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Equisetin

Cat. No. M8737
Equisetin Structure
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Biological Activity

Equisetin is a tetramic acid analog derived from Fusarium equisti. Equisetin is mainly known for its antibiotic and cytotoxic activity and for its inhibitory effect on HIV-1 integrase. Inhibition of HIV integrase by Equisetin was reported with IC50 values of 5-20 μM. Moreover, it was shown that Equisetin specifically inhibits the substrate anion carriers of the inner membrane of mitochondria and acts nonspecifically on protein membranes and protein hydrophobic domains. In addition, it was demonstrated that Equisetin causes phytotoxicity by causing root Necrosis and was also identified in a mycotoxin cocktail associated with cattle feeding problems.

Chemical Information
Molecular Weight 373.49
Formula C22H31NO4
CAS Number 57749-43-6
Solubility (25°C) DMSO: soluble 1 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Qi Zhang, et al. Equisetin Restores Colistin Sensitivity against Multi-Drug Resistant Gram-Negative Bacteria

[2] Erica C Larson, et al. Pyrrolocin C and equisetin inhibit bacterial acetyl-CoA carboxylase

[3] Mengmeng Zhang, et al. Equisetin as potential quorum sensing inhibitor of Pseudomonas aeruginosa

[4] Xiaojun Li, et al. Chemo-enzymatic synthesis of equisetin

[5] Jun Yin, et al. Biomimetic synthesis of equisetin and (+)-fusarisetin A

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