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Bioactive ingredients of rose hips (Rosa canina L) with special reference to antioxidative and anti-inflammatory properties: in vitro studies

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Kaj Winther,1 Anne Sophie Vinther Hansen,1 Joan Campbell-Tofte2 1Department of Nutrition, Exercise and Sports, University of Copenhagen, Frederiksberg C, Denmark; 2Coordinating Research Unit, Frederiksberg University Hospital, Copenhagen, Denmark Abstract: Rosa canina pseudo fruits, often referred to as rose hips, have been used as herbal medicine for more than 2,000 years, yet research has only recently begun to clarify specific mechanisms by which this plant product affects human health. Numerous compounds have been identified, and speculations of their bioactivity have implicated flavonoids, carotenoids, and fatty acids (FAs). With more than 4,500 representatives, flavonoids have been subjected to comprehensive research, with results that suggest various individual structures may be health-promoting compounds, also in rose hips. The importance of carotenoids from R. canina is currently being debated, because the demonstration of specific bioactivity among this group is presently less clear. The benefits of specific FAs have been investigated for decades, and several types of FAs are termed “essential” for human health. The specific mechanisms for bioactivity associated with three FAs that are abundant in R. canina fruits have been clarified in research. For example, linoleic acid, α-linolenic acid (mostly present in the seeds from R. canina) and a galactolipid ((2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-3-O-β-d-galactopyranosyl glycerol), referred to as GOPO, have been shown to have anti-inflammatory properties. The aim of this review is to critically analyze the published literature on rose hip research, with emphasis on the broadness and varying significance of the publications. Initially, we describe the chemical ingredients of R. canina pseudo fruits, with some focus on what ingredients are found in the whole pseudo fruit and what we know is confined to the seeds (achene seeds), and/or the shells (hypanthium). Then, we evaluate important papers describing the in vitro investigations of the bioactivity and impacts of the constituents of rose hip. Keywords: rose hip, Rosa canina, antioxidants, anti-inflammation, osteoarthritis, rheumatoid arthritis
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Bioactive ingredients of rose hips (Rosa canina L)
with special reference to antioxidative and anti-
inammatory properties: in vitro studies
Kaj Winther1
Anne Sophie Vinther
Hansen1
Joan Campbell-Tofte2
1Department of Nutrition, Exercise
and Sports, University of Copenhagen,
Frederiksberg C, Denmark;
2Coordinating Research Unit,
Frederiksberg University Hospital,
Copenhagen, Denmark
Correspondence: Kaj Winther
Department of Nutrition, Exercise
and Sports, University of Copenhagen,
26 Rolighedsvej, 1958 Frederiksberg C,
Denmark
Tel +45 3133 3067
Email kaha@nexs.ku.dk
Abstract: Rosa canina pseudo fruits, often referred to as rose hips, have been used as herbal
medicine for more than 2,000 years, yet research has only recently begun to clarify specific
mechanisms by which this plant product affects human health. Numerous compounds have been
identified, and speculations of their bioactivity have implicated flavonoids, carotenoids, and fatty
acids (FAs). With more than 4,500 representatives, flavonoids have been subjected to compre-
hensive research, with results that suggest various individual structures may be health-promoting
compounds, also in rose hips. The importance of carotenoids from R. canina is currently being
debated, because the demonstration of specific bioactivity among this group is presently less
clear. The benefits of specific FAs have been investigated for decades, and several types of FAs
are termed “essential” for human health. The specific mechanisms for bioactivity associated
with three FAs that are abundant in R. canina fruits have been clarified in research. For example,
linoleic acid, α-linolenic acid (mostly present in the seeds from R. canina) and a galactolipid
((2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-3-O-β-d-galactopyranosyl glycerol),
referred to as GOPO, have been shown to have anti-inflammatory properties. The aim of this
review is to critically analyze the published literature on rose hip research, with emphasis on
the broadness and varying significance of the publications. Initially, we describe the chemical
ingredients of R. canina pseudo fruits, with some focus on what ingredients are found in the
whole pseudo fruit and what we know is confined to the seeds (achene seeds), and/or the shells
(hypanthium). Then, we evaluate important papers describing the in vitro investigations of the
bioactivity and impacts of the constituents of rose hip.
Keywords: rose hip, Rosa canina, antioxidants, anti-inflammation, osteoarthritis, rheumatoid
arthritis
Introduction
In recent years, the rising interest in herbal remedies has spawned numerous studies
of a vast number of plants known and used in traditional medicine. This review aims
to clarify the known bioactive constituents of one such plant, Rosa canina L, also
termed “dog rose” (Figure 1). Specifically, the anti-inflammatory properties in the plant
as well as possible impacts of the plant constituents on obesity will be evaluated, as
obesity on its own is a major trigger of osteoarthritis – the most common joint disease
worldwide. In this review, much of the focus will be centered on the pseudo fruits of R.
canina, which are often alluded to as “fruits” in general medical literature. The pseudo
fruits, which are called rose hips, are aggregate fruits consisting of several achenes
(the actual seed-containing fruits of rose hips) enclosed by an enlarged, red, fleshy
floral cup (hypanthium) (Figures 1 and 2). While rose hips are not unique to R. canina,
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Figure 1 The ripe pseudo fruits, “rose hips”, of Rosa canina. Rose hips are the
aggregate fruits of rose plants, composed of enlarged, eshy, red oral cups, enclosing
multiple dry fruitlets (the thin membranes surrounding the individual seeds).
Note: Broadly, rose hips are often alluded to as the “fruits” of R. canina in medicinal
literature.
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Winther et al
but rather present in many types of roses, the rose hips of
R. canina are, to the knowledge of the authors, the only rose
hips with proven medicinal activities. In fact, R. canina has
been known as a medicinal plant for more than 2,000 years. It
consists of several subspecies,1 and several explanations have
been suggested for the plants’ health promoting properties.
These include R. canina’s composition and characteristics
of: 1) flavonoids, 2) carotenoids, 3) fatty acids (FAs), 4) high
content of vitamins (especially vitamin C), 5) antioxidant
properties, and 6) anti-inflammatory agents.
Rose hips contain vast numbers of ingredients, and are
subject to seasonal variation in their specific composition
(like all other plant products). For this reason, we have
strived to review research on standardized rose hip products
of R. canina, and have further chosen to focus our attention
on bioactive constituents. In other words, when referring
to phenolics, the emphasis will mainly be on bioactive
flavonoids. A description of the known active ingredients
and to what extent these components are present qualitatively
and quantitatively in R. canina seeds (seeds of the achenes),
which also contain oils in the seeds themselves or in the shells
(hypanthium), is also given. Finally, there is an evaluation
of the in vitro methodologies used (cell- and non-cell-based
assays) to assess bioactivity of rose hip constituents in the
laboratory.
There are more than 4,500 known flavonoids, making
them an enormous class of naturally occurring phenolic
compounds. Hence, the systematic screening of the flavonoids
is only in its infancy. Interestingly, new research suggests
that a kaempferol derivate (tiliroside), only present in the
seeds of rose hip, may play a role in antiobesity activity in
R. canina.2,3 The rich and diverse carotenoid composition
in R. canina has been known for over 10 years, but so far,
no significant bioactivity has been reported for this class of
compounds. Lately, carotenoids have been mentioned as a part
of a complex, alleged to be present in some Chilean versions
of rose hip powder. However, the complex failed to show any
potency when tested in a clinical trial.4 The FAs in R. canina
have also been investigated, and three major bioactive FA
compounds have been isolated: 1) a galactolipid, 2) linoleic
acid (a ω-6 polyunsaturated FA [PUFA]), and 3) α-linolenic
acid (a ω-3 PUFA). All three compounds have displayed anti-
inflammatory properties.5–7 In addition, the galactolipid has
also shown chondroprotective capacity in vitro.8
The evolution and history of
R. canina
Dog rose (R. canina L) is thought to have evolved in the last
European postglacial period from a different genus of wild-
growing Rosa spp. and an extinct ancestral “Protocaninae”.
The dog rose possesses a unique meiotic and reproductive
system consisting of a heterogamous meiosis with tetraploid
egg cells and haploid pollen forming a permanent pentaploid
organism. The unique meiotic behaviour of R. canina gives
the plant matroclinal characters because of the distribution
of 80% maternal genomes and 20% paternal genes.9
The plant was first described as a medicinal plant by
Pliny the Elder (23–79 BC), who encountered its use among
French tribes in the treatment of dog bites.10 This description
subsequently spawned the name of the species (R. canina).
In Europe, it was also described by the well-known German
nun Hildegard of Bingen (AD 1098–1179), who used it as a
strengthening tea in her treatments.11 Some medical uses of
R. canina are shown in Table 1. The plant has also been known
Figure 2 Simplied botanical anatomy of a rose hip, showing its major components.
Notes: The rose hip shell, the red eshy pulp, is called the hypanthium, and is in fact
not part of the botanical fruit. The botanical fruits of rose hip are the achenes, the
thin membranes surrounding the individual rose hip seeds. The aggregate fruit, the
entire rose hip, is called a “pseudo fruit”.
