Osteoarthritis (OA), a form of arthritis, is defined as a condition of
as a result of aging causes of wear and tear on a joint, affecting over 25 million people in the United States in alone.
Phytochemicals and osteoarthritis
1. Epigallocatechin, including catechins, is a phytochemical of
Flavan-3-ols, in the group of Flavonoids (polyphenols), found abundantly
in green tea, St John wort, black Tea, carob flour, Fuji apples, etc.
a. Inflammatory effects
In the determination of the up-regulated expressions of IL-8 or PGE(2)
in Streptococci or PAMP-stimulated HDPF were inhibited by catechins,
(-)-epicatechin gallate (ECG) and (-)-epigallocatechin gallate (EGCG).
In TLR2 ligand-stimulated HDPF, found that catechins might be useful
therapeutically as an anti-inflammatory modulator of dental pulpal
inflammation, according to “Tea catechins reduce inflammatory reactions
via mitogen-activated protein kinase pathways in toll-like receptor 2
ligand-stimulated dental pulp cells” by Hirao K, Yumoto H, Nakanishi T,
Mukai K, Takahashi K, Takegawa D, Matsuo T.(47)
b. Antiviral activities
In the observation of Catechin derivatives including (-)-epicatechin
gallate (ECG), (-)-epigallocatechin gallate (EGCG), (-)-epigallocatechin
(EGC) and green tea extract (GTE) and theirs inhibition of the
activities of cloned human immunodeficiency virus type 1 reverse
transcriptase (HIV-1 RT), duck hepatitis B virus replication complexes
reverse transcriptase (DHBV RCs RT), herpes simplex virus 1 DNA
polymerase (HSV-1 DNAP) and cow thymus DNA polymerase alpha (CT DNAP
alpha, found that GCG exerts a mixed inhibition with respect to external
template inducer poly (rA).oligo (dT) 12-18 and a noncompetitive
inhibition with respect to substrate dTTP for HIV-1 RT. Bovine serum
albumin significantly reduced the inhibitory effects of catechin
analogues and GTE on HIV-1 RT. In tissue culture GTE inhibited the
cytopathic effect of coxsackie B3 virus, but did not inhibit the
cytopathic effects of HSV-1, HSV-2, influenza A or influenza B viruses,
according to “[The inhibitory effects of catechin derivatives on the
activities of human immunodeficiency virus reverse transcriptase and DNA
polymerases].[Article in Chinese]” by Tao P.(48)
c. Antioxidants
In the evaluation of the effects of the main polyphenolic components
extracted from green tea leaves, i.e. (-)-epicatechin (EC),
(-)-epigallocatechin (EGC), (-)-epicatechin gallate (ECG),
(-)-epigallocatechin gallate (EGCG) and gallic acid (GA), against free
radical initiated peroxidation of human low density lipoprotein (LDL),
found that The antioxidative action of the green tea polyphenols
includes trapping the initiating and/or propagating peroxyl radicals
with the activity sequence EC>EGCG>ECG>EGC>GA for the AAPH
initiated peroxidation, and reducing the alpha-tocopheroxyl radical to
regenerate alpha-tocopherol with the activity sequence of
ECG>EC>EGCG>EGC>GA and ECG>EGCG>GA>EC>EGC for
the AAPH-initiated and BP-photosensitized peroxidations respectively,
according to “Antioxidative effects of green tea polyphenols on free
radical initiated and photosensitized peroxidation of human low density
lipoprotein” by Liu Z, Ma LP, Zhou B, Yang L, Liu ZL.(49)
2. Catechin is phytochemical of Flavan-3-ols, in the group of
Flavonoids (polyphenols), found abundantly in white tea, green tea,
black tea, grapes, wine, apple juice, cocoa, lentils, etc.
a. Body-weight regulation
Green tea has been proposed as a tool for obesity management as
strategies for weight loss and weight maintenance, as researchers found
that a green tea-caffeine mixture improves weight maintenance, through
thermogenesis, fat oxidation, and sparing fat free mass. The sympathetic
nervous system is involved in the regulation of lipolysis, and the
sympathetic innervation of white adipose tissue may play an important
role in the regulation of total body fat in general, according to “Green
tea catechins, caffeine and body-weight regulation”
byWesterterp-Plantenga MS.(50)
b. Antioxidant activity
In the research on polyphenolic compounds (included catechins) in the
berries of edible honeysuckle and their biological effects, including
recommended utilization, are reviewed found that These berries seem to
be prospective sources of health-supporting phytochemicals that exhibit
beneficial anti-adherence and chemo-protective activities, thus they may
provide protection against a number of chronic conditions, e.g.,
cancer, diabetes mellitus, tumour growth or cardiovascular and
neurodegenerative diseases, according to “Phenolic profile of edible
honeysuckle berries (genus lonicera) and their biological effects” by
Jurikova T, Rop O, Mlcek J, Sochor J, Balla S, Szekeres L, Hegedusova A,
Hubalek J, Adam V, Kizek R.(51)
c. Anti-inflammatory effect
In the preparation of the gel of Chinese medicine catechu, and to
observe the release mechanism in vitro and anti-inflammatory activity in
rats, found that the optimum condition of extraction from catechu was
as follows, the concentration of ethanol, ratio of raw material to
solvent, ultrasonic time, and extraction temperature were 50% , 1: 12,
35 min and 60 degrees C, respectively. The formulation of catechu gel
was carbomer-9 400.5 g, glycerol 5.0 g, the extracts of catechu 50.0 mL,
and triethanomine 0.5 mL The gel was semitransparent and stable. The
drugs released quickly. The catechu gel reduced the paw edema
considerably in dose-dependent manner compared to carrageenan-induced
rat, according to “[Preparation and pharmacodynamics studies on
anti-inflammatory effect of catechu gel].[Article in Chinese]” by Zheng
X, Zheng C.(52)
3. Theaflavin-3,3′-digallate, a theaflavin
derivative, is phytochemicals of Flavan-3-ols, in the group of
Flavonoids (polyphenols) found abundantly in black tea.
