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1.
Thrombin,the ultimate proteinase of the coagulation cascade,is an attractive target for the treatment of a variety of cardiovascular diseases.A bromophenol derivative named (+)-3-(2,3-dibromo-4,5-dihydroxy-phenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroiso-benzofuran 1,isolated from the brown alga Leathesia nana exhibited significant thrombin inhibitory activity.In this study,we investigated the inhibition of human thrombin in vitro with this bromophenol derivative,and its antithrombotic efficacy in vivo using th...  相似文献   

2.
To investigate the antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo, six bromophenol derivatives 6-(2,3-dibromo-4,5-dihydroxybenzyl)-2,3-dibromo-4,5-dihydroxy benzyl methyl ether (1), (+)-3-(2,3-dibromo-4,5-dihydroxyphenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroisobenzofuran (2), 3-bromo-4-(2,3-dibromo-4,5-dihydroxybenzyl)-5-methoxymethyl-pyrocatechol (3), 2,2′,3,3′-tetrabromo-4,4′,5,5′-tetrahydroxy-diphenylmethane (4), bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (5), 2,2′,3-tribromo-3′,4,4′,5-tetrahydroxy-6′-ethyloxymethyldiphenylmethane (6) were isolated from brown alga Leathesia nana, and their cytotoxicity were tested by MTT assays in human cancer cell lines A549, BGC-823, MCF-7, B16-BL6, HT-1080, A2780, Bel7402 and HCT-8. Their inhibitory activity against protein tyrosine kinase (PTK) with over-expression of c-kit was analyzed also by ELISA. The antitumor activity of ethanolic extraction of Leathesia nana (EELN) was evaluated on S180-bearing mice. All compounds showed very potent cytotoxicity against all of the eight cancer cell lines with IC50 below 10 μg/mL. In PTK inhibition study, all bromophenol derivatives showed moderate inhibitory activity and compounds 2, 5 and 6 showed significant bioactivity with the inhibition ratio of 77.5%, 80.1% and 71.4%, respectively. Pharmacological studies reveal that EELN could inhibit the growth of Sarcoma 180 tumor and increase the indices of thymus and spleen to improve the immune system remarkably in vivo. Results indicated that the bromophenol derivatives and EELN can be used as potent antitumor agents for PTK over-expression of c-kit and considered in a new therapeutic strategy for treatment of cancer. Supported by the National High Technology Research and Development Program of China (863 Program, No. 2007AA09Z410) and Knowledge Innovation Program of Chinese Academy of Sciences (No. KZCX2-YW-209)  相似文献   

3.
Plinabulin,a potent microtubule-targeting agent,is derived from marine natural diketopiperazine ‘phenylahistin'.To develop novel plinabulin analogue that could display better pharmacokinetic properties and less side effects,deuterated plinabulin 9 was synthesized and evaluated in vitro and in vivo.In comparison with plinabulin,in vivo pharmacokinetic studies indicated that the deuterated derivative 9 could alter blood circulation behavior obviously,which was proved by increased area under the plasma concentration-time curve(AUC_(0–∞)),reduced clearance(CL),and prolonged total body mean residence time(MRT).The derivative 9 also has higher inhibition rates against Bx PC-3,Jurkat and A-431 tumor cell lines as compared with its prototype plinabulin.Therefore,the deuterated compound 9 might be developed as a potential agent for different cancer treatments.  相似文献   

4.
The antithrombotic and antiplatelet effects of two fucoidan fractions with low molecular weight and different sulfate content from Laminaria japonica were compared in order to examine the influence of chemical character on their antithrombotic activity and the possible mechanism. Both LMW fucoidan fractions exhibited favorable antithrombotic activity in an Fecl3-induced arterial thrombosis. The antithrombotic activity of LMW fucoidan was related with decrease of TXB2 and whole blood viscosity and hematocrit. LMW fucoidan showed a correlation between anticoagulant, antiaggregant and antithrombotic effects in vivo. For LMW fucoidan, antithrombotic activity required high dose of 5-10 nmol kg-1, concomitantly with increase in anticoagulant activity and inhibition of platelet aggregation. Administration of LMW fucoidan significantly promoted the 6-keto-PGF1α content and decreased the TXB2 content, indicating its inhibition of tissue factor pathway and regulation of metabolism of arachidonic acid. By comparison, highly sulfated fucoidan LF2 with Mw 3900 seemed to be a more suitable choice for antithrombotic drug for its antithrombotic activity accompanied with specific inhibitory activity on platelet aggregation, low anticoagulant activity and low hemorrhagic risk in vivo.  相似文献   

