紫草素及其衍生物抗妇科肿瘤作用研究进展

紫草素是从传统中药紫草中提取的萘醌类化合物,具有抗炎、抗氧化、抗肿瘤、促进伤口愈合等作用。近年来,紫草素及其衍生物的抗肿瘤作用得到广泛研究。多项体外和体内研究表明紫草素及其衍生物可有效抑制乳腺癌、宫颈癌等妇科恶性肿瘤的发生与发展。从阻滞细胞周期、促进肿瘤细胞凋亡、抑制癌细胞转移和侵袭、诱导自噬和坏死等方面综述近几年紫草素及衍生物在抗妇科肿瘤领域的研究进展,为紫草素类化合物在妇科肿瘤中的临床研究提供参考。     

紫草素及其衍生物合成相关基因及信号传导研究进展

紫草素类化合物是紫草的有效成分,也是重要的工业原料。紫草素及其衍生物为萘醌类化合物,总结了紫草素类化合物生物合成途径中相关基因的研究进展,并介绍了这些基因的功能及表达特性;综述了紫草素类化合物合成调控过程的信号传导及相关基因的表达,并对今后紫草素及其衍生物的生物合成研究的发展方向进行了展望。     

中药紫草的临床应用

紫草是传统中草药,又名东紫草、地血、紫丹。近年来对紫草的研究不断加深,对其药理作用和药用价值多有报道,临床应用也更加广泛。现将其临床应用情况介绍如下: 一、实验研究 化学成分:紫草及新疆紫草根及根茎中主要含多种萘醌类化合物:紫草素(Shikonin)、乙酰紫草素(Acetylshikonin)、ββ──二甲基丙烯酰紫草素(ββ──Dimethylacrylshikonin)、异丁酰紫草素(lso-butyl-shikonin)等十多种紫草素衍生物;有报道紫草或其幼苗(Ⅱ)与紫草茸(Ⅰ)具不相同成分,实验表明紫草(Ⅱ)中主含萘醌类化合物──紫草素及其衍生物,紫草茸(Ⅰ)中主含树脂蜡及水溶性红色素等。     

紫草、紫草素、紫朱草素对鼠郎格罕氏细胞的诱导作用

两种来源于骨髓的树突状细胞:郎格罕氏细胞(LCs)和树状表皮T细胞(DETCs)构成了皮肤的免疫系统。研究表明,紫草素及其衍生物具有抗菌、抗炎、抗肿瘤等多种药理作用,然而,其对树状免疫细胞的作用还不明确。本次对紫草、紫草素、紫朱草素(Alkannin)等诱导的鼠体内LCs和DETCs进行形态学研究。 材料和方法:按照文献报道的条件经HPLC从紫草中制备紫草素(R型)、紫朱草素(S型)。紫草素、紫朱草素溶于含1％吐     

蛇床子素及其衍生物抗肿瘤作用机制研究进展

肿瘤是一种严重威胁人类生命的疾病,其治疗一直是临床的一大难题,但植物成份长春新碱等有效抗肿瘤药的出现为寻找此类新药找到了新的方向。蛇床子素是从蛇床子等植物中提取出来的香豆素类化合物,具有包括抗肿瘤作用的多种生物活性。蛇床子素的抗肿瘤作用包括细胞毒、促进肿瘤细胞凋亡、抑制肿瘤迁移和转移、逆转多药耐药性等多种复杂的分子机制。本文综述了以蛇床子素为先导化合物,筛选抗肿瘤衍生物的研究,这些研究结果显示:蛇床子素及其衍生物从各方面均显示出优异的抗肿瘤作用,是一种具有研究和应用前景的抗肿瘤植物成份。     

紫草素抗妇科恶性肿瘤作用机制的研究进展

紫草的主要有效成分之一紫草素是一种萘醌类化合物,已被证实具有抗病毒、抗肿瘤、抗炎等多种生物活性。有大量研究表明,紫草素在抑制细胞增殖、促进细胞凋亡、诱导细胞坏死、抑制侵袭转移等方面发挥重要作用。近年关于紫草素在妇科恶性肿瘤中的研究日益增多,故本文对该成分作用机制进行综述,以期为其深入研究和相关新药开发提供参考。     

