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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/27909956/docking-and-three-dimensional-quantitative-structure-activity-relationship-analyses-of-imidazole-and-thiazolidine-derivatives-as-aurora-a-kinase-inhibitors
#1
Chaeuk Im
Aurora A kinase is involved in the inactivation of apoptosis leading to ovarian, breast, colon, and pancreatic cancers. Inhibitors of Aurora A kinase promote aberrant mitosis resulting in arrest at a pseudo G1 state to induce mitotic catastrophe, ultimately leading to apoptosis. In this study, ligand-based and docking-based three-dimensional quantitative structure-activity relationship (3D-QSAR) analyses of imidazole and thiazolidine derivatives as potential Aurora A kinase inhibitors were performed. The results provided highly reliable and predictive 3D-QSAR comparative molecular similarity index analysis (CoMSIA) models with a cross-validated q(2) value of 0...
December 1, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27909955/suppressive-effects-of-dabrafenib%C3%A2-on-endothelial-protein-c-receptor-shedding
#2
Sae-Kwang Ku, Jongdoo Kim, Sang Chan Kim, Jong-Sup Bae
Beyond its role in the activation of protein C, the endothelial cell protein C receptor (EPCR) plays an important role in the cytoprotective pathway. EPCR can be shed from the cell surface, which is mediated by tumor necrosis factor-α converting enzyme (TACE). Dabrafenib (DAB) is a B-Raf inhibitor and initially used for the treatment of metastatic melanoma therapy. However, little is known about the effects of DAB on EPCR shedding. We investigated this issue by monitoring the effects of DAB on phorbol-12-myristate 13-acetate (PMA)-, tumor necrosis factor (TNF)-α-, interleukin (IL)-1β-induced EPCR shedding in human umbilical vein endothelial cells (HUVECs), and cecal ligation and puncture (CLP)-mediated EPCR shedding in mice and underlying mechanism...
December 1, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27888442/annulohpoxylotol-a-and-b-new-sesquiterpenoids-from-the-endophytic-fungus-annulohypoxylon-truncatum-are-natural-nf-%C3%AE%C2%BAb-inhibitors
#3
Wei Li, Ya Nan Sun, Changyeol Lee, Sung Hee Bang, Soonok Kim, Jin Yeul Ma, Young Ho Kim, Sang Hee Shim
Two sesquiterpenoids, annulohpoxylotol A and B, were isolated along with five sterols from an ethyl acetate extract of cultures of the endophytic fungus Annulohypoxylon truncatum growing on leaves of Zizania caduciflora. The structures of the isolated compounds were established using one-dimensional (1D) and two-dimensional (2D)-NMR and mass spectrometry. The nuclear factor-kappa B (NF-κB) inhibitory activities of the isolated compounds stimulated with tumor necrosis factor-alpha (TNF-α) were measured using a luciferase reporter system...
November 25, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27885462/the-cytoprotective-effect-of-rumex-aquaticus-herba-extract-against-hydrogen-peroxide-induced-oxidative-stress-in-ags-cells
#4
Eun Jeong Cho, Seung In Um, Jeong Hoon Han, Byeonghee Kim, Sang Beom Han, Ji Hoon Jeong, Hak Rim Kim, Inkyeom Kim, Wan Kyun Whang, Eunhwa Lee, Uy Dong Sohn
The Rumex Aquaticus Herba extract containing quercetin-3-β-D-glucuronopyranoside (ECQ) has been reported to exhibit various pharmacological activities, including anti-inflammatory and anti-oxidative effects. This plant has been traditionally used for the treatment of diarrhea, disinfestation, edema and jaundice, and as an antipyretic drug. The aim of the present study was to investigate the ability of ECQ to protect against oxidative damage and to determine its signaling mechanism in AGS cells. The protein expressions of heme oxygenase-1 (HO-1) and nuclear factor-erythroid 2 related factor 2 (Nrf2) were measured by Western blots...
November 24, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27885461/prevention-and-treatment-effect-of-evogliptin-on-hepatic-steatosis-in-high-fat-fed-animal-models
#5
Mi-Kyung Kim, Yu Na Chae, Gook-Jun Ahn, Chang Yell Shin, Song-Hyen Choi, Eun Kyoung Yang, Yong Sung Sohn, Moon-Ho Son
Dipeptidyl peptidase 4 (DPP4) is an adipokine that interrupts insulin signaling. The resulting insulin resistance exacerbates hepatic steatosis. We previously reported that the novel DPP4 inhibitor evogliptin improves insulin resistance. This study aimed to verify the therapeutic potential of evogliptin for fatty liver. Evogliptin treatment was initiated simultaneously with a high-fat diet (HFD) feeding in normal mice and in a post-24 week HFD-fed rats. In a prevention study, insulin sensitivity was preserved in evogliptin-treated mice after a 16-week treatment...