5.
Bromophenols are a set of natural products widely distributed in seaweed, most of which exhibit interesting and useful biological activities. To develop a reliable and efficient synthetic route to these natural bromophenols, three of them, 3,4-dibromo-5-(2′-bromo-3′,4′-dihydroxy-6′-methoxymethyl-benzyl)-benzene-1,2-diol (compound 9), 3,4-dibromo-5-(2′-bromo-6′-ethoxy methyl-3′,4′-dihydroxybenzyl)-benzene-1,2-diol (compound 10), and 3-bromo-4-(3′-bromo-4′,5′-dihydroxy benzyl)-5-(ethoxymethyl)-benzene-1,2-diol (compound 14), isolated from red marine algae, have been synthesized in eight steps with an overall yield of 14.4%, 14.4%, and 18.2% respectively, via a practical approach employing bromination, Wolff-Kishner-Huang reduction and a Friedel-Crafts reaction as key steps. The protein tyrosine phosphatase 1B (PTP1B) inhibitory activities of the synthetic compounds were evaluated by the colorimetric assay. The results show that these compounds are moderate PTP1B inhibitors. The synthesis of these bromophenol derivatives makes in vivo studies of their structure-activity relationships and inhibition activity against PTP1B possible.  相似文献   

6.
Hepatitis B virus（HBV） is a significant global pathogen and efficient cure for HBV patients is still a challenging goal. We previously reported that acidic mucopolysaccharide from stichopus japonicus selenka（SJAMP） could inhibit HBs Ag and HBe Ag expression in vitro. However, the potential anti-HBV effects of SJAMP in vivo have not yet been explored. In this study, we show that SJAMP exhibits potent anti-HBV activity in HBV transgenic mice in a dose-dependent manner. Specifically, sixty HBV transgenic male BALB/c mice were randomly selected to receive the treatment of PBS, low dose SJAMP(30 mg kg-1), middle dose SJAMP(40 mg kg-1), high dose SJAMP(50 mg kg-1) and IFN(45 IU kg-1) for 30 d. SJAMP treatment suppressed serum HBV-DNA, and liver HBs Ag and HBc Ag levels in HBV-transgenic mice. The present study highlights the potential application of SJAMP in HBV therapy.  相似文献   

7.
3-bromo-4,5-bis(2,3-dibromo-4,5-dihydroxybenzyl)-1,2-benzenediol (1) is a natural bromophenol isolated from the red algae Rhodomela confervoides that exhibits significant inhibition against protein tyrosine phosphatase 1B (PTP1B). Based on its activity, we synthesized two new synthetic bromophenols and their methoxy derivatives from vanillin using the structure of natural bromophenol 1 as a scaffold. The structures of these bromophenols were elucidated from 1H NMR, 13C NMR, and high resolution electron ionization mass spectrometry as 2,3-dibromo-1-(2p-bromo-6p-(3q,4q-dimethoxybenzyl)- 3p,4p-dimethoxybenzyl)-4,5-dimethoxybenzene(2),2,3-dibromo-1-(2p-bromo-6p-(2q-bromo-4q,5q-dimethoxy-benzyl)-3p,4p-dimethoxybenzyl)-4,5-dimethoxybenzene(3),3,4-dibromo-5-(2p-bromo-6p-(2q-bromo-4q,5q-dihydroxybenzyl)-3p,4p-dihydroxybenzyl)pyrocatechol(4)and 3,4-dibromo-5-(2p-bromo-6p-(3q,4q-dihydroxybenzyl)-3p,4p-dihydroxybenzyl)pyrocatechol (5).PTP1B inhibition activities of these compounds were evaluated using a colorimetric assay,and compounds 3 and 4 demonstrated interesting activity against PTP1B.  相似文献   

