抗癌活性天然产物Cryptophycins的研究进展

总结了具有强抗癌活性的天然产物cryptophycins及其结构类似物的研究进展, 内容包括cryptophycin的合成、 活性-结构关系规律以及结构类似物的研究情况.     

Bioactive Components of Salvia and Their Potential Antidiabetic Properties: A Review

The utilization of therapeutic plants is expanding around the globe, coupled with the tremendous expansion of alternative medicine and growing demand in health treatment. Plants are applied in pharmaceuticals to preserve and expand health—physically, mentally and as well as to treat particular health conditions and afflictions. There are more than 600 families of plants identified so far. Among the plants that are often studied for their health benefit include the genus of Salvia in the mint family, Lamiaceae. This review aims to determine the bioactive components of Salvia and their potential as antidiabetic agents. The search was conducted using three databases (PubMed, EMBASE and Scopus), and all relevant articles that are freely available in the English language were extracted within 10 years (2011–2021). Salvia spp. comprises many biologically active components that can be divided into monoterpenes, diterpenes, triterpenes, and phenolic components, but only a few of these have been studied in-depth for their health benefit claims. The most commonly studied bioactive component was salvianolic acids. Interestingly, S. miltiorrhiza is undoubtedly the most widely studied Salvia species in terms of its effectiveness as an antidiabetic agent. In conclusion, we hope that this review stimulates more studies on bioactive components from medicinal plants, not only on their potential as antidiabetic agents but also for other possible health benefits.     

漆酶在催化合成生物活性化合物中的研究进展

近年来市场对具有营养和药用价值的活性化合物的需求量逐年增加,传统的生产方法已无法满足该类化合物的大规模应用。漆酶是近些年广受欢迎的生物催化剂之一,它可以在温和的条件下催化活性化合物的高效合成,并且有极大潜力取代传统的工业生产方法。本文着重回顾了近十年来漆酶在催化合成活性化合物中的应用,并对漆酶的结构及作用机制进行了介绍;同时指出了漆酶工业化应用中存在的一些问题,比如漆酶产量不足、部分酶促反应介质不适于工业化应用等。通过异源表达、筛选高产菌株提高漆酶产量、使用固定化技术和蛋白质工程提高漆酶的使用寿命、开发更加高效低廉的反应介质系统与寻找新的漆酶底物相结合来降低漆酶的应用成本是今后主要的发展趋势。     

Plants of the Genus Zingiber: A Review of Their Ethnomedicine,Phytochemistry and Pharmacology

Plant of the genus Zingiber (Zingiberaceae) have primarily distributed in subtropical and tropical Asia, South America and Africa. The species of this genus have been widely used as food and in folk with a long history for treating various diseases. Reports related to the phytochemistry and phytochemistry of Zingiber species are numerous, but articles on the summary of the genus Zingiber remain scarce. This review aims at presenting comprehensive information about the genus Zingiber and providing a reference for the future application by systematically reviewing the literature from 1981 to 2020. Currently, a total of 447 phytochemical constituents have been isolated and identified from this genus, in which volatile oils, diarylheptanoids, gingerols, flavonoids and terpenoids are the major components. Gingerols, which are the main functional components, are the spicy and aromatic ingredients in the Zingiber species. Extracts and single compounds from Zingiber plants have been discovered to possess numerous biological functions, such as anti-inflammatory, anticancer, antimicrobial, larvicidal, antioxidant and hypoglycemic activities. This review provides new insights into the ethnomedicine, phytochemistry and pharmacology of the genus Zingiber and brings to the forefront key findings on the functional components of this genus in food and pharmaceutical industries.     

A Historical Review of the Total Synthesis of Natural Products Developed in Portugal

Total synthesis of natural products is an important discipline of organic chemistry that has enabled the development of new synthetic methods and strategies for the preparation and study of the structure and reactivity of complex naturally occurring products. In this review we summarize the synthetic strategies developed in Portugal by several research groups for the synthesis of bioactive natural products including alkaloids, cyclitols, fatty alcohols, phenylpropanoic acids, γ-butyrolactones, xanthones and nucleosides.     

A Review on Mechanistic Insight of Plant Derived Anticancer Bioactive Phytocompounds and Their Structure Activity Relationship

Cancer is a disorder that rigorously affects the human population worldwide. There is a steady demand for new remedies to both treat and prevent this life-threatening sickness due to toxicities, drug resistance and therapeutic failures in current conventional therapies. Researchers around the world are drawing their attention towards compounds of natural origin. For decades, human beings have been using the flora of the world as a source of cancer chemotherapeutic agents. Currently, clinically approved anticancer compounds are vincristine, vinblastine, taxanes, and podophyllotoxin, all of which come from natural sources. With the triumph of these compounds that have been developed into staple drug products for most cancer therapies, new technologies are now appearing to search for novel biomolecules with anticancer activities. Ellipticine, camptothecin, combretastatin, curcumin, homoharringtonine and others are plant derived bioactive phytocompounds with potential anticancer properties. Researchers have improved the field further through the use of advanced analytical chemistry and computational tools of analysis. The investigation of new strategies for administration such as nanotechnology may enable the development of the phytocompounds as drug products. These technologies have enhanced the anticancer potential of plant-derived drugs with the aim of site-directed drug delivery, enhanced bioavailability, and reduced toxicity. This review discusses mechanistic insights into anticancer compounds of natural origins and their structural activity relationships that make them targets for anticancer treatments.     

