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雷公藤内酯醇通过抑制SMYD3对骨髓瘤细胞凋亡及基质金属蛋白酶-9基因表达的影响 被引量:8
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作者 徐成波 沈建箴 +2 位作者 廖斌 付海英 林婷 《中国实验血液学杂志》 CAS CSCD 北大核心 2017年第4期1063-1068,共6页
目的:探讨雷公藤内酯醇(triptolide,TPL)抑制组蛋白甲基化酶SMYD3对多发性骨髓瘤RPMI8226细胞增殖和凋亡的影响及其作用机制。方法:采用MTT法检测不同浓度(10、20、40、80、160 nmol/L)TPL作用不同时间(24、48、72 h)对RPMI8226细胞增... 目的:探讨雷公藤内酯醇(triptolide,TPL)抑制组蛋白甲基化酶SMYD3对多发性骨髓瘤RPMI8226细胞增殖和凋亡的影响及其作用机制。方法:采用MTT法检测不同浓度(10、20、40、80、160 nmol/L)TPL作用不同时间(24、48、72 h)对RPMI8226细胞增殖的影响;应用流式细胞术检测不同浓度(40、80、160 nmol/L)TPL作用48 h后RPMI8226细胞的凋亡率;实时荧光定量PCR检测SMYD3和MMP-9基因的mRNA表达水平;Western blot法检测组蛋白H3K4me2,H3K4me3的甲基化水平。结果:TPL能够明显抑制RPMI8226细胞的增殖活性,且随作用时间延长及药物浓度增高,细胞增殖抑制率明显升高(P<0.05);不同浓度TPL作用RPMI8226细胞48 h后,随着药物浓度的增高,细胞凋亡比例逐渐增加,与空白对照组比较,差异均有统计学意义(r=0.974,P<0.05);实时荧光定量PCR结果显示,不同浓度TPL作用RPMI8226细胞48 h后,随着药物浓度的增高,SMYD3的mRNA相对表达水平呈浓度依赖性下降,与空白对照组比较,差异均有统计学意义(r=-0.882,P<0.05);siRNA-SMYD3转染RPM I8226细胞48 h后,siRNA-SM YD3组与空白对照组比较MMP-9的mRNA相对表达水平明显下降,与80nmol/L的TPL作用一致;Western blot结果显示,不同浓度的TPL作用RPM I8226细胞48 h后,随着药物浓度的增高,组蛋白H3K4me2和H3K4me3的甲基化水平呈浓度依赖性下降,分别与空白对照组比较,差异均有统计学意义(r=-0.971,r=-0.985,P<0.05);siRNA-SMYD3转染RPMI8226细胞48 h,组蛋白H3K4me2和H3K4me3的甲基化水平也明显下降,分别与siRNA阴性对照组、空白对照组比较,差异均有统计学意义(P<0.05)。结论:TPL对多发性骨髓瘤RPMI8226细胞增殖具有明显的抑制作用,并可诱导细胞凋亡,其机制与抑制SMYD3,调控组蛋白H3K4甲基化和MMP-9基因转录激活有关。 展开更多
关键词 雷公藤内醇酯 多发性骨髓瘤 凋亡 SMYD3 MMP-9
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16-Hydroxytriptolide" An Active Compound from Tripterygium wilfordii 被引量:1
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作者 马鹏程 吕燮余 +1 位作者 杨晶晶 郑启泰 《Journal of Chinese Pharmaceutical Sciences》 CAS 1992年第2期12-18,共7页
From the dried roots and leaves of Tripterygium wilfordii^(1.2),a new diter- penoid triepoxide,16-hydroxytriptolide was isolated,and its structure and stereochemistry elucidated as 16-(S)-hydroxy-triptolide on the bas... From the dried roots and leaves of Tripterygium wilfordii^(1.2),a new diter- penoid triepoxide,16-hydroxytriptolide was isolated,and its structure and stereochemistry elucidated as 16-(S)-hydroxy-triptolide on the basis of spectral data(IR, MS, UV,~1HNMR,^(13)CNMR,2d-NMR,Selective Long-range DEPT)and x-ray crystallographic analysis.This compound showed definite antiinflammatory action,strong immunosuppressive and antifertile activities.In addition,a known compound,triptolide was also isolated and all the spectral signals of^1 HNMR and ^(13)CNMR were assigned. 展开更多
关键词 Tripterygium wilfordii Diterpenoid lactone Diterpenoid epoxide 16-Hy-droxytriptolide TRIPTOLIDE
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Effect of Triptolide on Reproductive Endocrinology and Dihydrotestosterone Receptors in Rats 被引量:1
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作者 王英 孙亦彬 +3 位作者 陈巧琴 卢春燕 宗书东 钱志坚 《Journal of Chinese Pharmaceutical Sciences》 CAS 1993年第1期53-58,共6页
Triptolide was given orally to adult male Sprague-Dawley rat sat a dosage of 75 μg/kg for 35 days.After 28 days of treatment,the result of mating tests showed that all the drug treated rats were infertile.At the end ... Triptolide was given orally to adult male Sprague-Dawley rat sat a dosage of 75 μg/kg for 35 days.After 28 days of treatment,the result of mating tests showed that all the drug treated rats were infertile.At the end of drug treatment,the density of caudal spermatozoa and the weight of cpididymis were reduced significantly.All the spermatozoa were immobile.There was no detectable damage of spermatogenesis and epididymal epithelia in triptolide treated rats under microscopical examination.However,modcrate and severe damage of spermatozoa were seen in the corpus and caudal epididymis.The content of cytosolic and nuclear dihydrotestosterone (DHT) receptors in the caput and caudal epididymides was increased but insignificantly as compared with that of the controls.However, the content of DHT receptor in the cytosal of the ventral prostate was elevated very,significantly (P< 0.01).This result suggests that one of the sitcs of action of triptolide might be the epididymis. 展开更多
关键词 TRIPTOLIDE RAT Reproductive endocrinology DHT receptors
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