PHYSALIEN是一种脂溶性的类胡萝卜素类化合物。
Cas No.:144-67-2
Sample solution is provided at 25 µL, 10mM.
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PHYSALIEN is a lipophilic carotenoid compound[1-2]. PHYSALIEN exhibits antioxidant and anti-inflammatory properties, which contribute to its hepatoprotective effects by mitigating oxidative stress and alleviating hepatic fibrosis. PHYSALIEN is utilized in research related to liver diseases and ocular disorders[3-4].
In vitro, BRL-3A rat normal hepatocytes were pretreated with PHYSALIEN (1µM) for 2 hours before co-incubation with ethanol for 24 hours. The treatment restored the ethanol-suppressed expression of key autophagy-related proteins (Atg5, Beclin-1, and LC3A/B) and reduced the accumulation of the autophagy substrate p62. The pretreatment with PHYSALIEN targeted the cell membrane receptors P2X7 and AdipoR1, thereby modulating the AMPK/FoxO3a and PI3K/Akt signaling pathways, which restored ethanol-inhibited mitophagy and attenuated the activation of the NLRP3 inflammasome[5].
In vivo, in a murine model of alcoholic fatty liver disease (AFLD) using male C57BL/6 mice, oral administration of PHYSALIEN (25mg/kg/day) from weeks 5 to 10 of the experiment. PHYSALIEN significantly alleviated typical AFLD symptoms induced by ethanol consumption. This included amelioration of liver histopathology (reduced lipid droplet deposition and inflammatory foci), lowered serum alanine aminotransferase (ALT) levels, and mitigation of hepatic oxidative stress and inflammation. The hepatoprotective effect was mediated through the regulation of the CYP2E1, NF-κB, and MAPK (p38 and ERK) signaling pathways[6]. In N-methyl-N-nitrosourea (MNU)-induced photoreceptor degeneration in adult male C57BL/6J mice, daily oral administration of PHYSALIEN (approximately 0.27mg/kg), starting one week before injury and continuing for a total of two weeks. PHYSALIEN significantly improved photoreceptor survival, enhanced retinal electrophysiological responses to light, and increased visual acuity in the injured mice[7].
References:
[1] Long JT, Fan HX, Zhou ZQ, et al. The major zeaxanthin dipalmitate derivatives from wolfberry. J Asian Nat Prod Res. 2020 Aug;22(8):746-753.
[2] Liu F, Liu X, Zhou Y, et al. Wolfberry-derived zeaxanthin dipalmitate delays retinal degeneration in a mouse model of retinitis pigmentosa through modulating STAT3, CCL2 and MAPK pathways. J Neurochem. 2021 Sep;158(5):1131-1150.
[3] Kan X, Zhou W, Xu W, et al. Zeaxanthin Dipalmitate-Enriched Emulsion Stabilized with Whey Protein Isolate-Gum Arabic Maillard Conjugate Improves Gut Microbiota and Inflammation of Colitis Mice. Foods. 2022 Nov 16;11(22):3670.
[4] Bahaji Azami NL, Sun M. Zeaxanthin Dipalmitate in the Treatment of Liver Disease. Evid Based Complement Alternat Med. 2019 Aug 21;2019:1475163.
[5] Gao H, Lv Y, Liu Y, et al. Wolfberry-Derived Zeaxanthin Dipalmitate Attenuates Ethanol-Induced Hepatic Damage. Mol Nutr Food Res. 2019 Jun;63(11):e1801339.
[6] Xiao J, Wang J, Xing F, et al. Zeaxanthin dipalmitate therapeutically improves hepatic functions in an alcoholic fatty liver disease model through modulating MAPK pathway. PLoS One. 2014 Apr 16;9(4):e95214.
[7] Chen X, Zhang S, Yang L, et al. Zeaxanthin dipalmitate-enriched wolfberry extract improves vision in a mouse model of photoreceptor degeneration. PLoS One. 2024 May 20;19(5):e0302742.
