Background and purpose:Thalidomide can enhance the radiation sensitivity on tumor effectively, but the mechanism of radiosensitization is still unclear. The present study aimed to investigate whether thalidomide could enhance the radiation sensitivity on colon cancer transplanted tumor of mouse, and to investigate the underlying mechanism. Methods: We established the model of colon26 colonic carcinoma, and the mice were divided into 4 groups:Control group, the thalidomide group, the radiotherapy group and thalidomide+radiotherapy group. From the day of treatment, tumors were measured every other day. Then, the xenograft tumor growth curve was depicted. Tumor volumes were measured in different treatment groups, then, the inhibitory rates of tumor growth were calcutated. Using immunohistochemical method in to detect the expression of microvessel density (MVD) in tumor tissue. Results:The mean tumor volumes at day 22 were (4.97±1.20)cm3 (control group), (2.90±0.92)cm3 (T group), (2.66±0.88)cm3 (R group), and (1.89±0.76)cm3 (T+R group). The tumor inhibition rate in the combination group (61.9%) was signiifcantly higher than the other groups (41.7%, 46.5%, P<0.05). The radiotherapy sensitization enhancement ratio of the combined treatment group was 2.27 times than in the radiotherapy group. Thalidomide combined with radiation therapy can significantly inhibit microvessel density of tumor:The decreasing MVD of T+R group, T group and R group were respectively 46.8%, 40.7%and 37.7%, and there was statistical significance between T+R group and T group (P<0.05 ), so as between T+R group and R group. It could be found more necrotic cells in tumor of group, and there was statistical signiifcance between T+R group and control group (P<0.05). Conclusion:Thalidomide can enhance the radiosensitivity mice of colonic carcinoma, and its mechanism may be related to the inhibition of tumor angiogenesis related.

Objective To study the predictive value for adverse cardiac events (ACE) of left ventricular diastolic function measured by G-MPI. Methods Patients assessed by 2 days rest-stressed G-MPI during March 2012 to May 2013 in Beijing Hospital were collected and observed for the cumulative survival rate without ACE after G-MPI. ACE included cardiac death, non-fatal MI and late revascularization (60 d after the examination). Using quantitative gated SPECT (QGS) to get the LVEF and left ventricular peak filling rate (PFR). Using 17 segments, 5-point scoring system to get the summed stress score (SSS). Cox regression analysis was used to identify the independent predictors for ACE, and Kaplan-Meier method was used to investigate the cumulative survival rate without ACE.χ2 test was also used. Results A total of 11 patients who underwent early revascularization (within 60 d after G-MPI) were excluded and 139 patients (76 males, 63 females; average age 68.73 years) were assigned to different groups for outcome analysis, and 9 (6.5%, 9/139) patients had ACE in the whole group. Cox regression analysis showed that SSS, LVEF, PFR were the independent predictors for ACE (all P<0.05). Patients with PFR<2.1 EDV/s had a higher incidence of ACE than those with PFR≥2.1 EDV/s (14.3%(7/49) vs 2.2%(2/90), χ2=7.63, P<0.05). Kaplan-Meier survival analysis showed that the cumulative survival rate without ACE was lower in patients with PFR<2.1 EDV/s than that in patients with PFR≥2.1 EDV/s (67.7% vs 95.0%), and lower in patients with LVEF<50% than that in patients with LVEF≥50%(32.0% vs 90.8%), and also lower in patients with SSS≥8 than those with SSS<8(62.0% vs 94.7%; χ2 values: 11.92,11.27, 10.40, all P<0.01).Combining PFR with SSS and LVEF respectively, Kaplan-Meier survival analysis showed that the cumulative survival rate without ACE in patients with LVEF≥50% was higher than that in patients with LVEF<50% when PFR<2.1 EDV/s (76.7% vs 30.8%), and also higher in patients with SSS<8 than that in patients with SSS≥8 when PFR≥2.1 EDV/s (100% vs 72.2%; χ2 values: 7.14, 13.09, both P<0.01). Conclusion PFR of left ventricular diastolic function measured by G-MPI is one of the independent predictors for ACE, and it could effectively improve the predictive value for ACE if combined with LVEF and SSS.

Objective To investigate the diagnostic values of imaging techniques and endoscopy in detection the causes of post-hepatic obstructive jaundice.Methods The clinical data of 57 patients with post-hepatic obstructive jaundice were retrospectively studied.The causes of the obstruction and the findings of uhrasonography(US),computerized tomography(CT),magnetic resonance imaging(MRI)or MRIcholangiopancreatography(MRCP),endoscopic retrograde cholangiopancreatography(ERCP)and endoscopic ultrasonography(EUS)were compared.Results The causes of 57 patients with post-hepatic obstruetive jaundice were benign obstruction in 42(including stones in common bile duct in 38,ascariasis of CBD in 1,postoperative stricture in 2 and chronic pancreatitis in 1),and malignant lesions in 15(including pancreatic head carcinoma in 11 and ampullary carcinoma in 4).The diagnostic accuracy in terms of lesion location of US,CT,MRI+MRCP,ERCP and EUS were 71.93%(41/57),88.00%(22/25),94.59% (35/37),100.00%(47/47)and 96.77%(30/31),respectively;the diagnostic accuracy of cause of obstruction were 63.16%(36/57),80.00%(20/25),83.78%(31/37),100%(47/47)and 96.77% (30/31),respectively.Conclusion Benign diseases are the main causes of post-hepatic obstructive jaundice,but malignant ones are not rare.It is important to combine miscellaneous imaging techniques and endoscopy in diagnosis.

