灵芝三萜类化合物抗癌作用机制的研究进展

<正>INTRODUCTION Ganoderma lucidum(Fr.)P.Karst.,a species of higher fungus called"Lingzhi"in Chinaor"Reishi"and"Mannendake"in Japan,has been used in the traditional Chinese medicine(TCM)for prevention and treatment     

龙葵的营养成分及其开发利用

本文介绍了中国龙葵的资源概况及开发前景.它具有分布广、蕴藏量大、抗逆性强、易栽培、营养丰富等特点.龙葵有很高的营养价值和药用价值,它含有人体所需的多种营养元素:17种氨基酸、维生素、糖分和蛋白质等.龙葵除有抑菌作用外,对癌细胞有一定的抑制作用,有望成为抗癌新药.幼苗可食用,浆果是制作果酒和饮料的好原料.开发龙葵资源前景广阔.     

Mechanisms of the Anticancer Action of Ganoderma lucidum (Leyss. ex Fr.) Karst.: A New Understanding

Ganoderma lucidum (Leyss. ex Fr.) Karst., a medicinal fungus called "Lingzhi" in China, has been used in traditional Chinese medicine in China for the prevention and treatment of various types of diseases, such as cancer, hepatopathy, arthritis, hypertension, neurasthenia, and chronic hepatitis. It is clear that the anticancer activity of G. lucidum is mainly due to polysaccharides and/or triterpenoids of the fungus. However, until now, the mechanism of the anticancer action of G. lucidum has not been well understood and, previously, the activation of the immune response of the host was widely considered to be the only mechanism by which G. lucidum prevented and/or treated cancer. However, recent studies reviewed in the present paper have shown that the potential mechanisms of anticancer action include not only the activation of the immune response of the host, but also the induction of cell differentiation, the induction of Phase Ⅱ-metabolizing enzymes, the inhibition of angiogenesis, and the inhibition of the expression of the urokinase-type plasminogen activator (uPA) and the uPA receptor in cancer cells. To further elucidate the mechanisms of action of G. lucidum, more in vivo tests and randomized controlled clinical trials should be carried out, and the molecular mechanisms should be studied intensively. Additionally, whether the anticancer compounds in G. lucidum act synergistically or independently should be further studied.     

Mechanisms of the Anticancer Action of Ganoderma lucidum （Leyss. ex Fr.） Karst.： A New Understanding

Ganoderma lucidum (Leyss. ex Fr.) Karst., a medicinal fungus called “Lingzhi” in China, has been used in traditional Chinese medicine in China for the prevention and treatment of various types of diseases, such as cancer, hepatopathy, arthritis, hypertension, neurasthenia, and chronic hepatitis. It is clear that the anticancer activity of G. lucidum is mainly due to polysaccharides and/or triterpenoids of the fungus. However, until now, the mechanism of the anticancer action of G. lucidum has not been well understood and, previously, the activation of the immune response of the host was widely considered to be the only mechanism by which G. lucidum prevented and/or treated cancer. However, recent studies reviewed in the present paper have shown that the potential mechanisms of anticancer action include not only the activation of the immune response of the host, but also the induction of cell differentiation, the induction of Phase Ⅱ-metabolizing enzymes, the inhibition of angiogenesis, and the inhibition of the expression of the urokinase-type plasminogen activator (uPA) and the uPA receptor in cancer cells. To further elucidate the mechanisms of action of G. lucidum, more in vivo tests and randomized controlled clinical trials should be carried out, and the molecular mechanisms should be studied intensively. Additionally, whether the anticancer compounds in G. lucidum act synergistically or independently should be further studied.     

The nutritional value of holothurians

In the current decade, holothurians are becoming more popular among researchers due to the recently obtained data about the chemical structures and physiological activities of bioactive ingredients that are extracted from these marine invertebrates. In Southeast Asia, Japan, Korea, and China, the use of these animals as a valuable food product and an object of traditional folk medicine has had a long history. At the same time, in western countries, as well as in Russia, products from sea cucumbers are little known and are often considered as an exotic oriental cuisine. This paper provides an analytical review of the literature that is dedicated to the nutritional value of holothurians as a potential source of components for functional food and nutraceuticals.     

