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新齐墩果酸衍生物抑制人肝癌SMMC-7721细胞增殖及诱导凋亡的研究 被引量:4
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作者 范新凤 王鹏龙 +4 位作者 杜海渊 孙耀贵 段智变 雷海民 李宏全 《中国药学杂志》 CAS CSCD 北大核心 2016年第24期2114-2118,共5页
目的探讨一种新齐墩果酸衍生物(3β-hydroxyolea-12-en-28-oic acid-3,5,6-trimethylpyrazin-2-methyl ester,简称为受试物)对人肝细胞癌细胞株SMMC-7721细胞的抗肿瘤作用机制。方法应用四甲基偶氮唑蓝(MTT)法及细胞形态学观察新齐墩果... 目的探讨一种新齐墩果酸衍生物(3β-hydroxyolea-12-en-28-oic acid-3,5,6-trimethylpyrazin-2-methyl ester,简称为受试物)对人肝细胞癌细胞株SMMC-7721细胞的抗肿瘤作用机制。方法应用四甲基偶氮唑蓝(MTT)法及细胞形态学观察新齐墩果酸衍生物对SMMC-7721细胞增殖及形态的影响;Annexin V联合PI染色法检测新齐墩果酸衍生物对细胞膜以及用JC-1染色法检测线粒体膜电位的损伤程度;Western blotting检测新齐墩果酸衍生物对凋亡相关蛋白Bcl-2,Bax,caspase-9 and caspase-3的表达。结果新齐墩果酸衍生物能抑制人SMMC-7721细胞增殖力,与浓度和时间呈正相关,作用细胞48 h后,细胞出现核固缩,细胞裂解,产生凋亡小体等形态学改变,细胞膜完整性被破坏,线粒体膜电位(Δψm)被降低,Bax、pro-caspase-9、cleaved caspase-9、pro-caspase-3以及cleaved caspase-3蛋白表达水平被上调,Bcl-2蛋白表达水平被下调。结论这种新齐墩果酸衍生物在人SMMC-7721细胞中发挥抗癌作用可能与其破坏了线粒体功能有关。 展开更多
关键词 3β-hydroxyolea-12-en-28-oic acid-3 5 6-tnmethylpyrazin-2-methyl ESTER 人SMMC-7721细胞 凋亡 线粒体
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Abietane derived diterpenoids as Ca_(v)3.1 antagonists from Salvia digitaloides 被引量:1
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作者 Jianjun Zhao Shuzong Du +6 位作者 Kun Hu Yali Hu Fan Xia Yansong Ye Jian Yang Yin Nian Gang Xu 《Chinese Chemical Letters》 SCIE CAS CSCD 2023年第4期178-182,共5页
Nineteen diterpenoids, including saldigitin A(1) bearing an unprecedented 10-methylated 6/7/6 carbon ring system, two new icetexanes(2, 3), and two new nor-abietanes(5, 6) were characterized from the roots of Salvia d... Nineteen diterpenoids, including saldigitin A(1) bearing an unprecedented 10-methylated 6/7/6 carbon ring system, two new icetexanes(2, 3), and two new nor-abietanes(5, 6) were characterized from the roots of Salvia digitaloides. Their structures were elucidated by the analysis of the spectroscopic data,X-ray crystallography, and TDDFT calculations of ECD spectra. The novel architecture of 1 should be biogenetically derived through the cleavage and re-cyclization of the B/C rings from the normal abietane skeleton. Biologically, 1–5 exhibited noticeable inhibitions on Ca_(v)3.1 low voltage-gated Ca2+channel(LVGCC), with IC50values in the range of 3.43–11.70 μmol/L. They are the first example of diterpenoids with 6/7/6 carbon rings system as Ca_(v)3.1 antagonists. 展开更多
关键词 10-methylated 6/7/6 carbon ring system Icetexane DITERPENOID Salvia digitaloides Ca_(v)3.1 low voltage-gated Ca^(2+)channel (LVGCC)
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