Jiazhu LI, Anqi WANG, Yue TENG, Yuwei WANG, Yinghua LUO, Chenghao JIN

College of Life Science & Technology, Heilongjiang Bayi Agricultural University, Daqing 163319, China

Abstract 5-O-methylvisammioside is a chemical derived from the dry root of Saposhnikovia divaricata, which has the functions of expelling pathogenic wind from body surface, removing dampness to relieve pain, and relieving convulsion. Recent studies have found that 5-O-methylvisammioside can play a variety of pharmacological effects such as anti-tumor, anti-inflammation, anti-virus and anti-depression through a variety of ways. The paper reviews the pharmacological action and mechanism of 5-O-methylvisammioside in recent years.

Key words 5-O-methylvisammioside, Anti-tumor, Anti-inflammation, Anti-virus, Anti-depression

1 Introduction

Saposhnikoviadivaricata, a perennial herb belonging Umbelliaceae, is mainly produced in Hebei, Heilongjiang, Sichuan and Inner Mongolia. It is widely used in the treatment of diseases such as exterior syndrome, rubella pruritus, rheumatism arthralgia, tetanus, damp abundance due to splenic asthenia,etc.[1-3]. 5-O-methylvisammioside is a phenolic compound derived from the dry root ofS.divaricata, molecular formula C22H28O10, soluble in methanol, ethanol and other organic solvents, and has a variety of pharmacological activities such as anti-tumor, anti-inflammation, anti-virus and anti-depression. The research progress of pharmacological action and mechanism of 5-O-methylvisammioside in recent years is summarized, so as to provide some reference for further research, development and utilization of 5-O-methylvisammioside.

2 Anti-tumor

Cancer is a kind of diseases caused by the loss of normal regulation and excessive proliferation of body cells, and it is a serious threat to human health and life. Studies have found that 5-O-methylvisammioside can inhibit the proliferation of a variety of cancer cells. Depending on the cell line, 5-O-methylvisammioside mainly inhibits the proliferation of various cancer cells by blocking G1/G0phase or G2/M phase. Wangetal.[4]found that tumor necrosis factor (TNF-α) promoted the proliferation of vascular smooth muscle cells; if pretreated by 5-O-methylvisammioside, the proportion of cells in G1/G0phase was significantly increased, while the proportion of cells in S phase and G2/M phase was significantly decreased. These results indicated that 5-O-methylvisammioside could inhibit the proliferation of smooth muscle cells by blocking the proliferation of smooth muscle cells at G0/G1phase.

Apoptosis is an autonomic and orderly process of cell death, which involves the activation, expression and regulation of a series of genes. At present, inducing cell apoptosis has become one of the main means of treating cancer cells. Matusiewiczetal.[5]found that the content of 5-O-methylvisammioside was the highest in juice and extracts fromS.divaricataroot. Statistical analysis showed that Caco-2 cells incubated with juice and 50% extract ofS.divaricata(15.9×10-1mg/mL) significantly increased the number of early apoptotic cells after 24 h of treatment, while Caco-2 cells incubated with 50% extract ofS.divaricata(15.9×10-2mg/mL) significant induced the apoptosis of colon cancer cells (Caco-2 cells) after 72 h of treatment, and further significantly decreased the number of living cells.

Reactive oxygen species (ROS) play a very important role in the occurrence and development of tumors, which can induce apoptosis and autophagy of tumor cells, and inhibit the proliferation and survival rate of tumor cells. Louetal.[6]suggested that treatment of A549 cells with Yu Ping Feng San (YPFS) could increase the cisplatin-induced ROS level, thereby leading to cell death. Fifteen chemical markers were identified from extracts of YPFS, including 5-O-methylvisammioside (0.455 mg/g). Therefore, it could be speculated that 5-O-methylvisammioside in YPFS played a synergistic role with cisplatin to increase ROS levels, leading to the death of A549 cells.

3 Anti-inflammation

Inflammation is a common and important basic pathological process, which is the defense response of living tissue in the vascular system to injury factors. Xueetal.[7]found that 5-O-methylvisammioside had obvious antipyretic effect on rat fever induced by yeast. Duetal.[8]put forward that three key enzymes in inflammatory bowel disease (IBD), namely inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and intestinal alkaline phosphatase (IALP), mediated anti-inflammatory action through expression. In a lipopolysaccharide (LPS)-induced chronic inflammatory model of mouse macrophages, YPFS treatment inhibited the activation of iNOS and COX-2 genes in a dose-dependent manner. These gene expression changes suggested that YPFS mediated anti-inflammation by regulating inflammatory enzymes.

4 Anti-virus

Viruses are a kind of acellular microorganisms that proliferate by replication. Viruses can invade different tissues and organs, infecting cells and causing disease. According to the reports, 5-O-methylvisammioside inhibits respiratory virus infection and induces the expression of antiviral protein gene. Liuetal.[9]found that 5-O-methylvisammioside inhibited influenza virus (IFV) and human respiratory syncytial virus (HRSV) in a dose-dependent manner before, during and after viral infection, effectively preventing the invasion and infection of viruses. Duetal.[10]pointed out that 5-O-methylvisammioside inhibited the neuraminidase activity of influenza A virus in epithelial cells, thus preventing the release and spread of the virus. The above results proved that 5-O-methylvisammioside significantly inhibited respiratory virus infection and induced the expression of antiviral protein gene.

5 Anti-depression

Depression is a symptom of neurosis, and it is an illness caused by chronic mental stress. Sunetal.[11]suggested that pretreatment of 5-O-methylvisammioside significantly increased the activity and exploration ability of LPS-induced depression in mice, shortened the immovability time, and inhibited the production of pro-inflammatory cytokines such as interleukin-6 (IL-6) and tumor necrosis factor (TNF-α) in the serum of LPS-induced mice. Meantime, the superoxide dismutase (SOD) level was increased, and the expression of malondialdehyde (MDA) in hippocampus was decreased, thus alleviating the depressive symptoms of mice. Therefore, 5-O-methylvisammioside is a promising antidepressant drug.

6 Conclusions

In recent years, a large number of studies on 5-O-methylvisammioside show that 5-O-methylvisammioside has a wide range of biological activities, and no obvious toxic side effects. In addition to above effects of anti-tumor, anti-inflammation, anti-virus and anti-depression, 5-O-methylvisammioside still has many pharmacological effects. However, the specific mechanism of action is relatively little studied, and more and deeper systematic studies are needed at the animal, cellular and molecular levels, in order to provide the theoretical basis for the pharmacological study and development of 5-O-methylvisammioside.