98 BIOTECHNOLOGY
are pro-inflammatory leukotrienes produced by the metabolism of arachidonic acid, whose production is dependent on 5-lipoxygenase (5-LOX).5 (-)-α-Bisabolol can achieve anti-inflammatory
effects by inhibiting 5-lipoxygenase (5-LOX). In addition, (-)-α-Bisabolol can also produce effects by inhibiting pro-inflammatory factors IL-6, TNF-α, PGE2 and NO, as shown in Figure 5.6-7 There are many other messengers related to inflammation. For example, iNOS is a mediator and regulator of inflammatory response, and COX- 2 is a key enzyme that regulates the production of prostaglandins, which are the main mediators of inflammation. (-)-α-Bisabolol can reduce the expression of
iNOS and COX-2 genes by inhibiting the signaling channels of NF-kβ and AP-1 (ERK and p38), and relieve inflammation.7
Antibacterial activity The skin microbiota of people with sensitive muscles are often abnormal. The excessive reproduction of harmful bacteria and the overexpression of their information molecules will destroy the skin barrier and cause skin inflammation, which will aggravate the sensitivity of the skin.4 α-Bisabolol also has excellent antibacterial
activity and is effective against Staphylococcus aureus (143.9±0.0mM) and Candida albicans (36.0±0.0mM).8
Antioxidant activity Massive exogenous or endogenous stimuli produce a local protective tissue response usually referred to as ‘inflammation’. These inflammatory processes recruit different types of cells, especially polymorphonuclear neutrophils (PMN) and simultaneously produce inflammatory mediators that activate ‘stress signaling pathways’. PMN recruitment is initially a protective mechanism, but their activation leads to ‘respiratory bursts’ and release of reactive oxygen species (ROS), which damage target cells and the surrounding cells (lipid peroxidation, amino acid oxidation, protein fragmentation and DNA damage), thereby triggering a self-sustaining cycle of inflammation and oxidative stress.9 The aim of the luminol-amplified chemiluminescence (LACL) study was to examine whether α-Bisabolol interferes with ROS production during PMN respiratory bursts, and to determine the minimum concentration
3500 2800 2100 1400 700 0
* * Normal Vehicle 1µg/ml 3µg/ml 10µg/ml 1µg/ml
(-)-α-Bisabolol LPS
Dexamethasone
1500 1200 900 600 300 0
Figure 2: Mechanism of sensitive skin HO H
OH H
OH H
HO H
(-)-α-Bisabolol
(+)-α-Bisabolol Figure 3: Isomers of α-Bisabolol
at which it still exerts antioxidant activity. LACL has been widely used to detect ROS produced by PMN under various conditions. Significant LACL inhibition was observed
with α-Bisabolol at concentrations ranging from 3.8 to 31 g/ml, as reported in the literature. Likewise, similar effects were observed in cell- free systems such as SIN-1 and H2O2/HOCl–.9
Whitening activity Various inflammatory skin diseases are one of the causes of hyperpigmentation. Epidermal and dermal hyperpigmentation may depend on increased numbers of melanocytes or increased activity of melanogenic enzymes.
* * Normal Vehicle 1µg/ml 3µg/ml 10µg/ml 1µg/ml
(-)-α-Bisabolol LPS
Figure 4: Dose-response effect of (-)-α-Bisabolol on LPS induces inflammation in macrophages
PERSONAL CARE October 2023 Dexamethasone
45 40 35 30 25 20
LPS (500ng/ml) - (-)-α-Bisabolol(uM) - α-Melanocyte-stimulating hormone
(α-MSH) is one of the triggers of these diseases. Since the cyclic adenosine monophosphate (cAMP) response factor (CRE) was reported to be involved in the production of α-MSH, the cAMP response factor (CRE) luciferase reporter gene was used for the assay.10 The experiments showed that, as shown in
Figure 6a, α-Bisabolol inhibited the activation of α-MSH-induced CRE luciferase reporter gene. As shown in Figure 6b, the melanin content induced by α-MSH was suppressed by α-Bisabolol decreased. As shown in Figure 6c, α-Bisabolol reduced the cAMP production induced by α-MSH. As
# * * *
45 40 35 30 25 20
+ -
+ 5
+ 25 + 50 + 100 LPS (500ng/ml) - (-)-α-Bisabolol(uM) - # * * * *
(+)-epi-α-Bisabolol
(+)-epi-α-Bisabolol
+ -
+ 5
+ 25
+ 50
+ 100 Figure 5: (-)-α-Bisabolol inhibits NO and PGE2 production in RAW264.7 cells
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TNF (pg/ml)
IL-6 (pg/ml)
Nitrite (uM)
Nitrite (uM)
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