Phytochemistry and Pharmacology of Periploca Compounds

The genus Periploca, belonging to the family Apocynaceae, is notable for its rich inventory of structurally diverse natural products. Primary constituents include cardiac glycosides and pregnane steroids, supplemented by terpenoids, salicylaldehyde derivatives and volatile oils. These compounds exhibit a broad spectrum of biological activities, from cardiotonic and anti-inflammatory effects to anticancer, antimicrobial and insecticidal properties. Mechanistically, many Periploca-derived glycosides act through modulation of ion pumps and intracellular signalling pathways. Cardiac glycosides such as periplocymarin enhance myocardial contractility by promoting calcium influx via Na+/K+-ATPase inhibition, while insecticidal pregnane glycosides target proton-transporting V-type H+-ATPase in lepidopteran midgut epithelia. In oncology, periplocin and related steroids induce apoptosis through caspase activation and modulation of AMPK/mTOR, ERK and p38/JNK pathways, sensitising resistant tumour cells and reducing xenograft growth. Advances in analytical methods—ultra-high-performance liquid chromatography, mass spectrometry and multivariate pattern recognition—have refined the quality assessment and pharmacokinetic profiling of Cortex Periplocae, uncovering geographical variation in active marker concentrations. Collectively, these findings underscore the global significance of Periploca compounds as leads for novel therapeutics and sustainable agrochemicals.

Research from Nature Portfolio

A recent investigation into a pregnane glycoside isolated from Periploca sepium examined its mode of action against the midgut epithelium of the oriental armyworm. Using electrophysiological assays, the study demonstrated a rapid, dose-dependent collapse of apical membrane potential without affecting the basolateral voltage, implicating selective inhibition of the V-type H+-ATPase. This mechanistic insight offers a blueprint for the development of bio-insecticides that exploit insect-specific transport proteins while minimising off-target effects on non-pest organisms.

Phytochemistry and Pharmacology of Periploca Compounds publication trend

The graph below shows the total number of articles in phytochemistry and pharmacology of periploca compounds across all publications each year (not limited to Nature Index journals).

Technical terms

Cardiac glycoside: A class of steroid-like compounds that modulate cardiac contractility by inhibiting Na+/K+-ATPase.

Pregnane glycoside: A steroidal glycoside based on a pregnane backbone, often associated with diverse bioactivities.

V-type H+-ATPase: An enzyme complex that translocates protons across membranes, essential for cellular pH regulation.

Na+/K+-ATPase: A membrane pump exchanging sodium and potassium ions at the expense of ATP to maintain electrochemical gradients.

AMPK/mTOR pathway: A signalling cascade balancing cellular energy status and growth, frequently targeted in studies of apoptosis and proliferation.

Apoptosis: Programmed cell death involving caspase activation and DNA fragmentation, critical for tissue homeostasis and cancer therapy.

References

1. Periplocymarin Plays an Efficacious Cardiotonic Role via Promoting Calcium Influx. Frontiers in Pharmacology (2020).
2. Genus Periploca (Apocynaceae): A Review of Its Classification, Phytochemistry, Biological Activities and Toxicology. Molecules (2019).
3. Effects of Periplocoside P from Periploca sepium on the Midgut Transmembrane Potential of Mythimna separata Larvae. Scientific Reports (2016).
4. Antitumor Effect of Periplocin in TRAIL‐Resistant Human Hepatocellular Carcinoma Cells through Downregulation of IAPs. Evidence-based Complementary and Alternative Medicine (2013).
5. Periplocin inhibits the growth of pancreatic cancer by inducing apoptosis via AMPK‐mTOR signaling. Cancer Medicine (2020).
6. Periplocin mediates TRAIL-induced apoptosis and cell cycle arrest in human myxofibrosarcoma cells via the ERK/p38/JNK pathway. Phytomedicine (2020).
7. Correlation between Quality and Geographical Origins of Cortex Periplocae, Based on the Qualitative and Quantitative Determination of Chemical Markers Combined with Chemical Pattern Recognition. Molecules (2019).
8. An LC‐MS/MS Method for Simultaneous Determination of the Toxic and Active Components of Cortex Periplocae in Rat Plasma and Application to a Pharmacokinetic Study. International Journal of Analytical Chemistry (2019).