Antiproliferative Properties of Labdane Diterpenoids from Croton sylvaticus Hochst against Drug Sensitive and Resistant Leukemia cell lines
Okerio, Kefah N
Kenanda, Evans O
Omosa, Leonidah K
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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.
CitationOkerio 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.
University of Nairobi
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