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Nature medicine

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https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793179/nano-strategies-for-berberine-delivery-a-natural-alkaloid-of-berberis
#2
REVIEW
Elaheh Mirhadi, Mehdi Rezaee, Bizhan Malaekeh-Nikouei
Berberine, as a phytochemical component of some medicinal Chinese herbs (most frequently Berberis vulgaris), is an isoquinoline alkaloid with many therapeutic effects including anti-viral, anti-microbial, anti-diarrhea, anti-inflammatory and anti-tumor effects. Berberine has some significant effects on type 2 diabetes through adenosine monophosphate-activated protein kinase activation, glycolysis stimulation, and mitochondrial function inhibition which subsequently improves both lipid and glucose metabolism...
May 21, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29793137/3-o-sulfation-of-heparin-leads-to-hepatotropism-and-longer-circulatory-half-life
#3
Colton M Miller, Yongmei Xu, Katrina M Kudrna, Blake E Hass, Brianna M Kellar, Andrew W Egger, Jian Liu, Edward N Harris
INTRODUCTION: Heparins are common blood anticoagulants that are critical for many surgical and biomedical procedures used in modern medicine. In contrast to natural heparin derived from porcine gut mucosa, synthetic heparins are homogenous by mass, polymer length, and chemistry. MATERIALS & METHODS: Stable cell lines expressing the human and mouse Stabilin receptors were used to evaluate endocytosis of natural and synthetic heparin. We chemoenzymatically produced synthetic heparin consisting of 12 sugars (dodecamers) containing 14 sulfate groups resulting in a non-3-O sulfated structure (n12mer)...
May 17, 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29793124/how-to-manage-patellofemoral-pain-understanding-the-multifactorial-nature-and-treatment-options
#4
Simon Lack, Bradley Neal, Danilo De Oliveira Silva, Christian Barton
Patellofemoral pain (PFP) is one of the most prevalent conditions within sports medicine, orthopaedic and general practice settings. Long-term treatment outcomes are poor, with estimates that more than 50% of people with the condition will report symptoms beyond 5 years following diagnosis. Additionally, emerging evidence indicates that PFP may be on a continuum with patellofemoral osteoarthritis. Consensus of world leading clinicians and academics highlights the potential benefit of delivering tailored interventions, specific to an individual's needs, to improve patient outcome...
April 12, 2018: Physical Therapy in Sport
https://www.readbyqxmd.com/read/29792906/four-novel-antibacterial-sesquiterpene-%C3%AE-amino-acid-quaternary-ammonium-hybrids-from-the-mycelium-of-mushroom-stereum-hirsutum
#5
Yuan-Chang Duan, Jun Feng, Na Bai, Guo-Hong Li, Ke-Qin Zhang, Pei-Ji Zhao
The mushroom Stereum hirsutum is parasitized by Tremella aurantia to form a heterogeneous basidiocarp Jin'er, which has been used as food and folk medicine in Chinese society. In present work, the S. hirsutum was fermented in YMG broth, and four novel mixed terpenes, stereumamides A-D (1-4), which are sesquiterpenes combined with α-amino acids to form quaternary ammonium hybrids, were isolated from the Stereum hirsutum FP-91666 and their structures were elucidated by spectroscopic data analysis. Stereumamides A and D showed antibacterial activity against Escherichia coli, Staphylococcus aureus, and Salmonella typhimurium, with the minimum inhibitory concentration (MIC) values of 12...
May 21, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29792672/biosynthesis-of-lincosamide-antibiotics-reactions-associated-with-degradation-and-detoxification-pathways-play-a-constructive-role
#6
Daozhong Zhang, Zhijun Tang, Wen Liu
Natural products typically are small molecules produced by living organisms. These products possess a wide variety of biological activities and thus have historically played a critical role in medicinal chemistry and chemical biology either as chemotherapeutic agents or as useful tools. Natural products are not synthesized for use by human beings; rather, living organisms produce them in response to various biochemical processes and environmental concerns, both internal and external. These processes/concerns are often dynamic and thus motivate the diversification, optimization, and selection of small molecules in line with changes in biological function...
