Publication: Neuroprotective Properties of Bis-Sulfonamide Derivatives Against 6-OHDA-Induced Parkinson's Model via Sirtuin 1 Activity and in silico Pharmacokinetic Properties
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Issued Date
2022
Resource Type
Language
eng
File Type
application/pdf
ISSN
16625099
Rights Holder(s)
มหาวิทยาลัยศรีนครินทรวิโรฒ
Bibliographic Citation
Molecules. Vol 27, No.10 (2022), p.-
Suggested Citation
Apiraksattayakul S., Pingaew R., Prachayasittikul V., Ruankham W., Jongwachirachai P., Songtawee N., Suwanjang W., Tantimongcolwat T., Prachayasittikul S., Prachayasittikul V., Phopin K. Neuroprotective Properties of Bis-Sulfonamide Derivatives Against 6-OHDA-Induced Parkinson's Model via Sirtuin 1 Activity and in silico Pharmacokinetic Properties. Molecules. Vol 27, No.10 (2022), p.-. doi:10.3389/fnmol.2022.890838 Retrieved from: https://hdl.handle.net/20.500.14740/9635
Abstract
Parkinson's disease (PD) is considered one of the health problems in the aging society. Due to the limitations of currently available drugs in preventing disease progression, the discovery of novel neuroprotective agents has been challenged. Sulfonamide and its derivatives were reported for several biological activities. Herein, a series of 17 bis-sulfonamide derivatives were initially tested for their neuroprotective potential and cytotoxicity against the 6-hydroxydopamine (6-OHDA)-induced neuronal death in SH-SY5Y cells. Subsequently, six compounds (i.e., 2, 4, 11, 14, 15, and 17) were selected for investigations on underlying mechanisms. The data demonstrated that the pretreatment of selected compounds (5 μM) can significantly restore the level of cell viability, protect against mitochondrial membrane dysfunction, decrease the activity of lactate dehydrogenase (LDH), decrease the intracellular oxidative stress, and enhance the activity of NAD-dependent deacetylase sirtuin-1 (SIRT1). Molecular docking was also performed to support that these compounds could act as SIRT1 activators. In addition, in silico pharmacokinetic and toxicity profile prediction was also conducted for guiding the potential development. Thus, the six neuroprotective bis-sulfonamides were highlighted as potential agents to be further developed for PD management. Copyright © 2022 Apiraksattayakul, Pingaew, Prachayasittikul, Ruankham, Jongwachirachai, Songtawee, Suwanjang, Tantimongcolwat, Prachayasittikul, Prachayasittikul and Phopin.