Diglycerides

甘油二酯
  • 文章类型: Journal Article
    膜蛋白整合的调节涉及分子装置,例如Sec-tranlocons或插入酶YidC。我们已经确定了大肠杆菌内膜中的整合促进因子,称为膜蛋白整合酶(MPIase)。结构分析表明,尽管它的名字像酶一样,MPIase是一种糖脂,具有包含N-乙酰氨基糖的长聚糖,焦磷酸盐接头,和二酰基甘油(DAG)锚。此外,我们发现DAG,一个次要的膜组件,阻断自发整合。在这次审查中,我们使用包括合成化学和生物物理分析在内的综合方法证明了它们如何有助于细菌中不依赖Sec的膜蛋白整合。DAG通过抑制膜核心的移动性来阻止不利的自发整合,而MPIase弥补了这一点。此外,MPIase在捕获底物蛋白以防止其聚集中起关键作用,将其吸引到膜表面,促进其插入膜中,并将其传递给其他因素。DAG和MPIase的组合有效地调节膜蛋白的整合。
    Regulation of membrane protein integration involves molecular devices such as Sec-translocons or the insertase YidC. We have identified an integration-promoting factor in the inner membrane of Escherichia coli called membrane protein integrase (MPIase). Structural analysis revealed that, despite its enzyme-like name, MPIase is a glycolipid with a long glycan comprising N-acetyl amino sugars, a pyrophosphate linker, and a diacylglycerol (DAG) anchor. Additionally, we found that DAG, a minor membrane component, blocks spontaneous integration. In this review, we demonstrate how they contribute to Sec-independent membrane protein integration in bacteria using a comprehensive approach including synthetic chemistry and biophysical analyses. DAG blocks unfavorable spontaneous integrations by suppressing mobility in the membrane core, whereas MPIase compensates for this. Moreover, MPIase plays critical roles in capturing a substrate protein to prevent its aggregation, attracting it to the membrane surface, facilitating its insertion into the membrane, and delivering it to other factors. The combination of DAG and MPIase efficiently regulates the integration of membrane proteins.
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  • 文章类型: Journal Article
    鱼类对渔业和基本营养供应至关重要,包括脂质。这项研究采用了高通量脂质组学方法来评估和对比三种海洋鱼类的脂质谱(P。大黄鱼,S.Fuscens,和C.saira)和一种淡水物种(H.molitrix)横跨头部,肌肉,还有内脏.在17个亚类中鉴定了超过1000种分子脂质。值得注意的是,在这些物种中首次检测到酰化的单半乳糖二酰甘油(acMGDG),饱和脂肪酸的患病率较高(44.7%-87.7%)。甘油酯(67.7-86.3%)和PL(10.7-31.8%)被确定为主要的脂质类别。海洋鱼类肌肉显示出比淡水物种更高的PL含量,大黄杆菌的内脏含有超过30%的PLs的总脂质。特别是,醚磷脂酰乙醇胺比醚磷脂酰胆碱掺入更多的DHA。四种鱼类的内脏也表现出大量的二酰甘油(DG),表明它们作为功能性脂质来源的潜力。多变量分析确定了甘油三酯(TG)(59:13),DG(16:1/22:5),和MGDG(16:0/18:2)作为区分鱼类解剖部位的潜在生物标志物。这项研究加深了对这些鱼的营养价值的理解,为消费者的饮食选择提供指导,并为将以前未充分利用的副产品转化为具有高价值潜力的资源铺平道路。
    Fish are crucial for the fishing industry and essential nutrient provision, including lipids. This study employed a high-throughput lipidomic approach to evaluate and contrast the lipid profiles of three marine fish species (P. crocea, S. fuscens, and C. saira) and one freshwater species (H. molitrix) across head, muscle, and viscera. Over 1000 molecular lipid species across 17 subclasses were identified. Notably, acylated monogalactosyldiacylglycerol (acMGDG) was detected for the first time in these species, with a high prevalence of saturated fatty acids (44.7 %-87.7 %). Glycerolipids (67.7 - 86.3 %) and PLs (10.7 - 31.8 %) were identified as the dominant lipid classes. Marine fish muscles displayed higher PL content than freshwater species, and P. crocea viscera contained over 30 % PLs of total lipids. In particular, ether phosphatidyl ethanolamine incorporated more DHA than ether phosphatidylcholine. The viscera of four fish species also exhibited a significant abundance of diacylglycerol (DG), indicating their potential as functional lipid sources. Multivariate analysis identified triglyceride (TG) (59:13), DG (16:1/22:5), and MGDG (16:0/18:2) as potential biomarkers for differentiating among fish anatomical parts. This study deepens the understanding of the nutritional values of these fish, providing guidance for consumer dietary choices and paving the way for transforming previously underutilized by-products into resources with high-value potential.
