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Effects of silver nanoparticles on the morphology and membrane permeability of giant unilamellar vesicles and their mechanistic insights 银纳米粒子对巨型单层囊泡形态和膜通透性的影响及其机理
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2026-01-02 DOI: 10.1016/j.chemphyslip.2025.105564
Zarin Tasnim Rakhy , Tawfika Nasrin , Mir Jubair Ahamed , Md. Masum Billah , Md. Wahadoszamen , Aminul I. Talukder , Mohammad Abu Sayem Karal
Silver nanoparticles (AgNPs) are extensively used in healthcare, medicine, and environmental fields owing to their strong antiviral and antibacterial properties. Although these NPs interact with cellular biomembranes or vesicular lipid membranes, their mechanisms of interaction under physiological conditions using cell-mimetic giant unilamellar vesicles (GUVs) have been rarely investigated. In this study, we focused on the interaction of AgNPs with cell-sized GUVs and investigated deformation, membrane permeation, and change in membrane area under 0.3 – 5.0 μg/mL concentrations of AgNPs. The synthesized particles exhibited an average size of 58.1 nm and a zeta potential of –6.9 mV. The deformation of GUV and the fraction of deformation increase with the increase of AgNPs concentration. The encapsulating calcein of GUVs leaked out through the membranes while interacting the AgNPs, indicated the nano-sized pore formation in the membranes of vesicles. The leakage constant increased with the increase of NPs concentration, as well as the pore size. The membrane area of a GUV measured by micropipette technique exhibits a dynamic response: an initial rapid expansion, followed by a gradual contraction, and a subsequent slight increase over time. This provides insights into AgNPs-GUVs binding dynamics. These investigations help to understand the mechanism of interaction of AgNPs in the cell membranes which might be used in several biophysical and biomedical applications.
银纳米颗粒(AgNPs)由于其强大的抗病毒和抗菌特性而广泛应用于医疗保健、医药和环境领域。尽管这些NPs与细胞生物膜或囊泡脂质膜相互作用,但它们在生理条件下通过模拟细胞的巨大单层囊泡(GUVs)相互作用的机制很少被研究。在这项研究中,我们重点研究了AgNPs与细胞大小的guv的相互作用,并研究了0.3 - 5.0 μg/mL浓度下AgNPs的变形、膜渗透和膜面积的变化。合成的粒子平均尺寸为58.1 nm, zeta电位为-6.9 mV。随着AgNPs浓度的增加,GUV的变形量和变形率增大。在与AgNPs相互作用的过程中,包裹guv的钙黄蛋白从膜中泄漏出来,表明在囊泡膜上形成了纳米级孔。泄漏常数随NPs浓度的增加和孔径的增大而增大。微移液管技术测量的GUV膜面积表现出动态响应:最初快速膨胀,随后逐渐收缩,随后随着时间的推移略有增加。这为agnps - guv结合动力学提供了深入的见解。这些研究有助于了解AgNPs在细胞膜内相互作用的机制,这可能在许多生物物理和生物医学应用中使用。
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引用次数: 0
Molecular dynamics deciphers drug-dependent stability in therapeutic liposomes 分子动力学解释治疗性脂质体的药物依赖稳定性。
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-12-05 DOI: 10.1016/j.chemphyslip.2025.105563
F. Rostami , D.M. Aghaie , O. Bavi
Liposomal stability is critical for effective drug delivery, yet its dependence on drug-membrane interactions remains incompletely understood. Here, we employ atomic-scale molecular dynamics simulations to investigate the structural stability of a commercial liposome (composed of DMPC/DMPG phospholipids) when loaded with two therapeutic agents: amphotericin B (an antifungal) and 5-fluorouracil (5-FU, an anticancer drug). Our simulations reveal that amphotericin B maintains liposomal integrity, with minimal perturbations to membrane thickness, lipid order, and surface area. In contrast, 5-FU induces significant destabilization, including reduced membrane thickness, expanded lipid spacing, and disordered acyl chain packing-corroborated by alterations in deuterium order parameters, mass density profiles, and charge distributions. These findings demonstrate that while the liposome is an optimal carrier for amphotericin B, its composition requires modification for some anticancer drug delivery. The study provides mechanistic insights into drug-dependent liposomal stability, offering a framework for the rational design of tailored nanocarriers.
