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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/28315259/scutellarin-protects-against-doxorubicin-induced-acute-cardiotoxicity-and-regulates-its-accumulation-in-the-heart
#1
Xi-Peng Sun, Li-Li Wan, Quan-Jun Yang, Yan Huo, Yong-Long Han, Cheng Guo
The clinical use of doxorubicin (DOX) is limited by its dose-dependent cardiotoxicity. The present study investigated the effects of scutellarin against DOX-induced cardiotoxicity in rats using pharmacodynamic and pharmacokinetic approaches. DOX (20 mg/kg) was injected intraperitoneally (i.p.) as a single dose, and scutellarin (5 mg/kg/day) was injected intravenously (i.v.) for 3 days. Rats treated with DOX showed acute cardiotoxicity as indicated by the elevated serum lactate dehydrogenase (LDH) activity (4057...
March 17, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28299617/methyl-caffeate-and-some-plant-constituents-inhibit-age-related-inflammation-effects-on-senescence-associated-secretory-phenotype-sasp-formation
#2
Hyun Lim, Byung Kyu Park, Sook Young Shin, Yong Soo Kwon, Hyun Pyo Kim
During aging, cells secrete molecules called senescence-associated secretory phenotype (SASP). They constitute chronic low-grade inflammation environment to adjacent cells and tissues. In order to find inhibiting agents of SASP formation, 113 plant constituents were incubated with BJ fibroblasts for 6 days after treatment with bleomycin. Several plant constituents showed considerable inhibition of IL-6 production, a representative SASP marker. These plant constituents included anthraquinones such as aurantio-obtusin, flavonoids including astragalin, iristectorigenin A, iristectorigenin B, linarin, lignans including lariciresinol 9-O-glucoside and eleutheroside E, phenylpropanoids such as caffeic acid and methyl caffeate, steroid (ophiopogonin), and others like centauroside, rhoifolin and scoparone...
March 15, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28275987/smenospongidine-suppresses-the-proliferation-of-multiple-myeloma-cells-by-promoting-ccaat-enhancer-binding-protein-homologous-protein-mediated-%C3%AE-catenin-degradation
#3
Seoyoung Park, In Hyun Hwang, Jiseon Kim, Young-Hwa Chung, Gyu-Young Song, MinKyun Na, Sangtaek Oh
Abnormal up-regulation of β-catenin expression is associated with the development and progression of multiple myeloma and is thus a potential therapeutic target. Here, we screened cell-based natural compounds and identified smenospongidine, a metabolite isolated from a marine sponge, as an antagonist of the Wnt/β-catenin signaling pathway. Smenospongidine promoted the degradation of intracellular β-catenin that accumulated via Wnt3a or 6-bromoindirubin-3'-oxime, an inhibitor of glycogen synthase kinase-3β...
March 8, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28258481/diarylheptanoids-suppress-proliferation-of-pancreatic-cancer-panc-1-cells-through-modulating-shh-gli-foxm1-pathway
#4
Guang-Zhi Dong, Ji Hye Jeong, Yu-Ih Lee, So Yoon Lee, Hui-Yuan Zhao, Raok Jeon, Hwa Jin Lee, Jae-Ha Ryu
Pancreatic cancer is one of the leading causes of cancer, and it has the lowest 5-year survival rates. It is necessary to develop more potent anti-pancreatic cancer drugs to overcome the fast metastasis and resistance to surgery, radiotherapy, chemotherapy, and combinations of these. We have identified several diarylheptanoids as anti-pancreatic cancer agents from Alpinia officinarum (lesser galangal) and Alnus japonica. These diarylheptanoids suppressed cell proliferation and induced the cell cycle arrest of pancreatic cancer cells (PANC-1)...
March 3, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28258480/the-anti-hsv-1-effect-of-quercetin-is-dependent-on-the-suppression-of-tlr-3-in-raw-264-7-cells
#5
Seulki Lee, Hwan Hee Lee, Yu Su Shin, Hyojeung Kang, Hyosun Cho
Quercetin is a major component of the plant Glycyrrhiza uralensis, which is largely used as a traditional medicine in Asia. Quercetin has been reported to have several biological activities, which include anti-viral and anti-inflammatory effects. We explored the molecular mechanism linking anti-viral and anti-inflammatory activities using an in vitro herpes simplex virus-1 (HSV-1) infection model. Raw 264.7 cells were infected with HSV-1 in the presence or absence of different concentrations of quercetin and infected cell lysates were harvested 24 h later...
