Chronic Disease ; Diagnosis, Differential ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Gastritis ; diagnosis ; drug therapy ; Humans ; Medicine, Chinese Traditional ; Phytotherapy ; Reference Standards

Digestive System Diseases ; therapy ; Humans ; Integrative Medicine

Diagnosis, Differential ; Drug Therapy, Combination ; Drugs, Chinese Herbal ; therapeutic use ; Dyspepsia ; diagnosis ; drug therapy ; Humans ; Medicine, Chinese Traditional ; Phytotherapy

Diagnosis, Differential ; Drugs, Chinese Herbal ; therapeutic use ; Humans ; Irritable Bowel Syndrome ; diagnosis ; drug therapy ; Medicine, Chinese Traditional ; Phytotherapy ; Reference Standards

AIMTo investigate factors affecting the properties of antisense oligodeoxy nucleotides (ASON)-liposomes complex and their cellular uptake.

METHODSThree types of blank liposomes were prepared by reverse-phase evaporation vesicles, and the complex were obtained through physical absorption. The light microscope was used to observe morphology characteristics of the complex. Drug loading capacity was analyzed by agarose gel electrophoresis. The transfected cell percentage and means fluorescence intensity were determined by flow cytometric analysis using M3 myeloma cell as a model.

RESULTSThe neutral liposome showed no aggregation while the cationic liposomes appeared some different extent aggregation in different medium when associated antisense oligodeoxynucleotides. The drug loading capacity depended on the ratio of +/- and the cationic charge density on the lipid membrane. The two kinds of cationic liposomes appeared different principles of loading ASON. As far as cellular uptake, The neutral liposomes showed no improvement of cellular uptake of ASON. However, the cationic liposomes were shown to enhance the cellular uptake of ASON if the appropriate +/- charge ratio was used. The optimal cellular uptake was achieved when +/- charge ratio was at 0.5:1 and 1:1 for SA-I liposome and SA-II liposomes, respectively.

CONCLUSIONThe cationic liposomes improved the loading capacity and cell uptake of antisense oligodeoxynucleotides, which was determined by +/- charge ratio and charge density.

Amines ; metabolism ; Biological Transport ; Drug Carriers ; Drug Delivery Systems ; Humans ; Liposomes ; pharmacokinetics ; Multiple Myeloma ; Oligodeoxyribonucleotides, Antisense ; administration & dosage ; pharmacokinetics ; Random Allocation ; Tumor Cells, Cultured ; metabolism

Objective To study CD64 expression in neutrophilic granulocyte and its clinical effect in neonatal infection disease. Methods CD64 was detected among 59 neonatal patients(septicemia group 34 patients, local infection group 25 patients)hospitalized in our neonatal department diagnosed as neonatal infection disease in 48 h after hospitalized,2 weeks after therapy, then the results were compared with 27 patients as non - infection disease during the same period. Results CD64 in septicemia group was (6156. 21?3643. 32) molecula per cell,in local infection group was (2176.19 ? 946. 32)molecula per cell, in non- infection group was (2176. 19 ? 946. 32) molecula per cell.There were significant differences among three groups (all P0.05). Conclusions CD64 expression increases in bacterium infection disease. It is more obvious in widespread infection desease.and it can be the mark in early diagnosis of neonatal infection disease.

Racemic (±)-F18 (10-chloromethyl-11-demethyl-12-oxo-calanolide A), an analog of nature product (+)-calanolide A, is a new anti-HIV-1 nonnucleoside reverse transcript inhibitor (NNRTI). A successful enantioseparation of (±)-F18 offering (R)-F18 and (S)-F18 was achieved by a chiral stationary phase prepared HPLC. Their absolute configurations were determined by measurement of their electronic circular dichroisms combined with modem quantum-chemical calculations. Further investigation revealed that (R)-F18 and (S)-F18 shared a similar anti-HIV activities, however, (R)-F18 was more potent than (S)-F18 against wild-type virus, K101E mutation and P225H mutation pseudoviruses.
Anti-HIV Agents ; chemistry ; Chromatography, High Pressure Liquid ; HIV-1 ; drug effects ; Pyranocoumarins ; chemistry

OBJECTIVETo investigate the protective effect of melatonin on residual hair follicle cells of scald rats at early stage.

