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

Yunnan Strain Information System has been developed by using the Programming Lan guage and Database Engine It includes information of over 10,000 strains that are stored in Yunnan University Institute of Microbiology Strain Library The S ystem makes a convenience for management of Strain Library and supply i mportant information for study these

2cm~2.Conclusions The auto-cranial pedicle flap via endonasal repairing blow-out fractures of or- bital inferior wails is an effective technique.The results are good for improving eye movement especially for fracture ranged≤2cm~2. (Ophthalmol CHN,2007,16:388-390)

· AIM: To investigate the effect of β1-integrin overexpression on the apoptosis of rabbit corneal epithelial cells and the related mechanism. · METHODS: The plasmid expressing β1-integrin-GFP fusion protein was constructed by polymerase chain reaction (PCR), and this plasmid (β1 group) or the empty vector (mock group) was transfected into rabbit corneal epithelial cells, respectively. The expression of β1-integrin-GFP fusion gene was confirmed by reverse transcription-polymerase chain reaction (RT-PCR) and Western blot. The adhesion of transfected cells to extracellular matrix (ECM) proteins was determined by adhesion assay. The apoptosis of rabbit corneal epithelial cells was assayed by Hoechst 33342 staining and DNA ladder. The phosphorylation of mitogen-activated protein (MAP) kinase was examined by Western blot. · RESULTS: Rabbit corneal epithelial cells overexpressing β1 -integrin-GFP fusion gene were successfully established. Compared with mock group, β1-integrin transfection significantly promoted the adhesive of rabbit corneal epithelial cells to ECM proteins such as laminin, fibronectin, collagen Ⅰ and collagen Ⅳ. Β1-integrin overexpression inhibited apoptosis and induced MAP kinase phosphorylation in rabbit corneal epithelial cells (P<0.05).· CONCLUSION: These data suggest that overexpression of β1-integrin confers resistance to apoptosis in rabbit corneal epithelial cells, and MAP kinase pathway may play an important role in this process.

Objective To investigate knowledge, attitude and practice (KAP) on schistosomiasis control in transmission-interrupted areas in order to provide basis for making out intervention strategies of preventing re-epidemic of schistosomiasis. Methods A questionnaire survey was carried out for residents’ KAP on schistosomiasis control in the transmission-interrupted areas. A total of 608 residents were surveyed. Results The residents’ understanding rates of each item of schistosomiasis control were under 25.00% without exception. Residents refusing schistosomiasis examination, never surveying snails and never reporting snails accounted for 52.30%, 95.23% and 97.86% respectively. Conclusions Residents treat schistosomiasis control with indifference in transmission-interrupted areas. Therefore, intervention strategies of pertinent health education should be adopted to improve residents’ compliance to schistosomiasis examination and snail survey and report, and to prevent schistosomiasis re-epidemic.

OBJECTIVETo investigate the effect of a phosphorothioate antisense oligodeoxynucleotide "ASOND" combined with cis-Diamminedichloroplatinum (DDP), 5-fluorouracil (5-FU) and adriamycin (ADM) respectively on inhibiting the proliferation of HepG2 cells.

METHODSA phosphorothioate antisense oligodeoxynucleotide (5'-ACTCACTCAGG CCTCAGACT-3') targeted to human telomerase reverse transcriptase (hTERT) mRNA, which named cantide, was synthesized. ASODN was transfected into HepG2 by lipofectin. And cell growth activity was evaluated by MTT assay. SAS software and Jin Zhengjun Method were used to evaluate the interaction of ASODN and these chemotherapeutic drugs.

RESULTSCombination treatments with 0.1micromol/L ASODN reduced the IC50 of DDP, 5-FU and ADM from 1.07, 4.15 and 0.29microg/ml to 0.25, 1.52 and 0.12microg/ml respectively. The inhibitory ability of combination treatments on HepG2 cells was higher than that of these drugs alone (F=66.92, 25.96, 8.56, P<0.001). And synergism (Q>or=1.15) was observed at the lower concentration of DDP (

CONCLUSIONASODN may enhance therapeutic effectiveness of chemotherapeutic drugs in human hepatocellular carcinoma cells.

Antineoplastic Agents ; administration & dosage ; Cell Line, Tumor ; Cisplatin ; administration & dosage ; DNA-Binding Proteins ; Doxorubicin ; administration & dosage ; Drug Synergism ; Fluorouracil ; administration & dosage ; Humans ; Liver Neoplasms ; drug therapy ; Oligodeoxyribonucleotides, Antisense ; administration & dosage ; Telomerase ; antagonists & inhibitors ; genetics

OBJECTIVETo investigate the effect of ursolic acid (UA) on the alloxan-induced myocardial fibrosis in mice and discuss the possible mechanism.

METHODSDiabetes was produced by a single injection of alloxan (70 mg/kg, i.v.) in mice. The mice were randomly divided into four groups: normal control group, model group, ursolic acid group (UA, 35 mg/kg, p.o.) and benazepril group (5 mg/kg, p. o.), and continuous administrated for 8 weeks. The blood glucose was measured 24 hours after the last administration. Detected the specific biochemical of myocardial tissue: superoxide dismutase (SOD), malondialdehyde (MDA) and hydroxyproline(HYP). Using masson staining to observe the morphology of the myocardial tissue. Immunohistochemistry was employed to determine the protein levels of TGF-beta1.

