OBJECTIVETo explore the effects of high dose glycosides of Tripterygium wilfordii Hook. f (GTW) on the fertility of young rats.

METHODSFifty female SD young rats and 50 male SD young rats were randomly divided into the blank group and the GTW group, 25 in each. GTW was given at the daily dose of 9 mg/kg. After 12 weeks of medication, the male rats were caged together with healthy adult female rats in the ratio of 1:1. The female rats were caged together with healthy adult male rats in the ratio of 2:1. The cage process lasted for two weeks, totally for three times. The pregnant rate of female rats and the survival rate of baby rats were then observed.

RESULTSThere was no significant difference in the pregnant rate or the survival rate of baby rats in the GTW group.

CONCLUSIONHigh dose GTW showed no obvious effects on the fertility of adult rats or the growth and development of new born rats.

Animals ; Female ; Fertility ; drug effects ; Glycosides ; administration & dosage ; pharmacology ; Male ; Pregnancy ; Rats ; Rats, Sprague-Dawley ; Tripterygium

Tripterygium glycosides liposome(TPGL) were prepared by thin film-dispersion method, which were optimized accor-ding to their morphological structures, average particle size and encapsulation rate. The measured particle size was(137.39±2.28) nm, and the encapsulation rate was 88.33%±1.82%. The mouse model of central nervous system inflammation was established by stereotaxic injection of lipopolysaccharide(LPS). TPGL and tripterygium glycosides(TPG) were administered intranasally for 21 days. The effects of intranasal administration of TPG and TPGL on behavioral cognitive impairment of mice due to LPS-induced central ner-vous system inflammation were estimated by animal behavioral tests, hematoxylin-eosin(HE) staining of hippocampus, real-time quantitative polymerase chain reaction(RT-qPCR) and immunofluorescence. Compared with TPG, TPGL caused less damage to the nasal mucosa, olfactory bulb, liver and kidney of mice administered intranasally. The behavioral performance of treated mice was significantly improved in water maze, Y maze and nesting experiment. Neuronal cell damage was reduced, and the expression levels of inflammation and apoptosis related genes [tumor necrosis factor-α(TNF-α), interleukin-1β(IL-1β), BCL2-associated X(Bax), etc.] and glial activation markers [ionized calcium binding adaptor molecule 1(IBA1) and glial fibrillary acidic protein(GFAP)] were decreased. These results indicated that liposome technique combined with nasal delivery alleviated the toxic side effects of TPG, and also significantly ameliorated the cognitive impairment of mice induced by central nervous system inflammation.
Mice ; Animals ; Tripterygium ; Liposomes ; Glycosides/therapeutic use* ; Administration, Intranasal ; Lipopolysaccharides ; Central Nervous System ; Cognitive Dysfunction/drug therapy* ; Inflammation/metabolism* ; Tumor Necrosis Factor-alpha/metabolism* ; Cardiac Glycosides

To systematically evaluate the efficacy and safety of tripterygium glycosides (TG) combined with ACEI/ARB preparation in treating diabetic nephropathy stage IV. The computer retrievals were made in Cochrane Libarary, PubMed, Embase, SCI, Sinnomed, CNKI, Chinainfo and VIP, and hand retrievals were conducted for meeting and academic papers (updated to December 30, 2014), in order to collect randomized controlled trials and quasi-randomized control trials for TG combined with ACEI/ARB preparation in treating diabetic nephropathy stage IV and set the literature inclusion and elimination standards. Eligible literatures were included and evaluated according to standards in Cochrane Handbook. RevMan 5.3 and Stata 12.0 were used for a Meta-analysis. A total of 13 randomized controlled trials and quasi-randomized control trials involving 1119 patients with diabetic nephropathy were included. The Meta analysis result showed that compared with the control group, the combination group showed better effects in reducing the 24-hour urinary protein [MD = -0.84, 95% CI (-1.02, -0.66)], raising albumin [SMD = 0.98, 95% CI (0.81, 1.16)], the total efficiency [OR = 4.23, 95% CI (2.77, 6.46)] and the significant efficiency [OR = 5.35, 95% CI (2.70, 10.60)], with no statistical difference in Serum Creatinine between Both groups [MD = -0.82, 95% CI (-4.30, 2.66), P = 0.64]. However, the risk of adverse reactions increased by 7% [RD = 0.07, 95% CI (0.03, 0.12)]. The Egger's test showed no publication bias. Tripterygium Glycosides combined with ACEI/ARB in treating diabetic nephropathy stage IV is supper than the single administration of ACEI/ARB, with a good prospect in clinical application. Nevertheless, due to the small-size and low-quality samples in this study, more high-quality and large sample-size randomized controlled trials shall be conducted to verify the findings.
Angiotensin Receptor Antagonists ; administration & dosage ; Angiotensin-Converting Enzyme Inhibitors ; administration & dosage ; Diabetic Nephropathies ; drug therapy ; Drug Therapy, Combination ; Glycosides ; administration & dosage ; Humans ; Tripterygium ; chemistry

