Park, Hyun-Jin;Hong, Hee-Kyung;Song, Yi-Seul;Hong, Min-Sung;Seo, Han-Sol;Hong, Dong-Hyun;Lee, Dong-Won;Khang, Gil-Son
Polymer(Korea)
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v.34
no.4
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pp.300-305
/
2010
Zaltoprofen is a propionic acid derivative of non-steroidal anti-inflammatory drugs (NSAIDs) and has been widely used in the treatment of a number of arthritic conditions or lumbago. Zaltoprofen has low water solubility and low bioavailability, therefore great efforts have been devoted to enhance the extent of drug adsorption. In this study, zaltoprofen was formulated into a tablet to enhance the bioavailability and to achieve sustained-release using additives such as lactose monohydrate, carboxymethylcellulose (CMC), hydroxypropylmethylcellulose (HPMC). Fourier transform-infrared (FTIR) and differential scanning calorimeter (DSC) were employed to study the structure and crystallization of zaltoprofen in the tablet with various contents of additives. It was found that additives had interactions with zaltoprofen and inhibited the crystallization of zaltoprofen. Tablets containing low viscosity HPMC showed a higher release than those containing high viscosity HPMC. Also, as the amount of CMC increased zaltoprofen release increased.
The purpose of present study is to investigate the role of artesunate (ART) in enhancing anticancer effect of nonsteroidal anti-inflammatory drug (NSAID) on human cancer cells, and we elucidate a possible molecular mechanism of this combination effect. We showed that the combined effect of ART with NSAID such as celecoxib (CCB) or dimethyl-CCB (DMC) in various type of human cancer cells. After ART treatment, the expression of p62, nuclear factor erythroid 2-like 2 (NRF2) and cancer stemness (CS)-related proteins including CD44, CD133, aldehyde dehydrogenase 1 (ALDH1), octamer-binding transcription factor 4 (Oct4), mutated p53 (mutp53) and c-Myc was down-regulated. ART induced autophagy as reduction of the autophagy receptor p62, which was associated with up-regulation of activating transcription factor 4 (ATF4) and C/EBP homologous protein (CHOP), and simultaneous down-regulation of NRF2 and CS-related proteins was occurred in the human cancer cells. These results indicate a possibility that ART activates autophagy through ATF4-CHOP cascade leading to down-regulation of CS-related proteins and subsequently eradicated cancer stem cells. In addition, co-treatment with ART and imatinib was more effective than either drug alone on growth inhibition and apoptosis induction of cancer cells. In conclusion, induction of autophagy-dependent cell death by ART might play a critical role in mediating the synergistic effect of drug combination (ART/NSAID and ART/imatinib). Therefore, ART could be a promising candidate as a chemosensitizer to enhance the anticancer effects of NSAID and imatinib.
Sesquiterpene lactones (STLs) are terpenoids found mostly in the Asteraceae family and are known for their strong cytotoxic properties, among other notable bioactivities. Some STLs, such as artemisinin and mipsagargin, are already commercially available and are used to fight malaria and tumor growth, respectively. Although the interest in STLs was low for a time after their discovery due to their toxic nature, past decades have witnessed a soar in STL-based studies focused on developing novel pharmaceuticals via chemical diversification. These studies have reported several promising physiological effects for STLs, including lower toxicity and diverse modes of action, and have demonstrated the antimicrobial, antioxidant, hepatoprotective, antiviral, antiprotozoal, phytotoxic, antitumor, and antiaging properties of STLs. STLs are mainly considered as valuable natural molecules for the fight against cancer since most STLs induce death of different types of cancer cells, as shown by in vitro and in vivo studies. Some STLs can also enhance the effects of drugs that are already in clinical use. Medicinal chemists use various STLs as starting molecules for the synthesis of new STLs or different bioactive compounds. All these developments warrant future research to provide more information on STLs, their bioactivities, and their mode of action. In this context, this review has summarized the bioactivities of some of the widely studied STLs, namely artemisinin, costunolide, thapsigargin, arglabin, parthenolide, alantolactone, cynaropicrin, helenalin, and santonin.
