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https://www.readbyqxmd.com/read/28645782/cysteine-stabilised-peptide-extract-of-morinda-lucida-benth-leaf-exhibits-antimalarial-activity-and-augments-antioxidant-defense-system-in-p-berghei-infected-mice
#1
Joseph O Adebayo, Kayode E Adewole, Antoniana U Krettli
ETHNOPHARMACOLOGICAL RELEVANCE: Cysteine-stabilised peptides (CSP) are majorly explored for their bioactivities with applications in medicine and agriculture. Morinda lucida leaf is used indigenously for the treatment of malaria; it also contains CSP whose role in the antimalarial activity of the leaf has not been evaluated. AIM OF THE STUDY: This study was therefore performed to evaluate the antimalarial activity of partially purified cysteine-stabilised peptide extract (PPCPE) of Morinda lucida leaf and its possible augmentation of the antioxidant systems of liver and erythrocytes in murine malaria...
June 20, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28643535/efficacy-of-platelets-in-bone-healing-a-systematic-review-on-animal-studies
#2
Sabrina Marcazzan, Roberto Lodovico Weinstein, Massimo Del Fabbro
In presence of large bone defects, delayed bone union, non-union, fractures, and implant surgery, bone reconstruction may be necessary. Different strategies have been employed to enhance bone healing among which the use of autologous platelet concentrates. Due to the high content of platelets and platelet-derived bioactive molecules (e.g., growth factors, antimicrobial peptides), they are promising candidates to increase bone healing. However, a high heterogeneity of both preclinical and clinical studies resulted in contrasting results...
June 23, 2017: Platelets
https://www.readbyqxmd.com/read/28639641/incorporation-of-click-chemistry-glycomimetics-dramatically-alters-triple-helix-stability-in-an-adiponectin-model-peptide
#3
Katherine R Lutteroth, Paul W R Harris, Tom H Wright, Harveen Kaur, Kevin Sparrow, Sung-Hyun Yang, Garth J S Cooper, Margaret A Brimble
Adiponectin (Adpn) has been shown to be a possible therapeutic for Type II diabetes, however the production of a therapeutic version of Adpn has proved to be challenging. Biological studies have highlighted the importance of the glycosylated lysine residues for the formation of bioactive high molecular weight oligomers of Adpn. Through the use of 'click' glycopeptide mimetics, we investigated the role of glycosylated lysine and serine residues for the formation of triple helical structures of the collagenous domain of Adpn, in the context of a collagen model peptide scaffold...
June 22, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28639395/spatiotemporally-controllable-peptide-based-nanoassembly-in-single-living-cells-for-a-biological-self-portrait
#4
Yuanyuan Zhao, Xu Zhang, Zhipeng Li, Shuaidong Huo, Ke Zhang, Juntao Gao, Hao Wang, Xing-Jie Liang
Simultaneous precise localization and activity evaluation of a biomolecule in a single living cell is through an enzyme-specific signal-amplification process, which involves the localized, site-specific self-assembly, and activation of a presignaling molecule. The inactive presignaling tetraphenylethylene (TPE)-peptide derivative, TPE-YpYY, is nondetectable and highly biocompatible and these small molecules rapidly diffuse into living cells. Upon safely arriving at an active site, and accessing the catalytic pocket of an enzyme, TPE-YpYY immediately and quantitatively accumulates in situ in response to enzymatic activity, forms an enzyme anchor TPE-YYY nanoassembly, displays aggregation-induced emission behavior, and finally lights up the active enzyme, indicating its activity, and allowing its status in living cells to be tracked...
June 22, 2017: Advanced Materials
https://www.readbyqxmd.com/read/28636874/next-generation-matrix-metalloproteinase-inhibitors-novel-strategies-bring-new-prospects
#5
REVIEW
Maxim Levin, Yael Udi, Inna Solomonov, Irit Sagi
Enzymatic proteolysis of cell surface proteins and extracellular matrix (ECM) is critical for tissue homeostasis and cell signaling. These proteolytic activities are mediated predominantly by a family of proteases termed matrix metalloproteinases (MMPs). The growing evidence in recent years that ECM and non-ECM bioactive molecules (e.g., growth factors, cytokines, chemokines, on top of matrikines and matricryptins) have versatile functions redefines our view on the roles matrix remodeling enzymes play in many physiological and pathological processes, and underscores the notion that ECM proteolytic reaction mechanisms represent master switches in the regulation of critical biological processes and govern cell behavior...
