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Archives of Pharmacal Research

Dharmendra K Yadav, Saloni, Praveen Sharma, Sanjeev Misra, Harpreet Singh, Ricardo L Mancera, Kang Kim, Cheongyun Jang, Mi-Hyun Kim, Horacio Pérez-Sánchez, Eun Ha Choi, Surendra Kumar
The Gaussian-based 3D-QSAR studies for 58 selective COX-2 (cyclooxygenase-2) inhibitors belonging to benzopyran chemical class were performed. Partial least squares analysis produced statistically significant model with (R training(2)  = 0.866) and predictability (Q training(2)  = 0.66, Q test(2)  = 0.846). The 3D-QSAR model includes steric, electrostatic, hydrophobic, and hydrogen bond acceptor field indicators, whereas the potential field contributions indicate that the steric and hydrophobic features of the molecules play an important role in governing their biological activity...
August 18, 2017: Archives of Pharmacal Research
Changho Jhin, Chu Won Nho, Keum Taek Hwang
The aim of this study was to develop quantitative structure-activity relationship (QSAR) models for predicting antioxidant activities of phenolic compounds. The bond dissociation energy of O-H bond (BDE) was calculated by semi-empirical quantum chemical methods. As a new parameter for QSAR models, sum of reciprocals of BDE of enol and phenol groups (X BDE ) was calculated. Significant correlations were observed between X BDE and antioxidant activities, and X BDE was introduced as a parameter for developing QSAR models...
August 11, 2017: Archives of Pharmacal Research
Dong Wook Lee, Youra Kang, Mi Jeong Kang, Keumhan Noh, Ju Hyun Kim, Mahesh R Nepal, Rajina Shakya, Yu-Jeong Lee, Yurngdong Jahng, Sangkyu Lee, Jung-Ae Kim, Tae Cheon Jeong
Rutaecarpine, an alkaloid originally isolated from Evodia rutaecarpa, has been used for the treatment of gastrointestinal disorders in Asia. In the present study, the phase I and phase II metabolites of rutaecarpine were investigated in freshly isolated hepatocytes from male Sprague-Dawley rats. The individual metabolites were characterized via liquid chromatography-tandem mass spectrometry. The incubation of rutaecarpine with freshly isolated hepatocytes for 2 h yielded five major phase I metabolites. In addition, three glucuronide conjugates and four sulfate conjugates were observed...
August 10, 2017: Archives of Pharmacal Research
JungIn Lee, In Hyun Hwang, Jang Hoon Kim, Mi-Ae Kim, Jae Sam Hwang, Young Ho Kim, MinKyun Na
Edible insects have been reported to produce metabolites showing various pharmacological activities, recently emerging as rich sources of health functional food. In particular, the larvae of Protaetia brevitarsis seulensis (Kolbe) have been used as traditional Korean medicines for treating diverse diseases, such as breast cancer, inflammatory disease, hepatic cancer, liver cirrhosis, and hepatitis. However, only few chemical investigations were reported on the insect larvae. Therefore, the aim of this study was to discover and identify biologically active chemical components of the larvae of P...
August 5, 2017: Archives of Pharmacal Research
Su Jin Choi, Yu Su Shin, Byung Woog Kang, Jong Gwang Kim, Kyoung-Jae Won, Paul M Lieberman, Hyosun Cho, Hyojeung Kang
Epstein-Barr virus (EBV)-associated gastric carcinoma (EBVaGC) is a recently recognized disease entity defined by the presence of EBV in gastric carcinoma cells. EBV infection causes major epigenetic alterations in the EBV genome and its cellular host genome, suggesting that EBV acts as a direct epigenetic driver for EBVaGC. One of the major epigenetic events in the viral and cellular genomes to control transcription is DNA hypo- or hyper-methylation. Particularly, local and global hypermethylation have been reported in EBVaGC...
August 4, 2017: Archives of Pharmacal Research
Wenhua Kuang, Xu Zhang, Zhou Lan
Previous studies have shown that flavonoids (Fs) present in Linaria vulgaris inhibit lipid accumulation in vitro. This study was designed to evaluate the effects of Fs extracted from Linaria vulgaris ssp. sinensis (Bebeaux) Hong, on hyperlipidemia and hepatic steatosis induced by a western-type diet in mice. The major constituents of Fs were analyzed by LC-MS analysis. C57BL/6 mice were fed a western-type diet for 8 weeks to induce hyperlipidemia (model group), or fed a western-type diet followed by Fs treatment (90, 30 or 10 mg/kg/day) or atorvastatin treatment (1...
August 2, 2017: Archives of Pharmacal Research
Hyo-Jung Lee, Dong-Won Oh, Min-Ju Na, Dong-Wook Kim, Dong-Yeon Yuk, Hyoung-Chul Choi, Yong-Beom Lee, Kun Han, Chun-Woong Park
Minoxidil is widely used for treatment of androgenic alopecia. Commercial products containing minoxidil are usually in solution form. Repeated applications of minoxidil solution can lead to adverse effects such as skin irritation and horniness. The aims of this study were to prepare lecithin-based microparticle in minoxidil solution for enhancement of minoxidil topical delivery and skin protection and evaluate the ability of lecithin on in vitro delivery, in vivo hair growth, and skin trouble improvement compared to commercial minoxidil solution...
