Improved Epoxidation Methodology for Synthesis of the Highly Selective β2-Adrenoceptor Antagonist ICI 118551 [erythro (±)-3-Isopropylamino-1-(7-methylindan-4-yloxy)butan-2-ol]

1999 ◽  
Vol 52 (2) ◽  
pp. 153 ◽  
Author(s):  
Graham G. Pegg ◽  
Terry W. Badran ◽  
Andrew J. Hoey ◽  
Clifford M. Jackson ◽  
Martin N. Sillence
Keyword(s):  
Fractional Crystallization ◽  
Flash Chromatography ◽  
Pharmacological Properties ◽  
New Approach ◽  
Adrenoceptor Antagonist ◽  
Patent Literature ◽  
Original Preparation

In this communication we describe a much improved methodology for the synthesis of the selective β2-adrenoceptor antagonist ICI 118551 (1), a procedure which overcomes capricious fractional crystallization and epoxidation methodologies described for its original preparation. Our approach involving a bromohydrin precursor to the key epoxide intermediate (7) yielded an 85 : 15 mixture of the in threo/erythro isomers of (7) which could be conveniently separated by flash chromatography on amine-pretreated silica. This new approach proved much more successful than attempts to separate the precursor alkene isomers (6) by fractional crystallization as described in the original patent literature. The product (1) obtained by using our methodology was found to have identical pharmacological properties to authentic ICI 118551 when tested both in vitro and in vivo.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

Traceable Peptidic Ligands that Target Ghrelin Receptors

2020 ◽  
Vol 21 (10) ◽  
pp. 955-964 ◽  
Author(s):  
Mengjie Liu ◽  
John Wade ◽  
Mohammed Akhter Hossain
Keyword(s):  
In Vivo Imaging ◽  
Peptide Hormone ◽  
Structural Features ◽  
Pharmacological Properties ◽  
Imaging Studies ◽  
Cognate Receptor ◽  
Ghrelin Receptors ◽  
Biochemical Research

: Ghrelin is a 28-amino acid octanoylated peptide hormone that is implicated in many physiological and pathophysiological processes. Specific visualization of ghrelin and its cognate receptor using traceable ligands is crucial in elucidating the localization, functions, and expression pattern of the peptide’s signaling pathway. Here 12 representative radio- and fluorescently-labeled peptide-based ligands are reviewed for in vitro and in vivo imaging studies. In particular, the focus is on their structural features, pharmacological properties, and applications in further biochemical research.

scholarly journals Biological activity from indigenous medicinal plants of Mauritius

2005 ◽  
Vol 77 (1) ◽  
pp. 41-51 ◽  
Author(s):  
A. Gurib-Fakim ◽  
H. Subratty ◽  
F. Narod ◽  
J. Govinden-Soulange ◽  
F. Mahomoodally
Keyword(s):  
Medicinal Plant ◽  
Plant Extracts ◽  
Biological Properties ◽  
Pharmacological Properties ◽  
Plant Materials ◽  
In Vivo Screening ◽  
Medicinal Plant Extracts ◽  
Minor Ailments

The Mauritian population has a long tradition in the use of ethno-medicine, and the practice is still strong, especially in the treatment of minor ailments. Such interest stems from an existing culture, and many “tisanes” are still prepared from plant materials and sold in several markets around the island.This paper will focus on the various chemical/biological screening techniques currently being used to evaluate the biological properties of medicinal plant extracts. Particular emphasis will be put on extraction and various screening for biological/pharmacological properties. Due consideration will be given to the pharmacological approaches that utilize different animal models for the in vitro and in vivo screening of medicinal plant extracts.

Bioresorbable Microspheres as Injectable Cell Carrier: FRom Preparation to in Vitro Evaluation

1998 ◽  
Vol 550 ◽  
Author(s):  
Y. Senuma ◽  
S. Franceschin ◽  
J. G. Hilborn ◽  
P. Tissiéres ◽  
P. Frey
Keyword(s):  
Cultured Cells ◽  
Urothelial Cells ◽  
New Approach ◽  
Muscular Structure ◽  
Cell Carrier ◽  
Support Matrix ◽  
Vesico Ureteral Reflux

AbstractA new approach to the vesico-ureteral reflux could be a local regeneration of the defective vesicoureteral junction by transplanting living cells to the target site. The aim of this work is to provide a long-term effective treatment by producing bioresorbable microspheres which can act as support matrix for those cells, with the goal of an in vivo transfer of the in vitro cultured cells with a minimal surgical procedure. After microsphere degradation, the cells should be integrated into the muscular structure of the junction. Most innovative is that these are cultured muscle and urothelial cells from the bladder of the same patient.

scholarly journals In vivo measurement of intrauterine pressure by telemetry: a new approach for studying parturition in mouse models

2010 ◽  
Vol 42 (2) ◽  
pp. 310-316 ◽  
Author(s):  
Stephanie L. Pierce ◽  
William Kutschke ◽  
Rafael Cabeza ◽  
Sarah K. England
Keyword(s):  
Mouse Models ◽  
Accurate Method ◽  
Isometric Tension ◽  
Mouse Uterus ◽  
New Approach ◽  
In Vivo Measurement ◽  
Intrauterine Pressure

