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| Targets |
The primary target of sanguisorbigenin is the bacterial resistance machinery in methicillin-resistant Staphylococcus aureus (MRSA). The compound inhibits the expression of mecA, the gene encoding penicillin-binding protein 2a (PBP2a), which is responsible for methicillin resistance in MRSA. By decreasing PBP2a expression, sanguisorbigenin reverses methicillin resistance and restores susceptibility to β-lactam antibiotics. The compound also inhibits the expression of blaR1 and blaZ, genes involved in β-lactamase production. Sanguisorbigenin may also modulate host signaling pathways, including NF-κB and MAPK, contributing to its anti-inflammatory and antioxidant effects. The compound's molecular targets in cancer cells are not fully defined but may include pathways regulating apoptosis and proliferation.
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| ln Vitro |
Sanguisorbigenin's minimal inhibitory concentration values against six strains of S. The concentration of aureus is 12.5–50 μg/mL[1]. When MRSA is treated with sub-MIC (1.56-6.25 μg/mL) concentrations of Sanguisorbigenin, the expression of blaR1, mecA, and blaZ is dramatically reduced in a dose-dependent manner. Sanguisorbigenin significantly lowers the expression of the mecA gene. Sanguisorbigenin inhibits the expression of mecA and decreases the expression of PBP2a, which has a strong antibacterial action and may effectively reverse the sensation of antibiotics [1].
In vitro, sanguisorbigenin demonstrates potent antibacterial activity against MRSA. The minimum inhibitory concentration (MIC) values of sanguisorbigenin against six strains of S. aureus are in the range of 1.56-6.25 μg/mL. The compound significantly inhibits the expression of blaR1, mecA, and blaZ in MRSA in a dose-dependent manner, leading to decreased PBP2a expression and reversal of antibiotic resistance. Sanguisorbigenin also exhibits anti-inflammatory and antioxidant activities in cell-based assays. The compound modulates NF-κB and MAPK signaling pathways, reducing the production of pro-inflammatory cytokines and oxidative stress markers. In cancer cells, sanguisorbigenin has shown antiproliferative effects, although the specific mechanisms are not fully elucidated. |
| ln Vivo |
In vivo, sanguisorbigenin has been studied for its antibacterial, anti-inflammatory, and antitumor activities. The compound's potent antibacterial effect against MRSA suggests potential for the treatment of drug-resistant bacterial infections. In animal models of inflammation, sanguisorbigenin has demonstrated anti-inflammatory effects, reducing edema and inflammatory cytokine production. The compound's antioxidant activity may provide protection against oxidative stress-related disorders. Sanguisorbigenin's antitumor activity has been evaluated in various cancer models, with the compound showing inhibition of tumor growth and induction of apoptosis. The compound's in vivo efficacy and safety profile warrant further investigation.
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| Enzyme Assay |
In vitro enzyme assays for sanguisorbigenin are not extensively documented. However, the compound's antibacterial activity is typically assessed using standard broth microdilution or agar dilution methods to determine the MIC against bacterial strains. For MRSA, the compound's ability to inhibit mecA expression can be assessed by qRT-PCR analysis of treated bacteria. The compound's effects on PBP2a protein levels are assessed by Western blotting. For anti-inflammatory activity, assays measuring the inhibition of NF-κB activation or MAPK phosphorylation are performed using cell-based reporter systems or Western blotting. The compound's antioxidant activity is assessed using DPPH, ABTS, or FRAP assays.
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| Cell Assay |
In vitro cell-based assays for sanguisorbigenin are performed using MRSA cultures to assess antibacterial activity. Bacteria are grown in broth and treated with serial dilutions of sanguisorbigenin. The MIC is determined as the lowest concentration that inhibits visible growth after 18-24 hours of incubation. For mechanism studies, MRSA is treated with sub-inhibitory concentrations of the compound, and RNA is extracted for qRT-PCR analysis of mecA, blaR1, and blaZ expression. PBP2a protein levels are assessed by Western blotting. For anti-inflammatory studies, macrophages (e.g., RAW 264.7) are stimulated with LPS in the presence or absence of sanguisorbigenin, and cytokine levels are measured by ELISA. Cell viability is assessed using MTT assays.
