Designing of natural product-like compounds using natural products as template structures is an important strategy for the discovery of new drugs. Gambogic acid (GA), which is a Garcinia natural product with a unique caged xanthone scaffold, inhibits potent antitumor activity both in vitro and in vivo. This review summarized the researches on the identification of the antitumor pharmacophore of GA, and the design, structural optimization and structure-activity relationship (SAR) of natural product-like caged xanthones based on it.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Biological Products ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Drug Screening Assays, Antitumor ; Garcinia ; chemistry ; Humans ; Molecular Structure ; Structure-Activity Relationship ; Xanthones ; chemical synthesis ; chemistry ; isolation & purification ; pharmacology

Adolescent ; Adult ; Child ; Child, Preschool ; China ; epidemiology ; Female ; Humans ; Immunity ; Infant ; Infant, Newborn ; Male ; Measles ; epidemiology ; immunology ; Measles Vaccine ; immunology ; Risk Factors ; Transients and Migrants ; Young Adult

OBJECTIVETo study the effect of two kinds of silane coupling agent on bond strength of resin-ceramic adhesive.

METHODSFour hundred and thirty-two ceramic samples were divided into 9 groups (48 per group), and in each group the ceramic surface was treated with r-methacryloxypropyletrimethoxysilane (MPTS) (50 g/L) in 99% ethanol (Primer A) and the mixture of hydrochloric acid (0.10 mol/L), phosphoric acid (0.05 mol/L) and acetic acid (0.01 mol/L) in 99% ethanol with the same volume (Primer B). Then the treated ceramic was bonded with resin cement (Link Max). The shear bond strength was tested after 5000 and 10 000 thermo-cycles and standing for 24 h.

RESULTSThe highest shear bond strengths [(19.5 ± 3.7) MPa, (15.7 ± 3.0) MPa and (14.6 ± 3.0) MPa] of the specimens were obtained with 0.05 mol/L hydrochloric acid. At acid solution of 0.10 mol/L, the specimens using hydrochloric acid [(10.6 ± 3.5) MPa] and phosphoric acid [(9.5 ± 2.7) MPa] showed remarkably higher strength than that using acetic acid [(6.3 ± 2.5) MPa, P < 0.05] after 10 000 thermo-cycles. When the concentration of acid solution was 0.05 mol/L, the shear bond strength of specimens from hydrochloric acid [(14.6 ± 3.0) MPa] was significantly higher than that using phosphoric acid [(6.3 ± 1.9) MPa] and acetic acid [(4.7 ± 1.8) MPa, P < 0.05]. When the concentration of acid solution reached 0.01 mol/L, the specimens using hydrochloric acid exhibited a dramatically increase in shear strength [(12.7 ± 3.2) MPa] compared with that using phosphoric acid [(2.3 ± 1.2) MPa, P < 0.05] and acetic acid [(1.5 ± 1.2) MPa, P < 0.05].

CONCLUSIONSThe maximum adhesive bond strength with highest durability was obtained using hydrochloric acid of 0.05 mol/L hydrolysis catalysts to treat siline couple agent.

Acetic Acid ; chemistry ; Adhesives ; chemistry ; Ceramics ; chemistry ; Dental Bonding ; Dental Stress Analysis ; Hydrochloric Acid ; chemistry ; Hydrolysis ; Materials Testing ; Methacrylates ; chemistry ; Phosphoric Acids ; chemistry ; Resin Cements ; chemistry ; Shear Strength ; Silanes ; chemistry ; Surface Properties

OBJECTIVEThe present study aimed to evaluate the accuracy of the factorial method for estimating energy needs in individuals living in China.

METHODSSixteen healthy female adults aged 22.1±1.2 years with a body mass index (kg/m(2)) of 20.4±1.7 were selected as subjects. In free-living conditions, energy expenditure (EE) was determined by using the factorial method. At the same time, the doubly labeled water method (DLW) was also used to measure energy expenditure of the subjects and served as the criterion method. EE predicted by the factorial method (EE(factorial)) was compared with the simultaneous measurement of EE by the validated DLW method (EE(DLW)).

