AIM: Tranditional methods of screening drugs for benign prostatic hyperplasia(BPH)requires senile male animals such as dogs or rats.It consumes a long time to get the results. Over-expression of type Ⅱ5α-reductase in prastate induces BPH.A fast and efficient screening model of type Ⅱ5α-reductase inhibitors for BPH was set up in this paper.METHODS:Microsomes were extracted from male Sprague-Dawley rat livers by gradient centrifugation.Type Ⅱ5α-reductase enzyme-catalyzed reaction was assayed by UV-spectrophotometry using testosterone as a substrate and NADPH as hydrogen donor.The change of enzymatic activity was recorded with a NADPH wavelength of 340 nm by subtracted descending velocity of the control(without 5α-reductase).Effects at different conditions(temperatures,pH,enzyme and testosterone concentrations)on 5α-reductase were assayed.RESULTS:The suitable condition of type Ⅱ5α-reductase reaction Was defined as concentration of 109.05 mg protein/L enzyme(pH 6.00)with 2 μmol/L testosterone at 37℃.Michaelis'constant of type Ⅱ5α-reductase was 0.6μmol/L.Finasteride,a new drug for BPH,significantly inhibited activity of type Ⅱ 5α-reductase.IC50 of finasteride Was 64.1 nmol/L.As solvent of drugs,concentration of ethanol below 1.1% did not inhibite enzymatic activity(P＞0.05).Concentration of ethanol above 1.6%could obviouslv suppress enzymatic activity(P＜0.01).Daytime difference within five days had no significant difference(P＞0.05).CONCLUSION:A handy and fast screening method for type Ⅱ 5α-reductase inhibitors has been set up using UV-spectrophotometry.It may be used to screening drugs for BPH treatment.

OBJECTIVE:To evaluate the bioequiavailability of the domestic and the imported paracetamol and oxycodone tablets.METHODS:The blood concentrations of paracetamol and oxycodone in22healthy male volunteers were determined by HPLC-MS after a single dose orally1tablet of domestic or imported oxycodone tablet by a randomized crossover way.RE?SULTS:The main pharmacokinetic parameters of the domestic and the imported oxycodone tablets were as follows:C max were(10.4?2.2),(11.1?3.3)?g/L,respectively;t max were(1.05?0.35),(0.92?0.40)h,respectively;t 1/2 ke were(5.36?0.91),(5.53?1.25)h,respectively;AUC 0～t were(44.2?7.9),(44.5?8.3)(?g?h)/L,respectively;AUC 0～∞ were(49.3?9.4),(51.0?11.6)(?g?h)/L,respectively;the relative bioavailability of the domestic preparation was(102.8?27.4)%.The main pharmacokinetic parameters of the domestic and the imported paracetamol were the following:C max were(4612?696),(4592?825)?g/L,respectively;t max were(0.94?0.28),(0.96?0.23)h,respectively;t 1/2 ke were(3.99?0.77),(4.05?0.83)h,re?spectively;AUC 0～t were(15732?3450),(16265?3858)(?g?h)/L,respectively;AUC 0～∞ were(16618?3545),(17205?4194)(?g?h)/L,respectively;the relative bioavailability of the domestic one was(97.6?10.3)%.CONCLUSIONS:The2preparations are bioequivalent.

Objective To investigate the effects of crocodilian plasma on 12 bacteria(including G+ bacteria and G-bacteria) lines in vitro.Methods The bacteria CFUs on nutrient broth agar plates were determined after bacteria and crocodilian plasma incubated together for 1h.Then effects of the samples on the survival rate of various concentrations of bacteria were calculated.To evaluate the antibacterial spectrum of crocodilian plasma,the zones of bacterial inhibition were measured through agar disk method.Results and Conclusion Crocodilian plasma had superior bactericidal effects on Escherichia coli M421C1,O111B4,E240-3 LT,Micrococcus catarrhalis,Shiga's bacillus,Pseudomonas aeruginosa and Diplococcus pneumoniae.The results indicated why wound of crocodilian by tearing each other was not susceptible,and crocodilian plasma could be developed a natural antibacterials.

0.05).Concentration of ethanol above 1.6 % could obviously suppress enzymatic activity(P0.05).CONCLUSION: A handy and fast screening method for type Ⅱ5?-reductase inhibitors has been set up using UV-spectrophotometry.It may be used to screening drugs for BPH treatment.

OBJECTIVETo research the pharmacological action of curcumin solid dispersions (SDs, curcumin and polyvinylpyrrolidone (PVP) k30 in the ratio of 1:8) was investigated on experimental gastric ulcer in rats and mice.

