Ergosta-4,6,8(14),22-tetraen-3-one (ergone) is one of main components in many medicinal fungi. Ergone has been reported to possess the activities of diuresis, cytotoxicity, antitumor, immunosuppression, as well as treatment of chronic kidney disease. According to reported literatures, an overview of spectroscopy characteristics, content determination, pharmacological activity and pharmacokinetics, etc. for ergone is presented in this review. Furthermore, the present review can provide a certain reference value for the further study and development of ergone.
Animals ; Cholestenones ; chemistry ; pharmacokinetics ; pharmacology ; Drugs, Chinese Herbal ; chemistry ; pharmacokinetics ; pharmacology ; Humans

Metabonomics was employed to investigate the effect of Angelica sinensis volatile oil (ASVO) to the endogenous metabolites of normal rats, and to reveal the possible ways of metabolism in rats caused by ASVO. The fifty male Waster rats were randomly divided into five groups (each consists of 10 rats), such as control group, high dose group of ASVO, middle dose group of ASVO, low dose group of ASVO, and Aspirin group. They were given 0.9% saline, 0.352 mL x kg(-1) ASVO, 0.176 mL x kg(-1) ASVO, 0.088 mL x kg(-1) ASVO and ASP respectively with the equal volume of 0.2 mL. Drugs and vehicle were given for 3 successive days. The urine was collected at 12, 24, 36, 48 h after modeling with metabolic cages. Rat urine metabolic fingerprint in different stages was analyzed using GC-MS, based on which the principal component analysis (PCA)and orthogonal partial least-squares discriminant analysis (OPLS-DA) models were established for metabonomic analysis. Potential biomarkers were screened by using variable importance in the projection (VIP) and T test. It was revealed that the middle dose of ASVO at 36 h induces a substantial change in rat urine. Compared with control group, seven kinds of endogenous metabolites in ASP group and ASVO group change significantly (P < 0.05), among which aconitic acid, succinic acid, citric acid, alpha-ketone glutaric acid, glycine and malic acid content had an upward trend (P < 0.05) and prostaglandin content had a downward trend (P < 0.01). The mechanism of ASVO and ASP have the similarity. It is likely that ASVO intervenes the metabolic process by affecting the energy, amino acid and lipid metabolism. Our work also indicates that rats administrated with ASVO can increase the energy metabolism of the body, induce the production of inflammatory substances and strengthen the body's immune ability. The result has also provide a proof for futher interpret ASVO pharmacological effects.
Angelica sinensis ; chemistry ; metabolism ; Animals ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; analysis ; metabolism ; pharmacology ; Energy Metabolism ; drug effects ; Lipid Metabolism ; drug effects ; Male ; Metabolomics ; Oils, Volatile ; analysis ; metabolism ; pharmacology ; Plant Oils ; analysis ; metabolism ; pharmacology ; Rats ; Rats, Wistar ; Urine ; chemistry

OBJECTIVETo develop a colon-specific prodrug of Indomethacin microbially triggered, carry out in vitro/in vivo evaluation of drug release, and appraise its inhibitory effect on liver metastasis from colon cancer.

METHODSIndomethacin prodrugs were synthesized and characterized by FTIR and NMR, and dissolution test simulating gastrointestinal tract was employed to screen the colon-specific prodrug. Then, the pharmacokinetic profile of portal vein and peripheral blood in Sprague-Dawley rats was studied. Lastly, the inhibitory effect on liver metastasis from colon cancer in nude mice was observed.

RESULTSThe chemical structure characterized by FTIR and NMR demonstrated that six kinds of indomethacin-block-amylose with different drug loading (IDM-AM-1-6) were synthesized, among which IDM-AM-3 was degraded 1.3%, 9.3% and 95.3%, respectively, in simulated gastric fluid for 4 h, small intestine for 6 h, and colon for 36 h. The pharmacokinetic test of IDM-AM-3 showed that absorption was delayed significantly (P < 0.01), peak time [(11.35 + or - 2.45) h], elimination half-life [(16.74 + or - 4.04) h] and mean residence time [(22.27 + or - 0.52) h] were significantly prolonged (P < 0.01), as well as peak serum concentrations [(9.69 + or - 2.40) mg/L] and AUC(0-t) [(236.7 + or - 13.1) mg x L(-1) x h] were decreased markedly (P < 0.01) as compared with those of IDM regarding to portal vein. Additionally, its AUC(0-t) in peripheral blood was remarkably lower than that in Portal vein (P < 0.01). The tumor suppression observation showed that it could remarkably reduce the number of liver metastases in contrast to IDM (P < 0.05).

