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Tubeimoside I

Alias: Tubeimoside A; Tubeimoside-I; Tubeimoside I
Cat No.:V16925 Purity: ≥98%
Tubeimoside I is an extract of the traditional Chinese medicine Fritillaria fritillary, which has been proven to be an effective anti-tumor agent against a variety of cancers in humans.
Tubeimoside I
Tubeimoside I Chemical Structure CAS No.: 102040-03-9
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
Other Sizes
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Product Description
Tubeimoside I is an extract of the traditional Chinese medicine Fritillaria fritillary, which has been proven to be an effective anti-tumor agent against a variety of cancers in humans.
Tubeimoside I (CAS#: 102040-03-9) is a natural triterpenoid saponin originally isolated from the plant Bolbostemma paniculatum. It is an orally active compound that exhibits a broad range of pharmacological activities, including anticancer, anti-inflammatory, antiviral, and chemopreventive effects. Tubeimoside I has been shown to inhibit HSPD1, NF-κB, and MAPK signaling, as well as regulate eNOS-VEGF and induce cytoprotective autophagy. It is a potent apoptosis-inducing agent for various cancer cell lines.
Biological Activity I Assay Protocols (From Reference)
Targets
Tubeimoside I has multiple molecular targets. It is an orally active HSPD1 (heat shock protein family D member 1) inhibitor. It also inhibits NF-κB and MAPK signaling pathways, and regulates the eNOS-VEGF pathway. Furthermore, it has been reported to bind to tubulin at the colchicine site, inhibiting microtubule polymerization. This multi-targeting ability contributes to its diverse pharmacological effects, including the induction of apoptosis and autophagy.
ln Vitro
In vitro, tubeimoside I demonstrates potent anticancer activity against a wide range of cancer cell lines, including those from liver, lung, colorectal, cervical, breast, and nasopharyngeal cancers. It induces cytoprotective autophagy in human breast cancer cells via an Akt-mediated pathway. It also inhibits the viability of cervical cancer and colon cancer cells in a dose-dependent manner. Additionally, it attenuates LPS-induced inflammation in RAW 264.7 cells by inhibiting the production of pro-inflammatory cytokines like TNF-α, IL-6, and IL-1β.
ln Vivo
In vivo, tubeimoside I has shown significant anti-tumor efficacy in mouse xenograft models. Intraperitoneal administration inhibited the growth of tumors in nude mice without causing a decrease in body weight. It also reduced lung injury and down-regulated the secretion of inflammatory cytokines in a murine model of LPS-induced acute lung injury. Oral administration has also been shown to attenuate inflammation and oxidative damage in mice.
Enzyme Assay
In vitro enzyme or receptor binding (non-cell) assays for tubeimoside I involve studying its interaction with purified proteins. For example, its inhibition of HSPD1 can be measured using a biochemical assay where the chaperone activity of HSPD1 is monitored in the presence of the compound. Its binding to tubulin at the colchicine site can be assessed using a competition binding assay with [³H]colchicine. The activity of kinases in the NF-κB or MAPK pathways can also be tested using purified enzymes and specific peptide substrates.
Cell Assay
In vitro cell-based assays for tubeimoside I are performed using various cancer cell lines. Cells are treated with the compound at different concentrations for 24 to 72 hours. Cell viability is measured using MTT or CCK-8 assays. Apoptosis is detected using Annexin V/PI staining, and cell cycle analysis is performed using flow cytometry. Autophagy is assessed by detecting LC3-II conversion and p62 degradation via Western blotting. Inflammatory responses are evaluated by measuring cytokine levels in the culture medium using ELISA.
Animal Protocol
In vivo animal experiments for tubeimoside I are conducted using mouse models. For tumor growth studies, immunodeficient mice are subcutaneously implanted with cancer cells and then treated with tubeimoside I intraperitoneally or orally. Tumor size and weight are measured. In models of inflammation, such as LPS-induced acute lung injury, mice are treated with the compound before the LPS challenge, and lung tissues are analyzed for inflammatory cell infiltration and cytokine levels.
ADME/Pharmacokinetics
Pharmacokinetic (PK) properties of tubeimoside I indicate it is orally active. The compound has a large molecular weight (1319.43) and is a triterpenoid saponin, which may affect its absorption and bioavailability. It is soluble in DMSO and is typically stored as a powder at -20°C. Detailed PK parameters, such as half-life and volume of distribution, are determined in animal studies via LC-MS/MS analysis of plasma samples.
Toxicity/Toxicokinetics
Toxicology (toxicology) data for tubeimoside I are limited but suggest it is relatively safe at therapeutic doses. In animal studies, no significant decrease in body weight was observed in mice treated with the compound at doses up to 4 mg/kg intraperitoneally. However, as a saponin, it may cause hemolysis, and its safety profile requires thorough evaluation in long-term toxicology studies.
References

