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Low molecular-weight tannins of Phyllanthus emblica: Anti-aging effects

  • Sytheon, 10 Waterview Blvd. Parsippany NJ 07054, USA
uman skin colour is quite variable
around the world. It ranges from a
very dark brown among some
Africans, Australians and Asian-Indians to a
near pinkish yellow among some northwest
Europeans. There are no people who truly
have black, white, red or yellow skin.
These are commonly used terminologies
that do not reflect biological reality.
Pigmentation of the skin, due to synthesis
and dispersion of melanin in the
epidermis, is of great cosmetic and
societal significance. It is also the key
physiological defence against sun-induced
damage, such as sunburn, photo ageing
and photocarcinogenesis.
Skin lightening agents have been widely
used to either lighten or depigment the
skin. Preparations in the European market
tend to be used to treat age spots and
freckles or to obtain even-toning effects,
whereas the Asian market uses them to
change or modify skin colour. A wide
variety of skin-lighteners, namely
hydroquinone and its derivative arbutin,
kojic acid and its dalpmitate, ascorbic acid
and its derivatives such as sodium and
magnesium ascorbyl phosphates, ascorbyl
2-glucoside have been used for these
Due to the increasing use of skin
lightening agents among the global
population, it is apparent that both the
efficacy of a skin lightening formulation,
as well as safety and mildness of the skin
lightening ingredient, are equally
important. Many current skin lighteners
such as hydroquinone3,4 and Kojic acid5,6
have inadequate safety and stability
profiles. Based on the toxicity problems of
hydroquinone and kojic acid, it is quite
reasonable to question the safety of
arbutin and kojic acid dipalmitate for
human use.
Photo ageing of skin is a complex
biological process affecting various layers of
the skin, with major changes seen in the
connective tissue of the dermis.
The natural shift toward a more pro-oxidant
state in intrinsically aged skin can be
significantly accelerated by UV-irradiation.
The effects of UV-radiation from sun
exposure can induce or exacerbate oxidative
attack leading the generation of Reactive
Oxygen Species (ROS). The most severe
consequence of photo-damage is skin
cancer. Less severe photo ageing changes
result in wrinkling, scaling, dryness, and
uneven pigmentation consisting of
hyper- and hypo-pigmentation.7–10
The preliminary skin lightening profile of
Phyllanthus emblica fruits (trade named as
Emblica, standardised antioxidant fraction)
has been reported earlier11 (US Patent
6,649,150 and several US and foreign
pending patents). The purpose of the
present work is two-fold: (a) to show
broader applicability of Emblica as a
skin-lightener and (b) to investigate the
effectiveness of this material as an
anti-ageing ingredient.
About the product
P. emblica (syn. Emblica officinalis) is one
of the important Ayurvedic (science of life)
herbs in India, and has been used for
thousands of years for a wide variety of
human ailments. Its status ranges from
insignificant in the western world to
highly-prized in tropical Asia. The fruits are
selected, harvested and processed
according to strict criteria to ensure a
consistently high quality product. Emblica
antioxidant is extracted from premium
benefits of
benefits of
Ratan K Chaudhuri – EMD Chemicals Inc, Hawthorne, NY 10532, USA
January 2005 13
3 weeksKey:
Delta ITA degree
Kojic acid
Study 1 Study 2 Study 3 Study 4
6 weeks 9 weeks
Figure 1: Results of clinical studies of Emblica and other skin lighteners.
quality fruits using a water-based process
(US Patent 6,124,268 and several US and
foreign pending patents). Emblica
antioxidant is distinctly different from
other commercially available extracts of
P. emblica fruits as it is defined to the
extent of well over 50% (typically, 60 to
70%) in terms of its key chemical
components.12,13 None of the extracts
of P. emblica in the market compare to
Emblica antioxidant in composition and
consistency of composition, aqueous
stability and colour.
The low molecular weight (<1,000)
hydrolyzable tannins, namely Emblicanin A
and Emblicanin B, along with Pedunculagin
and Punigluconin are the key ingredients in
Emblica antioxidant.12–14 In nature,
Emblicanin A and Emblicanin B have
only been found in P. emblica plant.14,15
Emblica antioxidant has been
standardised16 by using high performance
thin layer chromatography (HPTLC).
Alternatively, the product can be
standardised by using high performance
liquid chromatography (HPLC).
Skin lightening property
Four separate clinical studies were done to
determine the potential of Emblica as a
skin lightener:
Study 1: Comparison of 2% Emblica
antioxidant vs 2% Hydroquinone
(13 Asians);
Study 2: Comparison of 2% Emblica
antioxidant vs 2% Hydroquinone
(13 Hispanics);
Study 3: Comparison of 1% Emblica
antioxidant vs 3% Magnesium Ascorbyl
Phosphate (MAP, 16 Asians);
Study 4: Comparison of 1% Emblica
antioxidant vs 2% Kojic Acid
(16 African-Americans).
