Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/42—Phosphorus; Compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
  • A61K31/19—Carboxylic acids, e.g. valproic acid
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/22—Anacardiaceae (Sumac family), e.g. smoketree, sumac or poison oak
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
  • A61K36/47—Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/88—Liliopsida (monocotyledons)
  • A61K36/889—Arecaceae, Palmae or Palmaceae (Palm family), e.g. date or coconut palm or palmetto
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/88—Liliopsida (monocotyledons)
  • A61K36/896—Liliaceae (Lily family), e.g. daylily, plantain lily, Hyacinth or narcissus
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/88—Liliopsida (monocotyledons)
  • A61K36/90—Smilacaceae (Catbrier family), e.g. greenbrier or sarsaparilla
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/12—Antivirals
  • A61P31/14—Antivirals for RNA viruses
  • A61P31/18—Antivirals for RNA viruses for HIV

Definitions

• the invention relates to compositions having in particular antiviral properties, and in particular antiretroviral.
• HIV human immunodeficiency viruses
• nucleoside derivatives including zidovudine, or AZT, which was the first antiviral available. Since the emergence of resistant mutants led to seek new treatments.
• the object of the invention is to provide new antiretroviral compositions capable of.
• compositions It also relates to a process for obtaining such compositions.
• compositions according to the invention are characterized in that they are prepared from coconut extract, solution of mineral salts, extracts of cactacea, liliaceae, anacardiaceae and euphorbiaceae, grass muskia, passiflora, rutaceae, artocarpea, bombaceae and lice of wood.
• the coconut is the fruit of the coconut tree. According to the invention, the grated white meat is advantageously used.
• Cactaceae particularly suitable for the implementation of the invention include opuntia.
• opuntia is the genetic name for snowshoes, nopal, prickly pears and other species native to tropical America. We use more especially the fruits of the green racket.
• Suitable lilies within the scope of the invention include sarsaparilla, and Paloes. Sarsaparilla root and aloe cream are used with advantage.
• mombin particularly the bark of mombin, is particularly used.
• Euphorbiaceae are castor and sweet cassava.
• Castor seeds especially in the toasted state and in the form of powder, are more particularly used for the invention.
• Cassava is used in grated form in the context of the invention.
• Suitable grasses in the context of the invention include maize and vetiver.
• the stigmas of maize (corn hair) and vetiver roots are used with advantage.
• a particularly preferred passiflora is the brown calabash.
• Rutaceae particularly suitable for the implementation of the invention include lemon.
• Appropriate artocargess within the scope of the invention include the breadfruit.
• the fruit of the breadfruit is advantageously used.
• Wood lice are also used in the context of the invention. Living lice are advantageously used in their nest.
• compositions are made from grated coconut, seawater, green racquet fruit, sarsaparilla root, mombin bark, ground seed powder grilled castor oil, aloe, corn, vetiver root, rotten and dried banana heart, wooden lice, brown callabasse, breadfruit lemon, mapou or baboal, grated sweet cassava.
• coconut powder preferably, shredded white flesh
• mineral salts especially sodium, potassium, magnesium, calcium, phosphates, chlorides, sulphates, carbonates and bicarbonates
• seawater 3 to 5 liters, in particular 4 liters
• grated green racket fruit 10 to 20 fruits corresponding to 1 or
• - roasted and ground castor seeds from 500 g to 1.5 kg, in particular approximately 1 kg - from 100 to 300 g of rotten banana heart center, and preferably 200 g
• Aloe can weigh from 75 to 125g, including 100g.
• One tablespoon of calabash is used.
• a lemon is used, preferably cut into at least three pieces.
• 15 to 35 centigrams of mapou or baobal bark are used, and preferably about 25 centigrams.
• Vetiver root is used at a rate of 10 to 30 g centigrams, preferably 20 g.
• the fruit of the barely ripe breadfruit represents a quantity in the composition of 10 to 30g. 1 to 2 liters of lustral water are used, in particular 1.51; obtained in the following manner: take the living wood lice in their nest, burn the nest with the lice; the ash obtained is placed on a cloth and passed to the rain water; the liquid thus obtained is lustral water. 400 to 600 ml of vinegar are used as acetic acid, in particular 500 ml.
• the invention aims to cure AIDS and cure and relieve prostate and cyst.
• 4 to 5 liters of vinegar are used.
• compositions of the invention are as obtained by macerating coconut powder with vinegar for about 24 hours, adding to the filtrate of the maceration mixture the various ingredients listed above, preferably in the proportions indicated, by bringing the mixture obtained to boiling for at least 1 h and recovering the filtrate. The solution is then subjected to a conventional active compound protocol.
