Androgen deprivation therapy can effectively suppress the progression of prostate cancer, but accumulating evidence for the relationship of testosterone with prostate cancer challenges the conventional wisdom. High levels of testosterone are not risk factors for prostate cancer, nor promote its development. On the contrary, a low testosterone level indicates a worse pathological stage. So far there has been no strong evidence to prove the role of testosterone in the occurrence and progression of prostate cancer. Therefore, the relationship between testosterone and prostate cancer is quite complicated and deserves further investigation.
Humans ; Male ; Prostatic Neoplasms ; Testosterone

Objective: To prepare sustained-release polylactic acid microspheres containing bupivacaine (BUP-PLA-MS) and to measure its dissolution in vitro. Methods: BUP-PLA-MS was prepared with polylactic acid (PLA) as carriers using the water-in-oil-in-water (W/O/W) emulsion solvent evaporation method. The powder particle characteristics of BUP-PLA-MS were evaluated comprehensively, and its dissolution characteristics in vitro were studied. Results: It was indicated that bupivacaine formed molecular dispersion within PLA matrix by differential thermal analysis(DTA). The in vitro release behavior of bupivacaine could be best described by Higuchi equation, with t 1/2 =22.76 h. Conclusion: Release of bupivacaine from microspheres is sustained in vitro.

Adolescent ; Child ; Female ; Humans ; Parotid Diseases ; pathology ; Parotid Gland ; pathology ; Recurrence

AIM: To quantitatively investigate transforming growth factor-β(TGF-β) and its receptors in normal bulbar conjunctival tissues and pterygium tissues. METHODS: Thirty cases of pterygium patients were randomly selected to undergo surgical resection of pterygium lesion, and the normal margin of bulbar con-junctival tissues were collected as control. Gene expres-sion was detected quantitatively by the method of quantitative real-time PCR (QRT-PCR) analysis. RESULTS: The expression level of TGF-β1 and TGF-β2 was 4.26×10-7±1.45×10-7 and 1.08×10-10±0.68×10-10 in normal bulbar conjunctival tissues, while 10.67×10-7±7.47×10-7 and 8.23×10-11±6.63×10-11 in pterygium tissues. The expression level of TGF-βRⅠand TGF-βRⅡwas 0.003015±0.0036 and 5.33×10-5±5.05×10-5in normal bulbar conjunctival tissues, while 0.000379±0.000281 and 1.002×10-5±9.04×10-6 in pterygium tissues. The expression level of TGF-β1 and TGF-β2 in pterygium was elevated (P<0.01). TGF-β1 expression level in pterygium increase 2.9±2.8 times than in normal conjunctiva. TGF-β2 expression level in pterygium increase 7.5±1.4 times than in normal conjunctiva. The expression level of TGF-βRⅠin pterygium was significantly lower (P<0.05). The expression level of TGF-βRII in pterygium was significantly lower (P<0.01). CONCLUSION: QRT-PCR is an effective method to quantitatively detect gene expression in eye. The upregulation of TGF-β1 and TGF-β2 and downregulation of their receptors expression may play an important role in the pathogenesis of pterygium, which is noteworthy further investigation in diagnosis and treatment of pterygium.real-time PCR; gene expression

Transforming growth factor-?(TGF-?) is a kind of multifunctional cytokine that regulates cell growth,differentiation,cellular senescence,apoptosis,wound healing and embryo development.As a tumor suppressor,deregulated or aberrant TGF-? signaling has been strongly implicated in human solid tumors,as well as in normal and malignant hematopoiesis.TGF? exerts an inhibitory role during the whole procedure of hematopoiesis.As a cell cycle inhibitor,it maintains cells in a quiescent state and can downregulate expression of hematopoiesis activators and oncoproteins.In malignant hematopoiesis,altered expression of coactivators or corepressors involve in TGF-?-induced transcriptional responses and loss/disruption of TGF-? target gene expression.Then malignant cells grow and differentiate abnormally.In acute promyelocytic leukemia,PML-RAR? may inhibit TGF-? signaling through inhibition of cPML and nPML.Degradation of PML-RAR? by ATRA restores this signaling pathway.