March 3, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28251489/evaluation-of-the-inhibitory-effects-of-eckol-and-dieckol-isolated-from-edible-brown-alga-eisenia-bicyclis-on-human-monoamine-oxidases-a-and-b
#6
Hyun Ah Jung, Anupom Roy, Jee H Jung, Jae Sue Choi
Eckol and dieckol are important phlorotannins found in edible brown algae including Eisenia bicyclis, Ecklonia stolonifera, and others. Inhibition of monoamine oxidase (MAO) play an important role in the early management of Parkinson's disease (PD). The aim of this study was to determine the effectiveness of eckol and dieckol isolated from the methanolic extract of E. bicyclis against PD by the inhibition of human MAO-A and MAO-B (hMAO-A and hMAO-B). A sensitive enzyme-based chemiluminescent assay and kinetics methods were used to investigate enzyme inhibition and mode of inhibition...
March 1, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28243833/current-understanding-of-methamphetamine-associated-dopaminergic-neurodegeneration-and-psychotoxic-behaviors
#7
REVIEW
Eun-Joo Shin, Duy-Khanh Dang, The-Vinh Tran, Hai-Quyen Tran, Ji Hoon Jeong, Seung-Yeol Nah, Choon-Gon Jang, Kiyofumi Yamada, Toshitaka Nabeshima, Hyoung-Chun Kim
Clinical and preclinical studies have indicated that chronic methamphetamine (MA) use is associated with extensive neurodegeneration, psychosis, and cognitive impairment. Evidence from animal models has suggested a considerable role of excess dopamine or glutamate, oxidative stress, neuroinflammation, and apoptosis in MA-induced neurotoxicity, and that protein kinase Cδ might mediate the interaction among these factors. In addition, the relatively long-lasting and recurrent nature of MA psychosis has been reproduced in animals treated with various dosing regimens of MA, which have shown behavioral sensitization, sociability deficits, and impaired prepulse inhibition...
February 28, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28229392/determination-of-rabeprazole-enantiomers-in-commercial-tablets-using-immobilized-cellulose-based-stationary-phase
#8
Miri Kim, Su Kyung Yu, Quoc-Ky Truong, Xuan-Lan Mai, Hyun Kyu Chung, Jong-Seong Kang, Kyeong Ho Kim
Rabeprazole is one of the latest proton-pump inhibitors used for treatment of several gastrointestinal disorders. For therapeutic applications, rabeprazole has been administered as a mixture of R-(+) and S-(-) enantiomers. Owing to pharmacological and toxicological differences between stereoisomers, chiral recognition has now become an integral part of drug research and development. A simple and rapid liquid chromatographic method for enantioselective separation and determination of R-(+) and S-(-) enantiomers of rabeprazole in bulk drug and pharmaceutical formulations was developed...
February 22, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28229391/kudsuphilactone-b-a-nortriterpenoid-isolated-from-schisandra-chinensis-fruit-induces-caspase-dependent-apoptosis-in-human-ovarian-cancer-a2780-cells
#9
Miran Jeong, Hye Mi Kim, Hyun Ji Kim, Jung-Hye Choi, Dae Sik Jang
A phytochemical study on the fruits of Schisandra chinensis led to the isolation and characterization of nineteen compounds. The structures of the isolates were determined to be schizandrin, deoxyschizandrin, angeloylgomisin H, gomisin A, gomisin J, (-)-gomisin L1, (-)-gomisin L2, wuweizisu C, gomisin N, meso-dihydroguaiaretic acid, kadsuphilactone B, α-ylangenol, α-ylangenyl acetate, β-chamigrenal, β-chamigrenic acid, 4-hydroxybenzoic acid, protocatechuic acid, p-methylcarvacrol, and indole-3-acetic acid...
February 22, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28211012/f4-80-inhibits-osteoclast-differentiation-via-downregulation-of-nuclear-factor-of-activated-t-cells-cytoplasmic-1
#10
Ju-Hee Kang, Jung-Sun Sim, Ting Zheng, Mijung Yim
Osteoclastogenesis is an essential process in bone metabolism, which can be induced by RANKL stimulation. The F4/80 glycoprotein is a member of the EGF-transmembrane 7 (TM7) family and has been established as a specific cell-surface marker for murine macrophages. This study aimed to identify the role of F4/80 in osteoclastogenesis. Using mouse bone marrow-derived macrophages (BMMs), we observed that the mRNA level of F4/80 was dramatically reduced as these cells differentiated into osteoclasts. Furthermore, osteoclastogenesis was decreased in F4/80(high) BMMs compared to F4/80(-/low) BMMs...