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Table 1 Documented historical therapeutic uses for Rosa canina
Plant part used Therapy type Symptoms and diseases treated
Roots Internal use Anal hemorrhoids, dysuria, *cough, *rheumatism14,15
Leaves Internal use *Colds, *u, *cough, itching, *eczema14
Branches Internal use
External use
Kidney stones15
Eczema15
Fruits (shells)
(seeds)
Internal use *Colds, *u, *cough, *bronchitis, asthma, *infection, immunologic nephritis, gallbladder diseases,
*burns, vitamin C deciency, colic, *lower urinary tract disorders, as a diuretic and for *arthritis
and *rheumatic disorders; for eyewash, diarrhea, and as prophylaxis for *intestinal catarrhs, as a
laxative, for diabetes and inadequate peripheral circulation14–16
For the kidneys and lower urinary tract, as a diuretic, for *osteoarthritis, *rheumatism, *gout,
and sciatica; for *colds and for *diseases with fever, for blood purication as an astringent, as a
laxative, and for vitamin C deciency16
External use *Rheumatism, hemorrhoids, *diarrhea, cardiac disorders, hypoglycemia and *infection15
Notes: Roots, leaves, and branches have been used in folk medicine since ancient times. Most research today is based on seeds and shells from the rose hips. *Inammatory
disease.
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Rose hip antioxidative and anti-inammatory properties: in vitro studies
by sailors as a means of protection against scurvy, due to its
high concentration of vitamin C, and thus it spread to several
continents. Indeed, the high concentration of vitamin C in R.
canina is well documented, for during the Second World War,
rose hips were the key source of vitamin C in Britain, and
massive harvest of rose hips were organized by the govern-
ment.12 In Scandinavia, it has been a tradition to use the fruits
for making marmalades and soups, although this has not been
associated with health promotion per se. An explanation may
very well be that the key ingredients responsible for health
effects are labile and disintegrate under high temperatures,
and that the boiling involved in the preparation of soups and
marmalades inactivates the bioactive components in the plant
material. Another aspect is that only the flesh (not the seeds)
is used in tea and soup. Details of the “anatomy” of a rose
hip are presented in Figures 2 and 3.
Some medical utilization of
R. canina
In European literature, the medicinal uses of R. canina are not
well described; however, The Complete German Commission
E Monographs: Therapeutic Guide to Herbal Medicines does
list it as a medicinal plant, suggesting the use of the pseudo
fruit’s seeds (seed of the achenes) and shells (the hypanthium
surrounding the achenes of the pseudo fruit) for treating
ailments, such as arthritic conditions, gout, sciatica, and
diseases of the kidney and lower urinary tract.13 In Turkish
folk medicine, however, R. canina is a very valued plant,
such that the roots, leaves, branches, and fruits are used in
the treatment of a number of ailments (Table 1).14–16 However,
it should be emphasized that, in this review, the focus will
only be on papers describing research on rose hip seeds and
shells, for R. canina roots, leaves, and branches are at present
the only species of academic interest.
In 2002, an extensive paper was published evaluating
the total antioxidant properties in dietary plants (vegetables
and fruits) from geographical locations all over the world.17
This paper demonstrated that there is a more than 1,000-fold
difference in total antioxidants in dietary plants – R. canina
was scored as containing the highest amount of antioxidant
of all the plants examined.17
Known compounds of R. canina
fruits
In recent years, several investigations have been launched to
determine the compounds contained in R. canina fruits using
high-performance liquid chromatography, thin-layer chroma-
tography, tandem mass spectrometry, gas chromatography,
and diode-array detection.18–21 From these investigations,
numerous compounds have been identified in R. canina fruits.
However, future investigations should be made to further
identify additional compounds, which may in fact be respon-
sible for some of the bioactive properties of the plant shown
in recent years’ corresponding medical research. In addition,
Figure 3 Separated seeds and shells from the hips of Rosa canina.
Note: Commercial rose hip products contain these structures in varying degrees;
some contain only shells.
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Table 2 A variety of known compounds of Rosa canina with
bioactive properties
Compound
type
Compound
name
Systematic nomenclature
and lipid number*
Triterpene acid Ursolic acid18
Oleanolic acid18
Betulinic acid18
FAs Lauric acid19,20 Dodecanoic acid (C 12:0)
Myristic acid20,21 Tetradecanoid acid (C 14:0)
Palmitic acid19–21 Hexadecanoic acid (C 16:0)
Palmitoletic acid20,21 (C 16:1 ω-7)
Stearic acid20,21 Octadecanoic acid (C 18:0)
Oleic acid20,21 (C 18:1 ω-9)
Linoleic acid19–21 All-cis-9,12-octadecadienoic acid
(cis-C 18:2 ω-6)
α-Linolenic acid19,20 All-cis-9,12,15-octadecatrienoic
acid (cis-C 18:3 ω-3)
Arachidic acid19,20 Eicosanoic acid (C 20:0)
Behenic acid20 Docosanoic acid (C 22:0)
Docosadienoic
acid19
All-cis-13,16-docosadienoic acid
(cis-C 22:2 ω-6)
Galactolipids GOPO5(2S)-1,2-di-O-[(9Z,12Z,15Z)-
octadeca-9-12-15trienoyl]-3-
O-β -d-galactopyranosyl glycerol
Note: *Lipid number only given for lipids.
Abbreviations: GOPO, (2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-
3-O-β-d-galactopyranosyl glycerol; FAs, fatty acids.
Table 3 The function of vitamins and deciency-related diseases
Vitamin Function Deciency
A#Roles in vision, growth,
and reproduction
Night blindness, corneal damage,
damage to respiratory and
gastrointestinal tracts
BCoenzymes Beriberi, cheilosis, and angular
stomatitis; dermatitis, depression,
confusion, convulsion, diarrhea,
hypertension, rash about the
eyebrows, muscle pain, fatigue
(rare), anemia, pernicious anemia,
methylmalonic acidosis
C Antioxidant Scurvy
D Regulation of calcium
and phosphate
metabolism
Rickets, skeletal deformities,
impaired growth, osteoporosis,
osteomalacia
E Antioxidant Inhibition of sperm production,
lesions in muscles ad nerves (rare)
K Blood coagulation Subdermal hemorrhaging
Note: #Rosa canina does not contain vitamin A, but carotenoids from R. canina are
vitamin A precursors.
quantitative investigations of the constituents are lacking,
and such studies may prove helpful in medicinal treatments,
as well as for developing proper control of the breeding and
postharvesting techniques for R. canina. Some compounds
with bioactive properties are shown in Table 2.
Vitamins
Vitamins are defined as organic compounds synthesized in
plants and in some lower animals, which are necessary in the
diets of higher animals, in minute amounts. Vitamins have a
diverse array of functions in the organism, such as coenzyme
activity, precursor activity, antioxidative effect, regulation of
calcium and phosphorus uptake, and regulation of coagula-
tion (blood clotting). Vitamin deficiency in humans leads to
numerous diseases and ailments (Table 3), and it is interesting
to note that sailors for centuries used rose hip as a remedy
against scurvy and brought the plant from Europe to South
America, not knowing that vitamin C was a key factor for
the relief of the disease.
Vitamins comprise a group of very different compounds
with very different chemical properties. Their solubility
varies, as some of the compounds have large numbers of
functional groups capable of forming hydrogen bonds with
water, while other structures are nonpolar. Water-soluble
vitamins like the vitamins C and B are not stored in the
body, but constantly need to be supplied through the diet.
