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去酰基化ghrelin抑制上皮性卵巢癌细胞的增殖 被引量:2
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作者 窦磊 庞晓燕 +2 位作者 李奇 尚海 张颐 《中国医科大学学报》 CAS CSCD 北大核心 2018年第12期1102-1106,共5页
目的探讨去酰基化ghrelin (DAG)对上皮性卵巢癌细胞增殖的作用及其相关分子机制。方法培养上皮性卵巢癌细胞SKOV3,以DAG处理,并予以激动剂干预哺乳动物雷帕霉素靶蛋白(m TOR)和经典Wnt信号途径,采用CCK-8法测定细胞增殖。结果DAG呈剂量... 目的探讨去酰基化ghrelin (DAG)对上皮性卵巢癌细胞增殖的作用及其相关分子机制。方法培养上皮性卵巢癌细胞SKOV3,以DAG处理,并予以激动剂干预哺乳动物雷帕霉素靶蛋白(m TOR)和经典Wnt信号途径,采用CCK-8法测定细胞增殖。结果DAG呈剂量依赖性抑制卵巢癌SKOV3细胞的增殖。DAG抑制m TOR信号途径,抑制经典Wnt信号转录活性以及下游靶基因的mRNA水平,mTOR和Wnt信号激活可在一定程度上翻转DAG对SKOV3细胞增殖的抑制作用。结论 DAG通过抑制m TOR和经典Wnt信号通路发挥其抑制卵巢癌细胞增殖的作用,为卵巢癌防治提供新思路。 展开更多
关键词 去酰基化ghrelin 上皮性卵巢癌 增殖 mTOR信号途径 WNT信号途径
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大豆异黄酮的去酰基化结合液质联用系统提高总异黄酮含量测定准确性的研究
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作者 胡鹏飞 李锦晶 +1 位作者 李凡 易渡 《中国食品工业》 2022年第24期87-92,共6页
为了准确测定原料和产品中的总大豆异黄酮含量,建立了通过碱水解法将不稳定形式的大豆异黄酮(含丙二酰基和乙酰基)转化为稳定形式(含葡萄糖苷和苷元)的液相色谱-三重串联四极杆液质联用仪(liquid chromatography-triple tandem quadrupo... 为了准确测定原料和产品中的总大豆异黄酮含量,建立了通过碱水解法将不稳定形式的大豆异黄酮(含丙二酰基和乙酰基)转化为稳定形式(含葡萄糖苷和苷元)的液相色谱-三重串联四极杆液质联用仪(liquid chromatography-triple tandem quadrupole liquid mass spectrometer,LC-MS/MS)测定方法,并进行了验证。去酰基化后总大豆异黄酮由大豆苷、黄豆苷、染料木苷、大豆苷元、黄豆苷元、染料木素这六种化合物组成。它们的线性范围分别为0.1~4.1μg/mL、0.11~4.36μg/mL、0.12~4.84μg/mL、0.1~4μg/mL、0.11~4.58μg/mL、0.11~4.37μg/mL。大豆异黄酮原料和产品药片的相对标准偏差(RSD)分别为4%和2%,原料和片剂中各成分的回收率均在90%~110%之间,且所有组分分析完成时间不超过10分钟。大豆异黄酮量的准确测定保证了大豆异黄酮类原料中规定的异黄酮量,以及产品标签上的正确异黄酮量。 展开更多
关键词 大豆异黄酮 去酰基化 液相色谱-三重串联四极杆液质联用仪(LC-MS/MS) 保健产品 准确测定
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酰基化、非酰基化ghrelin与动脉粥样硬化 被引量:1
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作者 朱颖竑 刘乃丰 《东南大学学报(医学版)》 CAS 2012年第5期635-638,共4页
Ghrelin是近年来发现的一种促进生长激素分泌的多肽,其在体内存在两种形式,即酰基化与去酰基化ghrelin。研究发现,这两种ghrelin具有降低血压、对抗炎症反应、保护血管内皮细胞等多种生物学效应,其作用机制并不完全相同。了解ghrelin对... Ghrelin是近年来发现的一种促进生长激素分泌的多肽,其在体内存在两种形式,即酰基化与去酰基化ghrelin。研究发现,这两种ghrelin具有降低血压、对抗炎症反应、保护血管内皮细胞等多种生物学效应,其作用机制并不完全相同。了解ghrelin对动脉粥样硬化的作用具有潜在的临床价值。 展开更多
关键词 酰基ghrelin 去酰基化ghrelin 动脉粥样硬 文献综述
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胺及其衍生物的非酰基化动力学拆分 被引量:2
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作者 唐亮 李雪薇 +1 位作者 谢芳 张万斌 《有机化学》 SCIE CAS CSCD 北大核心 2020年第3期575-588,共14页
光学纯胺在合成与药物化学领域都有着广泛的应用,发展其高效的合成方法一直以来是有机化学界的研究热点.其中通过N酰基化及去酰基化动力学拆分方法获得光学纯胺化合物,已经成为合成手性胺类化合物的重要方法.近年来,基于非酰基化(或去... 光学纯胺在合成与药物化学领域都有着广泛的应用,发展其高效的合成方法一直以来是有机化学界的研究热点.其中通过N酰基化及去酰基化动力学拆分方法获得光学纯胺化合物,已经成为合成手性胺类化合物的重要方法.近年来,基于非酰基化(或去酰基化)的不对称反应实现外消旋胺的动力学拆分的报道不断涌现,包括一些氨基不参与反应的非酰基化(或去酰基化)不对称反应的外消旋胺的动力学拆分.根据氮原子是否参与反应以及反应类型的不同,总结了外消旋胺的化学催化动力学拆分的研究进展. 展开更多
关键词 光学纯胺 动力学拆分 非酶催 酰基(去酰基化) 不对称催反应
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胃饥饿素对肥胖小鼠胰岛素抵抗的影响 被引量:6
