Claims
- 1. A purified and isolated or recombinantly produced compound which has antimicrobial or antiviral activity and which has the formula
- A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --A.sub.5 --A.sub.6 --A.sub.7 --A.sub.8 --A.sub.9 --A.sub.10 --A.sub.11 --A.sub.12 --A.sub.13 --A.sub.14 --A.sub.15 --A.sub.16 --A.sub.17 --A.sub.18 ( 1)
- or a pharmaceutically acceptable salt or an N-terminal acylated or a C-terminal amidated or esterified form thereof, which is either in a linear form or in a cystine-bridged form, wherein:
- each of A.sub.1 and A.sub.9 is independently a basic amino acid;
- each of A.sub.2 and A.sub.3 is independently a small amino acid;
- each of A.sub.5, A.sub.7, A.sub.12, A.sub.14 and A.sub.16 is independently a hydrophobic amino acid;
- A.sub.4 is a basic or a small amino acid;
- A.sub.10 is a basic or a small amino acid or is proline;
- A.sub.11 is a basic or a hydrophobic amino acid;
- A.sub.17 is not present or, if present, is a small amino acid;
- A.sub.18 is not present or, if present, is a basic amino acid; and
- each of C.sub.6, C.sub.8, C.sub.13 and C.sub.15 is independently selected from the group consisting of cysteine, a hydrophobic amino acid, a large polar amino acid and a small amino acid.
- 2. The compound of claim 1 which has one or more characteristics selected from the group consisting of:
- the C-terminal carboxyl is of the formula selected from the group consisting of COOH or salts thereof, COOR, CONH.sub.2, CONHR and CONR.sub.2 wherein each R is independently a hydrocarbyl (1-6C);
- the amino group at the N-terminus is of the formula NH.sub.2 or NHCOR wherein R is a hydrocarbyl (1-6C);
- each of A.sub.1 and A.sub.9 is independently selected from the group consisting of R, K and Har;
- each of A.sub.2 and A.sub.3 is independently selected from the group consisting of G, A, S and T;
- A.sub.4 is R or G;
- each of A.sub.5, A.sub.14, and A.sub.16 is independently selected from the group consisting of I, V, NLe, L and F;
- each of A.sub.7 and A.sub.12 is independently selected from the group consisting of I, V, L, W, Y and F;
- A.sub.10 is R, G or P; and
- A.sub.11 is R or W.
- 3. The compound of claim 1 which has antimicrobial or antiviral activity against a pathogen associated with a sexually transmitted disease.
- 4. The compound of claim 1 which has antimicrobial or antiviral activity against Escherichia coli, Listeria monocytogenes, Candida albicans, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhimurium, Staphylococcus aureus, Histoplasma capsulatum, Myobacterium avium-intracellulare, Mycobacterium tuberculosis, Vibrio vulnificus, Chlamydia trachomatis, Treponema pallidum, Neisseria gonorrhoeae, Trichomonas vaginalis, Herpes simplex virus type 1, Herpes simplex virus type 2, human immunodeficiency virus, Hemophilus ducreyi, or human papilloma virus.
- 5. A method of inhibiting the growth of a sexually-transmittable microbe or the replication of a sexually-transmittable virus which comprises the step of contacting said sexually-transmittable virus or said sexually-transmittable microbe with an amount of a compound according to claim 1 effective to inhibit said growth or said replication.
- 6. The method of claim 5 in which the sexually-transmittable microbe is a sexually-transmittable bacterium.
- 7. The method of claim 5 in which the sexually-transmittable microbe or virus is selected from the group consisting of human immunodeficiency virus type 1, Chlamydia trachomatis, Treponema pallidum, Neisseria gonorrhoeae, Trichonomis vaginalis, Herpes simplex virus type 1, Herpes simplex virus type 2, Hemophilus ducreyi and human papilloma virus.
- 8. The method of claim 5 in which the sexually-transmittable microbe or virus is human immunodeficiency virus.
- 9. A method to treat or prevent a sexually-transmitted microbial or viral infection in a subject, which method comprises administering to a subject in need of such treatment an amount of a compound according to claim 1 effective to treat or prevent said infection in the subject.
- 10. The method of claim 9 in which the infection is a bacterial infection.
- 11. The method of claim 9, in which the compound is administered therapeutically.
- 12. The method of claim 9 10 or 11 in which the infection is a bacterial infection.
- 13. The method of claim 9, 10 or 11 in which the sexually-transmitted infection is caused by a microbe or virus selected from the group consisting of human immunodeficiency virus type 1, Chlamydia trachomatis, Treponema pallidum, Neisseria gonorrhoeae, Trichonomis vaginalis, Herpes simplex virus type 1, Herpes simplex virus type 2, Hemophilus ducreyi and human papilloma virus.
- 14. The method of claim 9, 10 or 11 in which the infection is a human immunodeficiency virus infection.
- 15. The method of claim 9, 10 or 11 in which the compound is administered topically.
Parent Case Info
This application is a continuation of application Ser. No. 08/499,523, filed Jul. 7, 1995, and issued as U.S. Pat. No. 5,804,558 on Sep. 8, 1998, which is a continuation-in-part of U.S. Ser. No. 08/451,832, filed May, 26, 1995, and now abandoned, which is a continuation-in-part of U.S. Ser. No. 08/243,879 filed May 17, 1994, and issued as U.S. Pat. No. 5,708,145 on Jan. 13, 1998, which is a continuation-in-part of U.S. Ser. No. 08/182,483 filed Jan. 13, 1994, and issued as U.S. Pat. No. 5,693,486 on Dec. 2, 1997, which is a continuation-in-part of U.S. Ser. No. 08/095,769 filed Jul. 26, 1993, and issued as U.S. Pat. No. 5,464,823 on Nov. 7, 1995, which is a continuation-in-part of U.S. Ser. No. 08/093,926 filed Jul. 20, 1993, and now abandoned. The contents of these applications are incorporated herein by reference.
Government Interests
This invention was made with funding from NIH Grant No. A122839. The U.S. Government has certain rights in this invention.
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Continuations (1)
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499523 |
Jul 1995 |
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Continuation in Parts (1)
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