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Two new secoiridoids, swerpatic acid (1) with an unusual C8skeleton and swerpalactone (2), were isolated along with ten known compounds (3–12) from the whole plants ofSwertia patens. Their structures were elucidated by comprehensive spectroscopic analyses. Eight compounds were evaluated for their anti-hepatitis B virus (HBV) activities on Hep G 2.2.15 cell linein vitro. Compounds4and10showed moderate inhibitory activities on the secretion of HBsAg with IC50values of 1.96 and 0.50 mM. [ABSTRACT FROM PUBLISHER]

Three new flavones named 5-carboxymethyl-4′,7-dihydroxyflavone (1), its ethyl ester (2) and butyl ester (3) were isolated from the herb Selaginella moellendorffii Hieron., together with ten known compounds. Their structures were elucidated on the basis of spectroscopic and chemical analysis. Selected compounds were evaluated for their anti-HBV and cytotoxic activity. Among them, compounds 2 and 3 displayed inhibitory activity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the Hep G2.2.15 cell line with IC50 values of 0.17mg/ml and 0.46mg/ml, and on HBV e antigen (HBeAg) secretion with IC50 values of 0.42mg/ml and 0.42mg/ml, respectively. Compounds 7, 8, 10 and 12 exhibited selective cytotoxicity against the three human cancer cell lines tested. [Copyright &y& Elsevier]

Abstract Hepatitis B virus (HBV) infection causing acute and chronic hepatitis is a serious problem worldwide, whereas the current treatment methods are unsatisfactory. Traditional Chinese herbs that have long been used for medicinal purposes are fascinating sources for novel anti-HBV candidates. This paper summarizes the progress of anti-HBV constituents from diverse medicinal plants in China to provide information for searching new anti-HBV drugs from natural sources. Graphical Abstract

