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1.
Summary Excised embryos of Hibiscus spp. were treated with 1 kR to 6 kR of X-ray. Results indicate that germination was unaffected at this level of employed doses in both species, which in turn implies that the factors responsible for inhibition of germination are not present in the embryo. LD50 values differed between varieties and species. Early varieties of both species were more sensitive to radiation than late varieties. Strikingly similar effects were observed for the varieties with smaller embryos over those with larger ones. Allopolyploid H. sabdariffa (2n=72) was more susceptible than diploid H. cannabinus (2n=36).Differences in mutation frequency exist between species with different levels of ploidy and between varieties within the same species. Most of the HC mesta varieties yielded higher mutation frequencies than those of HS mesta. Optimal dose for triggering mutations in all varieties (except the chlorophyll mutation variety of HC mesta) of the two species lies within a narrow range of 1 kR to 2 kR. Cent per cent seedling abnormalities is concomitant to LD50; nevertheless, optimum dose for mutation frequency is independent of LD50. Hence, the response should be viewed in terms of respective genotype. The advantages of the embryo irradiation technique are mentioned.  相似文献   

2.
We investigated the in vivo effects of orally administered cariprazine (RGH-188; trans-N-{4-[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-N′,N′-dimethyl-urea), a D3/D2 dopamine receptor partial agonist with ∼10-fold preference for the D3 receptor. Oral bioavailability of cariprazine at a dose of 1 mg/kg in rats was 52% with peak plasma concentrations of 91 ng/mL. Cariprazine 10 mg/kg had good blood-brain barrier penetration, with a brain/plasma AUC ratio of 7.6:1. In rats, cariprazine showed dose-dependent in vivo displacement of [3H](+)-PHNO, a dopamine D3 receptor-preferring radiotracer, in the D3 receptor-rich region of cerebellar lobules 9 and 10. Its potent inhibition of apomorphine-induced climbing in mice (ED50 = 0.27 mg/kg) was sustained for 8 h. Cariprazine blocked amphetamine-induced hyperactivity (ED50 = 0.12 mg/kg) and conditioned avoidance response (CAR) (ED50 = 0.84 mg/kg) in rats, and inhibited the locomotor-stimulating effects of the noncompetitive NMDA antagonists MK-801 (ED50 = 0.049 mg/kg) and phencyclidine (ED50 = 0.09 mg/kg) in mice and rats, respectively. It reduced novelty-induced motor activity of mice (ED50 = 0.11 mg/kg) and rats (ED50 = 0.18 mg/kg) with a maximal effect of 70% in both species. Cariprazine produced no catalepsy in rats at up to 100-fold dose of its CAR inhibitory ED50 value. Cariprazine 0.02-0.08 mg/kg significantly improved the learning performance of scopolamine-treated rats in a water-labyrinth learning paradigm. Though risperidone, olanzapine, and aripiprazole showed antipsychotic-like activity in many of these assays, they were less active against phencyclidine and more cataleptogenic than cariprazine, and had no significant effect in the learning task. The distinct in vivo profile of cariprazine may be due to its higher affinity and in vivo binding to D3 receptors versus currently marketed typical and atypical antipsychotics.  相似文献   

3.
We present in this article syntheses of six new hybrids compounds (49) that were efficiently prepared in one or two steps (70–84.6%) from our previous prototype (±)-cis-4-chloro-6-(naphthalen-1-yl)-tetrahydro-2H-pyran-2-yl)methanol (3) and the NSAIAs: acetyl salicylic acid, indomethacin, ibuprofen, ketoprofen, naproxen and diclofenac. The acetic acid-induced writhing method is able to determine that all investigated new hybrids showed stronger antinociceptive properties (2- to 10-fold less ED50 values) than their precursors. The highest antinociceptive effect was observed for compound 9 showing more than 10-fold less ED50 values than diclofenac and ninefold less ED50 value than compound 2. All compounds presented greater activity than the control group in the tail-flick test confirming the central antinociceptive effect. New hybrids did not alter the motor performance of mice by rota-rod performance and open-field tests. Investigated compounds 49 were not toxic after oral administration (LD50 >2000 mg/kg).  相似文献   

