The flowers of this herbaceous plant of crawling stems are pentámeras: corola gamopétala, in tube in the base, with 5 extended lobes truncated, of violáceo blue color. Estambres Epi and alternipétalos, hipógino disc with fleshy nectários that alternate with 2 different carpelos but with an only style.
Origin
The crawling species, with lengths estolones, forms dense carpets in the fresh underbrushes, umbrios roadside ditches and rocky terrains. Common in all Europe, it does not grow in the Mediterranean region nor in the Arctic zones. It is cultivated in central Europe.
Chemical composition
Although some nonexcellent compounds have been described (bears, triterpenos, acids fenoles, flavonoides, logánico acid, etc... [ 366 ]), the indólicos alkaloids (0.5 to 1%) are the components that have given rise to a greater number of 367 published works [ ].
•Vincamina. This pentacíclico alkaloid - that approximately represents 10% of the total alkaloids - appears accompanied of other compounds that, like him, are related to the skeleton of the eburnano: vincina, eburnamonina, oxovincamina... The other alkaloids are aspidospermanos dihidroindólicos: metilen-indolenina like the vincadiformina, the minovina, the minovincina, or 2,16-dihidro like, for example, the aspidospermidina N-metil. Asimimo, the drug provides derivatives dry-7,21: quebracamina, vincadina, vincaminoreína, etc... and derived related to the corinano, for example, 369 norvincorina [ ]. A discovery has put of relief the presence of a "dímero" [ 370 ].
The vincamina used in therapeutic can come from the leaves of the minor Vinca. Also it is a product of total synthesis and hemisíntesis: by means of a called synthesis biomimética, the tabersonina, alkaloid with áspidospermano skeleton that is extracted of the seeds of African Voacanga Stapf., can industrially be transformed into vincamina [ 371 ].
Farmacológicos data
The numerous tradition attributes to the drug virtues: emenagoga, antihemorrágica, "antidermatósica", "antipapaya".... [ 372 ], but the one that more interest has provoked it is the simpaticolítica property of his alkaloids. Although also its activity has studied on the myocardium, the coronary ones and the 373.223 tension [ ], does not fit doubt that the studied activity more is the one than they exert the alkaloids on the cerebral circulation. The vincamina increases the flow cerebral in dog and cat, diminishes isquemia local produced by occlusion of the cerebral artery average in the cat. It is possible that this increase also must to a metabolic activity make clear in the animal: increase of the consumption of oxygen and glucose on the part of the brain of the dog previously altered by hyperventilation, increase of the time of survival of mice maintained in poor oxygen atmosphere. The increase of the aerobic glucolisis increases the production of A.T.P. (edema astrocitario diminishes and the connection of the neuron recovers) and it causes an elevation of the partial CO2 pressure: this increase would be the leading stimulus of the vasodilatación [ 374 ]. The eburnamonina (synthesized) is oxigenadora and antihipóxica, ] is "stimulating brain-metabolic" [ 375.376.
Observations in the Man
Be as they are the critics on the methodology of some tests, at the moment exists unamimity in recognizing the reality of active drugs on the cerebral circulation [ 377 ]. Some studies demonstrate to an increase of the cerebral sanguineous flow after the administration i.v. of vincamina [ 378 ]. Others confirm an improvement of the neurological symptoms by means of the administration, during a long period of time, vincamina to per you [ 374 ]. In order to show the metabolic and circulatory effects of the alkaloid 133Xe can be used and make the pertinent biochemical measures, including the evolutionary measurement of the lactato/piruvato relation (witness of the aerobic metabolism of the glucose). The administration by parenteral route can cause cardiac upheavals, concretely, ventricular arrhythmias.
