Recent Advances in Drug Discovery from South African Marine Invertebrates

Recent developments in marine drug discovery from three South African marine invertebrates, the tube worm Cephalodiscus gilchristi, the ascidian Lissoclinum sp. and the sponge Topsentia pachastrelloides, are presented. Recent reports of the bioactivity and synthesis of the anti-cancer secondary metabolites cephalostatin and mandelalides (from C. gilchristi and Lissoclinum sp., respectively) and various analogues are presented. The threat of drug-resistant pathogens, e.g., methicillin-resistant Staphylococcus aureus (MRSA), is assuming greater global significance, and medicinal chemistry strategies to exploit the potent MRSA PK inhibition, first revealed by two marine secondary metabolites, cis-3,4-dihydrohamacanthin B and bromodeoxytopsentin from T. pachastrelloides, are compared.     

Anticancer Activities of Plant Secondary Metabolites: Rice Callus Suspension Culture as a New Paradigm

Plant natural products including alkaloids,polyphenols,terpenoids and flavonoids have been reported to exert anticancer activity by targeting various metabolic pathways.The biological pathways regulated by plant products can serve as novel drug targets.Plant natural compounds or their derivatives used for cancer treatment and some novel plant-based compounds which are used in clinical trials were discussed.Callus suspension culture with secondary metabolites can provide a continuous source of plant pharmaceuticals without time and space limitations.Previous research has shown that rice callus suspension culture can kill>95%cancer cells with no significant effect on the growth of normal cells.The role of candidate genes and metabolites which are likely to be involved in the process and their potential to serve as anticancer and anti-inflammatory agents were discussed.Large scale production of plant callus suspension culture and its constituents can be achieved using elicitors which enhance specific secondary metabolites combined with bioprocess technology.     

寒兰根内生真菌诱导子对白芨种子萌发和幼苗生长的影响

真菌诱导子可在一定程度上提高植物次生代谢物的积累,而白芨是一种具有极高经济价值和药用价值的药材.本文从野生寒兰的根中培养分离得到23种内生真菌,再制成真菌诱导子添加到自制的液体培养基中,将白芨种子放入该液体培养基进行无菌震荡培养,以研究真菌诱导子对白芨种子萌发和幼苗生长的影响.结果表明,15号真菌诱导子能显著缩短白芨种...     

Effects of growing location on the contents of secondary metabolites in the leaves of four selected superior clones of Eucommia ulmoides

The interior quality of an herbal medicine is determined by its secondary metabolites. Secondary metabolites that are contained in medicinal plants may be different in types, contents, and proportions of the constituents because of the differences in production locations. Four excellent clones of Eucommia ulmoides, Qinzhong No. 1 to 4, which have been selected from 40 clones from all over China, were planted in 6 main cultivation locations. The contents of secondary metabolites, including chlorogenic acid, flavonoids and geniposidic acid contained in the leaves of each clone were measured. Gray correlation and path analysis were conducted among the contents of secondary metabolites and environmental factors, such as altitude, annual sunshine duration, annual precipitation, and annual average temperature. The results showed that environmental factors had significant impacts on the contents of secondary metabolites of the 4 clones. High degrees of association were found between altitude, annual average temperature in the locations tested and the contents of chlorogenic acid and flavonoids, between the annual sunshine duration, annual average temperature and the contents of geniposidic acid. Altitude and annual average temperature are key environmental factors for the accumulation of chlorogenic acid and flavonoids, while annual sunshine duration and annual average temperature are key ones for geniposidic acid. Altitude and annual average temperature were significantly and positively correlated to the contents of chlorogenic acid and flavonoids (P < 0.05). Annual sunshine duration was significantly and positively correlated to the content of geniposidic acid (P < 0.05), while annual average temperature was significantly and negatively correlated to the content of geniposidic acid (P < 0.05). No significant correlation was observed between the annul precipitation and the contents of each secondary metabolite. It was concluded that from the view of the contents of the secondary metabolites, Lueyang in Shaanxi Province, Lingbao in Henan Province, and Zunyi in Guizhou Province are preferable for the cultivation of E. ulmoides in China.     