Kwon, Huiyoung;Cho, Eunbi;Jeon, Jieun;Lee, Young Choon;Kim, Dong Hyun
Journal of Life Science
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v.29
no.5
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pp.564-569
/
2019
Heavy drinking disrupts the nervous system by activation of GABA receptors and inhibition of glutamate receptors, thereby preventing short-term memory formation. Degradation of cognition by alcohol induces blackouts, and it can lead to alcoholic dementia if repeated. Therefore, drugs need to be developed to prevent alcohol-induced blackout. In this study, we confirmed the effect of an ethanol extract of Cassia obtusifolia seeds (COE) on alcohol-induced memory impairment. The effects of COE and ethanol on cognitive functions mice were examined using the passive avoidance and Y-maze tests. The manner in which alcohol affects long-term potentiation (LTP) in relation to the learning and memory was confirmed by electrophysiology performed on mouse hippocampal slices. We also measured N-methyl-D-aspartate (NMDA) receptor-mediated field excitatory synapses (fEPSPs), which have a known association with cognitive impairment caused by ethanol. Ethanol caused memory impairments in passive avoidance and Y-maze tests. COE prevented these ethanol-induced memory impairments in these tests. Ethanol also blocked LTP induction in the mouse hippocampus, and COE prevented this ethanol-induced LTP deficit. Ethanol decreased NMDA receptor-mediated fEPSPs in the mouse hippocampus, and this decrease was prevented by COE. These results suggest that COE might be useful in preventing alcohol-induced neurological dysfunctions, including blackouts.
Journal of Practical Agriculture & Fisheries Research
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v.17
no.1
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pp.125-132
/
2015
The report about equine anesthesias in Korea are very rare. This paper aimed at the mortality rate during anesthesia in Thoroughbred horses at Equine Hospital of Busan Race Park, KRA in South Korea from 2005 to 2010. Drugs used in anesthesia was IV injection of detomidine hydrochloride (0.01 mg/kg) or xylazine(0.5mg/kg) for sedation and premedication, Guaifenesin(50-100 mg/kg) for muscle relaxation, ketamine hydrochloride(2 mg/kg) for induction of anaesthesia and Inhalational isoflurane(1.3-1.5 %) to maintain anesthesia. Total number of anesthetic cases was 190, 150 of inhalational anesthesia and 40 of general anesthesia, repectively. The purpose of anesthesia was highest in the disorder of musculoskeletal system, followed by urogenital system and respiratory system Mortality case due to anesthesia was one during arthroscopic surgery for removal of osteochondral chip fragments. The time of anesthesia was 150 min, fatal sign was hypoxemia and the reason was improper machine operation of the anesthetist. In conclusion, the perianesthetic mortality rate during anesthesia in Thoroughbred horses at Busan Race Park was 0.52%(1 death per 190 anesthetics).
