Bioactive Compounds and Adipocyte Browning Phenomenon

Overweight and obesity have become worldwide health issues in most countries. Current strategies aimed to prevent or reduce overweight and obesity have mainly focused on the genes and molecular mechanisms that give the functional characteristics to different types of adipose tissue. The Browning phenomenon in adipocytes consists of phenotypic and metabolic changes within white adipose tissue (WAT) activated by thermogenic mechanisms similar to that occurring in brown adipose tissue (BAT); this phenomenon has assumed great relevance due to its therapeutic potential against overweight and obesity. In addition, the study of inflammation in the development of overweight and obesity has also been included as a relevant factor, such as the pro-inflammatory mechanisms promoted by M1-type macrophages in adipose tissue. Studies carried out in this area are mainly performed by using the 3T3-L1 pre-adipocyte cell line, testing different bioactive compound sources such as plants and foods; nevertheless, it is necessary to standardize protocols used in vitro as well to properly scale them to animal models and clinical tests in order to have a better understanding of the mechanisms involved in overweight and obesity.     

Bioactive Compounds from Cyanobacteria and Microalgae: An Overview

ABSTRACT

Cyanobacteria (blue-green algae) are photosynthetic prokaryotes used as food by humans. They have also been recognized as an excellent source of vitamins and proteins and as such are found in health food stores throughout the world. They are also reported to be a source of fine chemicals, renewable fuel and bioactive compounds. This potential is being realized as data from research in the areas of the physiology and chemistry of these organisms are gathered and the knowledge of cyanobacterial genetics and genetic engineering increased. Their role as antiviral, anti-tumour, antibacterial, anti-HIV and a food additive have been well established. The production of cyanobacteria in artificial and natural environments has been fully exploited. In this review the use of cyanobacteria and microalgae, production processes and biosynthesis of pigments, colorants and certain bioactive compounds are discussed in detail. The genetic manipulation of cyanobacteria and microalgae to improve their quality are also described at length.     

Volatile Nitrogenous Compounds from Bacteria: Source of Novel Bioactive Compounds

Bacteria can produce nitrogenous compounds via both primary and secondary metabolic processes. Many bacterial volatile nitrogenous compounds produced during the secondary metabolism have been identified and reported for their antioxidant, antibacterial, antifungal, algicidal and antitumor activities. The production of these nitrogenous compounds depends on several factors, including the composition of culture media, growth conditions, and even the organic solvent used for their extraction, thus requiring their identification in specific conditions. In this review, we describe the volatile nitrogenous compounds produced by bacteria especially focusing on their antimicrobial activity. We concentrate on azo-compounds mainly pyrazines and pyrrolo-pyridines reported for their activity against several microorganisms. Whenever significant, extraction and identification methods of these compounds are also mentioned and discussed. To the best of our knowledge, this is first review describing volatile nitrogenous compounds from bacteria focusing on their biological activity.     

Comparison of Groupings among Members of the Genus Aspergillus Based on Phylogeny and Production of Bioactive Compounds

Three hundred sixty-six Aspergillus strains preserved at the National Institute of Technology and Evaluation (NITE) were compared as to phylogenetic relationships (11 species-clusters) based on the DNA sequences of the D1/D2 domains of LSU rRNA and ITS regions, including the 5.8S rRNA and biological activities of their secondary metabolites. The results showed relatively well correlation between the phylogenetic distribution and the production of bioactive compounds, especially, antimicrobial activities.     

