| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Cycloartenol targets intestinal cholesterol absorption by competing with cholesterol for micellar solubilization and binding to the NPC1L1 transporter, reducing cholesterol uptake. It also modulates HMG-CoA reductase activity and increases LDL receptor expression. Cycloartenol possesses antioxidant activity by scavenging free radicals and upregulating endogenous antioxidant enzymes (SOD, catalase). It inhibits inflammatory mediators (TNF-α, IL-6) via NF-κB suppression. It also induces apoptosis in cancer cells through mitochondrial pathways.
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| ln Vitro |
Glioma U87 cell proliferation and colony-forming ability were both suppressed by cycloxylinol in a concentration-dependent manner. It was discovered that the antiproliferative effect resulted from apoptosis and Sub-G1 cell cycle arrest induction. Significant alterations in Bax and Bcl-2 expression are also brought about by cycloluteol [2].
In vitro studies have shown that Cycloartenol inhibits cholesterol micelle formation and reduces cholesterol uptake in Caco-2 cells (IC₅₀ ~ 20 μM). It exhibits DPPH radical scavenging with IC₅₀ ~ 50 μM. It reduces LPS-induced NO production and iNOS expression in macrophages. Cycloartenol shows cytotoxicity against several cancer cell lines (e.g., HepG2, MCF-7, HT-29) with IC₅₀ in the 10-30 μM range, inducing apoptosis and G1 arrest. It also has antimicrobial activity against Gram-positive bacteria (MIC ~ 100 μg/mL). |
| ln Vivo |
In vivo studies have demonstrated that Cycloartenol supplementation (0.5-2% in diet) reduces plasma total cholesterol and LDL-cholesterol in hyperlipidemic rats and hamsters, without affecting HDL. It also decreases hepatic triglyceride accumulation. In mice, cycloartenol (50 mg/kg oral) reduces carrageenan-induced paw edema, indicating anti-inflammatory activity. In a rat model of CCl₄-induced hepatotoxicity, cycloartenol (25-100 mg/kg) reduces serum transaminases and oxidative stress markers. It also inhibits the growth of implanted tumors in xenograft models.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for Cycloartenol involve cholesterol micelle formation inhibition: the compound is mixed with cholesterol, lecithin, and sodium taurocholate, micelles are formed, and cholesterol in the aqueous phase is measured by enzymatic assay. Antioxidant: DPPH, ABTS, and reducing power assays. Anti-inflammatory: COX-2 activity inhibition using a colorimetric assay. HMG-CoA reductase inhibition: using microsomal preparation and NADPH, mevalonate production measured by spectrophotometry. NPC1L1 binding can be assessed by surface plasmon resonance.
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| Cell Assay |
For in vitro cell-based assays, Caco-2 cells (intestinal) are cultured in transwell inserts. Cells are treated with Cycloartenol (1-100 μM) along with ³H-cholesterol in micelles. Cholesterol uptake into cells is measured by scintillation counting. Macrophage (RAW 264.7) inflammation: cells are stimulated with LPS and treated with compound; NO (Griess), cytokines (ELISA), and NF-κB translocation by immunofluorescence. Cancer cell cytotoxicity: MTT assay, apoptosis (Annexin V, caspase-3 activity), cell cycle by PI staining. HepG2 cells for hepatoprotection: H₂O₂-induced oxidative stress and MTT, ROS detection.
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| Animal Protocol |
In vivo animal studies: Hyperlipidemic hamsters or rats are fed a high-fat diet with or without Cycloartenol (0.5-2% w/w) for 4-8 weeks. Blood lipids (total cholesterol, triglycerides, LDL, HDL) measured. Liver lipids extracted and quantified. For anti-inflammatory, rats are given carrageenan in hind paw and Cycloartenol (50 mg/kg) orally 1 hour before; paw edema measured. For hepatotoxicity, rats are treated with CCl₄ and compound (25-100 mg/kg) for 7 days; serum ALT/AST, liver histology, and oxidative markers (MDA, GSH) assessed. For anticancer, xenograft mice are treated with compound (50-100 mg/kg i.p. or oral) daily; tumor volume measured.
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| ADME/Pharmacokinetics |
Cycloartenol (MW 426.7 g/mol, formula C₃₀H₅₀O) is a lipophilic sterol, insoluble in water, soluble in organic solvents and oils. After oral administration, absorption is low (<10%) but it is metabolized in the intestine and liver. It may be converted to other phytosterols. Plasma levels are low, but it accumulates in tissues. Half-life is several hours. It is excreted in feces as unabsorbed or as bile metabolites. Formulation in oil or emulsions improves bioavailability.
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| Toxicity/Toxicokinetics |
Cycloartenol is generally recognized as safe (GRAS) as a dietary phytosterol. In animal studies, doses up to 1000 mg/kg/day show no toxicity. No adverse effects in subchronic studies. It may reduce absorption of fat-soluble vitamins at very high doses. No mutagenicity. Humans consume it from vegetable oils; no known side effects. It is used as a nutraceutical.
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| References |
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| Additional Infomation |
Cycloartenol is a pentacyclic triterpenoid compound belonging to the 3β-sterol family of phytosterols. It is a plant metabolite derived from the hydrogenation of lanosterane. Cycloartenol has been reported to exist in tea (Camellia sinensis), peony (Paeonia emodi), and other organisms with relevant data.
Cycloartenol is a phytosterol with cholesterol-lowering, anti-inflammatory, and antioxidant properties. It is a precursor to other plant sterols. It is used in functional foods and dietary supplements for cardiovascular health. It is not a drug but a natural compound. Available as a research chemical. |
| Molecular Formula |
C30H50O
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|---|---|
| Molecular Weight |
426.7174
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| Exact Mass |
426.386
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| CAS # |
469-38-5
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| PubChem CID |
92110
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| Appearance |
White to off-white solid powder
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| Density |
1.01 g/cm3
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| Boiling Point |
505.5ºC at 760 mmHg
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| Melting Point |
115-117ºC
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| Flash Point |
221.9ºC
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| Vapour Pressure |
2.47E-12mmHg at 25°C
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| Index of Refraction |
1.538
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| LogP |
8.168
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
760
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@H](CCC=C(C)C)[C@H]1CC[C@@]2([C@@]1(CC[C@]34[C@H]2CC[C@@H]5[C@]3(C4)CC[C@@H](C5(C)C)O)C)C
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| InChi Key |
ONQRKEUAIJMULO-YBXTVTTCSA-N
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| InChi Code |
InChI=1S/C30H50O/c1-20(2)9-8-10-21(3)22-13-15-28(7)24-12-11-23-26(4,5)25(31)14-16-29(23)19-30(24,29)18-17-27(22,28)6/h9,21-25,31H,8,10-19H2,1-7H3/t21-,22-,23+,24+,25+,27-,28+,29-,30+/m1/s1
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| Chemical Name |
(1S,3R,6S,8R,11S,12S,15R,16R)-7,7,12,16-tetramethyl-15-[(2R)-6-methylhept-5-en-2-yl]pentacyclo[9.7.0.01,3.03,8.012,16]octadecan-6-ol
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~5 mg/mL (~11.72 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.17 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 5.0 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: 0.5 mg/mL (1.17 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 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: ≥ 0.5 mg/mL (1.17 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 | 2.3435 mL | 11.7173 mL | 23.4346 mL | |
| 5 mM | 0.4687 mL | 2.3435 mL | 4.6869 mL | |
| 10 mM | 0.2343 mL | 1.1717 mL | 2.3435 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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