YeEun Hong;GwangYeel Seo;Byunghyun Kim;Kyuseok Kim;Haejeong Nam;YoonBum Kim
The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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v.36
no.4
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pp.30-50
/
2023
Objectives : To investigate the active compounds and therapeutic mechanisms of Atractylodes Lancea(Thunb.) D.C. and Magnolia Officinalis Rehder et Wilson in the treatment of dermatitis accompanied by pruritus, as well as their potential to complement or replace standard drugs. Methods : We conducted the network pharmacological analysis. We selected effective ingredients among the active compounds of research target herbs. Then we explore pathway/terms of the common target proteins among research target herbs, fexofenadine and disease. Results : We selected 9 active compounds are selected from Atractylodes lancea and identified 231 target proteins. Among them, 74 proteins are associated with inflammatory skin diseases that cause pruritus. These proteins are involved in various pathways including, 'Nitric-oxide synthase regulator activity', 'Hydroperoxy icosatetraenoate dehydratase activity, Aromatase activity', 'RNA-directed DNA polymerase activity', 'Arachidonic acid metabolism', 'Peptide hormone processing', 'Chemokine binding' and 'Sterol biosynthetic process'. Additionally, coregenes are involved in 'IL-17 signaling pathway'. Similarly, we selected 2 active compounds from Magnolia officinalis and identified 133 target proteins. Among them, 33 proteins are related to inflammatory skin diseases that cause pruritus. These proteins are primarily involved in 'Vascular associated smooth muscle cell proliferation' and 'Arachidonic acid metabolism'. There is no significant difference between the pathways in which coregenes are involved. Conclusions : It is expected that Atractylodes Lancea will be able to show direct or indirect anti-pruritus and anti-inflammatory effects on skin inflammation accompanied pruritus through suppressing inflammation and protecting skin barrier. Meanwhile, it is expected that Magnolia Officinalis will only be able to show indirect anti-inflammation effects. Therefore, Atractylodes Lancea and fexofenadine are believed to complement each other, whereas Magnolia Officialinalis is expected to provide supplementary support on skin disease.
Chiheon Kwon;Koung Mi Kang;Young Hun Choi;Roh-Eul Yoo;Chul-Ho Sohn;Seung Seok Han;Soon Ho Yoon
Korean Journal of Radiology
/
v.22
no.9
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pp.1547-1554
/
2021
Objective: We aimed to investigate whether repeated intravascular administration of iodinated contrast media (ICM) or gadolinium-based contrast agents (GBCAs) within a short interval was associated with an increased risk of post-contrast acute kidney injury (PC-AKI). Materials and Methods: This retrospective study included 300 patients (mean age ± standard deviation, 68.5 ± 8.1 years; 131 male and 169 female) who had undergone at least one ICM-enhanced perfusion brain CT scan, had their baseline and follow-up serum creatinine levels available, and had not undergone additional contrast-enhanced examinations 72 hours before and after a time window of interest were included. The study population was divided into three groups: single-dose group and groups of patients who had received multiple contrast administrations in the time window of interest with the minimum contrast repeat interval either within 4 hours (0-4-hour group) or between 4 to 48 hours (4-48-hour group). Multivariable logistic regression analysis was conducted to evaluate the association between AKI and repeated ICM administrations. A similar supplementary analysis was performed including both ICM and GBCA. Results: When ICM was only considered ignoring GBCA, among 300 patients, 207 patients received a single dose of ICM, 58 had repeated doses within 4 hours (0-4-hour group), and 35 patients had repeated doses between 4 to 48 hours (4-48-hour group). Most patients (> 95%) had a baseline estimated glomerular filtration rate (eGFR) of ≥ 30 mL/min/1.73 m2. AKI occurred in 7.2%, 13.8%, and 8.6% of patients in the single-dose, 0-4-hour, and 4-48-hour groups, respectively. In the 0-4-hour and 4-48-hour groups, additional exposure to ICM was not associated with AKI after adjusting for comorbidities and nephrotoxic drugs (all p values > 0.05). Conclusion: Repeated intravascular administrations of ICM within a short interval did not increase the risk of AKI in our study patients suspected of acute stroke with a baseline eGFR of ≥ 30 mL/min/1.73 m2.
