Licoricesaponin G2

Nat Prod Res . 2017 Mar;31(6):691-695.

Antimutagenic components in Glycyrrhiza against N-methyl-N-nitrosourea in the Ames assay[Pubmed: 27466044]

Abstract Antimutagenesis against N-nitroso compounds contribute to prevention of human cancer. We have found that Glycyrrhiza aspera ethanolic extract exhibits antimutagenic activity against N-methyl-N-nitrosourea (MNU) using the Ames assay with Salmonella typhimurium TA1535. In the present study, eight purified components from Glycyrrhiza, namely glabridin, glycyrrhetinic acid, glycyrrhizin, licochalcone A, licoricesaponin H2, Licoricesaponin G2, liquiritigenin and liquiritin were evaluated for their antimutagenicity against MNU in the Ames assay with S. typhimurium TA1535. Glycyrrhetinic acid, glycyrrhizin, Licoricesaponin G2, licoricesaponin H2 and liquiritin did not show the antimutagenicity against MNU in S. typhimurium TA1535. Glabridin, licochalcone A and liquiritigenin reduced revertant colonies derived from MNU in S. typhimurium TA1535 without showing cytotoxic effects, indicating that these compounds possess antimutagenic activity against MNU. The inhibitory activity of glabridin and licochalcone A was more effective than that of liquiritigenin. Thus, Glycyrrhiza contains antimutagenic components against DNA alkylating, direct-acting carcinogens. Keywords: Glabridin; Glycyrrhiza; N-methyl-N-nitrosourea; antimutagen; licochalcone A; liquiritigenin.

Chinese Traditional & Herbal Drugs,2016,47(8):1289-1296.

Screening of activity components with anti-inflammation in Sang Ju Yin and verification of monomer.[Reference: WebLink]

To investigate the anti-inflammatory activity of Sang Ju Yin (Mulberry Leaf and Chrysanthemum Decoction), and elucidate its bioactive components on nuclear factor-κappa B (NF-κB) inhibition, and to further clarify the anti-inflammatory mechanism of Sang Ju Yin, so as to provide the basis for establishing its quality standard.
METHODS AND RESULTS:
UPLC-Q/TOF MS coupled with NF-κB activity luciferase reporter assay system was applied to determine the potential anti-inflammatory components in Sang Ju Yin. And the human bronchial epithelial cells (BEAS-2B) were selected to set up the inflammatory injury model, caffeic acid, chlorogenic acid, glycyrrhizic acid, loganin, and malonic acid in Sang Ju Yin were investigated for their anti-inflammation. Sixteen components were screened to have the NF-κB inhibitory effects. Among them, malonic acid, 22β-acetoxyl-glycyrrhizic acid, and Licoricesaponin G2 were first reported to have the NF-κB inhibitory activity.
CONCLUSIONS:
Sang Ju Yin contains the potential NF-κB inhibitors. Sixteen potentially active ingredients are found to have the anti-inflammatory effects as NF-κB inhibitors.

J Pharm Biomed Anal. 2015;111:28-35.

Rapid screening and identification of active ingredients in licorice extract interacting with V3 loop region of HIV-1 gp120 using ACE and CE-MS.[Pubmed: 25854854]

The binding of envelope protein gp120 to glycosphingolipids is very important during the human immunodeficiency virus entering into the host cell. This step occurs in the V3 loop region in particularly. The conserved core sequence of V3 loop in gp120 was named R15K. Anti-HIV drug targeting to R15K would avoid the drug-resistance caused by HIV-1 genetic diversity.
METHODS AND RESULTS:
Here, for the first time, affinity capillary electrophoresis (ACE) and capillary electrophoresis-mass spectrometry (CE-MS) were used for establishing a simple, rapid and effective method of screening the licorice extract for biological activity (anti-HIV), which avoided the complicated isolation and purification process. R15K, 3'-sialyllactose (the positive control), and d-galactose (the negative control) were used for the development and validation of ACE method. After the interaction between licorice extract and R15K was confirmed by ACE, the relative active ingredients were isolated by SPE and their structures were determined by CE-ESI-MS online. In this research, two mixtures from licorice extract were found to be active. Furthermore, glycyrrhizin and Licoricesaponin G2 were verified as the main ingredients that significantly interacted with R15K via CE-MS and LC-MS. The results of quantitative assays showed that the active mixture contained glycyrrhizin of 74.23% and licorice saponin G2 of 9.52%. Calculated by Scatchard analysis method, glycyrrhizin/R15K complex had the highest binding constant (1.69 ± 0.08) × 10(7)L/mol among 27 compounds isolated from licorice extract.
CONCLUSIONS:
The anti-HIV activity of glycyrrhizin was further confirmed by bioactive experiment of cellular level. This strategy might provide a high throughput screening and identifying platform for seeking HIV-1 inhibitors in natural products.