Geranyl phenyl ethers from Illicium micranthum and their anti-HBV activity / 中国天然药物

Fourteen new geranyl phenyl ethers (1-14) along with three known compounds (15-17) were isolated from Illicium micranthum, and their structures were elucidated by comprehensive spectroscopic methods. Illimicranins A-H (1-8) were characterized as geranyl vanillin ethers, while 9 and 10 were dimethyl acetal derivatives. Illimicranins I and J (11 and 12) were rare geranyl isoeugenol ethers. Illimicranins K and L (13 and 14) represented the first example of geranyl guaiacylacetone ether and geranyl zingerone ether, respectively. Compounds 1, 2 and 15 exhibited anti-HBV (hepatitis B virus) activity against HBsAg (hepatitis B surface antigen) and HBeAg (hepatitis B e antigen) secretion, and HBV DNA replication.

Design, virtual screening, synthesis and anti-hepatitis B virus of oxime derivatives / 药学学报

A series of new oxime and oxime ethers compounds were designed and virtually screened with target using the Molecular Operating Environment (MOE) software. Twelve unreported compounds including 4 oximes and 8 oxime ethers were synthesized with benzene, toluene, methoxybenzene and chlorobenzene as initial raw materials. Structures of compounds were elucidated by 1H NMR, 13C NMR and MS. The results of bioactive screening showed that a part of compounds displayed obviously anti-HBV activities. Inhibitory activities of compounds 4B-2 in secretion of HBsAg and HBeAg were IC50 HBsAg=81.15 μmol·L-1, SIHBsAg=9.20 and IC50 HBeAg=90.66 μmol·L-1, SIHBeAg8.24, respectively. Preliminary structure-activity relationship study shows that methyl oxime ethers displayed better anti-HBV activities than the oximes.

Synthesis and anti-HBV activity evaluation of Matijin-Su derivatives with aromatic heterocycles / 中国药科大学学报

@#Hepatitis B virus(HBV)-infected hepatitis is one of the most common infectious disease worldwide. To find novel effective anti-HBV agents, a series of Matijin-Su(MTS)derivatives with aromatic heterocycles were synthesized and evaluated for their anti- HBV activities in HepG2 2. 2. 15 cells. Among them, compounds 7a(IC50=2. 94 μmol/L)and 9a(IC50=2. 21 μmol/L)exhibited more potent inhibitory activity against the replication of HBV DNA in HepG2 2. 2. 15 cells than that of lead compound MTS(IC50=11. 16 μmol/L). Notably, both 7a and 9a displayed a high selective index(SI)of 146. 39 and > 250, respectively, which were also much higher than that of MTS(SI=10. 78). Therefore, compounds 7a and 9a may be promising anti-HBV agents with safety profile for HBV infection.

A new sesquiterpene lactone from the fruits of Illicium henryi / 中国天然药物

AIM@#To study the chemical constituents of the fruits of Illicium henryi.@*METHOD@#Chromatographic separations on silica gel, Sephadex LH-20 gel and MCI gel were used to isolate the compounds. The structures were elucidated based on extensive spectroscopic data analyses.@*RESULTS@#Seven compounds were obtained and their structures were identified as 10-benzoyl-cycloparvifloralone (1), cycloparvifloralone (2), 2α-hydroxycycloparviforalone (3), henrylactone B (4), merrillianone (5), henrylactone C (6) and 7, 14-ortholactone- 3-hydroxyfloridanolide (7).@*CONCLUSION@#Compound 1 is a new sesquiterpene lactone. The tested compounds showed weak anti-HBV activities on HBV surface antigen (HBsAg) secretion and HBV e antigen (HBeAg) secretion using Hep G2.2.15 cell line.

Anti-hepatitis virus constituents from Corydalis saxicola / 中草药

Objective To study the anti-HBV constituents from Corydalis saxola. Methods The constituents were repeatedly purified by column chromatography and were identified on the basis of spectral analysis and comparison of their spectral data with those previously reported. Compounds isolated in large amounts were assayed against HBV. Results Sixteen compounds were identified to be dihydrosanguinarine (1), d-corydaline (2), cavidine (3), stylopine (4), 6-acetonyl-5, 6-dihydrosanguinarine (5), dihydrochelerythrine (6), tetrahydropalmatine (7), adlumidine (8), (-)-salutaridine (9), palmatine (10), protopine (11), berberine (12), coptisine (13), thalifaurine (14), dehydroapocavidine (15), and (+)-magnoflorine (16). Compounds 5, 6, 8-11, 13, and 16 with high amounts were chosen to detect anti-HBV activities. Compounds 5 and 8 were moderately active, compounds 11 and 16 showed weak inhibitory effects, while compound 6 exihibited the most potent activity against HBsAg and HBeAg secretions in HepG 2.2.15 cell line, followed by compound 9. Conclusion Compounds 1, 4-6, 8, 9, 13, 14, and 16 are isolated from C. saxicola for the first time. Compound 10 is the main constituent and compound 6 exihibits the most potent activity against HBV.

Expression of IL-29 cDNA in cos-7 cells and its anti-HBV activity in vitro / 中国免疫学杂志

Objective: To clone cDNA of human interleukin-29(IL-29) and express it in cos-7 cells, and to study its anti-HBV activity in vitro. Methods: Total RNA was extracted from PBMCs which had been infected with vesicular stomatitis virus(VSV) in vitro.IL-29 cDNA was amplified using one-step RT-PCR technique. The recombinant expressing plasimd of psectagB/His-myc-IL29 was constructed by inserting IL-29 cDNA into the vector and was then transfected into cos-7 cells. Stable expression stains were screened by Hygromycin B and limited dilution method. The target protein was purified through Ni2+-chelating Sepharose Fast Flow. Anti-viral bioactivity of the recombinant IL-29 fusion protein was analyzed through an in vitro model of production of HBV by the HepG2.2.2.15 cell line.ELISA was used for detection of the viral titers in the cell cultural supernants. Results: IL-29 was cloned and stably expressed in cos-7 cells successfully. SDS-PAGE and Western blot analysis showed multiple bands of the target protein with the molecular weights between 20 000 and 33 000, and the major band was located at about 33 000, indicating the fused IL-29 modified by additional glycosylation. The rhIL-29 was shown to dose-dependently inhibit secretion of HBsAg and HBeAg accompanied by the reduction of HBV genomic DNA in the cells tested. The inhibition ratio of HBsAg and HBeAg production was attained 85% at a concentration of 160 ?g/L of rhIL-29. Conclusion: The rhIL-29 with anti-HBV activity has been obtained.