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OBJECTIVE: To study the metabolism of gentiopicroside by rat intestinal flora in vitro and time profiles of gentiopicroside and its metabolites in rat serum after oral administration of gentiopicroside. METHOD: Using high performance liquid chromatography (HPLC) for determination of gentiopicroside, gentianine and gentianal content of rat intestinal flora culture medium in vitro and rat serum sample in vivo. RESULT: Gentiopicroside was metabolized quickly in vitro by rat intestinal flora, consequently gentianine and gentianal content appeared. Gentianine and gentianal were observed after gentiopicroside oral administration 4 times in rat serum sample, and gentiopicroside content decreased after oral administration 6 times. CONCLUSION: Gentianine and gentianal were the important bioactive metabolites of gentiopicroside in rats.
OBJECTIVE: To study the correlation between morphological variation and gentiopicroside content in cultivated Gentiana manshurica roots and to investigate the feasibility of breeding new varieties of high effective constituent content. METHOD: Gentiopicroside was determined in 5 morphological types of cultivated G. manshurica roots by HPLC, which are normal (or wild) type, white-flowered type, thick-rooted type, broad-leaved type I and broad-leaved type II. RESULT: Among different types gentiopicroside content is the highest in the roots of thick-rooted type, the contents decrease as following order: normal type, broad-leaved type I white-flowered type and broad-leaved type II, and the gentiopicroside contents in the same type root system are a positive correlation with root ages, as 3-years-age roots > 2-years-age roots > 1-year-age varied with roots. CONCLUSION: The contents of effective constituent vary with the morphological variation in cultivated G. manshurica. It is feasible to breed a new variety with high effective constituent with the morphological character as a selecting index.
Micellar electrokinetic electrophoresis was employed to determine two active components, gentiopicroside (GE) and swertiamarin (SW) in one Tibetan preparation medicine named shiweilongdankeli, two Tibetan herbal medicines named Gentiana rhodantha and Gentiana kitag and three other Chinese Gentiana medicines named Gentiana scabra, Gentiana rigescens and Gentiana macrophylla. The dissociation constants of gentiopicroside and swertiamarin determined by MEKC were 7.71 and 6.25. The optimum buffer system was 70 mm borate-10 mm sodium dodecylsulfate (SDS) -6% (v/v) ispropanol (pH 9.0). The voltage was 15 kV and detection was at 254 nm. The lower limits of detection (defined as a signal-to-noise ratio of about 3) were approximately 3.86 mg L(-1) for GE and 5.88 mg L(-1) for SW. The relative standard deviation of the migration time and peak area of the GE and SW were 2.33, 2.47 and 1.27, 2.19%, respectively and the recoveries of the two compounds were 96-104% for GE and 92-102% for SW.
Hairy root cultures of Gentiana macrophylla were established by infecting the different explants four Agrobacterium rhizogenes strains namely A(4)GUS, R1000, LBA 9402 and ATCC11325, and hairy root lines were established with A. rhizogenes strain R1000 in 1/2 MS + B(5) medium. Initially, 42 independent hairy root clones were maintained and seven clones belongs to different category were evaluated for growth, morphology, integration and expression of Ri T-DNA genes, and alkaloid contents in dry root samples. On the basis of total root elongation, lateral root density and biomass accumulation on solid media, hairy root clones were separated into three categories. PCR and Southern hybridization analysis revealed both left and right T-DNA integration in the root clones and RT-PCR analysis confirmed the expression of hairy root inducible gene. GUS assay was also performed to confirm the integration of left T-DNA. The accumulation of considerable amounts of the root-specific secoiridoid glucosides gentiopicroside was observed in GM1 (T +/L and T +/R) and the GM2 (T +/L and T -/R DNA) type clones in considerably higher amount whether as two T -/L but T +/R callus-type clones (GM3) accumulated much less or only very negligible amounts of gentiopicroside. Out of four media composition the 1/2 MS + B(5) vitamin media was found most suitable. We found that initial establishment of root cultures largely depends on root:media ratio. Maximum growth rate was recorded in 1:50 root:media ratio. The maximum biomass in terms of fresh weight (33-fold) was achieved in 1/2 MS + B(5) media composition after 35 days in comparison to sixfold increase in control. The biomass increase was most abundant maximum from 15 to 30 days. Influence of A. rhizogenes strains and Ri plasmid of hairy root induction, the possible role of the T(L)-DNA and T(R)-DNA genes on growth pattern of hairy root, initial root inoculum:media ratio and effect of media composition is discussed.