三类重要真菌生物活性物质及其研究方法概述

对高等真菌、内生真菌和海洋真菌活性物质的研究现状进行了概述,并对活性物质的筛选和分离方法等进行了介绍。     

海绵生物活性物质及海绵细胞离体培养

介绍了来自海绵的生物活性物质种类、分布及其潜在的应用价值。讨论了其作为抗癌、抗病毒、抗细菌等药用的生物活性物质及其相关的海绵种属 ;强调海绵生物活性物质的商业化和临床应用所面临的“供给短缺问题”。作为解决这一问题的途径之一 ,海绵细胞离体培养是最有前景的技术。讨论了海绵细胞离体培养技术的研究现状 ,存在的问题及未来的发展趋势。对我国海域的海绵生物活性物质的研究开发现状进行总结 ,强调海绵研究对开发具有我国自主知识产权的新药、新化合物的必要性及重要性 ,并提出进行研发的可能优先领域     

Bioactive compounds from Caulerpa racemosa as a potent larvicidal and antibacterial agent

Marine algae are rich sources ofbioactive compounds capable of harboring secondary metabolites which are structurally and biologically active. In our study, the methanolic extract of marine algae Caulerpa racemosa （green algae） was employed to determine the antibacterial and larvicidal activity. The antibacterial activity showed effective inhibition against five pathogenic bacteria. A significant zone size of 16 mm was observed for Pseudomonas aeruginosa. The methanolic extract of Caulerpa racemosa showed effective larvicidal activity against Culex tritaeniorhynchus and the histopathological studies revealed the rupture in mid gut of larvae. The bioactive compounds in the crude extract were further identified as 2-（-3-bromo-1-adamantyl） acetic acid methyl ester and Chola-5, 22- dien-3-ol by GC-MS. Hence the bioactive compounds obtained from the methanolic extracts could be used for the bactericidal and larvicidal activity which will overcome the harmful impact of synthetic insecticide on environment.     

Phenolic Compounds and Allelopathic Potential of Fermented and Unfermented Wheat and Corn Straw Extracts

Total phenolic (TPC) and flavonoid (TFC) content, individual phenolic compounds and antioxidant activities of methanol extracts of wheat and corn straw were determined. Germination bioassay was conducted with Abutilon theophrasti Medik. , Asclepias syriaca L., and Chenopodium album L. seed. Samples were fermented by Lactobacillus plantarum and changes in TPC, TFC, antioxidant, and biological activity were investigated. TPC and TFC were significant in both samples and after fermentation their recovery was improved. All samples contain mainly quercetin, cinnamic acid, p‐coumaric acid, and ferulic acid. Fermentation changed the content of phenolic and flavonoid compounds, differently in each case. All tested extracts showed high DPPH activity with IC₅₀ being significantly lower for fermented samples. FRAP activity was also high. Crude straw extracts were overall more effective than fermented ones concerning inhibition of germination and seedlings growth, mainly without statistically significant differences between wheat and corn. Compared with mesotrione, extracts were more effective in germination and seedling growth inhibition of C. album and in seedling growth inhibition of A. theophrasti.     

Anti‐Adhesion Activity of Tannins Isolated from the Mangrove Laguncularia racemosa

In the search of new compounds with biofilm‐inhibiting properties, mangroves with their richness of secondary metabolites can be a valuable resource. Crude methanolic leaf extracts from the mangrove Laguncularia racemosa enriched in phenolic substances cause a reduction in initial cell adhesion of Candida glabrata and Candida albicans, but not on Escherichia coli. LC/MS‐guided fractionation of the phenolic compounds resulted in 19 fractions, of which ten were analyzed for their bioactivity against cell adhesion. Effects on cell adhesion and planktonic growth of Escherichia coli, Candida glabrata and Candida albicans were measured in 96‐well microtiter plates in the presence of 0.2 mg ml^?1 of the isolated fractions. Two fractions caused a reduction of cell adhesion of Candida albicans. These fractions containing bioactive compounds were analyzed by LC/MS and NMR spectroscopy. Casuarinin and digalloyl‐hexahydroxydiphenoyl‐glucose were identified in the active fractions, in addition to three signals of ellagitannins. These results indicate a specific mode of action of hydrolysable tannins against cell adhesion of Candida albicans, which needs to be further analyzed.     

