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1.
乌药茎中鞣质类成分研究I.   总被引:1,自引:0,他引:1  
目的:从樟科药用植物乌药Hndera aggregata(Sims)Kosterm,的茎中分离鞣质类化合物。方法:采用60%丙酮冷浸提取,通过反复SephadexLH-20和MCI-gel CHP 20P柱层析从乌药茎中分离缩合鞣质类化合物,通过波谱解析和理化常数进行结构鉴定。结果:分离得到6个缩合鞣质类化合物并确定其结构:儿茶素( )-cateehin(1);表掊儿茶素(-)-eplgallocatechin(2);epicatechin-(4β-8,2-O-7)-epieatechin(3);epieateehin-(4β,2—O-7)-eatechin(4);表儿茶素(-)-epicatechin(5)epicatechin-(4β-8)-eateehin(6)。结论:化合物3,4和6为首次从该植物中分离得到。  相似文献   

2.
目的: 从樟科药用植物乌药Lindera aggregata (Sims) Kosterm.的茎中分离鞣质类化合物.方法: 采用60%丙酮冷浸提取,通过反复Sephadex LH-20和MCI-gel CHP 20P柱层析从乌药茎中分离缩合鞣质类化合物,通过波谱解析和理化常数进行结构鉴定.结果: 分离得到6个缩合鞣质类化合物并确定其结构:儿茶素(+)-catechin(1);表 儿茶素(-)-epigallocatechin(2);epicatechin-(4β-8,2-O-7)-epicatechin(3);epicatechin-(4β-8,2-O-7)-catechin(4);表儿茶素(-)-epicatechin(5)和epicatechin-(4β-8)-catechin(6).结论: 化合物3,4和6为首次从该植物中分离得到.  相似文献   

3.
目的探讨虎杖Polygonum cuspidatum富集活性组分体外对人类免疫缺陷病毒1型(HIV-1)的抑制作用及作用靶点。方法运用表面等离子共振HIV-1多靶点筛选系统对虎杖不同工艺提取物进行筛选,整合酶氨基耦联柱靶向富集提取物中高活性成分,在TZM-bl细胞和PBMC细胞中对富集产物进行抗HIV-1病毒活性评价;采用荧光共振能量转移分析法测定药物对HIV-1整合酶3’加工的抑制作用;运用高通量ELISA法测定虎杖60%乙醇提取物的整合酶靶向富集产物(HZ60-IN)对整合酶链转移的影响;试剂盒检测HZ60-IN对逆转录酶和蛋白酶的影响。结果 HZ60-IN对整合酶有高亲和性。细胞水平病毒感染实验表明,在TZM-bl细胞中,HZ60-IN对HIV-1 NL4.3和1084i的半数抑制浓度(IC_(50))分别为(31.94±8.96)、(38.07±11.25)μg/mL;在2株PBMC细胞中,HZ60-IN对HIV-1 NL4.3病毒均显示显著的抑制活性。HZ60-IN对整合酶的3’加工和链转移均有抑制作用,其中对3’加工的IC_(50)为(6.54±1.69)μg/mL,对链转移的IC_(50)为(2.56±0.97)μg/mL,其不作用于HIV感染的进入阶段,对逆转录酶抑制活性较弱,对蛋白酶活性没有影响。结论 HZ60-IN有抗HIV-1病毒活性,主要通过影响HIV-1的整合酶活性发挥作用。  相似文献   

4.
文摘     
塞内加尔刺桐中新的抑制HIV-1蛋白酶的异戊二烯基异黄酮类化合物 在从天然植物中筛选抗HIV-1蛋白酶的过程中,发现塞内加尔刺桐Erythrina senegalensis DC.对该酶显示抑制活性。从该植物茎皮的二氯甲烷提取物中分离了8个具抗HIV-1蛋白酶活性的化合物:8一异戊二烯基羽扇豆异黄酮(1)、耳形鸡血藤黄素(2)、erysenegalensein O(3)、erysenegalensein D(4)、erysenegalensein N(5)、derrone(6)、高山金链异黄酮(7)、6,8-二异戊二烯基染料木黄酮(8)。  相似文献   

5.
蔷薇科植物Rosa woodsii广泛分布于北美洲,从这种植物的叶中分离到没药烷类化合物(bisabolanoids)以及具有抗HIV活性的三萜类化合物。本次研究了这种植物叶的极性组分中的16种鞣质及相关多酚,这些成分具有显著抑制HIV-1逆转录酶(HIV-RT)的作用。  相似文献   

