Bisthiodiketopiperazines and Acorane Sesquiterpenes Produced by the Marine-Derived Fungus Penicillium adametzioides AS-53 on Different Culture Media.

Chemical investigation of the marine-sponge-derived fungus Penicillium adametzioides AS-53 resulted in the identification of two new bisthiodiketopiperazine derivatives, adametizines A (1) and B (2), from cultivation in a liquid potato-dextrose broth (PDB) culture medium, whereas two new acorane sesquiterpenes, adametacorenols A (3) and B (4), were isolated from a rice solid culture medium. The structures of these compounds were elucidated on the basis of spectroscopic analysis. The absolute configuration of compound 1 was determined by X-ray crystallographic analysis, and that of 3 was determined by modified Mosher's method.

Brocazines A-F, Cytotoxic Bisthiodiketopiperazine Derivatives from Penicillium brocae MA-231, an Endophytic Fungus Derived from the Marine Mangrove Plant Avicennia marina.

Six new disulfide-bridged diketopiperazine derivatives, brocazines A-F (1-6), along with one known analogue (7), were isolated and identified from the cytotoxic extract of Penicillium brocae MA-231, a fungus obtained from the fresh tissue of the marine mangrove plant Avicennia marina. The structures of these compounds were established on the basis of detailed interpretation of NMR and mass spectroscopic data. X-ray crystallographic analysis confirmed the structure of 1 and established the structure and absolute configuration of 5, while the absolute configurations for compounds 1, 4, and 6 were deduced by comparison of the CD data with those of 5.

Sulfur-containing cytotoxic curvularin macrolides from Penicillium sumatrense MA-92, a fungus obtained from the rhizosphere of the mangrove Lumnitzera racemosa.

Sumalarins A-C (1-3), the new and rare examples of sulfur-containing curvularin derivatives, along with three known analogues (4-6), were isolated and identified from the cytotoxic extract of Penicillium sumatrense MA-92, a fungus obtained from the rhizosphere of the mangrove Lumnitzera racemosa . Their structures were established by detailed interpretation of NMR and MS data, and compound 1 was confirmed by X-ray crystallographic analysis. Compounds 1-3 and 5 showed potent cytotoxicity against some of the tested tumor cell lines.

Asperolides A-C, tetranorlabdane diterpenoids from the marine alga-derived endophytic fungus Aspergillus wentii EN-48.

Bioassay-guided fractionation of the culture extract of Aspergillus wentii EN-48, an endophytic fungus isolated from an unidentified marine brown algal species of the genus Sargassum, led to the isolation of three new tetranorlabdane diterpenoids, asperolides A-C (1-3), and five related derivatives (4-8). The structures of these compounds were established on the basis of spectroscopic interpretation, and compound 1 was confirmed by X-ray crystallographic analysis. The absolute configuration of 1 was determined by application of the modified Mosher's method.

A new triterpenoid saponin from Abrus precatorius Linn.

A new triterpenoid saponin, 3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyranosyl subprogenin D (1), together with six known triterpenoids: subprogenin D (2), abrusgenic acid (3), triptotriterpenic acid B (4), abruslactone A (5), abrusogenin (6) and abrusoside C (7) were isolated from the leaves and stems of Abrus precatorius. Their structures were elucidated on the basis of physical and NMR analysis, respectively. Compounds 5 and 6 showed moderate cytotoxicity against MCF-7, SW1990, Hela, and Du-145 cell lines.

Tanghinigenin from seeds of Cerbera manghas L. induces apoptosis in human promyelocytic leukemia HL-60 cells.

Tanghinigenin, a cardiac glycoside, is isolated from the seeds of Cerbera manghas L. In this study, we demonstrated that tanghinigenin reduced the viability of human promyelocytic leukemia HL-60 cells in a time- and dose-dependent manner, and efficiently induced apoptosis in HL-60 cells as evidenced by the Annexin V/PI binding assay, DNA fragmentation and AO/EB staining studies. In addition, stimulation of HL-60 cells with tanghinigenin induced a series of intracellular events including the activation of caspase-3, -8, and -9, as well as up-regulation of Fas and FasL protein level.

Nigerapyrones A-H, α-pyrone derivatives from the marine mangrove-derived endophytic fungus Aspergillus niger MA-132.

Eight new α-pyrone derivatives, namely, nigerapyrones A-E (1-5) and nigerapyrones F-H (8-10), along with two known congeners, asnipyrones B (6) and A (7), were isolated from Aspergillus niger MA-132, an endophytic fungus obtained from the fresh tissue of the marine mangrove plant Avicennia marina. The structures of these compounds were elucidated on the basis of spectroscopic analysis. The undescribed geometries of the trisubstituted double bonds (C-9 and C-11) for asnipyrone B (6) have now been explicitly determined, while the incorrect placement of the methyl group at C-5 of asnipyrone A (7) has now been revised at C-3.

Propofol post-conditioning protects against cardiomyocyte apoptosis in hypoxia/reoxygenation injury by suppressing nuclear factor-kappa B translocation via extracellular signal-regulated kinase mitogen-activated protein kinase pathway.

Background And Objective: Perioperative myocardial ischaemia leads to an exceedingly high mortality. Previous studies have indicated that propofol pre-conditioning could mimic the cardioprotective effects of ischaemic pre-conditioning. The purpose of this study was to determine whether propofol post-conditioning is cardioprotective and to explore the possible molecular mechanism of propofol post-conditioning.

7-Nor-ergosterolide, a pentalactone-containing norsteroid and related steroids from the marine-derived endophytic Aspergillus ochraceus EN-31.

