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| Targets |
Steviol is a tetracyclic diterpenoid and the aglycon derivative of steviol glycosides, the natural sweeteners found in Stevia rebaudiana. It is a major metabolite of the sweetening compound stevioside. Steviol is an inhibitor of AQP2 (aquaporin 2) and CFTR (cystic fibrosis transmembrane conductance regulator). By inhibiting CFTR activity and reducing AQP2 expression, it slows down the growth of renal cysts. Steviol also inhibits human organic anion transporters (hOATs) in uptake assays. Its mechanism of action involves the modulation of ion transport and water homeostasis.
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| ln Vitro |
In vitro, Steviol inhibits the proliferation of gastrointestinal cancer cells and the human osteosarcoma U2OS cell line in a dose- and time-dependent manner. It inhibits human organic anion transporters (hOATs) in uptake assays using murine cells from the S2 segment of proximal tubules. Steviol is an inhibitor of AQP2/CFTR and slows down the growth of renal cysts by reducing AQP2 expression and promoting AQP2 degradation. Its in vitro activity is characterized by antiproliferative effects and inhibition of ion transporters.
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| ln Vivo |
In vivo, Steviol slows down the growth of renal cysts by reducing the expression of AQP2 and promoting the degradation of AQP2. It possesses antitumor activity. Steviol has been shown to inhibit the proliferation of gastrointestinal cancer cells and the human osteosarcoma U2OS cell line. Its in vivo efficacy is attributed to its ability to modulate AQP2/CFTR and inhibit tumor cell proliferation. The compound's safety is widely studied due to the use of steviol glycosides as sweeteners.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Steviol typically involve studying its interaction with AQP2 and CFTR. The compound inhibits CFTR activity and reduces AQP2 expression. These effects can be assessed using binding assays or functional assays measuring ion transport. Steviol's inhibition of human organic anion transporters (hOATs) can also be studied using uptake assays. These assays confirm the compound's mechanism of action as a modulator of ion transporters.
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| Cell Assay |
In vitro cellular assays for Steviol typically involve treating cancer cell lines, such as gastrointestinal cancer cells and U2OS osteosarcoma cells, with the compound and measuring cell viability and proliferation. The compound inhibits the proliferation of these cells in a dose- and time-dependent manner. Its effects on AQP2 and CFTR expression can be assessed using Western blotting or immunofluorescence. These cell-based studies demonstrate the compound's antiproliferative and ion transport-modulating activities.
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| Animal Protocol |
In vivo animal models for Steviol typically involve models of polycystic kidney disease to evaluate its effects on renal cyst growth. The compound is administered by appropriate routes, and cyst growth is measured. Steviol slows down the growth of renal cysts by reducing AQP2 expression and promoting AQP2 degradation. Its antitumor activity can also be studied in cancer xenograft models. Doses and administration routes are optimized based on the specific model and experimental endpoints.
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| ADME/Pharmacokinetics |
Steviol is a tetracyclic diterpenoid with a molecular formula of C20H30O3 and a molecular weight of 318.45 g/mol. It is the aglycon derivative of steviol glycosides, the natural sweeteners isolated from Stevia rebaudiana. The compound is typically stored under appropriate conditions to maintain stability. Its physicochemical properties support its use in pharmacological and toxicological research. Steviol's solubility and formulation for administration should be optimized based on specific experimental requirements.
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| Toxicity/Toxicokinetics |
Steviol is a metabolite of steviol glycosides and is widely studied for its safety due to the use of steviol glycosides as sweeteners. Its toxicity profile includes potential genotoxicity and effects on renal function. The compound's safety has been extensively evaluated in toxicological studies. Steviol is for research use only and is not approved for human therapeutic use. It represents a valuable tool for studying AQP2/CFTR biology and renal cyst growth.
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| References |
[1]. Steviol slows renal cyst growth by reducing AQP2 expression and promoting AQP2 degradation. Biomed Pharmacother. 2018 May;101:754-762. |
| Additional Infomation |
Steviol is an ent-kauriane diterpenoid compound with the chemical formula 5β,8α,9β,10α-kauri-16-en-18-acid, in which the hydrogen at position 13 is replaced by a hydroxyl group. It possesses antitumor activity. Steviol is a tetracyclic diterpenoid, tert-allyl alcohol, monocarboxylic acid, bridging compound, and ent-kauriane diterpenoid. It is the conjugate acid of steviol (1-). Steviol has been reported to exist in Bruguiera gymnorhiza, Ceriops decandra, and several other organisms with relevant data.
Steviol (CAS# 471-80-7) is the aglycon derivative of steviol glycosides, which are natural sweeteners isolated from Stevia rebaudiana. It is the main metabolite of stevioside and an inhibitor of AQP2/CFTR. Steviol slows down the growth of renal cysts by reducing the expression of AQP2 and promoting the degradation of AQP2 and CFTR. It inhibits the proliferation of gastrointestinal cancer cells and the human osteosarcoma U2OS cell line. The compound is for research use only and is not approved for human therapeutic use. |
| Molecular Formula |
C20H30O3
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|---|---|
| Molecular Weight |
318.457
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| Exact Mass |
318.219
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| Elemental Analysis |
C, 75.43; H, 9.50; O, 15.07
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| CAS # |
471-80-7
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| PubChem CID |
452967
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
464.5±45.0 °C at 760 mmHg
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| Melting Point |
215°
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| Flash Point |
248.8±25.2 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
4.44
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
583
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| Defined Atom Stereocenter Count |
6
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| SMILES |
O([H])C12C(=C([H])[H])C([H])([H])[C@@]3(C([H])([H])C([H])([H])[C@]4([H])[C@@](C(=O)O[H])(C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])[C@@]4(C([H])([H])[H])[C@]3([H])C([H])([H])C1([H])[H])C2([H])[H]
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| InChi Key |
QFVOYBUQQBFCRH-VQSWZGCSSA-N
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| InChi Code |
InChI=1S/C20H30O3/c1-13-11-19-9-5-14-17(2,7-4-8-18(14,3)16(21)22)15(19)6-10-20(13,23)12-19/h14-15,23H,1,4-12H2,2-3H3,(H,21,22)/t14-,15-,17+,18+,19+,20-/m0/s1
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| Chemical Name |
(1R,4S,5R,9S,10R,13S)-13-hydroxy-5,9-dimethyl-14-methylidenetetracyclo[11.2.1.01,10.04,9]hexadecane-5-carboxylic acid
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| Synonyms |
13-hydroxy Kaurenoic Acid; NSC 226902; Hydroxydehydrostevic Acid; 13-O-Glucosylsteviol; Steviol
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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 (~314.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.85 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 (7.85 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 (7.85 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 | 3.1401 mL | 15.7006 mL | 31.4011 mL | |
| 5 mM | 0.6280 mL | 3.1401 mL | 6.2802 mL | |
| 10 mM | 0.3140 mL | 1.5701 mL | 3.1401 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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