Unused water-soluble vitamins are excreted. Water-insoluble
vitamins like vitamins A and E are storable and are therefore
not excreted when consumed in excessive amounts. This
situation can, unfortunately, lead to illness.22–24 All vitamins
are bioactive, and research on the subject is extensive. In
particular, the antioxidant potential of vitamins C and E has
been subjected to numerous studies in recent years.17,25,26
Apart from its protection against scurvy, which is
explained by its participation in the synthesis of collagen,
vitamin C plays a part in several important enzymatic
syntheses. For example, vitamin C is important in the syn-
thesis of dopamine, carnitine, a number of neuroendocrine
peptides, and in the transformation of cholesterol into bile
acids.25 For its part, vitamin E is thought to mainly act as
an antioxidant, protecting PUFAs within plasma membrane
phospholipids and in plasma lipoproteins. Current research
has revealed that vitamin E inhibits protein kinase C activity,
although the physiological significance of this effect is yet
to be clarified.25
Carotenoids
Carotenoids are tetraterpenoids, which absorb light between
400 and 500 nm in wavelength. As a result, carotenoids
are evident as red, orange, and yellow colors in plants,
imparting these colors to fruits and flowers. In addition,
they are important light-harvesting molecules that transfer
energy to reaction centers during photosynthesis and that
suppress damaging photochemical reactions, particularly
oxidations (radical scavengers). Animals are unable to
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Rose hip antioxidative and anti-inammatory properties: in vitro studies
synthesize carotenoids, and are therefore dependent on
acquiring carotenoids through their diet. Most carote-
noids are 40-carbon structures with isoprene as their basic
structural unit. Carotenoids are generally divided into two
subgroups: 1) xanthophylls, which are molecules contain-
ing oxygen (eg, lutein, zeaxanthin, and cryptoxanthin) and
2) carotenes, which are non-hydroxylated hydrocarbons (ie,
alpha-carotene, beta-carotene, and lycopene). The colors of
carotenoids are linked directly to their structure (the number
of conjugated double bonds and presence or absence of
oxygen). Xanthophylls, which contain oxygen, are often
yellow, while carotenes, which lack oxygen, are orange or
red (BL Møller, University of Copenhagen, personal com-
munication, June, 2008).26
Studies in carotenoids have shown bioactivity, as caro-
tenoids are associated with antioxidation both in vitro and
in vivo.27–30 The antioxidant activities of carotenoids are a
direct consequence of their structure, as they consist of a
highly reactive electron-rich system of conjugated double
bonds, enabling them to form radicals stabilized from
attacks by electrophilic reagents.31 However, the use of
animal models for studying carotenoids is limited, since
most animals do not absorb or metabolize carotenoids like
humans do.32
Dietary carotenoids have been associated with induction
of apoptosis, inhibition of mammary cell proliferation, and
inhibition of angina pectoris.33–37 Carotenoids have also been
suggested to prevent prostate cancer in humans.38 However, a
recent meta-analysis of 68 reliable antioxidant supplementa-
tion experiments involving a total of 232,606 individuals sug-
gests that the consumption of additional beta-carotene from
supplements is unlikely to be beneficial, and may actually
be harmful.39 This may be due to the high doses of a single
carotenoid (beta-carotene). Any reported positive effects of
carotenoids may therefore suggest a “sparring effect”, due
to the fact that carotenoids are suited better as markers of a
high intake of vegetables and fruit,40 or that the epidemio-
logical results reported are caused by compounds with no
relation to carotenoids. However, a few carotenoids have been
reported as exhibiting interesting bioactivity. For instance,
studies of lutein and zeaxanthin in humans show that these
compounds are found in high concentrations in the macula
of the human retina, and may play a role in protecting the
macula and photoreceptor outer segments of the retina from
oxidative stress.41 Interestingly, lutein and zeaxanthin are also
constituents of rose hip,42 and volunteers with macular degen-
eration taking rose hip seed and shell product have claimed
visual improvement (K Winther, University of Copenhagen,
personal communication, August, 2014).
Diets rich in lutein and zeaxanthin have been moderately
associated with decreased prevalence of nuclear cataracts in
elderly women,43 as well as in the prevention of age-related
macular degeneration. Yet, there is no direct evidence
that there are more antioxidant protections of the macula
apart from the absorption of blue light.44 A previous study
have shown that incorporation of carotenoids in lipophilic
membranes and subsequent exposure to blue light reveals
a filter efficacy in the order of lutein . zeaxanthin .
beta- carotene . lycopene.45 Furthermore, lycopene has
been suggested to promote health when given as a tomato
extract or paste in cases of prostate cancer46 and in cases
of non-eosinophilic airway inflammation.47 These findings
are, however, problematic, because they are the result of the
administration of a mixture of compounds. Indeed, a review
written by Glovannucci concluded that a link between lyco-
pene and prostate cancer is doubtful.48
Flavonoids
Flavonoids are secondary plant metabolites belonging to the
phenylpropanoid group of compounds. The basic flavonoid
skeleton consists of two aromatic rings joined by a three-carbon
bridge. Two separate biosynthetic pathways contribute to the
formation of this skeletal structure; the three-carbon bridge and
one aromatic ring are derived from the shikimic acid pathway
via phenylalanine, and the other aromatic ring comes from the
condensation of three acetate units produced in the malonate
pathway. Flavonoids may, however, have diverse substituents,
the commonest being sugars, as most flavonoids exist naturally
as glycosides. Other common substitutions are methylations.
Examples of flavonoids are presented in Table 4.49
Flavonoids can be divided into the following six sub-
classes: 1) anthocyanins, 2) flavones, 3) flavanols, 4) isofla-
vones, 5) flavanols, and 6) flavanones. The most widespread
Table 4 Different avonoids present in Rosa canina
Flavonoid name Seeds Shells
Hyperoside 0.15±0.07 (0.05–0.31) 0.08±0.02 (0.03–0.12)
Tiliroside 0.07±0.03 (0.02–0.13) 0.00
Rutin 0.03±0.01 (0.00–0.06) 0.01±0.00 (0.00–0.01)
Quercetin 0.04±0.02 (0.01–0.09) 0.04±0.01 (0.02–0.06)
Catechin 0.19±0.06 (0.09–0.29) 0.39±0.19 (0.21–0.82)
Astragalin 0.04±0.02 (0.02–0.08) 0.05±0.04 (0.01–0.12)
Total sum of
avonoids
0.52±0.10 (0.32–0.68) 0.56±0.21 (0.33–0.99)
Notes: Some avonoids are very abundant in seeds and others are more abundant
in the shells, while some are equally represented in both seeds and shells. Data are
represented as means of ten different powders (mg/g dry weight).
Adapted from Fecka, Qualitative and quantitative determination of hydrolysable
tannins and other polyphenols in herbal products from meadowsweet and dog rose.
Phytochem Anal. 2009;20:177–190. John Wiley & Sons, Ltd. Copyright © 2009 John
Wiley & Sons, Ltd.49
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group of the colored flavonoids is anthocyanins, which are
beta-glycosides that have sugars in position 3. Anthocyanins
act as attraction agents, luring animals (ie, pollinators) to
flowers and fruits with visual signals. They may also serve
as deterrents of microbes and insects. Another main func-
tion of flavonoids is in protecting cells from ultraviolet B
(UV-B) radiation. They accumulate in epidermal layers and
harness damaging UV-B radiation, while allowing visible
wavelengths to pass through. Indeed, rose hip seed oil, which
is also rich in flavonoids, is used as protection of the skin
from sunburns in many countries. Flavones and flavanols
absorb light at shorter wavelengths than wavelengths utilized
by anthocyanins and carotenoids. As a result, flavones and
flavanols are not visible to the human eye. They may, however,
be visible to insects that see UV tones in the light spectrum,
as they have been associated with UV patterns in flowers
called “nectar guides”. Isoflavones have been shown to have
several biological activities, which also include antimicrobial
and insecticidal properties.50–52
Some of the health-promoting effects of fruit and veg-
etable intake have been attributed to their content of poly-
phenols and flavonoids. However, research has yet to clarify
the specific mechanism(s) by which these compounds affect
human health. In vitro data obtained from screening bio-
activity of the flavonoids have often conflicted with results
obtained from in vivo studies on the antioxidant capacity of
plasma or on the resistance of plasma and lipoproteins to oxi-
dation ex vivo after the consumption of flavonoid-rich foods
by human subjects.53 Consumption of flavonoid-rich foods,
in particular fruits and vegetables, has been associated with
a lower incidence of diseases such as cancer, inflammation,
heart disease, ischemic stroke, atherosclerosis, and other
chronic diseases.54–60 Quercetin is one of the few flavonoids
that shows interesting bioactive properties in vitro and in
some in vivo tests. For example, rutin and its glycoside
(rutin and quercitrin) have shown anti-inflammatory proper-
ties in models of intestinal inflammation, possibly through
down-regulation of the nuclear factor-kappa beta pathway.61
Quercetin has also been suggested to modify eicosanoid
biosynthesis, to protect low-density lipoprotein (LDL) from
oxidation, to have antithrombotic effects, and to relax the
cardiovascular smooth muscles.62 Interestingly, R. canina
contains the flavonoid, tiliroside (kaempferol 3-O-β-d-(6-p-
coumaryl)-glycopyranoside)2 that inhibits the oxidation of
human LDL in vitro and has been shown to possess signifi-
cant antiobesity, antioxidant, cytotoxic, and anticomplement
properties in humans.3,63 The molecular structures of tiliroside
and hyperoside are shown in Figure 4.
Conversely, some flavonoids have been associated with a
decrease in the nutritional value of some foods and fodders.
Explanations for the negative effect have been based on their
ability to form complexes with proteins, essential amino
acids, carbohydrates, and digestive enzymes.59,60
Triterpene acids
Triterpenes are one of the most numerous and diverse groups
of natural phytochemicals. These include more than 4,000 dif-
ferent complex molecules that are, for the most part, beyond
the reach of chemical synthesis. Simple triterpenes are compo-
nents of surface waxes and specialized membranes of plants.
Some simple triterpenes may act as signaling molecules,
whereas complex glycosylated triterpenes or the saponins
HO
OH
OH
OH
OH
OH
OH
OH
Tiliroside Hyperoside
OH
OH
OH
AB
HO
HO
HO
HO
O
O
O
O
O
O
OOO
O
Figure 4 The molecular structures of tiliroside (A) and hyperoside (B).
