By Kyle J. Norton(Scholar)
Osteoporosis is condition of thinning of bone and bone tissues as a result of the loss of bone density over a long period of time.
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).
