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Diosbulbin B

Catalog No.GC38448 Copy One-Click Copy Product Info

Diosbulbin B is the main hepatotoxic component of Dioscorea bulbifera L., exhibiting potent anti-tumor activity.

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Diosbulbin B Chemical Structure

Cas No.: 20086-06-0

Size Price Stock Qty
1mg
$16.00
In stock
5mg
$35.00
In stock
10mg
$50.00
In stock
25mg
$83.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Diosbulbin B

Diosbulbin B is the main hepatotoxic component of Dioscorea bulbifera L., exhibiting potent anti-tumor activity [1]. Diosbulbin B can significantly induce an increase in liver MPO enzyme activity and protein expression, reduce IκB expression and promote the increase in NF-κB p65 translocation, and lead to an increase in serum levels of TNF-α, IL-6 and IFN-γ[2]. Diosbulbin B has been widely used in establishing animal models of liver injury and inhibiting the tumor growth of xenograft models[3].

In vitro, Diosbulbin B treatment for 72h significantly inhibited the viability of A549 cells and PC-9 cells, with IC50 values of 44.61μM and 22.78μM, respectively[4]. Treatment with 200µM Diosbulbin B for 48 hours induced autophagy and apoptosis in L-02 cells, accompanied by an increase in the expression of LC3 II/I and Beclin-1, and a decrease in the expression of p62[5]. Treatment with 50µM Diosbulbin B for 48 hours induced G2/M phase arrest in CYP3A4-transfected L-02 cells and decreased the expression of CDK1[6].

In vivo, Diosbulbin B treatment via oral administration at a dose of 50mg/kg/day for 2 months led to hepatic infiltration of immune cells, swelling and necrosis of hepatocytes in mice, and promoted liver fibrosis in the mice[7]. Oral administration of 64mg/kg/day of Diosbulbin B for 12 consecutive days led to liver structure damage and extensive necrosis in mice, and caused oxidative stress injury[8].

References:
[1] Tan R, Hu Z, Zhou M, et al. Diosbulbin B: An important component responsible for hepatotoxicity and protein covalent binding induced by Dioscorea bulbifera L[J]. Phytomedicine, 2022, 102: 154174.
[2] Niu C, Sheng Y, Yang R, et al. Scutellarin protects against the liver injury induced by diosbulbin B in mice and its mechanism[J]. Journal of ethnopharmacology, 2015, 164: 301-308.
[3] Wang J, Sheng Y, Ji L, et al. Ferulic acid prevents liver injury and increases the anti-tumor effect of diosbulbin B in vivo[J]. Journal of Zhejiang University-SCIENCE B, 2014, 15(6): 540-547.
[4] Zhao J Q, Zhou Q Q, Sun Y, et al. The anti-non-small cell lung cancer effect of Diosbulbin B: Targeting YY1 induced cell cycle arrest and apoptosis[J]. Phytomedicine, 2024, 130: 155734.
[5] Ye J, Xue M, Liu Y, et al. Diosbulbin B-induced mitochondria-dependent apoptosis in L-02 hepatocytes is regulated by reactive oxygen species-mediated autophagy[J]. Frontiers in Pharmacology, 2019, 10: 676.
[6] Yang R, Wei M, Yang F, et al. Diosbulbin B induced G2/M cell cycle arrest in hepatocytes by miRNA-186-3p and miRNA-378a-5p-mediated the decreased expression of CDK1[J]. Toxicology and Applied Pharmacology, 2018, 357: 1-9.
[7] Zhang Y, Miao H, Guan H, et al. Long-term diosbulbin B treatment induced liver fibrosis in mice[J]. Chemico-biological interactions, 2019, 298: 15-23.
[8] Ma Y, Niu C, Wang J, et al. Diosbulbin B-induced liver injury in mice and its mechanism[J]. Human & experimental toxicology, 2014, 33(7): 729-736.

Protocol of Diosbulbin B

Cell experiment [1]:

Cell lines

A549 cells

Preparation Method

A549 cells were cultured in RPMI-1640 medium containing 10% fetal bovine serum (FBS) in 5% CO2 at 37°C. Cells were placed in 96-well plates at a concentration of 1×104 cells per well. Using 0.1% DMSO as a control, cells received diverse levels of Diosbulbin B (0, 5, 12.5, 25, 50, 100, 200, 400μM) treatment for 24, 48, and 72h. At the end of the administration, the supernatant was discarded, and the viable cell numbers were measured.

Reaction Conditions

0, 5, 12.5, 25, 50, 100, 200, 400μM; 24, 48, and 72h

Applications

Diosbulbin B treatment significantly reduced cell proliferation of A549 cells in a dose and time-dependent manner.
Animal experiment [2]:

Animal models

Male C57BL/6 mice

Preparation Method

Male C57BL/6 mice (20-24g) were housed in a specialized animal care facility, in a room with constant temperature (25°C), humidity control, and a 12/12h light/dark cycle with free access to food and water. Mice were randomly divided into 2 groups: (1) Control (n=11), (2) Diosbulbin B (50mg/kg) (n=13). Diosbulbin B was dissolved in 0.5% carboxymethylcellulose sodium (CMC-Na) solution. Mice were given (intragastric administration) with Diosbulbin B for 2 months. After treatment, mice were anesthetized with urethane and sacrificed, and the liver tissues were collected for analysis.

Dosage form

50mg/kg/day for 2 months; i.g.

Applications

Diosbulbin B treatment promoted liver fibrosis and increased liver hydroxyproline content, hepatic collagen deposition, and immune cell infiltration in mice.

References:
[1] Zhao J Q, Zhou Q Q, Sun Y, et al. The anti-non-small cell lung cancer effect of Diosbulbin B: Targeting YY1 induced cell cycle arrest and apoptosis[J]. Phytomedicine, 2024, 130: 155734.
[2] Zhang Y, Miao H, Guan H, et al. Long-term diosbulbin B treatment induced liver fibrosis in mice[J]. Chemico-biological interactions, 2019, 298: 15-23.

Chemical Properties of Diosbulbin B

Cas No. 20086-06-0 SDF
Canonical SMILES O=C1OC2([H])C3([H])[C@](CC4([H])OC(C3([H])C4)=O)([H])C5(C)C1(C2)O[C@@H](C6=COC=C6)C5
Formula C19H20O6 M.Wt 344.36
Solubility DMSO: 16 mg/mL (46.46 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Diosbulbin B

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.9039 mL 14.5197 mL 29.0394 mL
5 mM 580.8 μL 2.9039 mL 5.8079 mL
10 mM 290.4 μL 1.452 mL 2.9039 mL
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In vivo Formulation Calculator (Clear solution) of Diosbulbin B

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Review for Diosbulbin B

Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

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