Anti-inflammatory,cyclooxygenase (COX)-2, COX-1 inhibitory and antioxidant effects of Dysophylla stellata Benth.

The n-hexane and ethyl acetate extracts of whole plants of Dysophylla stellata significantly inhibited edema when applied topically at doses of 0.5 and 1 mg/ear in TPA-induced ear edema assay in mice. Further, both the extracts were evaluated for COX-1 and COX-2 inhibitory activities and showed 85.42 and 57.38%; and 71.79 and 89.27% inhibition at 50 µg/ml, respectively. Chromones (1 and 2) present in these extracts could be responsible for their COX-1 and COX-2 inhibitory and anti-inflammatory activities. The ethyl acetate extract showed antioxidant activity in DPPH and ABTS radical scavenging assay where as n-hexane extract found to be inactive.     

Reactive oxygen species scavenging activities and inhibition on DNA oxidative damage of dimeric compounds from the oxidation of (−)-epigallocatechin-3-O-gallate

The dimeric catechins dehydrotheasinensin A (2) and theacitrin C (3) were prepared from the oxidation of (−)-epigallocatechin-3-O-gallate (EGCG, 1), and their antioxidant activity was investigated using a chemiluminescence (CL) method in vitro. Both compounds showed significant inhibitory effects on reactive oxygen species (O₂⁻, H₂O₂ and •OH) and DNA oxidative damage, with 2 being more potent than 3 and EGCG itself.     

Na2SO4胁迫对沙枣幼苗生长和光合生理的影响

采用盆栽控制试验,研究了不同浓度(0、60、120和180 mmol·L-1)Na2SO4胁迫对沙枣幼苗生长和光合特性的影响。结果表明:(1)盐胁迫对沙枣幼苗生长具有显著的抑制效应。不同浓度Na2SO4胁迫沙枣的株高、侧枝数、总叶面积、单株叶片数、比叶面积以及各组织(除根)生物量均显著低于对照,且均随盐胁迫浓度的升高呈下降趋势,而根冠比值则由对照的0.153 1显著增加到180 mmol·L-1Na2SO4胁迫幼苗的0.348 7。(2)盐胁迫显著降低了沙枣幼苗的光合能力。随着Na2SO4胁迫的加剧,净光合速率(Pn)、气孔导度(Gs)、胞间CO2浓度(Ci)和蒸腾速率(Tr)均呈下降的趋势,而气孔限制值(Ls)和水分利用效率(WUE)则依次增加,且Pn下降主要受气孔限制;180 mmol·L-1Na2SO4胁迫沙枣幼苗的Pn、Gs、Ci和Tr分别为对照的71.57%、30.85%、67.15%和51.65%,而Ls和WUE则分别为对照的1.91、1.38倍。(3)盐胁迫强度与幼苗株高、总叶面积、单株叶片数、比叶面积、茎生物量、叶生物量、总生物量等生长指标以及Pn、Gs、Ci、Tr等光合参数呈极显著负相关,叶片的光合参数与总叶面积、单株叶片数呈显著或极显著正相关,而叶片的生长指标、光合参数与幼苗的株高生长和生物量累积也呈显著或极显著正相关。     

Effects of soil moisture and temperature on CH4 oxidation and N2O emission of forest soil

