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Hederacoside C (HSC) has attracted much attention as a novel modulator of inflammation, but its anti-inflammatory mechanism remains elusive. In the present study, we investigated how HSC attenuated intestinal inflammation in vivo and in vitro. HSC injection significantly alleviated TNBS-induced colitis by inhibiting pro-inflammatory cytokine production and colonic epithelial cell apoptosis, and partially restored colonic epithelial cell proliferation. The therapeutic effect of HSC injection was comparable to that of oral administration of mesalazine (200 mg·kg

As a biosynthetic precursor of the antimalarial drug artemisinin, artemisinic acid (AA) is abundant in Artemisia annua L. with a content of 8-10-fold higher than artemisinin, but less effective. In this study, the biotransformation of AA was carried out with an endophytic fungus Penicillium oxalicum B4 to extend its utility. After 10-day-culture of the endophyte with AA at 2 mg/mL, eight biotransformation metabolites were isolated from the culture broth, including five undescribed metabolites, namely 3α,14-dihydroxyartemisinic acid, 14-hydroxy-3-oxo-artemisinic acid, 15-hydroxy-3-oxo-artemisinic acid, 12, 15-artemisindioic acid and 1,2,3,6-tetradehydro-12, 15-artemisindioic acid. The fungal enzymes possess the selective capacity to hydroxylate, carbonylate and ketonize the allyl group of AA. The major biotransformation metabolite was the hydroxylated product 3-α-hydroxyartemisinic acid (33.3%) in the cultures of early stage (day 1–6), whereas most of the other biotransformation products were synthesized in the later stage (day 8–10). Compared with AA, some metabolites (3α,14-dihydroxyartemisinic acid, 15-hydroxy-3-oxo-artemisinic acid and 1,2,3,6-tetradehydro-12, 15-artemisindioic acid) possessed stronger cytotoxic activity to the human colon carcinoma cell line (LS174T) and promyelocytic leukemia cell line (HL-60). The metabolites 12, 15-artemisindioic acid and 3-α-hydroxyartemisinic acid exhibited significant inhibitory activity to the lipopolysaccharide-induced nitrite production of RAW 264.7 cells at 10.00 μM and 2.50 μM, respectively. The results demonstrated the potential of fungal endophytes on biotransforming AA to its bioactive derivatives.

Previous studies have indicated that the Ilex genus exhibits antioxidant, neuroprotective, hepatoprotective, and anti-inflammatory activities. However, the pharmacologic action and mechanisms of Ilex cornuta against cardiac diseases have not yet been explored. The present study was designed to investigate the antioxidant and cardioprotective effects of Ilex cornuta root with in vitro and in vivo models. The anti-oxidative effects of the extract of Ilex cornuta root (ICR) were measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free-radical scavenging and MTT assays as well as immunoassay. Furthermore, a rat model of myocardial ischemia was established to investigate the cardioprotective effect of ICR in vivo. Eight compounds were isolated and identified from ICR and exhibited DPPH free-radical scavenging activities. They also could increase cell viability and inhibit morphological changes induced by H2O2 or Na2S2O4 in H9c2 cardiomyocytes, followed by increasing the SOD activities and decreasing the MDA and ROS levels. In addition, it could suppress the apoptosis of cardiomyocytes. In the rat model of myocardial ischemia, ICR decreased myocardial infarct size and suppressed the activities of LDH and CK. Furthermore, ICR attenuated histopathological alterations of heart tissues and the MDA levels, while increasing SOD activities in serum. In conclusion, these results suggest that ICR has cardioprotective activity and could be developed as a new food supplement for the prevention of ischemic heart disease.

In the present study, three new triterpenoids, 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-α-L-arabinopyranoside (1), 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (2), and urs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (3), and a known triterpenoid, 3β-hydroxy-urs-2, 18-dien-28-oic acid (4, randialic acid B), were isolated from the aerial parts of Ilex cornuta. Their structures were identified by the spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, and 1D and 2D NMR) and chemical reactions. Compound 4 showed significant cell-protective effects against H2O2-induced H9c2 cardiomyocyte injury. Compounds 1-4 did not show any significant DPPH radical scavenging activity.