8.
Cytarabine(1-β-D-arabinofuranosylcytosine, Ara-C), isolated from a Caribbean sponge species Tethyacrypta, is the first antitumor drug from a marine resource. In 1980, the US Food and Drug Administration approved this drug for the treatment of different types of leukemia. This drug has a short plasma half-life, low stability, limited bioavailability, and severe side effects. To improve stability and bioavailability, we synthesized nine novel derivatives by blocking the cytarabine metabolic sites and improving lipophilicity. The c Log P values of the newly synthesized compounds were calculated. All the synthesized compounds were more lipophilic than cytarabine, resulting in membrane permeability and bioavailability improvement. The antitumor activities against leukemia cell line HL-60 were evaluated by using the MTT assay. The bioassay results revealed that the IC_(50) values of compounds 5, 8 and 9 were 0.080, 0.090 and 0.057 μmol L~(-1), respectively, which was similar with that of cytarabine(0.056 μmol L~(-1),). In comparison, compound 4 with a phosphate group at O5' was inactive. Because phosphoester bonds are easily hydrolyzed by alkaline phosphatase and are commonly used in producing prodrug strategies, compound 4 might also be metabolized in vivo and generate compound 3 or even cytarabine through a multi-step reaction. Thus, compound 4 might be a promising compound to be developed as a prodrug.  相似文献   

9.
The nitrogen （N） input and Spartina alterniflora invasion in the tidal marsh of the southeast of China are increasingly serious. To evaluate CH4 emissions in the tidal marsh as affected by the N inputs and S. alterniflora invasion, we measured CH4 emissions from plots with vegetated S. alterniflora and native Cyperus malaccensis, and fertilized with exogenous N at the rate of 0 （NO）, 21 （N1） and 42 （N2） g N/（m2.yr）, respectively, in the Shanyutan marsh in the Minjiang River estuary, the southeast of China. The average CH4 fluxes during the experiment in the C. malaccensis and S. alterniflora plots without N addition were 3.67 mg CHa/（m2.h） and 7.79 mg CH4/（m2-h）, respectively, suggesting that the invasion of S. alterniflora into the Minjiang River estuary stimulated CH4 emission. Exogenous N had positive effects on CH4 fluxes both in native and in invaded tidal marsh. The mean CH4 fluxes of NI and N2 treat- ments increased by 31.05% and 123.50% in the C. malaccensis marsh, and 63.88% and 7.55% in the S. alterniflora marsh, respectively, compared to that of NO treatment. The CH4 fluxes in the two marshes were positively correlated with temperature and pH, and nega- tively correlated with electrical conductivity and redox potential （Eh） at different N addition treatments. While the relationships between CH4 fluxes and environmental variables （especially soil temperature, pH and Eh at different depths） tended to decrease with N additions. Significant temporal variability in CH4 fluxes were observed as the N was gradually added to the native and invaded marshes. In order to better assess the global climatic role of tidal marshes as affected by N addition, much more attention should be paid to the short-term temporal variability in CH4 emission.  相似文献   

10.
Reference crop evapotranspiration(ET 0) is a key parameter to calculate crop water requirements.In the paper,ET 0 during 1960-2005 was calculated with FAO-56 PM in eastern agricultural areas of Qinghai,China.Then the sensitivity coefficients of ET 0 to meteorological variables were estimated through the nondimensional partial derivative in FAO-56 PM.Results show that the mean annual ET 0 of the whole area is 904 mm,and ET 0 portrays a very significant decrease during the 46 years.In spatial,ET 0 decreases from southeast to northwest,firstly increases then decreases from southwest to northeast.Through sensitivity analysis,in spring the most sensitive variable is relative humidity,while in summer is temperature.The temperature,sunshine duration and wind speed sensitivity coefficients(S(TA),S(n),S(u)) are higher in middle areas as opposed to surrounding areas,while the relative humidity sensitivity coefficient(S(RH)) has an opposite distribution rule.  相似文献   