• the invention also relates to a process for obtaining the compositions defined above, characterized by the steps previously reported.
• the two fractions F2 and F7 were solubilized in 200 ⁇ l of dimethysulfoxide o Inactivation of the virus
• the suspension of viral particles A in the RPMI 1640 culture medium (HIV-I HIB, reverse transcriptase activity 3.8 ⁇ 10 6 cpm / ml) is incubated with F 2 and F 7 for 20 min at 4 ° C. and then 1 hour at room temperature. finally 2 hours at 37 ° C. at the end of incubation, the mixture is diluted to 1 / 1O 0 "16, 1/20, 1/40, 1/100, 1/200 in the culture medium RPMI 1640 plus 10% fetal calf serum (FCS), preheated for 30 minutes at 56 ° C.
• FCS fetal calf serum
• Pellets of 5 ⁇ 10 5 MT4 cells (human cells of lymphoid origin transformed with HTLV-I) are resuspended in 250 ⁇ l of the various dilutions of the virus composition mixture.
• the unabsorbed virus is removed by centrifugation of the cells. These are washed twice with RPMI and then resuspended in RPMI 10% FCS medium at a concentration of 2 ⁇ 10 5 / ml.
• the infected cells are cultured in microtiter plates (Costar 96 scoops) at the rate of 200 ⁇ l / scoops.
• a series of control cultures are infected in parallel with the mixed virus (v / v) suspension A with RPMI medium. Incubations and dilutions are carried out strictly under the same conditions as for the virus treated with the composition.
• the production of HIV after infection of MP4 cells with virus preincubated with the composition is evaluated.
• F2 and F7 fractions inhibit HIV-I replication in MT-4 cells.
• compositions of the invention are characterized in that they contain an effective amount of at least one composition as defined above, in association with an inert pharmaceutical vehicle.
• compositions are particularly suitable for the prevention and treatment of AIDS, if necessary in combination with other drugs. 1538 cpm / test, whereas, for supernatants of uninfected cultures, they are 1400-2100 cpm / test. All cultures infected with the untreated virus produce J5 virus at J1.
• Experiment B HIV production after infection of CEM-SS cells by HIV-I Lai is evaluated
• a suspension of virus B (HIV-I Lai, reverse transcriptase activity 3x10 6 cmp / ml) incubated (v / v) with the composition. All other steps are those described for the MT4 cell experiment.
• Virus production after 5 and 8 days is strongly inhibited by preincubation of the virus with the composition.
• Example 3 Study of the Effect of the Composition of Example 1 on the Reverse Transcriptase Activity of HIV-1
• the measurements were performed on at least two samples.
• compositions according to the invention are capable of inhibiting the activity of the reverse transcriptase in vitro.
• compositions are preferably administered by injection in the form of isotonic injectable solutions or suspensions with respect to the blood plasma.
• compositions of the invention have demonstrated an inhibitory effect of the HFV-I reverse transcriptase activity that may exceed 90% relative to the activity measured in the controls. There is also a decrease in the cytopathic effect of HIV-I in cells infected with this virus, treated with compositions of the invention.
• the aim of the invention is to make use of the properties of these compositions for the preparation of pharmaceutical compositions.
• the amount of active ingredient varies according to the state of the patient, the dosage in humans being most often of the order of 1 to 500 mg per day of active ingredient (dry extract).
• the invention will be illustrated hereinafter by an example of preparation of a composition of high efficiency with respect to the HIV-I virus and by the results of in vitro and in vivo tests.
• mapou or baobal bark 25 centigrams
• the mixture thus obtained is boiled for approximately 1 h and then filtered.
• Example 2 Study of HIV-inactivity by the composition of Example 1 Virus production was measured by an assay of the reverse transcriptase activity associated with the viral particles released by the cells into the culture medium. Reverse transcriptase is also called reverse transcriptase or RT for short.
• the RT test is carried out on 65 ⁇ l of medium according to the protocol described by Moog et al., In Antiviral Research, 24 (1994), 275-288. The results are expressed in cpm / test "(table, bottom).
• Cell viability is measured by the MTT assay described by Moog et al. In the reference given above (table, top). The intensity of the coloration is expressed in mili DO.
• the production of HIV after infection of MT4 cell with virus preincubated with the composition is evaluated. After 5 or 7 days of infection, the RT values are between 699 and

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• Health & Medical Sciences (AREA)
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• General Health & Medical Sciences (AREA)
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• 2009
  • 2009-07-22 WO PCT/FR2009/000906 patent/WO2011010000A1/fr not_active Ceased
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