7-Nor-ergosterolide (1), a rare 7-norsteroid with an unusual pentalactone B-ring system, and two new steroid derivatives, 3β,11α-dihydroxyergosta-8,24(28)-dien-7-one (2) and 3β-hydroxyergosta-8,24(28)-dien-7-one (3), were characterized from the culture extract of Aspergillus ochraceus EN-31, an endophytic fungus isolated from the marine brown alga Sargassum kjellmanianum. In addition, nine known related steroids were isolated and identified. The structures of these compounds were established on the basis of extensive spectroscopic analysis.

β-D-Glucosyl-(1-4)-α-L-thevetosides of 17β-digitoxigenin from seeds of Cerbera manghas L. induces apoptosis in human hepatocellular carcinoma HepG2 cells.

β-D-Glucosyl-(1-4)-α-L-thevetosides of 17β-digitoxigenin (GHSC-73) is a cardiac glycoside isolated from the seeds of Cerbera manghas L. GHSC-73 reduced viability of HepG2 cells in a time- and dose-dependent manner without decreasing the viability of Chang human liver cells and Swiss albino 3T3 fibroblasts, induced efficiently stimulated apoptosis in HepG2 cells as evidenced by DNA fragmentation, annexin V/PI binding assay and DAPI staining. This apoptotic process was accompanied by the activation of the effector caspase-3, the loss of mitochondrial membrane potential (ΔΨ(m)) and translocation of AIF from the mitochondrion to the nucleus in HepG2 cells.

Synthesis and antitumor evaluation of methyl spongoate analogs.

A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 and NCI-H460 tumor cell lines. The pharmacological results confirmed that the α,β-unsaturated carbonyl moiety, a Michael acceptor in ring A, plays a pivotal role in the cytotoxic effect of these derivatives.

Sexangulic acid, a new cytotoxic triterpenoid from the Chinese mangrove Bruguiera sexangula.

A new cytotoxic lanostane-type triterpenoid, sexangulic acid (1), has been isolated from mangrove Bruguiera sexangula. The structure of the new compound was elucidated on the basis of chemical reaction and the analysis of spectroscopic data.

2'-epi-2'-O-Acetylthevetin B extracted from seeds of Cerbera manghas L. induces cell cycle arrest and apoptosis in human hepatocellular carcinoma HepG2 cells.

2'-epi-2'-O-Acetylthevetin B (GHSC-74) is a cardiac glycoside isolated from the seeds of Cerbera manghas L. We have demonstrated that GHSC-74 reduced the viability of HepG2 cells in a time- and dose-dependent manner. The present study was designed to explore cellular mechanisms whereby GHSC-74 led to cell cycle arrest and apoptosis in HepG2 cells.

2'-Epi-2'-O-acetylthevetin B induces apoptosis partly via Ca(2+)-mediated mitochondrial pathway in human hepatocellular carcinoma HepG2 cells.

2'-Epi-2'-O-acetylthevetin B (GHSC-74), a cardiac glycoside, can be isolated from the seeds of Cerbera manghas L. We demonstrated that GHSC-74 reduced the viability of HepG2 cells in a time- and dose-dependent manner, and efficiently induced apoptosis without significantly decreasing the viability of Chang human liver cells and Swiss albino 3T3 fibroblasts, as indicated by annexin-V/PI binding assay and Hoechst 33342 staining. In addition, stimulation of HepG2 cells with GHSC-74 induced a series of intracellular events: (1) loss of mitochondrial membrane potential; (2) sustained elevation of cytosolic [Ca2+]; and (3) downregulation of Bcl-2.

[Studies on phenylpropanoids from herbs of Eriophyton wallichii].

Objective: To study the chemical constituents of Eriophyton wallichii.

Method: Compounds were separated and purified by column chromatographic methods, and their structures were elucidated by spectroscopic methods.

Result: Eight phenylpropanoids were isolated and identified as martynoside (1), leucosceptoside A (2), citrusin B (3), (+)-dehydrodiconiferyl alcohol-4, 9-beta-D-glucopyranoside (4), liriodendrin (5), velutinoside 11[ (6), jionoside B, (7), stachysoside D (8), respectively.

Renierol from marine sponge Haliclona.SP.: a natural inhibitor of xanthine oxidase with hypouricemic effects.

The purpose of this study was to evaluate the inhibitory effect of renierol, extracted from marine sponge Halicdona.SP., on xanthine oxidase (XO) and its hypouricemic effect in vivo.

Hypouricemic effects of phenylpropanoid glycosides acteoside of Scrophularia ningpoensis on serum uric acid levels in potassium oxonate-pretreated Mice.

Phenylpropanoid glycoside acteoside was extracted from the traditional Chinese medicine Scrophularia ningpoenis Hemsl. In the present study, we investigated the effects of acteoside administration on serum uric acid levels in mice rendered hyperuricemic with the uricase inhibitor potassium oxonate. When administered orally for 3 days at doses of 50, 100 and 150 mg/kg, acteoside reduced serum uric acid levels by 15.

Effects of shark hepatic stimulator substance on the function and antioxidant capacity of liver mitochondria in an animal model of acute liver injury.

This study was carried out to investigate whether shark hepatic stimulator substance (HSS) can prevent acute liver injury and affect mitochondrial function and antioxidant defenses in a rat model of thioacetamide (TAA)-induced liver injury. The acute liver injury was induced by two intraperitoneal injections of TAA (400 mg/kg) in a 24 h interval. In the TAA plus shark HSS group, rats were treated with shark HSS (80 mg/kg) 1 h prior to each TAA injection.