|关键词||异叶青兰 黄酮类化合物 三萜类化合物 Mtt 法 Ptp-1b活性|
系统研究传统中药中的化学成分已成为发现活性化合物的重要途径之一。前期的调研我们发现，在新疆的阿图什和喀什地区生长的植物异叶青兰尚未得到系统研究。因此研究其化学成分，活性成分的分离方法及生物活性对于新药研发是非常重要的。异叶青兰约有60 种属于唇形科青兰属。它们分布在高山和半干地区，主要集中在亚洲温带地区，少数分布在欧洲，一种在北美。在中国有32种，7 个变种。在新疆民间，好几种青兰属药材经常用于治疗气管炎和心血管方面的疾病。异叶青兰为唇形科青兰属的物种之一，在中国新疆和西藏应用广泛。它是一种多年生草本植物，广泛分布在山西，内蒙，宁夏，甘肃，四川西北部，新疆和西藏等地。主要生长在山地草原和多石的半沙漠干旱地区，如青海和甘肃东部海拔1100 至2800 米，西部海拔5000 米和新疆海拔2200-3100 米的地方。在本论文中，我们系统研究了异叶青兰中的化学成分。研究发现，异叶青兰的地上部分主要包括黄酮类化合物、三萜类化合物和类固醇类化合物。共从醇提物中分离得到14 个化合物。基于光谱方法，它们分别被鉴定为：熊果酸（1）﹑猫眼草黄素（4,5 - 二羟基-3 ,6,7,3 四甲氧基黄酮）（2），香叶木素（5,7,3' - 三羟基-4'-甲氧基黄酮）（3）﹑木犀草素（5,7,3'，4'-四羟基黄酮）（4）﹑（金合
Dracocephalum heterophyllum B. (Labiatae) is one of 32 species of the genus Dracocephalum, distributed in China. It is traditionally used as a herb in Xinjiang and in Tibet region of China. Several species are used as folk medicine for the treatment of tracheitis and cardiovascular disease in Xinjiang Autonomous Region. Systematical study Dracocephalum heterophyllum growing in Atush, Kashgar (Xinjiang) had not been investigated systematically yet. Thus the sytstematical study on its chemical constituents was undertaken since such an effort is an important route to discover bioactive compounds. In addition, the methods for extracting selective class of naturally bioactive compounds were developed for discovery of new medicines and herbal remedies through further pharmacological studies. Systematical investigation of the EtOH extract of the aerial parts of Dracocephalum heterophyllum resulted in the isolation of 14 compounds including flavonoids, triterpenoids and steroids via various chromatographic methods. The structures of these compounds were elucidated on the basis of spectroscopic analysis, mainly 1D and 2D NMR. They were established as ursolic acid (1), chrysosplenetin (4',5-dihydroxy-3,6,7,3'-tetramethoxyflavone) (2), diosmetin (5,7,3′-trihydroxy-4′-methoxyflavone) (3), luteolin (5,7,3',4'-tetrahydroxyflavone) (4), (acacetin 7-O-rutinoside) (5), diosmetin 7-O-glucoside (6), diosmetin 7-O-rutinoside (7), oleanolic acid (8), stigmasterol (9), β-sitosterol (10), daucosterol (β-sitosterol 3-O-?-D-glucoside) (11), quercetin (3,5,7,3',4'-pentahydroxyflavone) (12), kaempferol (3,4',5,7-tetrahydroxyflavone) (13) and astragalin (kaempferol 3-O-β-D-glucoside) (14). Compounds 2 and 5–7 were isolated from the genus Dracocepahlum and compounds 2, 5–10, and 12–14 were isolated from D. heterophyllum for the first time. Quantitative HPLC analysis for some isolated flavonoids was developed. Under the optimized HPLC conditions mentioned in experimental section, good separation of D. Heterophyllum extract is obtained in 55 min with method 2, Waters sunfire C18 column 4.6×250mm, 5 μm, delivered by methanol/ 0.1% formic acid and detection at 254 nm. This condition yielded critical separation for chrysosplenetin, diosmetin, kaempferol and luteolin. Selective separation of the total flavonoids using various macroporous resins including AB-8, D 101, HPD-100, HPD-300, HPD-400, HPD-450, HPD-500, LD601, LS-303B, and LX-28 was attempted. Under optimized static adsorption-desorption process obtained by single factor and orthogonal array design methods, AB-8 macroporous resin gave a good extraction of D. Heterophyllum total flavonoids (DHTF) from the EtOH extract of the aerial part of the title plant. Dracocephalum heterophyllum Benth in traditional Uighur medicine is wildly used for the treatment of hypertension. In this study, the anti-hypertension effects were confirmed by examining DHTF on the rat model of renal hypertension. In addition to the effect on blood pressure and myocardial hypertrophy, the possible mechanism of DHTF was explored. The result thus provided a theoretical data and basic information for the development and effective use of Uighur local herbs. The process for extracting total triterpenoids from D. heterophyllum was developed by a fairly simple and accessible method, called remaceration. This method is characterized by minimal loss of BAC on diffusion, which contributes the most complete depletion of raw materials. Total triterpenoids are light green amorphous solid with a distinctive smell and the moisture content is less than 3.5%. Extraction solvents, fineness of the raw material, extraction duration and frequency, and temperature are key factors on the completeness of extraction. The impact of these factors on the extraction of total triterpenoids were evaluated. The total triterpenoids and isolated triterpenoids, oleanolic and ursolic acids, were subjected to PTP-1B and cell toxicity test - MTT assay. The results indicated that the total triterpenoids and these two isolated triterpenoids have good antidiabetic and anti-cancer activity. The bioactive fractions were screened for free radical scavenging activity by using DPPH and ABTS radical colorimetric assay. Results indicated that total flavonoids showed good antioxidant activity.
|SODIK NUMONOV. 异叶青兰的化学成分和总黄酮与三萜类化合物提取方法的研究[D]. 北京. 中国科学院大学,2013.|
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