The dried seeds of

A Cu-mediated stereoselective [4+2] annulation between N-hydroxybenzimidoyl cyanides and norbornene (NBE) has been developed for the synthesis of 4 H-1,2-oxazin-4-ones. The reaction proceeds through sequentially forming C-O/C-C bonds. The advantage of this reaction includes high stereoselectivity, excellent yields, as well as simple and mild reaction conditions. A total of 26 examples are presented along with some control experiments.

Doxorubicin (DOX) is a widely used antineoplastic agent in clinics. However, its clinical application is largely limited by its cardiotoxicity. Diethyl blechnic (DB) is a novel compound isolated from Salvia miltiorrhiza Bunge. Here, we study the effect of DB on DOX-induced cardiotoxicity and its underlying mechanisms. Cellular viability was tested by 3-[-4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) and protein level was evaluated by Western blotting. 5,5’,6,6’-tetrachloro-1,1’,3,3’-tetraethylbenzimidazolylcarbocyanine iodide (JC-1) staining was performed to determine the mitochondrial membrane potential (MMP). Hoechst 33342 staining and TUNEL staining was performed to test the apoptosis. Reactive oxygen species (ROS) generation was investigated by using flow cytometry. DB significantly inhibited DOX-induced apoptosis in H9c2 cells and primary cultured cardiomyocytes. Moreover, DB decreased cell apoptotic morphological changes and reversed the mitochondrial membrane potential induced by DOX. Meanwhile, pre-treatment with DB increased the expression levels of B-cell lymphoma 2 (Bcl-2), B-cell lymphoma-extra-large (Bcl-xl), and survivin and reduced the expression levels of Bcl-2-associated X protein (Bax), p-p53, cytochrome c (cyt c), and cleaved-caspase 3, 7, 8, 9 in the protein levels in DOX-treated H9c2 cells. Furthermore, DB suppressed ROS generation. The DB-mediated protective effects were accompanied by increased c-Jun N-terminal kinase1/2 (JNK1/2) expression. In addition, SP600125, the inhibitor of JNK1/2, abolished the protective effect of DB. We concluded that DB protected cardiomyocytes against DOX-induced cytotoxicity by inhibiting ROS and activating the JNK1/2 pathway. Therefore, DB is a promising candidate as a cardioprotective agent against DOX-induced cardiotoxicity.

Ten compounds were isolated and identified from green vegetable soya beans, of which five are new triterpenoid saponins (1-5) and five are known compounds (6-10). The chemical structures of the five triterpenoid saponins (1-5) were elucidated to be 3β,24-dihydroxy-22β,30-epoxy-30-oxoolean-12-en 3-O-α-l-rhamnopyranosyl-(1 → 2)-β-d-xylopyranosyl-(1 → 2)-β-d-glucuronopyranoside, 1; 3β,24-dihydroxy-22β,30-epoxy-30-oxoolean-12-en 3-O-α-l-rhamnopyranosyl-(1 → 2)-β-d-(3″-O-formyl)-galactopyranosyl-(1 → 2)-β-d-glucuronopyranoside, 2; 22-keto-3β,24-dihydroxy oleanane-12-ene 3-O-α-l-rhamnopyranosyl-(1 → 2)-β-d-(3″-O-formyl)-galactopyranosyl-(1 → 2)-β-d-glucuronopyranoside, 3; 3β,22β,24-trihydroxy oxyolean-18(19)-ene-29-acid 3-O-α-l-rhamnopyranosyl-(1 → 2)-β-d-galactopyranosyl-(1 → 2)-β-d-glucuronopyranoside, 4; and punicanolic acid 3-O-α-l-rhamnopyranosyl-(1 → 2)-β-d-galactopyranosyl-(1 → 2)-β-d-glucuronopyranoside, 5 from the spectroscopic data (IR, GTC/FID, HR-ESI-MS, and 1D and 2D NMR). The nitric oxide release inhibitions of compounds 1-10 in LPS-stimulated RAW264.7 cells were evaluated, and the data suggested that compounds 1, 2, and 5 might possess moderate anti-inflammatory activities, with IC

