Diterpenoid Alkaloids in Traditional Chinese Medicine

Summary

Diterpenoid alkaloids are a class of nitrogen-containing natural products derived from a diterpene backbone and found predominantly in Aconitum and Delphinium species. They have underpinned key remedies in Traditional Chinese Medicine (TCM) for pain relief, anti-inflammatory therapy and cardiovascular support. Structural diversity arises from variations in core ring systems—principally C20, C19 and C18 skeletons—which govern biological activity and toxicological profile. Modern advances in chromatography and nuclear magnetic resonance spectroscopy have refined isolation and structure elucidation of trace alkaloids, while mechanistic studies reveal interactions with ion channels and modulation of apoptotic and oxidative stress pathways. Safety concerns linked to neurotoxicity and cardiotoxicity have spurred the optimisation of traditional processing methods to reduce levels of the most toxic congeners. Concurrently, semi-synthetic modification and total synthesis efforts aim to improve therapeutic indices. Their promise has attracted multidisciplinary efforts worldwide, bridging ethnopharmacology, synthetic chemistry and pharmacology to develop safer, efficacious derivatives.

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Diterpenoid Alkaloids in Traditional Chinese Medicine publication trend

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Technical terms

Diterpenoid alkaloid: A nitrogenous secondary metabolite based on a 20-carbon diterpene scaffold, exhibiting variable ring systems (C20, C19, C18) and diverse pharmacological profiles.

Aconitine: A potent C19-diterpenoid alkaloid from Aconitum species, valued for analgesic activity but associated with marked cardiotoxic and neurotoxic risks.

Reactive oxygen species (ROS): Oxygen-derived free radicals and peroxides that, in pathological excess, induce oxidative damage and activate apoptotic pathways.

Haemoglobin subunit beta (HBB): A globin protein that, upon binding to aconitine, influences nitric oxide scavenging and predisposes to cardiomyocyte injury.

References

  1. Aconitum carmichaelii triggers neurotoxicity and Parkinson‐like symptoms through initiation of ROS‐mitochondrial apoptosis and the Nox5/DJ‐1 signaling pathway. BMEMat (2023).
  2. HBB contributes to individualized aconitine-induced cardiotoxicity in mice via interfering with ABHD5/AMPK/HDAC4 axis. Acta Pharmacologica Sinica (2024).
  3. Seeing the unseen of Chinese herbal medicine processing (Paozhi): advances in new perspectives. Chinese Medicine (2018).
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