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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/28229392/determination-of-rabeprazole-enantiomers-in-commercial-tablets-using-immobilized-cellulose-based-stationary-phase
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
https://www.readbyqxmd.com/read/28083853/design-synthesis-and-pharmacological-analysis-of-5-4-substituted-methyl-1-1-biphenyl-2-yl-1h-tetrazoles
#14
Atulkumar Kamble, Ravindra Kamble, Suneel Dodamani, Sunil Jalalpure, Vijaykumar Rasal, Mahadev Kumbar, Shrinivas Joshi, Sheshagiri Dixit
In the present paper 5-[4'-({4-[(4-aryloxy)methyl]-1H-1,2,3-triazol-1-yl}methyl)[1,1'-biphenyl]-2-yl]-1H-tetrazoles (5a-g) and [2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl-substituted-1-carbodithioates (11h-q) have been designed and synthesized. These compounds were subjected to docking (against AT1 receptor protein enzyme in complex with Lisinopril), in vitro angiotensin converting enzyme inhibition, anti-proliferative, anti-inflammatory screening (through egg albumin denaturation inhibition and red blood cell membrane stabilization assay) and finally anti-fungal activity analyses...
January 12, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28078525/chitosan-ceramide-coating-on-gold-nanorod-to-improve-its-physiological-stability-and-reduce-the-lipid-surface-related-toxicity
#15
Gantumur Battogtokh, Oyuntuya Gotov, Young Tag Ko
Gold nanoparticles are promising materials for many applications that include imaging, drug delivery, and photothermal therapy. However, AuNPs can be unstable and/or toxic. We purposed to improve the stability and reduce toxicity of gold nanorods (AuNR) upon coating with biocompatible polymer, chitosan-ceramide (CS-CE), without replacing the original layer, CTAB. CS-CE-coated AuNR was prepared by simple mixing for 24 h and purified by centrifugation. The coating was confirmed by UV-Vis absorption analysis and surface charge and size measurement...
January 11, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28074398/liquid-chromatographic-enantiomer-separation-of-1-naphthylamides-of-chiral-acids-using-several-amylose-and-cellulose-derived-chiral-stationary-phases
#16
Md Fokhrul Islam, Suraj Adhikari, Man-Jeong Paik, Wonjae Lee
The liquid chromatographic enantiomer separation of various chiral acids as 1-naphthylamides was performed using several chiral stationary phases (CSPs). The CSPs used in this study were six covalently bonded and four coated type CSPs derived from amylose and cellulose derivatives as chiral selectors. The degree of enantioseparation is affected by the structure of chiral acids and the CSPs used, which have different chiral selectors and types of immobilization. For the enantiomer resolution of chiral acids as 1-naphthylamide derivatives, the performance of the coated type Lux Cellulose-1 was superior to those of the other CSPs, except for 2-aryloxypropionic acid derivatives...
January 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28074397/anti-inflammatory-effects-of-secondary-metabolites-isolated-from-the-marine-derived-fungal-strain-penicillium-sp-sf-5629
#17
Nguyen Thi Thanh Ngan, Tran Hong Quang, Kwan-Woo Kim, Hye Jin Kim, Jae Hak Sohn, Dae Gill Kang, Ho Sub Lee, Youn-Chul Kim, Hyuncheol Oh
After the chemical investigation of the ethyl acetate extract of the marine-derived fungal strain Penicillium sp. SF-5629, the isolation and structural elucidation of eight secondary metabolites, including (3R,4S)-6,8-dihydroxy-3,4,7-trimethylisocoumarin (1), (3S,4S)-sclerotinin A (2), penicitrinone A (3), citrinin H1 (4), emodin (5), ω-hydroxyemodin (6), 8-hydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylate (7), and 3,8-dihydroxy-6-methyl-9-oxo-9H-xanthene-1-carboxylate (8) were carried out. Evaluation of the anti-inflammatory activity of these metabolites showed that 4 inhibited nitric oxide and prostaglandin E2 production in lipopolysaccharide-stimulated BV2 microglia, with IC50 values of 8...
January 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28063015/innate-immunity-against-legionella-pneumophila-during-pulmonary-infections-in-mice
#18
REVIEW
Bonggoo Park, Gayoung Park, Jiyoung Kim, Seon Ah Lim, Kyung-Mi Lee
Legionella pneumophila is an etiological agent of the severe pneumonia known as Legionnaires' disease (LD). This gram-negative bacterium is thought to replicate naturally in various freshwater amoebae, but also replicates in human alveolar macrophages. Inside host cells, legionella induce the production of non-endosomal replicative phagosomes by injecting effector proteins into the cytosol. Innate immune responses are first line defenses against legionella during early phases of infection, and distinguish between legionella and host cells using germline-encoded pattern recognition receptors such as Toll-like receptors , NOD-like receptors, and RIG-I-like receptors, which sense pathogen-associated molecular patterns that are absent in host cells...
January 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28054176/oleanane-triterpenoids-from-akebiae-caulis-exhibit-inhibitory-effects-on-a%C3%AE-42-induced-fibrillogenesis
#19
Md Anisuzzaman Chowdhury, Hae Ju Ko, Hwan Lee, Md Aminul Haque, Il-Seon Park, Dong-Sung Lee, Eun-Rhan Woo
Previous phytochemical investigations of Akebiae Caulis resulted in the isolation of triterpenes, triterpene glycosides, phenylethanoid glycosides and megastigmane glycoside. Amyloid beta (Aβ), the main component of the senile plaques detected in Alzheimer's disease, induces cell death. However, only a limited number of studies have addressed the biological and pharmacological effects of Akebiae Caulis. In particular, the inhibitory activity of Akebiae Caulis against Aβ42 fibrillogenesis remains unclear. Herein, a new triterpene glycoside, akequintoside F (1), along with nine known compounds pulsatilla saponin A (2), collinsonidin (3), akebonic acid (4), hederagenin (5), 1-(3',4'-dihydroxycinnamoyl) cyclopentane-2,3-diol (6), asperosaponin C (7), leontoside A (8), quinatic acid (9), and quinatoside A (10) were isolated from Akebiae Caulis using repeated column chromatography with silica gel, LiChroprep RP-18, and MCI gel...
January 4, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28040846/design-synthesis-and-evaluation-of-5-substituted-1-h-tetrazoles-as-potent-anticonvulsant-agents
#20
Ai-Mei Liao, Tiantian Wang, Bangrong Cai, Yi Jin, Seunghoon Cheon, ChangJu Chun, Zengtao Wang
A series of 5-substituted 1-H-tetrazoles were designed and synthesized as potent anticonvulsant agents. Their preliminary anticonvulsant activities were evaluated using maximal electroshock and subcutaneous pentylenetetrazole (scPTZ) seizure tests. Neurotoxicity was determined using rotarod test. The results indicated that the compound 2j in scPTZ model exhibited the ED50 values of 83.3 mg/kg, superior to the standard drug ethosuximide with the maximum activity. In addition, compound 2k showed the most potent activity in MES model with ED50 value of 9...
December 31, 2016: Archives of Pharmacal Research
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