keyword
MENU ▼
Read by QxMD icon Read
search

Bioactive compound

keyword
https://www.readbyqxmd.com/read/29457887/synthesis-of-highly-substituted-imidazole-uracil-containing-molecules-via-ugi-4cr-and-passerini-3cr
#1
Rudrakshula Madhavachary, Tryfon Zarganes-Tzitzikas, Pravin Patil, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Dömling
The synthesis of uracil/thymine containing tetra/tri-substituted imidazoles were demonstrated using Ugi/Passerini-reaction fol-lowed by a post-cyclization reaction sequence. The approach enables the one-pot facile construction of diverse compounds in moderate to excellent yields (47-82%). The 5-fluorouracil and 5-methyluracil moieties afford potentially bioactive molecules with drug-like properties. These scaffolds are being utilized in the screening deck of the European Lead Factory.
February 19, 2018: ACS Combinatorial Science
https://www.readbyqxmd.com/read/29457705/regulation-of-specialised-metabolites-in-actinobacteria-expanding-the-paradigms
#2
Paul A Hoskisson, Lorena T Fernández-Martínez
The increase in availability of actinobacterial whole genome sequences has revealed huge numbers of specialised metabolite biosynthetic gene clusters, encoding a range of bioactive molecules such as antibiotics, antifungals, immunosuppressives and anticancer agents. Yet the majority of these clusters are not expressed under standard laboratory conditions in rich media conditions. Emerging data from studies of specialised metabolite biosynthesis suggest that the diversity of regulatory mechanisms is greater than previously thought and these act at multiple levels, through a range of signals such as nutrient limitation, intercellular signalling and competition with other organisms...
February 19, 2018: Environmental Microbiology Reports
https://www.readbyqxmd.com/read/29457695/functionalization-of-a-nanostructured-hydroxyapatite-with-copper-ii-compounds-as-pesticide-in-situ-tem-and-esem-observations-of-treated-vitis-vinifera-l-leaves
#3
Enrico Battiston, Maria C Salvatici, Alessandro Lavacchi, Antonietta Gatti, Stefano Di Marco, Laura Mugnai
BACKGROUND: The present study evaluates a biocompatible material for plant protection to reduce the amount of active substance applied. We used a synthetic hydroxyapatite (HA) that has been studied extensively due its bioactivity and biocompatibility. Aggregation between HA nanoparticles and four copper(II) compounds applied in Vitis vinifera L. leaves as pesticide was studied. Formulations were characterised by XRD, DLS, electron microscopy and applied in planta to verify the particle aggregation and efficiency in controlling the pathogen, Plasmopara viticola...
February 19, 2018: Pest Management Science
https://www.readbyqxmd.com/read/29457449/catalytically-active-single-chain-polymeric-nanoparticles-exploring-their-functions-in-complex-biological-media
#4
Yiliu Liu, Silvia Pujals, Patrick J M Stals, Thomas Pauloehrl, Stanislav I Presolski, E W Meijer, Lorenzo Albertazzi, Anja R A Palmans
Dynamic single-chain polymeric nanoparticles (SCPNs) are intriguing, bioinspired architectures that result from the collapse or folding of an individual polymer chain into a nanometer-sized particle. Here we present a detailed biophysical study on the behavior of dynamic SCPNs in living cells and an evaluation of their catalytic functionality in such a complex medium. We first developed a number of delivery strategies that allowed the selective localization of SCPNs in different cellular compartments. Live/dead tests showed that the SCPNs were not toxic to cells while spectral imaging revealed that SCPNs provide a structural shielding and reduced the influence from the outer biological media...
February 19, 2018: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29457331/a-strain-of-streptomyces-sp-isolated-from-rhizospheric-soil-of-crataegus-oxycantha-producing-nalidixic-acid-a-synthetic-antibiotic
#5
Nidhi Arora, Sunil Kumar, N Satti, Asif Ali, Prasoon Gupta, Meenu Katoch
AIM: Exploration of microbes isolated from rhizospheric soil of Crataegus oxycantha for bioactive natural products. METHODS AND RESULTS: A strain of Streptomyces sp. (C-7) was isolated from rhizospheric soil of Crataegus oxycantha. The 16S rRNA gene sequence of strain C-7 displayed 99% sequence similarity with different Streptomyces species. The highest score was displayed for Streptomyces sp. strain Chy2-8 followed by Streptomyces violarus strain NBRC13104 and Streptomyces arenae strain ISP5293...
