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1.
An extract of Malleastrum sp. (Meliaceae) collected in Madagascar by the Madagascar International Cooperative Biodiversity Group was found to have antimalarial activity, with an IC 50 value between 2.5 and 5 μg ml?1. After purification by liquid‐liquid partition, chromatography on a Diaion open column, C 18 SPE and C 18 reversed phase HPLC , the new butanolide, malleastrumolide A, was isolated. The structure of malleastrumolide A was determined by mass spectrometry, NMR , and ECD . The double bond position was determined by cross‐metathesis and mass spectrometry. The compound has antiproliferative activity against the A2780 ovarian cancer cell line with an IC 50 value of 17.4 μm and antiplasmodial activity against the drug‐resistant Dd2 strain of Plasmodium falciparum with an IC 50 value of 2.74 μm .  相似文献   

2.
SUMMARY.
  • 1 Production of periphyton, nitrogen fixation and processing of leaf litter were examined in an oligotrophic Sierra Nevada stream and the responses of these processes to copper (2.5, 5 and 10μg 1-1 CuT [total filtrable copper]; approximately 12, 25 and 50 ng 1-1 Cu2+) were determined.
  • 2 Autotrophic and total production were estimated from 3-week accumulations of biomass on artificial substrates. Mean autotrophic production in the control ranged from 0.22 to 0.58 mg C m-2 h-1 in summer-autumn 1979, but declined to 0.08–0.28 mg C m 2 h-1 after peak discharge in summer 1980, apparently due to phosphorus-limited growth. Total production in the control ranged from 0.30 to 0.82 mg C m-2 h -1 in summer-autumn 1979 and from 0.16 to 0,68 mg C m -2 h -1 in 1980. Mean autotrophic productivity, estimated by l4C-bicarbonate uptake in daylight, ranged from 0.30 to 2.8 mg C m-2 h-1.
  • 3 Autotrophic productivity was reduced by 57–81% at 2.5μg 1-1 CuT, 55–96% at 5μg 1-1 CuT, and 81–100% at 10μg 1-1 CUT, Heterotrophic productivity (based on dark 35S-sulphate uptake) was inhibited to a lesser extent (28–63% at 2.5μg 1-1 CuT, 24–84% at 5μg 1-1 CuT, and 67–92% at 10μg 1-1 CuT), The inhibition of autotrophic and heterotrophic productivity persisted through the year of exposure. Production in stream sections previously exposed to 2.5 and 5μg 1-1CuT increased to control levels within 4 weeks after dosing, but remained depressed for more than 7 weeks after exposure to 10μg 1-1 CuT.
  • 4 The specific rate of photosynthesis (mg C mg chlorophyll a-1 h-1) of mature periphyton communities declined at all test concentrations of copper, but the rate for periphyton on newly-colonized surfaces did not change. The species composition of benthic algae shifted during exposure to an assemblage more tolerant of copper. Achrtanthes minutissima and Fragilaria crotonensis were the primary replacement species on newly-colonized surfaces.
  • 5 The nitrogenase activity of blue-green algae was low. with controls ranging from 2.4 to 12 nmol C2H2 m-2 h-1. Nitrogenase activity was inhibited during the initial weeks of exposure by 5 and 10μg 1-1 CuT. However, after 9 months of exposure, control and copper-treated sections did not differ.
  • 6 The rate of processing of leaf litter, estimated by microbial respiration and nutrient quality of litter of resident riparian woodland taxa, was inhibited at all test concentrations of copper.
  相似文献   