[1]. Natural plant extract tubeimoside I promotes apoptosis-mediated cell death in cultured human hepatoma (HepG2) cells. Biol Pharm Bull. 2011;34(6):831-8.

[2]. Intrinsic apoptotic pathway and G2/M cell cycle arrest involved in tubeimoside I-induced EC109 cell death. Chin J Cancer Res. 2013 Jun;25(3):312-21.

[3]. Tubeimoside-1 attenuates LPS-induced inflammation in RAW 264.7 macrophages and mouse models. Immunopharmacol Immunotoxicol. 2013 Aug;35(4):514-23.

[4]. Tubeimoside I sensitizes cisplatin in cisplatin-resistant human ovarian cancer cells (A2780/DDP) through down-regulation of ERK and up-regulation of p38 signaling pathways. Mol Med Rep. 2011 Sep-Oct;4(5):985-92.

[5]. Tubeimoside-1 induces G2/M phase arrest and apoptosis in SKOV-3 cells through increase of intracellular Ca2+ and caspase-dependent signaling pathways. Int J Oncol. 2012 Feb;40(2):535-43.

Additional Infomation
Other information: Tubeimoside I is a natural product derived from Bolbostemma paniculatum and is used as a research reagent. It has been studied for its potential in treating inflammatory diseases, various cancers, sepsis, and ischemic diseases. Its multi-targeting mechanism and ability to induce both apoptosis and autophagy make it a promising lead compound for drug development.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C63H98O29
Molecular Weight
1319.44
Exact Mass
1318.619
CAS #
102040-03-9
PubChem CID
3034097
Appearance
White to off-white solid powder
Density
1.5±0.1 g/cm3
Index of Refraction
1.637
LogP
6.38
Hydrogen Bond Donor Count
15
Hydrogen Bond Acceptor Count
29
Rotatable Bond Count
18
Heavy Atom Count
92
Complexity
2710
Defined Atom Stereocenter Count
31
SMILES
[C@@]12(CCC(C)(C)C[C@@]1([H])C1=CC[C@]3([H])[C@@]4(C)C[C@@H]([C@@H]5O[C@@H]6O[C@@H]([C@@H](O)[C@H](O)[C@H]6O[C@@H]6OC[C@H](O)[C@H](O)[C@H]6OC(=O)CC(O)(C)CC(=O)OC[C@@]5(C)[C@]4([H])CC[C@@]3(C)[C@]1(C)CC2)CO)O)C(=O)O[C@@H]1OC[C@H](O)[C@H](O)[C@H]1O[C@@H]1O[C@H]([C@H](O)[C@@H](O[C@@H]2OC[C@@H](O)[C@H](O)[C@H]2O)[C@H]1O)C
Synonyms
Tubeimoside A; Tubeimoside-I; Tubeimoside I
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~75.79 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (1.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.7579 mL 3.7895 mL 7.5790 mL
5 mM 0.1516 mL 0.7579 mL 1.5158 mL
10 mM 0.0758 mL 0.3789 mL 0.7579 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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