Germacrane Sesquiterpene Dilactones from Mikania micrantha and Their Antibacterial and Cytotoxic Activity.

Four new germacrane sesquiterpene dilactones, 2ß-hydroxyl-11ß,13-dihydrodeoxymikanolide (1), 3ß-hydroxyl-11ß,13-dihydrodeoxymikanolide (2), 1α,3ß-dihydroxy-4,9-germacradiene-12,8:15,6-diolide (3), and (11ß,13-dihydrodeoxymikanolide-13-yl)-adenine (4), together with five known ones (5-9) were isolated from the aerial parts of Mikania micrantha. Their structures were elucidated on the basis of extensive spectroscopic analysis. Compound 4 is featured with an adenine moiety in the molecule, which is the first nitrogen-containing sesquiterpenoid so far isolated from this plant species. These compounds were evaluated for their in vitro antibacterial activity against four Gram-(+) bacteria of Staphyloccocus aureus (SA), methicillin-resistant Staphylococcus aureus (MRSA), Bacillus cereus (BC) and Curtobacterium. flaccumfaciens (CF), and three Gram-(-) bacteria of Escherichia coli (EC), Salmonella. typhimurium (SA), and Pseudomonas Solanacearum (PS). Compounds 4 and 7-9 were found to show strong in vitro antibacterial activity toward all the tested bacteria with the MIC values ranging from 1.56 to 12.5 µg/mL. Notably, compounds 4 and 9 showed significant antibacterial activity against the drug-resistant bacterium of MRSA with MIC value 6.25 µg/mL, which was close to reference compound vancomycin (MIC 3.125 µg/mL). Compounds 4 and 7-9 were further revealed to show in vitro cytotoxic activity toward human tumor A549, HepG2, MCF-7, and HeLa cell lines, with IC50 values ranging from 8.97 to 27.39 µM. No antibacterial and cytotoxic activity were displayed for the other compounds. The present research provided new data to support that M. micrantha is rich in structurally diverse bioactive compounds worthy of further development for pharmaceutical applications and for crop protection in agricultural fields.

The DeltaN p63 Promotes EMT and Metastasis in Bladder Cancer by the PTEN/AKT Signalling Pathway.

Bladder cancer is a common tumour of the urinary system, and more than 90% is urothelial carcinoma. Therefore, it is important for discovering the key target genes and molecules of bladder tumour cell metastasis and invasion. Our research initially explored the regulation of deltaN p63 on the progression and metastasis of bladder cancer and found that deltaN p63 can influence the occurrence of EMT through PTEN and ultimately regulate the growth and metastasis of bladder cancer. In summary, this study identified a new EMT regulator, deltaN p63, further revealed the mechanism of the invasion and metastasis of bladder cancer cells, and provided a theoretical basis for finding new target molecules and drugs to treat bladder cancer. In conclusion, this study will further reveal the mechanism of tumour cell invasion and metastasis and provide a theoretical basis for cancer treatment to find new target molecules and drugs.

Comparative Study of Sargassum fusiforme Polysaccharides in Regulating Cecal and Fecal Microbiota of High-Fat Diet-Fed Mice.

Seaweed polysaccharides represent a kind of novel gut microbiota regulator. The advantages and disadvantages of using cecal and fecal microbiota to represent gut microbiota have been discussed, but the regulatory effects of seaweed polysaccharides on cecal and fecal microbiota, which would benefit the study of seaweed polysaccharide-based gut microbiota regulator, have not been compared. Here, the effects of two Sargassum fusiforme polysaccharides prepared by water extraction (SfW) and acid extraction (SfA) on the cecal and fecal microbiota of high-fat diet (HFD) fed mice were investigated by 16S rRNA gene sequencing. The results indicated that 16 weeks of HFD dramatically impaired the homeostasis of both the cecal and fecal microbiota, including the dominant phyla Bacteroidetes and Actinobacteria, and genera Coriobacteriaceae, S24-7, and Ruminococcus, but did not affect the relative abundance of Firmicutes, Clostridiales, Oscillospira, and Ruminococcaceae in cecal microbiota and the Simpson's index of fecal microbiota. Co-treatments with SfW and SfA exacerbated body weight gain and partially reversed HFD-induced alterations of Clostridiales and Ruminococcaceae. Moreover, the administration of SfW and SfA also altered the abundance of genes encoding monosaccharide-transporting ATPase, α-galactosidase, ß-fructofuranosidase, and ß-glucosidase with the latter showing more significant potency. Our findings revealed the difference of cecal and fecal microbiota in HFD-fed mice and demonstrated that SfW and SfA could more significantly regulate the cecal microbiota and lay important foundations for the study of seaweed polysaccharide-based gut microbiota regulators.

