Antiglycation

抗糖基化
  • 文章类型: Journal Article
    研究了金银花果汁基质改性和干燥技术对粉末特性的影响。评估包括酚类物质(514.7-4388.7mg/100g干物质),环烯醚萜类(高达337.5毫克/100克干物质),抗氧化和抗糖基化能力,以及使用麦芽糖糊精生产的粉末的抗老化性能,菊粉,海藻糖,以及作为载体的先锋角色的帕拉金糖。在粉末质量方面,喷雾干燥与冷冻干燥相比具有竞争力。载体的应用影响了果粉的性质。海藻糖保护果汁提取物产品中的酚类物质,而麦芽糊精在果汁粉末中显示出保护作用。环烯醚萜类化合物的浓度受基质类型和干燥技术的影响。与提取物产品相比,果汁粉末中抗糖基化能力受载体类型的影响更大。然而,随着载波的增加,后者对乙酰胆碱酯酶的选择性比其他样品高约12倍.了解矩阵组成之间的相互作用,干燥技术,和粉末特性为开发具有定制属性的植物基产品提供了见解,包括潜在的健康相关属性。
    The study investigated the impact of Lonicera caerulea L. juice matrix modification and drying techniques on powder characteristics. The evaluation encompassed phenolics (514.7-4388.7 mg/100 g dry matter), iridoids (up to 337.5 mg/100 g dry matter), antioxidant and antiglycation capacity, as well as anti-ageing properties of powders produced using maltodextrin, inulin, trehalose, and palatinose with a pioneering role as a carrier. Spray drying proved to be competitive with freeze drying for powder quality. Carrier application influenced the fruit powder properties. Trehalose protected the phenolics in the juice extract products, whereas maltodextrin showed protective effect in the juice powders. The concentrations of iridoids were influenced by the matrix type and drying technique. Antiglycation capacity was more affected by the carrier type in juice powders than in extract products. However, with carrier addition, the latter showed approximately 12-fold higher selectivity for acetylcholinesterase than other samples. Understanding the interplay between matrix composition, drying techniques, and powder properties provides insights for the development of plant-based products with tailored attributes, including potential health-linked properties.
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  • 文章类型: Journal Article
    包括糖尿病视网膜病变在内的糖尿病血管并发症是沙特阿拉伯的主要发病率。多元醇途径(又称醛糖还原酶(AR)途径)与糖尿病性视网膜病变有关,涉及长期增强的葡萄糖代谢。已经提出了相当多的研究来开发更有效的治疗策略以克服与糖尿病相关的血管并发症的压倒性挑战。在这方面,Cichoriumintybus的成分由于其强大的抗糖尿病特性,可以提供强大的AR抑制潜力。因此,本研究的目的是研究C.intybus提取物/化合物的AR抑制和抗糖基化潜力。初步的体外实验结果表明,英替巴氏杆菌甲醇提取物能显著抑制AR酶和糖基化终产物的形成。最终,根据以前的研究和评论,我们选择了115个C.intybus根成分,并通过Lipinski的5法则和ADMET分析对其进行了筛选。稍后,对8个化合物进行分子对接分析后,选择五个最佳的分子动力学模拟来推断它们与AR酶的结合亲和力。最后,在体外进一步测试了5个化合物中的3个的AR抑制潜力和抗糖基化特性。酶分析和动力学研究表明,所有三个测试化合物都具有有效的AR抑制特性,尽管程度低于鞣花酸和tolrestat。同样,山奈酚表现出与鞣花酸相当的强的抗糖基化特性,但大于氨基胍.有趣的是,测试化合物显著降低RBC中的山梨糖醇积累证实了这些化合物对AR的强烈抑制。此外,在高葡萄糖环境下山梨糖醇积累的减少也表明这些化合物在糖尿病性视网膜病变和其他血管并发症中的潜在应用。因此,总之,计算机模拟和体外研究相结合表明,C.intybus根是治疗化合物的宝库,可以进一步探索抗糖尿病视网膜病变的药物开发。
    Diabetic vascular complication including diabetic retinopathy is a major morbidity in Saudia Arabia. The polyol pathway aka aldose reductase (AR) pathway has gained significant association with diabetic retinopathy with regard to chronically enhanced glucose metabolism. Considerable research has been put forth to develop more effective therapeutic strategies to overcome the overwhelming challenges of vascular complications associated with diabetes. In this regard, constituents of Cichorium intybus can offer strong AR inhibitory potential because of their strong antidiabetic properties. Therefore, aim of this study was to investigate the AR inhibitory as well as antiglycation potential of C. intybus extract/compounds. The preliminary in vitro results showed that methanolic extract of C. intybus could significantly inhibit AR enzyme and advanced glycation end product formation. Eventually, based on previous studies and reviews, we selected one hundred fifteen C. intybus root constituents and screened them through Lipinski\'s rule of five and ADMET analysis. Later, after molecular docking analysis of eight compounds, five best were selected for molecular dynamics simulation to deduce their binding affinity with the AR enzyme. Finally, three out of five compounds were further tested in vitro for their AR inhibitory