Bioassay directed fractionation of the (1:1) chloroform-methanol extract of Gentiana spathacea H.B.K (Gentianaceae) led to the isolation of gentiopicroside (gentiopricrin) (1), the major spasmolytic component of the plant. Gentiopicroside inhibited, in a concentration-dependent manner, the spontaneous contractions of isolated guinea pig ileum. Contractions induced by histamine, acetylcholine, BaCl2 and KCl on the ileum were also significantly blocked by this monoterpene glucoside, which suggests that this compound might be interfering with calcium influx into the smooth muscle cells.
OBJECTIVE: To study gentiopicroside's determination and comparison of various parts of herb by TLCS and make it impossible to uncover resource of Gentian in Xinjiang area. METHOD: Gentiopicroside's determination and comparison of various parts of herb in Gentiana Plants were carried out by TLCS. RESULT: The average recovery rate was 98.66% (RSD = 1.33%, n = 5). The Contents were stable. The results kept a high degree of comparable with HPLC ones. CONCLUSION: This method was good-steady, high-accurate, simple, convenient, sensitive, reproducible.
INTRODUCTION: Parkinson's disease (PD) is a common neurodegenerative disorder characterized by classical symptoms including bradykinesia, rest tremor and rigidity. Oxidative stress and mitochondrial dysfunction are recognized as pivotal factors in PD progression. Gentiopicroside (GPS), a secoiridoid derived from Gentiana manshurica Kitagawa, exhibits antioxidant and mitophagy induction properties. Nonetheless, the effects and mechanisms by which GPS mitigates neurodegeneration in PD remain to be thoroughly elucidated. OBJECTIVES: The goal of this study was to investigate the neuroprotective effects and mechanisms of GPS in PD models. METHODS: We established the MPTP/MPP+-induced PD models to measure the neuroprotection of GPS. Transcriptomic analysis, oxidative biochemical kits, western blot and cell immunofluorescence were conducted to elucidate the fundamental mechanisms at play. Subsequently, the targeting and activation of the transmembrane G protein-coupled receptor-5 (TGR5) by GPS were measured by molecular docking, cellular thermal shift assay, microscale thermophoresis (MST) and cyclic adenosine monophosphate (cAMP) quantitation. Finally, we verified whether the neuroprotective and antioxidant effects of GPS were dependent on TGR5 by using specific small interfering RNA (siRNA), pharmacological antagonist and knockout mice. RESULTS: GPS significantly attenuated dopaminergic (DAergic) neuron loss and restored motor function in the MPTP-induced PD mouse model. Whole-genome RNA sequencing and subsequent mechanistic investigations revealed that GPS enhanced the expression and facilitated nuclear entry of factor erythroid-related 2-factor 2 (Nrf2), and reduced oxidative stress and mitochondrial dysfunction stimulated by neurotoxin. Additionally, GPS could target TGR5 and prevent its downregulation in PD model. TGR5's silencing or inhibition weakened the neuroprotective effect of GPS and blocked GPS-mediated activation of Nrf2 antioxidant signaling in PD model. Moreover, the therapeutic effect of GPS in mitigating motor deficits and neurodegeneration was also abolished in Tgr5 knockout mice. CONCLUSION: These findings collectively indicated that GPS targeted TGR5 to activate Nrf2 antioxidant signaling and ultimately ameliorated the pathological progression of PD.
The pharmacokinetics and tissue distribution of Gentiopicroside (GPS), one of the major active components of the Gentiana species of medicinal plants, was studied following oral and intravenous administration in mice. The distribution of GPS in mice after oral and intravenous doses could be fitted to a two-compartments open model. The serum half-life of GPS was 6.1 h and 2.8 h for intravenous and oral administration, respectively. The Tmax of GPS after oral administration was 0.50 h, and the bioavailability was 39.6%. The AUC gradient in individual tissues following intravenous administration was kidney >serum >liver >spleen >lung >thymus >fat >heart >muscle >stomach >intestinal >brain. The MRT gradient was muscle >serum >lung >spleen >lung >intestinal>heart >stomach >brain >liver >thymus >kidney >fat. Overall the data show that GPS could be absorbed rapidly in mice, but with a low bioavailability, and could distribute to tissues extensively, but was generally cleared quickly with short MRTs. The study demonstrates the need for repeated dosage, or better, a slow release formulation as an ideal means of administering GPS.
