Kinetic and toxicological effects of synthesized palladium(II) complex on snake venom (Bungarus sindanus) acetylcholinesterase

Abstract

Background: The venom of the krait ( Bungarus sindanus ), an Elapidae snake, is highly toxic to humans and contains a great amount of acetylcholinesterase (AChE). The enzyme AChE provokes the hydrolysis of substrate acetylcholine (ACh) in the nervous system and terminates nerve impulse. Different inhibitors inactivate AChE and lead to ACh accumulation and disrupted neurotransmission. Methods: The present study was designed to evaluate the effect of palladium(II) complex as antivenom against krait venom AChE using kinetics methods. Results: Statistical analysis showed that krait venom AChE inhibition decreases with the increase of Pd(II) complex (0.025-0.05 µM) and exerted 61% inhibition against the AChE at a fixed concentration (0.5 mM) of ACh. Kinetic analysis using the Lineweaver Burk plot showed that Pd(II) caused a competitive inhibition. The compound Pd(II) complex binds at the active site of the enzyme. It was observed that K m (Michaelis-Menten constant of AChE-ACh into AChE and product) increased from 0.108 to 0.310 mM (45.74 to 318.35%) and V max remained constant with an increase of Pd(II) complex concentrations. In AChE K Iapp was found to increase from 0.0912 to 0.025 µM (29.82-72.58%) and did not affect the V maxapp with an increase of ACh from (0.05-1 mM). K i (inhibitory constant) was estimated to be 0.029 µM for snake venom; while the K m was estimated to be 0.4 mM. The calculated IC 50 for Pd(II) complex was found to be 0.043 µM at constant ACh concentration (0.5 mM). Conclusions: The results show that the Pd(II) complex can be deliberated as an inhibitor of AChE.

Ex vivo antiacetylcholinesterase studies on silver nanoparticles synthesized using green approach

“…Santos et al 58 reported in their research study that the Ilex paraguariensis ‐induced AgNPs cause a significant inhibition of AChE ex vivo activity. The results are also supported by Ahmed et al, 19 Sher et al, 59 and Haider et al 60 reports that inhibit AChE to elevate the ACh level in AD patients.…”

“…Thus, the NDs can be cured by addressing one or more of the linked situations. The acetylcholine (ACh) hydrolyzes enzyme acetylcholinesterase (AChE) EC 3.1.1.7 has been reported to play a significant role in AD pathology 19 . According to the literature, researchers are working on the pathogenesis of neurodegenerative conditions, but yet no proper treatment is found 20 .…”

“…The acetylcholine (ACh) hydrolyzes enzyme acetylcholinesterase (AChE) EC 3.1.1.7 has been reported to play a significant role in AD pathology. 19 According to the literature, researchers are working on the pathogenesis of neurodegenerative conditions, but yet no proper treatment is found. 20 Increasing the ACh level in the brain by using AChE inhibitors is thought to be an important approach for the treatment.…”

Synthesis, optimization, and characterization of silver/gold allied bimetallic from Hippeastrum hybridum (L.) and their ex vivo anti‐acetylcholinesterase activity in rat brain

“…The acetylcholine (ACh) hydrolyzes enzyme acetylcholinesterase (AChE) EC 3.1.1.7 has been reported to play a significant role in AD pathology. [ 22 ] According to the literature, researchers are working on the pathogenesis of neurodegenerative conditions, but no proper treatment is found. [ 23 ] Increasing the ACh level in the brain by using AChE inhibitors is thought to be an important approach for the treatment.…”

Acetylcholinesterase Activity in the Brain of Rats: Presence of an Inhibitor of Enzymatic Activity in Heliotropium eichwaldi L. Induced Silver/Gold Allied Bimetallic Nanoparticles

“…In Pakistan, the prevalence of dementia was reported to be 2%-6% among older persons (>65 years of age) [14]. Furthermore, numerous factors, such as aging [15] and various pathological disorders (including protein deposition [16], cholinergic deficits [17], neuroinflammation [18], mitochondrial dysfunction [19], and oxidative stress [20]), have been reported as triggers of NDs. Thus, NDs can be cured by addressing one or more of these causative factors.…”