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Respiratory, endocrine, cardiac, and renal topics
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Heart failure is a state in which the heart, as a pump, is unable to sufficiently perfuse the organs at rest or during exercise, and to meet their metabolic demands. The approach to this condition has changed considerably over the last two decades, in both adult medicine and paediatrics. Traditionally, the approach was mainly “haemodynamic”, stimulating the failing heart muscle with inotropic drugs such as digitalis glycosides and vasoactive amines, or bipyridine derivatives such as amrinone and milrinone.
Inhalational Durg Abuse
Published in Jacob Loke, Pathophysiology and Treatment of Inhalation Injuries, 2020
Jacob Loke, Richard Rowley, Herbert D. Kleber, Peter Jatlow
In the marijuana eradication programs in the 1970s, particularly in Mexico, paraquat which was used as a defoliant, was sprayed onto the marijuana fields. Initially paraquat was thought to be quickly deactivated biologically, however, it was subsequently suggested that continuous heavy use of paraquat-sprayed marijuana may be hazardous (Smith et al., 1978) and cause lung fibrosis (Thurlbeck et al., 1976). Taken by mouth, paraquat has been shown to cause pulmonary fibrosis (Copland et al., 1974), and in experimental animals given paraquat by the intrabronchial route, the lung shows focal hemorrhage, congestion of capillaries, and moderate thickening of the alveolar septa (Zavala and Rhodes, 1978). Motivated by these findings, paraquat spraying was discontinued. However, there are no reported cases of lung damage or fibrosis due to paraquat sprayed marijuana in humans (Tashkin and Cohen, 1981; Tilles et al., 1986). Furthermore, when paraquat, which is highly water soluble, is pyrolyzed, the major portion is destroyed by pyrolysis, and it is changed to bipyridine, a respiratory irritant present also in tobacco smoke. These factors may account for the minimal effect, if any, of paraquat-sprayed marijuana on the lung.
Gold Complexes as Antitumor Agents
Published in Astrid Sigel, Helmut Sigel, Metal Ions in Biological Systems, 2004
Luigi Messori, Giordana Marcon
In summary, these novel gold(III) complexes bearing the 2,2′-bipyridine motif showed appreciable stability within physiological media while exhibiting important cytotoxic properties. Preliminary studies have pointed out that the interactions of these complexes with DNA are relatively weak whereas tight adducts are formed upon reaction with model proteins. Given their large stability within biological fluids, the organometallic members of this family hold great promise as potential antitumor drugs and will undergo more extensive biological testing in the near future.
Terpyridines as promising antitumor agents: an overview of their discovery and development
Published in Expert Opinion on Drug Discovery, 2022
Robert Musiol, Patryk Malecki, Marcin Pacholczyk, Jacek Mularski
Among the first attempts that were focused on the activity of terpyridines and bipyridines was the work of McFayden et al. [57]. A series of Tpy, bipyridine and phenanthrolines were synthesized and tested for their their DNA intercalating activity along with their cytotoxicity against L1210 murine leukemia cells, and also as complexes with platinum. Although the Tpy complexes were found to be among the most potent conjugates, the free ligand was even more active. The authors also suggested an intercellular complexation and metal deficiency as possible mechanisms of action for ligands; however, this hypothesis has not yet been investigated. Moreover, co-incubation with thiophenol or ethylenediamine has no effect on overall activity as can be observed in the case of the metal deprivation agents. Similar compounds have been investigated by Messori et al. [58] (18, 19 in Figure 2) and Shi et al. [59] (20). In the first work, both types of molecules appeared to be more active than cisplatin against lung and colon cancers and less active on the cervical or leukemia strains. However, once again, the free ligands were slightly more active than their complexes with gold in almost all cases. A further investigation confirmed DNA binding as a plausible mechanism.
In vitro cytotoxicity, cellular uptake, reactive oxygen species and cell cycle arrest studies of novel ruthenium(II) polypyridyl complexes towards A549 lung cancer cell line
Published in Drug and Chemical Toxicology, 2021
Muhammad Qasim Warraich, Alessandra Ghion, Laura Perdisatt, Luke O’Neill, Alan Casey, Christine O’Connor
The in-vitro cytotoxicity evaluation of all the ruthenium complexes have displayed a variable cytotoxic response against A549 cells in complex 1 [Ru(bpy)2o-CPIP].2PF6, complex 2 [Ru(phen)2o-CPIP].2PF6 and complex 3 [Ru(biq)2o-CPIP].2PF6. All three complexes contain different auxiliary ligands but the same main ligand CPIP=(4-(1H-Imidazo[4,5-f][1,10]phenanthrolin-2-yl)benzonitrile) with the CN group attached to the ortho-position in the phenyl ring. Complex 1 [Ru(bpy)2o-CPIP].2PF6 with the bipyridine auxiliary ligand exhibited the maximum activity (IC50 5.003 µM) as compared to its analogs complex 2 [Ru(phen)2o-CPIP].2PF6 (IC50 29.8 µM) and complex 3 [Ru(biq)2o-CPIP].2PF6 (32.75 µM) containing biquinoline and phenanthroline ligand respectively.
Novel Re(I) tricarbonyl coordination compounds based on 2-pyridyl-1,2,3-triazole derivatives bearing a 4-amino-substituted benzenesulfonamide arm: synthesis, crystal structure, computational studies and inhibitory activity against carbonic anhydrase I, II, and IX isoforms†
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
Yassine Aimene, Romain Eychenne, Sonia Mallet-Ladeira, Nathalie Saffon, Jean-Yves Winum, Alessio Nocentini, Claudiu T. Supuran, Eric Benoist, Achour Seridi
In this context, the efficient design and synthesis of chelating ligands represent the pivotal key to the successful application of this type of complexes. Most of the reported ligands which coordinate efficiently to the rhenium(I) tricarbonyl core are based on bidentate and tridentate chelating systems including N-heteroaromatic nitrogen, oxygen and to a lesser extend sulfur or phosphorus donor atoms7. While tridentate ligands lead to the most stable rhenium(I) tricarbonyl complexes, bidentate ligands based on α,α'-diimines are currently very popular. Indeed, their corresponding rhenium complexes exhibit interesting photo-physical properties which can be tuned by small changes in the ligand scaffold or around the rhenium centre by substituting the chlorine bound to the metal by a ternary ligand (generally, cyanides or N-heterocycles)8. Among efficient bidentate α,α'-diimine chelators, 2,2'-bipyridine (bpy) has been originally used9. More recently, similar chelating systems based on pyridine-triazole (pyta and tapy systems1) were developed as alternative ligands to 2,2′-bipyridines10. Obata et al. first reported that pyta moieties acted like a bipyridine mimic with strongly electron-donating substituents, the corresponding complexes of general formula fac-[Re(pyta)(CO)3Cl] exhibiting luminescence properties11.