Yunaconitine

Chinese Journal of Pharmacology & Toxicology, 1987(1).

Immunomodulating actions of yunaconitine.[Reference: WebLink]

Yunaconitine (YAc) is an alkaloid isolated from Aconi-tum hemsleyanum Pritz, var. circina-tum W. T. Tang and Aconitum ge-niculatum Flet.et Laue.var. unguicu-latum W. T. Wang. It is not only highly toxic, but also highly active biologically. Recently, anti-inflammatory, analgesic and antipyretic effects were found at very low dosages. In this paper immunomodula-ting actions of YAc were reported.Split heart tissue of new born C57 /BL mice were transplanted in adult male ICR mice ear pinna. ECG was followed every day to judge the survival time of allografts.YAc 50μg/ (kg·d)ip from the second day after heart transplantation markedly prolonged the survival time of allografts and was comparable to the well-known immunosuppressor predniso-lone. When they were given from the seventh day after operation, no marked effect of both drugs wasobserved. A tendency of inhibited delayed type hypersensitivity to EAE antigen was observed in EAE rats administered with YAc 5 and 10 μg/kg ip.YAc ip 20μg/kg×4 d showed no definite inhibition on serum hemoly-sin and IgG levels, 50 μg/kg×3 d suppressed the spleen PFC counts of SRBC challenged C57/BL mice. It is noticed that YAc increased serum total complement as well as the phag-ocytic activity of reticuloendothelial system in mice.
CONCLUSIONS:
These effects are considered to be beneficial in the clearance of pathogenic antigens, and may be the immunopharmacological basis of antiinflammatory actions of YAc.

J Anal Toxicol. 2006 Sep;30(7):426-33.

Hidden aconite poisoning: identification of yunaconitine and related aconitum alkaloids in urine by liquid chromatography-tandem mass spectrometry.[Pubmed: 16959134]

Poisoning from aconite occurs worldwide as a result of misuse of the potent plant. Laboratory investigation into suspected intoxication cases is challenging because the content of toxic aconitum alkaloids varies depending on the plant source, market processing, dosing protocol, hydrolytic degradation, and metabolic transformation.
METHODS AND RESULTS:
Using a triple-quadrupole tandem mass spectrometer, a group screening method was developed based on the mass-fragmentographic scheme of common aconitum alkaloids. The precursor-ion scans of m/z 105 and 135 permitted selective profiling of 14-O-benzoyl-norditerpenoids and the 14-O-anisoyl-norditerpenoids, respectively. Gradient reversed-phase liquid chromatography minimized coelution of isobaric compounds. The screening protocol was applied to a clinical investigation of suspected herbal poisoning. In total, 15 urine samples were thus screened positive for aconitum alkaloid over 5 years. The diagnoses of aconite poisoning in 11 patients were firmly established based on the known prescription history and the positive urine finding. In four patients, without aconitum herbs being listed in the herbal prescriptions, contamination of the herbal remedies by aconite was suspected to be the hidden cause of their acute poisoning.
CONCLUSIONS:
Yunaconitine, a highly toxic aconitum alkaloid, was thus identified in human urine for the first time. The group screening method of aconitum alkaloids in urine is an important diagnostic aid for acute poisoning by aconites of an unclear origin.

Chinese Journal of Pharmacology & Toxicology, 1987(3).

Anti-inflammatory and analgesic actions of yunaconitine.[Reference: WebLink]

Yunaconitine (YAc) has been extracted from several plants of Aconitum in China since 1955, but its pharmacologic action has not been investigated in detail as yet. In this paper, the anti-inflammatory and analgesic actions of YAc were reported.
METHODS AND RESULTS:
When given subcutaneously (10-80μg/kg) or orally (50-100 μg/kg) in rats and mice, YAc inhibited the increased vascular permeability caused byacetic acid and histamine, the leucocyte migratory response induced by injection of 1 % carrageenin 0.1 ml in rat's thoracic cavity, and the swelling of mouse ear caused by xylene and edema of hind paw elicited by carrageenin, fresh egg white or formaldehyde in intact or in adrenalecto-mized rats. YAc also showed positive effect in the granuloma inhibition test when it was subcutaneously injected, 10 μg/kg for 6 d, or added directly to the cotton-pellet. That YAc neither reduced the weights of thymus and adrenal in rats nor prolonged the survival time in adrenalectomized rats indicates that the action of YAc does not depend on stimulation of the pituitary-adreal axis.
CONCLUSIONS:
Assayed with writhing and hot plate method, the median analgesic doses (ED50) of YAc were found tobe 39 and 42 μg/kg in mice, respectively. YAc was shown to have antithermic effect in pyrexial rats when administered orally at a dose of 50 μg/kg.

J Sep Sci. 2013 Aug;36(16):2680-5.

Accelerated solvent extraction and pH-zone-refining counter-current chromatographic purification of yunaconitine and 8-deacetylyunaconitine from Aconitum vilmorinianum Kom.[Pubmed: 23784883]

This study aimed to seek an efficient method to extract and purify Yunaconitine and 8-deacetylYunaconitine from Aconitum vilmorinianum Kom. by accelerated solvent extraction combined with pH-zone-refining counter-current chromatography.
METHODS AND RESULTS:
The major extraction parameters for accelerated solvent extraction were optimized by an orthogonal test design L9 (3)(4). Then a separation and purification method was established using pH-zone-refining counter-current chromatography with a two-phase solvent system composed of petroleum ether/ethyl acetate/methanol/water (5:5:2:8, v/v) with 10 mM triethylamine in the upper phase and 10 mM HCl in the lower phase. From 2 g crude extract, 224 mg of 8-deacetylYunaconitine (I) and 841 mg of Yunaconitine (II) were obtained with a purity of over 98.0%. The chemical structures were identified by ESI-MS and (1)H and (13)C NMR spectroscopy.