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Biomolecules & Therapeutics

Eun Byeol Lee, Jun Hyeong Kim, Chang Wan An, Yeong Jee Kim, Yun Jeong Noh, Su Jin Kim, Ju-Eun Kim, Abinash Chandra Shrestha, Ha-Neul Ham, Jae-Yoon Leem, Hyung-Kwon Jo, Dae-Sung Kim, Kwang Hyun Moon, Jeong Ho Lee, Kyung Ok Jeong, Dae Keun Kim
In order to discover lifespan-extending compounds made from natural resources, activity-guided fractionation of Zingiber officinale Roscoe (Zingiberaceae) ethanol extract was performed using the Caenorhabditis elegans ( C. elegans ) model system. The compound 6-gingerol was isolated from the most active ethyl acetate soluble fraction, and showed potent longevity-promoting activity. It also elevated the survival rate of worms against stressful environment including thermal, osmotic, and oxidative conditions...
March 14, 2018: Biomolecules & Therapeutics
Ji-Woon Kim, Hyun Ah Oh, Sung Hoon Lee, Ki Chan Kim, Pyung Hwa Eun, Mee Jung Ko, Edson Luck T Gonzales, Hana Seung, Seonmin Kim, Geon Ho Bahn, Chan Young Shin
T-type calcium channels are low voltage-activated calcium channels that evoke small and transient calcium currents. Recently, T-type calcium channels have been implicated in neurodevelopmental disorders such as autism spectrum disorder and neural tube defects. However, their function during embryonic development is largely unknown. Here, we investigated the function and expression of T-type calcium channels in embryonic neural progenitor cells (NPCs). First, we compared the expression of T-type calcium channel subtypes (CaV3...
February 21, 2018: Biomolecules & Therapeutics
Chang Yell Shin, Hae-Sun Kim, Kwang-Ho Cha, Dong Han Won, Ji-Yun Lee, Sun Woo Jang, Uy Dong Sohn
A previous study in humans demonstrated the sustained inhibitory effects of donepezil on acetylcholinesterase (AChE) activity; however, the effective concentration of donepezil in humans and animals is unclear. This study aimed to characterize the effective concentration of donepezil on AChE inhibition and impaired learning and memory in rodents. A pharmacokinetic study of donepezil showed a mean peak plasma concentration of donepezil after oral treatment (3 and 10 mg/kg) of approximately 1.2 ± 0.4 h and 1...
February 21, 2018: Biomolecules & Therapeutics
Hyewon Moon, Jung-Hee Jang, Tae Chang Jang, Gyu Hwan Park
Carbon monoxide (CO) is well-known as toxic gas and intrinsic signaling molecule such as neurotransmitter and blood vessel relaxant. Recently, it has been reported that low concentration of CO exerts therapeutic actions under various pathological conditions including liver failure, heart failure, gastric cancer, and cardiac arrest. However, little has been known about the effect of CO in neurodegenerative diseases like Parkinson's disease (PD). To test whether CO could exert a beneficial action during oxidative cell death in PD, we examined the effects of CO on 6-hydroxydopamine (6-OHDA)-induced cell death in C6 glioma cells...
February 12, 2018: Biomolecules & Therapeutics
MinJeong Kim, Gyo Jeong Gu, Yun-Sook Koh, Su-Hyun Lee, Yi Rang Na, Seung Hyeok Seok, Kyung-Min Lim
Fasiglifam (TAK-875) a G-protein coupled receptor 40 (GPR40) agonist, significantly improves hyperglycemia without hypoglycemia and weight gain, the major side effects of conventional anti-diabetics. Unfortunately, during multi-center Phase 3 clinical trials, unexpected liver toxicity resulted in premature termination of its development. Here, we investigated whether TAK-875 directly inflicts toxicity on hepatocytes and explored its underlying mechanism of toxicity. TAK-875 decreased viability of 2D and 3D cultures of HepG2, a human hepatocarcinoma cell line, in concentration- (>50 μM) and time-dependent manners, both of which corresponded with ROS generation...
February 12, 2018: Biomolecules & Therapeutics
Onjeon Ryu, Bo Kyung Park, Minji Bang, Kyu Suk Cho, Sung Hoon Lee, Edson Luck T Gonzales, Sung Min Yang, Seonmin Kim, Pyeong Hwa Eun, Joo Young Lee, Kyu-Bong Kim, Chan Young Shin, Kyoung Ja Kwon
Benzalkonium chloride, diazolidinyl urea, and imidazolidinyl urea are commonly used preservatives in cosmetics. Recent reports suggested that these compounds may have cellular and systemic toxicity in high concentration. In addition, diazolidinyl urea and imidazolidinyl urea are known formaldehyde (FA) releasers, raising concerns for these cosmetic preservatives. In this study, we investigated the effects of benzalkonium chloride, diazolidinyl urea, and imidazolidinyl urea on ROS-dependent apoptosis of rat neural progenitor cells (NPCs) in vitro...