Ethnopharmacological relevance Artemisia capillaris (Yin-Chen) is a famous traditional Chinese medicine (TCM) for treating acute and chronic hepatitis in China. Enynes are one type of characteristic constituents in this herb, while their anti-hepatitis B virus (anti-HBV) properties have not been systemically investigated. Aim of the study This study is to reveal the active part of A. capillaris , and systemically investigate the enynes and their anti-HBV activity. Materials and methods The total extract and each fraction of A. capillaris were assayed for the anti-HBV activity to reveal the active part. Bioassay-guided fractionation using various chromatographic techniques yielded the enynes, whose structures were elucidated by spectroscopic analyses and ECD calculations. The anti-HBV properties inhibiting HBsAg and HBeAg secretions and HBV DNA replication were evaluated on HepG 2.2.15 cell line in vitro . Results ACT-2 and ACT-3 was revealed to be the respective active and toxic part of A. capillaris . Twelve enynes ( 1 – 12 ) involving four new ones ( 1 – 4 ) and two unusual enyne analogs ( 13 – 14 ) were isolated from the active part (ACT-2). All the isolates were assayed for their anti-HBV activity, and the preliminary structure-activity relationships were summarized based on the structural features. In particular, compound 4 could significantly inhibit the secretions of HBsAg and HBeAg, and HBV DNA replication with IC 50 values of 197.2 (SI > 5.1), 48.7 (SI > 20.5) and 9.8 (SI > 102) μM. Conclusions Enynes are responsible for the anti-HBV effects of A. capillaris . Hydroxyl and glycosyl groups are preferable for maintaining activity. This is the first time to systematically investigate the anti-HBV activity of enynes in A. capillaris , which provides valuable information for understanding the ethnopharmacological application of Yin-Chen. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Yin-Chen is a famous traditional Chinese medicine (TCM) in China for the treatment of acute and chronic hepatitis. Two species, namely Artemisia scoparia and Artemisia capillaris , are documented in Chinese Pharmacopoeia as the authentic resources for Yin-Chen. Previous investigation has proved that chlorogenic acid analogs and phenolic acids are two main types of the anti-HBV active constituents of A. capillaris . However, there is no investigation concerned with the anti-HBV components of A. scoparia. Aim of the study The aim of the present study is to recognize the new anti-HBV constituents of A. scoparia by detailed LCMS analyses. Materials and methods LCMS and bioassay-guided fractionation on the active part of A. scoparia led to the isolation of three new compounds. Their structures were determined by detailed spectroscopic analyses. Anti-HBV assay involving inhibition on HBsAg and HBeAg secretions and HBV DNA replication were performed in virto on HepG 2.2.15 cell line. Results The 90% ethanol extract of A. scoparia was revealed with anti-HBV activity for the first time, which was further separated into several fractions by column chromatography. Fr. D-4 was revealed with the highest anti-HBV activity, from which three new compounds including one unusual 4-pyridone glucoside ( 1 ) and two polyacetylene glucosides ( 2 – 3 ) were isolated under the guidance of LCMS analyses. Compounds 1 – 3 exhibited activity against the secretions of HBsAg and HBeAg, and HBV DNA replication. In particular, compounds 2 and 3 inhibited HBV DNA replication with IC 50 values of 0.07±0.04 and 0.012±0.05 mM, with SI values of 23.6 and 17.1, respectively. Based on the MS/MS experiment, the fragmentation pathways of 1 in both positive and negative modes, and 2 and 3 in negative mode were proposed. The ion pairs of 388–208 (positive) and 432–206 (negative) for 1 , 503–341 (negative) for 2 , and 503–203 (negative) for 3 , could be recognized as their respective diagnostic ions. Conclusions The first time investigation on the anti-HBV constituents of A. scoparia yielded three new active compounds, which will provide valuable information for understanding the ethnopharmacological usage of Yin-Chen, as well as the chemical difference with A. capillaris . [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The rhizome of Cyperus rotundus ( C. rotundus ) is a well-known traditional Chinese medicine to cure hepatitis in many formulae, but the active components responsible for hepatitis have not been elucidated. According to our bioassay on HepG2.2.15 cell line in vitro , the ethanol extract of C. rotundus demonstrated potent anti-HBV activity. This current study was designed to isolate and identify the anti-HBV active constituents from the rhizomes of C. rotundus . Material and methods Bioactivity and LC-MS guided fractionation on the extract of C. rotundus using various chromatographic techniques including open-column, Sephadex LH-20 and semi-preparative high performance liquid chromatography led to the isolation and identification of thirty-seven sesquiterpenoids. Structural elucidation of the isolates was carried out by extensive spectroscopic analyses (UV, IR, HRMS, 1D- and 2D –NMR). The anti-HBV activity and cytotoxicity were evaluated on the HBV-transfected HepG2.2.15 cell line in vitro . The cytotoxicity effects of the isolates were assessed by a MTT assay. The secretions of HBsAg and HBeAg in the culture medium were detected by ELISA method, and the load of HBV DNA was quantified by real-time fluorescent PCR technique. Results Five new patchoulane-type sesquiterpenoids, namely cyperene-3, 8-dione ( 1 ), 14-hydroxy cyperotundone ( 2 ), 14-acetoxy cyperotundone ( 3 ), 3 β -hydroxycyperenoic acid ( 4 ) and sugetriol-3, 9-diacetate ( 5 ), along with 32 known sesquiterpenoids were isolated from the active fractions of C. rotundus . Compounds 2 and 3 were the first cyperotundone-type sesquiterpenoids with a hydroxyl group at C-14 position. Nine eudesmane-type sesquiterpenoids ( 15 – 21 and 23 – 24 ) significantly inhibited the HBV DNA replication with IC 50 values of 42.7±5.9, 22.5±1.9, 13.2±1.2, 10.1±0.7, 14.1±1.1, 15.3±2.7, 13.8±0.9, 19.7±2.1 and 11.9±0.6 μM, respectively, of which, compounds 17 , 21 , 23 and 24 possessed high SI values of 250.4, 125.5,>259.6 and 127.5, respectively. Two patchoulane-type sesquiterpenoids ( 4 and 7 ) effectively suppressed the secretion of HBsAg in a dose-dependent manner with IC 50 values of 46.6±14.3 (SI=31.0) and 77.2±13.0 (SI=1.7) μM, respectively. Compounds 2 , 8 , 12 , 15 , 17 and 25 possessed moderate activities against HBeAg secretion with IC 50 values of 162.5±18.9 (SI=13.3), 399.2±90.0 (SI=10.6), 274.7±70.8 (SI=5.2), 313.9±87.5 (SI=7.2), 334.0±70.4 (SI=9.9) and 285.3±20.9 (SI=15.5) μM, respectively. Conclusions This is the first study to reveal the anti-HBV constituents of C. rotundus , demonstrating that the eudesmane-type sesquiterpenoids might contribute to the anti-HBV activity of the rhizomes of C. rotundus . [ABSTRACT FROM AUTHOR]