PHYSALIEN是一种脂溶性的类胡萝卜素类化合物[1-2]。PHYSALIEN可通过抗氧化和抗炎作用来保护肝脏细胞，同时通过减少氧化应激损伤以缓解肝纤维化。PHYSALIEN可用于肝脏疾病和眼部疾病的相关研究[3-4]。
在体外，PHYSALIEN（1μM）预处理大鼠正常肝细胞（BRL-3A）2小时后，再与乙醇共孵育24小鼠，PHYSALIEN能够恢复乙醇抑制的自噬蛋白（Atg5、Beclin-1、LC3A/B）的表达，并下调自噬底物p62的积累。PHYSALIEN预处理还通过靶向细胞膜受体P2X7和AdipoR1，进而调控AMPK/FoxO3a和PI3K/Akt信号通路，恢复被乙醇抑制的线粒体自噬功能，并减轻NLRP3炎性小体的激活[5]。
在体内，在雄性C57BL/6小鼠的酒精性脂肪肝病（AFLD）模型中，从实验第5周至第10周口服给予PHYSALIEN（25mg/kg/day），PHYSALIEN显著缓解了由乙醇摄入引起的典型AFLD症状，包括改善肝脏组织病理学（减少脂肪滴沉积和炎症灶），降低血清谷丙转氨酶（ALT）水平，减轻肝脏氧化应激和炎症反应，并通过调节CYP2E1、NF-κB和MAPK（p38和ERK）信号通路发挥肝保护作用[6]。在成年雄性C57BL/6J小鼠的N-甲基-N-亚硝基脲（MNU）诱导的光感受器变性模型中，从损伤前一周开始直至实验结束（共两周）每日灌胃给予PHYSALIEN（约0.27mg/kg），PHYSALIEN显著改善了光感受器的存活率，增强了视网膜对光的电生理反应，并提高了受损小鼠的视觉敏锐度[7]。
| Cell experiment [1]: | |
Cell lines | Rat normal hepatocyte BRL-3A cell line |
Preparation Method | BRL-3A cells were cultured in DMEM with 10%(v/v) fetal bovine serum at 37°C with 5% CO₂. Cells were pretreated with PHYSALIEN (1μM) for 2 hours prior to the addition of 250mM ethanol for 24 hours. |
Reaction Conditions | 1μM; 2-hour pretreatment. |
Applications | PHYSALIEN significantly counteracted ethanol-induced downregulation of key autophagy proteins (Atg5, beclin-1, LC3A/B) and upregulation of the autophagy substrate p62 in BRL-3A cells. PHYSALIEN also partially reversed ethanol-suppressed mitophagy, as evidenced by restored mitochondrial morphology (reduced swelling and disrupted cristae) and an increased percentage of intact mitochondria. Furthermore, PHYSALIEN attenuated ethanol-evoked NLRP3 inflammasome activation, reducing the expression levels of cleaved caspase-1 and secretion of IL-1β and IL-18. |
| Animal experiment [2]: | |
Animal models | Female Sprague-Dawley rats (Alcoholic fatty liver disease model) |
Preparation Method | Rats were intragastrically administered ethanol (4.0g/kg) for 10 weeks. PHYSALIEN was orally administered (25mg/kg/day) from the 5th week to the 10th week. Rats were sacrificed 8 hours after the last administration. |
Dosage form | 25mg/kg/day; Oral gavage; Daily administration for 5 weeks. |
Applications | PHYSALIEN treatment significantly alleviated alcoholic fatty liver disease (AFLD) symptoms, including reduced body weight loss, hepatic fat droplet deposition, and inflammatory cell infiltration. PHYSALIEN improved liver function by lowering serum ALT levels and triglycerides (TG). PHYSALIEN also attenuated hepatic oxidative stress (reducing CYP2E1 expression, MDA, and 8-isoprostane; restoring CAT and SOD1), diminished inflammation (reducing TNF-α, IL-1β, IL-6, MCP-1), and reduced hepatic apoptosis. |
References: | |
| Cas No. | 144-67-2 | SDF | |
| 别名 | 玉米黄素棕榈酸双酯; 玉米黄素二棕榈酸酯 | ||
| 分子式 | C72H116O4 | 分子量 | 1045.69 |
| 溶解度 | Ethanol : 1 mg/mL (0.96 mM; Need ultrasonic and warming) | 储存条件 | Store at -20°C,protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 956.3 μL | 4.7815 mL | 9.5631 mL |
| 5 mM | 191.3 μL | 956.3 μL | 1.9126 mL |
| 10 mM | 95.6 μL | 478.2 μL | 956.3 μL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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