The ischemic heart disease has been endangering human health seriously. Although there are many kinds of anti-ischemic drugs, most of them are lacking in tissue specificity, which together with a remarkably reduced blood circulation in the ischemic zone often lead to a quite low drug distribution in the targets. Myocardial ischemia can cause a lot of pathophysiological changes, such as the enhanced permeability of the endothelial cell membrane, the up-regulated expression of various cell adhesion molecules on endothelium, the exposure of intracellular antigenic components, the decrease of pH within the ischemic zone, and so on. To date, some of these changes have been exploited with limited success to gain the passive, active and physicochemical targeting of diagnostic or therapeutic drugs to myocardial ischemic regions. However, more effective delivery strategies are still eagerly needed. Here, we reviewed and discussed the potential targeting-delivery mechanisms and strategies, used or may be used in the future, for myocardial ischemic regions.
Animals ; Antibodies, Monoclonal ; immunology ; Capillary Permeability ; Drug Carriers ; Drug Delivery Systems ; methods ; Genetic Therapy ; Humans ; Liposomes ; chemistry ; metabolism ; Myocardial Ischemia ; therapy ; Myocardium ; metabolism ; pathology ; Polyethylene Glycols ; metabolism ; Ultrasonics

Combining the structural features of picotamide and linotroban, a series of N,N'-bis-(halogenophenyl)-4-methoxybenzene-1, 3-disulfonamides were designed and synthesized on the basic principles of drug design. The structures of target compounds were confirmed by IR, 1H NMR and HR-MS, and the in vitro antiplatelet aggregation activity was evaluated by Born turbidimetric method with adenosine diphosphate (ADP) as the platelet aggregation inducers. The assay results showed that twelve compounds (4b, 4f, 4l, 5b, 5d-5g, 5j, 5k, 5m and 5n) were found to have superior anti-platelet aggregation activities than the positive drug picotamide. The preliminary structure-activity relationship (SAR) has been explored.
Adenosine Diphosphate ; Drug Design ; Phthalic Acids ; Platelet Aggregation ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship ; Sulfonamides ; chemical synthesis ; chemistry

1.0?10~7 copies/mL. The HBsAg IHC staining positive cells could be observed in 6 placental tissues and 3 fetus' liver tissues,and HBcAg was also positive in 1 case of fetus' liver tissue.After co-incubating the tropho- blastic cells and HBV DNA positive serum in vitro,HBsAg expression and HBV DNA could be detected.Apoptosis of HBV-infected trophoblastic cells increased,which was demonstrated by in vivo and in vitro experiments and the apoptosis of placental cells was correlated with the cord blood HBV DNA level.The results of in vitro experiments showed that the apoptosis of trophoblastic cells increased with the elongation of infection time.After 6 months,1 of 12 newborns was positive for HBsAg,HBeAg and anti-HBc,6 was positive for anti-HBs.Conclusions The mechanism of HBV intra-uterine infection may be that HBV breaches the placental barrier and infects the fetus.The localization and replication of HBV in fetal tissues and organs are probably the important factors of chronic HBV infections in neonates.The apoptosis of trophoblastic cells may be the protective mecha- nism for the placental barrier to block the HBV intra-uterine transmission.

Syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid are three main bioactive ingredients in herbs of Saussurea involucrata with various pharmacological properties, while their contents are very low. In this study, the biosynthesis of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid in the cell suspension cultures of S. involucrata were regulated by feeding carbon sources and precursors, which resulted in a great increase of the contents and yields of the above three bioactive ingredients. After 16 days of fermentation, the yields of syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid reached 339.0, 225.3, 512.7 mg x L(-1), respectively. Meanwhile, their contents increased up to 67.9, 1.9, 10.6 times of wild medicinal material, respectively. The results provided a solid basis for further studies on application of cell suspension cultures of S. involucrata for large-scale production of bioactive compounds syringin, chlorogenic acid and 1,5-dicaffeoylquinic acid.
Cell Culture Techniques ; Cells, Cultured ; Chlorogenic Acid ; analysis ; metabolism ; Cinnamates ; analysis ; metabolism ; Glucosides ; analysis ; biosynthesis ; Phenylpropionates ; analysis ; Saussurea ; chemistry ; growth & development ; metabolism

OBJECTIVETo compare therapeutic effects between the normal rehabilitation and combined with manipulative method after arthroscopic capsular release for the treatment of severe frozen shoulder, and to evaluate the application value of manipulationp.