Three new secoiridoid aglycones of (−)-swermusic acid A ( 1 ) and B ( 3 ), and (−)-swerimuslatone A ( 2 ), and four new secoiridoid glycosides of 6′- O -formylsweroside ( 4 ), 6′- O -formylgentiopicroside ( 5 ), 6′- O -acetylamarogentin ( 6 ) and 6′- O -acetylamaronitidin ( 7 ), along with 40 known compounds ( 8 – 47 ) were isolated from Swertia mussotii . Their structures were elucidated on the basis of extensive spectroscopic analyses including MS, IR, UV, 1D- and 2D-NMR. Forty-five compounds from S. mussotii were evaluated for their anti-HBV activity on the HepG 2.2.15 cell line in vitro inhibiting the secretions of HBsAg and HBeAg, as well as HBV DNA replication. Six of the nine phenols 26 – 29 , 31 and 32 exhibited activities inhibiting HBsAg and HBeAg secretion with IC 50 values from 0.23 to 5.18 mM, and HBV DNA replication with IC 50 values from < 0.06 to 2.62 mM. Moreover, isooriention ( 45 ) displayed significant anti-HBV activities against secretions of HBsAg and HBeAg with IC 50 value of 0.79 and 1.12 mM, as well as HBV DNA replication with IC 50 value of 0.02 mM. [ABSTRACT FROM AUTHOR]

Five new secoiridoid glycosides, swericinctosides A and B ( 1 – 2 ), 9- epi swertiamarin ( 3 ), 2′- O - m -hydroxybenzoyl swertiamarin ( 4 ), 4″- O -acetyl swertianoside E ( 5 ), and one unusual lactonic enol ketone, 3-(hydroxymethyl ene) dihydro- 2H -pyran-2, 4( 3H )-dione ( 6 ), together with three known compounds, swertiaside ( 7 ), swertianoside C ( 8 ) and decentapicrin B ( 9 ) were isolated from Swertia cincta . The structures of the new compounds were determined by extensive spectroscopic analyses including 1D and 2D NMR, HRESIMS, UV, IR and [α] D spectra. Anti-HBV assay on HepG 2.2.15 cell line in vitro demonstrated that compounds 1 – 9 possessed inhibitory activity on HBV DNA replication with IC 50 values from 0.05 to 1.83 mM, and compounds 1 , 3 , 5 , 7 and 8 could inhibit the secretion of HBsAg with IC 50 values from 0.24 to 1.06 mM. [ABSTRACT FROM AUTHOR]

p -Hydroxyacetophenone ( p -HAP), as a main hepatoprotective and choleretic constituent of Artemisia capillaris , was revealed with anti-hepatitis B virus (HBV) effects in recent investigation. In addition to p -HAP, four derivatives of p -HAP were also isolated from A. capillaris by various chromatographic methods. Subsequent structural modification on p -HAP and its glycoside led to the synthesis of 28 additional derivatives, of which 13 compounds showed activity inhibiting hepatitis B surface antigen (HBsAg) secretion; and 18 compounds possessed inhibition on HBV DNA replication. The primary structure–activity relationships (SARs) suggested that the conjugated derivatives of p -HAP glycoside and substituted cinnamic acids ( 2a – 2i ) obviously enhanced the activity against HBV DNA replication with IC 50 values ranged from 5.8 to 74.4 μM. [ABSTRACT FROM AUTHOR]

