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https://www.readbyqxmd.com/read/28734162/extraction-and-in-vitro-screening-of-potential-acetylcholinesterase-inhibitors-from-the-leaves-of-panax-japonicus
#1
Sainan Li, Chengyu Liu, Chunming Liu, Yuchi Zhang
Ultrafiltration liquid chromatography-mass spectrometry (UFLC-MS) is an efficient method that can be applied to rapidly screen and identify ligands for acetylcholinesterase (AChE) from the leaves of Panax japonicus. Using this method, we identified 5 major compounds, chikusetsusaponins V, Ib, IV, IVa, and IVa ethyl ester, as potent AChE inhibitors, which were assessed for anti-Alzheimer disease activity using the PC12 cell model. A continuous online method, which consisted of microwave-assisted extraction, a solvent concentration tank, and centrifugal partition chromatography (MAE-SCT-CPC), was newly developed for scaled up production of these compounds with high purity and efficiency...
July 12, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28732430/bee-pollen-flavonoids-as-a-therapeutic-agent-in-allergic-and-immunological-disorders
#2
Masoomeh Jannesar, Maryam Sharif Shoushtari, Ahmad Majd, Zahra Pourpak
Bee pollen grains, as the male reproductive part of seed-bearing plants contain considerable concentrations of various phytochemicals and nutrients. Since antiquity, people throughout the world used pollens to cure colds, flu, ulcers, premature aging, anemia and colitis. It is now well-documented that some bee pollen secondary metabolites (e.g. flavonoid) may have positive health effects. In recent years, the flavonoids have attracted much interest because of their wide range of biological properties and their beneficial effects on human health...
June 2017: Iranian Journal of Allergy, Asthma, and Immunology
https://www.readbyqxmd.com/read/28732338/toxic-organic-substances-and-marker-compounds-in-size-segregated-urban-particulate-matter-implications-for-involvement-in-the-in%C3%A2-vitro-bioactivity-of-the-extractable-organic-matter
#3
Athanasios Besis, Alexandra Tsolakidou, Dimitra Balla, Constantini Samara, Dimitra Voutsa, Anastasia Pantazaki, Theodora Choli-Papadopoulou, Theodore S Lialiaris
Toxic organic substances and polar organic marker compounds, i.e. polychlorinated biphenyls (PCBs), organochlorine pesticides (OCPs), polybrominated diphenyl ethers (PBDEs), polycyclic aromatic hydrocarbons (PAHs) and their nitro-derivatives (N-PAHs), as well as dicarboxylic acids (DCAs) and sugars/sugar anhydrites (S/SAs) were analyzed in size-segregated PM samples (<0.49, 0.49-0.97, 0.97-3 and >3 μm) collected at two urban sites (urban traffic and urban background) during the cold and the warm season...
July 18, 2017: Environmental Pollution
https://www.readbyqxmd.com/read/28731316/phytochemical-analysis-of-myrtus-communis-plant-conventional-versus-microwave-assisted-extraction-procedures
#4
Nadia Bouaoudia-Madi, Lila Boulekbache-Makhlouf, Nabil Kadri, Farid Dahmoune, Hocine Remini, Sofiane Dairi, Sonia Oukhmanou-Bensidhoum, Khodir Madani
Background Myrtle (Myrtus communis L) may constitute an interesting dietary source of health protective compounds. Microwave-assisted extraction (MAE) of total phenolic compounds (TPC) from myrtle leaf, stems, pericarp, and seeds was studied and the results were compared with those of the conventional method extraction (CME) in terms of extraction time. Methods Extraction yield/efficiency and antioxidant activity were measured using radical scavenging assay (DPPH•) and reducing power. Results The results show that the MAE was higher in terms of saving energy, extraction time (62 s) and extraction efficiency of bioactive compound compared to CME (2 h)...
June 10, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28731312/gentiana-kurroo-royle-attenuates-the-metabolic-aberrations-in-diabetic-rats-swertiamarin-swertisin-and-lupeol-being-the-possible-bioactive-principles
#5
Khalid Ghazanfar, Khan Mubashir, Showkat A Dar, Tazeen Nazir, Iqra Hameed, Bashir A Ganai, Seema Akbar, Akbar Masood
Background Gentiana kuroo Royle is a medicinally important plant of north-western Himalayas used for various ailments. In the present study, the plant extracts were investigated for the antidiabetic effects in streptozotocin-induced diabetic rats. Methods The impact of the extracts on serum glucose levels of diabetic rats was compared with reference drug - glibenclamide-treated diabetic rats. Streptozotocin injection was used to induce diabetes in fasted rats. Various biochemical, physiological and histopathological parameters in diabetic rats were observed for assessing the antidiabetic activity...
