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  • 印枳碱

    Aegeline

    印枳碱
    产品编号 CFN91133
    CAS编号 456-12-2
    分子式 = 分子量 C18H19NO3 = 297.4
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源 The herbs of Cannabis sativa L.
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
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    印枳碱 CFN91133 456-12-2 10mg QQ客服:3257982914
    印枳碱 CFN91133 456-12-2 20mg QQ客服:3257982914
    印枳碱 CFN91133 456-12-2 50mg QQ客服:3257982914
    印枳碱 CFN91133 456-12-2 100mg QQ客服:3257982914
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    我们的产品现已经出口到下面的研究机构与大学,并且还在增涨
  • Shanghai University of TCM (China)
  • University of Toronto (Canada)
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  • Sant Gadge Baba Amravati University (India)
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  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • The University of Manitoba2021, 35690.
  • Pharmacognosy Magazine2018, 14(56):418-424
  • Nat Chem Biol.2018, 14(8):760-763
  • J Biosci.2020, 45:46.
  • Plant Cell Physiol.2018, 59(1):128-141
  • J Ethnopharmacol.2017, 198:91-97
  • Pharmaceutics2022, 14(2),376.
  • Korean Herb. Med. Inf.2020, 8(2):243-254.
  • Biomedicines.2021, 9(8):954.
  • Appl. Sci.2020, 10(16),5482.
  • Neurochem Res.2021, s11064-021-03449-0
  • J of the Korean Society of Food Science and Nutrition2019, 32(2):148-154
  • PLoS One.2015, 10(5):e0127060
  • Process Biochemistry2019, 87:213-220
  • Molecules.2019, 24(24),4583
  • Naunyn Schmiedebergs Arch Pharmacol.2021, 394(1):107-115.
  • Plants (Basel).2021, 10(6):1192.
  • Oxid Med Cell Longev2020, 12
  • Tropical Journal of Pharmaceutical Research 2021, 20(6):1165-1170.
  • LWT2020, 124:109163
  • J Biotechnol.2020, 318:10-19.
  • J Funct Foods2019, 54:449-456
  • Drug Des Devel Ther.2020, 14:5189-5204.
  • ...
  • 生物活性
    Description: Aegeline has anti-diabetic and anti-dyslipidemic activities, it inspired synthesis of novel amino alcohol and thiazolidinedione hybrids with antiadipogenic activity in 3T3-L1 cells, it also inspired synthesis of novel β3-AR agonist improves insulin sensitivity in vitro and in vivo models of insulin resistance. Aegeline mimics the yeast SNARE protein Sec22p in suppressing α-synuclein and Bax toxicity in yeast.
    Targets: PPARγ | C/EBPα | FAS | hMSCs
    In vitro:
    Bioorg Med Chem Lett. 2019 Feb 1;29(3):454-460.
    Aegeline, a natural product from the plant Aegle marmelos, mimics the yeast SNARE protein Sec22p in suppressing α-synuclein and Bax toxicity in yeast.[Pubmed: 30579794 ]
    Herein, we have identified yeast Sec22p (ySec22p), a SNARE protein essential for endoplasmic reticulum to Golgi trafficking, as a suppressor of Bax-induced yeast apoptosis and corroborated published observations that ySec22p suppresses α-synuclein's toxicity in yeast. It has been suggested that compounds which enhance expression, in neurons, of human homologues of ySec22p (Sec22Bp/Sec22p/Sec22A) would prevent synucleinopathies, such as Parkinson's disease.
    METHODS AND RESULTS:
    With the aim of finding a small molecule that would mimic ySec22p, a library of natural products consisting of 394-compounds was screened using yeast cells that express either human α-synuclein or human Bax. The antioxidant aegeline, an alkaloid-amide occurring in the leaves of the plant Aegle marmelos Correa, was the only molecule that overcame apoptosis induced by both α-synuclein and Bax in yeast. Besides, aegeline also prevented growth block in cells expressing the more toxic A53T α-synuclein mutant. Restoration of cell growth occurred through inhibition of increased ROS levels, mitochondrial membrane potential loss and nuclear DNA fragmentation, characteristics of apoptosis manifested in α-synuclein or Bax-expressing cells.
    CONCLUSIONS:
    These results highlight the importance of yeast systems to identify rapidly molecules that may prevent the onset of apoptosis that occurs in Parkinson's disease.
    Eur J Med Chem. 2018 Jan 1;143:780-791.
    Aegeline inspired synthesis of novel amino alcohol and thiazolidinedione hybrids with antiadipogenic activity in 3T3-L1 cells.[Pubmed: 29220798 ]
    Excess adiposity is a hallmark of obesity, which is caused due to an imbalance between energy intake and energy consumed. Obesity is often associated with several metabolic disorders like dyslipidemia, cardiovascular diseases and type 2 diabetes. Earlier, our group had reported natural product Aegeline (amino-alcohol) isolated from the plant Aegle marmelos as an anti-diabetic and anti-dyslipidemic compound.
    METHODS AND RESULTS:
    With this background, we synthesized a series of novel amino alcohol and thiazolidinedione hybrid molecules and studied their antiadipogenic activity. As a result, we have identified a potent hybrid compound 12c as an inhibitor of adipocyte differentiation. The compound 12c inhibits lipid accumulation and adipogenesis in 3T3-L1 preadipocyte cell line. Exposure of compound 12c blocks mitotic clonal expansion and arrests cells in S-phase of cell cycle. Detailed analysis showed that compound 12c decreases expression of two major transcription factors that are involved in adipocyte differentiation, PPARγ, C/EBPα, and other adipogenesis associated genes like aP2 and FAS.
    CONCLUSIONS:
    Thus, we concluded that compound 12c shows potential ability to inhibit adipocyte differentiation which can be used therapeutically for the treatment of obesity and its associated metabolic disorders.
    In vivo:
    Metabolism. 2018 Aug;85:1-13.
    Aegeline inspired synthesis of novel β3-AR agonist improves insulin sensitivity in vitro and in vivo models of insulin resistance.[Pubmed: 29524448 ]
    In our drug discovery program of natural product, earlier we have reported Aegeline that is N-acylated-1-amino-2- alcohol, which was isolated from the leaves of Aeglemarmelos showed anti-hyperlipidemic activity for which the QSAR studies predicted the compound to be the β3-AR agonist, but the mechanism of its action was not elucidated. In our present study, we have evaluated the β3-AR activity of novel N-acyl-1-amino-3-arylopropanol synthetic mimics of aegeline and its beneficial effect in insulin resistance. In this study, we have proposed the novel pharmacophore model using reported molecules for antihyperlipidemic activity. The reported pharmacophore features were also compared with the newly developed pharmacophore model for the observed biological activity.
    METHODS AND RESULTS:
    Based on 3D pharmacophore modeling of known β3AR agonist, we screened 20 synthetic derivatives of Aegeline from the literature. From these, the top scoring compound 10C was used for further studies. The in-slico result was further validated in HEK293T cells co-trransfected with human β3-AR and CRE-Luciferase reporter plasmid for β3-AR activity.The most active compound was selected and β3-AR activity was further validated in white and brown adipocytes differentiated from human mesenchymal stem cells (hMSCs). Insulin resistance model developed in hMSC derived adipocytes was used to study the insulin sensitizing property. 8 week HFD fed C57BL6 mice was given 50 mg/Kg of the selected compound and metabolic phenotyping was done to evaluate its anti-diabetic effect. As predicted by in-silico 3D pharmacophore modeling, the compound 10C was found to be the most active and specific β3-AR agonist with EC50 value of 447 nM. The compound 10C activated β3AR pathway, induced lipolysis, fatty acid oxidation and increased oxygen consumption rate (OCR) in human adipocytes. Compound 10C induced expression of brown adipocytes specific markers and reverted chronic insulin induced insulin resistance in white adipocytes. The compound 10C also improved insulin sensitivity and glucose tolerance in 8 week HFD fed C57BL6 mice.
    CONCLUSIONS:
    This study enlightens the use of in vitro insulin resistance model close to human physiology to elucidates the insulin sensitizing activity of the compound 10C and edifies the use of β3AR agonist as therapeutic interventions for insulin resistance and type 2 diabetes.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 3.3625 mL 16.8124 mL 33.6247 mL 67.2495 mL 84.0619 mL
    5 mM 0.6725 mL 3.3625 mL 6.7249 mL 13.4499 mL 16.8124 mL
    10 mM 0.3362 mL 1.6812 mL 3.3625 mL 6.7249 mL 8.4062 mL
    50 mM 0.0672 mL 0.3362 mL 0.6725 mL 1.345 mL 1.6812 mL
    100 mM 0.0336 mL 0.1681 mL 0.3362 mL 0.6725 mL 0.8406 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    4-羟基肉桂酰胺; 4-Hydroxycinnamamide CFN99895 194940-15-3 C9H9NO2 = 163.2 5mg QQ客服:1413575084
    N-对反式香豆酰酪胺; N-p-trans-Coumaroyltyramine CFN98494 36417-86-4 C17H17NO3 = 283.3 10mg QQ客服:2932563308
    N-反式-对香豆酰酪胺; N-trans-p-Coumaroyltyrosine CFN95279 77201-66-2 C18H17NO5 = 327.3 10mg QQ客服:2932563308
    N-对香豆酰-N’-咖啡酰腐胺; N-p-coumaroyl-N'-caffeoylputrescine CFN99238 1138156-77-0 C22H24N2O5 = 396.4 5mg QQ客服:2932563308
    N1,N10-双(对香豆酰)亚精胺; N1,N10-Bis(p-coumaroyl)spermidine CFN99248 114916-05-1 C25H31N3O4 = 437.5 5mg QQ客服:2932563308
    3,4-二羟基肉桂酰胺; 3,4-Dihydroxycinnamamide CFN99316 1202-41-1 C9H9NO3 = 179.2 5mg QQ客服:1413575084
    3-[3,4-双(乙酰氧基)苯基]-2-丙烯酰胺; 3,4-Diacetoxycinnamamide CFN99390 129488-34-2 C13H13NO5 = 263.3 5mg QQ客服:1413575084
    阿魏酸酰胺; Ferulamide CFN97041 61012-31-5 C10H11NO3 = 193.2 5mg QQ客服:2159513211
    印枳碱; Aegeline CFN91133 456-12-2 C18H19NO3 = 297.4 20mg QQ客服:215959384
    N-咖啡酰O-甲基酪胺; N-Caffeoyl O-methyltyramine CFN70295 189307-47-9 C18H19NO4 = 313.4 5mg QQ客服:1148253675

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