Marine Microbial-Derived Resource Exploration: Uncovering the Hidden Potential of Marine Carotenoids

Microbes in marine ecosystems are known to produce secondary metabolites. One of which are carotenoids, which have numerous industrial applications, hence their demand will continue to grow. This review highlights the recent research on natural carotenoids produced by marine microorganisms. We discuss the most recent screening approaches for discovering carotenoids, using in vitro methods such as culture-dependent and culture-independent screening, as well as in silico methods, using secondary metabolite Biosynthetic Gene Clusters (smBGCs), which involves the use of various rule-based and machine-learning-based bioinformatics tools. Following that, various carotenoids are addressed, along with their biological activities and metabolic processes involved in carotenoids biosynthesis. Finally, we cover the application of carotenoids in health and pharmaceutical industries, current carotenoids production system, and potential use of synthetic biology in carotenoids production.     

Cyanobacteria—From the Oceans to the Potential Biotechnological and Biomedical Applications

Cyanobacteria are photosynthetic prokaryotic organisms which represent a significant source of novel, bioactive, secondary metabolites, and they are also considered an abundant source of bioactive compounds/drugs, such as dolastatin, cryptophycin 1, curacin toyocamycin, phytoalexin, cyanovirin-N and phycocyanin. Some of these compounds have displayed promising results in successful Phase I, II, III and IV clinical trials. Additionally, the cyanobacterial compounds applied to medical research have demonstrated an exciting future with great potential to be developed into new medicines. Most of these compounds have exhibited strong pharmacological activities, including neurotoxicity, cytotoxicity and antiviral activity against HCMV, HSV-1, HHV-6 and HIV-1, so these metabolites could be promising candidates for COVID-19 treatment. Therefore, the effective large-scale production of natural marine products through synthesis is important for resolving the existing issues associated with chemical isolation, including small yields, and may be necessary to better investigate their biological activities. Herein, we highlight the total synthesized and stereochemical determinations of the cyanobacterial bioactive compounds. Furthermore, this review primarily focuses on the biotechnological applications of cyanobacteria, including applications as cosmetics, food supplements, and the nanobiotechnological applications of cyanobacterial bioactive compounds in potential medicinal applications for various human diseases are discussed.     

Rice Metabolomics

Metabolomics is a recently developed technology for comprehensive analysis of metabolites in organisms. Plant metabolites that are produced for the growth, development, and chemical defense of plants against climatic alterations or natural predators are also useful to us as nutrients or medicines; hence, it is important to comprehend the amounts and varieties of plant metabolites. Besides providing an understanding of the metabolic state in plants under various circumstances, metabolomic techniques are applicable to the clarification of the functions of unknown genes by using natural variants or mutants of the target plants. Furthermore, a metabolomic approach might be useful in the breeding of crops, since valuable plant traits such as taste and yield are closely related to metabolic conditions. Here, we describe the methodology of metabolomics including sample extraction and preparation, metabolite detection, and data processing and analysis, and introduce the application of metabolomic studies to rice.     

Identification of Rosellinia species as producers of cyclodepsipeptide PF1022 A and resurrection of the genus Dematophora as inferred from polythetic taxonomy

Rosellinia (Xylariaceae) is a large, cosmopolitan genus comprising over 130 species that have been defined based mainly on the morphology of their sexual morphs. The genus comprises both lignicolous and saprotrophic species that are frequently isolated as endophytes from healthy host plants, and important plant pathogens. In order to evaluate the utility of molecular phylogeny and secondary metabolite profiling to achieve a better basis for their classification, a set of strains was selected for a multi-locus phylogeny inferred from a combination of the sequences of the internal transcribed spacer region (ITS), the large subunit (LSU) of the nuclear rDNA, beta-tubulin (TUB2) and the second largest subunit of the RNA polymerase II (RPB2). Concurrently, various strains were surveyed for production of secondary metabolites. Metabolite profiling relied on methods with high performance liquid chromatography with diode array and mass spectrometric detection (HPLC-DAD/MS) as well as preparative isolation of the major components after re-fermentation followed by structure elucidation using nuclear magnetic resonance (NMR) spectroscopy and high resolution mass spectrometry (HR-MS). Two new and nine known isopimarane diterpenoids were identified during our mycochemical studies of two selected Dematophora strains and the metabolites were tested for biological activity. In addition, the nematicidal cyclodepsipeptide PF1022 A was purified and identified from a culture of Rosellinia corticium, which is the first time that this endophyte-derived drug precursor has been identified unambiguously from an ascospore-derived isolate of a Rosellinia species. While the results of this first HPLC profiling were largely inconclusive regarding the utility of secondary metabolites as genus-specific chemotaxonomic markers, the phylogeny clearly showed that species featuring a dematophora-like asexual morph were included in a well-defined clade, for which the genus Dematophora is resurrected. Dematophora now comprises all previously known important plant pathogens in the genus such as D. arcuata, D. bunodes, D. necatrix and D. pepo, while Rosellinia s. str. comprises those species that are known to have a geniculosporium-like or nodulisporium-like asexual morph, or where the asexual morph remains unknown. The extensive morphological studies of L.E. Petrini served as a basis to transfer several further species from Rosellinia to Dematophora, based on the morphology of their asexual morphs. However, most species of Rosellinia and allies still need to be recollected in fresh state, cultured, and studied for their morphology and their phylogenetic affinities before the infrageneric relationships can be clarified.     

