Aconitum carmichaeli Debx.

Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC₅₀=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.

Benzoylaconine (Benzoylaconitine) is an orally active monoester alkaloid found in the traditional Chinese medicine Aconitum carmichaelii. Benzoylaconine is an ACE2 agonist (EC₅₀: 1.5 μM) with antihypertensive and anti-heart failure effects. Benzoylaconine inhibits TLR-induced MAPK and NF-κB pathways to exert anti-inflammatory effects. Benzoylaconine upregulates the protein levels of P-gp, MRP2, and has anti-tumor effects.

Benzoylmesaconine is a monoester-type alkaloid and is the most abundant component of Wutou decoction, which is widely used in China for rheumatoid arthritis. Benzoylmesaconine exhibits potent anti-inflammatory properties by inhibiting NF-κB. Benzoylmesaconine can suppress NLRP3 inflammasome activation by inhibiting IL-1β secretion and GSDMD-N protein expression. Benzoylmesaconine reduces intracellular K⁺ efflux and disrupts NLRP3 inflammasome assembly.

Hypaconitine inhibits the KCNH2 current with an IC₅₀ of 8.1 nM, and exhibits cardiotoxicity. Hypaconitine inhibits TGF-β1-induced epithelial-mesenchymal transition (EMT) in A549 cell through the inhibition of NF-κB nuclear translocation. Hypaconitine acts as the neuromuscular blocker. Hypaconitine is orally active.

Talatisamine is an orally active cyclophilin D activator isolated from the roots of Aconitum carmichaeli Debx. Talatisamine exerts biological functions by activating cyclophilin D, inhibiting Ca²⁺-dependent opening of the mitochondrial permeability transition pore (mPTP) (IC₅₀=78 μM), and blocking delayed rectifier K⁺ channels (IC₅₀=146 μM). Talatisamine possesses both antioxidant and membrane-stabilizing properties, effectively inhibits lipid peroxidation and protects mitochondrial membrane function. Talatisamine exhibits multiple activities including antiarrhythmic, hypotensive, anti-inflammatory, anticancer and neuroprotective effects. Talatisamine finds applications in the research of ischemic diseases, rheumatoid arthritis, inflammation-related diseases and Alzheimer's disease.

Aconiti lateralis radix praeparata polysaccharide is a polysaccharide derived from Aconiti lateralis radix praeparata.

Senbusine A (compound 4) is a diterpenic alkaloid found in the dried roots of Aconitum carmichaeli from China. Senbusine A acts as an intermediate in the biosynthesis of aconitine.

Karacolidine (compound 9) is an aconitine-type alkaloid. Karacolidine can be found in the lateral root of Aconitum carmichaeli Debx. (Radix Aconiti Lateralis).

Aconine inhibits receptor activator of nuclear factor (NF)-κB ligand (RANKL)-induced NF-κB activation.

Mesaconitine is a nitric oxide synthase activator. Mesaconitine drives extracellular Na⁺ and Ca²⁺ influx into endothelial cells, increases intracellular Na⁺ and Ca²⁺ concentrations, and triggers nitric oxide release. Mesaconitine is applicable for pain-related research.

Benzoylhypaconine (Benzoylhypacoitine) is a monoester Aconitum alkaloid, is the main pharmacologic and toxic component.

Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression.

Fuziline is a alkaloid isolated from the lateral roots of Aconitum carmichaelii.

Beiwutine (10-Hydroxy mesaconitine) is a diester diterpenoid alkaloid.

Crassicauline A (Crassicaulin A) is a diester-type diterpenoid alkaloid. Crassicauline A exhibits feeding deterrent activity against adult Tribolium castaneum, with a EC₅₀ of 1134.5 ppm. Crassicauline A induces arrhythmia at a dose of 0.10 mg/kg.

3-Deoxyaconitine a diterpenoid alkaloid, is a sodium channel activator.

12-Epinapelline is a diterpene alkaloid isolated from Aconitum baikalense. 12-Epinapelline exhibits Anti-inflammatory activity and stimulates the growth of colonies from fibroblast precursors.

Karacoline is an orally active PPARγ activator and ERK/JNK MAPK inhibitor. Karacoline restricts ROS production, maintains mitochondrial membrane potential, and inhibits pulmonary cell apoptosis. Karacoline inhibits NF-κB pathway activation, reduces acetylation levels of p65 and the expression of MMP14 and MMP9, enhances the expression of type II collagen (collagen II) and aggrecan (aggrecan), and suppresses extracellular matrix degradation. In a mouse model of sepsis-induced acute lung injury, Karacoline alleviates lung injury, inhibits the release of IL-1β, IL-6 and TNF-α, increases the Bcl-2/BAX ratio, and reduces caspase 3 expression. Karacoline can be used in research related to acute lung injury and intervertebral disc degeneration.

Octodrine (2-Amino-6-methylheptane) is a central nervous stimulant that increases the uptake of dopamine and noradrenaline. Octodrine is found to increase the pain threshold, cardiac rate (positive chronotropic effect) and myocardial contractility (positive inotropic effect).

6-Benzoylheteratisine is an Aconitum alkaloid with potential neuroprotective activity. 6-Benzoylheteratisine can antagonize tetrodotoxin, inhibit the increase of [Na⁺]i, [Ca²⁺]i and glutamate release, and block sodium channels. 6-Benzoylheteratisine has an inhibitory effect on the neuronal activity underlying epileptiform burst discharge.