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  • 土莫酸

    Tumulosic acid

    产品编号 CFN95399
    CAS编号 508-24-7
    分子式 = 分子量 C31H50O4 = 486.7
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Triterpenoids
    植物来源 The roots of Wolfiporia cocos
    产品名称 产品编号 CAS编号 包装 QQ客服
    土莫酸 CFN95399 508-24-7 1mg QQ客服:2932563308
    土莫酸 CFN95399 508-24-7 5mg QQ客服:2932563308
    土莫酸 CFN95399 508-24-7 10mg QQ客服:2932563308
    土莫酸 CFN95399 508-24-7 20mg QQ客服:2932563308
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    2. 只要有可能,产品溶解后,您应该在同一天应用于您的实验。 但是,如果您需要提前做预实验,或者需要全部溶解,我们建议您将溶液以等分试样的形式存放在-20℃的密封小瓶中。 通常,这些可用于长达两周。 使用前,打开样品瓶前,我们建议您将产品平衡至室温至少1小时。

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    PMID: 30417089
  • Agricultural Research Organization (ARO) (Israel)
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  • University of Stirling (United Kingdom)
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  • 生物活性
    Description: Tumulosic acid, a triterpenoid, inhibits KLK5 protease activity (IC50= 14.84 μM). Tumulosic acid suppresses the proteolytic processing of LL-37 in keratinocytes at ≤10 μM. Tumulosic acid reduced, in a dose-dependent manner, nitric oxide (NO) production from lipopolysaccharide (LPS)-induced RAW 264.7 cells.
    In vitro:
    Molecules . 2017 Oct 27;22(11):1829.
    Inhibition of Human Kallikrein 5 Protease by Triterpenoids from Natural Sources[Pubmed: 29077044]
    Stratum corneum tryptic enzyme kallikrein 5 (KLK5) is a serine protease that is involved in the cell renewal and maintenance of the skin barrier function. The excessive activation of KLK5 causes an exacerbation of dermatoses, such as rosacea and atopic dermatitis. Some triterpenoids are reported to suppress the serine proteases. We aimed to investigate whether bioactive triterpenoids modulate the KLK5 protease. Nineteen triterpenoids occurring in medicinal crude drugs were evaluated using an enzymatic assay to measure the anti-KLK5 activity. The KLK5-dependent cathelicidin peptide LL-37 production in human keratinocytes was examined using immunoprecipitation and Western blotting. Screening assays for evaluating the anti-KLK5 activity revealed that ursolic acid, oleanolic acid, saikosaponin b₁, tumulosic acid and pachymic acid suppressed the KLK5 protease activity, although critical molecular moieties contributing to anti-KLK5 activity were unclarified. Ursolic acid and tumulosic acid suppressed the proteolytic processing of LL-37 in keratinocytes at ≤10 μM; no cytotoxicity was observed. Both triterpenoids were detected in the plasma of rats administered orally with triterpenoid-rich crude drug Jumihaidokuto. Our study reveals that triterpenoids, such as ursolic acid and tumulosic acid, modulate the KLK5 protease activity and cathelicidin peptide production. Triterpenoids may affect the skin barrier function via the regulation of proteases.
    J Nat Prod . 2002 Apr;65(4):462-465.
    Inhibition of tumor-promoting effects by poricoic acids G and H and other lanostane-type triterpenes and cytotoxic activity of poricoic acids A and G from Poria cocos[Pubmed: 11975480]
    The structures of two novel 3,4-seco-lanostane-type triterpenes isolated from the sclerotium of Poria cocos were established to be 16alpha-hydroxy-3,4-seco-lanosta-4(28),8,24-triene-3,21-dioic acid (1; poricoic acid G) and 16alpha-hydroxy-3,4-seco-24-methyllanosta-4(28),8,24(24(1))-triene-3,21-dioic acid (2; poricoic acid H) on the basis of spectroscopic methods. These two, and eight other known compounds isolated from the sclerotium, poricoic acid B (3), poricoic acid A (4), tumulosic acid (5), dehydrotumulosic acid (6), 3-epidehydrotumulosic acid (7), polyporenic acid C (8), 25-hydroxy-3-epidehydrotumulosic acid (9), and dehydroabietic acid methyl ester (10), showed potent inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA). Evaluation of the cytotoxicity of compounds 1 and 4 against human cancer cell lines revealed that 1 was significantly cytotoxic to leukemia HL-60 cells [GI(50) (concentration that yields 50% growth) value 39.3 nM], although it showed only moderate cytotoxicity to the other cells. Compound 4 exhibited moderate cytotoxicity to all of the cancer cell lines tested.
