A RAPID AND SIMPLE FLOUR-DISK BIOASSAY FOR TESTING SUBSTANCES ACTIVE AGAINST STORED-PRODUCT INSECTS

1996 ◽  
Vol 128 (5) ◽  
pp. 865-875 ◽  
Author(s):  
Y.S. Xie ◽  
R.P. Bodnaryk ◽  
P.G. Fields

AbstractA rapid and simple flour-disk bioassay was developed to assay biologically active substances on several species of stored-products insects. The speed, simplicity, and parsimony of the bioassay derive from a single-step mixing of the test substance in aqueous solution with flour. Aliquots (100 μL) of the stirred suspension are then pipetted onto a polystyrene Petri dish using an Eppendorf pipettor and allowed to dry at room temperature overnight to produce uniform flour disks containing the test substance. After equilibration at 30 ± 1°C and 70 ± 5% relative humidity for 24 h, the disks are individually weighed and transferred to Petri dishes with weighed stored-products insects. After 3 days, the remainder of the disk and the living insects are weighed again for calculations of food consumption, utilization, growth, and mortality. Based on the flour-disk bioassay, the neem-based insecticide, Margosan-O®, significantly reduced consumption, growth, feeding, and dietary utilization in Cryptolestes ferrugineus (Stephens), Sitophilus oryzae (L.), and Tribolium castaneum (Herbst) in a dose-dependent manner. Margosan-O® also caused mortality, but the species differed widely in sensitivity, C. ferrugineus being the most sensitive and T. castaneum the least. The mortality of C. ferrugineus and S. oryzae was a consequence of both toxic and antifeedant (starvation) effects, but mortality of T. castaneum was caused entirely by its toxic action. Using a whole-kernel bioassay, it was found that Margosan-O® caused a dramatic reduction in the F1 progeny of all three species.

2014 ◽  
Vol 25 (3-4) ◽  
pp. 24-33
Author(s):  
O. I. Dzjuba ◽  
M. V. Yatsenko

The article deals with the history of the study and the current state of research of physiological and biochemical properties of the plant genus Sedum that are useful for human and has been used in folk medicine for many years. It was noticed that antioxidant properties of extracts from plants S. sarmentosum, S. sempervivoides, S. takesimense were caused by the presence of phenolic compounds. Methanol extract of plants S. takesimense exhibited strong scavenging activities against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and superoxide radicals as well as significant inhibitory effects on lipid peroxidation and low density lipoprotein (LDL) oxidation induced by a metal ion Cu2+. Various immunomodulatory activities of various fractions of plants extracts (S. dendroideum, S. kamtschaticum, S. sarmentosum, S. telephium) are observed. It was shown that the ethanol extract of S. sarmentosum and it’s fractions suppressed specific antibody and cellular responses to ovalbumin in mice. The methanol extract of plants S. sarmentosum reduced the levels of anti-inflammatory markers, such as volume of exudates, number of polymorphonuclear leukocytes, suppressed nitric oxide synthesis in activated macrophages via suppressed induction of inducible nitric oxide synthase (iNOS). Polysaccharides fractions from plants S. telephium inducing productions of tumor necrosis factor alpha (TNF-α), increasing the intensity of phagocytosis in vitro and in vivo. Methanol extract from the whole part of S. kamtschaticum strongly inhibit PGE2 production from lipopolysaccharide-induced RAW 264.7 cells, a mouse macrophage cell line via modulating activity in gene expression of the enzyme cyclooxygenase-2 (COX-2). The methanol extract of plants S. sarmentosum and the major kaempferol glycosides from S. dendroideum have antinociceptive activity. It was noticed that anti-adipogenic activity of extracts from plants S. kamtschaticum were caused by inhibition of peroxisome-proliferator-activated receptor γ (PPARγ) expression and it’s dependent target genes, such as genes encoding adipocyte protein 2 (аР2), lipoprotein lipase (LPL), adiponectin and CD36. Polysaccharides fractions from S. telephium cause inhibition of cell adhesion of human fibroblast (MRC5) to laminin and fibronectin via interfere with integrin-mediated cell behaviour and they contributed to the role of polysaccharides in cell-matrix interaction. The methanol extract of plants S. sarmentosum exhibited a significant inhibitory activity in the chick embryo chorioallantoic membrane angiogenesis in a dose-dependent manner. The crude alkaloid fraction of S. sarmentosum caused a dose-dependent inhibition of cell proliferation on murine hepatoma cell line BNL CL.2 and human hepatoma cell line HepG2 without necrosis or apoptosis. Alkaloids from plants S. sarmentosum may improve survival of hepatoma patients via the inhibition of excessive growth of tumor cells. Plant’s juices have antiviral activity (S. sarmentosum, S. spurium, S. stahlii). Crude ethanol extract S. praealtum have spermicidal activity of the in mice and a relevant inhibitory effect of aqueous extract on human spermatozoa motility as well as an anti-fertilizing activity in rats. Hepatoprotective triterpenes, e.g., δ-amyrone, 3-epi-δ-amyrin, δ-amyrin and sarmentolin were isolated from S. sarmentosum. 2- and 2,6-substituted piperidine alkaloids (e.g., norsedamine, allosedridine, sedamine, allosedamine) are observed in plants S. acre, which in the presence of data on the use of pyridine and piperidine derivatives for treating neurodegenerative diseases (e.g., Alzheimer's disease), points on the promising research in this area. Taking into account that biologically active compounds are accumulated in the aboveground vegetative organs of plants of Sedum, the prospects of further study of the use of Sedum for the purposes of biotechnology and in the pharmaceutical industry becomes apparent. This work extends the existing views regarding the use of plants Sedum.


