Hesperidin (Hsd) and its aglycone,
hesperetin (Hst), are two
flavonoids from citrus species that have various
biological properties, particularly those for the prevention of
cancer and
cardiovascular diseases. Studies have shown both anti-
cancer and
cancer chemopreventive effects for Hsd and Hst.
Cancer chemopreventive properties of Hsd and Hst are mainly associated with their
antioxidant, radical scavenging and anti-inflammatory activities. In addition, Hsd and Hst interfere at different stages of
cancer. Unlike conventional anti-
cancer drugs, Hsd and Hst inhibit
tumor growth by targeting multiple cellular
protein targets at the same time, including
caspases, Bcl-2 (
B-cell lymphoma 2) and Bax (
Bcl-2 associated X protein) for the induction of apoptosis, and COX-2 (cyclooxygenase-2), MMP-2 (matrix metalloproteinase-2) and MMP-9 for the inhibition of angiogenesis and
metastasis. The results of the recent basic and clinical studies revealed the beneficial effects for Hst, Hsd and their derivatives in the treatment of
heart failure and cardiac remodeling,
myocardial ischemia and
infarction, and
hypertension. In addition, the valuable effects of Hst and Hsd in the treatment of diabetes and
dyslipidemia with their anti-platelet and
anticoagulant effects make them good candidates in the treatment of various
cardiovascular diseases. In this review, new findings regarding the molecular targets of Hsd and Hst, animal studies and clinical trials are discussed.