Page last updated: 2024-12-08

hypaconitine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Description

hypaconitine: RN given refers to the (1alpha,6alpha,14alpha,15alpha,16beta)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10008952
CHEMBL ID400315
MeSH IDM0162666

Synonyms (5)

Synonym
V0370 ,
hypaconitine
C08688 ,
CHEMBL400315
surecn2848738

Research Excerpts

Toxicity

ZT10 dosing of Fuzi generated higher systemic exposures of three toxic alkaloid ingredients aconitine, hypaconitine and mesacon itine compared to ZT22.

ExcerptReferenceRelevance
"Hypaconitine is an active and highly toxic constituent derived from Aconitum species."( Circadian Cyp3a11 metabolism contributes to chronotoxicity of hypaconitine in mice.
Gao, L; Lin, Y; Wang, S; Wu, B; Yang, Z; Yu, P; Zhou, Z, 2019
)
0.51
"Therapeutic applications of Fuzi (lateral root of Aconitum carmichaeli Debx) are seriously concerned with its toxic effects."( Circadian clock regulates metabolism and toxicity of Fuzi(lateral root of Aconitum carmichaeli Debx) in mice.
Dong, D; Gao, L; Lin, Y; Wang, S; Wu, B; Yang, Z; Zhou, Z, 2020
)
0.56
" ZT10 dosing of Fuzi generated higher systemic exposures of three toxic alkaloid ingredients aconitine (AC), hypaconitine (HA) and mesaconitine (MA) compared to ZT22."( Circadian clock regulates metabolism and toxicity of Fuzi(lateral root of Aconitum carmichaeli Debx) in mice.
Dong, D; Gao, L; Lin, Y; Wang, S; Wu, B; Yang, Z; Zhou, Z, 2020
)
0.56

Pharmacokinetics

Plasma pharmacokinetic profiles of aconitine, mesacon itine, and hypaconitine were investigated after once treatment of Fuzi extract. Area under the curve (AUC) values (reflective of systemic exposure) were significantly higher than those for herb dosing at ZT22.

ExcerptReferenceRelevance
" The validated method was employed to simultaneous quantitation and successfully used for the first time for the pharmacokinetic evaluation of the six Aconitum alkaloids after intravenous drop administration of "SHEN-FU" injectable powder in phase I clinical trial."( Simultaneous quantitation of aconitine, mesaconitine, hypaconitine, benzoylaconine, benzoylmesaconine and benzoylhypaconine in human plasma by liquid chromatography-tandem mass spectrometry and pharmacokinetics evaluation of "SHEN-FU" injectable powder.
Chen, LJ; Duan, JG; Li, R; Tang, MH; Wang, XH; Wei, YQ; Zhang, F; Zhao, X, 2008
)
0.35
" The intestinal absorption and pharmacokinetic characters of 3 diester diterpenoid alkaloids in the precipitation were investigated."( Study on intestinal absorption and pharmacokinetic characterization of diester diterpenoid alkaloids in precipitation derived from fuzi-gancao herb-pair decoction for its potential interaction mechanism investigation.
Fu, CM; He, Y; He, YX; Liao, W; Yan, D; Zhang, JM, 2013
)
0.39
" Moreover, by means of determination of the plasma concentration, the pharmacokinetic characters of 3 alkaloid compounds in rats have been developed."( Study on intestinal absorption and pharmacokinetic characterization of diester diterpenoid alkaloids in precipitation derived from fuzi-gancao herb-pair decoction for its potential interaction mechanism investigation.
Fu, CM; He, Y; He, YX; Liao, W; Yan, D; Zhang, JM, 2013
)
0.39
"05), while T1/2, AUC0-t and Cmax of BAC, BHA increased (P<0."( The effects of Rhizoma Zingiberis on pharmacokinetics of six Aconitum alkaloids in herb couple of Radix Aconiti Lateralis-Rhizoma Zingiberis.
Cai, BC; Cui, XB; Li, JS; Li, W; Peng, WW; Wen, HM; Yang, GM; Zhang, YX, 2013
)
0.39
" 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."( Simultaneous quantification and pharmacokinetics of alkaloids in Herba Ephedrae-Radix Aconiti Lateralis extracts.
Huo, H; Li, H; Luo, J; Song, S; Tang, Q; Xing, X,
)
0.13
" Plasma concentrations of HC were determined at designated points after oral administration, and main pharmacokinetic parameters were estimated."( Comparative pharmacokinetics of hypaconitine after oral administration of pure hypaconitine, Aconitum carmichaelii extract and Sini Decoction to rats.
Chen, J; Sun, FF; Sun, S; Zhang, GQ; Zhang, H; Zhang, W; Zhao, L, 2015
)
0.42
"To investigate therapeutic effects and pharmacokinetic profiles of aconitine-type alkaloids in CHF rats."( Pharmacokinetics of aconitine-type alkaloids after oral administration of Fuzi (Aconiti Lateralis Radix Praeparata) in rats with chronic heart failure by microdialysis and ultra-high performance liquid chromatography-tandem mass spectrometry.
Cao, Y; Xiong, YK; Yu, B, 2015
)
0.42
" Pharmacokinetic analyses showed that the area under the curve (AUC) values (reflective of systemic exposure) and renal distribution of aconitine, hypaconitine and mesaconitine (three putative active constituents) for Fuzi dosing at ZT10 were significantly higher than those for herb dosing at ZT22, suggesting a role of circadian pharmacokinetics in Fuzi chronoefficacy."( Pharmacokinetics-based chronoefficacy of Fuzi against chronic kidney disease.
Gao, L; Lin, J; Lin, Y; Su, C; Wang, S; Wang, Z; Wu, B; Yang, Z, 2021
)
0.62