Separation and isolation methods for analysis of the active principles of Sho-saiko-to (SST) oriental medicine

Sho-saiko-to (SST) was introduced into Japan as an oriental classical medicine from China approximately 1500 years ago, and it is currently the most representative Kampo medicine (traditional Japanese medicine). SST is manufactured in Japan as an ethical drug on a modern industrial scale in which the quality of ingredients is standardized with Good Manufacturing Practices (GMP) regulation. SST is widely used for the treatment of chronic hepatitis. Experimental and clinical studies including multi-center, placebo-controlled, double-blind studies have demonstrated the various pharmacological effects of SST. SST is prepared from the hot water extraction of seven raw materials, therefore many kinds of constituents are included. Three-dimensional (3D) HPLC analysis is useful for obtaining many kinds of constituents, especially low molecular ultraviolet (UV) quenching compounds, contained in SST as well as its fractions. Fingerprint pattern provided by 3D HPLC analysis makes possible to identify the overall-viewing of SST. Databases of UV spectra of the components of medicinal herbs obtained by reversed-phase (RP) HPLC using a photodiode array (PDA) and fingerprint patterns of crude drugs made by 3D HPLC analysis facilitate the identification, analysis and quality of herbal drugs. Studies using both PDA HPLC and an amino acid analysis with a fluorometric detector have found that SST contains fifteen major low molecular compounds (i.e. baicalin, wogonin-7-O-glucuronide, liquiritin, their three aglycons, liquiritin apioside, glycyrrhizin, saikosaponin b1, saikosaponin b2, ginsenoside Rg1, ginsenoside Rb1, (6)-gingerol, (6)-shogaol and arginine). These compounds have various pharmacological actions, and are assumed to be responsible, at least partly, for the pharmacological effects of SST. Although there have only been a few investigations on high molecular compounds with pharmacological actions contained in SST, several kinds of polysaccharides have been isolated from constituent herbs of SST. This review paper summarizes analytical methods of separation, isolation and identification of compounds with biological activities from SST, which is a mixture drug of medicinal herbs. Accordingly, this paper would not focus on methods of separation, isolation and analysis of particular compounds from each constituent herb of SST.     

灵芝对小鼠空间分辨学习与记忆的影响

本文用Y-型迷宫法测试小鼠空间分辨行为。实验结果表明,每日ig灵芝2.58/kg共7d,有明显促进学习的作用。每日ig灵芝2.5g/kg共7d或ig灵芝5g/kg共7d都能显著地拮坑东莨菪碱所致学习障碍的作用。此外,学习训练后立即ig灵芝2.5g/kg或ig灵芝5g/kg也有明显地改善东莨菪碱损害记忆巩固的作用。     

Discovery of quality-marker ingredients of Panax quinquefolius driven by high-throughput chinmedomics approach

BackgroundQuality control of traditional Chinese medicine (TCM) has always been a hot issue to TCM. However, due to the complexity of TCM ingredients, the current quality standards of TCM have problems that are difficult to guarantee clinical efficacy. American ginseng, the dried roots of Pawajc quinquefolium L. (Araliaceae), is a valuable herbal medicine due to various pharmacological effects and huge health benefit, which are associated with numerous active ingredients such as ginsenosides. Although a large number of studies have investigated the active ingredients of American ginseng, Q-markers reflecting comprehensive review on its efficacies has yet been unrevealed.PurposeThe study aims to discover the Q-markers of Panax quinquefolius (American ginseng), provides a powerful method to clarify the significant ingredents of TCM and help further discovering extensive quality evaluation model,contributing to a significant improvement of TCM quality standard.MethodsMice general status, biochemical indexes assay, urine metabolic profile, and serum metabolic profile were utilized for model replication and efficacy evaluation. The in vitro and in vivo constituents of American ginseng using ultra-high performance liquid chromatography coupled with mass spectrometry (UPLC-MS) with Serum Pharmacochemistry of TCM were in-depth investigated. Q-markers that were associated with core markers of therapeutic effects were excavated by a plotting of correlation between marker metabolites and serum constituents (PCMS) approach.ResultsCorrelation analysis of 41 blood and urine labeled metabolites with 14 serum components showed that 24-methyl-7-cholesten-3β-ol, zizybeoside II, betulin, ginsenoside Rd, cinnamyl alcohol, pseudoginsenoside F11 is highly correlated with the therapeutic effects of Compound Zaofan Pill (CZP), while pseudoginsenoside F11 and ginsenoside Rd are highly correlated with the therapeutic effects of American ginseng. The six absorbed blood compounds can be considered as potential Q-markers for compound, of which two compounds, such as pseudoginsenoside F11 and ginsenoside Rd, can be considered as potential Q-markers for American ginseng.ConclusionThe study has demonstrated that the Chinmedomics is an effective, comprehensive and fire-new method for discovering the Q-markers of TCM, and it may be more reasonable choices to establish quality standards of TCM.     