4.
Accurate repair of ultraviolet-induced damage in Micrococcus radiodurans   总被引:7,自引:0,他引:7  
The nature of the patterns of elimimation of chromosomal aberrations in both root and shoot has been studied in both the species of P. canariensis Linn (2n = 12) and P. minor Retz (2n = 28) after irradiating their dry seeds with filtered and unfiltered X-rays.Doses used are 10 kR and 30 kR filtered X-rays and 10 kR and 20 kR unfiltered X-rays.The elimination curves in both root and shoot have been fitted to the equation N1 = N0e?KT for both the species. The pattern of elimination for each type of aberrations was found to be exponential in both root and shoot.  相似文献   

5.
Conventional pesticides have suffered two main drawbacks: (a) broad spectrum of action and (b) selection of target species resistant to the different active ingredients. Thus compounds that are less harmful to the environment and to human health, more specific and that do not induce resistance need to be developed. One alternative are insect growth regulators, such as fluazuron. The present study examined the efficacy of fluazuron (active ingredient of the acaricide Acatak®) and the sensitivity of Rhipicephalus sanguineus nymphs exposed to different doses of this chemical, and determined the lethal doses of fluazuron: 95% – LD95 and 50% – LD50. Different doses of fluazuron were applied in duplicates on the dorsal region of hosts (“pour on”). Distilled water was used in the control group. On the first day after the treatment with fluazuron, hosts were artificially infested with R. sanguineus nymphs. After engorgement, nymphs were removed, placed on Petri dishes, identified, and maintained in BOD incubator for 15 days. Dead R. sanguineus nymphs after the treatment with 13 different doses of fluazuron were quantified and the LD95 was estimated to be 100 mg/kg and LD50, 19.544 mg/kg (12.478–22.636), with a confidence interval of 95%. Nymphs of R. sanguineus were sensitive to fluazuron at various levels, indicating that this insect growth regulator (IGR) may be used to control this parasite in this stage of its biological cycle, reducing the significant damage it causes.  相似文献   

6.
The anti-allatin substance, 7-ethoxy-precocene II (= “precocene III”) was topically applied to eggs of Locusta migratoria migratorioides with fully grown embryos in stage XX (about 64 ± 4% of the whole period of egg development). A day after precocene application the eggs were washed for 10–15 s in acetone and then transferred to clean containers for removing precocene residues and for preventing contamination at hatching. The treatment induced prothetelic morphogenetic disturbances which became overt in the subsequent hoppers; the effect was dose dependent and the ED50 (= effective anti-allatin dose 50%) was low, 20.5 μg precocene III per g fresh egg weight (= 0.37 μg per egg). Quite similar results were obtained following application of precocene III to eggs with embryos in stage XXI (73 ± 4% of the egg development). These findings and direct examination of histological sections of the embryonic corpora allata demonstrated that precocene chemically allatectomizes late Locusta embryos. The lethal effect of precocene III was dependent on the washing. When the eggs were washed in acetone a day after application, mortality did not occur in a dose-dependent way; even the highest dose applied, 256 μg precocene III per egg (= 14405 μg per g fresh weight), was less than the LD50 (lethal dose 50%). In contrast, without washing mortality was dose dependent, but it occurred later, at or after hatching; the LD50 was 1334.9 μg per g (= 22.7 μg/egg). The results show that the late embryos are highly susceptible to the anti-allatin effect of the precocene, but are extremely insusceptible to its lethal effect; toward hatching, however, susceptibility to the lethal effect becomes marked.With doses between 45–14405 μg precocene III per g fresh egg weight, the anti-allatin effect became overt by a quite-uniform belated morphogenetic response. All hoppers which hatched from precocenetreated eggs were morphogenetically normal in the 1st instar and in the beginning of the 2nd instar, but the duration of the 2nd instar was almost doubled and at the end of this instar over 96% of the locusts died in the moult, being unable to shed the exuvia. Artificial removal of the apolyzed old cuticle revealed 3rd instar prothetelic adultiforms. These results and some data in the literature indicate that allatectomy of the embryo does not result in prothetelic morphogenetic disturbances in the 1st and early 2nd instar larvae and may impose the question what is the role of the juvenile hormone in late embryos and early larvae.  相似文献   