June 18, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28632895/genome-mining-reveals-high-incidence-of-putative-lipopeptide-biosynthesis-nrps-pks-clusters-containing-fatty-acyl-amp-ligase-genes-in-biofilm-forming-cyanobacteria
#6
Tomáš Galica, Pavel Hrouzek, Jan Mareš
Cyanobacterial lipopeptides exhibit antimicrobial and antifungal bioactivities with potential for use in pharmaceutical research. However, due to their haemolytic activity and cytotoxic effects against human cells, they may pose a health issue if produced in substantial amounts in the environment. In bacteria, lipopeptides can be synthesized via several well-evidenced mechanisms. In one of them, fatty acyl-AMP ligase (FAAL) initiates the biosynthesis by activation of a fatty acyl residue. We have performed a bioinformatic survey of the cyanobacterial genomic information available in the public databases for the presence of FAAL-containing non-ribosomal peptide synthetase/polyketide synthetase (NRPS/PKS) biosynthetic clusters, as a genetic basis for lipopeptide biosynthesis...
June 20, 2017: Journal of Phycology
https://www.readbyqxmd.com/read/28632330/peptides-to-peptidomimetics-a-strategy-based-on-the-structural-features-of-cyclopropane
#7
Akira Mizuno, Kouhei Matsuda, Satoshi Shuto
Peptidomimetics, non-natural mimicries of bioactive peptides, comprise an important class of drug molecules. The essence of the peptidomimetic design is to mimic the key conformation assumed by the bioactive peptides upon binding to their targets. Regulation of the conformation of peptidomimetics is important not only to enhance target binding affinity and selectivity, but also to confer cell membrane permeability for targeting protein-protein interactions in cells. The rational design of peptidomimetics having suitable three-dimensional structures is challenging, however, due to the inherent flexibility of peptides and their dynamic conformational changes upon binding to the target biomolecules...
June 20, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28629983/self-assembly-nanostructure-controlled-sustained-release-activity-and-stability-of-peptide-drugs
#8
Xi-Rui Zhou, Yimeng Cao, Qiang Zhang, Xi-Bo Tian, He Dong, Long Chen, Shi-Zhong Luo
Peptides are considered as a new generation of drugs due to their high structural and functional diversity. However, the development of peptide drugs is always limited by their poor stability and short circulation time. Carriers are applied for peptide drug delivery, but there may be problems like poor loading efficiency and undesired xenobiotic toxicity. Peptide self-assembly is an effective approach to improve the stability and control the release of peptide drugs. In this study, two self-assembling anticancer peptides are designed by appending a pair of glutamic acid and asparagine to either the N-terminus or the C-terminus of a lytic peptide...
June 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28628299/dihydropyrimidine-thiones-and-clioquinol-synergize-to-target-%C3%AE-amyloid-cellular-pathologies-through-a-metal-dependent-mechanism
#9
Daniel F Tardiff, Lauren E Brown, Xiaohui Yan, Richard Trilles, Nathan T Jui, M Inmaculada Barrasa, Kim A Caldwell, Guy A Caldwell, Scott E Schaus, Susan Lindquist
The lack of therapies for neurodegenerative diseases arises from our incomplete understanding of their underlying cellular toxicities and the limited number of predictive model systems. It is critical that we develop approaches to identify novel targets and lead compounds. Here, a phenotypic screen of yeast proteinopathy models identified dihydropyrimidine-thiones (DHPM-thiones) that selectively rescued the toxicity caused by β-amyloid (Aβ), the peptide implicated in Alzheimer's disease. Rescue of Aβ toxicity by DHPM-thiones occurred through a metal-dependent mechanism of action...
June 19, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28627623/p18-peptide-a-functional-fragment-of-pigment-epithelial-derived-factor-inhibits-angiogenesis-in-hepatocellular-carcinoma-via-modulating-vegf-vegfr2-signalling-pathway
#10
Xin Wang, Peng Xiu, Fuhai Wang, Jingtao Zhong, Honglong Wei, Zongzhen Xu, Feng Liu, Jie Li
The P18 peptide is a functional fragment of pigment epithelial-derived factor (PEDF), which is an endogenic angiogenesis inhibitor. This study sought to determine the anti-angiogenic bioactivity of the P18 peptide in hepato-cellular carcinoma (HCC) and to elucidate the underlying mechanism. Xenograft tumour growth assays demonstrated the P18 peptide suppressed angiogenesis of HCC in vivo. Wound healing, Transwell and Matrigel-culture assays indicated that the P18 peptide inhibited the cell migration and tube formation of endothelial cells (ECs) in vitro...
