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https://www.readbyqxmd.com/read/28641017/nanpdb-a-resource-for-natural-products-from-northern-african-sources
#1
Fidele Ntie-Kang, Kiran K Telukunta, Kersten Döring, Conrad V Simoben, Aurélien F A Moumbock, Yvette I Malange, Leonel E Njume, Joseph N Yong, Wolfgang Sippl, Stefan Günther
Natural products (NPs) are often regarded as sources of drugs or drug leads or simply as a "source of inspiration" for the discovery of novel drugs. We have built the Northern African Natural Products Database (NANPDB) by collecting information on ∼4500 NPs, covering literature data for the period from 1962 to 2016. The data cover compounds isolated mainly from plants, with contributions from some endophyte, animal (e.g., coral), fungal, and bacterial sources. The compounds were identified from 617 source species, belonging to 146 families...
June 22, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28637209/purification-and-characterization-of-two-new-cell-bound-bioactive-compounds-produced-by-wildlactococcus-lactisstrain
#2
Margarete Alice Fontes Saraiva, Dag Anders Brede, Ingolf Figved Nes, Maria Cristina Baracat-Pereira, Marisa Vieira de Queiroz, Célia Alencar de Moraes
Novel compounds and innovative methods are required considering that antibiotic resistance has reached a crisis point. In the study, two cell-bound antimicrobial compounds produced by L. lactis ID1.5 were isolated and partially characterized. Following purification by cationic exchange and a solid phase C18 column, antimicrobial activity was recovered after three runs of RPC using 60% (v/v) and 100% (v/v) of 2-propanol for elution, suggesting that more than one antimicrobial compound were produced by L. lactis ID1...
June 20, 2017: FEMS Microbiology Letters
https://www.readbyqxmd.com/read/28636950/structural-evidence-of-quercetin-multi-target-bioactivity-a-reverse-virtual-screening-strategy
#3
Diego Carvalho, Margot Paulino, Fabio Polticelli, Florencia Arredondo, Robert J Williams, Juan A Abin-Carriquiry
The ubiquitous flavonoid quercetin is broadly recognized for showing diverse biological and health-promoting effects, such as anti-cancer, anti-inflammatory and cytoprotective activities. The therapeutic potential of quercetin and similar compounds for preventing such diverse oxidative stress-related pathologies has been generally attributed to their direct antioxidant properties. Nevertheless, accumulated evidence indicates that quercetin is also able to interact with multiple cellular targets influencing the activity of diverse signaling pathways...
June 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28636874/next-generation-matrix-metalloproteinase-inhibitors-novel-strategies-bring-new-prospects
#4
REVIEW
Maxim Levin, Yael Udi, Inna Solomonov, Irit Sagi
Enzymatic proteolysis of cell surface proteins and extracellular matrix (ECM) is critical for tissue homeostasis and cell signaling. These proteolytic activities are mediated predominantly by a family of proteases termed matrix metalloproteinases (MMPs). The growing evidence in recent years that ECM and non-ECM bioactive molecules (e.g., growth factors, cytokines, chemokines, on top of matrikines and matricryptins) have versatile functions redefines our view on the roles matrix remodeling enzymes play in many physiological and pathological processes, and underscores the notion that ECM proteolytic reaction mechanisms represent master switches in the regulation of critical biological processes and govern cell behavior...
June 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28636366/oxygenation-via-c-h-c-c-bond-activation-with-molecular-oxygen
#5
Yu-Feng Liang, Ning Jiao
The selective oxidation of organic molecules is a fundamentally important component of modern synthetic chemistry. In the past decades, direct oxidative C-H and C-C bond functionalization has proved to be one of the most efficient and straightforward methods to synthesize complex products from simple and readily available starting materials. Among these oxidative processes, the use of molecular oxygen as a green and sustainable oxidant has attracted considerable attention because of its highly atom-economical, abundant, and environmentally friendly characteristics...
June 21, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28635656/screening-and-identification-of-the-metabolites-in-rat-plasma-and-urine-after-oral-administration-of-areca-catechu-l-nut-extract-by-ultra-high-pressure-liquid-chromatography-coupled-with-linear-ion-trap-orbitrap-tandem-mass-spectrometry
#6
Lulu Li, Zhiqiang Luo, Yang Liu, Hao Wang, Aoxue Liu, Guohua Yu, Mengwei Li, Ruirui Yang, Xinjing Chen, Jialian Zhu, Baosheng Zhao
Areca catechu L. nut, a well-known toxic traditional herbal medicine, has been widely used to treat various diseases in China and many other Asian countries for centuries. However, to date the in vivo absorption and metabolism of its multiple bioactive or toxic components still remain unclear. In this study, liquid chromatography coupled with tandem mass spectrometry was used to analyze the major components and their metabolites in rat plasma and urine after oral administration of Areca catechu L. nut extract (ACNE)...
