Effect of commercial Rhodiola rosea on CYP enzyme activity in humans

Thu, Ole Kristian Forstrønen; Spigset, Olav; Nilsen, Odd G.; Hellum, Bent H.

doi:10.1007/s00228-015-1988-7

Cited by 22 publications

(20 citation statements)

References 15 publications

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“…Opposed to this, the study by Spanakis et al (2013), showed a significant inhibition in the metabolism of losartan [CYP3A4, CYP2C9 and CYP2C10 substrate (Sica et al 2005)] in rabbits after oral administration of a R. rosea product. Just recently, we found a 23% reduction in CYP2C9 activity in a cross-over study (including 13 human males) with the commercial R. rosea product Artic Root (Thu et al 2016). To our knowledge, no studies have been published comparing inhibitory potential between different commercial R. rosea products.…”

Section: Introductionmentioning

confidence: 83%

“…Five studies have previously been published on CYP inhibition by full extracts of R. rosea (Scott et al 2006;Panossian et al 2009;Hellum et al 2010;Spanakis et al 2013;Thu et al 2016). Hellum et al (2010) showed that ethanol extracts of R. rosea clones (raw plant material) significantly inhibited CYP3A4 in vitro, with IC 50 values ranging from 1.7-3.1 lg/mL.…”

Section: Introductionmentioning

confidence: 99%

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In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products

Thu

Nilsen

Hellum

2016

Pharmaceutical Biology

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Context: Rhodiola rosea L. (Crassulaceae) products are popular natural remedies with a worldwide distribution. Recent studies have revealed potent CYP inhibition by R. rosea extracts both in vitro and in vivo, but information on in vitro CYP inhibition by commercial products are lacking. Variations in commercial R. rosea product quality have also been published. Objective: This study evaluates the variation of in vitro CYP inhibition potential and product quality of six commercially available R. rosea products. Materials and methods: Human CYPs isolated from baculovirus-infected cell system were incubated with testosterone (CYP3A4), dextromethorphan (CYP2D6) or phenacetin (CYP1A2). Positive CYP inhibitors ketoconazole (CYP3A4), quinidine (CYP2D6) and b-naphtoflavone (CYP1A2) were used as controls. Quantification of rosavin, rosarin, rosin, tyrosol and salidroside were used to evaluate R. rosea content. Results: IC 50 values ranged from 7.2-106.6 lg/mL for CYP3A4, 13.0-186.1 lg/mL for 2D6 and 10.7-116.0 lg/mL for 1A2. The tincture formulation of R. rosea was the strongest inhibitor giving the lowest IC 50 values of 7.2 ± 0.7, 13 ± 1.7 and 10.7 ± 5.6 lg/mL, respectively. CYP3A4 was significantly more inhibited by the different products than CYP1A2 (p < .05). One of the six products did not contain any rosavin, rosarin or rosin and is not a R. rosea product. Constituent concentrations were not linked to enzyme inhibition. Discussion and conclusion: The present results show a large variation in inhibitory potential between the products. Several of the products demonstrate similar inhibition levels as the product Arctic Root already proven to inhibit CYP enzyme activity in man.ARTICLE HISTORY

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Section: Introductionmentioning

confidence: 83%

Section: Introductionmentioning

confidence: 99%

In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products

Thu

Nilsen

Hellum

2016

Pharmaceutical Biology

Self Cite

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“…It may be clinically relevant during concomitant use of Rhodiola rosea extract and CYP2C9 substrates with a narrow therapeutic index (e.g., phenytoin and warfarin). A full pharmacokinetic study with these substrates should be conducted to confirm and extend the results from Thu et al's study [40]. …”

Section: Resultsmentioning

confidence: 82%

“…Phenotyping cocktail approach indicated that pretreatment with Rhodiola rosea extract 290 mg daily for 14 days could reduce CYP2C9 activity by 21% without significant effects on CYP1A2, CYP2C19, CYP2D6, and CYP3A4 [40]. …”