Compound-Compound Interactions

The results indicated that the mRNA and protein expression levels of CaM were significantly decreased by hypaconitine used alone and combined with liquiritin.

ExcerptReferenceRelevance
"To study the effects of hypaconitine used alone and combined with liquiritin on calmodulin (CaM) expression and connexin43 (Cx43) phosphorylation on serine368 (Ser368), as well as to investigate the intervention of liquiritin on these hypaconitine-induced effects."( Effect of hypaconitine combined with liquiritin on the expression of calmodulin and connexin43 in rat cardiac muscle in vivo.
Chen, X; Chen, Y; Peng, W; Wang, J; Yi, M, 2012
)
0.38
"The results indicated that the mRNA and protein expression levels of CaM were significantly decreased by hypaconitine used alone and combined with liquiritin."( Effect of hypaconitine combined with liquiritin on the expression of calmodulin and connexin43 in rat cardiac muscle in vivo.
Chen, X; Chen, Y; Peng, W; Wang, J; Yi, M, 2012
)
0.38

Bioavailability

ExcerptReferenceRelevance
" These observations indicated that the three alkaloids may not only be P-gp inhibitors but also its substrates; they interact with each other and can potentially enhance their own bioavailability when taken concomitantly."( Intestinal transport of pure diester-type alkaloids from an aconite extract across the Caco-2 cell monolayer model.
Li, N; Liu, Z; Ma, J; Sui, Z; Tsao, R, 2012
)
0.38
" The absorption rate and degree of 6-gingerol in the ileum in the Sini Decoction group were significantly higher than those in the Zingiberis Rhizoma group(P<0."( [Comparative study on intestinal absorption kinetics of main active components in Sini Decoction and its separated recipes].
Chen, YL; Fu, CM; Fu, S; Gan, S; Gao, F; Lin, MS; Zhou, F, 2022
)
0.72
" For in-vitro experiment, the modified Franz diffusion cell method was used to determine the transdermal absorption rate and 24h cumulative transdermal absorption amount of the active ingredients of crossbow-medicine liquid."( Effect of microneedle roller on promoting transdermal absorption of crossbow-medicine liquid via transdermal administration of Traditional Chinese Medicine and the safety of crossbow-medicine needle therapy: An experimental study.
Cui, J; Luo, H; Zan, F, 2023
)
0.91
" The 24h cumulative transdermal absorption amount and transdermal absorption rate of each ingredient in microneedle-roller group were significantly higher than those in crossbow-medicine liquid application group (all P < 0."( Effect of microneedle roller on promoting transdermal absorption of crossbow-medicine liquid via transdermal administration of Traditional Chinese Medicine and the safety of crossbow-medicine needle therapy: An experimental study.
Cui, J; Luo, H; Zan, F, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
"Toxicity was determined based on assessment of heart injury and animal survival after dosing mice with Fuzi decoction at different circadian time points."( Circadian clock regulates metabolism and toxicity of Fuzi(lateral root of Aconitum carmichaeli Debx) in mice.
Dong, D; Gao, L; Lin, Y; Wang, S; Wu, B; Yang, Z; Zhou, Z, 2020
)
0.56
" ZT10 dosing of Fuzi generated higher systemic exposures of three toxic alkaloid ingredients aconitine (AC), hypaconitine (HA) and mesaconitine (MA) compared to ZT22."( Circadian clock regulates metabolism and toxicity of Fuzi(lateral root of Aconitum carmichaeli Debx) in mice.
Dong, D; Gao, L; Lin, Y; Wang, S; Wu, B; Yang, Z; Zhou, Z, 2020
)
0.56
" In this study, we uncovered that the therapeutic effect of Fuzi (the lateral root of Aconitum carmichaelii Debeaux) depended on the dosing time in mice with adenine-induced chronic kidney disease (CKD)."( Pharmacokinetics-based chronoefficacy of Fuzi against chronic kidney disease.
Gao, L; Lin, J; Lin, Y; Su, C; Wang, S; Wang, Z; Wu, B; Yang, Z, 2021
)
0.62
"The Fuzi efficacy was higher when the drug was dosed at ZT10 and was lower when the drug was dosed at other times (ZT2, ZT6, ZT14, ZT18 and ZT22) according to measurements of plasma CRE, BUN and urinary NAG."( Pharmacokinetics-based chronoefficacy of Fuzi against chronic kidney disease.
