Abstract
MiR-21, a non-coding miRNA with 22 nucleotides, plays an important part in the proliferation, invasion, and metastasis of tumor cells. The present study demonstrates that isomers of chiral ruthenium(II) complexes with alkynes (Λ-1 and Δ-1) were synthesized by Songogashira coupling reaction by using microwave-assisted synthetic technology. The isomers can recognize and stabilize miR-21, with the Λ-isomer showing a stronger binding capacity than the Δ-isomer. Further studies showed that both isomers can be uptaken by MDA-MB-231 cells and enriched in the nucleus. Treatment with the Λ-/Δ-isomer downregulated the expression of miR-21. In a word, the development of chiral ruthenium(II) complexes act as potential inhibitors against tumor cells by recognizing, stabilizing, and regulating the expression of miR-21.
Highlights
Increasing attention has been focused on small-molecule targeting drugs over the last decades, and some of these drugs, including NAMI-A, KP1019, and CX-3543, have been undergone clinical trials [1,2,3,4,5]
MiR-21 (Fig. 1b), a miRNA overexpressed in almost all types of human malignancy, is involved in multifarious cancerassociated processes, including proliferation, invasion, and metastasis [20,21,22]
We demonstrated that the effect of miR-21 on phosphatase and tensin homolog deleted on the chromosome ten/protein kinase B (AKT) signaling pathway is abrogated by the arene ruthenium complexes, and the miR-21 inhibitor could enhance the antitumor capability [53]
Summary
Increasing attention has been focused on small-molecule targeting drugs over the last decades, and some of these drugs, including NAMI-A, KP1019, and CX-3543, have been undergone clinical trials [1,2,3,4,5]. With the rapid development of tumor targeting small molecules, the multidrug resistance and dependencies of cancer cells have become more serious [6,7,8]. Novel compounds that suppress the proliferation of tumor cells by regulating the expression of target genetic fragments must be designed [9]. MiR-21 (Fig. 1b), a miRNA overexpressed in almost all types of human malignancy, is involved in multifarious cancerassociated processes, including proliferation, invasion, and metastasis [20,21,22]. Curcumin could suppress tumor cells growth, invasion and metastasis by significantly inhibiting miR21 expression [29]. A recent study has found that miR-21 regulates cell apoptosis. Sasaki indicated that the apoptosis induction of tumor cells can be suppressed by upregulating the expression of miR-21 [31].
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