influenza a virus-in-1

Influenza A virus-IN-1, a dihydropyrrolidones derivative, is a highly effective inhibitor of various subtypes of influenza A virus (IAV) with IC 50 values ranging from 3.11 μM to 7.13 μM. It effectively suppresses IAV replication and enhances the expression of key antiviral cytokines, such as IFN-β, and the antiviral protein MxA.

Influenza A virus-IN-15 (Compound 9b), a quinoline derivative, is a broad-spectrum anti-influenza inhibitor with an IC50 range of 0.88-6.33 μM and demonstrates acceptable cytotoxicity. It inhibits the transcription and replication of viral RNA, making it suitable for research on Influenza A virus (IAV).

Triton X-100 is a non-denaturing detergent that solubilizes lipid membranes. Triton X-100 is commonly used in laboratories and is applied to vaccines at different stages of the manufacturing process. Triton X-100 is listed as an excipient in certain vaccines including split virus influenza vaccines. Triton X-100 is a nonionic surfactant [1] [2].

Umifenovir is a potent, orally active broad-spectrum antiviral agent with activity against enveloped and non-enveloped viruses, suppressing virus propagation and modulating the expression of inflammatory cytokines for use as an anti-influenza virus agent [3]. It effectively inhibits the fusion of the virus with host cells [1] [2] and is an efficient inhibitor of SARS-CoV-2 in vitro [2].

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Cap-dependent endonuclease-IN-1 is a highly potent, orally active cap-dependent endonuclease inhibitor with antiviral activity for studying influenza virus infection.

Neuraminidase-IN-1 (Compound Y-1) is a novel neuraminidase inhibitor.

Colletodiol is a fungal metabolite found in D. grovesii with immunosuppressant and antiviral activities. It inhibits concanavalin A- or LPS-induced proliferation of isolated mouse splenocytes (IC50s = 12 and 5 μg ml, respectively) and inhibits influenza A viral replication in HeLa-IAV-Luc cells.

CAY10766 is an antiviral compound.1It inhibits entry of influenza virus-like particles pseudotyped with hemagglutinin A (HA) from H5N1 influenza A virus into A549 cells (EC50= 0.24 μM). CAY10766 (1 μM) reduces H1N1 and H5N1 influenza A viral titers in infected MDCK cells. It also exhibits synergy with oseltamivir carboxylate in MDCK cells infected with the influenza A reporter PR8-NS1-Gluc virus.

Australine is a pyrrolizidine alkaloid originally isolated fromC. australethat has enzyme inhibitory activities.1,2,3It is an inhibitor of glucoamylase (IC50= 5.8 μM) that also inhibits glucosidase I, sucrase, maltase, andA. nigerα-glucosidase (IC50s = 20, 28, 35, and 28 μM, respectively).2,3Australine is selective for these enzymes over glucosidase II, α- and β-mannosidase, and α- and β-galactosidase up to 500 μM, β-glucosidase, with only 5% inhibition at 66 μM, as well as isomaltase and trehalase (IC50= 97 and 160 μM, respectively). Australine (500 μg/ml) inhibits glycoprotein processing of viral glycoproteins in influenza virus-infected MDCK cells and induces the accumulation of glycoproteins.2 1.Molyneux, R.J., Benson, M., Wong, R.Y., et al.Australine, a novel pyrrolizidine alkaloid glucosidase inhibitor from Castanospermum australJ. Nat. Prod.51(6)1198-1206(1988) 2.Tropea, J.E., Molyneux, R.J., Kaushal, G.P., et al.Australine, a pyrrolizidine alkaloid that inhibits amyloglucosidase and glycoprotein processingBiochemistry28(5)2027-2034(1989) 3.Kato, A., Kano, E., Adachi, I., et al.Australine and related alkaloids: easy structural confirmation by 13C NMR spectral data and biological activitiesTetrahedron Asymmetry14(3)325-331(2003)

KBC-007 is a synthetic branched chain-containing analog of α-galactosylceramide (α-GalCer). It induces IL-4 and IFN-γ secretion by mouse splenocytes when used at a concentration of 0.5 ng/ml and IL-2 secretion by DN32.D3 NKT hybridoma cells co-cultured with CD1d-transfected RBL cells pre-loaded with KBC-007 at a concentration of 8 ng/ml. KBC-007 (1 μg per animal) increases levels of IL-4, but not IFN-γ, to a similar degree as α-GalCer in mouse serum. KBC-007 (0.5 μg per animal) increases the survival rate of mice immunized with the inactivated influenza A virus A/PR/8/34 in a model of influenza infection.

Defensin HNP-3 is a peptide secreted by human polymorphonuclear leukocytes (PMNs) that has antimicrobial properties. It induces lysis of mammalian cells when used at a concentration of 25 μg/mL. It also inhibits growth of E. faecalis (ED50 = 100 nM) and clinical isolates of P. aeruginosa (MIC90 = 4 μM). HNP-3 binds to recombinant HIV-1 envelope glycoprotein (gp120) and human CD4 (Kds = 52.8 and 34.9 nM, respectively). It also binds to recombinant, immobilized human surfactant protein D (SP-D; Kd = 55.7 nM) and inhibits focus formation in Madin-Darby canine kidney (MDCK) cells infected with influenza A virus (IAV).