METHODSFrom March 2007 to July 2010,arthroscopic capsular release was performed in 48 cases (48 shoulders, 23 left side, 25 right side). All the patients were divided into two groups: control group (11 males and 15 females) and manipulation group (9 males and 13 females). The patients in the control group were treated with conventional rehabilitation procedure, and the patients in the manipulation group were treated with additional manipulation procedure. From the 2nd day after operation, the manipulation was performed for 20 minutes every time, twice daily, and it continued for 10 days. All the cases were followed up and the scale of American Shoulder and Elbow Surgeons Standardized Assessment Form (ASES self-report section) and the range of motion (ROM) were recorded.

RESULTSThe mean follow-up period was (12.54 +/- 5.78) months (ranging from 4 to 25 months). Both ASES scores and ROM in the manipulation group were better than those in the control group at the 1st month after operation, and the difference between the ASES scores and flexion of the shoulder were significant. However, there was no significan difference at the latest follow-up.

CONCLUSIONCompared with the conventional rehabilitative procedure, manipulation following arthroscopic capsular release could promote the process of joint rehabilitation and help the patient back to normal life earlier, but there is no evidence of long term advantage.

Arthroscopy ; Bursitis ; physiopathology ; surgery ; therapy ; Case-Control Studies ; Combined Modality Therapy ; Female ; Humans ; Joint Capsule Release ; Male ; Middle Aged ; Musculoskeletal Manipulations ; Range of Motion, Articular ; Treatment Outcome

OBJECTIVETo observe the effect of Ganoderma lucidum decoction in treating Russula subnigricans poisoning (RSP) patients.

METHODSThe 14 patients of RSP in the treated group were treated with GLD (GLD, one dose was prepared by 100 g of Ganoderma lucidum decocted with water to 600 ml), on the base of conventional treatment, and 11 patients received conventional therapy in the previous year were taken as control. The clinical efficacy and parameters in them were compared, including the urine N-acetyl-D-glucosaminidase (NAG, which reflects the injury of kidney), the red blood cell and protein in urine, the alanine transaminase (ALT, which reflects the injury of liver), and the aspartate aminotransferase (AST, which reflects the injury of heart).

RESULTSA better clinical cure-markedly improving rate was showed in the treated group as compared with the control group, P < 0.01. In the treated group, red blood cell in urine disappeared after 24 hrs treatment in the majority of patients, urinary protein reduced obviously and the other three parameters reached the peak at the 3rd day then lowered gradually. In the control group, all the parameters increased continuously. Comparison between the parameters at corresponding time in the two groups showed significant difference (P < 0.01), those in the treated group were markedly lower than those in the control group respectively.

CONCLUSIONGLD has good effect in treating RSP, could obviously lower the fatat rate of RSP.

Acetylglucosaminidase ; urine ; Adolescent ; Adult ; Aged ; Alanine Transaminase ; blood ; Aspartate Aminotransferases ; blood ; Drugs, Chinese Herbal ; therapeutic use ; Female ; Humans ; Male ; Middle Aged ; Mushroom Poisoning ; drug therapy ; Phytotherapy ; Reishi ; chemistry

