Swertiajaponin
(Synonyms: 日当药黄素) 目录号 : GC37707
Swertiajaponin 是一种酪氨酸酶抑制剂，与酪氨酸酶结合囊形成多个氢键和疏水相互作用，IC50 值为 43.47 μM。Swertiajaponin 还能通过抑制氧化应激介导的 MAPK/MITF 信号导致酪氨酸酶蛋白水平下降。Swertiajaponin 能抑制黑色素积累，具有较强的抗氧化活性。
Cas No.:6980-25-2
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
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity[1]. IC50: 43.47 μM (tyrosinase)[1]
[1]. Lee B, et al. Swertiajaponin inhibits skin pigmentation by dual mechanisms to suppress tyrosinase. Oncotarget. 2017 Sep 15;8(56):95530-95541.
| Cas No. | 6980-25-2 | SDF | |
| 别名 | 日当药黄素 | ||
| Canonical SMILES | O=C1C=C(C2=CC=C(O)C(O)=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 | C22H22O11 | 分子量 | 462.4 |
| 溶解度 | DMSO : 250 mg/mL (540.66 mM; Need ultrasonic) | 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 | 2.1626 mL | 10.8131 mL | 21.6263 mL |
| 5 mM | 0.4325 mL | 2.1626 mL | 4.3253 mL |
| 10 mM | 0.2163 mL | 1.0813 mL | 2.1626 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。
Swertiajaponin as an anti-browning and antioxidant flavonoid
Food Chem 2018 Jun 30;252:207-214.PMID:29478533DOI:10.1016/j.foodchem.2018.01.053.
Enzymatic browning is a major issue that needs to be solved in the food industry. Although Swertiajaponin is a flavonoid rich in the whole herb of Swertia japonica that has been clinically used, its biological functions and application in the foods have not been fully elucidated. Here, we showed that Swertiajaponin efficiently blocked enzymatic browning in potatoes possibly by direct binding to and inactivating polyphenol oxidase. Furthermore, Swertiajaponin showed potent antioxidant activity proven by markedly suppressed reactive oxygen species. Swertiajaponin significantly increased antioxidant properties of potato extract when it is added since it additively elevated total flavonoid content. Considering numerous beneficial effects of antioxidants, Swertiajaponin may be used as a functional food additive to suppress enzymatic browning and elevate the antioxidant capacity of foods including beverages and soups by fortification of flavonoids.
Swertiajaponin inhibits skin pigmentation by dual mechanisms to suppress tyrosinase
Oncotarget 2017 Sep 15;8(56):95530-95541.PMID:29221146DOI:10.18632/oncotarget.20913.
Many skin-whitening compounds target tyrosinase because it catalyzes two rate-limiting steps in melanin synthesis. Although many tyrosinase inhibitors are currently available for a skin-whitening purpose, undesirable adverse effects are also reported. Thus, numerous efforts have been made to develop safer tyrosinase inhibitors from natural products. In line with this, we tested fifty flavonoids, a group of naturally occurring antioxidants and metal chelators, and screened Swertiajaponin as the strongest tyrosinase inhibitor in cell-free experiments. Swertiajaponin did not show cytotoxicity in B16F10, HaCat, and Hs27 cells and exhibited strong anti oxidative activity in experiments using the cell-free system and B16F10 cells. It markedly inhibited αMSH- or UVB-induced melanin accumulation in B16F10 cells and suppressed skin pigmentation in a human skin model. As underlying mechanisms, in silico and Lineweaver-Burk plot analyses exhibited that Swertiajaponin may directly bind to and inhibit tyrosinase activity by forming multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase. In addition, western blotting results indicated that Swertiajaponin inhibited oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Together, Swertiajaponin suppresses melanin accumulation by inhibiting both activity and protein expression levels of tyrosinase. Thus, it would be a novel additive for whitening cosmetics.
Identification of PTP1B regulators from Cymbopogon citratus and its enrichment analysis for diabetes mellitus
In Silico Pharmacol 2021 Apr 11;9(1):30.PMID:33928007DOI:10.1007/s40203-021-00088-9.