Human volunteers with skin Types III and
IV (as defined by the Fitzpatrick Photo type
Scale) were selected for Studies 1-3.
For Study 4, skin types IV to VI were used.
This study was conducted comparing
baseline, pre-treatment to final post-
treatment results of the selected test sites.
The length of the study was nine weeks.
Each subject was given two products with
identical formulation ingredients (one with
Emblica antioxidant and the other one with
a competitive material as a positive
control) – one for the left upper arm and
the other one for the right upper arm.
Panelists were instructed to apply
approximately 0.5 ml of the test materials
twice a day. The selected test application
site was photographed prior to the start of
the study. Rigid control of photographic
technique, from the aspects of lighting,
distance, angles and camera/film settings
and specifications, and subsequent
development of photographs was followed.
Skin colour measurements were done
using a tristimulus instrument (CR300 –
Minolta Chroma Meter). Repeated
measures analysis of variance was used to
14 January 2005
Figure 2: Cause and consequences of UV-induced skin damage.
Chelator Absorption Maxima of Complex (λ
in nm)
With Fe3+ N3- Induced Shift With Cu2+ N
- Induced Shift
EDTA 241, 283 241, 283, 410 240, 278 241, 279, 354
Emblica antioxidant 241, 294, 353, 377 241, 294, 353, 377 240, 272, 313 240, 272, 313
Pine Antioxidant 241, 294, 353, 384 241, 294, 353, 400,440 239, 279, 302, 331 239, 280, 307,430
Vitamin C 238, 262 241, 266, 295 239, 263, 239, 263, 284,364
Grape Antioxidant 247, 295, 353, 396 247, 295, 353, 415,430 240, 277, 328 240, 277, 328, 359
Green Tea Antioxidant 240, 272, 324, 390 240, 277, 325, 390 241, 276, 327, 403 240, 277, 336, 404
Trolox C 240, 284 240, 273, 284, 360 241, 288 241, 261, 352, 440
Gallic Acid 247, 295, 337 247, 295, 353,412 240, 258, 321 240, 258, 331,463
UV light
Skin damage
DNA Protein Lipids Carbohydrate
oxygen species
Release of matrix
Release of free
iron & copper
Strand breakage
SH oxidation
of Enzymes
Peroxidation Depolymerization
of hyaluronic acid
determine if any significant differences
were observed in the mean Individual
Typology Angle (ITA degree).
ITA value is calculated from the mean
L* and b* Chroma Meter values using the
ITA Degree = [Arc Tangent ((L* - 50)/b*)]
Where L* value is the lightness value, a* is
the colour value in the red-green axis, and b*
is the colour value in the blue-yellow axis.
E of ITA degree was calculated by
subtracting the average ITA degree of the
treated site from that of the average
baseline (first day of study). Results of
these clinical studies are summarised in
Figure 1.
The purpose of the four clinical studies
was to compare the skin lightening effect
of Emblica with other well-known and
well-documented skin lighteners, such as
hydroquinone, Magnesium ascorbyl
phosphate (MAP) and Kojic acid. Each
comparative study consists of two products
with identical formulation ingredients (one
with Emblica antioxidant and the other with
a competitive material, positive control).
No attempt has been made to optimise
the formulation and no skin penetration
enhancers were used in the formulations.
In all four studies, Emblica antioxidant-
containing product shows a significant
increase in ITA degree (meaning skin
lightening) versus the corresponding
baselines. Studies 1 and 2 clearly show
2% Emblica antioxidant has a comparable
skin lightening effect to that of 2%
Hydroquinone in Asian as well as Hispanic
subjects. Study 3 shows 1% Emblica
antioxidant is three times better in skin
lightening efficacy on a percentage-active
basis over the 3% MAP product.
Study 4 shows 1% Emblica antioxidant is
comparable to 2% Kojic Acid.
Anti-ageing property
The unifying pathogenic agents responsible
for photo-damage are UV-generated
Reactive Oxygen Species (ROS) that
deplete and damage the enzymatic and
non-enzymatic antioxidant defence
systems of the skin, and the release of
matrix metalloproteases (MMPs) such as
MMP-1 and MMP-3, that damage the
extracellular matrix proteins.9,17
Cause and consequences of UV-induced
skin damage can be schematically
represented in Figure 2.
Emblica antioxidant has been found to
have broad-spectrum antioxidant activity,
excellent iron- and copper-chelating activity
and MMP-1 and MMP-3 inhibitory activity.
