Naturally occurring 2′-hydroxyl-substituted flavonoids as high-affinity benzodiazepine site ligands

Therapeutic Potential of Wogonin: A Naturally Occurring Flavonoid

“…For example, studies of their anti-inflammatory action suggested that wogonin is the only flavonoid that inhibits COX-2 without any effect on COX-1 (6); apigenin affects CNS but its site of action appears to be different from that of wogonin, it does not act at BZD-S (46). In addition, even for flavonoids acting at the BZD-S, there are large differences in BZD-S binding affinity and efficacy with only slight differences in structure (20). For example K36 (5,7,2¢-trihydroxy-6,8-dimethoxyflavone) had 250-fold higher binding affinity for BZD-S than wogonin.…”

“…Furthermore, in Xenopus laevis oocytes, the positive allosteric modulatory effect of wogonin was present in á 1 â 2 ã 2 GABA A receptors but abolished in á 1 â 2 receptors, demonstrating that the effect of wogonin was ã-subunit dependent, a characteristic of BZD-S ligands. Together these in vitro experiments suggested that wogonin possesses partial allosteric modulatory action at the GABA A receptor complex, acting as a partial agonist, like other neuroactive flavonoids (20).…”

Plant Drugs Used to Combat Menace of Anxiety Disorders

“…In present review article, amongst 143 plants reported to possess antianxiety activity ( Anxiolytic [242,243] Flavonoid baicalin (67) and its aglycone baicalein (68) Baicalein ( Seven formulations of plant drugs, 02 well known classes of phytoconstitunts and 03 pure constituents present in various plants, and nutraceuticals reported to possess antianxiety activity in battery of experimental models of anxiety have been compiled in present work (Table 2). Twelve anxiolytic formulations containing plants have been patented (Table 3).…”

Targeting the Modulation of Neural Circuitry for the Treatment of Anxiety Disorders

“…For example, Targeted Modulation of Neural Circuits Implicated in Anxiolysis chrysin, one of the first flavonoids shown to interact with the BZD binding site, initiated the search for natural anxiolytics among traditional medicinal herbs (Medina et al, 1989(Medina et al, , 1990(Medina et al, , 1997Wolfman et al, 1994Wolfman et al, , 1996. A number of other naturally occurring flavonoids and their derivatives, such as K36 (5,7,29-trihydroxy-6,8-dimethoxyflavone) (Huen et al, 2003), hispidulin (Kavvadias et al, 2004), wogonin (Hui et al, 2000(Hui et al, , 2002, and related compounds (Nielsen et al, 1988;Häberlein et al, 1994;Wolfman et al, 1996;Goutman et al, 2003), are allosteric modulators at GABA A Rs. In a mouse study, wogonin (7.5-30 mg/kg p.o.)…”

“…was found to produce an anxiolytic response similar to diazepam in the elevated plus maze without accompanying sedation (Hui et al, 2002). K36, a naturally occurring flavonoid, increases entries onto the open arms of the elevated plus maze without changing locomotor activity, sedation, myorelaxation, or motor incoordination in mice (Huen et al, 2003).…”