OBJECTIVETo establish an HPLC-DAD/ESI-MS method for quickly identifying chemical constituents in diterpene lactone effective fraction of Andrographis panniculata and to study its pharmacodynamics.

METHODThe separation was performed on an Agilent SB-C18 column (2.1 mm x 150 mm, 5 μm) with a mobile phase of acetonitrile (A) and water (B). The flow rate was maintained at 0.4 mL x min(-1) and detection wavelength was set at 205 nm. The samples were analyzed in positive ion mode, and mass scan range was m/z 50-1 000. Using two kinds of tumor cell lines made living animal models, and studied preliminary pharmacodynamics on anti-tumor aspect.

RESULTFive diterpene lactones in the diterpene lactone effective fraction of A. panniculata could be separated in one run. Pharmacodynamic experiments showed that the effectve fraction had an inhibitory effect on the growth of tumor.

CONCLUSIONA rapid and efficient HPLC-ESI-MS method to determine the chemical constituents in diterpene lactone effective fraction of A. panniculata has been established, and the preliminary pharmacodynamics research has been done, which could be used for the quality control and further studies of diterpene lactone effective fraction of A. panniculata in vivo.

Andrographis ; chemistry ; Animals ; Antineoplastic Agents, Phytogenic ; administration & dosage ; chemistry ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; administration & dosage ; chemistry ; Female ; Humans ; Lung Neoplasms ; drug therapy ; physiopathology ; Mice ; Mice, Inbred C57BL ; Spectrometry, Mass, Electrospray Ionization

Biopsy, Fine-Needle ; methods ; Breast ; pathology ; Breast Neoplasms ; pathology ; Carcinoma, Ductal, Breast ; pathology ; Female ; Humans ; Immunohistochemistry ; methods ; Lymph Nodes ; pathology ; Lymphatic Metastasis ; Paraffin Embedding ; methods ; Receptor, ErbB-2 ; metabolism

Objective To investigate the significance and effect of ultrasonic diagnosis on the autologous bone marrow mesenchymal stem cells (MSC) in angiogenesis. Methods Twenty-four New Zealand rabbits were divided into experiment group (12) and the control group (12). Then rabbit bone marrow MSCs from experiment group were isolated, caltured and marked with Brdu. After ischemic hind limb animal model on all rabbits was set up, autologous bone marrow MSCs were directly injected into the ischemic hind limb muscles in experiment group while same volume normal saline was used in the control group. Two weeks after the implantation of autologous bone marrow MSCs, 2D and color Doppler flow imaging (CDFI) detection were used in rabbit femoral artery of the two groups to observe the inner diameter of the blood vessel, the peak velocity and the acceleration time. The disposition of transplaned cells and the state of angiogenesis in ischemic muscles were assessed using immunofluorescence staining. Results The results of 2D and Doppler ultrasound detection showed the inner diameter of the blood vessel and the peak velocity of the blood current in experiment group obviously higher than that of the control group , and the acceleration time was obviously smaller than that of the control group P<0.01. The immunofluorescence staining showed there were transplanted cells existed in transplanted portion and state of angiogenesis was supurior obviously than that of the control. Conclusions Bone marrow MSCs had the effect to promote angiogenesis. Implantation of autologous bone marrow MSCs was a simple and efficient therapeutic method for the ischemia hind limb. Using high-frequency ultrasound to detect femoral artery may provide a practical and useful method to evaluate the effect on implanted autologous bone marrow mesenchymal stem cells.

Pericellular matrix (PCM) is a narrow tissue region surrounding chondrocytes, which "chondron" with its enclosed cells. A number of studies suggested that PCM is rich in proteoglycans, collagen and fibronectin, and plays an important role in regulating microenvironment of chondrocytes. Direct measures of PCM properties through micropipette aspiration technique showed that PCM was different from mechanical property of chondrocytes and nature extracellular matrix. However, the function of PCM is not clear, and need further study.
Animals ; Biomechanical Phenomena ; Chondrocytes ; chemistry ; cytology ; metabolism ; Extracellular Matrix ; chemistry ; metabolism ; Humans

