Regulation of Na ions and channels

As previously mentioned in this book, alkaloid biological activity is rather diverse, and alkaloids, therefore, have biological significance as histological regulators of metabolism. This significance is pertinent to the development of the applications. One such important role of some alkaloids is their influence on Na+ channels and interaction with receptors. Aconitine, ajmaline, sanguinarine (Figure 93) and sparteine have clinical uses in this respect. Aconitine causes an influx of Na+ ions across membranes. Therefore, aconitine can first activate and in later stages also block the nerve of the receptor. This alkaloid regulates the activity of Na+ channels and consequently the receptor activity and enzymatic activity regulated by the receptor. Applications of this alkaloid are connected with the regulation of defects in neuro- and local disturbances in signalling and receptor nerve activity.

Although ajmaline also influences Na+ channels, its activity is to block these channels. This influences the refraction phase of the heart beat and also decreases heart rate. Ajmaline may be used to correct arrhythmic defects. Sanguinarine also influences Na+ ions and particularly inhibits esterase activity. This alkaloid has several other activities in the body and specifically in tissues. Possible applications are linked to the promotion discharge of mucus from the respiratory tract.

Sparteine is an alkaloid that inhibits N+ channels and Na+ ion flux and activating a muscarinergic acetylcholine receptor. In small doses this alkaloid acts as

a stimulant, while in large doses it has a paralyzing effect on autonomic ganglia. Medical applications may include possible correction of cardiac arrhythmia.

The regulation of Na+ ions and channels are the means for possible correction of abnormalities in tissue functioning and ganglic integrations. However, it is necessary to pay attention to the possible unwanted side effects. Alkaloids are complex agents. Smaller doses are safer when considering cell toxicity or other possible metabolic effects. Alkaloids and alkaloidal substances should be given serious consideration and precautions before use.

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