The isoflavonol glycoside Talosin A, genistein (GT)-7-alpha-L-6-deoxy talopyranose (GT-Tal), was first isolated from the culture broth of Kitasatospora kifunensis MJM341. The aim of the present study was to evaluate the oral absorption and metabolism of the newly isolated isoflavonol glycoside, GT-Tal compared to genistin (GT-7-O-beta-D-glucopyranoside; GT-Glu). Free GT-Glu and GT-Tal could not be detected prior to enzymatic hydrolysis of the corresponding conjugates in rat plasma. Following oral administration of GT-Tal (15 min), GT-Tal was rapidly absorbed through the gastrointestinal tract and metabolized into GT-Tal conjugates with a mean Cmax of 2.74 microg/mL. GT-Tal was further metabolized to its aglycone, free GT and conjugated GT. After oral administration, GT-Glu was absorbed after being convereted to its aglycone and then further metabolized into its conjugate metabolites (free GT with a mean Cmax of 0.24 mg/mL at 1.25 h; conjugated GT with a mean Cmax of 1.31 mg/mL at 2.00 h). Significant differences in absorption and metabolism of GT-Tal and GT-Glu were observed. GT-Tal was metabolized into its corresponding conjugates or underwent deglycosylation to form GT, whereas GT-Glu was metabolized into its aglycone, GT.
Actinobacteria/*chemistry ; Administration, Oral ; Animals ; Area Under Curve ; Glycosides/administration & dosage/*metabolism/pharmacokinetics ; Hydrolysis ; Intestinal Absorption ; Isoflavones/administration & dosage/*metabolism/pharmacokinetics ; Male ; Random Allocation ; Rats ; Rats, Sprague-Dawley

8-O-acetylharpagide and harpagide are two kinds of effective component of Ajuga decumbens extract. A sensitive LC-MS/MS method has been established for pharmacokinetics of 8-O-acetylharpagide and harpagide in beagle dog after oral administration of from A. decumbens extract. Female beagle dogs received orally 12.9, 25.7 mg x kg(-1) p. o. Concentrations of 8-O-acetylharpagide and harpagide in plasma were determined by LC-MS/MS method at different time points and all pharmacokinetic parameters were estimated by non-compartment analysis. The mobile phase consisted of 0.1% formic acid in water (A) and acetonitrile (B), which was run at a flow rate of 0.3 mL x min(-1). Chromatographic separation was achieved on an Agilent ZORBAX XDB-C18 column (2.1 mm x 50 mm, 3.5 microm) using a gradient elution of 5% B at 0-2 min, 95% B at 2. 1-5 min and 5% B at 5. 1-10 min. All analytes, including the IS, were monitored under positive ionization conditions and quantified in MRM mode with transitions of m/z 429.2-369.2 for 8-O-acetylharpagide, m/z 387.2-207.2 for harpagide, and m/z 149.2-103.1 for IS. High purity nitrogen was employed as both the nebulizing and drying gas. Other parameters of the mass spectrometer were optimized as follows: drying gas flow 10.0 L x min(-1); drying gas temperature 300 degrees C; capillary voltage 4 000 V. Results showed that 8-O-acetylharpagide and harpagide showed a dose-dependence profile. T(max) of 8-O-acetylharpagide is 1.7 h, and T(max) of harpagide is 1.57 h, which was higher than T(max) of 8-O-acetylharpagide and harpagide after oral administration of from A. decumbens extract in rats. The different pharmacokinetic parameters may be due to the species differences of rat and beagle dog.
Administration, Oral ; Ajuga ; Animals ; Dogs ; Female ; Iridoid Glycosides ; pharmacokinetics ; Plant Extracts ; metabolism ; Pyrans ; pharmacokinetics ; Rats ; Species Specificity

OBJECTIVETo compare the therapeutic effects of Radix Tripterygium hypoglaucum tablet (THT) and Tripterygium glycosides tablet (TGT) in treating erosive oral lichen planus (EOLP).

METHODSThe patients were randomized into two groups, and they were treated with THT (n = 47) or TGT (n = 47), respectively. The therapeutic effects were evaluated after 3 months treatment.

RESULTSFor the patients of grade 1, the total efficacy in TGT group was 85.71%, compared with 52.38% in THT group, the efficacy was statistically greater in the group receiving TGT (P = 0.043). However, for the patients of grade 2, the difference was not statistically significant (P = 0.173).

CONCLUSIONTGT is more effective in treating EOLP than THT for grade 1 patients. However, TGT is not suitable for patients of child bearing age.