11.
Chinese cabbage was cultivated in upland soil with the addition of biochar in order to investigate the potential for reduction of greenhouse gas emissions. Barley straw biochar (BSB) was introduced in a Wagner pot (1/5000a) in amounts of 0 (BSB0, control), 100 (BSB100), 300 (BSB300), and 500 (BSB500) kg 10a-1. After the addition of BSB into the upland soil, carbon dioxide (CO2) emission increased while methane (CH4) and nitrous oxide (N2O) emissions decreased. The highest CO2 flux was measured for the BSB500 sample, (84.6 g m-2) followed by BSB300, BSB100, and BSB0 in decreasing order. Relative to those of control, the total CH4 flux and N2O flux for the BSB500 treatment were lower by 31.6% and 26.1%, respectively. The global warming potential (GWP) of the treatment without biochar was 281.4 g CO2 m-2 and those for treatments with biochar were in the range from 194.1 to 224.9 g CO2 m-2. Therefore, introducing BSB into upland soil to cultivate Chinese cabbages can reduce the global warming potential.  相似文献   

12.
Two strains H2-410 and H2-419 were obtained from the chemically mutated survivors of wild Haematococcus pluvialis 2 by using ethyl methanesulphonate (EMS). Strains H2-410 and H2-419 showed a fast cell growth with 13% and 20% increase in biomass compared to wild type, respectively. Then H2-419-4, a fast cell growth and high astaxanthin accumulation strain, was obtained by exposing the strain H2-419 to ultraviolet radiation (UV) further. The total biomass, the astaxanthin content per cell, astaxanthin production of H2-419-4 showed 68%, 28%, and 120% increase compared to wild H. pluvialis 2, respectively. HPLC (High Performance Liquid Chromatography) data showed also an obvious proportional variation of different carotenoid compositions in the extracts of H2-419-4 and the wild type, although no peak of carotenoids appeared or disappeared. Therefore, the main compositions in strain H2-419-4, like its wild one, were free of astaxanthin, monoester, and diester of astaxanthin. The asexual reproduction in survivors after exposed to UV was not synchronous, and different from the normal synchronous asexual reproduction as the mother cells were motile instead of non-motile. Interestingly, some survivors from UV irradiation produced many mini-spores (or gamete?), the spores moved away from the mother cell gradually 4 or 5 days later. This is quite similar to sexual reproduction described by Elliot in 1934. However, whether this was sexual reproduction remains questionable, as no mating process has been observed.  相似文献   

13.
Inorganic lead （Pb） is one of the most common environmental pollutants. Much evidence indicates that Pb exposure could directly affect fish growth and development. In this study, we investigated the cytotoxic effects of Pb on cytoskeletal protein stability at both protein and mRNA level in crucian carp Carassius auratus. Pb（NO3）2 treatment in concentration of 100 μmol/L resulted in decreased expression of both α- and β-tubulin but γ-tubulin as assayed with SDS-PAGE, Western Blot, and ELISA. In vivo and in vitro analyses on protein expression of tubulins are consistent. The effect of Pb on mRNA expression varied among different tissues. Our results suggest that cytotoxicity of Pb at protein translation level is stronger than at mRNA expression level.  相似文献   