May 24, 2018: Accounts of Chemical Research
https://www.readbyqxmd.com/read/29791786/matrine-suppresses-kras-driven-pancreatic-cancer-growth-by-inhibiting-autophagy-mediated-energy-metabolism
#7
Young-Ra Cho, Ji Hyeon Lee, Ji Hye Kim, So-Yeon Lee, Suna Yoo, Min-Kyo Jung, Su Jung Kim, Hyun Ju Yoo, Chang-Gi Pack, Jin Kyung Rho, Jaekyoung Son
Matrine is a natural compound extracted from the herb Sophora flavescens Ait which is widely used in traditional Chinese medicine for treating various diseases. Recently, matrine was reported to have antitumor effects against a variety of cancers without any obvious side effects; however, the molecular mechanisms of its antiproliferative effects on cancer are unclear. Here, we report that matrine inhibits autophagy-mediated energy metabolism, which is necessary for pancreatic cancer growth. We found that matrine significantly reduces pancreatic cancer growth in vitro and in vivo by insufficiently maintaining mitochondrial metabolic function and energy level...
May 23, 2018: Molecular Oncology
https://www.readbyqxmd.com/read/29790516/ultrafast-excited-state-decay-of-natural-uv-filters-from-intermolecular-hydrogen-bonds-to-a-conical-intersection
#8
Peter S Sherin, Yuri P Tsentalovich, Eric Vauthey, Enrico Benassi
Kynurenines (KNs) are natural UV filters of the human eye lens, protecting the eye tissues from solar UV radiation. Key points of their effective protection are the intramolecular charge transfer (ICT) in the excited state and the fast dissipation of absorbed light energy into heat via the intermolecular H-bonds. Herein we report that the introduction of an unsaturated double bond in the amino acid side chain, operating as an ICT-enhancing electron donor group, drastically accelerates the internal conversion (IC) due to a conical intersection (CI) between the potential energy surfaces of the excited and ground states...
May 23, 2018: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29789647/microbial-production-of-novel-sulphated-alkaloids-for-drug-discovery
#9
Eitaro Matsumura, Akira Nakagawa, Yusuke Tomabechi, Shinichi Ikushiro, Toshiyuki Sakaki, Takane Katayama, Kenji Yamamoto, Hidehiko Kumagai, Fumihiko Sato, Hiromichi Minami
Natural products from plants are useful as lead compounds in drug discovery. Plant benzylisoquinoline alkaloids (BIAs) exhibit various pharmaceutical activities. Although unidentified BIAs are expected to be of medicinal value, sufficient quantities of such BIAs, for biological assays, are sometimes difficult to obtain due to their low content in natural sources. Here, we showed that high productivity of BIAs in engineered Escherichia coli could be exploited for drug discovery. First, we improved upon the previous microbial production system producing (S)-reticuline, an important BIA intermediate, to obtain yields of around 160 mg/L, which was 4-fold higher than those of the previously reported highest production system...
May 22, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29789364/bacterial-quorum-sensing-and-microbial-community-interactions
#10
REVIEW
Rhea G Abisado, Saida Benomar, Jennifer R Klaus, Ajai A Dandekar, Josephine R Chandler
Many bacteria use a cell-cell communication system called quorum sensing to coordinate population density-dependent changes in behavior. Quorum sensing involves production of and response to diffusible or secreted signals, which can vary substantially across different types of bacteria. In many species, quorum sensing modulates virulence functions and is important for pathogenesis. Over the past half-century, there has been a significant accumulation of knowledge of the molecular mechanisms, signal structures, gene regulons, and behavioral responses associated with quorum-sensing systems in diverse bacteria...
