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Biomolecules & Therapeutics

Ao Xuan Zhen, Mei Jing Piao, Yu Jae Hyun, Kyoung Ah Kang, Yea Seong Ryu, Suk Ju Cho, Hee Kyoung Kang, Young Sang Koh, Mee Jung Ahn, Tae Hoon Kim, Jin Won Hyun
Purpurogallin, a natural phenol obtained from oak nutgalls, has been shown to possess antioxidant, anticancer, and anti-inflammatory effects. Recently, in addition to ultraviolet B (UVB) radiation that induces cell apoptosis via oxidative stress, particulate matter 2.5 (PM2.5 ) was shown to trigger excessive production of reactive oxygen species. In this study, we observed that UVB radiation and PM2.5 severely damaged human HaCaT keratinocytes, disrupting cellular DNA, lipids, and proteins and causing mitochondrial depolarization...
November 12, 2018: Biomolecules & Therapeutics
Jong Soo Han, Su Jin Kim, Yoonjin Nam, Hak Yeong Lee, Geon Min Kim, Dong Min Kim, Uy Dong Sohn
Most diabetic patients experience diabetic mellitus (DM) urinary bladder dysfunction. A number of studies evaluate bladder smooth muscle contraction in DM. In this study, we evaluated the change of bladder smooth muscle contraction between normal rats and DM rats. Furthermore, we used pharmacological inhibitors to determine the differences in the signaling pathways between normal and DM rats. Rats in the DM group received an intraperitoneal injection of 65 mg/kg streptozotocin and measured blood glucose level after 14 days to confirm DM...
November 12, 2018: Biomolecules & Therapeutics
Asad Ul-Haq, Ming Li Jin, Kwang Won Jeong, Hwan-Mook Kim, Kwang-Hoon Chun
Mixed lineage leukemia proteins (MLL) are the key histone lysine methyltransferases that regulate expression of diverse genes. Aberrant activation of MLL promotes leukemia as well as solid tumors in humans, highlighting the urgent need for the development of an MLL inhibitor. We screened and isolated MLL1-binding ssRNAs using SELEX (<u>S</u>ystemic <u>E</u>volution of <u>L</u>igands by <u>E</u>xponential enrichment) technology. When sequences in sub-libraries were obtained using next-generation sequencing (NGS), the most enriched aptamers-APT1 and APT2-represented about 30% and 26% of sub-library populations, respectively...
November 12, 2018: Biomolecules & Therapeutics
Dong Zhao, Ming-Yao Gu, Jiu Liang Xu, Li Jun Zhang, Shi Yong Ryu, Hyun Ok Yang
Ginger, one of worldwide consumed dietary spice, in fact, it is not only famous as food supplements, and also believed to exert a variety of remarkable pharmacological activity as herbal remedies. In this study, a ginger constituent, 12-dehydrogingerdione (DHGD) was proven that has comparable anti-inflammatory activity with positive control 6-shogaol in inhibiting LPS-induce dinterleukin (IL)-6, tumor necrosis factor (TNF)-α, prostaglandin (PG) E2 , nitric oxide (NO), inducible NO synthase (iNOS) and cyclooxygenase (COX)-2, without interfering with COX-1 in cultured microglial cells...
October 26, 2018: Biomolecules & Therapeutics
John M Pezzuto
Resveratrol was first isolated in 1939 by Takaoka from Veratrum grandiflorum O. Loes. Following this discovery, sporadic descriptive reports appeared in the literature. However, spurred by our seminal paper published nearly 60 years later, resveratrol became a household word and the subject of extensive investigation. Now, in addition to appearing in over 20,000 research papers, resveratrol has inspired monographs, conferences, symposia, patents, chemical derivatives, etc. In addition, dietary supplements are marketed under various tradenames...
October 11, 2018: Biomolecules & Therapeutics
Young Hwan Park, Hyun Woo Kim, Hyuk Soon Kim, Seung Taek Nam, Dajeong Lee, Min Bum Lee, Keun Young Min, Jimo Koo, Su Jeong Kim, Young Mi Kim, Hyung Sik Kim, Wahn Soo Choi
Mast cells are the most prominent effector cells of Type 1 hypersensitivity immune responses. CYC116 [4-(2-amino-4-methyl-1,3-thiazol-5-yl)-N-[4-(morpholin-4-yl)phenyl] pyrimidin-2-amine] is under development to be used as an anti-cancer drug, but the inhibitory effects of CYC116 on the activation of mast cells and related allergy diseases have not reported as of yet. In this study, we demonstrated, for the first time, that CYC116 inhibited the degranulation of mast cells by antigen stimulation (IC50 , ~1.42 μM)...
