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Cláudia S F C Popov, Beatriz Simas Magalhães, Brian James Goodfellow, Anamélia Lorenzetti Bocca, David M Pereira, Paula B Andrade, Patrícia Valentão, Pedro José Barbosa Pereira, João Eduardo Rodrigues, Paulo H de Holanda Veloso Júnior, Taia M B Rezende
Inflammation is a natural defense mechanism of the immune system; however, when unregulated, it can lead to chronic illness. Glucocorticoids are the most commonly used agents to effectively treat inflammatory conditions, including autoimmune diseases, however these substances can trigger a number of side effects. Thus, viable alternatives to the use of these drugs would be advantageous. In this study, we have analyzed the anti-inflammatory profile of three synthetic peptides first identified in skin secretion of the tree frog Hypsiboas raniceps...
January 2, 2019: Peptides
Carolina Ayala, Gisela E Pennacchio, Marta Soaje, Jackson C Bittencourt, María E Celis, Graciela Jahn, Susana R Valdez, Alicia M Seltzer
The Neuropeptide EI (NEI, glutamic acid- isoleucine amide) participates in neuroendocrine function. Previously we demonstrated that NEI concentration is regulated by thyroid hormones in discrete hypothalamic areas in rats. We observed that the thyroid status affects the dopaminergic regulation of the pituitary hormones. In this study we explored possible interactions between NEI and tyrosine hydroxylase (TH) containing elements in selected hypothalamic areas of male rats. Neuronal somas, terminals and boutons were assessed by confocal microscopy, in hypo- and hyperthyroid animals...
December 24, 2018: Peptides
Jonathan M Tyrrell, Ali F Aboklaish, Timothy R Walsh, Timo Vaara, Martti Vaara
The antibiotic crisis has reinstated polymyxins, once abandoned because of their toxicity. Now, preclinical studies have revealed better tolerated and more effective derivatives of polymyxins such as NAB739. Simultaneously, polymyxin-resistant (PMR) strains such as the mcr-1 strains have received lots of justified publicity, even though they are still very rare. Here we show that NAB739 sensitizes the PMR strains to rifampin, a classic "anti-Gram-positive" antibiotic excluded by the intact outer membrane (OM) permeability barrier, as well as to retapamulin, the surrogate of lefamulin, an antibiotic under development against Gram-positive bacteria...
December 23, 2018: Peptides
Yuewu Zhao, Yong Li, Zhengzhang Li, Bing Xu, Peng Chen, Xiangjun Yang
The present study was designed to determine how apelin in paraventricular nucleus (PVN) modulates the renal sympathetic nerve activity (RSNA), arterial blood pressure (ABP), mean arterial pressure (MAP), and heart rate (HR), and whether superoxide anions regulate the performance of PVN apelin in spontaneously hypertensive rats (SHRs). Acute experiment was carried out with 13-week-old male Wistar-Kyoto rats (WKY) and SHRs under anaesthesia. RSNA, ABP, MAP and HR after PVN microinjection were measured. Apelin microinjection into PVN increased RSNA, ABP, MAP and HR in WKY rats and SHRs, more obviously in SHRs...
December 21, 2018: Peptides
Reiko Saito, Kentaro Tanaka, Haruki Nishimura, Kazuaki Nishimura, Satomi Sonoda, Hiromichi Ueno, Yasuhito Motojima, Mitsuhiro Yoshimura, Takashi Maruyama, Yukiyo Yamamoto, Koichi Kusuhara, Yoichi Ueta
Kisspeptin (KP), known as a hypothalamic neuropeptide, plays a critical role in the regulation of not only reproduction but also food intake. The anorectic neuropeptides, nesfatin-1 and oxytocin (OXT), are expressed in central nervous system, particulaly in various hypothalamic nuclei, and peripheral tissue. We examined the effects of the intracerebroventricular (icv) administration of KP-10 on feeding and nesfatin-1-immunoreactive (ir) or OXT-ir neurons in the rat hypothalamus, using Fos double immunohistochemistry in male rats...
December 15, 2018: Peptides
Alan R Gintzler, Nai-Jiang Liu, Emiliya M Storman, Martin W Wessendorf
Effective management of chronic pain is demanded by ethical as well as medical considerations. Although opioid analgesics remain among the most effective pharmacotherapies for ameliorating many types of pain, their use is clouded by concerns regarding their addictive properties, underscored by the current epidemic of prescription opioid abuse and attendant deaths. Medicinal harnessing of endogenous opioid antinociception could provide a strategy for continuing to take advantage of the powerful antinociceptive properties of opioids while avoiding their abuse potential...