potential and antiglycation properties. Enzyme assay and kinetic studies showed that all the three tested compounds were having potent AR inhibitory properties, although to a lesser extent than ellagic acid and tolrestat. Similarly, kaempferol showed strong antiglycation property equivalent to ellagic acid, but greater than aminoguanidine. Intriguingly, significant reduction in sorbitol accumulation in RBCs by the tested compounds substantiated strong AR inhibition by these compounds. Moreover, decrease in sorbitol accumulation under high glucose environment also signifies the potential application of these compounds in diabetic retinopathy and other vascular complications. Thus, in sum, the in silico and in vitro studies combinedly showed that C. intybus root is a treasure for therapeutic compounds and can be explored further for drug development against diabetic retinopathy.
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  • 文章类型: Journal Article
    晚期糖基化终产物(AGEs)通过碳水化合物与生物大分子的非酶促连接形成。这些AGEs与它们的同源受体结合,称为AGEs受体(RAGEs),成为几种疾病发生和发展的重要原因之一。深入了解RAGE的途径将有助于确定新的干预方式作为新治疗策略的一部分。尽管存在几种使用小分子靶向该途径的方法,植物来源的化合物等,纳米粒子已被证明是一种关键的方法,考虑到它的几个优点。高生物利用度,生物相容性,穿越血脑屏障的能力和可修饰的表面特性使纳米粒子比其他策略更具优势。在这一章中,我们将讨论AGEs,它们参与疾病和用于靶向该途径的纳米颗粒。
    Advanced glycation end products (AGEs) are formed by the non-enzymatic attachment of carbohydrates to a biological macromolecule. These AGEs bind to their cognate receptor called receptor for AGEs (RAGEs), which becomes one of the important causal factors for the initiation and progression of several diseases. A deep understanding into the pathways of RAGEs will help in identifying novel intervention modalities as a part of new therapeutic strategies. Although several approaches exist to target this pathway using small molecules, compounds of plant origin etc, nanoparticles have proven to be a critical method, given its several advantages. A high bioavailability, biocompatibility, ability to cross blood brain barrier and modifiable surface properties give nanoparticles an upper edge over other strategies. In this chapter, we will discuss AGEs, their involvement in diseases and the nanoparticles used for targeting this pathway.
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  • 文章类型: Journal Article
    杨梅素及其衍生物,杨梅素和二氢杨梅素,类黄酮广泛存在于食品和植物药中,具有巨大的健康潜力。在这项研究中,我们比较了杨梅素及其衍生物的抗糖基化活性,然后利用蛋白质组学修饰和荧光光谱分析研究了潜在的机制。所有三种化合物都表现出对非酶糖基化过程的彻底抑制,在40μmol/L时对AGEs的抑制作用达到85%。它们通过抑制蛋白质氧化来有效保护牛血清白蛋白(BSA)结构,防止从α-螺旋到β-折叠的转化,并减少淀粉样蛋白样交叉β结构的形成。在这三种化合物中,杨梅素显示出主要的抗糖基化活性。蛋白质组学分析确定了由杨梅素保护的早期糖基化位点,包括赖氨酸K235、256、336、421、420、489等。此外,荧光光谱显示了BSA和杨梅素之间的自发相互作用。总的来说,杨梅素作为抗糖基化剂在食品和药物行业都有希望。
    Myricetin and its derivatives, myricitrin and dihydromyricetin, are flavonoids widely presented in foods and phytomedicine that possess tremendous health potential. In this study, we compared the antiglycation activity of myricetin and its derivatives, then investigated the underlying mechanism using proteomic modification and fluorescence spectroscopy analysis. All three compounds exhibited thorough inhibition on nonenzymatic glycation process, with the inhibitory effects on AGEs reaching 85% at 40 μmol/L. They effectively protected bovine serum albumin (BSA) structure by inhibiting protein oxidation, preventing the conversion from α-helix to β-sheet, and reducing amyloid-like cross-β structure formation. Among the three compounds, myricetin showed a predominant antiglycation activity. Proteomic analysis identified the early glycated sites that were protected by myricetin, including lysine K235, 256, 336, 421, 420, 489, etc. Additionally, fluorescence spectroscopy revealed spontaneous interactions between BSA and myricetin. Overall, myricetin holds promise as an antiglycation agent in both the food and drug industries.