While most antioxidants go from an active
to an inactive form. Emblica antioxidant
utilises a multilevel cascade of antioxidant
compounds resulting in a long-lasting and
stable antioxidant activity18. These
multifunctional attributes are described in
the following sections.
Effects on Reactive Oxygen
Species (ROS)
Singlet oxygen, superoxide anion and
hydroxyl radicals are the three key ROS
responsible for skin damage. In-vitro
studies done with Emblica antioxidant and
a few commercially available antioxidants
clearly show superiority of Emblica
antioxidant over commercially available
antioxidants. Results are described below:
Singlet oxygen quenching: Singlet oxygen
quenching ability of Emblica antioxidant has
been evaluated by photooxidation of a
sensitiser (N,N-dimethyl-p-nitrosoaniline)
using a published method.19,20 Results show
that Emblica antioxidant (IC
= Inhibitory
concentration 50%; IC
61 µg/ml) is an
excellent singlet oxygen quencher and is
superior to Trolox C, a Vitamin E
water-soluble analog (IC
84 µg/ml). In
this test, vitamin C was found to be a
strong enhancer of singlet oxygen
Superoxide anion radical quenching:
Superoxide anion quenching ability of
Emblica antioxidant has been evaluated by
generating superoxide anion using a
hypoxanthine-xanthine oxidase test21
followed by reduction of nitroblue
tetrazolium (NBT) into nitroblue diformazan
by monitoring the light absorption of NBT at
560 nm. Results of this study show that
Emblica antioxidant is an excellent
quencher for superoxide anion. IC
for Emblica antioxidant is 12 µg/ml,
compared to IC50 26 µg/ml for vitamin C
and IC50 360 µg/ml for Trolox C, a vitamin
E water-soluble analog.
Hydroxyl radical quenching: Hydroxyl
radical quenching ability of Emblica
antioxidant has been evaluated by the
deoxyribose test method described by
Halliwell.22 Results show that Emblica
antioxidant is a significantly better hydroxyl
radical quencher than all other antioxidants
tested in this study. IC
values for Emblica
antioxidant is 0.92 mMol, compared to IC
of 2.10, 2.70 and 2.78 mMol for pine
antioxidant, Trolox C and grape antioxidant,
respectively. Vitamin C and green tea
antioxidant were found to be pro-oxidants.
Effects on iron and copper
Recognising the crucial role iron plays in
initiating oxidative stress23,24 to skin, we
envisioned that an antioxidant can be a
true photoprotective agent provided it
chelates all the coordination sites in iron or
copper.25 Using the UV spectrophotometric
method developed by Graf et al,25 we
have determined the presence of free
coordination site(s) in the Fe3+- and Cu2+-
antioxidant complexes comparing their
azide-induced shift. Table 1 shows that all
complexes except Emblica antioxidant
contain at least one coordinated water
molecule as shown by the presence of
spectral shift(s) induced by sodium azide.
Effects on Matrix
Metalloproteases (MMPs)
Collagenase (MMP-1) inhibitory activity:
A dose-dependant inhibition of
gelatinase/collagenase activity by about
55 to 70% was observed with Emblica
antioxidant at 150-300 µg/ml.13
Quantification of gelatinase/collagenase
January 2005 15
Figure 3: Collagenase (MMP-1) inhibitory activity of Emblica antioxidant.
(Phenan = 1,10-Phenathroline).
MMP-1 activity in % of control
Concentration of Emblica in microgm/ml
150 200 250 300 Phenan
inhibitory activity of Emblica antioxidant
was determined by using EnzChek
gelatinase/collagenase kit (E-12055) from
Molecular Probe by measuring the
substrate fluorescence emission at 515
nm. 1,10-Phenanthroline was used as a
positive control and collagenase without
inhibitor was used as a negative control.
Results of this study are summarised in
Figure 3.
Collagen synthesis in sun damaged skin
appears to remain similar to that of sun-
protected sites, although collagen content
decreases.17 Thus, evidence suggests that
the decrease in collagen content in photo
aged skin results from increased collagen
degradation without significant changes in
production. It seems that the protection of
existing collagen is more important in
controlling the human ageing process than
stimulating collagen production.
Stromelysin 1 (MMP-3) inhibitory
activity: An inhibition of Stromelysin 1
activity by over 50% was observed with
Emblica antioxidant at 100 µg/ml13.
Quantification of MMP-3 inhibitory activity
of Emblica antioxidant was determined by
using Chemicon MMP-3/Stromelysin
Activity Assay Kit (ECM 481). The principle
of the assay is based upon fluorescence
measurement of substrate fragments
released upon cleavage of a substrate by
MMP-3. Fluorescence intensity of the
resulting product is measured and
correlated with MMP-3 activity. Result of
this study is summarised in Figure 4.