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作者 郭展宏 臧璞 邵加庆 《医学研究生学报》 CAS 北大核心 2020年第2期122-126,共5页
目的胃饥饿素对机体糖代谢的影响目前尚有争议。文中旨在通过建立高脂饮食诱导的肥胖小鼠模型,探究长期应用酰基化胃饥饿素和去酰基化胃饥饿素对小鼠胰岛素抵抗及血清炎症因子水平的影响。方法选取32只雄性C57BL/6小鼠随机分为4组,每组... 目的胃饥饿素对机体糖代谢的影响目前尚有争议。文中旨在通过建立高脂饮食诱导的肥胖小鼠模型,探究长期应用酰基化胃饥饿素和去酰基化胃饥饿素对小鼠胰岛素抵抗及血清炎症因子水平的影响。方法选取32只雄性C57BL/6小鼠随机分为4组,每组8只。除对照组外,高脂组、高脂+酰基化组、高脂+去酰基化组给予高脂饮食诱导小鼠肥胖。对照组:标准饲料喂养,每日腹腔注射等渗盐水10 mL;高脂组:高脂饲料喂养,每日腹腔注射等渗盐水10 mL;高脂+酰基化组:高脂饲料喂养,酰基化胃饥饿素0.8 mg;高脂+去酰基化组:高脂饲料喂养,去酰基化胃饥饿素0.8 mg。16周后行腹腔葡萄糖耐量试验(IPGTT),分别于注射后0 min、30 min、60 min、120 min行尾静脉取血测定血糖,绘制血糖波动曲线并计算曲线下血糖面积。计算附睾脂肪指数。取血采用酶联免疫吸附(ELISA)法测定空腹胰岛素、白细胞介素-6(IL-6)和肿瘤坏死因子-α(TNF-α)水平。比较胰岛素抵抗指数(HOMA-IR)。结果高脂饮食6周后,高脂组体重明显高于对照组(P<0.05)。给药14周、12周后,高脂+酰基化组和高脂+去酰基化组小鼠体重较高脂组明显减轻(P<0.05)。高脂+去酰基化组小鼠附睾脂肪质量[(0.92±0.32)g]较高脂组[(1.08±0.11)g]显著下降(P<0.05);空腹胰岛素水平较高脂组显著降低(P<0.05)。高脂+酰基化组和高脂+去酰基化组胰岛素抵抗指数(4.94±1.27、4.08±1.35)、IL-6[(34.82±6.23)、(36.90±5.27)pg/mL]、TNF-α[(73.01±7.75)、(69.39±8.43)pg/mL]水平明显低于高脂组[(81.70±7.53)、(45.85±6.41) pg/mL、(81.70±7.53)pg/mL],差异有统计学意义(P<0.05)。高脂组小鼠血清IL-6及TNF-α水平较对照组显著升高(P<0.05)。结论长期应用酰基化和去酰基胃饥饿素均可改善高脂饮食诱导的肥胖小鼠胰岛素抵抗和炎症水平,去酰基胃饥饿素能够降低肥胖小鼠内脏脂肪含量。 展开更多
关键词 酰基胃饥饿素 去酰基化胃饥饿素 肥胖 胰岛素抵抗 炎症
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From Bench to Bedside: Targeting Epigenetics for Cancer Therapy 被引量:1
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作者 Gui-deng LI Jin-xu FANG 《Clinical oncology and cancer researeh》 CAS CSCD 2011年第4期191-201,共11页
The initiation and progression of cancer not only involves genetic abnormalities, but also epigenetic alterations, such as DNA methylation and histone modifications. Epigenetics refers to the heritable changes that do... The initiation and progression of cancer not only involves genetic abnormalities, but also epigenetic alterations, such as DNA methylation and histone modifications. Epigenetics refers to the heritable changes that do not involve any structural changes in the target gene, i.e., DNA sequence and protein sequence. Thus, these epigenetic aberrations are potentially reversible, allowing the malignant cells to revert to a state with more normal characteristics. The use of epigenetics is emerging as an effective and promising approach to treat cancer. Epigenetic drugs, which target two well- known epigenetic pathways, namely, DNA methyltransferases and histone deacetylases, are already being applied for the cancer treatment. In the current study, an overview regarding the under-standing of epigenetic alterations in the development of cancer and the current state of epigenetic drug discovery is provided. 展开更多
关键词 cancer epigenetics DNA methylation histonemodifications epigenetic drugs.
