OBJECTIVETo evaluate the impact of nicotine- and tar-free cigarette smoke extract (fCSE) on the serum testosterone (T) level and erectile function of male rats.

METHODSWe randomized 30 male SD rats to three groups of equal number to receive subcutaneous injection of PBS (1.0 ml / 300 g body weight per day), fCSE (1.0 ml/300 g body weight per day), and reduced glutathione hormone (GSH, 200 mg per kg body weight per day) in addition to fCSE (fCSE + GSH), respectively, all for 8 weeks. Then we evaluated the erectile function of the rats by measuring the maximal intracavernous pressure (MICP), mean arterial pressure (MAP), ICP/MAP ratio, time of stimulation to MICP (Tmax), and cavernosal filling fate (CFR). We determined the serum T level, the activities of superoxide dismutase (SOD) , malondialdehyde (MDA), and nitric oxide synthase (NOS) in the cavernosal tissue, and also observed the morphological changes of the corpus cavernosum.

RESULTSCompared with the controls, the rats of the fCSE group showed obvious decreases in the levels of serum T ([5.37 ± 1.43] vs [3.22 ± 1.11] μg/L), NOS ([2.90 ± 0.27] vs [1.67 ± 0.18] U/mg) , and SOD ([18.41 ± 1.09] vs [13.36 ± 1.18] U/mg prot) and erectile function-related indexes MICP ([85.92 ± 6.36] vs [58.99 ± 10.76] mmHg), MICP/MAP (0.86 ± 0.09 vs [0.56 ± 0.08]), and CFR (2.14 ± 0.44 vs 0.89 ± 0.44), but markedly increased Tmax ([29.90 ± 5.78] vs [42.90 ± 8.56]s), with a positive correlation between the serum T level and CFR (r = 0. 364, P < 0.05). Masson staining revealed a lower ratio of the corpus cavernosum smooth muscle tissue to collagen fiber in the fCSE group (0.27 ± 0.04) than in the control (0.98 ± 0.12). Compared with the fCSE group, the fCSE + GSH group exhibited significantly improved MICP ([58.99 ± 10.76 ] vs [77.95 ± 7.71] mmHg), MICP/MAP (0.56 ± 0.08 vs 0.77 ± 0.09), and CFR (0.89 ± 0.44] vs 1.76 ± 0.42) and shortened Tmax ([42.90 ± 8.56 ] vs [32.10 ± 5.84 ] s). The ratio of the corpus cavernosum smooth muscle tissue to collagen fiber was higher in the fCSE + GSH than in the fCSE group (0.77 ± 0.09 vs 0.27 ± 0.04) but still lower than in the control (0.98 ± 0.12).

CONCLUSIONNicotine- and tar-free cigarette smoke extract reduces the serum T level and erectile function of rats, which is related to oxidative stress. Antioxidant therapy can improve erectile function but has a limited value for morphological protection of the penile tissue.

Animals ; Erectile Dysfunction ; chemically induced ; Male ; Malondialdehyde ; metabolism ; Muscle, Smooth ; pathology ; Nicotine ; Nitric Oxide Synthase ; metabolism ; Penile Erection ; drug effects ; Penis ; pathology ; Rats ; Rats, Sprague-Dawley ; Smoke ; adverse effects ; Superoxide Dismutase ; metabolism ; Tars ; Tobacco ; adverse effects

Objective　To explore the relationship between hemolymph phenol oxidase and the melanization of Plasmodium yoelii oocysts in Anopheles dirus. Methods　An Anopheles dirus-Plasmodium yoelii system was used Anopheles dirus were divided into 3 groups, that is, non-blood-fedding (N), normal-blood-fedding (B) and infected-blood-fedding (I). The activities of MPO and o-DPO in hemolymph from 3 groups were determined with native polyacrylamide gel electrophoresis (PAGE) and density scanning at 5, 7, 11 and 15 d after blood feeding. Results　Both MPO and o-DPO activity were significantly higher in group I than group N and B (P<0.05). But with the melanization of Plasmodium yoelii oocysts, both MPO and o-DPO activity in group I were decreased in comparison with group N, especially on the 15 th day after infected-blood feeding. MPO and o-DPO activity in group B were significantly stronger than those of group N. Conclusion　Blood feeding and infection of Plasmodium yoelii both can activate the cascade. The heamolymph phenol oxidase may play an important role in the melanization of Plasmodium yoelii oocysts in Anopheles dirus.

OBJECTIVETo investigate the antiviral activity of 3-hydroxyphthalic anhydride-modified ovalbumin (HP-OVA) against herpes simplex virus 2 (HSV-2) in vitro.

METHODSBy chemical modification, ovalbumin (OVA) was treated with 3-hydroxyphthalic anhydride (HP) to prepare HP-OVA. The anti-HSV-2 activity against HSV-2 333 virus in vitro and the cytotoxicity of HP-OVA in African green monkey kidney cells (Vero cells) were detected by MTT colorimetric assay. The inhibitory effects of HP-OVA on 17 strains of vaginal lactobacilli were observed by microscopy.

