Benzoylhypacoitine

《Pharmacology and Clinics of Chinese Materia Medica》 2013-05

The effect of the active parts and components of Mahuangfuzixixin Decoction on RAW 264.7 cells[Reference: WebLink]

To research the effect of the active parts and components of Mahuang-Fuzi-Xixin Decoction on RAW 264. 7 cells which was induced by lipopolysaccharide.
METHODS AND RESULTS:
As the cells was deduced by lipopolysaccharide( 1μg / ml),the non-toxic concentrations of the active parts and components of Mahuang-Fuzi-Xixin Decoction were selected to be done,the change of viability of the cells was observed by MTT method. The total alkaloids of Mahuang( 100μg / L),volatile oil of Xixin( 2. 2μl / L) and ephedrine,methylephedrine, pseudoephedrine,Benzoylhypacoitine,benzoylaconine at the concentration of 10μg / L to 100μg / L could inhibited the proliferation of RAW 264. 7 induced by lipopolysaccharide,compared with controlled group,the differences was siginificant( P 0. 05). The others had no this effect.
CONCLUSIONS:
The effects were different of the active parts and components of Mahuang-Fuzi-Xixin Decoction on RAW 264. 7 cells.

J Anal Toxicol . Jan-Feb 2015;39(1):58-68.

Simultaneous quantification and pharmacokinetics of alkaloids in Herba Ephedrae-Radix Aconiti Lateralis extracts[Pubmed: 25324527]

Abstract The combination of Herba Ephedrae (Mahuang in Chinese) and Radix Aconiti Lateralis (Fuzi in Chinese) is a classical preparation in traditional Chinese medicine and used for treating colds and rheumatic arthralgia. However, herbal medicines containing ephedrines and Aconitum alkaloids are strictly regulated because of the potential for adverse effects on the cardiovascular system and the central nervous system. We aimed to investigate the pharmacokinetics of 11 alkaloids in the Mahuang-Fuzi combination and single-herb extracts after oral administration in rats. The alkaloids were norephedrine, norpseudoephedrine, ephedrine, pseudoephedrine, methylephedrine, aconitine, mesaconitine, hypaconitine, benzoylaconine, benzoylmesaconine and benzoylhypaconine. Simultaneous determination of the alkaloids, including two pairs of diastereomers, was achieved in 14.5 min by a simple, rapid and sensitive ultra-performance liquid chromatography-tandem mass spectrometry method. The separation was performed on a Zorbax SB-Aq column (100 mm × 2.1 mm, 3.5 μm) at a flow rate of 0.3 mL/min using acetonitrile-0.1% formic acid aqueous solution as the mobile phase. The validated method demonstrated adequate sensitivity, selectivity and process efficiency for the quantitative analysis of complex herbal components. Compared with single-herb extracts, alkaloids in plasma (except methylephedrine, benzoylmesaconine and benzoylhypaconine) showed slower elimination (the mean residence time or half-life was longer), although the maximum plasma concentration and area under the plasma concentration curve values decreased. Accumulation may occur with continuous drug intake. These results suggest that drug monitoring may be essential for the safe use of the Mahuang-Fuzi combination.

《Beijing Journal of Traditional Chinese Medicine》 2014-05

Safety of compound formula of fuzi for the treatment of arthralgia with cold-damp obstruction type[Reference: WebLink]

To explore the safety of compound formula of fuzi for the treatment of arthralgia with cold-damp obstruction type,so as to provide references for its safe clinical application.
METHODS AND RESULTS:
According to different TCM syndrome scores,56 cases were treated with TCM water decoction with different doses of fuzi. At predetermined time points,blood was collected to prepare the blood samples. Pharmacokinetic parameters in each sample were test to perform safety analysis. Only monoester-type Benzoylaconine( BAC),Benzoylmesaconine( BMA),Benzoylhypacoitine( BHA) and diesters-type hypaconitine( HA) were tested positive,which all had lower blood concentration than poison dosage of fuzi. The two compartment model was the best compartment model to fit the pharmacokinetic parameters,which was different from the results of animal experiment.
CONCLUSIONS:
The dosages used in this study are safe in clinic; the differences of each alkaloid metabolism are significant,which may be associated with other unknown factors.

Journal of ethnopharmacology (Impact Factor: 2.94). 03/2014; 153(3).

Spectrum-effect relationships between UPLC fingerprints and bioactivities of crude secondary roots of Aconitum carmichaeli Debeaux (Fuzi) and its three processed products on mitochondrial growth coupled with canonical correlation analysis.[Reference: WebLink]

Ethnopharmacological relevance: The crude secondary roots of Aconitum carmichaelii Debeaux (Fuzi), together with its processed products, including Yanfuzi, Heishunpian and Paofupian, are commonly applied in clinic using for thousands of years, such as collapse, syncope, rheumatic fever, painful joints and various tumors.
METHODS AND RESULTS:
To explore the different effects of Fuzi and its processed products on energy metabolism, with mitochondria as the model with the aim of guiding the clinical use of Fuzi and its products. fingerprints of Fuzi, Yanfuzi, Heishunpian and Paofupian were established by Ultra-high Performance Liquid Chromatography (UPLC) and effects of Fuzi and its processed products on rat's liver׳s mitochondrial metabolism were studied by microcalorimetry. Spectrum-effect relationships between UPLC fingerprints and energy metabolism of mitochondria were investigated using canonical correlation analysis (CCA). Because of their inherent differences in chemical compositions, the main activities of energy metabolism of mitochondria were different among Fuzi and its processed products. The potential bioactivity sequence of the tested products was Fuzi>Heishunpian>Paofupian>Yanfuzi. RESULTS of CCA showed that compounds mesaconitine, benzoylaconitine, and Benzoylhypacoitine might be the principal active components.
CONCLUSIONS:
Altogether, this work provides a general model of combination of UPLC and microcalorimetry to study the spectrum-effect relationships of Fuzi and its processed products which can offer some references for detecting principal components of traditional Chinese medicine on bioactivity to mitochondrial growth.