RESULTSCompared to normal group, the blood glucose, heart index, myocardial tissue MDA, HYP level were increased, and SOD activities were decreased in the diabetic mice, Masson stain showed that myocardial cells disarranged, myocardial collagen fibrosis hyperplasia. Meanwhile, the protein expression of TGF-beta1 was increased in model group. The UA group improved all the above significantly.

CONCLUSIONUA improves the myocardial collagen fibrosis in diabetic mice induced by alloxan, its mechanism may be related to inhibiting the expression of TGF-beta1 and antioxidation.

Animals ; Blood Glucose ; Collagen ; metabolism ; Diabetes Mellitus, Experimental ; metabolism ; pathology ; Fibrosis ; Hydroxyproline ; metabolism ; Male ; Malondialdehyde ; metabolism ; Mice ; Mice, Inbred Strains ; Myocardium ; metabolism ; pathology ; Oxidative Stress ; Superoxide Dismutase ; metabolism ; Transforming Growth Factor beta1 ; metabolism ; Triterpenes ; pharmacology

OBJECTIVETo investigate the influence of total flavonoids of epimedium (TFE) on the streptozocin (STZ)-induced kidney injury in diabetic rats and discuss the possible mechanism.

METHODSDiabetes was produced by a single injection of streptozocin (40 mg/kg, iv) in male SD rats. The rats were randomly divided into three groups (n = 10): control group, model group and TFE group (100 mg/kg, ig). Animals were sacrificed 12 weeks later. The level of blood glucose, blood urea nitrogen (BUN) and creatinine (Cr) as well as the renal index were determined. Detect the specific biochemical of renal tissue: superoxide dismutase (SOD), malondialdehyde (MDA). Use masson staining to observe the morphology of the renal tissue. Immunohistochemistry was employed to determine the protein levels of transforming growth factor-beta1 (TGF-beta1).

RESULTSCompared to control group, the enhancement of blood glucose, renal index, BUN and Cr was found in model group, which was significantly attenuated by treatment with TFE. Meanwhile, elevated MDA level in renal tissue as well as decreased SOD activities in renal tissue were significantly remitted by TFE. Furthermore, TFE decreased the expression of TGF-beta1.

CONCLUSIONTFE can evidently relieve renal damage in rats with diabetic nephropathy induced by STZ, which might be related to antioxidation and modulating the expression of TGF-beta1 protein.

Animals ; Diabetes Mellitus, Experimental ; metabolism ; Diabetic Nephropathies ; metabolism ; prevention & control ; Epimedium ; chemistry ; Flavonoids ; pharmacology ; Kidney ; drug effects ; metabolism ; Male ; Rats ; Rats, Sprague-Dawley

Undifferentiated and differentiated 3T3-L1 adipocytes were treated with 100 ng/ml tumor necrosis factor-?(TNF-?),and peroxisome proliferator-activated receptor-?2 (PPAR-?2) mRNA expression and adiponectin secretion in cultured cells were measured.The results showed that TNF-?suppressed PPAR-?2 mRNA expression and adiponeetin secretion in 3T3-L1 adipocytes (P

BackgroundIron-containing foreign body trapped in the eyeball wall without affecting the opticus occurs occasionally in clinic. Operation always is performed in an attempt to avoid the deposition of rust in different tissues of the eye-balls. However,a few animal experimental studies showed that a small foreign body does not affect the retina and opticus in the period of three months. The question of whether surgery needs to be carried out is worth discussion. ObjectiveThe aim of this study was to evaluate the influence of posterior intrascleral iron foreign body on the rabbit retina and opticus. MethodsTwelve healthy adult Japan flap-eared white rabbits were randomly divided into two groups. Medium carbon iron with rust or without rust( size of 2. 0 mm × 1. 0 mm×0. 2 mm) were implanted into the posterior sclera of the left eye to create the animal model with iron foreign body in the eyeball wall. The cornea, anterior chamber, crystalline lens, vitreous and fundus of the rabbits were observed under a slit lamp microscope 1weekbeforeoperationand 1week, 2weeks, 1monthand 3months after operation.Flash electroretinogram(F-ERG) and flash visual evoked potential (F-VEP) were recorded at the time points mentioned above. All the rabbits were sacrificed and the eye balls were extracted at the end of the experiment, and the position of the iron foreign body was determined. The histopathological examinations of the retina and opticus were performed under the light microscope. This experiment complied with the Regulations for the Administration of Affair Concerning Experimental Animals by State Science and Technology Commission. ResultsThere were no statistical differences for the a-wave amplitude of F-ERG among different time points( F =1. 885,P =0. 129 ) and different treatment groups ( F =1. 188, P =0. 340 ), as with the ERG b-wave amplitude ( time: F =2. 73, P =0. 064 ; group : F =1. 114, P =0. 367). The differences in the latencies of F-VEP N1-wave were insignificant among the different time points( F =1. 605, P =0. 263 ) as well as various groups ( F=1. 556, P =0.314 ), and those of F-VEP P1 -wave were not evidently changed ( time: F =2. 329, P =0. 092 ; group : F =2. 186, P =0. 103 ). No correlations were seen between the time factor and grouping factor ( P ＞ 0. 05 ). There was no apparent siderosis bulbi change during the follow-up duration. No morphological abnormality in the retina and optical nerve was found under the light microscope. At the end of the experiment,intrascleral iron foreign body was wrapped by surrounding tissue in a stable condition. Conclusions The small posterior intrascleral iron foreign body, whether it is oxidized or not, does not produce distinctive functional or pathological damage on retina and opticus in the short term.