Higenamine: Potential Treatment for Erectile Dysfunction and Respiratory Issues

Effects on Erectile Dysfunction

Higenamine demonstrated the ability to relax rat corpus cavernosum tissue, suggesting potential as a treatment for erectile dysfunction. Its effects were mediated by β-adrenoceptors and enhanced in combination with phosphodiesterase type-5 inhibitors. When administered intravenously, higenamine increased penile erection strength by raising intracavernous pressure.

Respiratory Benefits

Traditionally used in Japan, Nandina domestica Thunberg (ND) fruit extracts, containing higenamine, relaxed tracheal muscles in guinea pigs via stimulation of beta2 adrenoceptors. Higenamine showed comparable efficacy to synthetic analogs and could alleviate breathing problems.

Anti-HIV Properties

Compounds isolated from Nelumbo nucifera leaves, including higenamine, exhibited potent anti-HIV activity, presenting them as promising leads for anti-AIDS drug development.

Cardiovascular and Anti-inflammatory Effects

Higenamine affected cardiovascular activity in rats and demonstrated anti-inflammatory benefits by inhibiting NO production and iNOS expression, potentially useful against conditions like septic shock.

Pharmacokinetics and Detection

A developed LC-MS/MS method enabled the sensitive detection of higenamine in human plasma and urine, aiding pharmacokinetic studies. Higenamine displayed promising pharmacokinetic and pharmacodynamic properties in healthy Chinese volunteers.

Neurological and Muscle Effects

Research showed that higenamine could affect acetylcholine release and muscle tension. Additionally, it reduced dopamine production in PC12 cells, suggesting diverse neurological implications.

Conclusion

Overall, higenamine exhibits versatile pharmacological effects, including potential treatments for erectile dysfunction, respiratory issues, cardiovascular conditions, anti-HIV properties, and anti-inflammatory responses. Its pharmacokinetics are being studied for clinical applications.

References:

1. The relaxation effect and mechanism of action of higenamine in the rat corpus cavernosum
2. Beta2-adrenoceptor-mediated tracheal relaxation induced by higenamine from Nandina domestica Thunberg
3. Biphasic tracheal relaxation induced by higenamine and nantenine from Nandina domestica Thunberg
4. Anti-HIV benzylisoquinoline alkaloids and flavonoids from the leaves of Nelumbo nucifera, and structure-activity correlations with related alkaloids
5. Cytotoxic benzophenanthridine and benzylisoquinoline alkaloids from Argemone mexicana
6. Inotropic effects of (+/-)-higenamine and its chemically related components, (+)-R-coclaurine and (+)-S-reticuline, contained in the traditional sino-Japanese medicines "bushi" and "shin-i" in isolated guinea pig papillary muscle
7. Inhibition of activation of nuclear factor kappaB is responsible for inhibition of inducible nitric oxide synthase expression by higenamine, an active component of aconite root
8. Identification of higenamine in Radix Aconiti Lateralis Preparata as a beta2-adrenergic receptor agonist1
9. Hypotensive and cardio-chronotropic constituents of Tinospora crispa and mechanisms of action on the cardiovascular system in anesthetized rats
10. Functional analysis of norcoclaurine synthase in Coptis japonica
11. Determination of higenamine in human plasma and urine using liquid chromatography coupled to positive electrospray ionization tandem mass spectrometry
12. A phase I study on pharmacokinetics and pharmacodynamics of higenamine in healthy Chinese subjects
13. Determination of higenamine in plasma and urine by high-performance liquid chromatography with electrochemical detection
14. Counter effects of higenamine and coryneine, components of aconite root, on acetylcholine release from motor nerve terminal in mice
15. Inhibitory effects of higenamine on dopamine content in PC12 cells
16. A synopsis on the role of tyrosine hydroxylase in Parkinson's disease
17. Higenamine reduces HMGB1 during hypoxia-induced brain injury by induction of heme oxygenase-1 through PI3K/Akt/Nrf-2 signal pathways
18. Higenamine reduces apoptotic cell death by induction of heme oxygenase-1 in rat myocardial ischemia-reperfusion injury
19. Effects of higenamine and its 1-naphthyl analogs, YS-49 and YS-51, on platelet TXA2 synthesis and aggregation
20. Antithrombotic effects of YS-49 and YS-51--1-naphthylmethyl analogs of higenamine
21. Thromboxane A(2) receptors: where have you gone?
22. Anti-thrombotic effects of higenamine
23. The effects of higenamine on LPS-induced experimental disseminated intravascular coagulation (DIC) in rats
24. Enantioselective synthesis of (R)-(+)- and (S)-(-)-higenamine and their analogues with effects on platelet aggregation and experimental animal model of disseminated intravascular coagulation
25. Positive chronotropic and inotropic effects of higenamine and its enhancing action on the aconitine-induced tachyarrhythmia in isolated murine atria
26. Effects of higenamine on regulation of ion transport in guinea pig distal colon
27. Effects of higenamine on isolated heart adrenoceptor of rabbit
28. Measurement of effects of the Chinese herbal medicine higenamine on left ventricular function using a cardiac probe
29. Enantiomers of higenamine inhibit LPS-induced iNOS in a macrophage cell line and improve the survival of mice with experimental endotoxemia
30. Inhibition of lipopolysaccharide-induced inducible nitric oxide (iNOS) mRNA expression and nitric oxide production by higenamine in murine peritoneal macrophages