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Natural product chemistry

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https://www.readbyqxmd.com/read/27920947/the-daniel-k-inouye-college-of-pharmacy-scripts-poha-berry-physalis-peruviana-with-potential-anti-inflammatory-and-cancer-prevention-activities
#1
Leng Chee Chang, Mayuramas Sang-Ngern, John M Pezzuto, Carolyn Ma
The Daniel K. Inouye College of Pharmacy, during a historic event in Spring 2016, graduated the first two students in the Pacific region to earn a PhD in pharmaceutical sciences at the University of Hawai'i at Hilo. The college offers PhD programs in these five disciplines: Cancer Biology, Medicinal Chemistry, Pharmaceutics, Pharmacognosy, and Pharmacology. One of the Pharmacognosy dissertations focused on plant-derived natural products with potential anti-inflammatory and cancer chemopreventive activities...
November 2016: Hawai'i Journal of Medicine & Public Health: a Journal of Asia Pacific Medicine & Public Health
https://www.readbyqxmd.com/read/27916862/contrasting-roles-of-deoxynivalenol-and-nivalenol-in-host-mediated-interactions-between-fusarium-graminearum-and-sitobion-avenae
#2
Jassy Drakulic, Mohd Haziq Kahar, Olubukola Ajigboye, Toby Bruce, Rumiana V Ray
Fusarium graminearum is the predominant causal species of Fusarium head blight in Europe and North America. Different chemotypes of the species exist, each producing a plethora of mycotoxins. Isolates of differing chemotypes produce nivalenol (NIV) and deoxynivalenol (DON), which differ in toxicity to mammals and plants. However, the effect of each mycotoxin on volatile emissions of plant hosts is not known. Host volatiles are interpreted by insect herbivores such as Sitobion avenae, the English grain aphid, during host selection...
November 30, 2016: Toxins
https://www.readbyqxmd.com/read/27909555/effect-of-dual-type-oligosaccharides-on-constipation-in-loperamide-treated-rats
#3
Sung Hee Han, Ki Bae Hong, Eun Young Kim, So Hyun Ahn, Hyung Joo Suh
BACKGROUND/OBJECTIVES: Constipation is a condition that can result from intestinal deformation. Because humans have an upright posture, the effects of gravity can cause this shape deformation. Oligosaccharides are common prebiotics and their effects on bowel health are well known. However, studies of the physiological functionality of a product that contains both lactulose and galactooligosaccharides are insufficient. We investigated the constipation reduction effect of a dual-type oligosaccharide, Dual-Oligo, in loperamide-treated rats...
December 2016: Nutrition Research and Practice
https://www.readbyqxmd.com/read/27905166/50-and-more-years-of-propellane-chemistry-from-a-chemical-curiosity-to-explosive-applications-in-material-sciences-and-natural-product-chemistry
#4
Alicia Merve Dilmac, Eduard Spuling, Armin de Meijere, Stefan Bräse
Propellanes are a unique class of compounds with well over 10000 members with an inverted tetrahedral configuration featuring a weak single bond between two carbon atoms linked by three additional bridge. Not only structurally interesting, these propella-type compounds exhibit unusual reactivities. In this review, we highlight their synthesis and applications in material sciences, natural product chemistry and medicinal chemistry. We feature the chemistry of [1.1.1]propellane like the synthesis of oligomeric and polymeric structures derived from it such as bicyclo[1...
November 30, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27904956/some-nontoxic-metal-based-drugs-for-selected-prevalent-tropical-pathogenic-diseases
#5
REVIEW
Saliu A Amolegbe, Caroline A Akinremi, Sheriff Adewuyi, Amudat Lawal, Mercy O Bamigboye, Joshua A Obaleye
Metal coordination of bioorganic compounds from both natural and synthetic products is not only gaining recognition in drug design and medicinal inorganic chemistry research, also they are being considered in the improvement of the bioactivity of drugs. What is done in this paper is a review of recent advances in the study of coordination-driven drug delivery, i.e., metal-based drugs (MBDs). The role of some late first row transition metal ions namely Fe, Cu and Zn in the biological activities of metallodrugs such as antimalarials and antimicrobials are highlighted...
