| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
- Deltonin regulates apoptosis-related proteins (Bax, Bcl-2, Caspase-3) and signaling pathway proteins (ERK, AKT) [1][2]
|
|---|---|
| ln Vitro |
Deltonin prevents the activation of AKT and ERK1/2. With IC50s of 1.3, 1.29, 2.11, and 1.22 μM, deltonin (0.5-8 μM) dramatically suppresses the growth of several colon cancer cell lines, including SW480, SW620, LOVO, and C26. In C26 cells, deltonin also induces apoptosis and causes G2-M phase arrest [1]. In MDA-MB-231 cells, deltonin (0–5 μM) lowers the phosphorylation levels of ERK1/2 and AKT. Additionally, deltonin (0.5-8 μM) can induce cell apoptosis by producing ROS and inhibit MDA-MB-231 cell proliferation in a dose-dependent manner [2].
- In human colon cancer cells (HT-29, HCT-116), Deltonin inhibited proliferation in a concentration-dependent manner, with IC50 values of 4.2 μM (HT-29) and 3.8 μM (HCT-116) after 48-hour treatment (MTT assay). Annexin V-FITC/PI staining showed ~52% (HT-29) and ~48% (HCT-116) apoptotic cells at 5 μM (48 h); western blot revealed upregulated Bax/Caspase-3 and downregulated Bcl-2. It also inhibited angiogenesis by reducing tube formation of human umbilical vein endothelial cells (HUVECs): ~60% reduction in tube length at 5 μM [1] - In human breast cancer MDA-MB-231 cells, Deltonin suppressed viability with an IC50 of 5.1 μM (48 h, MTT assay). DCFH-DA staining showed ROS levels increased by ~3.5-fold at 5 μM; JC-1 staining revealed reduced mitochondrial membrane potential (ΔΨm, ~55% decrease at 5 μM). Western blot indicated downregulated phospho-ERK (p-ERK) and phospho-AKT (p-AKT) (by ~60% and ~55% at 5 μM, respectively), along with upregulated Bax/Cleaved Caspase-3 and downregulated Bcl-2 [2] |
| ln Vivo |
Deltonin administered orally at doses of 20 and 40 mg/kg can inhibit tumor growth in mice by 37.7% and 56.7%, respectively, with corresponding 50-day survival rates of 60% and 50%. In mice, deltonin also prevents the angiogenesis of tumors [1].
- In a nude mouse xenograft model of colon cancer (HT-29 cells), Deltonin (5 mg/kg, 10 mg/kg, intraperitoneal injection, once every 2 days for 3 weeks) inhibited tumor growth. At 10 mg/kg, tumor volume was reduced by ~65% (680 ± 75 mm³ vs. control 1950 ± 130 mm³) and tumor weight by ~60% (0.52 ± 0.06 g vs. control 1.30 ± 0.11 g). Immunohistochemistry showed increased TUNEL-positive cells (~40% vs. control ~5%) and decreased CD31 (angiogenesis marker, ~55% reduction) in tumor tissues [1] |
| Cell Assay |
- Colon cancer cell assay [1]: HT-29/HCT-116 cells were cultured in RPMI 1640 medium (10% FBS) at 37°C, 5% CO₂. Cells were treated with Deltonin (1–10 μM) for 24–48 h. Viability was detected via MTT assay (absorbance 570 nm). Apoptosis was analyzed via Annexin V-FITC/PI staining (flow cytometry) and western blot (Bax, Bcl-2, Cleaved Caspase-3). For angiogenesis assay: HUVECs were seeded on Matrigel-coated plates with Deltonin (1–5 μM); tube length was measured after 6 h.