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Facile Conversion of Alcohols to Olefins by Tosylation and Subsequent SiO_2-promoted β-elimination
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作者 RUAN Xiaohong SONG Gaopeng ZHANG Yichun LI Yingxia 《Journal of Ocean University of China》 SCIE CAS 2007年第2期196-198,共3页
A convenient and effective procedure was developed for the conversion of alcohol to olefin by tosylation and subsequent β-elimination promoted by silica gel in this study. Treatment of the alcohols with p-toluenesulf... A convenient and effective procedure was developed for the conversion of alcohol to olefin by tosylation and subsequent β-elimination promoted by silica gel in this study. Treatment of the alcohols with p-toluenesulfonyl chloride in pyridine at 0℃ af- fords tosylates which undergo β-elimination with silica gel in dichloromethane or chloroform at room temperature, yielding olefins with high productivity. 展开更多
关键词 alcohol TOSYLATION silica gel OLEFIN β-elimination
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The proliferation inhibition of Hela cells by histone deacetylases- 1 siRNA
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作者 Na Li Shiying Yu 《The Chinese-German Journal of Clinical Oncology》 CAS 2008年第6期365-367,共3页
Objective: To investigate the anti-proliferative effect of histone deacetylases-1 (HDAC-1) knockdown in Hela cells. Methods: The HDAC-1 protein was knockdowned using siRNA. The expression of HDAC-1 was detected by... Objective: To investigate the anti-proliferative effect of histone deacetylases-1 (HDAC-1) knockdown in Hela cells. Methods: The HDAC-1 protein was knockdowned using siRNA. The expression of HDAC-1 was detected by Western blotting. Apoptosis was assessed by flow cytometry. The inhibition of cell growth was assesses by MTT assay. Results: HDAC-1 siRNA knockdowned the expression of HDAC-1 protein. HDAC siRNA inhibited the proliferation of Hela cells. HDAC- 1 siRNA induced apoptosis. Conclusion: HDAC-1 siRNA may inhibit the growth of Hela cells by inducing apoptosis. 展开更多
关键词 histone deacetylases-1 siRNA cervical cancer APOPTOSIS
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Histone Deacetylase Inhibition:An Important Mechanism in the Treatment of Lymphoma 被引量:1
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作者 Shan-qi Guo Yi-zhuo Zhang 《Clinical oncology and cancer researeh》 CAS CSCD 2012年第2期85-89,共5页
Lymphomas enconlpass a group of malignancies that originate in the lymph nodes or other lymphoid tissues. Epigenetic modification, especially by histone deacetylase (HDACs), plays a key role during the occurrence an... Lymphomas enconlpass a group of malignancies that originate in the lymph nodes or other lymphoid tissues. Epigenetic modification, especially by histone deacetylase (HDACs), plays a key role during the occurrence and development of lymphomas. Consequently, HDAC inhibitors (HDACIs), a class of gene expression-modulating drugs, have emerged as promising mechanism-based agents for the treatment of lymphomas. This review presents the rationale of HDAC inhibition, describes the epigenetic-based mechanisms of action of HDACIs, discusses their clinical efficiency, and summarizes the current and future developments in this field. 展开更多
关键词 LYMPHOMA histone deacetylases THERAPEUTICS EPIGENOMICS
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Transcriptional changes in epigenetic modifiers associated with gene silencing in the intestine of the sea cucumber,Apostichopus japonicus(Selenka),during aestivation 被引量:5
