Abstract
In this work, we reviewed the progress in the phytochemical and biological investigations of bioactive components derived from medicinally valuable Lobelia species. In the last 60 years, Lobelia has garnered significant attention from the phytochemist from around the world, majorly due to the discovery of bioactive piperidine alkaloids (e.g., lobinaline and lobeline) in the early 1950s. Later, lobeline underwent clinical trials for several indications including the treatment of attention deficit hyperactivity disorder and a multicenter phase three trial for smoking cessation. Subsequently, several other alkaloids derived from different species of Lobelia were also investigated for their pharmacological characteristics. However, in the last few years, the research focus has started shifting to the characterization of the other novel chemical classes. The major shift has been noticed due to the structurally similar alkaloid components, which essentially share similar pharmacological, physicochemical, and toxicological profiles. In this review, we present an up-to-date overview of their progress with special attention to understanding the molecular mechanisms of the novel bioactive components.
Highlights
Lobelia, named after the botanist Matthias de lobel, is a large genus of medicinally valuable flowering plants belonging to the Campanulaceae family comprising more than 450 species distributed predominantly in tropical and temperate regions of the world
One of the alkaloids that garnered major attention was lobeline 1 (Figure 1), which was primarily derived from the aerial parts of Lobelia inflata, (Kaczmarek and Steinegger, 1959; Saldanha et al, 1959)
We have recently investigated the neuroprotection mechanism of the pharmacokinetically favorable, experimentally validated active compounds derived from the 17 Lobelia species (Table 2) based on network pharmacology and molecular modeling (Zheng et al, 2020)
Summary
Lobelia, named after the botanist Matthias de lobel, is a large genus of medicinally valuable flowering plants belonging to the Campanulaceae family comprising more than 450 species distributed predominantly in tropical and temperate regions of the world. In the 1950s, other studies began to reveal the distinctive pharmacological properties of the alkaloid constituents derived from different Lobelia species (Lendle and Richter, 1950).
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