February 19, 2018: Journal of Applied Microbiology
https://www.readbyqxmd.com/read/29456275/antimicrobial-packaging-based-on-%C3%A9-polylysine-bioactive-film-for-the-control-of-mycotoxigenic-fungi-in-vitro-and-in-bread
#6
C Luz, J Calpe, F Saladino, Fernando B Luciano, M Fernandez-Franzón, J Mañes, G Meca
ɛ-Poly-l-lysine (ɛ-PL) is a cationic peptide with a broad-spectrum antimicrobial activity. This study investigates the use of ɛ-PL as natural antimicrobial to inhibit fungal growth and to reduce aflatoxins (AFs) production. Antifungal activity of starch biofilms with different concentrations of ɛ-Poly-l-lysine (ɛ-PL) was determined in solid medium against Aspergillus parasiticus (AFs producer) and Penicillium expansum . Then, biofilms were tested as antimicrobial devices for the preservation of bread loaf inoculated with A...
January 2018: Journal of Food Processing and Preservation
https://www.readbyqxmd.com/read/29456101/ligand-based-modeling-of-akt3-lead-to-potent-dual-akt1-akt3-inhibitor
#7
Mahmoud A Al-Sha'er, Mutasem O Taha
Akt1 and Akt3 are important serine/threonine-specific protein kinases involved in G2 phase required by cancer cells to maintain cell cycle and to prevent cell death. Accordingly, inhibitors of these kinases should have potent anti-cancer properties. This prompted us to use pharmacophore/QSAR modeling to identify optimal binding models and physicochemical descriptors that explain bioactivity variation within a set of 74 diverse Akt3 inhibitors. Two successful orthogonal pharmacophores were identified and further validated using receiver operating characteristic (ROC) curve analyses...
February 13, 2018: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/29455836/the-rigidins-isolation-bioactivity-and-total-synthesis-novel-pyrrolo-2-3-d-pyrimidine-analogues-using-multicomponent-reactions
#8
Aletta E van der Westhuyzen, Liliya V Frolova, Alexander Kornienko, Willem A L van Otterlo
Rigidins (2-6) are pyrrolopyrimidine alkaloids isolated from marine tunicates. Since their isolation, refinement of their total syntheses, and biochemical evaluation, interest toward this pyrrolo[2,3-d]pyrimidine scaffold as a medicinal candidate has been triggered. The derivatization of these natural products has led to the discovery of a novel range of 7-deazahypoxanthines, which exhibit extremely potent anticancer activity in human cancer cell lines. A major breakthrough toward the synthesis of rigidin and various rigidin analogues has been the application of multicomponent reactions (MCRs)...
2018: Alkaloids. Chemistry and Biology
https://www.readbyqxmd.com/read/29455357/phytochemical-constituents-antioxidant-activity-and-antiproliferative-properties-of-black-red-and-brown-rice-bran
#9
Ali Ghasemzadeh, Mohamad Taghi Karbalaii, Hawa Z E Jaafar, Asmah Rahmat
BACKGROUND: In the recent years, the health benefits of the pigmented rice varieties have reported due to the presence of bioactive compounds. In this study, the phytochemical constituents (total phenolic, flavonoid and anthocyanin content) and individual phenolics and flavonoids of the extracts of sixteen genotypes of pigmented rice bran were evaluated using spectrophotometric and ultra-high performance liquid chromatography method. Antioxidative properties of the free and bound fractions were evaluated using nitric oxide and 1,1-diphenyl-2-picrylhydrazyl scavenging assays...
February 17, 2018: Chemistry Central Journal
https://www.readbyqxmd.com/read/29455277/guava-psidium-guajava-l-cv-red-suprema-crude-extract-protect-human-dermal-fibroblasts-against-cytotoxic-damage-mediated-by-oxidative-stress
#10
José M Alvarez-Suarez, Francesca Giampieri, Massimiliano Gasparrini, Luca Mazzoni, Tamara Y Forbes-Hernández, Sadia Afrin, Maurizio Battino
We analyzed guava fruits (Psidium guajava L. cv. Red Suprema) from Cuba to determine their chemical composition, total antioxidant capacity, as well as their protective effect against oxidative damage using an in vitro model of human dermal fibroblasts. The guava fruit is a natural source of bioactive compounds, such as polyphenols, vitamin C, folates and beta carotenes with proven health benefits. Human dermal fibroblasts were pre-incubated with different concentrations of guava crude extract and then subjected to oxidative stress using the AAPH stressor...
