Anti-cancer activities of diospyrin, its derivatives and analogues

• Published in: European journal of medicinal chemistry Vol. 45; no. 9; pp. 3519 - 3530
• Main Authors: Sagar, Sunil, Kaur, Mandeep, Minneman, Kenneth P., Bajic, Vladimir B.
• Format: Journal Article
• Language: English
• Published: Kidlington Elsevier Masson SAS 01.09.2010; Elsevier
• Subjects: Animals; Anti-cancer; Antineoplastic agents; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Apoptosis; Biological and medical sciences; Cell Line, Tumor; Computational Biology; Diospyrin; General aspects; Humans; Medical sciences; Naphthoquinones - chemistry; Naphthoquinones - pharmacology; Pharmacology. Drug treatments; Quinone; Reactive oxygen species; Reactive oxygen species; MCF-7; MTT; MG-63; HeLa; MPT; RBC; Cyp D; EBV; K-562; Anti-cancer; GSH; Quinone; EAC; HGF; SOD; GSTs; PBMC; A375; ECM; H 2O 2; CsA; ROS; Diospyrin; HL-60; Hep2; Apoptosis; Antineoplastic agent; Oxidative stress; Cytotoxicity; Naphthoquinone derivatives; In vitro; Biological activity; Cell line; Mechanism of action; Bioinformatics; Tumor cell
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2010.06.021

Natural products have played a vital role in drug discovery and development process for cancer. Diospyrin, a plant based bisnaphthoquinonoid, has been used as a lead molecule in an effort to develop anti-cancer drugs. Several derivatives/analogues have been synthesized and screened for their pro-apoptotic/anti-cancer activities so far. Our review is focused on the pro-apoptotic/anti-cancer activities of diospyrin, its derivatives/analogues and the different mechanisms potentially involved in the bioactivity of these compounds. Particular focus has been placed on the different mechanisms (both chemical and molecular) thought to underlie the bioactivity of these compounds. A brief bioinformatics analysis at the end of the article provides novel insights into the new potential mechanisms and pathways by which these compounds might exert their effects and lead to a better realization of the full therapeutic potential of these compounds as anti-cancer drugs. [Display omitted]