Sulfosuccinimidyl oleate sodium is an irreversible CD36 inhibitor [1]. Sulfosuccinimidyl oleate sodium blocks the binding of long-chain fatty acids to CD36 by covalently modifying the lysine residues of the CD36 receptor, thereby inhibiting the entry of fatty acids into cells [2]. Sulfosuccinimidyl oleate sodium is often used to study the CD36-mediated fatty acid uptake process [3].
In Chinese hamster ovary (CHO) cells, Sulfosuccinimidyl oleate sodium (100μM; 30min) treatment of these cells was effective in inhibiting the CD36-specific effects [4]. In BV2 cells, Sulfosuccinimidyl oleate sodium (20μM, 50μM; 2h) significantly reduced the lipopolysaccharide/interferon-γ-induced production of nitric oxide, interleukin-6 and tumor necrosis factor-α [5]. In in ARPE-19 cells, Sulfosuccinimidyl oleate sodium (50μM; 24h) inhibits 7KC-induced oxidative stress and cell death [6].
In High-fat diet (HFD) mice model, Sulfosuccinimidyl oleate sodium (50mg/kg; po; 8 weeks) reduces intestinal fatty acid absorption by reducing the inhibition of intestinal CD36 expression, followed by decreased TG and FFA levels, which attenuates HFD-induced fatty live [7]. In a mouse oral squamous cell carcinoma (OSCC) model, tumor growth was significantly delayed in OSCC mice treated with Sulfosuccinimidyl oleate sodium (20mg/kg; ip; 11d) [8].
References:
[1]. Drahota Z, Vrbacký M, Nůsková H, et al. Succinimidyl oleate, established inhibitor of CD36/FAT translocase inhibits complex III of mitochondrial respiratory chain. Biochemical and biophysical research communications. 2010 Jan 15; 391(3): 1348-1351.
[2]. Zhao J, Rui H, Yang M, et al. CD36‐mediated lipid accumulation and activation of NLRP3 inflammasome lead to podocyte injury in obesity‐related glomerulopathy. Mediators of Inflammation, 2019, 2019(1): 3172647.
[3]. Coort SL, Willems J, Coumans WA, et al. Sulfo-N-succinimidyl esters of long chain fatty acids specifically inhibit fatty acid translocase (FAT/CD36)-mediated cellular fatty acid uptake. Molecular and cellular biochemistry. 2002 Oct; 239: 213-219.
[4]. Kuda O, Pietka TA, Demianova Z, et al. Sulfo-N-succinimidyl oleate (SSO) inhibits fatty acid uptake and signaling for intracellular calcium via binding CD36 lysine 164: SSO also inhibits oxidized low density lipoprotein uptake by macrophages. Journal of Biological Chemistry. 2013 May 31; 288(22): 15547-15555.
[5]. Dhungana H, Huuskonen MT, Jaronen M, et al. Sulfosuccinimidyl oleate sodium is neuroprotective and alleviates stroke-induced neuroinflammation. Journal of Neuroinflammation. 2017 Dec; 14: 1-3.
[6]. Nury T, Ghzaiel I, Hichami A, et al. Lipid droplets dependent or independent cytoprotective activities of unsaturated fatty acids, Lorenzo’s oil and sulfo-N-succinimidyl oleate on 7-ketocholesterol-induced oxidative stress, organelle dysfunction and cell death on 158N and ARPE-19 cells: Cell targets and benefits of sulfo-N-succinimidyl oleate. Current Research in Biotechnology. 2024 Jan 1; 7: 100195.
[7]. Ma Q, Wen L, Tian Y, et al. Sulfosuccinimidyl oleate ameliorates the high-fat diet-induced obesity syndrome by reducing intestinal and hepatic absorption. Frontiers in Pharmacology. 2023 May 26; 14: 1193006.
[8]. Takaichi M, Tachinami H, Takatsuka D, et al. Targeting CD36-mediated lipid metabolism by selective inhibitor-augmented antitumor immune responses in oral cancer. International Journal of Molecular Sciences. 2024 Aug 30; 25(17): 9438.
Sulfosuccinimidyl oleate sodium是一种不可逆的CD36抑制剂 [1]。Sulfosuccinimidyl oleate sodium通过共价修饰CD36受体的赖氨酸残基，阻断长链脂肪酸与CD36的结合，从而抑制脂肪酸进入细胞 [2]。Sulfosuccinimidyl oleate sodium常用于研究CD36介导的脂肪酸吸收过程 [3]。
在中国仓鼠卵巢（CHO）细胞中，Sulfosuccinimidyl oleate sodium（100μM；30min）处理这些细胞可有效抑制CD36特异性作用 [4]。在BV2细胞中，Sulfosuccinimidyl oleate sodium（20μM、50μM；2h）显著降低脂多糖/干扰素-γ诱导的一氧化氮、白细胞介素-6和肿瘤坏死因子-α的产生 [5]。在ARPE-19细胞中，Sulfosuccinimidyl oleate sodium（50μM；24h）可抑制7KC诱导的氧化应激和细胞死亡 [6]。
在高脂饮食（HFD）小鼠模型中，Sulfosuccinimidyl oleate sodium（50mg/kg；po；8周）通过降低肠道CD36表达的抑制来减少肠道脂肪酸的吸收，进而降低甘油三酸酯（TG）和游离脂肪酸（FFA）水平，从而减轻HFD诱导的脂肪肝 [7]。在小鼠口腔鳞状细胞癌（OSCC）模型中，用Sulfosuccinimidyl oleate sodium（20mg/kg；ip；11d）治疗的OSCC小鼠的肿瘤生长显著延缓 [8]。