茶树生长光调控研究进展

茶树生长发育受外界环境因素的影响,光是重要的因素之一,可单独或与温度等其他环境因素协同调控茶树生长发育及次生代谢产物的合成。介绍了近年来国内外光调控茶树生长及其代谢方面的研究进展,重点探讨了不同光谱波段、光子通量和光周期对茶树生长、代谢产物组分的影响,明确茶树生长、代谢的光调控过程,解析光调控机制,为开发可用于生产实践的茶树光调控技术奠定理论基础。     

雷州半岛实荣村风水林植物调查及现状分析

断奶日龄的选择对养猪生产至关重要。在现代养猪生产中,早期断奶是制约规模化养猪的瓶颈问题,往往造成仔猪断奶后食欲差、消化不良、腹泻、免疫功能下降等“仔猪早期断奶综合症”,严重制约养猪业的发展,而产生这一后果的主要原因是断奶使肠粘膜屏障受损。因此,选择适宜的仔猪断奶日对养猪生产具有重要的意义。本文综述了断奶日龄对仔猪生产性能和肠粘膜屏障的影响,以期为实际生产中确定适合的断奶日龄提供参考依据。     

具有活性的红树林真菌的多样性研究进展——优势菌为子囊菌和半知菌

红树林作为一种特殊的植物群落具有丰富的真菌资源,红树林真菌是具有特殊结构的生物活性物质的重要来源,相关研究近来倍受关注。本文列举出近年来产生次级代谢产物的具有活性的红树林真菌,分析后发现,具有活性的红树林真菌主要以子囊菌和半知菌为优势菌,这与绝大多数具有活性的海洋真菌主要以子囊菌亚门和半知菌亚门为多数的分布情况是一致的。     

缩合单宁功能性研究探讨

缩合单宁作为一种植物次生代谢物，其含量的多少直接影响到牧草的营养品质和动物的适口性。本文从缩合单宁的结构入手，着重综述了缩合单宁的功能，探讨了其在生产应用中对动植物的影响，以期为牧草选育和畜牧业生产提供一些有益的参考。     

Comparative Study of the Pharmacological Properties of Luteolin and Its 7,3′-Disulfate

The global spread of the metabolic syndrome, oncological and viral diseases forces researchers to pay increased attention to the secondary metabolites of marine hydrobionts, which often have a high therapeutic potential in the treatment of these pathologies and are effective components of functional food. The flavone luteolin (LT), as one of the most widely distributed and studied plant metabolites, is distinguished by a diverse spectrum of biological activity and a pleiotropic nature of the mechanism of action at the molecular, cellular and organismal levels. However, there is still practically no information on the spectrum of biological activity of its sulfated derivatives, which are widely represented in seagrasses of the genus Zostera. In the present work, a comparative study of the pharmacological properties of LT and its 7,3′-disulfate was carried out with a brief analysis of the special role of sulfation in the pharmacological activity of flavonoids.     

A Comprehensive Update on the Bioactive Compounds from Seagrasses

Marine angiosperms produce a wide variety of secondary metabolites with unique structural features that have the potential to be developed as effective and potent drugs for various diseases. Recently, research trends in secondary metabolites have led to drug discovery with an emphasis on their pharmacological activity. Among marine angiosperms, seagrasses have been utilized for a variety of remedial purposes, such as treating fevers, mental disorders, wounds, skin diseases, muscle pain, and stomach problems. Hence, it is essential to study their bioactive metabolites, medical properties, and underlying mechanisms when considering their pharmacological activity. However, there is a scarcity of studies on the compilation of existing work on their pharmacological uses, pharmacological pathways, and bioactive compounds. This review aims to compile the pharmacological activities of numerous seagrass species, their secondary metabolites, pharmacological properties, and mechanism of action. In conclusion, this review highlights the potency of seagrasses as a promising source of natural therapeutical products for preventing or inhibiting human diseases.     