November 30, 2016: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/27898308/emerging-biopharmaceuticals-from-marine-actinobacteria
#6
REVIEW
Syed Shams Ul Hassan, Komal Anjum, Syed Qamar Abbas, Najeeb Akhter, Bibi Ibtesam Shagufta, Sayed Asmat Ali Shah, Umber Tasneem
Actinobacteria are quotidian microorganisms in the marine world, playing a crucial ecological role in the recycling of refractory biomaterials and producing novel secondary metabolites with pharmaceutical applications. Actinobacteria have been isolated from the huge area of marine organisms including sponges, tunicates, corals, mollusks, crabs, mangroves and seaweeds. Natural products investigation of the marine actinobacteria revealed that they can synthesize numerous natural products including alkaloids, polyketides, peptides, isoprenoids, phenazines, sterols, and others...
November 22, 2016: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/27885824/the-quest-for-value-added-products-from-carbon-dioxide-and-water-in-a-dielectric-barrier-discharge-a-chemical-kinetics-study
#7
Ramses Snoeckx, Alp Ozkan, Francois Reniers, Annemie Bogaerts
Recycling of carbon dioxide by its conversion into value-added products has gained significant interest owing to the role it can play for use in an anthropogenic carbon cycle. The combined conversion with H2 O could even mimic the natural photosynthesis process. An interesting gas conversion technique currently being considered in the field of CO2 conversion is plasma technology. To investigate whether it is also promising for this combined conversion, we performed a series of experiments and developed a chemical kinetics plasma chemistry model for a deeper understanding of the process...
November 25, 2016: ChemSusChem
https://www.readbyqxmd.com/read/27882198/design-synthesis-and-cytotoxic-evaluation-of-novel-tubulysin-analogues-as-adc-payloads
#8
Carolyn A Leverett, Sai Chetan K Sukuru, Beth C Vetelino, Sylvia Musto, Kevin Parris, Jayvardhan Pandit, Frank Loganzo, Alison H Varghese, Guoyun Bai, Bin Liu, Dingguo Liu, Sarah Hudson, Venkata Ramana Doppalapudi, Joseph Stock, Christopher J O'Donnell, Chakrapani Subramanyam
The tubulysin class of natural products has attracted much attention from the medicinal chemistry community due to its potent cytotoxicity against a wide range of human cancer cell lines, including significant activity in multidrug-resistant carcinoma models. As a result of their potency, the tubulysins have become an important tool for use in targeted therapy, being widely pursued as payloads in the development of novel small molecule drug conjugates (SMDCs) and antibody-drug conjugates (ADCs). A structure-based and parallel medicinal chemistry approach was applied to the synthesis of novel tubulysin analogues...
November 10, 2016: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27875779/novel-pyrimidine-2-4-dione-1-2-3-triazole-and-furo-2-3-d-pyrimidine-2-one-1-2-3-triazole-hybrids-as-potential-anti-cancer-agents-synthesis-computational-and-x-ray-analysis-and-biological-evaluation
#9
Tomislav Gregorić, Mirela Sedić, Petra Grbčić, Andrea Tomljenović Paravić, Sandra Kraljević Pavelić, Mario Cetina, Robert Vianello, Silvana Raić-Malić
Regioselective 1,4-disubstituted 1,2,3-triazole tethered pyrimidine-2,4-dione derivatives (5-23) were successfully prepared by the copper(I)-catalyzed click chemistry. While known palladium/copper-cocatalyzed method based on Sonogashira cross-coupling followed by the intramolecular 5-endo-dig ring closure generated novel 6-alkylfuro[2,3-d]pyrimidine-2-one-1,2,3-triazole hybrids (24b-37b), a small library of their 5-alkylethynyl analogs (24a-37a) was synthesized and described for the first time by tandem terminal alkyne dimerization and subsequent 5-endo-trig cyclization, which was additionally corroborated with computational and X-ray crystal structure analyses...
