Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1990-03-21
1994-05-24
Phelan, Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424430, 424436, 514556, 514931, 514934, 514967, 514969, A61F 1300
Patent
active
053146891
DESCRIPTION:
BRIEF SUMMARY
Viruses of the most divergent type present a major health hazard for humans, animals and plants and can result in harmless to highly dangerous infections. In contrast to bacteria, viruses require a living host cell for life, development of their activity and for propagation.
A disquieting increase in sexually transmitted viral infections, such as those involving Herpes simplex virus (HSV), types 1 and 2, Cytomegalo virus (CMV), human immune deficiency virus (HIV), human papilloma virus (HPV), etc., has recently occurred with the changes in sexual mores.
At the present time, no satisfactory wide-ranging antiviral drug is available, with the exception of acycloguanosine (ACYCLOVIR), which is used in the treatment of Herpes, and azidothymidine (AZT), which is used in the treatment of AIDS.
None of these drugs is problem-free. In principle, however, preventive modalities are not obtainable.
Prevention is particularly desirable in cases involving HSV, CMV, HIV and VCV, in which the virus persists during the lifetime of the host and frequently causes illness many years later and with different pathologies.
All the remedies proposed to date were directed toward a direct combatting of the virus after its entrance into the cell, in order to inactivate or kill it there.
Surprisingly, a remedy was now developed that acts not only directly on virus replication, but also completely inactivates the virus by means of a still unexplained change in the host cell and makes virus survival impossible.
The remedy according to the invention is defined in patent claim 1, while particular embodiments can be deduced from the subordinate claims.
The preferred compound, which was found to be active in this connection, is L-acetyl-carnitine .gamma.-trimethyl-.beta.-acetyl-butyrobetaine) with the formula: ##STR1##
Carnitine is a compound that occurs naturally in the body. The ortho-L-acetyl derivative is also a known one, occurring both in various organs and also commercially available in synthetic form; it is recommended for example for peroral use in the form of pills or drops for the treatment of age-induced neurological metabolic disorders. For example, such disturbances are memory loss, strange behavior and erratic manifestations, such as are commonly known as dementia senilis. The recommended dosage is 30 mg/kg/day.
It has now been found in a completely unexpected manner that L-acetyl-carnitine has a potent antiviral activity and can be used for treating viral infections, but also in particular for the prevention of such infections with surprising success.
The studies conducted to demonstrate the antiviral activity of L-acetyl-carnitine can be summarized as follows:
1. Effect of L-acetyl-carnitine on viral growth in tissue cultures
Two trial series were conducted. In the first series, various cell lines of animal and human origin (African green monkey; human cervical cancer cells) were infected with various viruses, including HSV, types 1 and 2, CMV, Adenovirus, Varicella-Zoster virus (VZV), respiratory syncytial virus (RSV), polio virus, Coxsackie virus, enterovirus and vaccinia virus.
Five cultures of each, which were infected with the above viruses, were treated with 100 mg/ml of L-acetyl-carnitine.HCl or control medium (no active substance).
The virus titers were determined at daily intervals for 12 days.
All the controls reacted positively to the viral growth with titers in the range between 10.sup.4 and 10.sup.8 colony-forming units (plaque forming units pfu) /ml, depending on the specific virus.
On the other hand, all the specimens treated with L-acetyl-carnitine.HCl were negative (0 pfu/ml), i.e., no viral propagation occurred.
In the second trial series, the action of the L-acetyl-carnitine dosage on the antiviral activity was determined.
Five cultures of each were infected and treated with 10, 20, 30, 40, 50, 60, 70, 80, 90, 100, 200 and 400 mg/ml of L-acetyl-carnitine.HCl or a control medium and the virus titers were determined as above.
The antiviral activity was observed in all dosages of more than 10-20 mg/ml. The
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T. Nakadate et al., "Inhibition of 12-O-Tetradecanoylphorbol-13-acetate-induced Tumor Promotion and Epidermal Ornitbine Decarboxylase Activity in Mouse Skin by Palmitoylcarnitine," Cancer Research, 44, 1583-1593 (1986).
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Aurelian Laure
Scandurra Laura
Bernardini Attilio
Phelan Gabrielle
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