August 2, 2017: Archives of Pharmacal Research
Hyun Kyu Chung, Quoc-Ky Truong, Xuan-Lan Mai, Yusung Choi, Jong-Seong Kang, Woongchon Mar, Kyeong Ho Kim
Capillary zone electrophoresis was successfully applied to the enantiomeric purity determination of dexlansoprazole using sulfobutyl ether-β-cyclodextrin and methyl-β-cyclodextrin as chiral selectors. Separations were carried out in a 50 μm, 64/56 cm fused-silica capillary. The optimized conditions included 90 mM phosphate buffer, pH 6.0, containing 30 mM sulfobutyl ether-β-cyclodextrin, 20 mM methyl-β-cyclodextrin as background electrolyte, an applied voltage of 25 kV and a temperature of 16 °C, detection was at 280 nm...
August 1, 2017: Archives of Pharmacal Research
Euna Jeong, Sung Ung Moon, Mee Song, Sukjoon Yoon
Cancer precision medicine requires clinically actionable biomarkers for patient stratification and a better prediction of clinical outcome. Although thousands of cancer-enriched mutated genes have been reported by global sequencing projects, to date, only a few oncogenic mutations have been confirmed as effective biomarkers in cancer therapies. The low frequency and varied profile (i.e., allele frequency, mutation position) of mutant genes among cancer types limit the utility of predictive biomarkers. The recent explosion of cancer transcriptome and phenotypic screening data provides another opportunity for finding transcript-level biomarkers and targets, thus overcoming the limitation of cancer mutation analyses...
August 1, 2017: Archives of Pharmacal Research
Yue Lin, Yuanyuan Zhang, Qiongtao Song, Tao Song, Xue Han, Ying Zhang, Xuan Zhang, Xi Chu, Fenghua Zhang, Li Chu, Jianping Zhang
To explore the cardiovascular protective effects of Magnesium isoglycyrrhizinate (MI), especially the underlying cellular mechanisms related to L-type calcium channels and myocardial contractility, and to examine the effects of MI on hERG K(+) current expressed in HEK293 cells. We used the whole-cell patch clamp technique, video-based edge detection and dual excitation fluorescence photomultiplier systems to explore the effect of MI on L-type Ca(2+) currents (ICa-L) and cell contraction in rat cardiomyocytes...
August 1, 2017: Archives of Pharmacal Research
Jae-Young Lee, Ju-Hwan Park, Ki-Taek Kim, Jinha Yu, Pramod K Sahu, Naewon Kang, Hyeon-Jong Shin, Min-Hwan Kim, Ji-Su Kim, In-Soo Yoon, Lak Shin Jeong, Dae-Duk Kim
LJ-2698, a highly potent human A3 adenosine receptor antagonist with nucleoside structure, was designed to have a minimal species dependence. For further pre-clinical studies, analytical method for the detection of LJ-2698 in rat plasma was developed by liquid chromatography-tandem mass. Plasma samples were processed by protein precipitation method with acetonitrile, using losartan as the internal standard (IS). Chromatographic separation was carried out using a Kinetex C18 column (100 × 4.6 mm; 100 Å; 2...
July 29, 2017: Archives of Pharmacal Research
Kyung-Ran Park, Ji-Youn Kim, Eun-Cheol Kim, Hyung-Mun Yun, Jin Tae Hong
Magnolol, honokiol, and obovatol are well known bioactive constituents of the bark of Magnolia officinalis and have been reported to have beneficial effects in various diseases. We recently isolated a novel active compound, 4-O-methylhonokiol (4-O-MH) from the ethanol extract of M. officinalis, which was previously reported to have pharmacological effects including anti-inflammatory, anti-oxidative, and anti-aging activities. Here, we examined the pharmacological properties of 4-O-MH on osteoblast (bone-forming cells) and osteoclast (bone-resorbing cells) differentiation, and its underlying signaling pathways in primary cultured pre-osteoblasts and bone marrow macrophages...
July 24, 2017: Archives of Pharmacal Research
Gyu-Lee Kim, Seungyeop Lee, Truc Thanh Luong, Cuong Thach Nguyen, Sang-Sang Park, Suhkneung Pyo, Dong-Kwon Rhee
Streptococcus pneumoniae (pneumococcus) is responsible for significant morbidity and mortality worldwide. It causes a variety of life-threatening infections such as pneumonia, bacteremia, and meningitis. In bacterial physiology, the metabolic pathway of branched-chain amino acids (BCAAs) plays an important role in virulence. Nonetheless, the function of IlvC, one of the enzymes involved in the biosynthesis of BCAAs, in S. pneumoniae remains unclear. Here, we demonstrated that downregulation of BCAA biosynthesis by ilvC ablation can diminish BCAA concentration and expression of pneumolysin (Ply) and LytA, and subsequently attenuate virulence...
