Thymol attenuates allergic airway inflammation in ovalbumin (OVA)-induced mouse asthma

Thymol, a naturally occurring monocyclic phenolic compound derived from Thymus vulgaris (Lamiaceae), has been reported to exhibit anti-inflammatory property in vivo and vitro. However, the mechanism of thymol is not clear. The aim of the present study was to investigate the effects of thymol on allergic inflammation in OVA-induced mice asthma and explore its mechanism. The model of mouse asthma was established by the induction of OVA. Thymol was orally administered at a dose of 4, 8, and 16 mg/kg body weight 1 h before OVA challenge. At 24 h after the last challenge, mice were sacrificed, and the data were collected by various experimental methods. The results revealed that pretreatment with thymol reduced the level of OVA-specific IgE, inhibited recruitment of inflammatory cells into airway, and decreased the levels of IL-4, IL-5, and IL-13 in BALF. Moreover, the pathologic changes of lung tissues were obviously ameliorated and goblet cell hyperplasia was effectively inhibited by the pretreatment of thymol. In addition, thymol reduced the development of airway hyperresponsiveness and blocked the activation of NF-κB pathway. All data suggested that thymol ameliorated airway inflammation in OVA-induced mouse asthma, possibly through inhibiting NF-κB activation. These findings indicated that thymol may be used as an alternative agent for treating allergic asthma.     

A new glucomannan from Bletilla striata: Structural and anti-fibrosis effects

A novel water-soluble polysaccharide, designated Bletilla striata polysaccharide b (BSPb), was isolated from a traditional Chinese medicinal herb, Bletilla striata. The crude polysaccharide was obtained by hot water extraction and purified by ion-exchange chromatography. The molecular weight was 260 kDa as determined by HPGPC (high performance gel permeation chromatography). Monosaccharide analysis showed that BSPb contained glucose and mannose with a molar ratio of 3:1. Methylation and spectroscopic analyses with 1D and 2D NMR spectroscopy showed that the backbone of BSPb is mainly composed of (1 → 2)-linked α-d-mannopyranose and (1 → 4)-linked β-d-glucopyranose residues. In this study, BSPb plays an important role in protection against the renal fibrosis effect, which is probably mediated by down-regulated TGF-β RI, TGF-β RII, and α-SMA in vitro.     

Purification,structural elucidation and antitumor activity of a novel mannogalactoglucan from the fruiting bodies of Lentinus edodes

A mannogalactoglucan, named LE-MGG, was isolated from the basidiocarps of Lentinus edodes by hot water-extraction, ethanol precipitation anion exchange chromatography, and further purified by gel-permeation chromatography (GPC). Its structural features were investigated by high performance liquid chromatography (HPLC), high performance gel-permeation chromatography (HPGPC), methylation analysis, periodate oxidation-Smith degradation, and by IR and NMR spectroscopy, including two-dimensional (2D) NMR. HPLC analysis revealed that LE-MGG contained mannose–galactose–glucose in the molar ratio of 10:18:72. GPC and HPGPC showed that LE-MGG was a homogeneous fraction (d = 1.34) and its molecular weight was estimated to be 18 kDa. Chemical and spectroscopic studies indicated that LE-MGG consists of (1 → 6)-, (1 → 4)- and (1 → 3)-linked β-d-glucopyranosyl residues, (1 → 6)-linked α-d-galactopyranosyl residues, (1 → 3,6)- and (1 → 2,4)-linked α-d-mannopyranosyl residues and terminal residues of β-d-glucopyranosyl. Cytotoxicity assay showed that LE-MGG presented higher antitumor activities against S-180 cell with a dose-dependent manner, and exhibited lower cytotoxicity to carcinoma HCT-116 and HT-29 cells. Our studies showed also that LE-MGG presented antitumor bioactivities on Sarcoma 180 solid tumor cell implanted in Kunming mice. This finding suggests that mannogalactoglucan should be explored as potential antitumor agents and could be potentially applied as a natural antitumor drug.     