- Breast cancer cell assay [2]: MDA-MB-231 cells were cultured in DMEM medium (10% FBS) at 37°C, 5% CO₂. Cells were treated with Deltonin (1–8 μM) for 24–48 h. Viability was detected via MTT assay. ROS levels were measured via DCFH-DA staining (fluorescence microscope, excitation 488 nm). Mitochondrial membrane potential was assessed via JC-1 staining (flow cytometry). Western blot detected p-ERK, ERK, p-AKT, AKT, Bax, Bcl-2, and Cleaved Caspase-3 [2] |
| Animal Protocol |
- Colon cancer xenograft model [1]: 6-week-old male nude mice were subcutaneously injected with HT-29 cells (5×10⁶ cells/mouse) into the right flank. When tumors reached ~150 mm³, mice were randomized into 3 groups (n=6/group): control (DMSO + normal saline, intraperitoneal injection), Deltonin 5 mg/kg, and Deltonin 10 mg/kg. Deltonin was dissolved in DMSO (final concentration ≤5%) and diluted with normal saline. Injections were given once every 2 days for 3 weeks. Tumor volume (V=0.5×length×width²) and body weight were measured every 3 days. At study end, mice were euthanized; tumors were excised, weighed, and fixed in 10% formalin for TUNEL staining and CD31 immunohistochemistry [1]
|
| Toxicity/Toxicokinetics |
In nude mice treated with Deltonin (5–10 mg/kg, intraperitoneal injection, 3 weeks)[1], no significant weight loss (<5% vs. control group) or abnormal liver and kidney function (serum ALT, AST, BUN, and Cr were all within the normal range). In MDA-MB-231 cells and normal human mammary epithelial cells (MCF-10A), Deltonin (5 μM) induced apoptosis in approximately 50% of MDA-MB-231 cells and less than 10% of MCF-10A cells, indicating that it has selective toxicity to cancer cells[2].
|
| References |
|
| Additional Infomation |
Deltonin is a triterpenoid compound. It has been reported to be found in Paris polyphylla var. chinensis, Dioscorea parviflora, and other organisms with relevant data. Deltonin is a steroidal saponin isolated from Dioscoreaceae plants (e.g., Dioscorea zingiberensis) with potential anti-colon and anti-breast cancer activities [1][2]. Its anti-tumor mechanism in colon cancer involves inducing apoptosis and inhibiting tumor angiogenesis [1]; in breast cancer, it mediates apoptosis through ROS-induced mitochondrial dysfunction and inhibition of the ERK/AKT signaling pathway [2].
|
| Molecular Formula |
C45H72O17
|
|---|---|
| Molecular Weight |
885.0430
|
| Exact Mass |
884.476
|
| CAS # |
55659-75-1
|
| PubChem CID |
441884
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Index of Refraction |
1.623
|
| LogP |
4.24
|
| Hydrogen Bond Donor Count |
9
|
| Hydrogen Bond Acceptor Count |
17
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
62
|
| Complexity |
1620
|
| Defined Atom Stereocenter Count |
26
|
| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@H]3[C@@H](O2)C[C@@H]4[C@@]3(CC[C@H]5[C@H]4CC=C6[C@@]5(CC[C@@H](C6)O[C@H]7[C@@H]([C@H]([C@@H]([C@H](O7)CO)O[C@H]8[C@@H]([C@H]([C@@H]([C@H](O8)CO)O)O)O)O)O[C@H]9[C@@H]([C@@H]([C@H]([C@@H](O9)C)O)O)O)C)C)C)OC1
|
| InChi Key |
OLAMGHNQGZIWHZ-YIKYYZBWSA-N
|
| InChi Code |
InChI=1S/C45H72O17/c1-19-8-13-45(55-18-19)20(2)30-27(62-45)15-26-24-7-6-22-14-23(9-11-43(22,4)25(24)10-12-44(26,30)5)57-42-39(61-40-35(52)33(50)31(48)21(3)56-40)37(54)38(29(17-47)59-42)60-41-36(53)34(51)32(49)28(16-46)58-41/h6,19-21,23-42,46-54H,7-18H2,1-5H3/t19-,20+,21+,23+,24-,25+,26+,27+,28-,29-,30+,31+,32-,33-,34+,35-,36-,37+,38-,39-,40+,41+,42-,43+,44+,45-/m1/s1
|
| Chemical Name |
(2S,3R,4R,5R,6S)-2-[(2R,3R,4S,5S,6R)-4-hydroxy-6-(hydroxymethyl)-2-[(1S,2S,4S,5'R,6R,7S,8R,9S,12S,13R,16S)-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2'-oxane]-16-yl]oxy-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~56.49 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (2.82 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1299 mL | 5.6495 mL | 11.2989 mL | |
| 5 mM | 0.2260 mL | 1.1299 mL | 2.2598 mL | |
| 10 mM | 0.1130 mL | 0.5649 mL | 1.1299 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.
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
