التفاصيل البيبلوغرافية
| العنوان: |
datasheet1_Short Chain (≤C4) Esterification Increases Bioavailability of Rosmarinic Acid and Its Potency to Inhibit Vascular Smooth Muscle Cell Proliferation.docx |
| المؤلفون: |
Tina Blažević (10014368), Gottfried Reznicek (1278432), Limin Ding (6020717), Gangqiang Yang (8452911), Patricia Haiss (10014371), Elke H. Heiss (404988), Verena M. Dirsch (404989), Rongxia Liu (683687) |
| سنة النشر: |
2021 |
| المجموعة: |
Smithsonian Institution: Digital Repository |
| مصطلحات موضوعية: |
Pharmacology, Basic Pharmacology, Clinical Pharmacology and Therapeutics, Clinical Pharmacy and Pharmacy Practice, Pharmaceutical Sciences, Pharmacogenomics, Toxicology (incl. Clinical Toxicology), Pharmacology and Pharmaceutical Sciences not elsewhere classified, vascular smooth muscle cells, rosmarinic acid, proliferation, pharmacokinetics, rosmarinic acid esters |
| الوصف: |
Rosmarinic acid is a natural phenolic acid and active compound found in many culinary plants, such as rosemary, mint, basil and perilla. Aiming to improve the pharmacokinetic profile of rosmarinic acid and its activity on vascular smooth muscle cell proliferation, we generated a series of rosmarinic acid esters with increasing alkyl chain length ranging from C1 to C12. UHPLC-MS/MS analysis of rat blood samples revealed the highest increase in bioavailability of rosmarinic acid, up to 10.52%, after oral administration of its butyl ester, compared to only 1.57% after rosmarinic acid had been administered in its original form. When added to vascular smooth muscle cells in vitro, all rosmarinic acid esters were taken up, remained esterified and inhibited vascular smooth muscle cell proliferation with IC 50 values declining as the length of alkyl chains increased up to C4, with an IC 50 of 2.84 µM for rosmarinic acid butyl ester, as evident in a resazurin assay. Vascular smooth muscle cells were arrested in the G 0 /G 1 phase of the cell cycle and the retinoblastoma protein phosphorylation was blocked. Esterification with longer alkyl chains did not improve absorption and resulted in cytotoxicity in in vitro settings. In this study, we proved that esterification with proper length of alkyl chains (C1–C4) is a promising way to improve in vivo bioavailability of rosmarinic acid in rats and in vitro biological activity in rat vascular smooth muscle cells. |
| نوع الوثيقة: |
dataset |
| اللغة: |
unknown |
| Relation: |
https://figshare.com/articles/dataset/datasheet1_Short_Chain_C4_Esterification_Increases_Bioavailability_of_Rosmarinic_Acid_and_Its_Potency_to_Inhibit_Vascular_Smooth_Muscle_Cell_Proliferation_docx/13620710 |
| DOI: |
10.3389/fphar.2020.609756.s001 |
| الاتاحة: |
https://doi.org/10.3389/fphar.2020.609756.s001 |
| Rights: |
CC BY 4.0 |
| رقم الانضمام: |
edsbas.2D350F62 |
| قاعدة البيانات: |
BASE |