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Archives of Pharmacal Research

Sang Jae Lee, Dong-Gyun Kim, Kyu-Yeon Lee, Ji Sung Koo, Bong-Jin Lee
Oxidative stresses, such as reactive oxygen species, reactive electrophilic species, reactive nitrogen species, and reactive chlorine species, can damage cellular components, leading to cellular malfunction and death. In response to oxidative stress, bacteria have evolved redox-responsive sensors that enable them to simultaneously monitor and eradicate potential oxidative stress. Specifically, redox-sensing transcription regulators react to oxidative stress by means of modifying the thiol groups of cysteine residues, functioning as part of an efficient survival mechanism for many bacteria...
May 17, 2018: Archives of Pharmacal Research
Jong Geol Lee, Young Hoon Sung, In-Jeoung Baek
The key to successful drug discovery and development is to find the most suitable animal model of human diseases for the preclinical studies. The recent emergence of engineered endonucleases is allowing for efficient and precise genome editing, which can be used to develop potentially useful animal models for human diseases. In particular, zinc finger nucleases, transcription activator-like effector nucleases, and the clustered regularly interspaced short palindromic repeat systems are revolutionizing the generation of diverse genetically-engineered experimental animals including mice, rats, rabbits, dogs, pigs, and even non-human primates that are commonly used for preclinical studies of the drug discovery...
May 17, 2018: Archives of Pharmacal Research
Xiang Dong Su, Irshad Ali, Madeeha Arooj, Young Sang Koh, Seo Young Yang, Young Ho Kim
Sanguisorba officinalis L. (Rosaceae) is a perennial herbaceous plant and its roots have been used as an important astringent medicine in Eastern Asian countries over many thousand years. In this phytochemical research, 23 compounds (1-23) were isolated from the roots of S. officinalis. Their chemical structures were identified by extensive spectroscopic methods, including 1D and 2D NMR experiments. The anti-inflammatory effects of extracts and isolated compounds were investigated by measuring the production of pro-inflammatory cytokine IL-12 p40, IL-6 and TNF-α in LPS-stimulated bone marrow-derived dendritic cell...
May 7, 2018: Archives of Pharmacal Research
Ji-Yeong Byeon, Yun Jeong Lee, Young-Hoon Kim, Se-Hyung Kim, Choong-Min Lee, Jung-Woo Bae, Choon-Gon Jang, Seok-Yong Lee, Chang-Ik Choi
Tamsulosin, a selective antagonist of the α1 -adrenoceptor, is primarily metabolized by CYP3A4 and CYP2D6, and tamsulosin exposure is significantly increased according to the genetic polymorphism of CYP2D6. In this study, we investigated the effects of diltiazem, a moderate inhibitor of CYP3A4, on the pharmacokinetics of tamsulosin in subjects with different CYP2D6 genotypes. Twenty-three healthy Korean male subjects with CYP2D6*wt/*wt (*wt = *1 or *2) and CYP2D6*10/*10 were enrolled in the prospective, open-label, two-phase parallel pharmacokinetic study...
May 4, 2018: Archives of Pharmacal Research
Eun Hye Kim, Chang Soo Jo, Shi Yong Ryu, Seong Hwan Kim, Ji Young Lee
Methanol (MeOH) extract of the aerial parts of Dendropanax morbifera (Araliaceae) has demonstrated a significant dose-dependent inhibitory effect on the RANKL-induced differentiation of bone marrow-derived macrophages to osteoclasts. Bioassay-guided fractionation of the extract resulted in the isolation of a novel diacetylene carboxylic acid (1), together with a known diacetylenic compounds (2) as phytochemicals to strongly inhibit the osteoclast differentiation. The chemical structure of 1 was determined by spectroscopic analyses as (9Z,16S)-16-O-acetyl-9,17-octadecadiene-12,14-diynoic acid, that is acetyl derivative of 2...
May 4, 2018: Archives of Pharmacal Research
Hyun Sook Kwon, Hanna Lee, Jin Su Lee, Kijun Lee, Jung-Hye Choi, Dae Sik Jang
Two new β-carboline alkaloids, 1-acetyl-4-methoxy-8-hydroxy-β-carboline (1) and 1-acetyl-4,8-dimethoxy-β-carboline (2), together with 10 known compounds; seven β-carboline alkaloids (3-9), two canthin-6-one alkaloids (10 and 11), and one quassinoid (12) were isolated from the stems of Picrasma quassioides. The structure of the new compounds 1 and 2 were determined by spectroscopic analyses including 1D- and 2D-NMR and HRMS interpretation. All the isolates (1-12) were evaluated for their cytotoxicity against human ovarian carcinoma A2780 and SKOV3 cell lines using MTT assays...
