Compounds obtained from sida acuta with the potential to induce quinone reductase and to inhibit 7,12-dimethylbenz[a]anthracene-induced preneoplastic lesions in a mouse mammary organ culture model.
ABSTRACT Activity-guided fractionation of the EtOAc-soluble extract of the whole plants of Sida acuta using a bioassay based on the induction of quinone reductase (QR) in cultured Hepa 1c1c7 mouse hepatoma cells, led to the isolation of ten active compounds of previously known structure, quindolinone (1), cryptolepinone (2), 11-methoxyquindoline (3), N-trans-feruloyltyramine (4), vomifoliol (5), loliolide (6), 4-ketopinoresinol (7), scopoletin (8), evofolin-A (9), and evofolin-B (10), along with five inactive compounds of known structure, ferulic acid, sinapic acid, syringic acid, (+/-)-syringaresinol, and vanillic acid. These isolates were identified by physical and spectral data measurement. A new derivative of quindolinone, 5,10-dimethylquindolin-11-one (1a) was synthesized and characterized spectroscopically. Of the active substances, compounds 1-3 and 1a exhibited the most potent QR activity, with observed CD (concentration required to double induction) values ranging from 0.01 to 0.12 microg/mL. Six compounds were then evaluated in a mouse mammary organ culture assay, with cryptolepinone (2), N-trans-feruloyltyramine (4), and 5,10-dimethylquindolin-11-one (1a) found to exhibit 83.3, 75.0, and 66.7% inhibition of 7,12-dimethylbenz[a]anthracene-induced preneoplastic lesions, respectively, at a dose of 10 microg/mL.
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ABSTRACT: The potential antiproliferative and antioxidant activities of extracts from five medicinal plants from Cameroon were evaluated in vitro on HepG-2 cells. The results showed the significant decrease of the viability of the cells in a concentration-dependent manner. According to the IC(50) obtained, the extracts of S. acuta (461.53±0.23) and U. lobata (454.93±0.12) showed significant antiproliferative activity. At fixed concentration (250μgmL(-1)), extracts demonstrated higher antiproliferative activity (67.05%; 65.42%), (52.62%; 56.64%) and (32.98%; 36.85%) respectively during 24, 48 and 72h. Extracts of S. cordifolia and V. album demonstrated significant antiproliferative property after 48h while S. rhombifolia exhibited weak cytotoxicity. The results of the antioxidant properties showed that theses extracts induced significantly increase of SOD, CAT and GsT activity after 48h. Taken together, the results extracts showed that of S. acuta and U. lobata may be a promising alternative to synthetic substances as natural compound with high antiproliferative and antioxidant activities.Environmental toxicology and pharmacology. 05/2010; 29(3):223-8.
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ABSTRACT: Some coumarins possess enhancing effects on lymphocyte mitogen responsiveness. In this investigation, the activity of scopoletin, a coumarin that has been isolated from different plants and in this case specifically from T. cordata Mill., was evaluated. For this purpose, normal T lymphocytes and a hyperproliferative T lymphoma cell line were used. Scopoletin was found to exert a dual action on tumoral lymphocytes exhibiting both a cytostatic and a cytotoxic effect. These effects varied with the concentrations analysed and the time of cell incubation (EC(50): 251+/-15 microg/ml) and were associated to the induction of apoptosis. Scopoletin induced cell proliferation on normal T lymphocytes (Proliferation stimulation index: 1 microg/ml scopoletin: 1.26+/-0.1; 10 microg/ml scopoletin: 3+/-0.25; 100 microg/ml scopoletin: 1.86+/-0.08); this stimulatory action was found to be due to the interaction with kinase C (PKC) protein. These results indicate that scopoletin could be a potential antitumoral compound to be used for cancer treatment.Life Sciences 11/2006; 79(21):2043-8. · 2.56 Impact Factor
- Synthetic Metals 01/1994; 70(1-3). · 2.11 Impact Factor