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Vietnamese Dalbergia tonkinensis: A Promising Source of Mono- and Bifunctional Vasodilators
Nguyen Manh Cuong1, Ninh The Son2, Ngu Truong Nhan3
1Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Caugiay, Hanoi 122100, Vietnam.
Insights
Flavonoids from Dalbergia tonkinensis show potential for new blood pressure drugs. These compounds affect key ion channels (KCa1.1 and CaV1.2) involved in hypertension, offering novel therapeutic avenues.
Area of Science:
- Pharmacology and Cardiovascular Research
- Natural Product Chemistry
- Computational Chemistry
Background:
- Hypertension is a major global risk factor for cardiovascular diseases.
- Ion channels KCa1.1 and CaV1.2 play critical roles in vascular function and are implicated in hypertension.
- Traditional medicine often utilizes plant-derived compounds for therapeutic purposes.
Purpose of the Study:
- To investigate the in vitro vascular effects of flavonoids from Dalbergia tonkinensis.
- To identify compounds that modulate KCa1.1 and CaV1.2 channels.
- To explore the potential of these flavonoids as antihypertensive agents.
Main Methods:
- Extraction and isolation of flavonoids from Dalbergia tonkinensis.
- In vitro assays using rat aorta rings and tail artery myocytes.
- Electrophysiological recordings to measure ion channel activity.
- Molecular docking and dynamics simulations to predict binding interactions.
Main Results:
- Several flavonoids, including formononetin, orobol, pinocembrin, and biochanin A, exhibited significant myorelaxant activity.
- Sativanone, 3'-O-methylviolanone, pinocembrin, and biochanin A blocked CaV1.2 channel currents, while ambocin stimulated them.
- Sativanone, dalsissooside, and eriodictyol inhibited KCa1.1 currents, whereas tectorigenin derivative, ambocin, butin, and biochanin A increased them.
- In silico analyses revealed high-affinity binding of biochanin A, sativanone, and pinocembrin to both target channels.
Conclusions:
- Dalbergia tonkinensis is a rich source of vasoactive flavonoids.
- Specific flavonoids demonstrate potent effects on KCa1.1 and CaV1.2 channels.
- These findings support the development of novel antihypertensive drugs based on Dalbergia tonkinensis scaffolds.
Abstract:
Hypertension is a risk factor for cardiovascular diseases, which are the main cause of morbidity and mortality in the world. In the search for new molecules capable of targeting KCa1.1 and CaV1.2 channels, the expression of which is altered in hypertension, the in vitro vascular effects of a series of flavonoids extracted from the heartwoods, roots, and leaves of Dalbergia tonkinensis Prain, widely used in traditional medicine, were assessed. Rat aorta rings, tail artery myocytes, and docking and molecular dynamics simulations were used to analyse their effect on these channels. Formononetin, orobol, pinocembrin, and biochanin A showed a marked myorelaxant activity, particularly in rings stimulated by moderate rather than high KCl concentrations. Ba2+ currents through CaV1.2 channels (IBa1.2) were blocked in a concentration-dependent manner by sativanone, 3'-O-methylviolanone, pinocembrin, and biochanin A, while it was stimulated by ambocin. Sativanone, dalsissooside, and eriodictyol inhibited, while tectorigenin 7-O-[β-D-apiofuranosyl-(1→6)-β-D-glucopyranoside], ambocin, butin, and biochanin A increased IKCa1.1. In silico analyses showed that biochanin A, sativanone, and pinocembrin bound with high affinity in target-sensing regions of both channels, providing insight into their potential mechanism of action. In conclusion, Dalbergia tonkinensis is a valuable source of mono- and bifunctional, vasoactive scaffolds for the development of novel antihypertensive drugs.
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