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作者 王天明 杨红生 +2 位作者 赵欢 陈慕雁 王兵 《Chinese Journal of Oceanology and Limnology》 SCIE CAS CSCD 2011年第6期1267-1274,共8页
The sea cucumber, Apostichopusjaponicus, undergoes aestivation to improve survival during periods of high-temperature. During aestivation, the metabolic rate is depressed to reduce the consumption of reserved energy. ... The sea cucumber, Apostichopusjaponicus, undergoes aestivation to improve survival during periods of high-temperature. During aestivation, the metabolic rate is depressed to reduce the consumption of reserved energy. We evaluated the role of epigenetic modification on global gene silencing during metabolic rate depression in the sea cucumber. We compared the expression of epigenetic modifiers in active and aestivating sea cucumbers. The expression of three genes involved in DNA methylation and chromatin remodeling (DNA (cytosine-5)-methyltransferase l, Methyl-CpG-binding domain protein 2), and Chromodomain-helicase-DNA-binding protein 5) was significantly higher during aestivation (Days 20 and 40). Similarly, we observed an increase in the expression of genes involved in histone acetylation (Histone deacetylase 3) and Histone-binding protein RBBP4) during the early (Days 5 and 10) and late phases (Days 20 and 40) of aestivation. There was no change in the expression of KAT2B, a histone acetyltransferase. However, the expression of histone methylation associated modifiers (Histone-arginine methyltransferase CARMER and Histone-lysine N-methyltransferase MLL5) was significantly higher after 5 d in the aestivating group. The results suggest that the expression of epigenetic modifiers involved in DNA methylation, chromatin remodeling, histone acetylation, and histone methylation is upregulated during aestivation. We hypothesize that these changes regulate global gene silencing during aestivation in A. japonicus. 展开更多
关键词 Apostichopus japonicus AESTIVATION epigenetic modification gene silencing mRNAexpression
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七味白术散对糖尿病KKAy小鼠糖脂代谢、胰岛素抵抗及胃饥饿素的影响 被引量:4
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作者 刘雪辉 周琳悦 +3 位作者 刘燕 刘柔 马旭红 王振宇 《时珍国医国药》 CAS CSCD 北大核心 2022年第11期2630-2632,共3页
目的 探讨七味白术散对糖尿病KKAy小鼠糖脂代谢、胰岛素抵抗及胃饥饿素的影响。方法 正常对照组选用SPF级C57BL/6J小鼠,使用KK饲料喂养KKAy小鼠制作2型糖尿病模型,随机将成模KKAy小鼠分为模型组、七味白术散组、二甲双胍组,每组12只。... 目的 探讨七味白术散对糖尿病KKAy小鼠糖脂代谢、胰岛素抵抗及胃饥饿素的影响。方法 正常对照组选用SPF级C57BL/6J小鼠,使用KK饲料喂养KKAy小鼠制作2型糖尿病模型,随机将成模KKAy小鼠分为模型组、七味白术散组、二甲双胍组,每组12只。连续灌胃8周后,检测小鼠血清中血脂(TG、TC)、胰岛素、炎症指标(TNF-α、IFN-γ、IL-6)、UAG、AG,计算胰岛素抵抗指数(HOMA-IR)。结果 七味白术散、二甲双胍能显著减轻KKAy小鼠体重,使血糖、血清TC、TG、HOMA-IR、TNF-α、IL-6、IFN-γ及UAG水平显著下降。结论 七味白术散及二甲双胍能有效改善KKAy小鼠糖脂代谢、胰岛素抵抗,其治疗机制可能与调节免疫炎症及UAG的血浆水平有关。 展开更多
关键词 七味白术散 胃饥饿素 2型糖尿病 酰基胃饥饿素 去酰基化胃饥饿素 胰岛素抵抗
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胃饥饿素与2型糖尿病 被引量:1
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作者 顾丹阳 臧璞 邵加庆 《中国临床研究》 CAS 2019年第11期1577-1579,1582,共4页
胃饥饿素(ghrelin)是一种主要由胃底部细胞分泌的脑肠肽,依据其N端丝氨酸残基是否酰基化分为酰基化ghrelin(AG)和去酰基化ghrelin(DAG)两种形式,在体内具有广泛生理作用,如促进生长激素(GH)释放、增加摄食、增强胃肠运动及抗炎等。近年... 胃饥饿素(ghrelin)是一种主要由胃底部细胞分泌的脑肠肽,依据其N端丝氨酸残基是否酰基化分为酰基化ghrelin(AG)和去酰基化ghrelin(DAG)两种形式,在体内具有广泛生理作用,如促进生长激素(GH)释放、增加摄食、增强胃肠运动及抗炎等。近年来诸多研究发现ghrelin在调控糖代谢方面具有重要作用,但其在体内的不同存在形式与2型糖尿病的关系仍存在一定争议,参与糖代谢调控的机制尚未完全阐明。明确ghrelin在糖代谢中的作用及机制有助于为糖尿病治疗提供的新的思路和治疗靶点。 展开更多
关键词 胃饥饿素 2型糖尿病 酰基胃饥饿素 去酰基化胃饥饿素 糖代谢 促进生长激素
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