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Archives of Pharmacal Research

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https://www.readbyqxmd.com/read/28547390/mono-substitution-effects-on-antimicrobial-activity-of-stapled-heptapeptides
#1
Huy X Luong, Do-Hee Kim, Ngoan T Mai, Bong-Jin Lee, Young-Woo Kim
We previously reported a de novo design of antimicrobial heptapeptide helices using Verdine's all-hydrocarbon peptide stapling system. One of the important structure-activity relationships we found from these previous studies was that extending of the hydrophobic face by replacing of alanine with leucine in positon 5 increases antimicrobial activity. In this study, to further improve the activity profile of this peptide series, we investigated the substitution effects of position 5 on conformational and proteolytic stability as well as antimicrobial and hemolytic activity...
May 25, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28547389/anti-inflammation-compounds-from-the-seedpods-of-pongamia-pinnata-l-pierre-guided-by-the-bioactivity-and-uplc-hresims
#2
Hong Guo, Zisong Bai, Yangyang Xu, Xueqin Wu, Ning Li, Yan Zhu, Xiaoming Wang, Peng Zhang
Pongamia pinnata (Linn.) Pierre has anti-inflammatory activity and could significantly decrease serum tumor necrosis factor-α and IL-10 in arthritic rats. Previous research indicated the typical chemical constituent in P. pinnata is furanoflavone. Guided by anti-inflammatory active assay and UPLC-HRESIMS chromatography, 22 compounds were isolated from the ethanol extract of P. pinnata seedpods. One novel furanoflavone, 4'-hydroxypinnatin, was elucidated by HRESIMS, 1D- and 2D-NMR spectra. The 21 known compounds, including 9 furanoflavone, were identified by comparing their NMR data with the previous data in reference...
May 25, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28508944/suppressive-effects-of-zingerone-on-tgfbip-mediated-septic-responses
#3
Gahee Min, Sae-Kwang Ku, Taeho Lee, Jong-Sup Bae
Zingerone (ZGR), a phenolic alkanone isolated from ginger, has been reported to possess various pharmacological activities. Transforming growth factor β-induced protein (TGFBIp) is an extracellular matrix protein whose expression in several cell types is greatly increased by TGF-β. TGFBIp is released by human umbilical vein endothelial cells and functions as a mediator of experimental sepsis. We hypothesized that ZGR could reduce TGFBIp-mediated severe inflammatory responses in human endothelial cells and mice...
May 16, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28508182/new-antimicrobial-flavonoids-and-chalcone-from-colutea-armata
#4
Farah Inamullah, Itrat Fatima, Sadia Khan, Mehdi Hassan Kazmi, Abdul Malik, Rasool Bakhsh Tareen, Tanveer Abbas
Colucins A (1) and B (2), new flavonoids and colucone (3), the new chalcone derivative, have been isolated from the CHCl3-soluble fraction of the whole plant of Colutea armata along with luteolin (4), luteolin 7-O-β-D-glucoside (5), isoliquiritigenin (6), trans-caffeic acid (7) and stigmasterol (8) reported for the first time from this species. Their structures were elucidated by spectroscopic techniques including MS and 2D-NMR spectroscopy. Compounds 1 and 2 showed significant antimicrobial activity against two Gram positive and three Gram negative bacterial strains while 3 was moderately active...
May 15, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28501973/neuroprotective-compounds-from-reynoutria-sachalinensis
#5
Min Rye Eom, Jin Bae Weon, Youn Sik Jung, Ga Hee Ryu, Woo Seung Yang, Choong Je Ma
Glutamate is a neurotransmitter in central nervous system. Overexpression of glutamate leads to oxidative stress, resulting in several neurodegenerative disorders that include Alzheimer's disease. The n-hexane fraction of stems and ethyl acetate (EtOAc) fraction of flowers of Reynoutria sachalinensis provide neuroprotection against glutamate-induced oxidative toxicity in HT22 cells. In this study, 1-decanol (1), β-amyrin (2), dammaran-3β-ol (3), campesterol (4), daucosterol (5), ergosterol peroxide (6), emodin 8-O-β-D-glucopyranoside (7), quercetin (8) and isoquercitrin (9) were isolated from n-hexane fractions of stems and EtOAc fractions of flowers of R...
May 13, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28484907/inhibition-of-cytochrome-p450-and-uridine-5-diphospho-glucuronosyltransferases-by-mam-2201-in-human-liver-microsomes
#6
Tae Yeon Kong, Ju-Hyun Kim, Soon-Sang Kwon, Jae Chul Cheong, Hee Seung Kim, Moon Kyo In, Hye Suk Lee
MAM-2201, a synthetic cannabinoid, is a potent agonist of the cannabinoid receptors and is increasingly used as an illicit recreational drug. The inhibitory effects of MAM-2201 on major drug-metabolizing enzymes such as cytochrome P450s (CYPs) and uridine 5'-diphospho-glucuronosyltransferases (UGTs) have not yet been investigated although it is widely abused, sometimes in combination with other drugs. We evaluated the inhibitory effects of MAM-2201 on eight major human CYPs (CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4) and six UGTs (UGTs 1A1, 1A3, 1A4, 1A6, 1A9, and 2B7) of pooled human liver microsomes; we thus explored potential MAM-2201-induced drug interactions...
