Aconitum(Ranunculaceae)has a long-standing history in traditional Chinese medicine(TCM),where it has been widely used to treat conditions such as rheumatoid arthritis(RA),myocardial infarction,and heart failure.Howeve...Aconitum(Ranunculaceae)has a long-standing history in traditional Chinese medicine(TCM),where it has been widely used to treat conditions such as rheumatoid arthritis(RA),myocardial infarction,and heart failure.However,the potency of Aconitum alkaloids,the primary active components of Aconitum,also confers substantial toxicity.Therefore,assessing the efficacy and toxicity of these Aconitum alkaloids is crucial for ensuring clinical effectiveness and safety.Metabolomics,a quantitative method for analyzing low-molecular-weight metabolites involved in metabolic pathways,provides a comprehensive view of the metabolic state across multiple systems in vivo.This approach has become a vital investigative tool for facilitating the evaluation of their efficacy and toxicity,identifying potential sensitive biomarkers,and offering a promising avenue for elucidating the pharmacological and toxicological mechanisms underlying TCM.This review focuses on the applications of metabolomics in pharmacological and toxicological studies of Aconitum alkaloids in recent years and highlights the significant role of metabolomics in exploring compatibility detoxification and the mechanisms of TCM processing,aiming to identify more viable methods for characterizing toxic medicinal plants.展开更多
Many herbal medicines have so far been utilized for the treatment of various ailments since the beginning of Chinese civilization. Aconitum is a botanical source for various pharmaceutically active components, which h...Many herbal medicines have so far been utilized for the treatment of various ailments since the beginning of Chinese civilization. Aconitum is a botanical source for various pharmaceutically active components, which has been commonly used in traditional Chinese medicine for thousands of years. Increasing interest in Aconitum pharmaceutical resources has led to further discoveries of diterpenoid alkaloids, polysaccharides, fiavonoids and many other compounds in various Aconitum species, and to investigations on their chemotaxonomy, molecular phylogeny and pharmacology. In continuation with our studies on Aconitum pharmacophylogeny, here we review the phytochemistry, chemotaxonomy, molecular biology and phylogeny of Aconitum and their relevance to therapeutic efficacy and toxicity. An exhaustive literature survey is used to summarize the global scientific effort in the phytochemical and biological studies of Aconitum. More diterpenoid alkaloids have been found in various Aconitum species, among which the aconitine type （type III） is predominant. The versatile bioactivities of alkaloids and extracts, as well as the bioactivities of polysaccharides and other ingredients, are summarized and discussed in this review. The morphology-based 11-series classification of section Aconitum, subgenus Aconitum, is not supported by chemotaxonomy and molecular phylogeny. Molecular phylogeny based on nuclear and chloroplast DNA sequences divided the nine morphologically similar series into two clusters, which is bolstered by the chemotaxonomic data. It is essential to integrate the emerging technologies into Aconitum studies for both the sustainable utilization of Aconitum pharmaceutical resources and finding novel compounds with potential clinical utility and less toxicity. Systems biology and omics technologies will play an increasingly important role in booming pharmaceutical research involving bioactive compounds of Aconitum.展开更多
[ Objective] The paper was to study the contact toxicity and antifeedant activity of Aconitum flavum against cabbage worm. [ Method ] In- sect dipping method was adopted to determine the contact toxicity of the extrac...[ Objective] The paper was to study the contact toxicity and antifeedant activity of Aconitum flavum against cabbage worm. [ Method ] In- sect dipping method was adopted to determine the contact toxicity of the extracts of A. fiavum extracted from five polar solvents including ethanol, petroleum ether, ether, ethyl acetate, n-butanol and water; leaf dish method was adopted to determine the antifeedant activities of five solvent ex- tracts including ethanol, petroleum ether, ether, ethyl acetate, n-butanol and water against cabbage worm, [ Result] Extracts of A. flavum had high contact toxicity against cabbage worm. When the concentration was 100.00 mg/ml, the corrected mortality at 48 h roached 97.24%, and the insec- ticidal activities of five solvent extracts against cabbage worm in sequence were water 〉 n-butanol 〉 ethyl acetate 〉 ether 〉 petroleum ether, the cor- rected mortality of water extract at 48 h was 95.87% ; the antifeedant activities of five solvent extracts in sequence were water 〉 n-butanol 〉 ethyl ac- etate 〉 ether 〉 petroleum ether. [ Conclusion] Extracts of A. flavum had strong contact toxicity and antifeedant activity against cabbage worm, and the active ingredients with contact toxicity and antifeedant activity might be a kind of polar compound.展开更多
