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Kaurenoic acid (KA) is a kaurane diterpene found in several medicinal plants that displays biological activities, such as anti-inflammatory, smooth muscle relaxant and hypotensive response. However, there are no pharmacokinetic data available about this molecule. The purpose of the study was to determine the pharmacokinetic profile and the oral bioavailability of KA in rats. Wistar rats submitted to jugular vein cannulation received 50 mg/kg of KA by intravenous or oral route. The implanted cannula allowed intravenous administration and serial blood collection along 10 h. Analytical quantification was performed by reversed phase HPLC-UV and mobile phase composed by acetonitrile:acidified water (70:30  v /v). The validated analytical method showed precision, accuracy, robustness, reliability and linearity between 0.75 and 100 μg/mL. KA administered intravenously showed a linear and two-compartment kinetic behavior at the tested dose. The following pharmacokinetic parameters were determined: C max  = 22.17 ± 1.65 mg/L; V = 14.53 ± 1.47 L/kg; CL = 17.67 ± 1.50 mL/min/kg; AUC 0-∞  = 2859.65 ± 278.42 mg·min/L, K = 0.073 ± 0.005 h −1 and t 1/2β  = 9.52 ± 0.61 h. Oral treatment did not provide detectable plasma levels of KA, avoiding the determination of its bioavailability. [ABSTRACT FROM AUTHOR]

Abstract: Montanoa tomentosa has been used in traditional medicine in Mexico to treat diverse female health disorders; it is particularly useful in inducing childbirth. Microscopic analysis of leaf surfaces of M. tomentosa revealed the presence of glandular trichomes. The chemical profile and distribution of glandular trichomes from different developmental stages of M. tomentosa leaves were investigated. Two diterpenic acids, kaurenoic and grandiflorenic were detected in glandular trichomes through the glandular microsampling technique and GC/MS analysis. In the glandular trichomes of the leaves also up to twenty-six volatile terpenes were identified, where β-eudesmol and valencene were the most abundant terpenes. [Copyright &y& Elsevier]

ent-kaurenoic acid (KA) isolated from Viguiera robusta was tested for activity on vascular smooth muscle contactility. Cumulative concentration–response curves were obtained for a stepwise increase (10−10–10−5 mol/l) in the concentration of phenylephrine (Phe), a selective α1-adrenergic agonist. The effects in the presence of KA (0.2, 2.0 and 20.0 μg/ml), and 90 min after the removal of KA from the medium bath were compared to controls. At 20.0 μg/ml, KA inhibited the in vitro contractility of rat carotid artery elicited by Phe, but had no effect at lower concentrations (0.2 and 2.0 μg/ml). The effect elicited by KA was reversible after 90 minutes. [Copyright &y& Elsevier]