Plant extracts enriched with ipolamiide derivatives as immunosuppressants for treating immunological disorders
AssigneeAché LaboratóRios FarmacêUticos S.A.
InventorsCristiano Ruch Werneck Guimaraes, Carlos Eduardo Vitor, Lisandra Ravanelli Pessa, Romulo Dragani Reis, Alessandra Mascarello, Fernando Henrique De Souza Gama
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Abstract
The invention describes extracts from plants of the genus Stachytarpheta enriched with ipolamiide derivatives as immunosuppressants for treating immunological disorders. The isolated active compounds and a process of producing these are also disclosed.
Claims32
Compounds comprising the general formula:
- wherein R corresponds to H, OH, OGlyc (Glycoside);
- R1, R1′, R1″ correspond to H, OH;
- R2 corresponds to H, COOH, COOCH3, CH3, CHO;
- R3 corresponds to H, OH, CH3;
- R4, R4′ correspond to H, OH, CH2OH, CH3;
- R5, R5′ correspond to H, CH3, COOCH3, CHO, CH2OH;
- R6 corresponds to CHO, COOH, COOCH3;
- R7 corresponds to H, CH3;
- R8, R8′, R8″ correspond to CHO, CH3, CH2OH, COOH and the dashed bonds represent single (C—C) or double (C═C) bonds between carbons (up to two double bonds per structure).
Method of treatment of immune disorders, comprising the step of administering to a patient one compound of general formula (I), (II) and/or (III), in sufficient amount to provide immunosuppressive effect.
Pharmaceutical composition comprising compounds derived from ipolamiide for the treatment of immune disorders, wherein the compounds comprise at least one compound selected from the group that comprises:
- wherein R corresponds to H, OH, OGlyc (Glycoside);
- R1, R1′, R1″ correspond to H, OH;
- R2 corresponds to H, COOH, COOCH3, CH3, CHO;
- R3 corresponds to H, OH, CH3;
- R4, R4′ correspond to H, OH, CH2OH, CH3;
- R5, R5′ correspond to H, CH3, COOCH3, CHO, CH2OH;
- R6 corresponds to CHO, COOH, COOCH3;
- R7 corresponds to H, CH3;
- R8, R8′, R8″ correspond to CHO, CH3, CH2OH, COOH and the dashed bonds represent single (C—C) or double (C═C) bonds between carbons (up to two double bonds per structure);
- and
- d) pharmaceutically acceptable vehicle.
Process for production of active compounds comprising the step of subjecting at least one ipolamiide compound to a heating step at high temperatures in a suitable solvent for a time sufficient to obtain the ipolamiide derivatives of formula (I), (II) and/or (III).
Process for production of extract enriched with compounds derived from ipolamiide comprising the steps of:
- a) selecting input vegetal biomass with a content of ipolamiide between 2.5% and 3.5% obtained from plants of the genus Stachytarpheta;
- b) submitting the selected biomass from a) to oven drying at temperature between 40 to 80° C., until obtaining the humidity stabilization between 10 to 12%;
- c) milling the vegetal biomass;
- d) performing the extraction of the vegetal biomass through the steps of:
- i. heating of the vegetal biomass at a temperature between 70 to 100° C., with constant stirring;
- ii. maceration of the vegetal biomass at room temperature;
- iii. heating of the vegetal biomass with temperature between 70 to 100° C.
Standardized extracts, wherein the extracts are obtained from the plants of the genus Stachytarpheta and comprises at least one compound of general formula (I), (II) and/or (III).
Enriched standardized extract fractions from plants of the genus Stachytarpheta comprising at least one compound of general formula (I), (II) and/or (III).
Use of extract and/or standardized fractions comprising compounds derived from ipolamiide of general formula (I), (II) and/or (III), for the manufacture of a medicament with immunosuppressive activity for the treatment of immunological disorders.
Dependencies are inferred from the claim text.