Swertianolin
(Synonyms: 当药醇甙) 目录号 : GC38982
Swertianolin 是可从Gentianella Acuta 分离得到的一种黄酮，能够抑制乙酰胆碱酯酶。Swertianolin 还具有抗 HBV 和抗菌活性。
Cas No.:23445-00-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Swertianolin, a xanthone isolated from Gentianella Acuta, inhibits acetylcholinesterase (AChE). Swertianolin also exhibits anti-HBV and anti-bacterial activity[1][2].
[1]. Urbain A, et al. Xanthones from Gentiana campestris as new acetylcholinesterase inhibitors. Planta Med. 2004 Oct;70(10):1011-4. [2]. Xiu-Qiao Zhang, et al. Anti-HBV Activities of Xanthones From Swertia Punicea Hemsl. N A J Med Sci. 2014;7(2):72-74.
| Cas No. | 23445-00-3 | SDF | |
| 别名 | 当药醇甙 | ||
| Canonical SMILES | O=C1C2=C(OC3=C1C(O[C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)=CC=C3O)C=C(OC)C=C2O | ||
| 分子式 | C20H20O11 | 分子量 | 436.37 |
| 溶解度 | Soluble in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2916 mL | 11.4582 mL | 22.9163 mL |
| 5 mM | 0.4583 mL | 2.2916 mL | 4.5833 mL |
| 10 mM | 0.2292 mL | 1.1458 mL | 2.2916 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Swertianolin ameliorates immune dysfunction in sepsis via blocking the immunosuppressive function of myeloid- derived suppressor cells
Eur J Histochem 2021 Sep 1;65(3):3292.PMID:34468107DOI:10.4081/ejh.2021.3292.
In this study, we studied the long-term proliferation trajectory of myeloid-derived suppressor cells (MDSCs) in murine sepsis model and investigated whether Swertianolin could modulate the immunosuppressive function of MDSCs. A murine sepsis model was established by cecal ligation and perforation (CLP), according to the Minimum Quality Threshold in Pre-Clinical Sepsis Studies (MQTiPSS) guidelines. The bone marrow and spleen of the mice were collected at 24 h, 72 h, 7 and 15 d after sepsis induction. The proportions of monocytic-MDSCs (M-MDSCs; CD11b+LY6G-LY6Chi) and granulocytic-MDSCs (G-MDSC, CD11b+ Ly6G+ Ly6Clow) were analyzed by flow cytometry. Then, we have investigated whether Swertianolin could modulate the immunosuppressive function of MDSCs in in vitro experiments. G-MDSCs and M-MDSCs increased acutely after sepsis with high levels sustained over a long period of time. G-MDSCs were the main subtype identified in the murine model of sepsis with polymicrobial peritonitis. Furthermore, it was found that Swertianolin reduced significantly interleukin-10 (IL-10), nitric oxide (NO), reactive oxygen species (ROS), and arginase production in MDSCs, while reducing MDSC proliferation and promoting MDSC differentiation into dendritic cells. Swertianolin also improved T-cell activity by blocking the immunosuppressive effect of MDSCs. Both subsets of MDSCs significantly increased in the bone marrow and spleen of the mice with sepsis, with G-MDSCs being the main subtype identified. Swertianolin effectively regulated the functions of MDSCs and reduced immune suppression.
Determination of Swertianolin in rat plasma by LC-MS/MS and its application to a pharmacokinetic study
Biomed Chromatogr 2014 Oct;28(10):1418-22.PMID:24687287DOI:10.1002/bmc.3184.
A sensitive and rapid LC-MS/MS method has been developed and validated for quantifying Swertianolin in rat plasma using rutin as an internal standard (IS). Following liquid-liquid extraction with ethyl acetate, chromatographic separation for Swertianolin was achieved on a C18 column with a gradient elution using 0.1% formic acid as mobile phase A and acetonitrile as mobile phase B at a flow rate of 0.3 mL/min. The detection was performed on a tandem mass spectrometer using multiple reaction monitoring via an electrospray ionization source and operating in the negative ionization mode. The optimized mass transition ion pairs (m/z) for quantitation were 435.1/272.0 for Swertianolin and 609.2/300.1 for IS. The lower limit of quantitation was 0.5 ng/mL within a linear range of 0.5-500 ng/mL. Intra-day and inter-day precision was less than 6.8%. The accuracy was in the range of -13.9 to 12.0%. The mean recovery of Swertianolin was >66.7%. The proposed method was successfully applied in evaluating the pharmacokinetics of Swertianolin after an oral dose of 50 mg/kg Swertia mussotii extract in rats.
Xanthone Biosynthetic Pathway in Plants: A Review
Front Plant Sci 2022 Apr 8;13:809497.PMID:35463410DOI:10.3389/fpls.2022.809497.