October 11, 2018: Biomolecules & Therapeutics
Yoon Sun Chun, Oh-Hoon Kwon, Hyun Geun Oh, Yoon Young Cho, Hyun Ok Yang, Sungkwon Chung
β-amyloid precursor protein (APP) can be cleaved by α-, and γ-secretase at plasma membrane producing soluble ectodomain fragment (sAPPα). Alternatively, following endocytosis, APP is cleaved by β-, and γ-secretase at early endosomes generating β-amyloid (Aβ), the main culprit in Alzheimer's disease (AD). Thus, APP endocytosis is critical for Aβ production. Recently, we reported that Monsonia angustifolia , the indigenous vegetables consumed in Tanzania, improved cognitive function and decreased Aβ production...
October 11, 2018: Biomolecules & Therapeutics
Jun-Ho Ahn, Sung-Hee Hwang, Hyun-Soo Cho, Michael Lee
Melanoma cells have been shown to respond to BRAF inhibitors; however, intrinsic and acquired resistance limits their clinical application. In this study, we performed RNA-Seq analysis with BRAF inhibitor-sensitive (A375P) and -resistant (A375P/Mdr with acquired resistance and SK-MEL-2 with intrinsic resistance) melanoma cell lines, to reveal the genes and pathways potentially involved in intrinsic and acquired resistance to BRAF inhibitors. A total of 546 differentially expressed genes (DEGs), including 239 up-regulated and 307 down-regulated genes, were identified in both intrinsic and acquired resistant cells...
October 4, 2018: Biomolecules & Therapeutics
Soo-Jin Park, Dong-Soon Im
Sphingosine 1-phosphate (S1P) levels are often found to be elevated in serum, bronchoalveolar lavage, and lung tissue of idiopathic pulmonary fibrosis patients and experimental mouse models. Although the roles of sphingosine kinase 1 and S1P receptors have been implicated in fibrosis, the underlying mechanism of fibrosis via Sphingosine 1-phosphate receptor 2 (S1P2 ) has not been fully investigated. Therefore, in this study, the roles of S1P2 in lung inflammation and fibrosis was investigated by means of a bleomycin-induced lung fibrosis model and lung epithelial cells...
October 4, 2018: Biomolecules & Therapeutics
Mengjie Xu, Feng Xiao, Mengshi Wang, Tingxu Yan, Huilin Yang, Bo Wu, Kaishun Bi, Ying Jia
Depression is a major mood disorder. Abnormal expression of glial glutamate transporter-1 (GLT-1) is associated with depression. Schisantherin B (STB) is one bioactive of lignans isolated from Schisandra chinensis (Turcz.) Baill which has been commonly used as a traditional herbal medicine for thousands of years. This paper was designed to investigate the effects of STB on depressive mice induced by forced swimming test (FST). Additionally, we also assessed the impairment of FST on cognitive function in mice with different ages...
September 27, 2018: Biomolecules & Therapeutics
Ching-Ying Wang, Chen-Sheng Lin, Chun-Hung Hua, Yu-Jen Jou, Chi-Ren Liao, Yuan-Shiun Chang, Lei Wan, Su-Hua Huang, Mann-Jen Hour, Cheng-Wen Lin
Cis-3-O-p -hydroxycinnamoyl ursolic acid (HCUA), a triterpenoid compound, was purified from Elaeagnus oldhamii Maxim. This traditional medicinal plant has been used for treating rheumatoid arthritis and lung disorders as well as for its anti-inflammation and anticancer activities. This study aimed to investigate the anti-proliferative and apoptotic-inducing activities of HCUA in oral cancer cells. HCUA exhibited anti-proliferative activity in oral cancer cell lines (Ca9-22 and SAS cells), but not in normal oral fibroblasts...
September 27, 2018: Biomolecules & Therapeutics
Joon Hee Kang, Seon-Hyeong Lee, Heesun Cheong, Chang Hoon Lee, Soo-Youl Kim
Transglutaminase 2 (TGase 2) plays a key role in p53 regulation, depleting p53 tumor suppressor through autophagy in renal cell carcinoma. We found that microtubule-associated protein 1A/1B-light chain 3 (LC3), a hallmark of autophagy, were tightly associated with the level of TGase 2 in cancer cells. TGase 2 overexpression increased LC3 levels, and TGase 2 knockdown decreased LC3 levels in cancer cells. Transcript abundance of LC3 was inversely correlated with level of wild type p53. TGase 2 knockdown using siRNA, or TGase 2 inhibition using GK921 significantly reduced autophagy through reduction of LC3 transcription, which was followed by restoration of p53 levels in cancer cells...
September 20, 2018: Biomolecules & Therapeutics
Zhicheng Fu, So Yoon Yun, Jong Hoon Won, Moon Jung Back, Ji Min Jang, Hae Chan Ha, Hae Kyung Lee, In Chul Shin, Ju Yeun Kim, Hee Soo Kim, Dae Kyong Kim
Ceramide metabolism is known to be an essential etiology for various diseases, such as atopic dermatitis and Gaucher disease. Glucosylceramide synthase (GCS) is a key enzyme for the synthesis of glucosylceramide (GlcCer), which is a main ceramide metabolism pathway in mammalian cells. In this article, we developed a liquid chromatography-tandem mass spectrometry (LC-MS/MS) method to determine GCS activity using synthetic non-natural sphingolipid C8-ceramide as a substrate. The reaction products, C8-GlcCer for GCS, could be separated on a C18 column by reverse-phase high-performance liquid chromatography (HPLC)...
