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dr.

Astrid Tilaar, MSi


HERBAL UNTUK PEMELIHARAAN
KECANTIKAN
BOTANICAL COMPOUNDS AND THEIR
DERMATOLOGIC AND COSMETIC USES

Phenol &
Lipids Terpenoids related
compounds

Flavonoid Alkaloids Carbohydrates

Glycosides Hydroxy Acids


LIPIDS

Vegetable oils detergents, creams, lotions,


ointments, and makeup simple emulsifiers but also
produce a variegate set of biological effects, including
skin moisturizing, smoothing and lubrication,
antieczema, anti-inflammation and arthritis, soothing
of sunburning, and the healing of wounds, ulcers, and
burns

Fatty acids, tryglicerides, and glycerol emollient and


hydrating components. useful, or essential, if the
skin is affected by irritative or inflammatory processes.
Cocoa butter extracted from the seeds of the cocoa plant
(Theobroma cacao), and mango kernel oil (Mangifera indica),
contains high amounts of the monounsaturated oleic acid,
and also the saturated palmitic and stearic acids, both
present as triglycerides and as free fatty acids. These fats are
widely used in cosmetics as emollients, moisturizers, and in
the treatment of dry skin. Sunflower oil (Helianthus annus) is
rich in polyunsaturated linoleic acid and is particularly useful
for scaly lesions due to essential fatty acid deficiency, or for
psoriasis and burns.
TERPENOIDS

Essential oils are also used in the cosmetic industry as


preservatives, in the formulation of perfumes and hair care
products, or to provide conditioning and a pleasant aroma
and shine.These oils can also be used as cooling agents,
giving a refreshing feeling to the skin.
A very specific use of essential oils concerns aromatherapy,
a kind of complementary medicine used to cure both
physical and psychological disturbances.
In aromatherapy essential oils can be vaporized or
administered through a massage onto the skin. In this latter
case, the essential oil must be diluted in a carrier, such as
grapeseed or sweet almond oil. A widely used essential oil is
the tea tree oil, extracted from Melaleuca alternifolia, not to
be confused with the tea plant, Camellia sinensis.
The tea tree oil has long been regarded as a useful topical
antiseptic agent, and is extensively used in cosmetics, hair
preparations, and skin creams.
Saponins are known to exert on the skin antioxidant effects; protection
against damage from UV-B; antiaging effects, due to the inhibition of
extracellular matrix degradation; and anti-irritation due to their anti-
inflammatory action. The antiseptic activity is particularly useful for the
treatment of acne. Saponins also strengthen dermal capillaries, thus
alleviating the symptoms of couperose and cellulite.

Other terpenoids of great importance for skin care practices are carotenoids,
retinoids, and the tocopherols-tocotrienols family.
These compounds are largely used as antioxidants, since they are effective in
quenching oxidative reactions and in retarding radical propagation. Their role
in skin care is particularly important because, owing to their lipophilic nature,
their action is directed to protect cellular membranes from processes of lipid
peroxidation.
Such a role is of primary importance for the maintenance of the integrity of
epithelia, And in particular of the epidermis, which is continuously threatened
by external prooxidant agents, including ultraviolet radiation, drugs, and air
pollutants. Besides external oxidants, the skin has also to contrast
endogenous reactive oxygen species and other radicals produced by cellular
metabolism.
PHENOLS AND RELATED COMPOUNDS
Simple phenolic compounds frequently bear diverse functional groups:
hydroxyls, aldehydes, carboxyls, and other substituents. Hydroxyl groups
are also frequently glycosylated. These compounds have in general an
antiseptic action and can be used for skin infections like acne. However,
they also show various other properties that can be exploited in skin
care. Salicylic acid, a simple phenolic acid extracted from willow trees
(Salix), is used as a nonirritative exfoliant in cosmetic treatments of fine
lines and wrinkles. Vanillin is extracted from the beans of the vanilla
orchid vine (Vanilla planifolia), and is one of the most important aromatic
flavors used in foods and cosmetics. Arbutin is a hydroquinone glucoside
present in bearberry plants in the genus Arctostaphylos, which can
reduce the formation of melanin via tyrosinase inhibition and is used to
contrast skin hyperpigmentations
FLAVONOIDS
Flavonoids are polyphenolic compounds, typical of higher plants,
which for their extreme diversification and biological properties
deserve a specific description.
Flavonoids are very common in plants, where they can be found in
fruits, seeds, stems, and flowers.

