Abstract
Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT3; serotonin) receptors in the pathogenesis and treatment of CINV. 5-HT3 receptors are members of ligand-gated ion channels that mediate the rapid and transient membrane-depolarizing effect of 5-HT in the central and peripheral nervous system. These receptors play important roles in nausea and vomiting, as well as regulation of peristalsis and pain transmission. The development of antagonists for 5-HT3 receptor dramatically improved the treatment of CINV in cancer patients. In fact, the most common use of 5-HT3 receptor antagonists to date is the treatment of nausea and vomiting. In recent years, there has been an increasing tendency to use natural plant products as important therapeutic entities in the treatment of various diseases. In this article, we examined the results of earlier studies on the actions of natural compounds on the functional properties of 5-HT3 receptors. It is likely that these natural modulators of 5-HT3 receptors can be employed as lead structures for the synthesis of therapeutic agents for treating CINV in future clinical studies.
Highlights
Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer treatment
We examine the results of earlier studies on the actions of natural negative allosteric modulators of 5-HT3 receptors
As 5-HT3 receptor antagonists were found to be effective antiemetic agents against CINV, much interest was drawn towards identifying agents that are capable of affecting/modulating the function of 5-HT3 receptors [11,39]
Summary
Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer treatment These side effects can lead to the development of serious clinical complications such as electrolyte imbalance, dehydration, weight loss, weakness, fractures and deterioration in behavioral and mental status of the patient. When combined with 5-HT3 receptor antagonist and dexamethasone, the neurokinin receptor antagonist aprepitant prevents CINV in patients receiving highly emetogenic chemotherapy [8] This four-drug regimen is recommended for the control of both acute and delayed. There has been an increasing tendency towards using natural plant products as important therapeutic entities in the treatment of different illnesses As such, these agents have advantages over synthetic drugs because they have fewer side effects (such as headache and constipation) in patients undergoing CINV [16] and are more cost-effective [17]. Plants have drawn significant interest in the field of treatment of CINV as compared to chemical drugs due to having more advantages, fewer side effects in patients undergoing CINV, as well as being more cost-effective [17]
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