| Title |
Combined analytical approaches to define biodistribution and biological activity of semi-synthetic berberrubine, the active metabolite of natural berberine
|
|---|---|
| Published in |
Analytical & Bioanalytical Chemistry, February 2018
|
| DOI | 10.1007/s00216-018-0884-2 |
| Pubmed ID | |
| Authors |
Emanuele Porru, Placido Franco, Donato Calabria, Silvia Spinozzi, Marinella Roberti, Cristiana Caliceti, Aldo Roda |
| Abstract |
Berberine (BBR) is a natural alkaloid obtained from Berberis species plants, known for its protective effects against several diseases. Among the primary BBR metabolites, berberrubine (M1) showed the highest plasma concentration but few and conflicting data are available regarding its concentration in biological fluids related to its new potential activity on vascular cells. A combined analytical approach was applied to study biodistribution of M1 in comparison with BBR. The optimization of sample clean-up combined with a fully validated HPLC-ESI-MS/MS tailored for M1 allows sufficient detectability and accuracy to be reached in the different studied organs even when administered at low dose, comparable to that assumed by human. A predictive human vascular endothelial cell-based assay to measure intracellular xanthine oxidase has been developed and applied to study unexplored activities of M1 alongside other common activities. Results showed that oral M1 treatment exhibits higher plasma levels than BBR, reaching maximum concentration 400-fold higher than BBR (204 vs 0.5 ng/mL); moreover, M1 exhibits higher concentrations than BBR also in all the biological compartments analyzed. Noteworthy, the two compounds follow two different excretion routes: M1 through urine, while BBR through feces. In vitro studies demonstrated that M1 inhibited intracellular xanthine oxidase activity, one of the major sources of reactive oxygen species in vasculature, with an IC50 = 9.90 ± 0.01 μg/mL and reduced the expression of the inflammatory marker ICAM-1. These peculiar characteristics allow new perspectives to be opened up for the direct use of M1 instead of BBR in endothelial dysfunction treatment. |
X Demographics
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Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 2 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Scientists | 1 | 50% |
| Science communicators (journalists, bloggers, editors) | 1 | 50% |
Mendeley readers
The data shown below were compiled from readership statistics for 10 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 10 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Doctoral Student | 2 | 20% |
| Professor > Associate Professor | 2 | 20% |
| Student > Master | 2 | 20% |
| Student > Bachelor | 1 | 10% |
| Student > Ph. D. Student | 1 | 10% |
| Other | 0 | 0% |
| Unknown | 2 | 20% |
| Readers by discipline | Count | As % |
|---|---|---|
| Medicine and Dentistry | 2 | 20% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 10% |
| Nursing and Health Professions | 1 | 10% |
| Biochemistry, Genetics and Molecular Biology | 1 | 10% |
| Agricultural and Biological Sciences | 1 | 10% |
| Other | 1 | 10% |
| Unknown | 3 | 30% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 17 May 2018.
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#20,663,600
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Outputs from Analytical & Bioanalytical Chemistry
#6,602
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Outputs of similar age from Analytical & Bioanalytical Chemistry
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