RESULTSThere was excellent agreement between EE(factorial) (7.46±0.59 MJ/d) and EE(DLW) (7.64 ± 0.49 MJ/d), with a difference of -2.6±4.9% (-0.18±0.36 MJ/d). No significant differences were found between the two methods. EE(factorial) was highly correlated with EE(DLW) (r=0.795, P<0.001) and a good agreement for individuals was found by using the Bland and Altman test.

CONCLUSIONThe factorial method gives satisfactory estimates of EE for both groups and individuals living in China.

Adult ; China ; Energy Metabolism ; physiology ; Female ; Humans ; Motor Activity ; physiology ; Radioisotope Dilution Technique ; Young Adult

BACKGROUNDTo evaluate the safety of intracytoplasmic sperm injection (ICSI) with epididymal or testicular sperm, this study compared children born after ICSI treatment with epididymal or testicular sperm with children conceived after ICSI with ejaculated sperm.

METHODSThis retrospective study included 317 children born after ICSI with percutaneous epididymal sperm aspiration (PESA), 103 children born after ICSI with testicular sperm aspiration (TESA), and a control group of 1008 children born after ICSI with ejaculated sperm. All of the patients received their assisted reproductive treatment in the Reproductive Medicine Center of the First Affiliated Hospital of Zhengzhou University from January 2004 to December 2011. Data, such as the rate of stillbirths, perinatal mortality, gestational age, birth weight, and the rate of congenital malformations of the three groups, were compared.

RESULTSPESA and TESA children were not different from ICSI children in the rate of stillbirths, perinatal mortality, infant mortality rate, gestational age, the rate of prematurity, and the rate of malformations (P > 0.05). A slight increase in birth defects was reported in the TESA group compared with those in the control group, but there was no significant difference between the groups (P > 0.05).

CONCLUSIONICSI with epididymal or testicular sperm does not lead to more stillbirths or congenital malformations compared with ICSI using ejaculated sperm.

Adult ; Congenital Abnormalities ; epidemiology ; Epididymis ; Female ; Fetal Death ; epidemiology ; Follow-Up Studies ; Humans ; Infant, Newborn ; Male ; Pregnancy ; Retrospective Studies ; Sperm Injections, Intracytoplasmic

This study is aimed to investigate the effects of high intracellular Mg²⁺ on L-type calcium channel in guinea-pig ventricular myocytes. The cardiomyocytes were acutely isolated with enzyme digestion method. By adopting inside-out configuration of patch clamp technique, single channel currents of the L-type calcium channel were recorded under different intracellular Mg²⁺ concentrations ([Mg²⁺]i). In control group, which was treated with 0.9 mmol/L Mg²⁺, the relative activity of calcium channel was (176.5 ± 34.1)% (n = 7). When [Mg²⁺]i was increased from 0.9 to 8.1 mmol/L (high Mg²⁺ group), the relative activities of calcium channel decreased to (64.8 ± 18.1)% (n = 6, P < 0.05). Moreover, under 8.1 mmol/L Mg²⁺, the mean open time of calcium channel was shortened to about 25% of that under control condition (P < 0.05), but the mean close time of calcium channel was not altered. These results suggest that high intracellular Mg²⁺ may inhibit the activities of L-type calcium channel, which is mainly due to the shortening of the mean open time of single L-type calcium channel.
Animals ; Calcium Channels, L-Type ; physiology ; Guinea Pigs ; Magnesium ; physiology ; Myocytes, Cardiac ; physiology ; Patch-Clamp Techniques

OBJECTIVESTo study the roles of leptin in the development during puberty in girls and the its relationship with insulin (INS), growth hormone (GH), estradiol (E(2)) and testosterone (T).

METHODSOne hundred and fifty girls with simple obese aged 7 to 17 years, and 150 normal healthy girls and 150 girls with malnutrition matched for age (+/- 3 months) and height (+/- 2 cm) were selected. Serum levels of leptin, INS, GH, E(2) and T were measured for them.

RESULTSTheir serum level of leptin positively correlated with body mass index (BMI) and age. Serum level of leptin in girls increased steadily from Tanner stage B(1) to stage B(5). At Tanner stage B(2), serum level of leptin in the normal groups (7.72 microg/L) was not significantly different from that in those with malnutrition (7.36 microg/L), but significantly lower than that in the obese groups (12.85 microg/L). At other Tanner stages, there was significant difference in serum level of leptin among obese, normal and malnutrition groups. Serum level of leptin correlated negatively with serum GH and positively with serum INS, but not correlated with E(2) and T.

