Properties |
Information |
PhytoCAT-ID |
PhytoCAT-1550 |
Phytochemical name or plant extracts |
Rhizoxin |
PMID |
1450065 |
Literature evidence |
Preclinical antitumour activity and animal toxicology studies of rhizoxin, a novel tubulin-interacting agent. |
IUPAC name |
(1S,3S,5R,8S,10S,11R,13R,14E,16R,17R)-10-hydroxy-8-[(2S,3R,4E,6E,8E)-3-methoxy-4,8-dimethyl-9-(2-methyl-1,3-oxazol-4-yl)nona-4,6,8-trien-2-yl]-11,16-dimethyl-4,7,12,18-tetraoxatetracyclo[15.3.1.03,5.011,13]henicos-14-ene-6,19-dione |
Phytochemicals’ class or type of plant extracts |
Lactone |
Source of phytochemicals or plant Extracts |
Rhizopus chinensis |
|
Geographical availability |
NA |
Plant parts |
NA |
Other cancers |
Breast cancer, Skin cancer, Lung cancer |
Target gene or protein |
NA |
Gene or Protein evidence |
NA |
Target pathways |
NA |
IC50 |
NA |
Potency |
In the present study, cytotoxic activity was observed in human tumour cell lines in vitro at very low concentrations (+/- 10(-10) M) particularly against melanoma, colon, renal, non-small cell and small cell lung cancer. In vivo antitumour activity was demonstrated in murine P388 and L1210 murine leukaemias, solid tumour models B16 melanoma and M5076 sarcoma, and in 5 out of 9 human solid tumour xenografts: LOX melanoma, MX-1 breast cancer, non-small cell lung cancer A549, and small cell lung cancers LXFS 605 and LXFS 650. |
Cell line/ mice model |
B16 melanoma, M5076 sarcoma, LOX melanoma, MX-1 breast cancer, A549 |
Additional information |
In addition, rhizoxin caused minor responses in three heavily pretreated patients with recurrent breast cancer.
Phase II clinical trials will start soon within the framework of the EORTC and CRC. |
PubChem ID |
6437358 |
Additional PMIDs |
25114240 1462165 8562349 |
Additional sources of information |
NA |
Safety |
The LD10 value of rhizoxin after a single intravenous injection was 2.8 mg/kg (8.4 mg/m2). One-tenth of the mouse equivalent LD10 (0.84 mg/m2), the starting dose for clinical phase I studies, was considered to be safe in rats. |