Kiridine, a new C18-diterpenoid alkaloid, was isolated from the roots of Aconitum kirinense. Its structure was elucidated by MS, 1D- and 2D- NMR, and mono-crystal X-ray analysis. It is the first norditerpene alkaloid ...Kiridine, a new C18-diterpenoid alkaloid, was isolated from the roots of Aconitum kirinense. Its structure was elucidated by MS, 1D- and 2D- NMR, and mono-crystal X-ray analysis. It is the first norditerpene alkaloid containing a 9,14-methylenedioxy group and the substituent at C-14 is (-configuration.展开更多
The composition and antimicrobial activities of the essential oil of Aconitum tanguticum from the southern part of Gansu Province of China were investigated. The essential oil of aerial parts was obtained by hydrodist...The composition and antimicrobial activities of the essential oil of Aconitum tanguticum from the southern part of Gansu Province of China were investigated. The essential oil of aerial parts was obtained by hydrodistillation with a 0.7% （v/w） yield. The chemical composition of the essential oil was analyzed by gas chromatography-mass spectrometry （GC-MS） method. Thirty-five compounds were characterized in the oil, which were mainly monoterpenoids （41.7%） and sequiterpenoids （12.7%）. The main compounds in the oil were （-）-tran-pinecarvyl acetate （15.6%）, heptane （14.88%）, cineole （6.82%）, 3-pinanone （3.64%）, pinocamphone （3.34%）, cadinol （2.93%）, and cubenol （2.33%）. These compounds are identified for the first time in Aconitum tanguticum. The antimicrobial activities of the oil were evaluated against 9 bacteria strains, 1 yeast strain and 3 fungi strains using agar diffusion and broth microdilution methods. It showed strong inhibition against Fusarium semitectum and methicillin-resistant Staphlococcus aureus, low activity against Escheriehia eoli, but no effect against Epidermophyton floccosum. Its MIC values ranged from 0.125 5.000 mg/mL. Thirty-five compounds are newly identified in Aconitum tanguticum.展开更多
[Objective] The purpose of this study was to clarify the structure,growth pattern and histochemical localization of alkaloids in root system of Aconitum flavum Hand.-Mazz.[Method] Paraffin sectioning and histochemistr...[Objective] The purpose of this study was to clarify the structure,growth pattern and histochemical localization of alkaloids in root system of Aconitum flavum Hand.-Mazz.[Method] Paraffin sectioning and histochemistry were employed for performing the analysis in this study.[Result] The root system of Aconitum flavum Hand.-Mazz.consists of taproot,lateral root and adventitious root.The primary structure of root system is normal,but secondary structure shows abnormal.The cambium and the extra cambium of taproot form a ＂U＂-shaped secondary vascular bundle and tertiary bundle in abnormal secondary structure.The sieve tube group is made of little sieve tube group which is differentiated from primary phloem and cambium.Meanwhile,the secondary xylem in tuberous root also appears to be a ＂U＂ shape.Parenchyma cells of secondary phloem occupy most of the tuberous root.The sieve tube group of tuberous root is mainly differentiated from parenchyma cell of secondary phloem.[Conclusion] The difference in abnormal secondary structure of taproot and tuberous root are attributed to their varied cambium compose and activity pattern.Alkaloids are mainly accumulated in parenchyma cell of the inside cortex and between bundle in taproot,while parenchyma of secondary phloem and pith in tuberous root.展开更多
wo diterpene alkaloids, lepenine and kirinine A were isolated for the first time from the roots of Aconitum kirinense Nakai. Their structures have been established by IR, HRMS, NMR analysis and chemical reactions,...wo diterpene alkaloids, lepenine and kirinine A were isolated for the first time from the roots of Aconitum kirinense Nakai. Their structures have been established by IR, HRMS, NMR analysis and chemical reactions, and kininine A was found to be a new C 20 diterpene alkaloid.展开更多