A Review on Gold Nanotriangles: Synthesis,Self-Assembly and Their Applications

Gold nanoparticles (AuNPs) with interesting optical properties have attracted much attention in recent years. The synthesis and plasmonic properties of AuNPs with a controllable size and shape have been extensively investigated. Among these AuNPs, gold nanotriangles (AuNTs) exhibited unique optical and plasmonic properties due to their special triangular anisotropy. Indeed, AuNTs showed promising applications in optoelectronics, optical sensing, imaging and other fields. However, only few reviews about these applications have been reported. Herein, we comprehensively reviewed the synthesis and self-assembly of AuNTs and their applications in recent years. The preparation protocols of AuNTs are mainly categorized into chemical synthesis, biosynthesis and physical-stimulus-induced synthesis. The comparison between the advantages and disadvantages of various synthetic strategies are discussed. Furthermore, the specific surface modification of AuNTs and their self-assembly into different dimensional nano- or microstructures by various interparticle interactions are introduced. Based on the unique physical properties of AuNTs and their assemblies, the applications towards chemical biology and sensing were developed. Finally, the future development of AuNTs is prospected.     

A Review: Meridianins and Meridianins Derivatives

Meridianins are a family of indole alkaloids derived from Antarctic tunicates with extensive pharmacological activities. A series of meridianin derivatives had been synthesized by drug researchers. This article reviews the extraction and purification methods, biological activities and pharmacological applications, pharmacokinetic characters and chemical synthesis of meridianins and their derivatives. And prospects on discovering new bioactivities of meridianins and optimizing their structure for the improvement of the ADMET properties are provided.     

Microencapsulation of Bioactive Ingredients for Their Delivery into Fermented Milk Products: A Review

The popularity and consumption of fermented milk products are growing. On the other hand, consumers are interested in health-promoting and functional foods. Fermented milk products are an excellent matrix for the incorporation of bioactive ingredients, making them functional foods. To overcome the instability or low solubility of many bioactive ingredients under various environmental conditions, the encapsulation approach was developed. This review analyzes the fortification of three fermented milk products, i.e., yogurt, cheese, and kefir with bioactive ingredients. The encapsulation methods and techniques alongside the encapsulant materials for carotenoids, phenolic compounds, omega-3, probiotics, and other micronutrients are discussed. The effect of encapsulation on the properties of bioactive ingredients themselves and on textural and sensory properties of fermented milk products is also presented.     

我国大戟二萜酯及其生理活性研究新进展

介绍了我国近１０年来从大戟属植物中发现的二萜酯类新化合物及它们的刺激性，抗癌活性和杀菌作用等生理活性的研究，其中包括５种新发现碳骨架的２０个高氧化型二萜多酯类化合物。     

Synthetic Studies of the Zoanthamine Alkaloids: Total Synthesis of Zoanthenol Based on an Isoaromatization Strategy

The total synthesis of zoanthenol, a unique aromatic member of the zoanthamine alkaloids, which has exhibited potent anti‐platelet activities on human platelet aggregation, is described in full detail. The key step involves a Brønsted acid‐promoted isoaromatization in the AB ring system to install the crucial aromatic ring. We have not only succeeded in the first total synthesis of zoanthenol, but also established an alternative efficient synthetic route from the commercially available norzoanthamine hydrochloride to zoanthenol.     

Acylhydrazones and Their Biological Activity: A Review

Due to the structure of acylhydrazones both by the pharmacophore –CO–NH–N= group and by the different substituents present in the molecules of compounds of this class, various pharmacological activities were reported, including antitumor, antimicrobial, antiviral, antiparasitic, anti-inflammatory, immunomodulatory, antiedematous, antiglaucomatous, antidiabetic, antioxidant, and actions on the central nervous system and on the cardiovascular system. This fragment is found in the structure of several drugs used in the therapy of some diseases that are at the top of public health problems, like microbial infections and cardiovascular diseases. Moreover, the acylhydrazone moiety is present in the structure of some compounds with possible applications in the treatment of other different pathologies, such as schizophrenia, Parkinson’s disease, Alzheimer’s disease, and Huntington’s disease. Considering these aspects, we consider that a study of the literature data regarding the structural and biological properties of these compounds is useful.     