6.
小花五味子中抗HIV活性的木脂素类化合物   总被引:5,自引:1,他引:5  
目的:从小花五味子中发现具有抗HW活性的化学成分。方法:采用多种柱层析分离进行化合物的分离和纯化.通过波谱分析鉴定化合物的结构,化合物的抗HIV-1活性通过对HIV-1感染C8166细胞致细胞病变的抑制试验得到。结果:从小花五味子的茎藤部分分离得到了4个木脂素,分别鉴定为micrantherin A(1),gomisin K3(2),gomisin G(3)和vladinol F(4)。化舍物4具有显著的抗HIV-1活性,IC50=3.51μg/mL,选择指数为27、45。结论:化合物1为新的木脂素,化合物4的抗HIV-1活性值得进一步研究。  相似文献   

7.
 目的 研究玉足海参(Holothuria leucospilota)具有生物活性的三萜皂苷类成分。方法 应用大孔树脂柱色谱、正相硅胶柱色谱、反相硅胶柱色谱和HPLC对玉足海参体内三萜皂苷活性成分进行分离纯化,根据化合物的理化性质和波谱数据鉴定其结构。结果 分离并鉴定了3个三萜皂苷类化合物,分别为:leucospilotaside D (1)、holothurin B (2) 和holothurin B2 (3)。 化合物1~3对人宫颈癌细胞HeLa,人胃癌细胞BEL-7402和人乳腺癌细胞MCF-7的抑制率较强。结论 化合物1为首次从玉足海参中分离得到。3个化合物均显示显著的体外细胞毒活性。  相似文献   

8.
丹参中的一个新化合物及其抗HIV活性   总被引:5,自引:0,他引:5  
目的研究甘西鼠尾草Salvia przewalskii根的化学成分,检测抗HIV活性。方法用溶媒法、色谱法提取分离单体,光谱法分析鉴定结构。用艾滋病毒1型整合酶(HIV-1 IN)和艾滋病毒1型逆转录酶(HIV-1 RT)测定抗HIV活性。结果分离得到4个化合物,分别鉴别为8-{[7‘-(3’,‘4-二羟基-苯基)-9‘-氧代-7’-丙烯基]氧)-3-(1“-O-β-D-葡萄糖基)-4-羟基-[R-(E)]-苯丙酸(I),迷迭香酸(Ⅱ),紫草酸(Ⅲ)和紫草酸B(IV)。结论I为新化合物,Ⅱ~IV为已知化合物。均具有抗HIV活性。  相似文献   

9.
樟科植物鼎湖山胡椒(Lindera chunii)的根常用作中药乌药(Laggtegata)的替代品,分布于中同广东、广西两省。本次对其根的化学成分及抑制HIV-1整合酶的活性进行研究,并采用HPLC法对主要的生物碱类成分进行了定量分析。  相似文献   

10.
雪胆素A和B的体外抗HIV-1活性   总被引:5,自引:0,他引:5  
目的:研究从药用植物金佛山雪胆分离的雪胆素A和雪胆素B两个三萜类化合物的体外抗HIV活性。方法:应用合胞体抑制实验、p24抗原产生的抑制实验、慢性感染细胞和正常细胞间的细胞融合抑制实验等技术检测化合物的体外抗HIV-1活性;利用HIV-1逆转录酶、蛋白酶抑制实验,NCp7锌离子逐出实验探讨化合物的作用机制。结果:雪胆素A和雪胆素B在体外有较好的抑制HIV-1活性,其活性主要表现为:(1)抑制HIV-1诱导合胞体形成,EC50值分别为3.09μg·mL^-1和2.53μg·mL^-1;(2)抑制HIV-1急性感染的C8166细胞p24抗原产生,EC50值分别为3.97μg·mL^-1和18.90μg·mL^-1;(3)抑制HIV-1慢性感染H9与正常C8166细胞间融合,EC50分别为1.76μg·mL^-1和11.95μg·mL^-1。雪胆素A和雪胆素B对HIV-1逆转录酶、蛋白酶、NCp7锌离子逐出均没有抑制作用。雪胆素A对HIV-1整合酶有微弱的结合活性,而雪胆素B对HIV-1整合酶没有结合活性。在共培养实验中,雪胆素A和雪胆素B预处理C8166细胞组比未经预处理细胞组能够更有效的抑制HIV-1活性。结论:化合物雪胆素A和雪胆素B体外有较好的杭HIV-1活性,可能主要作用于HIV-1病毒进入细胞阶段。  相似文献   

