scholarly journals Emetine Is Not Ipecac: Considerations for Its Use as Treatment for SARS-CoV2

2020 ◽  
Vol 13 (12) ◽  
pp. 428
Author(s):  
Martin D. Bleasel ◽  
Gregory M. Peterson
Keyword(s):  
Side Effects ◽  
Viral Inhibition ◽  
Response Data ◽  
Spanish Influenza ◽  
The Past ◽  
Inhibition Data ◽  
Potential Mode ◽  
Pure Drug ◽  
Anti Inflammatory ◽  
Higher Doses

Emetine is a potent antiviral that acts on many viruses in the low-nM range, with several studies in animals and humans demonstrating antiviral activity. Historically, emetine was used to treat patients with Spanish influenza, in the last stages of the pandemic in the early 1900s. Some of these patients were “black” with cyanosis. Emetine rapidly reversed the cyanosis and other symptoms of this disease in 12–24 h. However, emetine also has been shown to have anti-inflammatory properties and it appears it is these anti-inflammatory properties that were responsible for the effects seen in patients with Spanish influenza. Emetine, in the past, has also been used in 10s to 100s of millions of people at a dose of ~60 mg daily to treat amoebiasis. Based on viral inhibition data we can calculate a likely SARS-CoV2 antiviral dose of ~1/10th the amoebiasis dose, which should dramatically reduce the risk of any side effects. While there are no anti-inflammatory dose response data available, based on the potential mode of action, the anti-inflammatory actions may also occur at low doses. This paper also examines the toxicity of emetine seen in clinical practice and that seen in the laboratory, and discusses the methods of administration aimed at reducing side effects if higher doses were found to be necessary. While emetine is a “pure drug” as it is extracted from ipecac, some of the differences between emetine and ipecac are also discussed.

scholarly journals Anti-leishmanial and Anti-inflammatory Agents from Endophytes: A Review

2019 ◽  
Vol 9 (5) ◽  
pp. 311-328 ◽  
Author(s):  
Rufin Marie Kouipou Toghueo
Keyword(s):  
Side Effects ◽  
Inflammatory Diseases ◽  
The Other ◽  
Bioactive Metabolites ◽  
Chronic Inflammatory Diseases ◽  
The Past ◽  
The World ◽  
The Status ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Abstract Leishmaniases and chronic inflammatory diseases are the cause of millions of deaths in the world each year. The treatment of leishmaniasis is facing serious drawbacks particularly due to the limited number of effective medicines, the resistance, and the toxicity of available drugs. On the other hand, many drugs are used for the management of inflammatory disorders. However, the most commonly prescribed although efficient is highly toxic with multiples side effects. New leads compounds for the development of new anti-leishmanial and anti-inflammatory drugs are needed. Over the past decade, several studies on the potential of endophytes to produce bioactive metabolites have been reported. We are presenting in the present review the status of research from 2000 to 2019 on the anti-leishmanial and anti-inflammatory metabolites isolated from endophytes from diverse habitats. An emphasis was put on existing gaps in the literature to inspire and guide future investigations. We hope that this review will help accelerate the drug discovery against leishmaniases and inflammation-associated disorders. Graphic Abstract

Fluorocarbon Precursor for High Aspect Ratio via Milling in Focused Ion Beam Modification of Integrated Circuits

2004 ◽  
Author(s):  
Valery Ray
Keyword(s):  
Side Effects ◽  
Aspect Ratio ◽  
Integrated Circuits ◽  
High Aspect Ratio ◽  
Focused Ion Beam ◽  
Ion Beam ◽  
Enabling Technology ◽  
Si Substrate ◽  
Ion Beam Modification ◽  
The Past

Abstract Gas Assisted Etching (GAE) is the enabling technology for High Aspect Ratio (HAR) circuit access via milling in Focused Ion Beam (FIB) circuit modification. Metal interconnect layers of microelectronic Integrated Circuits (ICs) are separated by Inter-Layer Dielectric (ILD) materials, therefore HAR vias are typically milled in dielectrics. Most of the etching precursor gases presently available for GAE of dielectrics on commercial FIB systems, such as XeF2, Cl2, etc., are also effective etch enhancers for either Si, or/and some of the metals used in ICs. Therefore use of these precursors for via milling in dielectrics may lead to unwanted side effects, especially in a backside circuit edit approach. Making contacts to the polysilicon lines with traditional GAE precursors could also be difficult, if not impossible. Some of these precursors have a tendency to produce isotropic vias, especially in Si. It has been proposed in the past to use fluorocarbon gases as precursors for the FIB milling of dielectrics. Preliminary experimental evaluation of Trifluoroacetic (Perfluoroacetic) Acid (TFA, CF3COOH) as a possible etching precursor for the HAR via milling in the application to FIB modification of ICs demonstrated that highly enhanced anisotropic milling of SiO2 in HAR vias is possible. A via with 9:1 aspect ratio was milled with accurate endpoint on Si and without apparent damage to the underlying Si substrate.