Phytochemical Constituents and Biological Activities of Plants from the Genus Cissampelos

Cissampelos is a significant genus comprising of approximately 21 species of the medicinal plants (Menispermaceae). The plants of this genus are used in traditional medicine for the treatment of various ailments such as asthma, arthritis, dysentery, hyperglycemia, cardiopathy, hypertension and other related problems. These plants are rich in bioactive dibenzylisoquinoline and aborphine as well as small amounts of other ingredients. In recent years, the chemical constituents and pharmacological activities of Cissampelos genus have been paid more and more attention due to their diversity. Herein, we compile the chemical constituents and biological activities on this genus, and summarize the ¹³C-NMR data of the main bioactive ingredients. All information comes from scientific databases such as Google Scholar, PubMed, Sci-Finder, ScienceDirect, Web of Science and CNKI. It provides valuable data for the future research and development of Cissampelos genus.     

A highly contiguous genome assembly of red perilla (Perilla frutescens) domesticated in Japan

Perilla frutescens (Lamiaceae) is an important herbal plant with hundreds of bioactive chemicals, among which perillaldehyde and rosmarinic acid are the two major bioactive compounds in the plant. The leaves of red perilla are used as traditional Kampo medicine or food ingredients. However, the medicinal and nutritional uses of this plant could be improved by enhancing the production of valuable metabolites through the manipulation of key enzymes or regulatory genes using genome editing technology. Here, we generated a high-quality genome assembly of red perilla domesticated in Japan. A near-complete chromosome-level assembly of P. frutescens was generated contigs with N50 of 41.5 Mb from PacBio HiFi reads. 99.2% of the assembly was anchored into 20 pseudochromosomes, among which seven pseudochromosomes consisted of one contig, while the rest consisted of less than six contigs. Gene annotation and prediction of the sequences successfully predicted 86,258 gene models, including 76,825 protein-coding genes. Further analysis showed that potential targets of genome editing for the engineering of anthocyanin pathways in P. frutescens are located on the late-stage pathways. Overall, our genome assembly could serve as a valuable reference for selecting target genes for genome editing of P. frutescens.     

中草药在防治新型冠状病毒肺炎中的应用

新型冠状病毒肺炎(COVID-19)是由新型冠状病毒引起的突发性传染病,具有极强的传染性和致病性,感染者常伴有发烧、乏力、咳嗽等症状,自2019年12月首次发现以来,新型冠状病毒肺炎迅速席卷全球,受到国内外高度关注。中医药是我国传统特色文化,国家卫健委、中医药管理局在《新型冠状病毒感染的肺炎诊疗方案(试行第三版)》中首次推出中医药治疗方案,其中清热解毒、补气活血、清肺化痰等中药为新冠肺炎防治中常用中草药类型,槲皮素、山奈酚、黄芩素等黄酮类成分为主要活性成分。实践证明,中草药在抗病毒、抗炎、减轻患者症状等方面有显著效果,特别是我国新冠肺炎患者总体治愈率达94%以上,远高于其他国家。文中在概述新型冠状病毒特征的基础上,综述中医药治疗新冠肺炎中涉及的药用植物及其有效成分研究进展,为防治新冠肺炎药物研发提供参考。     

