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

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

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.

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.

Objective:To establish the test method for histamine-like substances in pirarubicin. Methods:According to the meth-od described in the appendix of Chinese Pharmacopoeia (2010 edition), the test for histamine-like substances was carried out. Re-sults:The test for histamine-like substances had no interference under the condition with pirarubicin concentration of 0. 01mg·ml-1 . The established test method for histamine-like substances in pirarubicin was applied in 10 samples, and the results were accordant with those of the test method for depressor substances. Conclusion:The test method for histamine-like substances in pirarubicin is feasible with the limit of 1 μg·mg-1 .

OBJECTIVE: To determine the normal range of the 33 elements (Li, Be, B, Mg, Al, Ca, Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Zn, Ga, As, Se, Rb, Sr, Zr, Mo, Ag, Cd, Sb, Cs, Ba Au, Hg, Tl, Pb, Th and U) in human whole blood of general population in Hunan province. METHODS: Blood samples were analyzed by inductively coupled plasma-mass spectrometry (ICP-MS) to determine the normal range. The influences of district, gender and age to the element content in blood samples were also observed. RESULTS: The normal range of 33 elements in blood samples from general population in Hunan province were obtained. Gender was shown to statistically influence the concentrations of B, Mg, Ca, Ti, Mn, Fe, Co, Cu, Zn, As, Se, Rb, Sr, Ag, Cd, Cs, Hg and Pb (P < 0.05), while age was shown to influence the concentrations of Co, Ni, Cs and Hg in women (P < 0.05) as well as Cu, Se and Hg in men (P < 0.05). CONCLUSION Although there are variables in different districts, the normal ranges of trace element in blood of the four cities in Hunan province are established.
Age Factors ; Asian People/ethnology* ; China ; Female ; Humans ; Male ; Mass Spectrometry/methods* ; Reference Standards ; Reference Values ; Residence Characteristics ; Sex Factors ; Trace Elements/blood*

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.