Piperine as an inhibitor of Rv1258c, a putative multidrug efflux pump of Mycobacterium tuberculosis

Sharma, Sandeep; Kumar, Manoj; Sharma, Sujata; Nargotra, Amit; Koul, Surrinder; Khan, Inshad Ali

doi:10.1093/jac/dkq186

Cited by 174 publications

(106 citation statements)

References 28 publications

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“…There are several reports in the literature where natural products have demonstrated enhancement of antimicrobial activity (Khan et al, 2006;Stavri et al, 2007;Werle, 2008;Kumar et al, 2008;Lechner et al, 2008;Sharma et al, 2010). However, the number of natural compounds behaving synergistically with antifungals is minimal.…”

Section: Introductionmentioning

confidence: 99%

In vitro antifungal activities of amphotericin B in combination with acteoside, a phenylethanoid glycoside from Colebrookea oppositifolia

Ali

Sharma

Suri

et al. 2011

Journal of Medical Microbiology

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This study was undertaken to investigate the synergistic interaction between amphotericin B (AmB) and acteoside, isolated from the aerial parts of the shrub Colebrookea oppositifolia (Lamiaceae). Acteoside alone exhibited no intrinsic antifungal activity but showed a potent synergism in combination with AmB against selected pathogenic species, with fractional inhibitory concentration indices in the range of 0.0312-0.1562. The combination of acteoside at 3.12 and 12.5 mg ml -1 with subinhibitory concentrations of AmB resulted in a potent fungicidal effect and also exhibited a significantly extended post-antifungal effect. Furthermore, the combination also reduced the minimum biofilm reduction concentration values of AmB (2-16-fold) in preformed biofilms of Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus. There was decreased viability of the cells, increased uptake of propidium iodide and enhanced leakage of 260 nm-absorbing material by Candida albicans cells when exposed to AmB in the presence of acteoside. The reason for potentiation is likely to be that the subinhibitory concentrations of AmB facilitated the uptake of acteoside, which resulted in increased killing of the fungal cells. Administration of acteoside in mice at up to 2000 mg (kg body weight) "1 by the intraperitoneal or oral route produced no overt toxicity. The data presented here support synergism between acteoside and AmB, and it is therefore proposed that a prospective new management strategy for therapeutic application of this combination should be explored.

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Section: Introductionmentioning

confidence: 99%

In vitro antifungal activities of amphotericin B in combination with acteoside, a phenylethanoid glycoside from Colebrookea oppositifolia

Ali

Sharma

Suri

et al. 2011

Journal of Medical Microbiology

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“…Among eleven piperic acid ester derivatives, 2-(3,4-dihydroxyphenyl)ethyl ester [4] showed the highest cytotoxicity against OSCC cell lines (mean CC 50 =17 μM), followed by (4-methoxyphenyl)methyl ester (38 μM) [1], 2-(4-methoxyphenyl)ethyl ester [5] (42 μM), 2-(4-hydroxyphenyl)ethyl ester (46 μM) [3], 2-phenylethyl ester [7] (61 μM) and 2-(3,4-dimethoxyphenyl)ethyl ester [6] (102 μM). On the other hand, (4-hydroxy-3-methoxyphenyl)methyl ester [2] (>368 μM), 3-phenylpropyl ester [8], 4-phenyl-2-butyl ester [9], 4-phenylbutyl ester [10] and decyl ester [11] (>400 μM) were essentially inactive (Table I).…”

Section: Resultsmentioning

confidence: 99%

“…When four OSCC cell lines and three normal oral cells were used, [1] showed the highest TS value (>10.5), followed by [4] (8.0), [7] (>6.6), [3] (2.6), [6] (1.9), [5] Table I). [4] showed the highest PSE value (47.0), followed by [1] (>27.8), [7] (>10.8), [3] (5.7), [5] Table I). …”

Section: Resultsmentioning

confidence: 99%

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Quantitative Structure–Cytotoxicity Relationship of Newly Synthesized Piperic Acid Esters

Sakagami

Uesawa

Masuda

et al. 2017

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“…; such as its role in inhibition of Rv1258c, a putative multidrug efflux pump of M. tuberculosis. 46 The piperine we obtained from the endophytic Periconia sp. was naturally functional and the spectroscopic study of this compound revealed 99% similarity with piperine from the host itself.…”

Section: Resultsmentioning

confidence: 99%

Piperine production by endophytic fungus Periconia sp. Isolated from Piper longum L.

et al. 2011

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The endophytic fungus Periconia sp. produces piperine (5-(3, 4-methylenedioxyphenyl)-1-piperidinopent-2, 4-dien-1-one) under liquid culture. This is the first report of the alternative source for this chemical other than its host, Piper longum. The highly functionalized fungus-derived piperine exhibits strong antimycobacterial activity against Mycobacterium tuberculosis and M. smegmetis with minimum inhibitory concentrations of 1.74 and 2.62 lg ml À1 , respectively. The compound was crystallized and the structure was elucidated by single-crystal X-ray crystallography. This finding is of significance as piperine is a potential cancer preventative agent. It is reaffirmed by this report that important pharmaceuticals can be produced by endophytic microbes, and these molecules appear to be mimetic to their host origin. Therefore, we can enhance the bioactive principles of medicinal plants by isolating and identifying the endophytes, thereby showing the importance of preserving the biodiversity of these plants.

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Piperine as an inhibitor of Rv1258c, a putative multidrug efflux pump of Mycobacterium tuberculosis

Abstract: The results of this study are suggestive of piperine's involvement in the inhibition of clinically overexpressed mycobacterial putative efflux protein (Rv1258c). Piperine may be useful in augmenting the antimycobacterial activity of rifampicin in a clinical setting.

Cited by 174 publications

References 28 publications

In vitro antifungal activities of amphotericin B in combination with acteoside, a phenylethanoid glycoside from Colebrookea oppositifolia

In vitro antifungal activities of amphotericin B in combination with acteoside, a phenylethanoid glycoside from Colebrookea oppositifolia

Quantitative Structure–Cytotoxicity Relationship of Newly Synthesized Piperic Acid Esters

Piperine production by endophytic fungus Periconia sp. Isolated from Piper longum L.

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