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Oxidative stress is well known to play a pivotal role in cerebral ischemia–reperfusion injury. On the basis of this fact, antioxidative agents have been demonstrated to be neuroprotective. Neohesperidin (NH) is abundant in citrus flavonoids and possesses reactive oxygen species scavenging activity and neuroprotective effectsin vitro. However, little is known about its effects on cerebral ischemia–reperfusion injury and the underlying mechanisms. In this study, we use a rat model of middle cerebral artery occlusion (MCAO) to investigate the neuroprotective effects of NH. NH significantly improved neurological functions and attenuated MCAO-induced infarct volume, pathological changes, and neuronal loss. Moreover, it enhanced antioxidant capacity and suppressed oxidative stress in the brain. NH inhibited the MCAO-induced upregulation of Bax, cytochromec, and cleaved caspase-9 and -3, as well as the downregulation of Bcl-2. Interestingly, NH treatment upregulated heme oxygenase-1 (HO-1) in a concentration-dependent manner, which was due to the NH-mediated activation of the protein kinase B (Akt)/nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. NH also abolished the MCAO-induced inhibition of the Akt/Nrf2 pathway. In conclusion, NH attenuates cerebral ischemia–reperfusion injury via the inhibition of neuronal apoptosis and oxidative stress through the regulation of the apoptotic pathway and the Akt/Nrf2/HO-1 pathway. NH might be a promising preventive agent for ischemic stroke. [ABSTRACT FROM PUBLISHER]

Abstract: Background: The purpose of this phase II study was to determine the efficacy and toxicity of cisplatin and weekly docetaxel combination chemotherapy as a first-line treatment in patients with recurrent or metastatic nasopharyngeal cancer. Patients and Methods: Recurrent or metastatic nasopharyngeal cancer patients were enrolled and received a combination of weekly docetaxel (35mg/m2 on Day1 and Day8) and cisplatin (70mg/m2 D1) every 21days, for up to a maximum of 6 cycles. The primary endpoint was objective response rate, and the secondary endpoints included toxicity of combination chemotherapy, progression-free survival, overall survival and 1-year survival rate. Results: In total, 47 patients were enrolled and analysed, and 46 patients (97.9%) completed the planned protocol. In an intent-to-treat analysis, 6 patients (12.8%) achieved complete response (CR) and 27 patients (57.4%) showed partial response (PR), with an objective response rate of 70.2%. The median progression-free survival and overall survival were 9.6months (95% C.I. 5.7–13.5months) and 28.5months (95% C.I. 16.9–40.1months), respectively, and the 1-year survival rate was 89.9%. The common grade 3 adverse events were stomatitis (1.2%), neutropenia (0.8%), anaemia (0.8%), infection (0.8%) and diarrhoea (0.8%). Grade 4 adverse events were not observed in this study. Conclusions: The combination chemotherapy of cisplatin and weekly docetaxel is highly effective and shows favourable toxicity as a first-line chemotherapy in patients with recurrent or metastatic nasopharyngeal cancer. [Copyright &y& Elsevier]

Simple Summary: In our prior study, we demonstrated that recombinant human epidermal growth factor (rhEGF) treatment is effective for managing epidermal growth factor receptor inhibitors (EGFRIs)-related skin toxicities and improves patients' quality of life (QoL) compared with placebo. Nevertheless, the mechanisms of rhEGF effects are unknown yet so basic study is needed to clarify the mechanisms. In this study, we revealed that treatment of rhEGF in human epidermal keratinocytes, 3d-cultured human skin tissue and patient lesions improved EGFRIs-induced skin eruption via normalizing proliferation and differentiation of keratinocytes, reducing inflammatory cytokines expression and inducing expression of AMPs. These findings provided an evidence for the use of rhEGF as a treatment for skin side effects derived from EGFRI. The mechanisms of epidermal growth factor (EGF) affecting EGF receptor inhibitor (EGFRI)-related skin toxicities are as yet unknown. We investigated which mechanisms are involved in EGF's positive effects. Two types of EGFRIs, cetuximab and gefitinib, were used to treat the cells or 3d-cultured human skin tissue with recombinant human EGF (rhEGF). As a result, rhEGF increased EGFR and pEGFR expression. Furthermore, rhEGF induces EGFR signaling by pAKT and pPI3K expression in gefitinib and rhEGF co-treated cells. In addition, rhEGF bound to EGFR after than cetuximab, but cetuximab bound to EGFR more strongly than rhEGF. Moreover, expressions of proliferation and differentiation proteins, both ki-67 and filaggrin, were decreased in EGFRI-treated tissue. However, in rhEGF and EGFRI co-treated tissue, those expressions were increased. Expression of IL-1α, IL-8, and TNF-α was increased by EGFRIs and down-regulated by rhEGF. Furthermore, hBD-2 and hBD-3 protein expressions were inhibited by cetuximab or gefitinib treatment, and those decrements were increased by rhEGF treatment. In patients' tissue evaluation, compared with controls, patients' Ki-67 and EGFR expression were decreased (p = 0.015, p = 0.001). Patients' IL-17 and TNF-α expression intensity was higher than that of the control group (p = 0.038, p = 0.037). After treatment with EGF ointment, average values of Ki-67, EGFR, and Melan-A were changed to normal values. Oppositely, patients' proportions of IL-17 and TNF-α were decreased to low stain level. In conclusion, treatment of rhEGF improved EGFRI-induced skin eruption via normalizing the proliferation and differentiation of keratinocytes, reducing inflammatory cytokines by the affected EGFRIs. [ABSTRACT FROM AUTHOR]

