Extracts of shark cartilage having an anti-angiogenic...

A - Human Necessities – 61 – K

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A61K 35/60 (2006.01)

Patent

CA 2188793

The present invention relates to shark cartilage extracts and to a method of producing the same, these extracts having anti-angoigenic properties (reduction of the area of blood vessels observed in vivo on experimentally induced tumors), tumor regressive activity in vivo as well as demonstrating a direct inhibitory effect on tumor cell lines. This process does not involve any denaturing solvent or product and does not involve the use of any enzymes. It consists of obtaining a blend of whole cartilage in an aqueous solution of neutral pH, preferably pure water, this blend being centrifuged and the pellet and supernatant kept for further processing. The pellet is iyophilized and tested for anti-tumor and anti-angiogenic activities in vivo and in vivo, with or without supernatant. The supernatant has been shown to have anti-angiogenic and tumor regressive activities in vivo. the composition of the supernatant has then been investigated by different ways. Fractionation of thissupernatant led to the characterization of some of its active components,The fractions were tested for their direct in vitro activity on cancer cell lines. Therefore, it is assumed that the non-fractionated supernatant has such an in vitro activity. Lyophilization substantially destroys the activity of these liquid fractions while no such abolition is observed in the solid extract.

L'invention concerne des extraits de cartilage de requin et un procédé permettant de les produire. Ces extraits présentent des propriétés anti-angiogéniques (réduction de la surface des vaisseaux sanguins observée in vivo sur des tumeurs induites au cours d'expériences), et font régresser les tumeurs in vivo, et ils manifestent un effet inhititeur direct sur des lignées de cellules tumorales. Le procédé de production n'implique aucun solvant ou produit dénaturant, ni l'utilisation d'enzymes, mais consiste à obtenir un mélange du cartilage entier dans une solution aqueuse à pH neutre, de l'eau pure de préférence, à centrifuger ce mélange et à réserver la boulette et le surnageant obtenus pour un traitement ultérieur. La boulette est lyophilisée et on en vérifie les activités anti-tumorales et anti-angiogénique in vivo et in vitro, avec ou sans surnageant. On a démontré que celui-ci est anti-angiogénique et fait régresser les tumeurs in vivo et sa composition a été étudiée de différentes façons. Son fractionnement a permis de définir des caractères de certains de ses composants actifs. On a expérimenté l'activité in vitro directe de ses fractions sur des lignées de cellules cancéreuses. On peut donc supposer que le surnageant non fractionné présente in vitro une telle activité. La lyophylisation détruit pour l'essentiel l'activité de ces fractions liquides mais cette destruction n'intervient pas dans l'extrait solide.

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