According to folk usage of Aconitum carmichaelii Debx., the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx. as a new medicinal resource. Fourteen alkaloid...According to folk usage of Aconitum carmichaelii Debx., the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx. as a new medicinal resource. Fourteen alkaloids in mother roots, fibrous roots, stems, and leaves of Aconitum carmichaelii Debx. were measured by HPLC-MS/MS. And multivariate analysis methods, such as clustering analysis and principal component analysis, were applied to analyze the difference among various parts. In addition, the acute toxicity, analgesia, and anti-inflammatory tests were carried out. The results suggested that the contents of alkaloids in mother roots and fibrous roots were approximate, but those of leaves and stems were different from mother roots and fibrous roots. The results of the acute toxicity testing demonstrated the toxicity of fibrous root was strongest, and mother roots were slightly less toxic than fibrous roots. The stems and leaves were far less toxic than mother and fibrous roots. In addition, the analgesia and inflammatory tests showed the effects of the various tissues had no difference each other. These results provided a basis for developing new complementary and alternative treatments for rheumatoid arthritis patients. Simultaneously, the approach may also turn wastes into treasure and promote the development of circular economy.展开更多
According to the Chinese Pharmacopoeia 2015, only processed Aconitum tubers can be clinically applied, and the effect of processing is unclear. This research aimed to explore the effect of processing on cardiac effica...According to the Chinese Pharmacopoeia 2015, only processed Aconitum tubers can be clinically applied, and the effect of processing is unclear. This research aimed to explore the effect of processing on cardiac efficacy of alkaloids in Aconitum tubers. First, the chemical ingredients in unprocessed and processed Aconitum tubers were identified and compared by using high performance liquid chromatography time-of-flight mass spectrometry(HPLC-TOF/MS) and multivariate pattern recognition methods. Then the representative alkaloids in Aconitum tubers, aconitine, benzoylaconine, and aconine, which belong to diester-diterpenoid alkaloids,monoester-diterpenoid alkaloids, and amine-diterpenoid alkaloids, respectively, were selected for further validation of attenuated mechanism. Subsequent pharmacological experiments with aconitine, benzoylaconine,and aconine in SD rats were used to validate the effect of processing on cardiac functions. After processing the Aconitum tubers, it was found that the contents of diester-diterpenoid alkaloids were reduced, and those of monoester-diterpenoid alkaloids and amine-diterpenoid alkaloids were increased, suggesting that diesterditerpenoid alkaloids were transformed into monoester-diterpenoid alkaloids and amine-diterpenoid alkaloids.Through further decocting the aconitine in boiling water, it was confirmed that the three alkaloids could be progressively transformed. Pharmacological experiments with aconitine, benzoylaconine, and aconine in SD rats showed that aconitine at a dose of 0.01 mg/kg and aconine at a dose of 10 mg/kg enhanced the cardiac function, while benzoylaconine at a dose of 2 mg/kg weakened the cardiac function. The effect of processing is attributed to the transformation of the most toxic diester-diterpenoid alkaloids into less toxic monoesterditerpenoid alkaloids and amine-diterpenoid alkaloids.展开更多
The tubers and roots of Aconitum(Ranunculaceae)are widely used as heart medicine or analgesic agents for the treatment of coronary heart disease,chronic heart failure,rheumatoid arthritis and neuropathic pain since an...The tubers and roots of Aconitum(Ranunculaceae)are widely used as heart medicine or analgesic agents for the treatment of coronary heart disease,chronic heart failure,rheumatoid arthritis and neuropathic pain since ancient times.As a type of natural products mainly extracted from Aconitum plants,Aconitum alkaloids have complex chemical structures and exert remarkable biological activity,which are mainly responsible for significant effects of Aconitum plants.The present review is to summarize the progress of the pharmacological,toxicological,and pharmacokinetic studies of Aconitum alkaloids,so as to provide evidence for better clinical application.Research data concerning pharmacological,toxicological and pharmacokinetic studies of Aconitum alkaloids were collected from different scientific databases(PubMed,CNKI,Google Scholar,Baidu Scholar,and Web of Science)using the phrase Aconitum alkaloids,as well as generic synonyms.Aconitum alkaloids are both bioactive compounds and toxic ingredients in Aconitum plants.They produce a wide range of pharmacological activities,including protecting the cardiovascular system,nervous system,and immune system and anti-cancer effects.Notably,Aconitum alkaloids also exert strong cardiac toxicity,neurotoxicity and liver toxicity,which are supported by clinical studies.Finally,pharmacokinetic studies indicated that cytochrome P450 proteins(CYPs)and efflux transporters(ETs)are closely related to the low bioavailability of Aconitum alkaloids and play an important role in their metabolism and detoxification in vivo.展开更多
