scholarly journals Diastereoselective synthesis of new O-alkylated and C-branched inositols and their corresponding fluoro analogues

2016 ◽  
Vol 12 ◽  
pp. 353-361 ◽  
Author(s):  
Charlotte Collet ◽  
Françoise Chrétien ◽  
Yves Chapleur ◽  
Sandrine Lamandé-Langle
Keyword(s):  
Hydroxy Group ◽  
Pet Imaging ◽  
Fluorine Atom ◽  
Biological Properties ◽  
Diastereoselective Synthesis ◽  
Different Types ◽  
Key Steps

Efficient routes were developed for the diastereoselective synthesis of new O-alkylated and C-branched inositols and their corresponding fluoro analogues. The key steps of the synthesis were the easy accessibility of different types of arms in term of configuration (myo and scyllo), the linking method and length, which could modulate the biological properties. These inositol derivatives, bearing an arm terminated either with a hydroxy group or a fluorine atom, could be interesting candidates for diastereoisomeric intermediates and biological evaluations, especially for PET imaging experiments.

NMR Assisted Antimicrobial Peptide Designing: Structure Based Modifications and Functional Correlation of a Designed Peptide VG16KRKP

2020 ◽  
Vol 27 (9) ◽  
pp. 1387-1404 ◽  
Author(s):  
Karishma Biswas ◽  
Humaira Ilyas ◽  
Aritreyee Datta ◽  
Anirban Bhunia
Keyword(s):  
Antimicrobial Agents ◽  
Biological Properties ◽  
Structure Characterization ◽  
Drug Resistant ◽  
Functional Correlation ◽  
Naturally Occurring ◽  
High Resolution Nmr ◽  
Different Types ◽  
Reduced Activity ◽  
Poor Stability

Antimicrobial Peptides (AMPs), within their realm incorporate a diverse group of structurally and functionally varied peptides, playing crucial roles in innate immunity. Over the last few decades, the field of AMP has seen a huge upsurge, mainly owing to the generation of the so-called drug resistant ‘superbugs’ as well as limitations associated with the existing antimicrobial agents. Due to their resilient biological properties, AMPs can very well form the sustainable alternative for nextgeneration therapeutic agents. Certain drawbacks associated with existing AMPs are, however, issues of major concern, circumventing which are imperative. These limitations mainly include proteolytic cleavage and hence poor stability inside the biological systems, reduced activity due to inadequate interaction with the microbial membrane, and ineffectiveness because of inappropriate delivery among others. In this context, the application of naturally occurring AMPs as an efficient prototype for generating various synthetic and designed counterparts has evolved as a new avenue in peptide-based therapy. Such designing approaches help to overcome the drawbacks of the parent AMPs while retaining the inherent activity. In this review, we summarize some of the basic NMR structure based approaches and techniques which aid in improving the activity of AMPs, using the example of a 16-residue dengue virus fusion protein derived peptide, VG16KRKP. Using first principle based designing technique and high resolution NMR-based structure characterization we validate different types of modifications of VG16KRKP, highlighting key motifs, which optimize its activity. The approaches and designing techniques presented can support our peers in their drug development work.

Inorganic Gold and Polymeric Poly(Lactide-co-glycolide) Nanoparticles as Novel Strategies to Ameliorate the Biological Properties of Antimicrobial Peptides

2020 ◽  
Vol 21 (4) ◽  
pp. 429-438 ◽  
Author(s):  
Bruno Casciaro ◽  
Francesca Ghirga ◽  
Deborah Quaglio ◽  
Maria Luisa Mangoni
Keyword(s):  
Antimicrobial Peptides ◽  
Biological Properties ◽  
Biological Profile ◽  
Innovative Strategy ◽  
Different Types ◽  
New Antibiotics ◽  
Interesting Class ◽  
Alternative Antimicrobials ◽  
Nanoparticulate Systems ◽  
Infective Activity

Cationic antimicrobial peptides (AMPs) are an interesting class of gene-encoded molecules endowed with a broad-spectrum of anti-infective activity and immunomodulatory properties. They represent promising candidates for the development of new antibiotics, mainly due to their membraneperturbing mechanism of action that very rarely induces microbial resistance. However, bringing AMPs into the clinical field is hampered by some intrinsic limitations, encompassing low peptide bioavailability at the target site and high peptide susceptibility to proteolytic degradation. In this regard, nanotechnologies represent an innovative strategy to circumvent these issues. According to the literature, a large variety of nanoparticulate systems have been employed for drug-delivery, bioimaging, biosensors or nanoantibiotics. The possibility of conjugating different types of molecules, including AMPs, to these systems, allows the production of nanoformulations able to enhance the biological profile of the compound while reducing its cytotoxicity and prolonging its residence time. In this minireview, inorganic gold nanoparticles (NPs) and biodegradable polymeric NPs made of poly(lactide-coglycolide) are described with particular emphasis on examples of the conjugation of AMPs to them, to highlight the great potential of such nanoformulations as alternative antimicrobials.

