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Antiaggregation Potential of Padina gymnospora against the Toxic Alzheimer's Beta-Amyloid Peptide 25-35 and Cholinesterase Inhibitory Property of Its Bioactive Compounds.

Shanmuganathan B, Sheeja Malar D, Sathya S, Pandima Devi K - PLoS ONE (2015)

Bottom Line: The results were further confirmed by confocal laser scanning microscopy (CLSM) analysis and Fourier transform infrared (FTIR) spectroscopic analysis.Finally, the active fraction was subjected to LC-MS/MS analysis for the identification of bioactive compounds.Overall, the results suggest that the bioactive compound alpha bisabolol present in the alga might be responsible for the observed cholinesterase inhibition with the IC50 value < 10 μg/ml for both AChE and BuChE when compared to standard drug donepezil (IC50 value < 6 μg/ml) and support its use for the treatment of neurological disorders.

View Article: PubMed Central - PubMed

Affiliation: Department of Biotechnology, Alagappa University (Science campus), Karaikudi- 630 004, Tamil Nadu, India.

ABSTRACT
Inhibition of β-amyloid (Aβ) aggregation in the cerebral cortex of the brain is a promising therapeutic and defensive strategy in identification of disease modifying agents for Alzheimer's disease (AD). Since natural products are considered as the current alternative trend for the discovery of AD drugs, the present study aims at the evaluation of anti-amyloidogenic potential of the marine seaweed Padina gymnospora. Prevention of aggregation and disaggregation of the mature fibril formation of Aβ 25-35 by acetone extracts of P. gymnospora (ACTPG) was evaluated in two phases by Thioflavin T assay. The results were further confirmed by confocal laser scanning microscopy (CLSM) analysis and Fourier transform infrared (FTIR) spectroscopic analysis. The results of antiaggregation and disaggregation assay showed that the increase in fluorescence intensity of aggregated Aβ and the co-treatment of ACTPG (250 μg/ml) with Aβ 25-35, an extensive decrease in the fluorescence intensity was observed in both phases, which suggests that ACTPG prevents the oligomers formation and disaggregation of mature fibrils. In addition, ACTPG was subjected to column chromatography and the bioactivity was screened based on the cholinesterase inhibitory activity. Finally, the active fraction was subjected to LC-MS/MS analysis for the identification of bioactive compounds. Overall, the results suggest that the bioactive compound alpha bisabolol present in the alga might be responsible for the observed cholinesterase inhibition with the IC50 value < 10 μg/ml for both AChE and BuChE when compared to standard drug donepezil (IC50 value < 6 μg/ml) and support its use for the treatment of neurological disorders.

No MeSH data available.


Related in: MedlinePlus

AChE inhibitory activity of the column fractions (F1-F18).The eluted fractions (F1-F18) were subjected to AChE inhibitory assay. Among the fractions, F10 (EA: MET-9:1) showed highest inhibitory activity (93%) against AChE, but similar when compared to positive control donepezil (97%). Values are expressed as Mean ± SD (n = 3).
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pone.0141708.g005: AChE inhibitory activity of the column fractions (F1-F18).The eluted fractions (F1-F18) were subjected to AChE inhibitory assay. Among the fractions, F10 (EA: MET-9:1) showed highest inhibitory activity (93%) against AChE, but similar when compared to positive control donepezil (97%). Values are expressed as Mean ± SD (n = 3).

Mentions: Bioactive fractions were eluted with linear gradient of solvent with increasing polarity and 18 fractions (F1-F18) were collected based on polarity from n-hexane to water as represented in Fig 4. Eluted fractions were subjected to cholinesterase inhibitory assays. Among the different fractions F10 showed potent cholinesterase inhibitory activity. Results of AChE and BuChE inhibitory activity were illustrated in Figs 5 and 6. Among the fractions, F10 (EA: MET-9:1) showed highest inhibitory activity (93 and 88%) against AChE and BuChE, but similar when compared to positive control donepezil (97 and 91% respectively).


