Homoplantaginin

A flavonoid glycoside with antioxidant and anti-inflammatory activities

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5mg

￥975.00

780.00

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10mg

￥1512.00

1210.00

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25mg

￥3125.00

2500.00

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50mg

￥5237.00

4190.00

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Background

Homoplantaginin is a flavonoid glycoside that has been found in S. plebeia and has antioxidant and anti-inflammatory activities.^1,2,3 It scavenges 2,2-diphenyl-1-picrylhydrazyl radicals with an IC₅₀ value of 0.35 ?g/ml in a cell-free assay.² Homoplantaginin reverses hydrogen peroxide-induced decreases in glutathione (GSH) levels and glutathione peroxidase (GPX) and superoxide dismutase (SOD) activity in HL-7702 cells when used at concentrations ranging from 1 to 100 ?g/ml. It reduces protein levels of toll-like receptor 4 (TLR4), MyD88, caspase-1, and IL-1β induced by palmitic acid in human umbilical vein endothelial cells (HUVECs) when used at concentrations of 1 and 10 ?M.³ Homoplantaginin (50 and 100 mg/kg) decreases serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), TNF-α, and IL-1 levels, as well as reduces liver inflammatory cell infiltration and hepatocyte necrosis in a mouse model of immunological liver injury induced by Bacillus Calmette-Guérin (BCG) vaccine and LPS.²

1.Weng, X.C., and Weng, W.Antioxidant activity of compounds isolated from Salvia plebiaFood Chem.71(4)489-493(2000) 2.Qu, X.-J., Xia, X., Wang, Y.-S., et al.Protective effects of Salvia plebeia compound homoplantaginin on hepatocyte injuryFood Chem. Toxicol.47(7)1710-1715(2009) 3.He, B., Zhang, B., Wu, F., et al.Homoplantaginin inhibits palmitic acid-induced endothelial cells inflammation by suppressing TLR4 and NLRP3 inflammasomeJ. Cardiovasc. Pharmacol.67(1)93-101(2016)

Protocol

Cell experiment:

The viability of cultured cells is determined using the MTT assay. Human umbilical vein endothelial cells are exposed to various concentrations of homoplantaginin (0.1, 1, 3, 10, 30, 100 μM) for 48 h. Subsequently, 20 μL of MTT (5 mg/mL) is added to each well for an additional 4 h at 37°C. The supernatant is removed, and DMSO is added to dissolvethe formazan crystals. The optical absorbance is measured at 540 nm[3].

Animal experiment:

Rats: Homoplantaginin is dissolved in a solution consistingof DMSO, PEG 400, ethanol and normal saline(2:2:3:3, v/v/v/v) at a concentration of 10 mg/mL. The rats are randomly divided into three groups to receive oral administration(150 mg/kg), tail vein injection (15 mg/kg) and peritoneal injectionv (15 mg/kg). Blood samples (approximately 0.5 mL) are collected from the retro-orbital plexus into heparinized microfugetubes at 5, 10, 20, 30, 45, 60, 90, 120, and 180 min after administration. The plasma samples, separated by centrifuging the blood samples at 10,000 rpm[4]. Mice: Homoplantaginin is dissolved in 5% amylum. Homoplantaginin is administered orally by gastric intubation during the experimental period at doses of 25, 50, 100 mg/kg/d, respectively. Eight hours after injection of LPS, the mice are anesthetized with ether and blood samples are collected by exsanguination from the inferior vein. The liver is removed and fixed in formalin for histological analysis[1].

参考文献:

[1]. Qu XJ, et al. Protective effects of Salvia plebeia compound homoplantaginin on hepatocyte injury. Food Chem Toxicol. 2009 Jul;47(7):1710-5.
[2]. He B, et al. Homoplantaginin Inhibits Palmitic Acid-induced Endothelial Cells Inflammation by Suppressing TLR4 and NLRP3 Inflammasome. J Cardiovasc Pharmacol. 2016 Jan;67(1):93-101.
[3]. Wu F, et al. Homoplantaginin modulates insulin sensitivity in endothelial cells by inhibiting inflammation. Biol Pharm Bull. 2012;35(7):1171-7.
[4]. Cong Y, et al. Pharmacokinetics of homoplantaginin in rats following intravenous, peritoneal injection and oral administration. J Pharm Biomed Anal. 2016 Sep 10;129:405-9.