Plant of great size with terminal solitary chapters of tubulosas flowers color purple surrounded by I involve of thorny external brácteas. The thistle Maria has leaves lampiñas, dentated-thorny, of winding and waved limb, with nerviaciones of marmóreo white color.
Origin
This biennial species grows in uncultivated, dry and rocky lands of southern Europe, northern Africa and western Asia. Also it is possible to be found in South America (Argentina), from where a part of the used drug comes.
Chemical composition
The fruits, rich in oil (20 to 30%) with a high 498 fatty acid content insaturados [ ], contain in addition, proteins, sugars and poliínos. Very particular the active compounds are cromanonas: the flavanolignanos whose set takes the silimarina name.
The main flavanolignanos come from the cicloadición of a fenilpropánico alcohol to a 2-fenil cromanona (i.e. 2,3-dihidro flavonol, the taxofolina). The result is a benzodioxano or a oxatriciclodeceno; the rest has a dihidrobenzofuránica structure [ 499 ].
• Benzodioxanos: silibina (one is a diasteroisomérica mixture),
In the variety of white flowers, are lacking derivatives of hidroxilo in 3: silandrina (= 3-desoxiisosilibina), silimonina (= 3-desoxisilidianina), silihermina (3-desoxi-silicristina) and 500 neosiliherminas [ ]. Other varieties have an absolutely similar composition [ 501 ], considering the existence of 502 quimiotipos [ ].
Farmacológicos data
The numerous published works [ 503-287 ] have corroborated their reputation in the field of the hepáticas affections.
The hepatoprotectora activity of the silimarina has been demonstrated in hepáticas animal injuries of experimentation in isolated organ and, more recently, in cultures of 505 hepatocitos [ ].
The antagoniza silimarina the toxic effect of the CCl4 (tetracloruro of carbon) on parénquima hepático, so that it prevents the extension with the time of dream caused by hexobarbital. Also, one is against to the poisoning by galactosamina, tioacetamida, N-acetil-p-aminofenol [ 509b ], praseodina...
The silimarina administered to the mouse (i.v., 15 mg/kg), one hour before a faloidina injection (i.p., 3 mg/kg), protects to the animals in a 100%. Injected after the toxic, it reduces mortality sensibly, but the protection becomes weaker according to is extended the moment of the administration.
The activity seems to be bound to a membrane stabilization [ 50ã ] thus, thinks that in case of poisoning with faloidina, an interaction with the places implied in the pick up of the toxic could take place [ 506b ]. Also it can be because a great structural analogy between the silibina and the antamanida one exists, antagonistic natural of the amanitina [ 499, 507 ]. The silimarina is antirust with a high antiperoxidante power [ 508, 509a, b ] with hepático tropismo whose action could be against to the destruction of membrane lipids of the hepatocitos.
Observations in the Man
It is difficult to appreciate the effectiveness of the drug in the field of the hepáticas pathologies: this explains without a doubt the great number of tests made with the silimarina, as much in ambulatory patients as in hospitable. The criteria of evaluation of the effectiveness are multiple: hepático volume, weight, evolution of the ictericia, edemas... and the habitual examinations of hepática exploration. Some authors show favorable criteria in the treatment of the 510 cirrhosis [ ]. It seems to be that the silimarina accelerates the return to normality in case of noncomplicated viral hepatitis, however, in case of chronic hepatitis, very has an effectiveness limited [ 511 and mentioned references ].
Use
The use of the silimarina and galénicas preparations of thistle Maria is advised in the treatment of the digestive functional upheavals originated by hepatitis, specially, of viral origin. Fitoterapeutas advises to the thistle use Maria in the chronic congestivos states of the liver and the functional digestive upheavals. Often, the thistle is associated Maria to a "hepático drenador"...
Tests of acute and subacute toxicología made in rat, reveal that the criomolturado dust is lacking of 512 toxicity [ ]. The flavanolignanos are not toxic: 20 doses of g/kg of silimarina (to per you) do not cause alterations in mouse, being the D.L.50 (i.v.) of this compound, 1 g/kg approximately for mouse and 900 mg/kg for rat. Signs of chronic toxicity have not been observed (rat, 5 months, 0.1 g/día, to per you), [ Hahn ET al., 1968 ].
In Spain the use of this plant for the treatment of digestive functional upheavals of hepático origin is authorized.
Precautions
They have not been described in spite of to be put under a prolonged and constant experimentation.