7.
The objective of this study was to investigate brine shrimp cytotoxicity, larvicidal, nematicidal, and antifeedant activities of novel piperidin-connected 2-thioxo-imidazolidin-4-one derivatives. The activities of target compounds were compared with some naturally occurring (?)-pinidinol, hydantocidin, and positive controls. Target compounds were synthesized via cyclocondensation method. The compounds were synthesized and then characterized by infrared spectroscopy, 1H NMR, 13C NMR, mass spectral, and elemental analyses. Brine shrimp cytotoxicity assay was investigated using freshly hatched, free-swimming nauplii of Artemiasalina. Larvicidal screening was performed against urban mosquito larvae (Culex quinquefasciatus). Nematicidal activity was evaluated using juvenile nematodes of Meloidogyne javanica. Regarding antifeedant activity, marine-acclimated Oreochromis mossambicus fingerlings were used. Compounds 3a-c (piperidin-connected 2-thioxoimidazolidin-4-one) were found to be lethal to the second instar larvae of mosquito, which produced LD50 values of 1.37, 6.66, 6.51 μg/mL, compared to compounds (?) pinidinol and hyantocidin LD50 values of 18.28 and 22.11 μg/mL respectively. Compound 3a-c was found to kill 100% of fish fingerlings within 6 h at 20 µg/mL, with LD50 values of 1.54, 1.79, 1.52 µg/mL, compared to compounds (?) pinidinol and hyantocidin with LD50 values of 10.21 and 21.05 μg/mL respectively. Compound 3c with LD50 value of 1.57 μg/mL demonstrated high nematicidal activity compared to compound 3a, 3b, (?) Pinidinol and Hyantocidin LD50 values of 6.45, 2.42, 14.25, 26.30 μg/mL respectively. Therefore, the 2-thioxoimidazolidin-4-one with piperidin ring showed high potential cytotoxic, larvicidal, nematicidal, and antifeedent activities.  相似文献   

8.
Treatment of diapausing pupae of M. configurata with dibutyryl cyclic AMP or 8-(4-chlorophenylthio) cyclic AMP (CPT cyclic AMP) reduced the incidence of eclosion to zero compared to about 15% for controls, whereas treatment with cyclic GMP increased eclosion to more than 90%. Treatment with the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (IBMX) resulted in a high incidence (79.8%) of eclosion, but treatment with dibutyryl cyclic AMP + IMBX or CPT cyclic AMP + IBMX gave low incidences (<9.1%) of eclosion. Other methylxanthines (theophylline, 8-phenyltheophylline, caffeine) and papaverine had relatively little effect on eclosion even at high doses.Treatment of post-diapause pupae with dibutyryl cyclic AMP or CPT cyclic AMP resulted in a low incidence (<5.0%) of eclosion compared to 98.8% eclosion in controls. Suppression of eclosion was more effective if dibutyryl cyclic AMP was given within the first 2 days of pupal-adult development at 20°C and became less effective as development progressed, indicating that dibutyryl cyclic AMP inhibits endocrine events initiating development rather than inhibiting subsequent metamorphic development. Treatment of post-diapausing pupae with cyclic GMP, IBMX, other methylxanthines or papaverine did not affect eclosion. These results are consistent with a dual control of pupal diapause in M. configurata by cyclic nucleotides, with cyclic AMP acting to maintain diapause and cyclic GMP acting to terminate it.  相似文献   

9.
Fifteen strains of Plasmodium falciparum have been cultivated since 1979 using the Trager and Jensen method of continuous culture on isolates from malaria patients. One hundred and two drug sensitivity studies have been carried out on these strains using a semimicro test. Three isolates, initially resistant to chloroquine, adapted rapidly to in vitro cultivation and maintained their high level of resistance (ED50 above 660 nM). Eleven isolates, initially chloroquine sensitive (ED50 under 90 nM) became resistant to this drug (ED50 = 190 to 1950 nM) after the 2–15 weeks required for their adaptation to continuous culture. The resistance of these strains never decreased during the following 15 months of continuous culture. The sensitivity to quinine varied initially from one strain to another (ED50= 160 to 660 nM) and fluctuated during cultivation in the ratio of 1, 3.5 for a given strain. The sensitivity of mefloquine remained high for all strains (ED50 under 150 nM) but one (ED50 = 560 nM). These results suggest that there might be a relationship between in vitro adaptation to culture of P. falciparum by the Trager-Jensen method and a chloroquine-resistant characteristic of the strain. There is the possibility of the emergence of a drug-resistant subpopulation or of changes in the metabolic pathways.  相似文献   

