Effect of Cleistanthin A and B on Adrenergic and Cholinergic Receptors

Overview

Journal Pharmacogn Mag

Publisher Sage Publications

Date 2011 Oct 5

PMID 21969796

Citations 9

Authors

S Parasuraman

R Raveendran

Affiliations

Soon will be listed here.

Abstract

Objective: The aim was to study the in vitro and in silico interactions of cleistanthin A and B on the adrenergic and cholinergic receptors using isolated animal tissues and bioinformatics tools.

Materials And Methods: The alpha adrenergic receptor activities of cleistanthin A and B were studied in vitro using a guinea pig vas deferens preparation. The beta adrenergic receptor activities of cleistanthin A and B on an isolated rat heart were studied in vitro using a modified Langendorff apparatus. The effects of cleistanthin A and B on the nicotinic and muscarinic cholinergic receptors were studied in vitro using rabbit vas deferens and rabbit jejunum, respectively. All the drug responses were recorded using a data acquisition system through a variable force transducer. The receptor-ligand interactions of cleistanthin A and B with adrenergic and cholinergic receptor proteins were determined using the ArgusLab molecular modeling and drug docking program.

Results: Cleistanthin A and B significantly inhibited the actions of the alpha adrenergic receptor and the nicotinic cholinergic receptor. Cleistanthin A and B shifted the dose-response curve to the right with an increased EC(50) value of phenylephrine and acetylcholine. Both cleistanthin A and B did not have any significant effect on the beta adrenergic and muscarinic cholinergic receptors.

Conclusion: Cleistanthin A and B block the alpha adrenergic and nicotinic cholinergic receptors, but these compounds do not interact at all with the beta adrenergic and muscarinic cholinergic receptors.

Citing Articles

Cleistanthins A and B Ameliorate Testosterone-Induced Benign Prostatic Hyperplasia in Castrated Rats by Regulating Apoptosis and Cell Differentiation.

S C S, R R, Ganesh R Cureus. 2023; 14(12):e32141.

PMID: 36601166 PMC: 9805890. DOI: 10.7759/cureus.32141.

Rapid Preparative Isolation of Cleistanthin A from the Leaves of Using Reverse-Phase Flash Chromatography.

Kumar S, Raveendran R, Achari K J Pharm Bioallied Sci. 2022; 14(2):93-98.

PMID: 36034488 PMC: 9416109. DOI: 10.4103/jpbs.jpbs_723_21.

Sub-chronic toxicological evaluation of cleistanthin A and cleistanthin B from the leaves of (Roxb.).

Parasuraman S, Raveendran R, Rajesh N, Nandhakumar S Toxicol Rep. 2017; 1:596-611.

PMID: 28962273 PMC: 5598356. DOI: 10.1016/j.toxrep.2014.08.006.

Antiproliferative Compounds from Cleistanthus boivinianus from the Madagascar Dry Forest.

Liu Y, Young K, Rakotondraibe L, Brodie P, Wiley J, Cassera M J Nat Prod. 2015; 78(7):1543-7.

PMID: 26091020 PMC: 4517784. DOI: 10.1021/np501020m.

Evaluation of the antihypertensive activity and alpha adrenergic receptor interaction of cleistanthins A and B.

Priyadharsini R, Parasuraman S, Raveendran R J Basic Clin Pharm. 2014; 5(4):109-14.

PMID: 25316991 PMC: 4194941. DOI: 10.4103/0976-0105.141950.

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