July 22, 2017: Archives of Pharmacal Research
Gyu-Lee Kim, Seung-Han Seon, Dong-Kwon Rhee
Pneumonia is an inflammatory disease of the lung, responsible for high morbidity and mortality worldwide. It is caused by bacteria, viruses, fungi, or other microorganisms. Streptococcus pneumoniae, a gram-positive bacterium with over 90 serotypes, is the most common causative agent. Moreover, comorbid factors including heart failure, renal disease, and pulmonary disease could increase the risk of pneumococcal pneumonia. Since the advent of the pneumococcal vaccine in the 1980s, the incidence of pneumonia has decreased significantly...
July 22, 2017: Archives of Pharmacal Research
Ajay Vijayakumar, Rengarajan Baskaran, Han-Joo Maeng, Bong Kyu Yoo
The aim of this study was to develop a ginsenoside-modified nanostructured lipid carrier (G-NLC) dispersion containing curcumin. The NLC was prepared by melt emulsification with slight modification process. Different G-NLC dispersion systems were prepared using lipid carrier matrix composed of ginsenoside, phosphatidylcholine, lysophosphatidylcholine, and hydrogenated bean oil. TEM image of the nanoparticles in the NLC dispersion showed core/shell structure, and there was corona-like layer surrounding the particles in the G-NLC...
July 15, 2017: Archives of Pharmacal Research
Xiaoping Peng, Yi Wang, Tonghan Zhu, Weiming Zhu
Five new pyrazin-2(1H)-one derivatives, ochramides A-D (1-4) and ochralate A (5), as well as three known analogues (6-8) were isolated from the fermentation broth of the marine coral-derived halotolerant Aspergillus ochraceus LCJ11-102 in a nutrient-limited medium containing 10% NaI. Their chemical structures were determined by analyzing NMR and X-ray diffraction data. Compounds 2, 5 and 6 showed antimicrobial activities against Enterobacter aerogenes with the MIC values of 40.0, 18.9, and 20.1 μM, respectively...
July 14, 2017: Archives of Pharmacal Research
Joon-Chul Kim, Min-Jeong Son, Jun Wang, Sun-Hee Woo
Cardiac contraction is controlled by a Ca(2+) signaling sequence that includes L-type Ca(2+) current-gated opening of Ca(2+) release channels (ryanodine receptors) in the sarcoplasmic reticulum (SR). Local Ca(2+) signaling in the atrium differs from that in the ventricle because atrial myocytes lack transverse tubules and have more abundant corbular SR. Myocardium is subjected to a variety of forces with each contraction, such as stretch, shear stress, and afterload, and adapts to those mechanical stresses...
July 12, 2017: Archives of Pharmacal Research
Jianbo Yang, Zheng Yan, Jin Ren, Zhong Dai, Shuangcheng Ma, Aiguo Wang, Yalun Su
Seven new dianthrone glycosides, named polygonumnolides A1-B3 (1-7), were isolated from the 70 % EtOH extract of the dried roots of Polygonum multiflorum Thunb. using column chromatography and preparative high-performance liquid chromatography. Their structures were determined by 1D and 2D NMR and mass spectroscopy. The isolated compounds were evaluated for their cytotoxic effects against KB tumor cell lines and compounds 1-4 showed moderate cytotoxicity.
July 5, 2017: Archives of Pharmacal Research
Eun Byeol Lee, Ming Ming Xing, Dae Keun Kim
This study contributes to the continual discovery of lifespan-extending compounds from plants, using the Caenorhabditis elegans model system. An ethyl acetate soluble fraction of methanol extract from the heartwood of Caesalpinia sappan showed a significant lifespan-extending activity. Subsequent activity-guided chromatography of the ethyl acetate-soluble fraction led to the isolation of brazilin. Brazilin showed potent 2,2-diphenyl-1-picrylhydrazyl radical scavenging and superoxide anion quenching activities and also revealed a lifespan-extending activity in C...
June 30, 2017: Archives of Pharmacal Research
Yeon Joo Lee, Su Jin Kim, Kyoung Wan Kwon, Won Mo Lee, Wi Joon Im, Uy Dong Sohn
Proteinase activated receptor 2 (PAR2), which is localized in the GI tract, the respiratory system, and the kidney tubules is a G protein-coupled receptor associated with inflammation, metabolism, and disease. The aim of this study was to explore the role of PAR2 in hydrogen peroxide (H2O2)-induced HepG2 cells by using FSLLRY-NH2 a PAR2 antagonist. H2O2 treatment resulted in induction of PAR2 in esophageal, gastric, and liver cells, with the most robust response being in HepG2 cells. Furthermore, this effect was dose-dependent in HepG2 cells...
June 22, 2017: Archives of Pharmacal Research
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