CONCLUSIONColon-specific IDM-AM-3 possesses advantage of sustained release in portal vein providing some experimental basis for colon-specific delivery system applied to sustained release in the portal vein.

Amylose ; administration & dosage ; chemical synthesis ; pharmacokinetics ; therapeutic use ; Animals ; Colon ; metabolism ; Colonic Neoplasms ; pathology ; Delayed-Action Preparations ; Drug Delivery Systems ; HT29 Cells ; Humans ; Indomethacin ; administration & dosage ; chemical synthesis ; pharmacokinetics ; therapeutic use ; Liver Neoplasms ; prevention & control ; secondary ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Neoplasm Transplantation ; Prodrugs ; administration & dosage ; chemical synthesis ; pharmacokinetics ; therapeutic use ; Random Allocation ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo study the epidemiological characters and risk factors of renal calculi in Shenzhen for future intervention.

METHODSRisk factors of renal calculi were analyzed by factor analysis and linear structural relation model, followed by fitting and evaluating the model.

RESULTSThe prevalence rates of renal calculi were 8.00% and 5.12% in males and females. The results of LISEREL showed that the total effect of age and sex affecting the development of renal calculi was 0.4614, with directly effect 0.3600 and indirect 0.1014. The direct effects of blood uric acid, blood calcium and body mass index, blood cholesterol, blood sugar were 0.3400 and 0.3200 respectively. The indirect effect of education, exercise and dietary habit affected the development of renal calculi through index of biochemistry and obesity, were -0.0416 and 0.1882.

CONCLUSIONSex, age, obesity and high blood cholesterol, high blood sugar, high blood uric acid, high blood calcium were the direct influencing factors to renal calculi. At the same time, education, exercise and dietary habit were also associated with the disease.

Age Factors ; Blood Glucose ; metabolism ; Body Constitution ; physiology ; Calcium ; blood ; China ; epidemiology ; Cholesterol ; blood ; Exercise ; physiology ; Feeding Behavior ; physiology ; Female ; Humans ; Kidney Calculi ; epidemiology ; Linear Models ; Male ; Prevalence ; Risk Factors ; Sex Factors ; Social Class ; Socioeconomic Factors ; Uric Acid ; blood

OBJECTIVETo explore the clinical application characteristics of sural neurocutaneous island flaps.

METHODSSural neurocutaneous island flaps were used to repair the skin defect accompanied bone and tendon exposure in the lower leg, around the ankle and foot in 21 cases, including 4 cases to repair the foreside of the foot back . Direct flap was used in 5 cases and reverse flap in 16 cases. Meanwhile the coverage and formation of sural nerve were surveyed together with the starting point of peroneal perforator.

RESULTSAll the 21 sural flaps were survived, including sural nerve (18 cases) anastomose 12 cases, single trunk 4 cases, double trunk 2 cases. The anastomose site of medial sural cutaneous nerve and the communicating branch of lateral sural cutaneous nerve was at the point of 11 - 14 cm above the ankle in 12 cases. The lower was the anastomose site, the shorter was the sural nerve. The site is 4 - 7 cm above the ankle in 15 out of 18 sural nerve perforator branch cases, and the other 3 cases is 10, 11, 11.5 cm above the ankle respectively.

CONCLUSIONSSural neurocutaneous island flaps are easy to separate. Major arteries are not injured. It is the ideal flap to repair the skin defect accompanied by bone and tendon exposure in lower leg, around ankle and foot. The nerve must be anastomosed when repairing the heel.

Adult ; Aged ; Arteries ; surgery ; Female ; Humans ; Male ; Middle Aged ; Reconstructive Surgical Procedures ; Skin Transplantation ; Sural Nerve ; surgery ; Surgical Flaps ; blood supply ; innervation ; Young Adult

OBJECTIVETo explore the clinical application of the expanded cross-leg flap for repairing instep soft tissue defects with bone exposure.

METHODSThe expanded cross-leg flap was used to repair instep defects in 10 patients. After flap transferring the donor site was closed directly without skin grafting.

RESULTSSatisfactory results were achieved in all the cases. The flaps survived well. The donor site had less scar and kept good appearance.

CONCLUSIONSThe expanded cross-leg flap is a better choice for repairing the soft tissue defects of the instep. It is simple and easy with less trauma to the donor site. After the operation, both the recipient and the donor areas had good appearance.

