| Description: |
Odoroside H has anticancer activities, the cytotoxic effects are induced by the inhibition of the plasma membrane bound Na(+)/K(+)-ATPase. |
| Targets: |
Sodium Channel | ATPase | Potassium Channel |
| In vitro: |
| J Ethnopharmacol. 2011 Apr 12;134(3):781-8. | | Characterization of the anticancer properties of monoglycosidic cardenolides isolated from Nerium oleander and Streptocaulon tomentosum.[Pubmed: 21291990] |
For identification of the active constituents we investigated the anticancer activity of cardenolides from Streptocaulon tomentosum Wight & Arn. (Asclepiadaceae) and from Nerium oleander L. (Apocynaceae) which are both used against cancer in the traditional medicine in their region of origin.
METHODS AND RESULTS:
The antiproliferative activity of cardenolides isolated from roots of Streptocaulon tomentosum (IC(50)<1-15.3 μM after 2 days in MCF7) and of cardenolide containing fractions from the cold aqueous extract of Nerium oleander leaves ("Breastin", mean IC(50) 0.85 μg/ml in a panel of 36 human tumor cell lines), their influence on the cellular viability and on the cell cycle (block at the G2/M-phase or at the S-phase in tumor cells, respectively) were determined using different cell lines. The murine cell line L929 and normal non-tumor cells were not affected. Bioactivity guided fractionation of Breastin resulted in the isolation of the monoglycosidic cardenolides oleandrine, oleandrigeninsarmentoside, neritaloside, Odoroside H, and odoroside A (IC(50)-values between 0.010 and 0.071 μg/ml).
CONCLUSIONS:
The observed anticancer activities of extracts and isolated cardenolides are in agreement with the ethnomedicinal use of Streptocaulon tomentosum and Nerium oleander. The most active anticancer compounds from both species are monoglycosidic cardenolides possessing the 3β,14β-dihydroxy-5β-card-20(22)-enolide structure with or without an acetoxy group at C-16. The results indicate that the cytotoxic effects are induced by the inhibition of the plasma membrane bound Na(+)/K(+)-ATPase. |
|
| In vivo: |
| Phytochemistry. 1999 Feb;50(3):435-8. | | Bio-active cardenolides from the leaves of Nerium oleander.[Pubmed: 9933955] |
METHODS AND RESULTS:
A bioactivity directed isolation of the methanolic extract of the fresh, uncrushed leaves of Nerium oleander showing a central nervous system (CNS) depressant effect in mice has been undertaken. As a result, four CNS depressant cardenolides including a new cardenolide, neridiginoside and three known constituents, nerizoside, neritaloside and Odoroside H, have been isolated which exhibited CNS depressant activity in mice at a dose of 25 mg/kg. The structure of neridiginoside was elucidated as 3 beta-O-(D-diginosyl)-5 beta, 14 beta-dihydroxy-card-20(22)-enolide, using spectroscopic methods including one-dimensional and two-dimensional NMR (COSY-45, NOESY, J-resolved, HMQC and HMBC).
CONCLUSIONS:
The known compounds have been indentified through spectral studies and comparison of data with those reported in the literature. |
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