Clinical trials: Reduction in
UV-induced erythema
Reduction in UV-induced erythema was
used as a criterion for photoprotection and
reversal of photo damage by Emblica. The
following protocol was followed:
Human volunteers
– Eleven (Protocol A)/Ten (Protocol B).
Test sites
– Subject’s back, 4 x 2.5 cm area.
Test substances
– 0.2 and 0.5% levels (creams).
Application frequency
– 2 mg/cm2once a day.
Evaluation criteria – Represented by using
the individual typology angle (ITA˚);
Measured by chromometric measurement.
E ITA˚ was calculated by subtracting
treated irradiated site from the untreated
irradiated site (Fig. 5).
Protocol A (Prevention) – Products were
applied for eight days and then on day
nine, pigmentation were induced by UV
light on 11 humans. Product applications
once a day were continued for 10 days.
Comparisons of untreated irradiated
control vs the sites with products were
done on day 10.
Protocol B (Reversal) – Pigmentation was
induced by UV light on 10 humans and
then products were applied and continued
the application of product once a day
for 10 days. Comparisons of untreated
irradiated control versus the product-
treated sites were done every day.
A statistically significant difference in ITA˚
was observed on day five.
Results: The results are shown in Figure 5.
For protocol A, 0.2% Emblica antioxidant
and 0.5% Vitamin E showed statistically
significant (p<0.05) reduction in
erythema. For Protocol B, only 0.2%
Emblica showed statistically significant
(p<0.05) reduction in erythema on day
five. Vitamin E and MAP failed to show any
statistically significant reversal in erythema.
Formulation guidelines
Emblica antioxidant can be used in
formulations from 0.1 to 0.5% level with
acceptable aesthetics. Skin care
formulation with higher levels of Emblica
antioxidant (>0.5%, w/w) requires the use
of light fragrance. Essential oils such as
lavender, peppermint, lemon and juniper
may be added to mask the odour of
Emblica at 1.0%. As a skin lightener, the
preferred use level is from 1 to 2%.
Nonionic or anionic emulsifiers can be
used for making stable emulsions. Skin
penetration enhancers like lecithin can be
included to enhance the efficacy of
Emblica. Other skin lightening agents can
also be included to exploit synergism as
long as the formulation pH is acidic. pH
requirement, therefore, precludes inclusion
of magnesium or sodium ascorbyl
phosphates. However, ascorbyl glucoside
can be included in the formulation.
Formulations containing Emblica will be
off-white to white in appearance and which
will, over time, either darken or yellow,
especially at higher temperature. This
colour shift can be reduced or eliminated
by adding a small amount of sodium
metabisulfite (0.1%) along with ascorbic
acid (0.05%). The colour of the finished
product can also be slightly improved by
the use of a small amount (~0.1%) of
Licorice Extract (with ~20% Glabridin
content). At room temperature (~25˚C),
formulation holds colour pretty well for well
over one year. pH of the formulations must
be acidic (preferably, below 5.5) to
maintain its antioxidant activity and
stability. An opaque base is preferred over
a translucent one due to the improved
colour of the finished product. Emblica
antioxidant as a suspension in water can
be added to the formulation with a
moderate agitation at around 40˚C.
Prolonged heating or exposure to sunlight
must be avoided as it causes darkening of
formulated products. Several formulations
using Emblica antioxidant have been
developed in the author’s laboratory.
A properly defined and standardised
extract of Phyllanthus emblica fruit
(Emblica antioxidant) may provide great
value as a photoprotective agent
(in combination with sunscreens and
other anti-ageing ingredients), or a skin
lightening agent (along with other skin
lighteners). In short, the multiplicity of skin
beneficial effects, formulation benefits
seen with Emblica antioxidant and
unsurpassed safety of the product make it
16 January 2005
Figure 4: Stromelysin 1 (MMP-3) inhibitory activity
of Emblica antioxidant.
MMP-3 activity in % of control
Concentration of Emblica in microgm/ml
100 200 300
Figure 5.
E of ITA degree
Protocol A (Prevention) Protocol B (Prevention)
0.2% EmblicaKey: 0.5% MAP 0.5% Vitamin E
an ideal choice for a variety of skin care
products targeting young and mature
skin alike.
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... Emblica antioxidant is distinctly different from other commercially available extracts of P. emblica fruits as it is defined to the extent of well over 50% (typically, 60 to 70%) in terms of its key chemical components. 12,13 None of the extracts of P. emblica in the market compare to Emblica antioxidant in composition and consistency of composition, aqueous stability and colour. The low molecular weight (<1,000) hydrolyzable tannins, namely Emblicanin A and Emblicanin B, along with Pedunculagin and Punigluconin are the key ingredients in Emblica antioxidant. ...