3.
The synthesized flavonoid derivatives were examined for their antioxidant, anti‐inflammatory, xanthine oxidase (XO), urease inhibitory activity, and cytotoxicity. Except few, all the flavonoids under this study showed significant antioxidant activity (45.6%–85.5%, 32.6%–70.6%, and 24.9%–65.5% inhibition by DPPH, ferric reducing/antioxidant power, and oxygen radical absorption capacity assays) with promising TNF‐α inhibitory activity (42%–73% at 10 μM) and IL‐6 inhibitory activity (54%–81% at 10 μM) compared with that of control dexamethasone. The flavonoids luteolin, apigenin, diosmetin, chrysin, O3?, O7‐dihexyl diosmetin, O4?, O7‐dihexyl apigenin, and O7‐hexyl chrysin, showed an inhibition with IC50 values (4.5‐8.1 μg/mL), more than allopurinol (8.5 μg/mL) at 5 μM against XO and showing more than 50% inhibition at a final concentration (5 mM) with an IC50 value of ranging from 4.8 to 7.2 (μg/mL) in comparison with the positive control thiourea (5.8 μg/mL) for urease inhibition. Thus, the flavonoid derivatives may be considered as potential antioxidant and antigout agents.  相似文献   

4.
Inside-out vesicles (IOV) were prepared from human red blood cells. Steady-state uptake of 22Na was observed to generally follow an exponential time course with a rate constant of 1.57 ± 0.09 h?1 (SE). One week of cold storage (0–4°C) increased the rate constant to 2.50 ± 0.12 h ?1 (SE). Mg2+, Ca2+, or Sr2+ decreased the rate of 22Na uptake with no observable differences between the three divalent cations when tested at concentrations of 50 μM. Mg2+ was shown to decrease the rate of 22Na uptake at concentrations as low as 5 μM with maximal effect at 50 to 100 μM. The decrease in rate of 22Na uptake induced by Mg2+ could be enhanced by exposure of IOV to Mg2+ for longer periods of time. Trypsin treatment of IOV increased the rate of uptake of 22Na and was dependent on the concentration of trypsin added between 5 to 25 μg/ml (treated for 5 min at 25°C). The ability of Mg2+ (50 μM) to decrease the rate of 22Na uptake was still observed after maximal trypsin treatment. Phospholipase A2 or phospholipase C treatment of IOV increased the rate of 22Na uptake and was dependent on the amount of phospholipase A2 (0.1 to 1.0 units/ml) or phospholipase C (0.25 to 2.5 units/ml) added (treated for 5 min at 25°C). After phospholipase A2 treatment, the observed decrease in the rate of 22Na uptake induced by Mg2+ (50 μM) was generally greater than controls. After phospholipase C treatment, the observed decrease in rate of 22Na uptake induced by Mg2+ (50 μM) was less or absent when compared with controls. Phospholipase C treatment was less effective in preventing the Mg2+ effect the longer IOV were exposed to Mg2+. The results suggest that Mg2+ binds to phospholipid head-groups to reduce Na permeability perhaps by inducing a change in bilayer structure or phospholipid association.  相似文献   

5.
A new bio-antimutagen, petasiphenol [3-(3,4-dihydroxyphenyl)-2-oxopropyl caffeate] (1) was isolated from scapes of Petasites japonicum (AD50 =95μg/ml against UV-induced mutagenic E. coli WP2 B/r Trp?. Petasiphenol (1) and its isomer (2) were synthesized. The activity of 1 was observed in the presence of soybean oil (glyceride), although the isomer (2) did not show any activity in doses up to 300, μg/ml.  相似文献   

6.
The formation of radical species during the reaction of tert-butyl hydroperoxide and hypochlorous acid has been investigated by spin trapping and chemiluminescence. A superposition of two signals appeared incubating tert-butyl hydroperoxide with hypochlorous acid in the presence of the spin trap &#102 -(4-pyridyl-1-oxide)-N-tert-butylnitrone (POBN). The first signal (aN = 1.537mT, a&#103H = 0.148mT) was an oxidation product of POBN caused by the action of hypochlorous acid. The second spin adduct (aN = 1.484mT, a&#103H = 0.233mT) was derived from a radical species that was formed in the result of reaction of tert-butyl hydroperoxide with hypochlorous acid. Similarly, a superposition of two signals was also obtained using the spin trap N-tert-butyl- &#102 -phenylnitrone (PBN). tert-Butyl hydroperoxide was also treated with Fe2+ or Ce4+ in the presence of POBN. Using Fe2+ a spin adduct with a N= 1.633mT and a&#103H = 0.276mT was observed. The major spin adduct formed with Ce4+ was characterised by αN = 1.480mT and a&#103H = 0.233mT. The reaction of tert-butyl hydroperoxide with hypochlorous acid was accompanied by a light emission, that time profile and intensity were identical to those emission using Ce4+. The addition of Fe2+ to tert-butyl hydroperoxide yielded a much smaller chemiluminescence. Thus, tert-butyl hydroperoxide yielded in its reaction with hypochlorous acid or Ce4+ the same spin adduct and the same luminescence profile. Because Ce4+ is known to oxidise organic hydroperoxides to peroxyl radical species, it can be concluded that a similar reaction takes place in the case of hypochlorous acid.  相似文献   