Antiaggregation Potential of Padina gymnospora against the Toxic Alzheimer's Beta-Amyloid Peptide 25-35 and Cholinesterase Inhibitory Property of Its Bioactive Compounds.

Shanmuganathan B, Sheeja Malar D, Sathya S, Pandima Devi K - PLoS ONE (2015)

AChE inhibitory activity of the column fractions (F1-F18).The eluted fractions (F1-F18) were subjected to AChE inhibitory assay. Among the fractions, F10 (EA: MET-9:1) showed highest inhibitory activity (93%) against AChE, but similar when compared to positive control donepezil (97%). Values are expressed as Mean ± SD (n = 3).
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4633220&req=5

pone.0141708.g005: AChE inhibitory activity of the column fractions (F1-F18).The eluted fractions (F1-F18) were subjected to AChE inhibitory assay. Among the fractions, F10 (EA: MET-9:1) showed highest inhibitory activity (93%) against AChE, but similar when compared to positive control donepezil (97%). Values are expressed as Mean ± SD (n = 3).
Mentions: Bioactive fractions were eluted with linear gradient of solvent with increasing polarity and 18 fractions (F1-F18) were collected based on polarity from n-hexane to water as represented in Fig 4. Eluted fractions were subjected to cholinesterase inhibitory assays. Among the different fractions F10 showed potent cholinesterase inhibitory activity. Results of AChE and BuChE inhibitory activity were illustrated in Figs 5 and 6. Among the fractions, F10 (EA: MET-9:1) showed highest inhibitory activity (93 and 88%) against AChE and BuChE, but similar when compared to positive control donepezil (97 and 91% respectively).

Bottom Line: The results were further confirmed by confocal laser scanning microscopy (CLSM) analysis and Fourier transform infrared (FTIR) spectroscopic analysis.Finally, the active fraction was subjected to LC-MS/MS analysis for the identification of bioactive compounds.Overall, the results suggest that the bioactive compound alpha bisabolol present in the alga might be responsible for the observed cholinesterase inhibition with the IC50 value < 10 μg/ml for both AChE and BuChE when compared to standard drug donepezil (IC50 value < 6 μg/ml) and support its use for the treatment of neurological disorders.

View Article: PubMed Central - PubMed

Affiliation: Department of Biotechnology, Alagappa University (Science campus), Karaikudi- 630 004, Tamil Nadu, India.

ABSTRACT
Inhibition of β-amyloid (Aβ) aggregation in the cerebral cortex of the brain is a promising therapeutic and defensive strategy in identification of disease modifying agents for Alzheimer's disease (AD). Since natural products are considered as the current alternative trend for the discovery of AD drugs, the present study aims at the evaluation of anti-amyloidogenic potential of the marine seaweed Padina gymnospora. Prevention of aggregation and disaggregation of the mature fibril formation of Aβ 25-35 by acetone extracts of P. gymnospora (ACTPG) was evaluated in two phases by Thioflavin T assay. The results were further confirmed by confocal laser scanning microscopy (CLSM) analysis and Fourier transform infrared (FTIR) spectroscopic analysis. The results of antiaggregation and disaggregation assay showed that the increase in fluorescence intensity of aggregated Aβ and the co-treatment of ACTPG (250 μg/ml) with Aβ 25-35, an extensive decrease in the fluorescence intensity was observed in both phases, which suggests that ACTPG prevents the oligomers formation and disaggregation of mature fibrils. In addition, ACTPG was subjected to column chromatography and the bioactivity was screened based on the cholinesterase inhibitory activity. Finally, the active fraction was subjected to LC-MS/MS analysis for the identification of bioactive compounds. Overall, the results suggest that the bioactive compound alpha bisabolol present in the alga might be responsible for the observed cholinesterase inhibition with the IC50 value < 10 μg/ml for both AChE and BuChE when compared to standard drug donepezil (IC50 value < 6 μg/ml) and support its use for the treatment of neurological disorders.

No MeSH data available.


Related in: MedlinePlus