Regulation mechanisms of humic acid on Pb stress in tea plant (Camellia sinensis L.).

Though the interaction between humic acid (HA) and heavy metals has been widely reported, the effects of HA on the toxicity of heavy metals to plants are still in debate. In this study, the regulation mechanisms of HA on Pb stress in tea plant (Camellia sinensis L.) was investigated through hydroponic experiments, and the experimental results were explained by using transmission electron microscope (TEM), scanning transmission X-ray microscopes (STXM) and isobaric tags for relative and absolute quantitation (iTRAQ) differential proteomics. Significant alleviation of Pb stress was found with HA coexistence. TEM results showed that HA greatly mitigated the damage of cells caused by Pb stress. Compared with sole Pb treatment, the addition of HA increased the contents of pectin and pectic acid in the cell wall by 10.5% and 30.5%, while arabinose (Ara) and galactose (Gal) decreased by 20.5% and 15.9%, respectively, which were beneficial for increasing Pb adsorption capacity of the cell wall and promoting cell elongation. Moreover, iTRAQ differential proteomics analysis proved that HA strengthened the antioxidant system, promoted the synthesis of cell wall, and stabilized protein and sulfur-containing substance metabolism in molecular level. Notably, the concentration of calcium (Ca) in the cell wall of HA coexistence treatment was 47.4% higher than Pb treatment. STXM results also indicated that the distribution of Ca in the cell wall was restored with the presence of HA. This might promote the formation of the egg-box model, thus alleviating Pb stress in cells. Our results reveal the regulation mechanisms of HA on Pb detoxification in plants and provide useful information for improving the safety of agricultural products.

Ganoderma lucidum spore ethanol extract attenuates atherosclerosis by regulating lipid metabolism via upregulation of liver X receptor alpha.

CONTEXT: Ganoderma lucidum (Leyss.ex Fr.) Karst (Ganodermataceae) is a fungus that has been used in traditional Chinese medicine. OBJECTIVE: This is the first investigation of the lipid-lowering and anti-atherosclerotic effects of Ganoderma lucidum spore ethanol extract (EEG) in hyperlipidemic rabbits. MATERIALS AND METHODS: Fifty-four Japanese rabbits were randomly divided into six groups (n = 9): control, model, atorvastatin and three EEG groups (6, 24 and 96 mg/kg/day, p.o.). Control group was administered a normal diet and other groups were administered a high-fat diet to induce hyperlipidaemia and atherosclerosis for 14 weeks. During this time, lipid profiles were recorded; lipid testing and histopathological examination of aorta and liver were conducted. LXRα and its downstream genes expression in the liver and small intestine were examined. The effect of EEG on macrophage cholesterol efflux and ABCA1/G1 expression was observed under silenced LXRα expression. RESULTS: EEG reduced serum cholesterol (20.33 ± 3.62 mmol/L vs 34.56 ± 8.27 mmol/L for the model group) and LDL-C, reduced the area of arterial plaques (24.8 ± 10% vs 53.9 ± 15.2% for the model group) and Intima/Medium thickness ratio, increased faecal bile acid content, upregulated LXRα, CYP7A1, ABCA1/G1, ABCG5/G8 expression in the liver, small intestine and macrophages. After silencing LXRα in macrophages, the ability of EEG to promote cholesterol efflux was inhibited. DISCUSSION AND CONCLUSION: EEG exert lipid-lowering and anti-atherosclerotic effects via upregulating expression of LXRα and downstream genes associated with reverse cholesterol transport and metabolism. However, whether PPARα/γ are involved in the up-regulation of LXR expression by EEG remains to be elucidated.