Soil samples were taken from depth of 0–12 cm in the virgin broad-leaved/Korean pine mixed forest in Changbai Mountain in April, 2000. 20 μL·L⁻¹ and 200 μL·L⁻¹ CH₄ and N₂O concentration were supplied for analysis. Laboratory study on CH₄ oxidation and N₂O emission in forest soil showed that fresh soil sample could oxidize atmospheric methane and product N₂O. Air-dried soil sample could not oxidize atmospheric methane, but could product N₂O. However, it could oxidize the supplied methane quickly when its concentration was higher than 20 μL·L⁻¹. The oxidation rate of methane was increased with its initial concentration. An addition of water to dry soil caused large pulse of N₂O emissions within 2 hours. There were curvilinear correlations between N₂O emission and temperature (r²=0.706, p<0.05), and between N₂O emission and water content (r²=0.2968, p <0.05). These suggested temperature and water content were important factors controlling N₂O emission. The correlation between CH₄ oxidization and temperature was also found while CH₄ was supplied 200 μL·L⁻¹ (r²=0.3573, p<0.05). Temperature was an important factor controlling CH₄ oxidation. However, when 20 μL·L⁻¹ CH₄ was supplied, there was no correlation among CH₄ oxidization, N₂O emission, temperature and water content. Foundation item: This paper was supported by Chinese Academy of Sciences. Biography: ZHANG Xiu-jun (1960-), female, Ph. Doctor, lecture in Laboratory of Ecological Process of Trace Substance in Terrestrial Ecosystem, Institute of Applied Ecology, Chinese Academy of Sciences, Shenyang 110015, P.R. China. Responsible editor: Song Funan     

Anti-inflammatory, cyclooxygenase inhibitory and antioxidant activities of standardized extracts of Tridax procumbens L.

The standardized EtOAc, MeOH and 70% EtOH extracts of Tridax procumbens aerial parts showed significant inhibition of rat paw edema at a medium dose of 200 mg/kg and the EtOAC extract was the most active. These extracts were standardized by HPLC with the help of chemical markers. Further, the extracts were evaluated for COX-1 and COX-2 inhibitory activity and EtOAc extract exhibited the highest inhibition of COX-1 and COX-2 at 50 μg/mL. Cent aurein, centaureidin and bergenin were isolated as COX-1 and COX-2 inhibitory principles from the EtOAc extract. The extracts also exhibited antioxidant activity against DPPH and ABTS free radicals. The anti-inflammatory activity of T. procumbens aerial parts could be at least in part due to COX-1, COX-2 enzyme inhibition and free radical-scavenging activities which may be attributed to the presence of flavonoids and other polyphenols in the extracts.     

Cytochrome P450 1 enzyme inhibition and anticancer potential of chromene amides from Amyris plumieri

Cytochrome P450 (CYP) enzyme inhibitory properties of six chromenylated amide compounds (CAs) from Amyris plumieri are described. Inhibition of CYP microsomes (CYP1A1, CYP1A2, CYP1B1, CYP2D6, CYP3A4 and CYP2C19) was monitored using a fluorescent assay. Potent inhibition was found against CYP1A1 with IC₅₀ and K_i for CA1 (acetamide), being the lowest at 1.547 ± 1.0 μM and 0.37 μM respectively, displaying non-competitive kinetics. The selectivity for CYP1A1 was increased in CA3 (butanamide), which also exhibited cytotoxicity against breast cancer cells, MCF7 with an IC₅₀ of 47.46 ± 1.62 μM. Structure-activity relationship studies provide insight at a molecular level for CAs with implications in chemoprevention and chemotherapy.     

HPLC-based activity profiling of Angelica pubescens roots for new positive GABAA receptor modulators in Xenopus oocytes

A petroleum ether extract of the traditional Chinese herbal drug Duhuo (roots of Angelica pubescens Maxim. f. biserrata Shan et Yuan), showed significant activity in a functional two-microelectrode voltage clamp assay with Xenopus oocytes which expressed recombinant γ-aminobutyric acid type A (GABA_A) receptors of the subtype α₁β₂γ_2S. HPLC-based activity profiling of the active extract revealed six compounds responsible for the GABA_A receptor modulating activity. They were identified by microprobe NMR and high resolution mass spectrometry as columbianetin acetate (1), imperatorin (3), cnidilin (4), osthol (5), and columbianedin (6). In concentration-dependent experiments, osthol and cnidilin showed the highest potentiation of the GABA induced chloride current (273.6% ± 39.4% and 204.5% ± 33.2%, respectively at 300 μM). Bisabolangelone (2) only showed minor activity at the GABA_A receptor. The example demonstrates that HPLC-based activity profiling is a simple and efficient method to rapidly identify GABA_A receptor modulators in a bioactive plant extract.     