Zanamivir-13C,15N2is intended for use as an internal standard for the quantification of zanamivir by GC- or LC-MS. Zanamivir is a sialic acid analog that inhibits neuraminidase release of newly replicated influenza virus particles.1It has been shown to selectively inhibit the growth of influenza A and B viruses in plaque reduction assays with IC50values ranging from 5 to 14 nM and to directly inhibit influenza A and B virus neuraminidases with IC50values ranging from 0.6 to 7.9 nMin vitro. Intranasal zanamivir administration at 0.4 mg/kg twice daily reduces mortality and viral titers in lung homogenates of mice infected with influenza. 1.Elliott, M.Zanamivir: From drug design to the clinicPhilos. Trans. R. Soc. Lond. B Biol Sci.356(1416)1885-1893(2001)

Ribavirin-13C5is intended for use as an internal standard for the quantification of ribavirin by GC- or LC-MS. Ribavirin is an antiviral guanosine nucleoside analog.1,2Upon entry into cells, ribavirin is metabolized to an active triphosphate form that induces viral RNA chain termination and inhibits viral polymerases. It reduces replication in a panel of seven RNA and four DNA viruses in Vero cells (EC50s = 2-95 μg/ml).3Ribavirin also reduces replication of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) in Vero cells (EC50= 109.5 μM).4Aerosol administration of ribavirin (30 mg/kg) reduces mortality in a mouse model of influenza A infection.5Formulations containing ribavirin have been used in the treatment of respiratory syncytial virus (RSV), hepatitis C virus (HCV), and viral hemorrhagic fevers. 1.Gilbert, B.E., and Knight, V.Biochemistry and clinical applications of ribavirinAntimicrob. Agents Chemother.30(2)201-205(1986) 2.Gordon, C.J., Tchesnokov, E.P., Woolner, E., et al.Remdesivir is a direct-acting antiviral that inhibits RNA-dependent RNA polymerase from severe acute respiratory syndrome coronavirus 2 with high potencyJ. Biol. Chem.295(20)6785-6797(2020) 3.Kirsi, J.J., North, J.A., McKernan, P.A., et al.Broad-spectrum antiviral activity of 2-β-D-ribofuranosylselenazole-4-carboxamide, a new antiviral agentAntimicrob. Agents Chemother.24(3)353-361(1983) 4.Wang, M., Cao, R., Zhang, L., et al.Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitroCell Res.30(3)269-271(2020) 5.Wilson, S.Z., Knight, V., Wyde, P.R., et al.Amantadine and ribavirin aerosol treatment of influenza A and B infection in miceAntimicrob. Agents Chemother.17(4)642-648(1980)

10-Norparvulenone is a fungal metabolite originally isolated fromMicrosphaeropsis.1It decreases viral sialidase activity in, and increases survival of, MDCK cells infected with the mouse-adapted influenza virus A/PR/8/34 when used at a concentration of 1 μg/ml. 1.Fukami, A., Nakamura, T., Kim, Y.P., et al.A new anti-influenza virus antibiotic, 10-norparvulenone from Microsphaeropsis sp. FO-5050J. Antibiot. (Tokyo)53(10)1215-1218(2000)

Influenza virus-IN-1 (compound 14) is a potent inhibitor of influenza A virus, demonstrating anti-influenza A virus activities with a CC50 of >200 μM and an EC50 of 2.46 μM. It exhibits concentration-dependent inhibition activity for PAN endonuclease with an EC50 of 312.36 nM [1].

Influenza virus-IN-2 (compound 19) is a potent inhibitor of influenza A virus with anti-influenza activities, exhibiting a CC50 of 150.85 μM and an EC50 of 2.58 μM. Concentration-dependently, Influenza virus-IN-2 inhibits the PAN endonuclease with an EC50 of 489.39 nM [1].

RSV-IN-4 (Compound 2) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza virus A (IAV), demonstrating anti-RSV activity with an EC50 of 11.76 μM.

RSV-IN-3 (Compound 1) is a dual inhibitor targeting both the respiratory syncytial virus (RSV) and influenza virus A (IAV), with an anti-RSV efficacy demonstrated by an EC50 of 32.70 μM [1].

Influenza A virus-IN-4 (compound 23b), a derivative of Oseltamivir, is a highly effective neuraminidase inhibitor that exerts potent inhibitory effects on influenza viruses [1].

Influenza A virus-IN-5 (Compound 16e) is a highly potent and orally active agent against influenza A virus (IAV), with an IC50 of 1.29 μM. It effectively inhibits viral RNA transcription and replication while maintaining acceptable levels of cytotoxicity [1].

Influenza virus-IN-5 (Compound 5f) is an inhibitor of influenza virus hemagglutinin (HA) with an EC50 of 1 nM against the A H3N2 virus.

Cap-dependent endonuclease-IN-9 is a potent cap-dependent endonuclease (CEN) inhibitor with notable efficacy against the influenza virus, minimal cytotoxicity, enhanced in vivo pharmacokinetics, and robust pharmacodynamics. It effectively suppresses the RNA polymerase activity of Influenza A virus[1].

Influenza virus-IN-6 (Compound 35) is a potent inhibitor of the N-terminal domain of the polymerase acidic protein (PA N) endonuclease subunit of the influenza virus, with an inhibitory concentration 50 (IC 50) value of 0.20 μM [1].