Chemical Constituents of Water Extract from Camptosorus sibiricus / 中国实验方剂学杂志

Objective::Camptosorus sibiricus is a kind of herbal medicine and famous folk medicine. However, the bioactivities or pharmacological effects of the C. sibiricus remain to be unclear. Therefore, it is necessary to make a systematic study on chemical constituents from C. sibiricus, so as to further study its potential medicinal value, and provide certain chemical basis and foundation for the comprehensive development and the search for pharmacological activity. Method::Various column chromatographic technologies, (silica gel, Sephadex LH-20 and ODS column chromatography) as well as HPLC were adopted to separate chemical constituents of C. sibiricus extract. The structure of the purified compounds was elucidated by nuclear magnetic resonance (NMR) and high-resolution electrospray ionization-mass spectrometry (HR-ESI-MS). Result::Totally 10 compounds have been isolated from water extract of C. sibiricus. By spectroscopic methods, they were elucidated as 7-dien-3-on-9-O-β-D-glucoside (1), bridelionoside F (2), (3R, 5S, 6S, 7E, 9S)-megastigm, an-7-ene-3, 5, 6, 9-tetrol 9-O-β-D-glucopyranoside (3), (6S, 7E, 9R)-roseoside (4), (3S, 5S, 6R, 9R)-3-hydroxy-5, 6-epoxy-β-ionol-9-O-β-glucopyranoside (5), 6, 9-dihydroxy-4, 7-megastigmadien-3-one (6), (3R, 6R, 7E, 9R)-3, 9-dihydroxy-4, elaphoside A (7), ptelatoside-A (8), n-butyl-a-β-D-fructofuranoside (9), dibutylphthalate(10)based on physical and chemical properties. Conclusion::All compounds were obtained from C. sibiricus for the first time. The discovery of these compounds further enriched the chemical constituents of C. sibiricus, and provided experimental and scientific basis for the comprehensive development and utilization of C. sibiricus.

Lead was mobilized in acid silty clay loam paddy soil with potassium dihydrogen phosphate (KDP) amendment.

The immobilization effectiveness between Pb and phosphorus in soil varies with soil types. To clarify the effect of phosphate on the availability of Pb in agricultural soil, a culture experiment with three types of paddy soil was performed with potassium dihydrogen phosphate (KDP) added. EDTA, DGT and in-situ solution extraction methods were used to represent different available Pb content. Results showed that the concentration of EDTA-Pb in HN soil was slightly elevated after exogenous KDP added. The supplement of 300 mg/kg KDP significantly increased the content of soluble Pb in both acid silty clay loam soil and neutral silty loam soil (increased by 104.65% and 65.12%, respectively). However, there was no significant influence of KDP on the concentration of DGT extracted Pb. XANES results showed that Pb(OH)2, PbHPO4, humic acid-Pb and GSH-Pb were the major speciation of Pb in soil colloids. The proportion of Pb(OH)2 and humic acid-bounded Pb in soil colloids were elevated after exogenous KDP added. Our results indicated that there was a mobilization effect of KDP on Pb by increasing the amount of colloidal Pb in soil solution, especially in acid silty clay loam paddy soil. Such colloid-facilitated transport might promote the uptake of Pb in rice and pose a potential threat to human health.

Rhizosphere priming of two near-isogenic wheat lines varying in citrate efflux under different levels of phosphorus supply.