Xanthones are secondary metabolites rich in structural diversity and possess a broad array of pharmacological properties, such as antitumor, antidiabetic, and anti-microbes. These aromatic compounds are found in higher plants, such as Clusiaceae, Hypericaceae, and Gentianaceae, yet their biosynthetic pathways have not been comprehensively updated especially within the last decade (up to 2021). In this review, plant xanthone biosynthesis is detailed to illuminate their intricacies and differences between species. The pathway initially involves the shikimate pathway, either through L-phenylalanine-dependent or -independent pathway, that later forms an intermediate benzophenone, 2,3',4,6-tetrahydoxybenzophenone. This is followed by a regioselective intramolecular mediated oxidative coupling to form xanthone ring compounds, 1,3,5-trihydroxyxanthone (1,3,5-THX) or 1,3,7-THX, the core precursors for xanthones in most plants. Recent evidence has shed some lights onto the enzymes and reactions involved in this xanthone pathway. In particular, several biosynthetic enzymes have been characterized at both biochemical and molecular levels from various organisms including Hypericum spp., Centaurium erythraea and Garcinia mangostana. Proposed pathways for a plethora of other downstream xanthone derivatives including Swertianolin and gambogic acid (derived from 1,3,5-THX) as well as gentisin, hyperixanthone A, α-mangostin, and mangiferin (derived from 1,3,7-THX) have also been thoroughly covered. This review reports one of the most complete xanthone pathways in plants. In the future, the information collected here will be a valuable resource for a more directed molecular works in xanthone-producing plants as well as in synthetic biology application.
The hepatoprotective effect and chemical constituents of total iridoids and xanthones extracted from Swertia mussotii Franch
J Ethnopharmacol 2014 May 28;154(1):259-66.PMID:24746481DOI:10.1016/j.jep.2014.04.018.
Ethnopharmacological relevance: Total iridoids and xanthones (TIXS) were extracted from Swertia mussotii Franch, one of the most important eight Tibetan medicines in China, which was recorded in the book of Jingzhu Bencao and used for clinical treatment of cholestatic hepatitis for many years. Our aim was to study the hepatoprotective effect and chemical constituents of the TIXS. Materials and methods: Crude extracts were prepared using 90% ethanol, and individual fractions were collected following HPD-300 macroporous resin column chromatography. HPLC/MS was applied to qualitatively and quantitatively analyze the TIXS. Then, the alpha-naphthylisot hiocyanate-induced liver damage model was used to assess the hepatoprotective effect of the TIXS. Results: A total of 12 compounds were identified by the fingerprint chromatography of the TIXS, and swertiamarin and Swertianolin were shown to be its two main components. Oral administration of the TIXS at a dose of 35, 70 or 140 mg kg(-1), swertiamarin at a dose of 20 mg kg(-1) or Swertianolin at a dose of 20 mg kg(-1), for 7 days in mice significantly reduced the alpha-naphthylisot hiocyanate-induced levels of alanine aminotransferase, aspartate aminotransferase and the total and direct bilirubins, and increased the bile flow (P<0.01). Conclusion: These findings suggest that the TIXS exhibits significant hepatoprotective effect in the liver damage model induced by alpha-naphthylisot hiocyanate. Its active constituents include swertiamarin and Swertianolin.
Determination and pharmacokinetic study of four xanthones in rat plasma after oral administration of Gentianella acuta extract by UHPLC-ESI-MS/MS
J Ethnopharmacol 2015 Nov 4;174:261-9.PMID:26297839DOI:10.1016/j.jep.2015.08.023.
Ethnopharmacological relevance: Gentianella acuta (Michx.) Hulten belonging to the family of Gentianaceae is an annual plant mainly distributed in north of China, Mongolia plateau, Siberia and Far East areas of Russia. The whole herb was used as folk medicine to treat hepatitis, jaundice, headache and fever in Mongolia native medicine. Xanthones are the main active compounds of G. acuta and possess a lot of pharmacological and biological activities Aim of the study: A selective and sensitive UHPLC-MS/MS method was developed and validated for the determination and pharmacokinetic study of Swertianolin, norswertianolin, bellidifolin and demethylbellidifolin (DMB) in rat plasma after oral administration of G. acuta extract. Materials and methods: Sample preparation involved a liquid-liquid extraction of the analytes with ethyl acetate. Butylparaben was employed as an internal standard. LC separation was achieved on an Agilent SB-C18 RRHD column (1.8 μm, 150 mm × 2.1 mm) at 30°C with an isocratic mobile phase consisting of acetonitrile-water (0.1% formic acid) (90:10, v/v). The detection was accomplished by multiple-reaction monitoring (MRM) scanning with electrospray ionization (ESI) source operating in the negative ionization mode. The optimized mass transition ion-pairs (m/z) monitored for Swertianolin, norswertianolin, bellidifolin, DMB and I.S. were 435.1/272.0, 420.8/258.9, 273.0/258.0, 258.9/214.9 and 193.0/92.0, respectively. Results: The current UHPLC-MS/MS assay was validated for linearity, intra-day and inter-day precisions, accuracy, extraction recovery and stability and was suitable for pharmacokinetic studies of the four xanthones after oral administration of G. acuta extract. The time to reach the maximum plasma concentration (Tmax) was 0.40 ± 0.12 h for Swertianolin, 0.27 ± 0.07 h for norswertianolin, 1.00 ± 0.18 h for bellidifolin and 0.94 ± 0.15 h for demethylbellidifolin. The elimination half-time (t1/2) of Swertianolin, norswertianolin, bellidifolin and DMB, was 19.7 ± 9.64 h, 11.3 ± 4.51 h, 19.9 ± 8.11 h and 24.9 ± 8.19 h, respectively. Conclusion: This study described a simple, sensitive and validated UHPLC-MS/MS method for simultaneous determination of four xanthones in rat plasma after oral administration of G. acuta extract, and investigated on their pharmacokinetic studies as well.