Biotransformation and brain distribution of the anti-COVID-19 drug molnupiravir and herb-drug pharmacokinetic interactions between the herbal extract Scutellaria formula-NRICM101

Chang, Cheng-Shang; Peng, Wen-Ya; Lee, Wan-Hsin; Lin, Tsai-Yun; Yang, Muh‐Hwa; Dalley, Jeffrey W.; Tsai, Tung Hu

doi:10.1016/j.jpba.2023.115499

Cited by 6 publications

(2 citation statements)

References 23 publications

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“…TCM has also contributed to COVID-19 treatment [ 14 , 15 ]. Taiwan Chingguan-Yihau (NRICM101), a TCM formula targeting viral respiratory infection and immunomodulation reported by the National Research Institute of Chinese Medicine, Taiwan (NRICM), has been commonly recommended and was clinically proven to be effective for the treatment of COVID-19 [ 16 , 17 , 18 ]. Based on the theoretical TCM system, the functions of Scutellaria baicalensis ( S. baicalensis ), Houttuynia cordata ( H. cordata ), and Isatis indigotica ( I. indigotica ) in NRICM101 are to clear heat, decrease dampness, promote diuresis, detoxify, and reduce swelling [ 19 , 20 , 21 ].…”

Section: Introductionmentioning

confidence: 99%

Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin-Converting Enzyme II

Lin,

Chang,

Lin

et al. 2024

IJMS

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Blocking the interaction between the SARS-CoV-2 spike protein and the human angiotensin-converting enzyme II (hACE2) protein serves as a therapeutic strategy for treating COVID-19. Traditional Chinese medicine (TCM) treatments containing bioactive products could alleviate the symptoms of severe COVID-19. However, the emergence of SARS-CoV-2 variants has complicated the process of developing broad-spectrum drugs. As such, the aim of this study was to explore the efficacy of TCM treatments against SARS-CoV-2 variants through targeting the interaction of the viral spike protein with the hACE2 receptor. Antiviral activity was systematically evaluated using a pseudovirus system. Scutellaria baicalensis (S. baicalensis) was found to be effective against SARS-CoV-2 infection, as it mediated the interaction between the viral spike protein and the hACE2 protein. Moreover, the active molecules of S. baicalensis were identified and analyzed. Baicalein and baicalin, a flavone and a flavone glycoside found in S. baicalensis, respectively, exhibited strong inhibitory activities targeting the viral spike protein and the hACE2 protein, respectively. Under optimized conditions, virus infection was inhibited by 98% via baicalein-treated pseudovirus and baicalin-treated hACE2. In summary, we identified the potential SARS-CoV-2 inhibitors from S. baicalensis that mediate the interaction between the Omicron spike protein and the hACE2 receptor. Future studies on the therapeutic application of baicalein and baicalin against SARS-CoV-2 variants are needed.

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Section: Introductionmentioning

confidence: 99%

Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin-Converting Enzyme II

Lin,

Chang,

Lin

et al. 2024

IJMS

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“…Molnupiravir (MK-4482 or EIDD-2801), a small molecule with broad-spectrum antiviral activity, has recently received FDA emergency use authorization in the USA for the treatment of symptomatic COVID-19 [ 27 ]. This drug inhibited the viral RdRp and was initially developed as an antiviral against different RNA viruses, including influenza [ 28 ].…”

Section: Introductionmentioning

confidence: 99%

Comparative Evaluation of GS-441524, Teriflunomide, Ruxolitinib, Molnupiravir, Ritonavir, and Nirmatrelvir for In Vitro Antiviral Activity against Feline Infectious Peritonitis Virus

Barua

Kaltenboeck

Juan

et al. 2023

Veterinary Sciences

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Feline infectious peritonitis (FIP), caused by feline coronavirus (FcoV), is considered one of the most enigmatic diseases in cats. Developing effective drugs for FIP is crucial due to its global prevalence and severity. In this study, six antiviral drugs were tested for their cytotoxicity, cell viability, and antiviral efficacies in Crandell-Reese feline kidney cells. A cytotoxicity assay demonstrated that these drugs were safe to be used with essentially no cytotoxicity with concentrations as high as 250 µM for ruxolitinib; 125 µM for GS441524; 63 µM for teriflunomide, molnupiravir, and nirmatrelvir; and 16 µM for ritonavir. GS441524 and nirmatrelvir exhibited the least detrimental effects on the CRFK cells, with 50% cytotoxic concentration (CC50) values of 260.0 µM and 279.1 µM, respectively, while ritonavir showed high toxicity (CC50 = 39.9 µM). In the dose–response analysis, GS441524, nirmatrelvir, and molnupiravir demonstrated promising results with selectivity index values of 165.54, 113.67, and 29.27, respectively, against FIPV. Our study suggests that nirmatrelvir and molnupiravir hold potential for FIPV treatment and could serve as alternatives to GS441524. Continued research and development of antiviral drugs are essential to ensure the well-being of companion animals and improve our preparedness for future outbreaks of coronaviruses affecting animals and humans alike.

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The anti-COVID-19 drug nirmatrelvir crosses the blood‒brain barrier and exhibits herb–drug pharmacokinetic interactions with Scutellaria baicalensis formulations

Lee,

Kung,

Sun

et al. 2024

Heliyon

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Biotransformation and brain distribution of the anti-COVID-19 drug molnupiravir and herb-drug pharmacokinetic interactions between the herbal extract Scutellaria formula-NRICM101

Cited by 6 publications

References 23 publications

Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin-Converting Enzyme II

Inhibitory Efficacy of Main Components of Scutellaria baicalensis on the Interaction between Spike Protein of SARS-CoV-2 and Human Angiotensin-Converting Enzyme II

Comparative Evaluation of GS-441524, Teriflunomide, Ruxolitinib, Molnupiravir, Ritonavir, and Nirmatrelvir for In Vitro Antiviral Activity against Feline Infectious Peritonitis Virus

The anti-COVID-19 drug nirmatrelvir crosses the blood‒brain barrier and exhibits herb–drug pharmacokinetic interactions with Scutellaria baicalensis formulations

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