Pyrrolizidine Alkaloids and Bisabolane Sesquiterpenes from the Roots of Ligularia cymbulifera

The new pyrrolizidine alkaloid glycoside 1 , and the three new highly oxygenated bisabolane sesquiterpenes 4 – 6 , together with the two known pyrrolizidine alkaloids 2 and 3 , were isolated from the roots of Ligularia cymbulifera (W. W. Smith ) Hand .‐Mazz . Their structures were established on the basis of spectroscopic analysis, especially 1D‐ and 2D‐NMR data. The cytotoxic activities of compounds 1, 2 , and 4 – 6 were evaluated against hepatoma (BEL‐7402), human leukemia (HL‐60), human ovarian carcinoma (HO‐8910), and nasopharyngeal carcinoma (KB) cell lines (Tables 1–3). Compound 6 s howed weak cell‐growth inhibition of BEL‐7402 cell.     

Extraction,Isolation and Characterization of Bioactive Compounds from Artemisia and Their Biological Significance: A Review

Diverse medicinal plants such as those from the genus Artemisia have been employed globally for centuries by individuals belonging to different cultures. Universally, Artemisia species have been used to remedy various maladies that range from simple fevers to malaria. A survey conducted by the World Health Organization (WHO) demonstrated that 80% of the global population is highly reliant on herbal medicine for their primary healthcare. WHO recommends artemisinin-based combination therapies (ACT) for the treatment of global diseases such as malaria. Artemisinin is a bioactive compound derived from Artemisia annua leaves. It is a sesquiterpene endoperoxide with potent antimalarial properties. This review strives to instill natural products to chemists and others in diverse fields with a heterogeneous set of knowledge compiled from multifaceted researchers and organizations in literature. In particular, the various Artemisia species and effective extraction, isolation, and characterization methodologies are discussed in detail. An in-depth investigation into the literature reveals that divergent species of Artemisia exhibit a vast array of biological activities such as antimalarial, antitumor, and anti-inflammatory activities. There is substantial potential for bioactive compounds from Artemisia to provide significant relief from differing human ailments, but more meticulous research in this field is needed.     

Biosynthetically Inspired Syntheses of Secu′amamine A and Fluvirosaones A and B

Presented here is a concise synthesis of secu′amamine A, and fluvirosaones A and B from readily available allosecurinine and viroallosecurinine. The key C2‐enamine derivative of (viro)allosecurinine, the presumed biosynthetic precursors of these natural products, was accessed, for the first time, by a VO(acac)₂‐mediated regioselective Polonovski reaction. Formal hydration and 1,2‐amine shift of this pluripotent enamine compound afforded secu′amamine A. Formal oxidative [3+2] cycloaddition reaction between this enamine and TMS‐substituted methallyl iodide reagent paved the way to the precursors of fluvirosaones A and B. The relative stereochemistry at the C2 position of these advanced intermediates governs the fate of 1,2‐amine shift leading to fluvirosaones A and B. The syntheses of potential biosynthetic precursors and investigations of their chemical reactivities have provided insights regarding the biogenesis of these natural products.     

The Genus Cladosporium: A Rich Source of Diverse and Bioactive Natural Compounds

Fungi are renowned as one of the most fruitful sources of chemodiversity and for their ubiquitous occurrence. Among the many taxonomic groupings considered for the implications deriving from their biosynthetic aptitudes, the genus Cladosporium stands out as one of the most common in indoor environments. A better understanding of the impact of these fungi on human health and activities is clearly based on the improvement of our knowledge of the structural aspects and biological properties of their secondary metabolites, which are reviewed in the present paper.     

Methods for the construction of [1,2]isoindolo-condensed benzazepines, benzazocines, quinolines, and isoquinolines. 1. Isoindolobenzazepines, isoindolobenzazocines. (Review)

Data on methods for the construction of tetracyclic systems in which an isoindole ring is condensed with benzazepines and benzazocines on the [1,2] side are reviewed. The reaction conditions and approaches leading to isoindolobenzazepines and isoindolobenzazocines are discussed. Examples of the synthesis of physiologically active natural alkaloids with the structure of the above-mentioned condensed isoindoles are presented. Data for 1959–2004 are included. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 7, pp. 963–994, July, 2006.     

Methods for the construction of [1,2]isoindolo-condensed benzazepines, benzazocines, quinolines, and isoquinolines. 2. Isoindoloquinolines, isoindoloisoquinolines. (Review)

Data for 1966–2004 on methods for the construction of tetracyclic systems in which an isoindole ring is condensed with quinoline and isoquinoline fragments on the [1,2] side are reviewed. Methods and conditions for the synthesis of isoindoloquinolines and isoindoloisoquinolines are examined. Examples of the synthesis of physiologically active natural alkaloids possessing the structure of these condensed isoindoles are presented. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1123–1157, August, 2006.