New cytotoxic triterpenoid saponins from the whole plant of Clematis lasiandra Maxim

Four new oleanane type triterpenoid saponins (1–4) and three known saponins (5–7) were isolated from the whole plant of Clematis lasiandra Maxim. The structures of the four new compounds were elucidated as 3-O-β-d-ribopyranosyl-(1 → 3)-α-l-rhamnopyranosyl-(1 → 2)-[β-d-glucopyranosyl-(1 → 4)]-β-d-xylopyranosyl hederagenin (1), 3-O-β-d-ribopyranosyl-(1 → 3)-α-l-rhamnopyranosyl-(1 → 2)-β-d-xylopyranosyl oleanolic acid 28-O-β-d-glucopyranosyl ester (2), 3-O-β-d-ribopyranosyl-(1 → 3)-α-l-rhamnopyranosyl-(1 → 2)-β-d-xylopyranosyl hederagenin (3) and 3-O-β-d-ribopyranosyl-(1 → 3)-α-l-rhamnopyranosyl-(1 → 2)-[β-d-glucopyranosyl-(1 → 4)]-α-l-arabinopyranosyl hederagenin (4) on the basis of extensive spectroscopic analysis and chemical evidence. Compounds 1–7 were evaluated for their cytotoxicity against human tumor cell lines HL-60, Hep-G2 and SGC-7901, and all of the evaluated saponins showed significant cytotoxicity to those three tumor cell lines with IC₅₀ in the range from 1.40 to 19.50 μmol/L except for compounds 2 and 6.     

Phenylethanoid glycosides from the stems of Callicarpa peii (hemostatic drug)

Two new trisaccharide intermediates of phenylethanoid glycosides, peiioside A₁/A₂ (1a/1b) and peiioside B (2), were isolated from the n-BuOH fraction of MeOH extract of the stems of Callicarpa peii H.T. Chang, together with five biogenetic relevant known compounds 3–7. The structures of compounds 1 and 2 were elucidated by extensive spectroscopic methods (especially 2D-NMR techniques) and acid-catalyzed hydrolysis as O-α-l-rhamnopyranosyl-(1″ → 3′)-O-[β-d-apiofuranosyl-(1‴ → 6′)] -4′-O-[(E)-caffeoyl]-d-glucopyranoside] (1a/1b), 3,4-dihydroxy-β-phenylethoxy-O-[β-d-apiofuranosyl-(1‴ → 6′)-α-l-rhamnopyranosyl-(1″ → 3′)-O-β-d-glucopyranoside] (2), respectively. On the basis of the isolated compounds, a presumable biogenetic pathway of the biologically interesting phenylethanoid glycosides about forsythoside B (3) and acteoside (4) isolated from this species was proposed. Isolation of five related intermediates (1–2, 5–7) provided further support for the biogenetic path. This is the first report about phytochemical research on C. peii and the biogenetic hypothesis of forsythoside B and acteoside.     

Protection of chronic renal failure by a polysaccharide from Cordyceps sinensis

A water-soluble polysaccharide (CPS-2), isolated from the cultured Cordyceps sinensis, was obtained by hot-water extraction, anion-exchange and gel permeation chromatography. Its structural characteristics were investigated by PMP pre-column derivation, periodate oxidation, methylation analysis, FTIR and NMR spectroscopy. CPS-2 was found to be mostly of α-(1 → 4)-d-glucose and α-(1 → 3)-D-mannose, branched with α-(1 → 4,6)-d-glucose every twelve residues on average. CPS-2 had a molecular weight of 4.39 × 10⁴ Da. The protective effect of CPS-2 on the model of chronic renal failure was established by fulgerizing kidney. The changes in blood urea nitrogen and serum creatinine revealed that CPS-2 could significantly relieve renal failure caused by fulgerizing kidney.     