Section: Resultsmentioning

confidence: 99%

“…The inductive effect of St. John's wort on CYP2C19 activity was only observed in CYP2C19 wild-genotype subjects rather than CYP2C19 poor metabolizers [37]. The inhibitory effect of Rhodiola rosea on CYP2C9 was more pronounced in CYP2C9 extensive metabolizers than in CYP2C9 intermediate and poor metabolizers [40]. Phenotype of poor CYP2C19 metabolizers occurs in 2%–5% of Caucasian population and in up to 11%–23% of Oriental population [92].…”

Section: Resultsmentioning

confidence: 99%

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Therapeutic Risk and Benefits of Concomitantly Using Herbal Medicines and Conventional Medicines: From the Perspectives of Evidence Based on Randomized Controlled Trials and Clinical Risk Management

Zhang

Chen

Zhu

et al. 2017

Evidence-Based Complementary and Alternative Medicine

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Despite increased awareness of the potential of herb-drug interactions (HDIs), the lack of rigorous clinical evidence regarding the significance provides a challenge for clinicians and consumers to make rational decisions about the safe combination of herbal and conventional medicines. This review addressed HDIs based on evidence from randomized controlled trials (RCTs). Literature was identified by performing a PubMed search till January 2017. Risk description and clinical risk management were described. Among 74 finally included RCTs, 17 RCTs (22.97%) simply addressed pharmacodynamic HDIs. Fifty-seven RCTs (77.03%) investigated pharmacokinetic HDIs and twenty-eight of them showed potential or actual clinical relevance. The extent of an HDI may be associated with the factors such as pharmacogenomics, dose of active ingredients in herbs, time course of interaction, characteristics of the object drugs (e.g., administration routes and pharmacokinetic profiles), modification of herbal prescription compositions, and coexistence of inducers and inhibitors. Clinical professionals should enhance risk management on HDIs such as increasing awareness of potential changes in therapeutic risk and benefits, inquiring patients about all currently used conventional medicines and herbal medicines and supplements, automatically detecting highly substantial significant HDI by computerized reminder system, selecting the alternatives, adjusting dose, reviewing the appropriateness of physician orders, educating patients to monitor for drug-interaction symptoms, and paying attention to follow-up visit and consultation.

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The Therapeutic Effects and Mechanisms of Salidroside on Cardiovascular and Metabolic Diseases: An Updated Review

Zhao

Huan

et al. 2021

Chemistry & Biodiversity

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The increasing incidence of metabolic and cardiovascular diseases has severely affected global human health and life safety. In recent years, some effective drugs with remarkable curative effects and few side effects found in natural compounds have attracted attention. Salidroside (SAL), a phenylpropane glycoside, is the main active ingredient of the plateau plant Rhodiola. So far, many animal experiments proved that SAL has good biological activity against some metabolic and cardiovascular diseases. However, most of these reports are scattered. This review systematically summarizes the pharmacological progress of SAL in the treatment of several metabolic (e. g., diabetes and non-alcoholic fatty liver disease) and cardiovascular (e. g., atherosclerosis) diseases in a timely manner to promote the clinical application and basic research of SAL. Accumulating evidence proves that SAL has beneficial effects on these diseases. It can improve glucose tolerance, insulin sensitivity, and β-cell and liver functions, and inhibit adipogenesis, inflammation and oxidative stress. Overall, SAL may be a valuable and potential drug candidate for the treatment of metabolic and cardiovascular diseases. However, more studies especially clinical trials are needed to further confirm its therapeutic effects and molecular mechanisms.

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Effect of commercial Rhodiola rosea on CYP enzyme activity in humans

Abstract: This study indicates that R. rosea inhibits the metabolic capacity of CYP2C9 in humans. Although the effect is modest, it might be clinically relevant during treatment with CYP2C9 substrates with a narrow therapeutic index, such as phenytoin and warfarin.

Cited by 22 publications

References 15 publications

In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products

In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products

Therapeutic Risk and Benefits of Concomitantly Using Herbal Medicines and Conventional Medicines: From the Perspectives of Evidence Based on Randomized Controlled Trials and Clinical Risk Management

The Therapeutic Effects and Mechanisms of Salidroside on Cardiovascular and Metabolic Diseases: An Updated Review

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