Adult ; Aged ; Drugs, Chinese Herbal ; administration & dosage ; adverse effects ; Female ; Glycosides ; administration & dosage ; adverse effects ; Humans ; Lichen Planus, Oral ; drug therapy ; Male ; Middle Aged ; Treatment Outcome ; Tripterygium

A rapid and validated UPLC-MS method was developed for investigating the absorbed components of Paederia scandens (Lour.) Merrill (P. scandensy) in rat plasma. The bioactive constituents in plasma samples from rats administrated orally with P. scandens extract were analyzed by Ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Four prototype compounds were identified in rat serum as potential bioactive components of P. scandens by comparing their retention times and mass spectrometry data or by mass spectrometry analysis and retrieving the reference literatures. Glucuronidation after deglycosylation was the major metabolic pathway for the iridoid glycosides in P. scandens. These results showed that the methods had high sensitivity and resolution and were suitable for identifying the bioactive constituents in plasma after oral administration of P. scandens. providing helpful chemical information for further pharmacological and mechanistic researched on the P. scandens.
Administration, Oral ; Animals ; Chromatography, Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; metabolism ; Iridoid Glycosides ; blood ; Male ; Rats ; Rats, Wistar ; Rubiaceae ; chemistry ; Sensitivity and Specificity ; Spectrometry, Mass, Electrospray Ionization ; methods

The present study was designed to evaluate the inhibitory effects of Tripterygium wilfordii multiglycoside (GTW) against testosterone-induced benign prostatic hyperplasia (BPH) in rats. A total of 45 rats were randomly divided into five groups: Group I, vehicle control group (sham-operated and treated with vehicle); Group II, BPH group; Group III, BPH rats treated with finasteride at a dose of 5 mg·kg(-1); and Groups IV and V, BPH rats treated with GTW at dose levels of 10 and 20 mg·kg(-1), respectively. The drugs were administered orally once a day for 14 days. Prostate weight, prostatic index, and the testosterone and dihydrotestosterone (DHT) levels in serum and prostate, and the serum prostate specific antigen (PSA) levels were measured; prostate tissues were taken for histopathological examination; and serum biochemical analysis was also performed. The BPH rats displayed an increase in prostate weight, prostatic index with increased testosterone and DHT levels in both the serum and prostate, and increased serum PSA levels. GTW treatment at both doses resulted in significant reductions in prostate weight, prostatic index, testosterone and DHT levels in both the serum and prostate, and serum PSA levels, compared with BPH group. Histopathological examination also indicated that GTW treatment at both doses inhibited testosterone-induced prostatic hyperplasia. Serum biochemical analysis showed that the liver and renal functions were normal. In conclusion, GTW inhibited testosterone-induced prostatic hyperplasia in rats, without host toxicity, providing a basis for the development of GTW as a novel therapy for BPH.
Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; Glycosides ; administration & dosage ; Humans ; Male ; Prostate ; drug effects ; metabolism ; Prostatic Hyperplasia ; drug therapy ; metabolism ; Rats ; Testosterone ; metabolism ; Tripterygium ; chemistry

OBJECTIVETo investigate the mechanism of action on compatible using of total alkaloids of Radix Aconiti Praeparata and total glycosides or polysaccharides of Radix Paeoniae Alba therapy on rheumatoid arthritis in rats.

METHODThe rat models of rheumatoid arthritis of cold and dampness syndrome were treated with total alkaloids of Radix Aconiti Praeparata and total glycosides or polysaccharides of Radix Paeoniae Alba. Observed the contents of hypothalamic L-ENK, hypothalamic-END, plasmatic SP, serumal IgG, serumal cell factors (IL-1beta, TNF-alpha, IL-6, IL-2, IL-10) by radioimmunity method and ultrastructural change of synovial cell in electron microscope.

RESULTTotal alkaloids of Radix Aconiti Praeparata and total glycosides or polysaccharides of Radix Paeoniae Alba could relieve arthrocele and arthralgia and elevate the contents of L-ENK, beta-END, IL-2 and degrade the contents of SP, IgG, IL-1beta, IL-6 and inhibit abnormal secretion accentuation of synovial cell like fiber.

CONCLUSIONTotal alkaloids of Radix Aconiti Praeparata and total glycosides or polysaccharides of Radix Paeoniae Alba could be used to treat rheumatoid arthritis of cold and dampness syndrome. The mechanism of action might be that the contents of center endogenous opioid peptides had increased, the synthesis and release of SP had been inhibited, the disturbance of serumal cell factor had been adjusted, and the synthesis and secretion of serum immune globulin and abnormal secretion accentuation of synovial cell had been inhibited.

Aconitum ; chemistry ; Alkaloids ; administration & dosage ; Animals ; Arthritis, Rheumatoid ; drug therapy ; genetics ; immunology ; Cytokines ; genetics ; immunology ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; Glycosides ; administration & dosage ; Humans ; Male ; Paeonia ; chemistry ; Polysaccharides ; administration & dosage ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo determine the content of linarin in Yuye Jiedu granule.

METHODA HPLC method was developed. The chromatographic conditions are as follows Luna C18 column and acetonitrile-0.05 mol x L(-1) phosphate buffer-phosphoric acid (30:70:0.06) as mobil phase, detection wavelenth at 327 nm.

RESULTThe linear range of linarin was 0.025-0.50 microg. The average recovery was 98.7% and RSD 2.7%.

CONCLUSIONThe method is simple and accurate, with good repeatability, and can be used for determination of linarin in Yuye Jiedu granule.

Chromatography, High Pressure Liquid ; methods ; Chrysanthemum ; chemistry ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; isolation & purification ; Glycosides ; analysis ; Lonicera ; chemistry ; Plants, Medicinal ; chemistry ; Quality Control