Use
Although in some countries, the popular medicine still uses the leaf in fresh state or in form of simple galénica preparation, the drug is used mainly on the part of the pharmaceutical industry for the extraction of vincamina. One sets out (60 mg/día, to per you) in the treatment of the cerebral circulatory insufficiency accompanied by a diminution of the watch, upheavals of the memory, the irritability and an instability of humor. Asimimo, can be used in neurology (postoperating sequels of craneales traumatismos and states), in O.R.L. (upheavals cocleo-vestibulares)... The vincamina is a little toxic alkaloid, its DL50 in the rat is of 500 mg/kg oral route, 76 mg/kg via i.p. and 24 mg/kg by via i.v. [ Quevauviller, 1954 ]. The tests of chronic toxicity do not reveal pathological signs. Other sources make reference to a DL50 much more elevated (4g/kg, to per you).
The drug
The oficinal drug is constituted by elliptical leaves, lanceoladas, coriáceas. They can get to measure up to 5 cm in length. The limb is of grayish green color with whole edges and a pinnada ribbing. In a cut, the main nerve is prominent and, in the superior face, it presents/displays unicellular tectores tricommas that also can be seen in the dust. In this one also fragments of epidermis inferior with cells of paracíticos winding walls and estomas can be. The French Farmacopea advises to the accomplishment of a chromatographic study (chromatography in fine layer) of the total alkaloids and the identification of the vincamina using an internal witness, but it does not anticipate the valuation of the total alkaloids.
Bibliography
[ 366 ] To BIANCO, M. GUISO and P. PASSACANTILI
Iridoid and phenylpropanoid glycosides from new sources.
J. Nat. Prod., 47, 901-902, 1984.
[ 367 ] W. DÖPKE
Eburnamine-vincamina The alkaloids. In: The Alkaloids, chemistry and physiology, R.G.A. RODRIGO, ed., New York, Academic Press, 20, p. 297-332, 1981.
[ 368 ] M. V. KISAKÜREK, A.J.M. LEEUWENBERG and M. HESSE
To chemotaxonomic investigation of the plant families of Apocynaceae, Loganiaceae, and Rubiaceae by to their kind alkaloid content. In: Alkaloids, biological chemical and perspectives, S.W. PELLETIER, ed., New M. V. KISAKÜREK, A.J.M. LEEUWENBERG and
[ 369 ] B. PROKSA, D. UHRIN, And GROSSMANN and Z. VOTICKY
(-)1 norvincorine, to new alkaloid from minor Vinca L. Planta Med., 53, 120 -, 1987.
[ 370 ] B. PROKSA, D. UHRIN, And GROSSMANN and Z. VOTICKI Vincarubine,
to novel bisindole alkaloid from minor Vinca L.
Tetrahedron letters, 27, 5413-5416, 1986.
[ 371 ] J. BRUNETON
Eléments of phytochimie ET of pharmacognosie, Tec. and Doc. - Lavoisier, Paris, 1987.
2000 Jahre Vinca minor-Kleines Immergrün. Vom Apotropaikum zum aktuellen Arzneistoffprodukten.
Dtsch. Apoth.-Ztg., 127, 2376-2380, 1987.
[ 374 ] L. VERECZKEY
Pharmacokinetics and metabolism of vincamine and related compounds.
Eur. J. Drug Met. Pharmacokin., 10, 89-103, 1985.
[ 223 ] J. TOTTE and A.J. VLIETINCK
Produits phytothérapeutiques ET système cardiovasculaire
J. Pharm. Belg., 41, 330-361, 1983.
[ 375 ] P. LINEE, P. LACROIX, J-b. HIM POLLES and To BERTHE
1-éburnamonine, molécule nouvelle ET originale.
Médecine praticienne, (03), 60-63, 1980.
[ 376 ] On the experimental and clinical pharmacology of (- the)-eburnamonina one, to consult, among others, a series of articles published in: Eur. Neurol., 17, sup. 1, 1-172, 1978.
[ 377 ] To SPAGNOLI and G. TOGNONI
Cerebroactive drugs. Clinical pharmacology and therapeutic role in cerebrovascular disorders.