Methods and compositions for the use of sargassum fusiforme for the inhibition of hiv-1 infection
OwnerDavid Yue-wei Lee, Mario Cankiinventors
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Abstract
The methods, kits, articles, and compositions of the invention feature a natural product (e.g., Sargassum fusiforme), an extract thereof, and fatty acid components of the extract (e.g., palmitic acid) for the treatment of a viral infection, e.g., HIV or herpes. The natural products used in the methods and compositions of the invention include brown algae, specifically algae of the Sargassum fusiforme species. The Sargassum fusiforme algae, extracts thereof, specific components of the extract, and related compounds of the invention may be used to treat or prevent HIV and herpes infections.
Claims48
A method of treating an HIV or herpes infection in a subject in need thereof, said method comprising administering to said subject a compound of formula (I):
- wherein Y is selected from —CH2CH2CH2COOH,
- R1 is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- each of R2 and R3 is, independently, selected from H, —ORA, —CH3, —CH2CH3, halide, cyano, and nitro;
- RA is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- R4 is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- and
- R5 is selected from H, —CH3, —CH2CH3, and CF3, or a salt thereof, in an amount sufficient to treat said infection.
A method of inhibiting the transmission of HIV or herpes infection between a first subject and a second subject, said method comprising topically applying to said first subject a compound of formula (I):
- wherein Y is selected from —CH2CH2CH2COOH,
- R1 is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- each of R2 and R3 is, independently, selected from H, —ORA, —CH3, —CH2CH3, halide, cyano, and nitro;
- RA is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- R4 is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- and
- R5 is selected from H, —CH3, —CH2CH3, and CF3, or a salt thereof, in an amount effective to inhibit said transmission.
An article comprising a compound of formula (I):
- wherein Y is selected from —CH2CH2CH2COOH,
- R1 is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- each of R2 and R3 is, independently, selected from H, —ORA, —CH3, —CH2CH3, halide, cyano, and nitro;
- RA is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- R4 is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- and
- R5 is selected from H, —CH3, —CH2CH3, and CF3,
- or a salt thereof,
- in an amount sufficient to inhibit transmission of HIV or herpes to an individual wearing the article.
A pharmaceutical composition formulated for topical administration comprising from about 1% to about 50% (w/w) of a compound of formula (I):
- wherein Y is selected from —CH2CH2CH2COOH,
- R1 is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- each of R2 and R3 is, independently, selected from H, —ORA, —CH3, —CH2CH3, halide, cyano, and nitro;
- RA is selected from H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- R4 is selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-7 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-8 heteroalkyl;
- and
- R5 is selected from H, —CH3, —CH2CH3, and CF3,
- or a salt thereof.
22-26. (canceled)
A method of treating HIV-1 infection in a subject in need thereof, said method comprising administering brown algae or an extract thereof to said subject in an amount sufficient to treat said infection.
(canceled)
A method of treating HIV-1 infection in a subject in need thereof, said method comprising administering an isolated bioactive fraction of a Sargassum fusiforme extract to said subject in an amount sufficient to treat said infection.
A method of treating HIV-1 infection in a subject in need thereof, said method comprising administering substantially pure saturated fatty acid, or a salt or ester thereof, to said subject in an amount sufficient to treat said infection.
A pharmaceutical composition comprising an isolated bioactive fraction of a Sargassum fusiforme extract and a pharmaceutically acceptable excipient.
A pharmaceutical composition comprising substantially pure palmitic acid, or a salt or ester thereof, and a pharmaceutically acceptable excipient.
45-53. (canceled)
A method of treating an HIV or herpes infection in a subject in need thereof, said method comprising administering to said subject linoleic acid, or a salt or ester thereof, in an amount sufficient to treat said infection.
A method of treating an HIV or herpes infection in a subject in need thereof, said method comprising administering to said subject oleic acid, or a salt or ester thereof, in an amount sufficient to treat said infection.
A method of treating an HIV or herpes infection in a subject in need thereof, said method comprising administering to said subject a mixture of (i) oleic acid, or a salt or ester thereof, and (ii) linoleic acid, or a salt or ester thereof, simultaneously or within 14 days of each other in amounts that together are sufficient to treat the infection.
A method of inhibiting the transmission of HIV or herpes infection between a first subject and a second subject, said method comprising topically applying to said first subject linoleic acid, or a salt or ester thereof, in an amount effective to inhibit said transmission.
A method of inhibiting the transmission of HIV or herpes infection between a first subject and a second subject, said method comprising topically applying to said first subject oleic acid, or a salt or ester thereof, in an amount effective to inhibit said transmission.
A method of inhibiting the transmission of HIV or herpes infection between a first subject and a second subject, said method comprising topically applying to said first subject a mixture of (i) oleic acid, or a salt or ester thereof, and (ii) linoleic acid, or a salt or ester thereof, simultaneously or within 14 days of each other in amounts that together are effective to inhibit said transmission.
60-63. (canceled)
Dependencies are inferred from the claim text.