新疆紫草及其毛状根中萘醌类化合物的研究

目的运用高效液相色谱-电喷雾离子阱液质联用技术(HPLC-ESI-MS/MS)鉴别新疆紫草中的萘醌类化合物,比较分析了9个样品中(新疆紫草原植物根及毛状根)萘醌类成分种类和含量的差异。方法采用BDS C18色谱柱,以0.1%甲酸(A)-甲醇(B)梯度洗脱,使用ESI离子源,流速1.0 m L·min-1,质量扫描范围(m/z)150~400,负离子模式下采集数据。结果新疆紫草中含有紫草素、β-羟基异戊酰紫草素、乙酰紫草素、去氧紫草素、异丁酰紫草素、β,β-二甲基丙烯酰紫草素、异戊酰紫草素或α-甲基-正丁酰紫草素7种萘醌类化合物;但其毛状根中不含紫草素成分,其他成分与新疆紫草相同。紫草素及其衍生物的种类及含量因不同区域、不同毛状根而有所差异。此外,硝酸银(Ag NO3)及营养成分能够增加毛状根中紫草素及其衍生物的种类且影响各成分的含量。结论萘醌类化合物的种类及含量受环境及培养条件的影响而变化。该方法可为新疆紫草及其毛状根的药效物质基础研究及其开发利用提供科学依据。     

新疆紫草中多糖的超声提取工艺优选

紫草根药用．含多种萘醌类化合物——紫草素及其衍生物，具有显著的抗生育、抗炎、抗肿瘤、杀菌、抗病毒、保肝和免疫调节等作用。紫草中还含有多糖。紫草多糖具有抗病毒活性，能够激活巨噬细胞的吞噬功能，增强T淋巴细胞的数量和活性，抑制DFH强度，促进T淋巴细胞的免疫应答作用，具有     

新疆紫草抗肿瘤作用机制研究进展

文章主要对新疆紫草抗肿瘤作用机制的研究成果进行了系统综述和评论。简要介绍了新疆紫草的物质基础,详细评述了其主要活性成分紫草素及其衍生物抑制多种肿瘤细胞的生长、增殖,致肿瘤细胞凋亡作用机制的最新进展,并对其应用前景进行了展望。     

紫草素抑制卵巢癌作用机制的研究进展

紫草为紫草科植物新疆紫草Arnebia euchroma或内蒙紫草A.guttata的干燥根,《中国药典》记载其具有清热凉血、活血解毒、透疹消斑的功效。紫草素是从紫草中提取出来的萘醌类化合物,目前,紫草素及其衍生物在各种癌症的治疗中被广泛研究。主要从机体的免疫系统、肿瘤细胞的侵袭和转移、肿瘤细胞凋亡、肿瘤细胞的有氧糖酵解及肿瘤细胞周期5个方面综述紫草素抑制卵巢癌作用机制的研究进展,为紫草素治疗卵巢癌的临床研究提供参考依据。     

Cellular pharmacology studies of shikonin derivatives

The naphthoquinone pigment, shikonin, isolated from Lithospermum erythrorhizon Sieb. et Zucc.(Boraginaceae) and its derivatives are the active components isolated from the Chinese herbal therapeutic, Zicao. Historically, Zicao root extracts have been used to treat macular eruption, measles, sore-throat, carbuncles and burns. Multiple pharmacological actions have been attributed to shikonin, e.g. antiinflammatory, antigonadotropic and anti-HIV-1 activity. In this review, several therapeutic applications of shikonin will be summarized including its pleiotropic, antiinflammatory and antitumour effects. Widely diverse and sometimes conflicting activities have been attributed to shikonin, e.g. wound healing, enhanced granuloma formation, suppression of local acute inflammatory reactions, inhibition of angiogenesis, inhibition of select chemokine ligands, inhibition of DNA topoisomerase activity, inhibition of platelet activation and antimicrobial activity. Comparison of the various reported mechanisms of action for shikonin lead us to hypothesize that shikonin is an effective inhibitor of protein-protein interaction with multiple targets in both the intracellular and extracellular compartments. This general inhibitory effect can account for the broad spectrum of shikonin biological and pharmacological activities.     

