ABSTRACT
"Non-classical" di- and trinuclear Pt(II) complexes with polydentate nitrogen ligands; ionic [(PtCl(2))(2)(tptz)(2)(mu-PtClNCPh)]Cl (1) [tptz =2,4,6-tris(2-pyridyl)-1,3,5-triazine], [(PtCl(2))(2)(bptz)(2)(mu-Pt)]Cl(2) (2) [bptz = 3,6-bis(2-pyridyl)-1,2,4,5-tetrazine] and neutral [(PtCl(2))(2)(tptz)(2)(mu-PtCl(2))](H(2)O)(4) (3), [(PtCl(2))(2)(mu-tppz)](CHCl(3)) (4) [tppz = 2,3,5,6-tetra(2-pyridyl)pyrazine] complexes, have been prepared and structurally characterized. The neutral tptz and tppz complexes present three and two separate PtCl(2) moieties, respectively, in a cis position, presumably acting in a bifunctional mode towards DNA; the cationic tptz and bptz complexes contain monofunctional and bifunctional bridging Pt(II) moieties, respectively, (other Pt(II) moieties in the complexes are bifunctional). All complexes were tested for their biological activity. Both tptz complexes, neutral and ionic, show a potent cytotoxic activity and reduced cell viability in a concentration-dependent manner that was evaluated in a panel of different cancer cell lines: human HT29 colon-rectal carcinoma, HepG2 hepatoma, MDA-MB-231 breast cancer and MG63 osteosarcoma cells; their activity was higher than cisplatin, IC50 values have been calculated for the active compounds and flow cytometric analysis for the tptz complexes performed. Therefore, these new platinum drugs warrant further investigation into their antitumor activity against different types of tumors.
Subject(s)
Heterocyclic Compounds/chemical synthesis , Platinum Compounds/chemical synthesis , Cell Line, Tumor , Cell Survival , Heterocyclic Compounds/chemistry , Heterocyclic Compounds/metabolism , Humans , Ligands , Magnetic Resonance Spectroscopy , Molecular Structure , Platinum Compounds/chemistry , Platinum Compounds/metabolism , Spectrophotometry, InfraredABSTRACT
Pulsatile administration of GnRH appears to be the most rational and physiological treatment of infertility in patients affected by hypothalamic amenorrhea. The authors conclude that the results obtained with this method of treatment in patients with severe hypothalamic amenorrhea suggest that the choice of pulsatile GnRH therapy is an effective and practical method for induction of ovulation.
Subject(s)
Amenorrhea/physiopathology , Androgens/physiology , Hypothalamic Diseases/complications , Infusion Pumps , Ovulation Induction/methods , Pituitary Hormone-Releasing Hormones/administration & dosage , Adult , Amenorrhea/etiology , Female , Humans , Infertility, Female/drug therapy , Pulsatile FlowABSTRACT
The possibility of a correlation between biological (E2) and morphological (U.S.) parameters, in view of obtaining a correct prevision of follicular maturation and ovulation is discussed. In this study normal patients with a tubal sterility were treated with clomiphene citrate and clomiphene plus H.M.G. The statistical analysis was performed by means of the linear correlation (r) and the relative test of significance (Student T.). The data obtained in this study show that notwithstanding that the rising plasma concentration of E2, which precedes ovulation, is the first and more constant marker of follicular maturation, because of its wide range of variability its usefulness in prediction of ovulation is nearly limited to spontaneous cycles. In fact in stimulated cycles the rising plasma-E2 concentration is rather an independent variable regarding the growth of single follicles (F.D.).
