ABSTRACT
In vitro and in vivo antibacterial activities on the Staphylococcus aureus and Escherichia coli of the amorphous cefuroxime axetil (CFA) ultrafine particles prepared by HGAP method were investigated in this paper. The conventional sprayed CFA particles were studied as the control group. XRD, SEM, BET tests were performed to investigate the morphology changes of the samples before and after sterile. The in vitro dissolution test, minimal inhibitory concentrations (MIC) and the in vivo experiment on mice were explored. The results demonstrated that: (i) The structure, morphology and amorphous form of the particles could be affected during steam sterile process; (ii) CFA particles with different morphologies showed varied antibacterial activities; and (iii) the in vitro and in vivo antibacterial activities of the ultrafine particles prepared by HGAP is markedly stronger than that of the conventional sprayed amorphous particles.
Subject(s)
Anti-Bacterial Agents/analysis , Anti-Bacterial Agents/therapeutic use , Cefuroxime/analogs & derivatives , Escherichia coli Infections/drug therapy , Staphylococcal Infections/drug therapy , Animals , Anti-Bacterial Agents/pharmacology , Cefuroxime/analysis , Cefuroxime/pharmacology , Cefuroxime/therapeutic use , Chemical Precipitation , Drug Compounding , Escherichia coli/drug effects , Mice , Mice, Inbred ICR , Particle Size , Solubility , Staphylococcus aureus/drug effects , X-Ray DiffractionABSTRACT
OBJECTIVE: To investigate the changes of the activity of both protein kinase A and C and the mechanisms of antipyretic action of Guizhi decoction. METHOD: The fever responses were observed after combination injection of H-89 (a selective inhibitor of PKA) and calphostin C (a selective inhibitor of PKC), and oral pretreatment of Guizhi decoction in fever rats induced by an intra-cerebroventricular (icv) injection of an EP3 agonist, and both PKA and PKC activity in hypothalamus were measured in rats pretreated with Guizhi decoction and vehicle using isotopic tracing assay. RESULT: The rise in rat body temperature was inhibited by H-89, Calphostin C, and Guizhi decoction, moreover, pretreatment with Guizhi decoction reduced PKA activity obviously. PKC activity in model rats exhibited a tendency to drop compared with that of control group, Oral administration of Guizhi decoction in large dose inhibited the response significantly, while the low dose of Guzhi decoction has no effect on PKC. CONCLUSION: Both PKA and PKC may participate in the mechanism of fever induction by EP3 agonist. The decrease of PKA and PKC may contribute to the antipyretic action of Guizhi decoction, some isoenzyme of PKC may play a role in the fever production.
Subject(s)
Cyclic AMP-Dependent Protein Kinases/metabolism , Drugs, Chinese Herbal/pharmacology , Fever/enzymology , Hypothalamus/enzymology , Protein Kinase C/metabolism , Analgesics, Non-Narcotic/pharmacology , Animals , Cinnamomum aromaticum/chemistry , Dinoprostone/analogs & derivatives , Dose-Response Relationship, Drug , Drug Combinations , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/isolation & purification , Fever/chemically induced , Male , Plants, Medicinal/chemistry , Random Allocation , Rats , Rats, Wistar , Receptors, Prostaglandin E/agonists , Receptors, Prostaglandin E, EP3 SubtypeABSTRACT
OBJECTIVE: To investigate the effect of Guizhi Tang and its active components on the fever induced by EP3 receptor agonist sulprostone in rats. METHOD: The rise in body temperature evoked by a LCV(lateral cerebroventricle)-injection of sulprostone was compared with that of sulprostone induced-fever rats pretreated with Guizgi Tang and its active compounds, cinnamaldehyde, cinnamic acid and total glucosides of paeony. RESULT: Pretreatments with Guizhi Tang and cinnamaldehyde inhibited the rise in body temperature induced by sulprostone, while cinnamic acid tended to augment the fever. The sulprostone-induced fever was blocked by an ip pretreatment of total glucosides of paeony even below the basement. CONCLUSION: Present data suggest that interruption with the down-stream events of EP3 receptor may contribute to the antipyretic action of Guizhi Tang, cinnamaldehyde and the total glucosides of paeony, while cinnamic acid may have no such effect.
