FlavonoidsApigenin

Constituents of Passiflora incarnata (apigenin, orientin, vitexin) interact with OATP2B1 and OATP1A2 transporters, potentially altering uptake of other compounds

The study found that apigenin, orientin, and vitexin from Passiflora incarnata inhibit and are substrates of OATP2B1 and OATP1A2 transporters, while valerenic acid from Valeriana officinalis only interacts with OATP2B1. Commercially available P. incarnata preparations also inhibited transporter-mediated uptake of estrone 3-sulfate, suggesting these constituents may affect the pharmacokinetics of other drugs relying on these transporters.

Last updated: Jul 7, 2026•0 RCTs•📖 Read as article →

Evidence Score

Evidence Score24/100
Human RCT☆☆☆☆☆
Meta-analysis☆☆☆☆☆
Mechanism★★★★★
Safety★★★★☆
Confidencelow

Study Evidence

Study 1. Constituents of Passiflora incarnata, but Not of Valeriana officinalis, Interact with the Organic Anion Transporting Polypeptides (OATP)2B1 and OATP1A2.

observational

Schäfer AM, Gilgen PM, Spirgi C, Potterat O, Meyer Zu Schwabedissen HE · Planta medica (2022)

Participants: N/A
Duration: N/A
Intervention: Constituents of Passiflora incarnata (apigenin, orientin, vitexin) and Valeriana officinalis (valerenic acid) tested in vitro
Outcome: Inhibition and transport of estrone 3-sulfate, pregnenolone sulfate, and dehydroepiandrosterone sulfate via OATP2B1 and OATP1A2
Effect Size: N/A
Population: Madin-Darby canine kidney cells overexpressing OATP2B1 or OATP1A2 (in vitro)

Result:

PubMed: 33511622DOI: 10.1055/a-1305-3936

Mechanism Graph

Constituents of P. incarnata (apigenin, orientin, vitexin) inhibit OATP2B1 and OATP1A2-mediated uptake of sulfated steroids
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Competitive counterflow experiments show orientin is a substrate of both transporters, apigenin of OATP1A2, and vitexin of OATP2B1
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Commercially available P. incarnata preparations inhibit transporter-mediated estrone 3-sulfate uptake
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HPLC-UV-MS confirms orientin and vitexin in these preparations, suggesting they contribute to transporter interaction

Limitations

  • ⚠In vitro cell model may not fully replicate in vivo human physiology
  • ⚠Only tested sulfated steroids as substrates; interactions with other compounds remain unknown

Frequently Asked Questions

Do Passiflora incarnata constituents affect drug transport?▼

Yes, apigenin, orientin, and vitexin inhibit and are transported by OATP2B1 and OATP1A2, which could alter the uptake of other drugs or compounds that rely on these transporters.

What transporters are affected by Passiflora incarnata?▼

The study found interactions with organic anion transporting polypeptides OATP2B1 and OATP1A2.

Does Valeriana officinalis interact with these transporters?▼

Valerenic acid from Valeriana officinalis only interacted with OATP2B1, not OATP1A2, and was not identified as a substrate.

What methods were used to test transporter interaction?▼

The study used Madin-Darby canine kidney cells overexpressing OATP2B1 or OATP1A2, measuring cellular accumulation of sulfated steroids, followed by competitive counterflow experiments.

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References

  1. 1.Schäfer AM, Gilgen PM, Spirgi C, Potterat O, Meyer Zu Schwabedissen HE. "Constituents of Passiflora incarnata, but Not of Valeriana officinalis, Interact with the Organic Anion Transporting Polypeptides (OATP)2B1 and OATP1A2.." Planta medica, 2022. PMID: 33511622 DOI: 10.1055/a-1305-3936
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