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简介：Thymoquinone(TQ),anactivecomponentderivedfromthemedialplantNigellasativa,hasbeenusedformedicalpurposesformorethan2000years.RecentstudieshavereportedthatTQblockedangiogenesisinanimalmodelandreducedmigration,adhesion,andinvasionofglioblastomacells.WehaverecentlyshownthatTQcouldexhibitapotentcytotoxiceffectandinduceapoptosisinmouseneuroblastoma(Neuro-2a)cells.Inthepresentstudy,TQtreatmentmarkedlydecreasedtheadhesionandmigrationofNeuro-2acells.TQdown-regulatedMMP-2andMMP-9proteinexpressionandmRNAlevelsandtheiractivities.Furthermore,TQsignificantlydown-regulatedtheproteinexpressionoftranscriptionfactorNF-κB(p65)butnotsignificantlyalteredtheexpressionofN-Myc.Takentogether,ourdataindicatedthatTQ'sinhibitoryeffectonthemigrationofNeuro-2acellswasmediatedthroughthesuppressionofMMP-2andMMP-9expression,suggestingthatTQtreatmentcanbeapromisingtherapeuticstrategyforhumanmalignantneuroblastoma.

简介：Thestereochemistryoftwo6,9-oxygenbridgedibenzocyclooctadienelignansfromKadsuracoccinea,aredifficulttoseparateandveryunstable.Thepresentstudywasdesignedtodevelopahigh-performanceliquidchromatographyusingcirculardichroismdetectionfortheanalysisofthestereochemistry.Anew6,9-oxygenbridgedibenzocyclooctadienelignansnamedKadsulignanQwasfirstlyfoundwithanS-biphenylconfiguration.TheothercompoundwasidentifiedasKadsulignanLwithanR-biphenylconfiguration.Inordertoobtainkineticdataontheirreversibleinterconversion,thestabilitywasmeasuredatdifferentdeuteratedsolventssuchasdeuteratedmethanol,deuteratedchloroformanddeuterateddimethylsulfoxide.Thelignansweremoreunstableandconvertedmoreeasilyindeuteratedmethanolthanindeuteratedchloroformanddeuterateddimethylsulfoxide.

简介：Capsaicin(trans-8-methyl-N-vanillyl-6-nonenamide)isthemaincomponentinhotpeppers,includingredchilipeppers,alapenos,andhabanero,belongingtothegenusCapsicum.Capsaicinisapotentantioxidantthatinterfereswithfreeradicalactivities.Inthepresentstudy,thepossibleprotectiveeffectofcapsaicinwasstudiedagainstmethylmethanesulphonate(MMS)inducedtoxicityinthirdinstarlarvaeoftransgenicDrosophilamelanogaster(hsp70-lacZ)Bg~9.ThethirdinstarwasallowedtofeedonthediethavingdifferentdosesofcapsaicinandMMSseparatelyandincombination.TheresultssuggestedthattheexposureofthirdinstarlarvaetothediethavingMMSaloneshowedsignificanthsp70expressionaswellastissueDNAandoxidativedamage,whereasthelarvaefeedonthediethavingMMSandcapsaicinshowedadecreaseinthetoxiceffectsfor48-hofexposure.Inconclusion,capsaicinshowedadose-dependentdecreaseinthetoxiceffectsinducedbyMMSinthethirdinstarlarvaeoftransgenicDrosophilamelanogaster.

简介：目的：研究四逆汤及拆方水煎液对体外培养的缺血缺氧大鼠心肌细胞H9C2的保护作用。方法：利用厌氧培养盒构建厌氧环境,以D-Hanks液模拟缺血液,构建H9C2的缺血缺氧模型;将加有D-Hanks稀释过的四逆汤及拆方水煎液的H9C2置于厌氧盒中培养,MTT法测定H9C2的存活率;ELISA法测定细胞培养上清中肿瘤坏死因子-α（TNF-α）、肌酸激酶同工酶（CK-MB）的含量。结果：四逆汤及拆方加药组（四逆汤加药组、附子＋干姜加药组、附子＋甘草加药组、甘草＋干姜加药组、甘草加药组、附子加药组、干姜加药组）在浓度均为5mg生药/ml时,与模型组比较均能提高H9C2的存活率;其中附子＋干姜组（108.2±5.0）、四逆汤全方组（82.3±2.0）、附子组（78.4±10.0）均能明显提高缺血缺氧H9C2的存活率;细胞上清中CK-MB含量与TNF-α含量呈正相关（r=0.866）,细胞存活率与TNF-α含量呈负相关（r=-0.0846）。结论：四逆汤及拆方水煎液通过抑制细胞TNF-α的释放,显著减少H9C2的凋亡,提高细胞存活率,对缺血缺氧的H9C2有直接保护作用。

简介：目的:观察温阳通脉方含药血清是否在内质网应激相关通路对心肌细胞缺氧/复氧损伤的作用,并探究体外培养时最佳给药剂量。方法:以20%含药血清处理,用四甲基偶氮唑盐(MTT)法测得CoCl2烫最佳浓度和各组细胞存活率;比色法检测各组半胱氨酸蛋白酶3(Caspase3)酶活性和上清液中乳酸脱氢酶(LDH)活性;Hoechst33342荧光染色观察各组细胞凋亡形态变化;流式细胞术检测各组细胞凋亡率;WesternBlot法检测各组内质网应激相关蛋白GRP78、Caspase12、CHOP表达以及凋亡相关蛋白Bcl-2、Bax表达情况。结果:与空白对照组血清相比,模型组细胞活性明显降低,Caspase3酶活性和LDH活性明显升高,细胞凋亡数量明显增多,凋亡率明显升高,GRP78、Caspase12、CHOP和Bax表达明显增多,Bcl-2表达明显减少;与模型组相比,3.24、6.48、12.96g/kg组含药血清能够不同程度改善细胞活性,Caspase3酶活性和LDH活性明显减少,凋亡率不同程度降低,GRP78、Caspase12、CHOP和Bax表达明显减少,Bcl-2表达不同程度增多。结论:温阳通脉方能减轻缺氧/复氧后H9C2心肌细胞损伤,其机制可能与温阳通脉方抵抗内质网应激介导的细胞凋亡有关,其抗凋亡程度呈剂量依赖性,以温阳通脉方12.96g/kg组效果最佳。

简介：Thepresentstudywasdesignedtosynthesize2-Cyano-3,12-dioxooleana-1,9(11)-en-28-oate-13β,28-olide(1),alactonederivativeofoleanolicacid(OA)andevaluateitsanti-inflammatoryactivity.Compound1significantlydiminishednitricoxide(NO)productionanddown-regulatedthemRNAexpressionofiNOS,COX-2,IL-6,IL-1β,andTNF-αinlipopolysaccharide(LPS)-stimulatedRAW264.7cells.FurtherinvivostudiesinmurinemodelofLPS-inducedacutelunginjury(ALI)showedthat1possessedmorepotentprotectiveeffectsthanthewell-knownanti-inflammatorydrugdexamethasonebyinhibitingmyeloperoxidase(MPO)activity,reducingtotalcellsandneutrophils,andsuppressinginflammatorycytokinesexpression,andthusamelioratingthehistopathologicalconditionsoftheinjuredlungtissue.Inconclusion,compound1couldbedevelopedasapromisinganti-inflammatoryagentforinterventionofLPS-inducedALI.