February 12, 2018: Biomolecules & Therapeutics
Myungguen Chung, Soo Young Cho, Young Seek Lee
We aimed to understand the molecular changes in host cells that accompany infection by the seasonal influenza A H1N1 virus because the initial response rapidly changes owing to the fact that the virus has a robust initial propagation phase. Human epithelial alveolar A549 cells were infected and total RNA was extracted at 30 min, 1 h, 2 h, 4 h, 8 h, 24 h, and 48 h post infection (h.p.i.). The differentially expressed host genes were clustered into two distinct sets of genes as the infection progressed over time...
February 5, 2018: Biomolecules & Therapeutics
Young Sil Min, Hyuk-Jun Yoon, Hyun Dong Je, Jong Hyuk Lee, Seong Su Yoo, Hyun Sub Shim, Hak Yeong Lee, Hyen-Oh La, Uy Dong Sohn
In this study, we investigated the effects of pelargonidin, an anthocyanidin found in many fruits and vegetables, on endotheliumindependent vascular contractility to determine the underlying mechanism of relaxation. Isometric contractions of denuded aortic muscles from male rats were recorded, and the data were combined with those obtained in western blot analysis. Pelargonidin significantly inhibited fluoride-, thromboxane A2-, and phorbol ester-induced vascular contractions, regardless of the presence or absence of endothelium, suggesting a direct effect of the compound on vascular smooth muscles via a different pathway...
February 1, 2018: Biomolecules & Therapeutics
Seung-In Choi, Sun Wook Hwang
Inflammation is one of the main causes of pathologic pain. Knowledge of the molecular links between inflammatory signals and pain-mediating neuronal signals is essential for understanding the mechanisms behind pain exacerbation. Some inflammatory mediators directly modulate the excitability of pain-mediating neurons by contacting the receptor molecules expressed in those neurons. For decades, many discoveries have accumulated regarding intraneuronal signals from receptor activation through electrical depolarization for bradykinin, a major inflammatory mediator that is able to both excite and sensitize pain-mediating nociceptor neurons...
January 30, 2018: Biomolecules & Therapeutics
Yeon-Joo Jung, Won-Suk Chung
Glial cells are receiving much attention since they have been recognized as important regulators of many aspects of brain function and disease. Recent evidence has revealed that two different glial cells, astrocytes and microglia, control synapse elimination under normal and pathological conditions via phagocytosis. Astrocytes use the MEGF10 and MERTK phagocytic pathways, and microglia use the classical complement pathway to recognize and eliminate unwanted synapses. Notably, glial phagocytosis also contributes to the clearance of disease-specific protein aggregates, such as β-amyloid, huntingtin, and α-synuclein...
January 10, 2018: Biomolecules & Therapeutics
Taddesse Yayeh, Yea-Hyun Leem, Kyung-Mi Kim, Jae-Chul Jung, Jessica Schwarz, Ki-Wan Oh, Seikwan Oh
Sleep is the most basic and essential physiological requirement for mental health, and sleep disorders pose potential risks of metabolic and neurodegenerative diseases. Tryptic hydrolysate of αS1-casein (αS1-CH) has been shown to possess stress relieving and sleep promoting effects. However, the differential effects of αS1-CH on electroencephalographic wave patterns and its effects on the protein levels of γ-aminobutyric acid A (GABAA) receptor subtypes in hypothalamic neurons are not well understood. We found αS1-CH (120, 240 mg/kg) increased sleep duration in mice and reduced sleep-wake cycle numbers in rats...
January 9, 2018: Biomolecules & Therapeutics
Hye Ji Kim, Seaung Youl Oh
The objective of this work is to evaluate the effect of polyamidoamine (PAMAM) dendrimers on electroosmotic flow (EOF) through skin. The effect of size and concentration of dendrimer was studied, using generation 1, 4 and 7 dendrimer (G1, G4 and G7, respectively). As a marker molecule for the direction and magnitude of EOF, a neutral molecule, acetoaminophen (AAP) was used. The visualization of dendrimer permeation into the current conducting pore (CCP) of skin was made using G4-fluorescein isothiocyanate (FITC) conjugate and confocal microscopy...
January 9, 2018: Biomolecules & Therapeutics
Mee Sook Park, Jin Il Kim, Ilseob Lee, Sehee Park, Joon-Yong Bae, Man-Seong Park
Defensins are antimicrobial peptides that participate in the innate immunity of hosts. Humans constitutively and/or inducibly express α- and β-defensins, which are known for their antiviral and antibacterial activities. This review describes the application of human defensins. We discuss the extant experimental results, limited though they are, to consider the potential applicability of human defensins as antiviral agents. Given their antiviral effects, we propose that basic research be conducted on human defensins that focuses on RNA viruses, such as human immunodeficiency virus (HIV), influenza A virus (IAV), respiratory syncytial virus (RSV), and dengue virus (DENV), which are considered serious human pathogens but have posed huge challenges for vaccine development for different reasons...