7.
2′,3′-Bis-O-tert-butyldimethylsilyl-5′-deoxy-5′-[N-(methylcarbamoyl)amino]-N6-(N-phenylcarbamoyl)adenosine, a new member of the N6,5′-bis-ureidoadenosine class of anticancer nucleosides, is found to exhibit broad spectrum antiproliferative activity. A majority of the cell lines in the NCI-60 are inhibited with an average GI50 = 3.13 μM. Selective toxicity against human colon cancer cell lines (COLO 205, HCC-2998, HCT-116, HT29, KM12) was also exhibited (LC50’s = 6-10 μM).  相似文献   

8.
The square planar Pt(II) complexes of the type [Pt(Ln)(Cl2)] (where Ln = L1?3 = thiophene-2-carboxamide derivatives and L4?6 = thiophene-2-carbothioamide derivatives) have been synthesized and characterized by physicochemical and various spectroscopic studies. MIC method was employed to inference the antibacterial potency of complexes in reference to free ligands and metal salt. Characteristic binding constant (Kb) and binding mode of complexes with calf thymus DNA (CT-DNA) were determined using absorption titration (0.76–1.61 × 105 M?1), hydrodynamic chain length assay and fluorescence quenching analysis, deducing the partial intercalative mode of binding. Molecular docking calculation displayed free energy of binding in the range of –260.06 to –219.63 kJmol?1. The nuclease profile of complexes towards pUC19 DNA shows that the complexes cleave DNA more efficiently compared to their respective metal salt. Cytotoxicity profile of the complexes on the brine shrimp shows that all the complex exhibit noteworthy cytotoxic activity with LC50 values ranging from 7.87 to 15.94 μg/mL. The complexes have been evaluated for cell proliferation potential in human colon carcinoma cells (HCT 116) and IC50 value of complexes by MTT assay (IC50 = 125–1000 μg/mL).  相似文献   

9.
The properties of the self-assembly of two lipophilic guanine derivatives, 2′,3′,5′-O-tris(tert-butyldimethylsilyl)-guanosine and N9-(3,5-bis(tert-butyldimethylsilyloxy)-benzyl)-guanine, are described. In the presence of K+, both guanine derivatives self-associate into D 4-symmetric octamers consisting of two G-quartets stacked around a central ion.  相似文献   

10.
Sclerotinia stem rot caused by Sclerotinia sclerotiorum is an important disease of oilseed rape in Henan province of China. Boscalid belongs to succinate dehydrogenase inhibitor (SDHI) fungicides, many of which have strong antifungal activity against S. sclerotiorum. In 2015, a total of 175 isolates of S. sclerotiorum were collected from diseased oilseed rape plants in seven different regions of Henan Province. The EC50 values of 175 isolates of S. sclerotiorum to boscalid ranged from 0.0073 to 0.3880 μg ml?1, and the mean EC50 value was 0.15 ± 0.09 μg ml?1. The frequency distribution was unimodal. There was no cross‐resistance between boscalid and carbendazim, procymidone, iprodione, dimethachlone, fludioxonil or fluazinam. Field experiments showed that control efficacies of treatments with boscalid (50% WG) at 225, 300 and 375 g ai ha?1 were 71%, 81% and 90%, respectively. In contrast, the control efficacy of carbendazim (50% WP) at 1,500 g ai ha?1 was only 52%.  相似文献   