Two new amide alkaloids with anti-leukaemia activities from Aconitum taipeicum

Two new amide alkaloids, named 3-isopropyl-tetrahydropyrrolo [1,2-a] pyrimidine-2,4(1H,3H)-dione (1) and 1-acetyl-2,3,6-triisopropyl-tetrahydropyrimidin-4(1H)-one (2), were isolated from the roots of Aconitum taipeicum. Their chemical structures were characterized on the basis of MS, 1D- and 2D NMR. The anti-leukaemia activities of the compounds were also tested. The results indicated that the compounds exhibited more significant cell growth inhibitory activities against HL-60 cells than adriamycin, with the IC₅₀ of 1.1 ± 0.03 μg/mL and 1.6 ± 0.07 μg/mL respectively. In addition, two compounds showed anti-tumor activities against K562 cells as well.     

Factors controlling N2O and CH4 fluxes in mixed broad-leaved/Korean pine forest of Changbai Mountain, China

Using the closed chamber technique, thein situ measurements of N₂O and CH₄ fluxes was conducted in a broad-leaved Korean pine mixed forest ecosystem in Changbai Mountain, China, from June 1994 to October 1995. The relationships between fluxes (N₂O and CH₄) and some major environmental factors (temperature, soil water content and soil available nitrogen) were studied. A significant positive correlation between N₂O emission and air/soil temperature was observed, but no significant correlation was found between N₂O emission and soil water content (SWC). This result showed that temperature was an important controlling factor of N₂O flux. There was a significant correlation between CH₄ uptake and SWC, but no significant correlation was found between CH₄ uptake and temperature. This suggested SWC was an important factor controlling CH₄ uptake. The very significant negative correlation between logarithmic N₂O flux and soil nitrate concentration, significant negative correlation between CH₄ flux and soil ammonium content were also found. This project is supported by Chinese Academy of Sciences Responsible editor: Chai Ruihai     

赤霉素GA_(4+7)处理下白桦无性系生长及差异基因表达分析

[目的]为研究赤霉素GA4+7对白桦生长的调控机制。[方法]试验利用1个白桦无性系的分株材料,连续2年分别叶面喷施浓度为0.2 g·L~(-1)(T1)、0.4 g·L~(-1)(T2)的GA4+7溶液,对实验苗木的生长情况进行跟踪调查,并对相应顶端生长组织进行转录组测序和差异基因分析。[结果]对2个年份的苗高、地径等性状分析发现,不同处理间苗高与地径的差异均达到显著或极显著水平,GA4+7对高生长有明显的促进作用,2年后的T2白桦苗高较CK提高了19.65%。于6月28日取GA4+7连续处理2年的白桦顶芽开展RNA-seq分析,结果显示:0.4 g·L~(-1)GA4+7(T2)处理与对照(CK)间的差异基因数量最多,即上调表达的基因有181个,下调表达的基因有55个,这些差异基因在叶绿体类囊体膜、红光、远红光及蓝光的细胞响应等方面富集明显。Pathway富集分析显示:氧化磷酸化途径与光合途径中的8条基因呈上调表达,认为施加0.4 g·L~(-1)GA4+7处理后,上述基因的上调表达加快电子传递进程、催化ATP的合成,从而促进白桦光合作用增强,提高苗期生长量。[结论]对白桦外源施加赤霉素GA4+7后,可上调氧化磷酸化途径和光合途径相关基因的表达,进而促进苗木的高和地径生长。研究结果可为白桦生长相关途径基因的克隆提供参考。     

Neuroprotective activity of galloylated cyanogenic glucosides and hydrolysable tannins isolated from leaves of Phyllagathis rotundifolia

The galloylated cyanogenic glucosides based on prunasin (1-7), gallotannins (8-14), ellagitannins (15-17), ellagic acid derivatives (18, 19) and gallic acid (20) isolated from the leaves of Phyllagathis rotundifolia (Melastomataceae) were investigated for their neuroprotective activity against hydrogen peroxide (H₂O₂)-induced oxidative damage in NG108-15 hybridoma cell line. Among these compounds, the gallotannins and ellagitannins exhibited remarkable neuroprotective activities against oxidative damage in vitro as compared to galloylated cyanogenic glucosides and ellagic acid derivatives in a dose-dependent manner. They could be explored further as potential natural neuroprotectors in various remedies of neurodegenerative diseases.     

