Pentacyclic triterpenoids are a class of widespread natural compounds containing six isoprene structures with a wide range of pharmacological activities, including antibacterial, anti-inflammatory, antiviral, antitumor, immune regulation, etc. The structural modifications of pentacyclic triterpenoid natural products and the drug development have always been a hot research topic. This article reviews the recent progresses in the structural modifications, pharmacological effects, and clinical studies of different kinds of pentacyclic triterpenoid natural products.

Objective To investigate the changes of pulmonary capillary wedge pressure(PCWP) before and after off-pump coronary artery bypass graft(OPCABG) using transesophageal echocardiography(TEE). Methods Mitral valve flow(MVF) and pulmonary veinous flow(PVF) were measured in 46 patients before and after OPCAB using TEE and PCWP was detected by cardiac catheter. The correlations between indices derived from TEE and catheterization-measured PCWP and the differences before and after OPCAB were studied. Results There were obvious differences in the indices derived from TEE and PCWP which could reflect the left ventricular function. The most indices measured in PVF and MVF correlated with PCWP(r=(0.30)-(0.76),P

Objective To investigate the changes of peripheral insulin resistance after lipid infusion and the effect of N-acetylcystein(NAC) intervention.Methods Thirty-seven normal male SD rats,eight weeks old,were randomly divided into three groups,FFA group,NS group and NAC group(using into NAC 300 mg/(kg?d) two weeks before infusion).Catheters were implanted into right atrium via the jugular vein and left carotid artery.A technique for a 48-h infusion in unrestrained rats was used for triglyceride and heparin or saline infusion.The infusion period started on day 2 after surgery.48-h after infusion,we determined free fat acid(FFA),nitrotyrosine,malonaldehyde(MDA),reduced glutathione hormone(GSH) level in plasma.The glucose infusion rat(GIR) was measured by hyperinsulinemia euglycemic clamp to evaluated the perpherial insulin resistance.The expressions of IRS-1,IRS-2 gene in muscle were detected by real time PCR.Results(1)The FFA,nitrotyrosine and MDA con-centrations in FFA group were higher than that in NS group,but GSH level in plasma was lower.NAC intervention could reverse these effects.(2)GIR was decreased significantly in FFA group as compared with NS group[(8.34?1.8)mg/(min?kg)] vs[(13.56?1.7)mg/(min?kg)],(P

The borneol was included with β-CD and prepared Fufang Danshen intestinal adhesion pellets. GC method for determination of borneol in Fufang Danshen intestinal adhesion pellets was established to study its in vitro dissolution and make a comparison with the Fufang Danshen tablet, in this way, the rationality of dosage form was evaluated. The first method of dissolution determination was used for determining the in vitro dissolution of borneol in Fufang Danshen intestinal adhesion pellets in artificial intestinal juice, and Fufang Danshen tablet in artificial gastric juice and intestinal juice, respectively. Result shows: the concentration of borneol in Fufang Danshen intestinal adhesion pellets and Fufang Danshen tablet was 0.79% and 0.80%, respectively. Its in vitro dissolution was nearly 70% within 12 h in Fufang Danshen intestinal adhesion pellets, and in Fufang Danshen tablet, the dissolution was about 60% within 20 min and more than 90% within 40 min, and in artificial gastric juice, was less than 20% within 40 min but more than 80% till 150 min. Research suggests that in comparison with Fufang Danshen tablet, in vitro dissolution of borneol in the Fufang Danshen intestinal adhesion pellets showed an obvious sustained release behavior. The borneol in Fufang Danshen intestinal adhesion pellets was included with β-CD and prepared enteric preparations. To some extent, the stimulation on stomach and intestinal mucosa can be reduced and safety can be improved.
Bornanes ; adverse effects ; chemistry ; pharmacology ; Chemistry, Pharmaceutical ; methods ; Dosage Forms ; Drugs, Chinese Herbal ; adverse effects ; chemistry ; pharmacology ; Humans ; Intestinal Mucosa ; drug effects ; metabolism ; Models, Biological ; Solubility

OBJECTIVETo estimate the prevalence of subcretins in 8 minorities of Yunnan province and to provide scientific basis for public health policy-making, as well as for prevention and control of iodine deficiency disorders.

METHODSFour thousand two hundred and twenty-two minority school children aged 8-12 years selected from 29 schools in 8 minority counties were measured by Combined Raven's Test in China (CRT-C(2)) and Jinyi Psychomotor test Battery (JPB).