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Rose hip antioxidative and anti-inammatory properties: in vitro studies
provide protection against pathogens and pests. Hence, the
triterpenes have a wide range of applications in food, health,
and industrial biotechnology sectors.18,64 Animals and plants
make triterpenes that are precursors to sterols. Sterols are
important structural components of membranes, and they also
have a role in cell signaling as steroidal hormones. However,
triterpenes are not regarded as essential for normal growth
and development. Both simple and conjugated triterpenes
are well represented among rose hip constituents. Triterpene
acids and other FAs are listed in Table 2.
FAs and galactolipids
FAs contain hydrocarbon chains of various lengths and
degrees of saturation, terminating with a carboxylic acid
group. FAs are key constituents of lipids, which by definition
are water-insoluble biomolecules that are highly soluble in
organic solvents. Lipids are key constituents of cell mem-
branes, serve as fuel molecules or highly concentrated energy
stores, act as signal molecules, and are also messengers in
signal-transduction pathways. Triglycerides are the major
storage lipids of both plants and animals. In animal triglyc-
erides, FAs often are saturated (do not contain double bonds),
resulting in molecules with linear chains that pack tightly and
generate solid fats. By contrast, FAs are often unsaturated in
plants. This prevents close packing, such that the resulting
lipid molecules tend to be liquid at room temperature and
are therefore termed “oils”. Fats and oils play vital roles in
nutrition and in the food industry, where they are divided into
groups according to their degree of saturation.51,65,66
In general, the consensus is that saturated FAs are abundant
in many average western meat-based diets, while PUFAs, such
as ω-3 and ω-6 FAs, are lacking. As earlier mentioned in Table
2, the seeds of R. canina fruits are rich in the ω-3 and ω-6
PUFAs; the extensive body of research into the physiological
significance of PUFAs show their numerous health benefits,
which include decreasing triglycerides and cholesterol in
blood, inhibition of thrombosis, dilatation of blood vessels,
enhancement of blood fluidity, increased plasticity of eryth-
rocytes, reduced cardiovascular disease, and inhibition of
inflammation.67–69 Furthermore, other PUFAs, such as linoleic
and α-linolenic acids isolated from R. canina seeds, are also
rich in oils and have been demonstrated to inhibit cyclooxyge-
nase (COX)-1 and COX-2, thus revealing anti-inflammatory
activity.6,7 Other FAs from plants and fish have also been
demonstrated to have similar anti-inflammatory proper-
ties.67,70–72 Galactolipids are glycolipids in which the sugar
molecule, galactose, is attached to the lipid backbone glycerol.
Galactolipids are especially abundant in thylakoid membranes
in plants. The galactolipid (2S)-1,2-di-O-[(9Z,12Z,15Z)-
octadeca-9-12-15-trienoyl]-3-O-β-d-galactopyranosyl glyc-
erol, also known as GOPO, has been isolated from R. canina
and has shown strong anti-inflammatory activities.5 Taking
rose hip seed and rose hip seed shell powder into account, FAs
and galactolipid GOPO can explain some of the improvement
observed in patients with inflammatory diseases.73
Seeds and shells
dried below 40°C
Mainly shells
dried at higher temperature
AB
Figure 6 Rose hip powders with different constituents and drying temperatures.
Notes: Powder from a seed and shell product that has not been heated to .40°C
during the drying process (A), compared to powder from a product mainly based
on shells, which has been dried at a higher temperature (B).
OH
OH
OH
HO
O
GOPO
O
O
O
O
O
H
H
Figure 7 The molecular structure of the galactolipid GOPO.
Abbreviation: GOPO, (2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-3-
O-β-d-galactopyranosyl glycerol.
Figure 5 The content of the galactolipid GOPO in different commercially available
rose hip products.
Note: Data from DB Lab A/S, Odense, Denmark.
Abbreviation: GOPO, (2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-3-
O-β-d-galactopyranosyl glycerol.
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Winther et al
Other compounds including dietary
bers
Beta-sitosterol is a phytosterol present in rose hip and is
thought to inhibit the absorption of dietary cholesterol.
Several reports54,55 have appeared in the literature indicating
that phytosterols have immunological and anti-inflammatory
activities in in vitro and in vivo models of cancer (colorectal
and breast cancer). However, it is only in the last 10 years
that their direct immune-modulatory activity on human
lymphocytes and their mechanism of action in cancer cells
have been investigated.74
Rose hips, and in particular their seeds, have high amounts
of dietary fibers, which include pectin. Although mammals
are unable to digest vegetable fibers, dietary fibers are very
important in human diets because they slow down the move-
ment of food through the intestinal tract, promoting better
digestion and the increased absorption of nutrients.76
Comparison of active ingredients in
seeds and shells
Schwager et al compared two rose hip products, a pure rose
hip shell (hypanthium) product and a product containing rose
hip shell (hypanthium) combined with a seed (seed of the
rose hip achenes), respectively.73 FA content in the seed-only
product was more than four times higher than that of the
product without seeds. Likewise, PUFA linoleic acid content
was more than seven times higher in the rose hip product
containing seeds as compared to the product made from the
shells alone, indicating that FAs are predominantly found in
rose hip seeds.73 In contrast, vitamin C and beta-carotene con-
tents were nearly identical in both products, while the amounts
of triterpenoids, galactolipids, lycopene, and vitamin E were
higher in the shell-only product, indicating dominance of these
constituents in this part of the fruit. Flavonoids are present
to the same extent in rose hip seeds and shells. However, the
distribution of flavonoids is different in rose hip seeds as
compared to the distribution found in the shells. Details of
these differences are presented in Table 4.
In rose hip seeds, linoleic and α-linolenic acids are found
as part of the triglycerides and are therefore not free FAs.
Generally, triglycerides of long-chain FAs have very low solu-
bility (Merck Index), while free FAs can easily form salts and
so possess improved solubility. These properties may explain
some of the inconsistencies experienced in bioassays when
extracts from seeds are compared to extracts from rose hip
shells or from combined seed and shell preparations.73,76 Con-
sequently, when evaluating bioassay studies based on extracts,
one should always consider the relevant physiologically active
form of the investigational medicines and the environment
in which the test is being conducted.
Differences in active ingredients between
species
The biological variation in phytochemicals of rose hip from
different species of R. canina is pronounced. Ten different
commercially available rose hip products were tested for their
contents of hydrolysable polyphenols in shells and in seeds.49
As can be seen from the range of species (Table 4), the varia-
tion of hyperoside in shells is above 600% and the variation
in seeds is approximately 400%. The variation of rutin in
seeds is likewise 600%, while for shells, this flavonoid was
detectible in only one out of nine products. Certain tannins
were not found in the seeds at all, and tiliroside, an important
flavonoid in obesity research, was only present in the seeds;
hyperoside in shells the varied more than 600%49 (Table 4).
In a different study, the amount of alpha-linoleic and linolenic
acids were tested in eight commercially available seed oils,
and the variation between products was 30%–70% which is
much lower than what was reported for flavonoids in Table 4
(A Guzman, Faculty of Pharmaceutical Science, University
of Copenhagen, personal communication, June, 2012). How-
ever, when the galactolipid GOPO content was determined in
ten different commercial rose hip powders that are available
in Denmark, GOPO content varied from less than 1% to 20%
of that found in the combined seed and shell powder based
on R. canina lito, that is produced using standardized and
patented methodology (Product no. 10, Figure 5).
The variation of active ingredients within the different
species of R. canina, the environments they grow in, eg,
number of hours with sun, altitude, soil, and amount of
rain, influence the biochemical composition of the plant
and thereby the quality of the product produced. In addi-
tion, active ingredient variations are influenced by rose hip
drying methodology, including the drying temperature and
time point of harvesting.77–81 It is interesting to note that in
countries where rose hip has been used as a tea (France) or
a soup (Sweden), for centuries there were, until recently,
hardly any reports on anti-inflammatory action. This may be
due to the fact that cooking destroys some active elements of
rose hip and perhaps, also due to the fact that the seeds were
never used in tea, soup, or marmalade. Rose hip powders also
exhibit huge differences in color and smell, depending on the
method of production, quality, and quantity of the different
ingredients. Hence, the powders may be brownish (possibly
caused by exposure to high temperatures during production),
as some drying facilities use temperatures as high as 800°C.
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Rose hip antioxidative and anti-inammatory properties: in vitro studies
Some rose hip powders are orange, especially when kept at
lower processing temperatures (Figure 6). It is important to
note here that the color is also determined by the amount of
seeds and shells. Variations in active ingredients are explored
in Figure 4.
In summary, the quality and amount of active ingredients
in rose hip powders vary widely depending on the subspecies
of R. canina used, method of production, growth environ-
ment, and time of harvest. As of now, it is very difficult for
the consumer to rely on the product information provided
by the store or on the Internet. It is therefore very important
that there is proper product regulation and quality control put
in place by the government or regulating agencies.