January 9, 2018: Biomolecules & Therapeutics
Hyejin Lee, Kyung Ah Cheong, Ji-Young Kim, Nan-Hyung Kim, Minsoo Noh, Ai-Young Lee
Extracellular interleukin 1 alpha (IL-1α) released from keratinocytes is one of the endpoints for in vitro assessments of skin irritancy. Although cells dying via primary skin irritation undergo apoptosis as well as necrosis, IL-1α is not released in apoptotic cells. On the other hand, active secretion has been identified in interleukin-1 receptor antagonist (IL-1ra), which was discovered to be a common, upregulated, differentially-expressed gene in a microarray analysis performed with keratinocytes treated using cytotoxic doses of chemicals...
January 9, 2018: Biomolecules & Therapeutics
Geum-A Lee, Kyung-Chul Choi, Kyung-A Hwang
Triclosan (TCS) and bisphenol A (BPA) are endocrine-disrupting chemicals that interfere with the hormone or endocrine system and may cause cancer. Kaempferol (Kaem) and 3,3'-diindolylmethane (DIM) are phytoestrogens that play chemopreventive roles in the inhibition of carcinogenesis and cancer progression. In this study, the influence of TCS, BPA, Kaem, and DIM on proliferation and apoptotic abilities of VM7Luc4E2 breast cancer cells were examined. MTT assay revealed that TCS (0.1-10 μM), BPA (0.1-10 μM) and E2 (0...
January 9, 2018: Biomolecules & Therapeutics
Yong-Hyun Ko, Kyu-Yeon Shim, Seok-Yong Lee, Choon-Gon Jang
Worldwide, caffeine is among the most commonly used stimulatory substances. Unfortunately, significant caffeine consumption is associated with several adverse effects, ranging from sleep disturbances (including insomnia) to cardiovascular problems. This study investigates whether treatment with the Evodia rutaecarpa aqueous extract (ERAE) from berries and its major molecular component, evodiamine, can reduce the adverse caffeine-induced sleep-related and excitation effects. We combined measurements from the pentobarbital-induced sleep test, the open field test, and the locomotor activity test in mice that had been dosed with caffeine...
January 9, 2018: Biomolecules & Therapeutics
Hye Eun Lee, Gabsik Yang, Kyu-Bong Kim, Byung-Mu Lee, Joo Young Lee
Cosmetics are primarily applied to the skin; therefore, the association of cosmetic dyes with skin diseases or inflammation is a topic of great interest. Thymic stromal lymphopoietin (TSLP) is an interleukin 7-like cytokine that activates dendritic cells to promote Th2 inflammatory immune responses. TSLP is highly expressed in keratinocytes under inflammatory conditions, which suggests that it may play a critical role in the development of skin diseases, such as atopic dermatitis. Therefore, we investigated whether cosmetic dyes influenced the production of TSLP by keratinocytes...
January 9, 2018: Biomolecules & Therapeutics
Tapan Dey, Prachurjya Dutta, Prasenjit Manna, Jatin Kalita, Hari Prasanna Deka Boruah, Alak Kumar Buragohain, Balagopalan Unni
Vasicinone, a quinazoline alkaloid from Adhatoda vasica Nees. is well known for its bronchodilator activity. However its anti-proliferative activities is yet to be elucidated. Here-in we investigated the anti-proliferative effect of vasicinone and its underlying mechanism against A549 lung carcinoma cells. The A549 cells upon treatment with various doses of vasicinone (10, 30, 50, 70 μM) for 72 h showed significant decrease in cell viability. Vasicinone treatment also showed DNA fragmentation, LDH leakage, and disruption of mitochondrial potential, and lower wound healing ability in A549 cells...
January 9, 2018: Biomolecules & Therapeutics
Qiuming Liu, Yali Cao, Ping Zhou, Shimin Gui, Xiaobo Wu, Yong Xia, Jianhong Tu
Because of the unsatisfactory treatment options for breast cancer (BC), there is a need to develop novel therapeutic approaches for this malignancy. One such strategy is chemotherapy using non-toxic dietary substances and botanical products. Studies have shown that Panduratin A (PA) possesses many health benefits, including anti-inflammatory, anti-bacterial, anti-oxidant and anticancer activities. In the present study, we provide evidence that PA treatment of MCF-7 BC cells resulted in a time- and dosedependent inhibition of cell growth with an IC₅₀ of 15 μM and no to little effect on normal human MCF-10A breast cells...
January 5, 2018: Biomolecules & Therapeutics
Taedong Han, Byoung Moon Lee, Yoo Hoi Park, Dong Hoon Lee, Hyun Ho Choi, Taehoon Lee, Hakwon Kim
G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as the secretion of glucagon-like peptide-1 (GLP-1) in intestinal L cells, consequently improving glucose-stimulated insulin secretion. Due to this dual mechanism of action, the development of small-molecule GPR119 agonists has received significant interest for the treatment of type 2 diabetes. We newly synthesized 1,2,4-triazolone derivatives of GPR119 agonists, which demonstrated excellent outcomes in a cyclic adenosine monophosphate (cAMP) assay...
March 1, 2018: Biomolecules & Therapeutics
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