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https://www.readbyqxmd.com/read/29778019/phoenix-dactylifera-protects-against-oxidative-stress-and-hepatic-injury-induced-by-paracetamol-intoxication-in-rats
#1
Gamal A Salem, Ahmed Shaban, Hussain A Diab, Wesam A Elsaghayer, Manal D Mjedib, Aomassad M Hnesh, Ravi P Sahu
The current studies were sought to determine effects of antioxidant potential of aqueous and methanolic extracts of Phoenix dactylifera leaves (PLAE and PLME) against the widely-used analgesic paracetamol (PCM) induced hepatotoxicity. Groups of rats were treated with or without PCM (1500 mg/kg), PLAE and PLME (300 mg/kg) and n-acetylcysteine (NAC, 50 mg/kg) followed by assessments of liver function tests, oxidative stress, antioxidant defenses, and hepatotoxicity. We observed that PCM significantly elevated serum liver markers, aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), and bilirubin compared to control (untreated) group...
May 16, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29777940/curcumin-attenuates-cerebral-ischemia-injury-in-sprague-dawley-rats-and-pc12-cells-by-suppressing-overactivated-autophagy
#2
Yan Zhang, Ming Fang, Yameng Sun, Ting Zhang, Nan Shi, Jinfeng Li, Lei Jin, Kangyong Liu, Jianliang Fu
The present study assessed whether the protective effects of curcumin against cerebral ischemia injury were due to the suppression of overactivated autophagy. Curcumin is a well-known natural polyphenolic compound that effectively counteracts oxidation, inflammation, and various types of cancer. Several studies have demonstrated the protective effects of curcumin against ischemia-reperfusion injury in tissues from the lungs, cardiomyocytes, and liver. The present study employed brain injury models induced by middle cerebral artery occlusion (MCAO) in rats and PC12 oxygen-glucose-deprived (OGD) cells...
May 7, 2018: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29777759/plant-nutraceuticals-as-antimicrobial-agents-in-food-preservation-terpenoids-polyphenols-and-thiols
#3
REVIEW
Ignacio Gutiérrez-Del-Río, Javier Fernández, Felipe Lombó
Synthetic food additives generate a negative perception in consumers. Therefore, food manufacturers search for safer natural alternatives as those involving phytochemicals and plant essential oils. These bioactives have antimicrobial activities widely proved in in vitro tests. Foodborne diseases cause thousands of deaths and millions of infections every year, mainly due to pathogenic bacteria as Salmonella spp., Campylobacter spp., Escherichia coli, Bacillus cereus, Listeria monocytogenes or Staphylococcus aureus...
May 16, 2018: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/29777586/platelets-autotaxin-and-lysophosphatidic-acid-signaling-win-win-factors-for-cancer-metastasis
#4
REVIEW
Raphael Leblanc, Audrey Houssin, Olivier Peyruchaud
Platelets play a crucial role in the survival of metastatic cells in the blood circulation. Interaction of tumor cells with platelets leads to the production of plethoric factors among which our review will focus on lysophosphatidic acid (LPA) because platelets are the highest producers of this bioactive lysophospholipid in the organism. LPA promotes platelet aggregation and blocking platelet function leads to inhibition of breast cancer cell metastasis through decreased LPA signaling. Autotaxin (ATX), a lysophospholipase D responsible for basal concentration of LPA in blood, was detected in platelet α-granules...
May 19, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29777509/improving-the-oral-bioavailability-of-tapentadol-via-a-carbamate-prodrug-approach-synthesis-bioactivation-and-pharmacokinetics
#5
Yingchao Li, Yongjun Wang, Ran Zhang, Cuiru Liu, Yue Wei, Jin Sun, Zhonggui He, Youjun Xu, Tianhong Zhang
Tapentadol suffers from rapid clearance due to extensive metabolism in vivo, which results in low oral bioavailability. In the present study, three novel prodrugs of tapentadol (WWJ01, WWJ02, and WWJ03) were synthesized to improve its metabolic stability and thereby improve its oral bioavailability. They all exhibited good stability in phosphate buffers, simulated gastrointestinal fluids, rat plasma, and intestinal and liver homogenates. Disappointingly, the N,N-diethylcarbamate prodrug of tapentadol (WWJ02) and the N,N-diisopropylcarbamate prodrug of tapentadol (WWJ03) were metabolized into inactive metabolites when incubated with liver microsomes...
