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박필훈 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.11
Adipose tissue acts as a dynamic endocrine organ playing critical roles in many metabolic and immune responses. Endocrine functions by adipose tissue are achieved by secretion of diverse cytokines and hormones, collectively called adipokines. Adiponectin and leptin the most abundantly expressed adipokines within adipose tissue have an impact on various physiological responses. While both adiponectin and leptin are secreted from the same location, their physiological functions are not identical. Adiponectin possesses potent anti-inflammatory properties and anti-tumor activities, whereas leptin acts as a pro-inflammatory hormone and generates tumor-promoting effects. Autophagy, a highly conserved intracellular self-digestive process, is implicated in the maintenance of diverse physiological responses. In particular, autophagy plays dual roles in the regulation of cell death/survival (e.g., inducing cell death and cytoprotection) and is associated with anti-inflammatory actions. Increasing recent evidence has indicated that autophagy is implicated in various biological responses by adipokines. Therefore, autophagy would be a promising target for the management of inflammation and tumor growth by adipokines. In this review, we summarize the effects of adiponectin and leptin on autophagy induction and highlight their implications in modulating inflammatory responses and tumor growth.
박필훈,Jin Hur,김윤철,Ren-Bo An,Dong Hwan Sohn 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.9
In the present study, we investigated an anti-inflammatory effect of ethyl gallate (EG) isolated from Galla Rhois as evaluated by inhibition of nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression, and a potential role of heme oxygenase-1 (HO-1) in the inhibition of NO production elicited by EG. Treatment of RAW264.7 macrophages with EG significantly inhibited the production of NO and iNOS expression stimulated by lipopolysaccharide (LPS). We also demonstrated that EG treatment increased HO-1 mRNA and protein expression, as assessed by quantitative RT-PCR and Western blot analysis. EG treatment also increased the levels of nuclear factor-erythroid 2-related factor 2, which is critical for transcriptional induction of HO-1. In addition, treatment with SnPP (tin protoporphyrin IX), a selective HO-1 inhibitor, counteracted the inhibitory effect of EG on nitrite production, suggesting that HO-1 is, at least in part, implicated in the inhibition of NO production induced by EG treatment. Taken together, these results indicate that EG isolated from Galla Rhois suppresses NO production in LPS-stimulated RAW 264.7 macrophages via HO-1 induction.
박필훈,김학성,허진,Xing Yu Jin,Ying Lan Jin,손동환 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.1
Chalcones, a group of phenolic compounds, exhibit potent anti-inflammatory properties. In the present study, we synthesized chalcone derivative, YL-I-108 ((E)-1-(2-methoxy-4,6-bis(methoxymethoxy)phenyl)- 3-(3-nitrophenyl)prop-2-en-1-one), and examined its effect on the production of pro-inflammatory mediators. Treatment of RAW 264.7 macrophages with YL-I-108 potently inhibited nitrite production stimulated by LPS. YL-I-108 treatment also markedly inhibited expressions of inducible nitric oxide synthase (iNOS) and tumor necrosis factor-α (TNF-α). Treatment of cells with YL-I-108 significantly inhibited LPS-stimulated activator protein-1 (AP-1)-dependent reporter gene expression, whereas nuclear factor-κB (NF-κB) activity was not affected, indicating that down-regulation of iNOS expression by YL-I-108 is attributed by blockade of AP-1. In addition, YL-I-108 treatment led to an increase in heme oxygenase-1 (HO-1) mRNA and protein expression, accompanied with the increased expression of nuclear factor-erythroid 2-related factor 2 (Nrf2). Treatment with SnPP, a selective HO-1 inhibitor, reversed YL-I-108-mediated suppression of nitrite production, suggesting that HO-1 induction is implicated in the suppression of NO production by YL-I-108. In contrast, SnPP treatment did not reverse YL-I-108-mediated suppression of AP-1 activation, suggesting that AP-1 inhibition by YL-I-108 is independent of HO-1 induction. Together, these results indicate that YL-I-108 suppresses NO production in LPS-stimulated macrophages via simultaneous induction of HO-1 expression and blockade of AP-1 activation.
