Swertisin
(Synonyms: 当药黄素) 目录号 : GC37708
A flavonoid C-glycoside with diverse biological activities
Cas No.:6991-10-2
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
Swertisin is a flavonoid C-glycoside that has been found in Swertia japonica and has diverse biological activities.1,2,3 It inhibits sodium-glucose cotransporter 2 (SGLT2) in HEK293 cells when used at a concentration of 7.5 ?g/ml and is an adenosine A1 receptor antagonist (IC50 = 137 ?M).1,2 Swertisin (0.2-5 ?M) inhibits hepatitis B virus (HBV) replication in HepG2 2.2.15 cells.3 It decreases blood glucose levels in a mouse model of diabetes induced by streptozotocin , as well as prevents scopolamine-induced increases in escape latency in the Morris water maze in mice.1,2
1.Bhardwaj, G., Vakani, M., Srivastava, A., et al.Swertisin, a novel SGLT2 inhibitor, with improved glucose homeostasis for effective diabetes therapyArch. Biochem. Biophys.710108995(2021) 2.Lee, H.E., Jeon, S.J., Ryu, B., et al.Swertisin, a C-glucosylflavone, ameliorates scopolamine-induced memory impairment in mice with its adenosine A1 receptor antagonistic propertyBehav. Brain Res.306137-145(2016) 3.Xu, H.-Y., Ren, J.-H., Su, Y., et al.Anti-hepatitis B virus activity of swertisin isolated from Iris tectorum MaximJ. Ethnopharmacol.257112787(2020)
| Cas No. | 6991-10-2 | SDF | |
| 别名 | 当药黄素 | ||
| Canonical SMILES | O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(OC)=C([C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)C(O)=C13 | ||
| 分子式 | C22H22O10 | 分子量 | 446.4 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 2.2401 mL | 11.2007 mL | 22.4014 mL |
| 5 mM | 0.448 mL | 2.2401 mL | 4.4803 mL |
| 10 mM | 0.224 mL | 1.1201 mL | 2.2401 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。
Swertisin, a novel SGLT2 inhibitor, with improved glucose homeostasis for effective diabetes therapy
Arch Biochem Biophys 2021 Oct 15;710:108995.PMID:34289381DOI:10.1016/j.abb.2021.108995.
Failing pancreas and subsequent loss of pancreatic β cells worsen diabetic conditions which are further alleviated by the mounting up of glucose levels. Inhibition of sodium glucose cotransporter 2 (SGLT2) in the kidney responsible for glucose reabsorption strikingly reduces blood glucose levels. Bioactive Swertisin showed a promising glucose-lowering effect. Hence, we aimed to mechanistically dissect the glucose lowering property of Swertisin. A systematic in silico, in vitro, and in vivo approach was directed for target analysis of Swertisin. Molecular docking was performed with Swertisn-hSGLT2 complex. Glucose uptake assay and protein expression for SGLT2 and regulatory proteins were performed under Swertisin effect. Various physiological and metabolic parameters were evaluated in STZ induced BALB/c mice using Swertisin treatment. SGLT2 expression was evaluated in the kidney tissue of mice. Swertisn-hSGLT2 molecularly docked complex showed similar binding energy compared to the Canagliflozin-hSGLT2 complex. Swertisin inhibited glucose uptake and decreased expression of SGLT2 in HEK293 cells. Swertisin does not affect GLUT mediated glucose transport. Swertisin treated diabetic mice demonstrated remarkable improvement in overall glucose homeostasis. Reduced expression of SGLT2 was found in kidney tissue along with reduced PKC expression which is one of the key regulators of SGLT2. Our study explored SGLT2 as a selective target of Swertisin for its swift glucose-lowering action which not only inhibits SGLT2 but also reduces its expression in diabetic condition. Thus, the potential property of Swertisin as a glucose-lowering agent is remarkable which points towards the likelihood of a wider avenue of diabetes therapy.
Swertisin dihydrate
Acta Crystallogr C 2004 Dec;60(Pt 12):o893-6.PMID:15579976DOI:10.1107/S0108270104028355.
The title compound, 6-C-glucopyranosyl-7-O-methylapigenin dihydrate, C(22)H(22)O(10).2H(2)O, is a natural C-glucosylflavone. The flavone skeleton is almost planar, the dihedral angle between the pyran moiety and the 4-hydroxyphenyl ring being 9.8 (3) degrees. The basal plane of the pyranosyl ring of the glucose moiety is almost perpendicular to the benzopyran ring system. The flavone skeletons are stacked along the a axis, forming layers parallel to (001). Between these hydrophobic layers, the glucose groups and water molecules of crystallization are connected via O-H...O hydrogen bonds, forming hydrophilic layers.
Swertisin ameliorates pre-pulse inhibition deficits and cognitive impairment induced by MK-801 in mice
J Psychopharmacol 2017 Feb;31(2):250-259.PMID:27729563DOI:10.1177/0269881116672098.
