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During term, oxytocin OT and prostaglandins act on the uterus, and induce contractions, that result in preterm labour [ 2 ]. Since F-A failed to inhibit this contraction as like calcium channel blockers, it is reasonable to postulate that F-A does not have intracellular action. The aerial parts of this plant are reported to dating Santa Cruz CA of wight pregnane glycosides with 2-deoxy sugars, brevinine, and brevine [ 56 ].
A fraction of this plant extract has been reported to have antiallergic and antiinflammatory activities [ 7 ]. This was allowed to stand for 5 min for stabilization of the contraction. Then buffer was changed to modified Ringer-Locke I.
The tissues were given few washouts immediately with modified Ringer-Locke I and were allowed to equilibrate for 50 min with intermittent washings. The relative concentration of alkaloid in the F-A was 3. The F-A at concentrations up to The IC 50 of F-A was found to be F-A was also found to inhibit the contraction induced by KCl in presence of propranolol 10 -5 M.
This in the influx of calcium into the smooth muscle cells, and le to contraction. However, these drugs are sometimes inadequate, and have adverse effects like tachycardia, increased cardiac output, pulmonary edema, hyperglycemia, cardiac depression, and inhibition of neuromuscular transmission4.
However, the uterine relaxant activity might not be specific, since the fraction of this plant extract was also reported to have smooth muscle relaxant activity on the isolated ileal and tracheal smooth muscles of guinea pig [ 8 ]. Merckusing Camag Linomat 5.
The Indian Journal of Pharmacy was started in as "a quarterly journal devoted to the Science and practice of Pharmacy in all its branches". This solution was successively and exhaustively extracted with hexane, ether, and chloroform. OT-induced rhythmic contractions, and its amplitude and frequency consists of two components, phasic and tonic, generated by different biochemical mechanisms [ 17 ].
The contractions obtained in these conditions, were related only to release of calcium from intracellular stores [ 3 ]. Further phytochemical and pharmacological studies are necessary to judge the possible clinical use of this phytomedicine. This was done to circumvent possible influence of F-A on beta-receptors.
Potassium chloride 60 mM induced contraction of the rat uterus by depolarizing the smooth muscle membrane. The tissues were then challenged with 0. The contraction is a biphasic response, that consists of an initial, rapid, transitory contraction, the phasic response, followed by a slower more sustained contraction, the tonic response [ 13 ].
It is therefore necessary, for search of effective and safe alternative drugs for the treatment of preterm labour. The percent inhibition at each dose level was averaged, and the standard deviation SD was calculated. It was then pressed, filtered, and concentrated to a syrupy mass. They were housed under standard laboratory conditions in polyacrylic cages, and were provided with rat food pellets and water ad libitum.
This observation was comparable with earlier report [ 8 ]. At concentrations of The F-A, at concentrations of The major cause of perinatal morbidity and mortality, is preterm labour [ 1 ]. It was then stirred for 12 h using a magnetic stirrer. Benaras Hindu University, Benaras.
After 24 h, they were sacrificed, and uterine horns were removed gently from the surrounding tissue and fat, and then placed in a petridish containing PSS. The tissues, approximately 2. The relative contributions of these two sources of calcium, depend on both the contractile agents and their concentrations. The tissues were equilibrated in Ringer-Locke II for 30 min, with intermittent washings. The coarse powder 25 g was mixed with ml of mixture of acetone and ammoniaand kept closed in a dark area for 24 h.
The tissues were again challenged with KCl 60 mM. In the present study, the fraction F-A of Sarcostemma brevistigma Wight was tested in one in vitro model only. Chemical analysis indicated the presence of alkaloid, and absence of steroid in the chloroform soluble fraction. OT induces contraction by stimulating their specific receptors, which activates second messenger systems to release the intracellularly stored calcium from the sarcoplasmic reticulum [ 17 ].
The Chief editor and the main guiding force behind the 'Journal' was Prof. After contraction attained steady state, cumulative amounts of F-A were added to the organ bath.
Sarcostemma brevistigma Wight Asclepiadaceaecommonly known as soma Sanskrit and somlata Hindiis a leafless, trailing shrub. The subsequent release of calcium from the intracellular stores, decreases either calcium extrusion, or intracellular calcium binding.
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The present study indicates, that the chloroform-soluble fraction F-A of the Acetone extract of the twigs of S. Though, we identified the presence of alkaloid and its relative concentration in the fraction, the tocolytic activity could not be attributed to it. After washout, the tissues were challenged with OT.
After the rhythmic contractions were stabilized, the effects of cumulative amounts of F-A were studied and recorded in a similar manner, as mentioned earlier. The tissues were then washed with PSS, till they relaxed to the baseline. The tissues were allowed to equilibrate for 1 h with a resting tension of 0.
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The phasic component is related to calcium influx, probably via VOC, and the tonic component involves the opening of ROC, or an increase in IP 3 turnover. Nicholas Piramal India Ltd. The were expressed as percent inhibition. The uterine horn pieces were mounted as mentioned above, using Ringer-Locke solution. It also inhibited the contractions induced by acetylcholine and histamine on isolated guinea pig ileum, and produced bronchospasmolytic activity [ 8 ]. Fine Chemicals Limited, Mumbai.
Consequently, the intracellular calcium level is increased through the receptor-operated calcium channel ROC. Agonists also open non L-type channels in addition to opening Ltype channels [ 18 ]. According to folklore, this plant extract is used for the treatment of asthma.
The effect of a chloroform soluble fraction F-A of the acetone extract of twigs of Sarcostemma brevistigma Wight on contractions induced by oxytocin and KCl, in the isolated rat uterine smooth muscles, has been evaluated. The Rf value of the alkaloid was found to be 0.
These investigations revealed that the uterine relaxant activity of F-A was possibly through interference with the mobilization of extracellular calcium across the cell membrane, like calcium channel antagonists. This suspension was used in the study. Figure 1: Densitogram curve of chloroform soluble fraction of acetone extract of Sarcostemma brevistigma Wight. Animal studies were approved by Institutional Animal Ethics Committee, and carried out in accordance with the Guidelines of the Committee for the Purpose of Control and Supervision of Experiments on Animals.
A mixture of chloroform: methanol: triethylamine Female Wistar rats g were used throughout the study.
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In the present study, we have evaluated the uterine relaxant effect of a chloroform soluble fraction F-A from the acetone extract of the twigs of S. The twigs of the plant S. The twigs were shade dried, pulverized in a mixer-grinder, and the coarse powder was stored in a nontoxic polyethylene bag. They were allowed to equilibrate for 40 min with a resting tension of 1 g, and with intermittent washings with PSS. The tissues were then challenged with KCl 60 mM final organ bath concentration.
After OT induced sustained contraction, the effects of cumulative amounts of F-A were studied and recorded, as mentioned earlier. The effect of test agents was recorded using force transducer and student physiograph, on an amplified recorder Omniscribe recorder, Digital electronics limited.
The tocolytic activity could be due to interference with the mobilization of extracellular calcium. It is distributed in various parts of India.
Materials and methods
Schroff, Head of the Department of Pharmaceutics. Loba Chemie, Mumbai. They were allowed to equilibrate for 40 min with a resting tension of 1 g, with frequent washings.