September 20, 2018: Biomolecules & Therapeutics
Jong Kook Park, Jung Seon Seo, Suk Kyeong Lee, Kenneth K Chan, Hyo-Jeong Kuh
Epigenetic silencing is considered to be a major mechanism for loss of activity in tumor suppressors. Reversal of epigenetic silencing by using inhibitors of DNA methyltransferase (DNMT) or histone deacetylases (HDACs) such as 5-Aza-CdR and FK228 has shown to enhance cytotoxic activities of several anticancer agents. This study aims to assess the combinatorial effects of gene-silencing reversal agents (5-Aza-CdR and FK228) and oxaliplatin in gastric cancer cells, i.e., Epstein-Barr virus (EBV)-negative SNU-638 and EBV-positive SNU-719 cells...
September 3, 2018: Biomolecules & Therapeutics
Peng-Fei Wang, Dan-Hua Yao, Yue-Yu Hu, Yousheng Li
Intestinal barrier dysfunction always accompanies cirrhosis in patients with advanced liver disease and is an important contributor facilitating bacterial translocation (BT), which has been involved in the pathogenesis of cirrhosis and its complications. Several studies have demonstrated the protective effect of Vitamin D on intestinal barrier function. However, severe cholestasis leads to vitamin D depletion. This study was designed to test whether vitamin D therapy improves intestinal dysfunction in cirrhosis...
September 3, 2018: Biomolecules & Therapeutics
Suji Kim, No-Joon Song, Seo-Hyuk Chang, Gahee Bahn, Yuri Choi, Dong-Kwon Rhee, Ui Jeong Yun, Jinhee Choi, Jeon Lee, Jae Hyuk Yoo, Donghan Shin, Ki-Moon Park, Hee Kang, Sukchan Lee, Jin-Mo Ku, Yoon Shin Cho, Kye Won Park
The global obesity epidemic and associated metabolic diseases require alternative biological targets for new therapeutic strategies. In this study, we show that a phytochemical sulfuretin suppressed adipocyte differentiation of preadipocytes and administration of sulfuretin to high fat diet-fed obese mice prevented obesity and increased insulin sensitivity. These effects were associated with a suppressed expression of inflammatory markers, induced expression of adiponectin, and increased levels of phosphorylated ERK and AKT...
August 22, 2018: Biomolecules & Therapeutics
Sony Maharjan, Byoung Kwon Park, Su In Lee, Yoongho Lim, Keunwook Lee, Hyung-Joo Kwon
The authors request to correct the author name from Yoonho Lim to Yoongho Lim page 322.
September 1, 2018: Biomolecules & Therapeutics
Dayoung Ryu, In-Geun Ryoo, Mi-Kyoung Kwak
Cluster of differentiation 44 (CD44), a cell surface receptor for hyaluronic acid (HA), is involved in aggressive cancer phenotypes. Herein, we investigated the role of the CD44 standard isoform (CD44s) in hypoxia-inducible factor-1α (HIF-1α) regulation using MCF7 overexpressing CD44s (pCD44s-MCF7). When pCD44s-MCF7 was incubated under hypoxia, levels of HIF-1α, vascular endothelial growth factor, and the HIF-1α response element-derived luciferase activity were significantly increased compared to those in the control MCF7...
September 1, 2018: Biomolecules & Therapeutics
Sajita Shah, Kyu-Tae Kang
Most angiogenesis assays are performed using endothelial cells. However, blood vessels are composed of two cell types: endothelial cells and pericytes. Thus, co-culture of two vascular cells should be employed to evaluate angiogenic properties. Here, we developed an in vitro 3-dimensional angiogenesis assay system using spheroids formed by two human vascular precursors: endothelial colony forming cells (ECFCs) and mesenchymal stem cells (MSCs). ECFCs, MSCs, or ECFCs+MSCs were cultured to form spheroids. Sprout formation from each spheroid was observed for 24 h by real-time cell recorder...
September 1, 2018: Biomolecules & Therapeutics
Qing Meng, Hyoung-Chun Kim, Seikwan Oh, Yong-Moon Lee, Zhenzhen Hu, Ki-Wan Oh
Cocaine- and amphetamine-regulated transcript (CART) peptide is a widely distributed neurotransmitter expressed in the central nervous systems. Previously, several reports demonstrated that nucleus accumbal-injected CART peptide positively modulated behavioral sensitization induced by psychostimulants and regulated the mesocorticolimbic dopaminergic pathway. It is confirmed that CART peptide exerted inhibitory effect on psychostimulant-enhanced dopamine receptors signaling, Ca2+ /calmodulin-dependent kinase signaling and crucial transcription factors expression...
September 1, 2018: Biomolecules & Therapeutics
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