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Biomolecules & Therapeutics

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https://www.readbyqxmd.com/read/28605834/absorption-study-of-genistein-using-solid-lipid-microparticles-and-nanoparticles-control-of-oral-bioavailability-by-particle-sizes
#1
Jeong Tae Kim, Sonia Barua, Hyeongmin Kim, Seong-Chul Hong, Seung-Yup Yoo, Hyojin Jeon, Yeongjin Cho, Sangwon Gil, Kyungsoo Oh, Jaehwi Lee
In this study, the effect of particle size of genistein-loaded solid lipid particulate systems on drug dissolution behavior and oral bioavailability was investigated. Genistein-loaded solid lipid microparticles and nanoparticles were prepared with glyceryl palmitostearate. Except for the particle size, other properties of genistein-loaded solid lipid microparticles and nanoparticles such as particle composition and drug loading efficiency and amount were similarly controlled to mainly evaluate the effect of different particle sizes of the solid lipid particulate systems on drug dissolution behavior and oral bioavailability...
June 14, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28605833/pig3-regulates-p53-stability-by-suppressing-its-mdm2-mediated-ubiquitination
#2
Min Jin, Seon-Joo Park, Seok Won Kim, Hye Rim Kim, Jin Won Hyun, Jung-Hee Lee
Under normal, non-stressed conditions, intracellular p53 is continually ubiquitinated by MDM2 and targeted for degradation. However, in response to severe genotoxic stress, p53 protein levels are markedly increased and apoptotic cell death is triggered. Inhibiting the ubiquitination of p53 under conditions where DNA damage has occurred is therefore crucial for preventing the development of cancer, because if cells with severely damaged genomes are not removed from the population, uncontrolled growth can result...
June 14, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28605832/comparison-of-reprogramming-methods-for-generation-of-induced-oligodendrocyte-precursor-cells
#3
Eun-Hye Lee, Chang-Hwan Park
Direct conversion by trans-differentiation is of growing interest in cell therapy for incurable diseases. The efficiency of cell reprogramming and functionality of converted cells are important considerations in cell transplantation therapy. Here, we compared two representative protocols for the generation of induced-oligodendrocyte progenitor cells (iOPCs) from mouse and rat fibroblasts. Then, we showed that induction of Nkx6.2, Olig2, and Sox10 (NOS) was more effective in mouse fibroblasts and that induction of Olig2, Sox10, and Zfp536 (OSZ) was more effective at reprogramming iOPCs from rat fibroblasts...
June 14, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28605831/age-related-changes-in-sulfur-amino-acid-metabolism-in-male-c57bl-6-mice
#4
Jang Su Jeon, Jeong-Ja Oh, Hui Chan Kwak, Hwi-Yeol Yun, Hyoung Chin Kim, Young-Mi Kim, Soo Jin Oh, Sang Kyum Kim
Alterations in sulfur amino acid metabolism are associated with an increased risk of a number of common late-life diseases, which raises the possibility that metabolism of sulfur amino acids may change with age. The present study was conducted to understand the age-related changes in hepatic metabolism of sulfur amino acids in 2-, 6-, 18- and 30-month-old male C57BL/6 mice. For this purpose, metabolite profiling of sulfur amino acids from methionine to taurine or glutathione (GSH) was performed. The levels of sulfur amino acids and their metabolites were not significantly different among 2-, 6- and 18-month-old mice, except for plasma GSH and hepatic homocysteine...
June 14, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28605830/sustained-intracellular-acidosis-triggers-the-na-h-exchager-1-activation-in-glutamate-excitotoxicity
#5
Bo Kyung Lee, Yi-Sook Jung
The Na(+)/H(+) exchanger-1 (NHE-1) is a ubiquitously expressed pH-regulatory membrane protein that functions in the brain, heart, and other organs. It is increased by intracellular acidosis through the interaction of intracellular H(+) with an allosteric modifier site in the transport domain. In the previous study, we reported that glutamate-induced NHE-1 phosphorylation mediated by activation of protein kinase C-β (PKC-β) in cultured neuron cells via extracellular signal-regulated kinases (ERK)/p90 ribosomal s6 kinases (p90RSK) pathway results in NHE-1 activation...
