•A UPLC-ESI-QTOF-MS2 method was used to identify the chemical constituents in THL.•The metabolites in rats after administration THL extract were also investigated.•The in vivo antioxidant activities of THL were evaluated for the first time.•A total of 75 compounds were detected and 26 metabolites were identified.•The phenolics of THL might play key role in the in vivo antioxidant activities.Tetrastigma hemsleyanum is a traditional edible and medicinal plant in China. The phytochemical composition of its leaf (THL) and the bioavailability and metabolism of these compounds and their metabolites in vivo are less known. A metabolomics approach was therefore taken by using UPLC-ESI-QTOF-MS2. A total of 75 compounds were tentatively characterized in THL. Ten original compounds and 11 metabolites observed in plasma, and 20 original compounds and 26 metabolites detected in urine. Meanwhile, rats treated with THL extract in an oxidative stress model showed significantly increased total antioxidant capacity (T-AOC), superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) activities and glutathione (GSH) content and decreased malondialdehyde (MDA) content in plasma and tissues. Results suggest THL phenolics are bioavailable, and these compounds and their metabolites are likely behind the observed activities. The present study demonstrates that THL extract as a good source of antioxidant ingredient for the safeguard against oxidative stress-related chronic diseases.

Radix Tetrastigma (RT), a herbal medicine and functional food in China, showed strong antiproliferative activities in vitro. However, the effects and the underlying mechanism of phenolic-rich extract of RT in H22 tumor-bearing mice are still unknown. Thus, the phenolic profiles and antitumor/antioxidant activities of a solid phase extraction (SPE) semi-purified extract of RT were investigated by a combination of chemical assays, LC-QTOF-MS/LC-QqQ-MS techniques and a tumor-bearing mice model. As a result, the total phenolic/flavonoid contents (TPC/TFC) and 24 individual phenolics were identified and quantified, which showed higher contents than that of crude extract. Results also indicated that RT extract could inhibit tumor growth and induce apoptosis by regulating the expression of Bcl-2 family proteins and activating the caspase family proteins as well as suppressing tumor angiogenesis by inhibiting vascular endothelial growth factor (VEGF) expression. Besides, the interleukin-2 (IL-2) levels, tumor necrosis factor-α (TNF-α) production, CD4+/CD8+ ratio, and NK cell levels were increased by RT administration, while RT significantly increased superoxide dismutase (SOD)/glutathione peroxidase (GSH-Px) activities and decreased malondialdehyde (MDA) content. Summarily, the findings clearly demonstrated that RT extract could inhibit tumor growth by inducing apoptosis and inhibiting angiogenesis as well as preventing cancer by improving the immune functions and antioxidant activities.

The effects of two fatty acids, oleic acid (OLA) and elaidic acid (ELA) on normal human umbilical vein endothelial cells (HUVEC) and non-rafts HUVEC were investigated in this study. The expression levels of inflammatory cytokines (ICAM-1, VCAM-1 and IL-6) were analyzed. Western blot was used to analyze the expression levels of inflammation-related proteins (NF-κB, ERK1/2) and toll-like receptors 4 (TLR4). The results showed that the levels of nuclear translocation of NF-κB p65 and phosphorylated ERK1/2 were significantly decreased only in non-lipid rafts cells pretreated with trans fatty acid (TFA). The expression of TLR4 in the ELA-treated normal cells was higher than that in non-lipid rafts HUVEC. When the lipid rafts was destroyed by methyl-β-cyclodextrin, the levels of nuclear translocation of NF-κB p65, phosphorylated ERK1/2 and TLR4 were decreased significantly. Therefore, lipid rafts may be involved in TFA induced-inflammation in HUVEC through blocking the inflammatory signal pathway. Lipid rafts might be a platform for specific receptors such as TLR4 for TFA to activate the pro-inflammation on cell membranes.

