Application of Chlorogenic Acid

Cardiovascular Protective Effects
Oxygen free radicals are among the important factors causing endothelial injury, and numerous experiments have demonstrated that chlorogenic acid acts as a free radical scavenger and antioxidant [23, 24]. By scavenging oxygen free radicals and inhibiting lipid peroxidation, it protects vascular endothelial cells, thereby exerting effective protective effects on the cardiovascular system. Studies have also shown that chlorogenic acid can protect myocardial cells.

Antioxidant Effects
The active hydroxyl groups in the chlorogenic acid molecule can form hydrogen free radicals with antioxidant properties, thereby eliminating the reactivity of hydroxyl free radicals and protecting tissues from oxidative damage. This may be related to chlorogenic acid's ability to inhibit the formation of 8-hydroxy-2'-deoxyguanosine (8-OH-dG) when DNA is attacked by reactive oxygen species.
Research indicates that chlorogenic acid exhibits free radical-scavenging activity in a dose-dependent manner. Other studies have confirmed that chlorogenic acid extracted from green tea, coffee, and Artemisia capillaris also demonstrates significant antioxidant effects.

Anti-UV and Anti-Radiation Effects
Studies have shown that natural polyphenols, represented by chlorogenic acid, can protect collagen from damage caused by reactive oxygen species and other free radicals, effectively preventing UV-induced harm to human skin. Several European patents have been granted for skin sunscreens and shampoos incorporating chlorogenic acid, which exhibit anti-radiation properties.

Antimutagenic and Anticancer Effects
Numerous experiments have demonstrated the antimutagenic and anticancer effects of chlorogenic acid. For example, chlorogenic acid in vegetables and fruits can inhibit the mutagenicity of carcinogens such as aflatoxin B1 and benzo[a]pyrene by inhibiting activating enzymes. Under alkaline conditions, chlorogenic acid induces significant DNA fragmentation and nuclear condensation in tumor cells. It also suppresses the elevation of 8-OH-dG induced by 4-nitroquinoline-1-oxide (4NQO), a critical biomarker in carcinogenesis and cellular oxidative stress. Additionally, chlorogenic acid reduces the bioavailability and hepatic transport of carcinogens, contributing to its chemopreventive effects.

Antibacterial and Antiviral Effects
In terms of antibacterial activity, chlorogenic acid is widely recognized for its efficacy against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, and Legionella. For instance, chlorogenic acid extracted from Lonicera japonica exhibits potent activity against S. aureus and E. coli.
Similarly, chlorogenic acid from tobacco demonstrates inhibitory effects against S. aureus, E. coli, and Bacillus subtilis. Its antimicrobial mechanism may involve non-competitive inhibition of bacterial arylamine acetyltransferase. Regarding antiviral activity, chlorogenic acid isolated from Farfarae Flos extracts has been shown to inhibit influenza virus, respiratory syncytial virus, and adenovirus.

Lipid-Lowering Effects
Studies indicate that oral administration of chlorogenic acid reduces visceral fat accumulation and body fat in rats. Intravenous administration of chlorogenic acid (5 mg/mL) for three weeks decreases plasma cholesterol and triglyceride levels by 44%. Lonicera japonica extracts also reduce serum and liver tissue lipids.

Antileukemic Effects
Research on the inhibitory effects of chlorogenic acid on leukemia cells reveals that chlorogenic acid sodium, stored at -20°C in the dark, selectively inhibits the proliferation of bcr-abl-positive K562 leukemia cells. Chlorogenic acid sodium stored at 4°C shows enhanced inhibitory effects on K562 cells and also suppresses the proliferation of bcr-abl-negative Jurkat cells. Screening of phenolic compounds from Sargentodoxa cuneata identified chlorogenic acid as an inhibitor of human chronic myelogenous leukemia K562 cells.

Immunomodulatory Effects
Chlorogenic acid significantly affects the levels of NF-γ and TNF-α in supernatants from intraepithelial lymphocytes (IEL) and intestinal lamina propria lymphocytes (LPL). In vitro studies show that chlorogenic acid enhances T-cell proliferation induced by influenza virus antigens and induces the production of IFN-γ and IFN-α in human lymphocytes and peripheral blood leukocytes.
Furthermore, chlorogenic acid increases IgE, IgG1, and IL-4 levels in rats and enhances macrophage function, indicating its immunomodulatory capacity.

Hypoglycemic Effects
Pharmacodynamic studies on the hypoglycemic effects of chlorogenic acid demonstrate that its crude extract effectively reduces blood glucose in alloxan-induced diabetic mice, with no significant dose-dependent differences observed among high-, medium-, and low-dose groups. However, it has no marked effect on normal mouse blood glucose. Lonicera japonica extracts also lower blood glucose in sucrose-induced hyperglycemic mice and alloxan-induced diabetic models.
Notably, the hypoglycemic effect of chlorogenic acid within 3 hours is statistically comparable to that of glibenclamide. Its mechanism may involve inhibition of glucose-6-phosphatase and glucose absorption.

Additional Pharmacological Activities
Beyond the aforementioned activities, chlorogenic acid exhibits anti-inflammatory effects by inhibiting hyaluronidase (HAase) activity. It also possesses hepatoprotective, choleretic, and antispasmodic properties.

