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Jatrorrhizine Sale

(Synonyms: 药根碱) 目录号 : GC38433

An alkaloid with diverse biological activities

Jatrorrhizine Chemical Structure

Cas No.:3621-38-3

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产品描述

Jatrorrhizine is an alkaloid that has been found in the Chinese herb C. chinensis and has diverse biological activities.1,2,3,4 It is active against P. falciparum (IC50s = 422 and 1,607 ng/ml for D-6 and W-2 clones, respectively) and E. histolytica (IC50 = 82.7 μM).1,2 Jatrorrhizine inhibits the growth of C8161 human melanoma cells in vitro (IC50 = 47.4 μM) and inhibits C8161 cell-mediated neovascularization in a Matrigel? plug assay in mice when administered at a dose of 50 μg/animal.3 It reduces serum levels of triglycerides, LDL cholesterol (LDL-C), aspartate transaminase (AST), and alanine aminotransferase (ALT) in a high-fat diet-induced mouse model of hyperlipidemia when administered at doses of 20 and 100 mg/kg.4 Jatrorrhizine is also a metabolite of berberine .5

1.Vennerstrom, J.L., and Klayman, D.L.Protoberberine alkaloids as antimalarialsJ. Med. Chem.31(6)1084-1087(1988) 2.Wright, C.W., Marshall, S.J., Russell, P.F., et al.In vitro antiplasmodial, antiamoebic, and cytotoxic activities of some monomeric isoquinoline alkaloidsJ. Nat. Prod.63(12)1638-1640(2000) 3.Liu, R., Cao, Z., Pan, Y., et al.Jatrorrhizine hydrochloride inhibits the proliferation and neovascularization of C8161 metastatic melanoma cellsAnticancer Drugs24(7)667-676(2013) 4.Yang, W., She, L., Yu, K., et al.Jatrorrhizine hydrochloride attenuates hyperlipidemia in a high-fat diet-induced obesity mouse modelMol. Med. Rep.14(4)3277-3284(2016) 5.Zuo, F., Nakamura, N., Akao, T., et al.Pharmacokinetics of berberine and its main metabolites in conventional and pseudo germ-free rats determined by liquid chromatography/ion trap mass spectrometryDrug Metab. Dispos.34(12)2064-2072(2006)

Chemical Properties

Cas No. 3621-38-3 SDF
别名 药根碱
Canonical SMILES COC1=C(OC)C2=C[N+]3=C(C4=CC(OC)=C(O)C=C4CC3)C=C2C=C1
分子式 C20H20NO4+ 分子量 338.38
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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5 mM 0.5911 mL 2.9553 mL 5.9105 mL
10 mM 0.2955 mL 1.4776 mL 2.9553 mL
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Research Update

Jatrorrhizine: a review of its pharmacological effects

J Pharm Pharmacol 2021 Apr 27;73(6):709-719.PMID:33822109DOI:10.1093/jpp/rgaa065.

Objectives: Jatrorrhizine is an isoquinoline alkaloid found in medicinal plants. It is the main bioactive compound of the Chinese herbs, Coptis chinensis, Rhizoma coptidis, and Phellodendron chinense Schneid, plants that are predominantly used in traditional Chinese medicine (TCM) for the treatment of metabolic disorders, gastritis, stomachache among a host of others. This manuscript aims to provide a comprehensive review of the pharmacological effects of Jatrorrhizine, proffer suggestions on research areas that need redress and potentially serve as a reference for future studies. Key findings: Published scientific literature was therefore retrieved from all credible sources including Pubmed, Elsevier, Research Gate, Web of Science, Google Scholar, Science Direct, Europe PMC and Wiley Online library using key words such as 'Jatrorrhizine', 'botanical sources', 'pharmacology', 'toxicology', 'pharmacokinetics' or their combinations. A cursory examination of relevant scientific literature using the aforementioned key words produced more than 400 publications. Conclusions: Using an inclusion/exclusion criteria the subject matter of this review was adequately addressed. It is our hope that this review will provide a good platform for further research on fully harnessing the potential of this bioactive compound.

Jatrorrhizine: A Review of Sources, Pharmacology, Pharmacokinetics and Toxicity

Front Pharmacol 2022 Jan 13;12:783127.PMID:35095493DOI:10.3389/fphar.2021.783127.

Jatrorrhizine, an isoquinoline alkaloid, is a bioactive metabolite in common medicinal plants, such as Berberis vernae Schneid., Tinospora sagittata (Oliv.) Gagnep. and Coptis chinensis Franch. These plants have been used for centuries in traditional medicine for their wide-ranging pharmacological properties. This review emphasizes the latest and comprehensive information on the sources, pharmacology, pharmacokinetics and toxicity of Jatrorrhizine. Studies on this alkaloid were collected from scientific internet databases, including the Web of Science, PubMed, ScienceDirect, Google Scholar, Elsevier, Springer, Wiley Online Library and Europe PMC and CNKI, using a combination of keywords involving "Jatrorrhizine", "sources", "pharmacology," "pharmacokinetics," and "toxicology". Jatrorrhizine exhibits anti-diabetic, antimicrobial, antiprotozoal, anticancer, anti-obesity and hypolipidemic properties, along with central nervous system activities and other beneficial activity. Studies of Jatrorrhizine have laid the foundation for its application to the treatment of various diseases, but some issues still exist. Further investigations might emphasize 1) specific curative mechanisms of Jatrorrhizine and clinical utility, 2) application prospect in the treatment of metabolic disorders, 3) comprehensive investigations of the toxicity mechanisms and 4) interactions of Jatrorrhizine with other pharmaceuticals and development of derivatives.