    Chem Biodivers . 2011 Nov;8(11):2135-43.
    Triterpenes from the fungus Poria cocos and their inhibitory activity on nitric oxide production in mouse macrophages via blockade of activating protein-1 pathway[Pubmed: 22083926]
    Two new triterpenes, 29-hydroxydehydrotumulosic acid (1) and 29-hydroxydehydropachymic acid (2), together with six known compounds, dehydropachymic acid (3), dehydrotumulosic acid (4), 29-hydroxypolyporenic acid C (5), polyporenic acid C (6), tumulosic acid (7), and pachymic acid (8), were isolated from the dried sclerotia of Poria cocos. In the in vitro bioassays, these isolated compounds reduced, in a dose-dependent manner, nitric oxide (NO) production from lipopolysaccharide (LPS)-induced RAW 264.7 cells, with compounds 5 and 6, the IC(50) values of which were 16.8±2.7 and 18.2±3.3 μM, respectively, exhibiting the greatest inhibition activity. Further Western blot analysis conducted on cells pre-treated with compounds 5 and 6, and luciferase assays on activator protein 1-dependent gene expression revealed that the inhibited NO release was attributed to the reduced expression of iNOs (=inducible NO synthase) enzymes, which might be regulated via the blockade of activator protein-1 signaling pathway.
    Arch Pharm Res. 2004 Aug;27(8):829-833.
    Cytotoxicity and DNA topoisomerases inhibitory activity of constituents from the sclerotium of Poria cocos[Pubmed: 15460443]
    The bioactivity-guided fractionation of the methylene chloride extract of the sclerotium of Poria cocos led to the isolation of (S)-(+)-turmerone (1), ergosterol peroxide (2), polyporenic acid C (3), dehydropachymic acid (4), pachymic acid (5), and tumulosic acid (6). Compounds 4-6 exhibited moderate cytotoxicities, with IC50 values of 20.5, 29.1, and 10.4 microM, respectively, against a human colon carcinoma cell line. However, 3-6 not only showed inhibitory activities as potent as etoposide used as a positive control on DNA topoisomerase II (36.1, 36.2, 43.9 and 66.7% inhibition at a concentration of 20 microM, respectively), but also inhibition of DNA topoisomerase I (55.8, 60.7, 43.5, and 83.3% inhibition at a concentration of 100 microM, respectively).
    In vivo:
    J Mass Spectrom . 2013 Aug;48(8):904-913.
    A UFLC-MS/MS method with a switching ionization mode for simultaneous quantitation of polygalaxanthone III, four ginsenosides and tumulosic acid in rat plasma: application to a comparative pharmacokinetic study in normal and Alzheimer's disease rats[Pubmed: 23893636]
    A fast, sensitive and reliable ultra fast liquid chromatography-tandem mass spectrometry (UFLC-MS/MS) method has been developed and validated for simultaneous quantitation of polygalaxanthone III (POL), ginsenoside Rb1 (GRb1), ginsenoside Rd (GRd), ginsenoside Re (GRe), ginsenoside Rg1 (GRg1) and tumulosic acid (TUM) in rat plasma after oral administration of Kai-Xin-San, which plays an important role for the treatment of Alzheimer's disease (AD). The plasma samples were extracted by liquid-liquid extraction using ethyl acetate-isopropanol (1:1, v/v) with salidrdoside as internal standard (IS). Good chromatographic separation was achieved using gradient elution with the mobile phase consisting of methanol and 0.01% acetic acid in water. The tandem mass spectrometric detection was performed in multiple reaction monitoring mode on 4000Q UFLC-MS/MS system with turbo ion spray source in a negative and positive switching ionization mode. The lower limits of quantification were 0.2-1.5 ng/ml for all the analytes. Both intra-day and inter-day precision and accuracy of analytes were well within acceptance criteria (±15%). The mean absolute extraction recoveries of analytes and IS from rat plasma were all more than 60.0%. The validated method has been successfully applied to comparing pharmacokinetic profiles of analytes in normal and AD rat plasma. The results indicated that no significant differences in pharmacokinetic parameters of GRe, GRg1 and TUM were observed between the two groups, while the absorption of POL and GRd in AD group were significantly higher than those in normal group; moreover, the GRb1 absorbed more rapidly in model group. The different characters of pharmacokinetics might be caused by pharmacological effects of the analytes.
    Talanta . 2018 Dec 1;190:450-459.