November 24, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27878514/emergence-of-hydrogen-bonds-from-molecular-dynamics-simulation-of-substituted-n-phenylthiourea-catechol-oxidase-complex
#6
Kyung-Lae Park
A series of N-phenylthiourea derivatives was built starting from the X-ray structure in the molecular mechanics framework and the interaction profile in the complex with the catechol oxidase was traced using molecular dynamics simulation. The results showed that the geometry and interactions between ligand and receptor were highly related to the position of the substituted side chains of phenyl moiety. At the end of molecular dynamics run, a concentrated multicenter hydrogen bond was created between the substituted ligand and receptor...
November 22, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27864660/effects-of-cyp2c9-genetic-polymorphisms-on-the-pharmacokinetics-of-celecoxib-and-its-carboxylic-acid-metabolite
#7
Se-Hyung Kim, Do-Hoon Kim, Ji-Yeong Byeon, Young-Hoon Kim, Dong-Hyun Kim, Hye-Jin Lim, Choong-Min Lee, Sang Sup Whang, Chang-Ik Choi, Jung-Woo Bae, Yun Jeong Lee, Choon-Gon Jang, Seok-Yong Lee
Celecoxib, a selective cyclooxygenase (COX)-2 inhibitor, is used for the treatment of rheumatoid arthritis and osteoarthritis. The predominant hepatic metabolism of celecoxib to celecoxib carboxylic acid (CCA) is mediated mainly by CYP2C9. We investigated the effects of the major CYP2C9 genetic variants in Asian populations, CYP2C9*3 and CYP2C9*13, on the pharmacokinetics of celecoxib and its carboxylic acid metabolite in healthy Korean subjects. A single 200-mg oral dose of celecoxib was given to 52 Korean subjects with different CYP2C9 genotypes: CYP2C9EM (n = 26; CYP2C9*1/*1), CYP2C9IM (n = 24; CYP2C9*1/*3 and *1/*13), and CYP2C9PM (n = 2; CYP2C9*3/*3)...
November 18, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27858280/a-simple-and-reliable-analytical-method-based-on-hplc-uv-to-determine-oleanonic-acid-content-in-chios-gum-mastic-for-quality-control
#8
Yan Jin, Jing Zhao, Kyung Min Jeong, Da Eun Yoo, Se Young Han, Su-Young Choi, Dong-Hyeon Ko, Hyun-Ji Kim, Na-Hye Sung, Jeongmi Lee
A reliable analytical method based on high-performance liquid chromatography-ultraviolet detection was established for the determination of oleanonic acid (OA) content in Chios gum mastic (CGM). A simple method involving methanol extraction of CGM powder followed by basification and ether extraction was developed to isolate the triterpenic fraction including OA. The triterpenic fraction was chromatographed on a Phenomenex Gemini C18 column (150 × 4.6 mm, 5 µm) under a simple gradient elution of a mobile phase containing acetonitrile and water at a flow rate of 1...
November 17, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27848145/monoterpene-esters-and-aporphine-alkaloids-from-illigera-aromatica-with-inhibitory-effects-against-cholinesterase-and-no-production-in-lps-stimulated-raw264-7-macrophages
#9
Jian-Wei Dong, Le Cai, Xue-Jiao Li, Jia-Peng Wang, Rui-Feng Mei, Zhong-Tao Ding
Three new monoterpene phenylpropionic acid esters, illigerates A-C (1-3), and one new aporphine alkaloid, illigeranine (4), as well as four known ones, actinodaphnine (5), nordicentrine (6), 8-hydroxy carvacrol (7), and 3-hydroxy-α,4-dimethyl styrene (8), were isolated from the tubers of Illigera aromatica. The structures of 1-4 were identified by HRESIMS, 1D and 2D NMR, and electronic circular dichroism spectra. Compound 1 potently inhibited NO production in LPS-stimulated RAW264.7 cells with an IC50 value of 18...