June 14, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28625136/using-%C3%AE-amino-acids-and-%C3%AE-peptide-templates-to-create-bioactive-ligands-and-biomaterials
#11
Mark P Del Borgo, Ketav Kulkarni, Marie-Isabel Aguilar
β-Amino acids are being increasingly used in the design of bioactive ligands and more recently in the generation of novel biomaterials. Peptides containing either individual β-amino acid substitutions or peptides comprised entirely of β-amino acids, display unique properties in terms of their structural and/or chemical characteristics. β-Peptides form well-defined secondary structures that exhibit different geometries compared to the corresponding α-peptides. β-Peptides, including α-peptides containing only one or two β-amino acids, can be easily modified with different functional groups and are metabolically stable and, together with the predictable side chain topography, have led to the design of a growing number of bioactive β-peptides with a range of biological targets and therapeutic applications...
June 15, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28624242/facile-access-to-modified-and-functionalized-pnas-through-ugi-based-solid-phase-oligomerization
#12
Jacques Saarbach, Daniela Masi, Claudio Zambaldo, Nicolas Winssinger
Peptide nucleic acids (PNAs) derivatized with functional molecules are increasingly used in diverse biosupramolecular applications. PNAs have proven to be highly tolerant to modifications and different applications benefit from the use of modified PNAs, in particular modifications at the γ position. Herein we report simple protocols to access modified PNAs from iterative Ugi couplings which allow modular modifications at the α, β or γ position of the PNA backbone from simple starting materials. We demonstrate the utility of the method with the synthesis of several bioactive small molecules (a peptide ligand, a kinase inhibitor and a glycan)-PNA conjugates...
June 14, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28621571/targeted-nanotechnologies-for-cancer-intervention-a-patent-review-2010-2016
#13
Priyamvada Pradeep, Pradeep Kumar, Yahya E Choonara, Viness Pillay
In recent years, several active targeting nanostrategies have been patented for application in cancer theranostics. The versatility of nanostructures in terms of composition, manufacturability, functionalization, and matrix formation make them ideal for carrying large dose of bioactive contents, high density of targeting ligands on their surface, efficient delivery to the site of interest, and capable of forming multicomponent platforms. Areas covered: The patents were classified into polymeric and non-polymeric nanostructures and their applicability in addressing the targeting paradigm related to cancer intervention was explored...
June 22, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28621254/use-of-microcomputed-tomography-to-measure-the-relaxin-induced-expansion-of-intrapubic-ligaments-in-mice
#14
Heather A Zimmerman, Richard P Kennan, Chunlian Zhang, Kashmira Shah, Douglas G Johns, Joseph J Lynch, Maya Dajee
Relaxin is a 6-kDa peptide in the insulin superfamily of hormones. In addition to its effects on reproductive and musculoskeletal ligaments, relaxin has demonstrated beneficial effects on cardiac, renal, and vascular systems in preclinical models. The mouse intrapubic ligament ex vivo bioassay is the current standard for measuring in vivo relaxin bioactivity. However, this bioassay necessitates euthanasia and dissection of large cohorts to measure the intrapubic ligament at specified time points. We hypothesized that μCT imaging could be used to reduce the number of animals necessary for the intrapubic ligament bioassay by enabling a single animal to be followed longitudinally throughout the study rather than euthanizing different cohorts at established time points...
June 15, 2017: Comparative Medicine
https://www.readbyqxmd.com/read/28620922/supraspinal-inhibitory-effects-of-chimeric-peptide-mcrt-on-gastrointestinal-motility-in-mice
#15
Chunbo He, Hailan Li, Jing Zhang, Yanping Kang, Fang Jia, Shouliang Dong, Lanxia Zhou
OBJECTIVES: Chimeric peptide MCRT, based on morphiceptin and PFRTic-NH2 , was a bifunctional ligand of μ- and δ-opioid receptors (MOR-DOR) and produced potent analgesia in tail-withdrawal test. The study focused on the supraspinal effects of morphiceptin, PFRTic-NH2 and MCRT on gastrointestinal motility. Moreover, opioid receptor antagonists, naloxone (non-selective), cyprodime (MOR selective) and naltrindole (DOR selective) were utilized to explore the mechanisms. METHODS: Intracerebroventricular administration was achieved via the implanted cannula...
