Crocetin
(Synonyms: 西红花酸单甲酯; β-Crocetin) 目录号 : GC35749
Crocetin (β-Crocetin) 是从 Crocus sativus 中分离得到的，拥有抗炎、神经保护和抗氧化作用。
Cas No.:25368-09-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Crocetin (β-Crocetin), isolated from Crocus sativus, possesses anti-inflammatory, neuroprotective and antioxidant activity[1][2].
[1]. Tseng TH, et al. Crocetin protects against oxidative damage in rat primary hepatocytes. Cancer Lett. 1995 Oct 20;97(1):61-7. [2]. Ahmad AS, et al. Neuroprotection by crocetin in a hemi-parkinsonian rat model. Pharmacol Biochem Behav. 2005 Aug;81(4):805-13. [3]. Nam KN, et al. Anti-inflammatory effects of crocin and crocetin in rat brain microglial cells. Eur J Pharmacol. 2010 Dec 1;648(1-3):110-6.
| Cas No. | 25368-09-6 | SDF | |
| 别名 | 西红花酸单甲酯; β-Crocetin | ||
| Canonical SMILES | OC(/C(C)=C/C=C/C(C)=C/C=C/C=C(C)/C=C/C=C(C)/C(OC)=O)=O | ||
| 分子式 | C21H26O4 | 分子量 | 342.43 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C, sealed storage, away from moisture and 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 | 2.9203 mL | 14.6015 mL | 29.203 mL |
| 5 mM | 0.5841 mL | 2.9203 mL | 5.8406 mL |
| 10 mM | 0.292 mL | 1.4602 mL | 2.9203 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Crocetin: A Systematic Review
Front Pharmacol 2022 Jan 14;12:745683.PMID:35095483DOI:10.3389/fphar.2021.745683.
Crocetin is an aglycone of crocin naturally occurring in saffron and produced in biological systems by hydrolysis of crocin as a bioactive metabolite. It is known to exist in several medicinal plants, the desiccative ripe fruit of the cape jasmine belonging to the Rubiaceae family, and stigmas of the saffron plant of the Iridaceae family. According to modern pharmacological investigations, Crocetin possesses cardioprotective, hepatoprotective, neuroprotective, antidepressant, antiviral, anticancer, atherosclerotic, antidiabetic, and memory-enhancing properties. Although poor bioavailability hinders therapeutic applications, derivatization and formulation preparation technologies have broadened the application prospects for Crocetin. To promote the research and development of Crocetin, we summarized the distribution, preparation and production, total synthesis and derivatization technology, pharmacological activity, pharmacokinetics, drug safety, drug formulations, and preparation of Crocetin.
Crocetin promotes clearance of amyloid-β by inducing autophagy via the STK11/LKB1-mediated AMPK pathway
Autophagy 2021 Nov;17(11):3813-3832.PMID:33404280DOI:10.1080/15548627.2021.1872187.
