稀有鳄鱼毒素通过调节脂质积累和凝血因子改善斑马鱼幼体的血栓形成。

IF 2.5 3区 医学 Q3 CHEMISTRY, MEDICINAL Fitoterapia Pub Date : 2024-10-28 DOI:10.1016/j.fitote.2024.106278
Guo Xu , Penghong Xu , Nan Wang , Weimin Qi , Yuxuan Pu , Nannan Kang , Jianlin Chu , Bingfang He
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摘要

类胡萝卜素-4 是一种水溶性类胡萝卜素,具有抗炎和抗氧化作用,对心血管有保护作用。然而,其类似物黄花素-1 和黄花素-2'的药效学效应和机制尚未见报道。在这项研究中,我们评估了稀有鳄鱼毒素对心血管系统的保护作用。在氧化-LDL诱导的HUVECs模型中,0.02、0.1、0.5、1、2、3、4、5、6 μg/mL的crocin-1和crocin-2'可提高细胞活力达80%。同时,浓度在 25-100 μg/mL 的稀有鳄鱼毒素可使胆固醇诱导的斑马鱼幼体的脂质积累减少 30%。此外,研究人员还探讨了稀有黄腐素对血栓形成的治疗潜力。在体外实验中,浓度为 0.02、0.05、0.2、0.5、1、2、5、10 μg/mL 的稀有鳄鱼素-1 和鳄鱼素-2'可保护人脐静脉内皮细胞(HUVECs)免受脂多糖诱导的氧化应激和炎症的影响。体内研究表明,25、50、100、150、200 和 300 μg/mL 浓度的稀有鳄鱼素对花生四烯酸(AA)诱导的斑马鱼具有显著的抗血栓作用,300 μg/mL 剂量几乎不存在导致斑马鱼畸形的潜在风险。简而言之,稀有鳄鱼毒素具有抗炎、抗氧化和抗凝血的特性,因此被视为治疗心血管疾病的潜在有效候选药物。
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Rare crocins ameliorate thrombus in zebrafish larvae by regulating lipid accumulation and clotting factors
Crocin-4 is a water-soluble carotenoid that exhibits cardiovascular protection effects through anti-inflammatory and antioxidant effects. However, the pharmacodynamic effects and mechanisms of its analogues crocin-1 and crocin-2′ have not been reported. In this study, we evaluated the protective effects of rare crocins on cardiovascular systems. In ox-LDL induced HUVECs model, 0.02, 0.1, 0.5, 1, 2, 3, 4, 5, 6 μg/mL crocin-1 and crocin-2′ can increase cell viability by up to 80 %. Meanwhile, rare crocins at concentrations between 25–100 μg/mL crocin-1 and crocin-2′ reduced the lipid accumulation by 30 % in cholesterol-induced zebrafish larvae. What's more, the therapeutic potential of rare crocins on thrombosis has also been explored. In vitro experiments, rare crocin-1 and crocin-2′ at concentrations of 0.02, 0.05, 0.2, 0.5, 1, 2, 5, 10 μg/mL protected Human Umbilical Vein Endothelial Cells (HUVECs) against lipopolysaccharides-induced oxidative stress and inflammation. In vivo studies revealed that rare crocins at concentrations of 25, 50, 100, 150, 200, and 300 μg/mL exerted significant antithrombotic effect on arachidonic acid (AA)-induced zebrafish and there was nearly no potential risk for the deformity of zebrafish at 300 μg/mL dosages. In brief, rare crocins was viewed as a potentially useful candidate for the treatment of cardiovascular diseases because of its anti-inflammatory, antioxidant, and anticoagulant properties.
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来源期刊
Fitoterapia
Fitoterapia 医学-药学
CiteScore
5.80
自引率
2.90%
发文量
198
审稿时长
1.5 months
期刊介绍: Fitoterapia is a Journal dedicated to medicinal plants and to bioactive natural products of plant origin. It publishes original contributions in seven major areas: 1. Characterization of active ingredients of medicinal plants 2. Development of standardization method for bioactive plant extracts and natural products 3. Identification of bioactivity in plant extracts 4. Identification of targets and mechanism of activity of plant extracts 5. Production and genomic characterization of medicinal plants biomass 6. Chemistry and biochemistry of bioactive natural products of plant origin 7. Critical reviews of the historical, clinical and legal status of medicinal plants, and accounts on topical issues.
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