11.
黔产乌药化学成分研究   总被引:2,自引:1,他引:1  
目的:研究樟科山胡椒属植物乌药块根Lindera aggregata的化学成分和抗氧化活性.方法:采用硅胶柱色谱、Sephadex LH-20色谱、D-101大孔树脂色谱等方法进行分离、纯化,通过光谱分析法鉴定它们的结构并对化合物进行抗氧化活性测试.结果:分离得到12个化合物,分别为hernangerine(1),syringgaresinol (2),香草醛(vanilin,3),α-cadinol (4),对羟基苯甲醛(p-hydroxybenzaldehyde,5),β-谷甾醇亚油酸酯(β-sistosterol linoleate,6),表儿茶素(epicatechin,7),boldine (8),norboldine(9),norboldine acetate (10),胡萝卜苷(daucosterol,11)和β-谷甾醇(β-sitosterol,12).用DPPH法测定化合物1,2,3,4,7,9,10的抗氧化活性.结论:化合物1~6均为首次从该植物中分离得到,化合物2,7有一定的抗氧化活性.  相似文献   

12.
HIV-1 integrase inhibitory substances from Coleus parvifolius   总被引:14,自引:0,他引:14  
For the purpose of discovering anti-HIV-1 agents from natural sources, water and EtOH extracts of 50 Thai plants were screened for their inhibitory activity against HIV-1 integrase (IN), an enzyme essential for viral replication. Of these plants, an EtOH extract of Coleus parvifolius Benth. (aerial parts) showed potent activity against HIV-1 IN with an IC50 value of 9.2 microg/mL. From this extract, 11 compounds were isolated and identified as luteolin 5-O-beta-d-glucopyranoside (1), luteolin (2), luteolin 7-methyl ether (3), luteolin 5-O-beta-d-glucuronide (4), 5-O-beta-d-glucopyranosyl-luteolin 7-methyl ether (5), rosmarinic acid (6), rosmarinic acid methyl ester (7), daucosterol (8), a mixture of alpha- and beta-amyrin (9, 10) and phytol (11). Of these compounds, rosmarinic acid methyl ester (7), rosmarinic acid (6), luteolin (2) and luteolin 7-methyl ether (3) exhibited inhibitory activities against HIV-1 IN with IC50 values of 3.1, 5.0, 11.0 and 11.0 microM, respectively. Among rosmarinic acid derivatives, the HIV-1 IN inhibitory activity increased in turn for a dimer (IC50 = 5.0 microM), a trimer (IC50 = 1.4 microM), and a tetramer (IC50 = 1.0 microM).  相似文献   

13.
乌药叶化学成分研究   总被引:8,自引:0,他引:8  
目的 :研究乌药叶的抗炎、抗菌的有效成分。方法 :柱色谱等进行分离 ,化学及波谱学等方法鉴定结构。结果 :分离得到 5个化合物和 1个互变异构体的混合物 ,6-acetyl lindenanolide B-1和B-2 (Ⅰ) ,去氢香樟内酯(Ⅱ) ,羟基香樟内酯 (Ⅲ) ,乌药内酯 (Ⅳ) ,山柰酚 (Ⅴ )和 β-谷甾醇 (Ⅵ)。 结论 :均首次从乌药叶中分离得到。  相似文献   

14.
The bioassay-guided fractionation for anti-HIV-1 integrase activity led to the isolation of six compounds from the whole plant extract of Eclipta prostrata extract. They were identified as 5-hydroxymethyl-(2,2':5',2')-terthienyl tiglate (1), 5-hydroxymethyl-(2,2':5',2')-terthienyl agelate (2), 5-hydroxymethyl-(2,2':5',2')-terthienyl acetate (3), ecliptal (4), orobol (5) and wedelolactone (6). Of these, compound 6 showed the highest activity against HIV-1 integrase (IN) with an IC50 value of 4.0+/-0.2 microm, followed by compound 5 (IC50=8.1+/-0.5 microm), whereas the four terthiophene compounds (1-4) were inactive (IC50>100 microm). Regarding HIV-1 protease (PR) inhibitory activity, compound 1 exhibited appreciable activity against HIV-1 PR with an IC50 of 58.3+/-0.8 microm, followed by compound 4 (IC50=83.3+/-1.6 microm) and compound 3 (IC50=93.7+/-0.8 microm), while compounds 2, 5 and 6 were inactive against HIV-1 PR (IC50>100 microm). This is the first report of anti-HIV-1 IN activities for wedelolactone (6), a coumarin derivative, and orobol (5), an isoflavone derivative. This study supports the use of E. prostrata in AIDS patients, which is in accord with its traditional use by Thai traditional doctors for curing blood related diseases.  相似文献   