Gao, L; Lin, J; Lin, Y; Su, C; Wang, S; Wang, Z; Wu, B; Yang, Z, 2021
)
0.62
"The efficacy of Fuzi against CKD depends on the dosing time in mice, which is associated with circadian pharmacokinetics of the three main active constituents (i."( Pharmacokinetics-based chronoefficacy of Fuzi against chronic kidney disease.
Gao, L; Lin, J; Lin, Y; Su, C; Wang, S; Wang, Z; Wu, B; Yang, Z, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID1193993Antiproliferative activity against human KB cells by sulforhodamine B assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Evaluation of Aconitum diterpenoid alkaloids as antiproliferative agents.
AID676150Cytotoxicity against human Ketr3 cells at 10 uM after 96 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676148Cytotoxicity against human A549 cells at 10 uM after 96 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676149Cytotoxicity against human MCF7 cells at 10 uM after 96 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676145Hepatoprotective activity against DL-galactosamine-induced cell death in rat WB-F344 cells at 10 uM incubated for 1 hr prior to DL-galactosamine-challenge measured after 24 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID1193992Antiproliferative activity against human DU145 cells by sulforhodamine B assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Evaluation of Aconitum diterpenoid alkaloids as antiproliferative agents.
AID676151Cytotoxicity against human Bel7402 cells at 10 uM after 96 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID1193991Antiproliferative activity against human A549 cells by sulforhodamine B assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Evaluation of Aconitum diterpenoid alkaloids as antiproliferative agents.
AID676142Analgesic activity in mouse assessed as reduction in acetic acid-induced writhing at 0.5 mg/kg, ip relative to vehicle-treated control2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676141Toxicity in ip dosed mouse acetic acid wrtihe model2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676140Toxicity in mouse acetic acid writhe model assessed as mortality at 5 mg/kg, ip2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID312019Growth inhibition of human A172 cells after 6 days2007Journal of natural products, Dec, Volume: 70, Issue:12
Inhibitory effects of diterpenoid alkaloids on the growth of A172 human malignant cells.
AID676152Cytotoxicity against human HCT8 cells at 10 uM after 96 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676147Cytotoxicity against human BGC823 cells at 10 uM after 96 hrs by MTT assay2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID676144Antioxidant activity in rat liver microsome assessed as inhibition of FeSO4-induced lipid peroxidation at 10 uM incubated for 15 mins prior to FeSO4-challenge measured after 15 mins by modified thiobarbituric acid method2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
AID1193994Antiproliferative activity against multidrug-resistant P-gp expressing human KBVIN cells by sulforhodamine B assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Evaluation of Aconitum diterpenoid alkaloids as antiproliferative agents.
AID1193995Selectivity ratio of GI50 for human KB cells to GI50 for multidrug-resistant P-gp expressing human KBVIN cells2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Evaluation of Aconitum diterpenoid alkaloids as antiproliferative agents.
AID676146Antiinflammatory activity in mouse peritoneal macrophages assessed as inhibition of nitric oxide production at 10 uM2012Journal of natural products, Jun-22, Volume: 75, Issue:6
Diterpenoid alkaloids from the lateral root of Aconitum carmichaelii.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (79)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901 (1.27)18.7374
1990's10 (12.66)18.2507
2000's16 (20.25)29.6817
2010's43 (54.43)24.3611
2020's9 (11.39)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (1.19%)6.00%
Case Studies2 (2.38%)4.05%
Observational0 (0.00%)0.25%
Other81 (96.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]