Anti‐hepatitis B virus activity and hepatoprotective effect of des(rhamnosyl) verbascoside from Lindernia ruellioides in vitro

Abstract

Although clinically approved hepatitis B virus (HBV) polymerase inhibitors (lamivudine‐3TC, entecavir, etc.) serve as effective therapeutics, the virus can easily generate resistance to them. Therefore, the treatment of HBV infection remains a public health problem. Numerous studies have shown that natural products have prospective anti‐HBV activity. The purpose of this study was to isolate and extract des(rhamnosyl) verbascoside from Lindernia ruellioides (Colsm.) Pennell and explore its anti‐HBV and hepatoprotective effects. Anti‐HBV activity was evaluated in HepG2.2.15 cells, a human hepatocellular carcinoma cell line with HBV‐stable infection, and its protective effect was evaluated in HL‐7702 cells, a normal human liver cell line. HepG2.2.15 cells maintained normal growth morphology within the selected concentration range of des(rhamnosyl) verbascoside. It also inhibited the expression of HBV antigens and HBV DNA in a dose‐ and time‐dependent manner in vitro. Further, western blot experiments showed that it could downregulate HBV X protein (HBx) expression in a dose‐dependent manner. In the H2O2‐induced hepatocyte injury model, the cell‐survival rate of the HL‐7702 cells with the highest drug dose reached 85.25%, which was significantly improved compared with that of the model group. Most of the cells returned to normal morphology, showing polygonal or fusiform structures. Thus, it may be stated that des(rhamnosyl) verbascoside exhibits anti‐HBV activity and hepatoprotective effects in vitro and may exert an anti‐HBV effect via antigen inhibition, HBV DNA secretion, and HBx protein expression.

Phytomedicines to Target Hepatitis B Virus DNA Replication: Current Limitations and Future Approaches

“…It significantly downregulated the expression of the HBV X protein (HBx) and inhibited DNA replication in a dose-dependent manner. In addition, it improved cell survival following H 2 O 2 -induced hepatocyte injury [71]. Another polysaccharide, heteropolysaccharide (FP-1), isolated from flaxseed hull using the hot water extraction method, reportedly exerted immunomodulatory effects by upregulating the mRNA expression levels of TNF-α, nitric oxide (NO), IL-6, and IL-12 in murine macrophages, and inhibited HBV DNA replication in HepG2.2.15 cells [72].…”

Acteoside ameliorates hepatic ischemia-reperfusion injury via reversing the senescent fate of liver sinusoidal endothelial cells and restoring compromised sinusoidal networks

“…Acteoside (ACT), a phenylpropanoid glycoside extracted from natural dicotyledonous plants, has been considered to be promising in the treatment of acute liver injury, hepatitis, and cancer [16]. Several studies stated that ACT may exert a direct protective effect on hepatocytes and improve steatosis and oxidative stress by inhibiting the nuclear factor kappa B pathway and further reducing the production of tumor necrosis factor-α (TNF-α) and ROS [17][18][19][20][21]. Moreover, ACT inhibited the expression of cell adhesion molecules (CAMs), including intercellular CAM-1 (ICAM-1) and vascular CAM-1 (VCAM-1), to exert anti-inflammatory activities and protected the vascular endothelial cells from oxidative stress and free radicals [22][23][24].…”