To analyze the specific mechanism of Jinxueyuan granules, the relationship between the Jinxueyuan granules increased the saliva secretion of xerostomia model SD rats and excitement of receptors were studied in this experiment. In the study, three groups of xerostomia model rats were successfully established by using M-receptor blockers-4-diphenyl-acetoxy-N-methyl-piperidine (4-DAMP) and atropine, or adrenergic receptor blocker phentolamine; after the modeling, the medicine Jinxueyuan granules were gavaged. According to the clinical dose of Jinxueyuan granules and SD rats body surface area, the rats in atropine group were divided three dose groups respectively, namely low, medium and high dose of Jinxueyuan granules groups. The 4-DAMP group and phentolamine group were gavaged medium dose of Jinxueyuan granules. And the amount of salivary secretion for 150 minutes in all groups continuously were measured, and the effect of Jinxueyuan granules increased salivation and the relationship between characteristics and the receptors were observed; and submandibular gland tissue of the rats was isolated, then the effect of Jinxueyuan Granules for expression of the water channel protein aquaporin-5 (AQP5) in submandibular gland cells was analyzed by the Western blot technology. It was found that the saliva secretion of Jinxueyuan Granules groups was increased significantly, and compared with the saline control group, phentolamine group, 4-DAMP group and atropine group, difference was significant, P < 0.05. There was no significant difference between the low-dose of Jinxueyuan granules group and the saline group, but the medium dose of Jinxueyuan granules group had a significant difference, compared with the saline group (P < 0.05). In the time distribution of increasing saliva secretion, there was a significant difference between the saline and Jinxueyuan granules group in the saliva secretion (P < 0.05). After administration of Jinxueyuan granules, the expression of AQP5 protein in the submandibular gland cells expressing of treatment groups was increased, and compared with the blocker groups, there was a significant difference, P < 0.05. Except the atropine group, there was no significant difference in Jinxueyuan granules relieving the inhibition induced by blocks in phentolamine group and 4-DAMP group, compared with the saline group. Compared the AQP5 expression in three blockers groups, there was no significant difference in the efficacy of Jinxueyuan granules between phentolamine group and 4-DAMP group; but there was a significant difference between the atropine group and other groups (P < 0.05). Therefore, it was considered that the mechanism of Jinxueyuan granules increasing saliva secretion (effectiveness of nourishing Yin and generating body fluid ) possibly through the pathway mediated by muscarinic M receptor, especially M3 receptor, or adrenergic receptor, and increased expression of salivary gland AQP5 membrane, and then stimulate saliva production.
Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; Humans ; Male ; Rats ; Saliva ; secretion ; Salivary Glands ; drug effects ; secretion ; Xerostomia ; drug therapy ; metabolism

Humans ; Hypophosphatemia ; blood ; complications ; Neoplasms ; blood ; complications ; Osteomalacia ; blood ; diagnosis ; drug therapy ; etiology ; surgery ; Phosphates ; blood

Diabetes Insipidus, Neurogenic ; diagnosis ; metabolism ; Humans ; Pituitary Neoplasms ; diagnosis ; secondary

To explore new agents of gamma-aminobutyric acid (GABA) derivatives with more potent antiepileptic activity, a series of 4-(2-acetoxybenzoylamino) butyramide derivatives were designed and synthesized. All of the novel compounds (5a-51) were synthesized from GABA as starting material, and their structures were confirmed with IR, 1H NMR, EI-MS and elemental analysis. Preliminary pharmacological test in vitro showed that all target compounds displayed strong antiepileptic activities and were worth for further study. The structure-activity relationship of 4-(2-acetoxybenzoylamino) butyramide derivatives was also discussed preliminarily.