Twenty-four derivatives of erythrocentaurin (ET) were synthesized and evaluated for their anti-HBV activities on HepG 2.2.15 cell line in vitro. Eight compounds 1 , 2 , 5 , 8 , 9 , 1e , 1k , and 1m increased activity against HBV DNA replication with the SI values higher than 11. In particular, derivatives 1e and 1k exhibited the most potent inhibition on HBV DNA replication with the IC 50 values of 0.026 mM (SI >70.8) and 0.045 mM (SI >36.0), respectively. The primary structure–activity relationships (SARs) of ET derivatives were summarized for exploring potent anti-HBV agents. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Hepatitis B induced by HBV is a serious health problem. Artemisia capillaris (Yin-Chen) has long been used to treat hepatitis in traditional Chinese medicine. Coumarins, flavonoids and organic acids were revealed as its hepatoprotective and choleretic components, but its anti-HBV active components remain unknown. This current study focused on its anti-HBV active constituents by various chromatographic methods. Material and methods LC/MS and bioassay-guided fractionation on the active extract of Artemisia capillaris led to the isolation of nine chlorogenic acid analogues. Structures of the isolates were elucidated by MS/MS and NMR techniques. Anti-HBV assay was performed on HepG 2.2.15 cell line in vitro : reduction of HBsAg and HBeAg secretions was measured by an ELISA method; inhibition of HBV DNA replication was monitored by real-time quantitative PCR and cellular toxicity was assessed by a MTT method. Results The 90% ethanol extract of Artemisia capillaris (Fr. AC) showed significantly inhibitory activity on HBV DNA replication with an IC 50 value of 76.1±3.9 μg/mL and low cytotoxic effects (SI>20.1). To clarify its active constituents, the extract was further separated into 3 sub-fractions (AC-1, AC-2 and AC-3), of which Fr. AC-2 was the most active fraction against HBeAg secretion and HBV DNA replication with IC 50 values of 44.2±2.8 and 23.2±1.9 μg/mL. Nine chlorogenic acid analogues were detected from the active part (Fr. AC-2) by a LC/MS technique and further separated by a HPLC method. The isolates were determined as chlorogenic acid ( 1 ), cryptochlorogenic acid ( 2 ), neochlorogenic acid ( 3 ), 3,5-dicaffeoylquinic acid ( 4 ), 4,5-dicaffeoylquinic acid ( 5 ), 3,4-dicaffeoylquinic acid ( 6 ), chlorogenic acid methyl ester ( 7 ), cryptochlorogenic acid methyl ester ( 8 ), neochlorogenic acid methyl ester ( 9 ). Compounds 1 – 6 possessed potent activity against HBV DNA replication with IC 50 values in the range of 5.5±0.9–13.7±1.3 μM. Di-caffeoyl analogues ( 4 – 6 ) also exhibited activity against the secretions of HBsAg and HBeAg. Esterified analogues ( 7 – 9 ) showed dramatically decreased anti-HBV activity, indicating that carboxyl group is closely associated to the anti-HBV activity. Conclusions This investigation was focused on the active fractions of Artemisia capillaris and their active compositions, which showed that Fr. AC-2 was the main active section of Artemisia capillaris and chlorogenic acid analogues were the main constituents contributing to its anti-HBV activity. These results support the ethnopharmacological use of Artemisia capillaris as anti-HBV agents. [ABSTRACT FROM AUTHOR]