November 15, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27826753/intracellular-interleukin-il-1-family-cytokine-processing-enzyme
#10
REVIEW
Areum Kwak, Youngmin Lee, Hyunwoo Kim, Soohyun Kim
The interleukin (IL)-1 family is the largest family of interleukins. Eleven members of the IL-1 family of ligands are intracellular molecules, except a single isoform of an IL-1 receptor antagonist (IL-1Ra; also known as IL-1RN), which contains a signal peptide at the N-terminus for effective secretion. The inflammasome is a complex of intracellular molecules that is responsible for the processing of IL-1β and IL-18, whereas the remaining IL-1 family members, including IL-1α, are processed in an inflammasome caspase-1-independent pathway...
November 9, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27826752/essential-role-of-interferon-regulatory-factor-4-irf4-in-immune-cell-development
#11
REVIEW
Sorim Nam, Jong-Seok Lim
The family of interferon regulatory factors, which includes nine mammalian members (IRF1-IRF9), acts as transcription factors for interferons and thus exerts regulatory functions in the immune system and in oncogenesis. Among these members, IRF4 expression is restricted to immune cells such as T and B lymphocytes, macrophages, and dendritic cells where it is a key factor in the regulation of differentiation and is required during the immune response for lymphocyte activation and the generation of immunoglobulin-secreting plasma cells...
November 9, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27826751/suppressive-effects-of-pelargonidin-on-polyphosphate-mediated-vascular-inflammatory-responses
#12
In-Chul Lee, Jong-Sup Bae
Previous reports suggest that human endothelial cells-derived PolyPhosphate (PolyP) is one of the pro-inflammatory mediators. As a well-known red pigment and found in plants, Pelargonidin (PEL) has been known to have several biological activates which are beneficial for human health. This study was undertaken to investigate whether PEL can modulate PolyP-mediated inflammatory responses in human umbilical vein endothelial cells (HUVECs) and in mice. The anti-inflammatory activities of PEL were determined by measuring permeability, leukocytes adhesion and migration, and activation of pro-inflammatory proteins in PolyP-activated HUVECs and mice...
November 8, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27798765/prunin-is-a-highly-potent-flavonoid-from-prunus-davidiana-stems-that-inhibits-protein-tyrosine-phosphatase-1b-and-stimulates-glucose-uptake-in-insulin-resistant-hepg2-cells
#13
Hyun Ah Jung, Md Yousof Ali, Himanshu Kumar Bhakta, Byung-Sun Min, Jae Sue Choi
Prunin is the main flavonoid in Prunus davidiana stems and improves hyperglycemia and hyperlipidemia in streptozotocin-induced diabetic rats. The aim of this study was to investigate the in vitro anti-diabetic potential of prunin via the inhibition of protein tyrosine phosphatase 1B (PTP1B), α-glucosidase, peroxynitrite (ONOO(-))-mediated tyrosine nitration, and stimulation of glucose uptake in insulin-resistant hepatocytes. In addition, a molecular docking simulation was performed to predict specific prunin binding modes during PTP1B inhibition...
October 31, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27796936/ajoene-restored-behavioral-patterns-and-liver-glutathione-level-in-morphine-treated-c57bl6-mice
#14
Jaesuk Yun, Sergiy Oliynyk, Yeonju Lee, Jieun Kim, Kyunghwa Yun, Raok Jeon, Jae-Ha Ryu, Seikwan Oh
Oxidative stress exacerbates drug dependence induced by administration of opiate analgesics such as morphine-induced tolerance and physical dependence associated with the reduction in hepatic glutathione (GSH) level. Ajoene obtained from garlic (Allium sativum L.) has been reported for anti-tumorigenic, anti-oxidative and neuroprotective properties, however, little is known about its effect on morphine-induced dependence. Therefore, this study aimed at the effect of ajoene on physical and/or psychological dependence and liver GSH content in morphine-treated mice...
October 28, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27778276/transcriptional-modulation-of-regulatory-t-cell-development-by-novel-regulators-nr4as
#15
Hee Yeon Won, Eun Sook Hwang
Regulatory T (Treg) cells with high expression of both CD25 and Foxp3 are developed in the thymus and also peripheral tissues. Treg cells suppress the activation and functions of effector T cells raised against specific antigens and are crucial for maintaining immune homeostasis. Treg cell development is associated with the induction of and epigenetic alterations of forkhead transcription factor Foxp3. Foxp3 expression is increased by the activation of several transcription factors including nuclear factor-kappa B (NF-κB), nuclear factor of activated T cells (NFAT), and Smad3 in response to various signals such as TGFβ, retinoic acid, and rapamycin...