Adult ; Aged ; Female ; Foot Injuries ; surgery ; Humans ; Male ; Middle Aged ; Skin Transplantation ; methods ; Soft Tissue Injuries ; surgery ; Surgical Flaps ; Tissue Expansion ; Young Adult

This study was aimed to retrospectively analyze and compare the clinical curative efficacy of patients with hematologic malignancies after G-CSF-mobilized sibling HLA-matched (sm) peripheral blood hematopoietic stem cell transplantation (sm-allo-PBHSCT) and sm-allo-PBHSCT combined with bone marrow transplantation (BMT). 100 patients received sm-allo-HSCT in a single center from October 2001 to October to 2010, included 38 patients received sm-allo-PBHSCT and 62 patients received sm-allo-PBHSCT combined with BMT. The myeloablative or reduced intensity conditioning regimens were chosen according to the condition of patients. All patients received standard cyclosporine (CsA) and mycophenolate mofetil (MMF) as prophylaxis for GVHD. The results showed that the rapid hematopoietic reconstitution was observed in all patients. The median time of ANC ≥ 0.5 × 10(9)/L in both groups were 12 days, the median time of platelet count ≥ 20 × 10(9)/L was 15 days in sm-allo-PBHSCT group and 16 days in sm-allo-PBHSCT + BMT group. The incidence of acute GVHD, acute GVHD of III-IV grade and chronic GVHD in sm-allo-PBHSCT and sm-allo-PBHSCT + BMT groups were 37.1% and 34.2%, 7.89% and 8.06%, 36.11% and 41.38% respectively, there were no statistical differences. The relapse rates were similar in two groups (sm-allo-PBHSCT 13.16% vs sm-allo-PBHSCT + BMT 12.9%). The 3-year disease-free survivals in sm-allo-PBHSC and sm-allo-PBHSCT + BMT groups were 57.1 ± 8.7% and 61.3 ± 6.4% respectively (p = 0.852). The 2-year overall survival of high-risk patients was 41.4 ± 12.8% in sm-allo-PBHSCT group, while 60.9 ± 9.6% in sm-allo-PBHSCT + BMT group (p = 0.071). It is concluded that the rhG-CSF mobilized sibling matched allo-PBHSCT + BMT is superior to the rhG-CSF mobilized sibling matched allo-PBHSCT in increasing the overall survival of high-risk hematologic malignancies.
Adolescent ; Adult ; Aged ; Bone Marrow Transplantation ; Child ; Child, Preschool ; Female ; Granulocyte Colony-Stimulating Factor ; therapeutic use ; HLA Antigens ; immunology ; Hematologic Diseases ; immunology ; therapy ; Humans ; Male ; Middle Aged ; Peripheral Blood Stem Cell Transplantation ; Retrospective Studies ; Siblings ; Tissue Donors ; Young Adult

OBJECTIVETo observe the ability of dengue virus type 1-4 envelope domain III fusion protein to inhibit virus infection and analyze the neutralizing ability of polyclonal antibodies against rE III.

METHODSAfter being connected by linker peptide, E III protein of Dengue virus serotypes 1-4 were expressed in E coli BL21 (DE3) then purified. Fusion proteins were verified by Western Blot and ELISA. Rabbits were immunized with fusion proteins to produce anti-rE III serum. The activity of anti-rE III serum were detected through indirect immunofluorescence assay test. Inhibition of dengue virus type 1 to 4 infection in BHK-21 cells by rE III fusion protein were tested. Neutralizing activity of anti-rE III serum was analyzed.

RESULTSDengue virus type 1 to 4 envelope domain III recombinant fusion protein was expressed in E coli BL21 and purified successfully. Then rE III fusion protein and anti-rE III serum were analyzed respectively and rE III fusion protein can effectively inhibit dengue virus type 1 to 4 from infecting BHK cells. The anti-rE III serums can neutralize dengue virus type 1 to 4 but with different neutralizing titer.

CONCLUSIONDengue virus type 1-4 envelope domain III fusion protein can directly inhibit DV infection. Antibodies induced by rE III fusion proteins can neutralize dengue virus type 1-4.

Animals ; Blotting, Western ; Cells, Cultured ; Dengue Virus ; classification ; drug effects ; growth & development ; Enzyme-Linked Immunosorbent Assay ; Escherichia coli ; genetics ; Gene Fusion ; genetics ; Gene Products, env ; genetics ; metabolism ; Immunization ; Rabbits ; Recombinant Fusion Proteins ; genetics ; immunology ; metabolism ; pharmacology ; Recombinant Proteins ; biosynthesis ; pharmacology ; Viral Envelope Proteins ; genetics ; immunology ; metabolism ; Virus Replication ; drug effects ; physiology

OBJECTIVETo investigate the effects of advanced oxidative protein products (AOPP) on the proliferation, apoptosis and matrix metalloproteinase-1 (MMP-1) synthesis of the human gingival fibroblast (HGF). To explore the possible mechanism of the periodontal destruction acceleration in diabetes through AOPP-mediated oxidative stress.