Objective: Nonsuicidal Self-Injury (NSSI) in China has increasingly interested clinicians, although few studies have investigated its risk and protective factors. This study examined the risk factors of NSSI among Chinese adolescents. Methods: The researchers recruited adolescent participants with NSSI from a hospital outpatient clinic to form a case group and recruited adolescents without NSSI who provided informed consent from the school to form a control group. Participants completed a questionnaire, and data were analyzed using logistic regression. Results: A total of 138 cases and 276 controls participated in this study. Binary multivariate logistic regression analysis with adjusting for age and sex showed that domestic violence (OR = 8.615, 95%CI: 3.081–24.091), parental overconcern (OR = 6.995, 95%CI: 3.447–14.192), guilt (OR = 4.949, 95%CI: 2.227–10.996), and school bullying (OR = 21.676, 95%CI: 6.799–69.109) increased the risk of NSSI, while peer support (OR = 0.068, 95%CI: 0.030–0.150) and living in an urban environment (OR = 0.157, 95%CI: 0.056–0.437) decreased the risk of NSSI. Conclusion: Some psychosocial factors were confirmed to be independent risk and protective factors for NSSI in this study. However, the clinical significance of the results needs to be interpreted with caution due to sample size limitations. [ABSTRACT FROM AUTHOR]

One unusual stilbene trimer-flavonoid hybrid, paeonilactiflobenoid (1), together with six known stilbenes (2–7) were isolated from the seeds of Paeonia lactiflora. The structure of 1 was elucidated with the aid of HRESIMS, 1D and 2D NMR, [ α ] D spectroscopic data and ECD calculation. Compounds 2 – 7 showed stimulative effects on GLP-1 secretion with promoting rates of 79.8%–880.4% (25 μM) and 217.6%–1089.4% (50 μM), more potent than the positive control, oleoylethanolamide (250.2% at 50 μ M). Moreover, compounds 4 and 6 exhibited agonistic activity on the G protein-coupled receptor (GPCR) TGR5 with stimulative ratios of 40.2% and 40.5% at 50 μM, and 54.2% and 49.1% at 100 μM, respectively. Docking study manifested that 6 well located in the catalytic pocket of TGR5 by hydrogen-bond and hydrophobic interactions. The GLP-1 promotion of 6 could be attenuated by IP 3 , Ca2+/CaMKII and MEK/ERK pathway inhibitors, suggesting that these pathways played important roles in GLP-1 secretion. Thus, stilbenes in peony seeds maybe regarded as potential GLP-1 secretagogues through TGR5-IP 3 -Ca2+/CaMKII-MEK/ERK pathways. [Display omitted] • One usual stilbene trimer-flavonoid hybrid was isolated from peony seeds. • Six stilbenes showed stimulative effects on GLP-1 secretion. • Compounds 4 and 6 exhibited agonistic activity on TGR5 receptor. • The GLP-1 promotion of 6 was attenuated by IP 3 , Ca2+/CaMKII and MEK/ERK inhibitors. [ABSTRACT FROM AUTHOR]

