Effects of combined extreme cold and drought stress on growth, photosynthesis, and physiological characteristics of cool-season grasses.

Abiotic stress is an important factor affecting turf establishment and limiting the sustainability of the turf industry. To alleviate the effects of combined cold and drought stress in cold- and drought-prone regions, it is essential to select and introduce turfgrass germplasms that are suitable for these conditions for successful turf establishment. Thus, we evaluated the effects of combined extreme cold and drought stress on the morphological, plant leaf functional, photosynthetic, and physiological and biochemical traits of 16 wild annual bluegrass (Poa annua) germplasms. We found that there were significant differences (P < 0.05) among different provenances, combined cold and drought stress, and the main interaction factors. Combined cold and drought stress altered the morphological characteristics of the 16 germplasms to varying degrees. Furthermore, combined cold and drought stress significantly reduced the net photosynthetic rate (Pn), stomatal conductance (gs), transpiration rate (Tr), instantaneous water use efficiency (WUE), chlorophyll content, chlorophyll fluorescence parameters, accumulated intercellular CO2 concentration (Ci), and relative electrical conductivity (REC) and malondialdehyde (MDA), proline (Pro), soluble protein (SP), soluble sugar (SS), superoxide anion (O2.-), hydrogen peroxide (H2O2), and hydroxyl radical (·OH) and other active oxygen, and increased the superoxide dismutase activity (SOD), peroxidase activity (POD), catalase activity (CAT), ascorbate peroxidase activity (APX) and glutathione reductase (GR) activities. Comprehensive evaluation using principal component analysis (PCA), membership function analysis, and clustered heatmaps indicated that the 'HZ' germplasm had stronger combined cold and drought tolerance, whereas the 'ZQ' germplasm was more sensitive to combined cold and drought, which was roughly consistent with the order of morphological damage symptoms. Therefore, it is recommended to use the 'HZ' germplasm for planting projects in cold- and drought-prone areas, while the 'ZQ' germplasm is more suitable for use under warmer and non-water-deficient conditions.

Effects of microbial deodorizer on pig feces fermentation and the underlying deodorizing mechanism.

Microbial deodorization is a novel strategy for reducing odor in livestock and poultry feces. Herein, 12 strains of ammonia (NH3) and 15 hydrogen sulfide (H2S) removing bacteria were obtained with a removal efficiency of 65.20-79.80% and 34.90-79.70%, respectively. A novel bacteria deodorant named MIX (Bacillus zhangzhouensis, Bacillus altitudinis, and Acinetobacter pittii at a ratio of 1:1:2) were obtained. MIX can shorten the temperature rising stage by 2 days and prolong the thermophilic stage by 4 days. The ability of MIX to remove NH3, H2S, and volatile fatty acids (VFAs) and the underlying removal mechanism were analyzed during pig feces fermentation. MIX can significantly reduce the concentrations of NH3 and H2S by 41.82% and 66.35% and increase the concentrations of NO3--N and SO42- by 7.80% and 8.83% (P < 0.05), respectively, on the 25th day. Moreover, the concentrations of acetic, propionate, iso-valerate, and valerate were significantly reduced. The dominant bacteria communities at the phylum level were Firmicutes, Proteobacteria, Bacteroidetes, and Spirochaetes. B. zhangzhouensis and B. altitudinis could convert NH4+-N to NO3--N, and A. pittii could transfer H2S to SO42-. This study revealed that bacteria deodorant can reduce the concentrations of NH3, H2S, and VFAs in pig feces and increase those of NH4+, NO3-, and SO42- and has excellent potential in deodorizing livestock and poultry feces composting.

Cytokinin and Metabolites Affect Rhizome Growth and Development in Kentucky Bluegrass (Poa pratensis).

