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Aconitine

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https://www.readbyqxmd.com/read/28638869/reducing-toxicity-and-increasing-efficiency-aconitine-with-liquiritin-and-glycyrrhetinic-acid-regulate-calcium-regulatory-proteins-in-rat-myocardial-cell
#1
Yuyan Zhang, Li Yu, Weifeng Jin, Hongjing Fan, Min Li, Tianmei Zhou, Haitong Wan, Jiehong Yang
BACKGROUND: Compatibility of Radix Aconiti Carmichaeli and Liquorice is known to treat heart diseases such as heart failure and cardiac arrhythmias. This work answers the question that whether the active components (Aconitine, Liquiritin and Glycyrrhetinic Acid) of Radix Aconiti Carmichaeli and Liquorice could result in regulating intracellular calcium homeostasis and calcium cycling, and thereby verifies the therapeutic material basis. MATERIALS AND METHODS: The myocardial cells were divided into twelve groups randomly as control group, Aconitine group, nine different dose groups that orthogonal combined with Aconitine, Liquiritin and Glycyrrhetinic Acid, and Verapamil group...
2017: African Journal of Traditional, Complementary, and Alternative Medicines: AJTCAM
https://www.readbyqxmd.com/read/28611679/icariin-a-novel-blocker-of-sodium-and-calcium-channels-eliminates-early-and-delayed-afterdepolarizations-as-well-as-triggered-activity-in-rabbit-cardiomyocytes
#2
Wanzhen Jiang, Mengliu Zeng, Zhenzhen Cao, Zhipei Liu, Jie Hao, Peipei Zhang, Youjia Tian, Peihua Zhang, Jihua Ma
Icariin, a flavonoid monomer from Herba Epimedii, has confirmed pharmacological and biological effects. However, its effects on arrhythmias and cardiac electrophysiology remain unclear. Here we investigate the effects of icariin on ion currents and action potentials (APs) in the rabbit myocardium. Furthermore, the effects of icariin on aconitine-induced arrhythmias were assessed in whole rabbits. Ion currents and APs were recorded in voltage-clamp and current-clamp mode in rabbit left ventricular myocytes (LVMs) and left atrial myocytes (LAMs), respectively...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28591742/andrographolide-inhibits-arrhythmias-and-is-cardioprotective-in-rabbits
#3
Mengliu Zeng, Wanzhen Jiang, Youjia Tian, Jie Hao, Zhenzhen Cao, Zhipei Liu, Chen Fu, Peihua Zhang, Jihua Ma
Andrographolide has a protective effect on the cardiovascular system. To study its cardic-electrophysiological effects, action potentials and voltage-gated Na+ (INa), Ca2+ (ICaL), and K+ (IK1, IKr, Ito and IKur) currents were recorded using whole-cell patch clamp and current clamp techniques. Additionally, the effects of andrographolide on aconitine-induced arrhythmias were assessed on electrocardiograms in vivo. We found that andrographolide shortened action potential duration and reduced maximum upstroke velocity in rabbit left ventricular and left atrial myocytes...
May 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28554514/remodeling-of-ventricular-repolarization-in-experimental-right-ventricular-hypertrophy
#4
S N Kharin, V V Krandycheva, A S Tsvetkova, K V Shumikhin
BACKGROUND: To understand electrophysiological mechanisms that underlie the progression of compensated right ventricular hypertrophy (RVH) to heart failure, the purpose of the study was to evaluate remodeling of ventricular repolarization in connection with hemodynamic abnormalities and vulnerability of the heart ventricles to arrhythmias in RVH rats with pulmonary arterial hypertension (PAH) and heart failure. METHODS: PAH followed by heart failure was induced by monocrotaline in adult female Wistar rats...
May 18, 2017: Journal of Electrocardiology
https://www.readbyqxmd.com/read/28552884/ranolazine-facilitates-termination-of-ventricular-tachyarrhythmia-associated-with-acute-myocardial-ischemia-through-suppression-of-late-ina-mediated-focal-activity
#5
Takashi Ogawa, Haruo Honjo, Masatoshi Yamazaki, Yasunori Kushiyama, Ichiro Sakuma, Itsuo Kodama, Kaichiro Kamiya
BACKGROUND: Ventricular tachycardia/fibrillation (VT/VF) associated with acute myocardial ischemia is the most common cause of sudden cardiac death, but its underlying mechanisms are incompletely understood. It is hypothesized that late Na(+)current (INa) contributes to arrhythmogenic activity in ischemic myocardium.Methods and Results:Langendorff-perfused rabbit hearts with regional ischemia in ventricles were optically mapped. Perfusion with ranolazine (10 μmol/L), a selective inhibitor of lateINa, significantly reduced excitation frequency and facilitated termination of VT/VF induced after occlusion of the left main coronary trunk...
