Plant extracts enriched with ipolamiide derivatives as immunosuppressants for treating immunological disorders

1 . A compound of compound VII as follows:

2 . A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable vehicle.

3 . The pharmaceutical composition according to claim 2 , further comprising ipolamiide.

4 . A process for preparing an extract enriched with a compound of claim 1 , comprising:

a) selecting an input vegetal biomass with a content of ipolamiide between 2.5% and 3.5% obtained from plants of the genus Stachytarpheta;

b) submitting the input vegetal biomass from step a) to oven drying at temperature between 40° C. to 80° C., until obtaining the humidity stabilization between 10 to 12%;

c) milling the oven dried vegetal biomass from step b;

d) performing an extraction of the vegetal biomass through the steps of:

i. heating the vegetal biomass at a temperature between 70° C. to 100° C., with constant stirring;

ii. macerating the vegetal biomass at room temperature; and

iii. heating of the vegetal biomass at a temperature between 70° C. to 100° C.

5 . The process according to claim 4 , further comprising:

iv. filtering and concentrating the extract; and

V. drying in a spray dryer for 1 to 60 seconds, wherein the spray dryer has an inlet temperature between 155° C. and 165° C. and outlet temperature between 85° C. to 95° C., coupled to a dehumidifier.

6 . The process according to claim 4 , in which the vegetal biomass heating of d) occurs for 5 to 30 minutes.

7 . The process according to claim 4 , in which the vegetal biomass heating of d) occurs for 5 to 15 hours.

8 . The process according to claim 4 , in which the input vegetal biomass comprises the aerial parts of the plants of the genus Stachytarpheta.

9 . The process according to claim 4 , in which the plant is Stachytarpheta cayennensis.

10 . The process according to claim 4 , in which the process comprises an aqueous extraction.

11 . The process according to claim 4 , further comprising predicting the theoretical content of ipolamiide and compound of formula C in the extract from the actual content of ipolamiide in the input vegetal biomass using Equation I:

% Theoretical content of ipolamiide and derivatives in the extract=% Actual content of ipolamiide in the vegetal biomass×DER/(actual content of ipolamiide and derivatives in the extract/actual content of ipolamiide in the input vegetal bio-mass>)±standard deviation  (Equation I),

Equation 1;

wherein the compound of formula C has the following formula:

wherein R corresponds to H, OH, OGlyc (Glycoside); R 1 , R 1′ , R 1″ correspond to H, OH; R 2 corresponds to H, COOH, COOCH 3 , CH 3 , CHO; R 3 corresponds to H, OH, CH 3 ; R 4 , R 4′ correspond to H, OH, CH 2 OH, CH 3 .

12 . A composition comprising one or more extracts obtained from the plants of the genus Stachytarpheta and the compound according to claim 1 .

13 . A composition, which is enriched with one or more compounds obtained by the process according to claim 5 .

14 . The composition of claim 12 , which comprises from 1% to 20% of ipolamiide or 1% to 20% of the compound of formula C

wherein the compound of formula C has the following formula:

wherein R corresponds to H, OH, OGlyc (Glycoside); R 1 , R 1′ , R 1″ correspond to H, OH; R 2 corresponds to H, COOH, COOCH 3 , CH 3 , CHO; R 3 corresponds to H, OH, CH 3 ; R 4 , R 4′ correspond to H, OH, CH 2 OH, CH 3 .

15 . The compound of claim 1 , wherein the compound is prepared by a process comprising:

a) selecting an input vegetal biomass with a content of ipolamiide between 2.5% and 3.5% obtained from one or more plants of the genus Stachytarpheta;

b) submitting the input vegetal biomass from a) to oven drying at temperature between 40° C. to 80° C., until obtaining humidity stabilization between 10% to 12%;

c) milling the oven dried vegetal biomass from b);

d) preforming an extraction of the vegetal biomass comprising:

i. heating the vegetal biomass at a temperature between 70° C. to 100° C., with constant stirring;

ii. macerating the vegetal biomass at room temperature; and

iii. heating the vegetal biomass at a temperature between 70° C. to 100° C.;

thereby obtaining an ipolamiide compound; and

e) performing acid hydrolysis on the ipolamiide compound at a temperature between 35-40° C.