February 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28211011/teoa-a-triterpenoid-from-actinidia-eriantha-induces-autophagy-in-sw620-cells-via-endoplasmic-reticulum-stress-and-ros-dependent-mitophagy
#11
Dandan Zhang, Cuixia Gao, Ruyi Li, Lin Zhang, Jingkui Tian
2α,3α,24-Thrihydroxyurs-12-en-28-oicacid (TEOA), a pentacyclic triterpenoid, isolated from the roots of Actinidia eriantha, exhibits significant cytotoxicity against SW620, BGC-823, HepG-2, A549 and PC-3 cancer cells. In this study, we investigated the underlying molecular mechanism of the anticancer activity of TEOA in SW620 cells. We demonstrated that TEOA induced apoptosis through cleavage of caspase-9 and PARP in SW620 cells. In addition, evidence of TEOA-mediated autophagy included the induction of autophagolysosomes and activation of autophagic markers LC-3B and p62...
February 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28205012/determination-of-urazamide-in-pharmaceutical-preparation-with-room-temperature-ionic-liquid
#12
Narae Seo, Yoo Rim Lee, Hyun Sun Park, Quoc-Ky Truong, Jae-Yong Lee, Hyun Kyu Chung, Yusung Choi, Byeonghee Kim, Sang Beom Han, Kyeong Ho Kim
A high performance liquid chromatographic method was developed and validated for the determination of urazamide in pharmaceutical preparation with novel green aqueous mobile phase modified with room temperature ionic liquids (RTILs). 1-Ethyl-3-methyl-imidazolium tetrafluoroborate ([EMIM][BF4]) was selected as a mobile phase additive to improve retention and avoid baseline disturbances at t0. Various mobile phase parameters such as cation moiety, chaotropic anion moiety, pH and concentration of RTILs were optimized to determine urazamide at the proper retention time...
February 15, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28194702/studies-on-the-reactions-of-3-2-polymethylene-2-phenylbenzo-b-1-10-phenanthrolines-with-ru-tpy-cl3-and-properties-of-the-products
#13
Yang Lu, A F M Motiur Rahman, Yurngdong Jahng
A series of 3,2-polymethylene-2-phenylbenzo[b]-1,10-phenanthrolines was reacted with Ru(tpy)Cl3 to afford two ruthenium (Ru) complexes, a pentaaza-coordinated (N5Cl) complex [Ru(tpy)(L)Cl](+) and a hexa-coordinated (N5C) complex [Ru(tpy)(L)](+). The ratio of these two complexes was found to be highly dependent on the length of the polymethylene bridge between terminal phenyl and central pyridine rings. The reaction between the dimethylene-bridged ligand and Ru(tpy)Cl3 afforded a hexa-coordinated (N5C) complex as an only isolatable product in 83% yield, while the others afforded pentaaza-coordinated products and hexa-coordinated products in ratios of 1:1...
February 13, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28160136/geniposide-attenuates-the-level-of-a%C3%AE-1-42-via-enhancing-leptin-signaling-in-cellular-and-app-ps1-transgenic-mice
#14
Zixuan Liu, Yonglan Zhang, Jianhui Liu, Fei Yin
An large body of evidence indicates that leptin has protective role against Alzheimer's disease, where it reduces β-amyloid (Aβ) production in both cell culture and animal models. Our previous studies revealed that geniposide could attenuate the production of Aβ1-42 and antagonize the neurotoxicity of Aβ1-42 in neurons. However, the mechanism that underlies these effects remains to be clarified. To investigate whether leptin signaling is involved in regulating the production of Aβ1-42 by geniposide, we treated primary neurons with leptin antagonist (LA), and determined the influence of LA on the activities of leptin signaling molecules and the expressions of secretases associated with the production of Aβ1-42...
February 3, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28110416/lasiokaurin-derivatives-synthesis-antimicrobial-and-antitumor-biological-evaluation-and-apoptosis-inducing-effects
#15
Da-Hong Li, Ping Hu, Sheng-Tao Xu, Chun-Yan Fang, Shuang Tang, Xin-Yu Wang, Xing-Yan Sun, He Li, Ying Xu, Xiao-Ke Gu, Jin-Yi Xu
Herein, a series of lasiokaurin derivatives were designed and synthesized. All the derivatives together with lasiokaurin and oridonin were tested for their antimicrobial and antiproliferative activity. Compound 16 showed the most promising antimicrobial activity with MICs of 2.0 and 1.0 μg/mL against Gram-Positive bacteria S. aureus and B. subtilis, respectively. All the synthetic lasiokaurin derivatives showed better antiproliferative activity than parent compound lasiokaurin 1. Compound 10 exhibited the strongest cytotoxicity with IC50 values of 0...