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  • 文章类型: Journal Article
    研究油菜籽二酰基甘油(RDG)对C57BL/6J小鼠脂质积累和代谢的影响。肥胖小鼠接受高脂肪饮食,其中45%的总能量来自RDG(RDGM组)或菜籽三酰甘油油(RTGM组).该饮食干预在肥胖小鼠模型建立后进行12周。实验结束时,RTGM和RDGM组小鼠的血清葡萄糖水平分别为13.0±1.3mmol/L和9.7±1.5mmol/L,分别。同时,RDGM组的血清甘油三酯水平比RTGM组低26.3%。RDGM组的减肥效果伴随着白色脂肪组织(WAT)指数的显着降低。RDG干预在体内没有显著改变菜籽油的抗氧化和抗炎特性。RDG饮食改善了高脂饮食引起的肝脏脂质代谢异常,导致降低肝损伤指数值(AST和ALT)。此外,与RTGM组相比,成脂基因PPAR-γ和DGAT在肝脏和肠道中的表达分别下降了21.7%和16.7%和38.7%和47.2%,分别,在RDGM组。Further,RDG干预后,BAT中大多数脂解基因均无明显变化。这意味着RDG通过改变肝脏中脂肪生成基因的表达来调节脂质代谢,肠,和脂肪组织,从而减少WAT的积累。此外,RDG饮食增强肠道菌群多样性,增加小鼠肠道中未分类的Muribaculaceae的相对水平,并降低Dubosiella和Faecalibaculum的水平,可能加速脂质代谢。因此,对肥胖小鼠进行为期三个月的RDG饮食干预在调节体型方面表现出益处,血清肥胖相关指标,肠道菌群结构,脂肪组织中的脂质代谢,肝脏,和肠。
    To investigate the effects of rapeseed diacylglycerol oil (RDG) intake on lipid accumulation and metabolism in C57BL/6J mice, obese mice were fed a high-fat diet in which 45% of the total energy content came from RDG (RDGM group) or rapeseed triacylglycerol oil (RTGM group). This diet intervention was conducted for 12 weeks following the establishment of the obese mouse model. By the end of the experiment, the serum glucose levels of the mice in the RTGM and RDGM groups were 13.0 ± 1.3 mmol/L and 9.7 ± 1.5 mmol/L, respectively. Meanwhile, the serum triglyceride level in the RDGM group was 26.3% lower than that in the RTGM group. The weight-loss effect in the RDGM group was accompanied by a significant decrease in the white adipose tissue (WAT) index. The RDG intervention did not significantly change the antioxidant and anti-inflammatory properties of the rapeseed oil in vivo. The RDG diet improved the liver lipid metabolism abnormalities induced by a high-fat diet, leading to decreased liver damage index values (AST and ALT). Additionally, compared to that in the RTGM group, the expression of the adipogenic genes PPAR-γ and DGAT decreased in both the liver and intestine by 21.7% and 16.7% and by 38.7% and 47.2%, respectively, in the RDGM group. Further, most lipolytic genes in BAT showed no significant change after the RDG intervention. This implies that RDG regulates lipid metabolism by altering the expression of adipogenic genes in the liver, intestine, and adipose tissue, thereby reducing the accumulation of WAT. Furthermore, the RDG diet enhanced gut flora diversity, increasing the relative levels of unclassified Muribaculaceae and decreasing the levels of Dubosiella and Faecalibaculum in the mouse gut, potentially accelerating lipid metabolism. Thus, a three-month RDG diet intervention in obese mice exhibited benefits in regulating the somatotype, serum obesity-related indices, gut flora structure, and lipid metabolism in the adipose tissue, liver, and intestine.
