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Identification of Neuroactive Constituents of the Ethyl Acetate Fraction from Cyperi Rhizoma Using Bioactivity-Guided Fractionation.

Sim Y, Choi JG, Gu PS, Ryu B, Kim JH, Kang I, Jang DS, Oh MS - Biomol Ther (Seoul) (2016)

Bottom Line: Cyperi Rhizoma (CR), the rhizome of Cyperus rotundus L., exhibits neuroprotective effects in in vitro and in vivo models of neuronal diseases.We first compared the anti-oxidative and neuroprotective activities of four fractions and the CRE total extract.These results provide evidence for the value of CRE as a source of multi-functional neuroprotectants, and constituents 1 and 2 may represent new candidates for further development in therapeutic use against neurodegenerative diseases.

View Article: PubMed Central - PubMed

Affiliation: Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, Republic of Korea.

ABSTRACT
Cyperi Rhizoma (CR), the rhizome of Cyperus rotundus L., exhibits neuroprotective effects in in vitro and in vivo models of neuronal diseases. Nevertheless, no study has aimed at finding the neuroactive constituent(s) of CR. In this study, we identified active compounds in a CR extract (CRE) using bioactivity-guided fractionation. We first compared the anti-oxidative and neuroprotective activities of four fractions and the CRE total extract. Only the ethyl acetate (EA) fraction revealed strong activity, and further isolation from the bioactive EA fraction yielded nine constituents: scirpusin A (1), scirpusin B (2), luteolin (3), 6'-acetyl-3,6-diferuloylsucrose (4), 4',6' diacetyl-3,6-diferuloylsucrose (5), p-coumaric acid (6), ferulic acid (7), pinellic acid (8), and fulgidic acid (9). The activities of constituents 1-9 were assessed in terms of anti-oxidative, neuroprotective, anti-inflammatory, and anti-amyloid-β activities. Constituents 1, 2, and 3 exhibited strong activities; constituents 1 and 2 were characterized for the first time in this study. These results provide evidence for the value of CRE as a source of multi-functional neuroprotectants, and constituents 1 and 2 may represent new candidates for further development in therapeutic use against neurodegenerative diseases.

No MeSH data available.


Related in: MedlinePlus

Inhibitory effects of constituents 1–9 on Aβ aggregation. Values are indicated as the mean ± SEM. ***p<0.001; mean values were significantly different from the control group.
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f5-bt-24-438: Inhibitory effects of constituents 1–9 on Aβ aggregation. Values are indicated as the mean ± SEM. ***p<0.001; mean values were significantly different from the control group.

Mentions: Aβ acts as a neurotoxin to cells in culture via multiple pathways and its toxicity is correlated with the degree of peptide aggregation (Rivière et al., 2010). Inhibition of Aβ fibril formation is an attractive therapeutic and preventive strategy in the development of disease-modifying drugs for AD (Fujiwara et al., 2009). We compared the inhibitory effects of constituents 1–9 on Aβ aggregation using fluorescence spectroscopy with ThT, a cationic benzothiazole dye, which is used widely for the identification and quantification of Aβ fibrils in vitro (Vassar and Culling, 1959). Treatment with curcumin and constituents 1, 2, 3, and 9 (100 μM) significantly inhibited the aggregation of monomeric Aβ1–42 (100 μM), as demonstrated by reduced ThT fluorescence intensity compared with the control group (Fig. 5).


Identification of Neuroactive Constituents of the Ethyl Acetate Fraction from Cyperi Rhizoma Using Bioactivity-Guided Fractionation.

Sim Y, Choi JG, Gu PS, Ryu B, Kim JH, Kang I, Jang DS, Oh MS - Biomol Ther (Seoul) (2016)

Inhibitory effects of constituents 1–9 on Aβ aggregation. Values are indicated as the mean ± SEM. ***p<0.001; mean values were significantly different from the control group.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4930289&req=5

f5-bt-24-438: Inhibitory effects of constituents 1–9 on Aβ aggregation. Values are indicated as the mean ± SEM. ***p<0.001; mean values were significantly different from the control group.
Mentions: Aβ acts as a neurotoxin to cells in culture via multiple pathways and its toxicity is correlated with the degree of peptide aggregation (Rivière et al., 2010). Inhibition of Aβ fibril formation is an attractive therapeutic and preventive strategy in the development of disease-modifying drugs for AD (Fujiwara et al., 2009). We compared the inhibitory effects of constituents 1–9 on Aβ aggregation using fluorescence spectroscopy with ThT, a cationic benzothiazole dye, which is used widely for the identification and quantification of Aβ fibrils in vitro (Vassar and Culling, 1959). Treatment with curcumin and constituents 1, 2, 3, and 9 (100 μM) significantly inhibited the aggregation of monomeric Aβ1–42 (100 μM), as demonstrated by reduced ThT fluorescence intensity compared with the control group (Fig. 5).

Bottom Line: Cyperi Rhizoma (CR), the rhizome of Cyperus rotundus L., exhibits neuroprotective effects in in vitro and in vivo models of neuronal diseases.We first compared the anti-oxidative and neuroprotective activities of four fractions and the CRE total extract.These results provide evidence for the value of CRE as a source of multi-functional neuroprotectants, and constituents 1 and 2 may represent new candidates for further development in therapeutic use against neurodegenerative diseases.

View Article: PubMed Central - PubMed

Affiliation: Department of Life and Nanopharmaceutical Sciences, Graduate School, Kyung Hee University, Seoul 02447, Republic of Korea.

ABSTRACT
Cyperi Rhizoma (CR), the rhizome of Cyperus rotundus L., exhibits neuroprotective effects in in vitro and in vivo models of neuronal diseases. Nevertheless, no study has aimed at finding the neuroactive constituent(s) of CR. In this study, we identified active compounds in a CR extract (CRE) using bioactivity-guided fractionation. We first compared the anti-oxidative and neuroprotective activities of four fractions and the CRE total extract. Only the ethyl acetate (EA) fraction revealed strong activity, and further isolation from the bioactive EA fraction yielded nine constituents: scirpusin A (1), scirpusin B (2), luteolin (3), 6'-acetyl-3,6-diferuloylsucrose (4), 4',6' diacetyl-3,6-diferuloylsucrose (5), p-coumaric acid (6), ferulic acid (7), pinellic acid (8), and fulgidic acid (9). The activities of constituents 1-9 were assessed in terms of anti-oxidative, neuroprotective, anti-inflammatory, and anti-amyloid-β activities. Constituents 1, 2, and 3 exhibited strong activities; constituents 1 and 2 were characterized for the first time in this study. These results provide evidence for the value of CRE as a source of multi-functional neuroprotectants, and constituents 1 and 2 may represent new candidates for further development in therapeutic use against neurodegenerative diseases.

No MeSH data available.


Related in: MedlinePlus