PTP1B is identified as the insulin signaling pathway downregulator; involved in pancreatic β-cell apoptosis. Further, it associates in regulating multiple pathways in diabetes mellitus; kindled us to identify the binding affinity of bioactives from Cymbopogon citratus by targeting PTP1B and identify the probably associated with it; further identifying the probable pathways involved in diabetes mellitus. In this regard, ChEBI database was used to retrieve bio-actives from C. citrates and 3D structures for the same were obtained from the PubChem database. The energy of bioactives was minimized and converted into ligand and the docking was carried using autodock 4.0 against PTP1B. Further, multiple characters of bio-actives like drug-likeness score, ADMET profile, probable adverse effects, and boiled egg model for bioavailability were also studied. Swertiajaponin was predicted for the highest drug-likeness score i.e. 0.26. However, Swertiajaponin was predicted with the highest probable side effect of nephrotoxicity with pharmacological activity of 0.478. Similarly, Swertiajaponin was predicted for the highest binding affinity with PTP1B with the binding energy of - 8.3 kcal/mol. Likewise, KEGG identified 80 pathways associated with PTP1B modulation in which 7 pathways were involved in diabetes mellitus in which FoxO signaling pathway was predicted to have the least false discovery rate by modulating 7 genes. Swertiajaponin could act as the potent inhibitor of PTP1B; scored highest druglikeness score but possessed minimum GIT absorptivity; further, PTP1B was identified to be linked with multiple pathways that are concerned with diabetes mellitus.
Simultaneous Determination of 10 Bioactive Components of Lophatherum gracile Brongn by HPLC-DAD
J Chromatogr Sci 2015 Jul;53(6):963-7.PMID:25527702DOI:10.1093/chromsci/bmu160.
A high-performance liquid chromatography method coupled with diode array detection (HPLC-DAD) was developed for simultaneous determination of two coumarins and eight flavonoids in Lophatherum gracile Brongn (Gramineae), namely 5-O-coumaroylquinic acid (i), 4-O-coumaroylquinic acid (ii), luteolin 6-C-β-d-galactopyranosiduronic acid (1→2)-β-d-glucopyranoside (iii), 7-O-β-d-glucopyranosyl-6-C-α-l-arabinopy ranoside (iv), isoorientin (v), Swertiajaponin (vi), luteolin 6-C-β-d-galactopyranosiduronic acid (1→2)-α-l-arabinopyranoside (vii), Saponaretin (viii), swertisin (ix) and apigenin 6-C-β-d-galactopyranosiduronic acid (1→2)-α-l-arabinopyranoside (x). The analysis was performed on Cosmosil MS-IIⅡ C18 column (250 × 4.6 mm, 5 µm) with gradient elution of 0.1% aqueous acetic acid and acetonitrile. The detection wavelength was 330 nm. The developed method was able to determine the bioactive compounds with excellent resolution, precision and recovery. The validated method was successfully applied for the analysis of the 10 bioactive compounds in n samples from different cultivated regions. The results indicated that the developed method can be used as a suitable quality control method for L. gracile.
Genotoxic Maillard byproducts in current phytopharmaceutical preparations of Echinodorus grandiflorus
An Acad Bras Cienc 2014 Sep;86(3):1385-94.PMID:25098311DOI:10.1590/0001-3765201420130065.
Extracts of Echinodorus grandiflorus obtained from dried leaves by three different techniques were evaluated by bacterial lysogenic induction assay (Inductest) in relation to their genotoxic properties. Before being added to test cultures, extracts were sterilized either by steam sterilization or ultraviolet light. Only the extracts prepared by infusion and steam sterilized have shown genotoxic activity. The phytochemical analysis revealed the presence of the flavonoids isovitexin, isoorientin, swertisin and Swertiajaponin, isolated from a genotoxic fraction. They were assayed separately and tested negative in the Inductest protocol. The development of browning color and sweet smell in extracts submitted to heat, prompted further chemical analysis in search for Maillard's reaction precursors. Several aminoacids and reducing sugars were cast in the extract. The presence of characteristic Maillard's melanoidins products was determined by spectrophotometry in the visible region and the inhibition of this reaction was observed when its characteristic inhibitor, sodium bisulfite, was added prior to heating. Remarkably, this is the first paper reporting on the appearance of such compounds in a phytomedicine preparation under a current phytopharmaceutical procedure. The genotoxic activity of such heat-prepared infusions imply in some risk of developing degenerative diseases for patients in long-term, uncontrolled use of such phytomedicines.