Anticonvulsants ; adverse effects ; Humans ; Seizures ; chemically induced

Objective To investigate the pathogenicity of transfusion transmitted virus (TTV) infection and assess the effect of genciclovir on TTV.Methods Serum TTV-DNA from 968 neonates was detected by a nested polymerase chain reaction technique and electropherosis. Alanine aminotrans ferase (ALT) and direct bilirubin (DB) were assayed in neonates with positive TTV-DNA.Genciclovir[10 mg/(kg?d)]was used to treat neonates with TTV-induced hepatitis.Results Among 968 neonates, 38 had positive TTV-DNA (4.0%). All neonates with positive TTV-DNA had normal serum levels of ALT and DB [(24.8?12.0) U/L and (17.6?6.8) ?mo l/L] 3 days after birth;But an elevated ALT and DB level [(95.5?16.4) U/L and (58.2?10.4) ?mol/L] occurred in 15 of them 2 weeks after birth,and were diagnosed as TTV-induced hepatitis.These patients had hypersomnia,jaundice and anorexia. Serum ALT and DB levels recovered to normal range one week after genciclovir therapy in 11 patients,so did the other 4 patients after 2 weeks therapy with genciclovir. Serum TTV-DNAs in all patients became negative 2 weeks after genciclovir therapy.Conclusion TTV infection exists in the neonates, and may be one of important causes of neonatal hepatitis.genciclovir might have a good anti-TTV effect.

Aim The study is to observe the clinical efficacy of losartan in hypertentive patientswith left ventricular hypertrophy. Methods 21 case were given losartan for 20 wk and 24h ambulatory blood pressure monitoring and color doppler echocardiography were per-formed in the patients before and after treatment.Results The 24 h SBP, 24 h DBP,dDBP, nSBP were from (151 ? 15) 、(93 ?9)、(155 ? 15)、(96 ? 10)、(146 ? 16)、(88 ? 11)mmHg before treatment to (132 ? 11)、(82 ? 8)、(137 ? 12)、(88 ? 9)、(120 ? 9)、(120 ? 15)、(74 ? 9) mmHg after treatment respectively and the IVST, PWT and LVMI were from(14.2 ? 1 .5) mm、(13. 9 ? 1. 45) mm、(152. 1 ? 24. 2) g? m2-1 BSA before treatment to(12. 1 ? 1. 31) mm、 (12. 2 ? 1. 41) mm、(130. 6 ? 23. 1) g? m2-1 BSA after treatment re-spectively. All the parameters after treatment in the patients were significantly decreased ascompared with those before treatment (P

OBJECTIVETo investigate the immunological activity of Streptomyces polysaccharide (SMP) on normal and immunosuppressed mice.

METHODSThe effect of SMP on the proliferating activity of normal mouse splenocytes was tested in the mixed lymphocyte culture, and the changes of peripheral blood T lymphocytes were evaluated with acid a-naphthyl acetate esterase (ANAE) method. The ratio of Lyt2+ and L3T4+ T cell subsets was measured by flow cytometry.

RESULTSSMP stimulated obvious proliferation of mixed lymphocytes, showed protective effects on T lymphocyte and increased the ratio of Lyt2+ and L3T4+ cell subsets to nearly normal level in immunosuppressed mice.

CONCLUSIONSSMP can regulate the immune function in mice.

Animals ; CD4-Positive T-Lymphocytes ; immunology ; Female ; Immunocompromised Host ; immunology ; Lymphocyte Culture Test, Mixed ; Male ; Mice ; Mice, Inbred BALB C ; Mice, Inbred C57BL ; Polysaccharides ; immunology ; Spleen ; cytology ; Streptomyces ; chemistry ; immunology ; T-Lymphocytes ; cytology ; immunology

Poly(ADP-ribose)polymerase-1 (PARP-1) plays a significant role in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trial. In this work, a series of 3-(2-oxo-2-substituted acetamido)benzamides have been synthesized and their inhibitory activities against PARP-1 were evaluated. Of all the tested compounds, six compounds displayed inhibitory activities with IC50 values ranging from 0.23 to 5.78 µmol.L-1 . The binding pose of compound 5a was predicted using molecular docking to facilitate further structural modification.
Antineoplastic Agents ; Benzamides ; chemistry ; DNA Repair ; Drug Design ; Humans ; Molecular Docking Simulation ; Poly(ADP-ribose) Polymerase Inhibitors ; chemical synthesis ; chemistry ; Poly(ADP-ribose) Polymerases

