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https://www.readbyqxmd.com/read/28822987/effects-of-a-water-extract-of-lepidium-meyenii-root-in-different-models-of-persistent-pain-in-rats
#1
Barbara Tenci, Lorenzo Di Cesare Mannelli, Mario Maresca, Laura Micheli, Giuseppe Pieraccini, Nadia Mulinacci, Carla Ghelardini
Lepidium meyenii (Walp.), commonly called maca, is an Andean crop belonging to the Brassicaceae family. Maca hypocotils are habitually consumed as customary food as well as traditional remedies for pathological conditions such as infertility. Moreover, the characterization of maca extracts revealed the presence of compounds that are able to modulate the nervous system. Aimed to evaluate the efficacy of L. meyenii in persistent pain, the present study analyzed the effects of a commercial root extract from maca in different animal models reproducing the most common causes of chronic painful pathologies...
August 21, 2017: Zeitschrift Für Naturforschung. C, A Journal of Biosciences
https://www.readbyqxmd.com/read/28822281/an-integrative-study-to-identify-novel-scaffolds-for-sphingosine-kinase-1-inhibitors
#2
Marcela Vettorazzi, Emilio Angelina, Santiago Lima, Tomas Gonec, Jan Otevrel, Pavlina Marvanova, Tereza Padrtova, Petr Mokry, Pavel Bobal, Lina M Acosta, Alirio Palma, Justo Cobo, Janette Bobalova, Jozef Csollei, Ivan Malik, Sergio Alvarez, Sarah Spiegel, Josef Jampilek, Ricardo D Enriz
Sphingosine kinase 1 (SphK1), the enzyme that produces the bioactive sphingolipid metabolite, sphingosine-1-phosphate, is a promising new molecular target for therapeutic intervention in cancer and inflammatory diseases. In view of its importance, the main objective of this work was to find new and more potent inhibitors for this enzyme possessing different structural scaffolds than those of the known inhibitors. Our theoretical and experimental study has allowed us to identify two new structural scaffolds (three new compounds), which could be used as starting structures for the design and then the development of new inhibitors of SphK1...
August 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28821847/overcoming-the-plasticity-of-plant-specialized-metabolism-for-selective-diterpene-production-in-yeast
#3
Codruta Ignea, Anastasia Athanasakoglou, Aggeliki Andreadelli, Maria Apostolaki, Minas Iakovides, Euripides G Stephanou, Antonios M Makris, Sotirios C Kampranis
Plants synthesize numerous specialized metabolites (also termed natural products) to mediate dynamic interactions with their surroundings. The complexity of plant specialized metabolism is the result of an inherent biosynthetic plasticity rooted in the substrate and product promiscuity of the enzymes involved. The pathway of carnosic acid-related diterpenes in rosemary and sage involves promiscuous cytochrome P450s whose combined activity results in a multitude of structurally related compounds. Some of these minor products, such as pisiferic acid and salviol, have established bioactivity, but their limited availability prevents further evaluation...
August 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28821620/arjunolic-acid-a-peroxisome-proliferator-activated-receptor-alpha-agonist-regresses-cardiac-fibrosis-by-inhibiting-non-canonical-tgf-%C3%AE-signaling
#4
Trisha Bansal, Emeli Chatterjee, Jasdeep Singh, Arjun Ray, Bishwajit Kundu, V Thankamani, Shantanu Sengupta, Sagartirtha Sarkar
Cardiac hypertrophy and associated heart fibrosis remain a major cause of death worldwide. Phytochemicals have gained attention as alternative therapeutics for managing cardiovascular diseases. These include the extract from the plant Terminalia arjuna which is a popular cardioprotectant and may prevent or slow progression of pathological hypertrophy to heart failure. Here, we investigated the mode of action of a principal bioactive T. arjuna compound, arjunolic acid (AA) in ameliorating hemodynamic load-induced cardiac fibrosis and identified its intracellular target...
August 18, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28820614/protective-effects-of-cryoprotectants-and-lyoprotectants-on-the-survival-of-persipeptide-producing-streptomyces-zagrosensis-utmc-1154
#5
Fatemeh Mohammadipanah, Leila Parvizi, Javad Hamedi, Farzaneh Azizmohseni
Streptomyces sp. are bacteria recognized as the producers of more than half of the known bioactive compounds. Developing appropriate preservation methods for industrial strains of Streptomyces is necessary, as continuous subculture could have significant negative effects on their characteristics, including their potential to produce secondary metabolites. The effects of two common preservation methods on a bioactive metabolite producer, Streptomyces zagrosensis UTMC 1154, were studied. In the cryopreservation method, glycerol and dimethyl sulfoxide (DMSO) were evaluated as cryoprotectants...