December 14, 2018: Peptides
Han-Ning Huang, Chi-Mu Chuang, Jyh-Yih Chen, Pan Chieh-Yu
Trichomoniasis is caused by infection with the protozoan parasite Trichomonas vaginalis, and prolonged persistence may lead to serious ill effects in patients. Thus, the development of new therapeutic strategies to combat drug-resistant T. vaginalis would be clinically beneficial. Antimicrobial peptides (AMPs) comprise an emerging class of molecules that may serve as effective alternatives to antibiotics. In this report, we demonstrate that the synthetic fish AMP, Epinecidin-1 (Epi-1), acts against T. vaginalis both in vitro and in vivo...
December 12, 2018: Peptides
Chiara Ruzza, Victor A Holanda, Elaine C Gavioli, Claudio Trapella, Girolamo Calo
Cebranopadol is a mixed NOP/opioid receptor agonist currently under development as innovative analgesic. In this study the liability of cebranopadol to produce opioid-type physical dependence has been evaluated in comparison with morphine in wild type mice and in mice knockout for the NOP receptor gene (NOP(-/-)). Mice were treated twice a day for 5 days with increasing doses of cebranopadol or morphine (cumulative doses 10.2 and 255 mg/kg, respectively) and the number of jumping in response to naloxone 10 mg/kg were measured after 2 h from the last injection...
December 11, 2018: Peptides
Brooke C Matson, Manyu Li, Claire E Trincot, Elizabeth S Blakeney, Stephanie L Pierce, Kathleen M Caron
Adrenomedullin (AM) and proadrenomedullin N-terminal 20 peptide (PAMP) are small peptides derived from a common precursor, pre-proadrenomedullin. Although AM and PAMP share hypotensive effects in the cardiovascular system, the peptides also exert diverse and distinct effects on endocrine physiology, innate immunity, cytoskeletal biology and receptor signaling pathways. Tremendous knowledge has been gleaned from the study of several genetic animal models of AM deletion or overexpression, some of which also simultaneously delete the coding region for PAMP peptide...
December 8, 2018: Peptides
Anneke Kuipers, Gert N Moll, Elizabeth Wagner, Rick Franklin
Native angiotensin-(1-7) exerts many therapeutic effects. However, it is rapidly degraded by ACE and other peptidases. This drawback is largely eliminated for lanthionine-stabilized angiotensin-(1-7), termed cAng-(1-7), which is fully resistant to ACE and has strongly increased resistance to other peptidases. Goal of the present study was to test whether cAng-(1-7) has therapeutic activity in diabetes mouse models: in a multiple low dose streptozotocin-induced model of type I diabetes and / or in a db/db model of type II diabetes...
December 4, 2018: Peptides
Beibing Di, Hong-Wei Li, Weiping Li, Bing Hua
Vascular smooth muscle cell (VSMC) phenotype transition is involved in diabetes-associated cardiovascular diseases. The mechanism of VSMCs phenotypic transition in T2DM was still unclear. Rat coronary artery SMCs were pretreated with liraglutide alone, liraglutide and H89(a PKA inhibitor), neutralizing anti-RAGE antibody or the antioxidant pyrrolidine dithiocarbamate (PDTC; a nuclear factor-κB (NF-κB) inhibitor), followed by treatment with AGE. The morphological change of the SMCs was observed. We also observed the α-actin positive myofilaments and F-actin distribution in SMC through immunofluorescence microscopy...
December 1, 2018: Peptides
Anna I Erdei, Adina Borbély, Anna Magyar, Edina Szűcs, Ferenc Ötvös, Dávid Gombos, Mahmoud Al-Khrasani, Azzurra Stefanucci, Marilisa Pia Dimmito, Grazia Luisi, Adriano Mollica, Sándor Benyhe
The endogenous ligand nociceptin (N/OFQ) and a positively charged synthetic peptide RYYRIK are both selective for the nociceptin opioid receptor (NOPr). Despite their structural dissimilarity, N/OFQ and RYYRIK compete for the same binding site of NOP receptor possessing full and partial agonistic character, respectively. In the view of the message-address concept, hybrid peptide constructs were probed for the NOP receptor combining different regions of N/OFQ and RYYRIK related peptide sequences. Nine novel nociceptin- or Ac-RYYRIK-NH2 peptide variants or hybrid peptides were synthesized and characterized...
December 1, 2018: Peptides
Alexander T May, Molly S Crowe, Bryan A Blakeney, Sunila Mahavadi, Hongxia Wang, John R Grider, Karnam S Murthy
The insulinotropic effects of the incretin hormone, glucagon-like peptide-1 (GLP-1) are mediated via GLP-1 receptors (GLP-1R) present on pancreatic β cells. GLP-1 causes a decrease in the motility of stomach and intestine which involves both central and peripheral nervous systems. The expression and function of GLP-1R in gastrointestinal smooth muscle, however, are not clear. Muscle strips and isolated muscle cells were prepared from mouse colon and the effect of GLP-1(7-36) amide on acetylcholine (ACh)-induced contraction was measured...
