In this study, the herpetin (HPT) lyophilized liposome was prepared, and its saftey and pharmacodynamics were evaluated. HPT lyophilized liposome was prepared by thin-film ultrasonication method. The lyoprotectant was optimized using particle size and encapsulation efficiency as indexes. Then, the influencing factors of HPT lyophilized liposome were investigated. In addition, preliminary safety and therapy efficiency of HPT lyophilized liposome to liver injury induced by CCl4 in the mice. The optimal lyoprotectant was 5% sucrose plus 5% lactose and the dispersed HPT lyophilized liposomes were spherical with the mean diameter of (107.0 ± 1.2) nm and the mean encapsulation efficiency of (99.7 ± 0.50)%. The lyophilized powder was sensitive to temperature, humidity and illumination. None of hemolysis, hemagglutination and vein irritation was observed after intravenous injection of HPT lyophilized liposomes into rabbits. HPT lyophilized liposome showed obviously therapy efficiency to liver injury induced by CCl4 in the mice. The improvements of ALT, AST and ALP were better than that in HPT free drug. The obtained HPT lyophilized liposome met the standard of CP with fine particle size and encapsulation efficiency after dispersion. The HPT lyophilized liposome showed good safety and enhanced the treatment efficacy of HPT. The HPT lyophilized liposome should be stored in low temperature, sealed condition far away from light.
Animals ; Chemistry, Pharmaceutical ; Cucurbitaceae ; chemistry ; Drug Carriers ; chemistry ; Drug Evaluation, Preclinical ; Drug Stability ; Drugs, Chinese Herbal ; adverse effects ; chemistry ; pharmacokinetics ; Liposomes ; chemistry ; Male ; Mice ; Mice, Inbred ICR ; Rabbits

Objective:To investigate the mechanism of intense noise-induced cochlea cells death in guinea pig,and the effect of JNK signal transduction pathway in the procedure of cochlea cells apoptosis by intense noise-induced.Method:Thirty-two guinea pigs were randomly divided into 4 groups.The guinea pigs in the experiment groups were exposed to 4 kHz narrow band noise at 120 dB SPL for 4 h.After the noise expose for 1,4,14 days of the experiment guinea pigs,ABR of the guinea pigs on experiment and control groups were tested before put them to death.Four guinea pig's cochleas of every group were taken to paraffin section,and the rest was extracted the total cochlear's protein.Apoptosis was tested by terminal deoxynucleotidyl Transferase(TdT)-mediated deoxyuridine triphosphate(d-UTP)nick and labeling method(TUNEL).The phosphorylation of JNK and c-Jun were tested by immunohistochemistry and western blot methods.Result:Tunel-Positve cells in the Corti's,SGC and SV of experiment groups,and there have significant differences compared with the control group(P＜0.01)and Tunel-Positve cells are most in 1 d experiment group.The positive cells of P-JNK and p-e-Jun could be dectected in guinea pig's cochleas after noise exposed,but no positive cells were found in the control.Protein levels of p-JNK,and P-c-Jun were risen up and activated quickly after noise exposed,and achieved peak in 1 d,4 d,and then fallen-offs,but still maintained higher levels within 14 d.Conclusion:Intense noise causes cochlea cell lesion by inducing apoptosis to result in and JNK signal transduction pathway plays an important role in the procedure of apoptosis.

