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题名: 1. 三种药用植物的化学成份和生物活性;2. 硝基烯类化合物合成与抗HIV-1 RT活性
作者: 江志勇
学位类别: 博士
答辩日期: 2005
授予单位: 中国科学院昆明植物研究所
授予地点: 中国科学院昆明植物研究所
导师: 周俊
关键词: 化学成份 ; 生物活性 ; 泽泻 ; 积雪草 ; 青钱柳 ; 硝基烯 ; 抗HBV活性 ; 抗抑郁活性 ; 降血糖活性 ; 抗HIV- IRT活性
中文摘要: 本论文共分为五章。第一章对泽泻科植物泽泻(A lisma orientalis Juzep.)的化学成份分离,结构鉴定以及部分化合物的抗HBV活性进行了研究。第二章对伞形科植物积雪草(Centella asiatica(L.)Urban.)的进行了化学成份分离、结构鉴定和抗忧郁行为活性研究。第三章介绍了民间药用植物青钱柳〔Cyclocarya paliurus(B atal.)Ijinakaja]叶的化学成份分离与结构鉴定,同时报告了有效部分的降血糖活性及毒性。从以上三种植物中分离鉴定了52个化合物,主要包括三菇及其昔,黄酮及其昔,倍半菇,长链脂肪烃,幽醇等。其中新化合物n个(9个为三猪类化合物,2个为倍半菇)。第四章报告了27个硝基烯类伽itroolefins,NoF)化合物的合成以及抗HIV-RT的活性研究。提示硝基烯类可作为抗HIV类药物的前体。第五章介绍了糖尿病的分型,发病机理,临床症状,同时总结了目前各类治疗糖尿病药物的作用机理及其毒副作用,并就当前中医药治疗糖尿病研究概况作了综述。第一章泽泻的化学成份及其抗HBv活性中药泽泻是泽泻科植物泽泻(Alismoorientalis JuzeP)的块茎,为常用中药。除有利尿,清湿热作用外,还具明显的降血脂、抑制动脉粥样硬化及抗脂肪肝的功效。为寻找活性成份,对泽泻的化学成份进行了研究,从中分离鉴定了20个化合物,其结构分别为:泽泻醇A(l),24-乙酰泽泻醇A侈),25一脱水泽泻醇A(3),13,17·环氧泽泻醇A(4),23·乙酞泽泻醇B(5),泽泻醇F(6),24-乙酰泽泻醇F(7)·泽泻醇0(8),25-脱水泽泻醇F(9),23-乙酞泽泻醇E(10),熊果酸(l1),allemoxid以12),alismolz(l3),泽泻菇醇E(14),泽泻菇醇J(15),泽泻砧醇K(16),lβ,4β,7β,11-四轻基按烷(17),mucrolidin(18),β-谷幽醇(19),胡萝卜贰(2 0).其中8,9,15,16为四个新化合物。对其中量大的化合物进行了抗HBV(h ePatitis B virus)活性研究。结果表明:泽泻醇A(1)和24-乙酞泽泻醇F(7)具有较好的抗HBv活性,对2.2.15细胞分泌表面抗原(HBsAg)和e抗原(H BeAg)抑制作用的选择指数(51)较大,化合物1:sIHBsg>641,sIHBeAg=57.24;化合物7:sIHBsg=18·63,SIHBeAg=28.15。化合物2-6,16也表现出对2·2·15细胞的HBsAg和HBeAg分泌有一定的抑制作用。对化合物1还进行了抗鸭乙肝病毒 (DHBV)活性研究,结果表明化合物1对DHBV有明显的抑制作用。这是我们首次发现该类化合物具有抗HBV活性,并已将活性最好的化合物申请了专利。第二章积雪草化学成份和抗抑郁行为活性中药积雪草(Centella asiatica)为伞形科植物,其主要功效是促进伤口愈合。其中三菇及其昔是主要活性成份。近期研究证明,积雪草中的三菇总皂昔和轻基积雪草酸具有一定的抗抑郁(dePressana)作用。为了深入研究其抗抑郁活性化合物,对积雪草的全草进行了化学成份研究,从中分离鉴定了16个化合物,它们的结构为:积雪草酸(1),p-谷幽醇(2),积雪草酸23-a-D-毗喃半乳糖昔 (3),轻基积雪草酸(4),medasiatic acid(5),3p,6p,23-三轻基齐墩果-12-烯-28酸(邓,6),邓,6p,23·三轻基熊果-12-烯-28酸(7),胡萝卜贰(8),积雪草昔(9),轻基积雪草普(10),scheffurosideB(11),积雪草普C(12),积雪草昔D(13),积雪草普E(14),积雪草昔F(15),其中化合物3,12-巧为5个新的三菇皂 昔,其研究结果已发表。对其中量大的化合物进行了抗抑郁行为学研究,结果表明在10mg/kg剂量时,三菇皂普9,10,12,15均有较好的活性,而昔元化合物4也有很好的抗抑郁活性。相关的深入研究正在进行中。第三章青钱柳的化学成份及其降血糖活性青钱柳「Cyclocarya paliurus(B atal.) ljinakaja]为我国特有的单种属植物。其叶有降血糖、降血压、清热解暑等功效。为了寻找其中的抗糖尿病活性成份,对其叶的化学成份进行了研究,从中分离得到16个化合物,其结构分别为:青钱柳苷B(1),青钱柳苷C(2),青钱柳苷A(3),青钱柳苷I(4),pterocarmosideA(5), pterocaryosideB(6),青钱柳着I戈(7),aroUnolic acid(8)·3p-droxyglutin-5-ene(9),afzelin(10),山奈酚-3-β·D-目比喃葡萄糖着(11),异棚皮昔(12),hyperoside(13),胡萝卜贰(14),β-谷幽醇(15),13-二甲基-2-14酮(16)。其中1,2为两个新的三菇皂昔(有关论文已经被接受发表在亚洲天然产物研究杂志上)。在此基础上我们对该植物的降血糖活性成份的工艺和质量标准进行了研究,建立了有效成份的生产方法和初步质量标准,生产出制剂JCz。随后对JCZ进行了抗糖尿病的活性和毒性研究,结果表明JCz对肾上腺素糖尿病小鼠和四氧喷吮糖尿病大鼠均有较好的降血糖作用,对正常小鼠血糖无影响,安全性好。第四章硝基烯类化合物的合成及其抗HIV- IRT活性 硝基烯类化合物是一类迄今为止尚未报道的抗Hl华1逆转录酶(RT)的化合本章介绍了27个硝基烯类化合物的合成及其对HIV-IRT抑制活性的测定,结果表明芳环上的取代位置和取代基的性质均会影响硝基烯类化合物抗HIV-1RT的活性。提示硝基烯类可作为抗HW类药物的前体。第五章综述 本章介绍了糖尿病的分型,发病机理,临床症状,概述了目前治疗糖尿病药物胰岛素,磺脉类药物,双肌类药物,-葡萄糖普酶抑制剂,醛糖还原酶抑制剂,胰岛素增敏剂和血糖调节剂的作用机理及毒副作用。最后对中草药抗糖尿病研究进展进行了综述。
