Department of Industrial Pharmacy, Daiichi University of Pharmacy, 22-1 Tamagawa-cho, Minami-ku, Fukuoka 815-8511, Japan.
Department of Pharmacology, University of Texas Health Science Center, San Antonio, TX 78229-3900, USA.
Langmuir. 2024 Mar 26;40(12):6484-6492. doi: 10.1021/acs.langmuir.4c00053. Epub 2024 Mar 12.
Interactions between the sigma receptor agonist PRE-084 and various lipid monolayers, including dipalmitoylphosphatidylcholine (DPPC), DPP-ethanolamine (DPPE), DPP-glycerol (DPPG), DPP-serine (DPPS), palmitoylsphingomyelin (PSM), and cholesterol (Ch), were investigated to elucidate the effects of PRE-084 on membrane fluidity and stability. Their interactions with sigma receptor agonists have potential implications for neuroprotection, antidepressant, analgesic, and cognitive enhancement effects. In this study, we observed that the presence of PRE-084 in the subphase led to increased fluidity in DPPC and DPPE monolayers, whereas decreasing fluidity was observed in DPPG, DPPS, and PSM monolayers. The interaction of PRE-084 with Ch monolayers was found to be distinct from its interaction with other lipids. Fluorescence microscopy images revealed changes in the size and shape of liquid-condensed domains in the presence of PRE-084, supporting the notion of altered membrane fluidity. Our findings provide new insights into the interaction of PRE-084 with lipid monolayers and its potential implications for biological and membrane science.
研究了西格玛受体激动剂 PRE-084 与各种脂质单层(包括二棕榈酰磷脂酰胆碱(DPPC)、二棕榈酰乙醇胺(DPPE)、二棕榈酰甘油(DPPG)、二棕榈酰丝氨酸(DPPS)、棕榈酰鞘氨醇(PSM)和胆固醇(Ch))之间的相互作用,以阐明 PRE-084 对膜流动性和稳定性的影响。它们与西格玛受体激动剂的相互作用可能对神经保护、抗抑郁、镇痛和认知增强作用具有潜在意义。在这项研究中,我们观察到亚相中存在 PRE-084 会导致 DPPC 和 DPPE 单层的流动性增加,而 DPPG、DPPS 和 PSM 单层的流动性则降低。PRE-084 与 Ch 单层的相互作用与与其他脂质的相互作用不同。荧光显微镜图像显示,在 PRE-084 的存在下,液-固凝聚域的大小和形状发生了变化,这支持了膜流动性改变的观点。我们的发现为 PRE-084 与脂质单层的相互作用及其对生物和膜科学的潜在意义提供了新的见解。