Guo, Z W Yang, S B Zhou
Ganoderma lucidum extracts have shown antiepileptic effects in in vivo and in vitro studies. In this work, primary hippocampal neurons cultured in magnesium-free medium were used to study the neuroprotective effects of ganoderic acid A and B (GA-A and GA-B) on superoxide dismutase (SOD) activity and mitochondrial membrane potential, to improve our understanding of their antiepileptic effect. The activity of SOD was determined by the xanthine oxidase assay, the variations of mitochondrial membrane potential and cell apoptosis were measured by JC-1 fluorescent staining and flow cytometry...
February 1, 2018: Die Pharmazie
Weihong Zhu, Xinzhan Mao, Wanchun Wang, You Chen, Ding Li, Hui Li, Pengcheng Dou
Cisplatin is an effective chemotherapeutic agent for osteosarcoma (OS) and has been shown to induce endoplasmic reticulum (ER) stress-associated apoptosis in human cancer cells. Ganglioside GD2-specific antibodies can inhibit tumor cell viability without involvement of the immune system. A recent study has shown that antiGD2 monoclonal antibody (mAb) 14G2a effectively inhibits the viability and invasiveness of human OS cells. In this study, we explored the effect of anti-GD2 mAb and cisplatin alone and in combination on ER stress-associated apoptosis in osteosarcoma cells...
February 1, 2018: Die Pharmazie
E Hagesaether
Orfiril® long is a widely used antiepileptic drug preparation despite being characterized by features associated with susceptibility to ethanol induced changes to drug release. In vitro dissolution studies revealed that 30 % ethanol was required in order to cause dose dumping of valproic acid within two hours at pH 1. However, after exposure to only 5 % of ethanol for 45 minutes at pH 1, the subsequent release of sodium valproate increased by ~ 10 % for the first two hours in ethanol-free media of pH 6.8. The drug solubility increases with pH, likely to also increase the vulnerability to ethanol...
February 1, 2018: Die Pharmazie
Cunchun Dai, Shaoqi Qu, Ruili Zhang, Li Zhao, Yuwen Li, Jiajia Zhu, Chunmei Wang, Hui Guo, Zhihui Hao
The objective of this study was to prepare a new compound fenbendazole tablet containing 29.7 % fenbendazole, 1.50 % praziquantel and 0.059 % ivermectin for oral administration. The tablets were successfully prepared using mannitol as filler agent, polyvinyl polypyrrolidone as disintegrant, 5 % povidone (PVAK30) as a binder agent and magnesium stearate as lubricant. The appearance, hardness, fragility, time limit of disintegration and fenbendazole dissolution at 45 min all met the technical standards of the Ministry of Agriculture for the People's Republic of China...
February 1, 2018: Die Pharmazie
J Al-Gousous, P Langguth
A scaled convolution-based in vitro-in vivo (IVIVC) model was constructed for two enteric-coated acetylsalicylic acid tablet formulations. The in vitro data used were the results of dissolution testing performed using three different dissolution methods: the United States Pharmacopoeia (USP) method, a method employing blank Fasted State Simulated Fluid (FaSSIF), and a new method developed in house. The in vivo data were obtained from a pharmacokinetic study on human subjects in the fasted state. When the new dissolution method results were used, an average prediction error less than 10% and a maximum prediction error less than 15% were obtained for the peak plasma concentration (Cmax) and area under the curve (AUC) parameters, thus meeting the internal validation criteria of the IVIVC guidance of the US Food and Drug Administration (FDA)...
February 1, 2018: Die Pharmazie
A N Hashim, N F Swilam, E S Moustafa, S M Bakry, R M Labib, H H Barakat, A B Singab, M W Linscheid, M A Nawwar
Leaves of Melaleuca leucadendra contain the novel flavonol glycoside, myricetin 3-O-β-4C1-galactopyranuronoid. In addition, known fifteen phenolics were identified. All isolates are characterized for the first time from this plant. Structures were established by conventional methods and confirmed by spectral methods of analysis, including one and two-dimensional nuclear magnetic resonance spectroscopy (1D and 2D-NMR) and high resolution electro-spray ionization mass spectrometry (HRESIMS), as well. Assessment of some immunological and biological efficacy, of the extract in combination with a parallel cytotoxicity evaluation, using the method of cellular reduction of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) technique was carried out...
January 2, 2018: Die Pharmazie
M Starbek Zorko, B Štrukelj, U Švajger, S Kreft, T Lunder
Silver fir (Abies alba) bark extract contains a mixture of bioactive polyphenols. We tested their effectiveness in the treatment of psoriasis in order to further investigate the potential topical anti-inflammatory activity of polyphenols by means of a randomized, double-blind, placebo-controlled add-on clinical trial, after having examined their ability to downregulate the expression of IL-1β cytokine in monocyte/macrophage primary cell culture. 61 patients with mild psoriasis met the inclusion criteria and were willing to comply with protocol requirements, were enrolled in the study...