Swertisin, a plant-derived C-glucosylflavone, is known to have antidiabetic, anti-inflammatory and antioxidant effects. In the present study, we investigated in mice the effects of Swertisin on glutamatergic dysfunction induced by dizocilpine (MK-801), a non-competitive N-methyl-D-aspartate receptor antagonist. In the Acoustic Startle Response test, their MK-801-induced (given 0.2 mg/kg i.p.) pre-pulse inhibition deficit was significantly attenuated by the administration of Swertisin (30 mg/kg p.o.). In the Novel Object Recognition Test, the recognition memory impairments that were induced by MK-801 (0.2 mg/kg, given i.p.) were also reversed by administration of Swertisin (30 mg/kg p.o.). In addition, Swertisin normalized the MK-801-induced elevation of phosphorylation levels of Akt and GSK-3β signaling molecules in the prefrontal cortex. These results indicated that Swertisin may be useful in managing the symptoms of schizophrenia, including sensorimotor gating disruption and cognitive impairment, and that these behavioral outcomes may be related to Akt-GSK-3β signaling in the prefrontal cortex.
Ultrasonic-assisted extraction of Swertisin from sour Jujube seed and comprehensive revelation of its antioxidant activity
J Food Biochem 2022 Dec;46(12):e14433.PMID:36198041DOI:10.1111/jfbc.14433.
As a typical flavonoid glycoside, Swertisin mainly exists in sour Jujube seed. In this study, Swertisin was extracted by ultrasound-assisted extraction method optimized with Box-Behnken design and response surface methodology. The antioxidant effect of Swertisin was determined in vitro and in Caenorhabditis elegans (C. elegans). Furthermore, the potential mechanisms of its antioxidant stress were comprehensively evaluated and explored with network pharmacology and molecular docking technology. The results showed obvious scavenging ability of Swertisin on free radical and Swertisin (50, 250, and 500 μmol/L) significantly enhanced antioxidative enzymes activity (GST-4, SOD-3, and GSH-PX ) and reduced the reactive oxygen species and malondialdehyde accumulation in C. elegans, thereby protecting them from oxidative stress (heat stress and hydrogen peroxide). A total of 139 antioxidant targets of Swertisin were screened and 70 signal pathways were enriched, including cancer-related pathways, lipid metabolism, liver injury-related pathways, acute lung injury, nervous system diseases, etc. This study provides the basis for further investigation on the antioxidant stress mechanism and contributes to the development of relevant drugs from natural products. PRACTICAL APPLICATIONS: The imbalance between the antioxidant defense system and reactive oxygen species is one of the main causes of neurodegenerative diseases, cardiovascular diseases, cancer, and aging. Therefore, alleviating oxidative stress injury has become a common strategy, which is helpful for the multi-target treatment of related diseases. The flavonoid of sour Jujube seed possesses potential antioxidant activity with multiple food health effects. From this study results, we optimized ultrasound-assisted extraction method for extracting the Swertisin from sour Jujube seed and supported the use of C. elegans as an in vivo experimental model. We can recommend that the Swertisin as a natural ingredient has a positive effect on antioxidation, which provided a scientific basis for treating related diseases through relevant pharmacological mechanisms and making antiaging functional food formula.
Swertisin, a C-glucosylflavone, ameliorates scopolamine-induced memory impairment in mice with its adenosine A1 receptor antagonistic property
Behav Brain Res 2016 Jun 1;306:137-45.PMID:26996316DOI:10.1016/j.bbr.2016.03.030.
Swertisin, a C-glucosylflavone isolated from Swertia japonica, has been known to have anti-inflammatory or antidiabetic activities. Until yet, however, its cognitive function is not investigated. In the present study, we endeavored to elucidate the effects of Swertisin on cholinergic blockade-induced memory impairment. Swertisin (5 or 10mg/kg, p.o.) significantly ameliorated scopolamine-induced cognitive impairment in the several behavioral tasks. Also, single administration of Swertisin (10mg/kg, p.o.) in normal naïve mice enhanced the latency time in the passive avoidance task. In addition, the ameliorating effect of Swertisin on scopolamine-induced memory impairment was significantly antagonized by a sub-effective dose of N6-cyclopentyladenosine (CPA, 0.1mg/kg, i.p). The adenosine A1 receptor antagonistic property of Swertisin was confirmed by receptor binding assay. Furthermore, the administration of Swertisin significantly increased the phosphorylation levels of hippocampal or cortical protein kinase A (PKA, 5 or 10mg/kg) and CREB (10mg/kg), and co-administration of CPA (0.1mg/kg, i.p) blocked the increased phosphorylated levels of PKA and CREB in the both cortex and hippocampus. Taken together, these results indicate that the memory-ameliorating effects of Swertisin may be, in part, mediated through the adenosinergic neurotransmitter system, and that Swertisin may be useful for the treatment of cognitive dysfunction observed in several diseases such as Alzheimer's disease.