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  • 文章类型: Journal Article
    这项研究检查了超声功率(0,150,300,450,600和750W)和超声持续时间(3,6,9,12和15分钟)对二酰甘油的物理化学性质和微观结构的影响(DAG)负载的乳液用大豆分离蛋白(SPI)和海藻酸钠(SA)稳定。研究结果表明,最小的颗粒尺寸,zeta电位,SPI-SA-DAG乳液的接触角分别为5.58μm,-49.85mV,和48.65°,在450W的超声功率下实现乳化性能,损耗模量,储能模量,乳液的表观粘度在该功率设定和9分钟的持续时间下是最佳的。分析技术,包括共聚焦激光扫描-,扫描电子-,和原子力显微镜,显示超声处理显着改变了乳液聚集状态,表面粗糙度(Rq)在450W时最小。这些结果表明,通过在450W下进行适当的超声处理9分钟,可以有效地增强SPI-SA-DAG乳液的稳定性。本研究为超声处理技术在食品工业中的广泛应用提供了理论支持。
    This study examined the impacts of ultrasonic power (0, 150, 300, 450, 600, and 750 W) and ultrasonic durations (3, 6, 9, 12, and 15 min) on the physicochemical properties and microstructure of diacylglycerol (DAG)-loaded emulsions stabilized with soybean protein isolate (SPI) and sodium alginate (SA). The findings indicated that the smallest particle size, zeta potential, and contact angle for SPI-SA-DAG emulsions were respectively 5.58 μm, -49.85 mV, and 48.65°, achieved at an ultrasonic power of 450 W. The emulsification properties, loss modulus, storage modulus, and apparent viscosity of the emulsions were optimal at this power setting and at a duration of 9 min. Analytical techniques, including confocal laser scanning-, scanning electron-, and atomic force microscopy, revealed that ultrasonication significantly altered emulsion aggregation state, with the surface roughness (Rq) being minimized at 450 W. These results demonstrated that the stability of SPI-SA-DAG emulsions can be effectively enhanced by an appropriate ultrasonic treatment at 450 W for 9 min. This research provides theoretical support for the broad application of sonication techniques in the food industry.
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  • 文章类型: Journal Article
    视网膜神经节细胞(RGC)功能受损并最终导致RGC死亡,患青光眼致盲或其他视神经病变的风险增加.差的RGC效率导致视网膜和大脑之间通过RGC轴突的视觉信号的有限传输。由于其潜在的轴突途径再生特性,因此越来越关注研究在神经元中发现的脂质信使,例如内源性大麻素(eCB)具有重要意义。2-花生四酰基甘油(2-AG),常见的eCB,由二酰甘油(DAG)和二酰甘油脂肪酶(DAGL)之间的sn-1水解反应合成。对DAG生产的检查允许未来与DAGL功能相关的下游分析。这里,我们描述了从小鼠视网膜中提取RGCs以及随后对RGCs中存在的DAG含量进行质谱分析的方案指南.
    With impaired retinal ganglion cell (RGC) function and eventual RGC death, there is a heightened risk of experiencing glaucoma-induced blindness or other optic neuropathies. Poor RGC efficiency leads to limited transmission of visual signals between the retina and the brain by RGC axons. Increased focus on studying lipid messengers found in neurons such as endocannabinoids (eCBs) has importance due to their potential axonal pathway regenerative properties. 2-Arachidonoylglycerol (2-AG), a common eCB, is synthesized from an sn-1 hydrolysis reaction between diacylglycerol (DAG) and diacylglycerol lipase (DAGL). Examination of DAG production allows for future downstream analysis in relation to DAGL functionality. Here, we describe protocol guidelines for extracting RGCs from mouse retinas and subsequent mass spectrometry analysis of the DAG content present within the RGCs.