The most frequent and abundant flavonoids and their


representative plant sources are the flavones apigenin (apple),
kaempferol (broccoli), luteolin (celery), and quercetin (lettuce,olives,
onions, and parsley); the flavanones fisetin, hesperetin (citrus), and
naringin(grapefruit); the catechins catechin (red wine), epicatechin,
and epigallocatechin gallate (green tea); and the anthocyanins
cyanidin (berries), delphinidin (cherries), malvidin, peonidin (red
grapes), and petunidin (fruit peels with dark pigments).
Flavonoids share the chromane ring with tocopherols, and similarly to
these latter show strong antioxidant activity. Major mechanisms for
such an effect include direct scavenging of oxygen and nitrogen free
radicals; iron chelation; inhibition of oxyradical-producing enzymes,
such as xanthine oxidase; and reduction of leukocyte adhesion to the
blood vessel wall during tissue inflammation and reperfusion.
Flavonoids also show a wide panel of clinical effects. Anticancer
properties possibly derive from antioxidant, antiproliferative, and
antiangiogenic effects.Cardiovascular protection might derive from
antioxidant and antithrombogenic effects and from the lowering of
blood cholesterol levels. Anti-inflammatory, and possibly antiallergic,
properties are probably linked to a series of mechanisms, including
reduced activation of complement and immobilization of leukocytes,
coupled to inhibition of myeloperoxidase, cycloxygenase, and 5-
lipoxygenase. Reduction of ischemia/reperfusion injury may also
derive from these effects, as well as from the neutralization of nitric
oxide.
ALKALOIDS
Alkaloids are a very heterogeneous group of natural organic bases, which
are biosynthesized starting from amino These compounds are produced
by various organisms, including plants, fungi, and bacteria, but also by a
few animals.

The most famous alkaloids include cocaine from the coca plant
(Erythroxylon coca), the opioids morphine and codeine from the opium
poppy (Papaver somniferum), atropine from the deadly nightshade
(Atropa belladonna), nicotine from tobacco (Nicotiana tabacum),
strychnine from the nux vomica tree (Strychnos nux-vomica), mescaline
from the peyote cactus (Lophophora williamsii) and related species, and
capsaicin from chili pepper plants of the genus Capsicum.

Caffeine can also block the destructive action of dihydrotestosterone on


hair follicles, thus being helpful to combat androgenic alopecia.
CARBOHYDRATES
The major carbohydrate fraction isolated from aloe, Aloe vera, known as
acemannan, is a potent immunoactivator and consists of a polydispersed
α-1,4-linked acetylated mannan interspersed with O-acetyl groups. Other
immunoactive polysaccharides are present in fungi and algae.

Glucans are also used as film formers, humectants, and skin


moisturizers, due to their capability of retaining mineral cations and
thereby producing osmotic accumulation of water

Among simple carbohydrates, ascorbic acid (vitamin C) is a sugar acid


with pronounced antioxidant properties that can be used in antiaging
cosmetics. Ascorbic acid exerts a synergistic action with tocopherol, by
serving as an electron donor that restores the reduced state of this
molecule and then favors its antioxidant defense role in cellular
membranes.
GLYCOSIDES

Hydroquinone glycosides, like arbutin, release


hydroquinones or methyl-hydroquinones
by hydrolysis. Their most relevant property is an
antiseptic action on the urogenital tract due to the
in loco release of the aglycone moiety.
HYDROXY ACIDS

The group of α-hydroxy acids (AHAs), also known


as fruit acids, includes glycolic, citric, malic, and
lactic acids. AHAs play a main role in skin care
and dermatological therapy. They are principally
used in the treatment of wrinkles as exfoliating
agents.
MOISTURIZING AGENTS

Mechanism Actions of
Moisturizers

Collagen
Skin barrier
Occlusives Humectants Emmolients and
components
polypeptide
1.OCCLUSIVES

Occlusives coat the SC to retard transepidermal water


loss (TEWL). They are usually oily substances that have
the ability to dissolve fats and are therefore widely used
as a component in skin care cosmetics.

