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    ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION
    7.
    发明申请
    ANTIPSYCHOTIC AGENTS AND STANDARDIZED ANTIPSYCHOTIC FRACTIONS FROM RAUWOLFIA TETRAPHYLLA AND PROCESS OF THEIR ISOLATION 有权
    来自RAUWOLFIA TETRAPHYLLA的抗菌药物和标准化抗肿瘤药物及其分离方法

    公开(公告)号：US20120184576A1

    公开(公告)日：2012-07-19

    申请号：US13262040

    申请日：2010-03-31

    申请人： Santosh Kumar Srivastava ,  Ashok Kumar Agrawal ,  Subhash Chandra Singh ,  Vinay Kumar Khanna ,  Janardan Singh ,  Chandeshwar Nath ,  Madan Mohan Gupta ,  Shikha Gupta ,  Ram Kishor Verma ,  Anirban Pal ,  Duyaneshwar Umrao Bawankule ,  Dharmendra Saikia ,  Anil Kumar Gupta ,  Anupam Maurya ,  Suman Preet Singh Khanuja

    发明人： Santosh Kumar Srivastava ,  Ashok Kumar Agrawal ,  Subhash Chandra Singh ,  Vinay Kumar Khanna ,  Janardan Singh ,  Chandeshwar Nath ,  Madan Mohan Gupta ,  Shikha Gupta ,  Ram Kishor Verma ,  Anirban Pal ,  Duyaneshwar Umrao Bawankule ,  Dharmendra Saikia ,  Anil Kumar Gupta ,  Anupam Maurya ,  Suman Preet Singh Khanuja

    IPC分类号： A61K31/4375 ,  C07D455/00 ,  A61P25/18 ,  A61K31/475

    CPC分类号： A61K36/24

    摘要： 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 alkabids 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=β-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).

    摘要翻译： 本发明涉及生物活性提取物，其部分和化合物从萝卜（Rauwolfia tetraphylla）分离。 基于动物模型的体内验证和针对抗精神病活性的多巴胺能D2，胆碱能（毒蕈碱）和血清素能（5HT2A）受体的比例结合亲和力，提取物和级分可用于治疗精神病。 本发明涉及式1和2的叶生物碱中的新型抗精神病活性，命名为四氢奥斯汀，10-甲氧基四氢奥斯汀，异丙基苯胺，10-脱乙氧基去甲苯胺，11-去甲氧基甲苯吡胺，储存蛋白和α-育亨宾。 本发明还涉及获得抗精神病药提取物以及分离来自罗非草（Rauwolfia tetraphylla）的叶子的式1和2的烷烃的方法。 本发明特别涉及在四氢叶酸甲酯的MeOH提取物，乙酸乙酯和氯仿级分中以及在分离的化合物α-育亨宾，储存器中和以1:1.5比例混合的10-脱甲氧基对苯二胺和11-脱甲氧基苯甲苯胺中的显着的抗精神病活性，用于治疗 精神病没有任何额外的锥体症状（EPS）。 R1 = R2 = OMe R3 =＆bgr; -H（Isoreserpiline）2.R1 = R2 = OMe R3 =＆bgr; -H（Reserpiline）“3。 R1 = OMe R2 = HR3 =＆bgr; -H（11-甲氧基乙酰胺）“4.R1 = H R2 = OMe R3 =＆bgr; -H（10-甲氧基乙胺） R1 = R2 = H R3 =α-H（四氢奥斯汀）* 7。 R1 = OMe R2 = H R3 =α-H（10-甲氧基四胡司汀）。

    Method for maximization of artemisinin production by the plant artemisia annua
    8.
    发明授权
    Method for maximization of artemisinin production by the plant artemisia annua 失效
    青蒿植物青蒿素生产最大化的方法

    公开(公告)号：US06393763B1

    公开(公告)日：2002-05-28

    申请号：US09538892

    申请日：2000-03-30

    申请人： Sushil Kumar ,  Shiv Kumar Gupta ,  Madan Mohan Gupta ,  Ram Kishor Verma ,  Dharam Chand Jain ,  Ajit Kumar Shasany ,  Mahendra Pandurang Darokar ,  Suman Preet Singh Khanuja

    发明人： Sushil Kumar ,  Shiv Kumar Gupta ,  Madan Mohan Gupta ,  Ram Kishor Verma ,  Dharam Chand Jain ,  Ajit Kumar Shasany ,  Mahendra Pandurang Darokar ,  Suman Preet Singh Khanuja

    IPC分类号： A01B7900

    CPC分类号： A01H3/00

    摘要： The invention provides a method for maximization of artemisinin yield of the plant Artemisia annua, said method comprising sowing seeds of Artemisia annua plant on raised bed nursery during second and third week of December and maintaining the moisture throughout; transplanting seedlings thus obtained bearing at least 5-15 leaves into the main field fertilized with fertilizer, preferably NPK @ 80,40,40 kg/ha to achieve a population density of 50,000 to 200,000 per ha followed by light irrigation in the second week of March and irrigation every fortnight thereafter; harvesting the crop four times by cutting the plant tops leaving 75-100 cm part of plant for further regeneration, the said harvests are performed in a manner that the first harvest is done in fourth week of May, second harvest in third week of July, third harvest in second week of September and fourth harvest in third week of October of each year; and at each harvesting time care is taken to care at least one green branch, and extracting artemisinin from the plant tissue immediately after each harvest.

    摘要翻译： 本发明提供了一种使青蒿植物青蒿素产量最大化的方法，所述方法包括在12月的第二和第三周在秧苗上播种蒿种子，并保持水分; 将由此获得的至少5-15叶的幼苗移植到用肥料施肥的主田中，优选为80,40,40kg / ha的NPK，以实现每公顷50,000至20万的人口密度，然后在第二周进行轻度灌溉 三月份之后每两周灌溉一次; 通过切割植物顶部将作物收割四次，留下75-100cm部分的植物进行进一步再生，所述收获的进行方式是在5月的第4周进行第一次收获，在7月的第3周进行第二次收获， 9月第二周第三次收获，每年10月第三周收获第四季; 并且在每个收获时间处理至少一个绿色分支，并且在每次收获后立即从植物组织中提取青蒿素。