April 29, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28731232/a-comprehensive-review-of-agrimoniin
#6
REVIEW
Daniel M Grochowski, Krystyna Skalicka-Woźniak, Ilkay Erdogan Orhan, Jianbo Xiao, Marcello Locatelli, Jakub P Piwowarski, Sebastian Granica, Michał Tomczyk
Plant tannins are a unique class of polyphenols with relatively high molecular weights. Within the ellagitannins group, agrimoniin--dimeric ellagitannin--is one of the most representative compounds found in many plant materials belonging to the Rosaceae family. Agrimoniin was first isolated in 1982 from roots of Agrimonia pilosa Ledeb. (Rosaceae), a plant traditionally used in Japan and China as an antidiarrheal, hemostatic, and antiparasitic agent. Agrimoniin is a constituent of medicinal plants, which are often applied orally in the form of infusions, decoctions, or tinctures...
July 21, 2017: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/28729856/biological-significance-of-marine-actinobacteria-of-east-coast-of-andhra-pradesh-india
#7
Alapati Kavitha, Handanahal S Savithri
An attempt was made to identify actinobacterial strains present in the marine soil of East Coast regions viz., Chirala, Bapatla, and Peddaganjam, Andhra Pradesh; Kanyakumari, Tamil Nadu and Goa, Goa along with the study of their antimicrobial potential. Eight out of 73 actinobacterial strains isolated from these regions showed strong antimicrobial activity against Gram positive bacteria, Gram negative bacteria, and Candida albicans. Molecular identification (16S rRNA analysis) of the eight strains revealed that they belong to Dietzia sp...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28729705/diterpenoid-alkaloids-from-delphinium-anthriscifolium-var-majus
#8
Lian-Hai Shan, Ji-Fa Zhang, Feng Gao, Shuai Huang, Xian-Li Zhou
Extensive phytochemical investigation on the whole herbs of Delphinium anthriscifolium var. majus led to the identification of fourteen diterpenoid alkaloids, including three new C20-diterpenoid alkaloids (anthriscifolsines A-C, 1-3), six new C19-diterpenoid alkaloids (anthriscifolrines A-F, 4-9), and five know compounds (10-14). Among them, anthriscifolsine A represents a novel C20-diterpenoid alkaloid characterized by a seco C-ring. The structures of the isolated compounds were elucidated by extensive spectroscopic methods, including HR-ESI-MS, X-ray, and 1D and 2D NMR experiments...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729053/bioactive-polyprenylated-benzophenone-derivatives-from-the-fruits-extracts-of-garcinia-xanthochymus
#9
Ui Joung Youn, Tawanun Sripisut, Gabriella Miklossy, James Turkson, Surat Laphookhieo, Leng Chee Chang
Two new polycyclic prenylated xanthones (1 and 2) and a new phenylpropanoid glycoside (3), along with seven known compounds (4-10) were isolated from the fruits of Garcinia xanthochymus. The structures were elucidated by 1D- and 2D-NMR, and HRMS experiments. The isolates were evaluated for their inhibitory effects against the viability of U251MG glioblastoma and MDA-MB-231 breast cancer cells that harbor an aberrantly active signal transducer and exhibit activation of transcription 3 (STAT3), and compared to normal NIH3T3 mouse fibroblasts...
July 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28728974/activation-of-cryptic-phthoxazolin-a-production-in-streptomyces-avermitilis-by-the-disruption-of-autoregulator-receptor-homologue-avar3
#10
Dian Anggraini Suroto, Shigeru Kitani, Kiyoko T Miyamoto, Yasuko Sakihama, Masayoshi Arai, Haruo Ikeda, Takuya Nihira
The genomes of actinomycetes encode many cryptic novel/useful bioactive compounds, but access to these cryptic secondary metabolites remains limited. Streptomyces avermitilis predominantly produces three polyketide antibiotics (avermectin, filipin, and oligomycin) but has the potential to produce more secondary metabolites based on the number of cryptic biosynthetic gene clusters. Here, we extensively investigated the metabolite profiles of a gene disruptant of AvaR3 (an autoregulator receptor homologue), which is involved in the pleiotropic regulation of antibiotic production and cell morphology...
