| In vitro: |
| Applied Mechanics & Materials, 2013, 395-396:587-590. | | The Effect and Mechanism of Apoptosis Induced by Desacetylcinobufotalin (DEBF) in Human Hepatocellular Carcinoma HepG2 Cells[Reference: WebLink] |
METHODS AND RESULTS:
The cytotoxicity of Desacetylcinobufotalin (DEBF) and apoptosis induced by DEBF was measured. Additionally the mechanism of Apoptosis induced by DEBF was studied through Western blot. The results show DEBF displayed the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml. The expression of Bax was significantly increased and the expression of Bcl-2 was markedly decreased, compared to the control.
CONCLUSIONS:
The data suggest DEBF had significant antitumor activity through induction apoptosis via mitochondria pathway. | | Journal of Molecular Catalysis B Enzymatic, 2003, 22(1):89-95. | | Biotransformation of cinobufagin by cell suspension cultures of Catharanthus roseus and Platycodon grandiflorum[Reference: WebLink] | The biotransformations of cinobufagin (1), an animal-originated bufadienolide, by cell suspension cultures of Catharanthus roseus and Platycodon grandiflorum were investigated.
METHODS AND RESULTS:
Incubation for 6 days of 1 with C. roseus yielded four products, Desacetylcinobufotalin (2), 3-epi-desacetylcinobufagin (3), 1β-hydroxyl desacetylcinobufagin (4) and 3-epi-Desacetylcinobufotalin (5), among which 4 is a new compound. Time course investigation revealed that the biotransformation rates of two major products, 2 and 3, reached their highest levels of 44.7 and 16.5%, respectively, on the third day after substrate administration. Compounds 2–5 showed more potent cytotoxic activities against HL-60 cell lines than the parent compound 1. A plausible biotransformation pathway is proposed to account for the formation of the observed products. From the culture supernatant of P. grandiflorum, 2 was isolated in 37.8% yield after 8 days of incubation with 1. Cinobufotalin (6) and desacetylcinobufagin (7) were also obtained as minor products. The two plant suspension cultures exhibited similar transformation patterns on compound 1. |
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