scholarly journals Snail mucus from the mantle and foot of two land snails, Lissachatina fulica and Hemiplecta distincta, exhibits different protein profile and biological activity

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Nattaphop Noothuan ◽  
Kantamas Apitanyasai ◽  
Somsak Panha ◽  
Anchalee Tassanakajon
Keyword(s):  
Biological Activities ◽  
Protein Pattern ◽  
Protein Profile ◽  
Antibacterial Properties ◽  
Biological Properties ◽  
Specific Protein ◽  
Land Snails ◽  
Snail Species ◽  
Significant Difference ◽  
Different Types

Abstract Objective Snails secrete different types of mucus that serve several functions, and are increasingly being exploited for medical and cosmetic applications. In this study, we explored the protein pattern and compared the biological properties of the mucus secreted from the mantle collar and foot of two snail species, Lissachatina fulica and Hemiplecta distincta. Result Protein profile showed a different pattern between the two species and between the two secretory parts. The mantle-specific protein bands were further characterized and among them was an antibacterial protein, achacin. Accordingly, the mucus from the mantle exhibited the higher antibacterial activity than that from the foot in both snail species. The mucus from H. distincta, first reported here, also showed antibacterial properties, but with a lower activity compared to that for L. fulica. Snail mucus also exhibited anti-tyrosinase activity and antioxidant activity but with no significant difference between the foot and mantle mucus. These results indicate some different protein compositions and biological activities of snail slime from the mantle and foot, which might be associated with their specific functions in the animal and are useful for medical applications.

scholarly journals Cytotoxic Agents in the Minor Alkaloid Groups of the Amaryllidaceae

Planta Medica ◽  
2021 ◽  
Author(s):  
Jerald J. Nair ◽  
Johannes van Staden
Keyword(s):  
Cancer Cells ◽  
Cancer Cell Line ◽  
Structural Features ◽  
Biological Properties ◽  
Cytotoxic Agents ◽  
Plant Family ◽  
Structure Activity ◽  
Significant Interest ◽  
Different Types ◽  
Minor Alkaloid

AbstractOver 600 alkaloids have to date been identified in the plant family Amaryllidaceae. These have been arranged into as many as 15 different groups based on their characteristic structural features. The vast majority of studies on the biological properties of Amaryllidaceae alkaloids have probed their anticancer potential. While most efforts have focused on the major alkaloid groups, the volume and diversity afforded by the minor alkaloid groups have promoted their usefulness as targets for cancer cell line screening purposes. This survey is an in-depth review of such activities described for around 90 representatives from 10 minor alkaloid groups of the Amaryllidaceae. These have been evaluated against over 60 cell lines categorized into 18 different types of cancer. The montanine and cripowellin groups were identified as the most potent, with some in the latter demonstrating low nanomolar level antiproliferative activities. Despite their challenging molecular architectures, the minor alkaloid groups have allowed for facile adjustments to be made to their structures, thereby altering the size, geometry, and electronics of the targets available for structure-activity relationship studies. Nevertheless, it was seen with a regular frequency that the parent alkaloids were better cytotoxic agents than the corresponding semisynthetic derivatives. There has also been significant interest in how the minor alkaloid groups manifest their effects in cancer cells. Among the various targets and pathways in which they were seen to mediate, their ability to induce apoptosis in cancer cells is most appealing.

scholarly journals Delivery of cancer therapies by synthetic and bio-inspired nanovectors

2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Tina Briolay ◽  
Tacien Petithomme ◽  
Morgane Fouet ◽  
Nelly Nguyen-Pham ◽  
Christophe Blanquart ◽  
...  
Keyword(s):  
Recent Literature ◽  
Biological Properties ◽  
Engineered Nanoparticles ◽  
Oncolytic Viruses ◽  
Cancer Therapies ◽  
Different Types ◽  
Therapeutic Molecules ◽  
Tumor Specificity ◽  
Smart Drug ◽  
Smart Drug Delivery

