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  • 1
    Language: English
    In: Molecular diversity, 2017-08, Vol.21 (3), p.547-564
    Description: Tubuloclustin [N-(7-adamant-2-yloxy-7-oxoheptanoyl)-N-deacetylcolchicine], a highly cytotoxic anti-tubulin compound is known for its ability to promote microtubule disassembly followed by the formation of tubulin clusters of unique morphology. Three series of antimitotic agents related to tubuloclustin were designed and synthesized in order to enhance the molecular diversity of “tubuloclustin-like” family of compounds. The series of compounds with modified adamantane moiety was highly potent in cytotoxic effect on human lung carcinoma A549 cells (EC50 = 6–400 nM) and was active in affecting the microtubule arrays and induction of strong tubulin clusterization. In two other sets of compounds, the colchicine moiety of tubuloclustin was replaced by podophyllotoxin or combretastatin A-4. All combretastatin A-4 derivatives displayed noticeable cytotoxic activity ( $$\hbox {EC}50=0.8{-}1.6\,\upmu \hbox {M}$$ EC 50 = 0.8 - 1.6 μ M ) but their effect on microtubules depended on the position of the linker attachment. Podophyllotoxin derivatives were also toxic to A549 cells ( $$\hbox {EC}50=0.38{-}0.50\,\upmu \hbox {M}$$ EC 50 = 0.38 - 0.50 μ M ) and caused both microtubule depolymerization and some tubulin clustering. The data obtained gave additional evidence that the whole panel of C7-colchicine, podophyllotoxin and combretastatin derivatives could manifest clustering effect, and the strength of this effect correlated with cytotoxic activity of the compounds.
    Subject(s): A549 Cells ; Adamantane ; Adamantane - analogs & derivatives ; Adamantane - chemistry ; Antimitotic agents ; Antimitotic Agents - chemical synthesis ; Antimitotic Agents - chemistry ; Antimitotic Agents - pharmacology ; Antineoplastic agents ; Biochemistry, general ; Cell Proliferation - drug effects ; Cell Survival - drug effects ; Chemical compounds ; Chemical synthesis ; Colchicine ; Colchicine - analogs & derivatives ; Colchicine - chemistry ; Combretastatin ; Cytotoxicity ; Humans ; Life Sciences ; Lung cancer ; Lungs ; Models, Molecular ; Molecular Structure ; Organic Chemistry ; Pharmacy ; Podophyllotoxin ; Polymer Sciences ; Tubulin - chemistry ; Tubulin - metabolism ; Tubulins ; Tubuloclustin
    ISSN: 1381-1991
    E-ISSN: 1573-501X
    Source: Alma/SFX Local Collection
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  • 2
    Language: English
    In: Journal of experimental biology, 2018-07-19, Vol.221
    Description: Optical imaging of gene expression by fluorescence hybridisation (FISH) in insects is often impeded by their pigmented cuticle. Since most chemical bleaching agents are incompatible with FISH, we developed a RNA interference-based method for clearing cuticular pigmentation which enables using whole-mount body appendages for RNA FISH. Silencing or in two leaf beetles species ( ) cleared their pigmented cuticle and decreased light absorbance. Subsequently, intact appendages (palps, antennae, legs) from RNAi-cleared individuals were used to image expression and spatial distribution of antisense mRNA of two chemosensory genes (gustatory receptor, odorant-binding protein). Imaging did neither work for RNAi-controls due to retained pigmentation, nor for FISH-controls (sense mRNA). Several bleaching agents were incompatible with FISH, either due to degradation of RNA, lack of clearing efficacy or long incubation times. Overall, silencing pigmentation genes is a significant improvement over bleaching agents enabling FISH in intact appendages.
    ISSN: 0022-0949
    E-ISSN: 1477-9145
    Source: HighWire Press (Free Journals)
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