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Abstract :
[en] The COVID-19 pandemic is now considered as an established and ongoing health issue according to the World Health Organization, presenting challenges worldwide despite available pharmaceutical interventions. In response to the pandemic, the Chinese government has proposed the use of Traditional Chinese Medicine (TCM) as a complementary approach to conventional treatments. TCM, deeply rooted in Asian healthcare, has gathered interest for its potential application in Western countries.
The present study focuses on preliminary investigations of halogenation processes applied to the ethanol extract obtained from Paeonia suffruticosa, a traditional Chinese plant, with the aim of enhancing its biological activity, particularly against SARS-CoV-2. Before achieving hemisynthesis on the crude extract, quercetin was choosen to find the optimal reaction conditions of the halogenation step, considering its presence in Paeonia suffruticosa, its abundance and cost-effectiveness. Various halogenation methods were evaluated, including the use of N-bromosuccinimide and an environmentally friendly (green) approach using sodium bromide and hydrogen peroxide. Both methods yielded promising results after LC-MS monitoring.
The green methodology was then used on the Paeonia suffruticosa ethanol extract, successfully generating brominated derivatives, such as dibromopaeonol and dibromooxypaeoniflorin. In conclusion, this preliminary study highlights the potential of halogenation processes to modify the ethanol extract from Paeonia suffruticosa and potentially enhance its anti-SARS-CoV-2 properties. These findings provide insights into the potential interest of TCM in the development of new lead compounds to fight the ongoing global COVID-19 pandemic.
Further investigations are however needed to validate these results and explore other promising late-stage functionalization strategies, using innovative green synthetic approaches.
