scholarly journals Novel CBG Derivatives Can Reduce Inflammation, Pain and Obesity

Molecules ◽  
2021 ◽  
Vol 26 (18) ◽  
pp. 5601
Author(s):  
Natalya M. Kogan ◽  
Yarden Lavi ◽  
Louise M. Topping ◽  
Richard. O. Williams ◽  
Fiona E. McCann ◽  
...  
Keyword(s):  
High Fat Diet ◽  
Unmet Need ◽  
Drug Candidates ◽  
The Past ◽  
Inflammatory Conditions ◽  
Therapeutic Benefits ◽  
Obesity In Mice ◽  
Anti Inflammatory ◽  
Novel Drug ◽  
Better Than

Interest in CBG (cannabigerol) has been growing in the past few years, due to its anti-inflammatory properties and other therapeutic benefits. Here we report the synthesis of three new CBG derivatives (HUM-223, HUM-233 and HUM-234) and show them to possess anti-inflammatory and analgesic properties. In addition, unlike CBG, HUM-234 also prevents obesity in mice fed a high-fat diet (HFD). The metabolic state of the treated mice on HFD is significantly better than that of vehicle-treated mice, and their liver slices show significantly less steatosis than untreated HFD or CBG-treated ones from HFD mice. We believe that HUM-223, HUM-233 and HUM-234 have the potential for development as novel drug candidates for the treatment of inflammatory conditions, and in the case of HUM-234, potentially for obesity where there is a huge unmet need.

scholarly journals Harnessing the medicinal properties of Cussonia barteri Seem. (Araliaceae) in drug development. A review

2018 ◽  
Vol 64 (3) ◽  
pp. 50-61 ◽  
Author(s):  
Ighodaro Igbe ◽  
Osaze Edosuyi ◽  
Agbonlahor Okhuarobo
Keyword(s):  
Drug Development ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Stem Bark ◽  
Deciduous Tree ◽  
Drug Candidates ◽  
Medicinal Properties ◽  
Phytochemical Constituents ◽  
Anti Inflammatory ◽  
Novel Drug

Summary Cussonia barteri Seem (Araliaceae) is a deciduous tree growing in savannah of Africa. Ethnomedicinally, it is used in Africa as an analgesic, anti-malarial, anti-inflammatory, anti-anaemic, anti-diarhoea, anti-poison, ani-pyschotic and anti-epileptic agent. This review provides a brief summary on the phytochemical screenings, ethnomedicinal and pharmacological applications of various parts of C. barteri. Leaves, stem bark and seed of C. barteri have been shown to be rich in saponins, flavonoids, phenols, sugars and alkaloids. Some of these constituents have been isolated and elucidated from C. barteri. Several compounds isolated from plant include triterpenes, saponins, polyenyne and quinic esters. Phytochemical constituents are also partly responsible for biological activities of C. barteri. Extracts and components isolated from the plant have demonstrated neuropharmacological, anti-larvicidal, anti-microbial, anti-inflammatory and antioxidant activities. Overall, the insights provided by this review reinforce the potential of C. barteri for drug development and create the need for further scientific probe of constituents of the plant with the aim of developing novel drug candidates.

scholarly journals Anti-Inflammatory Properties of Dendrimersper se

2011 ◽  
Vol 11 ◽  
pp. 1367-1382 ◽  
Author(s):  
Myriam Hayder ◽  
Séverine Fruchon ◽  
Jean-Jacques Fournié ◽  
Mary Poupot ◽  
Rémy Poupot
Keyword(s):  
Molecular Weight ◽  
Linear Polymers ◽  
Inflammatory Disorders ◽  
Drug Candidates ◽  
The Past ◽  
Anti Inflammatory

Dendrimers are polybranched and polyfunctionalized tree-like polymers. Unlike linear polymers, they have perfectly defined structure and molecular weight, due to their iterative step-by-step synthesis. Their multivalent structure and supramolecular properties have made them attractive nanotools for applications, particularly in biology and medicine. Among the different biological and medical properties of dendrimers that have been developed over the past decades, the anti-inflammatory properties of several groups of dendrimers are the most recently discovered. Thereof, dendrimers emerge as promising, although heretical, drug candidates for the treatment of still-uncured chronic inflammatory disorders. This mini-review is based on the five main scientific articles giving an overview of what can be the spectrum of anti-inflammatory characteristics displayed by dendrimers.