1986 ◽  
Vol 109 (1) ◽  
pp. 111-117 ◽  
Author(s):  
F. F. G. Rommerts ◽  
J. W. Hoogerbrugge ◽  
H. J. van der Molen

ABSTRACT After the addition of charcoal-treated testicular fluid to Leydig cells isolated from 22-day-old rats, pregnenolone production could be increased to a maximum of tenfold within 30 min in a dose-dependent manner. Testicular fluid, but not serum, further increased pregnenolone formation threefold when pregnenolone production by Leydig cells was stimulated by the addition of LH-releasing hormone (fourfold), LH (25-fold) and 22R-hydroxycholesterol (300-fold). The effect of testicular fluid on steroid production in the presence of 22R-hydroxycholesterol was not inhibited by cycloheximide whereas cycloheximide completely inhibited the effect of LH. It appears unlikely that steroids, lipoproteins or other plasma components constitute the stimulatory agents in testicular fluid. The biologically active principles may be locally produced factors with a molecular weight > 25 000. Similar biological activities could be shown in testicular lymph from boars but not in systemic lymph from boars nor in charcoal-treated bovine follicular fluid. The presumably locally produced factor(s) may amplify the effect of LH and can thus act as a local modulator(s). J. Endocr. (1986) 109, 111–117


Antioxidants ◽  
2020 ◽  
Vol 9 (5) ◽  
pp. 455 ◽  
Author(s):  
Simona Dobiasová ◽  
Kateřina Řehořová ◽  
Denisa Kučerová ◽  
David Biedermann ◽  
Kristýna Káňová ◽  
...  

