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五环三萜类化合物植物资源分布广泛,具有显著抗癌、抗炎、抗氧化、抑菌等生物活性.但五环三萜类化合物普遍生物利用度较低,且作用机制尚不明确,部分五环三萜类化合物在临床应用及推进方面受到极大的限制,故更为深入地探讨和明确五环三萜类化合物的吸收特征及其机制是亟待解决的问题.现就国内外学者对五环三萜类化合物吸收特征的研究概况进行综述. 相似文献
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心脑血管疾病是我国成年人群首要致死病因,且发病率呈上升和年轻化趋势,运用中药治疗心脑血管疾病十分必要。天然产物是治疗心脑血管药物的重要来源。三萜类化合物是植物体内重要的次生代谢产物,具有广泛的生物活性,其中五环三萜类表现出明显的抗炎、抗肿瘤、抗病毒等药理作用。近年来,越来越多的研究集中在五环三萜类化合物抗心脑血管疾病领域,对其结构进行衍生化从而提升活性、改善药性的研究也越发深入。通过查阅国内外五环三萜类化合物及其衍生物近10年的文献专利报道,综述了齐墩果烷、乌苏烷、羽扇豆烷、木栓烷4种类型五环三萜类化合物及其衍生物抗心脑血管疾病的研究进展,为治疗心脑血管疾病药物的研发提供依据和参考。 相似文献
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黄酮类化合物是一类在自然界分布广泛的天然产物,具有多方面的生物活性.黄酮类化合物在肠道细菌的作用下发生降解,进而影响其在体内的生物利用度.肠道细菌对黄酮类化合物的代谢研究能为筛选黄酮生物转化相关菌、阐明黄酮体内代谢过程提供依据.以黄酮类化合物为先导化合物,肠道细菌通过结构修饰可以产生高效、高生物利用度和吸收性良好的化合物,为新药研发、药物剂型选择和药物生产奠定基础.该文归纳总结了肠道细菌对黄酮类化合物生物转化的主要反应类型与影响因素,供生物转化研究借鉴. 相似文献
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植物五环三萜类化合物生物合成途径研究进展 总被引:3,自引:2,他引:1
五环三萜类化合物是一类重要的植物次生代谢产物,由6个异戊二烯单元组成,在自然界中普遍存在,具有广泛的药理作用。五环三萜类化合物结构丰富多样,根据其苷元的不同,可分为齐墩果烷型、羽扇豆烷型、乌苏烷型和木栓烷型4大类。植物五环三萜类化合物主要由甲羟戊酸途径和戊糖磷酸途径合成,2,3-环氧角鲨烯前体在氧化鲨烯环化酶的作用下环化为不同的骨架,继而在细胞色素P450以及糖基转移酶的修饰下形成多种皂苷。综述了植物五环三萜类化合物生物合成途径的研究进展,对参与合成途径的关键家族基因进行系统分析和催化机制的解读,为寻找未知五环三萜类化合物生物合成途径关键基因和五环三萜化合物异源生物合成提供参考。 相似文献
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中药活性成分生物转化的研究思路与方法 总被引:13,自引:0,他引:13
结合本课题组近几年来的研究结果,对中药活性成分的生物转化方法进行总结,并对今后生物转化的研究思路进行了展望。目前,生物转化在有机合成领域的应用比较广泛,而该技术用于中药活性成分的结构修饰还处于初级阶段,尤其缺乏对某类中药活性成分系统的生物转化研究,因此有很多方面的研究值得关注,尤其是生物催化酶的研究将是生物转化的重要发展方向。此外,生物转化在中药活性化合物合成中的应用以及利用“微生物模型”研究中药活性的体内代谢,也将成为今后生物转化研究中不可忽视的领域。 相似文献
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《云南中医中药杂志》2019,(4)
恶性肿瘤已经成为严重威胁人类健康最主要的疾病之一,肿瘤不仅具有极高的致死率,且肿瘤的发病率呈逐年上升趋势,发病人群也趋于年轻化,因此受到国内外医学界的高度重视。现代研究中发现五环三萜类化合物具有良好的抗肿瘤活性,也为将来开发抗肿瘤新药打下一定的基础,总结了近几年五环三萜类化合物抗肿瘤活性的研究情况。 相似文献
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目的:研究人参水提取物中的人参三萜在人源肠内细菌作用下的生物转化。方法:将人参水提取物中人参三萜样品与人源肠内细菌进行温孵培养,采用超快速液相色谱-质谱/质谱法(UFLC-MS/MS)进行定性定量分析,确定人肠内细菌转化前后人参皂苷的动态变化。通过人参三萜种类和含量的变化,总结原人参二醇(PPD)型、原人参三醇(PPT)型和齐墩果烷(OLE)型人参三萜在人肠内细菌作用下的转化途径。结果:与对照品比对,共鉴定了49个化合物。人参皂苷在肠内细菌的作用下以脱糖基转化为主,其中人肠内细菌对PPD型人参皂苷的转化能力要明显强于对PPT型人参皂苷的转化能力,尤其是人参皂苷化合物K和20(S)-PPD的含量上升明显,甚至能达到初始值的数十倍;随着温孵时间的延长,含有乙酰基的人参皂苷含量迅速下降。结论:人参皂苷经人肠内细菌生物转化后更利于其吸收进入系统循环,为人参皂苷在体的吸收代谢和生物学活性发挥提供了参考。 相似文献
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目的:利用灵芝菌对中药材茯苓药材进行固态生物转化,研究转化产物中总多糖和总三萜量的变化情况。方法:采用微波法提取茯苓及转化产物中的总多糖并采用苯酚-硫酸法进行含量测定;采用超声法提取茯苓及转化产物中总三萜并用香草醛-高氯酸法进行含量测定。结果:经生物转化后产物中的总多糖含量明显高于未经转化的茯苓药材(P<0.01),而总三萜含量明显升高(P<0.01),说明灵芝菌的生物转化过程改变了茯苓药材的原始特性;茯苓对灵芝生长具有促进作用,表现为灵芝菌丝生长旺盛未受抑制、转化产物中总多糖及总三萜含量显著高于茯苓原药材。结论:利用灵芝菌对中药茯苓进行生物转化来提高总多糖和总三萜含量,具有方法简单、成本低等优点,在中药现代化中有较高的应用价值。 相似文献
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Kashiwada Y Sekiya M Yamazaki K Ikeshiro Y Fujioka T Yamagishi T Kitagawa S Takaishi Y 《Journal of natural products》2007,70(4):623-627
Four new triterpenes, together with 16 known triterpenes, were isolated from the floral spikes of Betula platyphylla var. japonica in a search for compounds capable of reversing multidrug resistance in cancer cells. The structures of the new triterpenes were elucidated as 3,4-seco-olean-4(23),13(18)-dien-3-oic acid (1), 3,4-seco-urs-4(23),20(30)-dien-3-oic acid (2), 3-O-methylmalonylepiocotillol II (6), and 3-O-methylmalonylcabraleahydroxylactone (16) by spectroscopic examination. The cytotoxicity of the isolated triterpenes against human cancer cell lines as well as multidrug-resistant cancer cell lines was evaluated. Most of the