脂质体的稳定性对有效的药物传递至关重要,但其对药物-膜相互作用的依赖性仍不完全清楚。在这里,我们采用原子尺度的分子动力学模拟来研究商业脂质体(由DMPC/DMPG磷脂组成)在加载两种治疗药物时的结构稳定性:两性霉素B(一种抗真菌药物)和5-氟尿嘧啶(5-FU,一种抗癌药物)。我们的模拟显示两性霉素B维持脂质体的完整性,对膜厚度、脂质顺序和表面积的扰动最小。相比之下,5-FU诱导了显著的不稳定性,包括膜厚度减少、脂质间距扩大和酰基链堆积紊乱——氘有序参数、质量密度分布和电荷分布的改变证实了这一点。这些发现表明,虽然脂质体是两性霉素B的最佳载体,但其成分需要修改以用于某些抗癌药物的递送。该研究提供了药物依赖性脂质体稳定性的机制见解,为合理设计量身定制的纳米载体提供了框架。
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引用次数: 0
A comparison of the effect of SMA derivatives on the structural topology and dynamics of two bacteriophage peptides SMA衍生物对两种噬菌体肽的结构拓扑和动力学影响的比较
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-12-02 DOI: 10.1016/j.chemphyslip.2025.105562
Nancy C. Rotich , Evelyn A. Okorafor , Indra D. Sahu , Muhammad Zeeshan Shah , Dominik Konkolewicz , Gary A. Lorigan
Researchers have explored and cultivated suitable membrane mimetics to preserve a physiological solvent condition for membrane protein functions. This involves emulating the properties of lipid bilayers, particularly within the hydrophobic core. Membrane mimetics exist in diverse forms, such as micelles, bicelles, liposomes, and nanodiscs. Polymers, such as styrene-maleic acid (SMA), have been found to offer a potentially suitable means to solubilize membrane proteins without resorting to detergents. It is widely recognized that various membrane mimetics yield distinct structural and dynamic configurations in membrane proteins. Styrene-maleic acid derivatives (SMADs) are of particular significance in this study; they are known for their ability to generate lipid nanoparticles. It has been hypothesized that using SMA derivatives with the same charge as the target membrane protein preserves the protein's structural and dynamic attributes compared to other bilayer membrane mimetics. This study explores the impact of different charges of SMA derivatives on two bacteriophage-encoded peptides explicitly focusing on their influence as charged peptides. Positively charged, neutral, and negatively charged SMA derivatives interactions with pinholin S21 and the phage-encoded cationic antimicrobial peptide gp28 lipid vesicles were assessed. These interactions were characterized using dynamic light scattering (DLS) techniques and continuous wave electron paramagnetic resonance (CW-EPR) spectroscopy. From our DLS results, we observed a reduction in size compared to the vesicle control, which is consistent with the formation of SMADLPs (styrene maleic acid derivative lipid nanoparticles). The key outcome was in the identification of how various SMA derivatives affect the interaction of gp28 and pinholin membrane peptides, which is useful when trying to understand how the different SMA polymers can influence the behavior and stability of protein complexes. For gp28 peptide, CW-EPR spectral analysis indicates no line broadening in its profile, suggesting that binding interactions with SMA derivatives do not significantly disrupt the structural integrity or dynamic behavior of the gp28 peptide. SMA-Pos interaction with pinholin shows some minimal perturbation, confirming that it is not as compatible compared to SMA-Neut and SMA-Glu. This study will provide insights into the optimal conditions for studying membrane protein interactions, focusing on the structural dynamics of gp28 and pinholin in the presence of different SMA derivatives.
