Introduction
In the present study, ternary deep eutectic solvent‐based ultrasound‐assisted extraction was developed for the efficient extraction of plantamajoside, acteoside, quercetin and kaempferol from Plantago asiatica L.
Methodology
Six kinds of choline chloride‐based ternary deep eutectic solvents (TDESs) were prepared as potential extraction solutions. In order to obtain optimal extraction efficiency, a series of extraction conditions were investigated by single‐factor test and orthogonal test.
Results
The extraction efficiency of choline chloride/lactic acid/ethylene glycol (ChCl‐LA‐EG) was much higher than that of other TDESs. ChCl‐LA‐EG‐11 synthesised with choline chloride, lactic acid and ethylene glycol (1:4:2) was considered to have a higher extraction efficiency. The optimal ultrasound‐assisted extraction conditions were as follows: water content in ChCl‐LA‐EG‐11, 50%; extraction temperature, 70°C; ratio of solid/liquid, 20 mg/mL; ultrasonic power, 60 W; extraction time, 35 min; pH of the solution, 8. Under the optimal extraction conditions, the extraction efficiencies of plantamajoside, acteoside, quercetin and kaempferol were 3.83 ± 0.41, 4.23 ± 0.45, 0.56 ± 0.15 and 0.19 ± 0.08 mg/g, respectively. The extraction efficiency of the total target components was 9.21 ± 0.63 mg/g, which was much higher than that of conventional solvents (water, methanol, ethanol, 50% methanol, 50% ethanol). The target components were isolated efficiently from the TDES solution by an AB‐8 macroporous resin column with a recovery rate of 95.6%.
Conclusion
This study demonstrated that TDESs possessed excellent physical and chemical properties and had enormous potential for active component extraction of traditional Chinese medicinal materials.
Floxuridine (FUdR, 5-fluoro-2-deoxyuridine) was widely used in patients with tumor. But the poor activity and severe side effects have been observed in the clinic, which resulted from increased degradation cleavage of FUdR to 5-FU by thymidine phosphorylase and reduced transporter-mediated entry into cells. In this study, we have synthesized a series of L-aspartic acid β-esters and L-glutamic acid γ-esters of FUdR to improve the metabolic stability of FUdR and target FUdR to cancer cells via amino acid transporter ATB 0,+ which was exclusively up-regulated in some cancerous tissue. The uptake mechanism, stability, in vitro/in vivo antiproliferation action, pharmacokinetics, and tissue distribution were studied. The combined results showed the unusual 5′-β-L-Asp-FUdR possessed a better tumor inhibition rate and a better metabolic stability than FUdR through a ATB 0,+ -mediated prodrug approach. The present study provided the first proof-of-concept of exploiting ATB 0,+ for tumor-selective delivery of nucleoside analogues in the form of prodrug.
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