Totarol (Synonyms: NSC 299936, (+)-Totarol, trans-Totarol) |
Catalog No.GC40043
One-Click Copy Product Info
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Totarol is a non-specific inhibitor of the bacterial cell division protein FtsZ.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 511-15-9
Sample solution is provided at 25 µL, 10mM.
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Totarol is a non-specific inhibitor of the bacterial cell division protein FtsZ[1]. Totarol directly targets and binds to the FtsZ protein, inhibiting its assembly into the Z-ring, thereby blocking bacterial cell division and proliferation. Totarol is commonly used in research on novel antibacterial drugs, particularly against drug-resistant Gram-positive bacteria (such as Staphylococcus aureus) and Mycobacterium tuberculosis[2]. Totarol can also inhibit Fe(III)-ADP/NADPH-induced lipid peroxidation in rat liver microsomes and mitochondria, as well as the auto-oxidation of linoleic acid[3].
In SGC-7901 human gastric cancer cells and GES-1 cells, Totarol (0-400μM;24h) exhibited dose-dependent cytotoxicity in SGC-7901 cells, while GES-1 cells were less affected. This indicates that tocotrienol targets cancer cells and has less toxicity to normal cells (GES-1) [4]. In the hemolysis assay, Totarol（0.25-1μg/ml；30min） significantly inhibited the hemolytic effect when incubated with rabbit red blood cells at 37℃ for 30 minutes[5]. In RAW264.7 macrophages, when Totarol (0.25-1μg/ml; 16h) was co-cultured with Staphylococcus aureus culture supernatant, the release of TNF-α was reduced[6].
Totarol(0.1-10μg/kg; ip; 2-6h) reduced infarct volume and improved the neurological deficit after acute focal cerebral ischemia[7].
References:
[1]. Kelley C. Design and synthesis of novel FtsZ-targeting antibacterial agents[M]. Rutgers The State University of New Jersey, School of Graduate Studies, 2014.
[2]. Domadia P, Swarup S, Bhunia A, et al. Inhibition of bacterial cell division protein FtsZ by cinnamaldehyde[J]. Biochemical pharmacology, 2007, 74(6): 831-840.
[3]. Haraguchi H, Ishikawa H, Kubo I. Antioxidative action of diterpenoids from Podocarpus nagi[J]. Planta Medica, 1997, 63(03): 213-215.
[4]. Xu T, Huang L, Liu Z, et al. Totarol, a natural diterpenoid, induces selective antitumor activity in SGC-7901 human gastric carcinoma cells by triggering apoptosis, cell cycle disruption and suppression of cancer cell migration[J]. J. BUON., 2019, 24: 686-692.
[5]. Shi C, Zhao X, Li W, et al. Inhibitory effect of totarol on exotoxin proteins hemolysin and enterotoxins secreted by Staphylococcus aureus[J]. World Journal of Microbiology and Biotechnology, 2015, 31(10): 1565-1573.
[6]. Seca A M L, Pinto D, Silva A M S. The current status of bioactive metabolites from the genus Juniperus[J]. Bioactive phytochemicals: Perspectives for modern medicine, 2015, 3: 365-408.
[7]. Gao Y, Xu X, Chang S, et al. Totarol prevents neuronal injury in vitro and ameliorates brain ischemic stroke: Potential roles of Akt activation and HO-1 induction[J]. Toxicology and applied pharmacology, 2015, 289(2): 142-154.
| Antibacterial susceptibility testing[1]: | |
Preparation Method | The bacteria cultured at 37°C overnight with constant shaking were diluted with MH broth to adjust to a final concentration of 105 colony-forming units (CFU)/ml. Totarol was prepared in MH broth to aquire different subinhibitory concentrations (0.0625, 0.125, 0.25, 0.5, 1, 2, 4, 8, 16µg/ml) by serial microdilutions. Then a 50µl aliquot of Totarol dilutions of different subinhibitory concentrations and 50µl of the bacterial suspension were added into individual wells of a 96-well microtiter plate. Wells without Totarol treatment served as positive growth controls. Then the plates were incubated for 16 to 24h at 37°C. The MIC was defined as the lowest concentration of drug that inhibited>90% of the microorganism’s growth by optical density (OD) at 600nm using a microtiter plate reader. |
Reaction Conditions | 0.0625, 0.125, 0.25, 0.5, 1, 2, 4, 8, 16µg/ml；16-24h |
Applications | Totarol has an MIC value of 2μg/ml against Staphylococcus aureus ATCC 29213. |
| Cell experiment [2]: | |
Cell lines | Primary rat cerebellar granule cells (CGCs) |
Preparation Method | Excitotoxicity was induced by exposing cerebellar granule cells (CGCs) to 200μM glutamate for 24 hours, or by depriving them of the serum substitute B27 for 24 hours. To determine the neuroprotective effect of Totarol, cells were pretreated with different concentrations of Totarol for 24 hours. |
Reaction Conditions | 0.1-5μM; 24h |
Applications | Totarol prevents glutamate-, nutrient deprivation-, and OGD-induced neurotoxicity in CGCs in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Transient middle cerebral artery occlusion |
Preparation Method | Rats underwent transient middle cerebral artery occlusion (tMCAO) surgery. The right common carotid artery (CCA), internal carotid artery (ICA), and external carotid artery (ECA) of each rat were exposed. A single strand of nylon suture with a rounded tip (approximately 0.26mm in diameter) was inserted into the ICA through the ECA stump and gently advanced to the MCA. After 2 hours of MCAO, the suture was removed to restore blood flow (reperfusion). Body temperature was maintained at 37°C using a temperature control system. All animals had free access to food and water. Animals were randomly divided into six groups: sham group, vehicle group, Totarol (0.1μg/kg) group, Totarol (1μg/kg) group, Totarol (10μg/kg) group, and edaravone (3mg/kg) group. Edaravone was used as a positive control because of its therapeutic effect on ischemic stroke as a free radical scavenger. Totarol and edaravone were administered intravenously to the rats at 2, 4, and 6 hours after ischemia. |
Dosage form | 0.1-10μg/kg; ip; 2-6h |
Applications | Totarol reduced infarct volume and improved the neurological deficit after acute focal cerebral ischemia. |
References: | |
| Cas No. | 511-15-9 | SDF | |
| Synonyms | NSC 299936, (+)-Totarol, trans-Totarol | ||
| Chemical Name | (4bS,8aS)-4b,5,6,7,8,8a,9,10-octahydro-4b,8,8-trimethyl-1-(1-methylethyl)-2-phenanthrenol | ||
| Canonical SMILES | OC(C=C1)=C(C(C)C)C2=C1[C@]3(C)[C@](CC2)([H])C(C)(C)CCC3 | ||
| Formula | C20H30O | M.Wt | 286.5 |
| Solubility | 2mg/mL in ethanol, 10mg/mL in DMSO, 2.5mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4904 mL | 17.452 mL | 34.904 mL |
| 5 mM | 698.1 μL | 3.4904 mL | 6.9808 mL |
| 10 mM | 349 μL | 1.7452 mL | 3.4904 mL |
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)