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Nanodisc Technology: Direction toward Physicochemical Characterization of Chemosensory Membrane Proteins in Food Flavor Research 纳米盘技术:食品风味研究中化感膜蛋白的理化表征方向。
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-21 DOI: 10.1021/acs.jafc.4c01827
Sanjai Karanth, Julia Benthin, Marina Wiesenfarth, Veronika Somoza and Melanie Koehler*, 

Chemosensory membrane proteins such as G-protein-coupled receptors (GPCRs) drive flavor perception of food formulations. To achieve this, a detailed understanding of the structure and function of these membrane proteins is needed, which is often limited by the extraction and purification methods involved. The proposed nanodisc methodology helps overcome some of these existing challenges such as protein stability and solubilization along with their reconstitution from a native cell-membrane environment. Being well-established in structural biology procedures, nanodiscs offer this elegant solution by using, e.g., a membrane scaffold protein (MSP) or styrene–maleic acid (SMA) polymer, which interacts directly with the cell membrane during protein reconstitution. Such derived proteins retain their biophysical properties without compromising the membrane architecture. Here, we seek to show that these lipidic systems can be explored for insights with a focus on chemosensory membrane protein morphology and structure, conformational dynamics of protein–ligand interactions, and binding kinetics to answer pending questions in flavor research. Additionally, the compatibility of nanodiscs across varied (labeled or label-free) techniques offers significant leverage, which has been highlighted here.

G 蛋白偶联受体(GPCR)等化感膜蛋白驱动着食品配方的风味感知。为此,需要详细了解这些膜蛋白的结构和功能,而这往往受到提取和纯化方法的限制。拟议的纳米盘方法有助于克服现有的一些挑战,如蛋白质的稳定性和溶解性,以及从原生细胞膜环境中进行重组。纳米盘在结构生物学程序中已得到广泛应用,它通过使用膜支架蛋白(MSP)或苯乙烯-马来酸(SMA)聚合物等,在蛋白质重组过程中直接与细胞膜相互作用,从而提供了优雅的解决方案。这种衍生蛋白质在保持其生物物理特性的同时不会破坏膜结构。在此,我们试图表明,这些脂质系统可用于探索化学感受膜蛋白的形态和结构、蛋白质配体相互作用的构象动力学以及结合动力学,以回答风味研究中有待解决的问题。此外,纳米光盘在各种(标记或无标记)技术中的兼容性也提供了重要的优势,这一点已在此作了强调。
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引用次数: 0
Design, Synthesis, and Antifungal Activities of Novel Potent Fluoroalkenyl Succinate Dehydrogenase Inhibitors 新型强效氟烯基琥珀酸脱氢酶抑制剂的设计、合成和抗真菌活性。
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-21 DOI: 10.1021/acs.jafc.3c08693
Yu Chen, Weilong Xu, Mian Du, Longzhu Bao, Jun Li, Qianqian Zhai*, Dingce Yan and Huailong Teng*, 

The development of new fungicide molecules is a crucial task for agricultural chemists to enhance the effectiveness of fungicides in agricultural production. In this study, a series of novel fluoroalkenyl modified succinate dehydrogenase inhibitors were synthesized and evaluated for their antifungal activities against eight fungi. The results from the in vitro antifungal assay demonstrated that compound 34 exhibited superior activity against Rhizoctonia solani with an EC50 value of 0.04 μM, outperforming commercial fluxapyroxad (EC50 = 0.18 μM) and boscalid (EC50 = 3.07 μM). Furthermore, compound 34 showed similar effects to fluxapyroxad on other pathogenic fungi such as Sclerotinia sclerotiorum (EC50 = 1.13 μM), Monilinia fructicola (EC50 = 1.61 μM), Botrytis cinerea (EC50 = 1.21 μM), and also demonstrated protective and curative efficacies in vivo on rapeseed leaves and tomato fruits. Enzyme activity experiments and protein–ligand interaction analysis by surface plasmon resonance revealed that compound 34 had a stronger inhibitory effect on succinate dehydrogenase compared to fluxapyroxad. Additionally, molecular docking and DFT calculation confirmed that the fluoroalkenyl unit in compound 34 could enhance its binding capacity with the target protein through p−π conjugation and hydrogen bond interactions.