... The low molecular weight (<1,000) hydrolyzable tannins, namely Emblicanin A and Emblicanin B, along with Pedunculagin and Punigluconin are the key ingredients in Emblica antioxidant. [12][13][14] In nature, Emblicanin A and Emblicanin B have only been found in P. emblica plant. 14,15 Emblica antioxidant has been standardised 16 by using high performance thin layer chromatography (HPTLC). ...
... Collagenase (MMP-1) inhibitory activity: A dose-dependant inhibition of gelatinase/collagenase activity by about 55 to 70% was observed with Emblica antioxidant at 150-300 µg/ml. 13 Quantification of gelatinase/collagenase Results of this study are summarised in Figure 3. Collagen synthesis in sun damaged skin appears to remain similar to that of sunprotected sites, although collagen content decreases. 17 Thus, evidence suggests that the decrease in collagen content in photo aged skin results from increased collagen degradation without significant changes in production. ...
Full-text available
Di-2,2'-diethylhexyl-3,5-dimethoxy-4-hydroxy-benzylidenemalonate (INCI name diethylhexyl syringylidene malonate, DESM), the target photostabilizer, was synthesized in one step by condensation of 3,5-dimethoxy-4-hydroxy benzaldehyde (Syringaldehyde) with di-2,2'-diethylhexyl malonate. Photostability data in sunscreen formulations showed that DESM is photostable and improves the photostability of avobenzone significantly when compared to control (without a photostabilizer). Photostable broad-spectrum sunscreen formulations with high SPF (>30) have been achieved by combining avobenzone, DESM and UV-B sunscreens, such as homosalate, octisalate or other UV-B sunscreens. It seems that (a) triplet-state energy transfer from avobenzone to DESM and (b) scavenging of reactive species are responsible for the observed stabilization of avobenzone. In vitro study of the two formulations containing DESM clearly showed critical wavelength of well over 370 nm and can thus be categorized as broad-spectrum sunscreens. DESM does not have any contribution to in vivo SPF; instead it boosts SPF by about 5 units in high-SPF products. DESM was found to be an excellent singlet-oxygen quencher, thereby reducing photodegradation of avobenzone caused by singlet oxygen. In short, the multiplicity of effects and formulation benefits seen with DESM makes it an ideal choice as a unique antioxidant photostabilizer for a variety of cosmetic products targeting young and mature skin alike.
... It may be used as rejuvenative to promote longevity, and traditionally to enhance digestion, treat constipation, reduce fever, purify the blood, reduce cough, alleviate asthma, strengthen the heart, benefit the eyes, stimulate hair growth, enliven the body, and enhance intellect. They are useful in vitiated conditions of tridosha, diabetes, dyspepsia, colic, flatulence, hyperacidity, peptic ulcer, erysipelas, skin diseases, leprosy, haematogenesis, inflammations, anemia, emaciation, hepatopathy, jaundice, strangury, diarrhoea, dysentery, hemorrhages, leucorrhoea, menorrhagia, cardiac disorders, intermittent fevers and greyness of hair (Thakur, 1989; Saeed and Tariq, 2007; Jayaweera, 1980; Chaudhuri et al., 2003; Tasduq et al., 2005; Biswas et al., 2001). In Ayurvedic polyherbal formulations, Indian gooseberry is a common constituent, and most notably is the primary ingredient in an ancient herbal rasayana called Chyawanprash.http: ...
... The studies showed that Amla preparations contained high levels of the free-radical scavenger, superoxide dimutase (SOD), in the experimental subjects (Treadway, 1994). Emblica officinalis (Eo) reduced UV-induced erythema and showed free-radical quenching ability, chelating ability to iron and copper as well as MMP-1 and MMP-3 inhibitory activity (Chaudhuri, 2003). In another study, amla was studied against the cold stress-induced ...
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Wonder berry, Emblica officinalis Gaertn., commonly known as Indian gooseberry or amla, is used in Ayurveda as a potent Rasaayana. The traditional system of medicine used almost all of its parts i.e. roots, leaves, stems but mostly it is known for astonishing properties of fruits. The fruit is used either alone or in combination with other plants to treat many ailments such as common cold and fever, as a diuretic, laxative, liver tonic, refrigerant, stomachic, restorative, alterative, antipyretic, anti-inflammatory, hair tonic, to prevent peptic ulcer and dyspepsia, and as a digestive. The present review gives an account of updated information on its phytochemical and pharmacological properties. The fruit is rich in quercetin, phyllaemblic compounds, gallic acid, tannins, flavonoids, pectin and vitamin C and also contains various polyphenolic compounds. A wide range of phytochemical components including terpenoids, alkaloids, flavonoids and tannins have been shown to possess useful biological activities. In addition, experimental studies have shown that some of its phytochemicals such as gallic acid, ellagic acid, pyrogallol, some non-sesquiterpenoids, corilagin, geraniin, elaeocarpusin, and prodelphinidins B1 and B2 also possess anti-neoplastic effects. Preclinical studies have shown that amla possesses anti-pyretic, analgesic, cardioprotective, gastroprotective, anti-hypercholesterolemia, wound healing, hepatoprotective, chemopreventive, free radical scavenging, antioxidant, anti-inflammatory, anti-mutagenic and immunomodulatory properties. In view of its reported pharmacological properties and relative safety, it can be said that E. officinalis is a source of potential therapeutically useful products.