May 3, 2018: Archives of Pharmacal Research
Ga Young Lee, Byoung Ok Cho, Jae Young Shin, Seon Il Jang, In Sook Cho, Hyo Young Kim, Ji Su Park, Chong Woon Cho, Jong Seong Kang, Jang Hoon Kim, Young Ho Kim
Ten compounds (1-10) isolated from the seeds of Cassia tora were evaluated for tyrosinase inhibition. Compounds 3, 4, and 7 inhibited tyrosinase enzymatic activity in a dose-dependent manner, with IC50 values of 3.0 ± 0.8, 7.0 ± 0.4, and 9.2 ± 3.4 μM, respectively. Kinetic analyses revealed a mechanism consistent with competitive inhibition. In silico molecular docking showed that compounds 3 and 4 docked in the active site of tyrosinase, whereas 7 interacted with Ala246 and Val248 at outside of the active site, and His244 and Glu256 at inside...
May 2, 2018: Archives of Pharmacal Research
Minmi Jo, Sun-Woo Won, Dong Guk Lee, Jungeon Yun, Sunhong Kim, Young-Shin Kwak
4,4-Dimethyloxazolones derived from N-protected aminoisobutyric acid (AIB) are particularly known as poor electrophiles due to the steric hindrance around the carbonyl and not employed as useful intermediates for amidation whereas numerous examples have been reported to support the utility of other oxazolones in amidation. AIB is an important and strategical synthon in medicinal chemistry but the peptide bond formation of the N-protected urethane derivatives of AIB is known to be often unproductive due to the rapid formation of the stable 4,4-dimethyloxazolone via an intramolecular cyclization...
April 25, 2018: Archives of Pharmacal Research
Jiyeon Kweon, Yongsub Kim
The CRISPR-Cas9 system is a powerful tool for genome engineering, and its programmability and simplicity have enabled various types of gene manipulation such as gene disruption and transcriptional and epigenetic perturbation. Particularly, CRISPR-based pooled libraries facilitate high-throughput screening for functional regulatory elements in the human genome. In this review, we describe recent advances in CRISPR-Cas9 technology and its use in high-throughput genetic screening. We also discuss its potential for drug target discovery and current challenges of this technique in biomedical research...
April 10, 2018: Archives of Pharmacal Research
Hyoung Jin Kim, Seo Young Cho, Min-Hye Park, Hong-Jin Kim
Insect and yeast cells are considered the expression systems of choice for producing virus-like particles (VLPs), and numerous types of VLPs have been produced in these systems. However, previous studies were restricted to identifying the characteristics of individual VLP preparations. No direct comparison of the structures and immunogenic properties of insect and yeast-derived VLPs has so far been made. In the present study, the size distribution and immunogenic properties of human papillomavirus type 16 (HPV16) L1 VLPs produced in Spodoptera frugipedra-9 insect cells and Saccharomyces cerevisiae were compared...
April 10, 2018: Archives of Pharmacal Research
Łukasz Popiołek, Anna Biernasiuk, Kinga Paruch, Anna Malm, Monika Wujec
This article describes the synthesis and antimicrobial activity evaluation of new pipemidic acid derivatives. New compounds were obtained on the basis of Mannich reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with pipemidic acid. Antimicrobial tests revealed high antibacterial activity of obtained derivatives. Gram-negative rods belonging to Enterobacteriaceae family were particularly most sensitive to new pipemidic acid derivatives. Synthesized compounds exhibited very strong activity towards Proteus mirabilis ATCC 12453, Salmonella typhimurium ATCC 14028 and Escherichia coli ATCC 25922...
April 4, 2018: Archives of Pharmacal Research
Guangzhi Li, Junchi Wang, Xiaojin Li, Jianguo Xu, Zhao Zhang, Jianyong Si
2'-Z auraptene (1) is a synthesized monoterpene coumarin with anticancer activity against human gastric cancer cells. In order to find new potential anticancer agent, Mucor polymorphosporus was used to transform cis-auraptene. Four new terpene coumarins with notable changes in the skeletal backbone, 2'-Z auraptene A-D (2-5), were obtained and evaluated for their antiproliferative effects against human normal gastric epithelium cells and human gastric cancer cells. These new compounds showed selective cytotoxic activity against MGC-803 cells with IC50 values from 0...
April 4, 2018: Archives of Pharmacal Research
Jia Chen, Jianhua Shao, Chunchao Zhao, Jie Shen, Ziling Dong, Wenyan Liu, Min Zhao, Judi Fan
Three new neolignans, fordianoles A-C (1-3), characterized as (7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneolignan-7,7',9-triol, (7R,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneolignan-7,7',9-triol, and (7R,8R)-4-hydroxy-3,3',5'-trimethoxy-8,4'-oxyneolignan-7,9,9'-triol-7'-one, together with an unusual γ-lactone, 3-(3,4-dihydroxyphenyl)-4-pentanolide (4), and twenty-five known compounds (5-29) were isolated from the aerial parts of Viburnum fordiae Hance. Their structures including absolute configurations were determined by spectroscopic and chemical methods...
April 4, 2018: Archives of Pharmacal Research
Yingnan Wu, Senhua Chen, Hongju Liu, Xishan Huang, Yayue Liu, Yiwen Tao, Zhigang She
Five isocoumarin derivatives including three new compounds, aspergisocoumrins A-C (1-3), together with two known analogues, 8-dihydroxyisocoumarin-3-carboxylic acid (4) and dichlorodiaportin (5) were obtained from the culture of the endophytic fungus Aspergillus sp. HN15-5D derived from the fresh leaves of the mangrove plant Acanthus ilicifolius. Their structures were elucidated using comprehensive spectroscopic methods. The double bond geometry of compounds 1 and 2 were assigned as E and Z on the basis of the distinct coupling constants, respectively...