11.
Phytochemical investigations on the n-BuOH-soluble fraction of the whole plant of Buddleja davidii led to the isolation of the phenylpropanoid glycosides 1-10. Their structures were determined by 1D and 2D NMR spectroscopic techniques. All the compounds showed potent antioxidative activity in three different tests, with IC50 values in the range 4.15-9.47 μM in the hydroxyl radical (˙OH) inhibitory activity test, 40.32-81.15 μM in the total ROS (reactive oxygen species) inhibitory activity test, and 2.26-7.79 μM in the peroxynitrite (ONOO?) scavenging activity test. Calceolarioside A (1) displayed the strongest scavenging potential with IC50 values of (4.15?±?0.07, 40.32?± 0.09, 2.26?±?0.03μM) for ˙OH, total ROS and scavenging of ONOO?, respectively.  相似文献   

12.
Plant essential oils are potential sources of insecticidal compounds, but have rarely been explored for their effect on termites. In the present study, we assessed the chemical composition of essential oils of Lippia sidoides Cham. (pepper‐rosmarin; Verbenaceae) and Pogostemon cablin (Blanco) Benth. (patchouli; Lamiacaeae) and evaluated their toxicity, behavioral impairment, and repellence to termite species of the genera Amitermes and Microcerotermes (Isoptera: Termitidae: Termitinae). The main components of essential oils of L. sidoides and P. cablin were thymol (44.6%) and patchouli alcohol (36.6%), respectively. The essential oil of P. cablin was most potent against Amitermes cf. amifer Silvestri and had the lowest LD50 (0.63 μg mg?1). There was no difference in toxicity for Microcerotermes indistinctus Mathews between the essential oils of L. sidoides (LD50 = 1.49 μg mg?1) and P. cablin (LD50 = 1.67 μg mg?1). Pogostemon cablin essential oil was the most toxic to M. indistinctus (LC50 = 0.32 μl ml?1) and A. cf. amifer (LC50 = 0.29 μl ml?1). The essential oils analyzed exhibited high toxicity and repellence to the termites, in addition to reducing behavioral interactions among individuals, thus constituting potential termiticides.  相似文献   

13.
The study of chemistry of naturally occurring compounds and the synthesis of their derivatives is fundamentally important for the development of new drugs. In this work, dehydrodieugenol (DHDE) was obtained through oxidative coupling of eugenol, promoted by an aqueous mixture of potassium ferricyanide (K3[Fe(CN)6]) and NH· H2O. The partial methoxylation of DHDE with MeI and K2CO3 mainly resulted in the molecular‐shaped monomethyl ether (DHDE‐1MeO) and its dimethyl ether derivative (DHDE‐2MeO). The products from the reactions were characterized by 1H‐ and 13C‐NMR spectroscopy. Additionally, these studies have reported the antileishmanial activity of DHDE against Leishmania amazonensis (IC50 value of 42.20 μg ml?1) and shown that partial methoxylation of DHDE results in a significant increase in its antiparasitic activity (IC50 value of 13.68 μg ml?1). Based on in vitro bioassays, DHDE‐1MeO has shown the highest leishmanicidal activity in promastigota form. Production by direct one‐step synthesis of this monomethoxylated compound can be considered to be a cost‐effective and environmentally friendly method with a short reaction time.  相似文献   

14.
Six new transition metal complexes (M = Cu(II), Ni(II) and Mn(III)) of tridentate (H2L1, HL2) and/or bidentate (HL3, HL4) Schiff-base ligands, obtained from the condensation of salicylaldehyde with glycine, N-(2-aminoethyl)morpholine, 4-(2-aminoethyl)phenylic acid and 4-(2-aminoethyl)benzsulfamide, respectively, were synthesized and structurally determined by single-crystal X-ray analysis. Complexes 1-6 were evaluated for their effect on the jack bean urease and xanthine oxidase (XO). Copper(II) complexes 1-3 (IC50 = 0.43-2.25 μM) showed potent inhibitory activity against jack bean urease, comparable with acetohydroxamicacid (IC50 = 42.12 μM), which is a positive reference. And these copper(II) complexes (IC50 = 10.26-15.82 μM) also exhibited strong ability to inhibit activity of XO, comparable to allopurinol (IC50 = 10.37 μM), which was used as a positive reference. Nickel(II) and manganese(III) complexes 4-6 showed weak inhibitory activity to jack bean urease (IC50 = 4.36-8.25 μM) and no ability to inhibit XO (IC50 > 100 μM).  相似文献   