Rhizome growth and development is regulated by phytohormone. However, endogenous phytohormones affect rhizome initiation, and sustained growth in perennial grass species remains elusive. In this study, we investigated the morphological characteristics and the content of indole-3-acetic acid (IAA), zeatin (ZT), gibberellic acid (GA3), and abscisic acid (ABA) in the rhizomes of two different Kentucky bluegrass. Using ultra-performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS), we performed metabolite analysis of two different rhizomes. In our study, the multi-rhizome Kentucky bluegrass material 'Yuzhong' had an average of 1113 rhizomes, while the few-rhizome material 'Anding' had an average of 347 rhizomes. The diameter of rhizome and length of rhizome internode in 'Yuzhong' were 1.68-fold and 1.33-fold higher than that of the 'Anding', respectively. The rhizome dry weight of 'Yuzhong' was 75.06 g, while the 'Anding' was 20.79 g. 'Yuzhong' had a higher ZT content (5.50 µg·g-1), which is 2.4-fold that of 'Anding' (2.27 µg·g-1). In contrast, the IAA, ABA, and GA3 content of rhizome were markedly higher in 'Anding' than 'Yuzhong'. Correlation analysis revealed significant correlations between ZT and ZT/ABA with the number of rhizomes, diameter of rhizome, and length of rhizome internode, whereas IAA, ABA, GA3, and IAA/ZT were opposite. In the metabolic profiles, we identified 163 differentially expressed metabolites (DEMs) (60 upregulated and 103 downregulated) in positive ion mode and 75 DEMs (36 upregulated and 39 downregulated) in negative ion mode. Histidine metabolism and ABC transporters pathways were the most significantly enriched in the positive and negative ion mode, respectively, both of which are involved in the synthesis and transport of cytokinin. These results indicate that cytokinin is crucial for rhizome development and promotes rhizome germination and growth of Kentucky bluegrass.

Carbon and nitrogen metabolism affects kentucky bluegrass rhizome expansion.

BACKGROUND: Rhizome is vital for carbon and nitrogen metabolism of the whole plant. However, the effect of carbon and nitrogen in the rhizome on rhizome expansion remains unclear. RESULTS: Three wild Kentucky bluegrass (Poa pratensis L.) germplasms with different rhizome expansion capacity (strong expansion capacity, 'YZ'; medium expansion capacity, 'WY'; and weak expansion capacity, 'AD') were planted in the field and the rhizomes number, tiller number, rhizome dry weight, physiological indicators and enzyme activity associated carbon and nitrogen metabolisms were measured. Liquid chromatography coupled to mass spectrometry (LC-MS) was utilized to analyze the metabolomic of the rhizomes. The results showed that the rhizome and tiller numbers of the YZ were 3.26 and 2.69-fold of that of the AD, respectively. The aboveground dry weight of the YZ was the greatest among all three germplasms. Contents of soluble sugar, starch, sucrose, NO3--N, and free amino acid were significantly higher in rhizomes of the YZ than those of the WY and AD (P < 0.05). The activities of glutamine synthetase (GS), glutamate dehydrogenase (GDH) and sucrose phosphate synthase (SPS) of the YZ were the highest among all three germplasm, with values of 17.73 A·g- 1 h- 1, 5.96 µmol·g- 1 min- 1, and 11.35 mg·g- 1 h- 1, respectively. Metabolomics analyses revealed that a total of 28 differentially expressed metabolites (DEMs) were up-regulated, and 25 DEMs were down-regulated in both comparison groups (AD vs. YZ group and WY vs. YZ group). Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis demonstrated that metabolites related to histidine metabolism, tyrosine metabolism, tryptophan metabolism, and phenylalanine metabolism were associated with rhizomes carbon and nitrogen metabolism. CONCLUSIONS: Overall, the results suggest that soluble sugar, starch, sucrose, NO3--N, and free amino acid in rhizome are important to and promote rhizome expansion in Kentucky bluegrass, while tryptamine, 3-methylhistidine, 3-indoleacetonitrile, indole, and histamine may be key metabolites in promoting carbon and nitrogen metabolism of rhizome.