Adult ; Female ; Humans ; Insecticides ; poisoning ; Ivermectin ; analogs & derivatives ; poisoning ; Male ; Middle Aged

Objective To explore the risk factors of hyperbilirubinemia in late preterm infants. Methods Clinical data of 211 cases of late preterm infants with hyperbilirubinemia and 246 cases of late preterm infants without hyperbilirubinemia were retro-spectively analyzed between 2011 and 2012. The risk factors of hyperbilirubinemia were filtered. Results Twenty-seven cases of late premature infants with hyperbilirubinemia were severe. Hospital stay less than 3 days, birth asphyxia history, small for gestatio-nal age, head hematoma, delivery injury, hypoalbuminemia, polycythemia, infection, hemolytic disease, feeding intolerance, and fe-tal excretion delay were associated with hyperbilirubinemia (P<0.05). Rural origin, pregnancy-induced hypertension syndrome and premature rupture of membrane were also associated with hyperbilirubinemia (P<0.05). Multivariate logistic regression analysis showed the history of birth asphyxia , fetal excretion delay, hypoalbuminemia, pregnancy-induced hypertension syndrome were risk factors of hyperbilirubinemia in late preterm infants (OR=2.35-4.05). Pregnancy-induced hypertension syndrome and hemolytic dis-ease were risk factors of severe hyperbilirubinemia in late preterm infants (OR=5.74, 73.64). Conclusions Neonatal asphyxia, fetal excretion delay, hypoalbuminemia and pregnancy-induced hypertension syndrome are risk factors of hyperbilirubinemia in late pre-term infants. Strengthening the management of pregnancy-induced hypertension syndrome and the treatment of newborn hemolytic disease can reduce the occurrence of severe hyperbilirubinemia in late preterm infants.

α-Hederagenin (H), derived from Hedera nepalensis var.sinensis, is a pentacyclic oleane-type triterpenoid that exhibits clear cytotoxicity to different tumor cell lines.In this study,a series of novel C-28 derivatives of hederagenin (H) were designed and synthesized in attempt to develop potent tumor resistance reverse activities agents. Previous research showed that H6 displayed robust reverse activity for paclitaxel resistance in KBV cells. Importantly, Co-treatment of paclitaxel with H6 significantly reduced the tumor weight to 42%. Pleasingly, H6 enhanced the efficacy of paclitaxel against KBV cancer cell-derived xenograft tumors in nude mice.Mechanism studies had found that H6 activated permeability glycoprotein(P-gp)ATPase,reduced intracellular ATP levels and inhibited efflux of P-gp substrates,thus enhancing the antitumor activity of paclitaxel on KBV cells.Molecular docking analysis of homology P-gp and H6 then conducted using the Surflex-Dock module.H6 showed a high binding affinity docking score with a total score of 5.4148,much higher than that of H(0.1414).The nov-el C-28 derivatives of H was synthesized from H6 via three-step reaction. The reversal activity of all synthesized H derivatives were tested using the MTT assay.The results showed that the derivatives of nitrogen groups at C-28 displayed same even potent activity than parent compound H6.In addition,its underlying mechanism of action and in vivo activity are in explore.

The expressions of StAR (steroidogenic acute regulatory protein) mRNA in testes from 7,14,23 and 37 day-old piglets were studied by tissue in situ hybridization. The results indicated that in the testes of piglets, StARmRNA was expressed in Leydig cells of pig testes. The expression level of StARmRNA was lower in 7 days piglets but higher in 14,23,37 days. The results indicated that StAR gene played an important role in steroid biosynthesis.

Objective To develop a multiplex PCR-based reverse line blot(mPCR/RLB) hybridization assay to detect,simultaneously,seven genes encoding AR-erm(A/TR),erm(B),mef(A/ E),tet(M),tet(O),aphA-3,aad-6 and two AR-related genes,int-Tn and mreA in group B streptococcus.Methods Nine pairs of specific primers and Oligonucleotide probes targeting erm(A/TR), erm(B),mef(A/E),tet(M),tet(O),aphA-3,aad-6 int-Tn and mreA respectively were modified according to former studies or designed in this study.The primers and probes were labeled with biotin and amino,respectively.The nine genes were amplified simultaneously in the same tube.PCR product hybridized with the probes labeled in the BiodyneC nylon membrane to detect the nine genes.To detect the sensitivity and specificity of the method developed,PCR with single pair of primer targeting each gene were tested in 318 isolates tested and the results were compared with the one abtained by RLB.Results The nine resistance-related genes could be successfully detected by mPCR/RLB assay developed in this study.Based on sequencing,21 of 22 isolates with mef had mef(E)and eight of 353 with int-Tn had an atypical sequence.Except for the above 29 genes,all the others corresponded well with the results obtained by single pair primer PCR.Conclusion The mPCR/RLB assay developed in this study is simple,rapid and suitable for surveillance of antibiotic resistance in GBS.