March 28, 2018: Archives of Pharmacal Research
Youngbae Kim, Chan Seo, Suin Oh, Juhwan Kwak, Sumin Jung, Eunsu Sin, Hyunbin Kim, Moongi Ji, Hyeon-Seong Lee, Hyung-Jin Park, Gwang Lee, Jundong Yu, Minsoo Kim, Wonjae Lee, Man-Jeong Paik
Loxoprofen is a non-steroidal anti-inflammatory drug of the 2-arylpropionic acid type, which has used to treat musculoskeletal disorders in the horse racing industry. However, it has also used illicitly to mask clinical signs of inflammation and pain in racehorses. Thus, its accurate analysis has become an important issue in horse doping laboratories. In this study, an analytical method of loxoprofen was developed as tert-butyldimethylsilyl (TBDMS) derivative by gas chromatography-mass spectrometry (GC-MS)...
March 23, 2018: Archives of Pharmacal Research
Jing Jin, Yuanjin Chen, Dechuan Wang, Lingman Ma, Min Guo, Changlin Zhou, Jie Dou
Baicalin was identified as a neuraminidase (NA) inhibitor displaying anti-influenza A virus (IAV) activity. However, its poor solubility in saline has limited its use in the clinic. We generated sodium baicalin and showed that it exhibited greatly increased solubility in saline. Its efficacy against oseltamivir-resistant mutant A/FM/1/47-H275Y (H1N1-H275Y) was evaluated in vitro and in vivo. Results showed that 10 μM of sodium baicalin inhibited A/FM/1/47 (H1N1), A/Beijing/32/92 (H3N2) and H1N1-H275Y in MDCK cells in a dose-dependent manner, with inhibitory rates of 83...
March 23, 2018: Archives of Pharmacal Research
Md Saiful Islam Roney, Song-Kyu Park
Cancer is one of the deadliest diseases in the world. Despite extensive studies, treating metastatic cancers remains challenging. Years of research have linked a rare set of cells known as cancer stem cells (CSCs) to drug resistance, leading to the suggestion that eradication of CSCs might be an effective therapeutic strategy. However, few drug candidates are active against CSCs. New drug discovery is often a lengthy process. Drug screening has been advantageous in identifying drug candidates. Current understanding of cancer biology has revealed various clues to target cancer from different points of view...
March 19, 2018: Archives of Pharmacal Research
Jihyun Kim, Hyunhee Kim, Heewon Roh, Youngjoo Kwon
In the last 10 years, homocysteine has been regarded as a marker of cardiovascular disease and a definite risk factor for many other diseases. Homocysteine is biosynthesized from methionine through multiple steps and then goes through one of two major metabolic pathways: remethylation and transsulfuration. Hyperhomocysteinemia is a state in which too much homocysteine is present in the body. The main cause of hyperhomocysteinemia is a dysfunction of enzymes and cofactors associated with the process of homocysteine biosynthesis...
March 19, 2018: Archives of Pharmacal Research
Jung Jae Jo, Jun Hyun Jo, SunJoo Kim, Jae-Mok Lee, Sangkyu Lee
Cocktail substrates are useful in investigating drug-drug interactions (DDI) that can rapidly identify the cytochrome P450 (CYP) isoforms that interact with test drugs. In this study, we developed and validated five probe drugs for CYP1A, CYP2B, CYP2C, CYP2D, and CYP3A using LC-MS/MS to determine CYP activities in mice. The five probe substrates were caffeine (2 mg/kg), bupropion (30 mg/kg), omeprazole (4 mg/kg), dextromethorphan (40 mg/kg), and midazolam (2 mg/kg) for CYP1A, CYP2B, CYP2C, CYP2D, and CYP3A, respectively...
March 17, 2018: Archives of Pharmacal Research
Aonnicha Sombatsri, Yutthapong Thummanant, Thurdpong Sribuhom, Jaursup Boonmak, Sujittra Youngme, Suphanthip Phusrisom, Veerapol Kukongviriyapan, Chavi Yenjai
Three new limonoids, limonophyllines A-C (1, 4 and 5), along with two known limonoids (2 and 3) and 11 acridone alkaloids (6-16) were isolated from the stems of Atalantia monophylla. All isolates were evaluated against cholangiocarcinoma, KKU-M156, and HepG2 cancer cell lines. Compounds 12, 14 and 16 displayed cytotoxicity against KKU-M156 cell line with IC50 ranging from 3.39 to 4.1 μg/mL while cytotoxicity against HepG2 cell line with IC50 ranging from 1.43 to 8.4 μg/mL. The structures of all isolated compounds were established by spectroscopic methods including 1D and 2D NMR, IR and mass spectrometry...
March 15, 2018: Archives of Pharmacal Research
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