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Euscaphic acid Sale

(Synonyms: 野鸦椿酸) 目录号 : GC38392

A triterpene with diverse biological activities

Euscaphic acid Chemical Structure

Cas No.:53155-25-2

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1mg
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产品描述

Euscaphic acid is a triterpene that has been found in R. alceaefolius and has diverse biological activities.1,2,3 It inhibits the proliferation of CNE-1 and C666-1 nasopharyngeal carcinoma cells when used at concentrations of 5 and 10 ?g/ml.1 Euscaphic acid inhibits acetylcholinesterase (AChE; IC50 = 35.9 ?M) and α-glucosidase (IC50 = 24.9 ?M).2 It reduces the production of nitric oxide (NO) and levels of inducible nitric oxide synthase (iNOS) and COX-2 in LPS-stimulated RAW 264.7 cells.3 Euscaphic acid (10 mg/kg) reduces serum IgE and IgG2a levels, ear tissue mast cell infiltration, and pruritis in a mouse model of difluoroethane- and 2,4-dinitrochlorobenzene-induced atopic dermatitis.4

1.Dai, W., Dong, P., Liu, J., et al.Euscaphic acid inhibits proliferation and promotes apoptosis of nasopharyngeal carcinoma cells by silencing the PI3K/AKT/mTOR signaling pathwayAm. J. Transl. Res.11(4)2090-2098(2019) 2.Ado, M.A., Maulidiani, M., Ismail, I.S., et al.Acetylcholinesterase and α-glucosidase inhibitory compounds from Callicarpa maingayiNat. Prod. Res.35(17)2992-2996(2021) 3.Kim, I.-T., Ryu, S., Shin, J.-S., et al.Euscaphic acid isolated from roots of Rosa rugosa inhibits LPS-induced inflammatory responses via TLR4-mediated NF-κB inactivation in RAW 264.7 macrophagesJ. Cell. Biochem.113(6)1936-1946(2012) 4.Jeong, N.-H., Lee, S., Choi, Y.-A., et al.Inhibitory effects of euscaphic acid in the atopic dermatitis model by reducing skin inflammation and intense pruritusInflammation45(4)1680-1691(2022)

Chemical Properties

Cas No. 53155-25-2 SDF
别名 野鸦椿酸
Canonical SMILES OC([C@]12[C@]([C@](O)([C@H](C)CC2)C)([H])C3=CC[C@@]([C@@]4([C@@](C(C)([C@H](O)[C@H](O)C4)C)([H])CC5)C)([H])[C@]5(C)[C@]3(C)CC1)=O
分子式 C30H48O5 分子量 488.7
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 2.0462 mL 10.2312 mL 20.4625 mL
5 mM 0.4092 mL 2.0462 mL 4.0925 mL
10 mM 0.2046 mL 1.0231 mL 2.0462 mL
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Research Update

Euscaphic acid and Tormentic acid protect vascular endothelial cells against hypoxia-induced apoptosis via PI3K/AKT or ERK 1/2 signaling pathway

Life Sci 2020 Jul 1;252:117666.PMID:32298737DOI:10.1016/j.lfs.2020.117666.

Aims: Euscaphic acid and Tormentic acid are aglycones of Kaji-ichigoside F1 and Rosamultin, respectively. These four compounds are pentacyclic triterpenoid, isolated from the subterranean root of the Potentilla anserina L. Based on the protective roles against hypoxia-induced apoptosis of Euscaphic acid and Tormentic acid in vascular endothelial cells, this study was designed to determine the mechanisms. Main methods: The model of hypoxic injuries in EA. hy926 cells was established. Through applications of PI3K/AKT inhibitor, LY294002 and ERK1/2 inhibitor, PD98059, we explored the relationships between pharmacodynamic mechanisms and PI3K/AKT or ERK 1/2 signaling pathway. The anti-hypoxic effects were studied by methyl-thiazolyl-tetrazolium (MTT) assay, Hematoxylin-Eosin (HE) staining, DAPI staining, and flow cytometry. The mechanisms of anti-mitochondrial apoptosis were explored by western blot. The expressions of p-ERK 1/2, ERK 1/2, p-AKT, AKT, p-NF-κB, NF-κB, Bcl-2, Bax, Cyt C, cleaved caspase-9 and cleaved caspase-3 were detected. Key findings: Euscaphic acid protected vascular endothelial cells against hypoxia-induced apoptosis via ERK1/2 signaling pathway, and Tormentic acid brought its efficacy into full play via PI3K/AKT and ERK1/2 signaling pathways. In addition, PI3K/AKT signaling pathway positively regulated ERK1/2 pathway, and ERK1/2 pathway negatively regulated PI3K/AKT pathway. Significance: This evidence provides theoretical and experimental basis for the following research on anti-hypoxic drugs of Potentilla anserina L.

Inhibitory Effects of Euscaphic acid in the Atopic Dermatitis Model by Reducing Skin Inflammation and Intense Pruritus

Inflammation 2022 Aug;45(4):1680-1691.PMID:35257273DOI:10.1007/s10753-022-01652-x.

