Analgesic and Anti-Inflammatory Activities of Salicylaldehyde 2-Chlorobenzoyl Hydrazone (H2LASSBio-466), Salicylaldehyde 4-Chlorobenzoyl Hydrazone (H2LASSBio-1064) and Their Zinc(II) Complexes

Abstract

Salicylaldehyde 2-chlorobenzoyl hydrazone (H2LASSBio-466), salicylaldehyde 4-chlorobenzoyl hydrazone (H2LASSBio-1064) and their complexes [Zn(LASSBio-466)H2O]2 (1) and [Zn(HLASSBio-1064)Cl]2 (2) were evaluated in animal models of peripheral and central nociception, and acute inflammation. All studied compounds significantly inhibited acetic acid-induced writhing response. Upon coordination the anti-nociceptive activity was favored in the complex 1. H2LASSBio-466 inhibited only the first phase of the formalin test, while 1 was active in the second phase, like indomethacin, indicating its ability to inhibit nociception associated with the inflammatory response. Hence coordination to zinc(II) altered the pharmacological profile of H2LASSBio-466. H2LASSBio-1064 inhibited both phases but this effect was not improved by coordination. The studied compounds did not increase the latency of response in the hot plate model, indicating their lack of central anti-nociceptive activity. All compounds showed levels of inhibition of zymosan-induced peritonitis comparable or superior to indomethacin, indicating an expressive anti-inflammatory profile.

Gabapentin and its salicylaldehyde derivative alleviate allodynia and hypoalgesia in a cisplatin-induced neuropathic pain model

“…Salicylaldehyde(2-hydroxybenzaldehyde) Schiff base derivatives exhibit a broad range of biological activities. They possess promising anti-inflammatory, analgesic (Júnior et al, 2011), antiradical (Horackova et al, 2000), antidiabetic (Vančo et al, 2008), antiviral (Wang et al, 1990), nematicidal (Caboni et al, 2013), antitumor (Hodnett and Dunn, 1970), antifungal (Backes et al, 2014) and antibacterial (Kalaivani et al, 2012) activities. The lack of adverse effects up to 1000 mg/kg of GPS indicates that it is safe to the highest tested dose used in the in vivo behavioral studies.…”

Synthesis of novel macrocyclic Schiff's‐base and its complexes having N2O2 group of donor atoms. Characterization and anticancer screening are studied

“…[1][2][3][4] Positively charged metal centre combined with heteroaromatic periphery forms well-defined geometries, which facilitate the interaction with biomolecules and transport across membranes in biological systems. [5,6] Thiosemicarbazone heterocyclic compounds and their metal complexes have attracted considerable attention due to their coordination chemistry and broad range of pharmacological properties.…”

Zn(II)-Chlorido Complexes of Phytohormone Kinetin and Its Derivatives Modulate Expression of Inflammatory Mediators in THP-1 Cells

“…increasing production of metallothioneins, superoxide dismutase), and (iii) the inhibition of the NF-κB transcription factor (zinc causes zinc-finger protein up-regulation and the inhibition of the NF-κB activation through a TRAF pathway), resulting in the reduction of inflammatory cytokines and adhesion molecules [26]–[28]. Several zinc(II) complexes were also previously tested on different inflammatory models and showed significant diminution of induced inflammation [29]–[31].…”