植物苯丙烷代谢途径

众所周知,固着生长的植物经常受到环境中各种生物和非生物胁迫的威胁。所以在漫长的进化过程中,植物必须将多样的环境信号整合到其发育过程中,以实现适应性形态的发生和代谢途径的精确调控,最终使植物完成整个生长周期。研究显示,苯丙烷代谢作为植物重要的次级代谢途径之一,其代谢产物,例如木质素、孢粉素、花青素和有机酸等,在调控植物适应性生长的过程中发挥着重要功能。特别是在药用植物中,苯丙烷代谢还与众多药用活性成分的合成息息相关,几乎所有包含苯丙烷骨架的天然药效成分均由苯丙烷代谢途径直接或间接合成,例如黄酮类、萜类和酚类等。此外,经苯丙烷代谢途径产生的一些次级代谢产物还能由植物根系外泌到周际土壤中,通过改变根系微生物的菌群生态,而影响植物生长和抵抗生物或非生物胁迫的能力。同时,苯丙烷代谢介导的这种植物-微生物互作也与药用植物的道地品质密不可分。本文综述了近年来植物苯丙烷代谢途径的最新研究进展,重点对该代谢途径中代谢产物的生理功能及表达调控机制进行了介绍,以期更深入地理解药用植物苯丙烷代谢与药材性状之间的潜在关系,旨在指导优良中草药的遗传育种,以进一步促进我国中医药事业的蓬勃发展。     

Comparative chemical profiling of three TCM drugs in the Paeoniaceae family by UPLC-MS/MS combined with chemometric methods

Paeoniae Radix Rubra (Chi-Shao in Chinese) and Paeoniae Radix Alba (Bai-Shao in Chinese) are two valuable traditional Chinese medicine (TCM) drugs, usually indicated for menstrual disorders and viral infections. Paeonia anomala subsp. anomala (Xinjiang-Shaoyao in Chinese) is taken as Chi-Shao substitute in Xinjiang, China. Due to the diverse growing conditions, there are some differences in chemical compositions of three TCM drugs. An UPLC fingerprint analysis with chemometric methods, including similarity analysis and hierarchical clustering analysis, was applied in the study. By virtue of UPLC-QTOF-MS, 29 components including 18 monoterpene glycosides, 5 galloyl glucoses and 6 phenolic compounds were simultaneously identified. It could be concluded that the UPLC-QTOF-MS combined with chemometric methods could efficiently identify the three TCM drugs, and was a powerful approach for the chemical profiling of three TCM drugs. The developed method provide an available approach for quality control of three TCM drugs.     

Naturapotheke Mistel

The mistletoe in the un‐conventional and the molecular medicine The mistletoe is an evergreen semi‐parasite which is growing on trees. It is impressive by its unique appearance, its world‐wide dissemination and the great variety of its chemical components and active substances. Only in newer times the mistletoe with its ingredients have found a way into the un‐conventional, and finally into the molecular medicine. The spectrum of the active ingredients is rather well‐known now based on the extensively investigated European mistletoe (Viscum album).     

Active Ingredients and Anti‐Arthritic Mechanisms of Ba‐Wei‐Long‐Zuan Granule Revealed by 1H‐NMR‐Based Metabolomics Combined with Network Pharmacology Analysis

Ba‐Wei‐Long‐Zuan granule (BWLZ) is a traditional herbal preparation. It has been widely used for the treatment of rheumatoid arthritis (RA). However, its active ingredients and mechanisms of action are still unclear. The present study aims to reveal the active compounds and anti‐arthritic mechanisms of BWLZ against collagen‐induced arthritis (CIA) by using ¹H‐NMR‐based metabolomics, molecular docking and network pharmacology methods. After 30 days of administration, BWLZ could effectively improve the metabolic disorders in CIA rats. The anti‐arthritic effect of BWLZ was related to its restoration of 16 disturbed serum metabolites. Molecular docking and network analysis showed that 20 compounds present in BWLZ could act on multiple targets. Among them, coclaurine and hesperidin showed the highest hit rates for target proteins related to both metabolic regulation and RA, indicating that these two compounds might be potential active ingredients of BWLZ. Moreover, pathway enrichment analysis suggested that the anti‐arthritic mechanisms of BWLZ might be attributed to its network regulation of several biological processes, such as steroid hormone biosynthesis, mTOR signaling pathway, alanine, aspartate and glutamate metabolism, and synthesis and degradation of ketone bodies. These results provide further evidence for the anti‐arthritic properties of BWLZ and are beneficial for its quality control and clinical application. The potential targets and biological processes found in this study may provide valuable information for further studying the molecular mechanisms of BWLZ against RA. In addition, our work provides new insights for revealing the active ingredients and regulatory mechanisms of complex herbal preparations.     