Objective To investigate CT and MRI features of extragonadal primary seminoma and improve its diagnostic accuracy.Methods The clinical and imaging features of 8 patients with extragonadal primary seminoma proved by histopathology were analyzed retrospectively.Results In 8 cases,4 cases were located in intracranial regions,4 cases in the abdominal and pelvic cavity.Detailedly,roundlike solid and cystic tumors were seen in the basal ganglia and thalamus in 2 cases.The mass density and signal were inhomogeneous in the necrotic area with slight peritumoral edema and heterogeneous enhancement,and hemorrhage and metastasis of the third ventricle were occurred inone case.Shallow lobulated tumor was occurred in the pineal region forone case,which MRI features included slightly low signal on T1 WI,equal or higher signal on T2 WI,with obvious enhancement and peripheral cystic change.There was one case in the sella area with slight high density on CT routine scan,and on MRI,slight equal signal on T1 WI,equal or higher signal on T2 WI.The pituitary stalk was involved with thickening.Tumor in suprasellar region was obviously enhanced,with a small uniformity enhancement nodule in the mouth of corpus callosum.4 cases were occurred in the abdominal and pelvic cavity,shallow lobulated tumors with varying degrees of necrosis were found on CT with infiltrating growth and slight to moderate enhancement,and swollen lymph nodes were found in retroperitoneal and mesenteric root areas.Conclusion Extragonadal primary seminoma is rare,there are some characteristic imaging findings,which contributes to improve diagnosis accuracy when combining with clinical data.

A strain of yeast capable of hydrolyzing ethyl ester of racemic Ketoprofen with high enantioselectivity has been isolated from soil after two-step enrichment. The yeast was identified as Trichosporon brassicae. The process of growth and enzyme production was investigated. The catalytic performance of the resting cell of KET4 in kinetic resolution of Ketoprofen was also investigated. When the conversion of substrate reached 41% , enantiomeric excess of the (S) - Ketoprofen produced was 91 % , indicating a high enantiomeric ratio of 45.

Objective To investigate effects of emergent percutaneous coronary intervention(EPCI)on the prognosis of patients with cardiac arrest(CA)and cardiopulmonary resuscitation after acute myocardial infarction(AMI).Methods Thirty-two patients with CA and carcliopulmonary resuscitation after AMI were retrospectively reviewed and divided into EPCI group(n=12)and eonservative treatment group(n=20).EPCI was used during or after primary eardiopulmonary resuscitation in EPCI group but not in conservative treatment group.Mortality and occurrence rates of severe arrhythmia,of heart failure,of cardiac shock and of severe bleeding in hospital were compared between the two groups.Results The mortality in hospital was 17% in EPCI group and 70% in conservative treatment group,respectively(P＜0.001).Heart failure was developed in 3 patients from EPCI group and 16 patients from conservative treatment group,respectively(P＜0.01).There was no significant difference in severe arrhythmia,cardiac shock and severe bleeding between two groups(P＞0.05).Logistic regression showed that EPCI decreased mortality but the prolonged cardiopulmonary resuscitation(＞20 min)increased the mortality.Conclusion Early EPCI might improve the prognosis of patients with cardiac arrest and cardiopulmonary resuscitation after acute myocardial infarction.

Objective To explore the protection measures of tongue of patients during nasotracheal intubation anaesthesia received prone position operation of neurosurgery. Methods Eighty cases were divided into two groups, with 40 patients in each group. The patient' s tongue of treatment group patients were protected by sodium solution absorbent gauze pressurize obturation and the control group received no treatment during the operation. Results The rate of postoperative tongue complications in the protective group was obviously lower than that in control group. Conclusions the use of sodium solution can dramatically decrease the incidence of postoperative tongue complications.

Objective To investigate the effect of glutamine (Gln) on the content of reduced glutathione hormone (GSH) and aminoglutaminic acid (Glu) of spinal cord following ischemia-reperfusion injury. Methods Totally 40 healthy adult male rabbits were randomly divided into five groups: sham-operation group (S group), ischemia-reperfusion injury group (I/R group), low-dose glutamine group (L Gln group), median-dose glutamine group (M Gln group) and high-dose glutamine group (H Gln group). After glutamine preconditioning, the model of spinal cord ischemia-reporfasion injury was established according to Zivin's method. The general status of animals was observed and the changes of Jacobs scoring were recorded in each group. Malondialdehydes (MDA), GSH, Glu and superoxide dismutase (SOD) activity in lumbar spinal cord tissues were determined using chemical colorimetry. The neuron number and deviation rate in spinal cord anterior horn were observed histopathologically. Results There was no significant difference between L Gin group and I/R group in behavior scoring, SOD activity, content of MDA and Glu, neuron number and deviation rate of spinal cord (P>0.05); however, there was a significant difference in GSH content of spinal cord (P<0.05). M Gln group and I/R group differed significantly (P<0.05) in behavior scoring, SOD activity, content of MDA, Glu, GSH, neuron number and deviation rate of spinal cord. Between H Gln group and M Gln group, there was no significant difference in behavior scoring, content of MDA and Glu, SOD activity, neuron number and aberration rate in spinal cord (P>0.05), whereas there was a significant difference in SOD activity and Giu content (P<0.05). Conclusion Pretreatment with medium-dose glutamine has a protective effect on spinal cord ischemia-reporfasion injury in rabbits, which may be related to the maintenance of GSH content, increase of SOD activity and reduction of MDA.

