Diosbulbin B是Dioscorea bulbifera L.的主要肝毒性成分，具有强效的抗肿瘤活性。
Cas No.:20086-06-0
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
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.
Diosbulbin B是Dioscorea bulbifera L.的主要肝毒性成分，具有强效的抗肿瘤活性[1]。Diosbulbin B可显著诱导肝脏MPO酶活性和蛋白表达升高，降低IκB表达并促进NF-κB p65转位增加，同时导致血清中TNF-α、IL-6和IFN-γ水平升高[2]。Diosbulbin B已被广泛用于建立肝损伤动物模型和抑制异种移植模型的肿瘤生长[3]。
在体外，Diosbulbin B处理72小时显著抑制了A549细胞和PC-9细胞的活力，IC50值分别为44.61μM 和22.78μM[4]。使用200μM的Diosbulbin B处理L-02细胞48小时，诱导了自噬和凋亡，伴随LC3 II/I和Beclin-1表达增加，以及p62表达降低[5]。使用50μM的Diosbulbin B处理转染CYP3A4的L-02细胞48小时，诱导了G2/M期阻滞并降低了CDK1的表达[6]。
在体内，每日口服50mg/kg剂量的Diosbulbin B，持续2个月，导致小鼠肝脏免疫细胞浸润、肝细胞肿胀和坏死，并促进了小鼠肝纤维化[7]。连续12天口服64mg/kg/day剂量的Diosbulbin B，导致小鼠肝脏结构损伤和广泛坏死，并引起氧化应激损伤[8]。
| 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: | |
| Cas No. | 20086-06-0 | SDF | |
| 别名 | 黄独素B | ||
| 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 | ||
| 分子式 | C19H20O6 | 分子量 | 344.36 |
| 溶解度 | DMSO: 16 mg/mL (46.46 mM) | 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。 |
||
| 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 | |||
 |
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 |
| 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet