OBJECTIVETo study the selective dilatation effects of iptakalim (Ipt) on basilar and pulmonary arterioles, and endothelial cell function of these arterioles in hypoxic rats.

METHODSSD male rats were divided into 2 groups:control and hypoxic group fed in normobaric hypoxic environment (O2 7.8%, 8 h). Arteriole rings about (204 + 5) pm were isolated and the tension of hypoxic arterioles pre-contracted by 6 nmol/L endothelin-1 (ET-1) was observed with wire myograph system model (DMT 610 m). The relaxing response of hypoxic arterioles induced by different concentration of Ipt were detected and endothelial activity was also tested by acetylcholine.

RESULTS10(5) mol/L acetylcholine (ACh)-mediated vasodilatation of basilar and pulmonary arterioles was greatly reduced in the hypoxic group than those in control group (P < 0.05). Compared with normal group, a novel ATP-sensitive potassium channel opener Ipt at the concentration ranging from 10(-11) mol/L to 10(3) mol/L, caused stronger dose dependent vasodilatation on hypoxic pulmonary arterioles, and there was no significant difference between control and hypoxic basilar arterioles.

CONCLUSIONThe endothelial function of basilar and pulmonary arterioles was damaged under hypoxic state, and Ipt selectively increased dilatation effects on hypoxic pulmonary arterioles, but not on hypoxic basilar arterioles which could improve high altitude pulmonary edema pathological state and be the novel drug in the treatment of pulmonary hypertension.

Acetylcholine ; pharmacology ; Altitude ; Altitude Sickness ; physiopathology ; Animals ; Arterioles ; drug effects ; Dilatation ; Endothelin-1 ; pharmacology ; Hypoxia ; KATP Channels ; drug effects ; Male ; Propylamines ; pharmacology ; Rats ; Vasodilation ; Vasodilator Agents ; pharmacology

Objective To explore the gene expression of interleukin-13 receptor (IL-13R)?2 and its relationship to proliferation activity of human gliomas.Methods The gene expression of IL-13R?in 50 hu- man gliomas,2 malignant human glioma cell lines and 6 normal brain tissues were studied by RT-PCR.Ki-67 labeling index (Ki267 LI) of all sample were detecteded by immunohistochemical staining.Results Only one normal brain tissues expressed very low IL-13R?2 mRNA,whereas 35 (70%) of 50 human brain tumors expressed 1L-13R?2 mRNA.The positive rate and expression level of IL-13R?2 mRNA were increased with the ascending of WHO tumor grade.(former:rs=0.87;letter:rs=0.69,P＜0.01).The difference of posi- tive rate and expression level of IL-13R 2?mRNA between the low grade and high grade tumors was statistical- ly significant,the proliferation activity of gliomas evaluated by Ki-67LI (Ki-67 Labeling Index,Ki-67LI) was positively correlated with IL-13R?2 gene expression and the tumor grade.Conclusion In human cerebral gliomas,IL-13R?2 genes may play an role in the malignant progression.The expression level of malignancy in molecular level and selecting the target of gene therapy.

Objective To evaluate the efficacy of naloxone used in the postoperation of cerebral tumor.Methods Eighty patients were randomly assigned to receive (treated group:40 patients) or not re- ceive (control group:40 patients) naloxone.Both the two groups accepted the conventional therapy.Re- sults After operation,the content of?-EP,ET decreased continuously but the one of the treated groups was more obviously than that of the control groups (P

Objective To investigate the expression and significance of Smad 7,Smurf 1 and Smurf 2 in basal cell carcinoma and squamous cell carcinoma.Methods Biopsy specimens were resected from 14 patients with basal cell carcinoma,19 patients with squamous cell carcinoma and 30 normal controls.Quanti- tative real-time PCR and immunohistochemical techniques were utilized to assess the expression of Smad 7, Smurf 1 and Smurf 2 in these specimens.Results The gray scale for staining of Smad 7,Smurf 1 and Smurf 2 was 166.61?7.11,166.08?8.71,and 166.25?8.15 respectively in basal cell carcinoma,161.66?5.52,166.84?9.27,and 169.98?9.48 respectively in squamous cell carcinoma.The expression levels of Smad 7,Smurf 1 and Smurf 2 were all significantly increased in basal cell carcinoma and squamous cell car- cinoma in comparison with normal controls.Conclusions The over-expression of Smad 7,Smurf 1 and Smurf 2 may interfere with transforming growth factor?signaling transduction pathway through several links,therefore prevent the inhibitory effect of transforming growth factor?on epidermal proliferation,and accelerate the abnormal proliferation in above epidermal tumors.

Objective To observe the long term effects of arthroscopic knee debridement and reconstructing operation for treating osteoarthritis in patients with Kaschin-Beck disease. Methods Thirty-one cases of patients with Kaschin-Beck disease were followed for 6 years after operation of articular clearing by arthroscope. Index of pain, symptoms of self-evaluation, range of motion, walking distance, standing test by affected leg when bending at 30° or 60° were recorded and compared with the preoperative results. Results Twenty-four cases were followed up for 6 years. Six years after operation the pain index(3.38 ± 2.87) was dramatically decreased compared to that before operation (6.88 ± 1.45, t = 5.30, P ＜ 0.05). Patients symptoms markedly improved by subjective self-evaluation was 70.83% (17/24), the effective rate was 100% (24/24). The number of cases that could stand up when leg bending at 30° or 60° were 21,18 cases, respectively, compared with that of preoperative of 14, 11 cases, respectively, the difference was statistically significant(x2 = 5.17,4.27, all P ＜ 0.05). Six years after operation the walking distance(3 cases ＜ 1 km, 11 cases 1 - 5 km and 10 cases ＞ 5 km) were greatly improved compared to the results before operation (12 cases ＜ 1 km, 9 cases 1 - 5 km and 3 cases ＞ 5 km, U = 2.88, P ＜0.05). Six years after operation the knee activity[(132.25 ± 14.52)°] remained at the same level, compared with that of preoperative [(131 .58 ± 14.68) °], the difference was not statistically significant (t = 0.16, P ＞ 0.05) .Conclusions The method of arthroscopic joint debridement to cure Kaschin-Beck disease knee osteoarthritis can significantly reduce pain, improve function and walking distance, with more stable long-term satisfactory outcome.

Objective To explore the clinical and pathologic characteristic of deep fungus infection under mechanical ventilation in neonate. Method The clinical datas of 18 neonates under mechanical ventilation approved with deep fungus infection by autopsy from 1985 to 2003 in our department were collected and analyzed.Results In 18 infants who survived deep fungus infection,2 cases were premature and 16 cases were mature,the birth weight and the numbers of patients were:2500 g 2 cases;Time under mechanical ventilation was 8-86 days and the average time under mechanical ventilation was 13 days. The pathogen caused deep fungus infection was Aspergillus(8/18),Candida albicans(6/18) and Mucor(4/18),respectively. The infected organ were lung(12/18),brain(2/18),liver(4/18) and gastrointestinal tract(2/18),respectively.Two of them were found been infected in lung and liver at the same time.Conclusions We must attach importance to deep fungus infection in neonate under machine ventilation.Aspergillus and Candida albicans were the main pathogen bacteria and lung was the main infected organ of neonatal deep fungus infection.Early diagnosis may be the efficiency approach to increase livability.

OBJECTIVETo investigate the dynamic changes of the epididymal size 1 year after vasectomy.

METHODSFifty male volunteers received vasoligation. Before and at 1, 2, 3, 6, and 12 months after operation, we measured the size and detected the internal echoes of the epididymis using color Doppler ultrasonography.

RESULTSThe bilateral epididymides were both thickened post-operatively in all the 50 cases, with statistically significant differences between the baseline and the 1st month, the 1st and the 2nd month, the 2nd and the 3rd month, or the 3rd and the 6th month after surgery (all P < 0.01), but not between the 6th and the 12th month (P > 0.05).

CONCLUSIONWithin 6 months after vasectomy, the bilateral epididymides manifested a progressive thickening, but basically restored their balance of secretion-absorption after 6 months.

Epididymis ; diagnostic imaging ; pathology ; physiology ; Humans ; Male ; Organ Size ; Postoperative Period ; Time Factors ; Ultrasonography, Doppler, Color ; Vasectomy

Virginiamycin acetyltransferase D (VatD) plays a vital rule in streptogramins resistance by chemically inactivating streptogramin A. Therefore, it is desirable to discover novel small molecular weight inhibitors of VatD via state-of-the-art virtual screening techniques. This "cocktail" strategy by combining VatD inhibitor with streptogramins may provide new therapeutic opportunity for resistant bacteria infections. Structure-based virtual screening method (molecular docking) was applied to rank and score a chemical database containing 300 000 commercially available compounds against the VatD substrate binding site. Twenty six out of the 200 top scored compounds from the docking calculation were selected and submitted to the VatD enzymatic inhibition assay. The plasmid pRSET B/vatD was constructed and transformed into E. coli (trxB) host cells for over-expression, and VatD enzyme was purified and validated by showing acetyltransferase activity to Virginiamycin M1. Three out of these 26 tested compounds showed enzymatic inhibition on VatD with IC50 168.6, 91.0 and 55.2 micromol x L(-1), separately. Other compounds could not be dissolved in the system and/or had little effect on the enzyme (IC50 > 200 micromol x L(-1)). To our knowledge, it is first time that small molecular weight organic compounds were identified as VatD inhibitors. It is expected that the VatD inhibitors identified at present study could serve as lead compounds for the further development of the novel therapeutic agents to overcome streptogramins resistance.
Acetyltransferases ; antagonists & inhibitors ; genetics ; metabolism ; Catalysis ; drug effects ; Drug Design ; Drug Resistance, Bacterial ; Enzyme Inhibitors ; chemistry ; metabolism ; pharmacology ; Escherichia coli ; genetics ; Genetic Vectors ; Kinetics ; Molecular Structure ; Plasmids ; Streptogramin Group A ; chemistry ; metabolism ; pharmacology ; Transformation, Genetic