July 17, 2017: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/28728925/potential-anti-cancer-activity-of-7-o-pentyl-quercetin-efficient-membrane-targeted-kinase-inhibition-and-pro-oxidant-effect
#11
Nicola Sassi, Andrea Mattarei, Virginia Espina, Lance Liotta, Mario Zoratti, Cristina Paradisi, Lucia Biasutto
Quercetin is a redox-active plant-derived flavonoid with potential anticancer effects, stemming largely from its interaction with a number of proteins, and in particular from inhibition of pro-life kinases. To improve efficacy, we reasoned that a local increase in concentration of the compound at the level of cell membranes would result in a more efficient interaction with membrane-associated signaling kinases. We report here the synthesis of all five isomeric quercetin derivatives in which an n-pentyl group was linked via an ether bond to each hydroxyl of the flavonoid kernel...
July 17, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28728492/the-bioactivity-of-hedysarum-coronarium-extracts-on-skin-enzymes-and-cells-correlates-with-phenolic-content
#12
Bruno Burlando, Giulia Pastorino, Annalisa Salis, Gianluca Damonte, Marco Clericuzio, Laura Cornara
CONTEXT: The search for bioactive compounds from botanical sources is attracting much interest. However, differences in chemical composition may occur within the same species depending on different geographical origins. OBJECTIVES: We evaluated the properties on skin enzymes and cells of extracts from sulla legume crop Hedysarum coronarium L. (Fabaceae), collected at two Italian sites near Pisa and Ventimiglia, for possible dermatological and cosmetic applications...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28728067/an-optimized-hplc-uv-method-for-quantitatively-determining-sesquiterpenes-in-nardostachyos-radix-et-rhizoma
#13
Vu Ngoc Han Le, Trong Quan Khong, Min Kyun Na, Kyung Tae Kim, Jong Seong Kang
Nardostachyos Radix et Rhizoma (NR), the root and rhizome from either Nardostachys jatamansi Batal or Nardostachys jatamansi DC, is known to have biological functions including neuro-protective and anti-pancreatitis activity. The main bioactive compounds within NR are all classified as sesquiterpenes, and include desoxo-narchinol A, nardosinonediol, and nardosinone. Although NR is a valuable herb that is widely used in many Asian countries, robust quality control protocols for NR are still in question, especially those that can analyze the three main active compounds...
July 8, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28727452/catalytic-intermolecular-carboamination-of-unactivated-alkenes-via-directed-aminopalladation
#14
Zhen Liu, Yanyan Wang, Zichen Wang, Tian Zeng, Peng Liu, Keary M Engle
An intermolecular 1,2-carboamination of unactivated alkenes proceeding via a Pd(II)/Pd(IV) catalytic cycle has been developed. To realize this transformation, a cleavable bidentate directing group is used to control the regioselectivity of aminopalladation and stabilize the resulting organopalladium(II) intermediate, such that oxidative addition to a carbon electrophile outcompetes potential β-hydride elimination. Under the optimized reaction conditions, a broad range of nitrogen nucleophiles and carbon electrophiles were compatible coupling partners in this reaction, affording moderate to high yields...
July 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28727445/an-antibiotic-that-inhibits-the-atpase-activity-of-an-abc-transporter-by-binding-to-a-remote-extracellular-site
#15
Leigh Morgan Matano, Heidi Gabrielle Morris, Anthony R Hesser, Sara E S Martin, Wonsik Lee, Tristan W Owens, Emaline Laney, Hidemasa Nakaminami, David Hooper, Timothy C Meredith, Suzanne Walker
Antibiotic-resistant strains of Staphylococcus aureus pose a major threat to human health and there is an ongoing need for new antibiotics to treat resistant infections. In a high throughput screen (HTS) of 230,000 small molecules designed to identify bioactive wall teichoic acid (WTA) inhibitors, we identified one hit, which was expanded through chemical synthesis into a small panel of potent compounds. We showed that these compounds target TarG, the transmembrane component of the two-component ATP-binding cassette (ABC) transporter TarGH, which exports WTA precursors to the cell surface for attachment to peptidoglycan...