15.
To test the synthetic utility of bis(tert-butylamido)cyclodiphosph(III)azanes as ligands we extended the coordination chemistry of these diamides from Group 4 to Group 14. The syntheses of compounds of the formula cis-[tBuNP(μ-tBuN)2PNtBu]ECl2, E = Si (1), Ge (2), Sn (3) and the solid-state structures of 1 and 3 are reported. Silicon tetrachloride reacted with dilithiobis(tert-butylamido)cyclodiphosph(III)azane to cleanly produce cis-[tBuNP(μ-tBuN)2PNtBu]SiCl2, but for the germanium and tin analogues the interaction of GeCl4 or SnCl4 with the diazastannylene cis-[tBuNP(μ-tBuN)2PNtBu]Sn proved to be a better method. Single-crystal X-ray studies on both 1 and 3 revealed that they had Cs-symmetric structures, the central element being coordinated by two amide nitrogens and two chlorides, in addition to being weakly coordinated by one of the cyclodiphosph(III)azane ring nitrogens. Using structural comparisons between crystallographically-independent 1a and 1b, between 1 and 3, and between 3 and its isomorphous zirconium analogue, the nature of this donor bond is discussed.  相似文献   

16.
In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC50 value of 2.7 μM in inhibition of melanogenesis. The structure for potent inhibitory activity of these derivatives are required with the direct connection of π-planar structure to thiourea without steric hinderance in PTU derivatives and the hydrophobic substituent at para position in case of semicarbazones.  相似文献   

17.
The prawn Macrobrachium sintangense is likely to be subjected to occasional exposure to combined metal and saline stressors in its natural environment. This research evaluated the acute toxicity (96?h LC50) of cadmium (Cd) on the prawn M. sintangense, with respect to the osmoregulatory capacity (OC) of prawns and to document histological changes in the gills after exposure to sublethal Cd concentrations at different salinities. The 96?h LC50 of Cd to M. sintangense decreased with increasing salinity. The 96?h LC50 values were 89.12 (72.53–109.50), 681.26 (554.20–837.46) and 825.37 (676.99–1006.27) μg CdL?1 at 0, 10 and 20 ppt, respectively. The OC of prawns exposed to 30?μg?CdL?1 at 0 ppt and to 300?μg?CdL?1 at10 ppt decreased significantly compared with that of control prawns exposed to 0 and 10 ppt respectively. Swelling, hyperplasia and necrosis of gill lamellae resulting in the loss of marginal canals were observed in the gills of prawns exposed to 30?μg?CdL?1 at 0 ppt and to 300?μg?CdL?1 at 10 ppt for 7?days.  相似文献   

18.
The complexes [{Ru(tpy)(bpy)}2(μ-adpc)][PF6]2 where tpy is 4,4′,4″-tri-(tert-butyl)-2,2′:6′,2″-terpyridine, bpy is 2,2′-bipyridine, and adpc2− is 4,4′-azo-diphenylcyanamide dianion and trans,trans-[{Ru(tpy)(pc)}2(μ-adpc)] where pc is 2-pyrazine-carboxylato were prepared and characterized by cyclic voltammetry and spectroelectrochemical methods. Intervalence band properties and IR spectroelectrochemistry of the mixed-valence complexes [{Ru(tpy)(bpy)}2(μ-adpc)]3+ and trans,trans-[{Ru(tpy)(pc)}2(μ-adpc)]+ are consistent with delocalized and valence-trapped mixed-valence properties respectively. The reduction in mixed-valence coupling upon substituting a bipyridine ligand with 2-pyrazine carboxylato strongly suggests that hole-transfer superexchange is the dominant mechanism for metal-metal coupling in these complexes.  相似文献   

