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Bioactive compound

Lingjun Zhang, Yuriy Fedorov, Drew Adams, Feng Lin
Excessive complement activation contributes significantly to the pathogeneses of various diseases. Currently, significant developmental research efforts aim to identify complement inhibitors with therapeutic uses have led to the approval of one inhibitor for clinical use. However, most existing complement inhibitors are based on monoclonal antibodies, which have many drawbacks such as high costs and limited administration options. With this report, we establish an inexpensive, cell imaging-based high-throughput assay for the large-scale screening of potential small molecule complement inhibitors...
June 14, 2018: Molecular Immunology
Hend M Dawood, Reham S Ibrahim, Eman Shawky, Hala M A Hammoda, Aly M Metwally
ETHNOPHARMACOLOGICAL RELEVANCE: Aromatase enzyme (CYP19) is widely known as a critical target protein for treating hormone-dependent breast cancer. Natural products from traditional medicinal plants continue to be an active source of aromatase inhibitors. Meanwhile, high cost of experimental work and low hit rate associated with HTS have stimulated the implementation of in-silico virtual screening to resolve these pitfalls, where coupling of both classical wet lab procedure and VS may offer a more deepened access to bioactive compounds with less work and time waste...
June 14, 2018: Journal of Ethnopharmacology
Bruna Yhang Da Costa Silva, Helena Alves De Carvalho Sampaio, Nitin Shivappa, James Hébert, Larissa Da Silva Albuquerque, Antônio Augusto Ferreira Carioca, José Artur Costa D'Almeida, Carla Soraya Costa Maia, Maria Luisa Pereira De Melo
BACKGROUND & AIMS: The Dietary Inflammatory Index (DII) consists of a tool that assesses dietary inflammatory potential based on the assignment of an inflammatory score to a variety of nutrients, seasonings and bioactive compounds. Pro-inflammatory diets are associated to weight and abdominal fat excess. High Body Mass Index (BMI) and Waist Circumference (WC) seem to contribute to a worse prognosis in Multiple Sclerosis (MS) patients. Therefore, this study seeks to investigate the relation between anthropometric indexes and body adiposity with the clinical condition and the Dietary Inflammatory Index of MS individuals...
August 2018: Clinical Nutrition ESPEN
Krzysztof Kamil Wojtanowski, Tomasz Mroczek
The high performance liquid chromatography (HPLC) coupled to electrospray ionization (ESI) octopole orthogonal acceleration time-of-flight (TOF) mass spectrometry (MS) was developed to separate secondary metabolites belonging to different groups of compounds with a wide range of polarity, i.e. phenolic acids, flavonoids, sesquiterpenes and others present in minute amounts, in a single run. Moreover, application of ESI-TOF-MS with a simple in source type of fragmentation and high mass accuracy measurements (around 2 ppm) in both positive and negative ionization modes with different and optimized fragmentor voltages, enabled the identification of each single compound based on proposed fragmentation patterns...
October 31, 2018: Analytica Chimica Acta
Cesar H E C Poli, Kara J Thornton-Kurth, Jerrad F Legako, Carolina Bremm, Viviane S Hampel, Jeffery Hall, Ignacio R Ipharraguerre, Juan J Villalba
Plant bioactives can potentially benefit herbivores through their effects on health and nutrition. The objective of this study was to determine the importance of polyphenols and terpenes on the ability of lambs to self-select these compounds when challenged by a parasitic infection and the subsequent impact on their health and productivity. Thirty-five lambs were housed in individual pens and assigned to five treatment groups (7 animals/group), where they received: 1) A basal diet of beet pulp:soybean meal (90:10) (CONTROL); 2) The same diet, but containing 0...
