Cellular senescence activating compounds
AssigneesUniversidad Nacional Autonoma De Mexico, Guayulera San Salvador Y Plantas Del Desierto Spr De Rl De Cv
InventorsZaira TAVARES SANTAMARIA, Mariano MARTINEZ VAZQUEZ, Nadia Judith JACOBO HERRERA, Leticia ROCHA ZABALETA, Alejandro ZENTELLA DEHESA, Beatriz del Carmen COUDER GARCIA
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Abstract
The present invention describes a naturally occurring chemical compound, specifically guayulins A, B, C and D used in medicine having null cytotoxicity and genotoxicity on healthy lymphocyte cells. Said active compounds interfere with the inflammatory process and have antitumoral activity in human cancer cell lines, since they inhibit their growth through a senescence process.
Claims22
A guayulin compound A, B, C and D called:
- Argentatines A and C,
- Isoargentine B and
- Argentatine D, of formula (I) and (I′) that present null cytotoxicity or genotoxicity on healthy lymphocytic cells in an In vivo animal model, characterized in that it presents anti-inflammatory activity, inhibits the growth of cancer cells through a senescence process;
- wherein the compound of formula (I):
- (A)-(B)-(C)
- wherein:
- A is a group that is selected from one of:
- B is
- and
- C is a group that is selected from one of:
- and where:
- R1 represents a group that is selected from:
- R2 represents a group that is selected from:
- R3 represents a group that is selected from:
- R4 represents a group selected from:
- —OH,
- and wherein:
- R1 and R3 can be at the same time ;
- R3 and R4 can be at the same time —OH or —OAc;
- R1 and R2 are not at the same time
- and —Br, respectively;
- R5 is a group that is selected from one of:
- H, CH3, or an alkyl chain, and wherein
- when A is
- then R1 is not
- and R2 is not —Br, and R3 and R4 are at the same time a group selected from —OH or —OAc;
- when C is
- then R1 and R3 can be at the same time ═O and R2 is not —Br;
- or
- when A is
- then R1 and R2 can together form a group
- and enantiomers, diastereoisomers, mixtures of enantiomers, mixtures of diastereoisomers, anomers, hydrates, solvates, polymorphs, of the aforementioned compounds and pharmaceutically acceptable salts thereof,
- And the compound of formula (I′):
- (A)-(B)-T
- wherein:
- A and B have the meanings as defined above,
- R1 represents a group that is selected from:
- ═O,
- R2 represents a group that is selected from:
- R3 represents a group that is selected from:
- and wherein:
- R1 and R3 can be at the same time ═O;
- R1 and R2 are not at the same time
- and —Br, respectively;
- R5 is a group that is selected from one of:
- H, CH3, or an alkyl chain, and wherein
- when A is
- then R1 is not
- and R2 is not —Br;
- when A is
- then R1 and R2 can together
- form a group
- and where T represents a group
- and enantiomers, diastereoisomers, mixtures of enantiomers, mixtures of diastereoisomers, anomers, hydrates, solvates, polymorphs, of the aforementioned compounds and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.