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Chrysoeriol Sale

(Synonyms: 金圣草(黄)素) 目录号 : GC60109

A flavonoid with diverse biological activities

Chrysoeriol Chemical Structure

Cas No.:491-71-4

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1mg
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产品描述

Chrysoeriol is a flavonoid that has been found in Capsicum and has diverse biological activities.1,2,3,4 It is active against the Gram-positive bacteria E. faecalis, B. subtilis, and S. aureus (MICs = 1, 1, and 0.25 ?g/ml, respectively) and the Gram-negative bacteria P. aeruginosa, K. pneumoniae, and E. coli (MICs = 0.12, 0.25, and 0.06 ?g/ml, respectively).1 Chrysoeriol (7.5, 15, and 30 ?M) induces cell cycle arrest at the G1 phase and autophagy in A549 lung cancer cells.2 It reduces LPS-induced production of IL-6, IL-1β, and TNF-α in RAW 264.7 cells when used at a concentration of 20 ?M.3 Chrysoeriol (20 mg/kg) reduces plasma glucose, total cholesterol, free fatty acid, and phospholipid levels in a rat model of diabetes induced by streptozotocin .4

1.Nascimento, P.L.A., Nascimento, T.C.E.S., Ramos, N.S.M., et al.Quantification, antioxidant and antimicrobial activity of phenolics isolated from different extracts of Capsicum frutescens (pimenta malagueta)Molecules19(4)5434-5447(2014) 2.Wei, W., He, J., Ruan, H., et al.In vitro and in vivo cytotoxic effects of chrysoeriol in human lung carcinoma are facilitated through activation of autophagy, sub-G1/G0 cell cycle arrest, cell migration and invasion inhibition and modulation of MAPK/ERK signalling pathwayJ. BUON24(3)936-942(2019) 3.Wu, J.-Y., Chen, Y.-J., Bai, L., et al.Chrysoeriol ameliorates TPA-induced acute skin inflammation in mice and inhibits NF-κB and STAT3 pathwaysPhytomedicine68153173(2020) 4.Baskaran, K., Pugalendi, K.V., and Saravanan, R.Antidiabetic and antihyperlipidemic activity of chrysoeriol in diabetic rats, role of HMG CoA reductase, LCAT and LPL: In vivo and in silico approachesJ. Pharm. Res.9(9)597-605(2015)

Chemical Properties

Cas No. 491-71-4 SDF
别名 金圣草(黄)素
Canonical SMILES O=C1C=C(C2=CC=C(O)C(OC)=C2)OC3=CC(O)=CC(O)=C13
分子式 C16H12O6 分子量 300.26
溶解度 DMSO : 100 mg/mL (333.04 mM; Need ultrasonic) 储存条件
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1 mM 3.3304 mL 16.6522 mL 33.3045 mL
5 mM 0.6661 mL 3.3304 mL 6.6609 mL
10 mM 0.333 mL 1.6652 mL 3.3304 mL
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Research Update

Health Benefits and Pharmacological Aspects of Chrysoeriol

Pharmaceuticals (Basel) 2022 Aug 7;15(8):973.PMID:36015121DOI:10.3390/ph15080973.

A flavone, Chrysoeriol is synthetized in several plant species. It comes from several natural sources, especially medicinal plants. The identification and isolation of this compound has been carried out and verified by several research teams using different spectral methods. It seems that the concentration of this molecule is variable and fluctuating depending on the source, the part extracted, the region, and the methods of extraction and characterization. The aim of this paper is to highlight the in vitro and in vivo pharmacological properties of Chrysoeriol and to provide insight into its pharmacokinetics. Anticancer, anti-inflammatory, antibacterial, antifungal, anti-osteoporosis, anti-insecticide, and neuroprotective actions have been shown in a number of studies on this chemical. Different mechanisms in theses pharmacological effects include subcellular, cellular, and molecular targets. In vivo pharmacokinetic analysis has proved the good stability of this molecule, showing its promising potential to prevent or treat diseases including cancer, diabetes, inflammation, osteoporosis, Parkinson's disease, and cardiovascular diseases.

Effects of Chrysoeriol on Adipogenesis and Lipolysis in 3T3-L1 Adipocytes

Foods 2022 Dec 30;12(1):172.PMID:36613388DOI:10.3390/foods12010172.

