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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/28101738/synthesis-of-novel-oleanolic-acid-and-ursolic-acid-in-c-28-position-derivatives-as-potential-anticancer-agents
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
https://www.readbyqxmd.com/read/28035554/a-new-saponin-from-acanthopanax-koreanum-with-anti-inflammatory-activity
#12
Le Duc Dat, Nguyen Phuong Thao, Bui Thi Thuy Luyen, Bui Huu Tai, Mi Hee Woo, Zahid Manzoor, Irshad Ali, Young Sang Koh, Young Ho Kim
Twelve saponins were isolated from the leaves of Acanthopanax koreanum, including one new lupane-type triterpene glycoside, named acankoreoside R (1), together with 11 known triterpenoid saponins (2-12). Their structures were elucidated by 1D and 2D nuclear magnetic resonance (NMR), mass spectroscopic data (MS). All of the fractions and isolated saponins were evaluated for anti-inflammatory activities in lipopolysaccharide (LPS)-stimulated bone marrow-derived dendritic cells (BMDCs) by ELISA. Among them, compounds 1-5, 7, 10, and 12 showed strong inhibitions towards interleukin-12 (IL-12) production with IC50 values ranging from 1...
December 29, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28032317/cinnamomulactone-a-new-butyrolactone-from-the-twigs-of-cinnamomum-cassia-and-its-inhibitory-activity-of-matrix-metalloproteinases
#13
Geum Jin Kim, Jong Yeong Lee, Hyun Gyu Choi, So Young Kim, Eonmi Kim, Sang Hee Shim, Joo-Won Nam, Sang-Hyun Kim, Hyukjae Choi
Cinnamomum cassia (Lauraceae) has long been used as one of the most frequently used traditional oriental medicines for the treatment of gastritis, diabetes, blood circulation disturbance and inflammatory diseases. Cinnamomulactone (1), a new butyrolactone was isolated from the twigs of C. cassia together with nine known compounds, coumarin (2), trans-cinnamic acid (3), cinnamaldehyde (4), 2-hydroxycinnamaldehyde (5), 2-methoxycinnamaldehyde (6), 2-hydroxy-cinnamyl alcohol (7), benzoic acid (8), (+)-syringaresinol (9) and phenethyl (E)-3-[4-methoxyphenyl]-2-propenoate (10)...
December 28, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28028696/synthesis-and-anti-mycobacterial-activity-of-4-4-phenyl-1h-1-2-3-triazol-1-yl-salicylhydrazones-revitalizing-an-old-drug
#14
Hajjaj H M Abdu-Allah, Bahaa G M Youssif, Mostafa H Abdelrahman, Mohammed K Abdel-Hamid, Rudraraju Srilakshmi Reshma, Perumal Yogeeswari, Tarek Aboul-Fadl, Dharmarajan Sriram
The antitubercular drug; para-aminosalicylic acid (PAS) was used as the core scaffold for the design of a series of 1H-1,2,3-triazolylsalicylhydrazones upon coupling with triazole and arylhydrazone moietis to furnish a single molecular architecture. The obtained derivatives were screened against Mycobacterium tuberculosis H37Rv revealing good to high activity for the active compounds (MIC values of 0.39-1.5 μg/mL) compared to the marketed drugs isoniazid, rifampicin and ethambutol. Moreover, the most active analogue N-(1-(4-chlorobenzyl)-2-oxoindolin-3-ylidene)-2-hydroxy-4-(4-phenyl-1H-1,2,3-triazol-1-yl)-benzohydrazide (20) was found to be ten-fold more potent than PAS and equipotent to rifampicin (MIC 0...
December 27, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28028695/5-fluorouracil-inhibits-cell-migration-by-induction-of-sestrin2-in-colon-cancer-cells
#15
Kyuhwa Seo, Sung Hwan Ki, Eun Young Park, Sang Mi Shin
5-Fluorouracil (5-FU) is a chemotherapeutic agent used in the treatment of colorectal cancer. In this study, we investigated whether 5-FU induces Sestrin2 (SESN2), an antioxidant enzyme, and the role of SESN2 in 5-FU action in colon cancer cells. We found that 5-FU upregulated SESN2 protein expression in both HCT116 and HT29 cells. It also increased transcripts of SESN1 and SESN2, but not of SESN3. Furthermore, we investigated whether production of reactive oxygen species (ROS) was involved in 5-FU-induced SESN2 expression...
