Apigenina w regeneracji chrząstki stawowej

Apigenina (4’,5,7-trihydroxyflavone) występuje w wielu roślinach , należy do flawonoidów. Ma formę kryształków o żółtym kolorze.

Apigenina

Źródło apigeniny:

Rośliny mające w składzie najwyższe stężenie apigeniny to: Rdestowiec japoński(Polygonum japonicum), rumianek pospolity (Matricaria chamomilla L.),Przetacznik (Veronica) , Ciemiężyca(Veratrum grandiflorum) , Sosna Lamberta(Pinus Lambertiana) ,Kocanka(Helichrysum),Pietruszka zwyczajna (Petroselinum crispum) świeże ziele zawiera (302.00 mg/100 g ). Warto stosować ekstrakty z rumianku oraz tymianku bowiem wydają się być najlepszym źródłem apigeniny.

Pozostałe rośliny zawierające w swoim składzie apigenine:

Krwawnik pospolity L. – krwawnik pospolity

Apium graveolens L. – seler

Artemisia dracunculus L. – estragon

Camellia sinensis (L.) – herbata, liście

Nobile Chamaemelum (L.) – rumian rzymski

Coriandum sativum L. – kolendra

Digitalis purpurea L. – naparstnica

Echinacea spp. – jeżówka,liście

Gingko biloba L. – miłorząb , liście

Glycyrrhiza glabra L. – lukrecja , korzeń

Linum usitatissimum L. – len

Szanta zwyczajna L. – szanta zwyczajna

Matricaria recutita L. – rumianek

Mentha spicata L. – mięta, w liściach

Ocimum basilicum L. – bazylia

Origanum vulgare L. – oregano

Działanie farmakologiczne:

Apigenina jest silnym aktywatorem kanału jonowego TRPV4 który pobudza wzrost nowej chrząstki w stawach, naśladując efekt działania fizycznego ruchu który  również w umiarkowanym zakresie aktywuje jej wzrost. Kanał jonowy zwany TRPV4 jest potencjalnym celem dla nowych terapii do leczenia choroby zwyrodnieniowej stawów w tym regeneracji chrząstki [1,2]. Badania wykazały że zablokowanie kanału TRPV4 aktywuje zmiany zwyrodnieniowe w osteoartretyzmie [3].Apigenina również stymuluje neurogeneze i tworzenie nowych neronów (pamięć ,koncentracja)[4]. Apigenina ma działanie przeciwnowotworowe.

Wskazania: Choroby zwyrodnieniowe stawów, artretyzm , osteoartretyzm ,RZS, borelioza z Lyme z objawami stawowymi.

Farmakokinetyka:

Apigenine cechuje powolny metabolizm oraz powolna faza eliminacji z ustroju.
Maksymalne stężenie w organizmie apigenina osiąga od 1 do 4 godziny po podaniu doustnym . Okres półtrwania dla apigeniny to 12 godzin. Procent wydalonej dawki po spożyciu to 45,2 % (16,6 % w moczu , 28,6 % w kale ). Apigenina wchłania się z jelit o 50% słabiej u osób będących po kuracji antybiotykowej bądź z wyjałowioną florą bakteryjną.

Preparaty i dawkowanie:

Apigenina najskuteczniej rozpuszcza się w Dimetylosulfotleneku (CH3)2SO.

Intrakt z kwiatów rumianku na etanolu 50%-70% 1:3 . Dawkowanie 5-10 ml x 3/4 razy dziennie.

Ekstrakt z czystej apigeniny 100mg x 3 dziennie .

Świeże ziele pietruszki 3 razy dziennie po 20 gramów.

Synergizm:

Kozieradka (Trigonella foenum-graecum L.) oraz  resveratrol wzmacniają regeneracje chrząstki stawowej. Lukrecja oraz piperyna zwiększają przyswajalność apigeniny.

Źródła kupna apigeniny:

Swanson-ultra-apigenin-50-mg-90-caps    na stronie  www.swansonvitamins.com

Chamomile-20-1-Powder-500g  na www.ebay.pl

Nature’s Way Chamomile Standardized Digestive Soothing 60 Capsules 1.2% Apigenin na www.ebay.pl