Abstract: Three new polyacetylenes, 8-(Z)-decene-4, 6-diyne-1, 3, 10-triol (1), 1, 3S, 8S-trihydroxydec-9-en-4, 6-yne (2), 3S, 8S-dihydroxydec-9-en-4, 6-yne 1-O-β -D-glucopyranoside (3), and one new glucosyl caffeoate, 1-O-ethyl-6-O-caffeoyl-β -D-glucopyranose (4), together with 34 known compounds were isolated from Artemisia capillaris. The structures of the new compounds were determined by extensive spectroscopic analyses including 1D and 2D NMR, HRESIMS, [α]D and CD experiments. Among them, 19 compounds showed activity inhibiting HBsAg secretion; 20 compounds showed activity inhibiting HBeAg secretion; and 25 compounds possessed inhibitory activity against HBV DNA replication according to our anti-HBV assay on HepG 2.2.15 cell line in vitro. The most active compound 12 could inhibit not only the secretions of HBsAg and HBeAg, but also HBV DNA replication with IC50 values of 15.02μM (SI=111.3), 9.00μM (SI=185.9) and 12.01μM (SI=139.2). [Copyright &y& Elsevier]

Abstract: Dehydroandrographolide and andrographolide, two natural diterpenoids isolated from Andrographis paniculata possessed activity against HBV DNA replication with IC50 values of 22.58 and 54.07μM and low SI values of 8.7 and 3.7 in our random assay. Consequently, 48 derivatives of dehydroandrographolide and andrographolide were synthesized and evaluated for their anti-HBV properties to yield a series of active derivatives with lower cytotoxicity, including 14 derivatives against HBsAg secretion, 19 derivatives against HBeAg secretion and 38 derivatives against HBV DNA replication. Interestingly, compound 4e could inhibit not only HBsAg and HBeAg secretions but also HBV DNA replication with SI values of 20.3, 125.0 and 104.9. Furthermore, the most active compound 2c with SI value higher than 165.1 inhibiting HBV DNA replication was revealed with the optimal log P value of 1.78 and log D values. Structure–activity relationships (SARs) of the derivatives were disclosed for guiding the future research toward the discovery of new anti-HBV drugs. [Copyright &y& Elsevier]

Abstract: Three new secoiridoids, swermacrolactones A–C (1–3), together with fourteen known compounds were isolated from Swertia macrosperma. Their structures were elucidated based on extensive spectroscopic analyses (IR, UV, MS, 1D and 2D NMR). By anti-HBV assay on the Hep G 2.2.15 cell line in vitro, the most active compound, luteolin (9), inhibited the secretion of hepatitis B virus surface antigen (HBsAg) and hepatitis B virus e antigen (HBeAg) with IC50 values of 0.02 and 0.02mM, respectively. [Copyright &y& Elsevier]

Abstract: Four new triterpenoids, sweriyunnangenin A (1), sweriyunnanosides A (2), B (3) and C (4), along with nineteen known compounds (5–23) were isolated from Swertia yunnanensis. Based on extensive spectroscopic analyses (1D- and 2D-NMR, HRESIMS, UV, IR, [α]D), the structures of sweriyunnangenin A (1), sweriyunnanosides A (2), B (3) and C (4) were elucidated as taraxer-14-ene-3α,6β-diol, oleanolic acid 28-O-β-d-glucopyranosyl-(1→2)-O-β-d-glucopyranoside, 2α,3β-di-hydroxyolean-12-en-28-oic acid 28-O-β-d-glucopyranosyl(1→6)-β-d-glucopyranosyl (1→6)-β-d-glucopyranosyl(1→2)-β-d-glucopyranoside and hederagenin 28-O-β-d-glucopyranosyl(1→6)-β-d-glucopyranosyl(1→6)-β-d-glucopyranosyl(1→2)-β-d-glucopyranoside, respectively. Twenty-two compounds were evaluated for their anti-HBV activities on the HepG 2.2.15 cell line in vitro, of which nine compounds showed potent anti-HBV activities. Compounds 1, 5–6, 14–16 and 19 showed activities against the secretion of HBsAg (IC50 values from 0.10 to 1.76mM) and HBeAg (IC50 values from 0.04 to 1.41mM), and compounds 11 and 13–16 exhibited significant inhibition on HBV DNA replication (IC50 values from 0.01 to 0.09mM). [Copyright &y& Elsevier]