BACKGROUNDS AND AIMS: The rhizosphere priming effect (RPE) has been explained from the perspective of microbial responses to root exudates and nutrient availability. This study introduced a chemical process that could also contribute to RPE: root exudates (organic acid ligands) could liberate mineral-protected carbon (C) in soil for microbial degradation. METHODS: Wheat (Triticum aestivum L.) near-isogenic lines varying in citrate efflux were grown for 6 weeks in a C4 soil supplied with either low (10 µg g-1) or high P (40 µg g-1). Total below-ground CO2 was trapped and partitioned for determination of soil organic C decomposition and RPE using a stable isotopic tracing technique. Mineral dissolution was examined by incubating soil with citric ligand at a series of concentrations. KEY RESULTS: High P increased RPE (81 %), shoot (32 %) and root biomass (57 %), root-derived CO2-C (20 %), microbial biomass C (28 %) and N (100%), soil respiration (20 %) and concentrations of water-extractable P (30 %), Fe (43 %) and Al (190 %), but decreased inorganic N in the rhizosphere. Compared with Egret-Burke, wheat line Egret-Burke TaMATE1B with citrate efflux had lower inorganic N, microbial biomass C (16 %) and N (30 %) in the rhizosphere but greater RPE (18 %), shoot biomass (12 %) and root-derived CO2-C (low P 36 %, high P 13 %). Egret-Burke TaMATE1B also had higher concentrations of water-extractable P, Fe and Al in the rhizosphere, indicating the release of mineral-protected C. In addition, citrate ligand facilitated Fe and Al release from soil, with their concentrations rising with increasing ligand concentration and incubation time. CONCLUSIONS: While high P supply increased microbial growth and RPE possibly due to higher total root exudation, citrate efflux from the root might have facilitated the liberation of mineral-bound C, leading to the higher RPE under Egret-Burke TaMATE1B. Mineral dissolution may be an important process that regulates RPE and should be considered in future RPE research.

Modified Palygorskite Improves Immunity, Antioxidant Ability, Intestinal Morphology, and Barrier Function in Broiler Chickens Fed Naturally Contaminated Diet with Permitted Feed Concentrations of Fusarium Mycotoxins.

This study investigated effects of modified palygorskite (MPal) on immunity, antioxidant capacity, and intestinal barrier integrity in broiler chickens challenged with permitted feed Fusarium mycotoxin concentrations. One-day-old chicks were allocated into three treatments with eight replicates. Chickens in three groups were fed a basal diet with normal corn (control), contaminated diet containing moldy corn, with Fusarium mycotoxins contents in the diets lower than permitted feed mycotoxin concentrations, and the contaminated diet supplemented with 1 g/kg MPal for 42 days, respectively. Compared with control, moldy corn decreased bursa of Fabricius weight, jejunal secreted immunoglobulin A concentration, ileal superoxide dismutase (SOD) activity, jejunal and ileal villus height (VH) and VH/crypt depth (CD) ratio, and jejunal zonula occludens-1 and mucin 2 mRNA abundances at 42 days as well as ileal VH/CD ratio at 21 days; while they increased jejunal malondialdehyde accumulation at 21 and 42 days, jejunal SOD activity at 21 days, and serum diamine oxidase activity at 42 days, which were almost recovered by MPal. Moreover, dietary MPal upregulated ileal claudin-2 mRNA abundance compared with other two groups. The results indicated that MPal addition exerted protective effects on immunity, oxidative status, and intestinal barrier integrity in chickens challenged with permitted feed Fusarium mycotoxins levels.

Anti-MRSA Sesquiterpenes from the Semi-Mangrove Plant Myoporum bontioides A. Gray.

The striking rise of methicillin-resistant Staphylococcus aureus (MRSA) infections has become a serious threat to public health worldwide. In an effort to search for new anti-MRSA agents from natural products, a bioassay-guided phytochemical study was conducted on the semi-mangrove plant Myoporum bontioides A. Gray, which led to the isolation of two new sesquiterpene alkaloids (1 and 2) and six known furanosesquiterpenes (3⁻8). Their structures were elucidated on the basis of extensive analysis of their 1D, 2D NMR and mass spectroscopic data. These two new alkaloids (1 and 2) displayed potent anti-MRSA activity with MIC value of 6.25 µg/mL. This is the first report of sesquiterpene alkaloids from the plants of Myoporum genus and their anti-MRSA activity.