Effect of dietary Agriophyllum squarrosum on average daily gain, meat quality and muscle fatty acids in growing Tan lambs.

The herb A. squarrosum is reputed to possess medicinal properties for humans, and has the potential to be a feed resource for livestock. We hypothesized that this herb would improve the meat quality of lambs. To test this hypothesis, 24 Tan ewe-lambs (27.7 ± 0.45 kg) were offered diets containing 0 (CON), 100 (AS100), 200 (AS200) and 300 (AS300) g A. squarrosum/kg DM, and average daily gain, carcass traits, blood metabolites, meat quality and fatty acid profiles were determined. Drip loss % and cooking loss % decreased with the AS100 and AS200 diets (P < 0.05). Dietary A. squarrosum reduced muscle fiber area and diameter and increased density of the meat (P < 0.05), which indicated that the meat was more tender. The concentrations of C10:0 and C18:1n-9 t were 1ower and of C17:0 and C18:3n-3 were greater in the AS200 and AS300 treatments than CON (P < 0.05). Our results suggest that feeding lambs up to 200 g/kg DM of A. squarrosum can increase the water-holding capacity and L* value of meat without compromising growth. Further research is needed to determine the optimal level.

Effects of swine manure composting by microbial inoculation: Heavy metal fractions, humic substances, and bacterial community metabolism.

This study aimed to investigate the effect of swine manure composting with microbial inoculation (MI) and without MI (CK) on heavy metal (Cr, Cd, and Pb) fractions, humic substance (HS), and metabolism pathway. The results showed that MI could passivate the heavy metal Cr and reduce the proportion of exchangeable (EXC) fraction of Cd, but it does not affect the EXC fraction of Pb. Compared to CK, HS, humic acid (HA), and fulvic acid (FA) were significantly increased with MI at the maturity stage. The propagation of Proteobacteria (day 4) and Firmicutes (days 12 and 24) was strengthened with MI. Canonical correlation analysis found that HA and Firmicutes were positively correlated with heavy metal (Cr, Cd, and Pb) residual (RES) fraction, and FA was positively correlated with Proteobacteria. Moreover, MI can significantly increase amino acid metabolism and carbohydrate metabolism by day 4, enhance the metabolism of enzyme families and glycan biosynthesis by day 12, and improve membrane transport. Overall, MI could facilitates the increase in HA and FA content and transfer of heavy metal (Cr, Cd, and Pb) fractions, it particularly helps increase the RES fraction.

Polymer-functionalized mesoporous carbon nanoparticles on overcoming multiple barriers and improving oral bioavailability of Probucol.

Oral administration of nanoparticles is extremely limited due to the two processes of mucus permeation and epithelial absorption, which requires completely opposite surface properties of the nanocarriers. To tackle the contradiction, we developed a rational strategy to modify the surface of mesoporous carbon nanoparticles with chitosan concealed by a hydrophilic N-(2-hydroxypropyl) methacrylamide copolymer (pHPMA) layer. Probucol (PB) with the low poor permeability and solubility was loaded in optimal nanocarriers to realize the high loading efficacy and controlled release. The pHPMA polymer is a hydrophilic "mucus-inert" material, which could be dissociable from the surface of nanoparticles in the mucus, thus promoting their mucus permeation and causing exposure of chitosan in transepithelial transport. The swelling effect of chitosan under acidic conditions allowed regulation of PB release behavior. In conclusion, the mucus-permeable nanocarrier could effectively overcome multiple gastrointestinal absorption barriers and the oral bioavailability of PB-loaded HCMCN was 2.76-fold that of commercial preparation.

Microbial inoculation influences bacterial community succession and physicochemical characteristics during pig manure composting with corn straw.