Camellia oleifera C. Abel has been widely cultivated in China, and a group of bioactive constituents such as triterpeniod saponin have been isolated from C. oleifera C. Abel. In the current study, a new triterpeniod saponin was isolated from the EtOH extract of the roots of C. oleifera C. Abel, named as oleiferoside W, and the cytotoxic properties of oleiferoside W were evaluated in non-small cell lung cancer A549 cells. At the same time the inducing apoptosis, the depolarization of mitochondrial membrane potential (Δψ), the up-regulation of related pro-apoptotic proteins, such as cleaved-PARP, cleaved-caspase-3, and the down-regulation of anti-apoptotic marker Bcl-2/Bax were measured on oleiferoside W. Furthermore, the function, inducing the generation of reactive oxygen species (ROS) and apoptosis, of oleiferoside W could be reversed by N-acetylcysteine (NAC). In conclusion, our findings showed that oleiferoside W induced apoptosis involving mitochondrial pathway and increasing intracellular ROS production in the A549 cells, suggesting that oleiferoside W may have the possibility to be a useful anticancer agent for therapy in lung cancer.

The fruits of Physalis alkekengi L. var. franchetii (Mast.) Makino have been used in Chinese medicine for thousands of years because of its significant biological activities. A comprehensive phytochemical study of the chemical constituents of the fruits resulted in the isolation of three new steroids (1–3) as well as seven known steroids (4–10). Their structures were identified by the extensive analyses of 1D and 2D NMR, IR, HR-ESI-MS and other techniques. Compound 4 (physalin B) showed the most significant cytotoxic activities against HeLa human cervical, SMMC-7721 human hepatoma, and HL-60 human hepatoma tumor cell lines, with the IC50 values of 0.51, 0.86 and 1.12 μM, respectively. Compounds 1, and 5–9 showed potent cytotoxic activities.

In the present study, three new triterpenoids, 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-α-L-arabinopyranoside (1), 23-hydroxyurs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (2), and urs-12, 18-dien-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester (3), and a known triterpenoid, 3β-hydroxy-urs-2, 18-dien-28-oic acid (4, randialic acid B), were isolated from the aerial parts of Ilex cornuta. Their structures were identified by the spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, and 1D and 2D NMR) and chemical reactions. Compound 4 showed significant cell-protective effects against H

Two new 28-nor-oleanane-type triterpene saponins, oleiferoside U (1), and oleiferoside V (2) were isolated from the 50% EtOH extract of the roots of Camellia oleifera C. Abel. Their structures were elucidated as camellenodiol 3β-O-β-d-galactopyranosyl-(1→2)-β-d-xylopyranosyl-(1→2)-[β-d-galactopyranosyl-(1→3)]-β-d-glucuronopyranoside and camellenodiol 3β-O-β-d-galactopyranosyl-(1→3)-β-d-xylopyranosyl-(1→2)-[β-d-galactopyranosyl-(1→3)]-β-d-glucuronopyranoside. Their chemical structures were established mainly on the basis of integrated spectroscopic techniques. In vitro, cytotoxic activities of the two new triterpene saponins were evaluated against three human tumor cell lines (A549, SMMC-7721, and MCF-7) using the MTT assay. Both of them showed a certain cytotoxic activities toward the tested cell lines and gave IC50 values in the range of 45.04–63.22 μM.

The present study was undertaken to investigate whether hederacochiside C (HSC) possesses antischistosomal effects and anti-inflammatory response activities in Schistosoma japonicum-infected mice. Different concentrations of HSC were administrated to the mice infected by schistosomula or adult worm by intravenous injection twice a day for five consecutive days. The total worm burden, female worm burden, and the egg burden in liver of mice treated with 400 mg/kg HSC were fewer than those in non-treated ones. Murine immune responses following HSC treatment were investigated using enzyme-linked immunosorbent assays (ELISA). Our results indicated that 200 mg/kg HSC could reduce the expression of IgG, tumor necrosis factor (TNF)-α, interleukin (IL)-4 and IL-17 in comparison to infected group, exhibiting best immunomodulatory effects. In addition, scanning electron microscopical examination revealed that male worms treated with HSC lost their normal surface architecture since its surface showed extensive swelling, erosion, and peeling in tegumental regions. Remarkable amelioration was noticed in histopathological investigations, and 200 mg/kg HSC treatment could reduce the size of granulomatous inflammatory infiltrations in the liver which was reflected in nearly normalization of liver architecture. These results suggested that HSC had potential antischistosomal activity and provided a basis for subsequent experimental.