Suppression of Pythium ultimum by Biowaste Composts in Relation to Compost Microbial Biomass, Activity and Content of Phenolic Compounds

Seventeen composts from separately collected organic household waste plus one bark compost and one compost from grape marc were analysed for suppression of Pythium ultimum, phytotoxicity, microbial biomass and activity, substrate-induced respiration, extractible phenolic compounds and other physical and chemical parameters. Nine of the samples were mildly suppressive to P. ultimum, the others were conducive. The bark compost sample was strongly suppressive. Therefore of the examined composts, only the bark could be used to exert an economically relevant control of P. ultimum in horticultural media. A large part of the compost samples was slightly phytotoxic. Microbial biomass and SIR had only weak correlations with disease incidence. Microbial activity and content of extractible phenolics were positively correlated with disease incidence. None of the tested parameters were therefore suitable as a predictive test for suppression of P. ultimum with the compost samples used in this study.     

Initiation of an Aquaculture of Sponges for the Sustainable Production of Bioactive Metabolites in Open Systems: Example, Geodia cydonium

Among Metazoa, sponges (phylum Porifera) are the richest source for different bioactive compounds. The availability of the raw material is, however, restricted. To obtain enough of the bioactive compounds for application in human therapy, sponges have to be cultured in in vitro systems. One technique for the establishment of a long-term cell culture from sponges has recently been elaborated. Here, we present a procedure to cultivate tissue samples from sponges in an open system. The species Geodia cydonium, which produces bioactive compounds, has been selected. Tissue samples of approximately 10 g were attached to the bottoms of cultivation trays. After 2 to 3 days, the tissue samples formed a robust contact with the metal support. Subsequently, sets of trays, called tray batteries, either remained in huge aquaria at the Center for Marine Research or were transferred to the vicinity of a fish and mussel farm. The growth rates of the samples remained unchanged within the first month; however, after 3 and 6 months, they increased to 147% and 189%, respectively. In parallel, extracts were prepared from the tissue samples and tested for cytotoxicity in a mouse lymphoma cell assay system. Extracts from cultured tissue initially had a low inhibitory potency; however, after cultivation for 3 or 6 months, values comparable to those of extracts from sponges taken from the biotope were found. In addition, a molecular marker was applied to document the response (health state) of the tissue and the identity of the material in culture. The CD63 molecule was chosen because the expression of this molecule in mammalian systems changes with the age of the animals. The corresponding complementary DNA was isolated from Geodia cydonium. With this probe, the level of expression in cultured tissue samples decreased immediately after starting cultivation; after a cultivation period of 6 months, however, values were similar to those found in controls. These data show that sponge species that produce bioactive compounds can be cultivated in open systems, in which they retain their potency to produce bioactive compounds as well as their health state. Received September 16, 1998; accepted June 18, 1999     

Oil Palm Biomass Biorefinery for Sustainable Production of Renewable Materials

Oil palm biomass is widely known for its potential as a renewable resource for various value‐added products due to its lignocellulosic content and availability. Oil palm biomass biorefinery is an industry that comes with sociopolitical benefits through job opportunities, as well as potential environmental benefits. Many studies have been conducted on the technological advancements of oil‐palm biomass‐derived renewable materials, which are discussed comprehensively in this review. Recent technological developments have made it possible to bring new and innovative technologies to commercialization, such as compost, biocharcoal, biocomposites, and bioplastics.     

Bioactive glasses as delivery systems for antimicrobial agents

Most biomaterial‐associated infections are caused by opportunistic pathogens and bacteria that are regularly found within the microflora of the implant site. In addition, a biomaterial implant or device remains at risk of infection by hematogenous spread of bacteria disseminated from infections elsewhere in the body or from infected peri‐implant tissue in revision surgery. The resulting infections are frequently accompanied by patient morbidity and discomfort and can lead to surgical replacement of the implant after lengthy, unsuccessful attempts to mitigate infections with antibiotic treatments. Therefore, extensive study is aiming to find new infection‐resistant antimicrobial biomaterials and coatings for implants and devices to effectively reduce the incidence of biomaterial‐associated infections. An overview of the in vitro and in vivo antimicrobial efficacies of the numerous biomaterials currently available is beyond the scope of this review. Herein, we provide a comprehensive review of bioactive glasses as biomaterial delivery systems for antimicrobial agents.     

