| Description: |
Boeravinone B, a novel efflux pump inhibitor, apart from inhibiting the MdeA mediated efflux, also significantly inhibit the biofilm formation of S. aureus, boeravinone B may be used in combination with mupirocin for further development. Boeravinone B exhibits significant anti-inflammatory activity (56.6% at 50 mg/kg) when evaluated in an in vivo carrageenan-induced rat paw model. |
| Targets: |
Antifection | COX |
| In vitro: |
| Asm Microbe. 2017. | | Boeravinone B, a Natural Rotenoid from Boerhavia diffusa as Novel Inhibitor of MdeA Efflux Pump of Staphylococcus aureus[Reference: WebLink] | Role of Boeravinone B, a natural rotenoid isolated from Boerhavea diffusa, as a novel MdeA efflux inhibitor. Additionally its impact on biofilm inhibition and in vivo efficacy as topical agent is elucidated.
METHODS AND RESULTS:
Combination of Boeravinone B with mupirocin was evaluated against Staphylococcus aureus Mupr-1(MdeA over expressing) a laboratory generated mutant from S. aureus ATCC29213 using microdilution checkerboard. Time kill kinetics and mutation prevention concentration of mupirocin in combination were investigated. Mechanism of action of Boeravinone B was confirmed using ethidium bromide accumulation and efflux assay. Comparative enhancement in accumulation and efflux inhibition of ethidium bromide in presence of Boeravinone B using wild type and mutant (Mupr-1) strains indicates efflux as mechanism of resistance. A combination of 0.5% Boeravinone B with 2% mupirocin exhibited better efficacy resulting in clearance of infection in three days treatment as against 2% mupirocin which heals in 5 days when compared for CFU reduction.
CONCLUSIONS:
Boeravinone B, a novel efflux pump inhibitor, apart from inhibiting the MdeA mediated efflux, also significantly inhibit the biofilm formation of S. aureus. From these studies it is clear that Boeravinone B may be used in combination with mupirocin for further development. |
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| In vivo: |
| Journal of Natural Products, 2013 , 76 (8) :1393-8. | | Rotenoids from Boerhaavia diffusa as potential anti-inflammatory agents.[Pubmed: 23914900] |
METHODS AND RESULTS:
Five new (2, 3, 5, 7, and 9) and four known rotenoids (1, 4, 6, and 8) were isolated from a methanol extract of Boerhaavia diffusa roots. The structures of the new rotenoids were elucidated by spectroscopic data interpretation. The 70% ethanol extract, a rotenoid-rich fraction, and all isolated rotenoids were evaluated for their COX-1 and COX-2 inhibitory activities.
CONCLUSIONS:
Among the rotenoids tested, compound 7 showed the most potent COX-1 and COX-2 inhibition, with IC₅₀ values of 21.7 ± 0.5 and 25.5 ± 0.6 μM, respectively. Boeravinone B (6) exhibited significant anti-inflammatory activity (56.6% at 50 mg/kg) when evaluated in an in vivo carrageenan-induced rat paw model. |
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