Crocin
(Synonyms: 西红花苷; Crocin I) 目录号 : GC38423
Crocin是一种水溶性天然类胡萝卜素，来源于藏红花的柱头。
Cas No.:42553-65-1
Sample solution is provided at 25 µL, 10mM.
Crocin is a water-soluble natural carotenoid derived from the stigma of Crocus sativus [1]. Crocin significantly inhibits the phosphorylation activity of the JAK2/STAT3 and ERK signaling pathways, thereby blocking STAT3 transcriptional activity and reducing the expression of downstream pro-proliferation genes such as cyclin D1, VEGF, and CXCR4. It also upregulates the pro-apoptotic protein Bax and downregulates the anti-apoptotic protein Bcl-2, ultimately inducing cell cycle arrest (usually at the G0/G1 phase) and triggering mitochondria-dependent apoptotic pathways (caspase-9/caspase-3) [2-3]. Crocin is commonly used to treat various tumors, including colon, skin, thyroid, breast, and gastric cancers [4].
In A549 and SPC-A1 cells, Crocin (0-16mg/mL; 24-72h) inhibited the proliferation of cell in a concentration-dependent manner [5]. In HCT-116 cells, Crocin (0.25-3mg/mL; 48h) possesses significant anti-proliferation effects on human colorectal cancer cells [6]. In BV2 mouse microglial cells, Crocin (0-20μM; 30min) effectively inhibits LPS-induced nitric oxide (NO) release in cultured rat brain microglia [7].
In chronic mild stress (CMS) mice model, animals that received Crocin (4.84mg/kg, 9.69mg/kg, 19.38mg/kg; po; 21d) administration during the three CMS sessions had significantly shorter immobility times during the tail suspension test [8]. In dextran sodium sulfate (DSS)-induced UC mice model, Crocin (10mg/kg, 30mg/kg; ip; 3 weeks) prevents ulcerative colitis by inhibiting NF-κB-mediated inflammation [9].
References:
[1]. Zaghloul M S, Said E, Suddek G M, et al. Crocin attenuates lung inflammation and pulmonary vascular dysfunction in a rat model of bleomycin-induced pulmonary fibrosis[J]. Life sciences, 2019, 235: 116794.
[2]. Yang H, Zhang Y, Zhang D, et al. Crocin exerts anti-tumor effect in colon cancer cells via repressing the JaK pathway[J]. European Journal of Histochemistry: EJH, 2023, 67(3): 3697.
[3]. Boozari M, Hosseinzadeh H. Crocin molecular signaling pathways at a glance: A comprehensive review[J]. Phytotherapy Research, 2022, 36(10): 3859-3884.
[4]. Veisi A, Akbari G, Mard S A, et al. Role of crocin in several cancer cell lines: An updated review[J]. Iranian journal of basic medical sciences, 2020, 23(1): 3.
[5]. Chen S, Zhao S, Wang X, et al. Crocin inhibits cell proliferation and enhances cisplatin and pemetrexed chemosensitivity in lung cancer cells[J]. Translational lung cancer research, 2015, 4(6): 775.
[6]. Aung H H, Wang C Z, Ni M, et al. Crocin from Crocus sativus possesses significant anti-proliferation effects on human colorectal cancer cells[J]. Experimental oncology, 2007, 29(3): 175.
[7]. Nam K N, Park Y M, Jung H J, et al. Anti-inflammatory effects of crocin and crocetin in rat brain microglial cells[J]. European journal of pharmacology, 2010, 648(1-3): 110-116.
[8]. Alsanie W F, Alamri A S, Abdulaziz O, et al. Antidepressant effect of crocin in mice with chronic mild stress[J]. Molecules, 2022, 27(17): 5462.
[9]. Teng S, Hao J, Bi H, et al. The protection of crocin against ulcerative colitis and colorectal cancer via suppression of NF-κB-mediated inflammation[J]. Frontiers in Pharmacology, 2021, 12: 639458.