Influence of Humic Acid on Pb Uptake and Accumulation in Tea Plants.

A hydroponic experiment combined with synchronous radiation X-ray fluorescence (SRXRF) analysis was designed to understand the influence of humic acid (HA) in tea plants under lead stress. The results showed that the quantitative relationship (QR) between humic acid and Pb is an important factor affecting the regulation of humic acid with respect to the accumulation of Pb in tea plants. Besides, excess humic acid might stimulate the accumulation of Pb in the root cell wall and transfer to the shoot organs through undifferentiated casparian band structure. This study could provide a theoretical basis for the scientific evaluation of the effect of humic acid on tea uptake and the accumulation of Pb and the practical application of humic acid in reducing Pb pollution in the field.

Effects of different levels of modified palygorskite supplementation on the growth performance, immunity, oxidative status and intestinal integrity and barrier function of broilers.

This experiment was designed to investigate effects of different levels of modified palygorskite (MPal) supplementation on growth performance, immunity, oxidative status and intestinal integrity and barrier function of broilers. A total of 320 1-day-old Arbor Acres broilers were randomly assigned into 5 dietary treatments and fed a basal diet supplemented with 0, 0.25, 0.5, 1 and 2 g/kg MPal, respectively, for a 42-day feeding trial. Treatments quadratically reduced feed/gain ratio (F:G) during 1-21 days and linearly decreased average daily feed intake and F:G during 22-42 days, and linearly and quadratically decreased average daily feed intake and F:G during overall period (p < 0.05, 0.50 g/kg treatment showed the lowest F:G). MPal supplementation increased the contents of 21-day jejunal secretory immunoglobulin A (SIgA) quadratically, and 21-day jejunal immunoglobulin G (IgG), immunoglobulin M (IgM) and 42-day jejunal total superoxide dismutase (T-SOD) activity linearly and quadratically (0.50 g/kg treatment showed the highest immunoglobulin concentration), whereas linearly reduced 21-day ileal SIgA level and 42-day jejunal malondialdehyde (MDA) accumulation and serum diamine oxidase activity, and quadratically decreased 21-day ileal MDA level (p < 0.05). The 42-day jejunal SIgA, IgG and IgM concentrations, and T-SOD activity in jejunum at 21 days and ileum at both 21 days and 42 days were quadratically increased with MPal administration (p < 0.05, 0.50 g/kg treatment showed the highest T-SOD activity). The mucin 2 mRNA abundances in 42-day jejunum and 21-day ileum were quadratically increased with MPal supplementation (p < 0.05). Treatments linearly increased 42-day ileal zonula occludens-1, claudin-3 and jejunal claudin-3 mRNA level, whereas linearly and quadratically increased ileal claudin-2 mRNA level (p < 0.05). In conclusion, MPal supplementation exhibited beneficial effects on growth performance, intestinal immunity, antioxidant capacity and intestinal integrity and barrier function of broiler with its optimum dosage being 0.5 g/kg.

Dietary mannan oligosaccharide improves growth performance, muscle oxidative status, and meat quality in broilers under cyclic heat stress.

