Bioactive xanthones from whole plants of Gentianella acuta / 中草药·英文版

Objective: To study the constituents from the whole plants of Gentianella acuta and their biological activities. Methods: The compounds were isolated by multiple chromatographic methods and the structures of mentioned isolates were determined by routine NMR experiments and chemical methods. Results: A phytochemical investigation to obtain intestine motility inhibitor resulted in the isolation of one new xanthone glycoside, gentixanthonoside A (1), along with nine tetrahydroxanthones, 1,3,5R,8S-tetrahydroxy-5,6,7,8-tetrahydroxanthone (2), 1,3,5S,8S-tetrahydroxy-5,6,7,8-tetrahydroxanthone (3), amarellin E (4), amarellin F (5), swertiachoside B (6), amarellin D (7), amarellin C (8), amarellin A (9), and amarellin B (10) from the whole plants of G. acuta. Conclusion: Compounds 2–10 showed significant reduce effects on contraction tension at 40 µM.

Research advance on chemical constituents and pharmacological effects of Gentianella acuta / 中草药

Gentianella acuta is a commonly used Mongolian medicine and its mainly active constituents are xanthone, terpenoids, and phenylpropanoids. It has the effects of clearing heat and draining dampness, anti-tumor, liver protection, anti-depression, and anti-inflammation. This review summarizes the chemical components and pharmacology of G. acuta from the literatures in recent 30 years in order to provide basis for the development of this plant.

Bioassay-guided separation of effective components from Gentianella acuta and their protective effect on oxidative damage in PC12 cells induced by H2O2 / 中草药

Objective: To investigate the compounds of Gentianella acuta with strong protective effect on oxidative damage in PC12 cells induced by H2O2. Methods: Damage model of PC12 cells was established by H2O2 and real-time cell analysis (RTCA) was utilized to evaluate the protective effect of extracts and compounds. Meanwhile, bioassay-guided method was applied to separating effective components, and HPLC was used for the determination and structure confirmation of compounds. Results: Fractions of n-butanol and acetic ether showed protective effect on oxidative damage in PC12 cells induced by H2O2. The anti-oxidant activity of compounds 1 and 2 showed dose-dependent manner in the scope of 3.125-50.000 μmol/L, and the protective effect was the strongest at the concentration of 50.000 μmol/L. Compounds 3 and 5 showed the best protective effect at the concentration of 25.000 μmol/L and 3.125 μmol/L respectively. Compounds 1, 2, 3, and 5 were identified as bellidifolin, demethylbellidifolin, swertianolin and norswertianolin, respectively. Conclusion: Compounds 1, 2, 3, and 5 show protective effect on oxidative damage in PC12 cells induced by H2O2, maybe the main active components in G. acuta. But the mechanism is still uncertain, and further exploration is imperative.

Chemical constituents from Gentianella acuta / 中成药

AIM To study the chemical constituents from Gentianella acuta (Michx.) Hulten.METHODS The 30％ and 90％ ethanol fractions of 70％ ethanol extract from G.acuta were isolated and purified by silica,ODS and preparative HPLC column,then the structures of obtained compounds were identified by spectral data.RESULTS Nine compounds were isolated and identified as sinenoside Ⅰ (1),(+)-lariciresinol-4,4'-0-bis-β-D-glucopyranoside (2),(+)-8-hydroxylariciresinol-4'-O-β-D-glucopyranoside (3),(+)-lariciresinol-4-O-3-D-glucopyranoside (4),(7S,8R)-erythro-7,9,9'-trihydroxy-3,3'-dimethoxy-8-O-4'-neolignan-4-O-β-D-glucopyranoside (5),(7S,8R)-erythro-4,9,9'-trihydroxy-3,3'-dimethoxy-8-O-4'-neolignan-7-O-β-D-glucopyranoside (6),(7S,8R)-erythro-4,7,9-trihydroxy-3,3'-dimethoxy-8-O-4'-neolignan-9'-O-β-D-glucopyranoside (7),balanophonin (8),urolignoside (9).CONCLUSION Compounds 2-9 are isolated from genus Gentianella for the first time.

