Description
Ferulic acid is widely found in plants, especially in artichoke, eggplant and corn
bran. In addition, it is also present in a variety of Chinese herbal medicines, such as
angelica, dome, motherwort, snow ganoderma lucidum and so on.
Chemical Properties
Ferulic acid is a pale yellow solid, It belongs to the family of hydroxycinnamic acids. It is an abundant phenolic phytochemical found in plant cell wall components. Natural sources of ferulic acid are leaves and seeds of many plants, such as cereals, coffee, apples, artichokes, peanuts, oranges, pineapples and wine.
Physical properties
Appearance: light yellow crystalline powder. Solubility: slightly soluble in cold
water; soluble in hot water, with poor stability in aqueous solution; easily decomposed when encounter light; soluble in ethanol and ethyl acetate; slightly soluble in
ether; insoluble in benzene and petroleum ether. Melting point: 170–173?°C.
Indications
This product is mainly used for the treatment of atherosclerosis, coronary heart
disease and ischemic cerebrovascular disease.
Biotechnological Production
There are three different natural sources for ferulic acid. It could be produced from
low-molecular-weight ferulic conjugates. For example, ferulic acid has been
isolated from the waste material of rice bran oil production by hydrolyzing with
sodium hydroxide or potassium hydroxide at 90–100 C. Ferulic acid with a purity
of 70–90 % was produced within 8 h under atmospheric pressure
Another possibility is a direct extraction of ferulic acid from plant cell walls by
using feruloyl esterases. Various microorganism are able to secrete feruloyl
esterases (e.g. A. niger, Bacillus species and Clostridium thermocellum). The
enzymatic hydrolysis of sugar-beet pulp has been analyzed using a mixture of
carbohydrases from Aspergillus aculeatus with a final ferulic acid concentration of
200 mg.L-1 in the hydrolyzate. Moreover, a purification method to isolate
ferulic acid from sugar-beet pulp after enzymatic hydrolysis using a fixed-bed
adsorption with activated carbon has been developed. With this process, a purity of
50 % has been achieved. Finally, ferulic acid could be produced by cell
culture fermentations. For example, free ferulic acid (up to 50 mg.L-1) and
also conjugated to anthocyanins (up to 150 mg.L-1) has been accumulated in cell
cultures of Ajuga pyramidalis.
Pharmacokinetics
In clinical practice, Honghua and clopidogrel are often combined with FA-containing herbs to treat cardiovascular disease. Li et al. found that Ferulic acid (FA) was rapidly absorbed with a low bioavailability after a single oral administration. The pharmacokinetics profile of FA in rats was partly altered by the coadministration of FA with Honghua or clopidogrel. FA was rapidly absorbed following oral administration with a mean time to peak plasma concentration (T(max)) of 0.03 h. The corresponding maximum plasma concentration (C(max)) and the area under the concentration-time curve (AUC) were 8174.55 ng/L and 2594.45 h ng/mL, respectively. Coadministration of Honghua and clopidogrel resulted in a 63.5% and 79.7% increase in the AUC, respectively. The C(max) of FA was significantly increased by coadministration with clopidogrel (74.3%, p<0.01). Moreover, the T(max) of FA when coadministered with Honghua or clopidogrel was 3 and 3.76 times slower than when administered alone. The coadministrations also altered other pharmacokinetic parameters estimated for FA, but no statistically significant differences were observed[1].
Pharmacology
Orally administered ferulic acid completely prevents the formation of skin tumors, reverts the status of phase I and phase II detoxication agents, lipid peroxidaton byproducts and antioxidants to near-normal ranges in 7,12-DMBA-treated mice (Alias et al., 2009). The observation demonstrate that orally administered ferulic acid has potent suppressive effects on cell proliferation during DMBA-induced skin carcinogenesis.
Ferulic acid also has the capacity to prevent UV-induced damage to cells. Ferulic acid is often added as an ingredient to anti-aging supplements. When ferulic acid was incorporated into a formulation of α-tocopherol and/or ascorbic acid, the topical delivery of the vitamins was improved. There was enhanced chemical stability and the photoprotection to solar-simulated irradiation doubled (Lin et al., 2005; Cassano et al., 2009). For example, Murray et al. (2008) applied a stable topical formulation (containing 1% α-tocopherol, 15% L-ascorbic acid, and 0.5% ferulic acid) to normalappearing human skin and a pig skin model. These were then irradiated with solar-simulated UV. The results showed the complex of antioxidants provided substantial UV photoprotection against erythema, sunburnt cells, thymine dimmers, p53 as well as UV-induced cytokine formation including IL-1α, IL-6, IL-8, and IL-10, and TNF-α (Murray et al., 2008).
Clinical Use
At present, there are sodium ferulate tablets and ferulic acid injection used in clinic.
Sodium ferulate tablets are mainly used for the adjuvant therapy of atherosclerosis,
coronary heart disease, cerebrovascular disease, glomerular disease, pulmonary
hypertension, diabetic vascular disease, vasculitis and other vascular disorders.
Ferulic acid can also be used for the treatment of migraine headache and vascular
headache. Ferulic acid injection is mainly used for the treatment of ischemic cardiovascular and cerebrovascular disease. In addition, sodium ferulate combined with
atorvastatin can be used for the treatment of pulmonary hypertension, diabetic
nephropathy and chronic glomerulonephritis in clinic .
Ferulic acid is also used in combination with other drugs to treat other diseases.
Side effects
Ferulic acid serums and creams are generally safe for most skin types. However, it's not safe for everyone.
Sensitive skin. This can cause: Mild redness, Irritation.
Allergic to bran or oatmeal. People may also have an allergy to ferulic acid serums derived from bran or oats. Symptoms tend to be mild and may include: Redness, Swelling, Itching, Rash, and Peeling.
Purification Methods
Crystallise ferulic acid from H2O. [Beilstein 10 H 436, 10 IV 1776.]
References
[1] Wang, Mi Ningsheng . "Pharmacokinetics of ferulic acid and potential interactions with Honghua and clopidogrel in rats." Journal of Ethnopharmacology (2011).