Artemdubosides A-E (1–5), the first examples of natural polyacetylenes substituted by 6'- O -crotonyl β- glucopyranoside, and artemdubosides F-G (6–7) that were two unusual polyacetylenes featuring a 6'- O -acetyl β- glucopyranoside moiety, were isolated from Artemisia dubia var. subdigitata. Their structures were elucidated based on the spectral data including HRESIMS, UV, IR, 1D and 2D NMR, and ECD calculations. Antihepatoma assay suggested that compound 1 exhibited activity against HepG2, Huh7, and SK-Hep-1 cells with inhibitory ratios of 77.1%, 90.8%, and 73.1% at 200.0 μM, respectively. [Display omitted] • Artemdubosides A-G (1 – 7) were isolated from Artemisia dubia var. subdigitata. • Compounds 1 – 5 represented the first examples of natural polyacetylenes substituted by 6′-O-crotonyl β-glucopyranoside. • Compounds 6 – 7 represented the first examples of natural polyacetylenes substituted by 6′- O -acetyl β-glucopyranoside. • Compound 1 showed activity against HepG2, Huh7, and SK-Hep-1 cells at 200.0 μM. [ABSTRACT FROM AUTHOR]

Simple Summary: Immune checkpoint inhibitors (ICIs) are currently widely used in many types of cancer. However, some patients could not benefit from ICIs. In addition, a standardized biomarker for predicting the efficacy of ICIs is currently unavailable. Thus, we determined whether peripheral blood immune cells could be predicting markers. In contrast with previous studies, we focused on changes in immune cell fraction and the relationship between efficacy of ICIs including response rate and survival outcomes. Results revealed significant correlations between changes in NKp46-/CD56+ NK cell fraction and treatment outcomes with ICIs. Background: With the development of immunology, immune checkpoint inhibitors (ICIs) have been widely used in various cancer treatments. Although some patients can benefit from ICIs, other patients have no response to ICIs or suffer from hyperprogression. There has been no biomarker for predicting the efficacy of ICIs. Thus, the objective of this study was to find biomarkers for predicting the efficacy of ICIs using peripheral blood. Methods: Adults patients planned to be treated with ICIs were enrolled in this study. Blood sampling was carried out before and after administration of ICIs. Changes of immune cell fraction were analyzed for each patient. Results: Among 182 patients enrolled, immune cell analysis was performed for 90 patients. The objective response rate was 14.4% (n = 13/90). The median progression-free survival (PFS) was 6.0 months (95% CI: 3.1–8.9 months), and the median overall survival (OS) was 13.9 months (95% CI: 5.6–22.2 months). Significant benefits in ORR and OS were shown for patients with increased NKp46-/CD56+ NK cells (p = 0.033 and p = 0.013, respectively). The PFS tended to be longer in these patients, although the difference was not statistically significant (p = 0.050). Conclusion: Changes of immune cell fraction before and after administration of ICIs could be a novel biomarker for predicting the efficacy of immunotherapy. [ABSTRACT FROM AUTHOR]

Background: Vertebral augmentation (VA) techniques are used to treat acute osteoporotic vertebral compression fractures (OVCFs). However, the incidence of recurrent vertebral fractures after VA is controversial. Various factors have been discussed in the literature, but no convincing study on the quality of paraspinal muscles has been reported. The purposes of this study were to evaluate the changes in paraspinal muscles and discuss the relationship between paraspinal muscle degeneration and vertebral refractures after percutaneous kyphoplasty (PKP). Methods: This retrospective study was conducted in patients who underwent PKP for an initial OVCF between July 2017 and August 2018. Patients were followed up and categorized in the refractured or non-refractured group. A final magnetic resonance imaging (MRI) scan and a preoperative MRI scan were used to determine the measurements. The paraspinal muscles at the mid-height level of the initial fractured vertebral body were measured using regions of interest (ROIs), including the cross-sectional area (CSA) and signal intensity (SI). The changes in the observed data were compared between the groups using rank-sum tests. Results: Overall, 92 patients were enrolled in the study; 33 of them sustained vertebral refractures during the follow-up and the other 59 patients did not. There were no significant differences in terms of sex, age, preoperative bone mineral density, and body mass index between the groups (all, P > 0.05). The refractured group had a significantly higher decrease in the ROI-CSA and CSA/SI, and a higher increase in ROI-SI, compared with the preoperative data (all, P < 0.05). Conclusions: The quality of paraspinal muscles significantly decreased in patients with new OVCFs after PKP. This brings a new perspective to the study of postoperative recurrent fractures; patients and physicians need to pay more attention to the efficacy of bed rest and bracing. [ABSTRACT FROM AUTHOR]

