Pseudoprotodioscin
(Synonyms: 伪原薯蓣皂苷) 目录号 : GC38839
A steroidal saponin with diverse biological activities
Cas No.:102115-79-7
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
Pseudoprotodioscin is a steroidal saponin that has been found in D. panthaica and has diverse biological activities.1,2,3 It is cytotoxic to A375, L929, and HeLa cancer cells (IC50s = 5.73, 5.09, and 3.32 ?M, respectively).1 Pseudoprotodioscin (2 ?M) increases nuclear accumulation of estrogen receptor α (ERα) in 3T3-L1 preadipocytes cultured in differentiation medium.2 It inhibits LPS-induced increases in NF-κB activity in reporter assays using isolated mouse peritoneal macrophages and human umbilical vein endothelial cells (HUVECs) when used at a concentration of 2.5 ?M.3 Pseudoprotodioscin (1, 2.5, and 5 mg/kg) reduces atherosclerotic plaque area and inhibits increases in serum total cholesterol and triglyceride levels in ovariectomized ApoE-/- mice fed a high-cholesterol diet.
1.Dong, M., Feng, X.-Z., Wu, L.-J., et al.Two new steroidal saponins from the rhizomes of Dioscorea panthaica and their cytotoxic activityPlanta Med.67(9)853-857(2001) 2.Xiao, J., Wang, N.-L., Sun, B., et al.Estrogen receptor mediates the effects of pseudoprotodiocsin on adipogenesis in 3T3-L1 cellsAm. J. Physiol. Cell Physiol.299(1)C128-C138(2010) 3.Sun, B., Yang, D., Yin, Y.-Z., et al.Estrogenic and anti-inflammatory effects of pseudoprotodioscin in atherosclerosis-prone mice: Insights into endothelial cells and perivascular adipose tissuesEur. J. Pharmacol.869172887(2020)
| Cas No. | 102115-79-7 | SDF | |
| 别名 | 伪原薯蓣皂苷 | ||
| 分子式 | C51H82O21 | 分子量 | 1031.18 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,PBS (pH 7.2): 5 mg/ml | 储存条件 | Store at -20°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 | 0.9698 mL | 4.8488 mL | 9.6976 mL |
| 5 mM | 0.194 mL | 0.9698 mL | 1.9395 mL |
| 10 mM | 0.097 mL | 0.4849 mL | 0.9698 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。
Microbial transformation of Pseudoprotodioscin by Gibberella fujikuroi
J Asian Nat Prod Res 2018 Jul;20(7):624-632.PMID:29732923DOI:10.1080/10286020.2018.1468438.
Three new (6, 9, and 12) and nine known steroidal saponins were obtained from the fermentation broth of Pseudoprotodioscin (PPD) incubated with a fungus Gibberella fujikuroi CGMCC 3.4663. Structures of the metabolites were elucidated by 1-D (1H, 13C), 2-D (HMBC, HSQC, NOESY) NMR, and HR-MS analyses. The biotransformation pathway of Pseudoprotodioscin by Gibberella fujikuroi CGMCC 3.4663 was proposed. Compounds 1-11 were tested in vitro for their cytotoxic activities against two human cancer cell lines (HepG2 and Hela). Compounds 1, 6, 9, and 10 exhibited cytotoxic activity against HepG2 cells. Compound 10 exhibited cytotoxicity to Hela cells.
Pseudoprotodioscin inhibits SREBPs and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides
Fitoterapia 2019 Nov;139:104393.PMID:31669721DOI:10.1016/j.fitote.2019.104393.
The extract of Dioscorea zingiberensis C.H. Wright rhizomes is found to be effective in the therapy of cardiovascular disease. Steroidal saponins make substantial contribution. Previous study has proposed that methylprotodioscin (MP) may promote cholesterol efflux by increasing ABCA1 expression. But the other main saponins ingredients are not referred to. The aim of the present work was to reveal the effect and mechanism of protodioscin (PD), MP and Pseudoprotodioscin (PPD) on the synthesis-related gene expression of cholesterol and triglycerides. MTT assay apoptosis assay with annexin AV-APC and 7-AAD double staining were performed. MicroRNA assay and qRT-PCR were used to analyze the gene expression which regulates synthesis of cholesterol and triglycerides. Western blot was to demonstrate the levels of target proteins. Cholesterol efflux assay was executed to study the stimulative effect of saponins on cholesterol efflux. In Hep G2 cells, PPD increased ABCA1 protein and mRNA levels, and promoted the effluxion of ApoA-1-mediated cholesterol. The underlying mechanisms involved that PPD inhibited SREBP1c and SREBP2 transcription by decreasing microRNA 33a/b levels. This procedure reciprocally led to the increase of ABCA1 levels. In THP-1 macrophages, PPD showed the similar effect, which reduced HMGCR, FAS and ACC mRNA levels and promoted low density lipoprotein receptor by decreasing the PCSK9 levels. These studies demonstrated that PPD is a potential agent for cholesterol efflux, SREBPs and microRNA 33a/b inhibition, which related to the gene expression for the synthesis of cholesterol and triglycerides.
Microbial metabolism of Pseudoprotodioscin
Planta Med 2004 Jul;70(7):637-41.PMID:15254856DOI:10.1055/s-2004-827187.