June 12, 2018: Physiology & Behavior
Lissa Davis, Jooyeoun Jung, Ann Colonna, Aimee Hasenbeck, Virginia Gouw, Yanyun Zhao
Blueberry pomace (BP) and cranberry pomace (CP) are good sources of dietary fiber and phenolics. This study aimed to develop berry fruit pomace (FP)-fortified specialty mustard with elevated bioactive compounds and ascertain consumer acceptance of a new product. Wet BP and CP were ground and incorporated into Dijon-style mustard at concentrations of 15%, 20%, and 25% (w/w). Total dietary fiber (TDF), total phenolic content (TPC), and radical scavenging activity (RSA) were evaluated for samples obtained from both chemical extraction (CE) and simulated gastrointestinal digestion (SGD)...
June 15, 2018: Journal of Food Science
Malatee Tayeh, Sirinun Nilwarangkoon, Chantra Tanunyutthawongse, Wilawan Mahabusarakum, Ramida Watanapokasin
Rhodomyrtone is a bioactive compound extracted from Rhodomyrtus tomentosa leaves. It has been used as a traditional herb medicine for many years. Rhodomyrtone exhibits antibacterial activity, anti-inflammatory and antioxidant activities. However, the anticancer activity of rhodomyrtone has not been previously reported. The present study investigated the anticancer effect of rhomyrtone on human epidermoid carcinoma A431 cells. The cytotoxic and antiproliferative effects of rhodomyrtone on A431 cells were investigated by an MTT assay...
June 2018: Experimental and Therapeutic Medicine
Daiki Nomura, Masaaki Saito, Yosuke Takahashi, Yuki Takahashi, Yoshinobu Takakura, Makiya Nishikawa
Self-gelling DNA hydrogels with cytosine-phosphate-guanine (CpG) motifs have been shown to exhibit high potency as vaccine adjuvants. However, their oral use is limited because of their thermodynamic and chemical instability in the gastrointestinal tract. In this study, we aimed to develop DNA hydrogel microspheres (Dgel-MS) coated with chitosan to improve their stability. Chitosan-coated Dgel-MS (Cs-Dgel-MS) was prepared by emulsifying Dgel to obtain the D-gel core, followed by mixing with microemulsions of chitosan for electrostatic coating...
June 11, 2018: International Journal of Pharmaceutics
Yang Fei Tan, Luciana Lisa Lao, Gordon Minru Xiong, Subbu Venkatraman
This is a review of nanotherapeutic systems, specifically those that exhibit controlled release of the encapsulated bioactive compound. The survey includes the delivery of a range of bioactive compounds, from lipophilic small molecules to hydrophilic proteins and siRNA molecules. The research into enabling sustained delivery of these compounds from nanocarriers has been prolific, but clinical success has been harder to achieve. This is partly because achieving true sustained duration of action over several days is difficult when the carrier dimensions become less than about 400 nm, due to the much shorter diffusion path length compared to micron-sized carrier systems...
June 11, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Diana B Muñiz-Márquez, Jorge E Wong-Paz, Juan C Contreras-Esquivel, Raúl Rodríguez-Herrera, Cristóbal N Aguilar
Laurus nobilis leaves contain flavored and bioactive components with relevant biological properties for human health that are attributed to an abundant presence of highly bioactive secondary metabolites. However, the separation process for these bioactive molecules from plant matrix is seriously limited by the presence of a physical barrier (cell wall). Thus, the use of novel extraction procedures to enhance their release is particularly important. In this work, the potential use of microwave-assisted extraction (MAE) as a tool to improve the extraction efficiency of bioactive compounds from bay leaves and their characterization was evaluated...
June 14, 2018: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
Claudia Albrecht, María Laura Guzmán, María Cecilia Cittadini, Alejandra Mariel Canalis, Mirta Ana Valentich, María Eugenia Olivera, Elio Andrés Soria
BACKGROUND: Plant extracts can be obtained to carry bioactive compounds, useful for prevention and treatment of different illnesses. This also supports the intake of teas as functional beverages. Nonetheless, it is incompletely known whether these extracts can act as effective sources and vehicles de phenolic compounds (phenolics/polyphenols) to reach their targets. OBJECTIVE: To establish whether phytoextract ingestion modified in a sex-dependent manner the phenolic bioavailability and redox response in liver and kidney...