December 27, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28028694/a-new-model-of-flavonoids-affinity-towards-p-glycoprotein-genetic-algorithm-support-vector-machine-with-features-selected-by-a-modified-particle-swarm-optimization-algorithm
#16
Ying Cui, Qinggang Chen, Yaxiao Li, Ling Tang
Flavonoids exhibit a high affinity for the purified cytosolic NBD (C-terminal nucleotide-binding domain) of P-glycoprotein (P-gp). To explore the affinity of flavonoids for P-gp, quantitative structure-activity relationship (QSAR) models were developed using support vector machines (SVMs). A novel method coupling a modified particle swarm optimization algorithm with random mutation strategy and a genetic algorithm coupled with SVM was proposed to simultaneously optimize the kernel parameters of SVM and determine the subset of optimized features for the first time...
December 27, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28013489/rsk2-and-its-binding-partners-in-cell-proliferation-transformation-and-cancer-development
#17
REVIEW
Yong-Yeon Cho
RSK2 is a serine/threonine kinase and a member of the p90 ribosomal S6 kinase (p90(RSK); RSKs) family, which regulates cell proliferation and transformation induced by tumor promoters such as epithelial growth factor (EGF), 12-O-tetradecanoylphorbol-13-acetate (TPA), and ultraviolet (UV) radiation. RSKs respond to many growth factors, hormones, neurotransmitters and environmental stresses. In signaling cascades, RSK2 is regulated under the control of extracellular signal-regulated kinase 1 (ERK1) and 2 (ERK2) activities and is positioned upstream of transcription and epigenetic factors involved in cell proliferation, cell transformation and cancer development, as well as some kinases that modulate cell cycle progression...
December 24, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28012047/the-protective-mechanism-of-qgc-in-feline-esophageal-epithelial-cells-by-interleukin-1%C3%AE-treatment
#18
Hyun Soo Jang, Seung In Um, Sung Hee Lee, Wan Kyunn Whang, Young Sil Min, Sun Young Park, Uy Dong Sohn
In a previous study, Quercetin-3-O-β-D-glucuronopyranoside (QGC) has anti-oxidative and anti-inflammatory effects in vivo. QGC is a flavonoid glucoside extracted from Rumex Aquaticus. We investigated the downstream target proteins involved in IL-1β-stimulated ROS production and the ability of QGC to inhibit ROS production. Cell viability was determined using the MTT reduction assay. Western blot analysis was performed with antibodies to investigate the activation of three MAPKs, NF-κB, and phosphorylated IκB-α (pIB), and the expression of COX-2...
December 23, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27988882/beneficial-effects-of-the-src-inhibitor-dasatinib-on-breakdown-of-the-blood-retinal-barrier
#19
So Ra Kim, Wonhee Suh
Src kinase signaling is important in the regulation of microvascular barrier function and endothelial hyperpermeability. This study was designed to evaluate the protective effect of dasatinib, a potent Src inhibitor used clinically for the treatment of cancer, against the breakdown of the blood-retinal barrier (BRB) and the retinal vascular leakage caused by vascular endothelial growth factor (VEGF) and diabetes. We examined the effects of dasatinib on VEGF-induced endothelial hyperpermeability and the loss of vascular endothelial (VE)-cadherin, an endothelial junctional protein...
December 17, 2016: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/27988881/rapid-analysis-of-drugs-of-abuse-and-their-metabolites-in-human-urine-using-dilute-and-shoot-liquid-chromatography-tandem-mass-spectrometry
#20
Tae Yeon Kong, Ju Hyun Kim, Jin Young Kim, Moon Kyo In, Kyung Ho Choi, Hee Seung Kim, Hye Suk Lee
Liquid chromatography-tandem mass spectrometric method for analysis of 113 abuse drugs and their metabolites in human urine was developed and validated. A simple sample clean-up procedure using the "dilute and shoot" approach, followed by reversed phase separation, provided a fast and reliable method for routine analysis. Drugs were separated in a Capcell Pak MG-III C18 column using a gradient elution of 1 mM ammonium formate with 0.1% formic acid in water and acetonitrile. The total time for analysis was 32 min...
December 17, 2016: Archives of Pharmacal Research
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