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Evaluation of the Cholinergic and Adrenergic Effects of Two Tropane Alkaloids from Erythroxylum pervillei
| Content Provider | PubMed Central |
|---|---|
| Author | Chin, Young-won Kinghorn, A. Douglas Patil, Popat N. |
| Abstract | Pervilleine A is an aromatic ester tropane alkaloid from Erythroxylum pervillei that has shown promising activity as a multidrug resistance inhibitor. Due to its structural similarity with the well known (-)-hyoscyamine and (-)-cocaine, the cholinergic and adrenergic activities of pervilleine A were evaluated. At 30 μM (±)-pervilleine A hydrochloride exhibited non-competitive inhibition of the cholinergic response in the guinea pig ileum and did not affect the carbachol-induced contraction of the rat anococcygeus smooth muscle. (±)-Pervilleine A hydrochloride blocked nonspecifically the vascular response of (-)-norepinephrine in the rat aorta ring, while the contractile response of rat vas deferens to (-)-norepinephrine was not affected significantly at a 100 μM concentration. An analogue of pervilleine A, (±)-pervilleine H, without a 6-O-trans-3,4,5-trimethoxycinnamoyl ester substituent required for anti-multidrug resistance activity, did not exhibit any effects in these experiments. The data suggest that (±)-pervilleine A hydrochloride has weak nonspecific anticholinergic and vascular antiadrenergic activities. The lack of significant cholinergic and adrenergic receptor-mediated activities may be considered advantageous for the further development of pervilleine A as a new adjuvant in cancer chemotherapy. |
| Related Links | http://dx.doi.org/10.1002/ptr.2155 |
| Ending Page | 1005 |
| Page Count | 4 |
| Starting Page | 1002 |
| File Format | |
| ISSN | 0951418X |
| e-ISSN | 10991573 |
| Journal | Phytotherapy research : PTR |
| Issue Number | 10 |
| Volume Number | 21 |
| Language | English |
| Publisher Date | 2007-10-01 |
| Access Restriction | Open |
| Subject Keyword | Pharmacology Research in Higher Education |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
