Inhibition of Monoamine Oxidase by Hypercin

Сузукі, Осаму; Katsumata, Yoshinao; Oya, Mototsugu; Bladt, Sabine; Wagner, Hildebert

doi:10.1055/s-2007-969700

Cited by 202 publications

(91 citation statements)

References 7 publications

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“…22 Effects of monoamine oxidase A activity Initial reports suggested that hypericin, the major constituent of hypericum acts as an inhibitor of MAO-A activity. 23 However this finding has not been confirmed by subsequent studies. [24][25][26] Quercetin and Quercitrin, both flavonoide aglykone constituents of hypericum extract have also been shown to inhibit MAO-A, 27 although a therapeutic action of these compounds remains questionable because of their low plasma levels.…”

Section: Experimental Pharmacology Of Hypericummentioning

confidence: 71%

The experimental and clinical pharmacology of St John's Wort (Hypericum perforatum L.)

Nathan

1999

Mol Psychiatry

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Hypericum (St John's Wort) is a plant that has been used for centuries as a medicinal herb. Pre-clinical animals studies suggest that hypericum is effective in three major biochemical systems relevant for antidepressant activity, namely the inhibition of the synaptic re-uptake system for serotonin (5-HT), noradrenaline (NA) and dopamine (DA). It is the only antidepressant capable of inhibiting the re-uptake of 5-HT, NA and DA with similar potencies. The potencies for monoamine re-inhibition and chronic changes in receptors are also consistent with changes seen with known antidepressants. Behavioral studies suggest that hypericum is active in pre-clinical animal models of depression with comparable effects to known antidepressants. Supporting the pre-clinical pharmacology and efficacy, many clinical studies have shown that hypericum has superior efficacy compared to placebo and comparable efficacy to standard antidepressants in the treatment of mild-to-moderate depression. The advantage of hypericum over other antidepressants may result from its favorable side-effect profile. Although pre-clinical and short-term clinical studies demonstrate antidepressant activity, the lack of long-term use and efficacy, and the heterogeneity of patients, interventions, extract preparations from previous clinical studies suggests that more careful and controlled studies are needed to determine the long-term efficacy of hypericum in mild-to-moderate depression.

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Section: Experimental Pharmacology Of Hypericummentioning

confidence: 71%

The experimental and clinical pharmacology of St John's Wort (Hypericum perforatum L.)

Nathan

1999

Mol Psychiatry

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“…The most common SJW preparations used are hydroalcoholic extracts of the aerial portion of the plant that contain at least ten different kinds of biochemical compounds [16]. SJW interacts with the monoaminergic system through different mechanisms: the MAO-inhibitory properties of SJW were mainly due to hypericin [17,18] whereas the inhibition of serotonin, dopamine and noradrenaline synaptosomal uptake is related to the presence of hyperforin [19][20][21][22]. It has therefore been suggested that SJW may induce antidepressant activity through a mechanism similar to TCAs [23].…”

Section: Introductionmentioning

confidence: 99%

St. John's Wort reduces neuropathic pain through a hypericin-mediated inhibition of the protein kinase C γ and ɛ activity

Galeotti

Vivoli

Bilia

et al. 2010

Biochemical Pharmacology

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“…The rewarding effect of methamphetamine results from increased dopamine release in limbic terminal fields, which is regulated by the vesicular monoamine transporter (Takahashi et al, 1997). Methamphetamine increases extracellular dopamine concentrations by inhibiting the action of the vesicular monoamine transporter which sequesters dopamine into vesicular stores, as well as by inhibiting monoamine oxidase which diminishes dopamine metabolism, thereby making cytosolic dopamine more available for methamphetamineinduced reversal of the plasmalemma dopamine transporter (Dwoskin and Crooks, 2002;Suzuki et al, 1980). Although lobeline inhibits dopamine uptake into synaptic vesicles via the vesicular monoamine transporter, unlike methamphetamine, lobeline does not inhibit monoamine oxidase, and as a result, cytosolic dopamine is rapidly metabolized to dihydroxyphenylacetic acid, leading to a decrease in the cytosolic dopamine pool available for methamphetamine-induced reversal of the dopamine transporter.…”

Section: Introductionmentioning

confidence: 99%

Lobelane decreases methamphetamine self-administration in rats

Neugebauer

Harrod

Stairs

et al. 2007

European Journal of Pharmacology

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Lobelane, a minor alkaloid of Lobelia inflata and a synthetic, des-oxy analog of lobeline, has good affinity for the vesicular monoamine transporter and the dopamine transporter. The current study examined the ability of lobelane to specifically decrease methamphetamine self-administration. Rats were trained on a fixed ratio 5 schedule of reinforcement to self-administer methamphetamine (0.05 mg/kg/infusion, i.v.) or to respond for sucrose pellets. Upon reaching stable responding, rats were pretreated with lobelane (0.1, 1, 3, 5.6, or 10 mg/kg, s.c.) or saline, 15 min prior to the operant session. To assess the effect of repeated lobelane on methamphetamine self-administration, rats were pretreated with lobelane (5.6 or 10 mg/kg, s.c.) for 7 sessions. Behavioral specificity was further investigated by assessing the effects of lobelane (0.1, 1, 3, 5, or 10 mg/kg, s.c.) or saline on locomotor activity. Within the dose range tested, lobelane dose-dependently decreased methamphetamine selfadministration, while having no effect on sucrose-maintained responding. Locomotor activity was decreased following only the highest dose of lobelane (10 mg/kg). Across repeated pretreatments, tolerance developed to the effect of lobelane on methamphetamine self-administration, demonstrating that the ability of lobelane to specifically decrease methamphetamine selfadministration is a transient effect. Thus, taken together, the results show that although lobelane interacts with the pharmacological targets believed to be responsible for its ability to decrease methamphetamine self-administration, removal of the oxygen functionalities from the lobeline molecule may have afforded a compound with an altered pharmacokinetic and/or pharmacodynamic profile.

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Inhibition of Monoamine Oxidase by Hypercin

Cited by 202 publications

References 7 publications

The experimental and clinical pharmacology of St John's Wort (Hypericum perforatum L.)

The experimental and clinical pharmacology of St John's Wort (Hypericum perforatum L.)

St. John's Wort reduces neuropathic pain through a hypericin-mediated inhibition of the protein kinase C γ and ɛ activity

Lobelane decreases methamphetamine self-administration in rats

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