METHODSHGF were isolated by both tissue explant cultivation technique and enzyme digestion method. The culture media with 5, 50, 100 mg/L AOPP-HAS were added into each experimental group, but the culture media in the control group didn't contain AOPP-HAS. MTT colorimetric assay and ELISA were used to measure the changes of HGF proliferation and the levels of MMP-1 protein from HGF at different time periods, respectively. Seventy-two hours after co-culture with 50 mg/L AOPP-HSA, cell apoptosis was detected by flow cytometry with Annexin V/PI staining.

RESULTSCompared to the control group, the growth inhibition rate of HGF in 5, 50, 100 mg/L AOPP-HSA group was significantly different (P < 0.05). The peak value appeared at 48 hours of co-culture [(19.01 +/- 6.28)%, (30.48 +/- 5.75)%, (39.75 +/- 4.60)%, respectively]. There was a dose-dependent relationship between the growth inhibition rate and AOPP-HSA. No significant difference was detected on the apoptotic level between experimental group and the control (P > 0.05). The MMP-1 synthesis in 0.5, 5, 50, 100 mg/L AOPP-HAS group [(55.61 +/- 1.06), (65.78 +/- 4.04), (79.24 +/- 3.09), (89.76 +/- 28.88) mg/L, respectively] was significantly higher than that in the control [(34.90 +/- 3.15) mg/L] after 72 hours co-culture (P < 0.05). There was a dose-dependent relationship between MMP-1 and AOPP-HSA.

CONCLUSIONSAOPP may inhibit the proliferation of HGF and such effect was not achieved through apoptosis. AOPP may increase collagen degradation by promoting MMP-1 synthesis and thus may accelerate periodontal destruction process in diabetes.

Apoptosis ; drug effects ; Blood Proteins ; metabolism ; Cell Proliferation ; drug effects ; Cells, Cultured ; Gingiva ; cytology ; drug effects ; Humans ; Matrix Metalloproteinase 1 ; metabolism ; Oxidation-Reduction ; Oxidative Stress

Objective To observes the change of early effective biomarkers of endothelial injury with lowarsenic exposure in drinking water. MethodsNinety rurad residents, who had lived in Yanhe village, Xuyi county and Jiangsu province for at least 10 years, were recruited by simple random sampling in this study. The level of arsenic in their household shallow well were divided into three groups, which were ＜ 10 (32 people), 10 - 50(28 people) and ＞ 50 μg/L(30 people). Blood samples from individuals were collected. Malondialdehyde(MDA) in human plasma, which is considered as the most important marker for monitoring lipid peroxidation, was determined as conjugate with tetrabutylammonium hydrogen sulphate(TBA). The level of anti-superoxide anion radical(O-·2),C-reactive protein(CRP) and NO in human plasma was measured with colorimetry, turbidimetry and nitric acid reductase, respectively. The number of circulating endothelial progenitor cells(CEPCs) in peripheral blood was analyzed by CD133+/KDR+ antibodies and flow cytometry. Results Ninety cases underwent questionnaires. Between the groups, the difference of the levels of MDA (61.1, 65.5, 67.5 μmol/kg), O-·2 (4774.6, 5143.3, 4736.0 U/kg) ,CRP[(5.92 ± 2.44), (5.11 ± 2.40), (5.55 ± 2.96)mg/L], and NO[(659.8 ± 387.5), (667.4 ± 486.6), (762.1 ±763.2)μmol/kg], was not statistically significant (F =0.00, 0.46, 0.80, 0.47, all P ＞ 0.05). The difference of the number of CEPCs in different groups of arsenic in drinking water was statistically significant(0.96 x 10-5, 0.77 x 10-5,1.59 x 10-5, F=5.08, P＜ 0.05), where ＜ 10, 10 - 50 μg/L groups were significantly lower than ＞ 50 μg/L group (q =4.58, 6.65, all P ＜ 0.05). ConclusionsThe number of CEPCs in peripheral blood changes significantly with lower-arsenic exposure, whereas there are no obvious changes with the markers of oxidized damage and inflammation. This is the first human demonstration showing that lower-arsenic exposure may cause endothelial injury.