May 26, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28552596/gram-scale-purification-of-aconitine-and-identification-of-lappaconitine-in-aconitum-karacolicum
#6
M Tarbe, H de Pomyers, L Mugnier, D Bertin, T Ibragimov, D Gigmes, K Mabrouk
Aconitum karacolicum from northern Kyrgyzstan (Alatau area) contains about 0.8-1% aconitine as well as other aconite derivatives that have already been identified. In this paper, we compare several methods for the further purification of an Aconitum karacolicum extract initially containing 80% of aconitine. Reverse-phase flash chromatography, reverse-phase semi-preparative HPLC, centrifugal partition chromatography (CPC) and recrystallization techniques were evaluated regarding first their efficiency to get the highest purity of aconitine (over 96%) and secondly their applicability in a semi-industrial scale purification process (in our case, 150g of plant extract)...
May 26, 2017: Fitoterapia
https://www.readbyqxmd.com/read/28545288/-enhanced-tachycardia-arrhythmia-in-two-patients-with-aconitine-intoxication-treated-with-atropine
#7
F Q Ma, Y Wang, C X Suo
No abstract text is available yet for this article.
April 24, 2017: Zhonghua Xin Xue Guan Bing za Zhi
https://www.readbyqxmd.com/read/28528229/sensitive-uhplc-ms-ms-quantitation-and-pharmacokinetic-comparisons-of-multiple-alkaloids-from-fuzi-beimu-and-single-herb-aqueous-extracts-following-oral-delivery-in-rats
#8
Yanyan Xu, Yamei Li, Pengjie Zhang, Bin Yang, Huanyu Wu, Xuejun Guo, Yubo Li, Yanjun Zhang
Aconiti Lateralis Radix Praeparata- Fritillariae Thunbergii bulbus, namely Fuzi- Beimu in Chinese, is a classic herb pair whose combined administration was prohibited according to the rule of "Eighteen antagonisms". However, incompatibility of Fuzi and Beimu has become controversial because of the application supported by many recorded ancient prescriptions and increasing modern researches and clinical practice. The present study aimed to investigate the pharmacokinetic differences of multiple alkaloids from Fuzi- Beimu and the single herb aqueous extracts following oral delivery in rats...
May 15, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28491724/spectrum-of-cardiac-manifestations-from-aconitine-poisoning
#9
Swetha P Karturi, Hjalti Gudmundsson, Masood Akhtar, Arshad Jahangir, Indrajit Choudhuri
No abstract text is available yet for this article.
September 2016: HeartRhythm Case Reports
https://www.readbyqxmd.com/read/28472842/diterpene-lipo-alkaloids-with-selective-activities-on-cardiac-k-channels
#10
Tivadar Kiss, Botond Borcsa, Péter Orvos, László Tálosi, Judit Hohmann, Dezső Csupor
Aconitum diterpene alkaloids are known for their remarkable toxicity, which is due to their effect on ion channels. Activation of voltage-gated Na(+) channels is the major cause of their cardiotoxicity, however, influence on K(+) channels may also play a role in the overall effect.Here we report the synthesis of a series of lipo-alkaloids, including four new compounds, based on the 14-benzoylaconine structure, which is the core of a vast number of diterpene alkaloids naturally occurring in Aconitum species...
May 4, 2017: Planta Medica
https://www.readbyqxmd.com/read/28421842/the-management-of-ventricular-dysrhythmia-in-aconite-poisoning
#11
REVIEW
James M Coulson, Thomas M Caparrotta, John P Thompson
INTRODUCTION: Aconite poisoning is relatively rare but is frequently complicated by ventricular dysrhythmias, which may be fatal. Molecular basis of aconite alkaloid ventricular arrhythmogenicity: Aconite exerts its toxic effects due to the presence of an admixture of alkaloids present in all parts of the plant. The major target of these aconite alkaloids is the fast voltage-gates sodium channel, where they cause persistent activation. This blockade of the channel in the activated state promotes automaticity within the ventricular myocardium and the generation of ventricular arrhythmias...