Alzheimer disease (AD) is usually accompanied by two prominent pathological features, cerebral accumulation of amyloid-β (Aβ) plaques and presence of MAPT/tau neurofibrillary tangles. Dysregulated clearance of Aβ largely contributes to its accumulation and plaque formation in the brain. Macroautophagy/autophagy is a lysosomal degradative process, which plays an important role in the clearance of Aβ. Failure of autophagic clearance of Aβ is currently acknowledged as a contributing factor to increased accumulation of Aβ in AD brains. In this study, we have identified Crocetin, a pharmacologically active constituent from the flower stigmas of Crocus sativus, as a potential inducer of autophagy in AD. In the cellular model, Crocetin induced autophagy in N9 microglial and primary neuron cells through STK11/LKB1 (serine/threonine kinase 11)-mediated AMP-activated protein kinase (AMPK) pathway activation. Autophagy induction by Crocetin significantly increased Aβ clearance in N9 cells. Moreover, Crocetin crossed the blood-brain barrier and induced autophagy in the brains' hippocampi of wild-type male C57BL/6 mice. Further studies in transgenic male 5XFAD mice, as a model of AD, revealed that one-month treatment with Crocetin significantly reduced Aβ levels and neuroinflammation in the mice brains and improved memory function by inducing autophagy that was mediated by AMPK pathway activation. Our findings support further development of Crocetin as a pharmacological inducer of autophagy to prevent, slow down progression, and/or treat AD.Abbreviations: Aβ: amyloid-β; ABCB1/P-gp/P-glycoprotein: ATP-binding cassette, subfamily B (MDR/TAP), member 1; AD: Alzheimer disease; AMPK/PRKAA: AMP-activated protein kinase; APP: amyloid beta (A4) precursor protein; ATG: autophagy related; BBB: blood-brain barrier; BECN1: beclin 1, autophagy related; CAMKK2/CaMKKβ: calcium/calmodulin-dependent protein kinase kinase 2, beta; CSE: Crocus sativus extract; CTSB: cathepsin B; EIF4EBP1: eukaryotic translation initiation factor 4E binding protein 1; GFAP: glial fibrillary acidic protein; GSK3B/GSK3β: glycogen synthase kinase 3 beta; Kp: brain partition coefficient; LRP1: low density lipoprotein receptor-related protein 1; MAP1LC3B/LC3B: microtubule-associated protein 1 light chain 3 beta; MAP2: microtubule-associated protein 2; MAPK/ERK: mitogen-activated protein kinase; MAPT/tau: microtubule-associated protein tau; MTT: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; MTOR: mechanistic target of rapamycin kinase; MWM: Morris water maze; NFKB/NF-κB: nuclear factor of kappa light polypeptide gene enhancer in B cells; NMDA: N-methyl-d-aspartic acid; RPTOR: regulatory associated protein of MTOR; RPS6KB1/p70S6K: ribosomal protein S6 kinase 1; SQSTM1: sequestosome 1; SRB: sulforhodamine B; STK11/LKB1: serine/threonine kinase 11; TFEB: transcription factor EB; TSC2: TSC complex subunit 2; ULK1: unc-51 like kinase 1.
Crocetin and Crocin from Saffron in Cancer Chemotherapy and Chemoprevention
Anticancer Agents Med Chem 2019;19(1):38-47.PMID:30599111DOI:10.2174/1871520619666181231112453.
Introduction: Cancer is a disorder which has a powerful impact on the quality life and life expectancy despite the increase in drugs and treatments available for cancer patients. Moreover, many new therapeutic options are known to have adverse reactions without any improvement in outcome than before. Nowadays, natural products or plant derivatives are used as chemoprevention drugs and chemotherapy is the new approach that uses specific cell premalignant transformation in the malignant form. Natural substances derived from plants, such as polyphenols, flavonoids, carotenoids, alkaloids and others, can be biologically active and have a wide spectrum of effects. The protective effects of Saffron carotenoids (crocin and Crocetin) have been extensively studied mainly for their antioxidant properties, however, they have various other biological activities including tumor growth inhibition with the induction of cell death. Methods: The relevant information on Saffron and its carotenoids was collected from scientific databases (such as PubMed, Web of Science, Science Direct). To identify all published articles in relation to saffron, crocin and Crocetin, in different types of cancer, no language restriction has been used. Results: To date, crossing the words saffron and cancer, approximately 150 articles can be found. If crossing is made between crocin and cancer, approximately 60 articles can be found. With the crossing between Crocetin and cancer, the number is approximately 55, while between carotenoids and cancer, the number exceeds 16.000 reports. In all the papers published to date, there are evidences that saffron and its carotenoids exert chemopreventive activity through anti-oxidant activity, cancer cells apoptosis, inhibition of cell proliferation, enhancement of cell differentiation, modulation of cell cycle progression and cell growth, modulation of tumor metabolism, stimulation of cell-to-cell communication and immune modulation. Conclusion: Here, we have tried to offer an up-to-date overview of pre-clinical experimental investigations on the potential use of the main carotenoids of saffron in tumor models and focus the attention on the molecular mechanisms involved.