June 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28635654/the-identification-of-a-sirt6-activator-from-brown-algae-fucus-distichus
#7
Minna K Rahnasto-Rilla, Padraig McLoughlin, Tomasz Kulikowicz, Maire Doyle, Vilhelm A Bohr, Maija Lahtela-Kakkonen, Luigi Ferrucci, Maria Hayes, Ruin Moaddel
Brown seaweeds contain many bioactive compounds, including polyphenols, polysaccharides, fucosterol, and fucoxantin. These compounds have several biological activities, including anti-inflammatory, hepatoprotective, anti-tumor, anti-hypertensive, and anti-diabetic activity, although in most cases their mechanisms of action are not understood. In this study, extracts generated from five brown algae (Fucus dichitus, Fucus vesiculosus (Linnaeus), Cytoseira tamariscofolia, Cytoseira nodacaulis, Alaria esculenta) were tested for their ability to activate SIRT6 resulting in H3K9 deacetylation...
June 21, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28635652/fucaceae-a-source-of-bioactive-phlorotannins
#8
REVIEW
Marcelo D Catarino, Artur M S Silva, Susana M Cardoso
Fucaceae is the most dominant algae family along the intertidal areas of the Northern Hemisphere shorelines, being part of human customs for centuries with applications as a food source either for humans or animals, in agriculture and as remedies in folk medicine. These macroalgae are endowed with several phytochemicals of great industrial interest from which phlorotannins, a class of marine-exclusive polyphenols, have gathered much attention during the last few years due to their numerous possible therapeutic properties...
June 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28635649/the-sea-urchin-arbacia-lixula-a-novel-natural-source-of-astaxanthin
#9
Paola Cirino, Christophe Brunet, Martina Ciaravolo, Christian Galasso, Luigi Musco, Tomás Vega Fernández, Clementina Sansone, Alfonso Toscano
Several echinoderms, including sea urchins, are valuable sources of bioactive compounds but their nutraceutical potential is largely unexplored. In fact, the gonads of some sea urchin species contain antioxidants including carotenoids and polyhydroxylated naphthoquinones (PHNQ's), such as echinochrome A. Astaxanthin is known to have particular bioactivity for the prevention of neurodegenerative diseases. This carotenoid is produced by microalgae, while several marine invertebrates can bioaccumulate or synthetize it from metabolic precursors...
June 21, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28634711/%C3%AE-pyrone-derivatives-from-a-streptomyces-strain-resensitize-tamoxifen-resistance-in-breast-cancer-cells
#10
Rui-Min Yang, Xiu-Lei Zhang, Li Wang, Jian-Ping Huang, Jing Yang, Yi-Jun Yan, Jian-Ying Luo, Xiang-Ting Wang, Sheng-Xiong Huang
Tamoxifen resistance (TamR) is the underlying cause of treatment failure in many breast cancer patients receiving tamoxifen. In order to look for noncytotoxic natural products with the ability to reverse TamR, an extract from strain Streptomyces sp. KIB-H0495 was detected to be active. Subsequent large scale fermentation and isolation led to the isolation of four α-pyrone derivatives including two new compounds, violapyrones J (2) and K (3), and two known analogues, violapyrones B (1) and I (4). Further bioactivity assays indicated that only 1 and 3 exerted potent resensitization effects on MCF-7/TamR cells at a concentration of 1 μM...
June 20, 2017: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/28633858/effects-of-processing-parameters-in-the-sonic-assisted-water-extraction-sawe-of-6-gingerol
#11
Syaripah Zaimah Syed Jaapar, Noor Azian Morad, Yoshio Iwai, Mariam Firdhaus Mad Nordin
The use of water in subcritical conditions for extraction has several drawbacks. These include the safety features, higher production costs and possible degradation of the bioactive compounds. To overcome these problems, sonic energy and an entrainer were used as external interventions to decrease the polarity of water at milder operating conditions. The effect of low (28kHz) and high (800kHz) frequencies of sonication in the extraction of the main ginger bioactive compound (6-gingerol) were compared. Six parameters were studied: mean particle size (MPS, mm), time of extraction, applied power, sample to solvent ratio (w/v), temperature of extraction, and the percentage of entrainer...
