摘要
对高良姜(Alpinia officinarum Hance)二芳基庚烷有效组分10个单体化合物进行细胞毒活性及相关炎症因子检测。采用CCK-8法测试所有化合物对乙醇诱导人胃黏膜上皮细胞(GES-1)、脂多糖(LPS)刺激小鼠单核巨噬细胞白血病细胞(RAW 264.7)的细胞毒活性;采用Griess法检测单体化合物对LPS诱导的RAW 264.7细胞NO生成的抑制活性;采用Elisa试剂盒检测GES-1细胞中COX-2和PGE-2炎症因子,RAW 264.7细胞中TNF-α、IL-1β和IL-6炎症因子。结果表明:在GES-1细胞中,单体化合物浓度为100.00、50.00、25.00、12.50、6.25、3.13、1.56、0.78μmol/L时,对乙醇诱导的GES-1细胞的毒性均较低;化合物3、4、7、8、9和10在12.50、6.25或0.78μmol/L下具有抗炎活性,其中化合物8中剂量组抑制COX-2能力最强,化合物7低剂量组与化合物10中剂量组抑制PGE-2能力最强(p<0.01);药物浓度在12.50、6.25、3.13、1.56、0.78μmol/L时,对RAW 264.7细胞毒性较小;化合物1、3、6、8、9、10在体外抑制NO生成的IC50值为(6.67±1.61)、(6.89±0.63)、(7.26±0.92)、(0.62±0.51)、(4.01±1.72)、(6.25±0.54)μmol/L,表明其具有一定的抗炎活性,其中化合物8高剂量组抑制TNF-α释放能力较强(p<0.01),化合物8的中剂量组与化合物10中剂量组抑制IL-1β释放能力较强,化合物8高剂量组抑制IL-6释放能力较强,与阳性药地塞米松相当(p<0.01)。高良姜二芳基庚烷有效组分中二芳基庚烷单体化合物7、8、10具有抗炎活性,其抗炎活性作用可能与其抑制COX-2和PGE-2炎症因子的释放有关;其中化合物8和10的抗炎活性,还可能与其抑制TNF-α、IL-1β和IL-6炎症因子有关。
To detect the cytotoxicity and related inflammatory factors of 10 monomers of diarylheptane effective fraction from Alpinia officinarum Hance.The CCK-8 method was used to test the cytotoxicity of all compounds on ethanol-induced GES-1(human gastric epithelial cells)and lipopolysaccharide(LPS)stimulated mouse monocyte-macrophage leukemia cells(RAW 264.7);the Griess method was used to detect the inhibition of monomer compounds on LPS induced NO production in RAW 264.7 cells;the relevant inflammatory factors were detected with Elisa kit.In GES-1 cells,the toxicity of monomer compounds to ethanol-induced GES-1 cells is low at 100.00、50.00、25.00、12.50、6.25、3.13、1.56、0.78μmol×L^(–1);Compounds 3,4,7,8,9,and 10 have anti-inflammatory activity at 12.50、6.25、0.78μmol×L^(–1),among them,the high-dose group of compound 8 inhibited TNF-αrelease more(p<0.01),the medium-dose group of compound 8 and the medium-dose group of compound 10 inhibited IL-1βrelease more,and the high-dose group of compound 8 inhibited IL-6 release more,which was comparable to that of the positive drug dexamethasone(p<0.01);in RAW 264.7 cells,the cytotoxicity is low at 12.50、6.25、3.13、1.56、0.78μmol×L^(–1);the IC50 value of compounds 1,3,6,8,9,and 10 inhibiting NO production in vitro was(6.67±1.61),(6.89±0.63),(7.26±0.92),(0.62±0.51),(4.01±1.72),(6.25±0.54)μmol×L^(–1).It showed that it has some anti-inflammatory activity,and the high dose group of compound 8 inhibits TNF-α;the medium dose group of compound 8 and the medium dose group of compound 10 inhibited IL-1β;the ability to inhibit IL-6 release was better in the high-dose group of compound 8,comparable to the positive drug dexamethasone(p<0.01).Diarylheptane monomers 7,8,and 10 in the effective fraction of diarylheptane from Alpinia officinalis have anti-inflammatory activity,which may be related to the inhibition of the release of COX-2 and PGE-2 inflammatory factors;the anti-inflammatory activity of compounds 8 and 10 among them may also be related to their inhibition of TNF-α,IL-1β,and IL-6 inflammatory factors.
作者
欧虹雅
屈慧娟
周小妹
张迎
魏娜
OU Hongya;QU Huijuan;ZHOU Xiaomei;ZHANG Ying;WEI Na(School of Pharmaceutical Science,Hainan Medical University,Haikou,Hainan 571199,China)
出处
《热带农业科学》
2023年第7期90-97,共8页
Chinese Journal of Tropical Agriculture
基金
海南省重点研发项目(No.ZDYF2022SHFZ127)
国家自然科学基金资助项目(No.81660649)。
关键词
高良姜
二芳基庚烷
抗炎活性
Alpinia officinarum
diarylheptane
anti-inflammatory activity
