Antipsychotic agents and standardized antipsychotic fractions from rauwolfia tetraphylla and process of their isolation
The present invention relates to bioactive extracts its fractions and isolation of compound from RauwolSa 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, Cholinerg...
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| creator | JANARDAN SINGH ASHOK KUMAR AGRAWAI ANIRBAN PAL DNYANESHWAR UMRAO BAWANKULE RAM KISHOR VERMA SHIKHA GUPTA SUBBASH CHANDRA SINGH ANIL KUMAR GUPTA MADAN MOHAN GUPTA DHARMENDRA SAIKIA SANTOSH SRIVASTAVA ANUPAM MAURYA CHANDESHWAR NATH SUMAN PREET SINGH KHANUJA VINAY KUMAR KHANNA |
| description | The present invention relates to bioactive extracts its fractions and isolation of compound from RauwolSa 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). º1. R1=R2 = OMe R3 = α-H (Isoreserpiline) º 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) |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_GB2481179A</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>GB2481179A</sourcerecordid><originalsourceid>FETCH-epo_espacenet_GB2481179A3</originalsourceid><addsrcrecordid>eNqFjL0KwkAQhNNYiPoM7gtYRAW1jOLPA9iH5bJnFs7b43YlxKc3ioWdzcwwfDPjoquicdLetWLsAG8UTQFjA2qDYm74Sc1Q_FI-ozOWqEOSO2R8dBI8IxhZxtT2IeDnI2VxpAriwVriDKwS8D2dFiOPQWn29UkxPx2vh8uCktSkCR1Fsvq8X663ZbnZVav_xAtID0am</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>Antipsychotic agents and standardized antipsychotic fractions from rauwolfia tetraphylla and process of their isolation</title><source>esp@cenet</source><creator>JANARDAN SINGH ; ASHOK KUMAR AGRAWAI ; ANIRBAN PAL ; DNYANESHWAR UMRAO BAWANKULE ; RAM KISHOR VERMA ; SHIKHA GUPTA ; SUBBASH CHANDRA SINGH ; ANIL KUMAR GUPTA ; MADAN MOHAN GUPTA ; DHARMENDRA SAIKIA ; SANTOSH SRIVASTAVA ; ANUPAM MAURYA ; CHANDESHWAR NATH ; SUMAN PREET SINGH KHANUJA ; VINAY KUMAR KHANNA</creator><creatorcontrib>JANARDAN SINGH ; ASHOK KUMAR AGRAWAI ; ANIRBAN PAL ; DNYANESHWAR UMRAO BAWANKULE ; RAM KISHOR VERMA ; SHIKHA GUPTA ; SUBBASH CHANDRA SINGH ; ANIL KUMAR GUPTA ; MADAN MOHAN GUPTA ; DHARMENDRA SAIKIA ; SANTOSH SRIVASTAVA ; ANUPAM MAURYA ; CHANDESHWAR NATH ; SUMAN PREET SINGH KHANUJA ; VINAY KUMAR KHANNA</creatorcontrib><description>The present invention relates to bioactive extracts its fractions and isolation of compound from RauwolSa 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). º1. R1=R2 = OMe R3 = α-H (Isoreserpiline) º 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)</description><language>eng</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2011</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20111214&DB=EPODOC&CC=GB&NR=2481179A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25564,76547</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=20111214&DB=EPODOC&CC=GB&NR=2481179A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>JANARDAN SINGH</creatorcontrib><creatorcontrib>ASHOK KUMAR AGRAWAI</creatorcontrib><creatorcontrib>ANIRBAN PAL</creatorcontrib><creatorcontrib>DNYANESHWAR UMRAO BAWANKULE</creatorcontrib><creatorcontrib>RAM KISHOR VERMA</creatorcontrib><creatorcontrib>SHIKHA GUPTA</creatorcontrib><creatorcontrib>SUBBASH CHANDRA SINGH</creatorcontrib><creatorcontrib>ANIL KUMAR GUPTA</creatorcontrib><creatorcontrib>MADAN MOHAN GUPTA</creatorcontrib><creatorcontrib>DHARMENDRA SAIKIA</creatorcontrib><creatorcontrib>SANTOSH SRIVASTAVA</creatorcontrib><creatorcontrib>ANUPAM MAURYA</creatorcontrib><creatorcontrib>CHANDESHWAR NATH</creatorcontrib><creatorcontrib>SUMAN PREET SINGH KHANUJA</creatorcontrib><creatorcontrib>VINAY KUMAR KHANNA</creatorcontrib><title>Antipsychotic agents and standardized antipsychotic fractions from rauwolfia tetraphylla and process of their isolation</title><description>The present invention relates to bioactive extracts its fractions and isolation of compound from RauwolSa 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). º1. R1=R2 = OMe R3 = α-H (Isoreserpiline) º 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. 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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). º1. R1=R2 = OMe R3 = α-H (Isoreserpiline) º 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)</abstract><oa>free_for_read</oa></addata></record> |
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| subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS |
| title | Antipsychotic agents and standardized antipsychotic fractions from rauwolfia tetraphylla and process of their isolation |
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