hbv-in-4

HBV-IN-4, a derivative of phthalazinone, functions as a potent, orally active inhibitor of HBV DNA replication, exhibiting an IC50 value of 14 nM. It effectively induces the formation of genome-free capsids, demonstrating significant anti-HBV potency[1].

HBV-IN-48, an HBV inhibitor, exhibits potent antiviral activity against HBV in HepDE19 cells, demonstrated by its EC 50 value of 0.005 μM. Additionally, it effectively reduces serum HBV DNA levels in mouse models of HBV infection.

HBV-IN-44 (Compound (S)-2a) is an HBV inhibitor with an IC50 value of 23 nM against HbsAg. It exhibits minimal toxicity in HT22 cells and in the neurite outgrowth of ex vivo mouse DRG neurons.

HBV-IN-45 is a selective and orally bioavailable HBV capsid assembly modulator, with an IC50 of 0.51 μM for HBcAg in HBC cells. [HBV-IN-45] demonstrates potent anti-HBV activity.

HBV-IN-40 (Compound 11826096), with an IC50 of 0.7 µM, serves as a potent HBV inhibitor and exhibits antiviral activity [1].

HBV-IN-41 (compound 45) is a potent, orally active inhibitor of Hepatitis B Virus (HBV) with an EC50 value of 0.027μM [1].

HBV-IN-43 (compound 5832) serves as a potent inhibitor of HBV [1].

HBV-IN-46 (compound 1.6), an active metabolite, acts as an inhibitor of the HBVS antigen, exhibiting an EC50 value of 2.6 nM.

HBV-IN-47 (compound 4a) functions as a capsid assembly modulator with activity against the hepatitis B virus (HBV). It exhibits potent anti-HBV activity in HepAD38 cells and has low toxicity (EC50=0.24 μM). This compound is applicable for research into chronic hepatitis B (CHB).

Helioxanthin derivative 5-4-2 (Helioxanthin 5-4-2) is an analogue of helioxanthin that shows anti-HBV activity in vitro and can be used to study HBV.

Isothiafludine (NZ-4) is an orally active anti-HBV compound that acts by blocking the encapsulation of pre-genomic RNA (pgRNA) and interfering with nucleosome capsid assembly, and is used in the study of HBV infections.

Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 |1. Yeh, S.F., Pan, W., Ong, G.-T., et al. Study of structure-activity correlation in destruxins, a class of cyclodepsipeptides possessing suppressive effect on the generation of hepatitis B virus surface antigen in human hepatoma cells. Biochem. Biophys. Res. Commun. 229(1), 65-72 (1996).|2. Male, K.B., Tzeng, Y.-M., Montes, J., et al. Probing inhibitory effects of destruxins from Metarhizium anisopliae using insect cell based impedance spectroscopy: Inhibition vs chemical structure. Analyst 134(7), 1447-1452 (2009).|3. Buchwaldt, L., and Green, H. Phytotoxicity of destruxin B and its possible role in the pathogenesis of Alternaria brassicae. Plant Pathol. 41(1), 55-63 (1992).

1, 2, 3, 4, 6-Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) and gallic acid from Pistacia lentiscus have antimutagenic and antioxidant activities. 2. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose (PGG) possesses potent anti-proliferative and anti-invasive effects, it also has inhibition of inducible nitric oxide synthase and cyclooxygenase-2 activity. 3. PGG may serve as a model for the development of new types of anti-diabetic and anti-metabolic syndrome therapeutics. 4. 1, 2, 3, 4, 6-Penta- O -galloyl-β- d -glucose has vasodilatory and anti-inflammatory effects, it dilates vascular smooth muscle and suppresses the vascular inflammatory process via endothelium-dependent nitric oxide (NO)/cGMP signaling. 5. 1, 2, 3, 4, 6-Penta-O-galloyl-beta-D-glucose can decrease the level of extracellular hepatitis B virus (HBV) (IC5, 1. microg/ml) in a dose-dependent manner, it also can reduce the HBsAg level by 25% at a concentration of 4 microg/ml; the gallate structure of PGG may play a critical role in the inhibition of anti-HBV activity, suggests that PGG could be a candidate for developing an anti-HBV agent. 6. 1, 2, 3, 4, 6-Penta-O-galloyl-β-D-glucose has anti-parasitic activity, displays an EC5 value of 67 μM, at least 6.6-fold more effective than the standard drug benznidazole against trypomastigote forms of T. cruzi.

1. Swertianolin (Bellidifolin-8-O-Glucoside), mangiferin, rhodenthoside A-C, isoorientin, isovitexin, and amarogentin would serve as potential chemotaxonomic markers to differentiate Gentianaceae species. 2. Swertianolin and swertiamarin show significant hepatoprotective effect in the liver damage model induced by alpha-naphthylisot hiocyanate. 3. Swertianolin shows anti-acetylcholinesterase activity effects. 4. Swertianolin shows that it can scavenge superoxide and hydroxyl radicals with the studying method of the autoxidation of Pyrogallol and afenton.

HBV-IN-21 (Compound II-8b) is a potent inhibitor of HBV DNA replication with an IC50 of 2.2 μM and demonstrates favorable binding affinity (K D = 60.0 μM) for the HBV 4 capsid protein, enabling effective interaction [1].

TLR8 agonist 4 was effective in inhibiting both wild-type and drug-resistant (lamivudine and entecavir) HBV strains with their IC50 values of 0.15 and 0.10 μM, respectively.

Acutumidine (compound 4) is an alkaloid with anti-HBV activity that can be isolated from Hypserpa nitida Miers. It has an inhibitory effect on the production of HBsAg in the Hep G2.2.15 cell line, which is stably transfected with the HBV genome, with an IC50 of 2.023 mM.