Microbial transformation of the furostanol saponin Pseudoprotodioscin ( 1) using Aspergillus fumigatus resulted in the isolation of two new steroidal metabolites, 3- O-[bis- alpha- L-rhamnopyranosyl-(1-->2 and 1-->4)- beta- D-glucopyranosyl]-22 R,25 R-spirost-5-ene-3 beta,20 alpha-diol ( 2) and 3- O-[bis- alpha- L-rhamnopyranosyl-(1-->2 and 1-->4)- beta- D-glucopyranosyl]-25 R-furost-5-ene-3 beta,22 alpha,26-triol ( 3), in addition to the previously reported steroidal saponins: dioscin ( 4) and progenin II ( 5). The structure elucidation of these metabolites was based primarily on 1D and 2D NMR analyses. Metabolites 2 - 5 showed significant cytotoxicity against cancer cell lines A375, L929, and HeLa with IC (50) values ranging from 1.18 microM to 17.88 microM.
Protective effect of Di'ao Xinxuekang capsule against doxorubicin-induced chronic cardiotoxicity
J Ethnopharmacol 2022 Apr 6;287:114943.PMID:34954266DOI:10.1016/j.jep.2021.114943.
Ethnopharmacological relevance: Di'ao Xinxuekang capsule (DXXK) extracted from Dioscorea nipponica Makino is a well-known traditional Chinese herbal medicinal product widely used in the treatment of cardiovascular disease, such as myocardial ischemia and arrhythmia. The active ingredients of DXXK were also traditionally utilized for treating cardiovascular disease in the former Soviet Union after the 1960s. As a specific type of cardiovascular disease, doxorubicin (DOX)-induced cardiotoxicity is characterized by arrhythmia, myocardial ischemia, and heart failure. Aim of the study: This study aimed to investigate the potential protective effect of DXXK against chronic cardiotoxicity induced by DOX. Materials and methods: A mouse model of chronic cardiotoxicity induced by DOX and an in vitro model of DOX-induced myocardial damage were created to assess the protective effect of DXXK. Cardiac functional parameters, serum levels of CK-MB and LDH and cardiac histopathological indicators were determined in the mouse model. Moreover, cell viability was measured by the MTT method, and the effect of DXXK on the anticancer activity of DOX was also investigated by utilizing 4T1, HepG2, and H460 cell lines. Furthermore, the levels of markers of oxidative stress indexes (SOD, GSH, MDA) and inflammation (TNF-α, IL-1α) were measured using biochemical and Elisa kits, respectively. The level of ROS in H9c2 cardiomyocyte was determined by flow cytometry. The protein expression levels of HIF-1α and NF-κB p65 were measured by western blotting. Finally, molecular docking was performed to visualize the patterns of interactions between the effective molecule and targeted protein. Results: DXXK alleviated DOX-induced chronic cardiotoxicity as shown by the reversal of changes in levels of myocardial enzymes and left ventricular function and structure. DXXK exhibits antioxidant and anti-inflammatory activities. We also observed that DXXK might increase the protein expression level of HIF-1α and decrease the protein expression level of NF-κB p65. Further results of in vitro experiments showed that DXXK could protect cardiomyocyte against DOX-induced production of ROS, but DXXK had no effect on the anticancer activity of DOX. The results of molecular docking showed that dioscin and Pseudoprotodioscin were the top two compounds of DXXK, which had high affinity with HIF-1α and NF-κB p65. Conclusions: Our results indicated that DXXK could protect against cardiotoxicity induced by DOX and alleviate oxidative stress and inflammation in vivo and in vitro via the regulation of HIF-1α and down NF-κB p65.
Determination of Pseudoprotodioscin in rat plasma by UPLC-MS/MS: Assay development and application to pharmacokinetic study
J Chromatogr B Analyt Technol Biomed Life Sci 2016 Jul 15;1026:97-104.PMID:26012509DOI:10.1016/j.jchromb.2015.05.004.
An original and sensitive ultraperformance liquid chromatography-tandem mass spectrometric (UPLC-MS/MS) method for the determination of Pseudoprotodioscin (PPD) in rat plasma was developed and validated. Digitoxin was applied as an internal standard. Plasma samples were processed by acetonitrile-mediated plasma protein precipitation and chromatographed using a step gradient program on a C18 column (2.1×50mm i.d., 1.7μm). The mobile phase was comprised of acetonitrile and 0.1mmolL(-1) aqueous lithium acetate mixed with 0.03% formic acid at the flow rate of 0.2mLmin(-1). Multiple reaction monitoring (MRM) transitions were performed for detection and lithium adduct ions were employed with a significant improvement of the response of the analytes in electrospray positive ionization mode. The concentration range of calibration curve was linear over the range 2-5000ngmL(-1). The intra- and inter-day precisions were all less than 11.5% and accuracies were within the range of 94.1-103.5%, and the analytes exhibited no severe matrix effect. The validated method was successfully applied in the pharmacokinetics of PPD after intragastric (50mgkg(-1)) and intravenous (4mgkg(-1)) administration in rats. PPD showed rapid excretion and with bioavailability of simply about 5.7% in rats.