November 14, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27871089/water-balance-creates-a-threshold-in-soil-ph-at-the-global-scale
#10
E W Slessarev, Y Lin, N L Bingham, J E Johnson, Y Dai, J P Schimel, O A Chadwick
Soil pH regulates the capacity of soils to store and supply nutrients, and thus contributes substantially to controlling productivity in terrestrial ecosystems. However, soil pH is not an independent regulator of soil fertility-rather, it is ultimately controlled by environmental forcing. In particular, small changes in water balance cause a steep transition from alkaline to acid soils across natural climate gradients. Although the processes governing this threshold in soil pH are well understood, the threshold has not been quantified at the global scale, where the influence of climate may be confounded by the effects of topography and mineralogy...
November 21, 2016: Nature
https://www.readbyqxmd.com/read/27865713/platensimycin-and-platencin-inspirations-for-chemistry-biology-enzymology-and-medicine
#11
REVIEW
Jeffrey D Rudolf, Liao-Bin Dong, Ben Shen
Natural products have served as the main source of drugs and drug leads, and natural products produced by microorganisms are one of the most prevalent sources of clinical antibiotics. Their unparalleled structural and chemical diversities provide a basis to investigate fundamental biological processes while providing access to a tremendous amount of chemical space. There is a pressing need for novel antibiotics with new mode of actions to combat the growing challenge of multidrug resistant pathogens. This review begins with the pioneering discovery and biological activities of platensimycin (PTM) and platencin (PTN), two antibacterial natural products isolated from Streptomyces platensis...
November 16, 2016: Biochemical Pharmacology
https://www.readbyqxmd.com/read/27865702/biosynthetic-approaches-to-creating-bioactive-fungal-metabolites-pathway-engineering-and-activation-of-secondary-metabolism
#12
REVIEW
Takayuki Motoyama, Hiroyuki Osada
The diversity of natural products is greater than that of combinatorial chemistry compounds and is similar to that of drugs. Compounds rich in sp(3) carbons, such as natural products, typically exhibit high structural complexity and high specificity to molecular targets. Microorganisms can synthesize such sp(3) carbon-rich compounds and can be used as excellent factories for making bioactive compounds. Here, we mainly focus on pathway engineering of two sp(3) carbon-rich bioactive indole alkaloids, fumitremorgin C and terpendole E...
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27865033/selective-production-of-carbon-monoxide-via-methane-oxychlorination-over-vanadyl-pyrophosphate
#13
Vladimir Paunović, Guido Zichittella, Réne Verel, Amol P Amrute, Javier Pérez-Ramírez
A catalytic process is demonstrated for the selective conversion of methane into carbon monoxide via oxychlorination chemistry. The process involves addition of HCl to a CH4 -O2 feed to facilitate C-H bond activation under mild conditions, leading to the formation of chloromethanes, CH3 Cl and CH2 Cl2 . The latter are oxidized in situ over the same catalyst, yielding CO and recycling HCl. A material exhibiting chlorine evolution by HCl oxidation, high activity to oxidize chloromethanes into CO, and no ability to oxidize CO, is therefore essential to accomplish this target...
November 16, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27854340/a-green-approach-for-allylations-of-aldehydes-and-ketones-combining-allylborate-mechanochemistry-and-lanthanide-catalyst
#14
Viviane P de Souza, Cristiane K Oliveira, Thiago M de Souza, Paulo H Menezes, Severino Alves, Ricardo L Longo, Ivani Malvestiti
Secondary and tertiary alcohols synthesized via allylation of aldehydes and ketones are important compounds in bioactive natural products and industry, including pharmaceuticals. Development of a mechanochemical method using potassium allyltrifluoroborate salt and water, to successfully perform the allylation of aromatic and aliphatic carbonyl compounds is reported for the first time. By controlling the grinding parameters, the methodology can be selective, namely, very efficient for aldehydes and ineffective for ketones, but by employing lanthanide catalysts, the reactions with ketones can become practically quantitative...
November 16, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27847183/management-effects-on-greenhouse-gas-dynamics-in-fen-ditches
#15
Mike Peacock, Luke M Ridley, Chris D Evans, Vincent Gauci
Globally, large areas of peatland have been drained through the digging of ditches, generally to increase agricultural production. By lowering the water table it is often assumed that drainage reduces landscape-scale emissions of methane (CH4) into the atmosphere to negligible levels. However, drainage ditches themselves are known to be sources of CH4 and other greenhouse gases (GHGs), but emissions data are scarce, particularly for carbon dioxide (CO2) and nitrous oxide (N2O), and show high spatial and temporal variability...