Crocetin Prolongs Recovery Period of DSS-Induced Colitis via Altering Intestinal Microbiome and Increasing Intestinal Permeability
Int J Mol Sci 2022 Mar 30;23(7):3832.PMID:35409192DOI:10.3390/ijms23073832.
Crocetin is one of the major active constituents of saffron (Crocus sativus L.) which has a reputation for facilitating blood circulation and dispersing blood stasis in traditional Chinese medicine. However, there is little evidence showing the relationship between Crocetin intake and the risk of gastrointestinal diseases such as colitis. In order to investigate the effect of Crocetin on the regulation of intestinal barrier function and intestinal microbiota composition, mice were treated with Crocetin after 3% dextran sulfate sodium (DSS) administration for one week. We found that Crocetin intake at 10 mg/kg aggravated colitis in mice, showing increased weight loss and more serious histological abnormalities compared with the DSS group. The 16s rDNA sequencing analysis of the feces samples showed that mice treated with 10 mg/kg Crocetin had lower species diversity and richness than those treated with DSS. At the genus level, a higher abundance of Akkermansia and Mediterraneibacter, and a lower abundance of Muribaculaceae, Dubosiella, Paramuribaculum, Parasutterella, Allobaculum, Duncaniella, Candidatus Stoquefichus, and Coriobacteriaceae UCG-002 were observed in the Crocetin group. Untargeted metabolomic analyses revealed that Crocetin reduced the levels of primary and secondary bile acids such as 12-ketodeoxycholic acid, 7-ketodeoxycholic acid, 3-sulfodeoxycholic acid, 6-ethylchenodeoxycholic acid, chenodeoxycholate, glycochenodeoxycholate-7-sulfate, glycocholate, and sulfolithocholic acid in the colon. In conclusion, Crocetin intake disturbed intestinal homeostasis and prolonged recovery of colitis by promoting inflammation and altering gut microbiota composition and its metabolic products in mice. Our findings suggest that patients with gastrointestinal diseases such as inflammatory bowel disease should use Crocetin with caution.
Crocetin ameliorates chronic restraint stress-induced depression-like behaviors in mice by regulating MEK/ERK pathways and gut microbiota
J Ethnopharmacol 2021 Mar 25;268:113608.PMID:33242618DOI:10.1016/j.jep.2020.113608.
Ethnopharmacological relevance: This study aimed at determining the effects of saffron on depression as well as its neuroprotective and pharmacological effects on the intestinal function of Crocetin in mice exposed to chronic restraint stress. Materials and methods: Chronic stress was induced in two-week-old ICR mice by immobilizing them for 6 h per day for 28 days. The mice were orally administered with Crocetin (20, 40, 80 mg/kg), fluoxetine (20 mg/kg) or distilled water. The treatments were administered daily and open field and tail suspension tests were performed. Immunofluorescent and Western-bolt (WB) assays were conducted to determine the expression of mitogen-activated protein kinase phosphatase-1 (MKP-1), the precursor of brain-derived neurotrophic factor (proBDNF), extracellular signal-regulated kinase 1/2 (ERK1/2), phosphorylated cAMP response element-binding (CREB) protein in the hippocampus. Serum levels of dopamine (DA), proBDNF, MKP-1 and CREB were measured by Elisa kits. High-throughput sequencing was carried out to analyze the composition of intestinal microbiota. Results: Crocetin ameliorated depressive-like behaviors caused by chronic restraint stress-induced depressive mice. It significantly attenuated the elevated levels of MKP-1, proBDNF, alanine transaminase, aspartate transaminase and increased the serum levels of DA as well as CREB. Histopathological analysis showed that Crocetin suppressed hippocampus injury in restraint stress mice by protecting neuronal cells. Immunofluorescent and WB analysis showed elevated expression levels of ERK1/2, CREB and inhibited expression levels of MKP-1, proBDNF in the hippocampus. The intestinal ecosystem of the Crocetin group partially recovered and was close to the control group. Conclusions: Crocetin has neuroprotective properties and ameliorates the effects of stress-associated brain damage by regulating the MKP-1-ERK1/2-CREB signaling and intestinal ecosystem.