RESULTSAnhydride-modified ovalbumin significantly inhibited the infection by HSV-2 with an IC(50) of 23.56±8.33 µg/ml. HP-OVA showed only low cytotoxicity to the host cells with a CC(50) over 1 mg/ml. HP-OVA did not produce significant inhibitory effect on the 17 strains of vaginal lactobacilli (MIC>1 mg/ml).

CONCLUSIONAnhydride-modified protein HP-OVA exhibits potent anti-HSV-2 activity in vitro and can be a good microbicide candidate for prevention of sexually transmitted diseases.

Animals ; Antiviral Agents ; pharmacology ; Cercopithecus aethiops ; Herpesvirus 2, Human ; drug effects ; Ovalbumin ; chemistry ; pharmacology ; Phthalic Anhydrides ; chemistry ; pharmacology ; Vero Cells

OBJECTIVETo synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities.

METHODSA series of pyrimidines containing different arylamino and 1-(methylsulfonyl)piperidin moieties were designed by combining the segments 1-(methylsulfonyl)piperidin and pyrimidine heterocycles according to the super-position principle of the reinforcement of biological activities.

RESULTSTheir structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay.

CONCLUSIONThe preliminary bioassay showed that compound 3 b displayed good antitumor activity (IC(50)=13.6 µmol/L). The preliminary structure activity relationship analysis of these analogues suggest that the steric factor may have important impact on the anti-tumor activity.

Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Drug Screening Assays, Antitumor ; Humans ; Pyrimidines ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

OBJECTIVETo establish hepatitis C virus (HCV) infected cell model which is similar to the infection in vivo and can support HCV to replicate for a long time.

METHODSAfter infected with HCV-positive serum, Hep G2 cells were cultured for 60 days. Nested RT-PCR was used to detect plus and minus HCV RNA in cultured cells and supernatants.

RESULTSPlus HCV RNA was detected intermittently in Hep G2 cells during 2-30 days, minus HCV RNA was detected during 3-30 days after infection, the detection rate was similar to plus HCV RNA. Plus and minus HCV RNA can be still intermittently detected during 31-60 days after infection. However, the detection rate gradually declined. Plus HCV RNA was also found intermittently positive in the supernatant, and the detection rate was consistent to that in cells. Minus HCV RNA was not detected in the supernatant.

CONCLUSIONHep G2 cells were susceptible to HCV, and could support HCV to replicate for a relatively long time. Hep G2 is an ideal HCV infection cell model.

Cell Line, Tumor ; Hepacivirus ; genetics ; growth & development ; Humans ; RNA, Viral ; genetics ; isolation & purification ; Reverse Transcriptase Polymerase Chain Reaction ; Virus Replication

OBJECTIVETo establish the chromatographic fingerprint of supercritical carbon dioxide extract of Tripterygium wilfordii.

METHODHPLC method was applied for quality assessment of T. Wilfordii, HPLC analysis was performed on Kromasil C18 (4. 6 mm x 250 mm, 5 microm) with the mixture of acetonitrile-1% per thousand H3PO4, as mobile phase in gradient mode. The samples were detected at UV of 267 nm with column temperature of 35 degrees C, analytic time was 80 min; Flow-rate was 1.0 mL x min(-1). The chromatographic fingerprint of ten batches of samples was determined, for establishing the chromatographic fingerprint of T. Wilfordii.

RESULTIndicating 27 peaks in common, identified 21 peaks with chemical reference and HPLC-MS, and the HPLC fingerprint was established.

CONCLUSIONThe method is steady and accurate with a good repeatability and can be used as a quality control method for T. Wilfordii.

Carbon Dioxide ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Chromatography, Supercritical Fluid ; methods ; Plant Extracts ; analysis ; chemistry ; isolation & purification ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Reproducibility of Results ; Spectrometry, Mass, Electrospray Ionization ; methods ; Tripterygium ; chemistry

Xuezhikang capsule (ethanol extract of red yeast rice) which produced by Beijing WBL Peking University Biotech Co., Ltd., is a traditional Chinese medication with 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibiting activity. Clinical trials indicated that Xuezhikang with lipid-lowering action could reduce the risk of cardiac events and total mortality of Chinese coronary heart disease patients. To exactly explain the clinical features of Xuezhikang, we undertook a complete study of the chemical constituents of Xuezhikang. This study resulted in the isolation of a new monacolin analogue, named alpha, beta-dehydromonacolin L (1), along with two known compounds: monacolin L (2) and 3-(2, 6-dimethyl-1, 2, 4a, 5, 6, 7, 8, 8a-octahydronaphthalen-1-yl)propanoic acid (3). The chemical structures were determined by extensive 1D and 2D NMR and MS spectroscopic analysis.
Drugs, Chinese Herbal ; chemistry ; Molecular Structure ; Naphthalenes ; chemistry ; isolation & purification ; Propionates ; chemistry ; isolation & purification

OBJECTIVETo study the effects of phytoestrogen alpha-zearalanol (alpha-ZAL) on normal human breast.

