| Description: |
8-O-Acetylharpagide has anti-inflammatory, vasoconstrictor, antibacteria and antiviral activities, it also has a biological activity on isolated smooth muscle preparations from guinea pig. 8-O-Acetylharpagide presents the obvious inhibition on Epstein-Barr virus(EBV) infection, it not only apparently inhibits EBV-VCA,but also alleviates the hyperfunction and effusion of capillary permeability at the early inflammation.
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| Targets: |
Antifection |
| In vitro: |
| J Nat Prod. 1992 Aug;55(8):1145-8. | | Vasoconstrictor activity of 8-O-acetylharpagide from Ajuga reptans.[Pubmed: 1431938] | |
The traditional therapeutic indications for the use of Ajuga reptans (Labiatae) have been investigated. The H2O-soluble part of a crude and partially purified MeOH extract and two isolated iridoids (8-O-acetylharpagide and harpagide), were tested for a biological activity on isolated smooth muscle preparations from guinea pig. | | Insect Biochem Mol Biol. 2001 Oct;31(11):1077-82. | | 8-O-acetylharpagide is not an ecdysteroid agonist.[Pubmed: 11520686] |
METHODS AND RESULTS:
We have reinvestigated the activity of 8-O-acetylharpagide, an iridoid glucoside, as an ecdysteroid agonist. Elbrecht et al. (Insect Biochem. Mol. Biol. 26 (1996) 519) isolated a preparation of this compound from Ajuga reptans L. and ascribed ecdysteroid agonist activity on the basis of the induction of an ecdysteroid-like response in Drosophila melanogaster KcO cells, the displacement of [3H]ponasterone A from the Drosophila receptor and the activation of an ecdysteroid-regulated gene in a transactivation assay. We provide evidence that the agonist activity derives from contaminating ecdysteroids; A. reptans is a species rich in ecdysteroids.
CONCLUSIONS:
Purified 8-O-acetylharpagide is not active in the D. melanogaster B(II) cell bioassay, neither as an agonist nor as an antagonist, nor does it displace [3H]ponasterone A from dipteran or lepidopteran ecdysteroid receptor complexes. |
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| In vivo: |
| Zhongguo Zhong Yao Za Zhi. 2013 Jun;38(12):2015-8. | | Pharmacokinetics of 8-O-acetylharpagide and harpagide after oral administration of Ajuga decumbens extract in beagle dog.[Pubmed: 24066603] | 8-O-Acetylharpagide and harpagide are two kinds of effective component of Ajuga decumbens extract. A sensitive LC-MS/MS method has been established for pharmacokinetics of 8-O-Acetylharpagide and harpagide in beagle dog after oral administration of from A. decumbens extract.
METHODS AND RESULTS:
Female beagle dogs received orally 12.9, 25.7 mg x kg(-1) p. o. Concentrations of 8-O-Acetylharpagide and harpagide in plasma were determined by LC-MS/MS method at different time points and all pharmacokinetic parameters were estimated by non-compartment analysis. The mobile phase consisted of 0.1% formic acid in water (A) and acetonitrile (B), which was run at a flow rate of 0.3 mL x min(-1). Chromatographic separation was achieved on an Agilent ZORBAX XDB-C18 column (2.1 mm x 50 mm, 3.5 microm) using a gradient elution of 5% B at 0-2 min, 95% B at 2. 1-5 min and 5% B at 5. 1-10 min. All analytes, including the IS, were monitored under positive ionization conditions and quantified in MRM mode with transitions of m/z 429.2-369.2 for 8-O-Acetylharpagide, m/z 387.2-207.2 for harpagide, and m/z 149.2-103.1 for IS. High purity nitrogen was employed as both the nebulizing and drying gas. Other parameters of the mass spectrometer were optimized as follows: drying gas flow 10.0 L x min(-1); drying gas temperature 300 degrees C; capillary voltage 4 000 V. Results showed that 8-O-Acetylharpagide and harpagide showed a dose-dependence profile. T(max) of 8-O-Acetylharpagide is 1.7 h, and T(max) of harpagide is 1.57 h, which was higher than T(max) of 8-O-Acetylharpagide and harpagide after oral administration of from A. decumbens extract in rats.
CONCLUSIONS:
The different pharmacokinetic parameters may be due to the species differences of rat and beagle dog. |
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