The drug
The aquenios - similar to those of the sunflower they are black, rough, ended by a rest of floral crown that acquires the form of a cylindrical grudge of clear yellow color. The section has a consistency of waxen aspect, without flavor nor scent. The test of the drug can include the observation to the microscope of the pulverized drug, a study by chromatography in fine layer (revealed with difenilborato of aminoetanol) of the flavanolignanos extracted with metanol and a colorimétrica valuation by reaction of these with 2,4-dinitro fenilhidracina. Also a liquid chromatography of hi-res can take place.
Chemical studies on Silybum marianum (L.) Gaertn. wild-growing in Egypt. I. Oil and sterols
Fats and Oils, 38,93-97, 1987.
[ 499 ] H. WAGNER
Antihepatotoxic flavonoids. In: Plant flavonoids in biology and medicine: biochemical, pharmacological and structure-activity relationships, V. CODY, And MIDDLETON and J.B. HARBORNE, éds., New York, Alan R. Liss, p. 545-558, 1986.
[ 500 ] M. FIEBIG and H. WAGNER
Neue antihepatotoxisch wirksame. Flavonolignane aus to einer weißblühenden Silybum-Varietät
It plants Med., 50, 310-313, 1984.
[ 501 ] A.H. MERICLI
Flavonolignans, kaempferol 3-sulphate and to other flavonoids from Silybum marinum subsp. anatolicum
It plants Med., 54, 44-45, 1988.
[ 502 ] T. ADZET, M.R. COLL, J. IGLESIAS and M. PUIGMACIA
Selection and improvment of Silybum marianum. I. Characterization of populations from different origins
Plant Physiol. Biochem., 25, 129-135, 1987.
[ 503 ] H. WAGNER Plant constituents with antihepatotoxic activity. In: Natural products medicinal ace agents, J.L. BEAL and E. REINHARD, éds., Stuttgart, Hippokrates-Verlag, p. 217-242, 1981.
[ 504 ] G. VOGEL
To peculiarity among the flavonoids- silymarin to compound activates on the to liver. In: International Proceedings of the bioflavonoids symposium, 1981. L. FARKAS, F. KALLAY, M. GABOR and H. WAGNER, éds., Amsterdam, Elsevier, p. 461-474, 1982.
[ 287 ] M. GABOR
The pharmacology of benzopyrone derivatives and related compounds, Budapest, Akadémiai Kiadó, 1988.
[ 505 ] H. HIKINO, And KISO, H. WAGNER and M. FIEBIG
Antihepatotoxic actions of flavanolignans from Silybum marianum fruits
It plants Med., 50, 248-250, 1984.
[ 506 ] (a) R. MEIß, Or HEINRICH, H. ROBENEK and H. THEMANN
Effect of silybinin on hepatic cell membranes to after damage by polycyclic aromatic hydrocarbons
Agents and Actions, 12, 254-257, 1982.
(b) G. VOGEL, B. TUCHWEBER, W. TROST and U. MENGS
Protection by s(a) - R. MEIß, Or HEINRICH, H. ROBENEK and H. THEMANN
Effect of silybinin on hepatic cell membranes to after damage by
[ 507 ] H. LOTTER, G. ROHR and Th. WIELAND
Conformation of [ 4-cis-Br-Pro7 ] - antamanide crystallized from to methanol/water.
Naturwissenschaften, 71, 46-47, 1984.
[ 508 ] To VALENZUELA, C. LAGOS, K. SCHIMIDT and L.A. VIDELA
Silymarin protection against hepatic lipid peroxidation induced by acute ethanol intoxication in the Rat
Biochem. Pharmacol., 34, 2209-2212, 1985.
[ 509 ] (a) To VALENZUELA, R. GUERRA and L.A. VIDELA
Antioxidant properties of the flavonoids silybin and (+)-cyanidanol-3: comparison with butylated hydroxyanisole and butylated hydroxytoluene
It plants Med., 52, 438-440, 1986.
(b) R. FIELDS, To GARRIDO, R. GU(a) - To VALENZUELA, R. GUERRA and L.A. VIDELA
Antioxidant properties of the flavonoids silybin and (+)-cyanidanol-3: comparison with butylated hydroxyanisole and butylated hydro.
[ 510 ] M. FREY, S.A. Müller-lissner, G. MÜNST, K. STUBY and A.L. BLUM
Hépatologie
Méd. ET Hyp., 40, 31-34, 1982.
[ 511 ] M. PINKAS
To propos du chardon-Marie
Phytotherapy, (7), 5-7, 1983.
[ 512 ] Thistle Maria, toxicológico dossier of Laboratories ARKOPHARMA.