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| 5mg |
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| 10mg |
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| Targets |
Terrestrosin D interacts with multiple molecular targets. It has been shown to interact with HSP90AA1 (heat shock protein 90 alpha), CNR1 (cannabinoid receptor 1), and DRD2 (dopamine receptor D2). As an apoptosis inducer, Terrestrosin D triggers cell death through the mitochondrial pathway, reducing mitochondrial membrane potential and activating caspases. The compound induces cell cycle arrest at the G1 and S phases, suggesting that it may interfere with cell cycle regulatory proteins such as cyclins and CDKs. Its anti-angiogenic activity involves inhibition of endothelial cell proliferation and tube formation. The compound's ability to interact with multiple targets contributes to its diverse biological activities, including antitumor and anti-angiogenic effects.
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| ln Vitro |
In vitro studies demonstrate that Terrestrosin D inhibits the growth of cancer cells and endothelial cells. The compound induces cell cycle arrest at the G1 and S phases and reduces mitochondrial membrane potential. Terrestrosin D induces apoptotic cell death in cancer cells through the mitochondrial pathway, with activation of caspases and cleavage of PARP. The compound inhibits angiogenesis by suppressing endothelial cell proliferation and tube formation. In various cancer cell lines, Terrestrosin D reduces cell viability with IC50 values in the micromolar range. The compound's activity is mediated through its interactions with HSP90AA1, CNR1, and DRD2, which contribute to its pro-apoptotic and anti-proliferative effects. These in vitro activities make Terrestrosin D a promising candidate for cancer research.
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| ln Vivo |
In vivo studies of Terrestrosin D have demonstrated its antitumor and anti-angiogenic activities in animal models. The compound is orally active, making it suitable for convenient administration. In xenograft models of cancer, Terrestrosin D has been shown to inhibit tumor growth and induce apoptotic cell death in tumor tissues. The compound also inhibits angiogenesis, reducing tumor vascularization and limiting tumor growth. In vivo protocols typically involve oral administration of Terrestrosin D at doses determined from pharmacokinetic and toxicology studies. Pharmacodynamic endpoints include assessment of tumor growth inhibition, apoptosis in tumor tissues (by TUNEL staining), angiogenesis (by CD31 staining), and cell cycle analysis. The compound's efficacy in multiple cancer models supports its potential as an anticancer agent.
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| Cell Assay |
For cell viability and apoptosis assays, cancer cells and endothelial cells are cultured in appropriate medium (RPMI-1640 or DMEM) with 10% FBS and antibiotics. Cells are seeded in 96-well or 24-well plates. Terrestrosin D is dissolved in DMSO and diluted in culture medium to final concentrations (typically 0.1-100 µM). Cells are treated for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assays. Apoptosis is assessed by Annexin V/PI staining and flow cytometry, or by caspase-3/7 activity assays. Mitochondrial membrane potential is measured using JC-1 dye. For cell cycle analysis, cells are fixed, stained with propidium iodide, and analyzed by flow cytometry. For angiogenesis assays, endothelial cells (e.g., HUVECs) are seeded on Matrigel-coated plates and treated with Terrestrosin D. Tube formation is assessed after 6-18 hours by light microscopy. For Western blot analysis, cells are lysed and analyzed for apoptosis markers (cleaved PARP, caspase-3), cell cycle regulators (cyclins, CDKs), and signaling proteins (HSP90, CNR1, DRD2).
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| Animal Protocol |
For in vivo efficacy studies, 6-8 week old female immunodeficient mice (e.g., nude or SCID) are used. Mice are subcutaneously implanted with cancer cells (e.g., xenograft tumor cells) in the flank. When tumors reach approximately 50-100 mm³, animals are randomized into treatment groups (n = 6-10 per group). Terrestrosin D is formulated in vehicle (e.g., 0.5% methylcellulose or 10% DMSO in PEG400) and administered orally at doses of 1-50 mg/kg, typically once daily for 2-4 weeks. Tumor volumes are measured twice weekly using calipers. Body weights are monitored for toxicity. At study termination, tumors are excised, weighed, and processed for histopathological examination (H&E staining), apoptosis assessment (TUNEL staining), and angiogenesis assessment (CD31 immunohistochemistry). Blood samples may be collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Terrestrosin D indicate that it is orally active. The compound shows good oral bioavailability, supporting once-daily dosing. Specific pharmacokinetic parameters, including half-life, Cmax, Tmax, and AUC, may be available from published studies but are not extensively reported in the public domain. The compound's favorable pharmacokinetic properties contribute to its potential as an anticancer agent.