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  • 文章类型: Journal Article
    背景:已经表明,酪油的酯交换改变其脂质化学,从而改变脂肪的结晶。取决于所使用的催化剂的性质,反应动力学和所得的油的结晶不同。对与植物油的反应进行建模是一种更简单的方法,用于分析所得产物,以了解基于催化剂选择而发生的化学和生理化学变化。这项工作的目的是使用单价和二价催化剂进行椰子油和玉米油的化学酯交换反应,以研究发生的化学和结晶变化。
    结果:使用Ca(OH)2和KOH作为催化剂对椰子油和玉米油进行化学酯交换。在椰子油和玉米油样本中,酯交换导致甘油单酯(MAG)和甘油二酯(DAG)由每个样品中发现的最丰富的脂肪酸形成。椰子油的熔化温度,固体脂肪含量(SFC),和储能模量由于酯交换反应而降低,玉米油中开始形成晶体,导致融化热谱图明显,更高的SFC,结果是更粘稠的油。使用Ca(OH)2作为催化剂导致更多的MAG形成,和比KOH用作催化剂时更高的SFC和熔融温度。
    结论:结果表明,植物性油的酯交换导致的化学变化改变了油的结晶行为,因此可用于食品工业中的不同应用。©2024作者(S)。约翰·威利父子有限公司代表化学工业学会出版的《食品和农业科学杂志》。
    BACKGROUND: The transesterification of butteroil has been shown to alter its lipid chemistry and thus alter the crystallization of the fat. The reaction kinetics and resulting crystallization of the butteroil differ depending on the nature of the catalyst used. Modeling the reaction with vegetable oils is a simpler method for the analysis of resulting products to understand the chemical and physiochemical changes that occur based on catalyst selection. The objective of this work is to perform a chemical transesterification of coconut and corn oil using monovalent and divalent catalysts to investigate the chemical and crystal changes that occur.
    RESULTS: Coconut and corn oil were subjected to chemical transesterification using both Ca(OH)2 and KOH as catalysts. In both the coconut and corn oil samples, transesterification caused monoglycerides (MAGs) and diacylglycerides (DAGs) to form from the most abundant fatty acid found in each sample. Coconut oil\'s melting temperature, solid fat content (SFC), and storage modulus decreased as a result of the transesterification, and crystals began to form in the corn oil causing melting thermograms to be evident, higher SFC, and a more viscous oil as a result. Using Ca(OH)2 as a catalyst resulted in more MAG formation, and a higher SFC and melting temperature than when KOH was used as a catalyst.
    CONCLUSIONS: The results demonstrate that the chemical changes that result from transesterification of plant-based oils change the crystallization behavior of the oils and can therefore be used for different applications in the food industry. © 2024 The Author(s). Journal of The Science of Food and Agriculture published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
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  • 文章类型: Journal Article
    骨骼肌二酰甘油(DAG)和神经酰胺升高会损害胰岛素信号,和酰基肉碱(酰基CN)反映脂肪酸氧化受损,因此,肌内血脂谱表明胰岛素抵抗。急性(即,餐后)高胰岛素血症已被证明会升高健康肌肉中的脂质,并且是2型糖尿病(T2D)的独立危险因素。目前尚不清楚急性高胰岛素血症与肌肉脂质组之间的关系如何相互作用,从而导致或加剧胰岛素抵抗。我们调查了急性高胰岛素血症对肌肉脂质组的影响,以帮助表征高胰岛素血症升高T2D风险的生理基础。耐力运动员(n=12),久坐的瘦成年人(n=12),肥胖患者(n=13)和T2D患者(n=7)接受了高胰岛素-正常血糖钳夹术和肌肉活检。虽然总的1,2-DAG波动没有显著差异,运动员减少了2%,而T2D增加了53%.C181,2-DAG在仅使用T2D的夹具期间增加,与胰岛素敏感性呈负相关。基底肌肉C18:0神经酰胺随T2D升高,但不会被钳子改变。在高胰岛素血症期间,酰基肉碱普遍降低,与T2D的仅46%相比,运动员减少了80%。在雄性小鼠中观察到类似的波动,急性高胰岛素血症增加了胰岛素抵抗表型中的1,2DAG,并普遍降低了酰基肉碱。总之,急性高胰岛素血症会升高胰岛素抵抗表型的肌肉1,2-DAG水平。这表明胰岛素敏感性低的个体在进食状态下肌内脂质代谢可能失调。这可能会加剧胰岛素抵抗。
    Elevated skeletal muscle diacylglycerols (DAGs) and ceramides can impair insulin signaling, and acylcarnitines (acylCNs) reflect impaired mitochondrial fatty acid oxidation, thus, the intramuscular lipid profile is indicative of insulin resistance. Acute (i.e., postprandial) hyperinsulinemia has been shown to elevate lipid concentrations in healthy muscle and is an independent risk factor for type 2 diabetes (T2D). However, it is unclear how the relationship between acute hyperinsulinemia and the muscle lipidome interacts across metabolic phenotypes, thus contributing to or exacerbating insulin resistance. We therefore investigated the impact of acute