May 17, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29777161/genetic-diversity-analysis-reveals-genetic-differentiation-and-strong-population-structure-in-calotropis-plants
#6
Nkatha G Muriira, Alice Muchugi, Anmin Yu, Jianchu Xu, Aizhong Liu
The genus Calotropis (Asclepiadaceae) is comprised of two species, C. gigantea and C. procera, which both show significant economic potential for use of their seed fibers in the textile industry, and of their bioactive compounds as new medicinal resources. The available wild-sourced germplasm contains limited genetic information that restricts further germplasm exploration for the purposes of domestication. We here developed twenty novel EST-SSR markers and applied them to assess genetic diversity, population structure and differentiation within Calotropis...
May 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29776930/modifying-the-lantibiotic-mutacin-1140-for-increased-yield-activity-and-stability
#7
Mengxin Geng, Leif Smith
Mutacin 1140 belongs to the epidermin family of type AI lantibiotics. This family has a broad spectrum of activity against Gram-positive bacteria. The binding of mutacin 1140 to lipid II leads to the inhibition of cell wall synthesis. Pharmacokinetic experiments on type AI lantibiotics are generally discouraging for clinical applications due to their short half-life. The unprotected dehydrated and protease susceptible residues outside of the lanthionine rings may play a role in their short half-life in physiological settings...
May 18, 2018: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/29776716/two-step-senescence-focused-cancer-therapies
#8
REVIEW
Cynthia J Sieben, Ines Sturmlechner, Bart van de Sluis, Jan M van Deursen
Damaged cells at risk of neoplastic transformation can be neutralized by apoptosis or engagement of the senescence program, which induces permanent cell-cycle arrest and a bioactive secretome that is implicated in tumor immunosurveillance. While from an evolutionary perspective senescence is beneficial in that it protects against malignancies, the accumulation of senescent cells in tissues and organs with aging and at sites of various pathologies is largely detrimental. Because induction of senescence in cancer cells is emerging as a therapeutic concept, it will be important to consider these detrimental effects, including tumor-promoting properties that may drive the formation of secondary tumors or cancer relapse...
May 15, 2018: Trends in Cell Biology
https://www.readbyqxmd.com/read/29776647/-effect-of-green-alga-ulva-lactuca-polysaccharides-supplementation-on-blood-pressure-and-on-atherogenic-risk-factors-in-rats-fed-a-high-fat-diet
#9
Z I Tair, F Bensalah, F Boukortt
AIM OF THE STUDY: To highlight the benefits of green alga Ulva lactuca polysaccharides supplementation on blood pressure and atherogenic risk factors in rats fed a high fat diet. METHODS: Wistar male rats were fed a high fat diet (30% sheep fat) for 3 months. At an average body weight (BW) of 360g, the rats (n=18) were divided into 3 groups and consumed, for 28 days, either a high fat diet (HFD) or a high fat diet enriched with 1% of whole green algae (WGA) powder or with 1% of its polysaccharides (PLS)...
May 15, 2018: Annales de Cardiologie et D'angéiologie
https://www.readbyqxmd.com/read/29776417/sinomenine-exerts-anticonvulsant-profile-and-neuroprotective-activity-in-pentylenetetrazole-kindled-rats-involvement-of-inhibition-of-nlrp1-inflammasome
#10
Bo Gao, Yu Wu, Yuan-Jian Yang, Wei-Zu Li, Kun Dong, Jun Zhou, Yan-Yan Yin, Da-Ke Huang, Wen-Ning Wu
BACKGROUND: Epilepsy is a common neurological disorder and is not well controlled by available antiepileptic drugs (AEDs). Inflammation is considered to be a critical factor in the pathophysiology of epilepsy. Sinomenine (SN), a bioactive alkaloid with anti-inflammatory effect, exerts neuroprotective activity in many nervous system diseases. However, little is known about the effect of SN on epilepsy. METHODS: The chronic epilepsy model was established by pentylenetetrazole (PTZ) kindling...