August 18, 2017: Biopreservation and Biobanking
https://www.readbyqxmd.com/read/28820568/enhanced-drug-delivery-into-cell-cytosol-via-glycoprotein-h-derived-peptide-conjugated-nanoemulsions
#6
Teresa Fotticchia, Raffaele Vecchione, Pasqualina Liana Scognamiglio, Daniela Guarnieri, Vincenzo Calcagno, Concetta Di Natale, Chiara Attanasio, Maria De Gregorio, Chiara Di Cicco, Vincenzo Quagliariello, Nicola Maurea, Antonio Barbieri, Luca Raiola, Rosario Vincenzo Iaffaioli, Paolo Antonio Netti
The key role of nanocarriers in improving the pharmacological properties of commonly used drugs is recognized worldwide. It is also known that in the development of new effective nanocarriers the use of targeting moieties integrated on their surface is essential. Herein, we propose a nanocarrier based on an oil in water nanoemulsion coated with a membranotropic peptide derived from the glycoprotein H of Herpes simplex virus 1, known as gH625, in order to reduce endo-lysosomal accumulation and to enhance cytosolic localization...
August 18, 2017: ACS Nano
https://www.readbyqxmd.com/read/28820068/known-triterpenes-and-their-derivatives-as-scaffolds-for-the-development-of-new-therapeutic-agents-for-cancer
#7
Gregorio Peron, Giovanni Marzaro, Stefano Dall'Acqua
Plants produce several bioactive secondary metabolites whose are used as therapeutic agents to treat various diseases, among them cancer. Triterpenes are a category of secondary metabolites that exert inhibitory activity against multiple intracellular and extracellular targets in euchariotic cells. These targets are proteins involved in apoptosis, cell development and differentiation, angiogenesis, metastasis and inflammatory processes. The inhibition of their functions leads to decreased cellular growth, differentiation and migration, resulting in antitumor activity, as shown by the numerous published experimental results...
August 17, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28819580/analytical-method-for-the-validation-of-three-polyphenols-as-a-marker-compound-for-the-standardization-of-solidago-virgaurea-subsp-gigantea-extracts-and-antiadipogenesis-of-harvesting-time-and-location
#8
Seung Hwan Hwang, Ju Hee Kim, Zhiqiang Wang, Jae-Yong Lee, Soon Sung Lim
Protocatechuic acid (PC), chlorogenic acid (CA), and kaempferol-3-O-rutinoside (K-O-R), isolated from the Solidago virgaurea subsp. gigantea (SV) extract, were quickly and efficiently separated using HPLC. Our chromatographic method was found to effectively separate PC, CA, and K-O-R at retention times of 5.36, 8.22, and 17.04 min, respectively. Linearity of PC, CA, and K-O-R was found to be in the range of 4.85-485.00, 47.5-1900.00, and 8.50-850.00 μg/ml. Recoveries ranged between 101.32 and 103.30%, 95...
2017: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/28819542/mulberry-fruit-extract-affords-protection-against-ethyl-carbamate-induced-cytotoxicity-and-oxidative-stress
#9
Wei Chen, Yuting Li, Tao Bao, Vemana Gowd
Ethyl carbamate (EC) is a food and environmental toxicant and is a cause of concern for human exposure. Several studies indicated that EC-induced toxicity was associated with oxidative stress. Mulberry fruits are reported to have a wide range of bioactive compounds and pharmacological activities. The present study was therefore aimed to investigate the protective property of mulberry fruit extract (MFE) on EC-induced cytotoxicity and oxidative stress. Chemical composition analysis showed that total phenolic content and total flavonoid content in MFE were 502...
2017: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/28818747/antidepressant-like-activity-of-methyl-jasmonate-involves-modulation-of-monoaminergic-pathways-in-mice
#10
Solomon Umukoro, Adaeze Adebesin, Gladys Agu, Osarume Omorogbe, Stephen Babajide Asehinde
PURPOSE: The efficacy of current antidepressant drugs has been compromised by adverse effects, low remission and delay onset of action necessitating the search for alternative agents. Methyl jasmonate (MJ), a bioactive compound isolated from Jasminum grandiflorum has been shown to demonstrate antidepressant activity but its mechanism of action remains unknown. Thus, the role of monoaminergic systems in the antidepression-like activity of MJ was investigated in this study. MATERIALS AND METHODS: Mice were given i...