Silybin is considered to be the main biologically active component of silymarin. Its oxidized derivative 2,3-dehydrosilybin typically occurs in silymarin in small, but non-negligible amounts (up to 3%). Here, we investigated in detail complex biological activities of silybin and 2,3-dehydrosilybin optical isomers. Antioxidant activities of pure stereomers A and B of silybin and 2,3-dehydrosilybin, as well as their racemic mixtures, were investigated by using oxygen radical absorption capacity (ORAC) and cellular antioxidant activity (CAA) assay. All substances efficiently reduced nitric oxide production and cytokines (TNF-α, IL-6) release in a dose-dependent manner. Multidrug resistance (MDR) modulating potential was evaluated as inhibition of P-glycoprotein (P-gp) ATPase activity and regulation of ATP-binding cassette (ABC) protein expression. All the tested compounds showed strong dose-dependent inhibition of P-gp pump. Moreover, 2,3-dehydrosilybin A (30 µM) displayed the strongest sensitization of doxorubicin-resistant ovarian carcinoma. Despite these significant effects, silybin B was the only compound acting directly upon P-gp in vitro and also downregulating the expression of respective MDR genes. This compound altered the expression of P-glycoprotein (P-gp, ABCB1), multidrug resistance-associated protein 1 (MRP1, ABCC1) and breast cancer resistance protein (BCRP, ABCG2). 2,3-Dehydrosilybin AB exhibited the most effective inhibition of acetylcholinesterase activity. We can clearly postulate that silybin derivatives could serve well as modulators of a cancer drug-resistant phenotype.


2019 ◽  
Vol 47 (2) ◽  
pp. 253-262
Author(s):  
Umme Habiba ◽  
W Islam ◽  
Selina Parween

The present study was planned to evaluate the effect of spinosad on the survivability and development of Sitophilus oryzae on four wheat varieties viz., BARI-26, BARI-28, Shatabdi-21 and Prodip-24. Three doses in three replications for spinosad were applied to four wheat varieties. Spinosad concentrations significantly increased the total developmental period compared to the control in a dose-dependent manner on four wheat varieties. The highest developmental period took 41.67 ± 0.33 days to become adult was recorded in S-21 at 0.0003 μl/g of spinosad in F1. All adults of F1 did not reach in F2 because surprisingly all adults died after emergence. So, no developmental period was found in S-21 (0.00±0.00) and B-28 (0.00 ± 0.00) days at 0.0003 μl/g spinosad in F2. On the other hand, five mated females were released on the treated wheat with different concentrations of spinosad for 10 - 15 days; then they were removed. Treated wheat was checked for up to 30 to 60 days and observed the progeny for two successive generations (1st and 2nd). Each combination of insect species, insecticide rate, and exposure duration were replicated three times. Among four wheat varieties, the lowest adult emergence was recorded as 08.00 ± 0.58 in F1 and totally controlled in F2 generation in S-21 variety at 0.0003 μl/g. Spinosad concentrations significantly increased the total developmental period compared to the control in a dosedependent manner on four wheat varieties. Bangladesh J. Zool. 47(2): 253-262, 2019


2001 ◽  
Vol 280 (3) ◽  
pp. L421-L431 ◽  
Author(s):  
Ushma Savla ◽  
Heidi J. Appel ◽  
Peter H. S. Sporn ◽  
Christopher M. Waters

Repair of the airway epithelium after injury is critical for the maintenance of barrier function and the limitation of airway hyperreactivity. Airway epithelial cells (AECs) metabolize arachidonic acid to biologically active eicosanoids via the enzyme cyclooxygenase (COX). We investigated whether stimulating or inhibiting COX metabolites would affect wound closure in monolayers of cultured AECs. Inhibiting COX with indomethacin resulted in a dose-dependent inhibition of wound closure in human and feline AECs. Specific inhibitors for both COX-1 and COX-2 isoforms impaired wound healing. Inhibitors of 5-lipoxygenase did not affect wound closure in these cells. The addition of prostaglandin E2(PGE2) eliminated the inhibition due to indomethacin treatment, and the exogenous application of PGE2stimulated wound closure in a dose-dependent manner. Inhibition of COX with indomethacin only at initial time points resulted in a sustained inhibition of wound closure, indicating that prostanoids are involved in early wound repair processes such as spreading and migration. These differences in wound closure may be important if arachidonic acid metabolism and eicosanoid concentrations are altered in disease states such as asthma.