A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents ; chemical synthesis ; chemistry ; Biological Transport ; Drug Design ; Isoindoles ; chemical synthesis ; chemistry ; Serotonin Uptake Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship

BACKGROUND: Bupivacaine is widely used to alleviate post-operation pain and cure acute and chronic pain caused by inflammation or cancer.Its analgesic time cannot meet the request that drug is released slowly to prolong the analgesic time in clinic.OBJECTIVE: To detect the alleviating effect of bupivacaine polylactic acid microspheres taking high molecular polymer-polylactic acid as vector in rabbits with high performance liquid chromatograph (HPLC) and traditional skin test method.DESIGN: A completely randomized controlled animal experimental study.SETTING: School of Pharmacy, Second Military Medical University of Chinese PLAMATERIALS: Sixteen New Zealand rabbits, weighing (2.58±0.17)kg were used in this experiment.INTERVENTIONS: The experiment was carried out at the Department of pharmaceutics, School of Pharmacy, Second Military Medical University of Chinese PLA between September and November 2002. ① Animal models were established according to traditional skin test method. ② Totally 16 New Zealand rabbits were randomly divided into 2 groups: Group A and Group B, with 8 in each one. 5 mg/kg bupivacaine parenteral solution was injected subcutaneously in Group A, 5 mg/kg bupivacaine polylactic acid microspheres were implanted between subcutaneous tissue and sarcolemma in Group B. We took 1.5 mL blood from ear border vein at 5, 10, 20, 30,45 minutes, 1, 2, 3, 4, 6, 8, 12 and 24 hours after administration of bupivacaine parenteral solution respectively in Group A and another 1.5 mL at 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 24, 3 6, 48 and 60 hours after admistration of bupivacaine microsphere powder for index detection. ③ HPLC method was used to detect the concentration and releasing effect of bupivacaine in blood serum.MAIN OUTCOME MEASURES: Concentration change of bupivacaine in blood serum and efficacy diameter of local anesthetic.RESULTS:All the 16 rabbits entered the stage of result analysis. ①Change of bupivacaine concentration: Plasma bupivacaine concentration in Group A reached the peaked quickly after subutaneous injection with the high concentration of 2.466 4 mg/L, then declined quickly. Plasma bupivacaine concentration in Group B was relative stable, reached a peak much slowly after subcutaneous implantation, with peak concentration of 0.778 1 mg/L, and the plasma bupivacaine concentration maintained a relative low level, the mean retention time was obviously prolonged (P ＜ 0.05).② Alleviating effect of bupivacaine: The analgesic time was significantly longer in the bupivacaine microsphere group than in the bupivacaine parenteral solution group (P ＜ 0.05).CONCLUSION:Bupivacaine polylactic acid microspheres have sustained release effects in rabbits.

The effect of pioglitazone on mRNA expression of advanced glycosylation end products(AGE) receptor(RAGE)was observed in renal cortex of streptozotocin-induced diabetic rats.The RAGE mRNA expression was significantly raised in diabetic control group as compared with that in the normal control group(P

Objective To determine the correlation between the expression of interleukin 8 (IL 8) and vascularity in human gastric carcinoma speciemens,and to provide a possible new clinical way for anti angiogenesis of tumor . Methods IL 8 mRNA expression was examined with reverse transcription polymerase chain reaction (RT PCR).IL 8 protein secretion level and its specific expression were determined by enzyme linked immunosorbent assay (ELISA).The number of blood vessels in the gastric carcinoma was determined by antibody against factor Ⅷ associated antigen and immunohistochemical analysis. Results Most of the tumors (26/29,89.7%) and metastatic lymph nodes (17/20,85%) expressed IL 8 at higher levels than that in corresponding normal mucosa of resection end of stomach and negative metastatic lymph node.The expression of IL 8 protein and IL 8 mRNA were at the same level.The level of IL 8 mRNA in the gastric carcinoma tissue correlated strongly and positively with vascularization (P= 0.001).Conclusions There is a positive correlation between IL 8 mRNA expression and the vascularity of gastric carcinoma.IL 8 produced by tumor cells may up regulate the microvascularization in the gastric cancer, and enhance the growth,spreading and lymph node metastasis in human gastric carcinoma.So decreasing the IL 8 expression might inhibit the microvascularization,growth and metastasis of gastric cancer.

Objective To observe the changes of rotation behavior and tyrosine hydroxylase immunopositive neurons and investigate how Mrh-aFGF affects them in substantia nigra of Parkinson disease rats. Methods After building a rat model of Parkinson disease by injecting 6-OHDA into substantia nigra and ventral tegmental area,we used Mrh-aFGF to intervene rats by lateral ventricle injection to observe how behavior of rats induced by apomorphine and tyrosine hydroxylase immunopositive neurons in substantia nigra of rats changes,then quantitatively analyzed the change of tyrosine hydroxylase immunopositive neurons. Results Rotation behavior was not found in control group,otherwise,actuation time was shorted,time length was prolonged,and average velocity of rotation was accelerated in Parkinson disease rats(P