Two new phenylglycol derivatives, (S)-(+)-2-(3,4-dihydroxy phenyl)-2-ethoxyl- ethanol and (S)-(+)-2-(3,4-dihydroxy phenyl)-2-acetoxy-ethanol, were isolated from the leaves of Syringa reticulata var. mandshurica, along with two known phenethylols, p-hydroxyl phenethanol and 3,4-dihydroxy phenethanol. The planar structures of the new compounds were established on the basis of their spectral data, and their absolute stereochemistry was established by modified Mosher's method. The two known compounds were identified by comparison of spectral data with published references. The two new compounds showed conspicuous antifungal activities by agar medium assay.

Two new triterpenoid saponins, oleiferoside N and oleiferoside O, were isolated from the EtOH extract from the roots of Camellia oleifera C. Abel. Their structures were elucidated as 16α-acetoxy-21β,22α-O-diangeloyloxy-23,28-dihydroxyolean-12-ene 3β-O-β-d-xylopyranosyl-(1 → 3)-α-l-arabinopyranosyl-(1 → 3)-β-d-glucuronopyranoside (1), 16α-acetoxy-21β-O-angeloyloxy-23,28-dihydroxy-22α-O-(2-methylbutanoyloxy)olean-12-ene 3β-O-β-d-xylopyranosyl-(1 → 3)-α-l-arabinopyranosyl-(1 → 3)-β-d-glucuronopyranoside (2), on the basis of spectroscopic analyses (IR, ESI-MS, HR-ESI-MS, 1D and 2D NMR) and acid hydrolysis. Both were characterized to be oleanane-type saponins with sugar moieties linked to C-3 of the aglycone. Cytotoxic activities of two saponins were evaluated against four human tumor cell lines (A549, B16, BEL-7402, and MCF-7) by using the MTT in vitro assay. Compounds 1 and 2 showed moderate cytotoxic activities toward the tested cell lines.

Two new triterpenoid saponins (1 and 2) were isolated from the stems of Ilex cornuta, along with two known triterpenoids (3 and 4). The structures of compounds 1 and 2 were determined as ursane-12,19-diene-28-oic acid 3β-O-β-d-glucuronopyranoside-6-O-methyl ester (1), 3α,23α-dihydroxy-olean-9(11),12-diene-28-oic acid 28-O-β-d-glucopyranosyl ester (2), on the basis of hydrolysis and spectral evidence, including 1D and 2D NMR and high resolution electrospray ionization mass spectrometry (HR-ESI-MS) analyses. Protective effects of compounds 1–4 were tested against H2O2-induced H9c2 cardiomyocyte injury, and the data showed that all these compounds had no cell-protective effect.

To explore the effect of Pulsatilla chinensis (Bunge) Regel saponins (PRS) against juvenile and adult Schistosoma japonicum and to compare its efficacy with praziquantel (PZQ) in vitro.3 h, 7 d, 14 d schistosomula and 42 d adult schistosomes were incubated with 0, 1, 5, 10, 20 and 30 microg/ml PRS for 4, 24, 48 and 72 hours, then the states of them were observed. The changes of the surface of S. japonicum incubated with 30 microg/ml PRS and PZQ within 4 hours were observed by a scanning electron microscope.The sensitivity of 3 h, 7 d, 14 d schistosomula and adults of S. japonicum to 1, 5, 10, 20, 30 microg/ml PRS displayed a time and dose dependence. All the worms died in 30 microg/ml PRS after 4 hours. The dead worm body appeared a gray-white color accompanied with their altered morphogenesis and opaque body. The tegumental surface of adults with different degrees of damages was observed by the electron microscope within 4 hours affected by PRS in vitro.The effects of PRS against S. japonicum in different developmental stages in vitro show that PRS may eventually have a therapeutic potential in the treatment or prevention of S. japonicum infection and is expected to become a new anti-schistosome drug.