a. Antioxidant capacities
In the comparison of TF derivatives (theaflavin (TF(1)),
theaflavin-3-gallate (TF(2)A), theaflavin-3′-gallate (TF(2)B), and
theaflavin-3,3′-digallate (TF(3))) in scavenging reactive oxygen species
(ROS) in vitro, indicated that positive antioxidant capacities of
TF(2)B on singlet oxygen, hydrogen peroxide, hydroxyl radical, and the
hydroxyl radical-induced DNA damage in vitro were found, according to
“Evaluation of the antioxidant effects of four main theaflavin
derivatives through chemiluminescence and DNA damage analyses” by Wu YY,
Li W, Xu Y, Jin EH, Tu YY.(53)
b. Antimicrobial activities
In the evaluation of the antimicrobial activities of seven green tea
catechins and four black tea theaflavins, found that
(-)-gallocatechin-3-gallate, (-)-epigallocatechin-3-gallate,
(-)-catechin-3-gallate, (-)-epicatechin-3-gallate, theaflavin-3,
3′-digallate, theaflavin-3′-gallate, and theaflavin-3-gallate showed
antimicrobial activities at nanomolar levels; (ii) most compounds were
more active than were medicinal antibiotics, such as tetracycline or
vancomycin, at comparable concentrations; (iii) the bactericidal
activities of the teas could be accounted for by the levels of catechins
and theaflavins as determined by high-pressure liquid chromatography;
(iv) freshly prepared tea infusions were more active than day-old teas;
and (v) tea catechins without gallate side chains, gallic acid and the
alkaloids caffeine and theobromine also present in teas, and herbal
(chamomile and peppermint) teas that contain no flavonoids are all
inactive, according to “Antimicrobial activities of tea catechins and
theaflavins and tea extracts against Bacillus cereus” byFriedman M,
Henika PR, Levin CE, Mandrell RE, Kozukue N.(54)
c. anti inflammation
found that a single topical application of equimolar of black tea
constituents (TF, theaflavin-3-gallate, theaflavin-3′-gallate, and
theaflavin-3,3′-digallate) strongly inhibited TPA-induced edema of mouse
ears. Application of TFs mixture to mouse ears 20 min prior to each TPA
application once a day for 4 days inhibited TPA-induced persistent
inflammation, as well as TPA-induced increase in IL-1beta and IL-6
protein levels. TFs also inhibited arachidonic acid (AA) metabolism via
both cyclooxygenase (COX) and lipoxygenase pathways, according to
“Inhibitory effects of black tea theaflavin derivatives on
12-O-tetradecanoylphorbol-13-acetate-induced inflammation and
arachidonic acid metabolism in mouse ears” byHuang MT, Liu Y, Ramji D,
Lo CY, Ghai G, Dushenkov S, Ho CT.(55)
4. Myricetin is a flavonol, belong to the flavonoid
in Flavonoids (polyphenols), found in many grapes, berries, fruits,
vegetables, herbs, as well as other plants. It has been used as
antioxidant to lower cholesterol, treat certain types of cancer, etc.
