Platinum(ii) complexes with rutaecarpine and tryptanthrin derivatives induce apoptosis by inhibiting telomerase activity and disrupting mitochondrial function

Abstract

BrTry-Pt is a telomerase inhibitor targeting the c-myc promoter, and triggered T-24 cell apoptosis, which also caused mitochondrial dysfunction and S phase arrest.

Complexes of Zn(ii) with a mixed tryptanthrin derivative and curcumin chelating ligands as new promising anticancer agents

“…Accordingly, the A549/DDP cells were found to be more susceptible to Zn(TAC) than to Zn(TA) and Zn(PA) , which was undoubtedly related to the key roles of the novel tryptanthrin derivative ( TA ) and H-Cur in the Zn(TAC) complex. 51,52 Furthermore, for the tested tumor cells, Zn(TAC) demonstrated better anticancer activity than the Try derivative Pt( ii ) and Cu( ii ) complexes, 58,59 2,2′-bipyridine H-Cur Zn( ii ) complexes, and H-Cur Zn( ii )–BODIPY photosensitizers under the same conditions. 54–57 Notably, Zn(TA) and Zn(TAC) also displayed low cytotoxicity against normal HL-7702 cells (Table 1), indicating that Zn(TAC) could be a promising Zn( ii )-based therapeutic drug against cancer not only due to its treatment efficiency but also due to its tumor selectivity and anticisplatin resistance properties.…”

“…These findings support the theory that Zn(TA) and Zn(TAC) induce apoptosis-mediated cell death. In comparison with Zn(TAC) , the rates of apoptosis of tumor cells induced by Zn(TA) and Try derivative Pt( ii ) and Cu( ii ) complexes were low, 58,59 which was undoubtedly associated with the key roles of TA and H-Cur ligands in the Zn(TAC) complex. 51,52…”

“…51,52 Thus, it could be concluded that A549/DDP cells more readily took up Zn(TAC) than Zn(TA) , which resulted in a stronger and more prominent red fluorescence signal. The results also suggested that the anticancer mechanisms of Zn(TA) and Zn(TAC) are distinct from those of Zn( ii )–cryptolepine–H-Cur molecular probes, 51,52 2,2′-bipyridine H-Cur Zn( ii ) complexes, H-Cur Zn( ii )–BODIPY photosensitizers, 54–57 quinoline–coumarin Pt( ii ) complexes, 71 (ox)oisoaporphine Pt( ii ) and Ru( ii ) complexes, 72,73 Try derivative Pt( ii ) and Cu( ii ) complexes, 58,59 and jatrorrhizine and berberine Pt( ii ) complexes. 74,75…”

Synthetic Tryptanthrin Derivatives Induce Cell Cycle Arrest and Apoptosis via Akt and MAPKs in Human Hepatocellular Carcinoma Cells

“…Compared with sorafenib, A1 and A6 demonstrated a higher anti-proliferative effect in Hep3B cells. Qin et al reported that metal-tryptanthrin complexes cause S-phase arrest by inhibiting telomerase in bladder cancer cells [ 36 ]. Benzo[ b ]tryptanthrin suppresses cell growth by inhibiting Topo II, a ubiquitous enzyme that is essential in the regulation of DNA topology [ 37 ], in breast cancer cells [ 38 ].…”

Selection of Small Molecules that Bind to and Activate the Insulin Receptor from a DNA-Encoded Library of Natural Products

“…Metformin ( CSD-JAMRIY01) (Childs et al, 2004) , an oral diabetes medicine, showed striking structural similarity to Rutaecarpine (CSD-OGAXEC) Qin et al, 2018 , in that the arrangement of the five nitrogen hetero atoms of the bis-guanidine appears to be the same in both molecules (Figure 4A).…”