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1. (WO2010113180) ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION

Pub. No.:    WO/2010/113180    International Application No.:    PCT/IN2010/000208
Publication Date: Fri Oct 08 01:59:59 CEST 2010 International Filing Date: Thu Apr 01 01:59:59 CEST 2010
IPC: A61K 36/24
A61P 25/18
Applicants: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
SRIVASTAVA, Santosh, Kumar
AGRAWAL, Ashok, Kumar
SINGH, Subhash, Chandra
KHANNA, Vinay, Kumar
SINGH, Janardan
NATH, Chandeshwar
GUPTA, Madan, Mohan
GUPTA, Shikha
VERMA, Ram, Kishor
PAL, Anirban
BAWANKULE, Dnyaneshwar, Umrao
SAIKIA, Dharmendra
GUPTA, Anil, Kumar
MAURYA, Anupam
KHANUJA, Suman, Preet, Singh
Inventors: SRIVASTAVA, Santosh, Kumar
AGRAWAL, Ashok, Kumar
SINGH, Subhash, Chandra
KHANNA, Vinay, Kumar
SINGH, Janardan
NATH, Chandeshwar
GUPTA, Madan, Mohan
GUPTA, Shikha
VERMA, Ram, Kishor
PAL, Anirban
BAWANKULE, Dnyaneshwar, Umrao
SAIKIA, Dharmendra
GUPTA, Anil, Kumar
MAURYA, Anupam
KHANUJA, Suman, Preet, Singh
Title: ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
Abstract:
The present invention relates to bioactive extracts its fractions and isolation of compound from Rauwolfia tetraphylla. The extracts and fractions are useful for the treatment of psychosis based on in-vivo validation on animal model and proportional binding affinities for dopaminergic - D2, Cholinergic (muscarinic) and Serotonergic (5HT2A) receptors for antipsychotic activity. The present invention relates to novel antipsychotic activity in the leaf alkaloids of Formula 1 and 2 named tetrahydroalstonine, 10-methoxytetrahydroalstonine, isoreserpiline, 10- derαethoxyreserpiline, 11-demethoxyreserpiline, reserpiline and α -yohimbine. The present invention also relates to processes for obtaining antipsychotic extracts as well as for the isolation of alkaloids of formula 1 and 2 from the leaves of Rauwolfia tetraphylla. The present invention particularly relates to significant antipsychotic activity in the MeOH extract, ethylacetate and chloroform fractions of R. tetraphylla and in the isolated compounds α -yohimbine, reserpiline and in a mixture 10- demethoxyreserpiline and 11-demethoxyreserpiline in 1:1.5 ratios for treating psychosis without any extra pyramidal symptoms (EPS).►1. R1=R2 = OMe R3 = α-H (Isoreserpiline) ► 2. R1=R2 = OMe R3 = β-H (Reserpiline) "3. R1 = OMe R2 = HR3 = β-H (11-Demethoxy reserpiline) "4. R1 = H R2 = OMe R3 = β-H (10-Demethoxy reserpiline) "5. R1 = R2 = H R3 = α -H (Tetrahydroalstonine) * 7. R1 = OMe R2 = H R3 = α -H (10-Methoxytetrahudroalstonine).