英文摘要: The dissertation consists of five chapters. Chapter 1, 2 and 3 focused on the chemical constituents and bioactivities about anti-HBV, antidepressant, and anti-hyperglycemic activities of Alisma orientalis Juzep., Centella asiatica (L.) Urban, and Cyclocarya paliums (Batal.) Ijinakaja. Fifty-two compounds including eleven new ones were isolated from the three medicinal plants and identified based on spectral data [IR, *H NMR, 13C NMR, 2D NMR (HMQC, HMBC, COSY, ROESY)] and physical constants, and were classfied into triterpenes and glycosides, flavanones and glycosides, sesquiterpenoids, steroids and so on. Chapter 4 reported the synthesis of 27 nitroolefins and their anti-HIV-1 RT activities. The last chapter outlined the categories of diabetes mellitus (DM), the causes of DM, clinical medicines for DM and their side-effects, together with the research development of traditional Chinese medicines for DM. Chapter 1. The Chemical Constituents from Alisma orientalis and Their Anti-HBV Activities The rhizome of Alisma orientalis Juzep is a traditional Chinese medicine used for diuretic, hypolipidemic, and antipyretic. To search for an active compound, the rhizomes of A. orientalis were investigated to afford twenty compounds mainly including protostane-type triterpenes, guaiane-type sesquiterpenes and eudesmane-type sesquiterpenes. Based on spectral analysis (IR, MS, ID- and 2D-NMR) and comparison with known compounds, they were characterized to be alisol A (1), alisol A 24-acetate (2), 25-anhydroalisol A (3), 13p, 17(i-epoxyalisol A (4), alisol B 23-acetate (5), alisol F (6), alisol F 24-acetate (7), 25-anhydroalisol F (8), alisol O (9), alisol E 23-acetate (10), ursolic acid (11), alismoxide (12), alismol (13), orientaol E (14), orientaol J (15), orientaol K (16), 1(3, 4p, 7(3, 11 - tetrahydroxyeudesmane (17), mucrolidin (18), (3-sitosterol (19), and daucosterol (20), of which compound 8, 9, 15, and 16 were new ones. The anti-HBV bioassay suggested alisol A (1) and alisol F 24-acetate (7) possess significantly anti-HBV activities, the SI (selectivity index) values to HBsAg and HBeAg for compound 1 and respectively. Compounds 2-6 also showed activities of anti-HBeAg. An anti-DHBV DNA bioassay indicated alisol A (1) had a potency of anti-HBV activity. This is the first time to report the ant-HBV activity of compounds 1-7, which results had been applied the Chinese patent. Chapter 2. The Chemical Constituents from Centella asiatica and Their Antidepressant Activities Centella asiatica has been used for wound-healing. Of the chemical constituents from C. asiatica, the triterpenes and their glycosides are the active compounds. To search for an active antidepressant compound, the whole plant of C. asiatica