To study the in situ intestinal absorption kinetics and compatibility influence of peimine and peiminine in rats, the absorption of peimine and peiminine in small intestine (duodenum, jejunum and ileum) and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC-ELSD. Perfusion rate, pH, concentration of drug, gender and bile duct ligation can significantly affect the absorption of peimine and peiminine, the Ka, and Papp values in the condition of pH 6.8 and pH 7.4 had significant difference (P<0.01), as drug concentration irlcreased, the absorption parameters of peimine and peiminine decreased, Ka and Papp between low concentrations and middle concentrations was significant difference (P<0.01). Verapamil can not affect Ka and Papp of peimine and peiminine which are in the extract (P> 0.05). Bitter almonds and licorice can significantly reduce the absorption of peimine and peiminine with the usual dose (P<0.01), extracted separately and together had no significant difference on Ka and Papp (P> 0.05). Experimental results show that the absorption features of peimine and peiminine are basically the same, both of them could be absorbed at all segments of the intestine in rats and had no special absorption window, and with significant differences between male and female individuals. The absorption of peimine and peiminine complies with the active transport and facilitated diffusion in the general intestinal segments. Bitter almond and licorice can reduce the intestinal absorption rate ofpeimine and peiminine.
Animals ; Cevanes ; administration & dosage ; isolation & purification ; pharmacokinetics ; Colon ; metabolism ; Drugs, Chinese Herbal ; isolation & purification ; pharmacology ; Female ; Fritillaria ; chemistry ; Glycyrrhiza ; chemistry ; Glycyrrhizic Acid ; isolation & purification ; pharmacology ; Intestinal Absorption ; drug effects ; Intestine, Small ; metabolism ; Male ; Perfusion ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Prunus dulcis ; chemistry ; Rats ; Rats, Sprague-Dawley ; Sex Factors

OBJECTIVETo introduce different surgical treatment for gyncomastia at different grades.

METHODS37 cases with gynecomastia were divided into three grades as: grade I with fat as main tissue, grade II with proliferated fibro-gland as main tissue, grade III with big and ptosis breasts and sagging skin. Different surgical methods were chosen according to the different grades of gyncomastia. These include liposuction, subareolar fibroglandular tissue removing, combined technique of the two methods, and breasts resection with free transplantation of nipple-areola complex.

RESULTSAll patients were satisfied for the appearance of post-operative flat male chest. Complications, such as scar, numbness of nipple and areola were acceptable for them.

CONCLUSIONSDifferent surgical methods should be chosen for the gynecomastia at different grades. It can improve both the physical and psychological problems for patients.

Adolescent ; Gynecomastia ; classification ; surgery ; Humans ; Lipectomy ; Male ; Mammaplasty ; methods ; Nipples ; transplantation ; Retrospective Studies

BACKGROUND:Pathogenesis of Parkinson’s disease is not completely understood, and there is yet no effective therapy that can prevent the neurodegenerative process of the disease fundamentaly. OBJECTIVE:To explore the effects of pituitary adenylate cyclase-activating polypeptide (PACAP) on lactacystin-induced Parkinson’s disease dopaminergic PC12 cel apoptosis and its molecular mechanism. METHODS: Under induction by nerve growth factors, PC12 cels differentiated into dopaminergic neurons, and then were treated with different concentrations of lactacystin for different time. When the cel survival rate was about 50%,the concentration and action time oflactacystin were selected to establish cel models of Parkinson’s disease. In the study, there were control group, lactacystin group, PACAP1-27 group (intervention group 1) and PACAP1-27+PACAP6-27 co-intervention group (intervention group 2). Changes of cel morphology were observed under inverted microscope; cel viability was detected with MTT method; the expression of endoplasmic reticulum stress specific protein caspase-12 was detected by western blot. Then the action of PACAP1-27 and PACAP6-27 to the cytoxicity of lactacystin was observed. RESULTS AND CONCLUSION: With different concentrations and action time of lactacystin, the viability of PC12 cels presented a concentration- and time-dependent decline. When the lactacystin at 20μmol/L acted for 24 hours, the cel viability was declined by about 50%. Under same conditions of lactacystin concentration and action time (20 μmol/L, 24 hours), the cels in the lactacystin group appeared to have damaged changes, declined cel viability, and increased caspase-12 activity in comparison with the control group (P< 0.01). Compared with the lactacystin group, the cel damage was relieved and cel viability was increased significantly in the intervention group 1 as wel as the expression of caspase-12 was decreased (P < 0.01). Experimental findings in the intervention group 2 were similar to those in the lactacystin group. These results suggest that lactacystin, an ubiquitin proteasome inhibitor, can lead to cel damage; PACAP1-27 plays a protective role by regulating the above-mentioned signal pathway. As one PACAP1-27 receptor antagonist, PACAP6-27 can attenuate this effect of PACAP1-27.