19.
The effects of growth temperature on the marine chlorophyte Dunaliella tertiolecta Butcher were studied to provide a more mechanistic understanding of the role of environmental factors in regulating bio-optical properties of phytoplankton. Specific attention was focused on quantities that are relevant for modeling of growth and photosynthesis. Characteristics including chlorophyll a (chl z)-specific light absorption (a*ph(λ)), C:chl a ratio, and quantum yield for growth (φμ) varied as functions of temperature under conditions of excess light and nutrients. As temperature increased over the range examined (12°-28°C), intracellular concentrations of chl a increased by a factor of 2 and a*ph(λ) values decreased by more than 50% at blue to green wavelengths. The lower values of a*ph(λ) were due to both a decrease in the abundance of accessory pigments relative to chl a and an increase in pigment package effects arising from higher intracellular pigment concentrations. Intracellular pigment concentration increased as a consequence of higher cellular pigment quotas combined with lower cell volume. At high growth temperatures, slightly more light was absorbed on a per-cell-C basis, but the dramatic increases in growth rate from μ= 0.5 d?1 at 12° C to μ= 2.2 d?1 at 28°C were primarily due to an increase in φμ (0.015–0.041 mol C (mol quanta)?1). By comparison with previous work on this species, we conclude the effects of temperature on a*ph(λ) and φμ are comparable to those observed for light and nutrient limitation. Patterns of variability in a*ph(λ)and φμ as a function of growth rate at different temperatures are similar to those previously documented for this species grown at the same irradiance but under a range of nitrogen-limited conditions. These results are discussed in the context of implications for bio-optical modeling of aquatic primary production by phytoplankton.  相似文献   

20.
Ten essential oils were tested against the cabbage looper, Trichoplusia ni larvae for contact, residual and fumigant toxicities and feeding deterrent effects. Against third instar T. ni, Syzygium aromaticum (LD50 = 47.8 μg/larva), Thymus vulgaris (LD50 = 52.0 μg/larva) (the two positive controls) and Cinnamomum glanduliferum (LD50 = 76.0 μg/larva) were the most toxic via topical application. Litsea pungens (LD50 = 87.1 μg/larva), Ilex purpurea (LD50 = 94.0 μg/larva), Cinnamomum cassia (LD50 = 101.5 μg/larva) and Litsea cubeba (LD50 = 112.4 μg/larva) oils were equitoxic. Thymus vulgaris (LC50 = 4.8 mg/ml) and S. aromaticum (LC50 = 6.0 mg/ml) oils were the most toxic in residual bioassays. Cymbopogon citratus (LC50 = 7.7 mg/ml) and C. cassia (LC50 = 8.5 mg/ml) oils were equitoxic followed by Cymbopogon nardus (LC50 = 10.1 mg/ml) in this bioassay. The remaining five oils showed little or no residual effects. In a fumigation bioassay, L. cubeba (LC50 = 16.5 μl/l) and I. purpurea (LC50 = 22.2 μl/l) oils were the most toxic. Cinnamomum glanduliferum (LC50 = 29.7 μl/l) and Sabina vulgaris (LC50 = 31.2 μl/l) oils were equitoxic. Interestingly, S. aromaticum did not exhibit any fumigant toxicity. Cymbopogon citratus, C. nardus and C. cassia strongly deterred feeding by third instar T. ni (DC50s = 26.9, 33.8 and 39.6 μg/cm2, respectively) in a leaf disc choice bioassay. The different responses of T. ni larvae to the oils in different bioassays suggest that these essential oils exhibit different modes of action. Based on their comparable efficacy with essential oils already used as active ingredients in many commercial insecticides (i.e. clove oil and thyme oil), some of these essential oils may have potential as botanical insecticides against T. ni.  相似文献   

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