Our previous research had indicated that the octyl ester derivative of ginsenoside Rh2 (Rh2-O) might have a higher bioavailability than Rh2 in the Caco-2 cell line. The aim of this study was to investigate the cellular uptake and antitumor effects of Rh2-O in human HepG2 cells as well as its underlying mechanism compared with Rh2. Results showed that Rh2-O exhibited a higher cellular uptake (63.24%) than Rh2 (36.76%) when incubated with HepG2 cells for 24 h. Rh2-O possessed a dose- and time-dependent inhibitory effect against the proliferation of HepG2 cells. The IC50 value of Rh2-O for inhibition of HepG2 cell proliferation was 20.15 μM, which was roughly half the value of Rh2. Rh2-O induced apoptosis of HepG2 cells through a mitochondrial-mediated intrinsic pathway. In addition, the accumulation of ROS was detected in Rh2-O-treated HepG2 cells, which participated in the apoptosis of HepG2 cells. Conclusively, the findings above all suggested that Rh2-O as well as Rh2 inducing HepG2 cells apoptosis might involve similar mechanisms; however, Rh2-O had better antitumor activities than Rh2, probably due to its higher cellular uptake.
The influences of ultrasound-assisted, pharmacopeia, and supercritical fluid extraction methods on bioactive compounds and biological activities of propolis were evaluated. Results showed that propolis extracted by ultrasoundassisted method contained more phenolic compounds, and showed the highest total phenolic content (245.84 ± 6.41 mg GAE/g DW), total flavonoids content (198.82 ± 5.74 mg RE/g DW), and stronger in vitro antioxidant activity (DPPH·: 1.03 ± 0.04 mmol Trolox/g DW, ABTS+·: 2.19 ± 0.05 mmol Trolox/g DW, and FRAP: 1.48 ± 0.12 mmol FeSO 4 /g DW) than those of pharmacopoeia and supercritical fluid methods. A total of 36 phenolic compounds were identified in propolis. Among them, quercetin, quercetin-3-methyl-ether, kaempferol, isorhamnetin, luteolin-methyl-ether, and quercetin-7-methyl-ether could only be found in ultrasound-assisted and pharmacopoeia methods. Moreover, the phenolic compounds had the similar metabolic pathways in rats and were mainly metabolized by sulfation and glucuronidation pathways. Additionally, ultrasonic-treated propolis have good in vivo antioxidant activity and could repair D-galactoseinduced oxidative damage in rats. Therefore, ultrasound-assisted method could replace pharmacopeia method to be considered as bioactive compounds extraction from propolis, taking into consideration of yield, short extraction time, and high antioxidant activity.
The hydrophilic extracts of eggplant peel (HEEP) and purple sweet potato (HEPP) and lipophilic extracts of tomato (LET) and carrot (LEC) were mixed in different ratios to assess the significance of the compatibility of aliments, based on their antioxidant and anti-inflammatory interactions in H9c2 cells. The results indicated that groups of some combinational extracts (HEPP-HEEP F1/10, LEC-HEEP F3/10, LEC-HEPP F3/10) showed stronger synergistic antioxidant and anti-inflammatory effects than individual groups. For example, the glutathione peroxidase (GPx) activity of the LEC-HEEP (F3/10) group (86.71 ± 1.88) was higher than that in the HEEP (79.97 ± 1.68) and LEC (77.31 ± 1.85) groups. The level of reactive oxygen species (ROS) was 30.37 ± 0.25 in the LEC-HEEP (F3/10) group while the levels were 34.34 ± 0.36 and 46.23 ± 0.51 in the HEEP and LEC groups, respectively. And the level of malondialdehyde (MDA) was 1.82 ± 0.24 in the LEC-HEEP (F3/10) group while the levels were 2.48 ± 0.13 and 3.01 ± 0.24 in the HEEP and LEC groups, respectively. The expressions of inflammatory mediators (IL-1β, IL-6, IL-8) and cell adhesion molecules (VCAM-1, ICAM-1) showed similar tendencies. However, some groups (LET-LEC F5/10, LET-LEC F9/10, LET-HEPP F7/10) showed antagonistic effects based on these indicators. The principal component analysis showed that samples could be defined by two principal components: PC1, the main phenolic acids and flavonoids; PC2, carotenoids. Moreover, phenolics and anthoyanins were in the majority in synergistic groups, and carotenoids were in the majority in antagonistic groups. These results indicated that there exist synergistic or antagonistic interactions of aliments on antioxidation and anti-inflammation, which implied the significance of food compatibility.
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