开发新的杀真菌剂分子是农业化学家提高杀真菌剂在农业生产中有效性的一项重要任务。本研究合成了一系列新型氟烯基修饰琥珀酸脱氢酶抑制剂,并评估了它们对八种真菌的抗真菌活性。体外抗真菌试验结果表明,化合物 34 对根瘤菌(Rhizoctonia solani)具有卓越的活性,其 EC50 值为 0.04 μM,优于商用氟吡菌胺(EC50 = 0.18 μM)和啶酰菌胺(EC50 = 3.07 μM)。此外,化合物 34 对其他病原真菌,如 Sclerotinia sclerotiorum(EC50 = 1.13 μM)、Monilinia fructicola(EC50 = 1.61 μM)、Botrytis cinerea(EC50 = 1.21 μM)也显示出与 fluxapyroxad 相似的效果,并且在油菜叶片和番茄果实上也显示出体内保护和治疗效果。酶活性实验和通过表面等离子共振进行的蛋白质-配体相互作用分析表明,与氟吡菌胺相比,化合物 34 对琥珀酸脱氢酶具有更强的抑制作用。此外,分子对接和 DFT 计算证实,化合物 34 中的氟烯烃基单元可通过 p-π 共轭和氢键相互作用增强其与目标蛋白质的结合能力。
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引用次数: 0
Comparative Label-Free Proteomics Study on Celiac Disease-Active Epitopes in Common Wheat, Spelt, Durum Wheat, Emmer, and Einkorn 关于普通小麦、斯佩尔特小麦、硬质小麦、艾默尔小麦和裸麦中乳糜泻活性表位的无标签蛋白质组学比较研究。
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-21 DOI: 10.1021/acs.jafc.4c02657
Marie-Christin Norwig, Sabrina Geisslitz and Katharina A. Scherf*, 

Wheat species with various ploidy levels may be different regarding their immunoreactive potential in celiac disease (CD), but a comprehensive comparison of peptide sequences with known epitopes is missing. Thus, we used an untargeted liquid chromatography tandem mass spectrometry method to analyze the content of peptides with CD-active epitope in the five wheat species common wheat, spelt, durum wheat, emmer, and einkorn. In total, 494 peptides with CD-active epitope were identified. Considering the average of the eight cultivars of each species, spelt contained the highest number of different peptides with CD-active epitope (193 ± 12, mean ± SD). Einkorn showed the smallest variability of peptides (63 ± 4) but higher amounts of certain peptides compared to the other species. The wheat species differ in the presence and distribution of CD-active epitopes; hence, the entirety of peptides with CD-active epitope is crucial for the assessment of their immunoreactive potential.

不同倍性水平的小麦品种对乳糜泻(CD)的免疫反应潜力可能不同,但目前还缺乏对具有已知表位的肽序列的全面比较。因此,我们采用非靶向液相色谱串联质谱法分析了普通小麦、斯佩尔特小麦、硬质小麦、埃默尔小麦和黑麦这五种小麦中具有乳糜泻活性表位的肽的含量。共鉴定出 494 个具有 CD 活性表位的肽。从每个品种八个栽培品种的平均值来看,斯佩耳特小麦含有CD活性表位的不同肽的数量最多(193±12,平均值±标度)。Einkorn小麦的肽变异性最小(63 ± 4),但与其他品种相比,某些肽的含量较高。小麦物种在 CD 活性表位的存在和分布方面存在差异;因此,具有 CD 活性表位的肽的整体性对于评估其免疫反应潜力至关重要。
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引用次数: 0
Construction of a Novel Vanillin-Induced Autoregulating Bidirectional Transport System in a Vanillin-Producing E. coli Cell Factory 在生产香兰素的大肠杆菌细胞工厂中构建新型香兰素诱导自调节双向运输系统
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-20 DOI: 10.1021/acs.jafc.4c03128
Zhen Li, Lina Sun, Yulu Wang, Bolin Liu and Fengjiao Xin*, 

Vanillin is one of the world’s most extensively used flavoring agents with high application value. However, the yield of vanillin biosynthesis remains limited due to the low efficiency of substrate uptake and the inhibitory effect on cell growth caused by vanillin. Here, we screened high-efficiency ferulic acid importer TodX and vanillin exporters PP_0178 and PP_0179 by overexpressing genes encoding candidate transporters in a vanillin-producing engineered Escherichia coli strain VA and further constructed an autoregulatory bidirectional transport system by coexpressing TodX and PP_0178/PP_0179 with a vanillin self-inducible promoter ADH7. Compared with strain VA, strain VA-TodX-PP_0179 can efficiently transport ferulic acid across the cell membrane and convert it to vanillin, which significantly increases the substrate utilization rate efficiency (14.86%) and vanillin titer (51.07%). This study demonstrated that the autoregulatory bidirectional transport system significantly enhances the substrate uptake efficiency while alleviating the vanillin toxicity issue, providing a promising viable route for vanillin biosynthesis.

