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Potential antimutagenic activity of berberine, a constituent of Mahonia aquifolium.

Cernáková M, Kost'álová D, Kettmann V, Plodová M, Tóth J, Drímal J - BMC Complement Altern Med (2002)

Bottom Line: It was found that the antimutagenicity of the crude Mahonia extract resides in both bis-benzylisoquinoline (BBI) and protoberberine alkaloid fractions but only the protoberberine derivatives, jatrorrhizine and berberine, showed significant concentration-dependent inhibitory effect against the AO-induced chloroplast mutagenesis of E. gracilis.While the potent antimutagenic activity of the protoberberines most likely results from the inhibition of DNA topoisomerase I, the actual mechanism(s) for the BBI alkaloids is hard to be identified.Taken together, the results indicate that berberine possesses promising antimutagenic/anticarcinogenic potential that is worth to be investigated further.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Environmental Sciences, Faculty of Chemical Technology, Slovak Technical University, SK-81237 Bratislava, Slovak Republic. cernakm@chtf.stuba.sk

ABSTRACT

Background: As part of a study aimed at developing new pharmaceutical products from natural resources, the purpose of this research was twofold: (1) to fractionate crude extracts from the bark of Mahonia aquifolium and (2) to evaluate the strength of the antimutagenic activity of the separate components against one of the common direct-acting chemical mutagens.

Methods: The antimutagenic potency was evaluated against acridine orange (AO) by using Euglena gracilis as an eukaryotic test model, based on the ability of the test compound/fraction to prevent the mutagen-induced damage of chloroplast DNA.

Results: It was found that the antimutagenicity of the crude Mahonia extract resides in both bis-benzylisoquinoline (BBI) and protoberberine alkaloid fractions but only the protoberberine derivatives, jatrorrhizine and berberine, showed significant concentration-dependent inhibitory effect against the AO-induced chloroplast mutagenesis of E. gracilis. Especially berberine elicited, at a very low dose, remarkable suppression of the AO-induced mutagenicity, its antimutagenic potency being almost three orders of magnitude higher when compared to its close analogue, jatrorrhizine. Possible mechanisms of the antimutagenic action are discussed in terms of recent literature data. While the potent antimutagenic activity of the protoberberines most likely results from the inhibition of DNA topoisomerase I, the actual mechanism(s) for the BBI alkaloids is hard to be identified.

Conclusions: Taken together, the results indicate that berberine possesses promising antimutagenic/anticarcinogenic potential that is worth to be investigated further.

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A plot of percentage of bleached colonies of E. gracilis vs. concentration of berberine at 3 concentrations of acridine orange (AO). Symbols and brackets have the same meaning as in Fig. 2.
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Figure 4: A plot of percentage of bleached colonies of E. gracilis vs. concentration of berberine at 3 concentrations of acridine orange (AO). Symbols and brackets have the same meaning as in Fig. 2.

Mentions: The dose-dependent inhibitory effect of the crude Mahonia extract, BBI alkaloids fraction, berberine and jatrorrhizine on the mutagenicity of AO applied at the above 3 concentrations is displayed in Figs. 2,3,4,5. As shown in Figs. 2 and 3, the plot of the percentage of bleached mutants vs. concentration for the Mahonia extract and the BBI fraction respectively displays typical curving even though over different concentration ranges. The lowest concentration that causes statistically significant (p < 0.05) reduction in the percentage of white colonies (as compared to the positive control) is 0.7 and 11.0 μg/ml for the Mahonia extract and the BBI alkaloids, respectively. For both samples, the decrease of the percent proportion of mutant colonies gradually continued with further increasing the concentration; however, the antimutagenic efficiency was much higher for the BBI alkaloids sample, for which the bleaching percentage (corresponding to the AO 2.3 μM curve) reaches ~5% level for the highest concentration tested.


Potential antimutagenic activity of berberine, a constituent of Mahonia aquifolium.