In vitro studies of the effects of rose
hip
One of the first publications to show that rose hip might be
of relevance as an anti-inflammatory agent reported that a
water extract of rose hip inhibited chemotaxis of polymor-
phonucleated (PMN) cells isolated from healthy humans at
a dosage of 500 µg/mL.79 In the same study, a water extract
of rose hip shells alone was shown to be superior in reduc-
ing chemotaxis of PMN cells, as compared to the effects
achieved with extracts of the whole fruit, ie, from both shells
and seeds.79
As the 1999 study79 did not include extraction of FAs that
are abundant in the seeds, the authors may have arrived at the
wrong conclusion that R. canina shells are the most impor-
tant part of the fruit as regards chemotaxis and antioxidative
activity. This deduction can be made because subsequent
studies have revealed high levels of fat-soluble elements in
rose hip, including earlier mentioned FAs (in the section FAs
and galactolipids), with anti-inflammatory and antioxida-
tive activity.5–7,80,81 Polyphenolics (proanthocyanidins and
flavonoids) with antioxidative properties, as demonstrated
by their inhibition of chemotaxis in human PMN cells, were
found in rose hip extracted with lipophilic solvents.80 This
extract could inhibit reactive oxygen species in both cel-
lular and cell-free systems, with half maximal inhibitory
concentration (IC50) values ranging from 5.73 to 1.33 mg/L.
Furthermore, the antioxidative effects were clearly shown not
to be due to vitamin C alone, but were also due to substantial
contributions from polyphenols.80
Isolation of GOPO
Motivated by the earlier findings, a group of Danish sci-
entists5 decided to search for the biochemical background
of the anti-inflammatory properties reported in R. canina.
Thus, starting from milled powder of R. canina lito, which
contained the natural amount of shells and seeds, both water
and lipophilic extractions were made, fractionated, and the
resulting extracts and fractions were tested in in vitro PMN
bioassays. The fraction that showed high bioactivity in inhib-
iting chemotaxis of PMNs and monocytes in vitro contained
only one compound, GOPO (Figure 7). With the aid of
nuclear magnetic resonance (NMR), optical analysis, basic
methanolysis, and acidic hydrolysis, the fraction was found
to contain GOPO with a purity of .98%. The authors have
indicated their readiness to provide a detailed description of
the isolation procedure and identification data in the form of
tabulated hydrogen-1 (1H) and carbon-13 (13C) NMR data.
The molecule was later been tested in different settings to
confirm its strong anti-inflammatory and chondroprotective
effects.8 From the Larsen et al publication,5 it is not clear if
the galactolipid, GOPO, is mainly associated with rose hip
shells or the seeds. However, data from Schwager et al73
specify that GOPO is present mostly in the shells.
COX inhibition by linoleic- and
α-linolenic acid-containing rose hip
extract
With the aid of COX enzyme in vitro assay kits, extracts
of powdered whole fruits (seeds and shells) were tested
for their impacts on COX-1 and COX-2 enzyme activity.6
Water extracts did not show activity in the COX-1/COX-2
assay,6,7 whereas methanol, dichloromethane, and hexane
extracts all showed dose-dependent inhibition of COX-1 and
COX-2 enzyme activity. The lowest IC50 values for methanol
extracts of COX-1 and COX-2 inhibition were 12 µg/mL and
19 µg/mL, respectively. The data suggest that elements that
are soluble in organic solvents must account for some of the
effects on COX-1 and COX-2.6,7
Jäger et al have showed that GOPO is not the only FA
involved in anti-inflammation, as extracts of whole rose hip
fruits (containing seeds and shells) made with petroleum
ether, dichloromethane, or methanol all exhibited dose-
dependent inhibition of both COX-1 and COX-2 enzymes, as
opposed to the water extract, which did not show any activity.7
The IC50 value for linoleic acid was 85 µM for COX-1 and
0.6 µM for COX-2. For α-linolenic acid, the values were
52 µM for COX-1 and 12 µM for COX-2. The COX-2/
COX-1 ratio for linolenic and α-linolenic acids were 0.007
and 0.2, respectively, indicating that both acids are selective
COX-2 inhibitors. Authentic standard linoleic acid was also
tested, and this test confirmed previous results.7 As COX-2
inhibitors do not affect platelet aggregation in humans, the
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data from the Jäger et al,7 study are in agreement with an
earlier report from Rein et al,81,82 which showed that platelet
aggregation was not affected by rose hip powder when com-
pared with the effects of acetylsalicylic acid, a non-steroidal
anti-inflammatory drug that broadly inhibits the arachidonic
acid pathway.
In a Korean study that tested the effect of rose hip extracts
on the expression of the COX enzymes in isolated cartilage
cells, it was demonstrated that some of the active ingredients
in rose hips may be both heat stable and soluble in hot water.83
This result was fully supported, because extracts made by
heating the shells alone or the whole fruits (containing seeds
and shells) in boiling water inhibited COX-2 protein expres-
sion dose-dependently, whereas COX-1 expression remained
unaffected. As the heat treatment involved keeping the plant
materials at 1,000°C for more than 4 hours, one could argue
that the preparation of the extract had been harsh. However,
European cell-based studies showed that as it is lipophilic
compounds that inhibit COX-2 enzymes,7,76 it is conceivable
that the boiling water treatment that lasted several hours also
dissolved some additional active ingredients. However, boil-
ing for several hours is far from what happens in the living
organism; by boiling for so long, many active ingredients
from shells and from seeds may have been destroyed in
making the two preparations, which initially were very dif-
ferent, the same.
The triterpene acids ursolic acid, oleanolic acid, and
betulinic acid have also been identified in R. canina,
although only in minute amounts.76 In the same study and as
expected, linoleic and α-linolenic acids were also identified.
However, there were no clear correlations between the amount
of unsaturated FAs and COX-1 or COX-2 enzyme activity,
which led the authors to suggest that possibly, other yet-
undescribed lipophilic constituents might play a role in the
observed in vitro inhibition of arachidonic acid metabolism.
In particular, the methanolic extract exhibited potent radical
scavenger activity, which may be correlated to the relatively
high phenolic content of the preparation. The general con-
clusion was that extracts derived from powdered rose hip
shells (without seeds) were more effective in the assays,
as compared to extracts derived from powder consisting of
both shells and seeds.76 It should, however, be borne in mind
that FAs, especially those present in the seeds, are strongly
bound to triglycerides. The n-hexane and dichloromethane
extraction used in the study may have been less optimal
for obtaining the total amount of bioactive lipid-soluble
elements. This may also explain the difference in the amount
of extracted FAs from seeds and shells as compared to the
data from Wenzig et al76 and Schwager et al.73 What happens
in the gastrointestinal tract in animals or in humans ingesting
the rose hip powders may be very different from the biodata
obtained when testing extracts and fractions of rose hip in a
laboratory setting. Wenzig et al, however, demonstrated that
there seem to be other lipophilic elements than the known
FAs, including GOPO, which are responsible for observed
anti-inflammatory activity.76
Anti-inammatory triterpenes and
interleukins
The Mono Mac 6 cell line resembles mature human mono-
cytes and expresses interleukin (IL)-6 in a dose-dependent
manner following activation with lipopolysaccharides
(LPSs).18 Standardized rose hip powder containing the natural
amount of seeds and shells (R. canina lito) was extracted
with petroleum ether, dichloromethane, ethyl acetate, and
water. The dichloromethane extract significantly inhibited the
release of IL-6 from the cell line at the level of 10 µg/mL.
Oleanic, betulinic, and ursolic acid were isolated from this
dichloromethane extract. While only oleanolic and ursolic
acids exhibited concentration-dependent inhibition of IL-6
release from LPS-activated cells, a mixture of the three trit-
erpene acids exhibited an even stronger inhibition of IL-6,
with an IC50 value of 21±6 µM.18 Thus, it has been shown
that bioactivity of a plant product is often dependent on the
interplay between many different ingredients and not a
single molecule.
In another study, inflammatory processes were induced in
murine macrophage cells or human peripheral blood leuco-
cytes with LPS, and the level of inflammatory mediators such
as nitric oxide, prostaglandin E2, and cytokines/chemokines
that are released during activation was determined. In mac-
rophages and in blood peripheral blood leucocytes, rose hip
powder consisting of seeds and shells dissolved in dimethyl
sulfoxide (DMSO), as well as the isolated molecule GOPO,
inhibited the production of cytokines such as tumor necrosis
factor (TNF)-alpha, IL-1 beta, IL-6, and IL-12.8
Schwager et al have definitively demonstrated that rose
hip powder prepared from whole dried R. canina fruits and
purified GOPO attenuates inflammatory responses in cel-
lular systems such as PMNs and chondrocytes, in a way that
mirrors the reduction of the catabolic processes associated
with the breakdown of cartilage in osteoarthritis or rheu-
matoid arthritis.8,74 Specifically, the gene expression and
secretion of cytokines CCL5/RANTES, CXCL10/IP-10,
IL-6, and IL-12 were reduced in LPS/interferon-activated
peripheral blood leukocytes treated with rose hip powder
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Rose hip antioxidative and anti-inammatory properties: in vitro studies
or GOPO. Likewise, rose hip preparations reduced the
expression of matrix metalloproteinase (MMP)-1, MMP-3,
and MMP-13, and ADAMTS-4 in IL-1-treated normal
chondrocytes.8
In summary, the results from testing extracts of rose hip
powder on different cell-based and non-cell-based bioassay
systems indicate that rose hip powder based on shells alone
may be more active than that which is made from grinding
whole rose hip fruits (containing seeds and shells). The fact
that certain elements with lipophilic characteristics are not
extracted from seeds by using the common laboratory extrac-
tants may explain why the processes triggered in in vitro
assays may be very different from what goes on in a living
organism, which ingests the entire powdered rose hip that is
further exposed to influences from gastric acid and numerous
digestive enzymes in the gastrointestinal tract.