10.
Summary Tetrodotoxin (10–8 to 10–6 g/ml) blocked the contractile responses of isolated guinea-pig urinary bladder preparation to electrical (25 and 100 Hz) neural but not to transmural stimulation and to X-irradiation (50 kV, 20 kR/min, 20 kR). The irradiation had no influence on the bladder responses to electrical and hormonal (acetylcholine and histamine) stimulation. It is concluded that the X-ray-induced contraction is of myogenic origin and that it is possibly not related to the electro-mechanical coupling system.  相似文献   

11.
An amplified enzyme-linked immunosorbent assay (ELISA) for the detection of Clostridium botulinum complex neurotoxins was evaluated for its ability to detect these toxins in food. The assay was found to be suitable for detecting type A, B, E, and F botulinum neurotoxins in a variety of food matrices representing liquids, solid, and semisolid food. Specific foods included broccoli, orange juice, bottled water, cola soft drinks, vanilla extract, oregano, potato salad, apple juice, meat products, and dairy foods. The detection sensitivity of the test for these botulinum complex serotypes was found to be 60 pg/ml (1.9 50% lethal dose [LD50]) for botulinum neurotoxin type A (BoNT/A), 176 pg/ml (1.58 LD50) for BoNT/B, 163 pg/ml for BoNT/E (4.5 LD50), and 117 pg/ml for BoNT/F (less than 1 LD50) in casein buffer. The test could also readily detect 2 ng/ml of neurotoxins type A, B, E, and F in a variety of food samples. For specificity studies, the assay was also used to test a large panel of type A C. botulinum, a smaller panel of proteolytic and nonproteolytic type B, E, and F neurotoxin-producing Clostridia, and nontoxigenic organisms using an overnight incubation of toxin production medium. The assay appears to be an effective tool for large-scale screening of the food supply in the event of a botulinum neurotoxin contamination event.  相似文献   

12.
Bruchid larvae cause major losses in grain legume crops throughout the world. Some bruchid species, such as the cowpea weevil, are pests that damage stored seeds. Plants synthesize a variety of molecules, including proteinaceous proteinase inhibitors, to defend themselves against attack by insects. In this work, a trypsin inhibitor (DMTI-II) isolated from Dimorphandra mollis seeds was tested for anti-insect activity against Callosobruchus maculatus larvae. The inhibitor produced ca. 67% mortality to this bruchid when incorporated into an artificial diet at a level of 1%. The doses necessary to cause 50% mortality (LD50) and to reduce weight by 50% (ED50) for DMTI-II were ca. 0.50% and 0.60%, respectively. The action of DMTI-II on C. maculatus larvae may involve the inhibition of trypsin-like activity of larval midgut extracts, the absence of digestion by midgut preparations or with a mixture of pepsin and papain, and its association with a chitin column and chitinous structure in the midgut of this insect.  相似文献   

13.
Flocoumafen had good rodenticidal action against Apodemus agrarius and Rattus losea. The acute oral LD50 for male A. agrarius and R. losea was 1·22 mg kg−1 and 1·36 mg kg−1 respectively. Flocoumafen bait was more toxic to R. losea than to A. agrarius. At bait concentrations of 0·002–0·005%, flocoumafen had a single-feed potency with mortalities of 90–100% for R. losea and 77·8–100% for A. agrarius. Experimental baits prepared using the manufacturing 0·5% master mix of flocoumafen were palatable to both species.  相似文献   