A new sulfated triterpenoid, 3β, 24-dihydroxyurs-20-ene-24- O -sulphonyl-28-oic acid (fabagoin, 1 ) was isolated from the barks of Zygophyllum fabago L. Its structure was elucidated on the basis of spectroscopic data.

Five new triterpenoid saponins, 1-5, together with 10 known ones, 6-15 were isolated from the aerial parts of Ilex cornuta. The structures of compounds 1-5 were determined as 3β-O-α-L-arabinopyranosyl-19α,23-dihydroxy-20α-urs-12-en-28-oic acid 28-O-β-D-glucopyranosyl ester, 1; 3β-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-19-hydroxy-20α-urs-12-en-28-oic acid 28-O-β-D-glucopyranosyl ester, 2; 19α,23-dihydroxyurs-12-en-28-oic acid 3β-O-β-D-glucuronopyranoside-6-O-methyl ester, 3; 19α,23-dihydroxyurs-12-en-28-oic acid 3β-O-[β-D-glucuronopyranoside-6-O-methyl ester]-28-O-β-D-glucopyranosyl ester, 4; and 3β-O-[α-L-arabinopyranosyl-(1→2)-β-D-glucuronic acid]-oleanolic 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 1-15 were tested against H2O2-induced H9c2 cardiomyocyte injury, and the data showed that compounds 1, 4, 6, and 13 had significant cell-protective effects. No significant DPPH radical scavenging activity was observed for compounds 1-15.

To investigate the chemical constituents of the root of Ilex cornuta.The constituents were isolated by silica gel, Sephadex LH-20 gel, medium pressure column and semi-preparative liquid chromatography and their structures were elucidated by chemical properties and spectroscopic analyses.Ten compounds were isolated and their structures were identified as: Oleanolic acid (1), Siaresinolic acid (2), 28-O-beta-D-glucopyranosyl pomolic acid (3), Pomolic acid (4), 3beta-O-alpha-L-arabinopyranosyl rotundic acid (5), 3beta-[alpha-L-arabinopyranosyl) oxy]-19alpha-hydroxyolean-12-en-28-oic acid 28-beta-D-glucopyranosyl ester (6), Lup-20(29)-en-3beta,23-diol (7), Chikusetsusaponin IV a butyl ester (8), Oleanolic acid-3-O-( 6'-O-methyl)-beta-D-glucuronopyranoside (9), 3-O-[(alpha-L-arabinopyranosyl)-(1 --2)]-beta-D-glucuronopyranosyl-(6'-O-methyl-ester)-olean-12-ene-28-olic acid (10).Compounds 7 - 10 are isolated from this genus for the first time, and compounds 2 - 6 are isolated from this plant for the first time.

To investigate the effect of Pulsatilla chinensis (Bunge) Regel saponins (PRS) against the eggs, miracidia, cercariae of Schistosoma japonicum in vitro and compare its efficacy with praziquantel.ICR mice were infected with the cercariae of S. japonicum by the patching abdominal method. The livers of the mice were grinded, screened, and then the eggs of S. japonicum were obtained 42 days post-infection. The miracidia were hatched by using the eggs, and the cercariae were obtained by using the infected Oncomelania snails on the light. The eggs, miracidia and cercariae of S. japonicum were incubated with 0, 1, 2, 3, 4, 5, 6, 7, 8 microg/ml PRS for different time, and praziquantel (PZQ) was used as the control.PRS suppressed the hatching rates of eggs for 24 h slightly superior to that of the control drug PZQ at different concentrations, especially in the 4 microg/ml concentration. After the miracidia were incubated with 1, 2, 3, 4, 5, 6, 7, 8 microg/ml PRS for 30 min, the dead rates of miracidia were 13.47, 26.05, 60.99, 90.84, 100, 100, 100, 100%, respectively. After the cercariae were incubated with 1, 2, 3, 4, 5, 6, 7, 8 microg/ml PRS for 30 min, the dead rates of cercariae were 5.32, 18.81, 44.7, 76.87, 98.28, 100, 100, 100%, respectively. PRS showed time- and dose-dependent mortality effects on the miracidia and cercariae of S. japonicum.PRS has the effects against eggs, miracidia, cercariae of S. japonicum in vitro, and it may become a new anti-schistosome agent.

