FR2852842A1 - Process for preparing an active component from the resin exudate of fruits of Daemonorops or Croton, useful for dermatological application to protect against free radicals - Google Patents

Abstract

Preparing an active component from the resin exudate (dragon's blood) of fruits of Daemonorops or Croton, especially Daemonorops draco or Croton lechleri by dissolving this in a hydroglycolic solution containing 0 - 100 % glycol, separating the soluble material by filtration, decantation, or centrifuging, and concentrating the extract by filtration, ultrafiltration, osmosis, and/or nanofiltration, is new. ACTIVITY : Dermatological; Antiinflammatory; Antioxidant. No biological data given. MECHANISM OF ACTION : None given.

Description

PROCESS FOR PREPARING AN ACTIVE INGREDIENT FROM

  FRUIT RESIN EXUDUDATE OF Daemonorops draco or Croton lechieri, COMPOSITIONS INCLUDING IT AND USES The present invention relates to a process for the preparation of an active principle which makes it possible in particular to combat aging of the skin and also covers the compositions which include 'include.

  We know the natural compound known as dragon's blood which comes from the fruits of a tree of the family of Daemonorops or Crotons, more specifically Daemonorops draco or Croton lechieri.

  This red compound from where its name, in the form of resins, has been known for a very long time for its healing properties by migrating fibroblasts to the affected areas of a wound for example.

  This natural compound also has antibacterial, antiseptic and anti-inflammatory properties.

  We mainly isolated in these natural extracts a high richness in alkaloids, in particular taspine.

  As prior art, mention may be made of US Pat. No. 3,694,557 which describes a composition for anti-inflammatory purposes.

  Likewise, US Pat. No. 5,156,847 presents a pharmaceutical composition but the dissolution of which is carried out in a solvent of the non-aqueous type, more particularly DMSO, dimethylsulfoxide.

  There are also products on the market to which the known virtues are credited without having been found to be superior to the products of the modern pharmacopoeia. However, it has been found that it is very difficult to have extracts in an aqueous medium which are unstable.

  The present invention consists of a process for the preparation of an active principle from dragon blood which is stable in an aqueous medium. be more, these stabilized compositions find certain cosmetic applications whose results are verified in the present invention.

  To this end, the method is now described in detail according to a particular, nonlimiting embodiment, the results being integrated into the present.

description.

  1 / PROCESS BE PREPARATION OF A COMPOSITION BASED ON BLOOD OF BRAGON solubilization of dragon blood, that is to say an exudate of resin of 10 fruits of Daemnonorops or Crotons, more particularly of the variety Daemonorops draco or Croton lechieri, at a rate of at least 20 9 / I by weight, in a hydroglycolic solution, containing between 0 and 100% glycol, - filtration, decantation or centrifugation in order to separate the solubilized phase from the insoluble products, - successive concentrations of the active phase by filtration, ultrafiltration, osmosis and / or nanowire Itration.

  It is also possible to add between 0 and 1% o of salt, in the form of sodium bisulfite and from 0 to 1% of EDTA, ethylene diamine tetra acetic acid.

  be even, as glycol, we prefer butylene glycol.

  It is noted that, depending on the form of dragon blood used, the water / glycol ratio can be modified and that it is this compound which provides the stability of the composition as will be confirmed below.

  Salt has the advantage of keeping the color stable.

  2 / CHARACTERIZATION OF THE ACTIVE INGREDIENT THUS OBTAINED 2-1 / Dry matter: the dry matter content is obtained by passing through an oven at 105 C of 109 of product, until a constant weight is obtained.

  The dry matter content is between 1 and 100 g / l, more particularly between 20 and 60 g / l.

  2-2 / pH: The final pH is between 4.0 and 7.0, constant.

  2-3 / Polypenol content: The polyphenol content gives a content of between 0.4 and 40%.

  2-4 / Characterization of Taspine: The taspine contained in the preparation according to the present invention is identified according to the protocol described in the publication Persinos-Perdue G, and ai, (1979) "10 South american plants II, taspine isolation and anti inflammatory activity "Journal of Pharmaceutical Sciences 68 (1), pp 124-126.

  In the tests carried out, the taspine ratio relative to the polyphenols is 2.5% when salt and EbTA are added and 20% when the water / glycol mixture is used alone.

  The ratio of taspine to polyphenols is therefore always greater than 1.