14.
Summary Floronia bucculenta hibernates in the egg stage; the egg sacs are deposited on the leaves of grass tussocks without any shelter. The morphogenesis of the eggs was divided into 10 arbitrarily chosen stages, in order to test the dependence of embryonic development on temperature in the laboratory. The eggs developed slowly at 23°C, 16°, 12.5°; embryogenesis stopped after 70–45 days, when prosomal appendage rudiments began to form. At 10°, 7.5°, 5°, 0° complete embryogenesis was possible until the emergence of the first complete stage. The eggs developed most rapidly at 5° (mean developmental time 203 days). The egg development was normal at 5° and 0°, when compared with the timetable of the embryogenesis of the linyphiid Bathyphantes gracilis, a species which has no egg diapause. At 7.5° and 10° the embryogenesis was strongly delayed during the median phases of development (elongation of the germ band, formation of prosomal appendages); after reversion the development was accelerated (postdiapause phase). After long exposure to low temperatures (-10° to +10°) the diapause was terminated. A temperature of 0° was optimal (minimal time of exposure 8–9 weeks). The time required for embryonic development of postdiapause eggs decreased hyperbolically with increasing temperature. In the field the median phases of embryogenesis were retarded by low ambient temperatures; diapause was terminated from late December to mid-January. The spread of hatching in spring was 7–15 days.During the diapause phase the O2-consumption of the eggs at 25° was depressed. It rose from 1.55 (in late diapause) to 4.21 ml/100 eggs·h at the onset of postdiapause, whereas O2-utilization did not change significantly at 5° (from 0.54 to 0.61 ml/100 eggs·h just after the termination of diapause).The diapause phase was not characterized by higher resistance to cold, drought, or flooding. As compared with single eggs removed from the cocoon, the silken wall of the intact egg sac did not affect the survival of postdiapause eggs exposed to-15° (LD50=28 days); it raised, however, the survival time of eggs exposed to a R.H. of 32% (at 5°) or flooding by distilled water (at 5°): from LD50=37 to 68 days at drought, from LD50=30 to 92 days at flooding.Diapause is important for synchronizing the life-cycle of F. bucculenta with the seasonal fluctuations of environment. The egg stage is highly tolerant to the extreme factors of the winter. Some implications of the relation of the studied spider to its habitat are discussed.  相似文献   

15.
R. H. Cherry 《BioControl》1979,24(1):35-39
Seasonally acclimatized citrus blackfly (CBF),Aleurocanthus woglumi Ashby, and its parasite,Amitus hesperidum Silv. were exposed to extreme temperatures for 3-hour periods and survivorship measured. In summer experiments, the LD50 for CBF adults and 1st instar nymphs occurred between 40° and 45°C. The LD50 forA. hesperidum adults occurred between 35° and 40°C and increased with decreased humidity, although some adults could continue to emerge from parasitized CBF up to 45°C. In winter experiments, the LD50 for CBF eggs and adults occurred between ?5° and ?10°C and for other CBF stages between ?10° and ?15°C. The LD50 for adultA. hesperidum, and survival and emergence of the parasites from CBF both occurred between ?10° and ?15°C. Comparing data from the 2 seasons shows that adults are the most temperature sensitive stage of CBF and the parasite is more temperature sensitive than CBF, especially at higher temperatures. Correlating lethal temperature data with field meteorological conditions shows that short-term temperature exposures cannot be expected to stop the potential spread of CBF orA. hesperidum through Florida.  相似文献   

16.
《Journal of Asia》2002,5(1):131-133
Eighteen essential oils were tested for their fumigant toxicity towards Proisotoma minuta (Tullberg). The essential oils of citronella (LD50=0.65 μL/L air), petitgrain (LD50=2.3 μL/L air), and thyme (LD50=2.8 μI/L air) produced potent activity towards the species.  相似文献   

