Novel 1-(prop-2-yn-1-ylamino)-2,3-dihydro-1H-indene-4-thiol derivatives as potent selective human monoamine oxidase B inhibitors: Design, SAR development, and biological evaluation

Kong, H. S.; Meng, Xianshe; Hou, Rui; Yang, Xiaoxiao; Han, Jihong; Xie, Zhouling; Duan, Yajun; Liao, Chenzhong

doi:10.1016/j.bmcl.2021.128051

Cited by 2 publications

(1 citation statement)

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“…To assess the locomotor ability and various behaviors of mice after entering an open environment, we conducted an open field test (OFT) (ZS Ditron, Beijing, China), which consisted of nine compartments of the same size (100 cm × 100 cm × 40 cm). Briefly, mice were placed in the middle of the open field and allowed to explore the device autonomously for 5 min [38]. To avoid bias caused by odors left by the mice, the equipment was cleaned with 75% ethanol before each experiment.…”

Section: Open Field Testmentioning

confidence: 99%

L-Ergothioneine ameliorates MPTP-induced Parkinson's disease in C57BL/6J mice by activating DJ-1

Meng,

Hou

et al. 2024

Food Science and Human Wellness

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Parkinson's disease (PD) is one of the most common neurodegenerative diseases. The loss of dopaminergic (DAergic) neurons in the substantia nigra and the decrease of dopamine (DA) levels accelerate the process of PD. L-Ergothioneine (EGT) is a natural antioxidant derived from microorganisms, especially in edible mushrooms. EGT can penetrate blood-brain barrier and its levels are significantly decreased in the plasma of PD patients. Therefore, we speculated that EGT could ameliorate PD, and determined its effect on PD development by using 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced PD mouse models and neurotoxin 1-methyl-4-phenylpyridinium (MPP + )-induced cell models. Our results show that EGT alleviated MPTP-induced behavioral dysfunction in mice. Mechanistically, we innovatively revealed that EGT is a key regulator of DJ-1. EGT restored DA levels by activating the DJ-1-Nuclear receptor-related factor 1(Nurr1) axis. Furthermore, it reduced reactive oxygen species (ROS) levels by regulating the DJ-1-Nuclear factor erythroid 2-related factor 2 (Nrf2) pathway, which inhibited oxidative stress-induced DAergic neuronal apoptosis. Combined treatment with DJ-1-siRNA transfection revealed that blocking DJ-1 reversed EGT upregulated Nurr1 and Nrf2 expression in the nucleus, which significantly decreased the benefits of EGT. Taken together, our study suggests that EGT can ameliorate PD and be considered as a strategy for PD treatment.

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Section: Open Field Testmentioning

confidence: 99%