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  • 文章类型: Journal Article
    我们研究了从独特的丝状蓝细菌Pseudanabaenasp生产蓝色色素藻蓝蛋白(PC)的合适培养条件。ABRG5-3和Limnothrixsp。SK1-2-1.白色,绿色,与螺旋藻(螺旋藻)sp相比,以30μmol光子/m2/s的强度或红色LED照射对藻蓝蛋白的生产有效。NIES-39,通常在强光照射下生长。为了研究蓝藻的安全性,ABRG5-3细胞进行Ames(反向突变)测试和单次口服剂量大鼠研究,揭示了非诱变和无毒特性。当三个纯化的藻蓝蛋白(abPC,skPC,和spPC)进行琼脂糖凝胶电泳,他们表现出不同的流动性,表明每个藻蓝蛋白具有独特的性质。abPC表现出强的抗糖基化活性作为新功能。
    We investigated suitable culture conditions for the production of the blue pigment phycocyanin (PC) from the unique filamentous cyanobacteria Pseudanabaena sp. ABRG5-3 and Limnothrix sp. SK1-2-1. White, green, or red LED irradiation at 30 μmol photons/m2/s was effective for phycocyanin production when compared with Arthrospira platensis (Spirulina) sp. NIES-39, which is generally grown under high light irradiation. To investigate the safety of the cyanobacteria, ABRG5-3 cells were subjected to Ames (reverse mutation) tests and single oral-dose rat studies, which revealed non-mutagenic and non-toxic properties. When three purified phycocyanins (abPC, skPC, and spPC) were subjected to agarose gel electrophoresis, they showed different mobility, indicating that each phycocyanin has unique properties. abPC exhibited strong antiglycation activities as novel function.
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  • 文章类型: Journal Article
    活性氧和晚期糖基化终产物的增加通常与人类衰老和退行性疾病有关。BiancaeasappanL是Java中的药用植物和健康饮料成分。然而,本岛植物的药理研究仍缺乏深入。在目前的研究中,使用标记基因maturaseK(matk)的DNA条形码,化学成分的评估,总酚含量(TPC)和抗氧化性能,抗糖基化,抗β-淀粉样蛋白,抗炎,并进行了选择性细胞毒活性。B.sappan与Biancaea属的其他成员共享众所周知的植物成分。心材乙醇提取物具有最突出的抗氧化剂,抗炎,和抗β-淀粉样蛋白的作用.水性提取物表现出最显著的抗糖基化活性并且富含酚类物质。来自心材的乙醇提取物对SW-48表现出最高的细胞毒性,表明来自Java的B.sappan心材有望作为抗氧化剂,并且可以选择性地抑制结直肠癌。
    Increased reactive oxygen species and advanced glycation end products are often associated with human ageing and degenerative diseases. Biancaea sappan L serves as a medicinal plant and a healthy drinks ingredient in Java. However, the pharmacological investigation of the plant native to this island is still lacking in depth. In the current study, DNA barcoding using the marker gene maturase K (matK), evaluation of the chemical composition, total phenolic content (TPC) and antioxidant properties, antiglycation, anti-β-amyloid, anti-inflammatory, and selective cytotoxic activities were performed. B. sappan shares well-known phytoconstituents with other members of the genus Biancaea. The heartwood ethanol extract possesses the most prominent antioxidant, anti-inflammatory, and anti-β-amyloid effects. The aqueous extract demonstrated a most substantial anti-glycation activity and was rich in phenolics. The ethanol extract from heartwood exhibited the highest cytotoxicity against SW-48, indicating B. sappan heartwood from Java holds promise as antioxidants and may selectively inhibit colorectal cancer.