isolated triterpenes showed very weak cellular toxicities. Although no discernible differences were found in the cytotoxicities for the tested compounds against sensitive and resistant cell lines, the cytotoxicities for several triterpenes against multidrug-resistant cancer cell lines (KB-C2 or K562/Adr) were enhanced in the presence of nontoxic concentrations of colchicine or doxorubicin. Compound 10 reversed the cytotoxicity of colchicine against KB-C2 cells at 8.1 microM and showed comparable potency to 5 microM verapamil. 相似文献
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M C Wani J P Schaumberg H L Taylor J B Thompson M E Wall 《Journal of natural products》1983,46(4):537-543
Four new pentacyclic triterpenes have been isolated from Maprounea africana. These triterpenes are members of the previously unknown urs-12-en-29-oic acid series. The structures of these compounds were deduced from spectral and chemical evidence. The parent compound, maprounic acid, was identified as 3B-hydroxyurs-12-en-29-oic acid. The remaining three triterpenes were identified as maprounic acid 3-p-hydroxybenzoate, 7 beta-hydroxymaprounic acid 3-p-hydroxybenzoate, and 2 alpha-hydroxymaprounic acid 2,3-bis-p-hydroxybenzoate. Of the four triterpenes, only the 7 beta-hydroxy derivative exhibited in vivo P-388 activity. 相似文献
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Banskota AH Tezuka Y Tran KQ Tanaka K Saiki I Kadota S 《Journal of natural products》2000,63(1):57-64
Thirteen novel cycloartane-type triterpenes were isolated from Combretum quadrangulare, a Vietnamese medicinal plant. The structures of the novel triterpenes were determined by spectroscopic methods as well as by chemical transformations. Among those compounds, quadrangularic acids F (1), G (2), and H (4) and 24-epiquadrangularic acid G (3) are the first examples of cycloartane-type triterpenes bearing carboxylic acid groups at both C-4 and C-20. Furthermore, norquadrangularic acid A (13) is the first example of a trinorcycloartane-type triterpene isolated from the genus Combretum. 相似文献
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Abdel Bar FM Zaghloul AM Bachawal SV Sylvester PW Ahmad KF El Sayed KA 《Journal of natural products》2008,71(10):1787-1790
Three new 28-norlupane triterpenes, 28-norlup-20(29)-en-3beta-hydroxy-17beta-hydroperoxide (1), 28-norlup-20(29)-en-3beta-hydroxy-17alpha-hydroperoxide (2), and 20 S-17beta,29-epoxy-28-norlupan-3beta-ol (3), were isolated from the leaves of Melaleuca ericifolia along with eight known pentacyclic triterpenes. The structures of the new compounds were elucidated by spectroscopic methods including 1D and 2D NMR spectroscopy and mass spectrometry. The isolated triterpenes were evaluated for antiproliferative activity against the malignant +SA mammary epithelial cell line. 相似文献
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Rukachaisirikul V Saelim S Karnsomchoke P Phongpaichit S 《Journal of natural products》2005,68(8):1222-1225
Five new triterpenes, one 17,14-friedolanostane (garcihombronane F, 1), three 17,13-friedolanostanes (garcihombronanes G-I, 2-4), and one lanostane (garcihombronane J, 5), were isolated from the leaves of Garcinia hombroniana together with nine known compounds including five triterpenes, two ionone-derived glycosides, and two flavonoid glucosides. Their structures were identified by analysis of spectroscopic data and comparison of the NMR data with those previously reported. 相似文献