Search Results (7)

(1) Background: Establishment of a method for evaluating Gentianae Radix et Rhizoma (GRR) classes based on chemical composition and core efficacy; (2) Methods: Liquid chromatography–mass spectrometry (LC–MS) was used to determine the chemical constituents of GRR-first class (GF) and GRR-second class (GS). The cell viability, liver function, oxidative stress enzyme activity, and inflammatory factor levels of GF and GS on H₂O₂-induced HepG2 cells were determined with CCK-8, ELISA, and biochemical methods, and the antioxidant activity of the two was evaluated using bioefficacy; ELISA, biochemical methods, real-time fluorescence quantitative polymerase chain reaction (RT-qPCR) method, and Western blot (WB) were used to determine the liver function, oxidative stress enzyme activity, inflammatory factor levels, and expression of related genes and proteins in mice with acute liver injury (ALI) model induced with 0.3% CCl₄ olive oil solution after gavage administration; (3) Results: GF and GS had the same types of components, but the cyclic enol ether terpenes such as morinlon goside c, loganin, gentiopicroside, and swertiamarin differed significantly between the two; the effect of GF on CCl₄-induced acute hepatic injury in C57BL/6 mice was stronger compared to GS. It helped alleviate weight loss, increase hepatic and splenic indices, improve hepatic lobular structure and hepatocyte status, inhibit collagen deposition, enhance oxidative stress and anti-inflammatory-related genes and protein expression, and decrease apoptotic genes and proteins more significantly than GS; (4) Conclusions: In this study, we established a GRR class evaluation method combining chemical composition and core medicinal effects, which can rapidly determine the differential composition of GF and GS, detect the quality of GRR through antioxidant bioefficacy, and validate it with in vivo experiments, which provides references for the evaluation of the class of GRR and the rational use of medication in the clinic. Full article

Gentianae Scabrae Radix is used in traditional medicine and is known to possess bioactive compounds, including secoiridoid glycosides, flavonoids, lignans, and triterpenes. Trifloroside (TriFs) is a secoiridoid glycoside known for its antioxidant activity; however, its other effects have not been studied. In the present study, we investigated the biological effects of TriFs isolated from the roots of Gentianae Scabrae Radix using pre-osteoblast MC3T3E-1 cells. No cellular toxicity was observed with 1 μM TriFs, whereas 5–100 μM TriFs showed a gradual increase in cell viability. Alkaline phosphatase staining and microscopic observations revealed that 1–10 μM TriFs stimulated osteogenic activity during early osteoblast differentiation. Trifloroside also increased mineral apposition during osteoblast maturation. Biochemical analyses revealed that TriFs promoted nuclear RUNX2 expression and localization by stimulating the major osteogenic BMP2-Smad1/5/8-RUNX2 pathway. Trifloroside also increased p-GSK3β, β-catenin, p-JNK, and p-p38, but not Wnt3a, p-AKT, and p-ERK. Moreover, TriFs increased the MMP13 levels and promoted cell migration and adhesion. In contrast, TriFs-induced osteoblast differentiation and maturation had negligible effects on autophagy and necrosis. Our findings suggest that TriFs induces osteogenic effects through differentiation, adhesion, migration, and mineral apposition. Therefore, TriFs is suggested as a potential drug target in osteoblast-mediated bone diseases. Full article

Gentiana lutea L. is a medicinal plant the roots of which are primarily used in treatments of various human digestive disorders, but also the production of alcoholic liquors. The roots (radix) of G. lutea are described in the European Pharmacopeia, but knowledge about the chemical composition and biological activities of its aerial parts is still limited. Thus, until today aerial parts of this species have not been used in medical treatments or consumed. Therefore, flowers, leaves, and stems extracts of G. lutea obtained by using four different extraction solvents (petrol ether, chloroform, ethanol, and water) were examined for their chemical composition and biological activities. High concentrations of salicylic acid, apigenin, and naringenin were recorded for ethanol stem extracts, while significant amounts of kaempferol were detected in leaves and flowers in chloroform and water extracts, respectively. The highest antioxidant potential was recorded for flower and stem petrol ether extracts with the lowest IC₅₀ values, ranging from 94.46 ± 9.45 to 105.38 ± 10.54 μg/mL. Ethanol extracts of flowers and stems showed moderate antioxidant activity (IC₅₀ 143.15 ± 14.32 and 146.90 ± 14.69 μg/mL) as well as strong antimicrobial activity against Candida albicans (21.00 ± 1.00 and 27.50 ± 1.78 mm inhibition zones, respectively). In addition, ethanol extracts had higher antimycotic activity compared to naturally occurring phenolic compounds that are used as positive controls. Moreover, statistical analysis of the activities of plant extracts and single compounds showed that levels of chlorogenic and caffeic acids strongly correlate with the biological activities of the extracts, i.e., they are the main carriers of these biological activities. The presented results indicate the possible use of aerial parts of G. lutea as a natural preservative, as well as a antimicrobial agent, which significantly amplifies the benefits of this medicinal crop and greatly affects the sustainability of cultivated Gentiana plantation. Full article