Abstract: In the screening search for Hepatitis B virus inhibitory agents from medicinal plants, the ethanol extract of Piper longum Linn. was found to possess superior anti-HBV activity in vitro. Bioassay-guided fractionation coupled with repeated purification resulted in the isolation of four new compounds, involving two new glycosides longumosides A (1) and B (2) and two new amide alkaloids erythro-1-[1-oxo-9(3,4-methylenedioxyphenyl)-8,9-dihydroxy-2E-nonenyl]-piperidine (3), threo-1-[1-oxo-9(3,4-methylenedioxyphenyl)-8,9-dihydroxy-2E-nonenyl]-piperidine (4), as well as two compounds 3β,4α-dihydroxy-2-piperidinone (5), 5,6-dihydro-2(1H)-pyridinone (6) from natural source for the first time. The structures of the four new compounds were determined by extensive analyses of the MS, IR, 1D and 2D NMR data. Besides, the compounds 2–6, together with the known compounds 7–11 obtained previously, were assayed for their anti-HBV activity by using Hep G 2.2.15 cell line in vitro. Results suggested the compound piperine (7) possessed remarkable inhibitory HBV activity, against the secretion of hepatitis B virus surface antigen (HBsAg) and hepatitis B virus e antigen (HBeAg) with the Selectivity Index (SI) values of 15.7 and 16.8, respectively. [Copyright &y& Elsevier]

Abstract: Fifty-seven derivatives of glycyrrhetinic acid (GA) were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Among them, sixteen compounds showed greater anti-HBV activity than GA, especially, compounds 29, 32, 35, 41 exhibited significantly inhibitory activities against HBV DNA replication with IC50 values of 5.71, 5.36, 8.90 and 9.08μM, respectively. The structure–activity relationships (SARs) of GA derivatives were discussed for exploring novel anti-HBV agents. [Copyright &y& Elsevier]

Abstract: A series of caudatin derivatives were synthesized, and their anti-hepatitis B virus (HBV) activity was evaluated in HepG 2.2.15 cells. Most of the 3-O-substituted caudatin derivatives showed effective anti-HBV activity. Among the tested compounds, six compounds (2e–2h, 2l, 2r) exhibited significantly inhibitory activity against HBV DNA replication with IC50 values in the range of 2.82–7.48μM. Interestingly, two compounds (2e, 2f) had potent activity inhibiting not only the secretion of HBsAg (IC50 =18.68μM, 21.71μM), HBeAg (IC50 =13.16μM, 33.73μM), but also HBV DNA replication (IC50 =7.48μM, 3.63μM). The structure–activity relationships (SARs) of caudatin derivatives had been discussed, which were useful for caudatin derivatives to be explored and developed as novel anti-HBV agents. [Copyright &y& Elsevier]

Abstract: Thirty-two tetra-acylated derivatives of alisol A were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. Among the series of alisol A derivatives examined, five analogues were active against HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion in HepG 2.2.15 cells. These results also provide interesting structure–activity relationships of tetra-acylalisol A derivatives. Compounds tetra-acetyl alisol A (A1), tetra-methoxyacetyl alisol A (A23), and tetra-ethoxyacetyl alisol A (A24) exhibited high activities against secretion of HBsAg with IC50 values of 0.0048, 0.0044, and 0.014mM, respectively, HBeAg with IC50 values of 0.011, 0.012, and 0.018mM, respectively, and remarkable selective index values SIHBsAg >333, SIHBeAg >145; SIHBsAg =209, SIHBeAg =77; and SIHBsAg >200, SIHBeAg >156, respectively. Additional studies in rats showed that compound A1 has favorable pharmacokinetic prosperities for further development purpose, with elimination half-time (t 1/2) of 1.63h and oral bioavailability (F) of 40.9%. [Copyright &y& Elsevier]