Intracytoplasmic sperm injection (ICSI) is an crucial part of assistant reproductive technology nowadays, mainly used in severe male infertility. It's a very hot question whether different origin of sperms will affect the outcome and safety of ICSI. In this article,we reviewed the present researches on the outcome and safety of ICSI by different origin of sperms, including ejaculated sperms, testicular sperms,epididymal sperms and frozen-thawed sperms.
Cryopreservation ; Ejaculation ; Epididymis ; cytology ; Female ; Fertilization ; Humans ; Infertility, Male ; therapy ; Male ; Oligospermia ; therapy ; Pregnancy ; Pregnancy Outcome ; Safety ; Sperm Injections, Intracytoplasmic ; adverse effects ; statistics & numerical data ; Spermatozoa

OBJECTIVETo explore the essence of blood deficiency syndrome and the mechanism of the effects of siwutang based on the characteristic changes in metabolic profiles of C57 mice with blood deficiency induced by compound method of bleeding, starved feeding and exhausting before and after the treatment of Siwutang.

METHODThirty C57 mice were randomly divided into three groups of 10 animals: the control group and two blood deficiency model groups without or with siwutang treatment. The animals were sacrificed after induction by compound method of bleeding,starved feeding and exhausting for 10 days and the blood, spleen, thymus and bone marrow were obtained. The metabolic profiles of serum, aqueous and lipidic extracts of thymus, spleen and bone marrow were investigated using 1H nuclear magnetic resonance spectroscopy (NMR). The NMR spectra were integrated in segments of 0.01, normalized and then analyzed using SIMCA-P software to visualize the similarities and differences in metabolic profiles between these groups.

RESULTCompared with the control group, the model group contained different levels of lactate, choline, glucose, taurine, alanine, LDL, glycerin, UFA, creatinine, acetoacetate, glutamate and beta-hydroxybutyrate (beta-HB). In the Siwutang treated group, the above-mentioned changes were reversed.

CONCLUSIONThe disorder of energy metabolism, damage of lymphocyte, and disorder of immune function were observed in blood deficiency model by NMR-based-metabonomics method, and the Siwutang can improve these effects. Metabonomics may be a valuable tool in the pharmacological evaluation of siwutang.

Animals ; Disease Models, Animal ; Drugs, Chinese Herbal ; administration & dosage ; Hemorrhage ; complications ; drug therapy ; etiology ; Humans ; Magnetic Resonance Spectroscopy ; Metabolomics ; Mice ; Random Allocation ; Serum ; chemistry

Adenocarcinoma ; diagnosis ; metabolism ; pathology ; secondary ; Brain ; metabolism ; pathology ; Brain Neoplasms ; diagnosis ; metabolism ; pathology ; secondary ; Carcinoembryonic Antigen ; metabolism ; Diagnosis, Differential ; Female ; Humans ; Keratin-7 ; metabolism ; Lung Neoplasms ; pathology ; Magnetic Resonance Imaging ; Middle Aged ; Nuclear Proteins ; metabolism ; Thyroid Nuclear Factor 1 ; Transcription Factors ; metabolism

BACKGROUNDHeterotopic cesarean scar pregnancy (HCSP) is a very rare but life-threatening entity and there is no optimal management strategy. Here we report a successfully managed case of HCSP with expectant treatment in a tertiary referral hospital.

METHODSA woman with HCSP after in vitro fertilization-embryo transfer opted for expectant treatment after five days of mild bleeding and ultrasound demonstrated cardiac activity disappearance of the scar pregnancy at 8(+4) weeks of gestation.

RESULTSThe patient had mild to moderate bleeding during close monitoring. Three days later, speculum examination revealed the gestational mass was partly protruding at the os of the cervix and it was removed with forceps without massive hemorrhage. A healthy male baby was delivered by cesarean section at gestational age of 36(+4) weeks.

CONCLUSIONSThe expectant method might be an alternative option for a HCSP with loss of cardiac activity of the scar pregnancy, when applied under supportive management and with available emergency surgery facilities.

Adult ; Embryo Transfer ; Female ; Fertilization in Vitro ; Humans ; Male ; Pregnancy ; Pregnancy Outcome ; Pregnancy, Ectopic ; diagnostic imaging ; Ultrasonography

OBJECTIVETo prepare a new Wubei fast-release tablet and study the pharmacokinetics and bioequivalence of self-prepared Wubei fast-release tablet and Wubei powder in Beagle dogs.

