Gelsemium elegans Benth: Chemical Components, Pharmacological Effects, and Toxicity Mechanisms

Abstract

Gelsemium elegans Benth (GEB), also known as heartbreak grass, is a highly poisonous plant belonging to the family Loganiaceae and genus Gelsemium that has broad application prospects in medicine. This article reviews its chemical components, pharmacological effects, toxicity mechanisms, and research progress in clinical applications in recent years. Indole alkaloids are the main active components of GEB and have a variety of pharmacological and biological functions. They have anti-tumor, anti-inflammatory, analgesic, and immunomodulation properties, with the therapeutic dose being close to the toxic dose. Application of small-dose indole alkaloids fails to work effectively, while high-dose usage is prone to poisoning, aggravating the patient’s conditions. Special caution is needed, especially to observe the changes in the disease condition of the patients in clinical practice. In-depth research on the chemical components and mechanisms of GEB is essential to the development of promising lead compounds and lays the foundation for extensive clinical application and safe usage of GEB in the future.

Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium : a comprehensive review

“…In terms of structure type, gelsemium MIAs possess characteristic chemical structures containing polycyclic monoterpene portions and indole, oxindole, or bisindole nuclei 9 . Gelsemium MIAs can be classified into six categories: gelsedine-, gelsemine-, humantenine-, koumine-, sarpagine- and yohimbane-type, on the basis of their structural features 10 ( Figure 1) . Among them, gelsemine-type, humantenine-type and gelsedine-type alkaloids bear peculiar spiro -indolinone nuclei, while koumine-, sarpagine- and yohimbane-type alkaloids have normal indole groups.…”

Modulation of GABAA receptors and of GABAergic synapses by the natural alkaloid gelsemine

“…Gelsemium elegans extracts have been used to treat various common diseases, including neuralgia, sciatica, rheumatoid arthritis, chronic pain, and anxiety ( Rujjanawate et al, 2003 ; Dutt et al, 2010 ; Jin et al, 2014 ; Lin et al, 2021 ). Nevertheless, Gelsemium elegans preparations have been also classified as strong poisons and its clinical uses are limited by their intrinsic toxicity, which may include body tremors, dyspnea, convulsions, tremors, respiratory arrest, and even death ( Zhou et al, 2017 ; Lin et al, 2021 ; Qu et al, 2021 ; Yang et al, 2022 ). Interestingly, both the beneficial and toxic effects of Gelsemium elegans extracts in humans have been reproduced in experimental models ( Dutt et al, 2010 ; Jin et al, 2014 ; Lin et al, 2021 ).…”

“…Nevertheless, Gelsemium elegans preparations have been also classified as strong poisons and its clinical uses are limited by their intrinsic toxicity, which may include body tremors, dyspnea, convulsions, tremors, respiratory arrest, and even death ( Zhou et al, 2017 ; Lin et al, 2021 ; Qu et al, 2021 ; Yang et al, 2022 ). Interestingly, both the beneficial and toxic effects of Gelsemium elegans extracts in humans have been reproduced in experimental models ( Dutt et al, 2010 ; Jin et al, 2014 ; Lin et al, 2021 ). Purified alkaloids from Gelsemium plants have replicated several of the actions shown by extracts.…”

Molecular Mechanism of Gelsemium elegans (Gardner and Champ.) Benth. Against Neuropathic Pain Based on Network Pharmacology and Experimental Evidence

“…Benth. (Gelsemiaceae) (GEB) is a toxic plant indigenous to Southeast Asia especially China, which has long been used as Chinese folk medicine for the treatment of various types of pain, such as neuralgia, sciatica, rheumatoid arthritis, and acute pain ( Rujjanawate et al, 2003 ; Lin et al, 2021 ). Phytochemical studies have revealed that the main active ingredients of GEB are alkaloids, especially the indole alkaloids, such as koumine, gelsemine, gelsenicine, and gelsevirine ( Jin et al, 2014 ).…”