Antiproliferative Properties of Labdane Diterpenoids from Croton sylvaticus Hochst against Drug Sensitive and Resistant Leukemia cell lines
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Date
2019Author
Okerio, Kefah N
Kenanda, Evans O
Omosa, Leonidah K
Type
ArticleLanguage
enMetadata
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Background: Cancer treatment failure is majorly attributed to the emergency of multi-drug resistance of cancer cells towards most conventional
drugs used in chemotherapy hence the need for more active principles with less side effective from natural sources.
Methods: Characterization of isolated compounds was achieved using NMR spectroscopy and comparison of acquired data with literature
values. The antiproliferative properties were determined using resazurin reduction assay.
Results: Three labdane diterpenoids namely; 18-nor-labd-13(E)-ene-8α, 15-diol (1), labd-13(E)-ene-8α, 15-diol (2) and austroinulin (3) were
isolated from the stem bark of Croton sylvaticus. The crude extract was active at 10 µg/mL with cell inhibition of 86.96±4.86 against drug
sensitive CCRF-CEM and 77.57±2.84% against drug resistant CEM/ADR5000 leukemia cell lines. However, all the compounds displayed lower
antiproliferative potencies as they exhibited cell inhibitions<70% of the cell population at 10 µM. The cell inhibition of doxorubicin, was
94.89±0.86% and 24.20±2.89% against CCRF-CEM and CEM/ADR5000 cells, respectively. From these observations, it is clear that
CEM/ADR5000 are resistant to doxorubicin while the activities of the compounds were similar against the two cell lines. This could be attributed
to the similarities in their skeletal structures. Furthermore, 1 and 3 were more active than doxorubicin against CEM/ADR5000 cells.
Conclusion: The labdane diterpenoids displayed low cytotoxicity against CCRF-CEM cells and CEM/ADR5000 as compared to the crude
extract. Doxorubicin was inactive against CEM/ADR5000 cells. Furthermore, 1 and 3 were more active than doxorubicin against CEM/ADR5000
cells. These compounds could be modified to obtained analogues with improved activities against the drug resistant cells.
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https://profiles.uonbi.ac.ke/lkerubo/publications/antiproliferative-properties-labdane-diterpenoids-croton-sylvaticus-hochst-agaihttps://www.investchempharma.com/wp-content/uploads/2019/07/www.investchempharma.com-antiproliferative-properties-of-labdane-diterpenoids-from-croton-sylvaticus-hochst-against-drug-sensitive-and-resistant-leukemia-cell-lines-imcp31-okerio-et-al.pdf
http://erepository.uonbi.ac.ke/handle/11295/155497
Citation
Okerio KN, Kenanda EO, Omosa LK. "Antiproliferative Properties of Labdane Diterpenoids from Croton sylvaticus Hochst against Drug Sensitive and Resistant Leukemia cell lines." Investigational Medicinal Chemistry & Pharmacology. 2019;2(2):31.Publisher
University of Nairobi
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Attribution-NonCommercial-NoDerivs 3.0 United StatesUsage Rights
http://creativecommons.org/licenses/by-nc-nd/3.0/us/Collections
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