scholarly journals Comparative Study of the Antioxidant and Anti-Inflammatory Effects of Leaf Extracts from Four Different Morus alba Genotypes in High Fat Diet-Induced Obesity in Mice

Antioxidants ◽  
2020 ◽  
Vol 9 (8) ◽  
pp. 733
Author(s):  
Francisco Javier Leyva-Jiménez ◽  
Antonio Jesús Ruiz-Malagón ◽  
José Alberto Molina-Tijeras ◽  
Patricia Diez-Echave ◽  
Teresa Vezza ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Electrospray Ionization ◽  
High Fat Diet ◽  
High Fat ◽  
Ionization Time ◽  
Flight Mass Spectrometry ◽  
Diet Induced Obesity ◽  
Obesity In Mice ◽  
Anti Inflammatory ◽  
Tof Ms

Increased levels of reactive oxygen species (ROS) and a low-grade chronic inflammation in multiple organs have been demonstrated in obesity. Morus alba leaves extracts (MAEs) have been used in traditional medicine as anti-inflammatory agents. In this work, the bioactive compounds of different genotypes of M. alba L. (Filipina, Valenciana Temprana, Kokuso, and Italia) were analyzed not only by reverse phase high performance liquid chromatography–electrospray ionization-time of flight-mass spectrometry (RP-HPLC-ESI-TOF-MS) and hydrophilic interaction chromatography–electrospray ionization-time of flight-mass spectrometry (HILIC-ESI-TOF-MS), but also screened for in vitro and in vivo antioxidant activity by means of DPPH• radical scavenging assay and Caenorhabditis elegans model. These MAEs were administered daily in a model of diet-induced obesity in mice. Filipina and Italia genotypes significantly reduced weight gain, the glycemic levels in high fat diet, as well as, levels of LDL-cholesterol and triglycerides. Filipina and Italia MAEs also reduced the expression of proinflammatory mediators such as Tnf-α, Il-1β, Il-6 and increased the levels of adiponectin and AMPK, which exert anti-inflammatory effects. Moreover, Italia genotype ameliorated the intestinal barrier function. In conclusion, Filipina and Italia methanolic extracts show the highest antioxidant and anti-inflammatory effect, due to the presence of compounds such as protocatechuic acid or quercetin-3-glucoside, and they could be developed as a complementary treatment for obesity and metabolic disorders.

scholarly journals Promising Drug Candidates and New Strategies for Fighting against the Emerging Superbug Candida auris

2021 ◽  
Vol 9 (3) ◽  
pp. 634
Author(s):  
Muriel Billamboz ◽  
Zeeshan Fatima ◽  
Saif Hameed ◽  
Samir Jawhara
Keyword(s):  
Paradigm Shift ◽  
Fungal Infections ◽  
Point Of View ◽  
Candida Auris ◽  
Drug Candidates ◽  
Genomic Epidemiology ◽  
The Past ◽  
Physicochemical Descriptors ◽  
Novel Drug ◽  
New Strategies

Invasive fungal infections represent an expanding threat to public health. During the past decade, a paradigm shift of candidiasis from Candida albicans to non-albicans Candida species has fundamentally increased with the advent of Candida auris. C. auris was identified in 2009 and is now recognized as an emerging species of concern and underscores the urgent need for novel drug development strategies. In this review, we discuss the genomic epidemiology and the main virulence factors of C. auris. We also focus on the different new strategies and results obtained during the past decade in the field of antifungal design against this emerging C. auris pathogen yeast, based on a medicinal chemist point of view. Critical analyses of chemical features and physicochemical descriptors will be carried out along with the description of reported strategies.

scholarly journals Glucocorticoid Resistance: Interference between the Glucocorticoid Receptor and the MAPK Signalling Pathways

2021 ◽  
Vol 22 (18) ◽  
pp. 10049
Author(s):  
Lisa M. Sevilla ◽  
Alba Jiménez-Panizo ◽  
Andrea Alegre-Martí ◽  
Eva Estébanez-Perpiñá ◽  
Carme Caelles ◽  
...  
Keyword(s):  
Adverse Effects ◽  
Therapeutic Potential ◽  
Inflammatory Diseases ◽  
Cell Types ◽  
Inflammatory Conditions ◽  
Therapeutic Benefits ◽  
Therapeutic Outcomes ◽  
Mapk Signalling ◽  
Mitogen Activated Protein ◽  
Anti Inflammatory