研究人员已经探索并培养了合适的膜模拟物,以保持膜蛋白功能的生理溶剂条件。这包括模拟脂质双分子层的性质,特别是在疏水核心内。膜模拟物以多种形式存在,如胶束、双束、脂质体和纳米圆盘。聚合物,如苯乙烯-马来酸(SMA),已经被发现提供了一种潜在的合适的方法来溶解膜蛋白,而不需要求助于洗涤剂。人们普遍认为,各种膜模拟物在膜蛋白中产生不同的结构和动态构型。苯乙烯-马来酸衍生物(SMADs)在本研究中具有特殊意义;它们以产生脂质纳米颗粒的能力而闻名。据推测,与其他双层膜模拟物相比,使用与靶膜蛋白具有相同电荷的SMA衍生物可以保留蛋白质的结构和动态属性。本研究探讨了SMA衍生物的不同电荷对两种噬菌体编码肽的影响,明确地关注了它们作为带电肽的影响。评估了带正电荷、中性电荷和负电荷的SMA衍生物与pinholin S21和噬菌体编码的阳离子抗菌肽gp28脂质囊泡的相互作用。利用动态光散射(DLS)技术和连续波电子顺磁共振(CW-EPR)光谱对这些相互作用进行了表征。从我们的DLS结果中,我们观察到与囊泡对照相比,囊泡大小减小,这与SMADLPs(苯乙烯马来酸衍生物脂质纳米颗粒)的形成一致。关键的结果是确定了各种SMA衍生物如何影响gp28和pinholin膜肽的相互作用,这在试图了解不同SMA聚合物如何影响蛋白质复合物的行为和稳定性时是有用的。对于gp28肽,CW-EPR光谱分析显示其谱线没有变宽,这表明与SMA衍生物的结合相互作用不会显著破坏gp28肽的结构完整性或动态行为。SMA-Pos与pinholin的相互作用显示出一些最小的扰动,证实它与SMA-Neut和SMA-Glu相比不兼容。本研究将为研究膜蛋白相互作用的最佳条件提供见解,重点关注gp28和pinholin在不同SMA衍生物存在下的结构动力学。
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引用次数: 0
Sources and biological functions of nervonic acid: Advances and perspectives 神经酸的来源和生物学功能:进展与展望。
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-11-01 DOI: 10.1016/j.chemphyslip.2025.105554
Yihe Li , Xiaolong Gao , Zhuoao Gao , Zhonghong Cao , Peng Xiong , Xiutao Liu
Nervonic Acid (NA), as a critical component of neural myelin sheaths, maintains nerve cell structural integrity and function. Due to limited synthesis in humans, it is primarily obtained through plant extraction, chemical synthesis, or biosynthetic methods. Its bioactive properties and applications encompass: mitigating oxidative stress and improving cognitive function; balancing pro-/anti-inflammatory factors to alleviate inflammation in organs such as liver or colon while modulating gut microbiota; its level fluctuations being closely associated with psychiatric disorders and metabolic diseases, demonstrating biomarker potential for early diagnosis. Furthermore, nervonic acid exerts multi-dimensional protective effects on cardiovascular health and metabolic homeostasis, while serving as a functional ingredient in dietary supplements and infant formula. This review systematically elaborates on the three primary sources of nervonic acid, discusses its biological functions in neuroprotection, anti-inflammatory activity, and metabolic regulation, and explores its potential applications in biomarker development and functional foods. The review aims to provide an important theoretical foundation for future disease prevention strategies and the development of health-oriented products.
神经酸(NA)作为神经髓鞘的重要组成部分,维持神经细胞的结构完整性和功能。由于人体合成有限,它主要通过植物提取、化学合成或生物合成方法获得。其生物活性特性和应用包括:减轻氧化应激和改善认知功能;平衡促/抗炎因子,以减轻肝脏或结肠等器官的炎症,同时调节肠道微生物群;其水平波动与精神疾病和代谢性疾病密切相关,具有早期诊断的生物标志物潜力。此外,神经酸对心血管健康和代谢稳态具有多方面的保护作用,同时作为膳食补充剂和婴儿配方奶粉的功能性成分。本文系统阐述了神经酸的三种主要来源,讨论了其在神经保护、抗炎和代谢调节等方面的生物学功能,并探讨了其在生物标志物开发和功能食品中的潜在应用。旨在为今后的疾病预防策略和健康导向产品的开发提供重要的理论依据。
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引用次数: 0
Lipidomic profiling of of cutaneous surface lipid alterations in sensitive scalp in Beijing 北京敏感头皮皮肤表面脂质改变的脂质组学分析
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-11-01 DOI: 10.1016/j.chemphyslip.2025.105551
Ran Li , Qian Jiao , Liya Song , Youjie He , Huaming He , Cheng Zhou , Yan Jia

Background

Scalp sensitivity is an increasing global concern. While its pathophysiology remains unclear, evidence suggests its close association with skin barrier dysfunction caused by lipid secretion dysregulation.

Objective

To identify potential biomarkers for the sensitive scalp through comprehensive analysis of physiological parameters (pH, TEWL, erythera) and scalp lipidomic profiling.