Limitations
The literature search included articles from 1975 onward
to identify studies on rose hip, R. canina, or dog rose. The
search was restricted to English language articles. We fur-
ther searched the authors’ own files to improve the number
of relevant papers. Finally, relevant papers were extracted
independently by the three authors.
Conclusion
Much research has been conducted to investigate the
health-enhancing properties of R. canina pseudo fruits, and
the current review addresses only a small portion of those
enquiries, particularly those that are directed at understanding
the beneficial effects of rose hip on pain and inflammation in
joint diseases. From the current review, it is clear that active
research continues to be conducted worldwide on various
bioactive properties of the compounds found in R. canina
pseudo fruits (rose hips).
Although several active ingredients have been sug-
gested, it is too early to give a definite answer as to what
is the most important active ingredient in rose hip in
clinical settings. Current findings suggest that flavonoids
(especially tiliroside),2,3 GOPO,5 and the PUFAs, linoleic
and α-linolenic acids,6,7 are among the more interesting
ingredients. However, it is also evident that there are other
very important lipid-soluble compounds in rose hip that are
still unknown.76
There is a great variability in the different bioactive
ingredients in different species of R. canina. In addition, the
growth environment, period of harvesting, and the mode of
production of the final rose hip powder play important roles
in determining the quality of the powders that consumers
get. More quality control is therefore needed. As it stands
today, with so many different powders and capsules available
on the shelves of stores, there is a lack of adequate quality
declaration. For example, it is difficult to ascertain if the rose
hip preparation one is considering buying contains only rose
hip shell/husk powder or is a combination of seed plus shell/
husk powder.
In vitro studies carried out in non-cell and in cell-based
systems are very interesting and informative, and they teach
us much about the effects of rose hip constituents in important
and relevant cellular mechanisms. However, such studies are
normally based on extractions presented to cells in a test
tube a situation that can be very far from what actually
occurs in humans or in animals ingesting rose hip powder.
Thus, we should be critical of in vitro studies. Future animal
and human studies are therefore strongly warranted.
Disclosure
K Winther has been a consultant to Hyben Vital on veterinar-
ian products. The authors report no other conflicts of interest
in this work.
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... Furthermore, Takahashi et al. demonstrated that dLGG scavenges free radicals in promyeloblasts [20]. Moreover, botanical extracts (e.g., Rosa canina) containing galactolipids (e.g., monogalactosyl diacylglycerol and digalactosyl monoacylglycerol) have been shown to delay skin aging and ameliorate skin conditions in in vitro and clinical studies [22][23][24][25][26][27][28]. ...
... While little is known regarding the mechanisms involved in the improvement of skin health, a few in vitro and clinical studies point towards the role of galactolipids in slowing down skin aging [22][23][24][25][26][27][28]. Rose (R. canina) hips, which contain abundant galactolipids (e.g., (2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-3-O-β-d-galactopyranosyl glycerol), inhibit the expression of proinflammatory cytokines (e.g., tumor necrosis factor α and interleukins 1β and 6) and proinflammatory enzymes (e.g., MMPs and cyclooxygenase-2) while simultaneously reducing oxidative stress in cells [22,23]. ...
... While little is known regarding the mechanisms involved in the improvement of skin health, a few in vitro and clinical studies point towards the role of galactolipids in slowing down skin aging [22][23][24][25][26][27][28]. Rose (R. canina) hips, which contain abundant galactolipids (e.g., (2S)-1,2-di-O-[(9Z,12Z,15Z)-octadeca-9-12-15-trienoyl]-3-O-β-d-galactopyranosyl glycerol), inhibit the expression of proinflammatory cytokines (e.g., tumor necrosis factor α and interleukins 1β and 6) and proinflammatory enzymes (e.g., MMPs and cyclooxygenase-2) while simultaneously reducing oxidative stress in cells [22,23]. The galactolipids isolated from Impatiens parviflora DC exhibit anti-hyaluronidase activity [24], while M. integrifolia leaf extract, which is rich in monogalactosyl diacylglycerol 36:4 and digalactosyl monoacylglycerol 18:2, exerts a strong tyrosinase inhibitory activity [25]. ...
Full-text available
Article
Crassocephalum rabens (Asteraceae) is a common herb used in Taiwanese folk medicine to treat inflammation-related syndromes. Pharmacological studies have revealed that galactolipids exhibit anti-oxidative, anti-inflammatory, and anti-hyaluronidase activities and improve skin wrinkles, moisture, and elasticity in healthy subjects. However, the anti-aging effects of C. rabens and its primary active compound, 1,2-di-O-linolenoyl-3-O-β-galactopyranosyl-sn-glycerol (dLGG), remain elusive. Here, we investigated whether C. rabens can improve skin conditions in healthy individuals using a double-blind approach. Forty enrolled volunteers were randomly and equally assigned to the control or treatment group and were required to take either a placebo or a C. rabens extract capsule daily for one month. Skin parameters were measured before and after the study. The results showed significant differences in skin elasticity, wrinkles, collagen content, brightness, and hydration between the baseline and week 4 in the treatment group. Particularly, compared with those in the placebo group, skin wrinkles (p < 0.05), brightness (p < 0.001), collagen content (p < 0.01), and UV spots (p < 0.05) were notably improved after treatment with the C. rabens extract. Our study successfully demonstrated the application of C. rabens in preventing skin aging. Further investigations will be conducted to study the underlying anti-aging mechanism of dLGG.
... It has traditionally been used as a vitamin supplement or for health food products in many European countries. It is a rich source of vitamin C, minerals (Mg, Fe, Mn, Al), and phytochemicals [36][37][38]. ...
... These phytochemicals, mainly composed of polyphenols, flavonoids, and β-carotenes, are responsible for the antioxidant and anti-inflammatory activities of Rosehip extracts, J o u r n a l P r e -p r o o f both in vitro and in vivo [36][37][38], and known to have also antibacterial properties [38,39]. Due to this profile, functionalization of NPs with RH extracts are expected to yield more biocompatible and bioactive particles, expanding the range of applications. ...
... The suggested antioxidant activity of the RH-functionalized NPs might be an added value due to their potential in contributing to the cell and tissue redox balance to prevent oxidative stress, which plays a role in cell damage and the development of several pathologies. Accordingly, RH extracts have demonstrated protective effects in disorders associated with a disruption in the redox balance, such as arthritis, rheumatoid, osteoporosis, diabetes, hepatotoxicity, and neurodegenerative conditions [37,77]. Results presented in this section showed that Mg(OH) 2 NPs caused low toxicity to human cells, i.e., harmful effects were only observed at levels in the range of 1000 m/mL, namely ~30% inhibition in cell viability. ...
Article
The development of nanoparticles as antimicrobial agents against pathogenic bacteria has emerged as one of the leading global healthcare challenges. In this study, Mg(OH) 2 NPs with controlled morphology and nanometric size, using two distinct counterions, chloride or nitrate, have been synthesized using Rosehip (RH) extract that has privileges beyond conventional chemical and physical methods. Various physicochemical techniques were used to characterize the RH-functionalized Mg-based NPs. They exhibited a spherical shape with a diameter of ~10 nm, low crystallinity compared to non-functionalized NPs, high polyphenol content, and negative zeta potential in three different media (H 2 O, TSB, and cell medium). The resulting RH-functionalized Mg-based NPs also exhibited an increased antibacterial activity against Gram-positive (S. Epidermis and S. aureus) and Gram-negative (E. Coli) bacteria compared to those prepared in pure water (0% RH), an effect that was well evident with low NPs contents (250 g/mL). A preliminary attempt to elucidate their mechanism of action revealed that RH-functionalized Mg-based NPs could disrupt cellular structures (bacterial cell wall and cytoplasmic membrane) and damage the bacterial cell, as confirmed by TEM imaging. Noteworthy is that Mg-based NPs exhibited higher toxicity to bacteria than to eukaryotic cells. More significantly, was their enhanced in vivo efficacy in a Galleria mellonella invertebrate animal model, when infected with S. aureus bacteria. Overall, our findings indicate that well-engineered Rosehip magnesium-based nanoparticles can be used as a green non-cytotoxic polyphenolic source in different antibacterial applications for the biomedical industry.
... Finally, the use of flower petals to make healing compresses for the eyes should be noted. All these effects reflect the identification of numerous bioactive compounds, including vitamin C, flavonoids, tocopherols, carotenoids, organic acids, sugars and essential fatty acids [56,57]. Rosehip, made up of the receptacle and the remains of the dried sepals of rosehip, should have a minimum vitamin C content of 0.3% (dried drug) according to the European Pharmacopoeia [34]. ...
