ABSTRACT
Endoglin (CD105, END) is upregulated in proliferating endothelial cells, suggesting potential therapeutic properties. However, it is not clear whether endoglin mediates an enhanced proliferative rate or may be upregulated as part of a negative feedback loop. To gain insights into context-dependent and cell type-dependent regulatory effects of endoglin, we studied its role properties in human ovarian carcinoma-derived endothelial cells (ODMECs). We isolated and cultured primary ODMECs from epithelial ovarian carcinoma tissue. ODMECs had higher expression of endoglin and VEGFR-2, and also exhibited enhanced spontaneous formation of vessel-like structures in vitro. Transfection of siRNA targeting endoglin in ODMECs cells resulted in the reduction of the proliferation and tube formation. These results indicate that a subset of ODMECs display abnormal angiogenic properties and this phenotype was blocked by decreasing endoglin levels, suggesting endoglin is essential for stimulating angiogenesis, and targeting it may be an attractive approach to anti-angiogenesis therapy for ovarian carcinoma.
Subject(s)
Antigens, CD/metabolism , Endothelial Cells/metabolism , Neoplasms, Glandular and Epithelial/pathology , Neovascularization, Pathologic/metabolism , Ovarian Neoplasms/pathology , Receptors, Cell Surface/metabolism , Antigens, CD/genetics , Cell Movement , Cell Proliferation , Cell Shape , Endoglin , Endothelial Cells/physiology , Female , Gene Knockdown Techniques , Humans , Microvessels/pathology , Neoplasms, Glandular and Epithelial/blood supply , Ovarian Neoplasms/blood supply , Platelet Endothelial Cell Adhesion Molecule-1/metabolism , Primary Cell Culture , RNA, Small Interfering/genetics , Receptors, Cell Surface/genetics , Tumor Cells, Cultured , Vascular Endothelial Growth Factor Receptor-2/metabolism , von Willebrand Factor/metabolismABSTRACT
To study the relationship between the concentrations of INH B (Inhibin B), ACT A (Activin A), and FSH (Follicle stimulating hormone) in blood plasma and fecundity, Dazu black goat with high productivity and Sannen dairy goat with low productivity were used as experiment objects in this research. The concentrations of INH B, ACT A, and FSH in blood plasma were measured by enzyme-linked immunosorbent assay (ELISA) in order to study the secretion rule of INH B, ACT A, and FSH during an estrus cycle of two goat breeds. The results indicated that the secretion of FSH showed a positive correlation with ACT A and a negative correlation with INH B. The mean concentration of FSH in Dazu black goat was higher than that in Sanen dairy goat during a estrous cycle. However, during the time from obviously estrus to ovulation, the mean concentration of FSH in Dazu black goat was significantly higher than that in Sannen dairy goat (0.01Subject(s)
Activins/blood
, Dairying
, Estrous Cycle/blood
, Follicle Stimulating Hormone/blood
, Goats/blood
, Goats/physiology
, Inhibins/blood
, Activins/metabolism
, Animals
, Estrous Cycle/metabolism
, Female
, Follicle Stimulating Hormone/metabolism
, Goats/metabolism
, Inhibins/metabolism
ABSTRACT
BACKGROUND: The intermediate derivatisation method based on bioisosteric replacement led to the discovery of the lead strobilurin compound 5a. To produce new strobilurin analogues with improved activity, a series of substituted pyrimidines were synthesised and bioassayed. RESULTS: The compounds were identified by (1)H NMR, IR, MS and elemental analysis. The highly active compound 5 g was studied by X-ray diffraction. Preliminary bioassays demonstrated that some of the title compounds exhibited excellent acaricidal activity against Tetranychus cinnabarinus (Boisd.) at 10 mg L(-1). The relationship between structure and acaricidal activity is reported. CONCLUSION: The present work demonstrates that strobilurin derivatives containing pyrimidine moieties can be used as possible lead compounds for developing novel acaricides.
