The Potential of<i>Sutherlandia frutescens</i>for Herb-Drug Interaction

Fasinu, Pius S.; Gutmann, Heike; Schiller, Hilmar; James, Alexander-David; Bouic, Patrick; Rosenkranz, Bernd

doi:10.1124/dmd.112.049593

Cited by 37 publications

(17 citation statements)

References 34 publications

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“…The in vivo predictions of T30 ( H. hemerocallidea powdered leaves) and T41 ( H. hemerocallidea capsules) on CYP3A4 were in agreement with values reported by Fasinu et al [37] thus validating the predictive value of these in vitro screening assays. However, a weak inhibition of L. frutescens was observed on CYP3A4 compared to the previous study by Fasinu et al [38]. Fasinu and others used methanol as solvent of extraction which extracts more phytochemical constituents with strong inhibition potential compared to the aqueous extract used in our studies.…”

Section: Discussioncontrasting

confidence: 69%

Inhibition of Major Drug Metabolizing CYPs by Common Herbal Medicines used by HIV/AIDS Patients in Africa– Implications for Herb- Drug Interactions

Awortwe¹,

Bouic²,

Masimirembwa³

et al. 2014

DML

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The purpose of this study was to evaluate the potential risk of common herbal medicines used by HIV-infected patients in Africa for herb-drug interactions (HDI). High throughput screening assays consisting of recombinant Cytochrome P450 enzymes (CYPs) and fluorescent probes, and parallel artificial membrane permeability assays (PAMPA) were used. The potential of herbal medicines to cause HDI was ranked according to FDA guidelines for reversible inhibition and categorization of time dependent inhibition was based on the normalized ratio. CYPs 1A2 and 3A4 were most inhibited by the herbal extracts. H. hemerocallidea (IC50 = 0.63 μg/mL and 58 μg/mL) and E. purpurea (IC50 = 20 μg/mL and 12 μg/mL) were the potent inhibitors of CYPs 1A2 and 3A4 respectively. L. frutescens and H. hemerocallidea showed clear time dependent inhibition on CYP3A4. Furthermore, the inhibitory effect of both H. hemerocallidea and L. frutescens before and after PAMPA were identical. The results indicate potential HDI of H. hemerocallidea, L. frutescens and E. purpurea with substrates of the affected enzymes if maximum in vivo concentration is achieved.

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Section: Discussioncontrasting

confidence: 69%

Inhibition of Major Drug Metabolizing CYPs by Common Herbal Medicines used by HIV/AIDS Patients in Africa– Implications for Herb- Drug Interactions

Awortwe¹,

Bouic²,

Masimirembwa³

et al. 2014

DML

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“…Most showed relatively potent inhibitory activities on CYP3A4 (four plants with the potency order: PC > DL > DM > PI), followed by CYP2D6 (three plants with the potency order: DM > PI > DL), and CYP1A2 (two plants with the potency order: PC > AL), and CYP2C19 (two plants with the potency order: PI > DM). All plant extracts particularly PC and AL exhibited relatively more potent activities on CYP1A2 compared with other previously reported plants (Fasinu et al ., ; Han et al ., , ; Huang et al ., ). The activities on the other CYP isoforms (CYP2C19, CYP2D6 and CYP3A4) were comparable to other previously reported plants (Cho and Yoon, ; Fasinu et al ., ; Foti et al ., ; Han et al ., , ;Huang et al ., ; Kim et al ., ).…”

Section: Discussionmentioning

confidence: 99%

“…All plant extracts particularly PC and AL exhibited relatively more potent activities on CYP1A2 compared with other previously reported plants (Fasinu et al ., ; Han et al ., , ; Huang et al ., ). The activities on the other CYP isoforms (CYP2C19, CYP2D6 and CYP3A4) were comparable to other previously reported plants (Cho and Yoon, ; Fasinu et al ., ; Foti et al ., ; Han et al ., , ;Huang et al ., ; Kim et al ., ). With regard to the inhibitory activity of each plant extract on the four CYP isoforms, PI and DM showed potent inhibitory activities on most CYP isoforms (CYP2C19, CYP2D6 and CYP3A4).…”