February 17, 2018: Plant Foods for Human Nutrition
https://www.readbyqxmd.com/read/29455054/seco-labdane-diterpenoids-from-the-leaves-of-callicarpa-nudiflora-showing-nitric-oxide-inhibitory-activity
#11
Xiaocong Sun, Feng Liu, Xueyuan Yang, Jinghan Wang, Bangjian Dong, Chunfeng Xie, Da-Qing Jin, Jie Zhang, Dongho Lee, Yasushi Ohizumi, Jing Xu, Yuanqiang Guo
Nine previously undescribed seco-labdane diterpenoids, nudiflopenes A-I, were isolated from the leaves of Callicarpa nudiflora. Their structures were elucidated on the basis of extensive 1D and 2D NMR spectroscopic data analysis, and the absolute configurations of these compounds were established by the modified Mosher's method and experimental and calculated electronic circular dichroism spectra. Nudiflopenes A-I belong to the class of seco-labdane diterpenoids. All of the isolates showed inhibitory activities on lipopolysaccharide-induced nitric oxide (NO) production in murine microglial BV-2 cells...
February 15, 2018: Phytochemistry
https://www.readbyqxmd.com/read/29454985/a-non-toxic-microbial-surfactant-from-marinobacter-hydrocarbonoclasticus-sdk644-for-crude-oil-solubilization-enhancement
#12
Billal Zenati, Alif Chebbi, Abdelmalek Badis, Kamel Eddouaouda, Hocine Boutoumi, Mohamed El Hattab, Dorra Hentati, Manel Chelbi, Sami Sayadi, Mohamed Chamkha, Andrea Franzetti
This study aims to investigate the ability of a biosurfactant produced by Marinobacter hydrocarbonoclasticus strain SdK644 isolated from hydrocarbon contaminated sediment to enhance the solubilization rate of crude oil contaminated seawater. Phylogenetic analysis shows that strain SdK644 was very closely related to M. hydrocarbonoclasticus with 16S rRNA gene sequence similarity of 97.44%. Using waste frying oil as inducer carbon source, the producing biosurfactant by strain SdK644 was applied to improve crude oil solubilization in seawater...
February 15, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29454868/halophytic-herbs-of-the-mediterranean-basin-an-alternative-approach-to-health
#13
REVIEW
S A Petropoulos, A Karkanis, N Martins, I C F R Ferreira
Wild native species are usually grown under severe and stressful conditions, while a special category includes halophytic species that are tolerant to high salinity levels. Native halophytes are valuable sources of bioactive molecules whose content is higher in saline than normal conditions, since the adaptation to salinity mechanisms involve apart from changes in physiological functions the biosynthesis of protectant molecules. These compounds include secondary metabolites with several beneficial health effects which have been known since ancient times and used for medicinal purposes...
February 15, 2018: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/29454829/bioactive-triterpenoids-from-twigs-of-betula-schmidtii
#14
Kyoung Jin Park, Lalita Subedi, Sun Yeou Kim, Sang Un Choi, Kang Ro Lee
Investigation of the MeOH extract of Betula schmidtii twigs resulted in the isolation and identification of three new triterpenoids (1-3), along with ten known ones (4-13). The structures of new compounds (1-3) were elucidated by spectroscopic methods, including 1D, 2D NMR (1 H and13 C NMR, COSY, HSQC, HMBC, and NOESY), HR-MS, and chemical methods. All the isolated compounds were evaluated for their cytotoxicity against A549, SK-OV-3, SK-MEL-2, and HCT-15 cell lines. Compound 11 exhibited potent cytotoxic activities against four cell lines, and compounds 5 and 13 significantly induced nerve growth factor secretion in a C6 rat glioma cell line...
February 10, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29454560/bioactive-lipid-mediators-profiles-in-human-psoriasis-skin-and-blood
#15
Alexander V Sorokin, Anthony Domenichiello, Amit K Dey, Aditya Goyal, Shawn M Rose, Martin P Playford, Christopher E Ramsden, Nehal N Mehta
Psoriasis (PSO) is a chronic immune-mediated disease that represents a unique model for investigating inflammation at local and systemic levels. Bioactive lipid mediators (LM) are potent compounds reported to play a role in the development and resolution of inflammation. Currently, it is not known to what extent these LM are involved in PSO pathophysiology and related metabolic dysfunction. Here we use targeted and untargeted liquid chromatography-tandem mass spectrometry (LC-MS-MS) approaches to quantify LM in skin and peripheral blood from PSO and compared them to those of healthy subjects...