May 18, 2018: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29775778/the-genus-cordyceps-an-extensive-review-of-its-traditional-uses-phytochemistry-and-pharmacology
#11
REVIEW
Opeyemi Joshua Olatunji, Jian Tang, Adesola Tola, Florence Auberon, Omolara Oluwaniyi, Zhen Ouyang
The genus Cordyceps has about 750 identified species which are distributed in many regions of the World, but mainly found in South Asia, Europe and North America. The species of the genus are highly priced and are widely used as food and medicine for the treatment of various ailments. This present review compiles literature information on the ethno-medicinal, phytochemistry and pharmacological properties of species in the genus Cordyceps. In addition, the review also suggest recommendations for the future researches...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29775727/isolation-structure-elucidation-and-antibacterial-activity-of-methyl-4-8-dimethylundecanate-from-the-marine-actinobacterium-streptomyces-albogriseolus-ecr64
#12
Durairaj Thirumurugan, Ramasamy Vijayakumar, Chithravel Vadivalagan, Pushparaj Karthika, Md Khurshid Alam Khan
Around 120 actinobacterial colonies were isolated from various regions of marine East coast region of Tamil Nadu, India. Among them, 33 were morphologically distinct and they were preliminarily screened for their antibacterial activity against Pseudomonas fluorescens, Vibrio cholerae, V. parahaemolyticus, V. alginolyticus, and Aeromonas hydrophila by cross-streak plate technique. Among the isolated, the isolate ECR64 exhibited maximum zone of inhibition against fish pathogenic bacteria. The crude bioactive compounds were extracted from the isolate ECR64 using different organic solvents which exhibited maximum antibacterial activity...
May 15, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29775725/anti-hepatitis-c-virus-activity-and-synergistic-effect-of-nymphaea-alba-extracts-and-bioactive-constituents-in-liver-infected-cells
#13
Sidra Rehman, Usman Ali Ashfaq, Bushra Ijaz, Sheikh Riazuddin
BACKGROUND: Without an effective vaccine, hepatitis C virus (HCV) remains a global threat, inflicting 170-300 million carriers worldwide at risk of cirrhosis and hepatocellular carcinoma (HCC). Though various direct acting antivirals have been redeemed the hepatitis C treatment, a few restraints persist including possible side effects, viral resistance emergence, excessive cost which restricts its availability to a common person. HYPOTHESIS: There is no preventive HCV vaccine available today so the discovery of potent antiviral natural flora and their bioactive constituents may help to develop preventive cures against HCV infection...
May 15, 2018: Microbial Pathogenesis
https://www.readbyqxmd.com/read/29775716/ovalbumin-as-a-carrier-to-significantly-enhance-the-aqueous-solubility-and-photostability-of-curcumin-interaction-and-binding-mechanism-study
#14
Yujia Liu, Yanxue Cai, Danyang Ying, Yinlian Fu, Yahong Xiong, Xueyi Le
Egg ovalbumin (OVA) as a macromolecular carrier has the potential to improve the solubility and stability of insolubility bioactive molecules, however, their binding behavior and the mechanism is still ambiguous. In this work, the curcumin was selected as the target to study the interaction and binding mechanism between curcumin and OVA by thermodynamic titration technique in combination with molecular dynamic simulation. The results suggested that the binding included two steps: first, curcumin molecule entered into the hydrophobic pocket of OVA by hydrophobic interaction; and second the interaction was enhanced via hydrogen bonds, resulting in static fluorescence quenching and secondary structural change of OVA...
May 15, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29775541/molecular-characterization-and-bioactivity-of-coumarin-derivatives-from-the-fruits-of-cucumis-bisexualis
#15
Qin-Ge Ma, Rong-Rui Wei, Ming Yang, Xiao-Ying Huang, Fang Wang, Zhi-Pei Sang, Wen-Min Liu, Qing Yu
Cucumis bisexualis (Cucurbitaceae) is known as "mapao egg" or "muskmelon egg", which has been widely used as a wild melon in Chinese folk. Nine new coumarin derivatives (1-9), named 7-hydroxy-3-(4',6'-dihydroxy-5'-isopropyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (1), 7-hydroxy-3-(5'-prenyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (2), 3-(6'-hydroxy-5'-prenyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (3), 3-(5'-ethyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (4), 3-(4',6'-dihydroxy-5'-dimethylallyl-3'',3''-dimethyl-2H-chromen)-6-prenyl-2H-chromen-2-one (5), 3-[4',6'-dihydroxy-5'-(2-propenyl)-3'',3''-dimethyl-2H-chromen]-14,15-dimethyl-pyrano-chromen-2-one (6), 3-(6'-dihydroxy-5'-isopropanol-3'',3''-dimethyl-2H-chromen)-14,15-dimethyl-pyrano-chromen-2-one (7), 3-(5'-isopentenol-3'',3''-dimethyl-2H-chromen)-14,15-dimethyl-pyrano-chromen-2-one (8), 3-(4',6'-dihydroxy-5'-prenyl-3'',3''-dimethyl-2H-chromen)-14,15-dimethyl-pyrano-chromen-2-one (9), together with twelve known compounds (10-21), were isolated and identified by spectroscopic analysis and references from the active site (EtOAc soluble fraction) of the fruits of C...
