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Immunostimulating compound

Ahmad S Altiti, Xiaojing Ma, Lixing Zhang, Yi Ban, Richard W Franck, David R Mootoo
The identification of immunoactive agents for clinical and mechanistic applications is a very active area of research. In this vein, analogues of the potent immunostimulant KRN 7000 with diverse cytokine profiles have attracted considerable attention. These compounds have been shown to activate iNKT cells via presentation by CD1d. Herein, we report on the synthesis and activity for four new C-glycosides of KRN 7000, 11-phenylundecanoyl and 11-p-fluorophenylundecanoyl derivatives of C-KRN 7000, 2,3-bis-epi-C-KRN 7000 and the reverse amide of C-KRN 7000...
March 6, 2017: Carbohydrate Research
Alberto Finamore, Maura Palmery, Sarra Bensehaila, Ilaria Peluso
The highly nutritional and ecofriendly Spirulina (Arthrospira platensis) has hypolipidemic, hypoglycemic, and antihypertensive properties. Spirulina contains functional compounds, such as phenolics, phycocyanins, and polysaccharides, with antioxidant, anti-inflammatory, and immunostimulating effects. Studies conducted on Spirulina suggest that it is safe in healthy subjects, but attitude to eating probably affects the acceptability of Spirulina containing foods. Although the antioxidant effect of Spirulina is confirmed by the intervention studies, the concerted modulation of antioxidant and inflammatory responses, suggested by in vitro and animal studies, requires more confirmation in humans...
2017: Oxidative Medicine and Cellular Longevity
Nadin Schultze, Heike Wanka, Paula Zwicker, Ulrike Lindequist, Beate Haertel
The immune system is an important target of various xenobiotics, which may lead to severe adverse effects including immunosuppression or inappropriate immunostimulation. Mitochondrial toxicity is one possibility by which xenobiotics exert their toxic effects in cells or organs. In this study, we investigated the impact of three natural compounds, cyclosporine A (CsA), deoxynivalenol (DON) and cannabidiol (CBD) on mitochondrial functions in the THP-1 monocytic cell line. The cells were exposed for 24h to two different concentrations (IC10 and IC50 determined by MTT) of each compound...
December 21, 2016: Toxicology
Stéphanie Sutter, France Thevenieau, Anne Bourdillon, Joëlle De Coninck
Water extracts from solid-state fermentation (SSF) on rapeseed meal using filamentous fungi exhibit interesting immunomodulatory activities in vitro. Immunomodulation was determined by the capacity of the compounds to activate blood neutrophils and to influence cytokine production in human peripheral blood mononuclear cells (PBMC) and mouse bone marrow-derived macrophages (BMDM). Among the strains tested, Aspergillus sojae mycelium and SSF extracts were the most promising in terms of enhancing the immune response...
December 16, 2016: Applied Biochemistry and Biotechnology
Mohammad Islamuddin, Garima Chouhan, Muzamil Yaqub Want, Hani A Ozbak, Hassan A Hemeg, Farhat Afrin
BACKGROUND: The therapy of visceral leishmaniasis (VL) is limited by resistance, toxicity and decreased bioavailability of the existing drugs coupled with dramatic increase in HIV-co-infection, non-availability of vaccines and down regulation of cell-mediated immunity (CMI). Thus, we envisaged combating the problem with plant-derived antileishmanial drug that could concomitantly mitigate the immune suppression of the infected hosts. Several plant-derived compounds have been found to exert leishmanicidal activity via immunomodulation...
October 2016: PLoS Neglected Tropical Diseases
Mariangela Marrelli, Filomena Conforti, Fabrizio Araniti, Giancarlo A Statti
Obesity is one of the greatest public health problems. This complex condition has reached epidemic proportions in many parts of the world, and it constitutes a risk factor for several chronic disorders, such as hypertension, cardiovascular diseases and type 2 diabetes. In the last few decades, several studies dealt with the potential effects of natural products as new safe and effective tools for body weight control. Saponins are naturally-occurring surface-active glycosides, mainly produced by plants, whose structure consists of a sugar moiety linked to a hydrophobic aglycone (a steroid or a triterpene)...
October 20, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Seyed Hossein Hoseinifar, Fazel Zoheiri, Carlo C Lazado
Immunostimulation through the use of sustainable and eco-friendly dietary additives is one of the current prophylactic strategies in fish husbandry. Plant-based immunostimulants are highly considered for this intent, both for their scientific and practical advantages. Persian hogweed (Heracleum persicum) is a flower-bearing herb that possesses interesting pharmacological importance due to its bioactive compounds. It is commonly used as spice, food additive, dietary supplement and traditional remedy. The present study evaluated the potential of H...