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  • 文章类型: Journal Article
    晚期糖基化终产物(AGEs)在非酶促的美拉德反应的最后一步形成,这可能导致各种健康问题,如糖尿病,肾功能衰竭,慢性炎症。具有抗糖基化特性的生物活性化合物具有抑制AGE相关疾病的潜力。这项研究调查了开心果绿壳(PGH)和石榴皮(PP)提取物的抗糖基化潜力,富含多酚的农业残留物,防止荧光AGE形成,并将结果与吡哆醇(维生素B6)进行比较,二甲双胍,和EDTA(通常的化学抗糖基化剂)。结果表明,PGH和PP能有效抑制牛血清白蛋白-葡萄糖(BSA-Glu)和BSA-果糖(BSA-Fru)中AGEs的形成,抗糖基化活性在92%至97%之间。PP提取物(IC50为94mgml-1)比PGH提取物(IC50为142mgml-1)具有更大的抗糖基化能力。此外,结果表明,提取物的抗糖基化活性与吡哆醇相当,高于二甲双胍和EDTA。这些研究结果表明,这两种提取物可用于高附加值食品的可持续生产,对消费者的健康产生积极影响。
    Advanced glycation end products (AGEs) are formed in the final step of the nonenzymatic Maillard reaction, which can contribute to various health problems such as diabetes mellitus, renal failure, and chronic inflammation. Bioactive compounds with antiglycation properties have the potential to inhibit AGE-related diseases. This study investigated the antiglycation potential of pistachio green hull (PGH) and pomegranate peel (PP) extracts, which are polyphenol-rich agro-residues, against fluorescent AGE formation and compared the results with pyridoxine (vitamin B6), metformin, and EDTA (as usual chemical antiglycation agents). The results showed that PGH and PP effectively inhibited the formation of AGEs in bovine serum albumin-glucose (BSA-Glu) and BSA-fructose (BSA-Fru) with antiglycation activities ranging from 92% to 97%. PP extract (with an IC50 of 94 mg ml-1) had a greater antiglycation ability than PGH extract (with an IC50 of 142 mg ml-1). Also, results indicated that the antiglycation activities of the extracts were comparable to that of pyridoxine, and higher than metformin and EDTA. These findings suggest that the two studied extracts can be used for sustainable production of high-added-value food products with a positive effect on consumers\' health.
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  • 文章类型: Journal Article
    利用农业工业废物丰富食品蛋白质资源并探索其更广泛的应用对于解决粮食危机和实现可持续发展目标至关重要。在这项研究中,使用木瓜蛋白酶和胰蛋白酶水解来自cil的丝胶蛋白,制备丝胶蛋白肽(SRP),并用作高蛋白营养棒(HPNBs)的抗硬化成分。通过研究糖基化终产物和蛋白质氧化产物(羰基和游离巯基)的含量,阐明了SRP的抗硬化作用机理。以及添加SRP前后HPNBs在储存过程中的分子量变化。我们的结果证实了用SRP强化HPNB,这有利于促进和扩大丝胶在食品工业中的应用,对合理利用蛋白质资源和丰富食品蛋白质源具有积极意义。
    The utilization of agroindustrial wastes to enrich food protein resources and the exploration of their broader applications are crucial for addressing the food crisis and achieving sustainable development goals. In this study, reeling wastewater-derived sericin was hydrolyzed using papain and trypsin to prepare sericin peptide (SRP) and was used as an antihardening ingredient of high-protein nutrition bars (HPNBs). The mechanism of the antihardening effect of SRP was elucidated by investigating the content of advanced glycation end products and protein oxidation products (carbonyl and free sulfhydryl), and the molecular weight change of HPNBs during storage before and after the addition of SRP. Our results confirmed the fortification of HPNBs with SRP, which is beneficial for the promotion and expansion of sericin applications in the food industry, with positive implications for the rational utilization of protein resources and the enrichment of food protein sources.