We examined the effect of Chrysoeriol on adipogenesis and lipolysis and elucidated the underlying molecular mechanisms. Chrysoeriol inhibited fat deposition in adipocytes. Treatment with Chrysoeriol suppressed the expression of peroxisome proliferator-activated receptor γ, fatty acid synthase, fatty acid-binding protein, CCAAT/enhancer-binding proteins (C/EBP) α, C/EBPβ, and sterol regulatory element-binding protein-1. In addition, Chrysoeriol significantly elevated the activation of 5'-adenosine monophosphate-activated protein kinase. Moreover, Chrysoeriol increased free glycerol and fatty acid levels and promoted lipolysis in adipocytes. Overexpression of adipose triglyceride lipase and hormone-sensitive lipase by Chrysoeriol led to increased lipolysis in 3T3-L1 adipocytes. Taken together, Chrysoeriol showed anti-adipogenic and lipolytic properties in adipocytes.

Chrysoeriol suppresses hyperproliferation of rheumatoid arthritis fibroblast-like synoviocytes and inhibits JAK2/STAT3 signaling

BMC Complement Med Ther 2022 Mar 16;22(1):73.PMID:35296317DOI:10.1186/s12906-022-03553-w.

Background: Fibroblast-like synoviocytes (FLS) have cancer cell-like characteristics, such as abnormal proliferation and resistance to apoptosis, and play a pathogenic role in rheumatoid arthritis (RA). Hyperproliferation of RA-FLS that can be triggered by the activation of interleukin-6/signal transducer and activator of transcription 3 (IL-6/STAT3) signaling destructs cartilage and bone in RA patients. Chrysoeriol is a flavone found in medicinal herbs such as Chrysanthemi Indici Flos (the dried capitulum of Chrysanthemum indicum L.). These herbs are commonly used in treating RA. Chrysoeriol has been shown to exert anti-inflammatory effects and inhibit STAT3 signaling in our previous studies. This study aimed to determine whether Chrysoeriol inhibits hyperproliferation of RA-FLS, and whether inhibiting STAT3 signaling is one of the underlying mechanisms. Methods: IL-6/soluble IL-6 receptor (IL-6/sIL-6R)-stimulated RA-FLS were used to evaluate the effects of Chrysoeriol. CCK-8 assay and crystal violet staining were used to examine cell proliferation. Annexin V-FITC/PI double staining was used to detect cell apoptosis. Western blotting was employed to determine protein levels. Results: Chrysoeriol suppressed hyperproliferation of, and evoked apoptosis in, IL-6/sIL-6R-stimulated RA-FLS. The apoptotic effect of Chrysoeriol was verified by its ability to cleave caspase-3 and caspase-9. Mechanistic studies revealed that Chrysoeriol inhibited activation/phosphorylation of Janus kinase 2 (JAK2, Tyr1007/1008) and STAT3 (Tyr705); decreased STAT3 nuclear level and down-regulated protein levels of Bcl-2 and Mcl-1 that are transcriptionally regulated by STAT3. Over-activation of STAT3 significantly diminished anti-proliferative effects of Chrysoeriol in IL-6/sIL-6R-stimulated RA-FLS. Conclusions: We for the first time demonstrated that Chrysoeriol suppresses hyperproliferation of RA-FLS, and suppression of JAK2/STAT3 signaling contributes to the underlying mechanisms. This study provides pharmacological and chemical justifications for the traditional use of chrysoeriol-containing herbs in treating RA, and provides a pharmacological basis for developing Chrysoeriol into a novel anti-RA agent.

Chrysoeriol mediates mitochondrial protection via PI3K/Akt pathway in MPP+ treated SH-SY5Y cells

Neurosci Lett 2020 Jan 1;714:134545.PMID:31622648DOI:10.1016/j.neulet.2019.134545.