January 21, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28108939/exploration-of-sar-for-novel-2-benzylbenzimidazole-analogs-as-inhibitor-of-transcription-factor-nf-%C3%AE%C2%BAb
#16
PullaReddy Boggu, Eeda Venkateswararao, Manoj Manickam, Youngsoo Kim, Sang-Hun Jung
A novel series of 2-benzylbenzimidazole analogs was designed, synthesized and investigated for their in vitro activities against LPS induced NF-κB inhibition in RAW 264.7 cells using the SEAP assay. Among them, 4-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6e, >100% inhibition at 30 μM, IC50 = 3.0 μM), 4-((5-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6j, 96% inhibition at 30 μM, IC50 = 4.0 μM) and 2-((4-(cyclohexylmethoxy)-1H-benzo[d]imidazol-2-yl)methyl)phenol (6k, 95% inhibition at 30 μM, IC50 = 5...
January 20, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28101738/synthesis-of-novel-oleanolic-acid-and-ursolic-acid-in-c-28-position-derivatives-as-potential-anticancer-agents
#17
Tian Tian, Xinyu Liu, Eung-Seok Lee, Jingyang Sun, Zhonghua Feng, Longxuan Zhao, Chunhui Zhao
A series of nitrogen-containing derivatives of oleanolic acid and ursolic acid were prepared by a modification at C-28 position via esterification with 2-hydroxyacetic acid followed by amidation with amines, such as piperazine, N-methylpiperazine, and alkane-1, 2-diamines, alkane-1, 4-diamines, alkane-1, 6-diamines. In vitro antiproliferative activities of the compounds prepared towards MCF-7, Hela and A549 cell lines were evaluated by a MTT method to show that OA-5a, OA-5b, OA-5c and UA-5a showed somewhat improved antiproliferative activities against MCF-7, Hela and A549 cells comparing to that of the positive control, gefitinib...
January 18, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28101737/spatholobus-suberectus-dunn-constituents-inhibit-sortase-a-and-staphylococcus-aureus-cell-clumping-to-fibrinogen
#18
Hyunjoo Cho, Beomkoo Chung, Chang-Kwon Kim, Dong-Chan Oh, Ki-Bong Oh, Jongheon Shin
Sortases are a family of Gram-positive transpeptidases responsible for anchoring surface protein virulence factors to the peptidoglycan cell wall layer. In Staphylococcus aureus (S. aureus), deletion of sortase isoform results in a significant reduction in virulence and infection potential. Twenty flavonoids were isolated from the stem of the folk medicinal plant Spatholobus suberectus Dunn. These compounds were tested against S. aureus-derived sortase A (SrtA), a key transpeptidase for bacterial virulence...
January 18, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28093699/anti-alzheimer-s-disease-activity-of-compounds-from-the-root-bark-of-morus-alba-l
#19
Eun Bi Kuk, A Ra Jo, Seo In Oh, Hee Sook Sohn, Su Hui Seong, Anupom Roy, Jae Sue Choi, Hyun Ah Jung
The inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE1) plays important roles in prevention and treatment of Alzheimer's disease (AD). Among the individual parts of Morus alba L. including root bark, branches, leaves, and fruits, the root bark showed the most potent enzyme inhibitory activities. Therefore, the aim of this study was to evaluate the anti-AD activity of the M. alba root bark and its isolate compounds, including mulberrofuran G (1), albanol B (2), and kuwanon G (3) via inhibition of AChE, BChE, and BACE1...
January 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28084586/amelioration-of-high-fat-diet-induced-nephropathy-by-cilostazol-and-rosuvastatin
#20
Jeong-Hyeon Park, Bo-Hyun Choi, Sae-Kwang Ku, Dong-Hyun Kim, Kyeong-Ah Jung, Euichaul Oh, Mi-Kyoung Kwak
Multiple comorbidities of metabolic disorders are associated with facilitated chronic kidney disease progression. Anti-platelet cilostazol is used for the treatment of peripheral artery disease. In this study, we investigated the potential beneficial effects of cilostazol and rosuvastatin on metabolic disorder-induced renal dysfunctions. C57BL/6 mice that received high fat diet (HFD) for 22 weeks and a low dose of streptozotocin (STZ, 40 mg/kg) developed albuminuria and had increased urinary cystatin C excretion, and cilostazol treatment (13 weeks) improved these markers...
January 13, 2017: Archives of Pharmacal Research
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