RESULTSAverage of intelligence quotient (IQ) on 4,222 children was 91 +/- 19. Among 277 pupils with IQ between 55 - 69, 119 of them showed abnormal on JPB test and 5.4% of the children was found to have Goiter under ultrasonography. Median level of urinary iodine was 466.9 microg/L, and the qualified rate of iodized salt was 94.9%.

CONCLUSIONThe estimated prevalence rate of subcretin was 2.8%.

Child ; Child Development ; China ; epidemiology ; Congenital Hypothyroidism ; epidemiology ; Ethnic Groups ; Female ; Humans ; Intelligence Tests ; Male ; Prevalence

Objectives To address whether menopause affects outcome of catheter ablation (CA) for atrial fibrillation (AF) by comparing the safety and long-term outcome of a single-procedure in pre-and post-menopausal women. Methods A total of 743 female patients who underwent a single CA procedure of drug-refractory AF were retrospectively analyzed. The differences in clinical presentation and outcomes of CA for AF between the pre-menopausal women (PreM group, 94 patients, 12.7%) and the post-menopausal women (PostM group, 649 patients, 87.3%) were assessed. Results The patients in the PreM group were younger (P<0.001) and less likely to have hypertension (P<0.001) and diabetes (P=0.005) than those in the PostM group. The two groups were similar with regards to the proportion of concomitant mitral valve regurgitation coronary artery disease, left atrium dimensions, and left ventricular ejection fraction. The overall rate of complica-tions related to AF ablation was similar in both groups (P=0.385). After 43 (16-108) months of follow-up, the success rate of ablation was 54.3%in the PreM group and 54.2%in the PostM group (P=0.842). The overall freedom from atrial tachyarrhythmia recurrence was simi-lar in both groups. Menopause was not found to be an independent predictive factor of the recurrence of atrial tachyarrhythmia. Conclusions The long-term outcomes of single-procedure CA for AF are similar in pre-and post-menopausal women. Results indicated that CA of AF appears to be as safe and effective in pre-menopausal women as in post-menopausal women.

This study was aimed to explore the role of human fetal bone marrow stromal cells (FBMSC) in combination with exogenous cytokines in supporting the in vitro expansion of cord blood mononuclear cells and the expression of CXCR4(+) and CD49d(+) in CD34(+) cells. Mononuclear cells (MNC) separated from cord blood (CB) were cultured in a serum-free support culture system with FBMSC or exogenous cytokines or both of them. On day 0, 6, 10 and 14, total cells were counted, CD34(+), CD34(+)CXCR4(+) and CD34(+)CD49d(+) cells were quantitated by FACS, and hematopoietic progenitor cells were assessed by semisolid culture assay. The results showed that after culturing for 14 days, CD34(+) cells, CD34(+)CXCR4(+) cells, CD34(+) CD49d(+) cells and colony forming unit (CFU) were significantly increased (P < 0.05). Compared with other groups, expansion multiple of CD34(+), CD34(+)CXCR4(+), CD34(+)CD49d(+) cells and CFU were higher than that in FBMSC and cytokine group (P < 0.05). It is concluded that the culture system used in this study can not only support the expansion of CB MNCs but also increase the number of hematopoietic stem and progenitor cells which has chemokine and adhesion capacity. This culture system may be a feasible way for in vitro culture of cord blood cells.
Antigens, CD34 ; blood ; Bone Marrow Cells ; cytology ; immunology ; Cell Proliferation ; drug effects ; Cells, Cultured ; Coculture Techniques ; Cytokines ; pharmacology ; Fetal Blood ; cytology ; Fetus ; Flow Cytometry ; Granulocyte-Macrophage Colony-Stimulating Factor ; pharmacology ; Humans ; Integrin alpha4 ; blood ; Interleukin-3 ; pharmacology ; Leukocytes, Mononuclear ; cytology ; immunology ; Receptors, CXCR4 ; blood ; Stromal Cells ; cytology ; immunology ; Time Factors

OBJECTIVETo construct a morphine tolerance model in primarily cultured striatal neurons, and screen the differentially expressed genes in this model using suppression subtractive hybridization (SSH).