14.
To investigate the antitumor effect of bromophenol derivatives in vitro and Leathesia nana extract in vivo, six bromophenol derivatives 6-(2,3-dibromo-4,5-dihydroxybenzyl)-2,3-dibromo-4,5-dihydroxy benzyl methyl ether (1), (+)-3-(2,3-dibromo-4,5-dihydroxyphenyl)-4-bromo-5,6-dihydroxy-1,3-dihydroisobenzofuran (2), 3-bromo-4-(2,3-dibromo-4,5-dihydroxybenzyl)-5-methoxymethyl-pyrocatechol (3),2,2',3,3'-tetrabromo-4,4',5,5'-tetrahydroxy-diphenylmethane (4), bis(2,3-dibromo-4,5-dihydroxybenzyl) ether (5), 2,2',3-tribromo-3',4,4',5-tetrahydroxy-6'-ethyloxymethyldiphenylmethane (6) were isolated from brown alga Leathesia nana, and their cytotoxicity were tested by MTr assays in human cancer cell lines A549, BGC-823, MCF-7, B16-BL6, HT-1080, A2780, Bel7402 and HCT-8. Their inhibitory activity against protein tyrosine kinase (PTK) with over-expression of c-kit was analyzed also by ELISA. The antitumor activity of ethanolic extraction of Leathesia nana (EELN) was evaluated on S180-bearing mice.All compounds showed very potent cytotoxicity against all of the eight cancer cell lines with IC50 below 10 μg/mL. In PTK inhibition study, all bromophenol derivatives showed moderate inhibitory activity and compounds 2, 5 and 6 showed significant bioactivity with the inhibition ratio of 77.5%, 80.1% and 71.4%,respectively. Pharmacological studies reveal that EELN could inhibit the growth of Sarcoma 180 tumor and increase the indices of thymus and spleen to improve the immune system remarkably in vivo. Results indicated that the bromophenoi derivatives and EELN can be used as potent antitumor agents for PTK over-expression of c-kit and considered in a new therapeutic strategy for treatment of cancer.  相似文献   

15.
Measurements of pH,total alkalinity(TA),partial pressure of CO2(pCO2) and air-sea CO2 flux(FCO2) were conducted for the inner continental shelf of the East China Sea(ECS) during August 2011.Variations in pCO2 distribution and FCO2 magnitude during the construction of the Three Gorges Dam(TGD)(2003-2009),and the potential effects of the TGD on the air-sea CO2 exchange were examined.Results showed that the ECS acts as an overall CO2 sink during summer,with pCO2 ranging from 107 to 585 μatm and an average FCO2 of-6.39 mmol/(m2·d).Low pCO2(<350 μatm) levels were observed at the central shelf(28°-32°N,123°-125.5°E) where most CO2-absorption occurred.High pCO2(>420 μatm) levels were found in the Changjiang estuary and Hangzhou Bay which acted as the main CO2 source.A negative relationship between pCO2 and salinity(R2=0.722 0) in the estuary zone indicated the predominant effect of the Changjiang Diluted Water(CDW) on the seawater CO2 system,whereas a positive relationship(R2=0.744 8) in the offshore zone revealed the influence of the Taiwan Current Warm Water(TCWW).Together with the historical data,our results indicated that the CO2 sink has shown a shift southwest while FCO2 exhibited dramatic fluctuation during the construction of the TGD,which is located in the middle reaches of the Changjiang.These variations probably reflect fluctuation in the Changjiang runoff,nutrient import,phytoplankton productivity,and sediment input,which are likely to have been caused by the operations of the TGD.Nevertheless,the potential influence of the TGD on the CO2 flux in the ECS is worthy of further study.  相似文献   

16.
Dung deposition is an important pathway of nutrient return and redistribution in alpine grasslands of the Qinghai-Tibetan Plateau.To date,information on the greenhouse gas emissions of yak dung on alpine grasslands,especially where there are large amounts of rock fragments,is limited.Our aim,therefore,was to evaluate variations in N_2O,CH_4,and CO_2 emissions from yak dung(CCD),and compare it to dung placed on rock fragments(RCD),alpine steppe soil(CSD),and a soil and rock fragment mixture(RSD) over a 30-day incubation period.The results showed that the total N_2O emissions from treatments without soil were significantly(P 0.05) lower than those from treatments with soil.The highest total CH_4 emissions were detected in the CSD treatment,while CH_4 losses from treatments without rock fragments were significantly(P 0.05) greater than those with rock fragments.The total CO_2 emissions from the RSD treatment was 6.30%–12.0% lower than those in the other three treatments.The soil beneath yak dung pats elevated the globalwarming potential(GWP),while the addition of rock fragments to the soil significantly(P 0.05) decreased the GWP by reducing emissions of the three greenhouse gases.We therefore suggest that interactions between rock fragments and alpine steppe soil are effective in decreasing yak dung greenhouse gas emissions.This finding indicates that rock fragments are an effective medium for reducing greenhouse gas emissions from dung pats,and more attention should therefore be paid to evaluate its ecological impact in future studies.These results should help guide scientific assessments of regional GHG budgets in agricultural ecosystems where the addition of livestock manure to soils with large amounts of rock fragments is common.  相似文献   