December 2016: Fish & Shellfish Immunology
Shoji Takenaka, Masataka Oda, Hisanori Domon, Tatsuya Ohsumi, Yuki Suzuki, Hayato Ohshima, Hirofumi Yamamoto, Yutaka Terao, Yuichiro Noiri
An ideal antibiofilm strategy is to control both in the quality and quantity of biofilm while maintaining the benefits derived from resident microflora. Vizantin, a recently developed immunostimulating compound, has also been found to have antibiofilm property. This study evaluated the influence on biofilm formation of Streptococcus mutans in the presence of sulfated vizantin and biofilm development following bacterial adhesion on a hydroxyapatite disc coated with sulfated vizantin. Supplementation with sulfated vizantin up to 50 μM did not affect either bacterial growth or biofilm formation, whereas 50 μM sulfated vizantin caused the biofilm to readily detach from the surface...
October 11, 2016: Biochemical and Biophysical Research Communications
Paula Zwicker, Nadin Schultze, Sarah Niehs, Karen Methling, Martina Wurster, Dirk Albrecht, Jörg Bernhardt, Gerhild Wachlin, Michael Lalk, Ulrike Lindequist, Beate Haertel
The immune system is permanently exposed to several environmental influences that can have adverse effects on immune cells or organs leading to immunosuppression or inappropriate immunostimulation, called direct immunotoxicity. The natural compound Tulipalin A (TUPA), a lactone with α-methylene-γ-butyrolactone moiety, can influence the immune system and lead to allergic contact dermatitis. This in vitro study focused on effects of TUPA using two immune cell lines (Jurkat T cells and THP-1 monocytes). To evaluate the immunotoxic potential of the compound, a proteomic approach applying 2D gel electrophoresis and MALDI-TOF/TOF-MS in combination with metabolomic analysis was used after exposure of the cells to IC10 of TUPA...
December 2016: Proteomics
Priyatharsini Rajendran, Parasuraman Aiya Subramani, Dinakaran Michael
Immunostimulation by plant-derived compounds presents a fascinating alternative to vaccines and antibiotics in aquaculture. Fish farmers are longing for immunostimulants that activate both specific and nonspecific immune responses of fish and protect fishes from all possible infections. In this study, we observed that polysaccharide fraction from marine macroalga, Padina gymnospora stimulated the immune response of common carp Cyprinus carpio (Filed for patent, Indian patent no. 201641027311 dated:10-Aug-2016)...
November 2016: Fish & Shellfish Immunology
Stephanie M Roto, Young Min Kwon, Steven C Ricke
As the current poultry production system stands, there is a period of time when newly hatched chicks are prevented from access to feed for approximately 48-72 h. Research has indicated that this delay in feeding may result in decreased growth performance when compared to chicks that are fed immediately post-hatch. To remedy this issue, in ovo methodology may be applied in order to supply the embryo with additional nutrients prior to hatching and those nutrients will continue to be utilized by the chick post-hatch during the fasting period...
2016: Frontiers in Veterinary Science
Kawthar Ae Diab
BACKGROUND: In recent years, there has been considerable research on recycling of agroindustrial waste for production of bioactive compounds. The food processing industry produces large amounts of citrus peels that may be an inexpensive source of useful agents. OBJECTIVE: The present work aimed to explore the phytochemical content, antioxidant, anticancer, antiproliferation, and antigenotxic activities of lemon, grapefruit, and mandarin peels. MATERIALS AND METHODS: Peels were extracted using 98% ethanol and the three crude extracts were assessed for their total polyphenol content (TPC), total flavonoid content (TFC), and antioxidant activity using DPPH (1, 1diphenyl2picrylhydrazyl)...
2016: Asian Pacific Journal of Cancer Prevention: APJCP
Codruta Soica, Dorina Coricovac, Cristina Dehelean, Iulia Pinzaru, Marius Mioc, Corina Danciu, Adriana Fulias, Maria Puiu, Cassian Sitaru
BACKGROUND: Immune system related pathologies affect an increasing number of patients every year, having potentially lethal consequences and requiring expensive and difficult tolerated treatments. This area of pathologies offers an excellent potential for the development of innovative solutions such as nanoformulations; this review aims to describe the main categories of nanostructured drug delivery platforms that have been developed in order to achieve a more effective, low toxic treatment in autoimmune pathologies...
2016: Recent Patents on Nanotechnology
Fanny Matheis, Markus V Heppt, Saskia A Graf, Peter Düwell, Claudia Kammerbauer, Achim Aigner, Robert Besch, Carola Berking
Significant advancements of mutation-based targeted therapy and immune checkpoint blockade have been achieved in melanoma. Nevertheless, acquired resistance and nonresponders to therapy require different strategies. An innovative approach is presented here that is based on the combination of innate immune system activation and simultaneous targeting of the oncogene urokinase-type plasminogen activator receptor (uPAR). We generated two triphosphate-conjugated siRNAs targeting uPAR (ppp-uPAR) by in vitro transcription...