This study determined the physicochemical changes and bacterial community succession in the pig manure composting process with microbial inoculant. Microbial inoculant could prolong the thermophilic stage by 2 days and increased the germination index (GI). Analysis with 16S rDNA showed that the Chao1 and Shannon indices increased at the thermophilic stage in the treatment (T), while those of the control (C) decreased. Microbial inoculant increased the relative abundance of Flavobacterium and Solibacillus in 4-12 and 12-24 days, respectively. Acinetobacter was reduced at 4-12 days. The key physicochemical factors affecting microbial successions were revealed by canonical correspondence analysis (CCA) and correlation analysis. Linear discriminant analysis (LDA) effect size (LEfse) analysis showed that there were 78 biomarkers, while in piles T and C, there were 35 and 43 biomarkers, respectively. These results indicated the addition of microbial inoculant improved the maturity and fertility, as well as significantly regulating the microbial community structure.

Study on the inversion of doped concentration induced by millisecond pulsed laser irradiation silicon-based avalanche photodiode.

In this paper, an experimental study of silicon-based avalanche photodiode (Si-APD) with millisecond pulse laser irradiation was carried out, and the C-V curve of Si-APD was obtained by using a semiconductor analyzer. Based on the single-side abrupt junction character of n+p, combined with the corresponding theoretical derivation, the doping concentration varying with the axial depth of damaged Si-APD was obtained by inverse computation. The lattice dislocation and junction reduction were the fundamental causes of the reduced doping concentration. The research results provide a new method for the study of the internal doping concentration for detectors with millisecond pulse laser damage.

Size effect on oral absorption in polymer-functionalized mesoporous carbon nanoparticles.

In this manuscript, the effect of the particle size of polymer-functionalized mesoporous carbon (MPP) nanoparticles on enhancing oral absorption of a water-insoluble drug is first investigated. The insoluble drug, fenofibrate (Fen), was selected as the model drug loaded in the MPP nanoparticles. MPP nanoparticles with different particle sizes were designed for improving the oral bioavailability of drugs, in which the branched polyethyleneimine (PEI) and polyacrylic acid (PAA) were modified on the surfaces of mesoporous carbon nanoparticles (MCNs) with amide bonds. In addition, PEI-functionalized carbon quantum dots (PCA) and radioisotope 125I were applied to label the MPP nanoparticles to trace in the vivo process. According to the data, the MPP nanoparticles could markedly improve the dissolution rate and oral bioavailability of Fen. Interestingly, the MPP nanoparticle size had a notable effect on Fen oral absorption, and intermediate sized MPP nanoparticles were expected to be more ideal oral drug carriers. The nanoparticles were safe and easily excreted. These findings present the prospect of MPP nanoparticles for oral application, and guides the rational design of an oral delivery system with respect to particle size.

Synthesis and In Vitro Anti-Influenza Virus Evaluation of Novel Sialic Acid (C-5 and C-9)-Pentacyclic Triterpene Derivatives.

The emergence of drug resistant variants of the influenza virus has led to a great need to identify novel and effective antiviral agents. In our previous study, a series of sialic acid (C-2 and C-4)-pentacyclic triterpene conjugates have been synthesized, and a five-fold more potent antiviral activity was observed when sialic acid was conjugated with pentacyclic triterpene via C-4 than C-2. It was here that we further reported the synthesis and anti-influenza activity of novel sialic acid (C-5 and C-9)-pentacyclic triterpene conjugates. Their structures were confirmed by ESI-HRMS, ¹H-NMR, and 13C-NMR spectroscopic analyses. Two conjugates (26 and 42) showed strong cytotoxicity to MDCK cells in the CellTiter-Glo assay at a concentration of 100 µM. However, they showed no significant cytotoxicity to HL-60, Hela, and A549 cell lines in MTT assay under the concentration of 10 µM (except compound 42 showed weak cytotoxicity to HL-60 cell line (10 µM, ~53%)). Compounds 20, 28, 36, and 44 displayed weak potency to influenza A/WSN/33 (H1N1) virus (100 µM, ~20-30%), and no significant anti-influenza activity was found for the other conjugates. The data suggested that both the C-5 acetylamide and C-9 hydroxy of sialic acid were important for its binding with hemagglutinin during viral entry into host cells, while C-4 and C-2 hydroxy were not critical for the binding process and could be replaced with hydrophobic moieties. The research presented herein had significant implications for the design of novel antiviral inhibitors based on a sialic acid scaffold.