17.
The Pinus wallichiana, Daphne oleiodes and Bidens chinensis have a long history of being used traditionally for treatment of various types of disorders. Most of the uses have been without any scientific evidence and toxicological assessment. We evaluated the mutagenic and cytotoxic capabilities of various parts of P. wallichiana, D. oleoides and B. chinensis. Ames Salmonella mutagenicity assay determined the mutagenicity activity against TA 98 and TA 100 bacterial strains of Salmonella typhimurium without metabolic activator S9 system. The number of mutant colonies in negative control was considered as limit to determine the mutagenicity effects of every extract. Brine shrimps lethality bioassay was used to determine the cytotoxic capabilities of the selected plants. The P. wallichiana, D. oleiodes and B. chinensis did not showed any mutagenic activity both for frameshift mutation (TA98) and base-pair substitution (TA100) without S9 mixture. The crude methanolic extract of P. wallichiana stem showed moderate cytotoxicity (53.33%) at 1000 μg/ml with LD50 value 599.634. The D. oleoides fruit showed a toxicity of 60% at 1000 μg/ml with LD50 value 367.730. The B. chinensis (whole plant) showed lethality of 63.3% at 1000 μg/ml, with LD50 204.833. The absence of any mutagenic activity of crude extract of the tested plants in both bacteria strains, TA 98 and TA 100 without the S9 mix confirms the safety of these plants to the consumers.  相似文献   

18.
Three plant proteinase inhibitors BbKI (kallikrein inhibitor) and BbCI (cruzipain inhibitor) from Bauhinia bauhinioides, and a BrTI (trypsin inhibitor) from B. rufa, were examined for other effects in Callosobruchus maculatus development; of these only BrTI affected bruchid emergence. BrTI and BbKI share 81% identities in their primary sequences and the major differences between them are the regions comprising the RGD and RGE motifs in BrTI. These sequences were shown to be essential for BrTI insecticidal activity, since a modified BbKI [that is a recombinant form (BbKIm) with some amino acid residues replaced by those found in BrTI sequence] also strongly inhibited insect development. By using synthetic peptides related to the BrTI sequence, YLEAPVARGDGGLA-NH2 (RGE) and IVYYPDRGETGL-NH2 (RGE), it was found that the peptide with an RGE sequence was able to block normal development of C. maculatus larvae (ED50 0.16% and LD50 0.09%), this being even more effective than the native protein.  相似文献   

19.
Diapause and hatching of Brachionus plicatilis Müller resting eggs were examined through histological and optical approaches. Compound microscope observations on 1% toluidine blue-stained embryo sections suggests that the total number of nuclei in an embryo during the internal diapause period increased from 22 on Day 2 to 39 (each n = 1) on Day 6. The outer layer of embryo membrane gradually thickens from 1.2 (Day 0) to 4.0 µm (Day 8) (each n = 10).Resting eggs that have completed maturation and are in the external diapause period require light for hatching. The threshold of light (halogen lamp) intensity for hatching was estimated to be 4400 lux for 30 min. Hatching rate decreased with longer wavelength irradiation (mercury lamp). Irradiation at more than 350 nm caused 1–25% hatching, but it reached 50–60% at 250–310 nm light. The addition of hydrogen peroxide or prostaglandins (E 1, E 2 or F 2) caused resting egg hatching even in darkness. The production of peroxide in seawater caused by light as well as the oxidation of fatty acid to prostaglandins inside the embryo is a possible mechanism of resting egg hatching.  相似文献   

20.
PurposePost-implant CT-scanning is an essential part of permanent prostate brachytherapy. However, the evaluation of post-implant CT dosimetry is not straightforward due to the edema that can modify the dose to the prostate and to the organs at risk. The aim of this study is to evaluate the impact of the timing of the post-implant CT-scan on the dosimetric results and to verify if the Day 0 scan findings can predict Day 50 scanning.Methods136 consecutive patients who received monotherapy with I-125 implants were selected for this study. Two sets of 8 dosimetric quality parameters corresponding to 2 different CT-scans (Day 0 and Day 50) were calculated and compared. The dosimetric parameters included are the percentage volume of the post-implant prostate receiving 80%, 100% and 150% of the prescribed dose, the doses covering 80% and 90% of the prostate volume and the Dose Homogeneity Index. The values of the dose covering 1 cm3 of the rectum and urethra were assessed.ResultsAll the dosimetric parameters of the Day 50 were higher than those of the Day 0 scan. Linear functions were obtained that calculate D90 and V100 values at Day 50 based on the Day 0 findings. Rectal and urethral parameters tended to be underestimated on Day 0 CT-scan relative to Day 50 based dosimetry.ConclusionsPredicting the Day 50 dosimetry from the Day 0 scan could be a possible alternative to a Day 50 scan only in specific situations, but with a degree of uncertainty in the predicted values.  相似文献   

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