November 30, 2018: Peptides
Emil D Bartels, Song Guo, Birgitte S Kousholt, Jens R Larsen, J Michael Hasenkam, John Burnett, Lars B Nielsen, Messoud Ashina, Jens P Goetze
Drugs facilitating the cardioprotective effects of natriuretic peptides are introduced in heart failure treatment. ANP and BNP also stimulate lipolysis and increase circulating concentrations of free fatty acids (FFAs); an aspect, however, thought to be confined to primates. We examined the lipolytic effect of natriuretic peptide infusion in healthy young men and evaluated the effect in a porcine model of myocardial ischemia and reperfusion. Six young healthy normotensive men underwent infusion with ANP, BNP, or CNP for 20 min...
November 30, 2018: Peptides
Cristina Camó, Anna Bonaterra, Esther Badosa, Aina Baró, Laura Montesinos, Emilio Montesinos, Marta Planas, Lidia Feliu
Recent strong restrictions on the use of pesticides has prompted the search for safer alternatives, being antimicrobial peptides promising candidates. Herein, with the aim of identifying new agents, 15 peptides reported as plant defense elicitors, promiscuous, multifunctional or antimicrobial were selected and tested against six plant pathogenic bacteria of economic importance. Within this set, KSL-W (KKVVFWVKFK-NH2 ) displayed high antibacterial activity against all the tested pathogens, low hemolysis and low phytotoxicity in tobacco leaves...
November 30, 2018: Peptides
Fengjing Jia, Yi Zhang, Jiayi Wang, Jinxiu Peng, Ping Zhao, Lishi Zhang, Haiyan Yao, Jingman Ni, Kairong Wang
Antimicrobial peptides (AMPs) are believed to be a promising class of antimicrobial agents against bacteria and fungi. To promote the clinical use of AMPs, their antimicrobial activity and susceptibility to protease degradation should be further improved. The antimicrobial peptide Jelleine-I was originally isolated from the royal jelly of honeybees (Apis mellifera) with a short sequence of PFKLSLHL-NH2 (953.24 Da). Here, a series of halogenated derivatives of the antimicrobial peptide Jelleine-I were designed and synthesized...
November 27, 2018: Peptides
Mysuru Natarajan Savitha, Jalahalli Mariswamy Siddesha, Kanve Nagaraj Suvilesh, Manjunath Yariswamy, Hamse Kameshwar Vivek, Cletus J M D'Souza, Muddegowda Umashankar, Bannikuppe Sannanaik Vishwanath
Hypertension is the fundamental cause of cardiovascular and cerebrovascular disorders. Several natural and synthetic peptides are being used as anti-hypertensive agents, which target angiotensin converting enzyme (ACE), the master regulator of angiotensin (Ang) II production. In this study, we have evaluated ACE-inhibitory potential of the tripeptide L-Phenylalanyl-D-Histidyl-L-Leucine (L-Phe-D-His-L-Leu) in vitro and its antihypertensive effect in rat model of dexamethasone-induced hypertension. L-Phe-D-His-L-Leu was custom-designed by changing the configuration of penultimate amino acid residue (histidine) from C-terminal of Ang I, the site at which ACE acts upon and generates Ang II...
November 24, 2018: Peptides
J Michael Conlon, Karl-Heinz Herzig
No abstract text is available yet for this article.
November 24, 2018: Peptides
Jun Xu, Shuo Chen, Jing Jin, Lingman Ma, Min Guo, Changlin Zhou, Jie Dou
Influenza A virus is a leading cause of mortality in humans and poses a global health emergency due to its newly adapted and resistant strains. Thus, there is an urgency to develop novel anti-influenza drugs. Peptides are a type of biological molecule having a wide range of inhibitory effects against bacteria, fungi, viruses and cancer cells. The prospects of several peptides and their mechanisms of action have received significant attention. BF-30, a 30 amino acid residue peptide isolated from the venom of the snake, Bungarus fasciatus, is reported to have antibacterial and antitumor activities...
November 14, 2018: Peptides
Zsolt Bagosi, Krisztina Csabafi, Gergely Karasz, Miklós Jászberényi, Imre Földesi, Andrea Siska, Gyula Szabó, Gyula Telegdy
The urocortins (Ucn I, Ucn II and Ucn III) are structural analogues of corticotropin-releasing factor (CRF). The aim of our present experiments was to compare the effects of the urocortins on the hypothalamic-pituitary-adrenal (HPA) axis in rats and mice, including the hypothalamic adrenocorticotropic hormone (ACTH) secretagogues, such as CRF and arginine vasopressin (AVP). Therefore, male CFLP mice and male Wistar rats were injected intracerebroventricularly (icv) with 0.5, 1, 2 and 5 μg/2 μl of Ucn I, Ucn II or Ucn III...
November 8, 2018: Peptides
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