Positive Health Online

Abstract

DALL'ACQUA and COLLEAGUES, 1 Department of Pharmaceutical Sciences, University of Padova, Via F. Marzolo 5, 35131, Padova, Italy; 2 Faculty of Pharmacy, University of Ljubljana, Askerceva 7, SI-1000 Ljubljana, Slovenia; 3 National Laboratory of the Interuniversity Consortium for Biotechnology, Area Science Park - Padriciano 99, 34149, Trieste, Italy; 4 Department of Oncology, Johns Hopkins University School of Medicine, Baltimore, MD, USA; 5 Department of Oncology, Johns Hopkins University School of Medicine, Baltimore, MD, USA; Department of Biochemistry and Immunology, ICB, Federal University of Minas Gerais, Belo Horizonte, MG, Brazil; 6 Department of Agronomy, Food, Natural Resources, Animals and the Environment, Viale dell'Università 16 - 35020 Legnaro, Pd, Italy; 7 Institute for Maternal and Child Health, IRCCS Burlo Garofolo, via dell'Istria 65/1, 34143, Trieste, Italy; 8 Department of Life Sciences, University of Trieste, via Valerio, 28, 34127, Trieste, Italy; 9 Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy; 10 Department of Chemical and Pharmaceutical Sciences, University of Trieste, P.le Europa 1, 34127 Trieste, Italy.  vojnovic@units.it  studied pharmacokinetics and immunomodulatory effects of Echinacea angustifolia DC. and Zingiber officinale Roscoe assessed by gene expression profiling.

Background

Echinacea angustifolia DC. and Zingiber officinale Roscoe are two natural products with documented immunomodulatory activity, both able to modulate the expression of important immune-related genes. Thus, their use in combination seems to be particularly promising. In this context, we have considered the oral supplementation of a highly standardized lipophilic extract combining both above-mentioned phytocomplexes, formulated in attractive softgel capsules, with two objectives: on the one hand to study oral pharmacokinetic of main active extracts' components and on the other hand to examine the immunomodulation and anti-inflammatory properties by gene expression profiling.

Methodology

Softgel capsules containing a combination of E. angustifolia DC. and Z. officinale Roscoe (5 mg and 25 mg, respectively) were given by oral administration to 10 healthy volunteers. The plasma concentrations of dodeca-2E,4E,8Z,10E/Z-tetraenoic isobutylamide (tetraene) for E. angustifolia DC., 6-gingerol and 6-shogaol (free and glucuronide) for Z. officinale Roscoe were determined by LC-MS analysis, and the pharmacokinetic analysis was performed. To understand the functional mechanisms responsible for the documented health benefits, we also examined the overall transcriptional remodelling induced in the peripheral blood mononuclear cells and performed an integrative functional analysis on the generated gene expression.

Results

All bioactive components were absorbed very rapidly, and their tmax were detected in plasma from 30 min to 1.40 h. The peak concentrations of tetraene, 6-gingerol, 6-shogaol and their glucuronide metabolites were 14.74, 5.66, 9.25, 29.2 and 22.24 ng/ml, respectively. Integrated analysis performed on the generated gene expression data highlighted immunomodulatory and anti-inflammatory effects similar to those exerted by hydrocortisone.

Conclusion

These data demonstrated that the bioactive ingredients are highly and rapidly absorbed from softgel capsules containing the combination of the above-mentioned lipophilic extracts, providing evidence to support their immunomodulatory and anti-inflammatory properties. These data also help in defining the mechanistic pathways underlying the health benefits of these plant-derived bioactive compounds.

References

Stefano Dall'Acqua  1 , Iztok Grabnar  2 , Roberto Verardo  3 , Enio Klaric  3 , Luigi Marchionni  4 , Eddie Luidy-Imada  5 , Stefania Sut  6 , Chiara Agostinis  7 , Roberta Bulla  8 , Beatrice Perissutti  9 , Dario Voinovich  10. Combined extracts of Echinacea angustifolia DC. and Zingiber officinale Roscoe in softgel capsules: Pharmacokinetics and immunomodulatory effects assessed by gene expression profiling

Phytomedicine; 65:153090. Dec 2019. doi: 10.1016/j.phymed.2019.153090. Epub Sep 16 2019.