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| Toxicity/Toxicokinetics |
Toxicological data for Terrestrosin D are limited, as the compound is a research tool. In preclinical studies, the compound has been shown to be well-tolerated at pharmacologically active doses. No acute toxicity, organ-specific toxicity, or mutagenicity data have been reported. As with all research compounds, appropriate safety precautions should be taken when handling Terrestrosin D, including the use of personal protective equipment and work in a well-ventilated area.
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| References | |
| Additional Infomation |
16-[3,4-dihydroxy-5-[5-hydroxy-6-(hydroxymethyl)-3-[3,4,5-trihydroxy-6-(hydroxymethyl)oxetane-2-yl]oxy-4-(3,4,5-trihydroxyoxetane-2-yl)oxyoxetane-2-yl]oxy-6-(hydroxymethyl)oxetane-2-yl]oxy-5',7,9,13-tetramethylspiro[5-oxapentane[10.8.0.02,9.04,8.013,18]eicosano-6,2'-oxetane]-10-one has been reported in Tribulus terrestris, and relevant data are available.
Terrestrosin D (CAS 179464-23-4) is a steroidal saponin isolated from Tribulus terrestris L.. It is an orally active apoptosis inducer that induces cell cycle arrest at G1 and S phases, reduces mitochondrial membrane potential, and inhibits the growth of cancer cells and endothelial cells. The compound possesses anti-angiogenic activities and interacts with HSP90AA1, CNR1, and DRD2. Its molecular formula is C₅₀H₈₀O₂₃ with a molecular weight of 1049.16. Terrestrosin D induces apoptotic cell death and inhibits angiogenesis in xenograft tumor models. It is used as a research tool for studying apoptosis, cell cycle regulation, and angiogenesis in cancer research and is strictly for research use only. |
| Molecular Formula |
C50H80O23
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|---|---|
| Molecular Weight |
1049.1564
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| Exact Mass |
1048.509
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| CAS # |
179464-23-4
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| PubChem CID |
78177919
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Melting Point |
279-281 °C
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| Index of Refraction |
1.638
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| LogP |
0.29
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
23
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
73
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| Complexity |
1920
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[C@@H]1CC[C@@]2([C@H]([C@H]3[C@@H](O2)C[C@@H]4[C@@]3(C(=O)C[C@H]5[C@H]4CC[C@@H]6[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[C@H]9[C@@H]([C@H]([C@@H](CO9)O)O)O)O[C@H]2[C@@H]([C@H]([C@H]([C@H](O2)CO)O)O)O)O)O)C)C)C)OC1
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| InChi Key |
IXUNZKARBRITGN-WDJYAXNWSA-N
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| InChi Code |
InChI=1S/C50H80O23/c1-19-7-10-50(65-17-19)20(2)32-27(73-50)12-25-23-6-5-21-11-22(8-9-48(21,3)24(23)13-31(55)49(25,32)4)66-45-40(63)37(60)41(30(16-53)69-45)70-47-43(72-46-39(62)36(59)34(57)28(14-51)67-46)42(35(58)29(15-52)68-47)71-44-38(61)33(56)26(54)18-64-44/h19-30,32-47,51-54,56-63H,5-18H2,1-4H3/t19-,20+,21+,22+,23-,24+,25+,26-,27+,28-,29-,30-,32+,33+,34+,35-,36+,37-,38-,39-,40-,41+,42+,43-,44+,45-,46+,47+,48+,49-,50-/m1/s1
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| Chemical Name |
(1R,2S,4S,5'R,6R,7S,8R,9S,12S,13S,16S,18S)-16-[(2R,3R,4R,5R,6R)-3,4-dihydroxy-5-[(2S,3R,4S,5R,6R)-5-hydroxy-6-(hydroxymethyl)-3-[(2S,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4-[(2S,3R,4S,5R)-3,4,5-trihydroxyoxan-2-yl]oxyoxan-2-yl]oxy-6-(hydroxymethyl)oxan-2-yl]oxy-5',7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icosane-6,2'-oxane]-10-one
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~95.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.38 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 (2.38 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 (2.38 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 | 0.9531 mL | 4.7657 mL | 9.5314 mL | |
| 5 mM | 0.1906 mL | 0.9531 mL | 1.9063 mL | |
| 10 mM | 0.0953 mL | 0.4766 mL | 0.9531 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.
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