Full-text available
Article
Data on urban and rural diabetes prevalence ratios show a significantly lower presence of diabetes in rural areas. Several bioactive compounds of plant origin are known to exert anti-diabetic properties. Interestingly, most of them naturally occur in different plants present in mountainous areas and are linked to traditions of herbal use. This review will aim to evaluate the last 10 years of evidence-based data on the potential anti-diabetic properties of 9 plants used in the Piedmont Alps (North-Western Italy) and identified through an ethnobotanical approach, based on the Occitan language minority of the Cuneo province (Sambucus nigra L., Achillea millefolium L., Cornus mas L., Vaccinium myrtillus L., Fragaria vesca L., Rosa canina L., Rubus idaeus L., Rubus fruticosus/ulmifolius L., Urtica dioica L.), where there is a long history of herbal remedies. The mechanism underlying the anti-hyperglycemic effects and the clinical evidence available are discussed. Overall, this review points to the possible use of these plants as preventive or add-on therapy in treating diabetes. However, studies of a single variety grown in the geographical area, with strict standardization and titration of all the active ingredients, are warranted before applying the WHO strategy 2014–2023.
... These compounds provide anti-inflammatory, antidiabetic, antiproliferative and antimicrobial activity (Ali Asgar, 2013;Fan et al., 2014;Ghazghazi et al., 2010, Ali;Wenzig et al., 2008). In addition, rose hips contain minerals (calcium, phosphorus and potassium) (Ercisli, 2007), pectins, amino acids and essential oils (Nowak, 2005;Winther et al., 2016). The fruits of the most used Rosa species were often studied, but there is limited knowledge about the chemical composition and applicative features of Rosa leaves, which are often discarded as waste (Živković et al., 2015). ...
Article
In this study, the chemical composition, antioxidant, and hypoglycemic activity of Rosa arvensis Huds. leaves and fruits collected from Zlatibor, Stara Planina, Stolovi mountains and Pešter plateau (Serbia) were analysed. Phenolic and vitamin profiles, as well as in vitro antioxidant potential and enzyme inhibitory activity on α-amylase and α-glucosidase, were studied. Phytochemical analysis showed higher phenolic content in leaf extracts than in those obtained from fruits. Gallic, chlorogenic and syringic acids were the most abundant phenolic acids, while catechin was the major flavonoid compound. Furthermore, the highest level of α-tocopherol (1.94 mg/100 g fw) in achenes and ascorbic acid (9.60 mg/100 g fw) in hypanthium were quantified in the fruits sampled on the Veliki Krš Mt. High antioxidant capacity was observed for the leaf extracts. It was highly correlated with their chemical composition and primarily referred to the catechin content (r > 0.95, p < 0.01), while the quinic acid had the opposite effect (r > −0.97, p < 0.01). Leaf extracts also showed good α-glucosidase and moderate α-amylase inhibitory potential in contrast to hypanthium and achenes extracts with lower antidiabetic activity. The high phenolic content and noted antioxidative potential were strongly correlated with the α-glucosidase inhibitory activity (r > 0.80, p < 0.01), while the α-amylase inhibition was only moderately correlated with those compounds (r > 0.49, p < 0.01). Among the tested R. arvensis samples, those from Zlatibor Mt. contained the highest amount of target compounds and expressed the highest biological activity. The obtained results suggest that R. arvensis extracts present a new source of bioactive compounds that could be implemented as novel food ingredients.
... For many years, rosehips have been used in traditional and folk medicine for their anti-inflammatory and pain-relieving, properties [1,2]. Nowadays rosehip fruit is used as an ingredient in foods (e.g., jam, jellies, teas, syrup), in the manufacture of supplements, vitamins and in cosmetics (e.g., lotion, cream, shower gel) [3]. ...
Full-text available
Article
Studies on the mineral content of different rosehip species/cultivars during the ripening period are very limited. Therefore, the objective of this research was to evaluate the content and composition of the mineral elements of two species and two rosehip cultivars growing on an organic farm. The rosehip fruits were harvested at different ripening stages, five time per season. Mineral composition (K, Ca, Mg, P, Fe, Na, Ti, Cu, B, Mn, Al, Zn, Cr, Co, Ni, As, Mo, Cd and Pb) was analyzed by means inductively coupled plasma mass spectrometry (ICP–MS). The results showed that the ripening stage and species/cultivars had an effect on the contents of the mineral elements. Significantly, the highest content of mineral elements was determined at ripening stage I (Ca, Mg, Ti, Mn, Al and Cr) and IV (K, P, Fe, Cu and B). Species of the Rosa canina accumulated the highest content of mineral elements. Correlation analysis showed that the hue angle had a positive and very strong relationship with six mineral elements: K (r = 0.909), Ca (r = 0.962), Mg (r = 0.965), P (r = 0.945), Fe (r = 0.929) and Ti (r = 0.944).
... The plant was described for the first time by Pliny the Elder (23-79 BC), who attributed the plant's name to a belief that the root could cure the bite of a mad dog (Hass 1995). The plant had also been known by sailors as a means of protection against scurvy, due to its high concentration of vitamin C (up to 1500 mg/100 g), and thus it spread to several continents (Winther et al. 2016). Today, these deciduous flowering shrubs are widely grown in gardens for their flowers and fruits (Ercisli 2005). ...
Chapter
Wild fruits are underutilized plants that are well adapted to the local climatic conditions. Extreme environmental conditions due to climate change or variability are a threat to wild-growing species, crop production, productivity, and livelihood. Wild fruit fields could be affected by not meeting winter chilling requirements, which is specific for every fruit species. On the other hand, the plants’ secondary metabolites and other bioactive compounds can be attributed to the changing conditions as a response to various types of environmental stresses which affect their production. Secondary metabolites refer to small molecules that are non-essential for the growth and reproduction of plants, but have a wide range of effects on the plant itself and other living organisms. Blackthorn (Prunus spinosa L.), Cornelian cherry (Cornus mas L.), dog rose (Rosa canina L.), and hawthorn (Crataegus monogyna Jacq.) are important wild plants with powerful health-promoting properties. Due to their chemical composition and nutritive value, they have a strong effect on regional food security and poverty alleviation. Positive health effects, forceful impact on the quality of life, and market potential are additional attributes of these plants, which may have significant economic impact.
... Neuroprotective properties of rosehip extracts (Rosa cinnamonea L.) have been noted. Experimental studies have shown that a herbal preparation of rose hips, tansy herb, and nettle prevents memory impairment in Alzheimer's disease [124]. Valeriana officinalis L. extract improves cognitive functions caused by exposure to amyloid β in models of Alzheimer's disease [125]. ...
Full-text available
Article
Maintaining quality of life with an increase in life expectancy is considered one of the global problems of our time. This review explores the possibility of using natural plant compounds with antioxidant, anti-inflammatory, anti-glycation, and anti-neurodegenerative properties to slow down the onset of age-related changes. Age-related changes such as a decrease in mental abilities, the development of inflammatory processes, and increased risk of developing type 2 diabetes have a significant impact on maintaining quality of life. Herbal preparations can play an essential role in preventing and treating neurodegenerative diseases that accompany age-related changes, including Alzheimer’s and Parkinson’s diseases. Medicinal plants have known sedative, muscle relaxant, neuroprotective, nootropic, and antiparkinsonian properties. The secondary metabolites, mainly polyphenolic compounds, are valuable substances for the development of new anti-inflammatory and hypoglycemic agents. Understanding how mixtures of plants and their biologically active substances work together to achieve a specific biological effect can help develop targeted drugs to prevent diseases associated with aging and age-related changes. Understanding the mechanisms of the biological activity of plant complexes and mixtures determines the prospects for using metabolomic and biochemical methods to prolong active longevity.
Chapter
The plant species belonging the genus Rosa (Rosaceae) are the perennial shrubs mostly distributed in Europe, North Africa, Tunisia, Algeria, Morocoo, West Asia. The fruits are called rose hips and are the pseudo fruits which are oval in shape. These fruits are rich in bioactive compounds including vitamin C, carotenoids, tocopherol, phenolic acid, bioflavonoids, tannin, pectin, organic acids, amino acid, essential oil and unsaturated fatty acids which have great importance in human health. The fruits extracts exhibit different pharmacological activities like antioxidant, anti-diabetic, anti-hyperlipidaemic, anti-inflammatory, antiarthritic, gastroprotective and anti-cancer. The oil can be commercially produced from the rose hip especially from R. canina and R. rubiginosa which has the greater values in food and cosmetics industries. Various cosmeceuticals and herbal formulations are also available which contain rose hip oil or standardised rose hip powder. This chapter focuses on the scientific progress on the fruits of Rosa spp. related to nutritional and phytochemical composition and its potential in the nutraceutical market.