Abstract Background As a complement to the clinical development of new anticancer molecules, innovations in therapeutic vectorization aim at solving issues related to tumor specificity and associated toxicities. Nanomedicine is a rapidly evolving field that offers various solutions to increase clinical efficacy and safety. Main Here are presented the recent advances for different types of nanovectors of chemical and biological nature, to identify the best suited for translational research projects. These nanovectors include different types of chemically engineered nanoparticles that now come in many different flavors of ‘smart’ drug delivery systems. Alternatives with enhanced biocompatibility and a better adaptability to new types of therapeutic molecules are the cell-derived extracellular vesicles and micro-organism-derived oncolytic viruses, virus-like particles and bacterial minicells. In the first part of the review, we describe their main physical, chemical and biological properties and their potential for personalized modifications. The second part focuses on presenting the recent literature on the use of the different families of nanovectors to deliver anticancer molecules for chemotherapy, radiotherapy, nucleic acid-based therapy, modulation of the tumor microenvironment and immunotherapy. Conclusion This review will help the readers to better appreciate the complexity of available nanovectors and to identify the most fitting “type” for efficient and specific delivery of diverse anticancer therapies.

Role of the C(6)-Hydroxy Group in Bicyclomycin:  Synthesis, Structure, and Chemical, Biochemical, and Biological Properties

1998 ◽  
Vol 41 (7) ◽  
pp. 1185-1194 ◽  
Author(s):  
Alejandro Santillán, ◽  
Xiangdong Zhang ◽  
Jon Hardesty ◽  
William R. Widger ◽  
Kohn
Keyword(s):  
Hydroxy Group ◽  
Biological Properties

scholarly journals Honey dressing on a leg ulcer with tendon exposure in a patient with type 2 diabetes

2018 ◽  
Vol 2018 ◽  
Author(s):  
Ilaria Teobaldi ◽  
Vincenzo Stoico ◽  
Fabrizia Perrone ◽  
Massimiliano Bruti ◽  
Enzo Bonora ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Clinical Practice ◽  
Wound Dressing ◽  
Biological Properties ◽  
Healing Time ◽  
Foot Ulcers ◽  
Diabetic Foot Ulcers ◽  
Scientific Interest ◽  
Different Types

Summary Honey has been used as a wound dressing for hundreds of years by ancient civilizations, but only recently it has acquired scientific interest because of its relevant biological properties. In the last decade, indeed, several trials and observational studies have reported that, compared to conventional treatment (e.g. antiseptics, polyurethane film, paraffin gauze, soframycin-impregnated gauze), honey dressings seem to be better in healing time of different types of wounds, including diabetic foot ulcers. However, to date, information about a potential favorable biological effect of honey dressings on diabetic ulcers with exposed tendon are still scarce. Notably, foot or leg ulcers with exposed tendon are serious complications in patients with type 2 diabetes, as they are associated with an increased risk of adverse outcome. Therefore, the use of effective and safe treatments to bring these lesions to timely healing is very important in clinical practice. We herein report the case of a Caucasian adult patient with type 2 diabetes presenting a chronic right posterior lower limb ulcer (Texas University Classification (TUC) 2D) with tendon exposure that was successfully treated with honey dressings (glucose oxidase (GOX) positive with peroxide activity) in addition to systemic antibiotic therapy, surgical toilette and skin graft. In our case, the use of honey dressing for treating exposed tendon tissue probably allowed the timely wound healing. Although further studies are required, such treatment may constitute part of the comprehensive management of diabetic wounds, including those with tendon exposure, and should be considered by clinicians in clinical practice. Learning points: Honey has been used as a wound dressing for hundreds of years, but only recently it has acquired scientific interest for its biological properties. Several studies have documented that, compared to conventional dressings, honey seems to be better in healing time of different types of wounds, including diabetic foot ulcers. Our case report is the first to highlight the importance to use honey dressings also for the treatment of ulcers with tendon exposure in patients with type 2 diabetes, suggesting that this kind of dressing should be considered by clinicians in clinical practice.

scholarly journals Oxidized Cell-Free DNA Is a Factor of Stress Signaling in Radiation-Induced Bystander Effects in Different Types of Human Cells

2019 ◽  
Vol 2019 ◽  
pp. 1-7 ◽  
Author(s):  
Marina S. Konkova ◽  
Andrew A. Kaliyanov ◽  
Vasilina A. Sergeeva ◽  
Margarita S. Abramova ◽  
Svetlana V. Kostyuk
Keyword(s):  
Low Dose ◽  
Bystander Effect ◽  
Biological Properties ◽  
Stress Signaling ◽  
Cell Free Dna ◽  
Free Dna ◽  
Cytokine Levels ◽  
Different Types ◽  
Radiation Induced

