2011
DOI: 10.1021/np200181d
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Positive GABAA Receptor Modulators from Acorus calamus and Structural Analysis of (+)-Dioxosarcoguaiacol by 1D and 2D NMR and Molecular Modeling

Abstract: In a two-microelectrode voltage clamp with Xenopus laevis oocytes, a petroleum ether extract of Acorus calamus rhizomes enhanced the GABA-induced chloride current through GABA A receptors of the α 1 β 2 γ 2S subtype by 277% ± 9.7% (100 μg/mL). β-Asarone (1), (+)-dioxosarcoguaiacol (2), (+)-shyobunone (3), and (+)-preisocalamenediol (4) were subsequently identified as main active principles through HPLC-based activity profiling and targeted isolation. The compounds induced maximum potentiation of the chloride c… Show more

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Cited by 34 publications
(27 citation statements)
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“…Based on the latest finding that b-asarone potentiated the response of recombinant GABA A Rs expressed in Xenopus oocytes (Zaugg et al, 2011), we hypothesized that a-asarone might exert its effect through activation of GABA A Rs. As shown in Fig.…”
Section: Activation Of Gaba a Rs In Hippocampal Neurons By A-asaronementioning
confidence: 99%
“…Based on the latest finding that b-asarone potentiated the response of recombinant GABA A Rs expressed in Xenopus oocytes (Zaugg et al, 2011), we hypothesized that a-asarone might exert its effect through activation of GABA A Rs. As shown in Fig.…”
Section: Activation Of Gaba a Rs In Hippocampal Neurons By A-asaronementioning
confidence: 99%
“…This compound has now been isolated from Acorus calamus. 172 Chemical examinations of the roots of Nardostachys chinensis afforded two antimalarial guaiane endoperoxides, nardoperoxide 305 and isonardoperoxide 306, whose absolute stereochemistries were determined by CD spectra. The endoperoxide moiety of the molecules was assumed to relate to the antimalarial activity.…”
mentioning
confidence: 99%
“…Synergism may also involve multitarget effects by acting on enzymes, metabolites, proteins, receptors, and ionic channels (Wagner and Ulrich-Merzenich, 2009). There are several examples of synergism in plants or formulations with psychoactive effects, including Cannabis sativa L., which is a therapeutic agent with analgesic, muscle relaxant, sedative, appetite enhancement, and (Hazra et al, 2007); anticonvulsant (Manis et al, 1991); sedative (Bhattacharya, 1968); CNS depressant (Zaugg et al, 2011); anticholinesterasic and memory enhancer (Mukherjee et al, 2007); neuroprotective (Palani et al, 2010); behavioral changes (Shukla et al, 2006). (Wang et al, 2010); antioxidant (Saleem et al, 2006); antiparkinson (Ahmad et al, 2005); anxiolytic (Hosseinzadeh & Noraei, 2009); hypnotic (Hosseinzadeh & Noraei, 2009); memory enhancer (Pitsikas et al, 2007) 22.…”
Section: Discussionmentioning
confidence: 99%
“…Differently from the previous two species, sweet flag (Acorus calamus L.) is specifically used to treat rLung disorders. Indeed, Zaugg et al (2011) tested several compounds derived from a petroleum ether extract of this plant, and all of them showed potentiation of the GABA-A receptor chloride current. Its protective effect has been demonstrated in different rat models, as acetaminophen induced nephrotoxicity (Palani et al, 2010) and middle cerebral artery occlusion (Shukla et al, 2006).…”
Section: Enhances Appetitementioning
confidence: 99%