scholarly journals Dryopteris filix-mas (Dryopteridaceae) leaves inhibit mouse uterine activity

2017 ◽  
Vol 1 (1) ◽  
Author(s):  
Enitome E. Bafor ◽  
Wellington O. Omokaro ◽  
Osamuyi H. Uwumarongie ◽  
Uloma B. Elvis-Offiah ◽  
Osemelomen Omoruyi ◽  
...  
Keyword(s):  
Plant Extract ◽  
Inhibitory Effect ◽  
Mass Spectrometric ◽  
Uterine Contractility ◽  
River Bank ◽  
Uterine Activity ◽  
Uterine Contractions ◽  
Free Media ◽  
Relaxing Effect

Background: The plant Dryopteris filix-mas has been used traditionally for its uterine-stimulant effects.Aim: The current study is therefore aimed at investigating and determining the effect of the leaves of D. filix-mas on uterine contractility in vitro.Setting: Fresh leaves of D. filix-mas were collected from a river bank in the south-western part of Nigeria.Methods: The leaves of D. filix-mas were cleaned, dried and extracted in methanol. The extract (0.07 µg/mL–21.0 µg/mL) was tested on the isolated mouse uteri in order to determine activity on spontaneous-induced uterine contractions. Subsequently the extract (0.005 mg/mL and 0.05 mg/mL) was tested on oxytocin-induced contraction (0.00017 ng/mL–4.98 ng/mL) in calcium-containing media, submaximal oxytocin-induced contraction (0.116 ng/mL) in calcium-free media and in the presence of high KCl-induced uterine contractions (80 mM). The extract was also subjected to mass spectrometric determination of secondary metabolites.Results: The plant extract inhibited spontaneous-induced contractions with IC50 amplitude = 658.41 ng/mL ± 0.11 ng/mL and IC50 frequency = 175.32 ng/mL ± 0.53 ng/mL. The plant extract inhibited oxytocin-induced and high KCl-induced uterine contractions (p < 0.01 at 0.5 mg/mL). The plant extract had no effect on oxytocin-induced contractions under calcium-free conditions. Secondary metabolites belonging to classes of fatty acids, alkaloids, saponin glycosides, amino acids, limonoids, terpenes and porphyrins were identified.Conclusion: The current study reports an inhibitory effect of the plant on uterine contractility in this study, suggesting possible application as a tocolytic or as a contraceptive, as most contraceptive plants have shown uterine-relaxing effect.

scholarly journals Development of a Rapid Mass Spectrometric Determination of AMP and Cyclic AMP for PDE3 Activity Study: Application and Computational Analysis for Evaluating the Effect of a Novel 2-oxo-1,2-dihydropyridine-3-carbonitrile Derivative as PDE-3 Inhibitor

Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1817 ◽  
Author(s):  
Ilaria Cicalini ◽  
Barbara De Filippis ◽  
Nicola Gambacorta ◽  
Antonio Di Michele ◽  
Silvia Valentinuzzi ◽  
...  
Keyword(s):  
Phosphodiesterase Inhibitor ◽  
Parent Drug ◽  
Cyclic Adenosine Monophosphate ◽  
Adenosine Monophosphate ◽  
Binding Mode ◽  
Inhibitory Effect ◽  
Docking Studies ◽  
Mass Spectrometric ◽  
Inhibitory Potential

A simple, quick, easy and cheap tandem mass spectrometry (MS/MS) method for the determination of adenosine monophosphate (AMP) and cyclic adenosine monophosphate (cAMP) has been newly developed. This novel MS/MS method was applied for the evaluation of the inhibitory effect of a novel 2-oxo-1,2-dihydropyridine-3-carbonitrile derivative, also named DF492, on PDE3 enzyme activity in comparison to its parent drug milrinone. Molecule DF492, with an IC50 of 409.5 nM, showed an inhibition of PDE3 greater than milrinone (IC50 = 703.1 nM). To explain the inhibitory potential of DF492, molecular docking studies toward the human PDE3A were carried out with the aim of predicting the binding mode of DF492. The presence of different bulkier decorating fragments in DF492 was pursued to shift affinity of this novel molecule toward PDE3A compared to milrinone in accordance with both the theoretical and experimental results. The described mass spectrometric approach could have a wider potential use in kinetic and biomedical studies and could be applied for the determination of other phosphodiesterase inhibitor molecules.

scholarly journals Progesterone decreases the relaxing effect of the β3-adrenergic receptor agonist BRL 37344 in the pregnant rat myometrium