Atopic dermatitis (AD) is a complex and multifactorial skin disease characterized by skin inflammation and intense pruritus. There are many commercially available treatments such as topical corticosteroids and immunosuppressants to treat of AD, but their effectiveness is limited, and frequent use of these treatments can cause serious side effects. Therefore, the development of new therapeutic agents is necessary for the treatment of AD. Hence, an alternative agent that was derived from natural products that are effective and safe for AD treatment was investigated using experimental models. The biological activity of Euscaphic acid has anti-inflammatory, anticoagulant, and antioxidant effects. Despite the various biomedical properties of Euscaphic acid, its therapeutic effects on AD have not been well studied. In this study, we investigated the effects of Euscaphic acid on skin inflammation and pruritus in AD mouse model. The effects of Euscaphic acid were investigated in activated human epidermal keratinocytes and leukemia T lymphoblast cell lines, and Dermatophagoides farina extract and 2,4-dinitrochlorobenzene-induced AD mouse model. Euscaphic acid ameliorated AD properties, such as the expression of inflammatory cytokines and activation of transcription factors. In addition, Euscaphic acid reduced critical factors for pruritus such as immunoglobulin E hyperproduction, mast cell invasion, and interleukin-33 expression. Taken together, Euscaphic acid could be a potent therapeutic agent for the treatment of AD.

Euscaphic acid inhibits proliferation and promotes apoptosis of nasopharyngeal carcinoma cells by silencing the PI3K/AKT/mTOR signaling pathway

Am J Transl Res 2019 Apr 15;11(4):2090-2098.PMID:31105820doi

Rubus alceaefolius Poir. has been used for the treatment of nasopharyngeal carcinoma (NPC) in China for many years. Euscaphic acid is an active component of Rubus alceaefolius Poir. However, the mechanism of action of Euscaphic acid in NPC remains unclear. In this study, Euscaphic acid inhibited the proliferation of NPC cells, induced apoptosis, and led to cell cycle arrest in the G1/S phase. In addition, Euscaphic acid inhibited the expression of phosphatidylinositide 3-kinases (PI3K), phosphorylated protein kinase B (p-AKT), and phosphorylated mammalian target of rapamycin (p-mTOR) p-mTOR in NPC cells. The activation of the PI3K/AKT/mTOR signaling pathway by IGF-1 promoted cell proliferation, inhibited apoptosis, and cell cycle arrest in NPC cells. In conclusion, we demonstrated that Euscaphic acid reduced cell proliferation and induced apoptosis and cell cycle arrest in NPC cells by suppressing the PI3K/AKT/mTOR signaling pathway.

Euscaphic acid relieves fatigue by enhancing anti-oxidative and anti-inflammatory effects

Immunopharmacol Immunotoxicol 2023 Feb;45(1):114-121.PMID:36066092DOI:10.1080/08923973.2022.2121926.

Background: Oxidative stress and inflammation are involved in chronic fatigue. Euscaphic acid (EA) is an active compound of Eriobotrya japonica (Loquat) and has anti-oxidative effect. Methods: The goal of present study is to prove whether EA could relieve fatigue through enhancing anti-oxidant and anti-inflammatory effects in in vitro/in vivo models. Results: EA notably improved activity of superoxide dismutase (SOD) and catalase (CAT), while EA reduced levels of malondiadehyde (MDA) and inflammatory cytokines without cytotoxicity in H2O2-stimulated in myoblast cell line, C2C12 cells. EA significantly reduced levels of fatigue-causing factors such as lactate dehydrogenase (LDH) and creatin kinase (CK), while EA significantly incresed levels of anti-fatigue-related factor, glycogen compared to the H2O2-stimulated C2C12 cells. In treadmill stress test (TST), EA significantly enhanced activities of SOD and CAT as well as exhaustive time and decreased levels of MDA and inflammatory cytokines. After TST, levels of free fatty acid, citrate synthase, and muscle glycogen were notably enhanced by oral administration of EA, but EA decreased levels of lactate, LDH, cortisol, aspartate aminotransferase, alanine transaminase, CK, glucose, and blood urea nitrogen compared to the control group. Furthermore, in forced swimming test, EA significantly increased levels of anti-fatigue-related factors and decreased excessive accumulations of fatigue-causing factors. Conclusions: Therefore, the results indicate that potent anti-fatigue effect of EA can be achieved via the improvement of anti-oxidative and anti-inflammatory properties, and this study will provide scientific data for EA to be developed as a novel and efficient component in anti-fatigue health functional food.

Euscaphic acid, a new hypoglycemic natural product from Folium Eriobotryae

Pharmazie 2008 Oct;63(10):765-7.PMID:18972842doi

Folium Eriobotryae has been used as a medicinal plant for a long time, and it is known to have many physiological actions such as anti-inflammatory, anti-tussive, expectorant and anti-diabetic. We have reported that the 70% ethanol extract of Folium Eriobotryae exerted a significant hypoglycemic effect to alloxan-diabetic mice. In this study, we isolated Euscaphic acid, a natural product from Folium Eriobotryae, and investigated its hypoglycemic effect in normoglycemic and alloxan-diabetic mice. All effects had been compared with those of gliclazide. The plasma glucose levels were significantly lowered in normoglycemic mice treated with Euscaphic acid compared to mice treated with 0.5% CMC-Na solution only. Moreover, the dosage of 50 mg/kg exerted a significant (P < 0.05) hypoglycemic effect in alloxan-diabetic mice after orally administration. The research proved that Euscaphic acid is one of the active hypoglycemic constituents in Folium Eriobotryae, but the details of the mechanism need to be investigated further.