September 2017: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/28633346/tetramethylpyrazine-reverses-intracerebroventricular-streptozotocin-induced-memory-deficits-by-inhibiting-gsk-3%C3%AE
#12
Fen Lu, Xu Li, Wei Li, Ke Wei, Yong Yao, Qianlin Zhang, Xinliang Liang, Jiewen Zhang
Brain dysfunction, especially cognitive impairment, is one of the main complications in Alzheimer's disease (AD), which threatens the health of 46.8 million people worldwide. At present, the pathogenesis of cognitive dysfunction is only partially understood, and effective therapies for memory loss in AD remain elusive. Tetramethylpyrazine (TMP) is one of the major bioactive compounds purified from Chuanxiong, a Chinese herb used for the treatment of neurovascular and cardiovascular diseases. The neuroprotective properties of TMP are evident in some neurodegenerative diseases, including Parkinson's disease...
June 15, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/28633108/bioactivity-and-quantitative-analysis-of-isohexenylnaphthazarins-in-root-periderm-of-two-echium-spp-e-%C3%A2-plantagineum-and-e-%C3%A2-gaditanum
#13
Alexandra G Durán, M Teresa Gutiérrez, Carlos Rial, Ascensión Torres, Rosa M Varela, Manuel M Valdivia, José M G Molinillo, Dominik Skoneczny, Leslie A Weston, Francisco A Macías
Isohexenylnaphthazarins are commonly found in the root periderm of several Boraginaceous plants and are known for their broad range of biological activities. The work described herein concerns the biological activity of compounds from the roots of Echium plantagineum L. and Echium gaditanum Boiss (Boraginaceae) collected from field sites in southern Spain and Australia. Bioactivity was assessed using etiolated wheat coleoptile bioassay and in vitro growth inhibitory activity in HeLa and IGROV-1 cells. The quantification of four isohexenylnaphthazarins (shikonin/alkannin, deoxyshikonin/deoxyalkannin, acetylshikonin/acetylalkannin and dimethylacrylshikonin/dimethylacrylalkannin) was performed by LC-MS/MS using juglone as internal standard...
June 17, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28632894/flavonoids-as-modulators-of-metabolic-enzymes-and-drug-transporters
#14
REVIEW
Anca Miron, Ana Clara Aprotosoaie, Adriana Trifan, Jianbo Xiao
Flavonoids, natural compounds found in plants and in plant-derived foods and beverages, have been extensively studied with regard to their capacity to modulate metabolic enzymes and drug transporters. In vitro, flavonoids predominantly inhibit the major phase I drug-metabolizing enzyme CYP450 3A4 and the enzymes responsible for the bioactivation of procarcinogens (CYP1 enzymes) and upregulate the enzymes involved in carcinogen detoxification (UDP-glucuronosyltransferases, glutathione S-transferases (GSTs))...
June 20, 2017: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/28632415/synthesis-and-biological-evaluation-of-tanshinone-iia-derivatives-as-novel-endothelial-protective-agents
#15
Xiaoling Bi, Kuojun Zhang, Long He, Biao Gao, Qinlan Gu, Xueyan Li, Jun Chen, Jinxin Wang
AIM: Oxidative stress-induced endothelial injury is a main risk factor in the pathogenesis of cardiovascular diseases. Tanshinone IIA (Tan IIA) exerts protective functions on endothelial cells in response to oxidative stress. To exploit new bioactive compounds from this natural product, 12 derivatives were first synthesized and evaluated for endothelial protective activities. MATERIALS & METHODS: Title compounds were prepared according to high-yielded synthetic routes, and their protective effects on human endothelial EA...
June 20, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28632338/difluoromethylation-reactions-of-organic-compounds
#16
Damian E Yerien, Sebastian Barata-Vallejo, Al Postigo
The relevance of the -CF2H moiety has attracted considerable attention from organic synthetic and medicinal chemistry communities, because this group can act as a more lipophilic isostere of the carbinol, thiol, hydroxamic acid or amide groups. Being weakly acidic, the CF2H moiety can establish hydrogen bonding interactions to improve the binding selectivity of biologically active compounds. Therefore, the hydroxyl, amino, and thio substituents of lead structures are routinely replaced by a CF2H motif in drug discovery, with great benefits in the pharmacological activity of drugs and drug candidates and agrochemicals...