August 3, 2016: Journal of Investigative Dermatology
Jose A Reales-Calderón, Gloria Molero, Concha Gil, José L Martínez
The risks for toxicity of novel antifungal compounds, together with the emergence of resistance, makes the use of inhibitors of resistance, in combination with antifungal compounds, a suitable strategy for developing novel antifungal formulations. Among them, inhibitors of efflux pumps are suitable candidates. Increasing drug influx or interfering with the stress response may also improve the efficacy of antifungals. Therapies as induction of fungal apoptosis or immunostimulation are also good strategies for reducing the risks for resistance and to improve antifungals' efficacy...
August 2016: Future Medicinal Chemistry
Tabasum Ismail, Syed Shafi, Swarn Singh, Tabasum Sidiq, Anamika Khajuria, Abdul Rouf, Mahipal Yadav, Varma Saikam, Parvinder Pal Singh, Mohammad Sarwar Alam, Nasarul Islam, Kalicharan Sharma, Halmuthur Mahabalarao Sampath Kumar
A novel series (13) of isoxazoline functionalized coumarins was synthesized through 1,3-dipolar cyclization of nitrile oxides with Allylated coumarins. Synthesis of effective and target selective immunostimulators through conjugation of diversely substituted isoxazolines and 7-hydroxycoumarins is the focus of the present article. The proposed synthetic scheme was observed to be highly regiospecific yielding attempted conjugates in good yield (>90%). Kinetic resolution of the racemates was carried out by employing lipase B from Candida antarctica (CALB)...
November 10, 2016: European Journal of Medicinal Chemistry
Grace Anne A Dória, Paula P Menezes, Bruno S Lima, Bruno S Vasconcelos, Francilene A Silva, Raíssa M Henriques, Marcélia G D Melo, Ângela V F Alves, Manoel O Moraes, Cláudia Ó Pessoa, Adriana A Carvalho, Ana Paula N Prata, Ricardo Luiz C A Junior, Isabel B Lima-Verde, Lucindo J Quintans-Júnior, Daniel P Bezerra, Paulo C L Nogueira, Adriano A S Araujo
BACKGROUND: Remirea maritima has been widely used in the treatment of diarrhea, kidney disease, and high fever and for therapeutic purposes, such as an analgesic and anti-inflammatory. However, few scientific research studies on its medicinal properties have been reported. PURPOSE: The present study aimed to investigate the anticancer potential of aqueous extract (AE), 40% hydroalcoholic extracts (40HA) and 70% (70HA) from R. maritima in experimental models and to identify its phytochemical compounds...
August 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Birte Martin-Bertelsen, Karen S Korsholm, Carla B Roces, Maja H Nielsen, Dennis Christensen, Henrik Franzyk, Anan Yaghmur, Camilla Foged
The mycobacterial cell-wall lipid monomycoloyl glycerol (MMG) is a potent immunostimulator, and cationic liposomes composed of a shorter synthetic analogue (MMG-1) and dimethyldioctadecylammonium (DDA) bromide represent a promising adjuvant that induces strong antigen-specific Th1 and Th17 responses. In the present study, we investigated the supramolecular structure and in vivo adjuvant activity of dispersions based on binary mixtures of DDA and an array of synthetic MMG-1 analogues (MMG-2/3/5/6) displaying longer (MMG-2) or shorter (MMG-3) alkyl chain lengths, or variations in stereochemistry of the polar headgroup (MMG-5) or of the hydrophobic moiety (MMG-6)...
August 1, 2016: Molecular Pharmaceutics
Sirio Fiorino, Elisabetta Loggi, Gabriella Verucchi, Donatella Comparcola, Ranka Vukotic, Michele Pavoni, Elena Grandini, Carmela Cursaro, Silvia Maselli, Maria L Bacchi Reggiani, Cristina Puggioli, Lorenzo Badia, Silvia Galli, Pierluigi Viale, Mauro Bernardi, Pietro Andreone
BACKGROUND & AIMS: The treatment of chronic hepatitis B infection (CHB) in children is still an area of great uncertainty. Vitamin E is an immunostimulating/antioxidant compound proven to be safe and effective for the treatment of adult CHB. The aim of this phase 2 controlled study was to evaluate the safety and efficacy of vitamin E for the treatment of paediatric HBeAg-positive CHB. METHODS: Forty-six children were randomized in a 1:1 ratio to receive vitamin E at a dose of 15 mg/kg/day (in galenic preparation) or no treatment for 12 months and were monitored for the subsequent 12 months...
January 2017: Liver International: Official Journal of the International Association for the Study of the Liver
Janet Gould, Courtney M Callis, David G Dolan, Brad Stanard, Patricia A Weideman
Recently, a guideline has been published by the European Medicines Agency (EMA) on setting safe limits, permitted daily exposures (PDE) [also called acceptable daily exposures (ADE)], for medicines manufactured in multi-product facilities. The ADE provides a safe exposure limit for inadvertent exposure of a drug due to cross-contamination in manufacturing. The ADE determination encompasses a standard risk assessment, requiring an understanding of the toxicological and pharmacological effects, the mechanism of action, drug compound class, and the dose-response as well as the pharmacokinetic properties of the compound...
August 2016: Regulatory Toxicology and Pharmacology: RTP
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