An occlusive is one of the best choices to treat dry skin


because it provides an emollient effect as well as
decreases TEWL. Two of the best occlusive ingredients
currently available are petrolatum and mineral oil.
NATURAL OILS
2.HUMECTANTS

Humectants are water-soluble materials with high water absorption


capabilities. They have the capacity to attract water from the
atmosphere (if atmospheric humidity is greater than 80%) and from
the underlying epidermis. Although humectants may draw water
from the environment to help hydrate the skin, in low-humidity
conditions they may take water from the deeper epidermis and
dermis resulting in increased skin dryness.

For this reason, they work better when combined with occlusives.

Humectants are also popular additives to cosmetic moisturizers


because they prevent product evaporation and thickening, thereby
extending the shelf life of
various moisturizers. Some humectants have bacteriostatic activity
as well.
Examples of commonly used humectants
include glycerin, sorbitol, sodium hyaluronate,
urea, propylene glycol, alpha hydroxy acids, and
sugars.
DEPIGMENTING AGENTS

TYROSINASE INHIBITORS
Tyrosinase, the enzyme that controls the synthesis of melanin,
is a unique product of melanocytes . It is considered to be the
rate-limiting enzyme for the biosynthesis of melanin in
epidermal melanocytes. Therefore, tyrosinase activity is
thought to be a major regulatory step in melanogenesis.
Several products on the market contain ingredients that inhibit
tyrosinase and thus decrease melanin formation

Hydroquinone
Arbutin
Licorice
Aloesin
MELANOSOME-TRANSFER INHIBITORS
Niacinamide
Niacinamide, also known as nicotinamide, is the
biologically active amide of vitamin B3. Niacinamide
has been shown to exhibit anti inflammatory,
antioxidant, and immunomodulatory properties. In
addition, it has been demonstrated to inhibit the
transfer of melanosomes to epidermal keratinocytes.

Soy
The soybean plant belongs to the pea family,
Leguminosae. Soy is found in tofu products as well as
in soybeans and soymilk. Chinese folklore suggests
that Chinese women who work in the tofu industry
have beautiful skin.
MELANOCYTE-CYTOTOXIC AGENTS
Azelaic Acid
Monobenzone

ANTIOXIDANTS
Antioxidants are popular additives in skin care
preparations for several reasons. In addition to
exhibiting antiaging, anticarcinogenic, and anti
inflammatory activities, they may also decrease
pigmentation that occurs after exposure to UV
light.This may be useful in the treatment of melasma.
ACNE

Comedogenesis and acnegenesis are actually discrete processes,


but they are usually associated with one another, with the latter
often succeeding the former. Inflammation of the follicular
epithelium, which loosens hyperkeratotic material within the follicle
creating pustules and papules, characterizes acnegenesis.
Comedogenesis is best described as a noninflammatory follicular
reaction manifested by a dense compact hyperkeratosis of the
follicle, and usually precedes acnegenesis. Because the etiology of
such lesions varies from person to person and within individuals
also, it is difficult to categorically identify or isolate a basic cause of
acne; however, three principal factors have been identified. The
primary causal factors in acne work interdependently and are
mediated by such important influences as heredity and hormonal
activity.
A. Desquamation of keratinocytes occurs in the same way that it does on the
skin’s surface. However, instead of sloughing into the environment, the
keratinocytes slough into the hair follicle. This is a continuous and normal
process that represents the culmination of the cell cycle.
B. The first stage of acne is also known as comedogenesis. The sloughed
cells stick together inside the hair follicle, resulting in a clogged pore or
comedone. This is caused by several factors including increased amounts
of sebum, inflammation of the sides of the hair follicle preventing the
release of the desquamated keratinocytes, and inceased cohesion of
keratinocytes.
C. The keratinocyte plug and sebum is an excellent food source for bacteria.
The bacteria invade the comedone and release inflammatory factors that
lead to the next stage of acne.
D. Inflammation continues with increased redness and pus. This is clinically
detectable as a papule or pustule.
E. Continued inflammation may lead to so much inflammation that the hair
follicle ruptures and the bacteria and debris are released into the dermis.
When severe, this can lead to scarring.
The Five Steps
NORMALIZING KERATINIZATION/EXFOLIATION
The first step in controlling acne is to prevent the exfoliated
keratinocytes from sticking together