July 20, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28726718/inhibitory-effects-of-trapping-agents-of-sulfur-drug-reactive-intermediates-against-major-human-cytochrome-p450-isoforms
#16
Jasleen K Sodhi, Erlie Marie Delarosa, Jason S Halladay, James P Driscoll, Teresa Mulder, Patrick M Dansette, S Cyrus Khojasteh
In some cases, the formation of reactive species from the metabolism of xenobiotics has been linked to toxicity and therefore it is imperative to detect potential bioactivation for candidate drugs during drug discovery. Reactive species can covalently bind to trapping agents in in vitro incubations of compound with human liver microsomes (HLM) fortified with β-nicotinamide adenine dinucleotide phosphate (NADPH), resulting in a stable conjugate of trapping agent and reactive species, thereby facilitating analytical detection and providing evidence of short-lived reactive metabolites...
July 20, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28726493/chemical-profile-and-antihyperlipidemic-effect-of-portulaca-oleracea-l-seeds-in-streptozotocin-induced-diabetic-rats
#17
Jilan A Nazeam, Hala M El-Hefnawy, Gamal Omran, Abdel-Naser Singab
Hypolipidemic effect of Portulaca oleracea L. seed extract and its fractions have been studied on streptozotocin (STZ) at dose 75 mg/kg b.wt. After fractionation of the alcoholic extract; petroleum ether fraction was the most active fraction that decreased different hyperlipidemia biochemical parameters. After chromatographic analysis; oleamide, ethylpalmitate, β-amyrin, stigmasterol and β-sitosterol were identified. The GLC analysis of unsaponifiable matter revealed the presence of; lignoceric acid as a major constituent in the most bioactive fraction...
July 20, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28725146/lc-esi-ms-ms-profiling-of-phenolics-from-eleutherococcus-spp-inflorescences-structure-activity-relationship-as-antioxidants-inhibitors-of-hyaluronidase-and-acetylcholinesterase
#18
Daniel Załuski, Marta Olech, Rafał Kuźniewski, Robert Verpoorte, Renata Nowak, Helena D Smolarz
Nature is a source of many plant-based molecules used as pro- or drugs. Eleutherococcus species are native to Asia and the North Russia, and are traditionally used to treat various diseases. In turn, neither secondary metabolites of the species cultivated in the West Europe nor the bioactivity is known. No differences in the phenols and flavonoids content in the inflorescences were found. The richest in polyphenols was E. giraldii (5.18 mg/g), while in flavonoids it was E. gracilistylus (1.80 mg/g). Using LC-ESI-MS/MS, protocatechuic and trans-caffeic acids have been identified as the most abundant compounds in E...
July 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28724908/design-and-discovery-of-novel-monastrol-1-3-5-triazines-as-potent-anti-breast-cancer-agent-via-attenuating-epidermal-growth-factor-receptor-tyrosine-kinase
#19
Jitendra Kumar Srivastava, Girinath G Pillai, Hans Raj Bhat, Amita Verma, Udaya Pratap Singh
A novel series of hybrid analogues of monastrol-1,3,5-triazine were designed and developed via one-pot synthesis using Bi(NO3)3 as a catalyst. Entire compounds were evaluated for their anticancer activity against HeLa (cervical cancer), MCF-7 (breast cancer), HL-60 (Human promyelocytic leukemia), HepG2 (Hepatocellular carcinoma) and MCF 12A (normal epithelial breast cell line) using MTT assay, where they showed highest inhibitory activity against MCF-7. The molecules were also found to be non-toxic to MCF 12A cells...
July 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28724656/dietary-flavonoid-intake-reduces-the-risk-of-head-and-neck-but-not-esophageal-or-gastric-cancer-in-us-men-and-women
#20
Lucy Sun, Amy F Subar, Claire Bosire, Sanford M Dawsey, Lisa L Kahle, Thea P Zimmerman, Christian C Abnet, Ruth Heller, Barry I Graubard, Michael B Cook, Jessica L Petrick
Background: Flavonoids are bioactive polyphenolic compounds found in fruits, vegetables, and beverages of plant origin. Previous studies have shown that flavonoid intake reduces the risk of certain cancers; however, few studies to date have examined associations of flavonoids with upper gastrointestinal cancers or used prospective cohorts.Objective: Our study examined the association between intake of flavonoids (anthocyanidins, flavan-3-ols, flavanones, flavones, flavonols, and isoflavones) and risk of head and neck, esophageal, and gastric cancers...
July 19, 2017: Journal of Nutrition
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