June 14, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28605829/application-of-metabolomics-to-quality-control-of-natural-product-derived-medicines
#6
REVIEW
Kyung-Min Lee, Jun-Yeong Jeon, Byeong-Ju Lee, Hwanhui Lee, Hyung-Kyoon Choi
Metabolomics has been used as a powerful tool for the analysis and quality assessment of the natural product (NP)-derived medicines. It is increasingly being used in the quality control and standardization of NP-derived medicines because they are composed of hundreds of natural compounds. The most common techniques that are used in metabolomics consist of NMR, GC-MS, and LC-MS in combination with multivariate statistical analyses including principal components analysis (PCA) and partial least squares-discriminant analysis (PLS-DA)...
June 14, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554202/imperatorin-is-transported-through-blood-brain-barrier-by-carrier-mediated-transporters
#7
Temdara Tun, Young-Sook Kang
Imperatorin, a major bioactive furanocoumarin with multifunctions, can be used for treating neurodegenerative diseases. In this study, we investigated the characteristics of imperatorin transport in the brain. Experiments of the present study were designed to study imperatorin transport across the blood-brain barrier both in vivo and in vitro. In vivo study was performed in rats using single intravenous injection and in situ carotid artery perfusion technique. Conditionally immortalized rat brain capillary endothelial cells were as an in vitro model of blood-brain barrier to examine the transport mechanism of imperatorin...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554201/a-benzylideneacetophenone-derivative-induces-apoptosis-of-radiation-resistant-human-breast-cancer-cells-via-oxidative-stress
#8
Jeong Eon Park, Mei Jing Piao, Kyoung Ah Kang, Kristina Shilnikova, Yu Jae Hyun, Sei Kwan Oh, Yong Joo Jeong, Sungwook Chae, Jin Won Hyun
Benzylideneacetophenone derivative (1E)-1-(4-hydroxy-3-methoxyphenyl) hept-1-en-3-one (JC3) elicited cytotoxic effects on MDA-MB 231 human breast cancer cells-radiation resistant cells (MDA-MB 231-RR), in a dose-dependent manner, with an IC₅₀ value of 6 μM JC3. JC3-mediated apoptosis was confirmed by increase in sub-G1 cell population. JC3 disrupted the mitochondrial membrane potential, and reduced expression of anti-apoptotic B cell lymphoma-2 protein, whereas it increased expression of pro-apoptotic Bcl-2-associated X protein, leading to the cleavage of caspase-9, caspase-3 and poly (ADP-ribose) polymerase...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554200/the-memory-enhancing-effects-of-liquiritigenin-by-activation-of-nmda-receptors-and-the-creb-signaling-pathway-in-mice
#9
Yong-Hyun Ko, Seung-Hwan Kwon, Ji-Young Hwang, Kyung-In Kim, Jee-Yeon Seo, Thi-Lien Nguyen, Seok-Yong Lee, Hyoung-Chun Kim, Choon-Gon Jang
Liquiritigenin (LQ) is a flavonoid that can be isolated from Glycyrrhiza radix. It is frequently used as a tranditional oriental medicine herbal treatment for swelling and injury and for detoxification. However, the effects of LQ on cognitive function have not been fully explored. In this study, we evaluated the memory-enhancing effects of LQ and the underlying mechanisms with a focus on the N-methyl-D-aspartic acid receptor (NMDAR) in mice. Learning and memory ability were evaluated with the Y-maze and passive avoidance tests following administration of LQ...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554199/recombinant-human-thioredoxin-1-protects-macrophages-from-oxidized-low-density-lipoprotein-induced-foam-cell-formation-and-cell-apoptosis
#10
Hui Zhang, Qi Liu, Jia-Le Lin, Yu Wang, Ruo-Xi Zhang, Jing-Bo Hou, Bo Yu
Oxidized low-density lipoprotein (ox-LDL)-induced macrophage foam cell formation and apoptosis play critical roles in the pathogenesis of atherosclerosis. Thioredoxin-1 (Trx) is an antioxidant that potently protects various cells from oxidative stress-induced cell death. However, the protective effect of Trx on ox-LDL-induced macrophage foam cell formation and apoptosis has not been studied. This study aims to investigate the effect of recombinant human Trx (rhTrx) on ox-LDL-stimulated RAW264.7 macrophages and elucidate the possible mechanisms...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554198/role-of-taz-in-lysophosphatidic-acid-induced-migration-and-proliferation-of-human-adipose-derived-mesenchymal-stem-cells