Tumorous cells are characterized by distinctive metabolic reprogramming and living conditions. Understanding drug metabolizing features in tumor cells will not only favor the estimation of metabolic rate, elimination half life and the assessment of potency, but also facilitate the optimal design of anti-tumor drugs/prodrugs. This article reviewed the expression and activity features of major drug metabolizing enzymes (DMEs) in solid tumorous tissues, such as liver, intestine, breast and lung, and the difference from the correspondingly normal tissues, exemplified by the metabolic properties of some classic antitumor-agents in tumorous tissues. In combination with the data retrieved in vitro tumor cell lines, we discussed the similarities and differences of DMEs expression and function between tumor tissues (in vivo) and tumor cells (in vitro), and proposed the possible factors that cause the differences.
Antineoplastic Agents ; pharmacokinetics ; Cell Line, Tumor ; Humans ; Inactivation, Metabolic ; Liver ; metabolism ; Neoplasms ; enzymology ; Prodrugs ; pharmacokinetics

Fourteen compounds were isolated by column chromatography from the ethyl acetate extract of the seeds of Brassica campestris. Their structures were elucidated by physicochemical properties and spectroscopic data analysis. The isolated compounds were respectively identified as (5Z,7E)-4, 4-dimethyl-5-acetyl-5, 7-nonadienoic acid (1), indole-3-carboxaldehyde (2), blumenol A (3), vinylsyringol (4), sinapinic acid (5), sinapic acid ethyl ester (6), protocatechuic acid (7), crinosterol (8), campesterol (9), 7-oxo-stigmasterol (10), kaempferol (11), 2,5-dihydroxybenzoic acid (12), syringic acid (13) and daucosterol (14). Compound 1 was a new compound and the other compounds were isolated from this plant for the first time except for compounds 4, 5 and 13.
Brassica ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Seeds ; chemistry ; Spectrometry, Mass, Electrospray Ionization

Objective To study osteogenic courses and features of human osteoblasts cultured in vitro and seeded into alloplastic decalcified cancellous bone.Methods Human osteoblasts isolated from normal human perios- teum were cultured and amplified in vitro.Thy configuration and developing manners of osteoblasts were observed. Then osteoblasts were seeded into alloplastic decalcified cancellous bone.Thy composites were implanted and cultured in thy body of athymic mice.The specimens were obtained 8 weeks later.Osteogenic characteristics were observed by scanning electron microscope.Results Osteoblasts isolated from human periosteum developed well and proliferated rapidly in vitro.Island new bone formation could be observed histologically 8 weeks after the composites of os- teoblasts and alloplasric decalcified cancellous bone were implanted and cultured in the body of athymic mice.Conclu- sion Calcified bone can be formed by seeding osteoblasts into alloplastic decalcified cancellous bone,which may be a new kind of bone graft source to construct bone defects.

Signal transducer and activator of transcription 3 (STAT3) is an important regulatory factor of cell proliferation and metastasis, involved in the occurrence and development of a variety of malignant tumors, and it is one of the hot spots in the research of targeted anti-tumor drugs. Our group screened a novel benzobis (imidazole) structure small molecule compound LZJ541 through the screening model of Janus kinase (JAK)/STAT3 pathway inhibitors, which has definite STAT3 inhibitory activity. We examined the effect of LZJ541 on the proliferation of HepG2 and PC-3 cells by MTT assay in vitro, detected the effect of LZJ541 on the expression of STAT3-related proteins in HepG2 cells by Western blot, and measured the effect of LZJ541 on the apoptosis and cell cycle arrest of HepG2 cells via flow cytometry. The results indicated that LZJ541 significantly inhibited the activation of STAT3 signaling pathway and restrained the proliferation of HepG2 cells. Its half maximal inhibitory concentration (IC₅₀) was 13.8 μmol·L^-1, which was much lower than that of PC-3 cells (with low STAT3 expression, IC₅₀: 41.99 μmol·L^-1), LZJ541 can also inhibit the phosphorylation of STAT3 in HepG2 cells, thereby inducing apoptosis and cycle arrest and then exerting anti-tumor effects. In conclusion, LZJ541 has a certain anti-tumor effect in vitro, which provides an experimental basis for the development of new STAT3-targeted anti-tumor drugs around this kind of compounds.

Objective To establish a three- dimensional hindlimb gait data toolkit (THGT) for healthy and spinal cord injured (SCI) non-human primate (rhesus monkey) based on Matlab to realize upload of original data, automatic gait division, calculation and drawing of multiple gait parameters, etc. Methods Vicon system was used to collect three-dimensional hindlimb gait data of healthy and SCI (after 6 weeks) rhesus monkey to obtain the kinematics data of both hindlimbs in continuous strides. It was analyzed with THGT to process the gait division, calculation and drawing of multiple gait parameters. Results THGT read the data, distinguished cycles of gait, calculated 140 kinds of gait parameters and drew graphs of the results. Conclusion THGT extends the universality of the Vicon data, realizes automatically gait division and friendly interactive interface, and puts out the visible results.