Phytantriol (PT), ethanol (ET) and water were used to prepare in situ cubic liquid crystal (ISV2). The pseudo-ternary phase diagram of PT-ET-water was constructed and isotropic solution formulations were chosen for further optimization. The physicochemical properties of isotropic solution formulations were evaluated to optimize the composition of ISV2. In situ hexagonal liquid crystals (ISH2) were prepared based on the composition of ISV2 with the addition of vitamin E acetate (VitEA) and the amount of VitEA was optimized by in vitro release behavior. The phase structures of liquid crystalline gels formed by ISV2 and ISH2 in excess water were confirmed by crossed polarized light microscopy and small angle X-ray scattering, respectively. Rheological properties of ISV2 and ISH2 were studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using a dialysis membrane diffusion method. Pharmacokinetics was investigated by determination of sinomenine hydrochloride (SMH) concentration in synovial membrane after intra-articular injection of SMH-loaded ISH2 in adjuvant-induced arthritis rats. The optimal ISV2 (PT/ET/water, 64 : 16 : 20, w/w/w) loaded with 6 mg x g(-1) of SMH showed a suitable pH, injectable and formed a cubic liquid crystalline gel in situ with minimum water absorption in the shortest time. The optimal ISV2 was able to sustain the drug release for 144 h. The optimal ISH2 system was prepared by addition of 5% VitEA into PT in the optimal ISV2 system. This ISH2 (PT/VitEA/ET/water, 60.8 : 3.2 : 16 : 20, w/w/w/w) was an injectable isotropic solution with suitable pH. The new ISH2 was able to sustain the drug release for more than 240 h. Local pharmacokinetics study indicated that the retention time and AUC(0-∞) of ISH2 group were increased significantly compared with that of SMH solution group and the AUC(0-∞) of ISH2 group was 6.01 times higher than that of SMH solution group. The developed ISH2 was suitable for intra-articular injection that may apply to patients in the treatment of rheumatoid arthritis.
Animals ; Chemistry, Pharmaceutical ; Diffusion ; Ethanol ; Fatty Alcohols ; Gels ; Injections, Intra-Articular ; Liquid Crystals ; Morphinans ; administration & dosage ; chemistry ; Rats ; Rheology ; Water ; alpha-Tocopherol

Animals ; China ; epidemiology ; Epidemiologic Studies ; Molecular Epidemiology ; Rickettsia ; genetics ; isolation & purification ; Rickettsia Infections ; epidemiology ; transmission ; Ticks ; microbiology

Objective To obtain the gene fragment encoding human mannan-binding lectin (MBL)-associated serine protease-2 (MASP-2). Methods The target cDNA fragment was amplified from the total RNA extracted from human fetal liver tissue by RT-nested PCR, cloned into pGEM-T vector and identified by restriction analysis and sequencing. Results The cDNA fragment encoding MASP-2 polypeptide with the signal sequence was isolated, linked with pGEM-T vector and transformed into E.coli TG1. The restriction maps of the selected clones were consistent with those generated by computer analyses. The result of sequencing of one selected clone showed that its sequence was identical with that of reported human MASP-2 cDNA. Conclusion The human MASP-2 gene was successfully cloned, which prepares the ground for studying the molecular mecha- nisms by which MBL activates the complement lectin pathway and the mutations of MBL gene cause immunodeficiency.

Objective To obtain the gene fragment encoding human mannan-binding lectin (MBL)-associated serine protease-2 (MASP-2). Methods The target cDNA fragment was amplified from the total RNA extracted from human fetal liver tissue by RT-nested PCR, cloned into pGEM-T vector and identified by restriction analysis and sequencing. Results The cDNA fragment encoding MASP-2 polypeptide with the signal sequence was isolated, linked with pGEM-T vector and transformed into E.coli TG1. The restriction maps of the selected clones were consistent with those generated by computer analyses. The result of sequencing of one selected clone showed that its sequence was identical with that of reported human MASP-2 cDNA. Conclusion The human MASP-2 gene was successfully cloned, which prepares the ground for studying the molecular mecha- nisms by which MBL activates the complement lectin pathway and the mutations of MBL gene cause immunodeficiency.