Myeong-Eun Jegal;Yu-Seon Han;Shi-Young Park;Ji-Hyeok Lee;Eui-Yeun Yi;Yung-Jin Kim
Journal of Life Science
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v.34
no.6
/
pp.399-407
/
2024
Angiogenesis is the process by which new blood vessels form from existing blood vessels. This phenomenon occurs during growth, healing, and menstrual cycle changes. Angiogenesis is a complex and multifaceted process that is important for the continued growth of primary tumors, metastasis promotion, the support of metastatic tumors, and cancer progression. Impaired angiogenesis can lead to cancer, autoimmune diseases, rheumatoid arthritis, cardiovascular disease, and delayed wound healing. Currently, there are only a handful of effective antiangiogenic drugs. Recent studies have shown that natural marine products exhibit antiangiogenic effects. In a previous study, we reported that the hexane extract of H. fusiformis (HFH) could inhibit the development of new blood vessels both in vitro and in vivo. The aim of this study was to describe the inhibitory effect of chloroform extracts of H. fusiformis on angiogenesis. To investigate how chloroform extract prevents blood vessel growth, we examined its effects on HUVEC, including cell migration, invasion, and tube formation. In a mouse Matrigel plug assay, H. fusiformis chloroform extract (HFC) also inhibited angiogenesis in vivo. Certain proteins associated with blood vessel growth were reduced after HFC treatment. These proteins include vascular endothelial growth factor (VEGF), mitogen-activated protein kinase (MAPK)/extracellular signal transduction kinase, and serine/threonine kinase 1 (AKT). These studies have shown that the chloroform extract of H. fusiformis can inhibit blood vessel growth both in vitro and in vivo.
Shin, Hyeon Ju;Kim, Young Nam;Kim, Ju Hee;Son, In Sook;Bang, Kyung-Sook
Child Health Nursing Research
/
v.20
no.3
/
pp.215-224
/
2014
Purpose: This study was conducted to identify risk factors in hospitalized children, and to develop and validate a fall-risk assessment tool for hospitalized children. Methods: A retrospective chart review was performed at one university children's hospital, and an analysis was done of the characteristics of all patients who fell during a 44-month period (n=48). These patients were compared with another 149 hospitalized children who did not fall. Results: Significant predictors of falls as identified in a multivariate logistic regression analyses were age of less than 3 years old, neurological diagnosis including epilepsy, children's dependency of ADL, physical developmental delay, multiple usage of fall-risk-increasing drugs. The respective odds ratios ranged from 2.4 to 7.1 with 95% confidence interval (p<0.05). Accordingly, defining patients with either 5 risk factors as fall-prone hospitalized children provided a sensitivity of 93.6% and specificity of 16.2%. Conclusion: The results show that this tool has an acceptable level of sensitivity to assess the risk factors of fall in hospitalized children even though the specificity was low, suggesting that this tool may enable nurses to predict the risk level of childhood falls, and develop preventive strategies against pediatric falls in children's units.
Background : Non-steroidal anti-inflammatory drugs (NSAID) are useful in chemoprevention of colorectal cancers. Continuous NSAID administation causes 40% to 50% reduction in relative risk for colorectal cancer. Sulindac possesses an antiproliferative effect and induces apoptosis and tumor regression on colon cancer and other types of cancers. We intended to analyze the effects of sulindac in three non-small cell lung cancer cell lines. Materials and Methods : The human lung cancer cell lines, A549, NCI-H157 and NCI-H460 were used for this study. Viability was tested by MTT assay, and cell death rate was measured by lactate dehydrogenase(LDH) release. Apoptosis was estimated by flow cytometric analysis and nuclear staining. Results: Sulindac was able to decrease the viability of non-small cell lung cancer cells in a dose- and time- dependent manner. In a parallel effect of sulindac on cell death rate, LDH release was increased in sulindac-treated lung cancer cells. Sulindac significantly increased apoptosis characterized by an increase of $sub-G_0/G_1$ fraction and morphological change of nuclei. The rate of apoptotic cells after sulindac treatment in lung cancer cells increased in a time- and dose- dependent manner in flow cytometric analysis. Apoptotic cells were defined as nuclear shrinkage, chromatin condensation and nuclear fragmentation of cells. Conclusion : Sulindac decreases viability and induces the apoptosis of lung cancer cells. Further studies will be needed to elucidate the potential mechanism of sulindac-induced apoptosis in lung cancer cells.
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