Jatrorrhizine alleviates ulcerative colitis via regulating gut microbiota and NOS2 expression

Gut Pathog 2022 Oct 21;14(1):41.PMID:36271438DOI:10.1186/s13099-022-00514-z.

Background: The natural protoberberine Jatrorrhizine (JA) is reported to have several medicinal properties and a significant effect on the gut microbiota of mice. The regulation of gut microbiota is generally known to play an important role in the intestinal mucosal immune response to ulcerative colitis (UC). However, whether JA can be used in the treatment of UC is still unclear. Our study aimed to investigate the underlying therapeutic effects and mechanisms of JA in treating colitis. Results: Compared with the DSS-induced colitis model group, the JA + DSS treated group had more significant improvements in weight loss, disease activity index score, colon length shortening, and pathological inflammation. 16s rRNA sequencing analysis showed that JA treatment protected colitis mice against DSS-induced disturbance of gut microbiota. At the phylum level, reductions in Deferribacteres and Proteobacteria were observed in the JA-treated group; At the genus level, the JA-treated group showed an increased relative abundance of Akkermansia and decreased abundance of Escherichia-Shigella, Desulfovibrio, Mucispirillum, etc. Network pharmacology was then used to screen out five drug-disease target genes (NOS2, ESR1, CALM1, CALM2, CALM3). Transcriptomics analysis further validated that the NOS2 expression was significantly reduced in colon tissue of JA-administered mice compared with DSS control mice. Additionally, analysis of correlation suggested that NOS2 expression was negatively correlated with the relative abundance of AKKermansia and positively correlated with Desulfovibrio, Rikenella. Conclusion: JA alleviates ulcerative colitis via regulating gut microbiota and NOS2 expression.

Jatrorrhizine from Rhizoma Coptidis exerts an anti-obesity effect in db/db mice

J Ethnopharmacol 2022 Nov 15;298:115529.PMID:35835345DOI:10.1016/j.jep.2022.115529.

Ethnopharmacological relevance: Obesity is closely related to diabetes. Jatrorrhizine (JAT) from Rhizoma Coptidis (RC) can reduce blood glucose and lipid levels. However, the molecular mechanisms for JAT's anti-obesity effect are still not clear. Aim of the study: To explore the effect of JAT in the treatment of obesity and the underlying molecular mechanisms. Materials and methods: db/db mice were used as a typical obese animal model in current study. The anti-obesity effects of five alkaloids from RC were compared by feeding the mice for 8 weeks with a dosage of 105 mg/kg while the dose-dependent study (35 mg/kg and 105 mg/kg) of JAT on obese mice was conducted in another 8-week-long animal experiment. Meanwhile, RNA-seq analysis, in vitro experiments, and western blotting were utilized to predict and confirm the potential pathway that JAT participated in improving obesity. Results: The experimental results demonstrated that five RC alkaloids caused different degrees of weight loss in db/db obese mice. Among them, JAT showed the best effect. It could significantly reduce the body weight, blood lipid levels, and epididymal fat weight of db/db mice. H&E and Oil red O staining results showed that it could also dramatically improve liver lipid metabolism. The results from RNA-seq suggested that JAT had significantly altered 207 DEGs for the treatment of obesity, among which IRS1 changed the most. Next, GO and KEGG analysis enriched four major lipid metabolism-related pathways: biosynthesis of unsaturated fatty acids, PI3K-AKT signaling pathway, metabolic pathways, and fatty acid elongation. Finally, in vitro experiments and western blotting proved that JAT regulated the expression of IRS1/PI3K/AKT pathway-related proteins in a dose-dependent manner to address obesity. Conclusions: In conclusion, JAT from RC has an effect on treating obesity, and its anti-obesity effect may be exerted via the IRS1/PI3K/AKT signaling pathway.

Jatrorrhizine reduces myocardial infarction-induced apoptosis and fibrosis through inhibiting p53 and TGF-β1/Smad2/3 pathways in mice

Acta Cir Bras 2022 Oct 28;37(7):e370705.PMID:36327404DOI:10.1590/acb370705.

Purpose: To explore the mechanism of Jatrorrhizine on apoptosis and fibrosis induced by myocardial infarction (MI) in an animal model. Methods: The left anterior descending branch of coronary artery was surgically ligated to duplicate the mouse model of MI. The sham and infarcted mice were treated with normal saline once a day, while mice in experimental groups received low-dose (LD) and high-dose (HD) Jatrorrhizine once a day respectively. Two weeks later, cardiac function was detected by echocardiography, and histopathological examination was performed using hematoxylin and eosin (H&E) and Masson staining. The expressions of p53, TGF-β1, Smad/2/3, Bax, Bcl-2, collagen I and collagen III were quantified using qRT-PCR and western blot assays. Results: Jatrorrhizine significantly improved left ventricular ejection fraction (LVEF) and left ventricle end-systolic (LVES) in mice. Histopathological, administration of Jatrorrhizine weakened infiltration of inflammatory cells and cardiac fibrosis in myocardium of mice caused by MI. Additionally, Jatrorrhizine suppressed cardiomyocyte apoptosis exhibited as its capability to reverse changes of Bax and Bcl-2 levels in myocardium caused by MI. Jatrorrhizine statistically significantly downregulated expression of collagen I and collagen III, as well as TGF-β1, Smad2/3 and p53. Conclusions: Jatrorrhizine reduce cardiomyocyte apoptosis and fibrosis through inhibiting p53/Bax/Bcl-2 and TGF-β1/Smad2/3 signaling pathways.