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DOI: 10.1055/s-2002-32897
© Georg Thieme Verlag Stuttgart · New York
Effects of a Labdane Diterpene Isolated from Brickellia paniculata on Intracellular Ca2+ Deposit of Guinea-Pig Ileal Longitudinal Muscle
Publikationsverlauf
Received: October 19, 2001
Accepted: February 3, 2002
Publikationsdatum:
22. Juli 2002 (online)
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Introduction
Brickellia paniculata (Asteraceae) is a medicinal plant commonly used in Southeastern Mexico to treat colics, abdominal pains and watery diarrhoea [1], [2]. In a previous study, from the methanolic extract were isolated a flavonoid (xanthomicrol) and a labdane diterpene, this latter compound was structurally characterized as 3α-angeloyloxy-2α-hydroxy-13,14Z-dehydrocativic acid (AAHDD) [3]. The structures have already been reported and their identity was confirmed by comparison with published physical and spectroscopic data [4], [5], [6]. Both compounds relaxed the segments of isolated guinea-pig ileum stimulated with high K+ and the effect was correlated with an interference of Ca2+ mobilization in the cell. Furthermore, a competitive calcium-antagonistic activity was described for AAHDD, although the precise mechanism underlying this effect was not demonstrated. It is well documented that in the guinea pig ileum, K+ depolarization induces the opening of the voltage-dependent calcium channels increasing the influx of Ca2+ into the cell; as a response to the rise of free Ca2+ in the cytosol, the muscle contracts. Calcium entry is the primary but not the sole mechanism of increasing [Ca2+]i, since the release of the cation from intracellular deposits can also occur. Phasic response to K+ has been attributed to a rise in cytosolic free Ca2+ which is released from intracellular stores. On the other hand, the tonic component has been associated with the opening of the voltage-dependent calcium channels causing Ca2+ influx to increase [7], [8], [9].
As has been observed, the compound AAHDD inhibited with the same potency the K+ evoked phasic and tonic components of the contractile response. This work was undertaken to gain further information about a possible blocking action of AAHDD at intracellular Ca2+ stores.[]
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Mariana Meckes
Unidad de Investigación Médica en Farmacología de Productos Naturales
Hospital de Pediatría, Centro Médico Nacional Siglo XXI, IMSS
Av. Cuauhtémoc, 330, Col Doctores cp. 06725, México D.F
Fax: +57-61-0952
eMail: meck7707@prodigy.net.mx