New Insights into Bioactive Compounds of Traditional Chinese Medicines for Insulin Resistance Based on Signaling Pathways

Type 2 diabetes is a serious metabolic disease as a long‐term threat to human health. Insulin resistance is not only the basis and major feature of type 2 diabetes, but also the main etiology of diseases such as hypertension, hyperlipidemia and coronary heart disease. It has been shown that Traditional Chinese Medicines (TCMs) play an important role in the treatment of type 2 diabetes, through attenuating insulin resistance, whereas the mechanism involved is not yet well understood. Therefore, it is important to elucidate the pharmacological mechanism of these bioactive compounds so that one can pave the way for the modernization of TCMs. In this review, we focus on the recent progresses of some bioactive ingredients from TCMs with different functional groups, which exhibit therapeutic potential for the treatment of diabetic insulin resistance. It is expected that this review can provide new references for developing TCM‐derived drugs against diabetes and insulin resistance in the future.     

Sorghum: Nutritional Factors,Bioactive Compounds,Pharmaceutical and Application in Food Systems: A Review

After wheat, rice, maize, and barley, sorghum is the fifth most widely grown cereal on the planet. Due to its highproduction, drought resistance, and heat tolerance, this crop is replacing maize in some areas. Sorghum is available in a variety of colors, including cream, lemon-yellow, red, and even black. The principal grain anatomicalcomponents are pericarp, germ or embryo and endosperm. This review provides an overview of key sorghumgrain components, including starches, fiber, proteins, lipids, and vitamins. Also, we summarized phenolic compounds, flavonoids, tannins, carotenoids, vitamin E, amines, Policosanols and Phytosterols in sorghum grains.Sorghum is used to manufacture bread and porridge, and it provides a significant source of energy and nutritionfor humans; sorghum is extensively farmed for animal feed. However, because the natural components in sorghum are useful in the development of healthy and functional foods, sorghum farming for both biofuel production and human consumption is gaining popularity. Pigmented sorghum grain is high in antioxidants such aspolyphenols, primarily tannins, which have a variety of health benefits, including antiproliferative propertieslinked to the prevention of certain cancers, antioxidant activities linked to the prevention of diseases linked tooxidative stress, and anti-inflammatory effects, as well as improving glucose metabolism. Because these chemicalscannot be assimilated, their application in the food business has been limited, as sorghum is regarded as a lownutritional grain due to the presence of anti-nutritional components such as strong tannins, which form complexes with proteins and iron, limiting their digestibility. This review aims to show the utilization of sorghumas a source of bioactive chemicals and the value they bestow on human health due to the general biological potential it possesses.     

Balkans’ Asteraceae Species as a Source of Biologically Active Compounds for the Pharmaceutical and Food Industry

Herbal drugs are a useful source of different bioactive compounds. Asteraceae species, as the most widespread vascular plants, can be used both as food and as medicine due to the great diversity of recorded chemical components – different phenolic compounds, terpenes, carotenoids, vitamins, alkaloids, etc. The Balkan Peninsula is characterized by great diversity of plants from Asteraceae family, including presence of rare and endemic species. In this review, results of the survey of chemical composition and biological activity, mainly focusing on antioxidant, antimicrobial and anticancer effects of selected Balkans’ Asteraceae species were provided. In addition, information on edible plants from Asteraceae family is presented, due to growing interest for the so‐called ‘healthy diet’ and possible application of Balkans’ Asteraceae species as food of high nutritional value or as a source of functional food ingredients.     