C2H2-reduction byErythrina poeppigiana in a Costa Rican coffee plantation

Acetylene reduction activity by root nodules of the legumeErythrina poeppigiana, growing as shade tree in a Costa Rican coffee plantation, was estimated. The mean activity found was 15.7 nmole C₂H₄ · mg (dry weight)^–1 · h^–1. Root nodules collected at different distances from theErythrina stem showed the same activity per dry weight unit. However, as the biomass of the nodules was highest near the stem, was the acetylene reduction activity (expressed per soil volume) maximal near theErythrina stem and declined with distance.     

Flavonols attenuate the immediate and late-phase asthmatic responses to aerosolized-ovalbumin exposure in the conscious guinea pig

We previously reported that quercetin and rutin have potent, anti-asthmatic activity, but the structure-activity relationships of flavonoids and anti-asthmatic agents are still poorly understood. In the current study, the effects of kaempferol, fisetin, and morin on the immediate-phase response (IAR) and late-phase response (LAR) caused by exposure to aerosolized-ovalbumin (OA) in OA-sensitized guinea pigs were evaluated by determining the specific airway resistance (sRaw), recruitment of leukocytes and chemical mediators in bronchoalveolar lavage fluid (BALF), histopathological surveys, and determination of neutrophil chemotaxis. Fisetin and kaempherol (30 mg/kg, p.o.) significantly (P < 0.01) inhibited sRaw by 47.93% and 30.05% in IAR, and 54.45% and 40.50% in LAR, when compared to vehicle control, respectively. Furthermore, all three studied flavonols (30 mg/kg, p.o.) significantly (P < 0.05) inhibited the recruitment of total, as well as subtypes of, leukocytes into the lung BALF. This recruitment inhibition corresponded to the inhibition of leukocyte infiltration, particularly of eosinophils and neutrophils, into the lung in pathological surveys and formly-methionyl-leucyl-phenylalanine (FMLP)-induced neutrophil chemotaxis studies. Kaempferol inhibited FMLP-induced neutrophil chemotaxis in a concentration-dependent manner in a tested range of 1–100 μM. Fisetin inhibited histamine content and peroxidase (EPO) activity in BALF in a dose-dependent manner. All three tested flavonols significantly (P < 0.01) inhibited histamine content at 10 mg/kg, and phospholipase A₂ (PLA₂) and EPO activities at 30 mg/kg (p.o.) in BALF. Kaempherol had a greater anti-asthmatic effect than other flavonols. Fisetin demonstrated the greatest inhibition of sRaw, whereas morin had lesser effects. These results indicate that the lower the molecular weight, the greater the anti-asthmatic activities of these compounds.     

Transdermal behaviors comparisons among Evodia rutaecarpa extracts with different purity of evodiamine and rutaecarpine and the effect of topical formulation in vivo

Aim

Evodiamine (EVO) and rutaecapine (RUT), the major active components from Evodia rutaecarpa extract (EE), are recognized as a depended analgesic agent. This study was designed to investigate the effect of purity and chemical enhancers on the transdermal behavior of EVO and RUT, and the pharmacological effect of their topical cream in vivo.

Material and methods

Transdermal delivery across a full thickness pig abdominal skin was detected in vitro by Franz-type diffusion cell, with HPLC for quantification of the permeation of EVO and RUT. The activity of topical cream in vivo was evaluated by a mice pain model induced by formalin and hot plate.

Results

Transdermal characters of EVO and RUT showed a low transdermal rate, long lag time and low cumulative amount. The transdermal rate and cumulative amount could be promoted by lipophilic enhancers, whereas lag time was shortened by hydrophilic surfactant, but these permeation parameters were not markedly influenced by purity of EE (p > 0.05). The effect in vivo was confirmed by analgesic models in topical cream of EE, which produced a significant (p < 0.05) inhibitory effects on pain response in dose-dependent manner.

