Chapter 3 Distribution of Alkaloids in Traditional Chinese Medicinal Plants

Han, Gui-Qiu; Chen, Ya-Yan; Liang, Xiao‐Tian

doi:10.1016/s0099-9598(08)60217-5

Cited by 9 publications

(6 citation statements)

References 7 publications

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“…In the present study, we have examined the action of the aconitine derivative 3-acetylaconitine, the main alkaloid of the Chinese plant Aconitum flavum, that is employed as analgesic and antirheumatic in traditional Chinese folk medicine (Bisset 1981;Tang et al 1984;Han et al 1988). The analgesic action of this compound is not antagonized by naloxone suggesting that opioid receptors are not involved (Tang et al 1986).…”

Section: Introductionmentioning

confidence: 99%

Inhibition of rat hippocampal excitability by the plant alkaloid 3-acetylaconitine mediated by interaction with voltage-dependent sodium channels

Ameri

1997

Naunyn-Schmiedeberg's Arch Pharmacol

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The effects of the Aconitum alkaloid 3-acetylaconitine on neuronal activity were investigated in the slice preparation and on cultivated neurons of rat hippocampus by extracellular and patch-clamp recordings, respectively. 3-Acetylaconitine (0.01-1 microM) diminished the orthodromic and antidromic population spike in a concentration-dependent manner. The inhibitory action of the drug was preceded by a transiently enhanced excitability. The latency of onset of the inhibition was accelerated by increased stimulation frequency, whereas recovery during washout of the alkaloid was accelerated by decreased stimulation frequency. Moreover, the inhibitory effect of 3-acetylaconitine was evaluated in two different models of epileptiform activity induced either by blockade of GABA receptors by bicuculline (10 microM) or by a nominal Mg(2+)-free bathing medium. In accordance with the activity-dependent mode of action, this compound abolished the synaptically evoked population spikes in the presence of bicuculline or nominal Mg(2+)-free bathing medium, respectively. Whole-cell patch-clamp recordings revealed an interaction of 3-acetylaconitine with the voltage-dependent sodium channel. At a concentration of 1 microM, 3-acetylaconitine did not affect the peak amplitude of the sodium current, but shifted the current-voltage relationship in the hyperpolarized direction such that sodium currents were already activated at the resting potential.

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Section: Introductionmentioning

confidence: 99%

Inhibition of rat hippocampal excitability by the plant alkaloid 3-acetylaconitine mediated by interaction with voltage-dependent sodium channels

Ameri

1997

Naunyn-Schmiedeberg's Arch Pharmacol

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“…14-Benzoyltalitasamine and talitasamine (both purchased from O. Krishtal, Bogomoletz Institute, Kiev, Ukraine) were isolated by extraction of powdered roots from Aconitum nemorum and Aconitum talassicum, respectively followed by chromatography on an aluminium oxide column (Han and Chen 1988). For the present experiments, the alkaloids were dissolved in dimethylsulfoxide (DMSO) to give stock solutions of 10 or 100 µM.…”

Section: Methodsmentioning

confidence: 99%

Structure-dependent inhibitory action of the Aconitum alkaloids 14-benzoyltalitasamine and talitasamine in rat hippocampal slices

