新型苯并噁唑酮类衍生物4-邻甲基苯磺酰氧基-苯并噁唑酮(MBB)抗炎作用的研究
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- 英文论文题名：Study on Anti-Inflammatory Effects of 4-(2-methylphenylsulfonyloxy)-2(3H)-benzoxazolone(MBB)
- 论文作者：罗捷然 ; 唐莉 ; 葛睿 ; 李青山
- 英文论文作者：LUO Jieran ; TANG Li ; GE Rui ; LI Qingshan ; Schooi of Pharmaceutical Science ; Shanxi Medical University
- 年：2016
- 作者机构：山西医科大学药学院;
- 论文关键词：MBB ; 抗炎作用 ; 作用机制
- 英文论文关键词：MBB ; Anti-inflammation ; Action mechanism
- 会议召开时间：2016-09-27
- 会议录名称：中国药学会第十三届青年药学科研成果交流会论文集
- 语种：中文
- 分类号：R965
- 学会代码：YYWS
- 会议名称：中国药学会第十三届青年药学科研成果交流会
- 会议地点：中国江西南昌
- 主办单位：中国药学会
- 学会名称：中国药学会
- 页数：5
- 文件大小：466k
- 原文格式：O
- 会议级别：全国
摘要
目的:研究新型苯并噁唑酮衍生物4-邻甲基苯磺酰氧基-苯并噁唑酮(MBB)的抗炎作用,并初步探讨其抗炎作用机制。方法:采用二甲苯致小鼠耳肿胀和角叉菜胶致大鼠足跖肿胀炎症模型观察MBB的体内抗炎作用;采用脂多糖(LPS)诱导的小鼠单核巨噬细胞(RAW264.7)炎症模型观察MBB体外抗炎作用,Griess法测定细胞培养液中NO的释放量,ELISA法测定细胞培养液中TNF-α、IL-6和IL-1β的含量。结果:MBB对二甲苯所致的小鼠耳肿胀和角叉菜胶致大鼠足跖肿胀有明显的抑制作用;MBB对LPS诱导的RAW264.7细胞培养液中炎症因子NO、TNF-α、IL-6和IL-1β的分泌有显著的抑制作用,并呈现一定的量效关系。结论:MBB可以通过抑制NO的释放和TNF-α、IL-6、IL-1β的表达发挥抗炎作用。
OBJECTIVE To study the anti-inflammatory effects of 4-(2-methylphenylsulfonyloxy)-2(3H)-benzoxazolone(MBB).METHODS The anti-inflammatory effects in vivo were investigated using xylene-induced mouse ear swelling and carrageenan-induced rat paw edema models.Meanwhile,the contents of NO,TNF-α,IL-6 and IL-ip in LPS-induced RAW264.7 cell supernatant were detected by Griess and ELISA methods to evaluate the anti-inflammatory activity in vitro.RESULTS MBB could markedly suppress the ear swelling and the paw edema in vivo.The levels of NO,TNF-α,IL-6 and IL-ip on LPS-induced RAW264.7 cells were significantly reduced after treated with MBB,and presented dose-effect relationships.CONCLUSION MBB presented determined anti-inflammation activity through inhibiting the secretion of NO,TNF-α,EL-6 and IL-1β.
OBJECTIVE To study the anti-inflammatory effects of 4-(2-methylphenylsulfonyloxy)-2(3H)-benzoxazolone(MBB).METHODS The anti-inflammatory effects in vivo were investigated using xylene-induced mouse ear swelling and carrageenan-induced rat paw edema models.Meanwhile,the contents of NO,TNF-α,IL-6 and IL-ip in LPS-induced RAW264.7 cell supernatant were detected by Griess and ELISA methods to evaluate the anti-inflammatory activity in vitro.RESULTS MBB could markedly suppress the ear swelling and the paw edema in vivo.The levels of NO,TNF-α,IL-6 and IL-ip on LPS-induced RAW264.7 cells were significantly reduced after treated with MBB,and presented dose-effect relationships.CONCLUSION MBB presented determined anti-inflammation activity through inhibiting the secretion of NO,TNF-α,EL-6 and IL-1β.