Methods

A total of 100 females aged 18–25 years (50 with the sensitive scalp and 50 with the non-sensitive scalp) were recruited in Beijing area. Lipidomics analysis of the collected scalp lipid samples was conducted using UPLC-QTOF-MS to identify differential lipids. Additionally, physiological parameters of the scalp were measured using non-invasive methods.

Results

The sensitive scalp group exhibited higher levels of TEWL, pH, erythera, and scalp imaging revealed increased redness in the sensitive scalp group. The lipidomics analysis identified 46 characteristic lipids. Furthermore, lipids of the [ST], [PR], [GP], and [FA] categories were significantly negatively correlated with physiological parameters, while lipids of the [SP] and [GL] categories displayed a significant positive correlation.

Conclusion

This study reveals distinct differences in physical characteristics and surface lipid composition between sensitive and non-sensitive scalps, identifying specific lipids that play a critical role in scalp sensitivity.
背景:头皮敏感性是全球日益关注的问题。虽然其病理生理机制尚不清楚,但有证据表明其与脂质分泌失调引起的皮肤屏障功能障碍密切相关。目的通过对敏感头皮生理参数(pH、TEWL、红斑)和头皮脂质谱的综合分析,寻找潜在的生物标志物。方法选取北京地区18 ~ 25岁女性100例,其中敏感头皮50例,非敏感头皮50例。采用UPLC-QTOF-MS对采集的头皮脂质样品进行脂质组学分析,以鉴定差异脂质。此外,使用非侵入性方法测量头皮的生理参数。结果敏感头皮组TEWL、pH、红斑水平升高,头皮成像显示敏感头皮组发红增加。脂质组学分析鉴定出46种特征脂质。[ST]、[PR]、[GP]、[FA]类脂质与生理参数呈显著负相关,[SP]、[GL]类脂质与生理参数呈显著正相关。结论本研究揭示了敏感和非敏感头皮的物理特征和表面脂质组成的明显差异,确定了在头皮敏感中起关键作用的特定脂质。
{"title":"Lipidomic profiling of of cutaneous surface lipid alterations in sensitive scalp in Beijing","authors":"Ran Li ,&nbsp;Qian Jiao ,&nbsp;Liya Song ,&nbsp;Youjie He ,&nbsp;Huaming He ,&nbsp;Cheng Zhou ,&nbsp;Yan Jia","doi":"10.1016/j.chemphyslip.2025.105551","DOIUrl":"10.1016/j.chemphyslip.2025.105551","url":null,"abstract":"<div><h3>Background</h3><div>Scalp sensitivity is an increasing global concern. While its pathophysiology remains unclear, evidence suggests its close association with skin barrier dysfunction caused by lipid secretion dysregulation.</div></div><div><h3>Objective</h3><div>To identify potential biomarkers for the sensitive scalp through comprehensive analysis of physiological parameters (pH, TEWL, erythera) and scalp lipidomic profiling.</div></div><div><h3>Methods</h3><div>A total of 100 females aged 18–25 years (50 with the sensitive scalp and 50 with the non-sensitive scalp) were recruited in Beijing area. Lipidomics analysis of the collected scalp lipid samples was conducted using UPLC-QTOF-MS to identify differential lipids. Additionally, physiological parameters of the scalp were measured using non-invasive methods.</div></div><div><h3>Results</h3><div>The sensitive scalp group exhibited higher levels of TEWL, pH, erythera, and scalp imaging revealed increased redness in the sensitive scalp group. The lipidomics analysis identified 46 characteristic lipids. Furthermore, lipids of the [ST], [PR], [GP], and [FA] categories were significantly negatively correlated with physiological parameters, while lipids of the [SP] and [GL] categories displayed a significant positive correlation.</div></div><div><h3>Conclusion</h3><div>This study reveals distinct differences in physical characteristics and surface lipid composition between sensitive and non-sensitive scalps, identifying specific lipids that play a critical role in scalp sensitivity.</div></div>","PeriodicalId":275,"journal":{"name":"Chemistry and Physics of Lipids","volume":"273 ","pages":"Article 105551"},"PeriodicalIF":2.8,"publicationDate":"2025-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145413567","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"生物学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Corrigendum to "Effect of the CER[NP]:CER[AP] a ratio on the structure of a stratum corneum model lipid matrix - a molecular dynamics study" [Chem. Phys. Lipid. 250 (2023) 105259] “CER[NP]:CER[AP] a比值对角质层模型脂质基质结构的影响——分子动力学研究”的更正[化学]。理论物理。脂质。250 (2023)105259]
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-11-01 DOI: 10.1016/j.chemphyslip.2025.105553
Natalia Rivero, Martha C. Daza, Markus Doerr