Pritam THAPA,장영동,박필훈,지준구,권영주,이응석 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.10
Designed and synthesized twenty-four 2,4-diaryl benzofuro[3,2-b]pyridine derivatives were evaluated for topoisomerase I and II inhibitory activities as well as cytotoxicities against several human cancer cell lines. Various aryl groups such as phenyl, 2- or 3- furyl, 2- or 3-thienyl, and 2-pyridyl were substituted at 2- or 4- position of central pyridine. Compounds 8, 12, 13, and 14, with 2-furyl either at 2- or 4- position of central pyridine showed the significant topoisomerase II inhibitory activity at 100 μM.
Taraman Kadayat,김미진,남태규,박필훈,이응석 대한화학회 2014 Bulletin of the Korean Chemical Society Vol.35 No.8
Twelve thienyl/furanyl-hydroxyphenylpropenones were systematically designed and synthesized, and evaluated for their inhibitory effect on LPS-induced ROS and NO production in RAW 264.7 macrophages. Compound 11 displayed the most significant inhibitory activity of LPS-induced ROS and NO production in RAW 264.7 macrophages. Structure-activity relationship study indicated that para-hydroxyphenyl moiety plays an important role for inhibitory activities on both LPS-induced ROS and NO production as well as 3- thienyl moiety on molecule.
아라자나쉬레스타,Aastha Shrestha,박필훈,이응석 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.7
Oxidative stress due to overproduction of reactive oxygen species (ROS) plays a major role in inflammation, cancer, and neurodegenerative disorders. In this study, 60 chalcone derivatives with fluorine (F), trifluoromethyl (CF3), trifluoromethoxy (OCF3), chlorine (Cl), and bromine (Br) in ring A and with or without hydroxy (OH) in ring B were designed, synthesized, and screened for inhibitory activity against lipopolysaccharide (LPS)-stimulated ROS production in RAW 264.7 macrophages. Structure?activity relationship study revealed the importance of a hydroxyl moiety in ring B for enhancing inhibitory activity of ROS production. Furthermore, a hydroxyl group at the ortho-position is more essential for inhibition of ROS production followed by meta- and para-positions. Among all, compound 27 that contains para-chlorine moiety in ring A and ortho-hydroxy in ring B displayed the strongest inhibitory activity (IC50 = 3.42??M) against LPS-stimulated ROS production in RAW264.7 macrophages.
Pramila Katila,Aastha Shrestha,아라자나쉬레스타,Ritina Shrestha,박필훈,이응석 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.12
A new series of thirty-two fluorinated and/or hydroxylated 2-arylidene-1-indanone derivatives were systematically designed, synthesized, and evaluated for their inhibitory activity against LPS-stimulated ROS production in RAW 264.7 macrophages. 5/6-Fluoro-1-indanone or 4-, 5-, 6-, or 7-hydroxyindanone moiety along with ortho-, meta-, or para-hydroxyphenyl, furanyl or thiophenyl moiety was prepared and evaluated. Among the synthesized compounds, compound 11 possessing 6-hydroxy-1-indanone moiety along with 5-chlorothiophenyl moiety was found to have the most potent inhibitory effect on the production of ROS in LPS-stimulated RAW 264.7 macrophages with an IC50 value of 3.29??M.
Aarajana Shrestha,,Ritina Shrestha,Sumin Lee,박필훈,Eung-Seok Lee 대한화학회 2021 Bulletin of the Korean Chemical Society Vol.42 No.3
6-Hydroxy-benzofuran-3-(2H)-ones exhibiting LPS stimulated ROS inhibition in RAW 264.7 macrophage
Til Bahadur Thapa Magar,KADAYAT TARAMAN,오혜진,박필훈,이응석 대한화학회 2017 Bulletin of the Korean Chemical Society Vol.38 No.6
Chromanone-containing compounds have been reported to possess several important biological activities. As a part of our continuing effort for discovering potent anti-inflammatory agents, a series of halogen-containing 3-benzylidenechroman-4-ones (1–15) were synthesized, and evaluated for their inhibitory effect on lipopolysaccharide (LPS)-stimulated reactive oxygen species (ROS) production in RAW 264.7 macrophages. Compounds 4 and 10 exhibited significant inhibitory activity (IC50 = 5.09 ± 1.27 and 5.11 ± 0.51 μM, respectively) against LPS-stimulated ROS production in RAW 264.7 macrophages.