香兰素是世界上最广泛使用的调味剂之一,具有很高的应用价值。然而,由于底物吸收效率低以及香兰素对细胞生长的抑制作用,香兰素生物合成的产量仍然有限。在此,我们通过在生产香兰素的工程大肠杆菌菌株 VA 中过表达编码候选转运体的基因,筛选出了高效阿魏酸导入体 TodX 和香兰素导出体 PP_0178 和 PP_0179,并通过在香兰素自诱导启动子 ADH7 上共表达 TodX 和 PP_0178/PP_0179 进一步构建了自调节双向转运系统。与 VA 菌株相比,VA-TodX-PP_0179 菌株能高效地将阿魏酸跨细胞膜转运并转化为香兰素,从而显著提高了底物利用率(14.86%)和香兰素滴度(51.07%)。这项研究表明,自律性双向转运系统能显著提高底物吸收效率,同时缓解香兰素毒性问题,为香兰素的生物合成提供了一条可行的途径。
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引用次数: 0
Whole-Cell Bioconversion Systems for Efficient Synthesis of Monolignols from L-Tyrosine in Escherichia coli 在大肠杆菌中从 L-酪氨酸高效合成单木质素的全细胞生物转化系统。
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-20 DOI: 10.1021/acs.jafc.4c02611
Mingtao Zhao, Baohui Zhang, Xiaofeng Wu and Yi Xiao*, 

Monolignols and their derivatives exhibit various pharmaceutical and physiological characteristics, such as antioxidant and anti-inflammatory properties. However, they remain difficult to synthesize. In this study, we engineered several whole-cell bioconversion systems with carboxylate reductase (CAR)-mediated pathways for efficient synthesis of p-coumaryl, caffeyl, and coniferyl alcohols from l-tyrosine in Escherichia coli BL21 (DE3). By overexpressing the l-tyrosine ammonia lyase from Flavobacterium johnsoniae (FjTAL), carboxylate reductase from Segniliparus rugosus (SruCAR), alcohol dehydrogenase YqhD and hydroxylase HpaBC from E. coli, and caffeate 3-O-methyltransferase (COMT) from Arabidopsis thaliana, three enzyme cascades FjTAL–SruCAR–YqhD, FjTAL–SruCAR–YqhD–HpaBC, and FjTAL–SruCAR–YqhD–HpaBC–COMT were constructed to produce 1028.5 mg/L p-coumaryl alcohol, 1015.3 mg/L caffeyl alcohol, and 411.4 mg/L coniferyl alcohol from 1500, 1500, and 1000 mg/L l-tyrosine, with productivities of 257.1, 203.1, and 82.3 mg/L/h, respectively. This work provides an efficient strategy for the biosynthesis of p-coumaryl, caffeyl, and coniferyl alcohols from l-tyrosine.

单木质素及其衍生物具有多种药物和生理特性,如抗氧化和抗炎特性。然而,它们仍然难以合成。在本研究中,我们在大肠杆菌 BL21 (DE3) 中设计了几种以羧酸还原酶 (CAR) 为介导途径的全细胞生物转化系统,用于从 l-酪氨酸中高效合成对羟基香豆素、咖啡酰和松柏醇。通过过表达大肠杆菌中的黄杆菌(Flavobacterium johnsoniae)的酪氨酸氨化酶(FjTAL)、红球菌(Segniliparus rugosus)的羧酸还原酶(SruCAR)、醇脱氢酶 YqhD 和羟化酶 HpaBC利用大肠杆菌中的醇脱氢酶 YqhD 和羟化酶 HpaBC 以及拟南芥中的咖啡酸 3-O-甲基转移酶 COMT,构建了三个酶级联 FjTAL-SruCAR-YqhD、FjTAL-SruCAR-YqhD-HpaBC 和 FjTAL-SruCAR-YqhD-HpaBC-COMT,生产出 1028.5 mg/L 对迷迭香醇、1015.3 mg/L 咖啡醇和 411.4 mg/L 针叶醇,生产率分别为 257.1、203.1 和 82.3 mg/L/h。这项工作为从 l-酪氨酸中生物合成对迷迭香醇、咖啡醇和松柏醇提供了一种有效的策略。
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引用次数: 0
Cell Wall Modification Based on Combination Reagents to Improve Dimensional Stability of Wood with High Efficiency 基于组合试剂的细胞壁改性可高效改善木材的尺寸稳定性。
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-20 DOI: 10.1021/acs.jafc.4c02876
Yuhan Qiu, Chuanshuang Hu*, Jiewen Li, Qin Lai, Ziling Liu, Xiuyi Lin and Weiwei Zhang*, 