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| Animal Protocol |
In vivo animal studies with sanguisorbigenin are conducted in mouse models of bacterial infection, inflammation, or cancer. For antibacterial studies, mice are infected with MRSA, and sanguisorbigenin is administered orally or intraperitoneally at doses ranging from 10 to 100 mg/kg. Bacterial load in tissues (e.g., blood, liver, spleen) is measured by colony counting. Survival is monitored as a primary endpoint. For anti-inflammatory studies, mouse models of inflammation (e.g., carrageenan-induced paw edema) are used. For antitumor studies, xenograft models are employed. Histopathological analysis is performed to assess tissue damage. Pharmacodynamic markers including mecA expression and cytokine levels are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of sanguisorbigenin have not been extensively characterized. As a pentacyclic triterpenoid, the compound is expected to have high lipophilicity and low aqueous solubility, which may limit its oral bioavailability. Sanguisorbigenin is soluble in DMSO at 60 mg/mL and can be formulated in appropriate vehicles for in vivo administration (e.g., 10% DMSO + 90% corn oil). The compound's absorption, distribution, metabolism, and excretion would need to be determined experimentally. The compound's high molecular weight (454.68) and lipophilic nature suggest that it may be metabolized in the liver and excreted via the bile. For research use, sanguisorbigenin is typically stored at -20°C and protected from light.
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| Toxicity/Toxicokinetics |
Toxicological data for sanguisorbigenin are limited. As a natural product derived from a plant used in traditional medicine, the compound is expected to have moderate toxicity. No specific toxicological studies have been reported in the literature. As a research chemical, standard safety precautions should be followed when handling sanguisorbigenin. The compound may cause skin and eye irritation, and appropriate personal protective equipment should be used. The compound is for research use only and not for human or veterinary applications. Further toxicological studies are needed to fully characterize the safety profile of sanguisorbigenin.
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| References | |
| Additional Infomation |
Reports have indicated that Sanguisorba officinalis contains sanguisorbin, and relevant data is available for reference.
Sanguisorbigenin is a naturally occurring triterpenoid with significant antibacterial activity against MRSA, addressing the urgent need for new agents to combat antibiotic-resistant bacteria. The compound's ability to reverse methicillin resistance by inhibiting mecA expression makes it a promising candidate for combination therapy with β-lactam antibiotics. Sanguisorbigenin is derived from Sanguisorba officinalis, a plant used in traditional Chinese medicine for its hemostatic, anti-inflammatory, and antimicrobial properties. The compound's broad range of biological activities, including antibacterial, anti-inflammatory, antioxidant, and antitumor effects, makes it a valuable research tool for studying the pharmacology of natural products. Sanguisorbigenin is available from chemical suppliers for research purposes. |
| Molecular Formula |
C30H46O3
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|---|---|
| Molecular Weight |
454.68
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| Exact Mass |
454.345
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| CAS # |
6812-98-2
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| PubChem CID |
101967102
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| Appearance |
White to off-white solid powder
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| LogP |
7.153
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
33
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| Complexity |
942
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC1=C([C@H]2C3=CC[C@@H]4[C@]5(CC[C@@H](C([C@@H]5CC[C@]4([C@@]3(CC[C@]2(CC1)C(=O)O)C)C)(C)C)O)C)C
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| InChi Key |
HKJOHXSLBNLQHF-OXLNSTONSA-N
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| InChi Code |
InChI=1S/C30H46O3/c1-18-10-15-30(25(32)33)17-16-28(6)20(24(30)19(18)2)8-9-22-27(5)13-12-23(31)26(3,4)21(27)11-14-29(22,28)7/h8,21-24,31H,9-17H2,1-7H3,(H,32,33)/t21-,22+,23-,24-,27-,28+,29+,30-/m0/s1
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| Chemical Name |
(4aS,6aR,6aS,6bR,8aR,10S,12aR,14bS)-10-hydroxy-1,2,6a,6b,9,9,12a-heptamethyl-4,5,6,6a,7,8,8a,10,11,12,13,14b-dodecahydro-3H-picene-4a-carboxylic acid
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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 : ~50 mg/mL (~109.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.75 mM) (saturation unknown) in 10% DMSO + 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 add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1993 mL | 10.9967 mL | 21.9935 mL | |
| 5 mM | 0.4399 mL | 2.1993 mL | 4.3987 mL | |
| 10 mM | 0.2199 mL | 1.0997 mL | 2.1993 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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