Inhalational Durg Abuse
Jacob Loke in Pathophysiology and Treatment of Inhalation Injuries, 2020
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.
Designing Smart Nanotherapeutics
Suresh C. Pillai, Yvonne Lang in Toxicity of Nanomaterials, 2019
Gadolinium (III)-complex-grafted lead sulphide (GCGLS) nanoparticles were examined for CT and magnetic resonance dual-modality-imaging-guided PTT (Zou et al. 2018). The schematic representation of synthesis and theranostic functions (PTT, MRI, and CT) of GCGLS nanoparticles is displayed in Figure 6.9. At first, 3-chloropropionic acid (CPA) modified lead sulphide (PbS) was synthesized using the precursors such as lead acetate, 2-mercaptoethanol, sodium sulphide, CPA, and water under N2 atmosphere. The obtained product was centrifuged and washed with deionized water. Then, CPA-PbS and Gd(AA)3Phen were dispersed in polyethylene glycol monomethacrylate (PEGMA) monomer under N2 atmosphere. This mixture was further reacted with copper chloride (CuCl), bipyridine (Bpy), and tetrahydrofuran (THF). The product was centrifuged and washed with deionized water. The as-synthesized nanoparticles were injected into mice to detect and treat the tumour sites. PbS was responsible for the CT and the Gd complex was accountable for the MR imaging. GCGLS nanoparticles showed high stability and biocompatibility in vitro/vivo. The stability and dispersibility of GCGLS nanoparticles were influenced by the concentration of Gd complex. The cytotoxicity of GCGLS nanoparticles was evaluated using MTT assay in B16 cells. After 24 hours of incubation, the cell viability is up to 80%. However, the nanoparticles showed slight cytotoxicity at high concentrations during 48 hours of incubation. The photo-thermal effect was also tested after 24 hours of incubation. Under light irradiation, approximately 80% of the B16 cells were killed by 40 µg/mL of GCGLS nanoparticles. In contrast, the cytotoxicity is negligible under normal conditions (without light irradiation).
Gold Complexes as Antitumor Agents
Astrid Sigel, Helmut Sigel in Metal Ions in Biological Systems, 2004
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.
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.
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.
Cytotoxic substituted indolizines as new colchicine site tubulin polymerisation inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Monica-Cornelia Sardaru, Anda Mihaela Craciun, Cristina-Maria Al Matarneh, Isabela Andreea Sandu, Roxana Maria Amarandi, Lacramioara Popovici, Catalina Ionica Ciobanu, Dragos Peptanariu, Mariana Pinteala, Ionel I. Mangalagiu, Ramona Danac
The pyridinium salts 8a–l and 13a–d were prepared through the direct reaction of pyridine 1, 4,4′-bipyridine 2, 2,4′-bipyridine 3, or 2,2′-bipyridine 12, respectively, with 2-bromo-acetophenones 4–7 in acetone, at r.t. (Schemes 1 and 2) (for spectral data of pyridinium salts 8a–l and 13a–d see Supplementary data). In the next step, for the synthesis of the indolizine ring, we used the 1,3-dipolar cycloaddition of the pyridinium ylides generated in situ in basic medium from the salts 8a–l and 13a–d, to ethyl propiolate (Schemes 1 and 2)21,30,31,41.
Related Knowledge Centers
- Catalysis
- Chelation
- Diquat
- Ligand
- Organic Compound
- Paraquat
- Pyridine
- Supramolecular Chemistry
- 2,2′-Bipyridine
- Coordination Complex