Pharmacological evidence for the contribution of polyamines as mediators of the transcriptional component involved in smooth muscle relaxation elicited by forskolin

Revuelta, Manuel; Cantabrana, Begoña; Hidalgo, Agustı́n

doi:10.1016/s0024-3205(97)00979-x

Cited by 8 publications

(2 citation statements)

References 47 publications

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“…Further evidence indicates that some PDE-4 inhibitors could block the calcium influx, such as rolipram and the thalidomide analogs herein tested, because of their similar structure to nifedipine, verapamil and nicardipine, what leads to uterine relaxation [62935]; in fact, the present results again suggest that both analogs blocked the calcium influx. In sum, the results are in agreement with other reports where forskolin and rolipram [3637], as well as these thalidomide analogs cause uterine relaxation by increasing cAMP and perhaps by the novel mechanism of action of rolipram and thalidomide analogs as potential Ca 2+ -channel blockers [6]. …”

Section: Discussionsupporting

confidence: 92%

Relaxant and anti-inflammatory effect of two thalidomide analogs as PDE-4 inhibitors in pregnant rat uterus

Muñoz-Pérez

Fernández-Martínez

Ponce‐Monter

et al. 2017

Korean J Physiol Pharmacol

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The aim of this study was to evaluate the relaxant and anti-inflammatory effects of two thalidomide analogs as phosphodiesterase-4 (PDE-4) inhibitors in pregnant rat uterus. Uteri from Wistar female rats were isolated at 19 day of pregnancy. Uterine samples were used in functional studies to evaluate the inhibitory effects of the thalidomide analogs, methyl 3-(4-nitrophthalimido)-3-(3,4-dimethoxyphenyl)-propanoate (4NO2PDPMe) and methyl 3-(4-aminophthalimido)-3-(3,4-dimethoxyphenyl)-propanoate (4APDPMe), on prostaglandin-F2α (PGF2α)-induced phasic, K+-induced tonic, and Ca2+-induced contractions. Accumulation of cAMP was quantified in uterine homogenates by ELISA. Anti-inflammatory effect was assessed by using ELISA for determination of the pro-inflammatory cytokines tumor necrosis factor-α (TNFα) and interleukin (IL)-1β, and anti-inflammatory IL-10, from uterine explants stimulated with lipopolysaccharide (LPS). Nifedipine, forskolin and rolipram were used as positive controls where required. Both thalidomide analogs induced a significant inhibition of the uterine contractions induced by the pharmaco- and electro-mechanic stimuli. Nifedipine and forskolin were more potent than the analogs to inhibit the uterine contractility, but these were more potent than rolipram, and 4APDPMe was equieffective to nifedipine. Thalidomide analogs increased uterine cAMP-levels in a concentration-dependent manner. The LPS-induced TNFα and IL-1β uterine secretion was diminished in a concentration-dependent fashion by both analogs, whereas IL-10 secretion was increased significantly. The thalidomide analogs induced utero-relaxant and anti-inflammatory effects, which were associated with the increased cAMP levels as PDE-4 inhibitors in the pregnant rat uterus. Such properties place these thalidomide analogs as potentially safe and effective tocolytic agents in a field that urgently needs improved pharmacological treatments, as in cases of preterm labor.

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Section: Discussionsupporting

confidence: 92%

Relaxant and anti-inflammatory effect of two thalidomide analogs as PDE-4 inhibitors in pregnant rat uterus

Muñoz-Pérez

Fernández-Martínez

Ponce‐Monter

et al. 2017

Korean J Physiol Pharmacol

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“…The hypotensive effect induced by M. oleifera could be due to the presence of flavonoids. Indeed, many researchers indicated that flavonoids isolated from other medicinal plants possessed anti-calcium effects on different isolated organs (Revuelta et al, 1997;Gilani et al, 2007;Belemtougri et al, 2007) and showed hypotensive and vasodilator activities (Ajay et al, 2003). According to Kasolo (2010), flavonoids are present in the leaves of M. oleifera and it was possible that these compounds were present in our extract and lowered the blood pressure in vivo in our experiment.…”

Section: Discussionmentioning

confidence: 66%

Effects of Water Crude Leaf Extract of Moringa Oleifera Lam (Moringaceae) on Normotensive Rat Blood Pressure and Isolated Duodenum

Som¹,

Belemtougri²,

Ouédraogo³

et al. 2015

J. Phys. Pharm. Adv.

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Moringa oleifera is used in folk medicine for the treatment of many ailments among which, hypertension and intestinal disorders. The aim of this study was to investigate the hypotensive and/or antihypertensive activity of Moringa oleifera leaf extract on normotensive anaesthetized rats by direct measure of the arterial pression and in the other hand, to determine its antispasmodic effects on isolated rat duodenum. Intravenous administration of aqueous leaf extract of Moringa oleifera (EAMO 5mg/kg-75 mg/kg body weight), caused a transitory dose-dependent fail in the mean arterial blood pressure of normotensive anaesthetized rats (p< 0.05). Moreover, hypertensive arterial blood pressure induced by phenylephrine 100µg/kg rat body weight, was completely abolished by aqueous extract of Moringa oleifera 10mg-40mg/kg body weight. The studies on isolated rat duodenum smooth muscles demonstrated that the aqueous extract of Moringa oleifera produced a dose dependent relaxation of these muscles (p<0,05). The extract decreases the contractile effects of Ach on these tissues doses dependently. These results indicate that aqueous leaf extract of Moringa oleifera possesses hypotensive, antihypertensive activity on normotensive anaesthetized rats and antispasmodic effects on isolated duodenum smooth muscle. This result can explain the traditional use of Moringa oleifera leaf extracts in the treatment of hypertensive arterial blood pressure, diarrhea and dysentery.

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Mechanism of mifepristone-induced spasmolytic effect on isolated rat uterus

Parra¹,

Cantabrana²,

Hidalgo³

2000

Life Sciences

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Pharmacological evidence for the contribution of polyamines as mediators of the transcriptional component involved in smooth muscle relaxation elicited by forskolin

Cited by 8 publications

References 47 publications

Relaxant and anti-inflammatory effect of two thalidomide analogs as PDE-4 inhibitors in pregnant rat uterus

Relaxant and anti-inflammatory effect of two thalidomide analogs as PDE-4 inhibitors in pregnant rat uterus

Effects of Water Crude Leaf Extract of Moringa Oleifera Lam (Moringaceae) on Normotensive Rat Blood Pressure and Isolated Duodenum

Mechanism of mifepristone-induced spasmolytic effect on isolated rat uterus

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