•The TFC and antioxidant/antiproliferative activities of RT were investigated.•A UPLC-QTOF-MS method was established to identify the constituents and metabolites.•A UPLC-QqQ-MS method was employed to quantify the major flavonoids.•A total of 58 compounds and 33 metabolites were identified or tentatively characterized.•Five flavonoids were suggested to be the major antioxidant/antiproliferative compounds.Radix Tetrastigma (RT), the roots of Tetrastigma hemsleyanum Diels et Gilg, is consumed as both functional food and traditional medicinal herb in China, but there is rare report on its bioactive components. In the present study, the total flavonoid contents (TFC) and antioxidant/antiproliferative activities of RT were evaluated, and the chemical constituents of RT and their metabolites of rat after oral administration were identified and quantified by UPLC-ESI-QTOF-MS/MS and UPLC-ESI-QqQ-MS/MS. The extract of RT exhibited high TFC and antioxidant/antiproliferative activities in which there were 58 compounds characterized or tentatively identified. Nine original compounds and 12 metabolites were detected in plasma, while 11 original compounds and 13 metabolites were observed in urine. Nine flavonoids were quantified and 5 of them (catechin, kaempferol-3-rutinoside, rutin, isoquercitrin and astragalin) were up to 71.46% of TFC; their metabolites were also found in the plasma and urine, which was suggested to be the major antioxidant/antiproliferative compounds.

The present study was conduced to investigate the synergistic effects of combined treatments with Se-methylselenocysteine (SeMSC) and vitamin E (Vit E) in reversing oxidative stress induced by ethanol in serum and different tissues of rats. Sixty female rats were randomly divided into six groups for 30 days’ consecutive pretreatments as followed: control (I), physiological saline (II), 2.8 μg kg−1 Se as SeMSC (III), 2.8 μg kg−1 Se as sodium selenite (Na2SeO3, IV), 5 mg kg−1 α-tocopherol as α-tocopherol acetate (Vit E, V), 5 mg kg−1 α-tocopherol as α-tocopherol acetate and 2.8 μg kg−1 Se as SeMSC (VI). All animals in groups II–VI were treated by ethanol treatment to cause oxidative stress. After 6 h of ethanol treatment, the activities of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), the contents of total antioxidant capacity (T-AOC), malondialdehyde (MDA), glutathione (GSH) and carbonyl protein (CP) in the serum, liver, heart and kidney were measured. The result showed that the individual SeSMC, Na2SeO3 and vitamin E could effectively increase the SOD, T-AOC, GSH-Px and GSH contents as well as significantly decrease the MDA and CP concentrations in the tissues of ethanol-induced rats. At the same dose on different forms of Se, SeMSC showed greater antioxidant activity than Na2SeO3. Moreover, group VI (SeMSC and α-tocopherol acetate) showed much better antioxidant activity than individual group III (SeMSC) and V (α-tocopherol acetate) due to the synergistic effect.

New fertilizing strategies (with exogenetic N, P, Se, and Zn) were explored to regulate the element (Se, Zn, Mn, and Al) and functional component (polyphenol, catechins, free amino acid, polysaccharide, and caffeine) contents of new (a bud and two leaves, grown for about 10 days) and old tea leaves (grown for >3 months) cultivated in a hilly red soil region. Using four different fertilizing strategies (A, Se + Zn; B, Se + Zn + N; C, Se + Zn + P; D, Se + Zn + N + P), the Al and Mn contents of tea leaves in both new and old leaves were significantly decreased. Meanwhile, the contents of Se and Zn were increased, and the contents of some functional components as well as the antioxidant activities in tea leaves were improved. In particular, fertilizing strategy C showed the highest Se (0.444 μg/kg), total polyphenol (28.294%), and catechins (131.852 mg/g) contents and antioxidant activities (DPPH, 95.06%; FRAP, 3.81 mmol FeSO4/g; reducing power, 1.26) as well as the lowest Al (222.005 mg/kg) content among these four strategies, whereas fertilizing strategy B showed the highest Zn (34.235 mg/kg), total free amino acid (5.60%), tea polysaccharide (5.79%), and caffeine (56.684 mg/g) contents as well as the lowest Mn content (747.658 mg/kg). It has been proven that exogenetic elements (N, P, Se, and Zn) as fertilizers could be an effective way to produce tea leaves with higher Se, Zn, and functional component contents and antioxidant activity as well as lower Al and Mn contents in a red soil region.