Conclusion

The purity of EVO and RUT from EE has no significant effect on their permeation through porcine skin, but oleic acid or nerolidol can markedly elevate the transdermal rate of EVO and RUT. High purity of EE is the best choice for topical preparation to increase the drug loading. The effect of EE in vivo is verified by formalin model and hot plate test.     

Soil–atmosphere CO2, CH4 and N2O fluxes in boreal forestry-drained peatlands

Greenhouse gas emissions from managed peatlands are annually reported to the UNFCCC. For the estimation of greenhouse gas (GHG) balances on a country-wide basis, it is necessary to know how soil–atmosphere fluxes are associated with variables that are available for spatial upscaling. We measured momentary soil–atmosphere CO₂ (heterotrophic and total soil respiration), CH₄ and N₂O fluxes at 68 forestry-drained peatland sites in Finland over two growing seasons. We estimated annual CO₂ effluxes for the sites using site-specific temperature regressions and simulations in half-hourly time steps. Annual CH₄ and N₂O fluxes were interpolated from the measurements. We then tested how well climate and site variables derived from forest inventory results and weather statistics could be used to explain between-site variation in the annual fluxes. The estimated annual CO₂ effluxes ranged from 1165 to 4437 g m⁻² year⁻¹ (total soil respiration) and from 534 to 2455 g m⁻² year⁻¹ (heterotrophic soil respiration). Means of 95% confidence intervals were ±12% of total and ±22% of heterotrophic soil respiration. Estimated annual CO₂ efflux was strongly correlated with soil respiration at the reference temperature (10 °C) and with summer mean air temperature. Temperature sensitivity had little effect on the estimated annual fluxes. Models with tree stand stem volume, site type and summer mean air temperature as independent variables explained 56% of total and 57% of heterotrophic annual CO₂ effluxes. Adding summer mean water table depth to the models raised the explanatory power to 66% and 64% respectively. Most of the sites were small CH₄ sinks and N₂O sources. The interpolated annual CH₄ flux (range: −0.97 to 12.50 g m⁻² year⁻¹) was best explained by summer mean water table depth (r² = 64%) and rather weakly by tree stand stem volume (r² = 22%) and mire vegetation cover (r² = 15%). N₂O flux (range: −0.03 to 0.92 g m⁻² year⁻¹) was best explained by peat CN ratio (r² = 35%). Site type explained 13% of annual N₂O flux. We suggest that water table depth should be measured in national land-use inventories for improving the estimation of country-level GHG fluxes for peatlands.     

Pharmacological mechanisms of black cohosh in Sprague-Dawley rats

Background

Studies indicate that extracts and purified components from black cohosh inhibit the growth of human breast cancer cells, but the molecular targets and signaling pathways have not yet been defined.

Purpose

This study examines the pharmacological mechanisms and toxicological effects in the short term of the herb black cohosh on female Sprague–Dawley rats.

Materials and methods

To assess effects on gene activity and lipid content, we treated female Sprague–Dawley rats with an extract of black cohosh enriched in triterpene glycosides (27%) at 35.7 or 0 mg/kg. Four animals for each group were sacrificed at 1, 6 and 24 h after treatment; liver tissue and serum samples were obtained for gene expression and lipid analysis.

Results

Microarray analysis of rat liver tissue indicated that black cohosh markedly downregulated mitochondrial oxidative phosphorylation genes. Phospholipid biosynthesis and remodeling, PI3-Kinase and sphingosine signaling were upregulated, driven largely by an upregulation of several isoforms of phospholipase C. Hierarchical clustering indicated that black cohosh clustered with antiproliferative compounds, specifically tubulin binding vinca alkaloids and DNA alkylators. In support of this, black cohosh repressed the expression of cyclin D1 and ID3, and inhibited the proliferation of HepG2, p53 positive, liver cancer cells. Black cohosh reduced the level of free fatty acids at 6 and 24 h and triglycerides at 6 h in the serum, but increased the free fatty acid and triglyceride content of the treated livers at 24 h.

