Antagonistic control of fluid secretion by the Malpighian tubules ofTenebrio molitor: effects of diuretic and antidiuretic peptides and their second messengers

2002 ◽  
Vol 205 (4) ◽  
pp. 493-501 ◽  
Author(s):  
U. I. M. Wiehart ◽  
S. W. Nicolson ◽  
R. A. Eigenheer ◽  
D. A. Schooley
Keyword(s):  
Cyclic Amp ◽  
Cyclic Gmp ◽  
Second Messengers ◽  
Fluid Secretion ◽  
Tenebrio Molitor ◽  
Inhibitory Effect ◽  
Malpighian Tubules ◽  
Dependent Manner ◽  
Response Curves

SUMMARYFluid secretion by insect Malpighian tubules is controlled by haemolymph-borne factors. The mealworm Tenebrio molitor provides the first known example of antagonistic interactions between endogenous neuropeptides acting on Malpighian tubules. The two corticotropin-releasing-factor (CRF)-related diuretic peptides previously isolated from Tenebrio molitor, Tenmo-DH37 and Tenmo-DH47, were found to stimulate Tenebrio molitor tubules in vitro in a dose-dependent manner with EC50 values of 0.12 nmol l–1 and 26 nmol l–1 respectively. However, no synergistic or additive effect was observed when these two peptides were tested simultaneously. We then investigated antagonism between second messengers: dose–response curves were constructed for stimulation of Tenebrio molitor tubules by cyclic AMP and their inhibition by cyclic GMP. When both cyclic nucleotides were included in the bathing Ringer, the stimulatory effect of cyclic AMP was neutralised by cyclic GMP. Similarly, the stimulatory effect of Tenmo-DH37 was reversed on addition of an antidiuretic peptide (Tenmo-ADF), which was recently isolated from Tenebrio molitor and acts via cyclic GMP. The cardioacceleratory peptide CAP2b, originally isolated from Manduca sexta, also increases intracellular cyclic GMP levels and inhibited fluid secretion by Tenebrio molitor tubules, with an EC50 value of 85 nmol l–1. This inhibitory effect was reversed by Tenmo-DH37. Endogenous diuretic and antidiuretic peptides, effective at low concentrations and acting via antagonistic second messengers, have the potential for fine control of secretion rates in the Malpighian tubules of Tenebrio molitor.

Effect of Cyclic AMP and Cyclic GMP on Thromboplastin (Factor III) Synthesis in Human Monocytes In Vitro

1983 ◽  
Vol 50 (04) ◽  
pp. 804-809 ◽  
Author(s):  
Torstein Lyberg
Keyword(s):  
Cyclic Amp ◽  
Cyclic Gmp ◽  
Immune Complexes ◽  
Phosphodiesterase Inhibitors ◽  
Inhibitory Effect ◽  
Intracellular Camp ◽  
Human Monocytes ◽  
Purified Protein Derivative ◽  
A 23187

SummaryHuman monocytes in vitro respond to various agents (immune complexes, lectins, endotoxin, the divalent ionophore A 23187, 12-0-tetradecanoyl-phorbol 13-acetate [TPA], purified protein derivative [PPD] of Bacille Calmette-Guerin) with an increased synthesis of the protein component of thromboplastin. The effect of cyclic AMP and cyclic GMP on this response has been studied. Dibutyryl-cyclic AMP, prostaglandin E1 and the phosphodiesterase inhibitors 3-butyl-1-methyl-xanthine (MIX) and rac -4-(3-butoxy-4-methoxybenzyl)-2-imidazolidinone (Ro 201724), separately and in combination have a pronounced inhibitory effect on the response to immune complexes and PPD, and a moderate effect on the response to endotoxin and lectins. The effect on TPA response and on the response to A 23187 was slight. Dibutyryl-cyclic GMP (1 mM) gave a slight inhibition of the TPA arid IC response, but had essentially no effect on the response to other inducers. The intracellular cAMP level increased when monocytes were incubated with IC, TPA or A 23187 followed by a decrease to basal levels within 1-2 hr, whereas lectin (PHA) and PPD did not induce such changes. The cAMP response to endotoxin varied. Stimulation with IC induced an increase in monocyte cGMP levels, whereas the other stimulants did not cause such changes.