February 15, 2018: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/29454281/probing-the-%C3%AE-pocket-of-the-active-site-of-human-liver-glycogen-phosphorylase-with-3-c-%C3%AE-d-glucopyranosyl-5-4-substituted-phenyl-1-2-4-triazole-inhibitors
#16
Efthimios Kyriakis, Theodora G A Solovou, Sándor Kun, Katalin Czifrák, Béla Szőcs, László Juhász, Éva Bokor, George A Stravodimos, Anastassia L Kantsadi, Demetra S M Chatzileontiadou, Vassiliki T Skamnaki, László Somsák, Demetres D Leonidas
Human liver glycogen phosphorylase (hlGP), a key enzyme in glycogen metabolism, is a valid pharmaceutical target for the development of new anti-hyperglycaemic agents for type 2 diabetes. Inhibitor discovery studies have focused on the active site and in particular on glucopyranose based compounds with a β-1 substituent long enough to exploit interactions with a cavity adjacent to the active site, termed the β-pocket. Recently, C-β-d-glucopyranosyl imidazoles and 1, 2, 4-triazoles proved to be the best known glucose derived inhibitors of hlGP...
February 12, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29454280/8-chrysoeriol-as-a-potential-bcl-2-inhibitor-triggers-apoptosis-of-sw1990-pancreatic-cancer-cells
#17
Yiwen Zhang, Zhimei Li, Qiuxia Min, Abulizi Palida, Yiyuan Zhang, Ruotian Tang, Lixia Chen, Hua Li
8-Chrysoeriol, a bioactive flavanoid, was firstly identified to bind directly to BCL-2 as BH3 mimetics by structure-based virtual ligand screening. And 3D docking model revealed the molecular basis of 8-Chrysoeriol targeting to BCL-2. The interaction between 8-Chrysoeriol and BCL-2 was further confirmed using Microscale Thermophoresis (MST) technique. Meanwhile, high expression level of antiapoptotic protein BCL-2 was detected in SW1990 pancreatic cancer cells and 8-Chrysoeriol showed obvious proapoptosis effect against SW1990 in vitro...
February 2, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29454114/mitochondria-targeting-mitochondrial-reactive-oxygen-species-with-mitochondriotropic-polyphenolic-based-antioxidants
#18
José Teixeira, Cláudia M Deus, Fernanda Borges, Paulo J Oliveira
Mitochondrial function and regulation of redox balance is fundamental in controlling cellular life and death pathways. Antioxidants have been used to counteract disruption of redox networks, normally associated with progressive loss of cell homeostasis and disease pathophysiology, although therapeutic success is limited mainly due to pharmacokinetic drawbacks. Attempts to improve mitochondrial function in a range of diseases spurred active drug discovery efforts. Currently, the most effective strategy to deliver drugs to mitochondria is the covalent link of lipophilic cations to the bioactive compound...
February 14, 2018: International Journal of Biochemistry & Cell Biology
https://www.readbyqxmd.com/read/29454021/three-new-quinazolines-from-evodia-rutaecarpa-and-their-biological-activity
#19
Xiu-Li Su, Shu Xu, Yu Shan, Min Yin, Yu Chen, Xu Feng, Qi-Zhi Wang
In this research, we investigated the profile and bioactivities of quinazoline alkaloids, a class of natural products boasting multiple bioactivities, from the unripe fruit of Evodia rutaecarpa (Juss.) Benth. Three new quinazoline alkaloids, evodiamide A (1), evodiamide B (2), and evodiamide C (3), as well as eight known quinazolines, were isolated from the MeOH extract of E. rutaecarpa. The new compounds are rare quinazolinedione derivatives with linked heterocyclic nuclei. Among these quinazolines, rhetsinine (8) showed potential as a pesticide and exhibited excellent inhibition against Xanthomonas oryzae pv...
February 14, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29453649/reinereins-a-and-b-new-onocerane-triterpenoids-from-reinwardtiodendron-cinereum
#20
Alfarius Eko Nugroho, Daisuke Inoue, Chin Piow Wong, Yusuke Hirasawa, Toshio Kaneda, Osamu Shirota, A Hamid A Hadi, Hiroshi Morita
Bioactivity guided separation of Reinwardtiodendron cinereum barks methanol extract led to the isolation of two new onocerane triterpenoids, reinereins A and B (1 and 2), together with three known onocerane triterpenoids. Their structures were elucidated on the basis of NMR spectroscopic data. In vitro cytotoxic activities of the isolated compounds against several type of cancer cells were evaluated.
February 16, 2018: Journal of Natural Medicines
keyword
keyword
99418
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"