METHODSSbtracted cDNA libraries were constructed using SSH from normal primarily cultured striatal neurons and long-term morphine treated striatal neurons (10-5 mol/L for 72 hours). To check reliability of the cell culture model, RT-PCR was performed to detect the cAMP-responsive element-binding protein (CREB) mRNA expression. The subtracted clones were prescreened by PCR. The clones containing inserted fragments from forward libraries were sequenced and submitted to GenBank for homology analysis. And the expression levels of genes of interest were confirmed by RT-PCR. Results CREB mRNA expression showed a significant increase in morphine treated striatal neurons (62.85 ± 1.98) compared with normal striatal neurons (28.43 ± 1.46, P < 0.01). Thirty-six clones containing inserted fragments were randomly chosen for sequence analysis. And the 36 clones showed homology with 19 known genes and 2 novel genes. The expression of 2 novel genes, mitochondrial carrier homolog 1 (Mtch1; 96.81 ± 2.04 vs. 44.20 ± 1.31, P < 0.01) and thymoma viral proto-oncogene 1 (Akt1; 122.10 ± 2.17 vs. 50.11 ± 2.01, P < 0.01), showed a significant increase in morphine-treated striatal neurons compared with normal striatal neurons.

CONCLUSIONSA reliable differential cDNA library of striatal neurons treated with long-term morphine is constructed. Mtch1 and Akt1 might be the candidate genes for the development of morphine tolerance.

Analgesics, Opioid ; pharmacology ; Animals ; Cells, Cultured ; Corpus Striatum ; cytology ; Drug Tolerance ; physiology ; Gene Expression Profiling ; Gene Library ; Molecular Sequence Data ; Morphine ; pharmacology ; Neurons ; cytology ; drug effects ; Nucleic Acid Hybridization ; methods ; Rats ; Rats, Wistar ; Reverse Transcriptase Polymerase Chain Reaction ; methods

Objective: To discuss and compare the plasma pharmacokinetics after three oral Panax notoginseng saponin (PNS) administrations in beagle dogs. PNS is the main active ingredient of the traditional Chinese medicine (TCM) Panax notoginseng. Although its outstanding therapeutic efficacy has been demonstrated by various researchers, its broader application is restricted by the low bioavailability of PNS.Methods: An ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous quantification of notoginsenoside R1, ginsenoside Rg1, ginsenoside Rb1, ginsenoside Rd, and ginsenoside Re in beagle dog plasma was developed and validated. The plasma samples were subjected to liquid-liquid extraction with acetone and methanol, and separated on an ACQUITY C18 column (100 × 2.1 mm ID, 1.7μm) using acetonitrile and water as the mobile phase with a run time of 4.5 min. Results: The analytes were detected without interference in Selected Reaction Monitoring mode with positive electrospray ionization. The validated method was successfully used in comparative pharma-cokinetic studies of the five saponins in beagle dogs after oral administration of three PNS preparations. Blood samples were collected up to 192 h after administration and pharmacokinetic parameters were calculated using DAS 3.20 and SPSS 17.0. The AUC0-t values of Re and R1 were significantly higher in soft capsules than in hard capsules. However, the AUC0-t values between hard and soft capsules were not significantly different for the other three components—Rb1, Rd and Rg1. Conclusion: Our intuitive analysis suggests that the bioavailability of PNS in soft capsules is greater than in hard capsules.

Four crystalline forms of clopidogrel bisulfate were characterized by analytical techniques. Aiming to research the absorption characteristics of clopidogrel bisulfate polymorphs after taken orally by rat, and to estimate the influence of crystal form to pharmacodynamic action, four crystalline forms of clopidogrel bisulfate were administered intragastrically to rats, and high performance liquid chromatography (HPLC) was used to measure the contents of clopidogrel bisulfate and its metabolite in rat plasma. The metabolite of clopidogrel bisulfate was detected in rat plasma. There were significant deviations among four crystalline forms in the areas under curve of the metabolite of clopidogrel bisulfate. We concluded that the different crystal forms of clopidogrel bisulfate showed different pharmacokinetic characteristics, which might affect pharmacodynamic action.
Absorption ; Administration, Oral ; Animals ; Area Under Curve ; Calorimetry, Differential Scanning ; Chromatography, High Pressure Liquid ; Crystallization ; Male ; Platelet Aggregation Inhibitors ; administration & dosage ; chemistry ; pharmacokinetics ; Random Allocation ; Rats ; Rats, Wistar ; Spectrophotometry, Infrared ; Ticlopidine ; administration & dosage ; analogs & derivatives ; blood ; chemistry ; pharmacokinetics ; X-Ray Diffraction