May 8, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28456911/qsar-based-therapeutic-management-of-m-tuberculosis
#7
REVIEW
Shahzaib Ahamad, Safikur Rahman, Faez Iqbal Khan, Neeraja Dwivedi, Sher Ali, Jihoe Kim, Md Imtaiyaz Hassan
Mycobacterium tuberculosis is responsible for severe mortality and morbidity worldwide but, under-developed and developing countries are more prone to infection. In search of effective and wide-spectrum anti-tubercular agents, interdisciplinary approaches are being explored. Of the several approaches used, computer based quantitative structure activity relationship (QSAR) have gained momentum. Structure-based drug design and discovery implies a combined knowledge of accurate prediction of ligand poses with the good prediction and interpretation of statistically validated models derived from the 3D-QSAR approach...
April 29, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28439780/angelica-keiskei-an-emerging-medicinal-herb-with-various-bioactive-constituents-and-biological-activities
#8
REVIEW
Yun-Seo Kil, Sally T Pham, Eun Kyoung Seo, Mahtab Jafari
Angelica keiskei (Miq.) Koidz. (Umbelliferae) has traditionally been used to treat dysuria, dyschezia, and dysgalactia as well as to restore vitality. Recently, the aerial parts of A. keiskei have been consumed as a health food. Various flavonoids, coumarins, phenolics, acetylenes, sesquiterpene, diterpene, and triterpenes were identified as the constituents of A. keiskei. The crude extracts and pure constituents were proven to inhibit tumor growth and ameliorate inflammation, obesity, diabetics, hypertension, and ulcer...
April 24, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28397193/synthesis-and-anti-inflammatory-activities-of-novel-dihydropyranoaurone-derivatives
#9
Zheng Wang, Eun Ju Bae, Young Taek Han
A novel series of dihydropyranoaurone derivatives were synthesized and evaluated as potential anti-inflammatory agents. Late-stage derivatization by versatile piperazine-catalyzed aldol reaction between dihydropyanobenzofuran intermediate 2 and diverse aldehydes readily afforded the novel dihydropyranoaurone analogs. Evaluation of the synthesized dihydropyranoaurone derivatives and related compounds regarding their inhibiting inducible nitric oxide synthase and nitrite production of lipopolysaccaride-stimulated RAW 264...
April 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28397192/effects-of-asarinin-on-dopamine-biosynthesis-and-6-hydroxydopamine-induced-cytotoxicity-in-pc12-cells
#10
Hyun Jin Park, Kyung Sook Lee, Ting Ting Zhao, Kyung Eun Lee, Myung Koo Lee
This study investigated the effects of asarinin on dopamine biosynthesis and 6-hydroxydopamine (6-OHDA)-induced cytotoxicity in rat adrenal pheochromocytoma (PC12) cells. Treatment with asarinin (25-50 μM) increased intracellular dopamine levels and enhanced L-DOPA-induced increases in dopamine levels. Asarinin (25 μM) induced cyclic AMP-dependent protein kinase A (PKA) signaling, leading to increased cyclic AMP-response element binding protein (CREB) and tyrosine hydroxylase (TH) phosphorylation, which in turn stimulated dopamine production...
April 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28386742/4-parvifuran-inhibits-metastatic-and-invasive-actions-through-the-jak2-stat3-pathway-in-osteosarcoma-cells
#11
Hyung-Mun Yun, Kyung-Ran Park, Tran Hong Quang, Hyuncheol Oh, Jin Tae Hong, Youn-Chul Kim, Eun-Cheol Kim
This study was performed to examine the anticancer and anti-metastatic effects of 4-parvifuran (PVN), a novel flavonoid isolated from the heartwood of Dalbergia odorifera, and to study its underlying signaling pathway in human osteosarcoma cells. In the present study, PVN was found to inhibit cell proliferation in a concentration- and time-dependent manner in the human osteosarcoma cell lines studied (MG-63 and U-2 OS) and induce apoptosis, as evidenced by Annexin V(+) and TUNEL(+) cells. Cleaved poly (ADP-ribose) polymerase (PARP) and caspase-3 were up-regulated while anti-apoptotic proteins including Bcl-2, Bcl-xL, and survivin were down-regulated after treatment with PVN...
April 6, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28378219/cardioprotective-effect-of-kr-33889-a-novel-parp-inhibitor-against-oxidative-stress-induced-apoptosis-in-h9c2-cells-and-isolated-rat-hearts
#12
Eun-Seok Park, Do-Hyun Kang, Jun Chul Kang, Yong Chang Jang, Min-Ju Lee, Hun-Jong Chung, Kyu Yang Yi, Dae-Eun Kim, Bokyung Kim, Hwa-Sup Shin
Oxidative stress plays a critical role in cardiac injury during ischemia/reperfusion (I/R). Despite a potent cardioprotective activity of KR-33889, a novel poly (ADP-ribose) polymerase inhibitor, its underlying mechanism remains unresolved. This study was designed to investigate the protective effects of KR-33889 against oxidative stress-induced apoptosis in rat cardiomyocytes H9c2 cells and isolated rat hearts. H2O2 caused severe injury to H9c2 cells, mainly due to apoptosis, as revealed by TUNEL assay. However, KR-33889 pretreatment significantly attenuated H2O2-induced apoptosis of H9c2 cells, which was accompanied by decrease in expression of both cleaved caspase-3 and Bax and increase in Bcl-2 expression and the ratio of Bcl-2/Bax...
April 4, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28315259/scutellarin-protects-against-doxorubicin-induced-acute-cardiotoxicity-and-regulates-its-accumulation-in-the-heart
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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/28229392/determination-of-rabeprazole-enantiomers-in-commercial-tablets-using-immobilized-cellulose-based-stationary-phase
#19
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...
March 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/28205012/determination-of-urazamide-in-pharmaceutical-preparation-with-room-temperature-ionic-liquid
#20
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...
March 2017: Archives of Pharmacal Research
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