METHODWubei fast-release tablet was prepared with direct powder compression. Six Beagle dogs were randomly devided into two groups. They were orally administered with Wubei fast-release tablet and Wubei powder, respectively. Peimine concentrations in human plasma were determined by HPLC-MS/MS after administration. The pharmacokinetic parameters were calculated by DAS 2.0 using a non-compartmental analysis. The bioequivalence of fast-release tablet and powder was evaluated.

RESULTThe main pharmacokinetic parameters of peimine in Wubei fast-release tablet as follows: Cmax (7.4 +/- 2.3) microg x L(-1), AUC(0-t) (59.13 +/- 15.25) microg x L(-1) x h(-1), Tmax (1.5 +/- 0.0) h. The main pharmacokinetic parameters of peimine in Wubei powder as follows: Cmax (8.0 +/- 1.7) microg x L(-1), AUC(0-t) (68.78 +/- 16.27) microg x L(-1) x h(-1), Tmax (1.5 +/- 0.0) h. The 90% confidence interval of InAUC(0-t), and lnCmax of peimine in Wubei fast-release tablet were 95.4% - 104.6%, 90.9% - 109.1% of corresponding parameters of Wubei powder, respectively.

CONCLUSIONThe self-prepared Wubei fast-release tablet and Wubei powder were bioequivalent. And the self-prepared Wubei fast-release tablet had simple production process, easy administration.

Animals ; Dogs ; Drug Delivery Systems ; Drug Stability ; Drugs, Chinese Herbal ; chemistry ; metabolism ; pharmacokinetics ; Female ; Humans ; Sodium Bicarbonate ; chemistry ; Tablets ; Therapeutic Equivalency

Abstract: Our previous work revealed berberine can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, which suggested that berberine has synergistic antifungal activity with fluconazole. Preliminary SAR of berberine needs to be studied for the possibility of investigating its target and SAR, improving its drug-likeness, and exploring new scaffold. In this work, 13-substitutited benzyl berberine derivatives and N-benzyl isoquinoline analogues were synthesized and characterized by 1H NMR and MS. Their synergetic activity with fluconazole against fluconazole-resistant Candida albicans was evaluated in vitro. The 13-substitutited benzyl berberine derivatives 1a-1e exhibited comparable activity to berberine, which suggested that the introduction of functional groups to C-13 can maintain its activity. The N-benzyl isoquinolines, which were designed as analogues of berberine with its D ring opened, exhibited lower activity than berberine. However, compound 2b, 2c, and 4b showed moderate activity, which indicated that berberine may be deconstructed to new scaffold with synergistic antifungal activity with fluconazole. The results of our research may be helpful to the SAR studies on its other biological activities.
Antifungal Agents ; pharmacology ; Berberine ; pharmacology ; Candida albicans ; drug effects ; Drug Resistance, Fungal ; Drug Synergism ; Fluconazole ; pharmacology ; Isoquinolines ; pharmacology ; Microbial Sensitivity Tests

AIMTo investigate the antiepileptic effect of dizocilpine (MK-801) on amygdala kindling models in rats and the effects of its combination with general antiepileptic drugs.

METHODSTo establish amygdala kindling models in rats and observe the effect of dizocilpine on kindling models and its combination with general antiepileptic drugs (phenobarbital, valproate and nicardipine) at ineffective dose. The influence of dizocilpine on convulsions induced by semicarbazide (SCZ) in mice were also observed.

RESULTSDizocilpine (0.1-0.25 mg.kg-1, i.p.) was shown to dose-dependently inhibit amygdala kindled seizure, shorten the after discharge duration (ADD) and reduce the Racine's stage (P < 0.01). The combination of dizocilpine with phenobarbital, valproate, nicardipine at ineffective dose shortened ADD or reduced Racine's stages (P < 0.01). Dizocilpine (0.1-0.25 mg.kg-1, i.p.) significantly prolonged the latency and reduced the rate of convulsions and death in mice.

CONCLUSIONDizocilpine inhibits the seizure of the amygdala kindling and improve the antiepileptic activity of phenobarbital, valproate and nicardipine, indicating that these combination may provide a new approach for treating epilepsy.

Amygdala ; drug effects ; physiopathology ; Animals ; Anticonvulsants ; pharmacology ; therapeutic use ; Dizocilpine Maleate ; pharmacology ; therapeutic use ; Electric Stimulation ; Epilepsy ; chemically induced ; drug therapy ; Female ; Kindling, Neurologic ; drug effects ; Male ; Mice ; Nicardipine ; pharmacology ; Phenobarbital ; pharmacology ; Random Allocation ; Rats ; Rats, Wistar ; Semicarbazides ; Valproic Acid ; pharmacology