June 20, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28631525/polyphenol-profile-by-uhplc-ms-ms-anti-glycation-antioxidant-and-cytotoxic-activities-of-several-samples-of-propolis-from-the-northeastern-semi-arid-region-of-brazil
#17
Jadriane de Almeida Xavier, Iara Barros Valentim, Fabiana O S Camatari, Alberto M M de Almeida, Henrique Fonseca Goulart, Jamylle Nunes de Souza Ferro, Emiliano de Oliveira Barreto, Bruno Coelho Cavalcanti, Carla B G Bottoli, Marília Oliveira Fonseca Goulart
CONTEXT: Propolis has promising biological activities. Propolis samples from the Northeast of Bahia, Brazil - sample A from Ribeira do Pombal and B, from Tucano - were investigated, with new information regarding their biological activities. OBJECTIVE: This paper describes the chemical profile, antioxidant, anti-glycation and cytotoxic activities of these propolis samples. MATERIAL AND METHODS: Ethanol extracts of these propolis samples (EEP) and their fractions were analyzed to determine total phenolic content (TPC); antioxidant capacity through DPPH(•), FRAP and lipid peroxidation; anti-glycation activity, by an in vitro glucose (10 mg/mL) bovine serum albumine (1 mg/mL) assay, during 7 d; cytotoxic activity on cancer (SF295, HCT-116, OVCAR-8, MDA-MB435, MX-1, MCF7, HL60, JURKAT, MOLT-4, K562, PC3, DU145) and normal cell lines (V79) at 0...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28631409/exploration-of-a-ternary-deep-eutectic-solvent-of-methyltriphenylphosphonium-bromide-chalcone-formic-acid-for-the-selective-recognition-of-rutin-and-quercetin-in-herba-artemisiae-scopariae
#18
Wanwan Ma, Tangand Baokun, Kyung Ho Row
A methyltriphenylphosphonium bromide/chalcone/formic acid as a green ternary deep eutectic solvent was applied as a functional monomer and dummy template simultaneously in the synthesis of a new molecularly imprinted polymer. Ternary deep eutectic solvent based molecularly imprinted polymers were used as a solid-phase extraction sorbent in the separation and purification of rutin and quercetin from Herba Artemisiae Scopariae combined with high-performance liquid chromatography. FTIR spectroscopy and field-emission scanning electron microscopy were applied to characterize the deep eutectic solvent based molecularly imprinted polymers synthesized using different molar ratios of chalcone...
June 20, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28630399/dietary-mastic-oil-extracted-from-pistacia-lentiscus-var-chia-suppresses-tumor-growth-in-experimental-colon-cancer-models
#19
Katerina Spyridopoulou, Angeliki Tiptiri-Kourpeti, Evangeli Lampri, Eleni Fitsiou, Stavros Vasileiadis, Manolis Vamvakias, Haido Bardouki, Anna Goussia, Vasiliki Malamou-Mitsi, Mihalis I Panayiotidis, Alex Galanis, Aglaia Pappa, Katerina Chlichlia
Plant-derived bioactive compounds attract considerable interest as potential chemopreventive anticancer agents. We analyzed the volatile dietary phytochemicals (terpenes) present in mastic oil extracted from the resin of Pistacia lentiscus var. chia and comparatively investigated their effects on colon carcinoma proliferation, a) in vitro against colon cancer cell lines and b) in vivo on tumor growth in mice following oral administration. Mastic oil inhibited - more effectively than its major constituents- proliferation of colon cancer cells in vitro, attenuated migration and downregulated transcriptional expression of survivin (BIRC5a)...
June 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28629816/tinospora-species-an-overview-of-their-modulating-effects-on-the-immune-system
#20
REVIEW
Areeful Haque, Ibrahim Jantan, Syed Nasir Abbas Bukhari
ETHNOPHARMACOLOGICAL RELEVANCE: Studies on the effects of natural immunomodulators to heal various diseases related to the immune system have been a growing interest in recent years. Amongst the medicinal plants, Tinospora species (family; Menispermaceae) have been one of the widely investigated plants for their modulating effects on the immune system due to their wide use in ethnomedicine to treat various ailments related to immune-related diseases. However, their ethnopharmacological uses are mainly with limited or without scientific basis...
June 16, 2017: Journal of Ethnopharmacology
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