Chemical Diversity and Biological Properties of Secondary Metabolites from Sea Hares of Aplysia Genus

The marine environment is an important source of structurally-diverse and biologically-active secondary metabolites. During the last two decades, thousands of compounds were discovered in marine organisms, several of them having inspired the development of new classes of therapeutic agents. Marine mollusks constitute a successful phyla in the discovery of new marine natural products (MNPs). Over a 50-year period from 1963, 116 genera of mollusks contributed innumerous compounds, Aplysia being the most studied genus by MNP chemists. This genus includes 36 valid species and should be distinguished from all mollusks as it yielded numerous new natural products. Aplysia sea hares are herbivorous mollusks, which have been proven to be a rich source of secondary metabolites, mostly of dietary origin. The majority of secondary metabolites isolated from sea hares of the genus Aplysia are halogenated terpenes; however, these animals are also a source of compounds from other chemical classes, such as macrolides, sterols and alkaloids, often exhibiting cytotoxic, antibacterial, antifungal, antiviral and/or antifeedant activities. This review focuses on the diverse structural classes of secondary metabolites found in Aplysia spp., including several compounds with pronounced biological properties.     

Cyanobacterial Metabolite Calothrixins: Recent Advances in Synthesis and Biological Evaluation

The marine environment is host to unparalleled biological and chemical diversity, making it an attractive resource for the discovery of new therapeutics for a plethora of diseases. Compounds that are extracted from cyanobacteria are of special interest due to their unique structural scaffolds and capacity to produce potent pharmaceutical and biotechnological traits. Calothrixins A and B are two cyanobacterial metabolites with a structural assembly of quinoline, quinone, and indole pharmacophores. This review surveys recent advances in the synthesis and evaluation of the biological activities of calothrixins. Due to the low isolation yields from the marine source and the promise this scaffold holds for anticancer and antimicrobial drugs, organic and medicinal chemists around the world have embarked on developing efficient synthetic routes to produce calothrixins. Since the first review appeared in 2009, 11 novel syntheses of calothrixins have been published in the efforts to develop methods that contain fewer steps and higher-yielding reactions. Calothrixins have shown their potential as topoisomerase I poisons for their cytotoxicity in cancer. They have also been observed to target various aspects of RNA synthesis in bacteria. Further investigation into the exact mechanism for their bioactivity is still required for many of its analogs.     

Natural Products from Marine Fungi—Still an Underrepresented Resource

Marine fungi represent a huge potential for new natural products and an increased number of new metabolites have become known over the past years, while much of the hidden potential still needs to be uncovered. Representative examples of biodiversity studies of marine fungi and of natural products from a diverse selection of marine fungi from the author’s lab are highlighting important aspects of this research. If one considers the huge phylogenetic diversity of marine fungi and their almost ubiquitous distribution, and realizes that most of the published work on secondary metabolites of marine fungi has focused on just a few genera, strictly speaking Penicillium, Aspergillus and maybe also Fusarium and Cladosporium, the diversity of marine fungi is not adequately represented in investigations on their secondary metabolites and the less studied species deserve special attention. In addition to results on recently discovered new secondary metabolites of Penicillium species, the diversity of fungi in selected marine habitats is highlighted and examples of groups of secondary metabolites produced by representatives of a variety of different genera and their bioactivities are presented. Special focus is given to the production of groups of derivatives of metabolites by the fungi and to significant differences in biological activities due to small structural changes.     

珠海市凤凰山药用植物资源多样性研究

根据第4次全国中药资源普查的技术规范与要求,采用样地与样线调查法,对珠海市凤凰山野生药用植物资源的科属组成、区系特征、生活型、药用部位、药性、药味、药效等方面进行研究.结果显示:该地区野生药用维管植物共有106科276属385种;药用植物属的分布区类型以热带性质为主;根及根茎类药物是该地药用植物的主要组成部分,占总种数...     

The search for new natural herbicides – Strategic approaches for discovering fungal phytotoxins

Plant pathogens produce toxic metabolites which may play a role in affecting their plant hosts by the development of diseases. Such compounds present considerable potential as models for developing herbicides with new modes of action unrelated to those in current use. This study provides an overview on the chemical ecology of plant-pathogenic fungi interactions as a promising approach for discovering new molecules possessing herbicide activity, along with the main research strategies currently employed for the isolation and identification of such compounds. The steps involved in: a) isolating fungal phytotoxic metabolites; b) the factors affecting in vitro biosynthesis of phytotoxins, extraction and fractionation methods; c) the bioassay-guided fractionation procedure, and d) the bioassays most commonly used for monitoring isolation processes, are discussed.