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Related Concept Videos

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship01:22

Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
Direct-Acting Cholinergic Agonists: Therapeutic Uses01:11

Direct-Acting Cholinergic Agonists: Therapeutic Uses

Direct-acting cholinergic agonists have many therapeutic uses in various medical fields. Choline esters, including acetylcholine, have limited clinical utility due to their non-selectivity and short duration of action. Still, acetylcholine and carbachol are applied topically during ophthalmologic surgery to induce miosis. Pilocarpine, a muscarinic and ganglionic stimulator, effectively treats open-angle glaucoma and alleviates xerostomia and dry mouth caused by radiotherapy or Sjögren syndrome.
Global Regulatory Systems01:28

Global Regulatory Systems

Global regulatory systems in bacteria enable rapid and coordinated responses to environmental changes by integrating sensory inputs with gene expression, ensuring efficient adaptation to fluctuating conditions. Key global regulatory mechanisms include regulons, two-component systems, sigma factors, and secondary messengers.Regulons and Global RegulatorsA regulon is a collection of genes and operons controlled by a common global regulator. These regulators enable bacteria to prioritize resource...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship01:16

Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of the aromatic...
Direct-Acting Cholinergic Agonists: Pharmacological Actions00:59

Direct-Acting Cholinergic Agonists: Pharmacological Actions

Direct-acting cholinergic agonists exert their pharmacological actions by mimicking the effects of acetylcholine on postsynaptic muscarinic receptors to generate parasympathetic responses. These agents elicit a range of physiological responses, including cardiovascular effects. For example, activation of muscarinic receptors induces bradycardia, decreased cardiac output, reduced peripheral resistance, and consequent hypotension. In the eye, stimulation of M3 receptors leads to smooth muscle...

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Related Experiment Video

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Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay
09:11

Live-cell Measurement of Odorant Receptor Activation Using a Real-time cAMP Assay

Published on: October 2, 2017

PPARγ agonist from Chromolaena odorata.

Man-Li Zhang1, Dianne Irwin, Xiao-Ning Li

  • 1School of Pharmaceutical Sciences, Hebei Medical University, 361 Zhongshan East Road, Shijiazhuang 050017, People's Republic of China. zhang-manli@163.com

Journal of Natural Products
|November 29, 2012
PubMed
Summary

Phytochemical analysis of Chromolaena odorata yielded five new compounds and 12 known ones. Odoratin (6) demonstrated moderate PPARγ transactivation activity, indicating potential therapeutic applications.

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Area of Science:

  • Natural Product Chemistry
  • Pharmacology
  • Medicinal Plant Research

Background:

  • Chromolaena odorata is a plant with a history of traditional medicinal use.
  • Phytochemical studies aim to identify bioactive compounds from medicinal plants.
  • Understanding the biological activities of plant-derived compounds is crucial for drug discovery.

Purpose of the Study:

  • To isolate and identify new and known phytochemicals from Chromolaena odorata.
  • To evaluate the isolated compounds for their potential to activate peroxisome proliferator-activated receptor gamma (PPARγ).

Main Methods:

  • Phytochemical investigation involving extraction and chromatographic separation techniques.
  • Structure elucidation of isolated compounds using spectroscopic methods (e.g., NMR, MS).
  • In vitro assay to determine PPARγ transactivation activity of the compounds.

Main Results:

  • Five new compounds (1-5) and 12 known compounds (6-17) were isolated from Chromolaena odorata.
  • Odoratin (6) exhibited moderate PPARγ transactivation activity with an EC(50) of 3.10 μM.
  • The study identified a diverse range of chemical structures from the plant.

Conclusions:

  • The phytochemical investigation successfully identified novel and known compounds from Chromolaena odorata.
  • Odoratin shows potential as a PPARγ modulator, warranting further investigation for therapeutic development.
  • This study contributes to the understanding of Chromolaena odorata's chemical constituents and their biological activities.