Artemisinin permeability via Caco-2 cells increases after simulated digestion of Artemisia annua leaves

Desrosiers, Matthew R.; Weathers, Pamela J.

doi:10.1016/j.jep.2017.08.038

Cited by 26 publications

(22 citation statements)

References 29 publications

(31 reference statements)

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“…Integrity of cell monolayers was assessed by monitoring the lucifer yellow (LY) rejection (Fig. (c)), a paracellular marker across a cell monolayer, according to the report by Desrosiers and Weathers . The percentage of LY rejection value was calculated according to Eqn (5).…”

Section: Methodsmentioning

confidence: 99%

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Cellular antioxidant activity and in vitro intestinal permeability of phenolic compounds from four varieties of mango bark (Mangifera indica L.)

et al. 2019

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BACKGROUND Mango bark is an important agro‐industrial residue from mango pruning. In traditional medicine, the aqueous extract from mango bark (MBE) has been used in ethnomedicine for the treatment of many diseases. However, there is scarce information using cellular models to evaluate the potential use of this plant material for human consumption. In this study, the phenolic content from the MBE from four varieties (Kent, Keitt, Ataulfo and Tommy Atkins) was analyzed by high‐performance liquid chromatography coupled to photodiode array detector (HPLC‐DAD) and liquid chromatography coupled with time‐of‐flight mass spectrometry (LC/MS‐TOF). Additionally, the cellular antioxidant activity of the MBE from the four mango varieties were compared. Finally, the intestinal permeability of the main polyphenols found in the MBE (mangiferin and gallic acid) was evaluated. RESULTS Mangiferin and gallic acid were the main constituents in the MBE from the four mango varieties. Furthermore, the Ataulfo variety showed the highest cellular antioxidant activity (67%) at the concentration of 100 µg mL−1. The intestinal permeability of mangiferin present in the bark extracts was 3‐ to 4.8‐fold higher than those of mangiferin as standard, whereas the intestinal permeability of gallic acid varied among the tested extracts. CONCLUSION MBE has the potential to exert antioxidant activity at the cellular level and can have an impact on human health. It may also be a good source for the extraction of polyphenols mainly mangiferin. © 2019 Society of Chemical Industry

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Section: Methodsmentioning

confidence: 99%

“…3(c)), a paracellular marker across a cell monolayer, according to the report by Desrosiers and Weathers. 17 The percentage of LY rejection value was calculated according to Eqn (5).…”

Section: Intestinal Permeability Assaymentioning

confidence: 99%

Cellular antioxidant activity and in vitro intestinal permeability of phenolic compounds from four varieties of mango bark (Mangifera indica L.)

et al. 2019

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“…Chemical structures of artemisinin (A) and deoxyartemisinin (B).Artemisinin is metabolized by liver cytochrome P450s (CYPs), mainly CYP2B6 with a minor contribution from CYP3A4, to yield deoxyartemisinin ( Figure 1B), crystal 7, deoxydihydroartemisinin, and 9,10 dihydrodeoxyartemisinin [10,11], all of which are therapeutically inactive. While the enhanced bioavailability of artemisinin afforded by DLA is partially attributed to increased solubility and intestinal transport [7,8], we posit that inhibition of CYP2B6 and/or CYP3A4 by DLA phytochemicals also plays a role in significantly increasing artemisinin bioavailability because more artemisinin would pass through the liver unmetabolized. In turn, that should also increase artemisinin distribution in tissues and organs with greater impact on biological responses, e.g., effects on inflammation.Despite significant bioavailability and pharmacokinetic differences between pure artemisinin and DLA-delivered artemisinin [9,12,13], to our knowledge, no studies have been done to determine absorption, distribution, metabolism and excretion (ADME) of the drug in vivo when delivered as DLA.…”

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confidence: 89%

“…DLA was more effective than artemisinin in males at attenuating proinflammatory cytokine production; the data were less conclusive in females. These results suggest that the oral consumption of artemisinin as DLA enhances the bioavailability and anti-inflammatory potency of artemisinin.Biomolecules 2020, 10, x FOR PEER REVIEW 2 of 15 solubility than pure artemisinin [7][8][9]. DLA also does not require extraction and purification, making it an affordable alternative to ACTs.…”

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Dried Leaf Artemisia Annua Improves Bioavailability of Artemisinin via Cytochrome P450 Inhibition and Enhances Artemisinin Efficacy Downstream

2020

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Artemisia annua L. and artemisinin, have been used for millennia to treat malaria. We used human liver microsomes (HLM) and rats to compare hepatic metabolism, tissue distribution, and inflammation attenuation by dried leaves of A. annua (DLA) and pure artemisinin. For HLM assays, extracts, teas, and phytochemicals from DLA were tested and IC50 values for CYP2B6 and CYP3A4 were measured. For tissue distribution studies, artemisinin or DLA was orally delivered to rats, tissues harvested at 1 h, and blood, urine and feces over 8 h; all were analyzed for artemisinin and deoxyartemisinin by GC-MS. For inflammation, rats received an intraperitoneal injection of water or lipopolysaccharide (LPS) and 70 mg/kg oral artemisinin as pure drug or DLA. Serum was collected over 8 h and analyzed by ELISA for TNF-α, IL-6, and IL-10. DLA-delivered artemisinin distributed to tissues in higher concentrations in vivo, but elimination remained mostly unchanged. This seemed to be due to inhibition of first-pass metabolism by DLA phytochemicals, as demonstrated by HLM assays of DLA extracts, teas and phytochemicals. DLA was more effective than artemisinin in males at attenuating proinflammatory cytokine production; the data were less conclusive in females. These results suggest that the oral consumption of artemisinin as DLA enhances the bioavailability and anti-inflammatory potency of artemisinin.

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Artemisia annua and Artemisia afra Essential Oils and Their Therapeutic Potential

Desrosiers

Towler

Weathers

2019

Essential Oil Research

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Artemisinin permeability via Caco-2 cells increases after simulated digestion of Artemisia annua leaves

Abstract: These results shed light on the mechanisms by which DLA enhances the oral bioavailability of artemisinin.

Cited by 26 publications

References 29 publications

Cellular antioxidant activity and in vitro intestinal permeability of phenolic compounds from four varieties of mango bark (Mangifera indica L.)

Cellular antioxidant activity and in vitro intestinal permeability of phenolic compounds from four varieties of mango bark (Mangifera indica L.)

Dried Leaf Artemisia Annua Improves Bioavailability of Artemisinin via Cytochrome P450 Inhibition and Enhances Artemisinin Efficacy Downstream

Artemisia annua and Artemisia afra Essential Oils and Their Therapeutic Potential

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