Pharmacokinetic Interaction between Magnolol and Piperine in Rats

Chen, Xiaoying; Yang, Guanghua; Li, Cai-Lan; Yu, Xiu-Ting; Wang, Xiufen; Zheng, Yifeng; Xie, Jian-Hui; Lai, Xiaoping; Su, Zi‐Ren; Liang, Yingmin; Jiang, Lin

doi:10.4314/tjpr.v15i3.27

Cited by 4 publications

(5 citation statements)

References 11 publications

(10 reference statements)

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“…The pharmacokinetics of ciprofloxacin changed when piperine was co-administered, emphasizing the fact that it acts as bioenhancer [139]. Similar results were reported for amoxicillin [140], rosuvastatin [141], omeprazole [142], magnolol [143], ampicillin and norfloxacin [144]. Piperine, as a bio enhancer, improves the systemic availability of oral propranolol and theophylline in healthy volunteers [145].…”

Section: Bioavailability-enhancing Effect Of Piperinementioning

confidence: 72%

Piperine-A Major Principle of Black Pepper: A Review of Its Bioactivity and Studies

et al. 2019

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Piperine is the main compound present in black pepper, and is the carrier of its specific pungent taste, which is responsible for centuries of human dietary utilization and worldwide popularity as a food ingredient. Along with the application as a food ingredient and food preservative, it is used in traditional medicine for many purposes, which has in most cases been justified by modern scientific studies on its biological effects. It has been confirmed that piperine has many bioactive effects, such as antimicrobial action, as well as many physiological effects that can contribute to general human health, including immunomodulatory, hepatoprotective, antioxidant, antimetastatic, antitumor, and many other activities. Clinical studies demonstrated remarkable antioxidant, antitumor, and drug availability-enhancing characteristics of this compound, together with immunomodulatory potential. All these facts point to the therapeutic potential of piperine and the need to incorporate this compound into general health-enhancing medical formulations, as well as into those that would be used as adjunctive therapy in order to enhance the bioavailability of various (chemo)therapeutic drugs.

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Section: Bioavailability-enhancing Effect Of Piperinementioning

confidence: 72%

Piperine-A Major Principle of Black Pepper: A Review of Its Bioactivity and Studies

et al. 2019

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“…However, its infamous drug-drug and drug-food interaction profile, resulting from its significant protein binding and large interindividual variability, presents a challenge in dosing regimen and safety. In addition, piperine has been shown to interact with several drugs at different levels, 27,33,39,44,45 but its effect on the pharmacokinetics and pharmacodynamics of warfarin has not been investigated yet.…”

Section: Discussionmentioning

confidence: 99%

“…40 Moreover, piperine is known to affect the bioavailability of several drugs through alteration of their absorption resulting in increasing plasma levels of some 36,46,47 while decreasing these of others. 32,33 The involvement of one or more of the previous interactions should be demonstrated by alteration of pharmacological action of warfarin or changes in levels of the drug and its metabolite. In this study, therefore, we aimed to examine the effect of piperine on the pharmacokinetics of warfarin and 7-hydroxywarfarin and anticoagulation of warfarin in vivo.…”

Section: Discussionmentioning

confidence: 99%

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<p>Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats</p>

Zayed¹,

Babaresh²,

Darweesh³

et al. 2020

JEP

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Introduction: Piperine, the bioactive compound of black pepper, and warfarin are metabolized by cytochrome P450 enzymes and are both highly plasma protein-bound compounds. In this study, we evaluated the effect of co-administered piperine on the pharmacokinetics and anticoagulation of warfarin in rats. Methods: We studied four Sprague-Dawley rat groups: a negative control group receiving only oral warfarin, a test group receiving warfarin plus piperine, a positive control group receiving warfarin plus sulfaphenazole (CYP2C inhibitor), and another positive control group receiving warfarin plus ketoconazole (CYP3A inhibitor). We also analyzed plasma concentrations of warfarin and its major metabolite, 7-hydoxywarfarin. Blood clotting time, calculated as international normalized ratio (INR), was also measured. Results: Our results showed that although co-administration of piperine produced a nonsignificant decrease in warfarin concentrations, it resulted in significantly lower 7-hydroxywarfarin metabolite concentrations. Piperine significantly decreased, by sixfold, AUC 0-∞ , by eightfold, C max , but significantly increased, by fivefold, CL/F and, by sixfold, Vd/F of 7-hydroxywarfarin. The INR values were consistent with the decrease in warfarin concentration in the presence of piperine and showed a significant decrease at 24 h after warfarin dose. Conclusion:We conclude that piperine could be a potent inhibitor of cytochrome P450 metabolism of warfarin in vivo and, contrary to the expectation, may reduce the plasma concentration and anticoagulation of warfarin. This interaction could have a clinical significance and should be investigated in patients.

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“…However, at a high dosage of 40 mg/kg, the maximum concentration of piperine dropped significantly from 4.30 ± 1.47 µg/mL to 2.50 ± 0.78 µg/mL (p < 0.05). No significant differences were observed in the area under the curve (AUC) and half-life (t1/2) of piperine in the plasma when given alone or in combination with magnolol [123].…”

Section: Toxicological Profilementioning

confidence: 99%

Neuropharmacological potential of honokiol and its derivatives from Chinese herb Magnolia species: understandings from therapeutic viewpoint

Faysal,

Khan,

Zehravi

et al. 2023

Chin Med

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Honokiol is a neolignan biphenol found in aerial parts of the Magnolia plant species. The Magnolia plant species traditionally belong to China and have been used for centuries to treat many pathological conditions. Honokiol mitigates the severity of several pathological conditions and has the potential to work as an anti-inflammatory, anti-angiogenic, anticancer, antioxidant, and neurotherapeutic agent. It has a long history of being employed in the healthcare practices of Southeast Asia, but in recent years, a greater scope of research has been conducted on it. Plenty of experimental evidence suggests it could be beneficial as a neuroprotective bioactive molecule. Honokiol has several pharmacological effects, leading to its exploration as a potential therapy for neurological diseases (NDs), including Alzheimer's disease (AD), Parkinson’s disease (PD), cerebral ischemia, anxiety, depression, spinal cord injury, and so on. So, based on the previous experimentation reports, our goal is to discuss the neuroprotective properties of honokiol. Besides, honokiol derivatives have been highlighted recently as possible therapeutic options for NDs. So, this review focuses on honokiol's neurotherapeutic actions and toxicological profile to determine their safety and potential use in neurotherapeutics.

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Pharmacokinetic Interaction between Magnolol and Piperine in Rats

Cited by 4 publications

References 11 publications

Piperine-A Major Principle of Black Pepper: A Review of Its Bioactivity and Studies

Piperine-A Major Principle of Black Pepper: A Review of Its Bioactivity and Studies

<p>Piperine Alters the Pharmacokinetics and Anticoagulation of Warfarin in Rats</p>

Neuropharmacological potential of honokiol and its derivatives from Chinese herb Magnolia species: understandings from therapeutic viewpoint

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