scholarly journals Excretion in the House Cricket (Acheta Domesticus): Stimulation of Diuresis by Tissue Homogenates

1987 ◽  
Vol 129 (1) ◽  
pp. 63-81 ◽  
Author(s):  
JEFFREY H. SPRING ◽  
SHELIA R. HAZELTON
Keyword(s):  
Lethal Dose ◽  
Fluid Secretion ◽  
Sodium Concentration ◽  
Inhibitory Effect ◽  
Acheta Domesticus ◽  
Malpighian Tubules ◽  
Secretion Rate ◽  
Tissue Homogenates ◽  
Extreme Sensitivity

1. A new method is described for maintaining cricket Malpighian tubules in vitro. Warmed, oxygenated saline is circulated rapidly past the tubules, while the secreted urine is collected under oil for analysis. This technique allows the cricket tubules to be observed and manipulated for extended periods (6 h), in contrast to their short life (>1 h) using conventional methods. 2. Cricket tubules show extreme sensitivity to oxygen deprivation, such that 15 min of anoxia represents the median lethal dose (LD50) for in vitro preparations. 3. Homogenates of corpus cardiacum (CC) cause the rate of fluid secretion by the tubules to double. The maximum stimulation is dose-dependent over the range 0.01 to 1.0 CC. Homogenates of brain and other ganglia show much smaller stimulatory effects (0.01-0.02 CC-equivalents). Cyclic AMP mimics the increase in secretion rate, but has an inhibitory effect on the smooth muscle of the ureter. 4. Control preparations maintain a urine osmotic pressure (OP) that is hyperosmotic to the bath by 5–10 mosmol l−1. CC homogenate produces a decrease in urine OP to 10–12 mosmol l−1 hypo-osmotic to the bath. This suggests that active solute reabsorption is occurring in the lower tubule or ampulla. 5. Stimulation by CC homogenate increases the urine potassium concentration slightly less than two-fold, whereas the sodium concentration increases by a maximum of five-fold and remains at a higher concentration than potassium throughout the experiment. Tubule secretion rate is drastically inhibited in nominally sodium-free saline.

In vitro myometrial inhibition by the partitioned aqueous fraction of Anthocleista djalonensis leaves

2010 ◽  
Vol 88 (9) ◽  
pp. 880-887
Author(s):  
Enitome Evi Bafor ◽  
Lucky Osaro Okunrobo
Keyword(s):  
Uterine Contraction ◽  
Calcium Influx ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Response Curves ◽  
Concentration Dependent Manner ◽  
Aqueous Fraction ◽  
Uterine Contractions ◽  
Β Adrenergic Receptors

This study investigated the effect on the uterus of the aqueous fraction of the partitioned methanol crude extract of the leaves of Anthocleista djalonensis (AD) and the possible mechanism of AD activity. AD inhibited the concentration–response curves induced by oxytocin and CaCl2 on the rat uterus in vitro and significantly reduced the EC50 in a concentration-dependent manner (p < 0.05). A similar effect was observed with salbutamol and verapamil on the concentration–response curves obtained for oxytocin and CaCl2. The inhibitory effect of AD was not attenuated in the presence of propranolol. AD, salbutamol, and verapamil also produced a concentration-dependent relaxation on K+-induced sustained uterine contraction. In Ca2+-free medium, AD and salbutamol similarly inhibited oxytocin-induced contraction, but verapamil failed to produce this effect. The present results suggest that AD, being a mixture of phytochemicals, probably exerts inhibitory activity on in vitro uterine contractions of the nonpregnant, diethylstilboestrol-treated rat by multiple mechanisms that do not involve interaction with β-adrenergic receptors and do not solely depend on inhibition of calcium influx.