apigenin

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Bibliografia


[1] 
Chemical Signaling Simulates Exercise in Cartilage Cells
Jan. 13, 2014 — Cartilage is notoriously difficult to repair or grow, but researchers at Duke Medicine have taken a step toward understanding how to regenerate the connective tissue. By adding a chemical to cartilage cells, the chemical signals spurred new cartilage growth, mimicking the
effects of physical activity.
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The findings, published online in the Proceedings of the National Academy of Sciences the week of Jan. 13, 2014, point to an ion channel called TRPV4 as a potential target for new therapies to treat osteoarthritis or even regrow cartilage. Articular cartilage is the tissue that lines joints such as hips, knees and shoulders, providing cushioning and smooth movement. Similar to bones and muscles, cartilage only stays healthy and
strong through loading, or applying force, through physical activity.
Abnormal forces on the joints can cause a variety of problems leading to pain and loss of mobility. Overloading joints through overuse or injury can lead to the cartilage breaking down, while lack of use can result in cartilage wasting through atrophy. Both kinds of cartilage
deterioration leave joints prone to osteoarthritis, a degenerative and debilitating disease. Until recently, researchers did not know how cartilage converts mechanical loading into the ion channel signals that promote growth. Understanding how cartilage senses mechanical loading could
equip researchers with the knowledge needed to prevent or better treat joint diseases. „Mechanical loading plays a critical role in the overall health of the cartilage,” said Farshid Guilak, Ph.D., Laszlo Ormandy Professor of Orthopaedic Surgery at Duke and the study’s senior
author. „If we can figure out how cartilage cells sense mechanical loads, we can trick them into thinking they are being exercised or stop them from responding to abnormal loading. Think of it as
artificial exercise for your cartilage.” In the study, led by MD/PhD student Christopher O’Conor, the researchers looked at articular cartilage cells from pigs and focused on TRPV4, an ion channel abundant in cartilage cells that can be turned on during mechanical loading. When the researchers „exercised” the cartilage cells using mechanical loading, the cells sensed the loading and grew cartilage tissue. When they added
a compound that blocked TRPV4, essentially turning off signals from the ion channel, the cartilage did not grow and the effects of the mechanical loading were lost.Next, the researchers substituted mechanical loading for a chemical that activated TRPV4. Without having to exercise the cartilage, they observed the growth of cartilage even more so than with the mechanical loading. The findings suggest that TRPV4 is responsible for sensing mechanical loading in the cartilage. Now that they know that turning on TRPV4 can simulate the effects of mechanical loading in cartilage cells, the researchers are looking at ways to harness this potential. „Our next step is to see if this synthetic ‚exercising’ technology works on human cells that could be used to regrow new human cartilage,” said O’Conor, who is completing his MD/PhD degree at the
University of North Carolina at Chapel Hill and is performing his dissertation work with Guilak in the Duke Orthopaedic Bioengineering Laboratories. Beyond growing new cartilage, the researchers will investigate whether the compounds that activate or block TRPV4 could act as new therapies to prevent cartilage degeneration and joint disease.

[2] 
Br J Pharmacol. 2012 May;166(1):349-58. doi: 10.1111/j.1476-5381.2011.01767.x.
Apigenin, a plant-derived flavone, activates transient receptor potential vanilloid 4 cation
channel.
Ma X, He D, Ru X, Chen Y, Cai Y, Bruce IC, Xia Q, Yao X, Jin J.
Author information
Abstract
BACKGROUND AND PURPOSE:
Transient receptor potential vanilloid 4 (TRPV4) is a Ca(2+) -permeable channel with multiple modes of activation. Apigenin is a plant-derived flavone, which has potential preventive effects on the development of cardiovascular disease. We set out to explore the effects of apigenin on
TRPV4 channel activity and its role in vasodilatation.
EXPERIMENTAL APPROACH:
The effects of apigenin (0.01-30 µM) on TPRV4 channels were investigated in HEK293 cells over- expressing TRPV4, rat primary cultured mesenteric artery endothelial cells (MAECs) and isolated small mesenteric arterial segments using whole-cell patch clamp, fluorescent Ca(2+) imaging,
intracellular recording and pressure myography.
KEY RESULTS:
Whole-cell patch clamp and fluorescent Ca(2+) imaging in HEK cells over-expressing TRPV4 showed that apigenin concentration-dependently stimulated the TRPV4-mediated cation current and Ca(2+) influx. In MAECs, apigenin stimulated Ca(2+) influx in a concentration-dependent manner. These
increases in cation current and Ca(2+) influx were markedly inhibited by TRPV4-specific blockers and siRNAs. Furthermore, pressure myography and intracellular recording in small third-order mesenteric arteries showed that apigenin dose-dependently evoked smooth muscle cell membrane
hyperpolarization and subsequent vascular dilatation, which were significantly inhibited by TRPV4 -specific blockers. TRPV4 blocker or charybdotoxin (200 nM) plus apamin (100 nM) diminished the
apigenin-induced dilatation.
CONCLUSION AND IMPLICATIONS:
This is the first study to demonstrate the selective stimulation of TRPV4 by apigenin. Apigenin was found to activate TRPV4 channels in a dose-dependent manner in HEK cells over-expressing TRPV4
and in native endothelial cells. In rat small mesenteric arteries, apigenin acts on TRPV4 in endothelial cells to induce EDHF-mediated vascular dilatation.

[3] 
Experimental Arthritis
You have full text access to this OnlineOpen article
Chondroprotective role of the osmotically sensitive ion channel transient receptor potential vanilloid 4: Age- and sex-dependent progression of osteoarthritis in Trpv4-deficient mice Andrea L. Clark1, Bartholomew J. Votta2,†, Sanjay Kumar2,†, Wolfgang Liedtke1, Farshid Guilak1,*
Article first published online: 25 JUN 2010

[4]  Expert Opin Ther Pat. 2009 Apr;19(4):523-7. doi: 10.1517/13543770902721279.
Apigenin and related compounds stimulate adult neurogenesis. Mars, Inc., the Salk Institute for Biological Studies: WO2008147483.
Taupin P.
Author information
Abstract
The application is in the field of adult neurogenesis and its therapeutic potential. It aims to characterize the activity of apigenin and related compounds on adult neurogenesis in vivo and in vitro. Apigenin and related compounds are derivatives used in food products. They were
administered intraperitoneally and orally in adult rodents and assessed for their activity in promoting the generation of neuronal cells and learning and memory performance. They were also tested on adult rat hippocampal-derived neural progenitor and stem cells to assess their neurogenic property. Apigenin and related compounds stimulate adult neurogenesis in vivo and in vitro, by promoting neuronal differentiation. Apigenin promotes learning and memory performance in the Morris water task. The application claims the use of apigenin and related compounds for stimulating adult neurogenesis and for the treatment of neurological diseases, disorders and injuries, by stimulating the generation of neuronal cells in the adult brain.

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