Although γ-methacryloxypropyltrimethoxysilane (MPS) was proved to be an effective reagent for improving the dimensional stability of wood, a bottleneck in ASE value (around 50%) existed. The reason was that MPS with low polarity opened few hydrogen bonds in the amorphous region of cellulose, while these hydrogen bonds could be reopened by water. Therefore, citric acid (CA) is chosen to cooperate with MPS to further enhance the dimensional stability of wood. In this paper, MPS and CA were used to modify wood individually (MW and CW) or with different combinations, that is, one-step modification (M/CW) and two-step modification with MPS first (M-CW) or CA first (C-MW). CA and MPS concentrations were optimized at 5 wt%. The ASE value for M/CW was only 25.74% at a weight percent gain (WPG) of 6.43%, which was only 0.6 times to MW or 0.7 times to CW. For M-CW, the ASE value gradually decreased with the soaking cycles, from 65.64% at a WPG of 9.05% to 51.20%. The C-MW had the best dimensional stability, with the ASE value 75.35% at a WPG of 11.50%. Although it decreased during the first soaking cycle, it stabilized at 62.20% at last. SEM and EDS images showed that the polymer mainly distributed in cell walls and few in cell lumen in C-MW. Thus, the enhanced dimensional stability of C-MW could be explained by CA opening the hydrogen bonds in the amorphous region of cellulose first, which provided more binding sites for MPS.

虽然γ-甲基丙烯酰氧基丙基三甲氧基硅烷(MPS)被证明是一种有效的试剂,可以提高木材的尺寸稳定性,但 ASE 值(约 50%)存在瓶颈。原因是极性低的 MPS 在纤维素的无定形区域打开的氢键很少,而这些氢键可以被水重新打开。因此,人们选择柠檬酸(CA)与 MPS 配合使用,以进一步提高木材的尺寸稳定性。本文使用 MPS 和 CA 对木材进行单独改性(MW 和 CW)或不同组合的改性,即一步改性(M/CW)和先用 MPS 后用 CA 的两步改性(M-CW)。CA 和 MPS 的最佳浓度为 5 wt%。M/CW 的 ASE 值仅为 25.74%,增重百分比 (WPG) 为 6.43%,仅为 MW 的 0.6 倍或 CW 的 0.7 倍。对于 M-CW 而言,随着浸泡周期的增加,ASE 值逐渐降低,从 WPG 为 9.05% 时的 65.64% 降至 51.20%。C-MW 的尺寸稳定性最好,WPG 为 11.50%时的 ASE 值为 75.35%。虽然在第一个浸泡周期中,ASE 值有所下降,但最后稳定在 62.20%。SEM 和 EDS 图像显示,聚合物主要分布在 C-MW 的细胞壁中,很少分布在细胞腔中。因此,C-MW 尺寸稳定性增强的原因可能是 CA 首先打开了纤维素无定形区的氢键,从而为 MPS 提供了更多的结合位点。
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引用次数: 0
Discovery and Biosynthesis of Streptolateritic Acids A–D: Acyclic Pentacarboxylic Acids from Streptomyces sp. FXJ1.172 with Promising Activity against Potato Common Scab 链霉菌 FXJ1.172 中发现并生物合成的链霉菌酸 A-D:环状五羧酸,对马铃薯常见疮痂病具有良好活性。
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-20 DOI: 10.1021/acs.jafc.4c02572
Kairui Wang, Ning Liu, Minghao Liu*, Pan Zhao, Naiqin Zhong, Gregory L. Challis and Ying Huang*, 

Potato common scab (PCS) is a widespread plant disease that lacks effective control measures. Using a small molecule elicitor, we activate the production of a novel class of polyketide antibiotics, streptolateritic acids A–D, in Streptomyces sp. FXJ1.172. These compounds show a promising control efficacy against PCS and an unusual acyclic pentacarboxylic acid structure. A gene cluster encoding a type I modular polyketide synthase is identified to be responsible for the biosynthesis of these metabolites. A cytochrome P450 (CYP) and an aldehyde dehydrogenase (ADH) encoded by two genes in the cluster are proposed to catalyze iterative oxidation of the starter-unit-derived methyl group and three of six branching methyl groups to carboxylic acids during chain assembly. Our findings highlight how activation of silent biosynthetic gene clusters can be employed to discover completely new natural product classes able to combat PCS and new types of modular polyketide synthase-based biosynthetic machinery.