Effects of Ethyl Acetate Extracts of Gentianella acuta on IRS-1 and Akt in Insulin Resistance HepG2 Cells / 世界科学技术-中医药现代化

This paper was aimed to study the effect of ethyl acetate extracts of Gentianella acuta on the gene and protein of insulin significant signal IRS-1 and Akt in insulin resistance (IR) HepG2 cells.The CCK-8 method was used to detect the HepG2 cell activity.HepG2 cells of human liver cancer were cultured with high concentration insulin (10-6 mol· L-1)for 36 hours to establish IR cell model.According to the results of CCK-8,the control group,model (IR) group,ethyl acetate extracts of Gentianella acuta IR + 50 μg· mL-1,IR + 500 μg· mL-1 group,and the metformin group were divided.Glucose consumption was measured with a glucose assay kit.The expressions of IRS-1 and Akt gene in IR HepG2 cells were detected by RT-PCR after 6-hour using of ethyl acetate extracts of Gentianella acuta.Western blot was used to detect the expression of IRS-1 and Akt protein after 6-hour using of ethyl acetate extracts of Gentianella acuta.The results showed that when the concentration of ethyl acetate extracts of Gentianella acuta was 500 μg· mL-1,the survival rate reached 95％.When the concentration was higher than 500 μg· mL-1,the survival rate decreased.Compared with the IR group,the IR + 50 μg· mL-1 group and the IR + 500 μg· mL-1 group promoted glucose consumption of IR HepG2 cells,but its effect was less than that of the metformin hydrochloride group.The expression of IRS-1 and Akt in IR HepG2 cells was significantly increased by using RT-PCR in the group of IR + 50 μg· mL-1 and IR + 500 μg·mL-1 compared with the IR group after 6-hour using of ethyl acetate extracts of Gentianella acuta.The expression of IRS-1 and Akt protein in the group of IR + 50 μg· mL-1 and IR + 500 μg· mL-1 was significantly higher than that in the IR group after 6-hour medication detected by western blot.It was concluded that the ethyl acetate extracts of Gentianella acuta can increase the expression of IRS-1,Akt gene,the expression of IRS-1 and Akt protein in HepG2 cells,which may be the mechanism of IR improvement.

Isolation and identification of xanthones from Gentianella acuta / 中国中药杂志

Twelve xanthones compounds were isolated from the ethanol extract of Gentianella acuta by means of reversed-phase preparative HPLC and various kinds of column chromatography including silica gel and ODS . Their structures were fully elucidated on the basis of MS, 1D and 2D-NMR data. The structures of xanthones were identified as 1, 7-dihydroxy-3-methoxyxanthone-7-O-β-D-glucopyranoside (1), swertiapuniside (2), 1, 3, 8- trihydroxy -4, 5-dimethoxyxanthone-1-O-β-D-glucopyranosyl(6→1)-O-β-D-glucopyranoside (3), 1, 2, 8-trihydroxy-5, 6-dimethoxyxanthone-2-O-β-D-glucopyranoside (4), 1, 3, 7, 8-tetrahydroxyxanthone-1-O-β-D-glucopyranoside (5), 1, 3, 5, 8-tetrahydroxy-5, 6, 7, 8-tetrahydroxanthone (6), 1, 3, 5-thihydroxyxanthone (7),1, 3, 5, 8-tetrahydroxyxanthone (8), 1, 2, 8-trihydroxy-5, 6-dimethoxyxanthone (9), bellidifolin (10), mangiferin (11), swertianolin (12). Compounds 1-9 were isolated from Gentianella genus for the first time.

Determination of Three Xanthone Glycosides in Gentianella Acuta by HPLC / 世界科学技术-中医药现代化

To develop a method for determining 3 Xanthone glycosides (1, 5-dihydroxy- 3-methoxyxanthone 8-O-β-D-glucopyranoside(F1), 1-hydroxy-3, 4-dimethoxyxanthon 7-O-β-D-glucopyranoside (F2), 1, 8-dihydroxy-3, 4-dimethoxyxanthone 5-O-β- D-glucopyranoside (F3) of Gentianella acuta by HPLC. The Thermo syncronis C18 (4.6 mmí250 mm, 5 μm) was used for simultaneous determination of 3 Xanthone glycosides in G. acuta. Isocratic elution with water and acetonitrile was 75.5:24.5. The flow rate was 1.0 mL·min-1 and the detection wavelength was set at 254 nm. The column temperature was 35℃. The linear concentration ranges of F1,F2,F3 were 14.06 ~ 281.28 μg·mL-1 (R2=0.999 7),0.56~11.16 μg·mL-1 (R2=0.999 8),0.46~9.20 μg·mL-1 (R2=0.999 9), respectively; The average recov-eries (n = 9) were 99.70% (RSD=1.06%),99.78% (RSD=1.21%),100.28% (RSD=1.15%), respectively. The method is simple, accurate and sensitive, and can be used for the quality control of G. acuta as a reference.