Artemeriosides A–F (1 – 6), six novel sesquiterpenoids containing a 6′- O -crontonyl β -glucopyranoside, were isolated from Artemisia annua L. Their structures were determined by spectral data including HRESIMS, IR, UV, 1D and 2D NMR, and ECD calculations. Compounds 1 – 6 represented the first examples of natural sesquiterpenoid substituted by 6′- O -crontonyl β -glucopyranoside. By antihepatoma assay, compounds 1 and 2 demonstrated inhibitory effect against both HepG2 and SK-Hep-1 cells with inhibitory ratios of 77.0%, 88.8%, and 86.8%, 83.9% at 200.0 μM, and compound 1 showed inhibitory activity against Huh7 cells with inhibitory ratio of 56.8%. [Display omitted] • Artemeriosides A–F (1–6) were isolated from A. annua. • Their structures contained 6′- O -crontonyl β -glucopyranoside. • Compounds 1–6 represented the first examples of natural sesquiterpenoid. • Compounds 1 and 2 showed activity against HepG2 and SK-Hep-1 cells at 200.0 μM. • Compound 1 showed inhibitory activity against Huh7 cells. [ABSTRACT FROM AUTHOR]

Paeoveitols A–E ( 1 – 5 ), involving three monoterpenes and two benzofuran constituents, were isolated from Paeonia veitchii . Their structures were determined based on extensive spectral analyses (IR, UV, MS, 1D and 2D NMR), and the absolute configuration of compound 1 was confirmed by single-crystal X-ray diffraction. By the agitating human melatonin receptor 1 (MT1) assay on HEK293 cell line in vitro, compound 4 showed weak activity with the agitation rate of 22.52% at the concentration of 1.79 mM. [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]

Four new compounds swertiachiralatone A (1), swertiachoside A (2), swertiachirdiol A (3) and swertiachoside B (4), together with twenty-six known ones were isolated from the ethanol extract of Swertia chirayita . Their structures were elucidated by extensive spectroscopic analyses (1D- and 2D-NMR, HRESIMS, UV, IR and [ α ] D ). All compounds were evaluated for anti-hepatitis B virus (anti-HBV) activities on HepG 2.2.15 cells line in vitro , of which compounds 14 and 19 showed inhibitory activity on hepatitis B surface antigen (HBsAg) secretion with IC 50 values of 0.31 ± 0.045 and 1.49 ± 0.033 mM; compounds 14 and 28 exhibited activity against hepatitis B e antigen (HBeAg) secretion with IC 50 values of 0.77 ± 0.076 and 5.92 ± 1.02 mM; and eight compounds (8,9,13,14,24–26,29) possessed activity against HBV DNA replication with IC 50 values of 0.07–0.33 mM. In particular (+)-cycloolivil-4′- O - β - d -glucopyranoside (14) exhibited inhibition not only on the secretions of HBsAg and HBeAg with IC 50 values of 0.31 ± 0.045 mM (SI = 4.29) and 0.77 ± 0.076 mM (SI = 1.75), respectively, but also on HBV DNA replication with an IC 50 value of 0.29 ± 0.034 mM (SI = 4.66). [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: Six new 14-noreudesmane sesquiterpenoids, nicotabacosides A–F (1–6), along with five known sesquiterpenoids (7–11), were isolated from the leaves of Nicotiana tabacum. The structures of compounds 1–6 were elucidated as isorishitin 3-O-β-d-glucopyranoside (1), rishitin 3-O-β-d-glucopyranoside (2), rishitin 2-O-β- d-glucopyranoside (3), 1, 6-dehydro-rishitin 3-O-β-d-glucopyranoside (4), 2-hydroxyl-ligudentatol 3-O-β-d-glucopyranoside (5) and oxyglutinosone 3-O-β-d-glucopyranoside (6) based on extensive spectroscopic analyses (HRESIMS, UV, IR, 1D and 2D NMR). Their absolute configurations were determined by X-ray single-crystal diffraction and comparison of their electronic circular dichroism (ECD) spectra. [Copyright &y& Elsevier]

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: Four new C18-diterpenoid alkaloids, weisaconitines A–D (1–4), were isolated from Aconitum weixiense. Based on extensive UV, IR, MS, 1D and 2D NMR analyses, their structures were elucidated as 8-O-ethyldolaconine (1), 4-demethylgenicunine B (2), 14-oxoaconosine (3), and 8-O-ethylaconosine (4). The analgesic activity of compound 4 was studied with CH3COOH-induced writhing model in mice. Compound 4 showed writhing inhibitions of 24% (50mg/kg), 26% (100mg/kg) and 34% (200mg/kg), respectively, as compared to the reference drug aspirin (63%) at a dose of 200mg/kg. [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]