May 22, 2018: MBio
https://www.readbyqxmd.com/read/29788882/impact-of-drug-metabolism-pharmacokinetics-and-their-relevance-upon-taxus-based-drug-development
#11
Da-Cheng Hao, Guang-Bo Ge, Ping Wang, Ling Yang
Drug metabolism and pharmacokinetic (DMPK) studies of Taxus natural products, their semi-synthetic derivatives and analogs are indispensable in the optimization of lead compounds and clinical therapy. These studies can lead to development of new drug entities with improved absorption, distribution, metabolism, excretion and toxicity (ADME/T) profiles. To date, there have been no comprehensive reviews of the DMPK features of Taxus derived medicinal compounds.Natural and semi-synthetic taxanes may cause and could be affected by drug-drug interaction (DDI)...
May 22, 2018: Current Drug Metabolism
https://www.readbyqxmd.com/read/29788421/predicting-viral-failure-in-human-immunodeficiency-virus-perinatally-infected-youth-with-persistent-low-level-viremia-on-highly-active-antiretroviral-therapy
#12
Ruth Pereira, David A Ludwig, Sunil Mathew, Claudia Flores, Sady Dominguez, Ivan Gonzalez, Delia Rivera-Hernandez, Gwendolyn B Scott, Charles D Mitchell
Background: Less than optimal adherence with antiretroviral therapy occurs commonly among human immunodeficiency virus HIV)-infected youth. In this study, our object was to identify patterns in the prefailure measurement of viral load (VL) that can reliably predict virological failure (VF) in HIV perinatally infected youth on highly active antiretroviral therapy (HAART). Methods: We conducted a retrospective chart review of HIV-infected youth with low-level viremia (LLV), defined as an HIV VL between the lower limits of detection (20-75 copies/mL) and 1000 copies/mL...
May 19, 2018: Journal of the Pediatric Infectious Diseases Society
https://www.readbyqxmd.com/read/29786899/improved-stable-indocyanine-green-icg-mediated-cancer-optotheranostics-with-naturalized-hepatitis-b-core-particles
#13
Wenjun Shan, Ronghe Chen, Qiang Zhang, Jie Zhao, Binbin Chen, Xi Zhou, Shefang Ye, Shengli Bi, Liming Nie, Lei Ren
In recent years, hepatitis B core protein virus-like particle (HBc VLP) is an impressive biomaterial, which has attracted considerable attention due to favorable properties such as structural stability, high uptake efficiency, and biocompatibility in biomedical applications. Heretofore, only a few attempts have been made to apply it in physical, chemical, and biological therapy for cancer. In this study, a tumor-targeting RGD-HBc VLP is first fabricated through genetic engineering. For image-guided cancer phototherapy, indocyanine green (ICG) is loaded into RGD-HBc VLP via a disassembly/reassembly pathway and electrostatic attraction with high efficiency...
May 22, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29786571/-the-disorders-of-the-musculoskeletal-system-in-patients-hospitalized-in-the-geriatric-ward
#14
Maria Matla, Jakub Rajtar-Zembaty, Waldemar Zawada
OBJECTIVE: Introduction: In recent years the interest in the quality of life in old age has been rising, which no doubt is closely linked with the growing population of elderly people. The problems associated with declined functionality of the locomotor system, which naturally occur with age, contribute to increasing morbidity in elderly patients. It is known that lack of exercise can lead to increased aging and disability. Applying the Senior Fitness Test (SFT) allows to explore and assess the patient's mobility...
2018: Wiadomości Lekarskie: Organ Polskiego Towarzystwa Lekarskiego
https://www.readbyqxmd.com/read/29786558/new-substrates-for-stem-cell-control
#15
REVIEW
Sara Schmidt, Annamaria Lilienkampf, Mark Bradley
The capacity to culture stem cells in a controllable, robust and scalable manner is necessary in order to develop successful strategies for the generation of cellular and tissue platforms for drug screening, toxicity testing, tissue engineering and regenerative medicine. Creating substrates that support the expansion, maintenance or directional differentiation of stem cells would greatly aid these efforts. Optimally, the substrates used should be chemically defined and synthetically scalable, allowing growth under defined, serum-free culture conditions...