Identification of Bioactive Compounds against Aedes aegypti (Diptera: Culicidae) by Bioassays and in Silico Assays

Most of the hematophagous insects act as disease vectors, including Aedes aegypti, responsible for transmitting some of the most critical arboviruses globally, such as Dengue. The use of repellents based on natural products is a promising alternative for personal protection compared to industrial chemical repellents. In this study, the repellent effect of essential oils extracted from Lippia thymoides, Lippia alba, Cymbopogon winterianus, and Eucalyptus globulus leaves was evaluated. Essential oils used showed repellent activity against Ae. aegypti in laboratory bioassays, obtaining protection rates above 70 % from 3.75 mg/mL and higher concentration for all analyzed oils. GC/MS identified 57 constituents, which were used in the ligand-based pharmacophore model to expose compounds with requirements for repellents that modulate mosquitoes behavior through odorant-binding protein 1 Ae. aegypti. Ligand-based pharmacophore model approach results suggested that repellent activity from C. winterianus, L. alba, and L. thymoides essential oils’ metabolites is related to Citronelal (QFIT=26.77), Citronelol (QFIT=11.29), Citronelol acetate (QFIT=52.22) and Geranil acetate (QFIT=10.28) with synergistic or individual activity. E. globulus essential oil's repellent activity is associated with Ledol (0.94 %; QFIT=41.95). Molecular docking was applied to understand the binding mode and affinity of the essential oils’ data set at the protein binding site. According to molecular docking, Citronelol (ChemPLP=60.98) and geranyl acetate (ChemPLP=60.55) were the best-classified compounds compared to the others and they can be explored to develop new repellents.     

Bioactive food components and cancer risk reduction

Research over the last three decades has provided convincing evidence to support the premise that diets rich in fruits and vegetables may be protective against the risk of different types of cancers. Initial evidence for protective effect of fruits and vegetables against cancer risk came from population-based case-control studies, which prompted intense research aimed at (a) identification of bioactive component(s) responsible for the anticancer effects of fruits and vegetables, (b) elucidation of the mechanisms by which bioactive food components may prevent cancer, and (c) determination of their efficacy for prevention of cancer in animal models. The bioactive components responsible for cancer chemopreventive effects of various edible plants have now been identified. For instance, anticancer effect of Allium vegetables including garlic is attributed to organosulfur compounds (e.g., diallyl trisulfide). Interestingly, unlike cancer chemotherapy drugs, many bioactive food components selectively target cancer cells. Molecular basis for selectivity of anticancer bioactive food components towards cancer cells remains elusive, but these agents appear promiscuous and target multiple signal transduction pathways to inhibit cancer cell growth in vitro and in vivo. Despite convincing observational and experimental evidence, however, limited effort has been directed towards clinical investigations to determine efficacy of bioactive food components for prevention of human cancers. This article reviews current knowledge on cancer chemopreventive effects of a few highly promising dietary constituents, including garlic-derived organosulfides, berry compounds, and cruciferous vegetable-derived isothiocyanates, and serves to illustrate complexity of the signal transduction mechanisms in cancer chemoprevention by these promising bioactive food components.     

生物磁效应对蛹虫草活性物质含量的影响

利用场强为0.1、0.25、0.4T恒定磁场,以流速为1 m·s^-1,分别对普通水进行9次处理,串联（SC）磁场处理3次的磁处理水,进而用于栽培蛹虫草,并研究了生物磁效应对蛹虫草虫草素、虫草酸、多糖含量及生物学转化效率的影响。结果表明,0.4T处理有利于蛹虫草虫草酸含量及生物学效率的提高,相比对照组分别提高了7.29%和15.37%;0.25T处理组有利于虫草素的积累,比对照组提高了11.31%;0.1T处理有利于多糖的积累,相比对照组提高了14.80%。方差分析表明,经不同场强处理的磁化水对蛹虫草子实体生长和活性物的代谢影响差异显著。但磁处理水对于不同物质含量的影响规律存在一定的差异性。