METHODSEighteen male Sprague-Dawley rats were randomly divided into scald group, treatment group, sham group , with 6 rats in each group. The rats in scald group and treatment group were subjected to 30% TBSA partial thickness scald on the back, and were resuscitated with balanced solution after 1 hour, while those in sham group were immersed in water at 37 degrees C for 25 s to simulate scald, and did not receive fluid replacement. Rats in treatment group were intraperitoneally injected with 10 mg/kg melatonin solution at 1 minute, 8 hours and 12 hours after scald, while those in sham group and scald group were given equal volume of 1% alcohol sodium-isotonic saline instead. Tissue samples were harvested at 6, 12 and 24 post scald hours (PSH) for determination of MDA and GSH levels. Apoptosis of residul hair follicle was detected by TUNEL method and immunohistochemistry of caspase-3.

RESULTSThe level of MDA in scald group at each time point was much higher than that in sham group (P < 0.01) and treatment group (P < 0.05), and it peaked at 12 PSH. The changes in GSH were just opposite to that of MDA. Under fluorescence microscope, the residual hair follicle cells were blue, and the apoptotic cells appeared green. The apoptosis rate in scald group at 6, 12, 24 PSH was obviously higher than that in sham (P < 0.01) and treatment groups (P < 0.05), which was (20.2 +/- 3.4)% vs (4.3 +/- 2.3)% vs (10.9 +/- 3.2)%, (31.2 +/- 3.6)% vs (5.1 +/- 2.5)% vs (19.1 +/- 3.7)%, (22.4 +/- 2.7)% vs (4.1 +/- 2.4)% vs (13.1 +/- 3.4)%, respectively. The score of caspase-3 positive cell in scald group was higher than those in sham group (P < 0.01) and treatment group (P < 0.05).

CONCLUSIONSThere is obvious correlation between oxidative stress and apoptosis rate of hair follicle cells in rats with partial thickness scald. Early administration of melatonin may have anti-apoptosis ability for residual hair follicle cells by attenuation of oxidative stress.

Animals ; Apoptosis ; Burns ; drug therapy ; metabolism ; Hair Follicle ; cytology ; metabolism ; Male ; Melatonin ; therapeutic use ; Oxidative Stress ; Rats ; Rats, Sprague-Dawley

Poly(ADP-ribose) polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. It can polymerize ADP-ribose units on its substrate proteins which are involved in the regulation of DNA repair. In this work, a novel series of para-substituted 1-benzyl-quinazoline-2, 4 (1H, 3H)-diones was designed and synthesized, and the inhibitory activities against PARP-1 of compounds 7a-7e, 8a-8f, 9a-9c and 10a-10c were evaluated. Of all the tested compounds, nine compounds displayed inhibitory activities with IC50 values ranging from 4.6 to 39.2 micromol x L(-1). In order to predict the binding modes of the potent molecules, molecular docking was performed using CDOCKER algorithm, and that will facilitate to further develop more potent PARP-1 inhibitors with a quinazolinedione scaffold.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Drug Design ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Molecular Docking Simulation ; Molecular Structure ; Poly (ADP-Ribose) Polymerase-1 ; Poly(ADP-ribose) Polymerases ; Quinazolinones ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

The fundamental mechanism of gastrointestinal diseases is the imbalance between the attack factor and the protective factor of stomach mucous membrane. It can not outbreak if the protective factor is stronger than the attack factor; otherwise, it will. Attack and protective function inside the stomach are mediated by various factors. These related factors interaction constitutes a complicated network system. This kind of outbreak theories of imbalance in Western medicine is same as that, "The sense of right saves inside, the evil can't do" and "Evil is competing with right, all diseases occur", in Chinese medicine. So, it is the key which points to futher study the interaction between gastrointestinal attack factors and protective factors by traditional Chinese medicine, thus improving the clinical effect.
Gastrointestinal Diseases ; therapy ; Humans ; Integrative Medicine ; Medicine, Chinese Traditional