Gentianae Radix et Rhizome (Longdan in Chinese, GRR) in Chinese Pharmacopoeia is derived from the dried roots and rhizomes of Gentiana scabra and G. rigescens, that have long been used for heat-clearing and damp-drying in the medicinal history of China. However, the characterization of the chemical components of two species and the screening of chemical markers still remain unsolved. In current research, the identification and characterization of chemical components of two species was performed using ultra-high-performance liquid chromatography (UHPLC) coupled with linear ion trap-Orbitrap (LTQ-Orbitrap) mass spectrometry. Subsequently, the chemical markers of two species were screened based on metabolomics and multivariate statistical analysis. In total, 87 chemical constituents were characterized in G. scabra (65 chemical constituents) and G. rigescens (51 chemical constituents), with 29 common chemical constituents being discovered. Thereafter, 11 differential characteristic components which could differentiate the two species were designated with orthogonal partial least squares discriminant analysis (OPLS-DA) and random forest (RF) iterative modeling. Finally, seven characteristic components identified as (+)-syringaresinol, lutonarin, trifloroside, 4-O-β-d-glu-trifloroside, 4″-O-β-d-glucopyranosy1-6′-O-(4-O-β-d-glucaffeoyl)-linearroside, macrophylloside a and scabraside were selected as the chemical markers for the recognition of two Gentiana species. It was implied that the results could distinguish the GRR derived from different botanical sources, and also be beneficial in the rational clinical use of GRR. Full article

Gentiana radix is used in traditional Chinese medicine and has functions of clearing heat and drying dampness, as well as purging liver and gallbladder fire. A highly sensitive and effective strategy for rapid screening and identification of target constituents has been developed by using ultra high-performance liquid chromatography coupled with linear ion trap-Orbitrap mass spectrometry (UHPLC-LTQ-Orbitrap) in crude and wine-processed Gentiana radix. Based on the accurate mass measurement (<5 ppm), retention times, and MS fragmentation ions, 52 constituents were unambiguously or tentatively characterized from Gentiana radix, including 21 iridoids, 11 flavonoids, 19 xanthones, and a triterpenoid. This study demonstrated that the established method could be a rapid, effective analytical tool for screening and characterization of compounds in the complex systems of Gentiana radix. By comparing the structure and peak areas of chemical constituents in crude and wine-processed Gentiana radix, we found that some compounds in crude and wine-processed Gentiana radix were significantly different. Full article

Secoiridoid and iridoid glycosides are the main active components of Gentianae radix. In this work, one iridoid and three secoiridoid glycosides from Gentianae radix have been purified by high-speed counter-current chromatography in two runs using different solvent systems. Ethyl acetate–n-butanol–water (2:1:3, v/v/v) was the optimum solvent system to purify ca. 4.36 mg of loganic acid, 3.05 mg of swertiamarin, and 35.66 mg of gentiopicroside with 98.1%, 97.2% and 98.6% purities, respectively, while 31.15 mg of trifloroside with 98.9% purity was separated using hexane–ethyl acetate–methanol–water (1:3:1:3, v/v/v/v). The structures of the glycosides were identified by mass spectrometry and NMR. After separation, the anti-nitric oxide production effects of the compounds on lipopolysaccharide-induced BV-2 murine microglial cells were also evaluated. All of the compounds inhibited the production of nitric oxide in lipopolysaccharide-induced BV-2 cells with high cell viabilities in a concentration-dependent manner, which demonstrated that were able to be used as a nitric oxide inhibitor. Full article

Sorafenib has been used as a standard therapy for advanced hepatocellular carcinoma (HCC). In Asia, patients with HCC are potentially treated with the combination of sorafenib and Chinese herbal medicines to improve the efficiency and reduce the side effects of sorafenib. However, limited information about the herb-drug interactions is available. We hypothesize that the Chinese herbal medicine may exert hepatoprotective effects on the sorafenib-treated group. The aim of this study is to investigate the pharmacokinetic mechanism of drug-drug interactions of sorafenib including interacting with hepatoprotective formulation, Long-Dan-Xie-Gan-Tang formulation (LDXGT) and with two cytochrome P450 3A4 (CYP3A4) inhibitors, grapefruit juice and ketoconazole. Liver enzyme levels and histopathology of liver slices were used to evaluate sorafenib-induced hepatotoxicity and the potential hepatoprotective effects of the LDXGT formulation on subjects treated with the combination of sorafenib and the herbal medicine. In this study, a validated HPLC-photodiode array analytical system was developed for the pharmacokinetic study of sorafenib in rats. As the result of the pharmacokinetic data, pretreatment with the LDXGT formulation did not significantly interact with sorafenib compared with sorafenib oral administration alone. Furthermore, grapefruit juice and ketoconazole did not significantly affect sorafenib metabolism. Furthermore, pretreatment with variable, single or repeat doses of the LDXGT formulation did not suppress or exacerbate the sorafenib-induced hepatotoxicity and histopathological alterations. According to these results, the LDXGT formulation is safe, but has no beneficial effects on sorafenib-induced hepatotoxicity. A detailed clinical trial should be performed to further evaluate the efficacy or adverse effects of the LDXGT formulation in combination with sorafenib in humans. Full article