A comparison between sphere and rod nanoparticles regarding their in vivo biological behavior and pharmacokinetics.

In recent years, spherical nanoparticles has been studied extensively on biomedical applications including bioimaging and biosensing, diagnostics and theranostics, but the effect of the shape of nanoparticles has received little attention. In the present study, we designed three different shaped fluorescent mesoporous silica nanoparticles (MSNs), long rod nanoparticles (NLR), short rod nanoparticles (NSR), and spherical nanoparticles (NS) to systematically examine their behavior in vivo after oral administration. The results of the ex vivo optical imaging study in mice indicated that rod nanoparticles had a longer residence time in the gastrointestinal compared with spherical nanoparticles. The in vivo biodistribution showed that all the orally administered MSNs were mainly taken up by the liver, and kidney. NLR had a great capacity to overcoming rapid clearance by the RES and exhibited a longer circulation in the blood than NSR and NS. During renal excretion, the spherical nanoparticles were cleared faster than rod nanoparticles. In addition, it was also found that MSNs can be degraded in vivo and NSR were degraded faster than NLR and NS probably owing to their higher specific surface area. The pharmacokinetic results demonstrated that nifedipine(NI)-loaded NLR had a higher bioavailability than NI-loaded NSR and NS.

Proteasome Inhibitor YSY01A Enhances Cisplatin Cytotoxicity in Cisplatin-Resistant Human Ovarian Cancer Cells.

Cisplatin is one of the most common drugs used for treatment of solid tumors such as ovarian cancer. Unfortunately, the development of resistance against this cytotoxic agent limits its clinical use. Here we report that YSY01A, a novel proteasome inhibitor, is capable of suppressing survival of cisplatin-resistant ovarian cancer cells by inducing apoptosis. And YSY01A treatment enhances the cytotoxicity of cisplatin in drug-resistant ovarian cancer cells. Specifically, YSY01A abrogates regulatory proteins important for cell proliferation and anti-apoptosis including NF-κB p65 and STAT3, resulting in down-regulation of Bcl-2. A dramatic increase in cisplatin uptake was also observed by inductively coupled plasma-mass spectrometry following exposure to YSY01A. Taken together, YSY01A serves as a potential candidate for further development as anticancer therapeutics targeting the proteasome.

Anticancer Effect of a Novel Proteasome Inhibitor, YSY01A, via G2/M Arrest in PC-3M Cells in vitro and in vivo.

YSY01A is a new tripeptideboronic acid and an analog of PS341. However, YSY01A's antitumor effects and mechanism have not yet been elucidated. This study demonstrates that YSY01A inhibited proteasome activity by combining with the chymotrypsin-like (CT-L) site (ß5i/ß5), the post-glutamyl peptide hydrolase (PGPH) site (ß1i/ß1) and the trypsin-like (T-L) site (ß2i/ß2) in special fluorgonic substrates and proteasome probe tests. We explored the anticancer effect using methyl thiazolyltetrazolium (MTT) or sulforhodamine B (SRB), and PC-3M cells were sensitive to YSY01A among the four cancer cell types tested. The YSY01A antiproliferative effect was stronger than that of PS341. In vivo, YSY01A (1.25, 2.25, and 3.25 mg/kg) inhibited PC-3M cell xenograft tumor growth, and the tumor volume inhibition rate was approximately 40% to 60%. YSY01A arrested PC-3M cells in the G2/M phase of the cell cycle by flow cytometry (FCM). Many proteins related to the cell cycle were analyzed using western blot, and YSY01A was shown to increase p21, p27, cyclinB1, P-cdc2 (tyr15) and wee1 protein expression in both cells and tumor tissue in a concentration-dependent manner. YSY01A, a proteasome inhibitor, exerts anticancer effects on PC-3M cells in vitro and in vivo. The mechanism of the YSY01A-mediated antitumor effect is that the cell cycle is arrested at the G2/M stage. This study suggests that YSY01A may be a novel therapeutic agent for prostate cancer.

