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

Overview of attention for article published in Cancer Cell International, January 2017
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Title
Anticancer properties of ester derivatives of betulin in human metastatic melanoma cells (Me-45)
Published in
Cancer Cell International, January 2017
DOI 10.1186/s12935-016-0369-3
Pubmed ID
Authors

Małgorzata Drąg-Zalesińska, Marcin Drąg, Marcin Poręba, Sylwia Borska, Julita Kulbacka, Jolanta Saczko

Abstract

Betulinic 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. In 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. The 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. The 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.

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Mendeley readers

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Geographical breakdown

Country Count As %
Unknown 48 100%

Demographic breakdown

Readers by professional status Count As %
Student > Ph. D. Student 7 15%
Student > Bachelor 6 13%
Student > Master 5 10%
Researcher 4 8%
Lecturer 3 6%
Other 10 21%
Unknown 13 27%
Readers by discipline Count As %
Biochemistry, Genetics and Molecular Biology 14 29%
Medicine and Dentistry 6 13%
Pharmacology, Toxicology and Pharmaceutical Science 5 10%
Chemistry 4 8%
Agricultural and Biological Sciences 3 6%
Other 2 4%
Unknown 14 29%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 20 January 2017.
All research outputs
#18,518,987
of 22,940,083 outputs
Outputs from Cancer Cell International
#1,096
of 1,809 outputs
Outputs of similar age
#311,292
of 421,474 outputs
Outputs of similar age from Cancer Cell International
#5
of 7 outputs
Altmetric has tracked 22,940,083 research outputs across all sources so far. This one is in the 11th percentile – i.e., 11% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,809 research outputs from this source. They receive a mean Attention Score of 3.9. This one is in the 24th percentile – i.e., 24% of its peers scored the same or lower than it.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 421,474 tracked outputs that were published within six weeks on either side of this one in any source. This one is in the 15th percentile – i.e., 15% of its contemporaries scored the same or lower than it.
We're also able to compare this research output to 7 others from the same source and published within six weeks on either side of this one. This one has scored higher than 2 of them.