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  • 文章类型: Journal Article
    双曲皮果皮提取物(TBPE),富含可水解单宁,已报道抑制α-葡萄糖苷酶和糖基化反应。我们研究了对大鼠施用TBPE后可水解单宁和相关代谢物的体内行为。使用高压液相色谱-电喷雾电离串联质谱(HPLC-ESI-MS/MS),12种鞣花单宁代谢物,如尿石素和6胆单宁代谢物,在收集的血浆和尿液中产生的定量。尿石素和没食子酸代谢物在给药24和1小时后达到最大血液浓度,分别。相反,尿石素在尿液中的排泄需要长达72小时,并遵循S形曲线,而没食子酸代谢物在给药后较早迅速排出。结果表明,代谢产物gallotannin和ellagitannin负责TBPE的抗糖基化作用,通过不同的机制和时间进行。我们的发现提供了基本数据,证明了可水解单宁以及Trapa成分的功能。
    The pericarp extract of Trapa bispinosa (TBPE), which is rich in hydrolyzable tannins, has been reported to inhibit α-glucosidase and glycation reactions. We investigated the in vivo behavior of hydrolyzable tannins and related metabolites after administration of TBPE to rats. Using high pressure liquid chromatography-electrospray ionization-tandem mass spectroscopy (HPLC-ESI-MS/MS), 12 ellagitannin metabolites, such as urolithins and 6 gallotannin metabolites, produced in the collected plasma and urine were quantified. Urolithins and gallic acid metabolites reached their maximum blood concentration after 24 and 1 h of administration, respectively. Conversely, the excretion of urolithins in urine required up to 72 h and followed a sigmoidal curve, whereas gallic acid metabolites were rapidly excreted earlier after administration. The results suggest that the metabolites gallotannin and ellagitannin are responsible for the antiglycation effect of TBPE, which proceeds via different mechanisms and times. Our findings provide basic data demonstrating the functionality of hydrolyzable tannins as well as Trapa ingredients.
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  • 文章类型: Journal Article
    在我们寻找从Clinacanthusnutans(Burm.f.)Lindau叶发现晚期糖基化终产物(AGEs)抑制剂的过程中,我们进行了生物活性分子网络。该方法整合了LC-MS2概况和体外抗糖基化数据以预测生物活性化合物。我们开始筛选三种提取物:100%乙醇,70%乙醇和100%水的体外抗氧化活性,总酚含量(TPC)和沙己糖苷含量。在这些提取物中,100%乙醇提取物表现出最高的总AGEs抑制作用(IC50=80.18±11.6μg/mL),DPPH清除活性(IC50=747.40±10.30μg/mL)和总酚含量(26.54±2.09μgGAE/mg提取物)。有趣的是,100%乙醇提取物含有最低量的沙夫糖苷,表明其他植物化学物质参与了抗糖基化作用。在来自100%乙醇提取物的级分中检测到的401LC-MS特征的分子网络和计算机结构注释预测了21种生物活性化合物(p<0.05,r>0.90),包括几种C40类胡萝卜素,含有四吡咯结构和脂肪酸的生物碱。相反,所有酚类物质与抗糖基化作用的相关性均较弱.这些预测在体外进一步验证,其中类胡萝卜素叶黄素显示一半最大抑制浓度,IC50=96±8μM,选择的类黄酮-C-糖苷表现出较弱的抑制作用(IC50在568和1922μM之间)。值得注意的是,冻干叶片的叶黄素含量(12.42±0.82mg/100g)高于烘干叶片,尽管前者与汞含量升高有关。总之,坚果梭菌表现出潜在的抗糖基化和抗氧化活性,叶黄素被确定为主要的生物活性成分。
    In our quest to discover advanced glycation end products (AGEs) inhibitors from Clinacanthus nutans (Burm.f.) Lindau leaves, we conducted a bioactivity-based molecular networking. This approach integrates LC-MS2 profiling and in vitro antiglycation data to predict bioactive compounds. We began by screening three extracts: 100% ethanol, 70% ethanol and 100% water alongside the in vitro antioxidant activity, total phenolics content (TPC) and schaftoside content. Among these extracts, 100% ethanol extract exhibited the highest total AGEs inhibition effects (IC50 = 80.18 ± 11.6 μg/mL), DPPH scavenging activity (IC50 = 747.40 ± 10.30 μg/mL) and TPC (26.54 ± 2.09 μg GAE /mg extract). Intriguingly, 100% ethanol extract contained the lowest amount of schaftoside, suggesting the involvement of other phytochemicals in the antiglycation effects. The molecular networking and in silico structural annotations of 401 LC-MS features detected in the fractions from 100% ethanol extract predicted 21 bioactive compounds (p < 0.05, r > 0.90), including several C40 carotenoids, alkaloids containing tetrapyrrole structures and fatty acids. On the contrary, all phenolics showed weak correlations with antiglycation effects. These predictions were further validated in vitro, where carotenoid lutein showed half maximal inhibitory concentration, IC50 = 96 ± 8 μM and selected flavonoid-C-glycosides exhibited weaker inhibitions (IC50 between 568 and 1922 μM). Notably, lutein content was higher in freeze-dried leaves (12.42 ± 0.82 mg/100 g) than oven-dried, although the former was associated with elevated mercury levels. In summary, C. nutans exhibited potential antiglycation and antioxidant activity, and lutein was identified as the main bioactive principle.
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