COVID-19: Optimizing the Synthesis, Bioavailability and Scaling of Quercetin, a natural product potentially used for COVID-19 treatment

COVID-19：优化槲皮素的合成、生物利用度和规模化，槲皮素是一种可能用于 COVID-19 治疗的天然产品

• 批准号: 551382-2020
• 负责人: Dudding, Travis
• 金额: $ 3.64万
• 依托单位: Brock University
• 依托单位国家: 加拿大
• 项目类别: Alliance Grants
• 财政年份: 2020
• 资助国家: 加拿大
• 起止时间: 2020-01-01 至 2021-12-31
• 项目状态: 已结题
• 来源: https://www.nserc-crsng.gc.ca/ase-oro/Details-Detailles_eng.asp?id=702925
• 关键词: COVID; 19; Optimizing; Synthesis; Bioavailability

In late December 2019, the world as we knew was changed by the announcement in China of the novel coronavirus infectious disease 2019 (COVID-19). This devastating virus has now spread to more than 100 countries, infecting millions and causing more then two hundred thousand confirmed deaths globally as of April 20, 2020. Quercetin, a natural product and a major dietary flavonoid found in a wide range of fruits, vegetables, and beverages, such as tea and wine, has recently shown promise in treating COVID-19. Quercetin is also known to possess anti-inflammatory, anti-proliferative, and anti-atherosclerotic effects in humans and has further been applied to cancer prevention and therapy. While the therapeutic potential of quercetin is promising, the poor water solubility of this flavonoid hampers its bioavailability. Improving, the water solubility and bioavailability of quercetin would be a significant step forward to its wider use as a treatment for COVID-19. A Canadian company, Biolyse Pharma Corporation, has partnered up with Dr. Travis Dudding from Brock University to synthesize quercetin prodrugs for use as potential treatments of COVID-19. Key in this undertaking will be improving the solubility and with it bioavailability of quercetin. As well, these prodrugs will have the advantageous property of allowing for the controlled release of bioactive quercetin and/or analogous. This research and the resulting prodrugs will help position the company and Canada at a strategic place for offering low-cost, readily available therapies for potentially saving lives from COVID-19, while benefiting economically and fostering Canadian based Pharma production.

2019年12月下旬，中国宣布2019新型冠状病毒感染性疾病（COVID-19），改变了我们所知的世界。截至2020年4月20日，这种毁灭性的病毒已传播到100多个国家，感染了数百万人，并在全球范围内造成超过20万人确诊死亡。 槲皮素是一种天然产物，也是一种主要的膳食类黄酮，存在于各种水果、蔬菜和饮料（如茶和葡萄酒）中，最近显示出治疗COVID-19的前景。槲皮素还已知在人类中具有抗炎、抗增殖和抗动脉粥样硬化作用，并且已进一步应用于癌症预防和治疗。虽然槲皮素的治疗潜力是有希望的，但这种类黄酮的水溶性差阻碍了其生物利用度。提高槲皮素的水溶性和生物利用度将是其更广泛地用作COVID-19治疗的重要一步。 加拿大公司Biolyse Pharma Corporation与布洛克大学的Travis Dudding博士合作，合成槲皮素前药，用于COVID-19的潜在治疗。 这项工作的关键将是提高槲皮素的溶解度和生物利用度。同样，这些前药将具有允许生物活性槲皮素和/或类似物的受控释放的有利性质。这项研究和由此产生的前药将有助于公司和加拿大处于战略地位，提供低成本，易于获得的疗法，可能挽救COVID-19的生命，同时在经济上受益并促进加拿大的制药生产。