March 26, 2018: Revista de la Facultad de Ciencias Médicas
Zora Váradyová, Dominika Mravčáková, Monika Holodová, Ľubomira Grešáková, Jana Pisarčíková, Marcin Barszcz, Marcin Taciak, Anna Tuśnio, Svetlana Kišidayová, Klaudia Čobanová
Two experiments were conducted on sheep to determine the effect of dietary supplementation with zinc and a medicinal plant mixture on haematological parameters and microbial activity in the rumen and large intestine. In Experiment 1, 24 male lambs were randomly divided into four groups: One group was fed an unsupplemented basal diet (control), and three groups were fed a diet supplemented with 70 mg Zn/kg diet in the form of Zn sulphate (ZnSO4 ), a Zn-chelate of glycine hydrate (Zn-Gly) or a Zn-proteinate (Zn-Pro), for five months...
June 14, 2018: Journal of Animal Physiology and Animal Nutrition
Ralf Lopes, Sarina Tsui, Priscila J R O Gonçalves, Marisa Vieira de Queiroz
One of the major challenges of agriculture currently is to obtain higher crop yield. Environmental conditions, cultivar quality, and plant diseases greatly affect plant productivity. On the other hand, several endophytic Bacillus species have emerged as a complementary, efficient, and safe alternative to current crop management practices. The ability of Bacillus species to form spores, which resist adverse conditions, is an advantage of the genus for use in formulations. Endophytic Bacillus species provide plants with a wide range of benefits, including protection against phytopathogenic microorganisms, insects, and nematodes, eliciting resistance, and promoting plant growth, without causing damage to the environment...
June 13, 2018: World Journal of Microbiology & Biotechnology
Arunkumar Naik Bukke, Fathima Nazneen Hadi, K Suresh Babu, P Chandramati Shankar
This article contains data on in vitro cytotoxicity activity of chloroform, methanolic and water extracts of leaf and heartwood of Caesalpinia sappan L. a medicinal plant against Breast cancer (MCF-7) and Lung cancer (A-549) cells. This data shows that Brazilin A, a natural bioactive compound in heartwood of Caesalpinia sappan L. induced cell death in breast cancer (MCF-7) cells. The therapeutic property was further proved by docking the Brazilin A molecule against BCL-2 protein (an apoptotic inhibitor) using auto dock tools...
August 2018: Data in Brief
Ton That Huu Dat, Georg Steinert, Nguyen Thi Kim Cuc, Hauke Smidt, Detmer Sipkema
Sponge-associated prokaryotic diversity has been studied from a wide range of marine environments across the globe. However, for certain regions, e.g., Vietnam, Thailand, Cambodia, and Singapore, an overview of the sponge-associated prokaryotic communities is still pending. In this study we characterized the prokaryotic communities from 27 specimens, comprising 18 marine sponge species, sampled from the central coastal region of Vietnam. Illumina MiSeq sequencing of 16S ribosomal RNA (rRNA) gene fragments was used to investigate sponge-associated bacterial and archaeal diversity...
2018: PeerJ
Vitor Ramos, João Morais, Raquel Castelo-Branco, Ângela Pinheiro, Joana Martins, Ana Regueiras, Ana L Pereira, Viviana R Lopes, Bárbara Frazão, Dina Gomes, Cristiana Moreira, Maria Sofia Costa, Sébastien Brûle, Silvia Faustino, Rosário Martins, Martin Saker, Joana Osswald, Pedro N Leão, Vitor M Vasconcelos
Cyanobacteria are a well-known source of bioproducts which renders culturable strains a valuable resource for biotechnology purposes. We describe here the establishment of a cyanobacterial culture collection (CC) and present the first version of the strain catalog and its online database ( The LEGE CC holds 386 strains, mainly collected in coastal (48%), estuarine (11%), and fresh (34%) water bodies, for the most part from Portugal (84%). By following the most recent taxonomic classification, LEGE CC strains were classified into at least 46 genera from six orders (41% belong to the Synechococcales), several of them are unique among the phylogenetic diversity of the cyanobacteria...