November 12, 2016: Science of the Total Environment
https://www.readbyqxmd.com/read/27829917/the-direct-oxidative-diene-cyclization-and-related-reactions-in-natural-product-synthesis
#16
REVIEW
Juliane Adrian, Leona J Gross, Christian B W Stark
The direct oxidative cyclization of 1,5-dienes is a valuable synthetic method for the (dia)stereoselective preparation of substituted tetrahydrofurans. Closely related reactions start from 5,6-dihydroxy or 5-hydroxyalkenes to generate similar products in a mechanistically analogous manner. After a brief overview on the history of this group of transformations and a survey on mechanistic and stereochemical aspects, this review article provides a summary on applications in natural product synthesis. Moreover, current limitations and future directions in this area of chemistry are discussed...
2016: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27827902/chiral-alkyl-halides-underexplored-motifs-in-medicine
#17
REVIEW
Bálint Gál, Cyril Bucher, Noah Z Burns
While alkyl halides are valuable intermediates in synthetic organic chemistry, their use as bioactive motifs in drug discovery and medicinal chemistry is rare in comparison. This is likely attributable to the common misconception that these compounds are merely non-specific alkylators in biological systems. A number of chlorinated compounds in the pharmaceutical and food industries, as well as a growing number of halogenated marine natural products showing unique bioactivity, illustrate the role that chiral alkyl halides can play in drug discovery...
November 4, 2016: Marine Drugs
https://www.readbyqxmd.com/read/27816503/silver-nanoparticles-significance-of-physicochemical-properties-and-assay-interference-on-the-interpretation-of-in-vitro-cytotoxicity-studies
#18
REVIEW
Kausar B Riaz Ahmed, Amber M Nagy, Ronald P Brown, Qin Zhang, Subhas G Malghan, Peter L Goering
Silver nanoparticles (AgNPs) have generated a great deal of interest in the research, consumer product, and medical product communities due to their antimicrobial and anti-biofouling properties. However, in addition to their antimicrobial action, concerns have been expressed about the potential adverse human health effects of AgNPs. In vitro cytotoxicity studies often are used to characterize the biological response to AgNPs and the results of these studies may be used to identify hazards associated with exposure to AgNPs...
November 3, 2016: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/27807811/myceliophthora-thermophila-m77-utilizes-hydrolytic-and-oxidative-mechanisms-to-deconstruct-biomass
#19
Hévila Brognaro Dos Santos, Thaís Milena Souza Bezerra, José G C Pradella, Priscila Delabona, Deise Lima, Eleni Gomes, Steve D Hartson, Janet Rogers, Brian Couger, Rolf Prade
Biomass is abundant, renewable and useful for biofuel production as well as chemical priming for plastics and composites. Deconstruction of biomass by enzymes is perceived as recalcitrant while an inclusive breakdown mechanism remains to be discovered. Fungi such as Myceliophthora thermophila M77 appear to decompose natural biomass sources quite well. This work reports on this fungus fermentation property while producing cellulolytic enzymes using natural biomass substrates. Little hydrolytic activity was detected, insufficient to explain the large amount of biomass depleted in the process...
December 2016: AMB Express
https://www.readbyqxmd.com/read/27801813/substituent-inductive-effects-on-the-electrochemical-oxidation-of-flavonoids-studied-by-square-wave-voltammetry-and-ab-initio-calculations
#20
Netzahualcóyotl Arroyo-Currás, Víctor M Rosas-García, Marcelo Videa
Flavonoids are natural products commonly found in the human diet that show antioxidant, anti-inflammatory and anti-hepatotoxic activities. These nutraceutical properties may relate to the electrochemical activity of flavonoids. To increase the understanding of structure-electrochemical activity relations and the inductive effects that OH substituents have on the redox potential of flavonoids, we carried out square-wave voltammetry experiments and ab initio calculations of eight flavonoids selected following a systematic variation in the number of hydroxyl substituents and their location on the flavan backbone: three flavonols, three anthocyanidins, one anthocyanin and the flavonoid backbone flavone...
October 27, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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