Two novel saponins of 20, 26-epoxy derivatives of pseudojujubogenin from the seeds of Hovenia trichocarpa

Two new saponins of 20, 26-epoxy derivatives of pseudojujubogenin, hoduloside XI (1) and hoduloside XII (2) were isolated from the seeds of Hovenia trichocarpa. The structures of the new compounds were established by extensive NMR experiments and chemical methods. Hoduloside XI was confirmed to be 3-O-{β-d-glucopyranosyl(1 → 3)-[β-d-xylopyranosyl(1 → 2)]-α-l-arabinopyranosyl}-20, 26-epoxypseudojujubogenin. Hoduloside XII was identified as 3-O-{β-d-xylopyranose(1 → 2)glucopyranosyl(1 → 3)[rhamnopyranose(1 → 2)]β-d-glucopyranosyl}-20, 26-epoxypseudojujubogenin. The in vitro cytotoxic activity of compounds 1 and 2 was assayed. They displayed inhibitive activities against human cancer cell lines HL60 and K562.     

Curcumin attenuates allergic airway inflammation by regulation of CD4+CD25+ regulatory T cells (Tregs)/Th17 balance in ovalbumin-sensitized mice

The present study aimed to determine the protective effects and the underlying mechanisms of curcumin on ovalbumin (OVA)-induced allergic inflammation in a mouse model of allergic asthma. Asthma mice model was established by ovalbumin. A total of 60 mice were randomly assigned to six experimental groups: control, model, dexamethasone (2 mg/kg), and curcumin (50 mg/kg, 100 mg/kg, 200 mg/kg). Airway resistance (Raw) was measured by the forced oscillation technique, differential cell count in BAL fluid (BALF) was measured by Wright–Giemsa staining, histological assessment was measured by hematoxylin and eosin (HE) staining, BALF levels of Treg/Th17 cytokines were measured by enzyme-linked immunosorbent assay, Treg cells and Th17 cells were evaluated by flow cytometry (FCM). Our study demonstrated that curcumin inhibited OVA-induced increases in eosinophil count; interleukin (IL)-17A level were recovered in bronchoalveolar lavage fluid increased IL-10 level in bronchoalveolar lavage fluid. Histological studies demonstrated that curcumin substantially inhibited OVA-induced eosinophilia in lung tissue. Flow cytometry (FCM) studies demonstrated that curcumin remarkably inhibited Th17 cells and significantly increased Treg cells. The results in vivo show ovalbumin-induced significantly broke Treg/Th17 balance; curcumin treatments markedly attenuated the inflammatory in asthma model by regulating Treg/Th17 balance. Our findings support the possible use of curcumin as a therapeutic drug for patients with allergic asthma.     

Two new steroidal saponins from Selaginella uncinata (Desv.) Spring and their protective effect against anoxia

Four steroidal saponins were isolated from the anti-anoxic fraction of the 60% EtOH extract of Selaginella uncinata, including two new compounds, (3β, 7β, 12β, 25R)-spirost-5-ene-3, 7, 12-triol-3-O-α-L-rhamnopyranosyl-(1 → 2)-O-[α-L-rhamnopyranosyl-(1 → 4)]-O-β-d-glucopyranoside (1), (2α, 3β, 12β, 25R)-spirost-5-ene-2, 3, 12-triol-3-O-α-L-rhamnopyranosyl-(1 → 2)-O-[α-L-rhamnopyranosyl-(1 → 4)]-O-β-d-glucopyranoside (2) and two known compounds, (3β, 12β, 25R)-spirost-5-ene-3,12-diol-3-O-α-L-rhamnopyranosyl-(1 → 2)-O-[α-L-rhamnopyranosyl-(1 → 4)]-O-β-d-glucopyranoside, (3), (1α, 3β, 25R)-spirost-5-ene-2-diol-3-O-α-L-rhamnopyranosyl-(1 → 2)-O-[α-L-rhamnopyranosyl(1 → 4)]-O-β-d-glucopyranoside (4). The four compounds showed potent protective effect against anoxia in the anoxic PC12 cells assay, among which compounds 1 and 2 were the most active. To our knowledge, this is the first study to report the steroidal saponins in the plant S. uncinata and demonstrate their protective effect against anoxia in PC12 cell assay.     