hyperinsulinemia on the skeletal muscle lipid profile to help characterize the physiological basis in which hyperinsulinemia elevates T2D risk. In a cross-sectional comparison, endurance athletes (n = 12), sedentary lean adults (n = 12), and individuals with obesity (n = 13) and T2D (n = 7) underwent a hyperinsulinemic-euglycemic clamp with muscle biopsies. Although there were no significant differences in total 1,2-DAG fluctuations, there was a 2% decrease in athletes versus a 53% increase in T2D during acute hyperinsulinemia (P = 0.087). Moreover, C18 1,2-DAG species increased during the clamp with T2D only, which negatively correlated with insulin sensitivity (P < 0.050). Basal muscle C18:0 total ceramides were elevated with T2D (P = 0.029), but not altered by clamp. Acylcarnitines were universally lowered during hyperinsulinemia, with more robust reductions of 80% in athletes compared with only 46% with T2D (albeit not statistically significant, main effect of group, P = 0.624). Similar fluctuations with acute hyperinsulinemia increasing 1,2 DAGs in insulin-resistant phenotypes and universally lowering acylcarnitines were observed in male mice. In conclusion, acute hyperinsulinemia elevates muscle 1,2-DAG levels with insulin-resistant phenotypes. This suggests a possible dysregulation of intramuscular lipid metabolism in the fed state in individuals with low insulin sensitivity, which may exacerbate insulin resistance.NEW & NOTEWORTHY Postprandial hyperinsulinemia is a risk factor for type 2 diabetes and may increase muscle lipids. However, it is unclear how the relationship between acute hyperinsulinemia and the muscle lipidome interacts across metabolic phenotypes, thus contributing to insulin resistance. We observed that acute hyperinsulinemia elevates muscle 1,2-DAGs in insulin-resistant phenotypes, whereas ceramides were unaltered. Insulin-mediated acylcarnitine reductions are also hindered with high-fat feeding. The postprandial period may exacerbate insulin resistance in metabolically unhealthy phenotypes.
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  • 文章类型: Journal Article
    这项研究开发了基于二酰甘油(DAG)的Pickering乳液,该乳液具有通过自组装槲皮素/DAG/β-环糊精(β-CD)复合物(QDCC)使用一步搅拌法稳定的氧化稳定性。DAG含量的影响(5%,15%,40%,80%,w/w)关于自组装行为,界面性质,并研究了复杂颗粒的乳化能力。SEM,XRD和ATR-FTIR研究证实了三元复合颗粒的形成。80%DAG油中QDCC的槲皮素包封率最高(6.09±0.01%),最高的DPPH自由基清除率和铁还原抗氧化性能(FRAP)。80%DAG油乳剂中β-CD和槲皮素的吸附率分别为88.4±2.53%和98.34±0.15%,分别。具有80%DAG的Pickering乳液具有最小的液滴尺寸(8.90±1.87μm)和优异的氧化稳定性。这项研究开发了一种新的方法来调节DAG基乳液的物理化学稳定性,方法是通过一锅式自组装方法将天然抗氧化剂锚定在油-水界面。
    This research develops diacylglycerol (DAG) based Pickering emulsions with enhanced oxidative stability stabilized by self-assembled quercetin/DAG/β-cyclodextrin (β-CD) complexes (QDCCs) using a one-step agitation method. Influence of DAG content (5%, 15%, 40%, and 80%, w/w) on the self-assembly behavior, interfacial properties, and emulsifying ability of complex particles was investigated. SEM, XRD and ATR-FTIR studies confirmed the formation of ternary composite particles. QDCCs in 80% DAG oil had the highest quercetin encapsulation efficiency (6.09 ± 0.01%), highest DPPH radical scavenging rate and ferric reducing antioxidant property (FRAP). β-CD and quercetin adsorption rates in emulsion with 80% DAG oil were 88.4 ± 2.53% and 98.34 ± 0.15%, respectively. Pickering emulsions with 80% DAG had the smallest droplet size (8.90 ± 1.87 μm) and excellent oxidation stability. This research develops a novel approach to regulate the physicochemical stability of DAG-based emulsions by anchoring natural antioxidants at the oil-water interface through a one-pot self-assembly method.