Chapter
From ancient times, rose hip has been used as food source and as part of herbal remedies. Modern research has confirmed that rose hip, especially when containing seeds and shells, reduces pain and improves daily activity in animal models and in patients with osteoarthritis. The effect size on pain is comparable to that observed with nonsteroidal anti-inflammatory agents and superior to that obtained with paracetamol. For example, treatment with a subspecies of Rosa canina (Lito) resulted in 50% reduction in intake of pain killers. There are also strong indications that conditions such as rheumatoid arthritis, aging skin, and wrinkles benefit from treatment with rose hip. Cardiovascular diseases, especially where hyperlipidemia plays a major role, can be treated with rose hip, since a modest reduction of blood cholesterol levels as well as kidney and liver protection has been reported with the treatment. Variation in efficacy and amount of active ingredients in the different species, as well as with different ways of production, should be recognized. Rose hip can be collected from nature. It takes 5–7 Rosa canina berries to produce the daily dose of 5 gram of mixed shell-seed powder.
Article
Rosa roxburghii Tratt (Chestnut rose) is native to China where it is cultivated for its strongly aromatic hips (pseudo fruits); locally known as cili. Increasing interest in cili for food and beverage products prompted an evaluation of its aroma compounds and the influence of geographic source. Accordingly, the volatile compounds in cili from five locations in Guizhou province were analysed by headspace‐solid‐phase microextraction coupled with gas chromatography‐mass spectrometry. Sixty‐seven volatile compounds were identified. Principal component analysis distinguished three sample groups by geographic source. The aroma of cili juice from each location was characterized by quantitative descriptive analysis using six odour descriptors. Cili aroma was predominantly sweet/fruity, floral and green, but geographic source significantly influenced the intensity of the sweet/fruity and floral notes. Odour activity analyses indicated that 40 volatile compounds contribute appreciably to the aroma of cili. Of those compounds, only ten esters, two aldehydes, one alcohol and one aromatic compound were common to all regional samples. Those findings extend the range of volatiles detected in cili. These results identify those that are present in odour active amounts and provide the first evidence of the impact of geographic source on the aroma and flavour of cili. Chestnut rose (Rosa roxburghii) hips (cili) have 67 identified volatile compounds Cili from five Chinese geographic regions can be typified by volatile compounds. Over 40 volatile compounds contribute substantially to the aroma of cili. Sweet/fruity and floral cili rosehip aromas differ between regional samples. A benchmark for future elucidation and regional discrimination of cili quality.
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Obesity has become a great problem all over the world. We repeatedly screened to find an effective food to treat obesity and discovered that rosehip extract shows potent anti-obesity effects. Investigations in mice have demonstrated that rosehip extract inhibits body weight gain and decreases visceral fat. Thus, the present study examined the effect of rosehip extract on human body fat in preobese subjects. We conducted a 12-week, single-center, double-blind, randomized, placebo-controlled study of 32 subjects who had a body mass index of ≥25 but <30. The subjects were assigned to two random groups, and they received one tablet of placebo or rosehip that contained 100 mg of rosehip extract once each day for 12 weeks with no dietary intervention. Abdominal fat area and body fat percent were measured as primary outcomes. The other outcomes were body weight and body mass index. Abdominal total fat area, abdominal visceral fat area, body weight, and body mass index decreased significantly in the rosehip group at week 12 compared with their baseline levels (P<0.01) after receiving the rosehip tablet intake, and the decreases in these parameters were significantly higher when compared with those in the placebo group. Additionally, body fat percent tended to decrease compared with the placebo group and their baseline level. Moreover, the abdominal subcutaneous fat area was significantly lower in the rosehip group than in the placebo group at week 12 after the initiation of intake (P<0.05). In addition, there were no abnormalities, subjective symptoms, and findings that may indicate clinical problems during the study period. These results suggest that rosehip extract may be a good candidate food material for preventing obesity.
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Rose hip powder (RHP) alleviates osteoarthritis (OA) due to its anti-inflammatory and cartilage-protective properties. Substances contained in RHP might contribute to its clinical efficacy. The activity of two RHP (i.e., RH-A, from the whole fruit, RH-B, from fruits without seeds) was investigated in human peripheral blood leukocytes (PBL) and primary chondrocytes (NHAC-kn). RH-A and RH-B diminished the secretion of chemokines and cytokines in LPS/IFN- γ -activated PBL, including CCL5/RANTES, CXCL10/IP-10, interleukin- (IL-) 6, and IL-12. Most effects were transcriptional, since gene expression levels were significantly influenced by RH-A and RH-B. In IL-1 β treated normal chondrocytes (NHAC-kn), both RH preparations reduced the expression of matrix metalloproteinase- (MMP-) 1, MMP-3, and MMP-13 and ADAMTS-4. These changes are associated with diminished inflammatory damage or cartilage erosion. Principal component analysis revealed that (1) RH-A and RH-B modified a large pattern of biomarkers, and (2) RH-B outperformed RH-A. Furthermore, RH-B contained more chondroprotective and anti-inflammatory constituents than RH-A. Thus, RHP contributed to restore cellular homeostasis in PBL and chondrocytes. RH preparations from fruits without seeds are thus expected to have an improved OA-preventive or OA-therapeutic profile, as subsequently shown in a related clinical trial.
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The inhibitory effects of rose hip (Rosa canina L.) water extracts from two different manufactures on osteoarthritis was comparatively investigated in primary cultures of rat cartilage cells. To identify the effects of rose hip extracts against (300 , 2 hr) treatment, cell survival was measured by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell survival increased by rose hip extracts in the range of 100 to 600 of treatment. To determine the anti-inflammatory effects of rose hip extracts, tumor necrosis factor alpha (TNF-), nitric oxide (NO), and Cox-2 expression were measured after lipopolysaccharide (LPS) activation. TNF- level with rose hip extract treatment was decreased by 27.4% and 31.9% at 600 of treatment. Nitric oxide was inhibited by rose hip extract at 100~600 of treatment in a dose-dependent manner. In addition, Cox-2 protein expression was dose-dependently decreased while Cox-1 had no change in expression level. The severity of osteoarthritis is controlled by a balance between anabolic and catobolic factors in an articulation, therefore the expression of these factors plays a critical role in preventing osteoarthritis. In measuring anabolic factors, the genetic expression of collagen type I increased with rose hip treatment, while the genetic expression of collagen II did not change. In addition, the genetic expression of aggrecan (proteoglycan core protein) was significantly increased. while the genetic expression of matrix metalloproteinase (MMP) 3, 7 and 13, known catabolic factors, was significantly inhibited by treatment with rose hip extract. The expression of MMP13 was especially highly influenced. In conclusion, rose hip water extracts show inhibitory effects on cell death by mediated oxidative stress, which is related to inhibitory effects on inflammation due to TNF-, NO, and Cox-2. The ability of rose hip extracts to ameliorate inflammation in primary cultures of cartilage cells seems to associate with an increased genetic expression of specific anabolic factors, collagen type I and aggrecan, and a decreased expression of catabolic factors, MMPs (3, 7, and 13). However, there were no significant differences between rose hip extracts from the two manufacturers.
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The triterpenes are one of the most numerous and diverse groups of plant natural products. They are complex molecules that are, for the most part, beyond the reach of chemical synthesis. Simple triterpenes are components of surface waxes and specialized membranes and may potentially act as signaling molecules, whereas complex glycosylated triterpenes (saponins) provide protection against pathogens and pests. Simple and conjugated triterpenes have a wide range of applications in the food, health, and industrial biotechnology sectors. Here, we review recent developments in the field of triterpene biosynthesis, give an overview of the genes and enzymes that have been identified to date, and discuss strategies for discovering new triterpene biosynthetic pathways. Expected final online publication date for the Annual Review of Plant Biology Volume 65 is April 29, 2014. Please see http://www.annualreviews.org/catalog/pubdates.aspx for revised estimates.
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The lipid composition of chokeberry, black currant and rose hip seeds was investigated. The seeds contain 19.3 g kg⁻¹, 22.0 g kg⁻¹ and 8.2 g kg⁻¹ glyceride oil respectively. The content of phospholipids, mainly phosphatidylcholine, phosphatidylinositol and phosphatidylethanolamine, was 2.8 g kg⁻¹, 1.3 g kg⁻¹ and 1.4 g kg⁻¹, respectively. The total amounts of sterols were 1.2 g kg⁻¹, 1.4 g kg⁻¹ and 0.4 g kg⁻¹. The main component was β-sitosterol, followed by campesterol and Δ⁵ -avenasterol. In the tocopherol fraction (55.5 mg kg⁻¹ in chokeberry oil, 249.6 mg kg⁻¹ in black currant oil and 89.4 mg kg⁻¹ in rose hip oil), α-tocopherol predominated in chokeberry oil (70.6 mg kg⁻¹). γ-Tocopherol was the main component in black currant oil (55.4 mg kg⁻¹) and rose hip oil (71.0 mg kg⁻¹). The fatty acid composition of triacylglycerols, individual phospholipids and sterol esters was also identified. In the phospholipids and sterol esters, the more saturated fatty acids, mainly palmitic, stearic, and long chain fatty acids predominated.