Objective To evaluate the accuracy of the delay time after contrast media administration in intracranial CTA study during brain CT perfusion study.Methods 14 patients with history of episodes of typical transient ischemic attack(TIA)or ischemic cerebrovascular disease were included.After cerebral CT perfusion study,the CTA study of Willis circle was performed with the delay time by measuring the different value between the time to peak(TTP)and beginning scan time of anterior cerebral artery in CT perfusion.The quality of the CTA images were evaluated.Results All the CTA images of the Willis circle were satisfactory.Conclusion It's a satisfactory method based on successful cerebral CTA study to take the time to peak in CT perfusion as the delay time.

Objective:To study age distribution of attention deficit hyperactivity disorder(ADHD) comorbidities in a relatively large sample,and exam the hypothesis of bad prognosis for ADHD.Methods:Using semi-structured clinical diagnosis interview scale,we investigated comorbidities of 1 002 ADHD children and adolescents from psychiatric out-patient clinic,and compared comorbidity frequency in 4 age groups.Results:The comorbidity frequencies of disruptive behavior disorder(DBD),mood disorder,tics disorder and learning disorder(LD) in different age groups of ADHD patients differed significantly(P

BACKGROUND:Endogenous stem cells have no repair effects on the process of disc degeneration. Authors assumed that this maybe associate with abnormal effects of related etiological factor, resulting in an inhibitory effect on the function of nucleus pulposus-derived mesenchymal stem cells. OBJECTIVE:To investigate the effects of inflammatory cytokine interleukin-1βon biological characteristics of nucleus pulposus-derived mesenchymal stem cells of rats. METHODS:Lumbar spinal nucleus pulposus was obtained from 3-month-old male Sprague-Dawley rats. Nucleus pulposus-derived mesenchymal stem cells were isolated and cultured with col agenase and sequential trypsin digestion. The expression of CD24, CD34, CD45, CD90 and CD105 was detected using flow cytometry. Stem cellgene SOX2 and Nanog expression was measured using RT-PCR. Adipogenic, osteogenic and chondrogenic abilities of nucleus pulposus-derived mesenchymal stem cells were observed. The apoptotic rate of interleukin-1β-treated nucleus pulposus-derived mesenchymal stem cells was detected using flow cytometry. Fluorescent quantitative PCR was used to measure the expression of SOX9, proteoglycan, type II col agenase and caspase-3 gene after nucleus pulposus-derived mesenchymal stem cells were treated with interleukin-1β.