Reproduction ◽  
2009 ◽  
Vol 138 (2) ◽  
pp. 383-390 ◽  
Author(s):  
Renáta Minorics ◽  
Róbert Gáspár ◽  
Adrienn Gál ◽  
Anna Klukovits ◽  
George Falkay
Keyword(s):  
Functional Activity ◽  
Contractile Activity ◽  
Relaxation Effect ◽  
Inhibitory Effect ◽  
Uterine Contractility ◽  
Pregnant Rats ◽  
Pregnant Rat ◽  
The Right ◽  
Brl 37344 ◽  
Relaxing Effect

Although the published results regarding the function of the β3-adrenergic receptors (β3-ARs) in the regulation of smooth muscle activity are very promising, the question of the mechanism of β3-ARs' action in the pregnant myometrium cannot be fully answered by human investigations. To assess whether it possesses an essential role in the regulation of uterine contractility in pregnant rats, as in humans, we performed functional, western blotting and molecular biology experiments on the late-pregnant rat myometrium. The influence of progesterone on the function of the β3-ARs was also investigated. We demonstrated the presence and the functional activity of the β3-ARs in the late-pregnant rat myometrium. The maximum dose-dependent uterus-relaxing effect of the selective β3-agonist BRL 37344 was recorded at the end of pregnancy in rats, similarly as in humans. The extent of its relaxing action was regarded as moderate. The expression of β3-AR protein and mRNA remained unchanged during the investigated period. The administration of progesterone had no effect on the β3-AR mRNA and protein expression or the maximum relaxation effect of BRL 37344, but shifted the dose–response curve to the right and decreased the synthesis of the second messenger, cAMP. It can be concluded that the β3-ARs play an additional role in the regulation of the contractile activity of the pregnant rat uterus. The inhibitory effect of progesterone on the functional activity of the β3-ARs may have important consequences in the case of human application if this effect is also demonstrated in pregnant human myometrial tissue.

scholarly journals Modulation of ex-vivo uterine contraction by the methanol leaf extract of Alchornea laxiflora Benth. (Euphorbiaceae) and preliminary spectrometric identification of associated secondary metabolites

2018 ◽  
Vol 2 (1) ◽  
Author(s):  
Enitome E. Bafor ◽  
Juliet K. Nwogu ◽  
Uloma B. Elvis-Offiah ◽  
Fabian Amaechina ◽  
Josephine Ofeimun ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Plant Extract ◽  
Uterine Contraction ◽  
Ex Vivo ◽  
Preterm Births ◽  
Flavonoid Glycosides ◽  
Spectrometric Analysis ◽  
Uterine Contractility ◽  
Benin City ◽  
Uterine Contractions

Background: The leaves of Alchornea laxiflora are traditionally used in the south of Nigeria to prevent preterm births. Aim: This study was designed to investigate the activity of A. laxiflora on uterine contractility. Setting: The leaves of the plant were collected from forests in Egor, Benin City, Nigeria. Methods: The leaves were cleaned and extracted in methanol. The extract (0.005 mg/mL–3.5 mg/mL) was tested on spontaneous uterine contraction and on oxytocin-induced contraction in normal and Ca2+-free media. The plant extract (0.0035 mg/mL, 0.035 mg/mL, 0.35 mg/mL and 3.5 mg/mL) was tested on high KCl-induced uterine contractions (80 mM). The plant extract (3.5 mg/mL) was also studied in the presence of amiodarone and glibenclamide in separate experiments. Mass spectrometric analysis was additionally performed on the plant extract in order to identify significant secondary metabolites that may have contributed to the activity of the plant. Results: The plant extract inhibited spontaneous, oxytocin and high KCl-induced uterine contractions and also significantly inhibited (p < 0.01) oxytocin-induced uterine contraction in Ca2+-free medium. The plant extract significantly inhibited (p < 0.01 and p < 0.05) oxytocin’s amplitude in the presence of amiodarone and glibenclamide, respectively. Secondary metabolites belonging to classes of fatty acids, glycols, terpenes, flavonoid glycosides and porphyrins were identified. Conclusion: Alchornea laxiflora inhibited mouse uterine contractility possibly through interaction with potassium and calcium channels. Of the known metabolites identified, 3-deoxy-arabino-hept-2-ulosonic acid, 17-hydroxyingenol and phaeophorbide-a methyl inhibit uterine contractility and may contribute to the activity of A. laxiflora in utero.

scholarly journals Ex-Vivo Uterine Activity of Theobroma Cacao (Malvaceae) Aqueous Seed Extract and Cymbopogon Citratus (Poaceae) Aqueous Leaf Extract - A Preliminary Investigation