Sending out Biased Signals: an Appropriate Proposition for Pain?

2019 ◽  
Vol 32 (2) ◽  
pp. 108-110 ◽  
Author(s):  
E. Besserer-Offroy ◽  
P. Sarret
Keyword(s):  
Side Effects ◽  
Acute Pain ◽  
Gold Standard ◽  
Pain Treatment ◽  
Opioid Analgesics ◽  
Mu Opioid Receptor ◽  
Clinical Development ◽  
Mu Opioid ◽  
Development Stages ◽  
The Past

In the past few years, several biased ligands acting at the mu-opioid receptor were reported in the literature. These agonists are aimed at reducing pain while having fewer side effects than morphine, the gold standard of opioid analgesics. In this mini-review, we describe and discuss the recent advances in mu-biased ligands actually in preclinical and clinical development stages, including the latest U.S. Food and Drug Administration review of oliceridine, a biased mu-agonist for moderate to severe acute pain treatment developed by the company Trevena.

Anti-Inflammatory Properties of Plant Derived Natural Products – A Systematic Review

2019 ◽  
Vol 26 (24) ◽  
pp. 4506-4536 ◽  
Author(s):  
Iris E. Allijn ◽  
René P. Brinkhuis ◽  
Gert Storm ◽  
Raymond M. Schiffelers
Keyword(s):  
Systematic Review ◽  
Natural Products ◽  
Positive Control ◽  
Therapeutic Effects ◽  
Reference Compound ◽  
Individual Molecular Species ◽  
The Past ◽  
Anti Inflammatory ◽  
The Individual ◽  
Natural Medicines

Traditionally, natural medicines have been administered as plant extracts, which are composed of a mixture of molecules. The individual molecular species in this mixture may or may not contribute to the overall medicinal effects and some may even oppose the beneficial activity of others. To better control therapeutic effects, studies that characterized specific molecules and describe their individual activity that have been performed over the past decades. These studies appear to underline that natural products are particularly effective as antioxidants and anti-inflammatory agents. In this systematic review we aimed to identify potent anti-inflammatory natural products and relate their efficacy to their chemical structure and physicochemical properties. To identify these compounds, we performed a comprehensive literature search to find those studies, in which a dose-response description and a positive control reference compound was used to benchmark the observed activity. Of the analyzed papers, 7% of initially selected studies met these requirements and were subjected to further analysis. This analysis revealed that most selected natural products indeed appeared to possess anti-inflammatory activities, in particular anti-oxidative properties. In addition, 14% of the natural products outperformed the remaining natural products in all tested assays and are attractive candidates as new anti-inflammatory agents.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

scholarly journals Periplaneta americana Oligosaccharides Exert Anti-Inflammatory Activity through Immunoregulation and Modulation of Gut Microbiota in Acute Colitis Mice Model

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1718
Author(s):  
Kaimin Lu ◽  
Jing Zhou ◽  
Jie Deng ◽  
Yangjun Li ◽  
Chuanfang Wu ◽  
...  
Keyword(s):  
Side Effects ◽  
Pathogenic Bacteria ◽  
Periplaneta Americana ◽  
Biochemical Characterization ◽  
Antioxidant Activities ◽  
Inflammatory Activity ◽  
Mice Model ◽  
Acute Colitis ◽  
Anti Inflammatory

The incidence and prevalence of inflammatory bowel disorders (IBD) are increasing around the world due to bacterial infection, abnormal immune response, etc. The conventional medicines for IBD treatment possess serious side effects. Periplaneta americana (P. americana), a traditional Chinese medicine, has been used to treat arthritis, fever, aches, inflammation, and other diseases. This study aimed to evaluate the anti-inflammatory effects of oligosaccharides from P. Americana (OPA) and its possible mechanisms in vivo. OPA were purified and biochemical characterization was analyzed by HPGPC, HPLC, FT-IR, and GC–MS. Acute colitis mice model was established, the acute toxicity and anti-inflammatory activity were tested in vivo. The results showed OPA with molecular mass of 1.0 kDa were composed of 83% glucose, 6% galactose, 11% xylose, and the backbone was (1→4)-Glcp. OPA had potent antioxidant activities in vitro and significantly alleviated the clinical symptoms of colitis, relieved colon damage without toxic side effects in vivo. OPA exhibited anti-inflammatory activity by regulating Th1/Th2, reducing oxidative stress, preserving intestinal barrier integrity, and inhibiting TLR4/MAPK/NF-κB pathway. Moreover, OPA protected gut by increasing microbial diversity and beneficial bacteria, and reducing pathogenic bacteria in feces. OPA might be the candidate of complementary and alternative medicines of IBD with low-cost and high safety.

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