May 18, 2018: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/29775538/discovery-of-potent-and-centrally-active-6-substituted-5-fluoro-1-3-dihydro-oxazine-%C3%AE-secretase-bace1-inhibitors-via-active-conformation-stabilization
#16
Kenji Nakahara, Kouki Fuchino, Kazuo Komano, Naoya Asada, Genta Tadano, Tsuyoshi Hasegawa, Takahiko Yamamoto, Yusuke Sako, Masayoshi Ogawa, Chie Unemura, Motoko Hosono, Hisanori Ito, Gaku Sakaguchi, Shigeru Ando, Shuichi Ohnishi, Yasuto Kido, Tamio Fukushima, Deborah Dhuyvetter, Herman Borghys, Harrie J M Gijsen, Yoshinori Yamano, Yasuyoshi Iso, Ken-Ichi Kusakabe
β-Secretase (BACE1) has an essential role in the production of amyloid β peptides that accumulate in patients with Alzheimer's disease (AD). Thus, inhibition of BACE1 is considered to be a disease-modifying approach for the treatment of AD. Our hit-to-lead efforts led to a cellular potent 1,3-dihydro-oxazine 6, which however inhibited hERG and showed high P-gp efflux. The close analog of 5-fluoro-oxazine 8 reduced P-gp efflux; further introduction of electron withdrawing groups at the 6-position improved potency and also mitigated P-gp efflux and hERG inhibition...
May 18, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29775495/enantioselective-synthesis-of-all-carbon-quaternary-centers-structurally-related-to-amaryllidaceae-alkaloids
#17
Jiří Mikušek, Petr Jansa, Pratap R Jagtap, Tomáš Vašíček, Ivana Císařová, Eliška Matoušová
Enantioselective synthesis of all-carbon quaternary centers remains a considerable challenge for synthetic organic chemists. Here, we report a two-step protocol to synthesize such centers including tandem cyclization/Suzuki cross-coupling followed by halocarbocyclization. During this process, two rings, three new C-C bonds and a stereochemically defined all-carbon quaternary center are formed. The absolute configuration of this center is controlled by the stereochemistry of the adjacent stereocenter, which derives from an appropriate enantioenriched starting material...
May 18, 2018: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29775214/pressurized-hot-water-extraction-of-bioactive-compounds-from-artichoke-by-products
#18
Imma Pagano, Anna Lisa Piccinelli, Rita Celano, Luca Campone, Patrizia Gazzerro, Mariateresa Russo, Luca Rastrelli
Artichoke by-products are a suitable source of health-promoting ingredients for the production of dietary supplements and food additives. A pressurized hot water extraction (PHWE) was developed to recover caffeoylquinic acids (CQAs) and flavone glycosides (FLs) from agro-industrial artichoke by-products. The main factors influencing PHWE efficiency and CQA isomerization (temperature, numbers of cycles, modifier and extraction time) were carefully studied and optimized by response surface design. The proposed PHWE procedure provides an exhaustive extraction of CQAs and FLs (recoveries: 93-105 and 90-105%) from artichoke external bracts and leaves of different cultivars (p > 0...
May 18, 2018: Electrophoresis
https://www.readbyqxmd.com/read/29774913/biosynthesis-of-the-teleocidin-type-terpenoid-indole-alkaloids
#19
REVIEW
Takayoshi Awakawa, Ikuro Abe
Teleocidin B is a terpenoid indole alkaloid with unique structures including indolactam and cyclic terpenoid, and is a strong protein kinase C activator. Its unique structure and bioactivity have drawn vast interest from chemists and biologists, and numerous isolation and bioactivity studies on this molecule have been performed. Recently, its biosynthetic enzymes were identified, and some of their crystal structures were reported. In this review, we describe the isolation of teleocidin derivatives, biosynthetic studies, and detailed analyses of biosynthetic enzymes, to clarify their biosynthetic reactions toward the enzymatic synthesis of bioactive teleocidin compounds...
May 18, 2018: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29774654/a-photoactivatable-%C3%AE-5%C3%AE-1-specific-integrin-ligand
#20
Aranzazu Del Campo, Roshna V Nair, Aleeza Farrukh
The integrin α5β1 is overexpressed in colon, breast, ovarian, lung and brain tumors and has been identified as key component in mechanosensing. In order to study how dynamic changes of α5β1 engagement affect cellular behaviour, photoactivatable derivatives of α5β1 specific ligands are presented in this article. A photoremovable protecting group (PRPG) was introduced into the ligand structure at a relevant position for integrin recognition. The presence of the chromophore temporally inhibited ligand bioactivity...
May 18, 2018: Chembiochem: a European Journal of Chemical Biology
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