Objective The inhibitor of differentiation 3 (Id3) is an important transcriptional regulation factor, which participates in tumorigenesis, cell proliferation, and cell apoptosis.β-catenin, as a central molecule of the Wnt signaling pathway, is critical for tumor development.This study aimed to evaluate the expressions of these two molecules and the regulatory effect of Id3 on β-catenin in different tumor cells.Methods Total RNA was extracted using the Trizol Reagent.The relative mRNA expression levels of Id3 and β-catenin in tumor cells were detected by quantitative real-timePCR(qRT-PCR).The recombinant eukaryotic expression vector pEGFP/Id3 with the human Id3 gene was transfected into A549, A549/ DDP and SW-480 cells using the non-liposome-mediated method.The protein expressions of Id3 and β-catenin were determined by Western blot.Results The expression of Id3 was significantly lower in the colorectal cancer cell lines SW-480 and HT-29 than in A549 and other tumor cells (P<0.05), but remarkably higher in nasopharyngeal carcinoma CNE and 5-8F cells than in other tumor cells (P<0.05).The expression of β-catenin was the highest in SW-480in comparison withother malignant tumor cells(P<0.05), and the second highest was in gastric cancer AGS and colorectal cancer HT-29 cell lines, but low in H446, A549, SPC-A-1, A549/DDP, and SK-MES-1 cell lines and extremely low or almost absent in CNE and 5-8F cells (P<0.05).After transfected with pEGFP/Id3, the cells showed a decreased volume, wrinkled membrane and absent refraction under the fluorescence microscope, which, however, were not observed in most of the cells transfected with the empty vector pEGFP.Compared with the control, the Id3/pEGFP group showed remarkably increased expressions of Id3 mRNA in the A549, A549/DDI, and SW-480 cells (1.24±0.12 vs 193.12±2.80, 1.09±0.11 vs 188.30±2.60, and 0.92±0.29 vs 19.08±0.59, P<0.01), and the expression of β-catenin was significantly down-regulated in the transfected SW-480 cells with an overexpression of Id3 (0.98±0.05 vs 0.32±0.03, P<0.01), but exhibited no statistically significant differences from those in the transfected A549 and A549/DDP cells (0.98±0.07 vs 1.04±0.08 and 0.98±0.05 vs 0.32±0.03, P>0.05).Western blot showed the same results.Conclusion The expression levels of Id3 and β-catenin vary in different tumor cell lines.Anabnormally high level of β-catenin is an important risk factor for colorectal cancer, and the down-regulatedexpression of β-catenin after eogenous transfection of Id3 may provide some new ideas for target gene therapies of colorectal cancer.

Ferulic acid (FA), a natural product of phenylpropanoids containing phenolic hydroxyl groups, has a wide range of pharmacological activities and some therapeutic effect on Alzheimer's disease (AD).Using FA as the raw material, the ferulic acid carbamate aniline derivatives were first synthesized by 4-step esterification reaction, splicing carbamate active functional groups, hydrolysis reaction and amide condensation.These FA derivatives were evaluated for in vitro cholinesterase inhibition activity by the Ellman method.A total of 15 novel FA derivatives were designed and synthesized, and their structures were confirmed by 1H NMR, 13C NMR and ESI-MS.Cholinesterase activity tests showed that compounds 5c, 5f, 5j, 5g, 5m possessed good acetylcholinesterase inhibition activity.Except for 5l, 5m, almost all compounds have inhibition activity on butyrylcholinesterase, which is much higher than that on acetylcholinesterase.In conclusion, compounds 5c, 5f, 5j and 5g can be used as potential anti-AD inhibitors targeting cholinesterase..