January 2, 2018: Die Pharmazie
Yongwei Li, Zhengfei Shan, Bin Yang, Diandong Yang, Changping Men, Yuanshan Cui, Jitao Wu
AIMS: Adipose-derived stem cells (ADSCs), a source of mesenchymal stem cells, are able to differentiate into numerous cell lineages, including epithelial and smooth muscle cells. The use of ADSCs in tissue engineering technology has become the most promising therapeutic approach for urethral reconstruction. This study aimed to explore the effect of lncRNA highly upregulated in liver cancer (HULC) on the induction of ADSCs to differentiate into epithelial and smooth-muscle-like cells. METHODS: ADSCs were isolated from a male dog, and the expression of HULC in ADSCs was overexpressed by transfection with HULC expressing vector lentivirus...
January 2, 2018: Die Pharmazie
Yuqiang Shan, Wencheng Kong, Akao Zhu, Panpan Yu, Qi Xie, Sixin Zheng, Huicheng Jin
AIMS: Long non-coding RNAs (lncRNAs) play key roles in cancers, yet their potential molecular mechanisms are not well understood. The objective of this study is to examine the expression, biological functions and mechanism of lncRNA CCAL in gastric cancer (GC). METHODS: MTT and Colony formation assay were used to detect cell proliferation and the colony formation ability of gastric cancer cells. Wound healing, Migration, and invasion assay were respectively used to explore the migration, and invasion in gastric cancer cell lines...
January 2, 2018: Die Pharmazie
M Isawa, R Tashiro, C Naruse, Y Yamaguchi, H Itoh, T Nishimura, M Tomi, H Shimada, H Saito, M Mochizuki, E Nakashima
Patients benefit from drug therapy not only through pharmacological mechanisms, but also through non-pharmacological action (placebo effect), which may be mediated in part by the prefrontal area of the brain. We consider that the difference between responders and non-responders to placebo might be related to polymorphisms in the serotonin transporter-linked polymorphic region (5-HTTLPR). To study this idea, we performed a randomized double-blind clinical trial using caffeine and lactose (placebo). Activity in the prefrontal area of the brain was measured in terms of blood flow by means of near-infrared spectroscopy (NIRS) as an objective indicator...
January 2, 2018: Die Pharmazie
Yuyu Huang, Hongwu Wang, Yanhui Wang, Xiaohui Peng, Jing Li, Wenlong Gu, Ting He, Minjun Chen
AIM: MicroRNAs (miRs) are endogenous substances that act as important diagnostic and treatment targets in renal diseases. miR-146 plays an important role in the development of endotoxin tolerance through NF-κB pathway, but the underlying mechanism is not clearly understood. The aim of this study was to determine the molecular regulation and function of miR-146 and also the expression of miR-146 in an experimental model of renal ischemia reperfusion injury (IRI). METHODS: IRI was induced in mouse by bilateral IRI for 45 min followed by reperfusion...
January 2, 2018: Die Pharmazie
S Honma, K Kouno, S Takasaka, S Mitazaki, S Abe, H Kikuchi, Y Oshima, M Yoshida
Malignant gliomas are highly resistant to chemotherapy and radiation and more effective options for treatment are urgently needed. We reported previously that the aromatic amide brefelamide, which is isolated from methanolic extracts of the cellular slime molds Dictyostelium giganteum and D. brefeldianum, hinders cellular proliferation in a glioma model utilizing 1321N1 human astrocytoma cells. Herein, we examined the mechanisms underlying the inhibition of 1321N1 cell proliferation by brefelamide. Glial cell line-derived neurotrophic factor (GDNF) was found to enhance the rate of proliferation of serum-free cultured 1321N1 cells, but did not affect proliferation in PC12 cells...
January 2, 2018: Die Pharmazie
M Otręba, E Buszman
Phenothiazine derivatives possess biological properties very useful for cancer therapy, such as antiemetic and sedative activity as well as good blood-brain barrier permeability. Our goal was to determine if perphenazine and prochlorperazine are possessing cytotoxic activity towards U87-MG cells. It has been shown that the analyzed drugs induce concentration-dependent loss in cell viability, what correlates with their chemical structure. The calculated EC50 values for perphenazine (0.98 μM) and prochlorperazine (0...
January 2, 2018: Die Pharmazie
D Nemes, Z Ujhelyi, P Arany, A Pető, P Fehér, J Váradi, F Fenyvesi, M Vecsernyés, I Bácskay
Aqueous pharmaceutical solutions provide prosperous living conditions for microbiological agents. In order to eliminate these microbes, we use preservatives which can harm human cells as well. Their cytotoxicity is concentration-dependent and the aim of our study was to find how other pharmaceutical excipients modify the cytotoxic attributes of preservatives. We tested the following compounds: methylparaben, benzalkonium chloride, polysorbate 20, Labrasol® and hydroxyethyl cellulose. The MTT tests indicated that surfactants increase the cytotoxicity while polymers may decrease it in some cases...
January 2, 2018: Die Pharmazie
J A Alkrad, A S Alruby
Gentamicin sulfate (GS) is used usually as intravenous or intramuscular solution because of its poor oral bioavailability. However, the intravenous administration is associated with pain and needs some skills. In this study, five nonionic microemulsions (MEs) for oral and transdermal application were developed using nonionic surfactants. The MEs were characterized for their droplets sizes and rheological properties. Moreover, GS encapsulation in the MEs was studied using Fourier Transform Infrared Spectroscopy (FTIR)...
January 2, 2018: Die Pharmazie
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