| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Boeravinone B primarily targets two distinct efflux pumps: the NorA bacterial efflux pump of Staphylococcus aureus and human P-glycoprotein (P-gp, also known as ABCB1/MDR1). It is a dual (bifunctional) inhibitor of these transporters. By inhibiting NorA, it reduces bacterial multidrug resistance; by inhibiting P-gp, it may increase the intracellular accumulation of chemotherapeutic agents and reverse multidrug resistance in cancer cells.
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| ln Vitro |
Additionally effective against a methicillin-resistant S is boeravinone B. aureus (MRSA) strain, whose ciprofloxacin MIC was reduced by four times[1].
In vitro, Boeravinone B acts as a dual inhibitor of the NorA bacterial efflux pump of S. aureus and human P-gp. It reduces the formation of bacterial biofilm and inhibits the intracellular invasion of bacteria. The compound has also been shown to have anti-aging and anti-apoptotic effects during oxidative stress. At a concentration of 50 ug, it exhibits approximately 56.6% anti-inflammatory activity. It is also active against methicillin-resistant S. aureus (MRSA) strains. |
| ln Vivo |
In vivo, Boeravinone B exhibits significant anti-inflammatory activity in the carrageenan-induced rat paw edema model at a concentration of 50 ug (56.6% inhibition). Additionally, as a P-glycoprotein inhibitor, it may reverse multidrug resistance and enhance the efficacy of co-administered chemotherapeutic agents in resistant tumor models. However, detailed in vivo efficacy data for this specific compound in other disease models is limited.
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| Enzyme Assay |
The in vitro protocol for evaluating P-gp inhibition by Boeravinone B typically involves a rhodamine-123 accumulation assay. Multidrug-resistant cancer cells (e.g., MCF-7/ADR) are seeded in 96-well plates and treated with varying concentrations of Boeravinone B (0.1-50 uM) for 1-2 hours, followed by the addition of rhodamine-123 (a fluorescent P-gp substrate). After incubation, cells are washed and the intracellular fluorescence intensity is measured using a microplate reader (Ex/Em = 485/528 nm). An increase in fluorescence compared to the untreated control indicates P-gp inhibition.
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| Cell Assay |
For in vitro cellular assays, S. aureus strains (including MRSA) are cultured in broth medium overnight. The culture is diluted to an OD600 of 0.05 and treated with Boeravinone B at concentrations of 10-100 ug/mL in 96-well plates. Biofilm formation is quantified by staining with 0.1% crystal violet for 15 minutes, followed by solubilization in 95% ethanol and measuring absorbance at 570 nm. The intracellular invasion of bacteria into host cells (e.g., A549 lung epithelial cells) can be assessed using a gentamicin protection assay. Cell viability is assessed via the MTT assay to confirm that observed effects are not due to cytotoxicity.
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| Animal Protocol |
The in vivo anti-inflammatory activity of Boeravinone B is assessed using the carrageenan-induced rat paw edema model. Male Wistar rats (150-200 g) are randomly divided into groups (n=6). Boeravinone B is administered intraperitoneally at a dose of 50 ug/rat (formulated in 0.5% carboxymethylcellulose) 1 hour prior to the subplantar injection of 0.1 mL of 1% carrageenan into the right hind paw. Paw volume is measured using a plethysmometer at 0, 1, 2, 3, and 4 hours after carrageenan injection. The percentage inhibition of edema is calculated by comparing the increase in paw volume between treatment and control groups.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Boeravinone B is not extensively published. As a natural rotenoid isolated from plant sources, it is expected to have moderate oral bioavailability and is likely metabolized by hepatic cytochrome P450 enzymes. Its lipophilic nature suggests good tissue penetration. For research purposes, it is typically administered intraperitoneally to achieve systemic exposure. ADMET studies have been performed using in silico molecular docking targeting the cannabinoid receptor, but experimental PK parameters such as T1/2, Cmax, and AUC are not available.
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| Toxicity/Toxicokinetics |
Boeravinone B has been evaluated for in vitro safety using cell viability assays (e.g., MTT assay) and was found to have no significant cytotoxicity at effective concentrations. ADMET analysis has been conducted via in silico docking to predict potential toxicity. As a natural product, it is generally considered to have a low toxicity profile, though comprehensive toxicological studies (e.g., acute and repeat-dose toxicity in rodents) have not been published. Standard safety precautions for handling natural products should be followed.
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| References |
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| Additional Infomation |
According to existing data, boravirone B has been reported in Mirabilis jalapa and Hedyotis diffusa.
Boeravinone B is a research-grade natural product and is not approved for clinical use. Its molecular formula is C17H12O6 with a molecular weight of 312.27. It is a dual inhibitor of NorA (S. aureus) and human P-glycoprotein, making it a valuable tool for studying bacterial efflux pump inhibition, reversal of multidrug resistance, and anti-inflammatory mechanisms. The compound is isolated from Boerhaavia diffusa, a plant traditionally used in Indian medicine for its diuretic and kidney-protective properties. |
| Molecular Formula |
C17H12O6
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|---|---|
| Molecular Weight |
312.27
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| Exact Mass |
312.063
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| CAS # |
114567-34-9
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| PubChem CID |
14018348
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
640.1±55.0 °C at 760 mmHg
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| Flash Point |
244.3±25.0 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.772
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
23
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| Complexity |
543
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C2=C(C=C1O)OC3=C(C2=O)C4=CC=CC=C4OC3O)O
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| InChi Key |
YVVDYYFGAWQOGB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12O6/c1-7-9(18)6-11-13(14(7)19)15(20)12-8-4-2-3-5-10(8)23-17(21)16(12)22-11/h2-6,17-19,21H,1H3
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| Chemical Name |
6,9,11-trihydroxy-10-methyl-6H-chromeno[3,4-b]chromen-12-one
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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: 50 mg/mL (160.12 mM)
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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 | 3.2024 mL | 16.0118 mL | 32.0236 mL | |
| 5 mM | 0.6405 mL | 3.2024 mL | 6.4047 mL | |
| 10 mM | 0.3202 mL | 1.6012 mL | 3.2024 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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