1988 ◽  
Vol 254 (3) ◽  
pp. G300-G306
Author(s):  
D. A. Dartt ◽  
M. Shulman ◽  
K. L. Gray ◽  
S. R. Rossi ◽  
C. Matkin ◽  
...  

To determine whether biologically active peptides can stimulate lacrimal gland secretion, we measured fluid and protein secretion from the cannulated lacrimal gland excretory duct of anesthetized rabbits after arterial injection of various peptides. Vasoactive intestinal peptide (VIP, 0.003-3 nmol) and porcine histidine isoleucine-containing peptide (PHI, 0.01-3 nmol) stimulated fluid and protein secretion in a dose-dependent manner. Cholecystokinin octapeptide (CCK-8, 0.01-3 nmol) stimulated fluid but not protein secretion. Neither bombesin nor eledoisin in doses as high as 3 nmol stimulated fluid or protein secretion. When combinations of high or low doses of VIP and the cholinergic agonist acetylcholine (ACh) were injected simultaneously, fluid and protein secretion was additive. We concluded that VIP and PHI stimulated secretion of lacrimal gland fluid and protein, CCK-8 stimulated secretion of fluid, and bombesin and eledoisin did not stimulate either fluid or protein secretion. VIP and ACh, both found in lacrimal gland nerve endings, stimulate lacrimal gland fluid and protein secretion by separate pathways.


2015 ◽  
Vol 309 (5) ◽  
pp. H835-H843 ◽  
Author(s):  
Ryan C. Jupiter ◽  
Daniel Yoo ◽  
Edward A. Pankey ◽  
Vishwaradh V. G. Reddy ◽  
Justin A. Edward ◽  
...  

Hydrogen sulfide (H2S) is a biologically active endogenous gasotransmitter formed in penile tissue that has been shown to relax isolated cavernosal smooth muscle. In the present study, erectile responses to the H2S donors sodium sulfide (Na2S) and sodium hydrosulfide (NaHS) were investigated in the anesthetized rat. Intracavernosal injections of Na2S in doses of 0.03–1 mg/kg increased intracavernosal pressure and transiently decreased mean arterial pressure in a dose-dependent manner. Blood pressure responses to Na2S were rapid in onset and short in duration. Responses to Na2S and NaHS were similar at doses up to 0.3 mg/kg, after which a plateau in the erectile response to NaHS was reached. Increases in intracavernosal pressure in response to Na2S were attenuated by tetraethylammonium (K+ channel inhibitor) and iberiotoxin (large-conductance Ca2+-activated K+ channel inhibitor), whereas glybenclamide [ATP-sensitive K+ (KATP) channel inhibitor] and inhibitors of nitric oxide (NO) synthase, cyclooxygenase, and cytochrome P-450 epoxygenase had no effect. These data indicate that erectile responses to Na2S are mediated by a tetraethylammonium- and iberiotoxin-sensitive mechanism and that KATP channels, NO, or arachidonic acid metabolites are not involved. Na2S did not alter erectile responses to sodium nitroprusside (NO donor) or cavernosal nerve stimulation, indicating that neither NO nor cGMP metabolism are altered. Thus, Na2S has erectile activity mediated by large-conductance Ca2+-activated K+ channels. It is suggested that strategies that increase H2S formation in penile tissue may be useful in the treatment of erectile dysfunction when NO bioavailability, KATP channel function, or poor responses to PGE1 are present.


