Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves
Background: Isoespintanol is a monoterpene isolated from the leaves of <i>Oxandra xylopioides</i> Diels. (Annonaceae) with antioxidant and antiinflammatory effects. It was of interest to know whether it has antispasmodic effects such as other known drugs, phloroglucinol and trimethoxyben...
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| Autores principales: | , , , , , , |
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| Formato: | Articulo Preprint |
| Lenguaje: | Inglés |
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2018
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| Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/98217 https://ri.conicet.gov.ar/11336/85350 https://www.sciencedirect.com/science/article/abs/pii/S0944711318301831?via%3Dihub |
| Aporte de: |
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I19-R120-10915-98217 |
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dspace |
| institution |
Universidad Nacional de La Plata |
| institution_str |
I-19 |
| repository_str |
R-120 |
| collection |
SEDICI (UNLP) |
| language |
Inglés |
| topic |
Ciencias Médicas Antispasmodic Calcium Detrusor Intestine Isoespintanol Uterus |
| spellingShingle |
Ciencias Médicas Antispasmodic Calcium Detrusor Intestine Isoespintanol Uterus Gavilánez Buñay, Tatiana Carolina Colareda, Germán Andrés Ragone, María Inés Bonilla Bonilla, Adriana Milena Rojano, Benjamín A. Schinella, Guillermo Raúl Consolini, Alicia Elvira Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves |
| topic_facet |
Ciencias Médicas Antispasmodic Calcium Detrusor Intestine Isoespintanol Uterus |
| description |
Background: Isoespintanol is a monoterpene isolated from the leaves of <i>Oxandra xylopioides</i> Diels. (Annonaceae) with antioxidant and antiinflammatory effects. It was of interest to know whether it has antispasmodic effects such as other known drugs, phloroglucinol and trimethoxybenzene, used in therapeutics for treating biliary, urinary and uterine spasms.
Purpose: To assess whether isoespintanol possesses antispasmodic effects on intestine, uterus and bladder.
Study design: A preclinical study was performed in which isoespintanol, phloroglucinol and trimethoxybenzene were evaluated with concentration–contractile response curves (CRC) of carbachol in isolated rat intestine and bladder, and with CRC of serotonin (5-HT) in rat uterus. Moreover, it was assessed whether isoespintanol interferes with Ca<sup>2+</sup> influx by making CRC of Ca<sup>2+</sup> in high-K<sup>+</sup> medium in intestine and bladder.
Results: Isoespintanol non-competitively inhibited the CRC of carbachol with affinity constant (pK) of 4.78 ± 0.09 in intestine and 4.60 ± 0.09 in bladder. Phloroglucinol and trimethoxybenzene were also non-competitive antagonists, but isoespintanol was 8 times more potent than trimethoxybenzene and similarly potent than phloroglucinol in intestine. In bladder, isoespintanol resulted 8 times more potent than trimethoxybenzene. The maximal inhibition of contraction followed the order of isoespintanol > trimethoxybenzene > phloroglucinol in intestine, and isoespintanol > trimethoxybenzene in bladder. Moreover, isoespintanol also completely and non-competitively inhibited the CRC of Ca<sup>+2</sup>, with a pK of 5.1 ± 0.1 in intestine, and 4.32 ± 0.07 in bladder. In uterus isoespintanol reduced, completely and non-competitively, the contraction produced by 5-HT with pK of 5.05 ± 0.07.
Conclusion: Results demonstrate that isoespintanol is a very good intestinal, urinary and uterine antispasmodic, with higher potency than the other drugs used in therapeutics. The mechanism of action of isoespintanol is the interference with Ca<sup>+2</sup> influx, at a difference of trimethoxybenzene and phloroglucinol. |
| format |
Articulo Preprint |
| author |
Gavilánez Buñay, Tatiana Carolina Colareda, Germán Andrés Ragone, María Inés Bonilla Bonilla, Adriana Milena Rojano, Benjamín A. Schinella, Guillermo Raúl Consolini, Alicia Elvira |
| author_facet |
Gavilánez Buñay, Tatiana Carolina Colareda, Germán Andrés Ragone, María Inés Bonilla Bonilla, Adriana Milena Rojano, Benjamín A. Schinella, Guillermo Raúl Consolini, Alicia Elvira |
| author_sort |
Gavilánez Buñay, Tatiana Carolina |
| title |
Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves |
| title_short |
Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves |
| title_full |
Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves |
| title_fullStr |
Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves |
| title_full_unstemmed |
Intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>Oxandra xylopioides</i> leaves |
| title_sort |
intestinal, urinary and uterine antispasmodic effects of isoespintanol, metabolite from <i>oxandra xylopioides</i> leaves |
| publishDate |
2018 |
| url |
http://sedici.unlp.edu.ar/handle/10915/98217 https://ri.conicet.gov.ar/11336/85350 https://www.sciencedirect.com/science/article/abs/pii/S0944711318301831?via%3Dihub |
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