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  • 文章类型: Journal Article
    香菇蜡(TGW),一种新的坚果蜡和精制香菇油的副产品,缺乏足够的研究和应用。在这项研究中,研究了二酰基甘油(DAG)的胶凝行为和TGW的化学成分。与四种典型的天然蜡相比,TGW表现出最低的临界胶凝浓度(Cg,1%wt)在DAG。结果表明,Cg时的TGW-DAG油凝胶具有最高的G\'LVR和G”,最高临界应力,良好的热稳定性,中等粘度恢复,OSC。产生应力,表明强烈的凝胶。微观结构和相关性分析表明,TGW-DAG油凝胶的优良胶凝行为是由于棒状TGW晶体形成的固体三维网络,和TGW中的高级烃化合物(HC)含量和HC/蜡酯。配方优化表明,含有3.2%TGW和1.0%皂苷元(DSG)的油凝胶在硬度方面更好地模拟了缩短的特征,粘附性,可传播性。用TGW/DSG-DAG油凝胶制备的面包具有均匀致密的毛孔,最佳的保湿能力,和柔软和坚定的味道,证明TGW/DSG-DAG油凝胶是一种很好的起酥油替代品。因此,这项研究提供了TGW的系统基础知识,并开发了DSG-TGW-DAG油凝胶作为有希望的缩短剂替代品。
    Torreya grandis wax (TGW), a new nut wax and by-product of refined Torreya grandis oil, lacks sufficient research and application. In this study, the gelling behavior in diacylglycerol (DAG) and chemical compositions of TGW were investigated. Compared with four typical natural waxes, TGW exhibited the lowest critical gelling concentration (Cg, 1 %wt) in DAG. The results performed that TGW-DAG oleogels at Cg possessed the highest G\'LVR and G″, highest critical stress, good thermal stability, moderate viscosity recovery, and osc. yields stress, indicating strong gel. The microstructure and correlation analysis revealed that excellent gelling behaviors of TGW-DAG oleogels were due to the solid three-dimensional network formed by rod-like TGW crystal, and the higher hydrocarbon compound (HC) content and HC/wax ester in TGW. Formulation optimization suggested that oleogel containing 3.2 % TGW and 1.0 % diosgenin (DSG) better mimicked the characteristics of shortening in terms of hardness, adhesiveness, spreadability. The bread prepared with TGW/DSG-DAG oleogel owned uniform and dense pores, the best moisture retention capability, and soft and firm taste, demonstrating that TGW/DSG-DAG oleogel was a good shortening substitute. Therefore, this study provides the systematically fundamental knowledge of TGW and develops DSG-TGW-DAG oleogels as promising shortening substitutions.
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  • 文章类型: Journal Article
    人类免疫缺陷病毒1型(HIV-1)治愈,潜伏感染HIV-1的细胞必须从HIV-1感染者中清除。我们以前开发了蛋白激酶C(PKC)激活剂,二酰基甘油(DAG)-内酯衍生物3,具有高HIV-1潜伏期逆转活性,基于YSE028(2)作为先导化合物,发现该活性与对PKC的结合亲和力和对酯酶介导的水解的稳定性相关。这里,我们合成了新的DAG-内酯衍生物,不仅含有叔酯基或异恶唑替代物,而且还含有几个对称的亚烷基部分,以改善HIV-1潜伏期逆转活性。化合物9a,在酯基的α位具有二甲基基团,具有异恶唑部分的化合物3和化合物26具有两倍高的HIV-1潜伏期逆转活性,非常活跃。此外,具有中等疏水性和强生物稳定性的DAG-内酯衍生物显示出较高的生物活性。
    Toward human immunodeficiency virus type-1 (HIV-1) cure, cells latently infected with HIV-1 must be eliminated from people living with HIV-1. We previously developed a protein kinase C (PKC) activator, diacylglycerol (DAG)-lactone derivative 3, with high HIV-1 latency-reversing activity, based on YSE028 (2) as a lead compound and found that the activity was correlated with binding affinity for PKC and stability against esterase-mediated hydrolysis. Here, we synthesized new DAG-lactone derivatives not only containing a tertiary ester group or an isoxazole surrogate but also several symmetric alkylidene moieties to improve HIV-1 latency reversing activity. Compound 9a, with a dimethyl group at the α-position of the ester group, exerted twice higher HIV-1 latency reversing activity than compound 3, and compound 26, with the isoxazole moiety, was significantly active. In addition, DAG-lactone derivatives with moderate hydrophobicity and potent biostability showed high biological activity.
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