Cytotoxic steroidal glycosides from Allium flavum

Three new spirostane-type glycosides (1–3) were isolated from the whole plant of Allium flavum. Their structures were elucidated mainly by 2D NMR spectroscopic analysis and mass spectrometry as (20S,25R)-2α-hydroxyspirost-5-en-3β-yl O-β-d-xylopyranosyl-(1 → 3)-[β-d-galactopyranosyl-(1→2)]-β-d-galactopyranosyl-(1→4)-β-d-galactopyranoside (1), (20S,25R)-2α-hydroxyspirost-5-en-3β-yl O-β-d-xylopyranosyl-(1 → 3)-[β-d-glucopyranosyl-(1→2)]-β-d-galactopyranosyl-(1→4)-β-d-galactopyranoside (2), and (20S,25R)-spirost-5-en-3β-yl O-α-l-rhamnopyranosyl-(1 → 4)-[β-d-glucopyranosyl-(1→2)]-β-d-glucopyranoside (3). The three saponins were evaluated for cytotoxicity against a human cancer cell line (colorectal SW480).     

Cyclodepsipeptides from the ascocarps and insect-body portions of fungus Cordyceps cicadae

A new cyclodepsipeptide cordycecin A (1), together with four known ones beauvericin E (2), beauvericin J (3), beauvericin (4), and beauvericin A (5) was isolated from the ascocarps and insect-body portions of fungus Cordyceps cicadae. Their structures were identified by NMR and MS analyses. The absolute configuration of 1 was confirmed by crystal X-ray diffraction. Compounds 2–5 exhibited a significant inhibitory effect on HepG2 and HepG2/ADM cells with IC₅₀ values ranging from 2.40 ± 0.37 to 14.48 ± 1.68 μM. Interestingly, compounds 3–5 showed cytotoxic activity against multiple drug resistant HepG2 cell line (HepG2/ADM) with IC₅₀ value 25-fold more sensitive to doxorubicin.     

Chemical constituents of Swertia yunnanensis and their anti-hepatitis B virus activity

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 1.76 mM) and HBeAg (IC₅₀ values from 0.04 to 1.41 mM), and compounds 11 and 13–16 exhibited significant inhibition on HBV DNA replication (IC₅₀ values from 0.01 to 0.09 mM).     

Individual and combined effects of rhynchophylline and ketamine on proliferation,NMDAR1 and GluA2/3 protein expression in PC12 cells

Rhynchophylline is an active component of the Uncaria species, which is a member of the Rubiaceae family. Our studies show that the downregulation of N-methyl-d-aspartate (NMDA) receptor subunit GluN2B expression in the nucleus accumbens, amygdala, medial prefrontal cortex, and hippocampal CA1 area by rhynchophylline is beneficial for the treatment of psychological dependence on amphetamines. The individual and combined effects of rhynchophylline and ketamine on proliferation and GluN1 and GluA2/3 protein expression in PC12 cells were investigated. PC12 cells were differentiated into neuron-like cells by treatment with nerve growth factor (50 ng/mL). After treatment for 48 h, differentiated PC12 cell proliferation and GluN1 and GluA2/3 protein expression were analyzed. The viability of PC12 cells was reduced by ketamine at doses of 0.50, 1.00, 1.50, and 2.00 mmol/L, with the viability of cells treated with 1.50 and 2.00 mmol/L of ketamine significantly lower than that of the control cells. However, PC12 cells treated with rhynchophylline showed no toxicity at doses of 0.25, 0.50, 0.75, or 1.00 mmol/L. While GluA2/3 protein expression was upregulated by ketamine, it was not influenced by rhynchophylline. GluN1 protein expression was downregulated by rhynchophylline (1 mmol/L), while treatment with ketamine, either alone or with rhynchophylline, had no effect. These findings demonstrate that rhynchophylline suppresses GluA2/3 expression in ketamine-induced PC12 cells and downregulates GluN1 expression. Ketamine's lack of effect on GluN1 expression offers a partial explanation for ketamine addiction and the anti-addictive properties of rhynchophylline.     

