Epigenetic modification of fungi and uses thereof

Patent metadata

Field	Value
Publication number	US-2022136019-A1
Application number	US-202117406025-A
Country	US
Kind code	A1
Filing date	Aug 18, 2021
Priority date	Aug 16, 2018
Publication date	May 5, 2022
Grant date	—

Abstract

Described herein are methods of epigenetic modification of fungi and uses thereof. Also described herein are compounds that can have antileishmanial activity and formulations thereof. Also described herein are methods of treating leishmanial infection in a subject that include the step of administering a compound or formulation thereof described herein to the subject.

First claim

1 . A method of producing compounds in a fungus, the method comprising: culturing a population of fungal cells in vitro;
exposing the population of fungal cells to an epigenetic modulator; and extracting compounds from the population of fungal cells to obtain extracted compounds.

2 . The method of claim 1 , wherein the culturing is performed in a media, wherein the media is rice, action agar glycerol, potato dextrose+agar, Sabaurough dextrose broth+agar, or malt broth+agar.

3 . The method of claim 1 , wherein the culturing is performed at a temperature of about 20° C. to about 40° C.

4 . (canceled)

5 . The method of claim 1 , wherein the culturing is performed with an amount of fungus pieces inoculated, wherein the amount is about 1 piece to about 10 pieces.

6 . The method of claim 1 , wherein the culturing is performed at acidic or basic pH.

7 . The method of claim 1 , wherein the culturing is performed at a salinity of about 0.0001% to about 1%.

8 . The method of claim 1 , wherein the culturing is performed for a cultivation period of about 7 days to about 40 days.

9 . The method of claim 1 , further comprising the step of partitioning the extracted compounds to obtain partitioned compounds.

10 . The method of claim 1 , further comprising purifying the extracted compounds to obtain purified compounds.

11 . The method of claim 10 , wherein the purified compounds comprise Compound (1):

12 . The method of claim 10 , wherein purification is carried out using liquid chromatography.

13 . The method of claim 1 , wherein the fungus is an endophytic fungus.

14 . The method of claim 1 , wherein the fungus is a mangrove fungus.

15 . The method of claim 1 , wherein the epigenetic modifier is an HDAC inhibitor

16 . The method of claim 1 , wherein the epigenetic modifier is a DNMT inhibitor

17 . A composition comprising Compound (1)

18 . The composition of claim 17 , wherein the composition comprises an amount of Compound 1 effective to kill and/or inhibit a leishmanial parasite.

19 . A pharmaceutical formulation comprising:
an amount of Compound (1)

and
a pharmaceutically acceptable carrier.

20 . The pharmaceutical formulation of claim 19 , wherein the amount is an effective amount sufficient to kill a leishmanial parasite, inhibit a leishmanial parasite, or both.

21 . The pharmaceutical formulation of claim 19 , wherein the amount of Compound (1) can range from about 0.01 μg to about 1000 mg or more.

Assignees

• Univ South Florida
• Inst Politecnico Nacional
• Univ King Abdulaziz

Inventors

• Baker Bill J
• Kyle Dennis E
• Rodriguez-Pérez Mario Alberto
• Limon Anne-Claire D
• Azhari Ala

Classifications

• C12N1/14

  Fungi (culture of mushrooms A01G18/00; as new plants A01H15/00); Culture media therefor · CPC title

• C12R2001/645

  Fungi {; Processes using fungi} · CPC title

• C12P17/181 Primary

  Heterocyclic compounds containing oxygen atoms as the only ring heteroatoms in the condensed system, e.g. Salinomycin, Septamycin · CPC title

• Y02A50/30

  Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change · CPC title

• A61K31/366 Primary

  having six-membered rings, e.g. delta-lactones · CPC title