共查询到18条相似文献,搜索用时 734 毫秒
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天然产物是抗肿瘤药物的重要来源。三萜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,其中五环三萜羽扇豆烷型天然产物对多种肿瘤细胞生长均表现出很强地抑制活性,同时由于毒性较低且作用机制独特,使其成为优秀的抗肿瘤先导化合物。近年来,针对羽扇豆烷型天然产物的抗肿瘤机制研究越发深入,对其结构进行衍生化从而提升活性、改善成药性的研究也越来越多。本文综述了五环三萜中白桦酸、23-羟基白桦酸、桦木醇和羽扇豆醇4个天然活性化合物的来源、抗肿瘤活性、作用机制及结构衍生化等方面国内外的研究进展。 相似文献
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甘草次酸属五环三萜类化合物,是中药甘草的重要组分,具有广泛的生物活性.近年来,随着甘草次酸药理活性、临床应用及结构修饰等方面的研究不断深入,展现出广泛的应用前景.对甘草次酸的药理活性及结构修饰等的研究进展情况进行综述. 相似文献
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《中国药理学通报》2015,(5)
目的研究3种不同类型的马铃薯三糖五环三萜能否通过抑制H5N1流感病毒进入靶细胞,作为潜在的新型抗流感药物进行研发。方法以马铃薯三糖薯蓣皂苷衍生物1为先导化合物,设计并合成3个目标化合物,利用建立的H5N1假病毒活性检测方法,测试化合物的抑制活性。结果目标化合物1a、1b和1c对源自A/Thailand/Kan353/2004的H5N1假病毒毒株均具有明显的抑制作用,且化合物1b的活性最好,其IC50达到(1.25±0.22)μmol·L-1。结论初步构效关系研究表明,将先导化合物1结构中的薯蓣皂苷苷元替换成五环三萜苷元后可提高其抗病毒活性;五环三萜的苷元类型对抗病毒活性有重要影响,乌苏烷型的五环三萜为苷元其抗病毒活性最强。 相似文献
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《中国药理学与毒理学杂志》2019,(10)
三萜类化合物包括多种来自动植物的天然产物,这些产物因为具有多种多样的药理学活性而备受关注。在民间传统药用植物中,三萜类物质无处不在。"三萜"这一术语一般代表天然合成的萜类物质,但广义的"三萜化合物"也包括了它们的次级代谢产物。迄今为止,估计已经区分出80种结构和化学性质不同的三萜类化合物。很多这类化合物既可以直接产生药理活性,又能进行结构修饰增强药效和作用选择性后使用。本文对四环三萜及五环三萜化合物广泛的生物活性进行了综述,这些生物活性包括免疫调节、抗癌、抗炎、抗焦虑、压力减轻、改善记忆、止痛、神经保护以及其他中枢作用。现已证明有数个结构类型的三萜能够特异性地拮抗转录因子,因此它有望成为治疗炎症、癌症及免疫疾病的候选药物。 相似文献
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大黄酸是大黄素型羟基蒽醌,主要存在于大黄等中药中。大黄酸具有抗癌、抗炎、抗菌、抗阿尔茨海默病等广泛的药理活性,但由于其水溶性差、生物利用度低等缺点,限制了其临床应用。为了克服这些缺点,研究者通过对其进行结构修饰研究,设计并合成了大量生物活性更为突出的大黄酸衍生物。本文综述了近年来大黄酸的结构修饰及其生物活性研究进展,为大黄酸类衍生物的进一步研究提供参考依据。 相似文献
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刺梨酸的分离与结构研究 总被引:5,自引:0,他引:5
从刺梨中分离出一种新的五环三萜酸,命名为刺梨酸。通过光谱分析和衍生物的制备,确定其化学结构为2β,3α,7β,19α-四羟基乌苏-12-烯-28-羧酸。 相似文献
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赖氨大黄酸盐的合成工艺及活性研究 总被引:1,自引:1,他引:0
目的制备水溶性大黄酸衍生物。方法以大黄酸为起始原料,制备大黄酸的赖氨酸水溶液,在30℃反应24 h,然后加入一定量丙酮使其结晶析出,得到晶体物质。根据2005年药典方法检测其在水中溶解度,用MTT法检测新化合物对细胞增殖的影响。结果目标化合物经HPLC、红外光谱和1H-NMR确证。赖氨大黄酸在水中溶解度为15 g.L?1,其在抑制肿瘤细胞和内皮细胞增殖方面与大黄酸相当。结论获得了水溶性好的大黄酸衍生物——赖氨大黄酸,并且其活性与大黄酸相当。 相似文献
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熊果酸衍生物构效关系研究进展 总被引:2,自引:0,他引:2
综述了近年来对熊果酸的结构修饰及其衍生物构效关系的研究进展。熊果酸是一种广泛存在于天然植物中的五环三萜类化合物,具有抗肿瘤、降血糖、抗炎、抗HIV等药理活性,故而受到研究人员的广泛关注。对熊果酸进行结构修饰及构效关系探索,以获得高效低毒的候选化合物,已成为该化合物的研究热点之一。 相似文献
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Advances in the study of structural modifications and biological activities of betulinic acids 总被引:1,自引:0,他引:1
Betulinic acids are lupine-type pentacyclic triterpenoid saponins commonly found in some plants of Betulaceae family, especially in the bark of betula alba (birch). The potent anti-HIV and anti-tumor activities of betulinic acids have been greatly concerned. The natural betulinic acids include betulinic acid, 23-hydroxy betulinic acid, betulin and so on. Some investigations on the structural modifications of betulinic acids were carried out, and many derivatives with excellent biological activity have been obtained nowadays. In this paper, the research advances of the structural modification of betulinic acids, as well as their anti-HIV and anti-tumor activities are reviewed. 相似文献
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Myricadiol and other taraxerenes from Scaevola spinescens 总被引:1,自引:0,他引:1