Five new triterpenoidal saponins from the roots of Ilex cornuta and their protective effects against H2O2-induced cardiomyocytes injury

Five new ursane-type triterpenoidal saponins (1–5), together with five known ones (6–10), were isolated from the EtOH extract of the roots of Ilex cornuta. The structures of saponins 1–5 were elucidated as 19α-hydroxyurs-12-en-28-oic acid 3β-O-β-D-glucuronopyranoside (1), 19α-hydroxyurs-12-en-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-ethyl ester (2), 19α-hydroxyurs-12-en-28-oic acid 3β-O-α-L-arabinopyranosyl-(1 → 2)-β-D-glucuronopyranoside (3), 3β-O-[α-L-arabinopyranosyl-(1 → 2)-β-D-glucuronopyranosyl]-19α-hydroxyurs-12-en-28-oic acid 28-O-β-D-glucopyranosyl ester (4) and 3β-O-[α-L-arabinopyranosyl-(1 → 2)-β-D-glucuronopyranoside-6-O-methyl ester]-19α-hydroxyurs-12-en-28-oic acid 28-O-β-D-glucopyranosyl ester (5), on the basis of spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, 1D and 2D NMR) and chemical reactions. Protective effects of compounds 1–10 against H₂O₂-induced H9c2 cardiomyocyte injury were tested. Compounds 1–5, 7, and 10 showed cell-protective effects. Among them compound 5 exhibited the highest activity. No significant DPPH radical scavenging activity was observed for compounds 1–10.     

Desmodeleganine,a new alkaloid from the leaves of Desmodium elegans as a potential monoamine oxidase inhibitor

Desmodeleganine (1), a new potential monoamine oxidase inhibitor, along with three known alkaloids, bufotenin (2), hydroxy-N, N-dimethyltryptamine N¹²-oxide (3), 2-(5-methoxy-1H-indol-3-yl)-N, and N-dimethylethylamine (4) were isolated from the leaves of Desmodium elegans. Their structures were elucidated by IR, MS, 1D and 2D NMR spectra. 1 showed strong monoamine oxidase inhibitory activity with IC₅₀ value of 13.92 ± 1.5 μM, when the IC₅₀ value of iproniazid as a standard was 6.5 ± 0.5 μM. The molecular modeling was also performed to explore the binding mode of compounds 1, 2 at the active site of MAO-A and MAO-B.     

Estrogenic and anti-estrogenic activities of hispolon from Phellinus lonicerinus (Bond.) Bond. et sing

Hispolon was the main antitumor active ingredient in Phellinus sensu lato species. In order to confirm the dual regulating estrogenic ingredient and obtain more effective natural estrogen replacement drugs, hispolon was separated from Phellinus lonicerinus (Bond.) Bond. et sing. Hispolon exhibited significant anti-proliferative effect against estrogen-sensitive ER (+) MCF-7 cells in the absence of estrogen, and exhibits antagonistic effects on 17β-estradiol (E₂)-induced MCF-7 cell proliferation when E₂ and the different concentrations of hispolon were treated simultaneously. Hispolon also inhibited the proliferation of estrogen-negative ER (−) MDA-MB-231 cells at the concentration of 5.00 × 10^− 5 M. The yeast two-hybrid experiments showed that hispolon had strong and non-selective effects on the estrogen receptor (ER) α and ERβ at a concentration of 1.00 × 10^− 6 M. The ERβ-binding ability of hispolon was larger than ERα in the concentration range of 1.00 × 10^− 9 M and 1.00 × 10^− 7 M. Hispolon could increase the body weight coefficient, serum E₂ and progesterone contents in immature female mice at dose of 9.10 × 10^− 6 mol/kg, and increase coefficient of thymus and spleen in mice. The Gscores of hispolon-ERα and hispolon-ERβ docked complexes were − 7.93 kcal/mol and − 7.79 kcal/mol in docking simulations. Hispolon presented dual regulating estrogenic activities, which showed estrogenic agonist activity at low concentration or lack of endogenous estrogen, and the estrogenic antagonistic effect was stimulated at high concentrations or too much endogenous estrogen. Hispolon could be used for treating the estrogen deficiency-related disease with the benefit of non-toxic to normal cells, good antitumor effects and estrogenic activity.     