Endogenous glucocorticoids (GCs) are steroid hormones that signal in virtually all cell types to modulate tissue homeostasis throughout life. Also, synthetic GC derivatives (pharmacological GCs) constitute the first-line treatment in many chronic inflammatory conditions with unquestionable therapeutic benefits despite the associated adverse effects. GC actions are principally mediated through the GC receptor (GR), a ligand-dependent transcription factor. Despite the ubiquitous expression of GR, imbalances in GC signalling affect tissues differently, and with variable degrees of severity through mechanisms that are not completely deciphered. Congenital or acquired GC hypersensitivity or resistance syndromes can impact responsiveness to endogenous or pharmacological GCs, causing disease or inadequate therapeutic outcomes, respectively. Acquired GC resistance is defined as loss of efficacy or desensitization over time, and arises as a consequence of chronic inflammation, affecting around 30% of GC-treated patients. It represents an important limitation in the management of chronic inflammatory diseases and cancer, and can be due to impairment of multiple mechanisms along the GC signalling pathway. Among them, activation of the mitogen-activated protein kinases (MAPKs) and/or alterations in expression of their regulators, the dual-specific phosphatases (DUSPs), have been identified as common mechanisms of GC resistance. While many of the anti-inflammatory actions of GCs rely on GR-mediated inhibition of MAPKs and/or induction of DUSPs, the GC anti-inflammatory capacity is decreased or lost in conditions of excessive MAPK activation, contributing to disease susceptibility in tissue- and disease- specific manners. Here, we discuss potential strategies to modulate GC responsiveness, with the dual goal of overcoming GC resistance and minimizing the onset and severity of unwanted adverse effects while maintaining therapeutic potential.

A Review on Fast Dissolving Tablet

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Sagar T. Malsane ◽  
Smita S. Aher ◽  
R. B. Saudagar
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Research Area ◽  
Oral Route ◽  
Dosage Forms ◽  
The Novel ◽  
The Past ◽  
Orally Disintegrating Tablets ◽  
Novel Drug ◽  
Experience Difficulty

Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery resulting in highest patient compliance. Over the past three decades, orally disintegrating tablets (FDTs) have gained considerable attention due to patient compliance. Usually, elderly people experience difficulty in swallowing the conventional dosage forms like tablets, capsules, solutions and suspensions because of tremors of extremities and dysphagia. In some cases such as motion sickness, sudden episodes of allergic attack or coughing, and an unavailability of water, swallowing conventional tablets may be difficult. One such problem can be solved in the novel drug delivery system by formulating “Fast dissolving tablets” (FDTs) which disintegrates or dissolves rapidly without water within few seconds in the mouth due to the action of superdisintegrant or maximizing pore structure in the formulation. The review describes the various formulation aspects, superdisintegrants employed and technologies developed for FDTs, along with various excipients, evaluation tests, marketed formulation and drugs used in this research area.

Implementasi Algoritma Hamming Distance dan Brute Force dalam Mendeteksi Kemiripan Source Code Bahasa Pemrograman C

2017 ◽  
Vol 8 (2) ◽  
Author(s):  
Andreas Budiman ◽  
Dennis Gunawan ◽  
Seng Hansun
Keyword(s):  
College Presidents ◽  
Hamming Distance ◽  
Source Code ◽  
Structural Type ◽  
Brute Force ◽  
Important Thing ◽  
The Past ◽  
Index Terms ◽  
Better Than

Plagiarism is a behavior that causes violence of copyrights. Survey shows 55% of college presidents say that plagiarism in students’ papers has increased over the past 10 years. Therefore, an application for detecting plagiarism is needed, especially for teachers. This plagiarism checker application is made by using Visual C# 2010. The plagiarism checker uses hamming distance algorithm for matching line code of the source code. This algorithm works by matching the same length string of the code programs. Thus, it needs brute will be matched with hamming distance. Another important thing for detecting plagiarism is the preprocessing, which is used to help the algorithm for detecting plagiarized source code. This paper shows that the application works good in detecting plagiarism, the hamming distance algorithm and brute force algorithm works better than levenstein distance algorithm for detecting structural type of plagiarism and this thesis also shows that the preprocessing could help the application to increase its percentage and its accuracy. Index Terms—Brute Force, Hamming Distance, Plagiarisme, Preprocessing.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

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