High-performance liquid chromatography was employed to determine the contents of several marker substances such as gentiopicroside, mangiferin, palmatine, berberine, baicalin, wogonin and glycyrrhizin in Sann-Joong-Kuey-Jian-Tang. The separation was performed on a Cosmosil 5C18-AR column by gradient elution with 0.03% (v/v) phosphoric acid-acetonitrile (0 min, 90:10; 10 min, 87:13; 17-27 min, 77:23; 40 min, 62:38; 50 min, 55:45) as the mobile phase at a flow-rate of 1.0 ml/min, with detection at 254 nm. n-Propylparaben was used as the internal standard and seven regression equations revealed linear relationships between the peak-area ratios (marker substances/internal standard) and concentrations. The repeatability and reproducibility (relative standard deviation) of the method were in the ranges 0.02-1.78% and 1.44-4.95%, respectively.
Gentiopicroside (1), a secoiridoid glycoside isolated from the methanol extract of the aerial parts of Centaurium erythraea, has been assessed for antibacterial and free radical scavenging activities. General toxicity of 1 has also been determined by brine shrimp lethality bioassay.
Wound healing properties of Gentian (Gentiana lutea ssp. symphyandra) extract and its main constituents, gentiopicroside, sweroside and swertiamarine (compounds 1-3, respectively) were evaluated by comparison with dexpanthenol on cultured chicken embryonic fibroblasts. The extract was also analyzed by HPLC to quantify its constituents. Chicken embryonic fibroblasts from fertilized eggs were incubated with the plant extract and its constituents, compounds 1-3. Using microscopy, mitotic ability, morphological changes and collagen production in the cultured fibroblasts were evaluated as parameters. Wound healing activity of Gentian seems to be mainly due to the increase in the stimulation of collagen production and the mitotic activity by compounds 2 and 3, respectively (p < 0.005 in all cases). All three compounds also exhibited cytoprotective effects, which may cause a synergism in terms of wound healing activity of Gentian. The findings demonstrated the wound healing activity of Gentian, which has previously been based only on ethnomedical data.
Gentiopicroside (GPS), a main bitter secoiridoid constituent of roots of Gentiana macrophylla Pall., was tested for therapeutic effects on the two hepatic injury models, the CCl4-induced and lipopolysaccharide (LPS)/bacillus Calmette-Guerin (BCG)-induced hepatitides. An increase in serum level of hepatic aminotransferases (GOT: EC 2.6.1.1. and GPT: EC 2.6.1.2.) induced by a p.o. treatment of CCl4 was suppressed by pretreatment with GPS at 30-60 mg/kg/day for 5 consecutive days. An increase of these enzymes triggered by an i.v. treatment with LPS in mice primed with bacillus Calmette-Guerin (BCG) was also inhibited by GPS pretreatment at the same dose of GPS. In the BCG/LPS model, tumor necrosis factor (TNF), a major inflammatory mediator, was increased in serum with a peak at 90-120 min, followed by an increase of serum transaminase activities. GPS treatment significantly suppressed the increase of TNF in serum at the therapeutic doses, suggesting that GPS protected against hepatitis by inhibiting the production of TNF.
As a part of our studies on the metabolism of crude drug components by intestinal bacteria, gentiopicroside (a secoiridoid glucoside isolated from Gentiana lutea), was anaerobically incubated with various defined strains of human intestinal bacteria. Many species had ability to transform it to a series of metabolites. Among them, Veillonella parvula ss parvula produced five metabolites, which were identified as erythrocentaurin, gentiopicral, 5-hydroxymethylisochroman-1-one,5-hydroxymethylisochromen-1- one and trans-5,6-dihydro-5-hydroxymethyl-6-methyl-1H,3H-pyrano[3,4-c]pyra n-1-one.
A quantitative method to determine loganic acid and gentiopicroside in Gentiana macrophylla Pall. and Gentiana straminea Maxim. by RP-HPLC was established in this paper. The two compounds were base-isolated on the coloumn of Zorbax SB-C18 (250 mm x 4.6 mm i.d., 5 microm) which eluted with MeOH and H2O (0.04% H3PO4). The methol ratio increased from 18% to 28% in 15 min with detective wave at 254 nm and coloumn temperature at 30 degree C, flow rate at 1 ml/min. A wide range of linearity and the good linear relationships were achieved on above condition. The contents of the two compounds in different parts of the two plants were also determined and compared in this paper.
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