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The Labdane Ent-3-Acetoxy-Labda-8(17), 13-Dien-15-Oic Decreases BloodPressure In Hypertensive Rats

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ABSTRACT

Background: Labdane-type diterpenes induce lower blood pressure via relaxation ofvascular smooth muscle; however, there are no studies describing the effectsof labdanes in hypertensive rats.

Objective: The present study was designed to investigate the cardiovascular actions ofthe labdane-type diterpene ent-3-acetoxy-labda-8(17), 13-dien-15-oic acid(labda-15-oic acid) in two-kidney 1 clip (2K-1C) renal hypertension.

Methods: Vascular reactivity experiments were performed in aortic rings isolated from2K-1C and normotensive (2K) male Wistar rats. Nitrate/nitrite (NOx)measurement was performed in aortas by colorimetric assay. Blood pressuremeasurements were performed in conscious rats.

Results: Labda-15-oic acid (0.1-300 µmol/l) and forskolin (0.1nmol/l - 1 µmol/l) relaxed endothelium-intact andendothelium-denuded aortas from both 2K-1C and 2K rats. Labda-15-oic acidwas more effective at inducing relaxation in endothelium-intact aortas from2K pre-contracted with phenylephrine when compared to theendothelium-denuded ones. Forskolin was more potent than labda-15-oic acidat inducing vascular relaxation in arteries from both 2K and 2K-1C rats.Labda-15-oic acid-induced increase in NOx levels was lower in arteries from2K-1C rats when compared to 2K rats. Intravenous administration oflabda-15-oic acid (0.3-3 mg/kg) or forskolin (0.1-1 mg/kg) inducedhypotension in conscious 2K-1C and 2K rats.

Conclusion: The present findings show that labda-15-oic acid induces vascular relaxationand hypotension in hypertensive rats.

No MeSH data available.


Relaxation responses induced by forskolin on rat aortic rings. Therelaxation induced by the labdane was studied on endothelium-intact(E+) and endothelium‑denuded (E-) rat aortic rings contracted witheither phenylephrine (0.1 µmol/l) or KCl (30 mmol/l). Steadytension was evoked by phenylephrine or KCl and then forskolin (0.1nmol/l - 1 µmol/l) was added cumulatively.
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f3: Relaxation responses induced by forskolin on rat aortic rings. Therelaxation induced by the labdane was studied on endothelium-intact(E+) and endothelium‑denuded (E-) rat aortic rings contracted witheither phenylephrine (0.1 µmol/l) or KCl (30 mmol/l). Steadytension was evoked by phenylephrine or KCl and then forskolin (0.1nmol/l - 1 µmol/l) was added cumulatively.

Mentions: Forskolin reduced the sustained contractions induced by phenylephrine and KCl inendothelium-intact and endothelium-denuded aortas from both 2K-1C and 2K rats(Figure 3). The Emax valuesfor the relaxant effect of forskolin in endothelium-intact andendothelium-denuded rings pre-contracted with phenylephrine were notsignificantly different in aortas from 2K-1C and 2K rats (Table 2). However, differences were found in thepD2 values for forskolin in endothelium-intact and denuded ringspre-contracted with phenylephrine in aortas from both 2K-1C and 2K rats. In thearteries pre-contracted with KCl, there was no difference between theEmax or pD2 values for forskolin in endothelium-intactor denuded rings from both 2K-1C and 2K rats (Table 2).


The Labdane Ent-3-Acetoxy-Labda-8(17), 13-Dien-15-Oic Decreases BloodPressure In Hypertensive Rats
Relaxation responses induced by forskolin on rat aortic rings. Therelaxation induced by the labdane was studied on endothelium-intact(E+) and endothelium‑denuded (E-) rat aortic rings contracted witheither phenylephrine (0.1 µmol/l) or KCl (30 mmol/l). Steadytension was evoked by phenylephrine or KCl and then forskolin (0.1nmol/l - 1 µmol/l) was added cumulatively.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4940147&req=5

f3: Relaxation responses induced by forskolin on rat aortic rings. Therelaxation induced by the labdane was studied on endothelium-intact(E+) and endothelium‑denuded (E-) rat aortic rings contracted witheither phenylephrine (0.1 µmol/l) or KCl (30 mmol/l). Steadytension was evoked by phenylephrine or KCl and then forskolin (0.1nmol/l - 1 µmol/l) was added cumulatively.
Mentions: Forskolin reduced the sustained contractions induced by phenylephrine and KCl inendothelium-intact and endothelium-denuded aortas from both 2K-1C and 2K rats(Figure 3). The Emax valuesfor the relaxant effect of forskolin in endothelium-intact andendothelium-denuded rings pre-contracted with phenylephrine were notsignificantly different in aortas from 2K-1C and 2K rats (Table 2). However, differences were found in thepD2 values for forskolin in endothelium-intact and denuded ringspre-contracted with phenylephrine in aortas from both 2K-1C and 2K rats. In thearteries pre-contracted with KCl, there was no difference between theEmax or pD2 values for forskolin in endothelium-intactor denuded rings from both 2K-1C and 2K rats (Table 2).

View Article: PubMed Central - PubMed

ABSTRACT

Background: Labdane-type diterpenes induce lower blood pressure via relaxation ofvascular smooth muscle; however, there are no studies describing the effectsof labdanes in hypertensive rats.

Objective: The present study was designed to investigate the cardiovascular actions ofthe labdane-type diterpene ent-3-acetoxy-labda-8(17), 13-dien-15-oic acid(labda-15-oic acid) in two-kidney 1 clip (2K-1C) renal hypertension.

Methods: Vascular reactivity experiments were performed in aortic rings isolated from2K-1C and normotensive (2K) male Wistar rats. Nitrate/nitrite (NOx)measurement was performed in aortas by colorimetric assay. Blood pressuremeasurements were performed in conscious rats.

Results: Labda-15-oic acid (0.1-300 µmol/l) and forskolin (0.1nmol/l - 1 µmol/l) relaxed endothelium-intact andendothelium-denuded aortas from both 2K-1C and 2K rats. Labda-15-oic acidwas more effective at inducing relaxation in endothelium-intact aortas from2K pre-contracted with phenylephrine when compared to theendothelium-denuded ones. Forskolin was more potent than labda-15-oic acidat inducing vascular relaxation in arteries from both 2K and 2K-1C rats.Labda-15-oic acid-induced increase in NOx levels was lower in arteries from2K-1C rats when compared to 2K rats. Intravenous administration oflabda-15-oic acid (0.3-3 mg/kg) or forskolin (0.1-1 mg/kg) inducedhypotension in conscious 2K-1C and 2K rats.

Conclusion: The present findings show that labda-15-oic acid induces vascular relaxationand hypotension in hypertensive rats.

No MeSH data available.