Back to Search
Start Over
Cytotoxic Biotransformed Products from Triptonide byAspergillus niger
- Source :
- Planta Medica. 69:804-808
- Publication Year :
- 2003
- Publisher :
- Georg Thieme Verlag KG, 2003.
-
Abstract
- The diterpenoid triepoxides are the major active constituents of Tripterygium wilfordii with potent antitumor and immune activities. But the strong toxicity of these compounds has restricted their application to a great extent. In order to find more effective compounds with less toxicity, structural modifications of triptonide (1) by Aspergillus niger (AS 3.739) were investigated and four biotransformed products were obtained. Based on their chemical and spectral data, their structures were elucidated as 5alpha-hydroxytriptonide (2), triptolide (3), 17-hydroxytriptonide (4), and 16-hydroxytriptonide (5), among which 2, 4 and 5 are new compounds. All the three new transformed products showed cytotoxic activities against the majority of the human tumor cell lines tested, however, they are found to possess less cytotoxic activity when compared with 1. Both compounds 4 and 5 showed similar cytotoxic activity and their IC (50) values were 5-15 fold less than 1, while 2 is about 100 times less active than 1.
- Subjects :
- Stereochemistry
Pharmaceutical Science
Analytical Chemistry
Inhibitory Concentration 50
chemistry.chemical_compound
Biotransformation
Cell Line, Tumor
Drug Discovery
Humans
Cytotoxicity
Pharmacology
biology
Plant Extracts
Organic Chemistry
Aspergillus niger
Biological activity
Triptolide
biology.organism_classification
Antineoplastic Agents, Phytogenic
Triterpenes
Terpenoid
Complementary and alternative medicine
Biochemistry
chemistry
Molecular Medicine
Tripterygium wilfordii
Diterpene
Phytotherapy
Subjects
Details
- ISSN :
- 14390221 and 00320943
- Volume :
- 69
- Database :
- OpenAIRE
- Journal :
- Planta Medica
- Accession number :
- edsair.doi.dedup.....a8148ada0f10d5989db7d2d400567deb