METHODAnimals were randomly divided into several experimental groups. Each group consisted of 10 animals. The control group received PVP vehicle (720 mg x kg(-1), po) throughout the course of the experiments. The treatment groups received different doses of curcumin SDs (equivalent to curcumin 10, 30 and 90 mg x kg(-1), po), and ranitidine (27 mg x kg(-1), po) was used as the positive control. In acetic acid-induced gastric ulcers model, serum NO, plasma ET and gastric ulcer indexes of rats were measured after oral administration for 14 d. In rat ulcer model induced by pylorus-ligature, gastric volume pepsin and gastric ulcer indexes of rats were measured after oral administration for 3 d and pylorus-ligature inducement for 16 h. Gastric ulcer indexes of mice were measurement after oral administration for 3 d and subcutaneous injection reserpine 10 mg x kg(-1).

RESULTThe results showed that curcumin SDs (equivalent to curcumin 30, and 90 mg x kg(-1), po) could reduce the ulcer indexes 4.59 +/- 0.96 and 3.33 +/- 0.93 (P < 0.01), and increase serum NO level (29.75 +/- 5.90) mmol x L(-1) (P < 0.05) and (39.63 +/- 12.73) mmol x L(-1) (P < 0.01), compared to gastric index 5.87 +/- 0.48 and NO level (23.63 +/- 5.73) mmol x L(-1) in control group. Compared to plasma ET (163.65 +/- 63.84) ng x L(-1) in control group, curcumin SDs (equivalent to 90 mg x kg(-1), po) could decrease plasma ET level (104.22 +/- 63.84) ng x L(-1) (P < 0.05). Compared to gastric ulcer indexes 4.25 +/- 0.71 of control group in rat pylorus-ligature model, curcumin SDs (equivalent to curcumin 90 mg x kg(-1)) could reduce gastric ulcer to 2.38 +/- 0.74 (P < 0.01). Compared to gastric volume (14.61 +/- 1.80) mL, acidity of gastric juice (87.70 +/- 9.84) mmol x L(-1), and the activity of pepsin (408.63 +/- 41.75) U x mL(-1), curcumin SDs (equivalent to curcumin 30, 90 mg x kg(-1)) could reduce gastric volume to (12.68 +/- 1.46) mL (P < 0.05) and (9.99 +/- 0.79) mL (P < 0.01), reduce acidity of gastric juice to (77.62 +/- 8.34) mmol x L(-1) (P < 0.05) and (65.77 +/- 8.19) mmol x L(-1) (P < 0.01), inhibit the activity of pepsin to (358.13 +/- 37.44) U x mL(-1) (P < 0.05) and (292.13 +/- 41.93) U x mL(-1) (P < 0.01). In reserpine-induce gastric ulcer model, curcumin SDs (equivalent to curcumin 30, 90 mg x kg(-1)) could reduce gastric ulcer indexes to 3.88 +/- 0.40 and 3.03 +/- 0.64 (P < 0.01), compared to that of control group 5.13 +/- 0.59.

CONCLUSIONSeveral animal gastric ulcer models prove that curcumin SDs has anti-gastric ulcer effects by inhibiting gastric acid secretion, reducing gastric juice acidity, inhibiting the activity of pepsin and promoting healing of ulcer. These findings show a potential application of curcumin SDs as an anti-ulcerogenic drug.

Animals ; Anti-Ulcer Agents ; administration & dosage ; chemistry ; Curcumin ; administration & dosage ; chemistry ; Disease Models, Animal ; Female ; Humans ; Male ; Plant Extracts ; administration & dosage ; chemistry ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Stomach Ulcer ; drug therapy

Echinococcus granulosus is an important zoonotic parasite globally causing cystic echinococcosis (CE) in humans and animals. In this study, prevalence of CE and variation of cox1 gene sequence were analyzed with isolates E. granulosus collected from different areas in northern Xinjiang, China. The survey showed that 3.5% of sheep and 4.1% of cattle were infected with CE. Fragment of cox1 was amplified from all the positive sheep and cattle samples by PCR. In addition, 26 positive samples across the 4 areas were included. The isolates were all E. granulosus sensu stricto (s.s.) containing 15 haplotypes (Hap1-15), and clustered into 2 genotypes, G1 (90.1%, 91/101) and G3 (9.9%, 10/101). Hap1 was the most common haplotype (48.5%, 49/101). Hap9 were found in humans samples, indicating that sheep and cattle reservoir human CE. It is indicate that E. granulosus may impact on control of CE in livestock and humans in the region.
Animals ; Cattle ; China ; Cross-Sectional Studies ; Echinococcosis ; Echinococcus granulosus ; Echinococcus ; Genotype ; Haplotypes ; Humans ; Livestock ; Parasites ; Polymerase Chain Reaction ; Prevalence ; Sheep