赤霉属真菌诱导龙血竭形成的HPLC指纹图谱

龙血竭为百合科植物龙血树所产的树脂类药材,常常因树干部位受损伤后,经微生物侵染并分泌树脂,经提而成。本研究以活性菌株诱导所得龙血竭药材为研究对象,采用HPLC指纹图谱与对照药材相比较,为其质量控制提供评价及分析方法。采用ZORBAX SB-C18色谱柱（5μm,4.6mm×250mm）,流动相A为30%乙腈+0.3%乙酸,流动相B为100%乙腈,梯度洗脱,流速1.0mL/min,检测波长278nm与309nm,柱温25℃。结果发现,各龙血竭样品指纹图谱与对照样品相似度高,确定14个共有峰,并通过对照指认了7,4’-二羟基黄酮、龙血素A、龙血素B和白藜芦醇共4个特征性化学成分。本研究发现活性真菌菌株诱导产物可作为天然龙血竭的替代品,诱导药材质量佳,诱导效果好。     

Review: Insects and former foodstuffs for upgrading food waste biomasses/streams to feed ingredients for farm animals

The increasing global need to find alternative protein/energy sources has triggered research in the field of non-conventional feed ingredients, with insects and former foodstuffs being the most promising. Insects contain high level of protein and fat, whereas former foodstuffs contain high energy in the form of carbohydrates and fats; therefore, both should be considered as promising alternative feed ingredients for livestock production. In addition to the nutritional value, they also represent a way by which food waste biomasses/streams can be upgraded to valuable feed ingredients. This review outlines the main nutritional and safety issues of insects and former foodstuffs, and also considers the legal framework involved. The importance of the type of insect metamorphosis and tailored substrates that could lead to the production of a premium feed is also described. This is also the first time that a review discusses the nutritional quality of former foodstuffs. Energy and the main nutrient content of former foodstuff are compared with the composition of common cereals as the principal energy sources in animal feed. For both ingredients a critical review of the safety issues is provided. Based on the current data available, both insects and former foodstuffs have an excellent potential use as alternative feed ingredients for livestock production. When produced in line with the criteria set by major feed/food authorities, they are characterized by high quality and safety standards. This makes them comparable to other feed materials and ingredients currently available on the market, although their full nutritional, functional, safety and sustainability evaluation cannot be considered complete.     

中药渣降解特性及养分资源循环利用研究

中药渣是药效成分在提取加工过程中产生的中药废弃物，若作为一种新的资源应用于其他领域，不仅能充分利用其中残留的有效成分，还能解决传统药渣处理方式造成的环境污染问题。本文围绕不同种类药渣的降解特性，综述其养分资源的综合利用途径，探讨药渣处理过程中存在的问题及理论可行的处理方法，从而为中药废弃物资源化利用提供参考，为中医药事业的可持续发展提供新的思路。     

灵芝抗氧化清除自由基作用的研究

文中综述了灵芝的抗氧化清除自由基作用。灵芝对各种因素引起的脑、心脏、胰腺、肝脏、胃肠道、肾脏和其他重要脏器的脂质过氧化损伤具有明显的保护作用。灵芝可显著减少脂质过氧化产物丙二醛(MDA)的含量,增强抗氧化酶如超氧化物歧化酶(SOD)、谷胱甘肽过氧化物酶(GSH-PX)以及其他抗氧化酶的活性。稹灵芝对体外培养的巨噬细胞(小鼠)、胰岛细胞(小鼠)、大脑皮层细胞(大鼠)、嗜铬细胞瘤细胞(大鼠)、血管内皮细胞(大鼠、人)和皮肤角质细胞(人)的氧化损伤具有明显保护作用。灵芝在体内外对不同动物模型和细胞模型的抗氧化清除自由基作用可能与其免疫调节、抗肿瘤、降血压、降血糖、保肝、心血管保护和抗衰老作用的机制有关。