2018: Journal of Applied Phycology
Haiyang Yu, Shuangshuang Yin, Shiyue Zhou, Yingying Shao, Jiachen Sun, Xu Pang, Lifeng Han, Yi Zhang, Xiumei Gao, Chengyun Jin, Yuling Qiu, Tao Wang
Magnolin is a multi-bioactive natural compound that possesses underlying anti-cancer properties. However, the mechanisms underlying remain to be elucidated. Here, we report the role of magnolin in suppressing human colorectal cancer (CRC) cells via activating autophagy and cell cycle arrest in vitro and in vivo. Pre-treatment of cells with specific autophagy inhibitor (3-methyladenine) or knockdown of endogenous LC-3B by siRNA significantly abrogates magnolin-induced cell cycle arrest. Molecular validation mechanistically shows that magnolin-induced autophagy and cell cycle arrest in CRC cells is correlated with decreased transcriptional levels of leukemia inhibitory factor (LIF), and we further find that inhibition of LIF decreases phosphorylation level of Stat3 and represses transcriptional expression of Mcl-1...
June 13, 2018: Cell Death & Disease
Maria Irakli, Fotis Kleisiaris, Kalliopi Kadoglidou, Dimitrios Katsantonis
Rice by-products are extensively abundant agricultural wastes from the rice industry. This study was designed to optimize experimental conditions for maximum recovery of free and bound phenolic compounds from rice by-products. Optimized conditions were determined using response surface methodology based on total phenolic content (TPC), ABTS radical scavenging activity and ferric reducing power (FRAP). A Box-Behnken design was used to investigate the effects of ethanol concentration, extraction time and temperature, and NaOH concentration, hydrolysis time and temperature for free and bound fractions, respectively...
June 13, 2018: Foods (Basel, Switzerland)
Jean-Étienne R L Morlighem, Chen Huang, Qiwen Liao, Paula Braga Gomes, Carlos Daniel Pérez, Álvaro Rossan de Brandão Prieto-da-Silva, Simon Ming-Yuen Lee, Gandhi Rádis-Baptista
Marine invertebrates, such as sponges, tunicates and cnidarians (zoantharians and scleractinian corals), form functional assemblages, known as holobionts, with numerous microbes. This type of species-specific symbiotic association can be a repository of myriad valuable low molecular weight organic compounds, bioactive peptides and enzymes. The zoantharian Protopalythoa variabilis (Cnidaria: Anthozoa) is one such example of a marine holobiont that inhabits the coastal reefs of the tropical Atlantic coast and is an interesting source of secondary metabolites and biologically active polypeptides...
June 13, 2018: Marine Drugs
Roy A Meoded, Reiko Ueoka, Eric J N Helfrich, Katja Jensen, Nancy Magnus, Birgit Piechulla, Jörn Piel
Enzymatic core components from trans-acyltransferase polyketide synthases (trans-AT PKSs) catalyze exceptionally diverse biosynthetic transformations to generate structurally complex bioactive compounds. Here we focus on a group of oxygenases identified in various trans-AT PKS pathways, including those for pederin, oocydins, and toblerols. Using the oocydin pathway homolog (OocK) from Serratia plymuthica 4Rx13 and N-acetylcysteamine (SNAC) thioesters as test surrogates for acyl carrier protein-tethered intermediates, we show that the enzyme inserts oxygen into β-ketoacyl moieties to yield malonyl ester SNAC products...
June 13, 2018: Angewandte Chemie
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