June 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28330159/in-silico-characterization-and-differential-expression-pattern-analysis-of-conserved-hmg-coa-reductase-domain-isolated-from-aconitum-balfourii-stapf
#12
Eti Sharma, Saurabh Pandey, A K Gaur
The 3-hydroxy-3-methyl glutaryl CoA reductase (HMGR) is the key enzyme of mevalonate pathway in plants. A partial genomic DNA fragment encoding HMGR conserved domain (denoted as AbHMGR) is isolated from Aconitum balfourii Stapf. It comprises 871 bp encoding 290 amino acids. In silico analysis reveals that it had extensive similarities to other plant HMGR gene. Domain analysis of AbHMGR showed two highly conserved NADPH and HMG CoA domains. Docking study predicted inhibitor, substrate and cofactor binding sites in the protein...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28327597/molecular-signaling-underlying-bulleyaconitine-a-baa-induced-microglial-expression-of-prodynorphin
#13
Teng-Fei Li, Hai-Yun Wu, Yi-Rui Wang, Xin-Yan Li, Yong-Xiang Wang
Bulleyaconitine (BAA) has been shown to possess antinociceptive activities by stimulation of dynorphin A release from spinal microglia. This study investigated its underlying signal transduction mechanisms. The data showed that (1) BAA treatment induced phosphorylation of CREB (rather than NF-κB) and prodynorphin expression in cultured primary microglia, and antiallodynia in neuropathy, which were totally inhibited by the CREB inhibitor KG-501; (2) BAA upregulated phosphorylation of p38 (but not ERK or JNK), and the p38 inhibitor SB203580 (but not ERK or JNK inhibitor) and p38β gene silencer siRNA/p38β (but not siRNA/p38α) completely blocked BAA-induced p38 phosphorylation and/or prodynorphin expression, and antiallodynia; (3) BAA stimulated cAMP production and PKA phosphorylation, and the adenylate cyclase inhibitor DDA and PKA inhibitor H-89 entirely antagonized BAA-induced prodynorphin expression and antiallodynia; (4) The Gs-protein inhibitor NF449 completely inhibited BAA-increased cAMP level, prodynorphin expression and antiallodynia, whereas the antagonists of noradrenergic, corticotrophin-releasing factor, A1 adenosine, formyl peptide, D1/D2 dopamine, and glucagon like-peptide-1 receptors failed to block BAA-induced antiallodynia...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28302448/aconitine-a-potential-novel-treatment-for-systemic-lupus-erythematosus
#14
Xiaodong Li, Liwei Gu, Lan Yang, Dong Zhang, Jianying Shen
BACKGROUND: Aconitum plants have been widely used in China for thousands of years. Recent evidences indicate that aconitine, the main active ingredient of Aconitum, has immunomodulatory properties that might be useful for treating autoimmune diseases, such as rheumatoid arthritis. In this study, we conducted a pilot study to explore the effect and mechanisms of aconitine on the treatment of systemic lupus erythematosus. METHODS: A pristane-induced murine model was used...
February 24, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28259253/establishment-of-one-step-approach-to-detoxification-of-hypertoxic-aconite-based-on-the-evaluation-of-alkaloids-contents-and-quality
#15
Ding-Kun Zhang, Xue Han, Peng Tan, Rui-Yu Li, Ming Niu, Cong-En Zhang, Jia-Bo Wang, Ming Yang, Xiao-He Xiao
Aconite is a valuable drug and also a toxic material, which can be used only after detoxification processing. Although traditional processing methods can achieve detoxification effect as desired, there are some obvious drawbacks, including a significant loss of alkaloids and poor quality consistency. It is thus necessary to develop a new detoxification approach. In the present study, we designed a novel one-step detoxification approach by quickly drying fresh-cut aconite particles. In order to evaluate the technical advantages, the contents of mesaconitine, aconitine, hypaconitine, benzoylmesaconine, benzoylaconine, benzoylhypaconine, neoline, fuziline, songorine, and talatisamine were determined using HPLC and UHPLC/Q-TOF-MS...