Acetylcholine ; Adult ; Aged ; Coronary Vasospasm ; diagnosis ; Electrocardiography ; Humans ; Middle Aged ; Sensitivity and Specificity

PURPOSE: Methylenetetrahydrofolate reductase (MTHFR) has been implicated in lung cancer risk and response to platinum-based chemotherapy in advanced non-small cell lung cancer (NSCLC). However, the results are controversial. We performed meta-analysis to investigate the effect of MTHFR C677T polymorphism on lung cancer risk and response to platinum-based chemotherapy in advanced NSCLC. MATERIALS AND METHODS: The databases of PubMed, Ovid, Wanfang and Chinese Biomedicine were searched for eligible studies. Nineteen studies on MTHFR C677T polymorphism and lung cancer risk and three articles on C677T polymorphism and response to platinum-based chemotherapy in advanced NSCLC, were identified. RESULTS: The results indicated that the allelic contrast, homozygous contrast and recessive model of the MTHFR C677T polymorphism were associated significantly with increased lung cancer risk. In the subgroup analysis, the C677T polymorphism was significantly correlated with an increased risk of NSCLC, with the exception of the recessive model. The dominant model and the variant T allele showed a significant association with lung cancer susceptibility of ever smokers. Male TT homozygote carriers had a higher susceptibility, but the allelic contrast and homozygote model had a protective effect in females. No relationship was observed for SCLC in any comparison model. In addition, MTHFR 677TT homozygote carriers had a better response to platinum-based chemotherapy in advanced NSCLC in the recessive model. CONCLUSION: The MTHFR C677T polymorphism might be a genetic marker for lung cancer risk or response to platinum-based chemotherapy in advanced NSCLC. However, our results require further verification.
Carcinoma, Non-Small-Cell Lung/*drug therapy/enzymology/genetics ; Genetic Predisposition to Disease ; Humans ; Lung Neoplasms/drug therapy/*enzymology/*genetics ; Methylenetetrahydrofolate Reductase (NADPH2)/*genetics ; Platinum/*therapeutic use ; Polymorphism, Genetic/genetics

OBJECTIVETo study the chemical constituents in rhizome of Pinellia ternata.

METHODThe constituents were isolated by silica-gel and Sephadex LH-20 chromatography. The structures were identified by spectroscopic analysis including 2D NMR techniques.

RESULTSix compounds were obtained and identified as stigmast-4-en-3-one(I), cycloartenol(II), 5alpha,8alpha-epidioxyergosta-6,22-dien-3-ol(III), beta-sitosterol-3-O-beta-D-glucoside-6'-eicosanate(IV), alpha-monpalmitin(V), beta-sitosterol(VI). The bioactive assay indicated that: compound III was active against the human tumor cell lines HCT-8, Bel-7402, BGC-823, A549, A2780.

CONCLUSIONCompounds I-IV were isolated from Pinellia ternata for the first time, compound II was the first triterpene isolated from this genus. Compound III may be one of the antitumor constituents of P. ternata.

Antineoplastic Agents, Phytogenic ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Ergosterol ; analogs & derivatives ; chemistry ; isolation & purification ; pharmacology ; Humans ; Phytosterols ; chemistry ; isolation & purification ; Pinellia ; chemistry ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry ; Stigmasterol ; analogs & derivatives ; chemistry ; isolation & purification ; Triterpenes