Objective To improve the diagnosis accuracy and treatment quality of juxtaglomerular cell tumor.Methods The clinical data of 2 female patients(20 and 36 years,respectively)with juxtaglo- merular cell tumor were presented and discussed in combination with review of the literature,including the onset characteristics,imaging features,treatment,pathology and prognosis.Case 1 presented with hyperten- sion of 180/110 mm Hg.The laboratory examinations showed that in decubitus and standing position,the plasma rennin activity(PRA)was 3.2?g - L~(-1)?h~(-1)and 36.5?g?L~(-1)?h~(-1);angiotensinⅡwas 54.3 pg/ml and 183.5 pg/ml;aldosterone was 193.5 prnol/L and 489.4 pmol/L,respectively;serum kalium was 2.6 mmol/L.Case 2 presented with hypertension of 210/120 mm Hg.The laboratory examination results were as follows:in decubitus and standing position,PRA was 4.3?g?L~(-1)?h~(-1)and 37.0?g?L~(-1)?h~(-1);angio- teusinⅡwas 55.6 pg/ml and 200.4 pg/ml;aldosterone was 162.4 pmol/L and 506.3 pmol/L,respectively; serum kalium was 3.0 mmol/L.On CT scan,both cases had renal tumor,with the diameter of 3.0 cm and 3. 5 cm,respectively.Results Case 1 underwent laparoscopic partial nephrectomy.Case 2 who had artery stricture and severe functional injure of the right kidney underwent laparoscopic right nephrectomy.The oper- ative time was 3.0 h and 2.0 h,and the blood loss was 175 ml and 112 ml,respectively.There was no mor- tality or postoperative complication.In 1 or 2 postoperative weeks,Case 1 had blood pressure(BP)of 120/70 mm Hg;in deeubitus and standing position,PRA was 1.5?g ~ L~(-1)?b~(-1)and 12.8?g?L~(-1)?h~(-1);angio- tensinⅡwas 30.6 pg/ml and 97.5 pg/ml;aldosterone was 78.5 pmol/L and 192.2 pmol/L,respectively ;se- rum kalium was 4.2 mmol/L.Case 2 had BP of 125/75 mm Hg;in decubitus and standing position,PRA was 1.6?g.L~(-1)?h~(-1)and 12.3?g.L~(-1)?h(-1);angiotensinⅡwas 34.3 pg/ml and 83.5 pg/ml;aldoste- rone was 62.6 pmol/L and 292.5 pmol/L,respectively;serum kalium was 4.8 mmol/L.Pathology showed that the juxtaglomerular cell tumor had intact envelop.Light microscopically,the tumor was very much like a hemangiopericytoma,showing active proliferation and nuclear atypia.The immunohistochemical staining showed positive Vimentin,CD_(34)expression,and negative MSA,EMA,Bcl-2,?-SmA,AG/AG3,34?En, CD_(117),CD_(31),Iv glue,Ki-G~-(＜2%)expression.Ultrastructural changes of the nuclei and some organelles in the cytoplasm were observed under electron microscope.The conspicuous ultrastructural feature was the pres- ence of secretion granules and rhomboid-shaped,crystal-like structures in the dilated cisternae of rough endo- plasmic reticulum and vesicles of Golgi complex.The follow-up was 14 and 6 months,respectively;the renal function was normal and no tumor recurrence was found.Conelusions Juxtaglomerular cell tumor is a rare tumor which can produce renin.It is characterized by severe hypertension and low serum potassium.La- boratory examination results are helpful for the diagnosis:PRA and angiotensinⅡincrease obviously ;aldoste- rone is 1-10 times more than normal;serum kalium is commonly between 2.1-3.5 mmol/L.The definite diagnosis depends on clinical presentations,immunohistochemistry,light and electron microscopic examina- tions.Laparoscopie operation is the first choice of surgical treatment.

OBJECTIVETo study the effect of solid dispersion technology and inclusion technology on dissolution performance of Pulsatillae total saponins, and preliminarily investigate its mechanism.

METHODThe solid dispersion of Pulsatillae total saponins-PEG 4000 was prepared by the melting method. The inclusion compound of Pulsatillae total saponins-hydroxypropyl-beta-cyclodextrin ( HP-beta-CD) was prepared by the freeze-drying method. The properties of solid dispersion and inclusion compound were identified by using IR, DSC and NMR. And the dissolution of solid dispersion and inclusion compound were also determined by the small glass method.

RESULTIR, DSC and NMR results showed the formation of solid dispersion and inclusion compound. In terms of the dissolution, the inclusion compound ranked first, which was followed by solid dispersion and bulk pharmaceutical chemicals.

CONCLUSIONThe inclusion technology could significantly increase the dissolution of Pulsatillae total saponins, whereas the solid dispersion showed no notable solubilization effect.

Drug Compounding ; methods ; Drugs, Chinese Herbal ; chemistry ; Saponins ; chemistry ; Solubility ; Spectrophotometry, Infrared