METHODSTen specimens of normal human breast tissues were subcutaneously implanted into 30 athymic nude mice aged 9-10 weeks, one for 3 mice. These mice were then randomly divided into three groups: control group (without hormone treatment, n = 10), 1 mg/kg alpha-ZAL group (n = 10), and 5 mg/kg alpha-ZAL group (n = 10). All breast tissues were taken out 6 weeks later. Immunohistochemistry was used to determine the protein expressions of proliferating cell nuclear antigen (PCNA), inhibiting apoptosis gene Bcl-2, estrogen receptor (ER), and progesterone receptor (PR). Reverse transcription polymerase chain reaction (RT-PCR) was used to measure the expression levels of estrogen sulfotransferase (EST) mRNA and bridging integrator protein-1 (BIN1) mRNA. Morphological features of grafts before and after treatment were also observed.

RESULTSAlpha-ZAL had no significant effects on Bcl-2, PCNA, ER, and PR expression of mammary epithelial cells in graft specimens. Alpha-ZAL upregulated BIN1 mRNA expression in grafts, but had no significant effect on ESTmRNA expression.

CONCLUSIONSAlpha-ZAL does not affect the morphology, proliferating, and apoptosis of epithelial cells in normal human breast tissues implanted into nude mice, but it may increase the gene expression of tumor-inhibiting BIN1, suggesting that alpha-ZAL may have potential proteotive effect on normal human breast.

Adult ; Animals ; Breast ; chemistry ; drug effects ; Estrogens, Non-Steroidal ; pharmacology ; Female ; Humans ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Phytoestrogens ; pharmacology ; Proliferating Cell Nuclear Antigen ; analysis ; Random Allocation ; Receptors, Estrogen ; analysis ; Receptors, Progesterone ; analysis ; Zeranol ; pharmacology

Semen-derived enhancer of viral infection(SEVI) is a peptide fragment (PAP248-286) from prostatic acid phosphatase(PAP), which can enhance human immunodeficiency virus infection. The mechanisms of SEVI include: (1) SEVI with several cationic amino acid residues reduced electrostatic repulsion between HIV virus and the target cells; (2) The disorder state of SEVI in the human body fluids was helpful to the interaction between virus and the target cell membranes; (3) SEVI could capture HIV particles directly and speed the velocity of virus on the surface of the target cells and improve adsorption and fusion. Currently, the substances of inhibiting SEVI activity include: EGCG from green tea, small molecule compound of aminoquinoline Surfen, ThT analogs BTA-EG6. Those compounds might block the combination of HIV and SEVI or prevent the formation of amyloid fibers, and then reduce the enhancement of SEVI. The studies on the biological characteristics and mechanisms of SEVI have a big benefit for the prevention and treatment of HIV infection.
HIV Infections ; etiology ; transmission ; Humans ; Male ; Semen ; physiology ; Sexually Transmitted Diseases, Viral ; etiology ; Static Electricity

Objective: To understand status of amphetaminetype stimulants (ATS) use among residents aged 15-64 in a border city of Yunnan province. Methods: Using the stratified cluster random sampling method, a total of 3 130 residents were recruited through both anonymous questionnaire and interview, regarding their health-related behaviour and ATS use. Results: Among 3 130 residents aged 15-64 years in this city, the overall prevalence rates of ATS use were 4.0% (126/3 130) in the lifetime and 2.6% (82/3 130) in the past one year, while the prevalence of ATS use disorder in the past year was 2.3% (73/3 130). The prevalence rates of lifetime ATS use and in the past year were 7.5% (108/1 443) and 5.1% (73/1 443) in the high epidemic area, 7.3% (122/1 682) and 4.8%(80/1 682) in males, 5.2% (118/2 260) and 3.4% (77/2 260) in 18-45 age group, 4.6%(63/1 361) and 3.4% (46/1 361) in the ones having had elementary school education, 10.3% (50/487) and 8.6% (42/487) in unmarried group, 17.1% (19/111) and 12.6% (14/111) in either divorced, widowed or separated group, 4.8% (108/2 256) and 3.2% (72/2 256) in the farmers group, 6.0% (99/1 643) and 4.4% (73/1 643) in the non-religious groups (neither Buddhism nor Christianity), 15.2% (97/639) and 11.9% (76/639) in groups with negative hobbies which were 1.3% (29/2 314) and 0.3%(6/2 314) higher than the ones with positive hobbies, 8.5% (84/992) and 6.3% (62/992) in the ones negatively managing the stress which were 2.0% (42/2 138) and 0.9% (20/2 138) higher than the ones that treating the stress in a positive way. Conclusions The prevalence rates of ATS use and ATS use disorder in the past one year appeared high among those residents aged 15-64 years in the border city of Yunnan province. Prevention and intervention programs should be carried out for the target groups as soon as possible.