| In vitro: |
| Bioorg Med Chem. 2009 Sep 1;17(17):6251-6. | | Tessaric acid derivatives induce G2/M cell cycle arrest in human solid tumor cell lines.[Pubmed: 19664930 ] |
METHODS AND RESULTS:
A series of analogs were synthesized in a straightforward manner from naturally available sesquiterpenes ilicic acid and Tessaric acid. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, HBL-100, HeLa, SW1573, T-47D and WiDr. The most potent analog induced considerably growth inhibition in the range 1.9-4.5 microM.
CONCLUSIONS:
Cell cycle studies for Tessaric acid derivatives indicated a prominent arrest of the cell cycle at the G(2)/M phase. Damage to the cells was permanent as determine by the so called 24+24 drug schedule. | | Z Naturforsch C. 2005 Nov-Dec;60(11-12):855-61. | | Antifeedant/insecticidal terpenes from asteraceae and labiatae species native to Argentinean semi-arid lands.[Pubmed: 16402545 ] | To validate the potential as added-value resources of Asteraceae and Labiatae species of Argentinean semi-arid lands, we have selected 13 of their major terpenoids belonging to several chemical classes and tested their insect antifeedant and toxic activity on the herbivorous insects Spodoptera littoralis and Leptinotarsa decemlineata.
METHODS AND RESULTS:
The antifeedant effects of the test compounds were structure- and species-dependent. The most active antifeedant to L. decemlineata was the eudesmane sesquiterpene gamma-costic acid (13), followed by the labdane diterpene 2alpha,3alpha-dihydroxycativic acid (8), the clerodane diterpenes 6-acetylteucjaponin B (5), bacchotricuneatin A (1), bartemidiolide (7), butanolide (4), and the sesquiterpenes ilicic acid (11) and Tessaric acid (10) (eudesmane and eremophilane type, respectively). S. littoralis was only affected by the clerodanes and showed the strongest response to salviarin (3) and 5, followed by hawtriwaic acid (6) and 12-epi-bacchotricuneatin A (2).
CONCLUSIONS:
Orally injected S. littoralis larvae were negatively affected by 5. Most of the diterpenes had selective cytotoxic effects to insect-derived Sf9 cells with the clerodane 1 being the most active, followed by the eudesmane costic acid (12), the only cytotoxic sesquiterpene. None of these compounds was cytotoxic to mammalian CHO cells. | | J Chem Ecol. 2003 Jan;29(1):175-87. | | Allelochemical effects of eudesmane and eremophilane sesquiterpenes on Tribolium castaneum larvae.[Pubmed: 12647861] |
METHODS AND RESULTS:
Eight eudesmane and eremophilane sesquiterpenes administered to Tribolium castaneum larvae caused different allelochemical effects. Topical application of 3-oxo-gamma-costic acid produced the greatest lengthening in the duration of the pupal stage. Morphological deformities were found, specifically when ilicic, costic, and gamma-costic acids and costic aldehyde were used. Ilicic acid exhibited the major toxicity 72 hr following topical application. All compounds were significantly toxic at the end point of the experiment (60 days). Treated surface toxicity was lower than when topical assays were carried out.
CONCLUSIONS:
Responses to Tessaric acid in choice bioassays had the highest attractive effect. Maximum repellency was caused by the 3-oxo-gamma-costic acid. However, experimental series carried out using gamma-costic acid, eremophilan-1(10),2,11(13)-trien-12-oic acid, costic aldehyde, and ilicic aldehyde showed no clear response. |
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