马铃薯普通疮痂病(PCS)是一种广泛传播的植物病害,缺乏有效的防治措施。利用小分子诱导剂,我们激活了链霉菌 FXJ1.172 产生一类新型多酮抗生素--链霉菌酸 A-D。这些化合物对 PCS 具有良好的防治效果,并具有不寻常的无环五羧酸结构。经鉴定,一个编码 I 型模块化多酮合成酶的基因簇负责这些代谢物的生物合成。该基因簇中的两个基因编码的细胞色素 P450(CYP)和醛脱氢酶(ADH)被认为在链组装过程中催化起始单元衍生的甲基和六个分支甲基中的三个氧化成羧酸。我们的研究结果强调了如何通过激活沉默的生物合成基因簇来发现能够对抗 PCS 的全新天然产品类别以及基于多酮合成酶的新型模块化生物合成机制。
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引用次数: 0
Structural Variances in Curcumin Degradants: Impact on Obesity in Mice 姜黄素降解物的结构差异:对小鼠肥胖症的影响
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-20 DOI: 10.1021/acs.jafc.4c03768
Yen-Chun Koh, Han-Wen Hsu, Pin-Yu Ho, Kai-Yu Hsu, Wei-Sheng Lin, Kalyanam Nagabhushanam, Chi-Tang Ho and Min-Hsiung Pan*, 

Some thermal degradants of curcuminoids have demonstrated moderate health benefits in previous studies. Feruloyl acetone (FER), recently identified as a thermal degradant of curcumin, has been previously associated with anticancer and antioxidative effects, yet its other capabilities remain unexplored. Moreover, earlier reports suggest that methoxy groups on the aromatic ring may influence the functionality of the curcuminoids. To address these gaps, an animal study was conducted to investigate the antiobesity effects of both FER and its demethoxy counterpart (DFER) on mice subjected to a high-fat diet. The results demonstrated the significant prevention of weight gain and enlargement of the liver and various adipose tissues by both samples. Furthermore, these supplements exhibited a lipid regulatory effect in the liver through the adiponectin/AMPK/SIRT1 pathway, promoted thermogenesis via AMPK/PGC-1α activation, and positively influenced gut-microbial-produced short-chain fatty acid (SCFA) levels. Notably, DFER demonstrated superior overall efficacy in combating obesity, while FER displayed a significant effect in modulating inflammatory responses. It is considered that SCFA may be responsible for the distinct effects of FER and DFER in the animal study. Future studies are anticipated to delve into the efficacy of curcuminoid degradants, encompassing toxicity and pharmacokinetic evaluations.

在以往的研究中,一些姜黄素热降解剂显示出了适度的健康益处。阿魏酰丙酮(FER)最近被确认为姜黄素的一种热降解剂,以前曾被认为具有抗癌和抗氧化作用,但它的其他功能仍有待探索。此外,早前的报告表明,芳香环上的甲氧基可能会影响姜黄素的功能。为了填补这些空白,我们开展了一项动物实验,研究 FER 及其去甲氧基对应物(DFER)对高脂饮食小鼠的抗肥胖作用。结果表明,这两种样品都能明显防止体重增加以及肝脏和各种脂肪组织的增大。此外,这些营养补充剂还通过脂肪连通素/AMPK/SIRT1途径对肝脏中的脂质产生调节作用,通过激活AMPK/PGC-1α促进产热,并对肠道微生物产生的短链脂肪酸(SCFA)水平产生积极影响。值得注意的是,DFER 在对抗肥胖方面表现出更优越的整体功效,而 FER 则在调节炎症反应方面表现出显著效果。在动物实验中,SCFA 可能是 FER 和 DFER 产生不同效果的原因。预计未来的研究将深入探讨姜黄素降解剂的功效,包括毒性和药代动力学评估。
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引用次数: 0
Enniatins A1 and B1 Modulate Calcium Flux through Alternative Pathways beyond Mitochondria Enniatins A1 和 B1 通过线粒体以外的替代途径调节钙通量
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-19 DOI: 10.1021/acs.jafc.4c04242
Nadia Pérez-Fuentes, Rebeca Alvariño*, Amparo Alfonso*, Jesús González-Jartín, Mercedes R. Vieytes and Luis M. Botana, 

