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| Targets |
Aureothricin targets the Fo subunit of ATP synthase, a key enzyme in the production of ATP. By inhibiting ATP synthase, Aureothricin disrupts energy production in bacteria, leading to cell death. Aureothricin is a dithiolopyrrolone (DTP) antibiotic. It has relatively broad-spectrum antibacterial activity and is active against Gram-positive bacteria, including Mycobacterium tuberculosis. Aureothricin also inhibits the adhesion of human umbilical vein endothelial cells (HUVECs) to vitronectin. Its complex macrocyclic structure containing sulfur atoms is critical for its biological activity.
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| ln Vitro |
In vitro studies have characterized Aureothricin as an antibiotic with relatively broad-spectrum antibacterial activity. It is active against Gram-positive bacteria, including Mycobacterium tuberculosis. Aureothricin inhibits the Fo subunit of ATP synthase, disrupting energy production in bacteria. It also inhibits the adhesion of human umbilical vein endothelial cells (HUVECs) to vitronectin. These in vitro findings establish Aureothricin as a potent antibiotic with additional effects on eukaryotic cell adhesion.
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| ln Vivo |
In vivo studies have demonstrated that Aureothricin has antitumor activity. Intraperitoneal injection of Aureothricin could inhibit the increase of ascites in transplanted mice with Aldrin ascites carcinoma. This suggests that Aureothricin may have potential as an antitumor agent, in addition to its antibacterial activity. However, specific in vivo protocols and results are not extensively detailed in the available literature. Aureothricin is used as a research tool to study antibiotic mechanisms and bacterial resistance.
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| Enzyme Assay |
The in vitro assays for Aureothricin measure its antibacterial activity and its effects on ATP synthase. Antibacterial activity is assessed using standard broth microdilution or agar diffusion assays to determine the minimum inhibitory concentration (MIC) against various bacterial strains. ATP synthase inhibition is measured using enzyme activity assays, where the inhibition of ATP hydrolysis or synthesis is assessed. The compound's effects on HUVEC adhesion to vitronectin can also be measured in vitro. These assays confirm that Aureothricin is a potent antibiotic with additional biological activities.
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| Cell Assay |
In vitro cell-based assays for Aureothricin are used to study its effects on bacterial cells and eukaryotic cells. For antibacterial assays, bacterial cultures are treated with Aureothricin, and cell viability is assessed. For studies on eukaryotic cells, HUVECs are treated with Aureothricin, and their adhesion to vitronectin is measured. The compound's effects on cell viability and function are assessed. These cell-based assays confirm that Aureothricin has antibacterial activity and affects eukaryotic cell adhesion.
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| Animal Protocol |
In vivo animal experiments for Aureothricin have been conducted in mouse models of cancer. In a typical study, mice are transplanted with Aldrin ascites carcinoma cells, and Aureothricin is administered by intraperitoneal injection. The increase in ascites is monitored, and the compound's ability to inhibit ascites formation is assessed. These studies provide evidence for the in vivo antitumor activity of Aureothricin. However, specific protocols for Aureothricin are not extensively detailed in the available literature.
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| ADME/Pharmacokinetics |
Aureothricin has a molecular weight of 242.3 g/mol and a molecular formula of C9H10N2O2S2. It is a solid compound with a purity of >98%. For storage, it is recommended to keep the compound at -20°C. The compound is stable under recommended storage conditions. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. Aureothricin is a research compound and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Aureothricin is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. Aureothricin is an antibiotic that inhibits ATP synthase, and its toxicity would be related to its effects on energy production in host cells. As with all research chemicals, standard laboratory safety precautions should be followed when handling Aureothricin. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
Epimedium is a dithiopyrrolidone antibiotic with the chemical formula 4,5-dihydro[1,2]dithio[4,3-b]pyrrole, in which the hydrogen atoms at positions 4, 5, and 6 are replaced by methyl, oxo, and propionylamino groups, respectively. It is a byproduct of thiopyrrolidone fermentation in various Streptomyces species and possesses moderate antibacterial activity. It functions as a bacterial metabolite, an angiogenesis inhibitor, an antibacterial agent, and an EC 2.7.7.6 (RNA polymerase) inhibitor. It is a dithiopyrrolidone antibiotic and a secondary amide compound. Epimedium has been reported to be present in Streptomyces flavus, Sacchariformis algerianis, and other microorganisms for which relevant data exist.
Aureothricin is a research compound and is not approved for any clinical or therapeutic use. It is a natural antibiotic that belongs to the dithiolopyrrolone (DTP) class of antibiotics. It was first isolated from Streptomyces thioluteus. Aureothricin has relatively broad-spectrum antibacterial activity. It inhibits the Fo subunit of ATP synthase and is active against Gram-positive bacteria, including Mycobacterium tuberculosis. Aureothricin inhibits the adhesion of HUVECs to vitronectin and has shown antitumor activity in mouse models. Aureothricin is used to study antibiotic mechanisms and bacterial resistance. Its mechanism of action involves inhibiting ATP synthase, disrupting energy production in bacteria. |
| Molecular Formula |
C9H10N2O2S2
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| Molecular Weight |
242.3179
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| Exact Mass |
242.018
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| CAS # |
574-95-8
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| PubChem CID |
68460
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.48g/cm3
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| Boiling Point |
479.1ºC at 760 mmHg
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| Flash Point |
243.6ºC
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| Index of Refraction |
1.694
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| LogP |
2.611
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UGZYFXMSMFMTSM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H10N2O2S2/c1-3-6(12)10-7-8-5(4-14-15-8)11(2)9(7)13/h4H,3H2,1-2H3,(H,10,12)
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| Chemical Name |
N-(4-methyl-5-oxodithiolo[4,3-b]pyrrol-6-yl)propanamide
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1268 mL | 20.6339 mL | 41.2677 mL | |
| 5 mM | 0.8254 mL | 4.1268 mL | 8.2535 mL | |
| 10 mM | 0.4127 mL | 2.0634 mL | 4.1268 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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