... E. officinalis elicits its biological activity by several different mechanisms, i.e. as an antioxidant by increasing superoxide dismutase, catalase, and glutathione peroxidase activities, chelation of transition metal ions e.g. iron and copper (Bhattacharya et al., 1999(Bhattacharya et al., , 2002, and enzyme inhibitory action (matrix metalloprotease proteins, aldolase reductase inhibitory activity) (Chaudhuri et al., 2006) and thus was chosen for this study. ...
... Capros ® , an aqueous extract of the edible fruits of E. officinalis (Indian Gooseberry, P. emblica), standardized (by HPLC) to at least 60% w/w of low molecular weight hydrolyzable tannoids, comprising of Emblicanin-A, Emblicanin-B, Pedunculagin and Punigluconin (Ghosal et al., 1996) (Natreon Inc., New Brunswick, NJ, USA), was used, because extensive in vitro, in vivo and ex vivo antioxidant and stability studies have been carried out on this product (Ghosal et al., 1996;Chaudhuri et al., 2006;Bhattacharya et al., 1999Bhattacharya et al., , 2002). An HPLC chromatogram supplied by Natreon Inc. is shown in Fig. 1 ...
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Emblica officinalis (Indian Goosebery, Phyllanthus emblica) was evaluated for cardio-respiratory and anti-oxidant status in human volunteers with a long smoking history, using a randomized, double-blind, placebo controlled pilot study. E. officinalis fruit extract (EOE) standardized to contain not less than 60% (w/w) of low molecular weight hydrolyzable tannoids (Emblicanin-A, Emblicanin-B, Pedunculagin, Punigluconin) was used in this randomized, double-blind, placebo-controlled clinical study, with Group I consisting of 20 subjects receiving 250 mg of EOE twice a day for 60 days and Group II consisting of 10 subjects receiving 250 mg of placebo twice a day for 60 days. Subjective parameters – mouth hygiene, cough with expectoration, shortness of breath on exertion, loss of appetite, feelings of impending doom, palpitation, sleep deprivation, irritability, heart burn and tiredness were evaluated at 0 (baseline), 30 and 60 days. Objective parameters – hemogram, lipid profile, cardiovascular risk factors, genotoxicity, antioxidant status and pulmonary function were assessed at days 0 (baseline) and 60 of the study.EOE treated group showed a significant improvement compared to the placebo group in all the subjective and objective parameters tested with no reports of adverse events.This pilot study provides some further evidence of the protective effect of E. officinalis in cardio-respiratory and antioxidant status of volunteers with chronic smoking history.KeywordsCaprosEmblica officinalisSmokingCardio-respiratory improvementAntioxidant
... Photo aging of the skin is a complex biologic process affecting various layers of the skin with major changes seen in the connective tissue within the dermis. EO was shown to reduce ultra violet-induced erythema and had excellent free-radical quenching ability, chelating ability to iron and copper as well as matrix metalloproteinase (MMP-1) and MMP-3 inhibitory activity [59]. ...
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Emblica officinalis (Amla, EO, and E. officinalis) is one of the most important herbs in the Indian traditional medicine system, especially Ayurveda and also known as the king of all medicinal plants. EO is famous ayurvedic herb (the name means sour in Sanskrit) is likely one of the most useful drug treatments within the Indian pharmacopoeia, and is considered to be one of the most strongest uvenatives (Rasayana), particularly for the blood, bones, liver, and heart. It is an exceptionally rich source of vitamin C containing 30 times the amount found in oranges. It is one of the oldest oriental medicines mentioned in Ayurveda as potential remedy for various ailments. EO (Amla) is widely used in the ayurvedic medicines and believed to increase defense or immune power against diseases. Several parts of the plant are used to treat a variety of diseases, but the most important is the “fruit.” The fruit is rich in quercetin, phyllemblic compounds, gallic acid, tannins, flavonoids, pectin, and vitamin C and also contains various polyphenolic compounds. A wide range of phytochemical components including terpenoids, alkaloids, flavonoids, carbohydrates, and tannins have been shown to possess useful biological activities. Many pharmacological studies have demonstrated the ability of EO as antioxidant, anticarcinogenic, antitumor, antigenotoxic, anti-inflammatory activities, anticancer, anti HIV-reverse transcriptase, antidiabetic, inhibitory effects, antidepressant, antiulcerogenic, hair growth tonic, wound healing activities, cardiovascular diseases, neurodegenerative diseases, cancer, and many other traditional uses of the plant. The present study also includes macroscopy, microscopy, preliminary phytoconstituent, and physico-chemical evaluation.