Crocin是一种水溶性天然类胡萝卜素，来源于藏红花的柱头 [1]。Crocin能显著抑制JAK2/STAT3和ERK信号通路的磷酸化活性，从而阻断STAT3的转录活性，并降低下游促增殖基因（如细胞周期蛋白D1、VEGF和CXCR4）的表达。它还能上调促凋亡蛋白Bax，下调抗凋亡蛋白Bcl-2，最终诱导细胞周期停滞（通常处于G0/G1期）并启动线粒体依赖性凋亡途径（caspase-9/caspase-3） [2-3]。Crocin常用于治疗多种肿瘤，包括结肠癌、皮肤癌、甲状腺癌、乳腺癌和胃癌 [4]。
在A549和SPC-A1细胞中，Crocin（0-16mg/mL；24-72h）以浓度依赖性方式抑制细胞增殖 [5]。在HCT-116细胞中，Crocin（0.25-3mg/mL；48h）对人结肠直肠癌细胞具有显著的抗增殖作用 [6]。在BV2小鼠小胶质细胞中，Crocin（0-20μM；30min）有效抑制LPS诱导的培养大鼠脑小胶质细胞一氧化氮（NO）释放 [7]。
在慢性轻度应激（CMS）小鼠模型中，在三个CMS周期中分别给予Crocin（4.84mg/kg，9.69mg/kg，19.38mg/kg；po；21d）的小鼠在尾部悬吊实验中的静止时间显著缩短 [8]。在葡聚糖硫酸钠（DSS）诱发的UC小鼠模型中，Crocin（10mg/kg，30mg/kg；ip；3周）通过抑制NF-κB介导的炎症来预防溃疡性结肠炎 [9]。
| Cell experiment [1]: | |
Cell lines | A549 and SPC-A1 cells |
Preparation Method | A549 and SPC-A1 cells were seeded in 96-well plates at a density of 5×104 cells/mL in 100µL medium. Twenty-four hours later, the culture medium was changed to fresh medium with different concentrations of crocin (0, 1, 2, 4, 8 and 16mg/mL). The cells were synchronized by starvation in serum-free medium before treatment with crocin. Each concentration of crocin was added into 5 wells. After 24, 48, and 72h, 20µL MTT (5mg/mL) was added into each well and then incubated for an additional 4h at 37℃. Following removal of the supernatant, 100µL crystalline in dimethyl sulfoxide was added to each well. Absorbance (OD) at 570nm was measured in a microplate reader. |
Reaction Conditions | 0-16mg/mL; 24-72h |
Applications | Crocin inhibited the proliferation of A549 and SPC-A1 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Chronic mild stress (CMS) mice model |
Preparation Method | All the mice utilized in the study were split into ten groups with eight mice in each group. Carboxy methyl cellulose (CMC) was given to group I as a vehicle, while groups II, III, and IV received doses of Crocin of 4.84mg/kg (low dosage of Crocin—LC), 9.69mg/kg (medium dose of Crocin—MC), and 19.38mg/kg (high dose of Crocin—HC), respectively. The group V animals received imipramine (15mg/kg). For three weeks, all treatments were administered orally 30min prior to the onset of stress (chronic mild stress—CMS) (21 days). On the 21st day, the mice’s locomotor activity was assessed after being exposed to stress for 60min. On the 22nd day, a tail suspension test (TST) was performed on the mice. |
Dosage form | 4.84mg/kg, 9.69mg/kg, 19.38mg/kg; po; 21d |
Applications | Animals that received Crocin administration during the three CMS sessions had significantly shorter immobility times during the TST. |
References: | |
| Cas No. | 42553-65-1 | SDF | |
| 别名 | 西红花苷; Crocin I | ||
| Canonical SMILES | O[C@@H]([C@H](O)[C@H]1O)[C@H](O[C@H]1OC(/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(C)/C(O[C@@H]([C@@H]([C@@H](O)[C@@H]2O)O)O[C@@H]2CO[C@@H]([C@@H]([C@@H](O)[C@@H]3O)O)O[C@@H]3CO)=O)=O)CO[C@@H]([C@@H]([C@@H](O)[C@@H]4O)O)O[C@@H]4CO | ||
| 分子式 | C44H64O24 | 分子量 | 976.96 |
| 溶解度 | DMSO : 125 mg/mL (127.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0236 mL | 5.1179 mL | 10.2358 mL |
| 5 mM | 0.2047 mL | 1.0236 mL | 2.0472 mL |
| 10 mM | 0.1024 mL | 0.5118 mL | 1.0236 mL |
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