CONCLUSIONSLeptin may play a role in triggering development during puberty in girls. Serum level of leptin at Tanner stage B(2) may be the threshold dose to trigger the onset of puberty in girls. Quickly increasing level of leptin at Tanner stage B(5) may inhibit the increase of GH, which ushered the end of puberty in girls.

Adolescent ; Body Height ; physiology ; Body Mass Index ; Body Weight ; physiology ; Child ; Female ; Growth Hormone ; metabolism ; Humans ; Leptin ; blood ; physiology ; Puberty ; physiology ; Testosterone ; metabolism

OBJECTIVETo evaluate the clinical value of perioperative adjuvant chemotherapy in prevention of tumor recurrence and improvement of patient survival after liver transplantation for advanced hepatocellular carcinoma (HCC).

METHODSTwenty patients with advanced HCC (pTNM stages III and IV a) receiving liver transplantation with preoperative transcatheter arterial chemoembolization (TACE) and postoperative adjuvant chemotherapy (ADM+5-Fu+CDDP) were retrospectively reviewed in comparison with 16 patients receiving liver transplantation only for tumor recurrence, cumulative and tumor-free survivals. The feasibility and side-effects of the treatments were also studied.

RESULTSThe recurrence rate was lower in the perioperative treatment group than in non-treatment group (12/20, 60.0% vs 11/16, 87.5%, P<0.05). The 1- and 2-year overall survival rates were 70.8% and 47.1% for the chemotherapy group and 43.8% and 20.5% for the non-chemotherapy group respectively, showing significant differences between them (P<0.05). The 1- and 2-year tumor-free survival rates were 60.6%, 40.5% and 33.6%, 15.6% in the two groups, respectively, with also significant differences (P<0.05).

CONCLUSIONSPerioperative adjuvant treatment may significantly decrease the likeliness of tumor recurrence and prolong the survival of patients with advanced HCC after liver transplantation. Chemotherapy with ADM+5-Fu+CDDP can be effective and safe with only mild side-effects.

Adult ; Carcinoma, Hepatocellular ; drug therapy ; Chemotherapy, Adjuvant ; Female ; Humans ; Liver Neoplasms ; drug therapy ; Liver Transplantation ; Male ; Middle Aged ; Neoplasm Recurrence, Local ; Perioperative Care ; Retrospective Studies ; Survival Rate ; Treatment Outcome

OBJECTIVETo study the plasma homocysteine (Hcy) distributive characteristics in different sex and age groups of the community residents in Guangdong, and to analyze its associated factors as well as its effects on cerebral artery stenosis.

METHODSIn this study, we presented data concerning 2500 residents who had undergone a systematic health checkup,including clinical and biologic examinations. Plasma was saved from 1020 residents who were asymptomatic but having TCD examination. Hcy concentration was measured by fluorescence ration biochemical assay kit.

RESULTSThe average plasma Hcy levels of males (15.0 micromol/L+/-5.8 micromol/L) were significantly higher than those of females (12.4 micromol/L-I 3.9 micromol/L, P< 0.05). Hcy level increased parallel with age. The prevalence rate of hyperhomocysteinemia in males (47.2%) was higher than in females (23.2%). Hcy levels in MCA stenosis group (18.3 micromol/L+ 5.3 micromol/L) were significantly higher than that in control group (12.9 micromol/L+/- 4.6 micromol/L, P< 0.05). Based on logistic regression analysis, Hcy was only associated with sex and age, but not with blood lipids etc.

CONCLUSIONHcy levels were different in sex and age groups which emerged as independent predictors of hyperhomocysteinemia but had no association with blood lipids in the community residents, suggesting that hyperhomocysteinemia might worsen cerebral artery stenosis.

China ; epidemiology ; Female ; Homocysteine ; blood ; Humans ; Hyperhomocysteinemia ; epidemiology ; Male ; Prevalence ; Reference Values

OBJECTIVETo investigate the effects of three kinds of artificial dermal scaffolds on vascularization and scar formation of wounds in pigs with full-thickness burn.