Pharmacological and analytical aspects of alkannin/shikonin and their derivatives: An update from 2008 to 2022

Alkannin/shikonin (A/S) and their derivatives are naturally occurring naphthoquinones majorly found in Boraginaceae family plants. They are integral constituents of traditional Chinese medicine Zicao (roots of Lithospermum erythrorhizon). In last two decades significant increase in pharmacological investigations on alkannin/shikonin and their derivatives has been reported that resulted in discovery of their novel mechanisms in various diseases and disorders. This review throws light on recently conducted pharmacological investigations on alkannin/shikonin and their derivatives and their outputs. Various analytical aspects are also discussed and brief summary of patent applications on inventions containing alkannin/shikonin and its derivatives is also provided.     

Evidence for Shikonin acting as an active inhibitor of human carboxylesterases 2: Implications for herb–drug combination

Shikonin, a natural naphthoquinone compound derived from the herb Lithospermum erythrorhizon, is widely used for its various pharmacological activities. However, its potential interactions with other medications by inhibiting human carboxylesterases 2 (hCE2) remain unknown. In this study, the inhibitory effects of shikonin on the activity of hCE2 in human liver microsomes are investigated by using fluorescein diacetate (FD), N‐(2‐butyl‐1,3‐dioxo‐2,3‐dihydro‐1H‐phenalen‐6‐yl)‐2‐chloroacetamide (NCEN), and CPT‐11 as substrates of hCE2. The results demonstrate that shikonin significantly inhibits the activity of hCE2 when FD and NCEN are used as substrates, whereas the half inhibition concentration value of shikonin increased by 5–30 times when CPT‐11 was used as the substrate. The inhibition types of shikonin against hCE2 activity reflected by 3 substrates were all best fit to noncompetitive manners. In addition, shikonin was found to distinctly suppress endogenous hCE2 activity, characterized with attenuated fluorescence. Furthermore, for drugs metabolized by hCE2 with the similar binding sites with FD or NCEN, the estimated magnitudes of area under the curve variation were approximately 9–357% in the presence of shikonin. Also, the area under the curve of CPT‐11 could be increased by 1–14% following administration of shikonin. These findings have clear clinical implications for the combination of shikonin and hCE2‐metabolizing prodrugs.     

白桦酯酸及其衍生物的生物活性及作用机制研究进展

白桦酯酸是一种天然存在的五环戊烷型三萜类物质,通常是从白桦Betula platyphylla树皮中分离出来,在其他植物中也有发现,以游离糖苷和糖基衍生物的形式存在于不同植物中。通过对其化学结构的修饰可以得到多种多样的衍生物,研究表明白桦酯酸及其衍生物在抗肿瘤、抗病毒、消炎止痛、抑制脑神经及血管损伤和对其他常见疾病的治疗作用等方面具有积极的作用。综述了白桦酯酸及其衍生物的种类、生物活性及作用机制,以期为今后对其进一步的研究与应用提供理论参考。     

Fibroblast growth stimulation by extracts and compounds of Onosma argentatum roots

The roots of Onosma argentatum are used traditionally in Turkey for wound healing and burns. The n-hexane-dichloromethane extract of the roots, and four shikonin derivatives (deoxyshikonin, acetyl shikonin, 3-hydroxy-isovaleryl shikonin and 5,8-O-dimethyl acetyl shikonin) isolated from the n-hexane-dichloromethane extract were investigated for their ability to stimulate the growth of human amnion fibroblasts. A range of concentrations was studied and the extract found to stimulate the growth of human amnion fibroblasts in vitro at 0.1 microg/mL whilst 5,8-O-dimethyl acetyl shikonin had the same effect at 0.05-5 microg/mL, although cytotoxicity was observed at 50 microg/mL for all samples. The extract and all the other isolated compounds showed cytotoxicity at 10 microg/mL with the extract and 3-hydroxy-isovaleryl shikonin showing cytotoxicity at 5 microg/mL. It is suggested that any wound healing effect of the roots of Onosma argentatum might be partly due to an additive effect of the shikonin derivatives present.     

