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1536955 
Journal Article 
The Molecular Basis for the Pharmacological Activity of Anthocyans 
Domitrovic, R 
2011 
Yes 
Current Medicinal Chemistry
ISSN: 0929-8673
EISSN: 1875-533X 
18 
29 
4454-4469 
21864288 
WOS:000299011500003 
This review summarizes the current knowledge of the
regulatory role of pure anthocyans in cellular signaling pathways and gene expression. The
molecular basis for anthocyans pharmacological activity includes the regulation of plethora of
mechanisms mainly involved in: (1) suppression of the inflammatory response through targeting the
phospholipase A2 and PI3K/Akt and NF-kappa B pathways, (2) protection from cardiovascular disease
by exerting (i) antihypertensive and endothelium-protective activity through targeting the
Akt/eNOS and ACE pathways (ii) antiatherogenic activity through targeting NF-kappa B mediated
VCAM and ICAM expression, (3) growth/differentiation control and tumor suppression by exerting
(i) anticancerogenic activity through targeting the EGF and HGF signaling pathways (ii) tumor
anti-invasive activity through targeting the VEGF signaling pathway and ECM degrading enzymes
(iii) cell cycle arrest and induction of apoptosis through the JNK/p38 MAPK mediated caspase
activation (iv) modulation of chemotherapeutic efficacy by affecting resistance to anticancer
drugs, (4) reduction of diabetes incidence through modulation of insulin sensitivity and glucose
utilization, (5) neuroprotection through amelioration of oxidative stress and A beta deposition,
and (6) hepatoprotective activity through interference with TNF-alpha and TGF-beta in the liver.
The estrogen-like activity of anthocyans could be utilized in cancer and hormone-replacement
therapy. These data provide a concise insight into molecular mechanisms of protective and
therapeutic activity of anthocyans in various pathological conditions, which may not be
attributed solely to their antioxidant activity but also to direct blockage of signaling
pathways. Structure-activity analysis reveals that the number of hydroxyl groups and presence of
sugar moiety are crucial for their specific modulatory actions. 
Anthocyanins; anthocyanidins; signaling pathway; inflammation; cancer; cardiovascular disease; diabetes mellitus; neuronal damage; liver fibrosis