Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Antiasthma Drugs: Leukotriene Modifiers01:19

Antiasthma Drugs: Leukotriene Modifiers

Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Adrenergic Antagonists: ɑ and β-Receptor Blockers01:31

Adrenergic Antagonists: ɑ and β-Receptor Blockers

Third-generation β-blockers, such as labetalol and carvedilol, represent a significant advancement in managing cardiovascular conditions. Unlike conventional β-blockers, which can induce peripheral vasoconstriction, third-generation drugs block α1 adrenoceptors. This promotes vasodilation through several mechanisms, such as increased nitric oxide production, inhibition of calcium ion entry, opening of potassium ion channels, and antioxidant action. Labetalol, for instance, is clinically...
Local Anesthetics: Chemistry and Structure-Activity Relationship01:30

Local Anesthetics: Chemistry and Structure-Activity Relationship

Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...
Local Anesthetics: Common Agents and Their Applications01:23

Local Anesthetics: Common Agents and Their Applications

Local anesthetics (LAs) are commonly used for various applications in medical and dental procedures. Some of the common agents used are cocaine, lidocaine, and bupivacaine.
Cocaine is an ester of benzoic acid and methylecgogine. It is used to anesthetize and vasoconstrict locally. Currently, it is used primarily for topical applications. It is beneficial for surgeries on the upper respiratory tract, providing anesthesia and shrinking the mucosa. Cocaine in the form of cocaine hydrochloride is...
Antiasthma Drugs: β2-Adrenoceptor Agonists01:25

Antiasthma Drugs: β2-Adrenoceptor Agonists

Bronchodilators are critical in managing asthma, a chronic respiratory condition characterized by airway constriction due to inflammation and hyper-reactivity. Specifically, bronchodilators ease this constriction by relaxing the bronchial muscles, facilitating easier breathing.
One class of bronchodilators includes β2-adrenoceptor agonists. These agents target the β2-adrenoceptors located on bronchial smooth muscle cells. By stimulating these receptors, β2-agonists induce relaxation in these...
Local Anesthetics: Adverse Effects01:12

Local Anesthetics: Adverse Effects

While local anesthetics are generally safe and well-tolerated, they can occasionally cause adverse effects that vary in severity. Local anesthetics can induce toxicity at two distinct levels. They can either produce local effects through direct contact with the neural elements or be absorbed into the bloodstream from the injection site, leading to systemic effects.
Once absorbed into the systemic circulation, local anesthetics can affect the organs that depend on the functioning of sodium...

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

GPCR Biased Signaling: Opportunities and Challenges.

Biochemistry·2026
Same author

Structural characterization of kappa-opioid receptor dimer in complex with two G proteins.

Nature communications·2026
Same author

Toward a Random Background for Ligand Optimization.

bioRxiv : the preprint server for biology·2026
Same author

De novo design of miniproteins targeting GPCRs.

Nature·2026
Same author

The Selectivity Implications of Docking Libraries with Greater and Lesser Similarities to Bio-like Molecules.

Journal of medicinal chemistry·2026
Same author

The polypharmacological profiles of xanomeline and N-desmethylxanomeline.

British journal of pharmacology·2026
Same journal

Five undescribed compounds isolated from Gerbera delavayi with their anti-inflammatory activity.

Phytochemistry·2026
Same journal

Ingenane diterpenoids with anti-inflammatory activity from the whole plants of Euphorbia peplus.

Phytochemistry·2026
Same journal

Discovery of cytotoxic 1,4-benzodioxane oxyneolignan analogues from Glechoma longituba.

Phytochemistry·2026
Same journal

Cinnamolides A-G, seven previously undescribed phytoconstituents from the peels of Cinnamomum chago and their anti-inflammatory activity.

Phytochemistry·2026
Same journal

Antiviral amide derivatives from Uvaria siamensis.

Phytochemistry·2026
Same journal

COX-2 inhibitors from Laportea bulbifera: Structure-activity relationship, kinetic investigation, and molecular docking.

Phytochemistry·2026
See all related articles

Related Experiment Video

Updated: May 23, 2026

A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
07:59

A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products

Published on: October 4, 2019

Labdane diterpenoids from Leonotis leonurus.

Hankui Wu1, Jun Li, Frank R Fronczek

  • 1Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University, MS 38677-1848, USA.

Phytochemistry
|March 27, 2012
PubMed
Summary
This summary is machine-generated.

Researchers isolated eleven labdane diterpenoids from Leonotis leonurus, with several showing activity at central nervous system (CNS) receptors. Leoleorin C demonstrated moderate binding affinity for the Sigma 1 receptor.

More Related Videos

Applications of Liquid-Chromatography Tandem Mass Spectrometry in Natural Products Research: Tropane Alkaloids as a Case Study
09:36

Applications of Liquid-Chromatography Tandem Mass Spectrometry in Natural Products Research: Tropane Alkaloids as a Case Study

Published on: March 8, 2024

Related Experiment Videos

Last Updated: May 23, 2026

A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products
07:59

A Customizable Approach for the Enzymatic Production and Purification of Diterpenoid Natural Products

Published on: October 4, 2019

Applications of Liquid-Chromatography Tandem Mass Spectrometry in Natural Products Research: Tropane Alkaloids as a Case Study
09:36

Applications of Liquid-Chromatography Tandem Mass Spectrometry in Natural Products Research: Tropane Alkaloids as a Case Study

Published on: March 8, 2024

Area of Science:

  • Natural Products Chemistry
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Leonotis leonurus is a plant source of bioactive compounds.
  • Labdane diterpenoids represent a class of natural products with diverse biological activities.
  • Central nervous system (CNS) receptors are crucial targets for therapeutic interventions.

Purpose of the Study:

  • To isolate and characterize labdane diterpenoids from Leonotis leonurus leaves.
  • To investigate the binding affinities of these compounds to various CNS receptors.
  • To determine the absolute configurations of novel isolated compounds.

Main Methods:

  • Isolation and purification of compounds using chromatographic techniques.
  • Structure elucidation using spectroscopic methods (e.g., NMR, MS).
  • X-ray crystallographic analysis for absolute configuration determination.
  • Competitive binding assays for CNS receptor interaction studies.

Main Results:

  • Eleven labdane diterpenoids were isolated: three known (leoleorins A-C) and eight unknown (leoleorins D-J and 16-epi-leoleorin F).
  • Absolute configurations of leoleorins A and D were confirmed via X-ray crystallography.
  • All isolated compounds exhibited >50% inhibition at various CNS receptors in binding assays.
  • Leoleorin C displayed moderate binding affinity (Ki = 2.9 µM) for the Sigma 1 receptor.

Conclusions:

  • Leonotis leonurus is a rich source of structurally diverse labdane diterpenoids.
  • The isolated compounds possess potential CNS activity, warranting further investigation.
  • Leoleorin C is a promising ligand for the Sigma 1 receptor, suggesting therapeutic potential.