2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Jnyanaranjan Panda ◽  
Biswa Mohan Sahoo ◽  
Nikunja Kishor Mishra ◽  
Sai Krushna Padhi ◽  
Jitendriya Mishra

A simple and efficient method has been developed for the synthesis of 1,3-dihydro-2H-indol-2-one derivatives using microwave irradiation technique. By taking advantage of the efficient source of energy of microwave, compound libraries for lead generation and optimization can be assembled in a fraction of time. In the present work, first the Schiff’s bases are synthesized by reaction of isatin with substituted anilines in the presence of acetic acid under microwave heating. Then the condensation of Schiff bases with different secondary amines in the presence of formaldehyde produces Mannich bases. The newly synthesized Mannich bases were characterized by means of spectral data and then evaluated for anthelmintic activity againstPheretima posthuma(Indian earthworm) and compared with standard albendazole. The compounds were evaluated at the concentrations of 10, 20, and 50 mg/mL. The effect of the standard drug albendazole at 10 mg/mL was also evaluated. The results of the present study indicate that some of the test compounds significantly demonstrated paralysis and also caused death of worms in a dose-dependent manner.


1984 ◽  
Vol 247 (6) ◽  
pp. G623-G631 ◽  
Author(s):  
C. S. Hyun ◽  
G. A. Kimmich

The interaction of biologically active 125I-labeled cholera toxin with isolated chick intestinal epithelial cells involves a large number (approx 1.7 10(6)/cell) of high-affinity (Kd = 8–9 X 10(-9) M) binding sites that belong to a single class. Binding of iodotoxin to the cells occurs rapidly, is half-maximal within 1 min, and is complete in 3–7 min (at 37 degrees C) depending on the toxin concentration. Toxin binding is saturable and includes only a small contribution from nonspecific sites. Ligand competition studies suggest that the isolated B subunit of choleragen (CT-B) behaves in an almost identical fashion to the holotoxin (CT), whereas the A subunit shows no detectable activity in competitive binding. Assays for cAMP indicate that neither that A nor the B subunits of CT contain any activity for increasing the level of intracellular cAMP. B subunit, when incubated with CT, inhibits CT-induced elevation of cAMP in a dose-dependent manner. Preincubation of 125I-CT with various concentrations of ganglioside GM1 also shows a dose-dependent inhibitory effect on the binding activity of the toxin. Pretreatment of CT with increasing concentrations of GM1 results in a progressive decrease in toxin-induced formation of cAMP. Escherichia coli heat-labile enterotoxin, which is known to alter intestinal function via a mechanism similar to that of CT, has binding and biological effects very similar to thoseof CT.


2016 ◽  
Vol 35 (12) ◽  
pp. 1264-1275 ◽  
Author(s):  
S Sharma ◽  
S Rana ◽  
V Patial ◽  
M Gupta ◽  
S Bhushan ◽  
...  

Industrial apple pomace, a biowaste generated during apple processing, is rich in cell wall polysaccharides and phenolics. These biologically active compounds are reported to be highly beneficial from the nutritional and health point of view. In the present study, the total phenolic content in the apple pomace aqueous extract (APE) was estimated and evaluated for its possible antioxidant and hepatoprotective efficacy in carbon tetrachloride (CCl4)-induced liver injury mice model. The aqueous extract exhibited 2,2-diphenyl-2-picrylhydrazyl free radical scavenging activity in vitro. Under in vivo study, mice were treated with APE (200 mg and 400 mg/kg body weight) for 2 weeks prior to the administration of CCl4 (30% v/v). The serum liver injury markers alanine transaminase, aspartate transaminase, and alkaline phosphatase were significantly lowered by APE in a dose-dependent manner. The levels of antioxidant parameters superoxide dismutase (SOD), reduced glutathione (redGSH), and lipid peroxidation were also improved by APE in liver homogenate. Histopathological studies revealed that APE treatment significantly lowered the CCl4-induced necrotic changes in the liver. Furthermore, terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick end-labeling assay showed that CCl4-induced apoptosis in the liver was significantly inhibited by APE in a dose-dependent manner. Immunohistochemistry results showed higher expression of nuclear erythroid 2-related factor 2 (Nrf2) in the liver of the APE-treated mice, a key regulator of antioxidative response. In conclusion, the results of the present study revealed the hepatoprotective efficacy of APE by inhibiting CCl4-induced apoptosis, which is due to its antioxidant activity and the ability to induce Nrf2 protein expression.


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