Flavonoids inhibit MCT1-mediated transport of gamma-hydroxybutyrate, reducing sleep time in rats
In vitro, flavonoids such as luteolin, morin, and phloretin inhibited MCT1-mediated uptake of GHB in rat MCT1-transfected cells, with IC50 values of 0.41, 6.41, and 2.57 μM respectively. In vivo, intravenous luteolin (10 mg/kg) increased renal and total clearance of GHB and significantly reduced sleep time from 165 to 121 minutes in rats given 1000 mg/kg GHB.
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Flavonoids inhibit MCT1-mediated transport of gamma-hydroxybutyrate, reducing sleep time in rats The current body of evidence comprises 1 study. EvidenceHub rates the overall confidence at 26/100 (low).
The Claim
Flavonoids inhibit MCT1-mediated transport of gamma-hydroxybutyrate, reducing sleep time in rats
This conclusion is most relevant to: Male Sprague-Dawley rats.
What the Research Shows
The conclusion draws on 1 linked study. Highlights from the cited literature:
- ▸Flavonoids modulate monocarboxylate transporter-1-mediated transport of gamma-hydroxybutyrate in vitro and in vivo. (Drug metabolism and disposition: the biological fate of chemicals, 2007) —
How It Works
The proposed biological pathway:
- ▸Flavonoids (e.g., luteolin) competitively inhibit MCT1 transporter
- ▸Inhibition reduces renal reabsorption of GHB in kidney
- ▸Increased renal and total clearance of GHB
- ▸Result: Decreased GHB brain levels and reduced sleep time
Who Might Benefit
Evidence fit by population:
- ▸Male Sprague-Dawley rats
Recommended Dose
Luteolin 10 mg/kg i.v.; GHB 1000 mg/kg i.v.
Limitations & Caveats
Important context when interpreting this evidence:
- ▸Animal study (rats) may not directly translate to humans
- ▸Only one flavonoid (luteolin) tested in vivo; others only in vitro
- ▸Single dose of GHB and luteolin; dose-response not fully explored
Frequently Asked Questions
What flavonoids were found to inhibit GHB transport?▼
Apigenin, biochanin A, chrysin, diosemin, fisetin, genistein, hesperitin, kaempferol, luteolin, morin, narigenin, phloretin, and quercetin inhibited MCT1-mediated GHB uptake in vitro.
Did luteolin reduce sleep time in rats?▼
Yes, luteolin (10 mg/kg i.v.) significantly decreased sleep time from 165 to 121 minutes after GHB administration.
Are flavonoids substrates for MCT1?▼
No, kaempferol and biochanin A were not taken up via MCT1, suggesting flavonoids are inhibitors but not substrates.
What was the mechanism of inhibition for luteolin?▼
Luteolin competitively inhibited MCT1-mediated GHB transport with an IC50 of 0.41 μM.
References
- 1.Wang Q, Morris ME. “Flavonoids modulate monocarboxylate transporter-1-mediated transport of gamma-hydroxybutyrate in vitro and in vivo..” Drug metabolism and disposition: the biological fate of chemicals, 2007. PMID: 17108059 DOI: 10.1124/dmd.106.012369