Pseudolaric acid B inhibits inducible cyclooxygenase-2 expression via downregulation of the NF-κB pathway in HT-29 cells.

PURPOSE: Pseudolaric acid B (PAB) is a diterpene acid isolated from the root and trunk bark of Pseudolaric kaempferi Gordon. Previous work has found that PAB has anti-inflammatory and anti-tumor effects in xenograft models of human hepatocellular carcinoma. The aim of this study is to evaluate the correlation between anti-cancer and anti-inflammatory effects of PAB and its molecular mechanisms on HT-29 cells. METHODS: Production of prostaglandin E2 (PGE2) in HT-29 cells was evaluated by ELISA. mRNA of cyclooxygenase-2 (COX-2) was analyzed by RT-PCR assay. High-content screening (HCS) method was adopted to detect the cytokine mixture (CM)-induced transcription activity of NF-κB and STAT3. Western blotting was used to evaluate the protein expression levels of inflammatory mediators induced by CM. After treatment with PAB in various concentrations, the inhibition rate of cell proliferation was measured with sulforhodamine B assays. For the in vivo studies, tumor-bearing models xenografted with HT-29 cells were developed in nude mice, and following oral administration with PAB, tumor inhibition rate was calculated. RESULTS: PAB inhibited the PGE2 production in HT-29 cells significantly (P < 0.05) with similar results detected at the COX-2 mRNA level. Furthermore, PAB suppressed the COX-2 protein expression and significant nuclear translocation of NF-κB and STAT3 induced by CM, which correlated with a concomitant degradation of I-κB and a decrease in constitutive STAT3 phosphorylation (P < 0.05). Moreover, various concentrations of PAB inhibited the proliferation of HT-29 cells in a dose- and time-dependent manner. In vivo, after treatment with PAB for 17 days, the tumor weight of the 50 and 100 mg/kg treated groups was 0.62 ± 0.15 and 0.54 ± 0.06 g, respectively. When compared to the control group (0.82 ± 0.16 g), the inhibition rate of tumor weight was 24.2% at 50 mg/kg (P < 0.05) and 34.7% at 100 mg/kg (P < 0.001). CONCLUSIONS: PAB shows potential anti-cancer activity in HT-29 cells, and its molecular mechanisms are related to the anti-inflammatory action.

ß-Escin sodium inhibits inducible nitric oxide synthase expression via downregulation of the JAK/STAT pathway in A549 cells.

ß-escin, a triterpene saponin, is one of the major active compounds extracted from horse chestnut (Aesculus hippocastanum) seed. Previous work has found that ß-escin sodium has antiinflammatory and antitumor effects. In the present study, we investigated its effect on cell proliferation and inducible nitric-oxide synthase (iNOS) expression in human lung carcinoma A549 cells. ß-escin sodium (5-40 µg/mL) inhibited cytokine mixture (CM)-induced nitric oxide (NO) production in A549 cells by reducing the expression of iNOS. ß-escin sodium suppressed phosphorylation and nuclear translocation of STAT1 (Tyr701) and STAT3 (Tyr705) induced by CM but did not affect the activation of c-Jun and NF-κB. ß-escin sodium inhibited the activation of protein tyrosine kinase JAK2. Pervanadate treatment reversed the ß-escin sodium-induced downregulation of STAT3 and STAT1. ß-escin sodium treatment enhanced an activating phosphorylation of the phosphatase SHP2. Small interfering RNA-mediated knockdown of SHP2 inhibited ß-escin sodium-induced phospho-STAT dephosphorylation. Moreover ß-escin sodium reduced the activation of p38 MAPK. Finally, ß-escin sodium inhibited the proliferation of A549 cells, did not change the cell membrane's permeability, nuclear morphology and size and the mitochondria's transmembrane potential of A549 cells. Taken together, these results demonstrate that ß-escin sodium could downregulate iNOS expression through inhibiting JAK/STAT signaling and p38 MAPK activation in A549 cells. ß-escin sodium has a marked antiproliferative effect on A549 cells at least in part by inhibiting the JAK/STAT signaling pathway, but not by a cytotoxic effect. ß-escin sodium would be useful as a chemopreventive agent or a therapeutic against inflammatory-associated tumor. © 2011 Wiley Periodicals, Inc.