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引用次数: 0
Coexistence of domains composed of intercellular lipids in stratum corneum as studied by X-ray diffraction and differential scanning calorimetry 用x射线衍射和差示扫描量热法研究角质层中细胞间脂质结构域的共存。
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-11-01 DOI: 10.1016/j.chemphyslip.2025.105552
Ichiro Hatta , Yoshitomo Furushima , Masaru Nakada , Tsuneyuki Yamane
The intercellular lipid matrix of stratum corneum is composed of many lipid components, including ceramides, free fatty acids, and cholesterol, which nonetheless form regularly arranged structures; short- and long-period lamellar structures, and hexagonal and orthorhombic hydrocarbon-chain packing structures. From the viewpoint of compatibility among the structures, there should be a correlation between a lamellar structure arranged periodically along the long axis of the lipid molecules and a packing structure of the hydrocarbon chains in the plane orthogonal to the long axis. To address this issue, differential scanning calorimetry and temperature-dependent X-ray diffraction experiment were performed on human stratum corneum. A detailed comparative analysis of the results on phase transitions obtained by the two methods revealed that the short-period lamellar structure has the orthorhombic hydrocarbon-chain packing structure that is normally observed, while the long-period lamellar structure has another orthorhombic hydrocarbon-chain packing structure hidden in the normal structure, and furthermore, the hexagonal hydrocarbon-chain packing structure does not appear to form a corresponding multilamellar structure and start to undergo a phase transition to the liquid state approximately at 33 °C. The domain constructed with the short-period lamellar structure and the orthorhombic hydrocarbon-chain packing structure is important in considering the water regulation mechanism in stratum corneum, since it provides evidence not only of the water layer of the former but also of changes in the head group of the latter.
角质层的细胞间脂质基质由许多脂质成分组成,包括神经酰胺、游离脂肪酸和胆固醇,但它们仍形成规则排列的结构;短周期和长周期片层结构,六方和正方烃链充填结构。从结构相容性的角度看,沿脂质分子长轴周期性排列的层状结构与与长轴正交平面上烃链的排列结构之间应该存在一定的相关性。为了解决这一问题,对人体角质层进行了差示扫描量热法和温度依赖x射线衍射实验。对两种方法的相变结果进行了详细的对比分析,发现短周期片层结构具有通常观察到的正构烷烃链充填结构,而长周期片层结构在正构烷烃链充填结构中隐藏着另一种正构烷烃链充填结构。六方烃链充填结构未形成相应的多层结构,在33℃左右开始相变为液态。由短周期层状结构和正方烷烃链充填结构构成的区域,不仅为角质层的水层结构提供了证据,也为角质层头群的变化提供了证据,对角质层水分调节机制具有重要意义。
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引用次数: 0
Branched-chain fatty acids with different structure exhibit distinct anti-hepatoma activities and characteristics 不同结构的支链脂肪酸具有不同的抗肝癌活性和特性。
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-10-10 DOI: 10.1016/j.chemphyslip.2025.105549
Yaqi Huang, Houyue Li, Jialing Gu, Zongrun Li, Weijia Bao, Xiaosan Wang
Branched-chain fatty acids (BCFAs) exhibit potential anticancer activity, but their systematic evaluation and comparison with straight-chain saturated fatty acids (SSFAs) remain limited due to monomer accessibility issues. This study utilized lanolin, a rich BCFA/SSFA mixture, to systematically assess anti-hepatoma activities of 50 fatty acids using multiple linear regression (MLR) and orthogonal partial least squares (OPLS) models combined with HepG2 cell viability, apoptosis, and cell cycle assays. MLR identified iso-C13:0 as a unique protective fatty acid, while OPLS revealed strong explanatory power (R2X = 0.827–0.997, R2Y = 0.718–0.782) and key anti-hepatoma fatty acids, including SSFAs (C12:0, C13:0, C14:0, C19:0, C21:0) and BCFAs (16–19-carbon iso-BCFAs, 14–19-carbon anteiso-BCFAs). Notably, SSFAs outperformed BCFAs in certain activities, and a structure-activity trend emerged: odd-carbon BCFAs favored cell cycle arrest, even-carbon BCFAs promoted apoptosis, and 13–21-carbon fatty acids showed stronger activity. The integrated approach validated lanolin as an ideal matrix for functional lipid screening, providing a methodology to identify anticancer fatty acids in complex mixtures and challenging the conventional superiority of BCFAs.