Chrysoeriol is a plant flavone extracted from the roots and leaves of the genus Phyllanthus. Although many biological properties of Chrysoeriol have been reported, such as its antioxidant and anti-inflammatory activities, the effects of Chrysoeriol on the cellular models of Parkinson's disease (PD) have not yet been elucidated. In the present study, we aimed to investigate whether Chrysoeriol prevents neurotoxicity induced by 1-methyl-4-phenylpyridinium iodide (MPP+) in SH-SY5Y cells, a typical in vitro PD model. The cell viability was measured by MTT assay. The morphological changes of apoptotic cell nuclei were observed by Hoechst 33,342 staining. The expression of Bax, Bcl-2 and Caspase-3 were detected by western blot analysis. The mitochondria location in the cells was observed by Mitotracker staining. Mitochondrial membrane potential was evaluated by the JC-10 assay. Treatment with MPP+ significantly caused a decrease in the viability of cells and an increase in apoptosis, as evidenced by the upregulation of apoptotic cells, caspase-3 activity and antiapoptotic ratio. These effects were all reversed by pretreatment with Chrysoeriol in SH-SY5Y cells. Moreover, pretreatment with Chrysoeriol markedly mitigated the MPP+-caused increases in the levels of the prosurvial signaling proteins, phosphorylated Akt and phosphorylated mTOR. The presence of a specific PI3K inhibitor, wortmannin, particularly abolished the chrysoeriol-induced activation of Akt phosphorylation and prevented the chrysoeriol-induced survival effect. These results indicate that the neuroprotective effect of Chrysoeriol against MPP+ treatment requires the activation of PI3K/Akt pathway. Ultimately, Chrysoeriol could be a promising therapeutic agent for the further experiment on the treatment of PD.

Chrysoeriol ameliorates TPA-induced acute skin inflammation in mice and inhibits NF-κB and STAT3 pathways

Phytomedicine 2020 Mar;68:153173.PMID:31999977DOI:10.1016/j.phymed.2020.153173.

Background: Chrysoeriol is a flavone found in diverse dietary and medicinal herbs such as Lonicerae Japonicae Flos (the dried flower bud or newly bloomed flower of Lonicera japonica Thunb.). These herbs are commonly used for treating inflammatory diseases. Herbal extracts containing Chrysoeriol have been shown to have anti-inflammatory effects and inhibit nuclear factor-kappa B (NF-κB) signaling. Some of these extracts can inhibit signal transducers and activators of transcription 3 (STAT3) signaling in cancer cells. Purpose: This study aimed to determine whether Chrysoeriol has anti-inflammatory effects and whether NF-κB and STAT3 pathways are involved in the effects. Study design and methods: A TPA (12-O-tetradecanoylphorbol-13-acetate)-induced ear edema mouse model and LPS-stimulated RAW264.7 cells were used to evaluate the effects of Chrysoeriol. Griess reagent was used to measure the production of nitric oxide (NO). Western blot and enzyme-linked immunosorbent assays were employed to detect protein levels. RT-qPCR analyses were used to detect mRNA levels. Haematoxylin and eosin (H&E) staining was employed to examine the pathological conditions in animal tissues. Results: In the mouse model, Chrysoeriol ameliorated acute skin inflammation, evidenced by reduced ear thickness, ear weight and number of inflammatory cells in inflamed ear tissues. The compound lowered protein levels of phospho-p65 (Ser536), phospho-STAT3 (Tyr705), inducible nitric oxide synthases (iNOS), cyclooxygenase-2 (COX-2), interleukin 6 (IL-6), IL-1β and tumor necrosis factor α (TNF-α) in mouse swollen ears. In LPS-stimulated RAW264.7 cells, Chrysoeriol also lowered levels of these proteins. In addition, Chrysoeriol decreased the production of NO and prostaglandin E2; inhibited the phosphorylation of inhibitor of κB (Ser32), p65 (Ser536) and Janus kinase 2 (Tyr1007/1008); decreased nuclear localization of p50, p65 and STAT3; and down-regulated mRNA levels of pro-inflammatory cytokines IL-6, IL-1β and TNF-α that are transcriptionally regulated by NF-κB and STAT3 in the cell model. Conclusion: We for the first time demonstrated that Chrysoeriol ameliorates TPA-induced ear edema in mice, and that inhibition of JAK2/STAT3 and IκB/p65 NF-κB pathways are involved in the anti-inflammatory effects of Chrysoeriol. This study provides chemical and pharmacological justifications for the use of chrysoeriol-containing herbs in treating inflammatory diseases, and provides pharmacological groundwork for developing Chrysoeriol as a novel anti-inflammatory agent.