    LC-ESI-MS/MS method for simultaneous determination of eleven bioactive compounds in rat plasma after oral administration of Ling-Gui-Zhu-Gan Decoction and its application to a pharmacokinetics study[Pubmed: 30172532]
    A sensitive and robust LC-MS/MS method has been developed and validated to simultaneous determine the concentrations of tumulosic acid, dehydrotumulosic acid, polyporenic acid C, cinnamic acid, Atractylenolide I, Atractylenolide II, Atractylenolide III, glycyrrhizic acid, glycyrrhetinic acid, liquiritigenin and isoliquiritin in plasma from rats who received Ling-Gui-Zhu-Gan Decoction extract oral administration. The samples were prepared by a liquid-liquid extraction procedure using ethyl ether as the extraction solvent and schisandrin as the internal standard. Chromatographic separation was achieved using a Thermo Hypersil GOLD C18 column (2.1 mm × 100 mm, 1.9 μm) and a gradient mobile phase consisting of acetonitrile-water with 0.1% formic acid. All of the analytes were quantified using negative and positive multiple reaction monitoring mode. The method was validated for selectivity, linearity, accuracy, precision, recovery, matrix effect and sample stability under various storage conditions, whose values are all fell in the acceptable limits. We report the lowest limit of quantification for tumulosic acid, dehydrotumulosic acid and polyporenic acid C as 2 ng/mL. This is the first study for simultaneous determination of so many analytes in rat plasma after oral administration of Ling-Gui-Zhu-Gan Decoction. This validated method was successfully used to study the pharmacokinetics of multiple compounds in rat plasma after oral administration of Ling-Gui-Zhu-Gan Decoction.
    Fitoterapia . 2012 Jan;83(1):117-124.
    Comparative pharmacokinetics of three triterpene acids in rat plasma after oral administration of Poria extract and its formulated herbal preparation: GuiZhi-FuLing capsule[Pubmed: 22008604]
    A sensitive liquid chromatographic-mass spectrometric technique coupled with liquid-liquid extraction method was developed and validated for simultaneous determination of dehydro-tumulosic acid, tumulosic acid and polyporic acid C in rat plasma. The analytes were separated on a Kromasil C(18) column with a total running time of 12.5 min. Author had compared the pharmacokinetics of dehydro-tumulosic acid, tumulosic acid and polyporic acid C after oral administration of the extract of Poria and its formulated herbal preparation (GuiZhi-FuLing capsule). The improved pharmacokinetic profiles of the three compounds were found in the GuiZhi-FuLing capsule, indicating the more effective absorption and the slower elimination, compared with the Poria extract. Furthermore, this study revealed that as far as the Poria extract was concerned, it is very valuable to be used as a clinical instruction of GF capsule.
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.0547 mL 10.2733 mL 20.5465 mL 41.0931 mL 51.3663 mL
    5 mM 0.4109 mL 2.0547 mL 4.1093 mL 8.2186 mL 10.2733 mL
    10 mM 0.2055 mL 1.0273 mL 2.0547 mL 4.1093 mL 5.1366 mL
    50 mM 0.0411 mL 0.2055 mL 0.4109 mL 0.8219 mL 1.0273 mL
    100 mM 0.0205 mL 0.1027 mL 0.2055 mL 0.4109 mL 0.5137 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.
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    茯苓新酸A; Poricoic acid A(F) CFN92838 137551-38-3 C31H46O5 = 498.7 20mg QQ客服:1413575084
    Poricoic acid AE ; Poricoic acid AE CFN96980 1159753-88-4 C33H50O5 = 526.75 5mg QQ客服:215959384
    24(31)-Dehydrocarboxyacetylquercinic acid; 24(31)-Dehydrocarboxyacetylquercinic acid CFN96179 127970-62-1 C34H50O7 = 570.8 5mg QQ客服:2159513211
    齿孔酸; 齿孔菌酸; Eburicoic acid CFN90414 560-66-7 C31H50O3 = 470.73 10mg QQ客服:3257982914
    土莫酸; Tumulosic acid CFN95399 508-24-7 C31H50O4 = 486.7 5mg QQ客服:1148253675
    茯苓酸; 茯灵酸; Pachymic acid CFN99590 29070-92-6 C33H52O5 = 528.76 20mg QQ客服:2932563308
    二氢齿孔酸; Dehydroeburicoic acid CFN92740 6879-05-6 C31H48O3 = 468.7 5mg QQ客服:2932563308
    去氢土莫酸; Dehydrotumulosic acid CFN92837 6754-16-1 C31H48O4 = 484.7 5mg QQ客服:215959384
    去氢茯苓酸; Dehydropachymic acid CFN92742 77012-31-8 C33H50O5 = 526.8 10mg QQ客服:2159513211
    3-表去氢土莫酸; 3-Epidehydrotumulosic acid CFN92743 167775-54-4 C31H48O4 = 484.7 5mg QQ客服:1148253675





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