Abstract: Chemical modifications were performed on hydroxyl groups at C-11,23,24,25 positions and C-13(17) double bond of alisol A for structure–activity relationship study. Forty-one derivatives of alisol A were synthesized and assayed for their in vitro anti-hepatitis B virus (HBV) activities and cytotoxicities. Of them, 14 compounds were active against HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) secretion in HepG 2.2.15 cells, and the most promising compound 25 exhibited high activities against secretion of HBsAg (IC50 =0.028mM), HBeAg (IC50 =0.027mM) and remarkable selective indices (SIHBsAg >90, SIHBeAg >93). [Copyright &y& Elsevier]

Abstract: A class of C29 triterpene dilactones (1–6) featuring 18(13→14)-abeo-schiartane skeleton have been isolated from the stems of Schisandra propinqua var. propinqua. The structures of new compounds, propindilactones K–O (1–5), were determined on the basis of comprehensive spectroscopic means. Biogenetic pathway of 1–6 was proposed and then chemically mimicked. The absolute stereochemistries of new compounds were established on biosynthetic consideration coupled with CD experiments. Compound 2 showed promising anti-HBV activity in vitro. [Copyright &y& Elsevier]

Abstract: A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC50 =0.024mM), HBV e antigen (IC50 =0.028mM) and remarkable selective indices (SIHBsAg >108, SIHBeAg >93), which was selected for further evaluation as a novel HBV inhibitor. [Copyright &y& Elsevier]

Abstract: Two new alkaloids, hypserpanines A and B (1, 11), together with eleven known compounds, phenolbetain (2), acutumine (3), acutumidine (4), dechloroacutumine (5), dauricumine (6), dauricumidine (7), pronuciferine (8), glaziovine (9), S-reticuline (10), magnoflorine (12) and laurifoline(13), were isolated from Hypserpa nitida Miers. (Menispermaceae) and chemically elucidated through spectral analyses. All the isolated alkaloids were evaluated for their anti-HBV activities in vitro using the HBV transfected Hep G2.2.15 cell line. The most active compound, dauricumidine (7), exhibited an IC50 value of 0.450mM (SI=4.13) on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the Hep G2.2.15 cell line. [Copyright &y& Elsevier]

Abstract: Swerpunilactones A (1) and B (2), two novel xanthone and secoiridoid heterodimers, together with their presumed biosynthetic precursors (±)-gentiolactone (3), bellidifolin (4), and norbellidifolin (5), were isolated from the whole plants of Swertia species. A plausible biogenetic pathway for swerpunilactones A and B was proposed. In vitro anti-hepatitis B virus assay on the Hep G 2.2.15 cell line showed that both compounds 1 and 2 exhibited activities against the secretion of HBsAg (IC50 =0.25 and 0.29mM), HBeAg (IC50 =0.86 and 0.31mM), and HBV DNA replication (IC50 =0.18 and 0.19mM). [Copyright &y& Elsevier]

Abstract: A series of 4-aryl-6-chloro-quinolin-2-ones and 5-aryl-7-chloro-1,4-benzodiazepine were synthesized and assayed for their in vitro anti-hepatitis B virus activities and cytotoxicities for the first time. Some of the tested compounds were active against HBsAg and HBeAg secretion in Hep G2.2.15 cells. Compound 5c showed IC50 of 0.074 and 0.449mM on HBsAg and HBeAg secretions, respectively, which were 10 times higher than that of its analog 4c and led to better selective index (SI) values (SI=23.2 and 3.4, respectively). [Copyright &y& Elsevier]