  2-5 / Physical characterization: The color of the active ingredient is red, its appearance is clear and the aqueous or glycol composition is stable. 20 3 / EFFECTS OF THE ACTIVE INGREDIENT ACCORDING TO THE INVENTION: 3-1 / Anti-free radical activity: 3-1-1 / DPPH Diphenyl picrylhydrazyl hydrate is a free radical, absorbing in violet at 25,517 nm.

  in the case of an anti-radical activity, there is disappearance of the violet coloration, this is what we observe in the following table: Anti-radical activity in% Control 0 Active principle at 0.0050% 71 0.0025% active ingredient 64 3-1-2 / Cell cultures: The protocol consists in cultivating human fibroblasts or keratinocytes in the presence and absence of the active ingredient according to the present invention at different concentrations, the active ingredient being diluted directly in the culture medium.

  These cultures are chemically attacked with a solution of hypoxanthinexantine oxidase.

  The deleterious effects of this chemical attack are evaluated on the pretreated and non pretreated cultures.

  The study consists in measuring cell viability by means of the so-called MTT method at 540 nm in order to determine the protective effects with respect to chemo-induced free radicals of the active principle according to the invention.

  The results are indicated in the table below Human fibroblasts: Anti-radical activity in% Control 0 Active principle at 0.25% 10 Active principle at 1.00% 100 Active principle at 2.00% 100 There is a strong activity anti-radical of the active principle according to the present invention.

HaCaT Keratinocytes :.

  Anti-radical activity in% Control 0 Active principle at 0.5% 58 Active principle at 1.0% 70 Active principle at 2.0% 88 There is an anti-radical protection of 88% of HaCaT keratinocytes.

  3-2 / Detoxifying Activity: Human keratinocyte cultures, in the presence or absence of the active principle according to the present invention, are subjected to radical aggression by the Fenton reagent (mixture of FeCl2 with hydrogen peroxide).

  Viability is again assessed by the MTT method.

  The following results are obtained: Human fibroblasts: Chelating activity in% Control 0 Active principle 0.25% 51 Active principle 0.50% 67 Human keratinocytes | Chelating activity in% Control 0 Active principle 0.25% 26 Active principle 0.50% 50 It is noted that the active principle limits the radical damage induced by the Fenton's reagent both on fibroblasts and on keratinocytes.

  3-3 / Effect on the release of PGE2: In this evaluation, human keratinocytes grown in the presence or absence of the active ingredient are subjected to chemical inflammation (arachidonic acid).

  The PGE2 level is measured in the supernatant, using a specific Elisa kit.

  The results are as follows: Variation in the level of PGE2 / control Control 0 Active principle 0.50 -31 There is a decrease in the expression of PGE2, which provides a soothing effect.

  The active principle is introduced into any suitable cosmetic support, cream, ointment, emulsion, lotion or dispersion.

  The active principle is introduced at a rate of 1 to 10% in these dosage forms.

Claims (6)

  1. Process for the preparation of an active principle, characterized in that it comprises the following stages: - solubilization of dragon blood, in particular in the form of an exudate of fruit resin from Daetnonorops or Crotons, in particular the variety 5 Daemonorops draco or Croton lechieri, in a hydroglycolic solution containing between 0 and 100% glycol, - filtration, decantation or centrifugation in order to separate the solubilized phase from the insoluble products, - successive concentration of the active phase by filtration, ultrafiltration, 10 osmosis and / or nanofiltration.   2. Process for the preparation of an active principle according to claim 1, characterized in that between 0 and 1% of salt is added, in particular in the form of sodium bisulfite.   3. Process for the preparation of an active principle according to claim 1 or 2, characterized in that between 0 and 1% of EbTA, ethylene diamine tetra acetic acid is added.   4. Method for preparing an active ingredient according to any one of the preceding claims, characterized in that the glycol is butylene glycol.   5. Active principle obtained from the process according to one of claims 1 to 4, characterized in that it comprises - 1 to 100 g / I of dry matter, in particular between 20 and 60 g / I - the pH is understood between 4.0 and 7.0 - rate of polyphenols between 0.4 and 40 g / I 25 - rate of taspine greater than 1%.   6. Use of the active principle according to claim 5 obtained from the process according to one of claims 1 to 4, characterized in that it consists in introducing from 1 to 10% of this active principle in a suitable cosmetic support in order to be able to apply it to the skin to obtain a soothing and anti-radical effect.