January 2017: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/28193520/mdr1a-plays-a-crucial-role-in-regulating-the-analgesic-effect-and-toxicity-of-aconitine-by-altering-its-pharmacokinetic-characteristics
#16
Lijun Zhu, Jinjun Wu, Min Zhao, Wenjie Song, Xiaoxiao Qi, Ying Wang, Linlin Lu, Zhongqiu Liu
Aconitine (AC) is the primary bioactive/toxic alkaloid in plants of the Aconitum species. Our previous study demonstrated that Mdr1 was involved in efflux of AC. However, the mechanism by which Mdr1 regulates the efficacy/toxicity of AC in vivo remains unclear. The present study aimed to determine the effects of Mdr1a on the efficacy/toxicity and pharmacokinetics of AC in wild-type and Mdr1a(-/-) FVB mice. After oral administration of AC, significantly higher analgesic effect was observed in Mdr1a(-/-) mice (49% to 105%) compared to wild-type mice (P<0...
April 1, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28104561/assessment-of-in-vitro-cardiotoxicity-of-extract-fractions-and-diterpene-alkaloids-from-aconitum-leucostomum-worosch-a-short-communication
#17
Jihong Nie, Fang Wang, Tengfei Ji, Jun Zhao, Feicui Zhao
Aconitum leucostomum Worosch is a traditional Chinese medicine (TCM) and has a broad spectrum of health effects, but with a narrow therapeutic window. It is important to identify both the therapeutic ingredients and the toxic components to better utilize this TCM. The present study investigated the cardiotoxicity of the selected compounds in Aconitum leucostomum Worosch. The effects of extract of A. leucostomum Worosch and the isolated compounds on cardiocardiomyocytes were evaluated in vitro. Five known compounds in this TCM, including three C18-diterpene alkaloids, lappaconitine (2), N-deacetyllappaconitine (3), and ranaconitine (5), and two C19-diterpene alkaloids, delvestidine (1) and anthranoyllycoctonine (4), were isolated from A...
April 15, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28056545/histone-deacetylase-high-mobility-group-box-1-pathway-targeted-by-hypaconitine-suppresses-the-apoptosis-of-endothelial-cells
#18
Ye Bai, Shaohui Du, Fei Li, Fengyuan Huang, Rudong Deng, Jianhong Zhou, Dongfeng Chen
Hypaconitine is an active component of Aconitum carmichaelii Debx, a Chinese medicinal herb for the treatment of cardiovascular diseases, but the mechanism underlying its effect remains elusive. In this study, we found that hypaconitine, rather than aconitum alkaloids in A. carmichaelii (e.g. aconitine, mesaconitine and benzoylaconitine), prevented endothelial cells from damage due to oxidized low-density lipoprotein (oxLDL) challenge. Cleaved caspase 3 expression in endothelial cells was up-regulated by oxLDL and markedly attenuated by hypaconitine, suggesting that hypaconitine inhibited the oxLDL-induced cell apoptosis...
March 2017: Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28056022/l-type-calcium-channel-inhibition-contributes-to-the-proarrhythmic-effects-of-aconitine-in-human-cardiomyocytes
#19
Jianjun Wu, Xiangchong Wang, Ying Ying Chung, Cai Hong Koh, Zhenfeng Liu, Huicai Guo, Qiang Yuan, Chuan Wang, Suwen Su, Heming Wei
Aconitine (ACO) is well-known for causing lethal ventricular tachyarrhythmias. While cardiac Na+ channel opening during repolarization has long been documented in animal cardiac myocytes, the cellular effects and mechanism of ACO in human remain unexplored. This study aimed to assess the proarrhythmic effects of ACO in human induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). ACO concentration-dependently (0.3 ~ 3.0 μM) shortened the action potentials (AP) durations (APD) in ventricular-like hiPSC-CMs by > 40% and induced delayed after-depolarization...
2017: PloS One
https://www.readbyqxmd.com/read/28051355/pharmacokinetic-interaction-of-aconitine-liquiritin-and-6-gingerol-in-a-traditional-chinese-herbal-formula-sini-decoction
#20
Sen Sun, Qingshan Chen, Jiyun Ge, Xiang Liu, Xinxia Wang, Qi Zhan, Hai Zhang, Guoqing Zhang
1. This study aimed to investigate the pharmacokinetic interaction of the three ingredients in a traditional Chinese herbal formulation, Sini Decoction, and provide evidence for its compatibility mechanism. 2. First, the effect of liquiritin and 6-gingerol on the pharmacokinetic parameters of aconitine was investigated in rats by using a sensitive and reliable LC-MS/MS method. Then the Caco-2 cell monolayer model and Rhodamine-123 uptake assay were used to investigate the effect of liquiritin and 6-gingerol on the absorption of aconitine and the activity of P-gp...
January 25, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
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