a. Antioxidant and cytotoxic activity
In the evaluation of extracted from plants containing phenolic compound,
including flavonoid-galloyl glycoside [myricetin
3-O-(2',3'4'-tri-O-galloyl)-α-l-rhamnopyranoside] and theirs antioxidant
and cytotoxic effect found that the methanol extract exhibited high
antioxidant activity (SC(50) = 3.94 µg/ml), which is correlated with its
phenolic content. The extract also showed cytotoxic activity against
Hep G2 (IC(50) value 1.41 µg/ml) confirming its anticancer activity
against hepatocellular carcinoma, according to the study of “Antioxidant
and cytotoxic activity of polyphenolic compounds isolated from the
leaves of Leucenia leucocephala” by Haggag EG, Kamal AM, Abdelhady MI,
El-Sayed MM, El-Wakil EA, Abd-El-Hamed SS.(56)
b. Antitumour and anti-inflammatory activities
In the observation of of flavonoids isolated from Byrsonima crass and
its effect on mammary tumour cells LM2, found that almost all the
samples showed inhibitory activity to the release of NO but not of
TNF-alpha. Of all substances tested, flavonoids 2 (quercetin) and 6
(myricetin) may show promising activity in the treatment of murine
breast cancer by immunomodulatory and antiproliferative activities,
according to “Isolated flavonoids against mammary tumour cells LM2″ by
Carli CB, de Matos DC, Lopes FC, Maia DC, Dias MB, Sannomiya M,
Rodrigues CM, Andreo MA, Vilegas W, Colombo LL, Carlos IZ.(57)
5. Cyanidin is an anthocyanins (flavonals), in the group of
Flavonoids (polyphenols), found abundantly in red apple and pear,
bilberry, blackberry, blueberry, cherry, cranberry, peach, plum,
hawthorn, etc.
a. Antioxidants
In the verification of the chemical properties included composition of
anthocyanins and other polyphenols, antioxidant activity and profiles of
antioxidants by HPLC post-column derivatization or TLC of Polish
cultivars of blue-berried honeysuckles (Lonicera caerulea L.), wild and
bog bilberr, found that The antioxidant activity of different
blue-berried honeysuckle cultivars was similar to that of wild growing
bilberries (range from 170 to 417 μmol TE/g dm in ABTS and from 93-166
μmol TE/g dm in DPPH and Folin-Ciocalteu tests). The major anthocyanin
in the blue-berried honeysuckle was cyanidin-3-glucoside that
constituted 84-92% of the total anthocyanins. The TLC and HPLC
post-column antioxidant profiles indicated that anthocyanins are the
major antioxidants in all berries studied, according to “Phenolic
Composition and Antioxidant Properties of Polish Blue-Berried
Honeysuckle Genotypes by HPLC-DAD-MS, HPLC Post-Column Derivatization
with ABTS or FC, and TLC with DPPH Visualization” by Kusznierewicz B,
Piekarska A, Mrugalska B, Konieczka P, Namiesnik J, Bartoszek A (58)
b. Anti-inflammatory Effects
In the investigation of the cartilage-protecting and anti-inflammatory
effects of a polyphenolic-enriched red raspberry extract (RRE;
standardized to total polyphenol, anthocyanin, and ellagitannin
contents), found that On treatment with RRE (50 μg/mL), there was a
decrease in the rate of degradation of both proteoglycan and type II
collagen. In the in vivo antigen-induced arthritis rat model, animals
were gavaged daily with RRE (at doses of 30 and 120 mg/kg, respectively)
for 30 days after adjuvant injection (750 μg of Mycobacterium
tuberculosis suspension in squalene). At the higher dose, animals
treated with RRE had a lower incidence and severity of arthritis
compared to control animals, according to “Anti-inflammatory Effects of
Polyphenolic-Enriched Red Raspberry Extract in an Antigen-Induced
Arthritis Rat Model” by Jean-Gilles D, Li L, Ma H, Yuan T, Chichester
CO, Seeram NP.(59)
c. Obesity
In the demonstration of Cyanidin-3-O-β-glucoside (Cy-3-g)-rich foods
have been reported to inhibit the onset of obesity, found that Cy-3-g
improves obesity and triglyceride metabolism in KK-Ay mice. The
underlying mechanism is found to be partly related to the activation of
LPL in plasma and skeletal muscle, and inhibition of LPL in adipose
tissue following the activation of pAMPK, according to
“Cyanidin-3-O-β-glucoside improves obesity and triglyceride metabolism
in KK-Ay mice by regulating lipoprotein lipase activity” by Wei X, Wang
D, Yang Y, Xia M, Li D, Li G, Zhu Y, Xiao Y, Ling W.(60)
6. Etc.
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Sources
(47) http://www.ncbi.nlm.nih.gov/pubmed/20176036
(48) http://www.ncbi.nlm.nih.gov/pubmed/1284389
(49) http://www.ncbi.nlm.nih.gov/pubmed/10878235
(50) http://www.ncbi.nlm.nih.gov/pubmed/20156466
(51) http://www.ncbi.nlm.nih.gov/pubmed/22269864
(52) http://www.ncbi.nlm.nih.gov/pubmed/22256752
(53) http://www.ncbi.nlm.nih.gov/pubmed/21887850
(54) http://www.ncbi.nlm.nih.gov/pubmed/16496576
(55) http://www.ncbi.nlm.nih.gov/pubmed/16404705
(56) http://www.ncbi.nlm.nih.gov/pubmed/21595573
(57) http://www.ncbi.nlm.nih.gov/pubmed/19323263
(58) http://www.ncbi.nlm.nih.gov/pubmed/22264130
(59) http://www.ncbi.nlm.nih.gov/pubmed/22111586
(60) http://www.ncbi.nlm.nih.gov/pubmed/21360538
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