were investigated to afford sixteen compounds which were elucidated as asiatic acid (1), P-sitosterol (2), asiatic acid 23-O-a-D-galactopyranoside (3), madecassic acid (4), medasiatic acid (5), 3p, 6(3, 23-trihydroxyolean-12-en-28-oic acid(6), 3p, 6p, 23-trihydroxyurs-12-en-28-oic acid (7), daucosterol (8), asiaticoside (9), madecassoside (10), scheffiiroside B (11), a'siaticoside C (12), asiaticoside D (13), asiaticoside E (14), asiaticoside F (15), of which compounds 3,12,13,14 and 15 were new ones. The antidepressant bioassay suggested the tested triterpene glycosides (9, 10, 12, 15) and an aglycone (4) had a significantly antidepressant activity at the dose of 10 mg/kg by forced-swimming test. Chapter 3. The Chemical Constituents from Cyclocarya paliurus and Anti -hyperglycemic Effects Cyclocarya paliurus is an endemic species growing in the Southern China, and its leaves can be used for the treatment of anti-diabetes, anti-hypertention and so on. To reveal an active compound for anti-diabetes, the leaves of C. paliurus were investigated to obtain sixteen compounds which were identified to be cyclocarioside B (1), cyclocarioside C (2), cyclocarioside A(3) [11], cyclocarioside I (4), pterocaryoside A (5), pterocaryoside B (6), cyclocarioside I A2 (7), arjunolic acid (8), 3p-hydroxyglutin-5-ene (9), afzelin (10) [22] [23], kaempferol - 3 - O - p - D -glucopyranoside (11), isoquercitrin (12), hyperoside (13), daucosterol (14), p-sitosterol (15), and 3,13-dimethyl-2-ketone-14 alkyl (16). On the other hand, JCZ, the active fraction from C. paliurus, was bioassayed for anti-hyperglycemic effects and acute toxicity. The results showed that JCZ can reduce the glucose level of the diabetic mice model caused by adrenalin and the diabetic rat model caused by alloxan, Chapter 4. The Synthesis ofNitroolefms (NOF) and Their Anti-HIV-1 RT Activities Nitroolefins(NOFs) are a lead compound inhibiting HIV-1 RT reported so far by our group. Herein, the synthesis of 27 NOFs were synthesized and the anti-HIV-1 RT activity were investigated. The relationship between structure and activity was obviously revealed, which suggested that the NOF can be considered as a pre-drug against HIV/AIDS. Chapter 5. Review on Diabetes In this chapter, the categories of diabetes mellitus (DM), the causes of DM, clinical medicines for the treatment of DM and their side-effects were reviewed, together with the advance of anti-diabetic traditional Chinese herbs.
语种: 中文
内容类型: 学位论文
URI标识: http://ir.kib.ac.cn/handle/151853/772
Appears in Collections:昆明植物所硕博研究生毕业学位论文_学位论文

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1. 三种药用植物的化学成份和生物活性;2. 硝基烯类化合物合成与抗HIV-1 RT活性.江志勇[d].中国科学院昆明植物研究所,2005.20-25
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