This study investigated the effects of dietary mannan oligosaccharide (MOS) supplementation on growth performance, serum corticosterone level, and antioxidant ability, meat quality as well as chemical composition of breast muscle in broilers exposed to cyclic heat stress (HS). 144 one-day-old male broiler chicks (Arbor Acres plus) were randomly allocated to 3 treatments with 6 replicates each. Broilers in the control and HS groups were fed a basal diet, and in the MOS group were given the basal diet supplemented with 1 g/kg MOS for 42 days, respectively. The temperature was maintained 32-33 °C for the first 3 days for all broilers, and it was gradually reduced by 3 °C per week to a final temperature of 20 °C in the control group, whereas it remained unchanged for 8 h and reduced to the same level to the control group for the remaining 16 h daily in the both HS and MOS groups. Compared with the control group, cyclic HS resulted in retarded growth performance and increased serum corticosterone level (P < 0.05). The supplementation of MOS promoted growth performance and reduced serum corticosterone concentration in broilers subjected to cyclic HS (P < 0.05). Cyclic HS increased drip loss48 h, cooking loss, malondialdehyde accumulation, and moisture content, whereas decreased pH24 h value, glutathione peroxidase (GSH-Px) activity, and crude protein content in the breast muscle (P < 0.05). In contrast, dietary MOS supplementation reduced drip loss48 h and malondialdehyde concentration, and increased GSH-Px activity in breast muscle compared with the HS group (P < 0.05). The results indicated that dietary MOS supplementation could improve growth performance, and oxidative status and meat quality of breast muscle in broilers under cyclic HS.

Elevated and super-elevated CO2 differ in their interactive effects with nitrogen availability on fruit yield and quality of cucumber.

BACKGROUND: Elevated carbon dioxide (CO2 ) and nitrogen (N) availability can interactively promote cucumber yield, but how the yield increase is realized remains unclear, whilst the interactive effects on fruit quality are unknown. In this study, cucumber plants (Cucumis sativus L. cv. Jinmei No. 3) were grown in a paddy soil under three CO2 concentrations - 400 (ambient CO2 ), 800 (elevated CO2 , eCO2 ) and 1200 µmol mol-1 (super-elevated CO2 ) - and two N applications - 0.06 (low N) and 0.24 g N kg-1 soil (high N). RESULTS: Compared with ambient CO2 , eCO2 increased yield by 106% in high N but the increase in total biomass was only 33%. This can result from greater carbon translocation to fruits from other organs, indicated by the increased biomass allocation from stems and leaves, particularly source leaves, to fruits and the decreased concentrations of fructose and glucose in source leaves. Super-elevated CO2 reduced the carbon allocation to fruits thus yield increase (71%). Additionally, eCO2 also increased the concentrations of fructose and glucose in fruits, maintained the concentrations of dietary fiber, phosphorus, potassium, calcium, magnesium, sulfur, manganese, copper, molybdenum and sodium, whilst it decreased the concentrations of nitrate, protein, iron, and zinc in high N. Compared with eCO2 , super-elevated CO2 can still improve the fruit quality to some extent in low N availability. CONCLUSIONS: Elevated CO2 promotes cucumber yield largely by carbon allocation from source leaves to fruits in high N availability. Besides a dilution effect, carbon allocation to fruits, carbohydrate transformation, and nutrient uptake and assimilation can affect the fruit quality. © 2018 Society of Chemical Industry.

Effect of percutaneous electrical nerve stimulation for the treatment of migraine.

BACKGROUND: This study aimed to assess the effectiveness and safety of percutaneous electrical nerve stimulation (PENS) in migraine treatment. METHODS: Sixty-two patients with at least 2 migration attacks each month were recruited and randomly divided into a verum PENS group and a sham PENS group in a ratio of 1:1. All patients received verum or sham PENS 30 minutes daily, 5 times weekly for 12 weeks. The primary outcomes were change in monthly migraine days (MMD) and the 50% responder rate (RR). Secondary outcomes were evaluated using the monthly migraine attacks (MMA), monthly headache days (MHD), and monthly acute antimigraine drug intake (MAADI). All outcome measurements were performed at treatment initiation to establish a baseline and again after 12 weeks of treatment. RESULTS: At the end of the 12 weeks, the group receiving verum PENS exhibited statistically significant decrease in the mean MMD compared with the group receiving sham PENS intervention (P < .05). Additionally, the 50% RR was significantly higher in the verum PENS group than that in the sham PENS group (P < .05). Furthermore, the MMA, MHD, and MAADI were also significantly lower in the verum PENS group that those in the sham PENS group (P < .05). CONCLUSION: The results of this study demonstrated that verum PENS is more effective and safe than Sham PENS for the treatment of migraine.