June 16, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28616359/bioactive-antimicrobial-peptides-as-therapeutics-for-corneal-wounds-and-infections
#16
REVIEW
Gina L Griffith, Anne Kasus-Jacobi, H Anne Pereira
Significance: More than 2 million eye injuries and infections occur each year in the United States that leave civilians and military members with reduced or complete vision loss due to the lack of effective therapeutics. Severe ocular injuries and infections occur in varied settings including the home, workplace, and battlefields. In this review, we discuss the potential of developing antimicrobial peptides (AMPs) as therapeutics for the treatment of corneal wounds and infections for which the current treatment options are inadequate...
June 1, 2017: Advances in Wound Care
https://www.readbyqxmd.com/read/28614788/apelin-modulates-pathological-remodeling-of-lymphatic-endothelium-after-myocardial-infarction
#17
Florence Tatin, Edith Renaud-Gabardos, Anne-Claire Godet, Fransky Hantelys, Francoise Pujol, Florent Morfoisse, Denis Calise, Fanny Viars, Philippe Valet, Bernard Masri, Anne-Catherine Prats, Barbara Garmy-Susini
Lymphatic endothelium serves as a barrier to control fluid balance and immune cell trafficking to maintain tissue homeostasis. Long-term alteration of lymphatic vasculature promotes edema and fibrosis, which is an aggravating factor in the onset of cardiovascular diseases such as myocardial infarction. Apelin is a bioactive peptide that plays a central role in angiogenesis and cardiac contractility. Despite an established role of apelin in lymphangiogenesis, little is known about its function in the cardiac lymphatic endothelium...
June 15, 2017: JCI Insight
https://www.readbyqxmd.com/read/28614698/sardine-procalcitonin-amino-terminal-cleavage-peptide-has-a-different-action-from-calcitonin-and-promotes-osteoblastic-activity-in-the-scales-of-goldfish
#18
Yoichi Kase, Takahiro Ikari, Toshio Sekiguchi, Masayuki Sato, Shouzo Ogiso, Tsuyoshi Kawada, Shin Matsubara, Honoo Satake, Yuichi Sasayama, Masato Endo, Kei-Ichiro Kitamura, Atsuhiko Hattori, Takushi X Watanabe, Yusuke Maruyama, Yoshinari Watanabe, Hisayuki Funahashi, Akira Kambegawa, Nobuo Suzuki
The nucleotide sequence of a sardine preprocalcitonin precursor has been determined from their ultimobranchial glands in the present study. From our analysis of this sequence, we found that sardine procalcitonin was composed of procalcitonin amino-terminal cleavage peptide (N-proCT) (53 amino acids), CT (32 amino acids), and procalcitonin carboxyl-terminal cleavage peptide (C-proCT) (18 amino acids). As compared with C-proCT, N-proCT has been highly conserved among teleosts, reptiles, and birds, which suggests that N-proCT has some bioactivities...
June 11, 2017: Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology
https://www.readbyqxmd.com/read/28611768/innate-immunity-and-breast-milk
#19
REVIEW
Nicole Theresa Cacho, Robert M Lawrence
Human milk is a dynamic source of nutrients and bioactive factors; unique in providing for the human infant's optimal growth and development. The growing infant's immune system has a number of developmental immune deficiencies placing the infant at increased risk of infection. This review focuses on how human milk directly contributes to the infant's innate immunity. Remarkable new findings clarify the multifunctional nature of human milk bioactive components. New research techniques have expanded our understanding of the potential for human milk's effect on the infant that will never be possible with milk formulas...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28609429/reciprocal-evolution-of-opiate-science-from-medical-and-cultural-perspectives
#20
George B Stefano, Nastazja Pilonis, Radek Ptacek, Richard M Kream
Over the course of human history, it has been common to use plants for medicinal purposes, such as for providing relief from particular maladies and self-medication. Opium represents one longstanding remedy that has been used to address a range of medical conditions, alleviating discomfort often in ways that have proven pleasurable. Opium is a combination of compounds obtained from the mature fruit of opium poppy, papaver somniferum. Morphine and its biosynthetic precursors thebaine and codeine constitute the main bioactive opiate alkaloids contained in opium...
June 13, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
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