METHODSEighteen Bama miniature pigs were divided into chitosan scaffold (CS) group, sulfonated carboxymethyl chitosan scaffold (SCCS) group, and acellular dermal matrix (ADM) scaffold group according to the random number table, with 6 pigs in each group. Every pig in all groups was inflicted with 4 or 8 full-thickness scald wounds on the back (totally 96 wounds). Forty-eight hours after injury, eschars of all wounds were excised. Twenty-four wounds in CS group were transplanted with double-layer artificial dermis of collagen-chitosan and silicone rubber, those in SCCS group with double-layer artificial dermis of collagen-sulfonated carboxymethyl chitosan and silicone rubber, and those in ADM scaffold group with ADM. The rest 24 wounds in the three groups were dressed with vaseline gauze as control group. After 2 weeks of treatment, all wounds of every group were covered with skin. In post treatment (scaffold transplantation or gauze covering) week (PTW) 1, 2, 3, and 4, gross condition of wound was observed, and specimens from central parts of wounds were harvested for observation and assessment of vessels or cells with positive expression of CD31, α smooth muscle actin (α-SMA), TGF-β(1) and TGF-β(3) with SP staining. Data were processed with one-way analysis of variance and LSD test.

RESULTS(1) Degree of vascularization in SCCS group was better than that in the other three groups. (2) The number of vessels with positive expression of CD31 in CS, SCCS, ADM scaffold, and control groups increased gradually from PTW 1 to PTW 3, and decreased in PTW 4. There were statistical differences among 4 groups from PTW 1 to PTW 4 (with F value respectively 24.005, 38.822, 25.274, 3.856, P < 0.05 or P < 0.01). The numbers of vessels that expressed CD31 in SCCS group from PTW 1 to PTW 3 were more than those in the other three groups (with P values all below 0.05). (3) The numbers of vessels that expressed α-SMA in CS, SCCS, and ADM scaffold groups from PTW 1 to PTW 3 showed the similar trend of change to those of vessels that expressed CD31, which increased gradually in control group from PTW 1 to PTW 4. There were obvious differences among 4 groups from PTW 1 to PTW 4 (with F value respectively 22.637, 28.087, 62.651, 18.055, P values all below 0.01). The number of vessels that expressed α-SMA in SCCS group from PTW 1 to PTW 4 was more than that in the other three groups (with P values all below 0.05). (4) From PTW 1 to PTW 4, the number of cells with expression of TGF-β(1) in CS group was respectively (127 ± 8), (167 ± 19), (170 ± 18), (144 ± 10) per 400 times visual field, that in SCCS group was respectively (171 ± 17), (207 ± 25), (130 ± 30), (69 ± 16) per 400 times visual field, that in ADM scaffold group was respectively (106 ± 8), (159 ± 17), (171 ± 11), (145 ± 11) per 400 times visual field, and that in control group was respectively (100 ± 20), (150 ± 18), (200 ± 14), (172 ± 20) per 400 times visual field. There were statistical differences among 4 groups from PTW 1 to PTW 4 (with F value respectively 29.675, 9.503, 13.107, 54.515, P values all below 0.01). Compared with those in SCCS group, the number of cells that expressed TGF-β(1) in the other three groups was decreased in PTW 1, 2 but increased in PTW 3, 4 (with P values all below 0.05). (5) The number of cells that expressed TGF-β(3) in 4 groups increased gradually from PTW 1 to PTW 3, and decreased or increased continually in PTW 4. There were statistical differences among 4 groups from PTW 1 to PTW 4 (with F value respectively 140.612, 945.850, 714.037, 119.147, P values all below 0.01). The number of cells with positive expression of TGF-β(3) in SCCS group from PTW 1 to PTW 4 was more than that in the other three groups (with P values all below 0.05).

CONCLUSIONSThe collagen-sulfonated carboxymethyl chitosan dermal scaffold can rapidly induce growth and maturation of blood vessels during wound healing after burn. It is beneficial for wound repair at early stage with inhibition of scar proliferation.

Acellular Dermis ; Animals ; Burns ; surgery ; Chitosan ; analogs & derivatives ; Cicatrix ; pathology ; Collagen ; Dermis ; transplantation ; Female ; Neovascularization, Physiologic ; Skin Transplantation ; Skin, Artificial ; Swine ; Tissue Scaffolds ; Wound Healing