Cardiovascular Protective Effects
Oxygen free radicals are among the important factors causing endothelial injury, and numerous experiments have demonstrated that chlorogenic acid acts as a free radical scavenger and antioxidant [23, 24]. By scavenging oxygen free radicals and inhibiting lipid peroxidation, it protects vascular endothelial cells, thereby exerting effective protective effects on the cardiovascular system. Studies have also shown that chlorogenic acid can protect myocardial cells.

Antioxidant Effects
The active hydroxyl groups in the chlorogenic acid molecule can form hydrogen free radicals with antioxidant properties, thereby eliminating the reactivity of hydroxyl free radicals and protecting tissues from oxidative damage. This may be related to chlorogenic acid's ability to inhibit the formation of 8-hydroxy-2'-deoxyguanosine (8-OH-dG) when DNA is attacked by reactive oxygen species.
Research indicates that chlorogenic acid exhibits free radical-scavenging activity in a dose-dependent manner. Other studies have confirmed that chlorogenic acid extracted from green tea, coffee, and Artemisia capillaris also demonstrates significant antioxidant effects.

Anti-UV and Anti-Radiation Effects
Studies have shown that natural polyphenols, represented by chlorogenic acid, can protect collagen from damage caused by reactive oxygen species and other free radicals, effectively preventing UV-induced harm to human skin. Several European patents have been granted for skin sunscreens and shampoos incorporating chlorogenic acid, which exhibit anti-radiation properties.

Antimutagenic and Anticancer Effects
Numerous experiments have demonstrated the antimutagenic and anticancer effects of chlorogenic acid. For example, chlorogenic acid in vegetables and fruits can inhibit the mutagenicity of carcinogens such as aflatoxin B1 and benzo[a]pyrene by inhibiting activating enzymes. Under alkaline conditions, chlorogenic acid induces significant DNA fragmentation and nuclear condensation in tumor cells. It also suppresses the elevation of 8-OH-dG induced by 4-nitroquinoline-1-oxide (4NQO), a critical biomarker in carcinogenesis and cellular oxidative stress. Additionally, chlorogenic acid reduces the bioavailability and hepatic transport of carcinogens, contributing to its chemopreventive effects.

Antibacterial and Antiviral Effects
In terms of antibacterial activity, chlorogenic acid is widely recognized for its efficacy against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, and Legionella. For instance, chlorogenic acid extracted from Lonicera japonica exhibits potent activity against S. aureus and E. coli.
Similarly, chlorogenic acid from tobacco demonstrates inhibitory effects against S. aureus, E. coli, and Bacillus subtilis. Its antimicrobial mechanism may involve non-competitive inhibition of bacterial arylamine acetyltransferase. Regarding antiviral activity, chlorogenic acid isolated from Farfarae Flos extracts has been shown to inhibit influenza virus, respiratory syncytial virus, and adenovirus.

Lipid-Lowering Effects
Studies indicate that oral administration of chlorogenic acid reduces visceral fat accumulation and body fat in rats. Intravenous administration of chlorogenic acid (5 mg/mL) for three weeks decreases plasma cholesterol and triglyceride levels by 44%. Lonicera japonica extracts also reduce serum and liver tissue lipids.

Antileukemic Effects
Research on the inhibitory effects of chlorogenic acid on leukemia cells reveals that chlorogenic acid sodium, stored at -20°C in the dark, selectively inhibits the proliferation of bcr-abl-positive K562 leukemia cells. Chlorogenic acid sodium stored at 4°C shows enhanced inhibitory effects on K562 cells and also suppresses the proliferation of bcr-abl-negative Jurkat cells. Screening of phenolic compounds from Sargentodoxa cuneata identified chlorogenic acid as an inhibitor of human chronic myelogenous leukemia K562 cells.

Immunomodulatory Effects
Chlorogenic acid significantly affects the levels of NF-γ and TNF-α in supernatants from intraepithelial lymphocytes (IEL) and intestinal lamina propria lymphocytes (LPL). In vitro studies show that chlorogenic acid enhances T-cell proliferation induced by influenza virus antigens and induces the production of IFN-γ and IFN-α in human lymphocytes and peripheral blood leukocytes.
Furthermore, chlorogenic acid increases IgE, IgG1, and IL-4 levels in rats and enhances macrophage function, indicating its immunomodulatory capacity.

Hypoglycemic Effects
Pharmacodynamic studies on the hypoglycemic effects of chlorogenic acid demonstrate that its crude extract effectively reduces blood glucose in alloxan-induced diabetic mice, with no significant dose-dependent differences observed among high-, medium-, and low-dose groups. However, it has no marked effect on normal mouse blood glucose. Lonicera japonica extracts also lower blood glucose in sucrose-induced hyperglycemic mice and alloxan-induced diabetic models.
Notably, the hypoglycemic effect of chlorogenic acid within 3 hours is statistically comparable to that of glibenclamide. Its mechanism may involve inhibition of glucose-6-phosphatase and glucose absorption.

Additional Pharmacological Activities
Beyond the aforementioned activities, chlorogenic acid exhibits anti-inflammatory effects by inhibiting hyaluronidase (HAase) activity. It also possesses hepatoprotective, choleretic, and antispasmodic properties.