Phenolics from Mikania micrantha and Their Antioxidant Activity.

A phytochemical study on the aerial parts of Mikania micrantha led to the isolation of two new phenolic compounds, benzyl 5-O-ß-d-glucopyranosyl-2,5-dihydroxybenzoate (1) and (7S,8R)-threo-dihydroxydehydrodiconiferyl alcohol 9-acetate (2), together with twelve known compounds, benzyl 2-O-ß-d-glucopyranosyl-2,6-dihydroxybenzoate (3), 4-allyl-2,6-dimethoxyphenol glucoside (4), (+)-isolariciresinol (5), icariol A2 (6), 9,10-dihydroxythymol (7), 8,9,10-trihydroxythymol (8), caffeic acid (9), p-coumaric acid (10), ethyl protocatechuate (11), procatechuic aldehyde (12), 4-hydroxybenzoic acid (13), and hydroquinone (14). Their structures were elucidated on the basis of extensive spectroscopic analysis. Except 8 and 9, all the other compounds were isolated from this plant species for the first time. The antioxidant activity of those isolated compounds were evaluated using three different assays. Compounds 1, 2, 3, 9, 10, 13, and 14 demonstrated significant 2,2'-azinobis-(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) free radical cation scavenging activity ranging from SC50 0.31 to 4.86 µM, which were more potent than l-ascorbic acid (SC50 = 10.48 µM). Compounds 5, 9, 11, and 12 exhibited more potent 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity (SC50 = 16.24-21.67 µM) than l-ascorbic acid (39.48 µM). Moreover, the ferric reducing antioxidant power (FRAP) of compounds 2, 5, 9, and 11 were discovered to be also comparable to or even more potent than l-ascorbic acid.

Two New Thymol Derivatives from the Roots of Ageratina adenophora.

Two new thymol derivatives, 7,9-diisobutyryloxy-8-ethoxythymol (1) and 7-acetoxy-8-methoxy-9-isobutyryloxythymol (2), were isolated from fresh roots of Ageratina adenophora, together with four known compounds, 7,9-di-isobutyryloxy-8-methoxythymol (3), 9-oxoageraphorone (4), (-)-isochaminic acid (5) and (1α,6α)-10-hydroxycar-3-ene-2-one (6). Their structures were established on the basis of detailed spectroscopic analysis, and they were all isolated from the roots of A. adenophora for the first time. All the compounds were tested for their in vitro antibacterial activity toward three Gram-positive and two Gram-negative bacterial strains. Thymol derivatives 1-3 only selectively showed slight in vitro bacteriostatic activity toward three Gram-positive bacteria. The two known carene-type monoterpenes 5 and 6 were found to show moderate in vitro antibacterial activity against all five tested bacterial strains, with MIC values from 15.6 to 62.5 µg/mL. In addition, compounds 5 and 6 were further revealed to show in vitro cytotoxicity against human tumor A549, HeLa and HepG2 cell lines, with IC50 values ranging from 18.36 to 41.87 µM. However, their cytotoxic activities were inferior to those of reference compound adriamycin.

Opposite Effects of Two-Derived Antioxidants from Physalis pubescens L. on Hepatocellular Carcinoma Cell Line Malhavu.

