New Progress in Study on Mechanism of Lianhua Qingwen Capsules for Treatment of COVID-19

Recently, Prof. Caisheng Wu and Prof. Yifeng Chai from the School of Pharmacy, Xiamen University have made new progress in the study of the pharmacologically active ingredients and mechanism of Lianhua Qingwen Capsules, developed and produced by Yiling Pharmaceutical, in the prevention and treatment of COVID-19. The study result, "Screening of the Anti-COVID-19 Pharmacological Active Ingredients of Traditional Chinese Medicine Lianhua Qingwen Capsules Based on Human Exposure and ACE2 Biochromatography", was published in the top journal of pharmacology, Acta Pharmaceutica Sinica B. This is the latest evidence of the prevention and treatment of COVID-19 by the Chinese medicine Lianhua Qingwen.

This study was based on HRMS and intelligent non-targeted data mining techniques, and comprehensively analyzed the components of Lianhua Qingwen Capsules in human plasma and urine after multiple administrations, synthesized a novel ACE2 biochromatographic stationary phase, and screened the potential ACE2-targeted components of Lianhua Qingwen Capsules extracts and human urine samples. The experimental results showed that 85 relevant components of Lianhua Qingwen were successfully identified in human after multiple administrations, and a small number of components were selected to verify the ACE2 binding ability by SPR analysis. The components, Amygdalin, Prunasin, Glycyrrhizic Acid, Forsythoside A, Forsythoside I, Rhein, and Aloe-emodin, all showed binding affinity to ACE2. It should be noted that these components not only showed good affinity to ACE2, but also could effectively bind to the contact surface of ACE2 and S protein complex as confirmed by computer-aided docking results. These ACE2-binding components may inhibit the Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) by effectively affecting the binding between ACE2 and S protein, providing an experimental basis for the prevention and treatment of Coronavirus Disease 2019 (COVID-19) with Lianhua Qingwen Capsules.

Lianhua Qingwen Capsules is an innovative Chinese medicine developed and produced by Yiling Pharmaceutical, which is mainly used for the treatment of cold, flu and other diseases. Since the outbreak of COVID-19, Lianhua Qingwen Capsules have been recommended by the official Chinese "Diagnosis and Treatment Protocol for COVID-19" (Trial 4th-8th Edition) and used in designated admission hospitals for COVID-19 in China. Currently, the drug has been approved for marketing in 21 countries and regions, including Canada, Russia, Singapore and Kuwait.

The study results published in this publication are the first elaboration of information on the human in vivo composition of Lianhua Qingwen Capsules, providing a chemical and pharmacological theoretical basis for the study of its pharmacologically active ingredients and mechanism of action in anti-coronavirus disease 2019 (COVID-19), and further elaborating how Lianhua Qingwen works from the human in vivo perspective, which is an extension of the experimental studies and clinical evidence of Chinese medicine for the treatment of COVID-19.