Influenza Virus Inhibitor

Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC₅₀=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions.

Baloxavir marboxil (S-033188) is a selective inhibitor of influenza cap-dependent endonuclease. Baloxavir marboxil, a potent antiviral agent, shows activity against influenza A and B virus.

Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.

Baloxavir (Baloxavir acid), derived from the proagent Baloxavir marboxil, is a first-in-class, potent and selective cap-dependent endonuclease (CEN) inhibitor within the polymerase PA subunit of influenza A and B viruses. Baloxavir inhibits viral RNA transcription and replication and has potently antiviral activity.

Isoliquiritigenin is an anti-tumor flavonoid from the root of Glycyrrhiza uralensis Fisch., which inhibits aldose reductase with an IC₅₀ of 320 nM. Isoliquiritigenin is a potent inhibitor of influenza virus replication with an EC₅₀ of 24.7 μM.

Crystal Violet, also known as Gentian violet, methyl violet 10B, is a triphenyl-methane, an alkaline dye that binds to DNA in the nucleus of a cell, staining it a deep purple. It is often used for Gram staining to classify bacteria, or for cell or histological staining[1].

Oseltamivir (GS 4104) is an orally active influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC₅₀s of 0.67, 0.9, 1.34 and 13 nM, respectively.

Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.

Catechin ((+)-Catechin) inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 1.4 μM.

Oseltamivir phosphate (GS 4104) is a neuraminidase inhibitor recommended for the treatment and prophylaxis of influenza A and B.

SC75741 is a broad and efficient NF-κB inhibitor with an IC₅₀ of 200 nM for p65. SC75741 blocks influenza viruses (IV) replication. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins.

Zanamivir is an influenza viral neuraminidase inhibitor with IC₅₀ values of 0.95 nM and 2.7 nM for influenza A and B, respectively.

AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC₅₀ of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).

N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia.

Molnupiravir (EIDD-2801) is an orally bioavailable proagent of the ribonucleoside analog EIDD-1931. Molnupiravir has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Molnupiravir has the potential for the research of COVID-19, and seasonal and pandemic influenza.

Dihydromyricetin is a potent inhibitor with an IC₅₀ of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC₅₀ of 22 μM.

Hyperoside is a NF-κB inhibitor, found from Hypericum monogynum. Hyperoside shows anti-tumor, antifungal, anti-inflammatory, anti-viral, and anti-oxidative activities, and can induce apoptosis.

Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis.

Nitazoxanide (NTZ), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans. Nitazoxanide inhibits Giardia lamblia trophozoite proliferation in axenic culture with an IC₅₀ of 2.4 μM. Nitazoxanide can be used for the research of parasitic gastroenteritis. Nitazoxanide shows anti-Japanese encephalitis virus (JEV) activity in a mouse model.

N6-Methyladenosine is the most prevalent internal (non-cap) modification present in the messenger RNA (mRNA) of all higher eukaryotes. N6-Methyladenosine can modifies viral RNAs and has antiviral activities.