October 25, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27778275/anti-septic-effects-of-pelargonidin-on-hmgb1-induced-responses-in-vitro-and-in-vivo
#16
Gahee Min, Sae-Kwang Ku, Mi Seon Park, Tae-Joo Park, Hyun-Shik Lee, Jong-Sup Bae
A certain nucleosomal protein-high mobility group box-1 (HMGB1)-has recently been established as a late mediator of sepsis, with a relatively wide therapeutic window for pharmacological intervention. Pelargonidin (PEL) is a well-known red pigment found in plants; it has important biological activities that are potentially beneficial for human health. In the present study, we investigated whether PEL can modulate HMGB1-mediated inflammatory responses in human umbilical vein endothelial cells (HUVECs) and in mice...
October 24, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27778274/moisturizing-effect-of-serine-loaded-solid-lipid-nanoparticles-and-polysaccharide-rich-extract-of-root-phragmites-communis-incorporated-in-hydrogel-bases
#17
Sonia Barua, Hyeongmin Kim, Seong-Chul Hong, Seung-Yup Yoo, Dohyun Shin, Chung-Lyol Lee, Seon-Jeong Na, Yeong Hyo Kim, Kanghee Jo, Gyiae Yun, Joong-Hark Kim, Uy Dong Sohn, Jaehwi Lee
This study evaluated the moisturizing effect of serine-loaded solid lipid nanoparticles (serine-SLN) and polysaccharide-rich reed (Phragmites communis) root extract (RRE) incorporated in hydrogel bases. The hydrogels with serine-SLN and/or RRE were carefully applied on the volar forearm of human volunteers. Their moisturizing efficacy was evaluated by monitoring conductance values using a skin surface hygrometer. The values of the area under the normalized conductance-time curve (AUCC) were developed and compared as a parameter for the water holding capacity of the skin...
October 24, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27770383/chalcone-templated-hsp90-inhibitors-and-their-effects-on-gefitinib-resistance-in-non-small-cell-lung-cancer-nsclc
#18
Ju Hui Jeong, Yong Jin Oh, Taeg Kyu Kwon, Young Ho Seo
The molecular chaperone Hsp90 has emerged as an attractive cancer therapeutic target due to its role in cellular homeostasis by modulating the stabilization and maturation of many oncogenic proteins. In this study, we designed and synthesized a series of Hsp90 inhibitors that hybridized NVP-AUY992 (2) and PU3 (3) in the chalcone scaffold using a structure-based approach. Our results indicate that compound 1g inhibited the proliferation of gefitinib-resistant non-small cell lung cancer (H1975) cells, downregulated the expression of client proteins of Hsp90 including EGFR, MET, Her2 and Akt, and up-regulated the expression of Hsp70...
October 21, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27761800/investigation-of-biomimetic-shear-stress-on-cellular-uptake-and-mechanism-of-polystyrene-nanoparticles-in-various-cancer-cell-lines
#19
Taehee Kang, Chulhun Park, Beom-Jin Lee
Cancer cells in the tumor microenvironment are affected by fluid shear stress generated by blood flow in the vascular microenvironment and interstitial flows in the tumor microenvironment. Thus, we investigated how fluidic shear stress affects cellular uptake as well as the endocytosis mechanism of nanoparticles using a biomimetic microfluidic system that mimics the human dynamic environment. Positively charged amino-modified polystyrene nanoparticles (PSNs) at 100 μg/mL were delivered to cancer cells under static and biomimetic dynamic conditions (0...
October 19, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27757770/protective-effect-of-sesquiterpene-lactone-parthenolide-on-lps-induced-acute-lung-injury
#20
You Jin Jang, Moon Jung Back, Zhicheng Fu, Joo Hyun Lee, Jong Hoon Won, Hae Chan Ha, Hae Kyung Lee, Ji Min Jang, Jong Min Choi, Dae Kyong Kim
Acute lung injury (ALI) is a respiratory failure disease and the major source of mortality in the critically ill patients. The main pathological changes involved in ALI include the excessive recruitment and activation of neutrophils by increased pro-inflammatory mediators. However, any specific therapy for ALI has not been developed. The objective of this study was to investigate protective effects of parthenolide, a sesquiterpene lactone produced in feverfew, on LPS-induced lung injury. In the present study, parthenolide treatment reduced infiltration of inflammatory cells, airway permeability and production of pro-inflammatory cytokines in LPS-induced ALI mouse model...
October 18, 2016: Archives of Pharmacal Research
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