Sibiricasaponins A–E,five new triterpenoid saponins from the aerial parts of Polygala sibirica L.

Five new triterpenoid saponins, named as sibiricasaponins A–E (1–5), were isolated and identified from the aerial parts of Polygala sibirica L., together with nine known triterpenoid saponins (6–14). The chemical structures of the five new triterpenoid saponins (1–5) were elucidated as 3β,19α-dihydroxyurso-12-ene-23,28-dioic acid 3-O-β-d-glucuronopyranoside (1), pomolic acid 3-O-(3-O-sulfo)-α-l-arabinopyranoside (2), pomolic acid 3-O-(4-O-sulfo)-β-d-xylopyranoside (3), pomolic acid 3-O-(2-O-acetyl-3-O-sulfo)-α-l-arabinopyranoside (4), and 3-O-β-d-glucopyranosyl medicagenic acid 28-O-β-d-galactopyranosyl (1 → 4)-β-d-xylopyranosyl (1 → 4)-α-l-rhamnopyranosyl (1 → 2)-(4-O-acetyl)-[β-d-apiofuranosyl (1 → 3)]-β-d-fucopyranosyl ester (5), respectively, on the basis of spectroscopic data and physicochemical evidences. These isolated compounds (1–14) were evaluated for their anti-ischemic effects on oxygen/glucose deprivation (OGD) model in vitro, and only compound 7 showed a weak anti-ischemia effect, with EC₅₀ value of 46.7 μM.     

Developing general allometric relationships for regional estimates of carbon sequestration—an example using Eucalyptus pilularis from seven contrasting sites

General non-site-specific allometric relationships are required for the conversion of forest inventory measurements to regional scale estimates of forest carbon sequestration. To determine the most appropriate predictor variables to produce a general allometric relationship, we examined Eucalyptus pilularis aboveground biomass data from seven contrasting sites. Predictor variables included diameter at breast height (dbh), stem volume, dbh² × H, dbh × H and height (H). The data set contained 105 trees, ranging from 6 to over 20,000 kg tree⁻¹, with dbh ranging from 5 to 129 cm. We observed significant site differences in (1) partitioning of biomass between the stem, branch wood and foliage; (2) stem wood density and (3) relationship between dbh and height. For all predictor variables, site had a significant effect on the allometric relationships. Examination of the model residuals of the site-specific and general relationship indicated that using dbh alone as the predictor variable produced the most stable general relationship. Furthermore, the apparent site effect could be removed by the addition of a constant value to the measured diameter (dbh + 1), to account for the differing diameter distribution across the seven sites. Surprisingly, the inclusion of height as a second predictor variable decreased the performance of the general model. We have therefore demonstrated that for E. pilularis a general allometric relationship using dbh alone as the predictor variable can be as accurate as site-specific allometry, whilst being applicable to a wide range of environments, management regimes and ages. This simplifies regional estimates of aboveground biomass from inventory measurements, eliminating the need for site-specific allometric relationships or modifiers such as height, wood density or expansion factors.     

Three new phenolic compounds from the leaves of Rosa sericea

Two new flavonoids, quercetin-3-O-β-d-xylopyranosyl-(1 → 2)-α-d-ribopyranoside (1) and kaempferol-3-O-β-d-xylopyranosyl-(1 → 2)-α-d-ribopyranoside (2), and one new phenolic derivative, gallicin-p-O-(6′-O-caffeoyl)-β-d-glucoside (3), together with twelve known compounds were isolated from the leaves of Rosa sericea (Rosaceae family). The structures of the new compounds were established by means of spectroscopic analysis including one- and two-dimensional NMR spectroscopy. Some of the isolated compounds were tested for the cytotoxicity of a breast cancer cell (MCF-7) line. The results showed that rubanthrone A (4) has moderate cytotoxicity against the MCF-7 cell line.     

Polyacetylenes and anti-hepatitis B virus active constituents from Artemisia capillaris

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 15.02 μM (SI = 111.3), 9.00 μM (SI = 185.9) and 12.01 μM (SI = 139.2).