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.

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.

Efecto hepatoprotector del extracto acuoso de Gentianella nitida en un modelo experimental inducido por paracetamol / Hepatoprotective effect of the aqueous extract of Gentianella nitida in an experimental model induced by paracetamol

El objetivo fue evaluar el efecto hepatoprotector del extracto acuoso de Gentianella nitida (hercampuri) en un modelo experimental inducido por paracetamol. Para evaluar el efecto de hepatoprotección del extracto de Gentianella nitida se empleó paracetamol como inductor del daño hepático. Se analizó in vitro la capacidad antioxidante (DPPH, ABTS, FRAP), el contenido de fenoles totales y flavonoides del extracto acuoso de Gentianella nitida. En el modelo in vivo se trabajó con 24 ratas Holtzman hembras de 2 meses, formándose 4 grupos (n= 6): grupo control, grupo paracetamol, grupo silimarina y grupo Gentianella nitida. Al grupo Gentianella nitida se administró una dosis de 200 mg/kg de peso corporal durante 7 días, seguido del paracetamol 300 mg/kg de peso corporal por 4 días más. Se utilizó silimarina 50 mg/kg de peso como estándar de referencia. En el homogenizado de hígado se midió catalasa, superóxido dismutasa, glutatión S- transferasa, glutatión, TBARs, proteínas totales. En el análisis estadístico se aplicó prueba Kruskal-Wallis, y como prueba pos hoc Mann Whitney. Se trabajó con una significancia p < 0,05. La capacidad antioxidante equivalente a ácido ascórbico (AAEAC-DPPH) fue 56 g AA/mg ss y la capacidad antioxidante equivalente a trolox (TEAC-ABTS) fue 87,7 g trolox/mg ss. Expresado en FRAP fue 98,5 g FeSO4/mg ss. Fenoles totales fue 65,8 g EAG/mg ss y de flavonoides, 11,7 g EQ/mg ss. En el modelo in vivo, el grupo Gentianella nitida tuvo resultados significativos en la actividad de SOD y TBARs (aumento; p< 0,05) y en la actividad de glutatión S-transferasa y glutatión (disminución; p < 0,05). El extracto de Gentianella nitida exhibe capacidad antioxidante en correlación con el contenido de fenoles totales, protegiendo la actividad de las enzimas antioxidantes hepáticas frente al daño de las ROS producidas por el paracetamol.

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.

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.

Características fisicoquímicas y capacidad antioxidante in vitro del extracto de Gentianella nitida / Physicochemical properties and in vitro antioxidant capacity of the Gentianiella nitida extract

Introducción. La Gentianella nitida (hercampuri) es usada como hepatoprotector en la medicina tradicional. Objetivo. Determinar las características fisicoquímicas y capacidad antioxidante in vitro del extracto acuoso de Gentianella nitida. Diseño. Observacional, analítico. Lugar. Centro de Investigación de Bioquímica y Nutrición, Facultad de Medicina, Universidad Nacional Mayor de San Marcos, Lima, Perú. Material. Extracto acuoso al 4% p/v de la planta entera Gentianella nitida procedente de Junín. Intervenciones. Observación y análisis de las características fisicoquímicas y capacidad antioxidante in vitro. Principales medidas de resultados. Características fisicoquímicas (densidad aparente y materia soluble); capacidad antioxidante total empleando DPPH, ABTS, FRAP; contenido de fenoles totales y flavonoides. Resultados. La Gentianella nitida presentó una densidad aparente 1,032 g/mL. Con el método de DPPH y ABTS tuvo IC50=145 µg/mL y 1,49 mg/mL respectivamente. La capacidad antioxidante equivalente a ácido ascórbico (AAEAC-DPPH) fue 56 (µg AA/mg ss) y la capacidad antioxidante equivalente a trolox (TEAC-ABTS) fue 87,7 (µg trolox/mg ss). Expresado en FRAP, fue 98,5 (µg FeSO4/mg ss) y 55,6 (µg EAA/mg ss). El contenido de fenoles totales fue 65,8 µg EAG/mg ss y de flavonoides 11,7 µg EQ/mg ss. Conclusiones. El extracto acuoso de la Gentianella nitida exhibió capacidad antioxidante que guardó correlación con el contenido de compuestos fenólicos.

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.

Genus Gentianella Moench:A Phytochemical and Ethnopharmacological Review / 中草药·英文版

The plants in genus Gentianella Moench (Gentianaceae) which comprised approximately 250 species, are mainly distributed in temperate regions of the world.Many Gentianella plants are intensely bitter and employed in traditional medicine to stimulate appetite, treat disorders of the gallbladder, and treat fever like the other bitter gentians in various regions of the world.Some species exhibit other remarkable therapeutic effects in the treatments of obesity,diabetes, and heart diseases.Eleven iridoids, twenty-eight xanthones, three C-glucoflavonoids, and eight other compounds have been isolated from the genus.Most of these compounds are associated with antimicrobial,anti-inflammatory, anti-oxidant, hypoglycemic, and antitumor activities, which provide an empirical base for the traditional utilization of the plants in genus Gentinella Moench.

Gentianaceae endémicas del Perú

La familia Gentianaceae es reconocida en el Perú por presentar alrededor de 15 géneros y aproximadamente de 170 especies (Brako & Zarucchi, 1993; Ulloa Ulloa et al., 2004; S. Castillo, com.pers.), mayormente hierbas y arbustos. En este trabajo se reconoce 103 especies endémicas en siete géneros. Los géneros con mayor número de especies endemicas son Gentianella y Macrocarpaea. Las especies endémicas ocupan principalmente las regiones de la Puna Húmeda y Seca, Páramo y Bosque Muy Húmedo Montano, entre los 1000 y 5100 m de altitud. Se aplicaron las categorías y criterios de la UICN a 99 especies. Treinta y tres especies endémicas se encuentran representadas dentro de un área protegida.

The Gentianaceae are represented in Peru by 15 genera and nearly 170 species (Brako & Zarucchi, 1993; Ulloa Ulloa et al., 2004; S. Castillo, pers. comm.), mainly herbs and shrubs. Here we recognize 103 endemic species in seven genera. Gentianella and Macrocarpaea are the genera with the largest number of endemic species. Endemic Gentianaceae are found in the Humid and Dry Puna, Paramo and Very Humid Montane Forests regions, between 1000 and 5100 m elevation. We applied IUCN categories and criteria to 99 species. Thirty-three endemic species have been found to date in Peruvian protected areas.