... It has also been found that vitamin C accounts for approximately 45-70% of the antioxidant activity. Amla (Emblica officinalis) contained high levels of the free-radical scavenger, superoxide dimutase (SOD), in the experimental subjects (Scartezzini et al., 2006; Bhattacharya 1999; Chaudhuri 2003;). ...
... The blue or black coloration is most probably due to the impurities of iron powder or iron salts associated with loha bhasma. To confirm the origin of this coloration, its chemical interpretation and source of impurities responsible for the colour, a detail study of this test is carried out.It has been reported that emblica act as chelating agent with iron and copper [12] which supports this observation. ...
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Characterization of the genuine metallic bhasmas and confirmation of their identity and authenticity is very important for their safer use. Complete conversation of metallic powder to the bhasma is essential for this purpose. In ancient days traditional test like test of Phyllanthus emblica with loha bhasma was one of the significant test to identify genuine loha bhasma.In the present study, five commercial samples of Loha bhasma ie bhasma of iron are subjected to this test to find presence or absence of free iron in the samples, using traditional ayurvedic test and chemical basis for the same is provided using UV-Visible spectroscopy. Importance and practical utility of the test is also discussed in this communication.
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ARTICLE INFO ABSTRACT Article history Received 16/05/2013 Available online 30/06/2013 Keywords Amla, anti-diabetic, anti-oxidant, anti-cancer, anti-hyperlipidemic anti-inflammatory. Phytogenic agents have traditionally been used by herbalists and indigenous healers for the prevention and treatment of various diseases. Emblica officinalis (Amla) is a deciduous tree belonging to family Euphorbiacea. Growing body of evidences have shown that amla possess anti diabetic activity and have been used to treat diabetes-induced complications. Amla is a potent antioxidant. Wide array of studies such as hepatoprotective, anticancer, anti inflammatory, analgesic, anti hyperlipidemic etc are associated with this plant. The present review demonstrates the pleiotropic actions of amla in various disorders. Moreover, the underlying mechanisms of amla-induced protection in various diseases have been delineated. Please cite this article in press as Jagdeep Kaur Emblica officinalis: A Meritocratic Drug for Treating Various Disorders. Indo American Journal of Pharm Research.2013:3(6).
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The catalysis by iron of the formation of reactive oxygen species in biological systems has been well documented. In this present study, we have investigated the hypothesis that iron-catalyzed formation of hydroxyl radical (.OH) from superoxide anion radical (O-.2) and H2O2 requires the availability of at least one iron coordination site that is open or occupied by a readily dissociable ligand such as water. This hypothesis was tested by measuring the catalytic activity of 12 different iron chelates using hypoxanthine and xanthine oxidase to generate O-.2. In these same chelates, we also determined the presence or absence of coordinated water by UV-visible spectroscopy and 1H NMR relaxation measurements. Of all chelates tested, only Fe3+ coordinated to diethylenetriamine pentaacetic acid; ethylenediamine di(o-hydroxyphenylacetic acid), phytate, and Desferal lacked coordination water; and only these four complexes failed to produce hydroxyl radical. Separate determinations of the two redox half-reactions involved (i.e. Fe3+ + O-.2----Fe2+ + O2 and Fe2+ + H2O2----Fe3+ + .OH + OH-) indicate that an available coordination site is necessary for the latter (Fenton) reaction. This principle governing iron reactivity may help advance our understanding of the mechanism of oxidative damage in biological systems and may also permit the design of more effective chelators for the control of iron in biological systems.
The absence of L-ascorbic acid, in free or conjugated form, in the fruits of Emblica officinalis Gaertn. (Hindi : amla) has been established by comprehensive chromatographic (column, TLC, HPLC, HPTLC), spectroscopic (1H and 13C NMR, MS) and crucial chemical analyses of its fresh juice and solvent extractives. The long-lived belief that the therapeutic effects of amla is due to its rich vitamin C (L-ascorbic acid) content has thus been dispelled. The potent vitamin C-like activity (antioxidative effect against reactive oxygen species, ROS) of amla fruits has now been located in the low Mr (Mol. wt < 1000) hydrolysable tannins. Four such compounds, emblicanin-A (1), emblicanin-B (2), punigluconin and pedunculagin, have been isolated from the fresh pericarp and their structures established by spectroscopic analyses and chemical transformation. The first two compounds are new naturally occurring galloellagi-tannins, while the other two similar compounds have been reported earlier in other plant species. The mechanism of antioxidative action of 1 and 2 is appraised.