支链脂肪酸(BCFAs)具有潜在的抗癌活性,但由于单体可及性问题,其与直链饱和脂肪酸(SSFAs)的系统评价和比较仍然有限。本研究利用富含BCFA/SSFA混合物的羊毛脂,采用多元线性回归(MLR)和正交偏最小二乘(OPLS)模型,结合HepG2细胞活力、凋亡和细胞周期测定,系统评估了50种脂肪酸的抗肝癌活性。MLR鉴定出iso-C13:0是一种独特的保护性脂肪酸,而ops具有很强的解释力(R2X = 0.827-0.997, R2Y = 0.675-0.782)和关键的抗肝癌脂肪酸,包括SSFAs (C12:0, C13:0, C14:0, C19:0, C21:0)和BCFAs(16-19碳的异-BCFAs, 14-19碳的前-BCFAs)。值得注意的是,SSFAs在某些活性上优于BCFAs,并且出现了结构-活性趋势:奇数碳BCFAs有利于细胞周期阻滞,偶数碳BCFAs促进细胞凋亡,13-21碳脂肪酸表现出更强的活性。该综合方法验证了羊毛脂作为功能性脂质筛选的理想基质,提供了一种在复杂混合物中识别抗癌脂肪酸的方法,挑战了BCFAs的传统优势。
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引用次数: 0
Cholesterol and related sterols differentially modulate lipid domain dynamics in model membranes: A dual-probe analysis of domain-specific effects 胆固醇和相关的固醇在模型膜中差异调节脂质结构域动力学:结构域特异性效应的双探针分析。
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-10-10 DOI: 10.1016/j.chemphyslip.2025.105550
Jesus Ayala-Sanmartin , Antonin Lamazière
The role of cholesterol in the organization and ordering of membrane domains has been well established over the past decades. However, the involvement of cholesterol precursors and byproduct sterols in modulating the physicochemical properties of cell membranes remains less thoroughly explored. In this study, we investigated the effects of cholesterol, two hydroxylated catabolites (24-hydroxycholesterol and 25-hydroxycholesterol), and two biosynthesis precursors (desmosterol and lanosterol) on model of liquid-ordered (Lo) and liquid-disordered (Ld) membrane domains. Membrane ordering and molecular mobility were assessed using two fluorescent probes; Laurdan, which senses polarity near the membrane aqueous interface and cholesterol-pyrene, which senses ordering closer to the center of the membrane bilayer. The results showed that Laurdan can distinguish between environmental polarity and the contribution of membrane domains. The probe mobility varied depending on the sterol and did not strictly correlate with membrane order. Cholesterol–pyrene revealed that the sterols induce varying degrees of ordering around the bilayer center. A notable observation in Ld membranes using different probes was that the ordering effect of sterols was similar near the lipid head groups and at the center of the bilayer. Hydroxycholesterols exhibited a low ordering effect, whereas cholesterol and desmosterol induced a strong effect. In contrast, in Lo membranes, hydroxycholesterols produced a strong ordering effect near the head groups but a reduced effect near the bilayer center.