OBJECTIVETo observe the expression of galectin-3 in the liver metastasis of colon cancer in mice and the inhibitory effect of modified citrus pectin (MCP) on galectin-3 expression.

METHODSSeventy-five Balb/c mice were randomized into 5 groups, namely the negative control, positive control, low-concentration MCP, moderate-concentration MCP and high-concentration MCP groups. CT26 colon cancer cells were injected into the subcapsule of the mouse spleen to establish liver metastasis models of colon cancer, but the mice in the negative control group received no tumor cell injection. MCP was added into the drinking water of the mice at the concentrations of 0, 1.0%, 2.5% and 5.0% (m/V). The liver metastasis was observed 3 weeks after tumor cell inoculation. Enzyme-linked immunosorbent assay was performed to determine the serum galectin-3 level. A tissue microarray of the liver metastasis was prepared for immunohistochemical detection of galectin-3 expression in the liver metastasis.

RESULTSIn the positive control, low-, moderate- and high-concentration MCP groups, the rates of liver metastasis were 100%, 80%, 73.3% and 60%, respectively. The number of liver metastases in high-concentration MCP group was significantly smaller than that in the positive control group (P<0.05). In the 4 groups with tumor cell inoculation, the median volume of the primary lesions in the spleen was 1.51, 0.93, 0.77 and 0.70 cm(3), respectively, which were significantly smaller in the moderate- and high-concentration MCP groups than in the positive control group (P<0.05). The serum galectin-3 level in the positive control group and MCP-treated groups were significantly higher than that in the negative control group (P<0.01), but similar between the positive control group and the MCP-treated groups (P>0.05). In the positive control and the MCP-treated groups, the expression of galectin-3 in the liver metastases showed no significant differences (P>0.05).

CONCLUSIONThe expression of galetin-3 is significantly increased in the liver metastasis of colon cancer, and MCP can effectively inhibit the liver metastasis.

Animals ; Cell Line, Tumor ; Citrus ; chemistry ; Colonic Neoplasms ; drug therapy ; metabolism ; pathology ; Female ; Galectin 3 ; biosynthesis ; Immunohistochemistry ; Liver Neoplasms ; drug therapy ; metabolism ; secondary ; Mice ; Mice, Inbred BALB C ; Pectins ; therapeutic use ; Phytotherapy ; Random Allocation

To study the effect of steaming and baking process on contents of alkaloids in Aconite Lateralis Radix (Fuzi), 13 alkaloids were analyzed by UPLC-MS/MS equipped with ESI ion source in MRM mode. In steaming process, the contents of diester-diterpenoid alkaloids decreased rapidly, the contents of monoester-diterpenoid alkaloids firstly increased, reached the peak at 40 min, and then deceased gradually. The contents of aconine alkaloids (mesaconine, aconine and hypaconine) increased all the time during processing, while the contents of fuziline, songorine, karacoline, salsolionl were stable or slightly decreased. In baking process, dynamic variations of alkaloids were different from that in the steaming process. Diester-diterpenoid alkaloids were degraded slightly slower than in steaming process. Monoester-diterpenoid alkaloids, aconine alkaloids and the total alkaloids had been destroyed at different degrees, their contents were significantly lower than the ones in steaming Fuzi at the same processing time. This experiment revealed the dynamic variations of alkaloids in the course of steaming and baking. Two processing methods which can both effectively remove the toxic ingredients and retain the active ingredients are simple and controllable, and are valuable for popularization and application.
Aconitine ; analogs & derivatives ; isolation & purification ; Aconitum ; chemistry ; Alkaloids ; isolation & purification ; Chromatography, High Pressure Liquid ; Drug Stability ; Drugs, Chinese Herbal ; isolation & purification ; Hot Temperature ; Plant Extracts ; isolation & purification ; Steam ; Tandem Mass Spectrometry ; Time Factors