Ameri

1998

Naunyn-Schmiedeberg's Arch Pharmacol

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In the present study the effects of the two Aconitum alkaloids 14-benzoyltalitasamine and talitasamine on neuronal activity were investigated in order to obtain further insight into structure-dependent effects of this group of alkaloids on central nervous activity. Both alkaloids are closely related to aconitine, the main alkaloid of plants of Aconitum species. However, they have shortened side chains at position C3 and C8 of the molecule. The experiments were performed as extracellular recordings of orthodromically and antidromically evoked population spikes as well as of field excitatory potentials (EPSPs) from the CA1 region of rat hippocampal slices. 14-Benzoyltalitasamine exerted a reversible inhibition of the field potentials in a concentration-dependent manner. The orthodromic population spike was attenuated at concentrations higher than 1 microM, while the field EPSP was already affected at a concentration of at least 0.3 microM. Both responses were completely blocked at a concentration of 30 microM. The alkaloid failed to affect the presynaptic fiber spike at concentrations less than 10 microM. There was only a up to 30% decrease in the antidromic population spike (10-100 microM). The inhibition of the antidromic spike was increased by using a higher stimulus frequency. In contrast to 14-benzoyltalitasamine, the alkaloid talitasamine which is lacking the benzoylester side chain was a less effective inhibitor of the orthodromic population spike and even failed to affect the antidromic spike. Furthermore, the effects of the alkaloids on experimentally induced epileptiform activity was examined. While talitasamine was lacking any significant effect at concentrations less than 100 microM, 14-benzoyltalitasamine reversibly reduced both stimulus-triggered epileptiform activity in area CA1 elicited by omission of Mg2+ from the bathing medium as well as spontaneously occurring epileptiform activity in CA3 elicited by omission of Mg2+ and elevation of K+ to 5 or 8 mM. The antiepileptiform efficacy of this compound was concentration-dependent (0.3-10 microM) and manifested itself as a decrease in burst frequency as well as in burst amplitude and was significantly increased by the higher K+ concentration.

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“…Although its clinically therapeutic mechanism remains obscure, 1) the extracts of Aconitum plants are widely used in clinic in China and other East Asian countries 2) owing to the good eŠect against pain and in‰ammations. 3,4) Additionally, in in vitro tests in the human tumor cell lines of the National Cancer Institute, USA, the IC50 value of aconitine (NSC 56464) in the SNB-75 cell line that originated from a central nervous system tumor, was less than 100 mM, therefore warranting further investigations on its applications in the treatment of cancer. Aconitine is currently commercially available in various pharmaceutical forms, such as injections, capsules, etc.…”

Section: Introductionmentioning

confidence: 99%

Crystalline Drug Aconitine-loaded Poly(d,l-Lactide-CoGlycolide) Nanoparticles: Preparation and <i>in Vitro</i> Release

Xiang

et al. 2010

YAKUGAKU ZASSHI

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This paper reports both the optimization of aconitine entrapment and its release from biodegradable poly(d,l-lactide-coglycolide) (PLGA) nanoparticles prepared using the O/W single-emulsion/solvent-evaporation technique. The in‰uence of several parameters, such as the initial aconitine mass, aqueous-phase pH, volume ratio of aqueous/organic phase (W/O), PLGA concentration in the organic phase, etc., on aconitine encapsulation were investigated. The optimized nanoparticles had an entrapment e‹ciency of 88.40±3.02％ with drug loading capacity of 9.42±2.93％. Crystallization growth, which played a crucial role in hindering the incorporation of aconitine into the polymer carrier, was proposed. DiŠerential scanning calorimetry and X-ray powder diŠraction demonstrated that aconitine existed in an amorphous state or as a solid solution in the polymeric matrix. The in vitro release proˆles exhibited a sustained release of aconitine from nanoparticles and a pH-dependent character in phosphate-buŠered saline with diŠerent pH values. Moreover, aconitine-loaded PLGA nanoparticles could lead to improvement in the stability of aconitine. This work demonstrated the feasibility of encapsulating aconitine into PLGA nanoparticles using the O/W single-emulsion/solvent-evaporation technique.

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Chapter 3 Distribution of Alkaloids in Traditional Chinese Medicinal Plants

Cited by 9 publications

References 7 publications

Inhibition of rat hippocampal excitability by the plant alkaloid 3-acetylaconitine mediated by interaction with voltage-dependent sodium channels

Inhibition of rat hippocampal excitability by the plant alkaloid 3-acetylaconitine mediated by interaction with voltage-dependent sodium channels

Structure-dependent inhibitory action of the Aconitum alkaloids 14-benzoyltalitasamine and talitasamine in rat hippocampal slices

Crystalline Drug Aconitine-loaded Poly(d,l-Lactide-CoGlycolide) Nanoparticles: Preparation and <i>in Vitro</i> Release

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