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OBJECTIVE: To study the metabolic differences of the effective fractions of total glycosides of Jinkui Shenqi Pills in liver homogenate and blood by high performance liquid chromatography-electrospray ion trap mass spectrometry (HPLC-ESI/MSn). METHODS: The in vitro metabolism of the glycosides was studied using rat liver homogenate and the in vivo metabolism was investigated in rats. The metabolites were detected by HPLC-ESI/MS/MS. According to the molecular ion peak in negative ion mode, the molecular weight information of the compound was obtained. RESULTS: A total of 13 chemical components were detected in the rat liver homogenate after incubation for 20 min. Eight prototype components were detected in both liver homogenate and plasma while pentagalloylglucose was only found in the liver homogenate. A total of nine metabolites were detected in plasma, and only four metabolites were found in the liver, which were shared by those in plasma. CONCLUSION: The four common metabolites are produced through liver metabolism of the total glycosides. The RESULTS of this study have important implications for revealing the metabolic mechanisms of the total glycoside constituents in vitro and in vivo.
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Objective: To investigate the effects of total paeony glucoside on brain Notch signaling pathway in focal cerebral infarction rats. Methods: Stroke rats were prepared and divided into 5 groups: model group, low dosetotal peony glucoside group, medium dosetotal peony glucoside group, and high dosetotal paeony glucoside group, with 20 rats in each group. All groups received the medication for 20 days. The body weight, brain water content, cerebral infarction size, brain tissue NICD, Hes1 and Hes5 proteins and Hes1 and Hes5 mRNA expressions were measured in each group. Results: There was no significant difference in body weight before administration within these groups (P>0.05). After treatment, compared with those in the control group, the body weight significantly decreased (P<0.05); NICD, Hes1 and Hes5 significantly increased; Hes1 and Hes5mRNA significantly increased in the model group (P<0.05). Compared with those in the model group, the body weight significantly increased (P<0.05); the NICD, Hes1 and Hes5 significantly decreased; Hes1 and Hes5mRNA significantly decreased (P<0.05) in a dose-dependent manner. Conclusion: Total peony glucoside can treat focal cerebral infarction by inhibiting Notch signaling pathway in rat brain tissue.
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The aim of this study was to investigate the regulatory effect of the total glycoside extracted from leaves of Rehmannia (TLR) and Dihuangye total glycoside capsule (DTG) on intestinal microflora in diabetic nephropathy rats. Forty-eight rats were randomly divided into the control group (C), model group (M), Huangkui capsule group (0.75 g·kg-1·d-1, HK), irbesartan group (27 mg·kg-1·d-1, YX), TLR low dose group (4.3 g·kg-1·d-1, DHYL), TLR high dose group (7.2 g·kg-1·d-1, DHYH), DTG low dose group (216 mg·kg-1·d-1, JNL), DTG high dose group (360 mg·kg-1·d-1, JNH). Rat model of diabetic nephropathy was induced by intraperitoneal injection of small dose of streptozotocin (45 mg·kg-1, STZ) and feeding high-fat diet and 5% glucose drinking water. After oral administration for two weeks, the 16S rDNA sequencing method was used to study the effects of the TLR and DTG on intestinal flora in diabetic nephropathy rats. The results showed that compared with the control group, the intestinal flora of diabetic nephropathy rats had changed from phylum units to the genus units. Moreover, the proportion of lactobacilli in the intestinal bacteria of the model group was significantly decreased, and the proportion of lactobacilli in the administration group was increased, especially the YX group, TLR low dose group and DTG low dose group. The data suggest that the total glycosides of Rehmannia glutinosa improved the disorder of intestinal flora in STZ-induced diabetic nephropathy rats.
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Objective: To investigate the anti-inflammatory and analgesic activity of Eucommiae ulmoides seed total glycoside(EUG). Methods: Dimethyl benzene (DB)-induced mouse ear edema model and carrageein-induced rat paw edema model were employed for the anti-inflammatory activity experiment. The experiment for analgesic activity was done using hot plate test, photoelectricity-induced test and acetic acid-induced writhing method. Results: EUG at 110, 220 mg/kg showed an obvious inhibitory effect against DB-induced mouse ear edema volume, and at 55, 110, 220 mg/kg it showed an obvious analgesic effect against carrageein-induced rat paw edema rate 4 hours after oral administration. At 220 mg/kg EUG notably raised the pain threshold in the mice stimulated by hot plate and photoelectricity. At 110, 220 mg/kg EUG greatly reduced the number of acid-induced writhing. Conclusion: The result suggests that EUG has potential anti-inflammatory and analgesic activity.
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Objective To investigate the antitumor effects of total glycoside of Cimicifuga dahurica (TGCD) in vivo and in vitro, and further explore its mechanisms. Methods The anti-tumor activity in vitro was determined by MTT assay and the anti-tumor activity in vivo was evaluated using experimental mouse tumor (S180) model and human tumor (A549) xenografts in nude mice. After treatment, A549 cell apoptosis and morphologic change were evaluated by Annexin V/PI flow cytometry and HE staining. Results Inhibitory concentration 50% (IC50) of TGCD on A549, HepG2, HL60, Eca-109 and MDA-MB231 cells were 20.3, 27.1, 21.2, 23.4 and 32.7 ?g/mL respectively. Administration of TGCD (100 or 200 mg/kg) inhibited S180 solid tumor development in mice, the inhibition rates were 42.8% and 54.6% respectively. Administration of TGCD (100 or 200 mg/kg) inhibited A549 tumor growth with a T/C (mean value of treated group/mean value of control group) value of 58.1% and 52.2% respectively. In addition, increased percentage of apoptotic cells induced by TGCD in human A549 nude mice xenografts and the histopathological changes including cell shrinkage and condensation of chromosomes were observed. Conclusion TGCD has demonstrated antitumor bioactivity both in vitro and in vivo, which may be related to its effects of inducing apoptosis activity.
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Objective To choose the optimum extraction process for capsule of Buyang Huanwu.Methods With the orthogonal method,the main factors effecting the water-extraction process,such as the quantity of water,the time,pH and degree for decoction,were reviewed according the content of total glycoside and Astragalus Glycoside A.Results The optimum condition of water-extraction was extracting with 8 times amount of water for the first time and 4 times amount for the second and third time,1 hour for each time,pH was 12.Conclution The experimental results provide the basis for the water extraction process for capsule of Buyang Huanwu.
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The total glycoside extracted from the root of cynanchum oiophy-llum schneid ( COS ) has anticonvulsant activity. Its effect on synap-tosomal amino acid contents and brain enzyme activities in mice were studied in this paper. After the ip administration of COS, the content of GABA was increased, and that of Glu and Asp decreased, in synaptosomes of both normal and TSC induced convulsant mice, while the content of Gin remained unchanged. A fall in the activities of GDH, glutaminase and asparaginase in whole brain was seen. No changes were observed in the activities of GPT, GOT and glutamine synthetase.
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The electrical potential difference (PD) was measured across the wall of reverted intestinal sacs. The effect of the effective component of Rhubarb on transmural potential related to Na+ and glucose transport were investigated. It was found that total glucoside of Rhubarb, Emodin and Sen-nosides decreased the PD. The experimental resuilts provide new scientific basis for explaining the mechanism of Rhubarb's purgative action.