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[1]陳曉明 蔡 蕾 黃劍清 黃舒燕 鄭從燊 黃衛(wèi)東.mTOR抑制劑西羅莫司及其衍生物對(duì)黑色素瘤細(xì)胞株A375的 抑制作用[J].福建醫(yī)藥雜志,2019,41(04):110-114.
 CHEN Xiaoming,CAI Lei,HUANG Jianqing,et al.Effectiveness of mTOR inhibitor Sirolimus and its derivates on melanoma cell line A375[J].FUJIAN MEDICAL JOURNAL,2019,41(04):110-114.
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mTOR抑制劑西羅莫司及其衍生物對(duì)黑色素瘤細(xì)胞株A375的 抑制作用()
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《福建醫(yī)藥雜志》[ISSN:1002-2600/CN:35-1071/R]

卷:
41
期數(shù):
2019年04期
頁(yè)碼:
110-114
欄目:
基礎(chǔ)研究
出版日期:
2019-08-15

文章信息/Info

Title:
Effectiveness of mTOR inhibitor Sirolimus and its derivates on melanoma cell line A375
文章編號(hào):
1002-2600(2019)04-0110-05
作者:
陳曉明 蔡 蕾1 黃劍清1 黃舒 燕1 鄭從燊 黃衛(wèi)東12
福建省微生物研究所(福州 350007)
Author(s):
CHEN Xiaoming CAI Lei HUANG Jianqing HUANG Shuyan ZHENG Congshen HUANG Weidong
Fujian Institute of Microbiology, Fuzhou, Fujian350007, China
關(guān)鍵詞:
西羅莫司 依維莫司 替西羅莫司 黑色素瘤
Keywords:
sirolimus everolimus temsirolimus melanoma
分類號(hào):
R739.5
文獻(xiàn)標(biāo)志碼:
A
摘要:
目的 比較臨床上使用的mTOR抑制劑西羅莫司、依維莫司和替西羅莫司對(duì)黑色素 瘤細(xì)胞株A375的抑制作用,為mTOR抑制劑治療黑色素瘤提供參考。方法 SRB 蛋白染色法檢測(cè) 藥物對(duì)A375細(xì)胞增殖的影響,Annexin V-FITC/PI雙染法檢測(cè)藥物對(duì)A375細(xì)胞凋亡的影響,PI 標(biāo)記檢測(cè)藥物對(duì)A375細(xì)胞周期的影響,Western blot檢測(cè)藥物對(duì)A375細(xì)胞mTOR及其下游蛋白 磷酸化的影響。結(jié)果 mTOR抑制劑西羅莫司、依維莫司和替西羅莫司具有很強(qiáng)的抑制黑色素 瘤細(xì)胞株A375增殖的作用,能夠誘導(dǎo)A375細(xì)胞凋亡、阻滯細(xì)胞周期于G1期,并抑制A375細(xì)胞 mTOR及其下游蛋白激酶4EBP1和p70S6K1的磷酸化。在這3個(gè)mTOR抑制劑中,依維莫司較西羅莫 司和替西羅莫司表現(xiàn)出對(duì)A375更強(qiáng)的活性。結(jié)論 依維莫司較替西羅莫司和西羅莫司在黑色 素瘤的治療上可能更有意義。
Abstract:
Objective To compare the effectiveness of clinic mTOR inhibitors Sirolimus, Everolimus and Temsirolimus on melanoma cell line A375, which will provide insights into clinic application of mTOR inhibitors in melanoma. Methods Sulforhodamine B(SRB)assay was used to investigate the effectiveness of inhibitors on A375 cell proliferation. Annexin V-FITC/PI staining was performed to detect apoptosis. Propidium iodide(PI)staining was to analyze the influence of inhibitors on cell cycle. Western blot was applied to determine the regulation of mTOR as well as its downstream signaling. Results All of three mTOR inhibitors showed potent cell growth inhibition on A375. Mechanistically, they can promote A375 cell apoptosis, lead to cell cycle arrest at G1 phase by blocking mTOR and phosphorylation of its downstream targets 4EBP1 and p70S6K1. Everolimus exhibited more potent activity against Sirolimus and Temsirolimus. Conclusion Everolimus is a more promising drug for melanoma treatment.

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備注/Memo

備注/Memo:
基金項(xiàng)目:福建省自然科學(xué)基金資助項(xiàng)目(2015J01362); 福州市臨床重點(diǎn)專科建設(shè)項(xiàng)目 (201807111); 福州市皮膚病與醫(yī)學(xué)中心建設(shè)項(xiàng)目(2018080309) 1 福建省福州市皮膚病防治院; 2 通信作者,Email:[email protected]
更新日期/Last Update: 2019-08-15