Comprehensive Review on Betulin as a Potent Anticancer Agent

Król, Sylwia; Kiełbus, Michał; Rivero-Müller, Adolfo; Stepulak, Andrzej

doi:10.1155/2015/584189

Cited by 170 publications

(114 citation statements)

References 79 publications

(169 reference statements)

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Numerous anticancer strategies are based on inhibition of cell proliferation and promotion of cell death [12]. Natural compounds derived from plants are frequently used as potential anticancer substances [13, 14]; these compounds are easily available because of their common occurrence in nature. Our results obtained from proliferation assay indicated that the highest cytotoxicity in metastatic Me-45 melanoma cells was obtained after 72 h incubation with new betulin derivatives containing lysine and ornithine (IC 50 = 2.456 μM; IC 50 = 2.465 μM, respectively).…”

Section: Resultsmentioning

confidence: 99%

Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)

Drąg-Zalesińska¹,

Drąg²,

Poręba³

et al. 2017

Cancer Cell Int

View full text Add to dashboard Cite

BackgroundBetulinic acid and betulin are triterpenes that have anticancer properties in various types of cancer. Unfortunately, the bioavailability and the bio-distribution of betulinic acid and its metabolic precursor, betulin are very low because of poor solubility in aqueous buffers.MethodsIn this study, we examined the anticancer properties of the ester derivatives of betulin compared to their precursors in a malignant melanoma cell line. We assessed five amino acid esters of betulin. The compounds contained four basic amino acids—natural lysine (l-Lys-OH) and three of its derivatives (l-Dap-OH, l-Dab-OH, and l-Orn-OH)—and alanine (l-Ala-OH) as a negative control (amino acid without an amine group in the side chain). The derivatives were more soluble than their precursors (betulin and betulinic acid) in water. The betulin esters were tested in the malignant melanoma cell line Me-45. To evaluate the cytotoxicity, MTT test was performed after 24, 48 and 72 h of incubation with the test compounds at a concentration range of 0.75–100 μM. For analysis of the apoptotic activity, TUNEL assay was performed. Additionally, expression of caspase-3 and PARP-1 was investigated immunocytochemically.ResultsThe highest biological activity was observed with the lysine ester. The results showed that the highest cytotoxicity and the highest number of positively stained nuclei in metastatic melanoma Me-45 cells were obtained after 72 h of incubation with betulin derivatives containing lysine and ornithine.ConclusionsThe betulin ester derivatives showed enhanced antitumor activity compared to their non-modified precursors. Esters of betulin can be more potent anticancer agents than their precursor as a consequence of the rapid bioavailability and increased concentration in cancer cells.

show abstract

Section: Resultsmentioning

confidence: 99%

Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)

Drąg-Zalesińska¹,

Drąg²,

Poręba³

et al. 2017

Cancer Cell Int

View full text Add to dashboard Cite

show abstract

“…Reviews on anticancer properties of betulinic acid (5) and its derivatives have been provided [25][26][27][28][29][30]. A review on the anticancer and chemopreventive potential of betulin (4) in vitro and in vivo has also been provided [31].…”

Section: Resultsmentioning

confidence: 99%

Triterpenes From Ceriops Decandra (Griff.) W. Theob.

Perez

Shen

Ragasa

2017

Asian J Pharm Clin Res

View full text Add to dashboard Cite

Objective: To isolate and identify the chemical constituents of Ceriops decandra. Methods:The chemical constituents of C. decandra (Griff.) W. Theob. were isolated by silica gel chromatography. The structures of the isolated compounds were identified by nuclear magnetic resonance (NMR) spectroscopy.Results: Chemical investigation of the dichloromethane extracts of the leaves of C. decandra has led to the isolation of 3β-E-coumaroylbetulinic acid (1), lupeol fatty acid esters (2), betulonic acid (3), betulin (4), betulinic acid (5), lupeol (6), lupenone (7), and a mixture of 3β-E-feruloyllupeol (8) and 3β-Z-feruloyllupeol (9), and chlorophyll a (10). The structures of 1-10 were identified by comparison of their NMR data with literature data. Conclusion:To the best of our knowledge, this is the first report on the isolation of 1-3 from C. decandra. Literature search revealed that the triterpenes isolated from C. decandra exhibited anticancer properties.

show abstract

“…Fatostatin, a chemical SREBP inhibitor, has been found to suppress prostate cancer cell proliferation and reduce tumor growth 50. In addition, the natural compound betulin, which inhibits SREBP activation, has been shown to have broad spectrum of anticancer activity in vitro and in vivo 51. Inhibition of ACS by Triacscin C significantly induces apoptosis in p53-defective human cancer cells and suppresses growth of xenograft tumors 52…”

Section: Anticancer Agents Targeting Lipid Metabolic Reprogrammingmentioning

confidence: 99%

Targeting Lipid Metabolic Reprogramming as Anticancer Therapeutics

Young

Lee

2016

J Cancer Prev

View full text Add to dashboard Cite

Cancer cells rewire their metabolism to satisfy the demands of growth and survival, and this metabolic reprogramming has been recognized as an emerging hallmark of cancer. Lipid metabolism is pivotal in cellular process that converts nutrients into energy, building blocks for membrane biogenesis and the generation of signaling molecules. Accumulating evidence suggests that cancer cells show alterations in different aspects of lipid metabolism. The changes in lipid metabolism of cancer cells can affect numerous cellular processes, including cell growth, proliferation, differentiation, and survival. The potential dependence of cancer cells on the deregulated lipid metabolism suggests that enzymes and regulating factors involved in this process are promising targets for cancer treatment. In this review, we focus on the features associated with the lipid metabolic pathways in cancer, and highlight recent advances on the therapeutic targets of specific lipid metabolic enzymes or regulating factors and target-directed small molecules that can be potentially used as anticancer drugs.

show abstract

Comprehensive Review on Betulin as a Potent Anticancer Agent

Cited by 170 publications

References 79 publications

Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)

Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)

Triterpenes From Ceriops Decandra (Griff.) W. Theob.

Targeting Lipid Metabolic Reprogramming as Anticancer Therapeutics

Contact Info

Product

Resources

About