#11
Won Min Mo, Yang Woo Kwon, Il Ho Jang, Eun Jung Choi, Sang Mo Kwon, Jae Ho Kim
Transcriptional co-activator with a PDZ-binding motif (TAZ) is an important factor in lysophosphatidic acid (LPA)-induced promotion of migration and proliferation of human mesenchymal stem cells (MSCs). The expression of TAZ significantly increased at 6 h after LPA treatment, and TAZ knockdown inhibited the LPA-induced migration and proliferation of MSCs. In addition, embryonic fibroblasts from TAZ knockout mice exhibited the reduction in LPA-induced migration and proliferation. The LPA1 receptor inhibitor Ki16425 blocked LPA responses in MSCs...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554197/a-new-neolignan-derivative-balanophonin-isolated-from-firmiana-simplex-delays-the-progress-of-neuronal-cell-death-by-inhibiting-microglial-activation
#12
Soo Young Lim, Lalita Subedi, Dongyun Shin, Chung Sub Kim, Kang Ro Lee, Sun Yeou Kim
Excessive activation of microglia causes the continuous production of neurotoxic mediators, which further causes neuron degeneration. Therefore, inhibition of microglial activation is a possible target for the treatment of neurodegenerative disorders. Balanophonin, a natural neolignoid from Firmiana simplex, has been reported to have anti-inflammatory and anti-cancer effects. In this study, we aimed to evaluate the anti-neuroinflammatory effects and mechanism of Balanophonin in Lipopolysaccharide (LPS)-stimulated BV2 microglia cells...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28554196/production-of-recombinant-anti-cancer-vaccines-in-plants
#13
REVIEW
Jeong Hwan Lee, Kisung Ko
Plant expression systems have been developed to produce anti-cancer vaccines. Plants have several advantages as bioreactors for the production of subunit vaccines: they are considered safe, and may be used to produce recombinant proteins at low production cost. However, several technical issues hinder large-scale production of anti-cancer vaccines in plants. The present review covers design strategies to enhance the immunogenicity and therapeutic potency of anti-cancer vaccines, methods to increase vaccine-expressing plant biomass, and challenges facing the production of anti-cancer vaccines in plants...
May 30, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28441795/yji-7-suppresses-ros-production-and-expression-of-inflammatory-mediators-via-modulation-of-p38mapk-and-jnk-signaling-in-raw-264-7-macrophages
#14
Hye Jin Oh, Til Bahadur Thapa Magar, Nirmala Tilija Pun, Yunji Lee, Eun Hye Kim, Eung-Seok Lee, Pil-Hoon Park
Chalcone, (2E)-1,3-Diphenylprop-2-en-1-one, and its synthetic derivatives are known to possess anti-oxidative and anti-inflammatory properties. In the present study, we prepared a novel synthetic chalcone compound, (E)-1-(4-hydroxyphenyl)-3-(2-(trifluoromethoxy)phenyl)prop-2-en-1-one name (YJI-7), and investigated its inhibitory effects on endotoxin-stimulated production of reactive oxygen species (ROS) and expression of inflammatory mediators in macrophages. We demonstrated that treatment of RAW 264.7 macrophages with YJI-7 significantly suppressed lipopolysaccharide (LPS)-stimulated ROS production...
April 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28365977/spermidine-protects-against-oxidative-stress-in-inflammation-models-using-macrophages-and-zebrafish
#15
Jin-Woo Jeong, Hee-Jae Cha, Min Ho Han, Su Jung Hwang, Dae-Sung Lee, Jong Su Yoo, Il-Whan Choi, Suhkmann Kim, Heui-Soo Kim, Gi-Young Kim, Su Hyun Hong, Cheol Park, Hyo-Jong Lee, Yung Hyun Choi
Spermidine is a naturally occurring polyamine compound that has recently emerged with anti-aging properties and suppresses inflammation and oxidation. However, its mechanisms of action on anti-inflammatory and antioxidant effects have not been fully elucidated. In this study, the potential of spermidine for reducing pro-inflammatory and oxidative effects in lipopolysaccharide (LPS)-stimulated macrophages and zebrafish was explored. Our data indicate that spermidine significantly inhibited the production of pro-inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2), and cytokines including tumor necrosis factor-α and interleukin-1β in RAW 264...