地黄多糖的提取纯化及药理作用研究进展

地黄多糖是地黄Rehmannia glutinosa的主要活性成分之一,主要由葡萄糖、鼠李糖、甘露糖等单糖组成。地黄多糖的提取方法有很多种,不同的提取方法具有其独特的优势并且影响了地黄多糖的得率。纯化是获取地黄多糖不可或缺的步骤,经过除蛋白、色素等操作,可以保证地黄多糖的纯度,使其后续研究更加准确。地黄多糖及其衍生物具有免疫调节、神经调节、抗氧化、抗炎、抗肿瘤、治疗糖尿病等多种药理功能,具有潜在的药用价值。综述了地黄多糖的提取纯化方法、药理活性和载体新剂型等方面的研究进展,为地黄多糖及其衍生物的进一步研究提供了基础。     

Shikonin derivatives protect immune organs from damage and promote immune responses in vivo in tumour-bearing mice

Shikonin, a major component of Lithospermum erythrorhizon and Arnebia euchroma, exhibits antiinflammatory, immunomodulatory and antitumour activities. Although many recent studies have focused on the antitumour effects of shikonin, the exact mechanisms underlying its antitumour and immunomodulatory effects in tumour‐bearing mice remain unclear. The aim of the present study was to investigate the antitumour and immunomodulatory effects of shikonin derivatives (ShD) in tumour‐bearing mice. Swiss mice inoculated with hepatoma HepA₂₂ or sarcoma 180 (S₁₈₀) cells were treated with ShD or 5‐fluorouracil (5Fu). Survival time, immune organs, natural killer cell activity, lymphocytes, lymphocyte transformation and interleukin (IL)‐2 production were analysed. ShD significantly prolonged the survival (median survival time prolonged by >7 days) of tumour‐bearing mice in a dose‐dependent manner, inhibited the growth of transplantable neoplasms (inhibitory rate, > 33%), and recovered (at [ShD] = 2.5 mg/kg/day) or increased (at [ShD] > 5 mg/kg/day) the number of CD3‐ and CD19‐positive cells. ShD also played a role in protecting the immune organs from damage and reversed or enhanced immune responses, as noted by the nearly normal thymic structure; enlarged splenic corpuscles; and improved natural killer cell activity, lymphocyte transformation and IL‐2 production in ShD‐treated mice. ShD reduced the tumour load of tumour‐bearing mice and protected the immune organs against tumour‐induced damage and immune function impairment. Copyright © 2011 John Wiley & Sons, Ltd.     

九节龙皂苷抗肿瘤作用研究进展

九节龙皂苷是金牛科紫金牛属植物川产九节龙Ardisia pusilla中分离出的1种三萜皂苷单体。皂苷大多具有抑瘤、抗菌等重要的生物活性,而其抗肿瘤作用具有重要的研究价值和诱人的开发前景。文章调研了有关九节龙皂苷的国内外文献报道,并分析了其相关抗肿瘤机制。研究表明,九节龙皂苷对肿瘤细胞有一定的抑制作用,对胶质瘤细胞较为突出。其诱导肿瘤细胞凋亡与促进Fas/Fas L表达及Caspase-3/Caspase-8活化,促进Bax表达,抑制Bcl-2表达,及BAD去磷酸化途径以及核内Ca2+浓度等有关;诱导肿瘤细胞自噬与促进Beclin-1及LC-3等表达有关;诱导肿瘤细胞侵袭与转移与下调MMP-2/MMP-9表达及E-钙黏素活性等有关。同时,体内药效学及药代动力学研究也证实了九节龙皂苷具有一定的抑制肿瘤作用。通过对九节龙皂苷体外抗肿瘤机制及体内抗肿瘤活性研究进展概述,以期为后期肿瘤治疗的临床前研究提供参考。