ELIMINATING OR REDUCING P. ACNES


BACTERIA The use of antibiotics or
Benzoyl peroxide attacks the bacterial population thereby
decreasing the level of inflammatory extracellular products
induced by P. acnes

REMOVING THE MATERIAL THAT CLOGS THE


PORES
Comedolytics, such as salicylic acid (BHA) and AHAs, are
used to loosen the keratinocytes and “unclog” the pores.
BHA is more effective in reducing the number of
comedones than are AHAs.
Comedone extractions and “acne surgery” can also be
performed.
ATTACKING THE INFLAMMATORY RESPONSE
The use of anti-inflammatory products, such as salicylic acid, is
an effective approach to the most physically troublesome
symptom of acne. Steroid injections and topical corticosteroids,
especially potent topical corticosteroids, pose important risks
such as steroid atrophy and steroid acne

DECREASING THE LEVEL OF SEBUM


The use of oral and topical retinoids decreases sebaceous gland
activity. Hormonal stabilization, using oral contraceptives, is also
an effective way for females to reduce sebaceous secretions
HERBS IN COSMECEUTICALS : ARE THEY SAFE
AND EFFECTIVE?
Unfortunately, two major myths taint herbal medicine. Most patients
believe the myth that there are no side effects because herbal medicine
uses “natural substances.” In fact, experienced Chinese practioners are
concerned about the well-known side effects of hepatotoxicity and
contact dermatitis with oral and topical Chinese herbal medicinal and
preparations, respectively.

The understanding of the function, metabolism, and interaction of these


herbal medicines is often lacking. The specific scientific issues include
documenting:
(i) complete characterization of the multiple active compounds in each
plant source
(ii) activity and synergistic or additive interaction of each of these
compounds and their metabolites
(iii) interaction of these active components with food, nutrients,
nutritional supplements, and other medicines, and
(iv) how the potential toxicity of specific compounds is blunted
FACTORS AFFECTING CONCENTRATION AND
QUALITY OF ACTIVE INGREDIENTS

1. Growing conditions of the plant contribute to variation in botanical extracts.


These variables include climate, habitat, weather including catastrophes such as
hurricanes, time of year, elevation, number of sunny days, hours of daylight,
amount of rain or lack thereof, soil conditions such as leaching of nitrogen in a
year of heavy rain fall, wind conditions, type and amount of fertilizer, ambient
temperatures, pests,
and plant disease exposure, and if cultivated or in its natural habitat, plant
growth periods and diurnal variation.

2. The conditions following harvesting may also affect the constituents of the
botanical. These variables include harvesting time, care of botanical products
during transport, storage time for the botanical, processing methods, and
manufacturing of the finished product.

3. The biologic activity of the herbal extract is affected by the condition of the
plant, which must be healthy anddisease free.
4. Botanicals are affected by the portion of the plant selected for harvesting.
There are differences in the mix and concentrations of the active ingredients
between flowers, berries, stems, bark, roots, and rhizomes. Familiarity with
phytomedicine is important to ensure the recommended product contains
the correct plant parts for the desired effect.

5. Proper processing is necessary to insure herbal potency.


The timing, degree, and type of processing determine the functionality of the
herbal product. The first step in processing is air or oven drying to achieve a
moisture content ≤ 10% and prevent mildew. This material is then milled into
pieces less than 1 cm in diameter. If the desired actives are highly sensitive
to light, heat, dessication, oxygen, or enzymes, they need to be extracted
without drying as soon as the plant is harvested.
SUMMARY

There are multiple herbs currently incorporated into


cosmeceuticals with valid scientific rationale and supported with
human clinical studies or have documented biologic activity by in
vitro, in vivo, or animal studies.

Cosmeceuticals containing these herbs may currently be or


potentially will be valuable contributions to dermatology and skin
care if clinical efficacy can be confirmed by controlled human
clinical trials conducted by thirdparty researchers with the
finished marketed product.

The cosmeceutical only has scientific integrity if the herbal


components are stable, of therapeutic concentrations, and can
be adequately delivered across human stratum corneum.

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