| In vitro: |
| Zhongguo Zhong Yao Za Zhi. 2014 Nov;39(22):4356-9. | | [Coumarins from Leonurus japonicus and their anti-platelet aggregative activity].[Pubmed: 25850267] | Chemical constituents of Leonurus japonicus were isolated and purified by a combination of various chromatographic techniques including column chromatography over silica gel, Sephadex LH-20, MCI, and Rp C18.
METHODS AND RESULTS:
Structures of the isolates were determined by spectroscopic analysis as 10 coumarins: bergapten (1), xanthotoxin (2), isopimpinellin (3), isogosferal (4), imperatorin (5), meransin hydrate(6), isomeranzin(7), murrayone(8) , Auraptenol(9), and osthol(10). In addition to compound 9, the others were isolated from the genus Leonurus for the first time.
CONCLUSIONS:
In the in vitro assay, compounds 4 and 8 significantly inhibited the abnormal increase of platelet aggregation induced by ADP. | | Int J Mol Sci. 2013 Jan 9;14(1):1197-206. | | Coumarins from the Herb Cnidium monnieri and Chemically Modified Derivatives as Antifoulants against Balanus albicostatus and Bugula neritina Larvae.[Pubmed: 23303279] |
METHODS AND RESULTS:
In the search for new environmental friendly antifouling (AF) agents, four coumarins were isolated from the herbal plant Cnidium monnieri, known as osthole (1), imperatorin (2), isopimpinellin (3) and Auraptenol (4). Furthermore, five coumarin derivatives, namely 8-epoxypentylcoumarin (5), meranzin hydrate (6), 2'-deoxymetranzin hydrate (7), 8-methylbutenalcoumarin (8), and micromarin-F (9) were synthesized from osthole. Compounds 1, 2, 4, 7 showed high inhibitory activities against larval settlement of Balanus albicostatus with EC(50) values of 4.64, 3.39, 3.38, 4.67 μg mL-1. Compound 8 could significantly inhibit larval settlement of Bugula neritina with an EC(50) value of 3.87 μg mL-1.
CONCLUSIONS:
The impact of functional groups on anti-larval settlement activities suggested that the groups on C-5' and C-2'/C-3' of isoamylene chian could affect the AF activities. |
|
| In vivo: |
| Sci Rep. 2013 Nov 29;3:3377. | | Auraptenol attenuates vincristine-induced mechanical hyperalgesia through serotonin 5-HT1A receptors.[Pubmed: 24287473] | Common chemotherapeutic agents such as vincristine often cause neuropathic pain during cancer treatment in patients. Such neuropathic pain is refractory to common analgesics and represents a challenging clinical issue. Angelicae dahuricae radix is an old traditional Chinese medicine with demonstrated analgesic efficacy in humans. However, the active component(s) that attribute to the analgesic action have not been identified.
METHODS AND RESULTS:
This work described the anti-hyperalgesic effect of one coumarin component, Auraptenol, in a mouse model of chemotherapeutic agent vincristine-induced neuropathic pain. We reported that Auraptenol dose-dependently reverted the mechanical hyperalgesia in mice within the dose range of 0.05-0.8 mg/kg. In addition, the anti-hyperalgesic effect of Auraptenol was significantly blocked by a selective serotonin 5-HT1A receptor antagonist WAY100635 (1 mg/kg). Within the dose range studied, Auraptenol did not significantly alter the general locomotor activity in mice.
CONCLUSIONS:
Taken together, this study for the first time identified an active component from the herbal medicine angelicae dahuricae radix that possesses robust analgesic efficacy in mice. These data support further studies to assess the potential of Auraptenol as a novel analgesic for the management of neuropathic pain. |
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