ABILITY OF VARIOUS FACTORS TO OPPOSE THE STIMULATORY EFFECT OF DIBUTYRYL CYCLIC AMP ON THE RELEASE OF MELANOCYTE-STIMULATING HORMONE BY THE RAT PITUITARY IN VITRO

1976 ◽  
Vol 68 (2) ◽  
pp. 283-287 ◽  
Author(s):  
BRIDGET I. BAKER
Keyword(s):  
Cyclic Amp ◽  
Cyclic Gmp ◽  
Inhibitory Effect ◽  
Aminobutyric Acid ◽  
Intermediate Lobe ◽  
Dibutyryl Cyclic Amp ◽  
Melanocyte Stimulating Hormone ◽  
Rat Pituitary ◽  
Stimulating Hormone

SUMMARY Various agents were tested for their ability to oppose the stimulatory effect of dibutyryl cyclic AMP on the release of the melanocyte-stimulating hormone from the rat neuro-intermediate lobe in vitro. Only dopamine exhibited an inhibitory effect; serotonin, γ-aminobutyric acid, tocinoic acid, tocinamide, the tripeptide Pro-Leu-Gly-NH2 and dibutyryl cyclic GMP were all ineffective.

scholarly journals SYNERGISM OF HORMONES CONTROLLING EPITHELIAL FLUID TRANSPORT IN AN INSECT

1993 ◽  
Vol 174 (1) ◽  
pp. 65-80 ◽  
Author(s):  
S. H. P. Maddrell ◽  
W. S. Herman ◽  
J. A. Farndale ◽  
J A Riegel
Keyword(s):  
Adenylate Cyclase ◽  
Fluid Transport ◽  
Fluid Secretion ◽  
Rapid Onset ◽  
Threshold Concentration ◽  
Malpighian Tubules ◽  
Dependent Manner ◽  
Response Curves ◽  
Diuretic Hormone ◽  
Dose Dependent

Forskolin stimulates rapid fluid secretion by the Malpighian tubules of Rhodnius prolixus at concentrations above 5x10–6 mol l-1. In the presence of a threshold concentration of forskolin, the tubules are 30–50 times more sensitive to 5-hydroxytryptamine (5-HT) than in its absence. Similar synergism is seen between 5-HT and extracts of the mesothoracic ganglionic mass (which is rich in the peptide diuretic hormone, DH) and between 5-HT and samples of haemolymph, also rich in peptide DH, from fed insects 1–2 h after feeding. The dose-response curves for mixtures of forskolin and 5-HT and of peptide DH and 5-HT are all very steep, approximately five times steeper than for any one stimulant alone. Forskolin, 5-HT and extracts of the ganglionic mass all stimulated adenylate cyclase from broken membrane preparations from the Malpighian tubules in a dose-dependent manner and at doses similar to those required to stimulate fluid secretion by intact tubules. Mixtures of ganglionic extract and 5- HT stimulated adenylate cyclase activity in a synergistic fashion. Injections into fifth-instar Rhodnius, 24 h before feeding, of 5,7-dihydroxytryptamine, which is known to block or reduce 5-HT release, caused delays in the onset of the consequent diuresis or prevented it altogether. This is consistent with the proposal that the rapid onset of diuresis after feeding is caused by the simultaneous release of 5-HT and peptide DH acting synergistically.

scholarly journals Effect of Manduca Sexta Diuretic Hormone and related Peptides on isolated Malpigfflan Tubules of the House Cricket Acheta Domesticus (L.)

1992 ◽  
Vol 162 (1) ◽  
pp. 331-338
Author(s):  
GEOFFREY M. COAST ◽  
TIMOTHY K. HAYES ◽  
IAIN KAY ◽  
JUM-SOOK CHUNG
Keyword(s):  
Cyclic Amp ◽  
Manduca Sexta ◽  
Pieris Rapae ◽  
Fluid Secretion ◽  
Acheta Domesticus ◽  
Malpighian Tubules ◽  
In Vivo Studies ◽  
Methionine Residues

Previously, a corticotropin releasing factor (CRF)-like diuretic peptide (Manduca-DH) has been isolated from Manduca sexta and shown to stimulate fluid excretion in vivo in post-eclosion Pieris rapae adults and in pre-wandering postfeeding Manduca sexta larvae. However, Manduca- DH was reported to have no effect on Malpighian tubules in vitro. Manduca-DH and [Nle2,11]-Manduca-DH were synthesized in Texas and assayed in London on isolated Malpighian tubules of Acheta domesticus. Manduca- DH stimulated fluid secretion by about 60% of the maximum response achievable with extracts of corpora cardiaca and increased the production of cyclic AMP. In combination with 10−4 mol l−1 3-isobutyl-l-methyl xanthine (IBMX), Manduca-DH stimulated maximal secretion. A number of CRF-related peptides also stimulated fluid secretion and cyclic AMP production in cricket tubules, and the CRF antagonist α-helical-CRF[9-14] blocked the stimulation of fluid secretion by Manduca-DH. [Nle2,11]-Manduca-DH was more active than Manduca-DH in both assays, suggesting that methionine residues in the natural peptide may become oxidized. Taken in conjunction with previous in vivo studies, the present findings suggest that a Manduca-DH-Mke diuretic peptide is the hormone controlling post-eclosion diuresis in butterflies, and Manduca-DH was shown to stimulate both fluid secretion and cyclic AMP production in Malpighian tubules from 1–12 h posteclosion Pieris rapae adults. The function of the peptide in Manduca sexta is discussed.