Section: Discussionmentioning

confidence: 99%

Inhibitory Activities of Thai Medicinal Plants with Promising Activities Against Malaria and Cholangiocarcinoma on Human Cytochrome P450

2015

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Malaria and cholangiocarcinoma remain important public health problems in tropical countries including Southeast Asian nations. Newly developed chemotherapeutic and plant-derived drugs are urgently required for the control of both diseases. The aim of the present study was to investigate the propensity to inhibit cytochrome P450-mediated hepatic metabolism (CYP1A2, CYP2C19, CYP2D6 and CYP3A4) of the crude ethanolic extract of eight Thai medicinal plants with promising activities against malaria and cholangiocarcinoma, using human liver microsomes in vitro. Piper chaba Linn. (PC) and Atractylodes lancea (thung.) DC. (AL) exhibited the most potent inhibitory activities on CYP1A2-mediated phenacetin O-deethylation with mean IC50 of 0.04 and 0.36 µg/mL, respectively. Plumbago indica Linn. (PI) and Dioscorea membranacea Pierre. (DM) potently inhibited CYP2C19-mediated omeprazole 5-hydroxylation (mean IC50 4.71 and 6.92 µg/mL, respectively). DM, Dracaena loureiri Gagnep. (DL) and PI showed the highest inhibitory activities on dextromethorphan O-demethylation (mean IC50 2.93-9.57 µg/mL). PC, DM, DL and PI exhibited the most potent inhibitory activities on CYP3A4-mediated nifedipine oxidation (mean IC50 1.54-6.43 µg/mL). Clinical relevance of the inhibitory potential of DM, PC and PI is of concern for the further development of these plants for the treatment of malaria and/or cholangiocarcinoma.

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“…Since clinically consuming herbs has become quite prevalent, issue of the potential HDIs should be brought into attention . Although well‐documented reports about HDIs have been recorded, underlying mechanisms involved in the potential HDIs have not been well clarified.…”

Section: Discussionmentioning

confidence: 99%

Mulberroside A suppresses PXR‐mediated transactivation and gene expression of P‐gp in LS174T cells

Huang

Sun

et al. 2016

J Biochem & Molecular Tox

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Mulberroside A (Mul A) is the main bioactive constituents of Sangbaipi, which is officially listed in the Chinese Pharmacopoeia. The pregnane X receptor (PXR) has been recognized as the critical mediator of human P-glycoprotein (P-gp) gene transactivation. In this study, the effect of Mul A on PXR-mediated transactivation and gene expression of P-gp was investigated. It was found that Mul A significantly suppressed PXR-mediated P-gp luciferase activity induced by rifampicin (Rif). Furthermore, Rif induced an elevation of P-gp expression and transport activity, which was apparently suppressed by Mul A. However, Mul A did not suppress the P-gp luciferase activity, P-gp expression, and function in the absence of Rif. These findings suggest that Mul A suppresses PXR-mediated transactivation and P-gp expression induced by Rif. This should be taken into consideration to predict any potential herb-drug interactions when Mul A or Sangbaipi are co-administered with Rif or other PXR agonist drugs.

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The Potential ofSutherlandia frutescensfor Herb-Drug Interaction

Cited by 37 publications

References 34 publications

Inhibition of Major Drug Metabolizing CYPs by Common Herbal Medicines used by HIV/AIDS Patients in Africa– Implications for Herb- Drug Interactions

Inhibition of Major Drug Metabolizing CYPs by Common Herbal Medicines used by HIV/AIDS Patients in Africa– Implications for Herb- Drug Interactions

Inhibitory Activities of Thai Medicinal Plants with Promising Activities Against Malaria and Cholangiocarcinoma on Human Cytochrome P450

Mulberroside A suppresses PXR‐mediated transactivation and gene expression of P‐gp in LS174T cells

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