2020 ◽  
Vol 27 (2) ◽  
pp. 108-118
Author(s):  
E.E. Bafor ◽  
G.U. Omogiade
Keyword(s):  
Natural Products ◽  
Theobroma Cacao ◽  
Leaf Extract ◽  
Ex Vivo ◽  
Seed Extract ◽  
Uterine Contractility ◽  
Cymbopogon Citratus ◽  
Uterine Activity ◽  
Uterine Contractions ◽  
Aqueous Leaf Extract

There is a need to develop new drugs from natural products for the safe and effective management of female reproductive disorders. This research was therefore aimed at the investigation of two commonly consumed natural products on uterine function. The ex vivo uterine activity of Theobroma cacao aqueous seed extract and Cymbopogon citratus aqueous leaf extract was investigated on non pregnant mouse uteri. The effect of T. cacao (0.1 mg/mL) and C. citratus (0.1 mg/mL) on spontaneous uterine contractility and in the presence of oxytocin (11.54 nM) was examined. This study showed that T. cacao elicited a significant increase (p < 0.05) in the amplitude of spontaneous uterine contractions with no significant ch ange in the frequency, which was similarly observed with C. citratus leaf extract. An increase in amplitude and frequency of oxytocin induced uterine  contractions was observed in the presence of T. cacao while with C. citratus there was a significant (p< 0.05) reduction in amplitude and non significant reduction in frequency of oxytocin induced uterine contractions. The uterotonic effect of both extracts in the absence of agonists observed maybe as a result of constituents with agonistic activity on intra cellular calcium. This study has shown that T. cacao and C. citratus could stimulate uterine activity and may therefore be useful in the management of uterine contractility disorders. Keywords : Theobromacacao Cymbopogoncitratus , uterus, spontaneous contractions

Tandem Mass Spectrometric Evaluation of Core Structures of Aromatic Compounds after Catalytic Deoxygenation

2017 ◽  
Author(s):  
Xueming Dong
Keyword(s):  
Aromatic Compounds ◽  
Supported Catalyst ◽  
Mass Spectrometric ◽  
Spectrometric Method ◽  
Mass Spectrometric Method ◽  
Aromatic Rings ◽  
Tandem Mass Spectrometric ◽  
Catalytic Deoxygenation ◽  
Oxygen Atoms

Catalytic deoxygenation of coal enhances the stability and combustion performance of coal-derived liquids. However, determination of the selectivity of removal of oxygen atoms incorporated in or residing outside of aromatic rings is challenging. This limits the ability to evaluate the success of catalytic deoxygenation processes. A mass spectrometric method, in-source collision-activated dissociation (ISCAD), combined with high resolution product ion detection, is demonstrated to allow the determination of whether the oxygen atoms in aromatic compounds reside outside of aromatic rings or are part of the aromatic system, because alkyl chains can be removed from aromatic cores via ISCAD. Application of this method for the analysis of a subbituminous coal treated using a supported catalyst revealed that the catalytic treatment reduced the number of oxygen-containing heteroaromatic rings but not the number of oxygen atoms residing outside the aromatic rings.<br>

Tandem Mass Spectrometric Evaluation of Core Structures of Aromatic Compounds after Catalytic Deoxygenation

2017 ◽  
Author(s):  
Xueming Dong
Keyword(s):  
Aromatic Compounds ◽  
Supported Catalyst ◽  
Mass Spectrometric ◽  
Spectrometric Method ◽  
Mass Spectrometric Method ◽  
Aromatic Rings ◽  
Tandem Mass Spectrometric ◽  
Catalytic Deoxygenation ◽  
Oxygen Atoms

Catalytic deoxygenation of coal enhances the stability and combustion performance of coal-derived liquids. However, determination of the selectivity of removal of oxygen atoms incorporated in or residing outside of aromatic rings is challenging. This limits the ability to evaluate the success of catalytic deoxygenation processes. A mass spectrometric method, in-source collision-activated dissociation (ISCAD), combined with high resolution product ion detection, is demonstrated to allow the determination of whether the oxygen atoms in aromatic compounds reside outside of aromatic rings or are part of the aromatic system, because alkyl chains can be removed from aromatic cores via ISCAD. Application of this method for the analysis of a subbituminous coal treated using a supported catalyst revealed that the catalytic treatment reduced the number of oxygen-containing heteroaromatic rings but not the number of oxygen atoms residing outside the aromatic rings.<br>

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