Enniatins (ENNs) A1 and B1, previously considered ionophores, are emerging mycotoxins with effects on Ca2+ homeostasis. However, their exact mechanism of action remains unclear. This study investigated how these toxins affect Ca2+ flux in SH-SY5Y cells. ENN A1 induced Ca2+ influx through store-operated channels (SOC). The mitochondrial uncoupler FCCP reduced this influx, suggesting that the mitochondrial status influences the toxin effect. Conversely, ENN B1 did not affect SOC but acted on another Ca2+ channel, as shown when nickel, which directly blocks the Ca2+ channel pore, is added. Mitochondrial function also influenced the effects of ENN B1, as treatment with FCCP reduced toxin-induced Ca2+ depletion and uptake. In addition, both ENNs altered mitochondrial function by producing the opening of the mitochondrial permeability transition pore. This study describes for the first time that ENN A1 and B1 are not Ca2+ ionophores and suggests a different mechanism of action for each toxin.

烯萘啶(ENNs)A1 和 B1 以前被认为是离子促进剂,是对 Ca2+ 平衡有影响的新兴霉菌毒素。然而,它们的确切作用机制仍不清楚。本研究调查了这些毒素如何影响SH-SY5Y细胞中的Ca2+通量。ENN A1通过储存操作通道(SOC)诱导Ca2+流入。线粒体解耦剂 FCCP 可减少这种流入,这表明线粒体状态会影响毒素效应。相反,ENN B1 不影响 SOC,但作用于另一个 Ca2+ 通道,如加入直接阻断 Ca2+ 通道孔的镍时所示。线粒体功能也影响 ENN B1 的作用,因为用 FCCP 处理可减少毒素诱导的 Ca2+ 耗竭和摄取。此外,这两种 ENN 还能通过打开线粒体通透性转换孔来改变线粒体功能。这项研究首次描述了ENN A1和B1不是Ca2+离子促进剂,并提出了两种毒素的不同作用机制。
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引用次数: 0
Unambiguous Characterization of Commercial Natural (Dihydro)phenanthrene Compounds Is Vital in the Discovery of AMPK Activators 明确商用天然(二氢)菲化合物的特性对发现 AMPK 激活剂至关重要
IF 5.7 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2024-06-19 DOI: 10.1021/acs.jafc.4c01616
Denis Barron*, Yann Ratinaud, Simona Rambousek, Benjamin Brinon, Martine Naranjo Pinta, Matthew J Sanders, Kei Sakamoto and Olivier Ciclet, 

These days, easy access to commercially available (poly)phenolic compounds has expanded the scope of potential research beyond the field of chemistry, particularly in the area of their bioactivity. However, the quality of these compounds is often overlooked or not even considered. This issue is illustrated in this study through the example of (dihydro)phenanthrenes, a group of natural products present in yams, as AMP-activated protein kinase (AMPK) activators. A study conducted in our group on a series of compounds, fully characterized using a combination of chemical synthesis, NMR and MS techniques, provided evidence that the conclusions of a previous study were erroneous, likely due to the use of a misidentified commercial compound by its supplier. Furthermore, we demonstrated that additional representatives of the (dihydro)phenanthrene phytochemical classes were able to directly activate AMPK, avoiding the risk of misinterpretation of results based on analysis of a single compound alone.

如今,由于可以方便地从市场上获得(多)酚类化合物,潜在的研究范围已经扩展到化学领域之外,尤其是在其生物活性方面。然而,这些化合物的质量往往被忽视,甚至根本没有被考虑到。本研究通过(二氢)菲类化合物(山药中的一类天然产品)作为 AMP 激活蛋白激酶(AMPK)激活剂的例子来说明这一问题。我们小组对一系列化合物进行了研究,并结合化学合成、核磁共振和质谱技术对其进行了全面鉴定,结果证明之前的研究结论是错误的,这很可能是由于供应商使用了一种识别错误的商业化合物。此外,我们还证明了(二氢)菲类植物化学物质的其他代表能够直接激活 AMPK,从而避免了仅根据对单一化合物的分析而误读结果的风险。
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引用次数: 0
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