Physalis pubescens L. (P. pubescens) is an edible plant used in folk medicine in China. There is traditional, but not scientific, evidence for the anti-tumour effects of P. pubescens. This study aimed to identify whether, or not, antioxidants rich in phenols and flavonoids from fruits and calyxes of P. pubescens can be the candidates for further development of an anti-hepatoma fraction, and if such biological effects coupled with reactive oxygen species (ROS) changes, can provide a direction for subsequent biological action. The effects of calyx-origin (or fruit-origin) total phenol and flavonoid (CTPF or FTPF) from P. pubescens on Malhavu cell viability were evaluated by using a counting-kit-8 (CCK-8) method. Morphological characterisation of cells was undertaken and the structures were photographed (200 × magnification) using Hoechst 3348 staining after exposure to different concentrations of CTPF or FTPF. Induced-apoptosis activity was determined using flow cytometry (FC) after Annexin VFITC/ PI staining. The corresponding ROS changes in Malhavu cells were observed and quantified by the uploading of 2', 7'-dichlorofluorescin diacetate (DCFH-DA). Anti-oxidation was evaluated by a cellular oxidation-stress model and chemical assessments for DPPH, hydroxyl radial, super-oxide radicals, and reducing power. Result shows that CTPF led to significant anti-proliferation in a time- and dosedependent manner. However, FTPF promoted cell viability at 100-1000 µg/mL with a dose-response manner in 24 h. With the extension of exposure time to 48 h, the cell viability did not increase with the growth of FTPF. Morphological characterisation and FC assay both demonstrated that CTPF, and not FTPF possessed induced-apoptotic activity. CTPF potentially induced cell apoptosis by promoting oxidative stress. FTPF indicated pro-oxidation at a concentration of 10 µg/mL and anti-oxidation capabilities at higher concentrations. ROS scavenging assay by oxidation-stress model indicated that CTPF (10 - 400 µg/mL) had ROS inhibitory capacity (R2 = 0.5156, p < 0.0001). FTPF (10 - 100 µg/mL) boosted the level of ROS (p < 0.0001) and inhibited the generation of ROS at 100-400 µg/mL (R2 = 0.5951, p < 0.0001). CTPF is a potential candidate requiring further exploration for the development of antihepatoma ingredients. The down-regulation of cell viability was related to production and reduction of cellular ROS.

[Chemical Constituents from Sphagneticola trilobata].

OBJECTIVE: To study the chemical constituents of the whole plant of Sphagneticola trilobata. METHODS: The compounds were isolated and purified by column chromatography and their structures were determined by spectroscopic techniques. RESULTS: Three lignans, two indolics and two phenolic glycosides were isolated from the whole plant of Sphagneticola trilobata and identified as syringaresinol-4-O-ß-D-glucopyranoside(1), pinoresinol-4-sulfate(2), pinoresinol-4-O-ß-D-glucopyranoside(3), 1H-indole-3-carboxylic acid (4), 1H-indole-3-carbaldehyde(5), 2,6-dimethoxy-4-hydroxyphenol-1-O-ß-D-glucopyranoside (6), and 3,5-dimethoxy-4-hydroxyphenol-1-O-ß-D-glucopyranoside (7). CONCLUSION: Compounds 1 - 7 are isolated from the genus Wedelia for the first time. Compound 4 demonstrates significant inhibitory activity against α-glucosidase.

Antibacterial oleanane-type triterpenoids from pericarps of Akebia trifoliata.

Three new oleanane triterpenoids, 2α,3ß,29-trihydroxyolean-12-en-28-oic acid (1), 2α,3ß-dihydroxy-23-oxo-olean-12-en-28-oic acid (2) and 2α,3ß,21ß,22α-tetrahydroxyolean-12-en-28,29-dioic acid (3), and ten known ones, maslinic acid (4), arjunolic acid (5), oleanolic acid (6), 3-epi-oleanolic acid (7), stachlic acid A (8), serratagenic acid (9), gypsogenic acid (10), 2α,3ß-dihydroxyol-ean-13(18)-en-28-oic acid (11), mesembryanthemoidigenic acid (12) and 12α-hydroxy-δ-lactone (13), were isolated from the pericarps of Akebia trifoliata, a new valued fruit crop in China. Their structures were elucidated on the basis of extensive spectroscopic analysis. Compounds 8, 10, 11 and 13 were isolated for the first time from the genus Akebia. All the compounds were tested for their antimicrobial activity against five bacterial strains. Compounds 4, 6 and 11 showed significant antibacterial activity toward all the assayed microorganisms with MIC values ranging from 0.9 to 15.6µg/mL, which were close or even more potent than the reference compound Kanamycin (MIC values ranging from 1.9 to 3.9µg/mL).