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. 2021 Apr 22;26(9):2438. doi: 10.3390/molecules26092438

Table 3.

Summary of the most recent researches that have studied the potential of lipophenols for their use in the prevention and treatment of several human diseases and pathologies.

Lipophenol Dose Model Health Effects of the Combination Reference
  • In vitro studies

Isopropyl-phloroglucinol (IP)-DHA; IP–D2-DHA; IP–D4-DHA. 0–80 µM for 1 h. ARPE-19 cells. Reduced radical lipid peroxidation status on cells under oxidative conditions as a model of age-related macular degeneration and Stargardt’s disease. [101]
IP-DHA. 0–80 µM for 1 h. Primary rat RPE, mouse neural retina and human ARPE-19 cells. Both polyphenol and PUFAs are needed for anti-carbonyl and anti-oxidative capacities;
Protection against a lethal dose of all-trans-retinal;
Long term protection effects.
[102]
Quercetin conjugated to DHA (Q-3-DHA). 0–80 µM for 1 h. ARPE-19 cells. Less toxicity that quercetin alone and better anti-carbonyl capacity. [103]
Q-3-DHA-7OiP (quercetin-isopropyl DHA). 0–80 µM for 1 h. ARPE-19 cells. Highly capacity against carbonyl and oxidative stresses. [104]
Quercetin-3-O-glucoside (Q3G)-EPA and -DHA. 1 mM for 48 h at 37 °C. Normal diploid human fetal lung fibroblast cell line (WI-38);
Fresh human normal primary hepatocytes (h-NHEPS™).
Greater cell viability upon H2O2 exposure in lung and liver;
Lower production of lipid hydroperoxides under induced oxidative stress.
[105]
Quercetin-3-O-glucoside (Q3G)-EPA and -DHA. 1 mM for 48 h at 37 °C. Normal diploid human fetal lung fibroblast cell line (WI-38). Protection against nicotine- and Cr(VI)-induced cell death and membrane lipid peroxidation;
A less inflammatory response (lesser COX-2 and PGE2).
[106]
DHA linked to resveratrol (RES-DHA). 10, 20, 40, or 80 μM for 72 h. THP-1 monocytes. Capacity for inhibiting MMP-9. [107]
  • In vivo studies

IP-DHA. An intravenous injection at doses from 5 to 30 mg/kg body weight;
An orally gavaged administration at doses from 40 to 150 mg/kg body weight.
Albino Abca4−/− mice. A dose-dependently decreased light-induced photoreceptor degeneration and preserved visual sensitivity by reducing carbonyl stress in the retina;Long term protection effects. [108]
Acylated phloridzin-DHA (PZ-DHA). In vitro: 10, 50, 100 µM for 24 h at 37 °C;
In vivo: 5 intra-tumoral injections of PZ-DHA: 0.75 mg/kg;
15-days.
Mammary carcinoma (MDA-MB-231, MDA-MB-468, 4T1, MCF-7 and T-47D) cells;
Female non-obese diabetic severe combined immunodeficient (NOD-SCID) mice.
Selectively cytotoxic to breast cancer cells in vitro and in vivo. [109]
Acylated phloridzin-DHA (PZ-DHA). In vitro: 10 µM for 24 h at 37 °C;
In vivo: Intraperitoneal injection of PZ-DHA (100 mg/kg body weight) every second day for 9 days;
17-days.
Mammary carcinoma (MDA-MB-231, MDA-MB-468, 4T1, MCF-7 and T-47D) cells;
BALB/c and NOD-SCID female mice.
Potential prevention or inhibition of triple-negative breast cancer (TNBC). [110]