In pathology or under damaging conditions, the properties of cell-free DNA (cfDNA) change. An example of such change is GC enrichment, which drastically alters the biological properties of cfDNA. GC-rich cfDNA is a factor of stress signaling, whereas genomic cfDNA is biologically inactive. GC-rich cfDNA stimulates TLR9-MyD88-NF-κB signaling cascade, leading to an increase in proinflammatory cytokine levels in the organism. In addition, GC-rich DNA is prone to oxidation and oxidized cfDNA can stimulate secondary oxidative stress. This article is a review of works dedicated to the investigation of a low-dose ionizing radiation effect, a bystander effect, and the role of cfDNA in both of these processes.

scholarly journals Cancer Nano-Immunotherapy from the Injection to the Target: The Role of Protein Corona

2020 ◽  
Vol 21 (2) ◽  
pp. 519
Author(s):  
Idoia Mikelez-Alonso ◽  
Antonio Aires ◽  
Aitziber L. Cortajarena
Keyword(s):  
Protein Corona ◽  
Biological Properties ◽  
Immune Reactivity ◽  
Target Tissue ◽  
Physiological Conditions ◽  
Different Types ◽  
Cancer Remission ◽  
New Strategies

Immunotherapy has become a promising cancer therapy, improving the prognosis of patients with many different types of cancer and offering the possibility for long-term cancer remission. Nevertheless, some patients do not respond to these treatments and immunotherapy has shown some limitations, such as immune system resistance or limited bioavailability of the drug. Therefore, new strategies that include the use of nanoparticles (NPs) are emerging to enhance the efficacy of immunotherapies. NPs present very different pharmacokinetic and pharmacodynamic properties compared with free drugs and enable the use of lower doses of immune-stimulating molecules, minimizing their side effects. However, NPs face issues concerning stability in physiological conditions, protein corona (PC) formation, and accumulation in the target tissue. PC formation changes the physicochemical and biological properties of the NPs and in consequence their therapeutic effect. This review summarizes the recent advances in the study of the effects of PC formation in NP-based immunotherapy. PC formation has complex effects on immunotherapy since it can diminish (“immune blinding”) or enhance the immune response in an uncontrolled manner (“immune reactivity”). Here, future perspectives of the field including the latest advances towards the use of personalized protein corona in cancer immunotherapy are also discussed.

Total Synthesis of Bis-anthraquinone Antibiotic BE-43472B

Synthesis ◽  
2018 ◽  
Vol 50 (13) ◽  
pp. 2490-2515 ◽  
Author(s):  
Yu Yamashita ◽  
Yoichi Hirano ◽  
Akiomi Takada ◽  
Hiroshi Takikawa ◽  
Keisuke Suzuki
Keyword(s):  
Total Synthesis ◽  
Hydroxy Group ◽  
Three Dimensional ◽  
Crystal Structure Analysis ◽  
Aryl Group ◽  
Full Account ◽  
Ring Fusion ◽  
Enantiomerically Pure ◽  
Pinacol Rearrangement ◽  
Key Steps

This is a full account of our synthetic endeavor on the total synthesis of bis-anthraquinone antibiotic BE-43472B, an unusual octacyclic aromatic polyketide with a bis-anthraquinone scaffold. Three key steps enabled a facile access to the anthraquinone unit corresponding to the ABCF rings; (1) cyclo-condensation or -addition of benzonitrile oxides with cyclic enone derivatives, (2) benzoin cyclization for the stereoselective ring fusion with an angular hydroxy group, and (3) pinacol rearrangement for stereoselective installation of the angular aryl group. Other keys for the success include, (4) diastereoselective methylation of a lactol derivative, and (5) late-stage installation of the C3 hydroxy group through stereoselective oxirane ring formation via halohydrin derivatives. Whereas oxidation of the double bond in the enone with an adjacent 1,3-diketone moiety failed, the projected oxidation was achieved with the alkene keeping the isoxazole moiety intact as a 1,3-diketone equivalent. In the racemic total synthesis, X-ray crystal structure analysis of the target was achieved, proving the three-dimensional architecture for the first time. The asymmetric total synthesis was also achieved by exploiting a cycloadduct of the nitrile oxide and the enantiomerically pure cyclohexenone, which was convertible to the common intermediate via dehydrogenation followed by alkoxycarbonylation.

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