Bioactive Glycosides from Cynanchum Species

Bioactive glycosides isolated from Cynanchum species represent a chemically diverse class of natural products typified by steroidal frameworks linked to one or more sugar moieties. The roots of C. auriculatum, C. bungei and C. wilfordii have yielded over two hundred distinct compounds, including C21-steroidal glycosides, acetophenones and terpenoid derivatives, which display a broad spectrum of pharmacological activities. Mechanistic studies in cell culture and animal models have demonstrated potent tumour-suppressive effects via induction of cell cycle arrest and caspase-dependent apoptosis, as well as hepatoprotective actions mediated through modulation of oxidative stress pathways such as Nrf2 and NF-κB. Anti-inflammatory and immunomodulatory effects have also been reported, with certain glycosides attenuating adhesion molecule expression in vascular smooth muscle cells and inhibiting key cytokine cascades. Recent phytochemical investigations continue to uncover novel glycosidic entities with antiviral and cytoprotective potential, while pharmacokinetic analyses are refining our understanding of bioavailability and tissue distribution in disease models. Collectively, these findings underscore the global relevance of Cynanchum glycosides as lead structures for drug development and as functional ingredients in traditional and modern therapeutic formulations.

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Bioactive Glycosides from Cynanchum Species publication trend

The graph below shows the total number of articles in bioactive glycosides from cynanchum species across all publications each year (not limited to Nature Index journals).

Technical terms

Glycoside: A molecule in which a sugar moiety is bound to a non-sugar aglycone, affecting solubility and bioactivity.

C21-steroidal glycoside: A steroidal compound with 21 carbon atoms conjugated to one or more sugar residues, often displaying cytotoxic or cardiotonic properties.

Caspase-dependent apoptosis: Programmed cell death mechanism mediated by activation of caspase proteases, leading to orderly cellular dismantling.

Toll-like receptor 4 (TLR4)/MyD88/NF-κB pathway: A signalling cascade in innate immunity where TLR4 engagement recruits MyD88 adaptor protein, triggering NF-κB activation and transcription of inflammatory genes.

References

1. Cynanchum auriculatum Royle ex Wight., Cynanchum bungei Decne. and Cynanchum wilfordii (Maxim.) Hemsl.: Current Research and Prospects. Molecules (2021).
2. A C21‐Steroidal Glycoside Isolated from the Roots of Cynanchum auriculatum Induces Cell Cycle Arrest and Apoptosis in Human Gastric Cancer SGC‐7901 Cells. Evidence-based Complementary and Alternative Medicine (2013).
3. Baishouwu Extract Suppresses the Development of Hepatocellular Carcinoma via TLR4/MyD88/NF-κB Pathway. Frontiers in Pharmacology (2019).
4. An ethanol root extract of Cynanchum wilfordii containing acetophenones suppresses the expression of VCAM-1 and ICAM-1 in TNF-α-stimulated human aortic smooth muscle cells through the NF-κB pathway. International Journal of Molecular Medicine (2015).
5. Pharmacokinetics and Tissue Distribution Study of Caudatin in Normal and Diethylnitrosamine-Induced Hepatocellular Carcinoma Model Rats. Molecules (2015).
6. Two New C21 Steroidal Glycosides from the Roots of Cynanchum paniculatum. Natural Products and Bioprospecting (2019).