Transgenic and knockout mouse models have proven useful in the study of genes necessary for parturition—including genes that affect the timing and/or progression of labor contractions. However, taking full advantage of these models will require a detailed characterization of the contractile patterns in the mouse uterus. Currently the best methodology for this has been measurement of isometric tension in isolated muscle strips in vitro. However, this methodology does not provide a real-time measure of changes in uterine pressure over the course of pregnancy. Recent advances have opened the possibility of using radiotelemetric devices to more accurately and comprehensively study intrauterine pressure in vivo. We tested the effectiveness of this technology in the mouse, in both wild-type (WT) mice and a mouse model of defective parturition (SK3 channel-overexpressing mice), after surgical implant of telemetry transmitters into the uterine horn. Continuous recordings from day 18 of pregnancy through delivery revealed that WT mice typically deliver during the 12-h dark cycle after 19.5 days postcoitum. In these mice, intrauterine pressure gradually increases during this cycle, to threefold greater than that measured during the 12-h cycle before delivery. SK3-overexpressing mice, by contrast, exhibited lower intrauterine pressure over the same period. These results are consistent with the outcome of previous in vitro studies, and they indicate that telemetry is an accurate method for measuring uterine contraction, and hence parturition, in mice. The use of this technology will lead to important novel insights into changes in intrauterine pressure during the course of pregnancy.

Pharmacological Applications of Saffron (Crocus sativus)

2020 ◽  
pp. 85-92
Author(s):  
Priyanka Singh
Keyword(s):  
Health Management ◽  
Crocus Sativus ◽  
In Vivo Studies ◽  
Pharmacological Properties ◽  
The Family ◽  
Anti Oxidant ◽  
Tumour Activity ◽  
Different Parts

Saffron spice also known as Crocus sativus (Saffron crocus) belongs to the family of iridaceae. Many studies have proved its potential role in disease eradication. It has been reported to possess the attributes of a sedative, an anti-asthma, an emmenagogue, an expectorant, and an adaptogenic agent. Crocin, crocetin, and safranal are the most important biochemically active ingredients that were found in different parts of the plants in varying proportions like the peels, fruits, seeds, and rind of Crocus sativus. The in vitro and in vivo studies showed that saffron has got its therapeutic implication in health management via anti-oxidant, anti-microbial, hepatoprotective, and anti-tumour activity. This review attempts to reveal the potential pharmacological properties of Crocus sativus. It also draws attention towards the use of herbs and spices in various ailments without facing the harmful side effects of chemically derived medicine.

Pharmacological Properties of Curcumin

2020 ◽  
pp. 235-248
Author(s):  
Anuradha Singh
Keyword(s):  
Clinical Trial ◽  
Natural Product ◽  
Mechanisms Of Action ◽  
Clinical Settings ◽  
Pharmacological Properties ◽  
Pharmacological Effects ◽  
The Poor ◽  
Cellular Factors

Curcumin, the polyphenol natural product, is a constituent of the traditional medicine known as turmeric. Extensive research over the last 50 years has indicated that this polyphenol displays potent pharmacological effects by targeting many critical cellular factors through a diverse array of mechanisms of action. However, there are some obstacles that prevent this wonder molecule to be effective in clinical settings and limit its use to topical applications only. Curcumin has recently been classified as both PAINS (panassay interference compounds) and an IMPS (invalid metabolic panaceas) candidate. Due to likely false activity of curcumin in vitro and in vivo has resulted unsuccessful clinical trial of curcumin against several disease. The chapter will review the essential medicinal chemistry of curcumin as well as envisage a compilation and discussion on the poor bioavailability of curcumin.

scholarly journals New Approach Methods to Evaluate Health Risks of Air Pollutants: Critical Design Considerations for In Vitro Exposure Testing

2020 ◽  
Vol 17 (6) ◽  
pp. 2124 ◽  
Author(s):  
Jose Zavala ◽  
Anastasia N. Freedman ◽  
John T. Szilagyi ◽  
Ilona Jaspers ◽  
John F. Wambaugh ◽  
...  
Keyword(s):  
Air Pollution ◽  
Lessons Learned ◽  
Air Pollutant ◽  
In Vivo Studies ◽  
Design Parameters ◽  
Vast Number ◽  
New Approach ◽  
In Vitro Exposure

Air pollution consists of highly variable and complex mixtures recognized as major contributors to morbidity and mortality worldwide. The vast number of chemicals, coupled with limitations surrounding epidemiological and animal studies, has necessitated the development of new approach methods (NAMs) to evaluate air pollution toxicity. These alternative approaches include in vitro (cell-based) models, wherein toxicity of test atmospheres can be evaluated with increased efficiency compared to in vivo studies. In vitro exposure systems have recently been developed with the goal of evaluating air pollutant-induced toxicity; though the specific design parameters implemented in these NAMs-based studies remain in flux. This review aims to outline important design parameters to consider when using in vitro methods to evaluate air pollutant toxicity, with the goal of providing increased accuracy, reproducibility, and effectiveness when incorporating in vitro data into human health evaluations. This review is unique in that experimental considerations and lessons learned are provided, as gathered from first-hand experience developing and testing in vitro models coupled to exposure systems. Reviewed design aspects include cell models, cell exposure conditions, exposure chambers, and toxicity endpoints. Strategies are also discussed to incorporate in vitro findings into the context of in vivo toxicity and overall risk assessment.

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