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Purity: ≥98%
β-Sitosterol (also known as SKF 14463), a lipid regulating agent, is one of several natural phytosterols (plant sterols) with chemical structures similar to that of cholesterol. It is a typical plant steroid with anticholesteremic properties. Recent research has demonstrated that β-Sitosterol causes G2/M arrest, endoreduplication, and apoptosis via the Bcl-2 and PI3K/Akt signaling pathways.
| Targets |
lipid regulating agent
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|---|---|
| ln Vitro |
Beta-Sitosterol is one of the most abundant dietary phytosterols. According to one study, beta-sitosterol has the ability to prevent leukemia, ovarian cancer, breast, prostate, colon, lung, stomach, and colon cancer.
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| ln Vivo |
The total cells and eosinophils in the bronchoalveolar lavage (BAL) fluid markedly decreased (p<0.05) after L-BS or beta-sitosterol (BS) administration (1 mg/kg; i.p.), and the ROS production also decreased in comparison to the asthma control. Histopathological features were detected by performing histochemistry, including H&E and alcian blue & P.A.S staining. Both L-BS and beta-sitosterol (BS) mitigated the inflammation by eosinophil infiltration and mucus hypersecretion by goblet hyperplasia. These effects of L-BS were superior to those of BS. L-BS and BS inhibited the increased mRNA and protein expression of IL-4 and IL-5 in the lung tissue and BAL fluid, respectively. The IgE concentration in the BAL fluid and serum was measured by performing ELISA and the ovalbumin-specific IgE in the BAL fluid was uniquely inhibited by L-BS (p<0.05). The splenocytes were isolated from the normal and asthmatic mice and incubated in the absence and presence of 100 microg/ml ovalbumin, respectively. L-BS blocked the survival rate of the splenocytes of the mice (p<0.01). This finding indicates the possibility of L-BS and BS as potential therapeutic molecules in asthma and may contribute to the need to improve current therapeutic drugs. [2]
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| Cell Assay |
Viability of mouse splenocytes [2]
We performed MTT assay and apoptosis assay to determine the cell viability with using the MTT assay kit and annexinV-fluorescein isothiocyanate (FITC) apoptosis detection kit (Beckton Dickinson, San Jose, CA). The splenocytes were isolated from the spleens of normal and asthmatic control mice by syringe pumping. After three washings with 10 ml of DMEM supplemented with antibiotics–antimycotics (Life Technologies, NY), the splenocytes were incubated with 3 ml of RBC lysis buffer (Sigma, MI) for 10 min at room temperature, and then this was washed twice with 10 ml of the wash medium. 2 × 105 splenocytes in 100 μl of DMEM medium containing 10% FBS were seeded onto a 96-well culture plate. L-BS, BS or dexamethasone (1 μg/ml) in the absence or presence of 100 μg/ml ovalbumin was added to the individual well and then the plate was incubated for 48 h at 37 °C in a CO2 incubator. After the addition of 10 μl of MTT solution in each well, the plate was incubated at 37 °C for 4 h in a CO2 incubator and 100 μl of solubilization solution was added to each well for MTT assay. After 24 h incubation, the absorbance was measured by using an ELISA reader (Bio-Tek Instruments, VT) at 550 nm. For the apoptosis assay, the cells were harvested and resuspended in binding buffer. Annexin V-FITC and PI were added and incubated for 15 min at room temperature. The cells were analyzed by FACSort cytofluorimeter using CellQuest software. Negative cells against annexin V and PI staining were considered as viable or non-apoptotic cells.[2] |
| Animal Protocol |
Induction of asthma in mice[2]
Six to eight-week-old female BALB/c mice were obtained from Daehan Biolink Co. LTD. They were maintained in an air-conditioned room. The room temperature (about 22 ± 1 °C) and humidity (about 55 ± 10%) were automatically controlled. The mice were divided into five groups (n = 5), and airway inflammation was induced in four groups. Each mouse was immunized through intraperitoneal (i.p.) injection with 20 μg of chicken OVA and 1 mg of aluminum hydroxide on days 1 and 14, as shown in Fig. 2. The mice were exposed to a 5% ovalbumin solution aerosolized using an ultrasonic nebulizer for 1 h per day from days 21 to 27 after the second sensitization. The mice were placed in a Plexiglass chamber (30 × 30 × 15 cm3) that contained small ventilation holes on one side during the inhalation challenge. The aerosol was generated with a nebulization rate of 1 ml/min. Three groups of asthma-induced mice were treated through i.p. injection with 1 mg/kg of L-BS, BS or dexamethasone between days 14 and 27. Both L-BS and BS dissolved in DMSO diluted less than 1/100 by phosphate-buffered saline (PBS). The negative control group was sensitized and challenged with PBS without drug administration. |
| References |
| Molecular Formula |
C29H50O
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|---|---|---|
| Molecular Weight |
414.71
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| Exact Mass |
414.3862
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| Elemental Analysis |
C, 83.99; H, 12.15; O, 3.86
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| CAS # |
83-46-5
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| Related CAS # |
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| Appearance |
White to off-white solid powder
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| LogP |
9.3
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| tPSA |
20.2Ų
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| SMILES |
CC[C@H](CC[C@@H](C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC=C4[C@@]3(CC[C@@H](C4)O)C)C)C(C)C
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| InChi Key |
KZJWDPNRJALLNS-VJSFXXLFSA-N
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| InChi Code |
InChI=1S/C29H50O/c1-7-21(19(2)3)9-8-20(4)25-12-13-26-24-11-10-22-18-23(30)14-16-28(22,5)27(24)15-17-29(25,26)6/h10,19-21,23-27,30H,7-9,11-18H2,1-6H3/t20-,21-,23+,24+,25-,26+,27+,28+,29-/m1/s1
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| Chemical Name |
(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,5R)-5-ethyl-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
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| Synonyms |
(-)-beta-Sitosterol; 22,23-Dihydrostigmasterol; 24-alpha-Ethylcholesterol; AI3-26020; alpha-Dihydrofucosterol; Rhamnol; Angelicin; beta-Sitosterol; CCRIS 5529; Azuprostat; Cinchol; Cupreol; Harzol; Nimbosterol; Prostasal; Quebrachol; Triastonal
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| HS Tariff Code |
2934.99.03.00
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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. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 20 mg/mL (48.23 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 40% PEG300 + 5% Tween80 + + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can take 100 μL of 25 mg/mL EtOH + stock solution and add to 400 μL of PEG300, mix well; Then add 50 μL of Tween 80 to the above solution, mix well; Finally, add 450 μL of saline to the above solution, mix well. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 90% (20% SBE-β-CD in saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. Solubility in Formulation 4: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 90% Corn oil (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 take 100 μL of 25 mg/mL EtOH + stock solution and add to 900 μL of corn oil, mix well (clear solution). Solubility in Formulation 5: ~5 mg/mL (12.1 mM) in 15% Cremophor EL + + 85% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution. Solubility in Formulation 6: ~10 mg/mL (24.1 mM) in Corn Oil , clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4113 mL | 12.0566 mL | 24.1132 mL | |
| 5 mM | 0.4823 mL | 2.4113 mL | 4.8226 mL | |
| 10 mM | 0.2411 mL | 1.2057 mL | 2.4113 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01736865 | Completed | Drug: Placebo Drug: Cholecalciferol |
Type 2 Diabetes | Tufts Medical Center | December 2012 | Phase 2 Phase 3 |
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