Antiproliferative Effects of Honey and of Its Polyphenols: A Review
Table 2
Summary of in vitro studies of honey polyphenols.
Compound
Cell line tested
Observation/result
Reference no.
CA, MC, PEDMC, PEC
HT -29
Toxicity: CA 2500 M PEC 60 M PEDMC 60 M MC 225 M Inhibition of DNA/RNA: 150 M MC, 40 M PEC and 20 M PEDMC TPK activity downregulation: 100 M of MC, 30 M of PEC and 20 M of PEDMC ODC activity downregulation: 150 M MC, 40 M PEC and 20 M PEDMC
(a) Maximum inhibition of NFB at 25 g/mL after TNF treatment (b) No inhibitory effect on AP-1, TFIID, and Oct-1 (c) Structural analogue 5, 6 dihydroxy strongly inhibited the NF-B
(a) CA and CAPE inhibited MMP-2 and 9 with IC50 of 10–20 M and 2–5 M (b) CA at the concentration of 200 g/mL reduced the cell viability to 61% viability compared to the controls, and the treatment with CAPE (20 g/mL) in HepG2 cells reduced the viability to 72% of the controls
(a) Galangin of 1–10 M also promoted antiproliferative effect which is evident after 48 hours of incubation (b) Active Caspase 3 , a hallmark of apoptosis process, was detected after 24 hours and 72 hours of incubation with 50 and 10 M of galangin respectively (c) Cell cycle analysis indicated the increase in the subG1 phase of galangin (10 M) treated cells
(a) Quercetin had a remarkable inhibitory effect on the activities of cytosolic PKC and membrane TPK from HL-60 cells in vitro, with IC50 values of about 30.9 and 20.1 M, respectively (b) Quercetin repressed the complete activity of phosphoinositides like PI, PIP, and PIP2 at the concentration of 80 M
(a) Quercetin in low concentration (1–20 M) promoted the cell proliferation whereas higher concentration (50–200 M) showed the concentration dependent cyotoxicity (b) Increase in TAC of cell extracts but higher concentrations of the quercetin led to a progressive decrease in the TAC
(a) Mitochondrial potential decreased caspase-3 level increased (b) Kaempferol growth inhibitory effect on HL-60 leukemia cells is due to heterogeneous response mainly dominated by cell cycle alternation although some degree of cytotoxicity results from apoptotic as well as nonapoptotic process
(a) IC50 was observed to be 8.02 g/mL for HepG2, 2.16 g/mL for Hep3B and 22.73 g/mL for PLC/PRF/5 (b) G2/M cell cycle arrest (c) Increase of p53 and p21/WAF1