August 14, 2017: Advances in Medical Sciences
https://www.readbyqxmd.com/read/28818464/one-pot-synthesis-of-bioactive-cyclopentenones-from-%C3%AE-linolenic-acid-and-docosahexaenoic-acid
#11
Daniel Maynard, Sara Mareike Müller, Monika Hahmeier, Jana Löwe, Ivo Feussner, Harald Gröger, Andrea Viehhauser, Karl-Josef Dietz
Oxidation products of the poly-unsaturated fatty acids (PUFAs) arachidonic acid, α-linolenic acid and docosahexaenoic acid are bioactive in plants and animals as shown for the cyclopentenones prostaglandin 15d-PGJ2 and PGA2, cis-(+)-12-oxophytodienoic acid (12-OPDA), and 14-A-4 neuroprostane. In this study an inexpensive and simple enzymatic multi-step one-pot synthesis is presented for 12-OPDA, which is derived from α-linolenic acid, and the analogous docosahexaenoic acid (DHA)-derived cyclopentenone [(4Z,7Z,10Z)-12-[[-(1S,5S)-4-oxo-5-(2Z)-pent-2-en-1yl]-cyclopent-2-en-1yl] dodeca-4,7,10-trienoic acid, OCPD]...
August 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28817965/trametes-versicolor-ethanol-extract-a-promising-candidate-for-health-promoting-food-supplement
#12
Ljiljana Janjušević, Boris Pejin, Sonja Kaišarević, Stanislava Gorjanović, Ferenc Pastor, Kristina Tešanović, Maja Karaman
This study aimed to estimate antiradical, antioxidant (AO) and cytotoxic activities of the fungus Trametes versicolor ethanol fruiting body extract. The extract was found to effectively scavenge both O2(•-) and NO(•) (29.62 and 52.48 μg/mL, respectively). It also showed a good AO activity in the polarographic HPMC assay (950%/mL). p-Hydroxybenzoic acid may be one of the responsible compounds for the afore-mentioned activities. The same extract also exhibited a concentration-dependent cytotoxicity against MCF-7 and HepG2 tumour cell lines reaching IC50 values of 123...
August 18, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28817272/cysteine-isocyanide-in-multicomponent-reaction-synthesis-of-peptido-mimetic-1-3-azoles
#13
Thimmalapura M Vishwanatha, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Dömling
An alternative approach towards the simple and robust synthesis of highly substituted peptidic thiazole derivatives by using Ugi-multicomponent reaction (U-MCR) is described. Thus, we introduced the enantiopure (R)-2-methyl-2-isocyano-3-(tritylthio)propanoate as novel class of isocyanide in MCR. This bifunctional isocyanide was found to undergo mild cyclodehydration to afford thiazole containing peptidomimetics in a short synthetic sequence. Several examples of bis-heterocyclic rings were also synthesized through the proper choice of the aldehyde component in the U-4CR...
August 17, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28817233/evaluation-and-quantitative-analysis-of-11-compounds-in-morinda-officinalis-using-ultra-high-performance-liquid-chromatography-and-photodiode-array-detection-coupled-with-chemometrics
#14
Xiangsheng Zhao, Weijun Kong, Yakui Zhou, Jianhe Wei, Meihua Yang
Morinda officinalis (Rubiaceae) is a traditional Chinese medicine widely used for the treatment of impotence and osteoporosis in clinical therapy. In the present study, a rapid and simple ultra high performance liquid chromatography with photodiode array detection method was developed and validated for the simultaneous determination of 11 bioactive compounds in M. officinalis. This assay method was validated with respect to linearity (R(2)( ) > 0.9991), precision, repeatability, limit of detection, limit of quantification, and accuracy (with observed recovery rates between 94...
August 17, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28817221/neuroprotective-effects-of-honokiol-from-chemistry-to-medicine
#15
REVIEW
Sylwia Talarek, Joanna Listos, Davide Barreca, Ester Tellone, Antoni Sureda, Seyed Fazel Nabavi, Nady Braidy, Seyed Mohammad Nabavi
The incidence of neurological disorders is growing in developed countries together with increased lifespan. Nowadays, there are still no effective treatments for neurodegenerative pathologies, which make necessary to search for new therapeutic agents. Natural products, most of them used in traditional medicine, are considered promising alternatives for the treatment of neurodegenerative diseases. Honokiol is a natural bioactive phenylpropanoid compound, belonging to the class of neolignan, found in notable amounts in the bark of Magnolia tree, and has been reported to exert diverse pharmacological properties including neuroprotective activities...