Conclusion

Our results suggest that black cohosh warrants further study for breast cancer prevention and therapy.     

Bioactive flavones and biflavones from Selaginella moellendorffii Hieron

Three new flavones named 5-carboxymethyl-4′,7-dihydroxyflavone (1), its ethyl ester (2) and butyl ester (3) were isolated from the herb Selaginella moellendorffii Hieron., together with ten known compounds. Their structures were elucidated on the basis of spectroscopic and chemical analysis. Selected compounds were evaluated for their anti-HBV and cytotoxic activity. Among them, compounds 2 and 3 displayed inhibitory activity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the Hep G2.2.15 cell line with IC₅₀ values of 0.17 mg/ml and 0.46 mg/ml, and on HBV e antigen (HBeAg) secretion with IC₅₀ values of 0.42 mg/ml and 0.42 mg/ml, respectively. Compounds 7, 8, 10 and 12 exhibited selective cytotoxicity against the three human cancer cell lines tested.     

A new seco-friedelolactone acid from the bark and twigs of Itoa orientalis

A new seco-friedelolactone, named itoaic acid, together with 5 known compounds was isolated from the bark and twigs of Itoa orientalis. The structure was elucidated by means of MS, 1D and 2D NMR techniques. Anti-inflammatory activity against COX-2 was evaluated for several compounds from I. orientalis and another Flacourtiaceae plant Xylosma controversum.     

Intestinal absorption of forsythoside A in different compositions of Shuang-Huang-Lian

Shuang-Huang-Lian (SHL), a traditional Chinese formula containing Lonicerae japonicae flos (LJF), Scutellariae radix (SR) and Forsythiae fructus (FF), is commonly used to treat acute upper respiratory tract infection, acute bronchitis and light pneumonia. Forsythoside A is one of the main active ingredients in Forsythiae fructus, a key herb in SHL. In the present study, effects of different compositions in SHL on the intestinal absorption of forsythoside A were investigated. The observations from in situ intestinal circulation model showed that A/%(h^− 1) of forsythoside A in FF + LSF, FF + SR and SHL were all reduced greatly compared with that in FF. However, in pharmacokinetics study, C_max and AUC_0 → 1440 of forsythoside A all increased and T_1/2 prolonged in SHL, FF + LJF and FF + SR compared with FF. The results indicated that the different compositions of SHL decreased absorption but increased bioavailability of forsythoside A, which may be related to its metabolism inhibited in intestine or liver.     

Identification of non-alkaloid acetylcholinesterase inhibitors from Ferulago campestris (Besser) Grecescu (Apiaceae)

Inhibition of Acetylcholinesterase (AChE) is still considered as a strategy for the treatment of neurological disorders such as Alzheimer's disease. Many plant derived alkaloids (such as galantamine and rivastigmine) are known for their AChE inhibitory activity. Recently, other classes of natural compounds such as terpenoids, sesquiterpene glycosides and coumarins have been studied as new AChE inhibitors, with the aim to discover less toxic compounds compared to alkaloidal ones. The Ferulago campestris roots dichloromethane extract was used for a bioassay-guided fractionation for the search of AChE inhibitors. Three coumarin derivatives (umbelliprenin 1, coladonin 2 and coladin 3), three daucane ester derivatives (siol anisate 4, ferutinin 5 and 1-acetyl-5-angeloyl lapiferol 6), two phenol derivatives (2-epilaserine 7 and epielmanticine 8) and one polyacetylene (9-epoxyfalcarindiol 9) were isolated by the bioassay-guided approach. Their structures were characterized on the basis of spectral methods (1D and 2D NMR, and MS spectroscopy). All the isolated compounds were able to inhibit the AChE (IC₅₀ 1.2–0.1 mM) although at higher doses if compared to galantamine (6.7 μM) measured in the same conditions. The most active compounds were the daucane derivative siol anisate 4 and the epielmanticine 8, with IC₅₀ of 0.172 and 0.175 mM respectively.