在过去的几十年里,胆固醇在膜结构域的组织和排序中的作用已经得到了很好的证实。然而,胆固醇前体和副产物甾醇在调节细胞膜物理化学性质中的作用尚未得到充分探讨。在这项研究中,我们研究了胆固醇、两种羟基化分解产物(24-羟基胆固醇和25-羟基胆固醇)和两种生物合成前体(去氨甾醇和羊毛甾醇)对液体有序(Lo)和液体无序(Ld)膜结构域模型的影响。用两种荧光探针测定膜的有序性和分子迁移率;Laurdan在膜水界面附近感知极性,而胆固醇-芘在靠近膜双分子层中心的地方感知有序。结果表明,Laurdan能够区分环境极性和膜结构域的贡献。探针的迁移率随甾醇的变化而变化,与膜的顺序没有严格的相关性。胆固醇-芘表明,甾醇在双分子层中心周围诱导不同程度的有序。使用不同探针在Ld膜中观察到的一个值得注意的现象是,在脂质头基团附近和双分子层中心,甾醇的排序作用是相似的。羟基胆固醇表现出低排序效应,而胆固醇和去氨甾醇则表现出强排序效应。相反,在Lo膜中,羟基胆固醇在头基团附近产生强烈的排序效应,但在双层中心附近的作用减弱。
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引用次数: 0
Tucumã (Astrocaryum vulgare Mart.) oil-composed nanostructured lipid carriers for topical administration: Optimization by 22 experimental factorial design and stability assessment 外用给药的astrocaryvulgare M.油组成的纳米结构脂质载体:22因子设计优化和半固体配方的开发。
IF 2.8 3区 生物学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY Pub Date : 2025-09-30 DOI: 10.1016/j.chemphyslip.2025.105548
Maria Eugênia B. Rocha , Raquel da Ana , Faezeh Fathi , M. Beatriz P.P. Oliveira , Leticia Kakuda , Wanderley P. Oliveira , Eliana B. Souto
The selection of lipids and their ratios play a critical role in determining drug loading capacity and the structural properties of nanostructured lipid carriers (NLCs), directly impacting their stability. Among liquid lipids, vegetable oils have been explored both as active pharmaceutical ingredients (APIs) and as excipients in NLCs intended for topical use. The pulp oil of Tucumã, derived from Brazilian biodiversity, is known for its anti-inflammatory and antioxidant properties, attributed to its high content of carotenoids. This study focused on evaluating the compatibility of Tucumã oil with various solid lipids (SLs) commonly used in NLC production, developing an optimized NLC formulation containing this oil, and monitoring its stability over a 28-days’ period. Lipid screening was performed to assess the compatibility of Tucumã oil with a series of SLs, followed by preliminary formulations to determine the type of SL and surfactant for the experimental design. A 22 experimental factorial design was used to understand and identify the significant effects and interactions of lipid phase and surfactant concentrations on Tucumã oil-loaded NLCs, and the stability of the optimized formulation was monitored by determining the mean particle size (z-Ave), polydispersity index (PI), zeta potential (ZP), and recrystallization index (RI%) over 28 days. Compritol® was identified as the most suitable SL, resulting in round shaped NLCs with z-Ave of 309 nm, PI of 0.23 and high ZP (−25.5 mV). The RI% was shown to be influenced by the storage time and temperature. The optimal formulation contained 8 % of lipid phase (at a 20:80 ratio of oil to SL) and 3 % of Tween® 80 as surfactant, showing stability at 5ºC, 25ºC and 40ºC. The experimental factorial design revealed a positive effect of surfactant concentration on z-Ave and PI, with no significant impact on ZP. Over time, NLCs exhibited a gradual color loss (becoming whiter), with no other signs of instability. These findings support the potential use of Tucumã oil for producing stable NLCs suitable for topical delivery.
脂质及其比例的选择对纳米结构脂质载体(nlc)的载药能力和结构特性起着至关重要的作用,直接影响其稳定性。在液体脂类中,植物油已被探索作为活性药物成分(api)和外用nlc的赋形剂。Tucumã的果肉油来源于巴西的生物多样性,因其高含量的类黄酮和类胡萝卜素而具有抗炎和抗氧化特性。本研究的重点是评估Tucumã油与NLC生产中常用的各种固体脂类(SLs)的相容性,开发含该油的优化NLC配方,并监测其在28天内的稳定性。进行脂质筛选以评估SL的相容性,然后进行中试配方以确定SL和表面活性剂的类型和浓度范围,以进行实验设计。采用22因子设计来了解和确定脂质和表面活性剂浓度对Tucumã载油NLC的显著影响和相互作用,并通过测定平均粒径(z-Ave)、多分散性指数(PI)、ζ电位(ZP)和再结晶指数(RI%)来监测优化后配方的稳定性。Compritol®被确定为最合适的SL,形成圆形NLC, z-Ave为309nm, PI为0.23,ZP高(-25.5mV)。RI%受贮藏时间和温度的影响。最佳配方含有8%的总脂相(油与SL的比例为20:80)和3%的Tween®80作为表面活性剂,在5ºC, 25ºC和40ºC下具有稳定性。实验设计表明,表面活性剂浓度对z-Ave和PI有正影响,对ZP无显著影响。随着时间的推移,NLCs逐渐失去颜色(变白),没有其他不稳定的迹象。这些发现支持Tucumã油用于生产适合局部递送的稳定NLC的潜在用途。
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Chemistry and Physics of Lipids
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