Cytotoxic activity of some Asarum plants.

The cytotoxic activity against some tumor cell lines of 16 commonly used species of Asarum was evaluated in this study. All of these plants were widely used in Asian countries as traditional medicines or folk medicines. Their inhibitory activities against four tumor cell lines (HL-60, BGC-823, KB and Bel-7402) were compared. It was observed that 10 of the tested extracts (eight ethanol extracts and two water extracts) among 32 extracts of these plants showed cytotoxic activity. Those 95% ethanol extractions from A. caudigerellum, A. forbesii, A. inflatum and A. maximum exhibited the highest cytotoxic activity, and 95% ethanol extracts or water extracts of A. sieboldii var. seoulense, A. himalaicum, A. splendens and A. crispulatum showed selective activity against one or two cells among the tested tumor cells. This is the first report of Asarum plants possessing cytotoxic activity against tumor cell lines.

Cardenolides from Saussurea stella with cytotoxicity toward cancer cells.

Three new cardenolides, 3-O-beta-D-fucopyranosylstrophanthidin (1), 3-O-beta-D-quinovopyranosylperiplogenin (2), and 3-O-beta-D-glucopyranosyl-(1 --> 4)-alpha- l-rhamnopyranosylcannogenin (3), together with seven known cardenolides (4- 10), were isolated from a cytotoxic ethanol extract of the whole dried plants of Saussurea stella. The structures of these compounds were established by spectroscopic and chemical methods. When the cytotoxicity of compounds 2- 10 toward Bel-7402 human hepatoma cells and BGC-823 human gastric cancer cells was evaluated, all compounds showed IC 50 values of <1 microM for both cell lines. This is the first report of cardenolides occurring in a species of the family Asteraceae.

[Inhibitory effects of 11 coumarin compounds against growth of human bladder carcinoma cell line E-J in vitro].

OBJECTIVE: To screen antitumor active compounds, drug-like or leading compounds from Chinese traditional and herbal drugs. METHODS: Eleven coumarin compounds isolated from the Chinese traditional and herbal drugs were studied for their antitumor activities in vitro by determining the inhibition rates against growth of human bladder carcinoma cell line E-J. RESULTS: It showed that umbelliferone, scoparone, demethylfuropinarine, isopimpinellin, forbesoside, columbianadin, decursin and glycycoumarin inhibited the growth of human bladder carcinoma cell line E-J in vitro and their activities showed a concentration-effect relationship. The inhibitory effects of forbesoside, columbianadin, decursin and umbelliferone, with IC50 values of 7.50x10(-7), 2.30x10(-6), 6.00x10(-6) and 1.30x10(-6) mol/L, respectively, were stronger than those of the other tested compounds. However, xanthotoxin, esculin and sphondin did not inhibit the growth of human bladder carcinoma cell line E-J in this assay condition. CONCLUSION: These findings indicate that forbesoside, columbianadin, esculin, decursin and umbelliferone would be effective or regarded as potent drug-like or leading compounds against human bladder carcinoma.