Cernáková M, Kost'álová D, Kettmann V, Plodová M, Tóth J, Drímal J - BMC Complement Altern Med (2002)

A plot of percentage of bleached colonies of E. gracilis vs. concentration of berberine at 3 concentrations of acridine orange (AO). Symbols and brackets have the same meaning as in Fig. 2.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC101396&req=5

Figure 4: A plot of percentage of bleached colonies of E. gracilis vs. concentration of berberine at 3 concentrations of acridine orange (AO). Symbols and brackets have the same meaning as in Fig. 2.
Mentions: The dose-dependent inhibitory effect of the crude Mahonia extract, BBI alkaloids fraction, berberine and jatrorrhizine on the mutagenicity of AO applied at the above 3 concentrations is displayed in Figs. 2,3,4,5. As shown in Figs. 2 and 3, the plot of the percentage of bleached mutants vs. concentration for the Mahonia extract and the BBI fraction respectively displays typical curving even though over different concentration ranges. The lowest concentration that causes statistically significant (p < 0.05) reduction in the percentage of white colonies (as compared to the positive control) is 0.7 and 11.0 μg/ml for the Mahonia extract and the BBI alkaloids, respectively. For both samples, the decrease of the percent proportion of mutant colonies gradually continued with further increasing the concentration; however, the antimutagenic efficiency was much higher for the BBI alkaloids sample, for which the bleaching percentage (corresponding to the AO 2.3 μM curve) reaches ~5% level for the highest concentration tested.

Bottom Line: It was found that the antimutagenicity of the crude Mahonia extract resides in both bis-benzylisoquinoline (BBI) and protoberberine alkaloid fractions but only the protoberberine derivatives, jatrorrhizine and berberine, showed significant concentration-dependent inhibitory effect against the AO-induced chloroplast mutagenesis of E. gracilis.While the potent antimutagenic activity of the protoberberines most likely results from the inhibition of DNA topoisomerase I, the actual mechanism(s) for the BBI alkaloids is hard to be identified.Taken together, the results indicate that berberine possesses promising antimutagenic/anticarcinogenic potential that is worth to be investigated further.

View Article: PubMed Central - HTML - PubMed

Affiliation: Department of Environmental Sciences, Faculty of Chemical Technology, Slovak Technical University, SK-81237 Bratislava, Slovak Republic. cernakm@chtf.stuba.sk

ABSTRACT

Background: As part of a study aimed at developing new pharmaceutical products from natural resources, the purpose of this research was twofold: (1) to fractionate crude extracts from the bark of Mahonia aquifolium and (2) to evaluate the strength of the antimutagenic activity of the separate components against one of the common direct-acting chemical mutagens.

Methods: The antimutagenic potency was evaluated against acridine orange (AO) by using Euglena gracilis as an eukaryotic test model, based on the ability of the test compound/fraction to prevent the mutagen-induced damage of chloroplast DNA.

Results: It was found that the antimutagenicity of the crude Mahonia extract resides in both bis-benzylisoquinoline (BBI) and protoberberine alkaloid fractions but only the protoberberine derivatives, jatrorrhizine and berberine, showed significant concentration-dependent inhibitory effect against the AO-induced chloroplast mutagenesis of E. gracilis. Especially berberine elicited, at a very low dose, remarkable suppression of the AO-induced mutagenicity, its antimutagenic potency being almost three orders of magnitude higher when compared to its close analogue, jatrorrhizine. Possible mechanisms of the antimutagenic action are discussed in terms of recent literature data. While the potent antimutagenic activity of the protoberberines most likely results from the inhibition of DNA topoisomerase I, the actual mechanism(s) for the BBI alkaloids is hard to be identified.

Conclusions: Taken together, the results indicate that berberine possesses promising antimutagenic/anticarcinogenic potential that is worth to be investigated further.

Show MeSH
Related in: MedlinePlus