Depressive effects on the central nervous system and underlying mechanism of the enzymatic extract and its phlorotannin-rich fraction from Ecklonia cava edible brown seaweed.
Marine plants have been reported to possess various pharmacological properties; however, there have been few reports on their neuropharmacological effects. Terrestrial plants have depressive effects on the central nervous system (CNS) because of their polyphenols which make them effective as anticonvulsants and sleep inducers. We investigated in this study the depressive effects of the polyphenol-rich brown seaweed, Ecklonia cava (EC), on CNS. An EC enzymatic extract (ECEE) showed significant anticonvulsive (>500 mg/kg) and sleep-inducing (>500 mg/kg) effects on the respective mice seizure induced by picrotoxin and on the mice sleep induced by pentobarbital. The phlorotannin-rich fraction (PTRF) from ECEE significantly potentiated the pentobarbital-induced sleep at >50 mg/kg. PTRF had binding activity to the gamma aminobutyric acid type A (GABA(A))-benzodiazepine (BZD) receptors. The sleep-inducing effects of diazepam (DZP, a well-known GABA(A)-BZD agonist), ECEE, and PTRF were completely blocked by flumazenil, a well-known antagonist of GABA(A)-BZD receptors. These results imply that ECEE produced depressive effects on CNS by positive allosteric modulation of its phlorotannins on GABA(A)-BZD receptors like DZP. Our study proposes EC as a candidate for the effective treatment of neuropsychiatric disorders such as anxiety and insomnia.
Korea Food Research Institute, Sungnam, Republic of Korea. smcho@kfri.re.kr
Suengmok
S
Cho
Daeseok
D
Han
Seon-Bong
SB
Kim
Minseok
M
Yoon
Hyejin
H
Yang
Young-Ho
YH
Jin
Jinho
J
Jo
Hyeim
H
Yong
Sang-Hoon
SH
Lee
You-Jin
YJ
Jeon
Makoto
M
Shimizu
D000818:Animals; D000927:Anticonvulsants / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D001569:Benzodiazepines / Q000378:metabolism; D002490:Central Nervous System / Q000187:drug effects* / Q000378:metabolism; D002491:Central Nervous System Agents / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D004798:Enzymes / Q000378:metabolism*; D008297:Male; D051379:Mice; D000459:Phaeophyceae / Q000737:chemistry* / Q000378:metabolism; D010852:Picrotoxin / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D010945:Plants, Edible / Q000737:chemistry* / Q000378:metabolism; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism; D012624:Seaweed / Q000737:chemistry* / Q000378:metabolism; D012640:Seizures / Q000139:chemically induced / Q000188:drug therapy; D012890:Sleep / Q000187:drug effects; D013634:Tannins / Q000737:chemistry*
D000927:Anticonvulsants; D001569:Benzodiazepines; D002491:Central Nervous System Agents; D004798:Enzymes; D010852:Picrotoxin; D010936:Plant Extracts; D011963:Receptors, GABA-A; D013634:Tannins