Ayurveda has made a major contribution in the field of pharmaceutical research by identifying active compounds. The approach has been time and cost saving in the process of providing leads in search of new molecules. In continuation, there has been tremendous interest in finding plant-originated bioenhancers as potential alternative options to the conventional ones. In course of time, herbal bioenhancers have revolutionized the area of therapeutics by their involvement in modern system of medicine. Herbal bioenhancers do not possess pharmacological activity, but when co-administered with active pharmaceutical ingredients, they tend to improve the pharmacokinetic parameters and hence, bioefficacy of varied classes of drugs. Alkaloids and their modified derivatives have gained widespread attention in the recent times as herbal bioenhancers because of their diverse range of physiological functions. Amongst other alkaloids, lysergol, a clavine alkaloid is a pharmaceutically acceptable additive with potential and acts as a novel herbal bioenhancer due to its unique properties. The latter is likely to influence on multiple fronts leading to reduction in drug toxicity and drug resistance, shortened duration of treatment and hence reduced cost of treatment where ever the concept of bioenhancement is applicable. Lysergol maintains the blood flow under normal conditions and tends to enhance the biological activity of drugs when co-administered by facilitating transfer across the membrane towards the target site. The present review is an effort to give a detailed description on the varied aspects of lysergol and its derivatives with special emphasis on its role in the field of medicine. The manuscript also highlights on recent developments in isolation of lysergol and its toxicity profile. Patents and other aspects related to lysergol and their derivatives have also been included, in addition. Finally, it was concluded that lysergol while finding strong potential and interest, needs to be further explored to make its fullest possible use in adding value to the existing drug therapy.
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