scholarly journals Changes in cyclic AMP and cyclic GMP concentrations during the action of 5-hydroxytryptamine on an insect salivary gland

1980 ◽  
Vol 192 (1) ◽  
pp. 247-255 ◽  
Author(s):  
J P Heslop ◽  
M J Berridge
Keyword(s):  
Salivary Gland ◽  
Cyclic Amp ◽  
Cyclic Gmp ◽  
Time Course ◽  
Phosphodiesterase Inhibitor ◽  
Fluid Secretion ◽  
Fast Response ◽  
Bathing Medium ◽  
Calliphora Erythrocephala

Salivary glands from adult blowflies (Calliphora erythrocephala Meigen) were studied in vitro. The time course of changes in cyclic AMP content of the glands was followed at different concentration of 5-hydroxytryptamine. There was an immediate biphasic rise and fall in cyclic AMP content, following by a slower rise and subsequent gradual decline. The initial rise preceded the onset of fluid secretion by the glands. Rises in cyclic AMP content were inhibited by compound RMI 12330 A (an adenylate cyclase inhibitor) and were halted after about 15-20s if the glands were deprived of Ca2+. Theophylline (a phosphodiesterase inhibitor) abolished the decline phase of the fast response, Losses of cyclic AMP from the glands either to the bathing medium or to the saliva were small and could not account for the rapid fall found. Evidence is presented that cyclic GMP is not involved in the process of initiating secretion in the blowfly salivary gland.

scholarly journals THE EFFECTS OF ACHETA DIURETIC PEPTIDE ON ISOLATED MALPIGHIAN TUBULES FROM THE HOUSE CRICKET ACHETA DOMESTICUS

1994 ◽  
Vol 187 (1) ◽  
pp. 225-243 ◽  
Author(s):  
G M Coast ◽  
I Kay
Keyword(s):  
Cyclic Amp ◽  
Unit Length ◽  
Phosphodiesterase Inhibitor ◽  
Fluid Secretion ◽  
Acheta Domesticus ◽  
Malpighian Tubules ◽  
Membrane Receptors ◽  
Dependent Manner ◽  
House Cricket ◽  
Dose Dependent

Acheta diuretic peptide (Acheta-DP) is a corticotropin-releasing factor (CRF)-related peptide found in head extracts of the house cricket Acheta domesticus. The peptide causes a dose-dependent increase in fluid secretion by cricket Malpighian tubules isolated in vitro, and the apparent EC50 is 1.3 nmol l-1, which is within the physiological range for a peptide hormone. The CRF antagonist alpha-helical CRF(9-41) blocks the action of Acheta-DP in a dose-dependent manner, and the IC50 is estimated to be in the micromolar range. Addition of Acheta-DP to isolated Malpighian tubules is followed by a rapid and marked increase in the level of intracellular cyclic AMP. This precedes any change in voltage or fluid secretion, which strongly suggests that cyclic AMP is the intracellular mediator of Acheta-DP activity. Consistent with this, diuretic activity is potentiated by the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine, and there is a close relationship between the dose&shy;response curves for cyclic AMP production and for fluid secretion. However, exogenous 8-bromo-cyclic AMP does not mimic all the effects of Acheta-DP, and the peptide may have a dual action on isolated tubules. Fluid secretion by tubules dosed repeatedly with Acheta-DP returns to near basal levels after 3&shy;5 h. This cannot be explained by degradation of the peptide, but might be due in part to oxygen and/or metabolite deficiency. However, tubules that are refractory to Acheta-DP can be stimulated by forskolin, 8-bromo-cyclic AMP and extracts of corpora cardiaca, which is indicative of a homologous desensitization of membrane receptors for the diuretic peptide. Differences in the rate of secretion by morphologically distinct regions of cricket Malpighian tubules have been assessed. In unstimulated tubules, the rate of secretion per unit length by the short distal segment is about twice that of the main tubule. However, diuretic peptides (Acheta-DP and achetakinin-I) have little effect on distal tubule secretion, but evoke a two- to fourfold increase in fluid secretion by the main tubule segment.