July 5, 2018: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/29785774/thymol-thyme-and-other-plant-sources-health-and-potential-uses
#16
REVIEW
Bahare Salehi, Abhay Prakash Mishra, Ila Shukla, Mehdi Sharifi-Rad, María Del Mar Contreras, Antonio Segura-Carretero, Hannane Fathi, Nafiseh Nasri Nasrabadi, Farzad Kobarfard, Javad Sharifi-Rad
Thymol is a naturally occurring phenol monoterpene derivative of cymene and isomer of carvacrol. Thymol (10-64%) is one of the major constituent of essential oils of thyme (Thymus vulgaris L., Lamiaceae), a medicinal plant with several therapeutic properties. This plant, native to Mediterranean regions, is commonly used as a culinary herb and also with a long history of use for different medicinal purposes. Nowadays, thymol and thyme present a wide range of functional possibilities in pharmacy, food, and cosmetic industry...
May 22, 2018: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/29785715/current-advances-in-screening-for-bioactive-components-from-medicinal-plants-by-affinity-ultrafiltration-mass-spectrometry
#17
Guilin Chen, Bill X Huang, Mingquan Guo
INTRODUCTION: Medicinal plants have played an important role in maintaining human health for thousands of years. However, the interactions between the active components in medicinal plants and some certain biological targets during a disease are still unclear in most cases. OBJECTIVE: To conduct the high-throughput screening for small active molecules that can interact with biological targets, which is of great theoretical significance and practical value. METHODOLOGY: The ultrafiltration mass spectrometry (UF-LC/MS) is a powerful bio-analytical method by combining affinity ultrafiltration and liquid chromatography-mass spectrometry (LC/MS), which could rapidly screen and identify small active molecules that bind to biological targets of interest at the same time...
May 21, 2018: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/29785194/genus-spondias-a-phytochemical-and-pharmacological-review
#18
REVIEW
Salma Sameh, Eman Al-Sayed, Rola M Labib, Abdel Nasser Singab
It is believed that many degenerative diseases are due to oxidative stress. In view of the limited drugs available for treating degenerative diseases, natural products represent a promising therapeutic strategy in the search for new and effective candidates for treating degenerative diseases. This review focuses on the genus Spondias which is widely used in traditional medicine for the treatment of many diseases. Spondias is a genus of flowering plants belonging to the cashew family (Anacardiaceae). This genus comprises 18 species distributed across tropical regions in the world...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29785193/gallnuts-a-potential-treasure-in-anticancer-drug-discovery
#19
REVIEW
Jiayu Gao, Xiao Yang, Weiping Yin, Ming Li
Introduction. In the discovery of more potent and selective anticancer drugs, the research continually expands and explores new bioactive metabolites coming from different natural sources. Gallnuts are a group of very special natural products formed through parasitic interaction between plants and insects. Though it has been traditionally used as a source of drugs for the treatment of cancerous diseases in traditional and folk medicinal systems through centuries, the anticancer properties of gallnuts are barely systematically reviewed...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29784973/significance-of-prohibitin-domain-family-in-tumorigenesis-and-its-implication-in-cancer-diagnosis-and-treatment
#20
Jie Yang, Bin Li, Qing-Yu He
Prohibitin (PHB) was originally isolated and characterized as an anti-proliferative gene in rat liver. The evolutionarily conserved PHB gene encodes two human protein isoforms with molecular weights of ~33 kDa, PHB1 and PHB2. PHB1 and PHB2 belong to the prohibitin domain family, and both are widely distributed in different cellular compartments such as the mitochondria, nucleus, and cell membrane. Most studies have confirmed differential expression of PHB1 and PHB2 in cancers compared to corresponding normal tissues...
May 21, 2018: Cell Death & Disease
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