Scaevola spinescens R. Br. (Goodeniaceae), a West Australian semi-arid native plant, has been found to contain a number of pentacyclic triterpenoid compounds of the taraxerene type in high yield compared with other species in which these compounds are known to occur. Isolation of these molecules, which are potential lead compounds for synthetic anti-cancer drugs, was achieved by partitioning the diethyl ether-soluble fraction, of the methanol Soxhlet extract, between hexane and aqueous methanol, followed by base extraction of minor components from the methanol isolate and recrystallisation or column chromatography. The major component isolated from the extract, and main subject of this report, is the pentacyclic triterpenoid, 14-taraxerene-3,28-diol (1; myricadiol). 相似文献
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Sarek J Klinot J Dzubák P Klinotová E Nosková V Krecek V Korínková G Thomson JO Janost'áková A Wang S Parsons S Fischer PM Zhelev NZ Hajdúch M 《Journal of medicinal chemistry》2003,46(25):5402-5415
Cellular screening of various synthetic triterpenoid compounds formally derived from lupane has identified a number of analogues as potential anticancer drug candidates. Here we describe the synthesis and structure-activity relationships of betulin and betulinic acid derivatives containing an E-ring modified with different oxygen functions. Thus compounds containing the lup-18-en-21-one, lup-18-ene-21,22-dione, 18,19-secolupane, and the highly oxygenated 18,19-secolupane systems, as well as des-E-lupane derivatives, were prepared from the readily available natural pentacyclic triterpene betulin using oxidative procedures. These compounds were named betulinines. We demonstrate that only selected compounds, particularly those containing a lupane E-ring-derived unsaturated ketone or diketone function, possessed in vitro cytotoxic activity against tumor cell lines, suggesting a structure-activity relationship. 相似文献
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Yili Dai Linjun Sun Yan Tan Wenyu Xu Shu Liu Jing Zhou Yalin Hu Jieying Lin Xu Yao Pengbing Mi Xing Zheng 《Chemical biology & drug design》2023,102(6):1643-1657
Ursolic acid (UA) is a pentacyclic triterpenoid, which exhibits many biological activities, particularly in anti-cardiovascular and anti-diabetes. The further application of UA is greatly limited due to its low bioavailability and poor water solubility. Up to date, various UA derivatives have been designed to overcome these shortcomings. In this paper, the authors reviewed the development of UA derivatives as the anti-diabetes anti-cardiovascular reagents. 相似文献
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自木瓜属植物光皮木瓜(Chaenomeles Sinensis(Thouin.)Koehne)的果实90%乙醇的提取物中分离得到20个化合物,根据其理化性质和波谱分析确定了化合物1-19的结构,依次为硬脂酸,棕榈酸,10-廿九烷醇,β-谷甾醇,齐墩果酸,熊果酸-3-O-山嵛酸酯,熊果酸,酒石酸,3-乙酰熊果酸,3-乙酰坡模醇酸,胡萝卜甙,桦木酸,槲皮素,富马酸,2α-羟基熊果酸,原儿茶酸,琥珀酸,芦丁,苯甲酸。以上化合物除酒石酸外均为首次从该植物中分得,其中熊果酸-3-O-山嵛酸酯为一新的化合物。 相似文献
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Isotamarixen - a new antioxidant and prolyl endopeptidase-inhibiting triterpenoid from Tamarix hispida 总被引:2,自引:0,他引:2
Sultanova N Makhmoor T Yasin A Abilov ZA Omurkamzinova VB Atta-ur-Rahman Choudhary MI 《Planta medica》2004,70(1):65-67
A new pentacyclic triterpenoid, 3alpha-(3",4"-dihydroxy- trans-cinnamoyloxy)- D-friedoolean-14-en-28-oic acid ( 1) has been isolated along with two known compounds, rhamnocitrin ( 2) and isorhamnetin ( 3) from the aerial parts of Tamarix hispida Willd. Compound 1 was found to be a potent antioxidant. In addition, compounds 1 - 3 showed significant inhibitory activity against prolylendopeptidase (PEP). 相似文献