Median Effective Concentration

2016 ◽  
Author(s):  
John H. Duffus ◽  
Monica Nordberg ◽  
Douglas M. Templeton
2021 ◽  
Vol 22 (7) ◽  
pp. 3450
Author(s):  
Lei Liu ◽  
Li-Peng Shan ◽  
Yan Zhou ◽  
Jiong Chen

Rapid production of prawn (Litopenaeus vannamei) under artificial pressure can result in a series of obvious challenges and is vulnerable to serious losses related to aquatic environmental issues and the unrestrained outbreak of white spot syndrome (WSS). However, to date, there are no therapeutic strategies to contain the spread of the virus. Here, we synthesized 27 coumarin deriv-atives and evaluated their anti-white spot syndrome virus (WSSV) activity in L. vannamei larvae. We demonstrated that electron-withdrawing and electron-giving substituent groups play an im-portant role in reducing toxicity and WSSV replication, respectively. Two coumarin C2 (2-amino-5-oxo-4-(p-tolyl)-4H,5H-pyrano[3,2-c]chromene-3-carbonitrile) and C7 (2-amino-4-(4-chlorophenyl)-5-oxo-4H,5H-pyrano[3,2-c]chromene-3-carbonitrile) were regarded as the most promising anti-WSSV compounds with maximum antiviral response <5% and median effective concentration <10 mg/L. The mortality of WSSV-infected larvae decreased by more than 60% after exposure to C2 and C7. With continuous immersion of C2 and C7 exchange, the mortality further decreased to 40% at 120 h.Additionally, C2 and C7 are the relatively stable in aquacultural water, making these agents


1996 ◽  
Vol 85 (4) ◽  
pp. 901-912 ◽  
Author(s):  
Michael C. Crowder ◽  
Laynie D. Shebester ◽  
Tim Schedl

Background The nematode Caenorhabditis elegans offers many advantages as a model organism for studying volatile anesthetic actions. It has a simple, well-understood nervous system; it allows the researcher to do forward genetics; and its genome will soon be completely sequenced. C. elegans is immobilized by volatile anesthetics only at high concentrations and with an unusually slow time course. Here other behavioral dysfunctions are considered as anesthetic endpoints in C. elegans. Methods The potency of halothane for disrupting eight different behaviors was determined by logistic regression of concentration and response data. Other volatile anesthetics were also tested for some behaviors. Established protocols were used for behavioral endpoints that, except for pharyngeal pumping, were set as complete disruption of the behavior. Time courses were measured for rapid behaviors. Recovery from exposure to 1 or 4 vol% halothane was determined for mating, chemotaxis, and gross movement. All experiments were performed at 20 to 22 degrees C. Results The median effective concentration values for halothane inhibition of mating (0.30 vol%-0.21 mM), chemotaxis (0.34 vol%-0.24 mM), and coordinated movement (0.32 vol% - 0.23 mM) were similar to the human minimum alveolar concentration (MAC; 0.21 mM). In contrast, halothane produced immobility with a median effective concentration of 3.65 vol% (2.6 mM). Other behaviors had intermediate sensitivities. Halothane's effects reached steady-state in 10 min for all behaviors tested except immobility, which required 2 h. Recovery was complete after exposure to 1 vol% halothane but was significantly reduced after exposure to immobilizing concentrations. Conclusions Volatile anesthetics selectively disrupt C. elegans behavior. The potency, time course, and recovery characteristics of halothane's effects on three behaviors are similar to its anesthetic properties in vertebrates. The affected nervous system molecules may express structural motifs similar to those on vertebrate anesthetic targets.


Parasitology ◽  
2013 ◽  
Vol 140 (8) ◽  
pp. 952-958 ◽  
Author(s):  
ZE-HONG LI ◽  
JIA-YU WAN ◽  
GUI-QIN WANG ◽  
FU-GUANG ZHAO ◽  
JI-HONG WEN

SUMMARYThe present study was designated to ascertain the anthelmintic activity of the rhizomes of Paris polyphylla and to isolate and characterize the active constituents. The methanol extract from rhizomes of P. polyphylla showed significant anthelmintic activity against Dactylogyrus intermedius with the median effective concentration (EC50) 22·5 mg L−1. Based on this finding, the methanol extract was fractionated by silica gel column chromatography in a bioassay-guided fractionation yielding 2 bioactive compounds, the structures of these compounds were elucidated as formosanin C and polyphyllin VII. The in vivo tests revealed that formosanin C and polyphyllin VII were significantly effective against D. intermedius with EC50 values of 0·6 and 1·2 mg L−1, respectively. The acute toxicities (LC50) of formosanin C and polyphyllin VII for grass carp were 2·8 and 2·9 mg L−1, respectively. The overall results provide important information for the potential application of formosanin C and polyphyllin VII in the therapy of serious infection caused by D. intermedius.


Molecules ◽  
2019 ◽  
Vol 24 (14) ◽  
pp. 2607
Author(s):  
Zhang ◽  
Meng ◽  
Xie ◽  
Yang ◽  
Zhang ◽  
...  

In order to explore more efficient sulfonamides against Botrytis cinereal, 36 novel cyclohexylsulfonamides were synthesized by N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide (EDCI) and 1-hydroxybenzotriazole (HOBt) condensation reaction using chesulfamide as a lead compound, introducing thiazole and pyrazole active groups. Their structures were characterized by 1H-NMR, 13C-NMR, mass spectrum (MS), and elemental analysis. Compound III -31 was further confirmed by X-ray single crystal diffraction. The in vitro and in vivo fungicidal activities against B. cinerea were evaluated by three bioassay methods. The results of mycelial growth demonstrated that median effective concentration (EC50) values of nine compounds were close to boscalid (EC50 = 1.72 µg/mL) and procymidone (EC50 = 1.79 µg/mL) against B. cinerea (KZ-9). In the spore germination experiment, it was found that compounds III-19 and III-31 inhibited germination 93.89 and 98.00%, respectively; at 10 µg/mL, they approached boscalid (95.97%). In the tomato pot experiment, the control effects of two compounds (III-21 and III-27) were 89.80 and 87.90%, respectively, at 200 µg/mL which were significantly higher than boscalid (81.99%). The structure–activity relationship (SAR) was also discussed, which provided a valuable idea for developing new fungicides.


Sign in / Sign up

Export Citation Format

Share Document