April 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28365976/new-anticoagulants-for-the-prevention-and-treatment-of-venous-thromboembolism
#16
REVIEW
Joo Hee Kim, Kyung-Min Lim, Hye Sun Gwak
Anticoagulant drugs, like vitamin K antagonists and heparin, have been the mainstay for the treatment and prevention of venous thromboembolic disease for many years. Although effective if appropriately used, traditional anticoagulants have several limitations such as unpredictable pharmacologic and pharmacokinetic responses and various adverse effects including serious bleeding complications. New oral anticoagulants have recently emerged as an alternative because of their rapid onset/offset of action, predictable linear dose-response relationships and fewer drug interactions...
April 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28365975/neuroprotective-effect-of-duloxetine-on-chronic-cerebral-hypoperfusion-induced-hippocampal-neuronal-damage
#17
Jin-A Park, Choong-Hyun Lee
Chronic cerebral hypoperfusion (CCH), which is associated with onset of vascular dementia, causes cognitive impairment and neuropathological alterations in the brain. In the present study, we examined the neuroprotective effect of duloxetine (DXT), a potent and balanced serotonin/norepinephrine reuptake inhibitor, on CCH-induced neuronal damage in the hippocampal CA1 region using a rat model of permanent bilateral common carotid arteries occlusion. We found that treatment with 20 mg/kg DXT could attenuate the neuronal damage, the reduction of phosphorylations of mTOR and p70S6K as well as the elevations of TNF-α and IL- 1β levels in the hippocampal CA1 region at 28 days following CCH...
April 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28365974/diosmetin-alleviates-lipopolysaccharide-induced-acute-lung-injury-through-activating-the-nrf2-pathway-and-inhibiting-the-nlrp3-inflammasome
#18
Qinmei Liu, Xinxin Ci, Zhongmei Wen, Liping Peng
Acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) is a common clinical syndrome of diffuse lung inflammation with high mortality rates and limited therapeutic methods. Diosmetin, an active component from Chinese herbs, has long been noticed because of its antioxidant and anti-inflammatory activities. The aim of this study was to evaluate the effects of diosmetin on LPS-induced ALI model and unveil the possible mechanisms. Our results revealed that pretreatment with diosmetin effectively alleviated lung histopathological changes, which were further evaluated by lung injury scores...
April 6, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28449555/capsanthin-inhibits-both-adipogenesis-in-3t3-l1-preadipocytes-and-weight-gain-in-high-fat-diet-induced-obese-mice
#19
Sung Jun Jo, Jeung Won Kim, Hye Ok Choi, Jung Hwan Kim, Hyung Joong Kim, Sun Hee Woo, Byung Hoon Han
Adipogenesis in murine preadipocyte 3T3L-1 has been used as a model system to study anti-obese bioactive molecules. During adipogenesis in 3T3-L1 preadipocytes, we found that capsanthin inhibited adipogenesis (IC₅₀; 2.5 μM) and also showed lipolytic activity in differentiated adipocytes from the preadipocytes (ED₅₀; 872 nM). We identified that the pharmacological activity of capsanthin on adipogenesis in 3T3-L1 was mainly due to its adrenoceptor-β₂-agonistic activity. In high-fat diet animal model study, capsanthin significantly enhanced spontaneous locomotive activities together with progressive weight-loss...
May 1, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28365978/establishment-of-immortalized-primary-human-foreskin-keratinocytes-and-their-application-to-toxicity-assessment-and-three-dimensional-skin-culture-construction
#20
Moonju Choi, Minkyung Park, Suhyon Lee, Jeong Woo Lee, Min Chul Cho, Minsoo Noh, Choongho Lee
In spite of frequent usage of primary human foreskin keratinocytes (HFKs) in the study of skin biology, senescence-induced blockage of in vitro proliferation has been a big hurdle for their effective utilization. In order to overcome this passage limitation, we first isolated ten HFK lines from circumcision patients and successfully immortalized four of them via a retroviral transduction of high-risk human papillomavirus (HPV) E6 and E7 oncogenes. We confirmed expression of a keratinocyte marker protein, keratin 14 and two viral oncoproteins in these immortalized HFKs...
May 1, 2017: Biomolecules & Therapeutics
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