In the inflammatory process, monocytes leave the blood and enter the tissue at the site of inflammation as part of the cellular infiltrate. The tissue endothelial cells in inflammation express adhesion molecules to which monocytes adhere, then they penetrate through the endothelium into the tissue along a gradient of inflammation signals. The metabolites of the arachidonic acid cascade (Fig. 1), like leukotriene, prostaglandin, as well as oxygen radicals, play an important role.

Chamomile is one of the most popular plants in medicine as well as in cosmetics. Its active ingredients are essential oils with a blue color coming from chamazulen—yellow flavonoids as well as some coumarins and mucilage among others.

The essential oil has an excellent anti-inflammatory effect according to its chamazu-lene, (-)-a-bisabolol, -oxides, and enindicycloether content [1]. This is the reason why we have chosen chamomile ingredients, and especially Bisabolol, as an example of antiirritants and how these ingredients actually work.

The major constituents of chamomile are: Matricin, (- )-a-bisabolol, bisabololoxides A and B, flavonoids (apigenin, apigenin-7-glucosides), and cis-trans-en-in-dicycloether. Chamazulen is formed from matricin. Matricin will be transferred by steam distillation into chamazulencarbonacid and further to chamazulen during extraction of the essential oil (Fig. 2).

Alpha-bisabolol is a sesquiterpene component (Fig. 3), which was detected by Isaac et al. [2] The antiphlogistic property was demonstrated in several animal tests [3-5]. In an in vitro study, Ammon et al. [6] described the mechanism of the activity of chamomile ingredients. (-)-a-Bisabolol works by inhibiting 5-lipoxygenase and cyclooxygenase. There is no inhibition of the 12-lipoxygenase and (-)-a-bisabolol does not have any antioxidant properties. The author found that bisabolol is effective at a concentration level of about 30 to 80 micromoles to inhibit 50% of the enzyme activity.

In 1983, Guillot et al. [7] compared the anti-irritant properties of various ingredients used in cosmetic products (Table 1). In this study, he made an emulsion irritating by the

Phospholipid J'

Fhospholipase A2

Arachidoriic Acid

12-Lipoxygenase 15-Lipoxygenase 5-Lipoxygenase Cyclooxygenase

Hydroxys icasa- Leukotriens tetraenoic acid LTBi, LTC-t. LTD-t LTE? Prostaglandin

12-HETE 5-HPETE Thromboxane


Figure 1 Arachidonic acid cascade.

Figure 2 Transfer of matricin via steam distillation into chamazulen.

Matricin Chamazulencarbonacid Cham azulen

Figure 2 Transfer of matricin via steam distillation into chamazulen.

Figure 3 Chemical structure of (-)-a-bisabolol.

Figure 3 Chemical structure of (-)-a-bisabolol.

Table 1 Anti-irritant Properties of Ingredients Used in Cosmetic Products

Product % used Irritation index

Glycyrrhetinic acid 1.0% -0.42

Lidocaine 0.5% -0.79

Phenylsalicylate 0.5% -0.62

Bisabolol 1.0% -0.55

Bisabolol 3.0% -0.25

Guaiazulene 0.1% -0.13

addition of croton oil in sufficient quantities to provoke a clearly adverse reaction. The primary cutaneous irritation index was close to 2 according to the French method. The smaller the number, the more active the product. Interestingly, he found that bisabolol at 1% was more effective than bisabolol at 3%. Unfortunately, he did not mention what type of bisabolol he tested, because in a study conducted by Jakovlev [8], this investigator demonstrated that the various isomers of bisabolol show different activities. He found that (-) alpha-bisabolol was the most effective isomer. He set the efficacy of (-) alpha-bisabo-lol as 1,000 and compared the efficacy of the other substances to (-) alpha.

(-) alpha-bisabolol 1,000

(+) alpha-bisabolol 595

We conducted a clinical study to demonstrate in vivo the anti-inflammatory effects of natural (-)-a-bisabolol and synthetic bisabolol, which contains four stereoisomeric molecules (Fig. 4). The aim of this study was to find the concentration at which these ingredients are most active. A second test was designed to prove that the synthetic bisabolol also has protective properties against sodium hydroxide-induced irritation.

Figure 4 Molecular structure of bisabolol isomers.

Figure 4 Molecular structure of bisabolol isomers.

Aromatherapy Aura

Aromatherapy Aura

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