17.
The aim of this study was to investigate the effects of light intensity and enhanced nitrogen supply on the growth and photosynthesis of the green-tide macroalga, Ulva prolifera. Thalli of U. prolifera were grown in natural or NH 4 +-enriched seawater under two different light intensities for 7 days, and then the growth rate, pigmentation, and photosynthetic performance of the thalli were evaluated. The results show that the relative growth rate(RGR) was markedly higher under the high light level than under the low light level. Enrichment with NH 4 + enhanced the RGR under high light intensity, but did not affect RGR under low light intensity. In low light conditions, NH 4 +-enrichment resulted in a marked decrease in the maximal photosynthetic rate( P m) and the maximum carbon fixation rate( V max), but it did not affect the half saturation constant for carbon( K 0.5) or the ratio of V max to K 0.5, which reflects the carbon acquisition efficiency. In high light conditions, P m, K 0.5, and the dark respiration rate( R d) increased under NH 4 + enrichment, but V max and the V max / K 0.5 ratio decreased. Regardless of the light intensity, NH 4 +-enrichment did not affect the apparent photosynthetic efficiency( α), which refl ects the ability of the alga to use light energy at low light levels. Under both low and high light intensities, the chlorophyll a(Chl a), chlorophyll b(Chl b), and carotenoids(Car) contents in thalli were higher in NH 4 +-enriched than in natural seawater, except that there was a decrease in the Chl b content of thalli in NH 4 +-enriched seawater under low light intensity. Therefore, NH 4 + enrichment improved the growth and photosynthetic performance of U. prolifera under high light intensity, but not under low light intensity. We discuss the possible mechanisms underlying these physiological responses.  相似文献   

18.
Eutrophication, which is the enrichment of a water mass with inorganic and organic nutrients that support plant growth, is a key factor in stimulating phytoplankton growth. In this study, we determined the effects of various nitrogen sources, different nitrogen concentrations in the culture medium, and two culture methods on the growth of the green alga, Enteromorpha prolifera. The relationship between the specific growth rate of E. prolifera and NO3--N concentration was consistent with that estimated using the Monod equation (R2 = 0.9713, P < 0.01). In the NO3--N medium, the maximum specific growth rate was calculated to be 0.1634/d and the semi-saturation constant was calculated to be 16.86 μmol/L. Our results show that E. prolifera can effectively utilize NH4+-N, NO3--N, and NO2--N and urea-N in the range of 5 to 50 μmol/L. NH4+-N was preferentially assimilated by E. prolifera, and urea-N was favorable for long-term growth.  相似文献   

19.
With the global ban on the application of organotin-based marine coatings by the International Maritime Organization, the development of environmentally friendly, low-toxic and nontoxic antifouling compounds for marine industries has become an urgent need. Marine microorganisms have been considered as a potential source of natural antifoulants. In this study, the antifouling potential of marine dinoflagellate Amphidinium carterae, the toxic and red-tide microalgae, was investigated. We performed a series of operations to extract the bioactive substances from Amphidinium carterae and tested their antialgal and antilarval activities. The crude extract of Amphidinium carterae showed significant antialgal activity and the EC50 value against Skeletonema costatum was 55.4 μg mL?1. After purification, the isolated bioactive substances (the organic extract C) exhibited much higher antialgal and antilarval activities with EC50 of 12.9 μg mL?1 against Skeletonema costatum and LC50 of 15.1 μg mL?1 against Amphibalanus amphitrite larvae. Subsequently, IR, Q-TOFMS, and GC-MS were utilized for the structural elucidation of the bioactive compounds, and a series of unsaturated and saturated 16- to 22-carbon fatty acids were detected. The data suggested the bioactive compounds isolated from Amphidinium carterae exhibited a significant inhibiting effect against the diatom Skeletonema costatum and Amphibalanus amphitrite larvae, and could be substitutes for persistent, toxic antifouling compounds.  相似文献   

20.
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