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Synthesis and cytotoxic activities of novel 4-methoxy-substituted and 5-methyl-substituted (3′S,4′S)-(-)-cis-khellactone derivatives that induce apoptosis via the intrinsic pathway

Overview of attention for article published in Drug Design, Development and Therapy, June 2017
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Title
Synthesis and cytotoxic activities of novel 4-methoxy-substituted and 5-methyl-substituted (3&prime;<em>S</em>,4&prime;<em>S</em>)-(-)-<em>cis</em>-khellactone derivatives that induce apoptosis via the intrinsic pathway
Published in
Drug Design, Development and Therapy, June 2017
DOI 10.2147/dddt.s131753
Pubmed ID
Authors

Jingrun Chen, Junjie Liu, Dongxiao Cui, Chaoqun Yan, Liqiang Meng, Liqian Sun, Shurong Ban, Rui Ge, Taigang Liang, Qingshan Li

Abstract

This study deals with the design and synthesis of a series of novel 4-methoxy-substituted and 5-methyl-substituted (3'S,4'S)-(-)-cis-khellactones. The newly synthesized compounds were characterized by (1)H nuclear magnetic resonance (NMR), (13)C-NMR, mass spectrometry, and elemental analysis. All the derivatives were subjected to in vitro cytotoxicity screening against HEPG-2 (human liver carcinoma), SGC-7901 (human gastric carcinoma), and LS174T (human colon carcinoma), by using the MTT assay. The results revealed that several of the 4-methoxy-substituted compounds exhibited potent cytotoxicity. Among these, compound 12e showed the highest activity against cancer cells which 50% inhibitory concentration (IC50) values were in the range of 6.1-9.2 μM with low toxicity on normal human hepatocyte. Preliminary investigation of possible mechanisms of action of compound 12e against HEPG-2 cells indicated possible induction of apoptosis, as determined by morphological observations and Annexin V/propidium iodide (PI) double staining, in addition to apparent dissipation of mitochondrial membrane potential (MMP), as measured by 5,5',6,6'-tetrachloro-1,1',3,3'-tetraethyl-imidacarbocyanine iodide (JC-1) staining in combination with the activation of caspase-9 and caspase-3 by Western blot analysis. Overall, the data suggest that compound 12e may be a promising potential anti-cancer agent that could act primarily by inducing apoptosis through the mitochondria-mediated intrinsic pathway in human hepatoma cells.

Twitter Demographics

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Mendeley readers

The data shown below were compiled from readership statistics for 5 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 5 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 2 40%
Student > Bachelor 1 20%
Unknown 2 40%
Readers by discipline Count As %
Medicine and Dentistry 2 40%
Biochemistry, Genetics and Molecular Biology 1 20%
Unknown 2 40%

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 12 July 2017.
All research outputs
#10,167,524
of 11,459,905 outputs
Outputs from Drug Design, Development and Therapy
#849
of 1,206 outputs
Outputs of similar age
#217,410
of 258,572 outputs
Outputs of similar age from Drug Design, Development and Therapy
#27
of 31 outputs
Altmetric has tracked 11,459,905 research outputs across all sources so far. This one is in the 1st percentile – i.e., 1% of other outputs scored the same or lower than it.
So far Altmetric has tracked 1,206 research outputs from this source. They receive a mean Attention Score of 3.8. This one is in the 1st percentile – i.e., 1% of its peers scored the same or lower than it.
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We're also able to compare this research output to 31 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.