Hypoxia is a general characteristic of most solid malignancies and intimately related to cancer progression. Homeostatic response to hypoxia is primarily mediated by hypoxia inducible factor-1alpha (HIF-1alpha) that elicits transcriptional activity through recruitment P300 coactivator. Targeting the interaction of HIF- alpha and P300 would thus constitute a novel approach for cancer treatment by suppressing tumor angiogenesis and metastasis. Here, a screening assay was developed for inhibitors targeting the interaction between HIF-1alpha and P300. The nucleotide sequence of human HIF-1alpha and P300 were cloned into pBIND and pACT vectors, named pBIND-HIF1alpha and pACT-P300. The interaction of HIF-1alpha and P300 was identified in HEK293 cell using mammalian two-hybrid system. And compound chetomin decreased their interaction in this mammalian two-hybrid system. We further verified HIF-1 inhibition effect of chetomin in U251-HRE cells. Therefore, we established a screening assay combined HIF-1alpha and P300 mammalian two-hybrid system and U251-HRE reporter assay for HIF-1 selective inhibitors.
Cell Hypoxia ; Disulfides ; pharmacology ; Drug Screening Assays, Antitumor ; E1A-Associated p300 Protein ; antagonists & inhibitors ; HEK293 Cells ; Humans ; Hypoxia-Inducible Factor 1, alpha Subunit ; antagonists & inhibitors ; Indole Alkaloids ; pharmacology ; Two-Hybrid System Techniques

A series of novel sorafenib analogues were designed and synthesized. The cytotoxic activities of these compounds were tested in four tumor cell lines. Some of the compounds showed potent antiproliferative activity against the tested cell lines with IC50 = 4-20 micromol x L(-1). Some compounds demonstrated competitive antiproliferative activities to sorafenib against tested cancer cell lines. Among them, compound 7c demonstrated significant inhibitory activities on ACHN, HCT116 and MDA-MB-231 cell lines with IC50 values of 9.01, 4.97, 6.61 micromol x L(-1), respectively.
Antineoplastic Agents ; chemical synthesis ; chemistry ; pharmacology ; Cell Line, Tumor ; Cell Proliferation ; drug effects ; Humans ; Inhibitory Concentration 50 ; Molecular Structure ; Niacinamide ; analogs & derivatives ; chemical synthesis ; chemistry ; pharmacology ; Phenylurea Compounds ; chemical synthesis ; chemistry ; pharmacology ; Structure-Activity Relationship

Une new flavonoids named as notabilisin K (1), together with four known compounds, morusin (2), mulberrofuran A (3), neocyclomorusin (4) and mornigrol F (5) are separated from 95% ethanol extracts of the twigs of Morus notabilis. Compounds 2-5 are separated from this plant for the first time. Notabilisin I, notabilisin J exhibits certain effect against cells of HCT-116, HepG2 and A2780 with IC50 values ranging from 1.47 μmol x L(-1) to 5.46 μmol x L(-1). Morusin exhibits strong effect against five kinds of human cancer cells (BGC823, A2780, HCT-116, HepG2 and NCI-H1650) with IC50 values ranging from 0.74 μmol x L(-1) to 1.58 μmol x L(-1).
Antineoplastic Agents, Phytogenic ; chemistry ; Benzofurans ; chemistry ; Flavonoids ; chemistry ; Hep G2 Cells ; Humans ; Inhibitory Concentration 50 ; Morus ; chemistry ; Plant Extracts ; chemistry ; Terpenes ; chemistry

Objective To study CT-guided localization of additional pulmonary nodules with microcoils prior to video-assisted thoracoscopic surgery (VATS) resection in patients with suspected lung cancer.Methods Eleven patients suspected lung cancer underwent preoperative microcoils localization towards additional small pulmonary nodules.The head of microcoil was pinpointed adjacent to the target nodule while its end tail remained above the visceral pleura.VATS were performed within 24 hours, and comprehensive assessments were conducted according to surgical and pathological outcomes of primary and additional lesions, and suitable surgical processes were followed.Results All 11 localizing pulmonary nodules (4-15 mm in diameter) were successfully removed after VATS, 9 microcoils'' end tails of which were placed above visceral pleural surface.There were no serious complications related with localizing procedure.Other 16 lesions including 11 primary ones were resected.The surgical and pathological outcomes for lung lesions were utterly assessed.Conclusion Microcoil preoperative localization provides helpful orientation for complete resection and assessment of multiple pulmonary lesions in patients with suspected lung cancer.

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.