15.
From the screening of a microbial extract library, isocomplestatin (1), a new axial-chiral isomer of complestatin (2) which is a known rigid bicyclic hexapeptide, was identified as a potent natural product inhibitor of HIV-1 integrase, a unique enzyme responsible for viral replication. Isocomplestatin showed inhibitory activities (IC(50)) in coupled 3'-end processing/strand transfer (200 nM), strand transfer (4 microM), and HIV-1 replication (200 nM) in virus-infected cells. Attempted large-scale isolation of 1 by the literature method, used for the isolation of complestatin, led to lower yield and limited availability. We have developed several new, two-step, high-yielding absorption/elution methods of isolation based on reverse-phase chromatography at pH 8 that are applicable to scales from one gram to potential industrial quantities. We have also discovered and determined the structure of two new congeners of 1, namely, complestatins A (4) and B (5), with almost equal HIV-1 integrase activity. They differ from 1 at C2' and C3' of the tryptophan moiety (residue F). Selective acid hydrolysis of chloropeptin I (3), itself a known acid-catalyzed rearranged isomer of 1 and 2 (8'- vs 7'-substitution in tryptophan residue F, respectively), an isomer of complestatin, and isocomplestatin resulted in a number of fragments (6-10) with retention of most of the HIV-1 integrase activity. The structure-activity relationship as revealed by these compounds could possibly lead to the design of better inhibitors or understanding of the HIV-1 integrase target.  相似文献   

16.
Five new triterpenoids, caloncobic acids A and B (1 and 2), caloncobalactones A and B (3 and 4), and glaucalactone (5), along with the known compounds 3β,21β-dihydroxy-30-nor-(D:A)-friedo-olean-20(29)-en-27-oic acid (6) and acetyltrichadenic acid B (7), were isolated from the leaves of Caloncoba glauca. The structures of 1-5 were elucidated using spectroscopic methods. Compounds 1-7 were evaluated for their inhibitory activities against two isozymes of 11β-hydroxysteroid dehydrogenase (11β-HSD1 and 11β-HSD2). Compounds 1 and 2 exhibited strong inhibitory activities against mouse (EC(50) 132 and 13 nM) and human (EC(50) 105 and 72 nM) 11β-HSD1.  相似文献   

17.
To identify substances with anti-human immunodeficiency virus (HIV) activity in traditional medicines, water and methanol extracts of crude drugs used in Indian traditional medicine (Ayurveda) were subjected to screening for their inhibitory effects on HIV type 1 protease (PR). The enzyme activity was determined by HPLC and of the 39 crude drugs tested, the extracts of the seeds of Areca catechu, the bark of Eugenia jambolana, the bark of Saraca indica and the stem bark of Terminalia arjuna inhibited the HIV-1 PR activity by more than 70% at a concentration of 0.2 mg/mL. The most potent inhibition was shown by the A. catechu extract, from which some procyanidins were isolated. One of them, arecatannin B1 showed significant HIV-1-PR inhibitory activity.  相似文献   

18.
Bioassay-directed chromatographic fractionation of an ethyl acetate extract of Gardenia jasminoides (Gardeniae Fructus) afforded a new vanillic acid 4-O-beta-d-(6'-sinapoyl)glucopyranoside (1) and five new quinic acid derivatives, methyl 5-O-caffeoyl-3-O-sinapoylquinate (2), ethyl 5-O-caffeoyl-3-O-sinapoylquinate (3), methyl 5-O-caffeoyl-4-O-sinapoylquinate (4), ethyl 5-O-caffeoyl-4-O-sinapoylquinate (5), and methyl 3,5-di-O-caffeoyl-4-O-(3-hydroxy-3-methyl)glutaroylquinate (6), together with three known quinic acid derivatives, two flavonoids, two iridoids, and two phenolic compounds. The structures of new compounds were elucidated by the aid of spectroscopic methods. These compounds were assessed for antioxidant activity using three different cell-free bioassay systems and for HIV-1 integrase inhibitory activity. Five new quinic acid derivatives showed potent DPPH radical scavenging, superoxide anion scavenging, and lipid peroxidation inhibition activities. These new quinic acid derivatives also exhibited HIV-1 integrase inhibitory activity.  相似文献   

19.
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