In Vitro Effects of Ethanol on Rabbit Platelet Aggregation, Secretion of Granule Contents, and Cyclic AMP Levels in the Presence of Prostacyclin

1989 ◽  
Vol 61 (02) ◽  
pp. 254-258 ◽  
Author(s):  
Margaret L Rand ◽  
Peter L Gross ◽  
Donna M Jakowec ◽  
Marian A Packham ◽  
J Fraser Mustard
Keyword(s):  
Cyclic Amp ◽  
Inhibitory Effect ◽  
Rabbit Platelet ◽  
Inhibitory Effects ◽  
Low Concentrations ◽  
Rabbit Platelets ◽  
High Concentrations ◽  
In Vitro Effects ◽  
Aggregation Of Platelets

SummaryEthanol, at physiologically tolerable concentrations, inhibits platelet responses to low concentrations of collagen or thrombin, but does not inhibit responses of washed rabbit platelets stimulated with high concentrations of ADP, collagen, or thrombin. However, when platelet responses to high concentrations of collagen or thrombin had been partially inhibited by prostacyclin (PGI2), ethanol had additional inhibitory effects on aggregation and secretion. These effects were also observed with aspirin- treated platelets stimulated with thrombin. Ethanol had no further inhibitory effect on aggregation of platelets stimulated with ADP, or the combination of ADP and epinephrine. Thus, the inhibitory effects of ethanol on platelet responses in the presence of PGI2 were very similar to its inhibitory effects in the absence of PGI2, when platelets were stimulated with lower concentrations of collagen or thrombin. Ethanol did not appear to exert its inhibitory effects by increasing cyclic AMP above basal levels and the additional inhibitory effects of ethanol in the presence of PGI2 did not appear to be brought about by further increases in platelet cyclic AMP levels.

scholarly journals In vitro study on the effect of cornin on the activity of cytochrome P450 enzymes

2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Qun Zhang ◽  
Zengqiang Qu ◽  
Yanqing Zhou ◽  
Jin Zhou ◽  
Junwei Yang ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Drug Interaction ◽  
Liver Microsomes ◽  
In Vitro Study ◽  
Inhibitory Effect ◽  
Dependent Manner ◽  
Cytochrome P450 Enzymes ◽  
Drug Drug Interaction ◽  
Dose Dependent

Abstract Background Cornin is a commonly used herb in cardiology for its cardioprotective effect. The effect of herbs on the activity of cytochrome P450 enzymes (CYP450s) can induce adverse drug-drug interaction even treatment failure. Therefore, it is necessary to investigate the effect of cornin on the activity of CYP450s, which can provide more guidance for the clinical application of cornin. Methods Cornin (100 μM) was incubated with eight isoforms of CYP450s, including CYP1A2, 2A6, 3A4, 2C8, 2C9, 2C19, 2D6, and 2E1, in pooled human liver microsomes. The inhibition model and corresponding parameters were also investigated. Results Cornin exerted significant inhibitory effect on the activity of CYP3A4, 2C9, and 2E1 in a dose-dependent manner with the IC50 values of 9.20, 22.91, and 14.28 μM, respectively (p < 0.05). Cornin inhibited the activity of CYP3A4 non-competitively with the Ki value of 4.69 μM, while the inhibition of CYP2C9 and 2E1 by cornin was competitive with the Ki value of 11.31 and 6.54 μM, respectively. Additionally, the inhibition of CYP3A4 by cornin was found to be time-dependent with the KI/Kinact value of 6.40/0.055 min− 1·μM− 1. Conclusions The inhibitory effect of cornin on the activity of CYP3A4, 2C9, and 2E1 indicated the potential drug-drug interaction between cornin and drugs metabolized by these CYP450s, which needs further investigation and validation.

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