August 17, 2017: BioFactors
https://www.readbyqxmd.com/read/28817105/bioactive-compounds-from-mexican-varieties-of-the-common-bean-phaseolus-vulgaris-implications-for-health
#16
REVIEW
Celia Chávez-Mendoza, Esteban Sánchez
As Mexico is located within Mesoamerica, it is considered the site where the bean plant originated and where it was domesticated. Beans have been an integral part of the Mexican diet for thousands of years. Within the country, there are a number of genotypes possessing highly diverse physical and chemical properties. This review describes the major bioactive compounds contained on the Mexican varieties of the common bean. A brief analysis is carried out regarding the benefits they have on health. The effect of seed coat color on the nutraceutical compounds content is distinguished, where black bean stands out because it is high content of anthocyanins, polyphenols and flavonoids such as quercetin...
August 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28814950/morinda-citrifolia-l-leaf-extract-prevent-weight-gain-in-sprague-dawley-rats-fed-a-high-fat-diet
#17
Najla Gooda Sahib Jambocus, Amin Ismail, Alfi Khatib, Fawzi Mahomoodally, Nazamid Saari, Muhammad Waseem Mumtaz, Azizah Abdul Hamid
Background: Morinda citrifolia L. is widely used as a folk medicinal food plant to manage a panoply of diseases, though no concrete reports on its potential anti-obesity activity. This study aimed to evaluate the potential of M. citrifolia leaf extracts (MLE60) in the prevention of weight gain in vivo and establish its phytochemical profile. Design: Male Sprague-Dawley rats were divided into groups based on a normal diet (ND) or high fat diet (HFD), with or without MLE60 supplementation (150 and 350 mg/kg body weight) and assessed for any reduction in weight gain...
2017: Food & Nutrition Research
https://www.readbyqxmd.com/read/28814827/anticholinesterase-constituents-from-the-leaves-of-spondias-mombin-l-anacardiaceae
#18
Taiwo Olayemi Elufioye, Efere M Obuotor, Joseph M Agbedahunsi, Saburi A Adesanya
Spondias mombin has been used in traditional medicine for the management of several diseases, including memory loss. This study aimed to evaluate the cholinesterase inhibitory activity of the methanol extract of the leaves and its derived fractions, as well as carry out detailed phytochemical investigations leading to the isolation and characterization of bioactive compounds from the plant. The acetyl cholinesterase (AChE) and butyryl cholinesterase (BUChE) inhibitory activities were evaluated by colorimetric and thin-layer chromatography bioautographic assay techniques...
2017: Biologics: Targets & Therapy
https://www.readbyqxmd.com/read/28814238/structural-insights-for-drugs-developed-for-phospholipase-d-enzymes
#19
Kimberly Stieglitz
BACKGROUND: In recent years human phospholipase D enzymes (PLD1 and PLD2 isozymes) have emerged as drug targets for various diseases such as cardiovascular disease, cancer, infectious diseases and neurodegenerative conditions such as Alzheimer's and Parkinson's disease. The interest in PLD as a drug target is due to the fact that PLD enzymes belong to a superfamily of phospholipases that are essential to intracellular and extracellular signaling. Many bioactive lipid signaling molecules are generated by these enzymes including phosphatidic and lysophosphatidic acid, arachidonic acid, and diacylglycerol (DAG)...
August 15, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28814115/neuraminidase-inhibitory-activity-by-compounds-isolated-from-aerial-parts-of-rhinacanthus-nasutus
#20
Hee Jae Kwak, SeonJu Park, Nanyoung Kim, Guijae Yoo, Jun Hyung Park, Youngse Oh, Nguyen Xuan Nhiem, Seung Hyun Kim
Rhinacanthus nasutus (L.) Kurz (Acanthaceae) is known as traditional medicine for the treatment of various diseases, such as cancer, fungal infections, herpes virus infections and several types of skin diseases in South-East Asian countries. In this study, eight compounds 1-8 were isolated from the aerial parts of R. nasutus. The structures of compounds were determined by the spectroscopic methods, including 1D and 2D NMR. The isolated compounds were evaluated for neuraminidase inhibitory activity. Several lignans, 2,3-bis[(4-hydroxy-3,5-dimethoxyphenyl)methyl]-1,4-butanediol (5) and 8,8'-bisdihydrosiringenin glucoside (6), significantly inhibited neuraminidase activity, which was comparable to the positive controls, mangiferin and oseltamivir...
August 17, 2017: Natural Product Research
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