引文
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[6]Li Y Y,Huang ShyhShyun,Lee M M,et al.Anti-inflammatory activities of cardamonin from Alpinia katsumadai through heme oxygcnasc-linduction and inhibition of NF-kappaB and MAPK signaling pathway in the carragccnan-induced paw edema[J].International immunopharmacoloigy,2015,25(2):332-339.
[7]SUN T,WANG C X,LI D H,et al.C57BL/6J Establishment and evaluation of acute model of C57BV6 paw edema inflammation mice.Journal of Chongqing Medical University(重庆大学学报),2016,41(2):175-178.
[8]CHEN J S,WU H,CAO Y.Effect of nitric oxide(NO)on TNF-α,IL-2,IL-10 in rat with inflammation.Modern Journal of Integrated Traditional Chinese and Western Medicine(现代中西医结合杂志),2013,22(21):2294-2296.
[9]Atsushi Suzuki,Teshikatsu Hanada,Keiichi Mitsuyama,et al.CIS3/SOCS3/SSI3 plays a negative regulatory role in STAT3 activation and intestinal inflammation[J].Journal of Experimental Medicine,2001,193(4):471-481.
[10]Li Yi,de Haar Colin,Chen Min,et al.Disease-related expression of the IL-6/STAT3/SOCS3 signalling pathway in ulcerativa colitis and ulcerative colitis-related carcinogenesis[J].GUT,2010,59(2):227-235.
[2]DENG B L,Cullen M D,ZHOU Z,et al.Synthesis and anti-HIV activity of new alkenyldiaryl-methane(ADAM)non-nucleoside reverse transcriptase inhibitors(NNRTIs)incorporating benzoxazolone and benzisoxazole rings[J].Bioorganic&Medicinal Chemistry,2006,14(7):2366-2374.
[3]FENG L,ZHANG T C,JU X L.Synthesis and characterization of benzoxazolone derivatives.Journal of Wuhan Institute of Technology(武汉工程大学学报),2011,33(5):12-14.
[4]XU S Y,BINA R L,CHEN X.Methodology of Pharmacological Experiment(药理实验方法学)[M].Vol 3.Beijing:People's Medical Publishing House,2001:1758-1765.
[5]SHOU G L.Advancements in Understanding of Relationship Between TNF-αand Essential Hypertension.Advances in Cardiovascular Diseases(心血管病学进展),2010,31(3):430-431.
[6]Li Y Y,Huang ShyhShyun,Lee M M,et al.Anti-inflammatory activities of cardamonin from Alpinia katsumadai through heme oxygcnasc-linduction and inhibition of NF-kappaB and MAPK signaling pathway in the carragccnan-induced paw edema[J].International immunopharmacoloigy,2015,25(2):332-339.
[7]SUN T,WANG C X,LI D H,et al.C57BL/6J Establishment and evaluation of acute model of C57BV6 paw edema inflammation mice.Journal of Chongqing Medical University(重庆大学学报),2016,41(2):175-178.
[8]CHEN J S,WU H,CAO Y.Effect of nitric oxide(NO)on TNF-α,IL-2,IL-10 in rat with inflammation.Modern Journal of Integrated Traditional Chinese and Western Medicine(现代中西医结合杂志),2013,22(21):2294-2296.
[9]Atsushi Suzuki,Teshikatsu Hanada,Keiichi Mitsuyama,et al.CIS3/SOCS3/SSI3 plays a negative regulatory role in STAT3 activation and intestinal inflammation[J].Journal of Experimental Medicine,2001,193(4):471-481.
[10]Li Yi,de Haar Colin,Chen Min,et al.Disease-related expression of the IL-6/STAT3/SOCS3 signalling pathway in ulcerativa colitis and ulcerative colitis-related carcinogenesis[J].GUT,2010,59(2):227-235.