To evaluate the killing effect of BTW5 on both juvenile and adult worms of Schistosoma japonicum in vitro.The mice were infected with cercariae of Schistosoma japonicum obtained from infected Oncomelania hupensis. The juvenile worms were obtained from the liver and mesenteric veins of the mice by perfusion 18 d after the infection, and the adult worms were obtained from the liver and mesenteric veins of the mice by perfusion 5 weeks after the infection. The adult and juvenile worms were cultivated in DMEM medium containing different concentrations of BTW5 and were observed for 3 d. After the observation, the worms were stained by hydrochloric acid carmine to observe the injuries.The death rates and motility reducing rates of adult and juvenile worms in DMEM medium containing different concentrations of BTW5 were significantly higher than those in the controls. The staining suggested that BTW5 had a damage effect on the tegument and the intestinal canal of the male and female worms, in addition to the ovaries of the female worms.BTW5 has an antischistosomal effect on adult and juvenile worms of Oncomelania hupensis.

To observe the toxicity of Pulsatilla chinensis (Bunge) Regel saponins (PRS) against Oncomelania hupensis (O. hupensis).O. hupensis snails were exposed to 40% and 80% of 24 h LC50 of PRS for 24 h, and then choline esterase (CHE), alanine aminotransferase (ALT), alkaline phosphatase (ALP), lactate dehydrogenase (LDH) activities in cephalopodium and liver of snails were determined. Niclosamide (NIC) was used as the reference molluscicide. Zebra fish lethality test was evaluated to non-target aquatic species of PRS.The molluscicidal activity of PRS (LC50 at 24 h: 0.48 mg/L) was similar to that of NIC (LC50 at 24 h: 0.16 mg/L). Significant alterations about CHE, ALP, and ALT activities both in the cephalopodium and the liver of snails were observed when O. hupensis was exposed to 40% and 80% LC50 of PRS or NIC for 24 h. PRS and NIC could not affect LDH activity in the cephalopodium and the liver. Lower toxicity to fish of PRS was observed up to the highest concentration tested than NIC.PRS, as compared with the reference molluscicide NIC, is thought to be used for the control of harmful vector snails safely.

Two new phenylglycol derivatives, (S)-(+)-2-(3,4-dihydroxy phenyl)-2-ethoxyl- ethanol and (S)-(+)-2-(3,4-dihydroxy phenyl)-2-acetoxy-ethanol, were isolated from the leaves of Syringa reticulata var. mandshurica, along with two known phenethylols, p-hydroxyl phenethanol and 3,4-dihydroxy phenethanol. The planar structures of the new compounds were established on the basis of their spectral data, and their absolute stereochemistry was established by modified Mosher's method. The two known compounds were identified by comparison of spectral data with published references. The two new compounds showed conspicuous antifungal activities by agar medium assay.

Uvaria kweichowensis is a folk nongovernmental herb used to treat cure inflammation and tumour in the Southwest area of China. During the course of our investigation for antitumour agents from the stems of Uvaria kweichowensis, six amides were obtained by means of solvent extraction, chromatography on silica gel and Sephadex LH-20 repeatedly. And their structures were identified as uvariadiamide (1), cepharanone (2), aristololactam A II (3), enterocarpam II (4), aristololactam A Ia (5), and 4,5-dioxodehydroasimilobine (6) on the basis of chemical methods and spectral analyses (EI-MS, 1H NMR, 13C NMR). Among them, compound 1 is a new compound; the other compounds were obtained from this plant for the first time.