Abstract— In experiments on the interception of reactive intermediates of strongly oxidizing character in dye (S) sensitized photooxidations using p-nitrosodimethylaniline (RNO) as a selective scavenger, it has been observed that some substrates (A) or 1O2 acceptors (like imidazole derivatives) induce the bleaching of RNO as followed spectrophotometrically at 440 nm. Since singlet oxygen (1O2) does not react chemically with RNO, this bleaching is a consequence of 1O2 capture by the imidazole ring which results in the formation of a trans-annular peroxide intermediate [1O2] capable of inducing the bleaching of RNO (-RNO). In the absence of RNO, [1O2] decomposes or rearranges into the final oxygenation product 1O2: 1Δg Thus, the system imidazole plus RNO can be used as a sensitive and selective test for the presence of 1O2 in aqueous solutions. The method can also be applied in the presence of sensitizing dyes which, under visible irradiation, can partially bleach RNO even in the absence of imidazole derivatives. In such a case, the bleaching of RNO is strongly increased by the presence of imidazoles with a characteristic dependence on their concentration. The separation of the product of RNO bleaching by thin layer chromatography can serve as additional proof of the presence of 1O2 in the system. The imidazole plus RNO method has been applied to a number of sensitizing and non-sensitizing dyes.
Sixteen plant-derived or synthetic coumarins with various hydroxyl and other substitutions were tested for their ability to inhibit lipid peroxidation and to scavenge hydroxyl radicals, superoxide radicals and hypochlorous acid. Seven unsubstituted or monosubstituted coumarins were essentially inactive in all tests except for ability to scavenge OH with rate constants approximately greater than 1 x 10(9) M-1. sec-1. Of the remaining nine, six containing dihydroxy substitutions were effective inhibitors of Fe3+-ascorbate-dependent microsomal lipid peroxidation (IC50 less than 20 microM), with ortho-dihydroxy + one additional substitution optimal (IC50 less than 10 microM). ortho-Dihydroxylated coumarins were pro-oxidant (enhanced OH generation) in the Fe3+-EDTA-H2O2 deoxyribose system but decreased OH' generation in the Fe3+-ascorbate-H2O2 deoxyribose system, indicating that these compounds can both chelate iron ions and also readily donate electrons for redox cycling of Fe3+. The meta-dihydroxycoumarin did not show this behaviour, but was an effective scavenger of hypochlorous acid, a property shared by only one other compound. Several other coumarins with one or more hydroxyl substituents were also capable of effectively removing superoxide anions (IC50 3.7-72 microM), although some could not be quantified due to direct rapid reduction of cytochrome c. We conclude that several compounds, notably 5,7-dihydroxy-4-methylcoumarin, possess beneficial biochemical profiles of interest in relation to pathophysiological processes dependent upon reactive oxygen species.
Hydroxyl radicals, generated by reaction of an iron-EDTA complex with H2O2 in the presence of ascorbic acid, attack deoxyribose to form products that, upon heating with thiobarbituric acid at low pH, yield a pink chromogen. Added hydroxyl radical "scavengers" compete with deoxyribose for the hydroxyl radicals produced and diminish chromogen formation. A rate constant for reaction of the scavenger with hydroxyl radical can be deduced from the inhibition of color formation. For a wide range of compounds, rate constants obtained in this way are similar to those determined by pulse radiolysis. It is suggested that the deoxyribose assay is a simple and cheap alternative to pulse radiolysis for determination of rate constants for reaction of most biological molecules with hydroxyl radicals. Rate constants for reactions of ATP, ADP, and Good's buffers with hydroxyl radicals have been determined by this method.
A novel series of 2-O-alkylascorbic acids (5a-u) was synthesized, and their scavenging activities against active oxygen species as well as their suppressive effects on the arrhythmias in rat heart ischemia-reperfusion models were evaluated. Some 2-O-alkylascorbic acids (5e-1) exhibited potent inhibiting activities against lipid peroxidation in rat brain homogenates and in alleviating effects in the ischemia-reperfusion models. Studies on the structure-activity relationship demonstrated that a free 3-enolic hydroxyl group and the longer alkyl chains substituted on the 2-hydroxyl group of ascorbic acid were beneficial for the biological and pharmacological activities. 2-O-Octadecylascorbic acid (5k, CV-3611), one of the most potent and promising compounds, markedly inhibited lipid peroxidation (IC50 = 4.3 X 10(-6) M) and alleviated myocardial lesions induced by ischemia-reperfusion at an oral dose of 1 mg/kg in rats.