Two new norditerpenoid alkaloids, spicatine A (1) and spicatine B (2) were isolated from the root of Aconitum spicatum. The new compounds were deduced on the basis of their spectral data (IR, HREIMS, EIMS, 1D, 2D-NM...Two new norditerpenoid alkaloids, spicatine A (1) and spicatine B (2) were isolated from the root of Aconitum spicatum. The new compounds were deduced on the basis of their spectral data (IR, HREIMS, EIMS, 1D, 2D-NMR). This is the first whole report on the isolation of diterpenoid alkaloids from the A.spicatum Stapf.展开更多
In continuation of our studies on Aconitum hemsleyanum Pritz. var. pengzhouense, two new norditerpenoid alkaloids, pengshenines A (1) and B (2), have been isolated from the roots of the plants and their structures wer...In continuation of our studies on Aconitum hemsleyanum Pritz. var. pengzhouense, two new norditerpenoid alkaloids, pengshenines A (1) and B (2), have been isolated from the roots of the plants and their structures were elucidated by 1D- and 2D-NMR.展开更多
In the present study,we aimed to investigate the chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb. The isolation and purification of components were achieved by a series of chromatography, i...In the present study,we aimed to investigate the chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb. The isolation and purification of components were achieved by a series of chromatography, including silica gel, Sephadex LH-20 and HPLC. By using spectroscopic analysis, their structures were identified. Using PDE-4A as analgesic target, moleculardocking was conducted between isolated compounds by using Schrodinger software. Neoline is a typical non-ester diterpene alkaloid. It was studied by using the mouse torsion body method and hot plate method. A total of 12 diterpene alkaloids were obtainedand identified as Mesaconitine(1), Bewutine (2), Bewudine (3), Songoramine (4), Songorine (5), Neoline (6), Talasamine (7), isotalatizidine (8), Hokbusine A (9), Mesaconine (10), 8-OEt-14-benzoylmesaconine (11), 8-Methoxy-14-benzoyl-beiwutinine (12).Compounds 9 and 12 were isolated from Aconitum kusnezoffii Reichb. for the first time. Twelve diterpenealkaloids could act on the analgesic target. Neoline is a typical non-ester diterpene alkaloid. It had significant analgesic effect. Diterpene alkaloids were the main components of Aconitum kusnezoffiiReichb., and they had good analgesic activity.展开更多
Two new norditerpenoid alkaloids were isolated from the roots of Aconitum nagarum.Their structures were elucidated as 13-hydroxyfranchetine 1 and 10-dehydroxyflavaconitine 2,respectively, by 1D and 2D NMR experiments.
The chemical constituents from Aconitum richardsonianum var.pseudosessiliflorum were investigated.The roots of this plant were extracted three times with 90% EtOH at the room temperature.The ethanol extracts were comb...The chemical constituents from Aconitum richardsonianum var.pseudosessiliflorum were investigated.The roots of this plant were extracted three times with 90% EtOH at the room temperature.The ethanol extracts were combined and concentrated under reduced pressure to yield residue,which was suspended in water and successively partitioned with chloroform.The chloroform extraction was isolated and purified by silica gel and Sephadex LH-20 column chromatography.Six compounds were isolated and elucidated as delelatine（1）,isodelpheline（2）,3-acetylaconitine（3）,isoatisine（4）,nordhagenine A（5）and yunaconitine（6）.Compounds 1-5 were obtained from Aconitum Brunneum for the first time.Compound（1）showed significant cytotoxic activities（IC50=4.36 μM）against the human tumor cell line P388.展开更多
OBJEVTIVE: To investigate the effects of extracts from Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) on the excisional wound healing in a rat's model.METHODS: Rats were performed a surgical lesion w...OBJEVTIVE: To investigate the effects of extracts from Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) on the excisional wound healing in a rat's model.METHODS: Rats were performed a surgical lesion with a 2.0 cm resected tissue in the dorsal fascia.Following, animals were randomly divided into model group, YNB group and APE group those were respectively treated with saline, 1 mg/mL of Yunnan Baiyao and 1 mg/mL of Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) extracts. Wound contractions in days 0, 3, 7, 14 and 21 were calculated by an image analyzer. Histological analysis was analyzed using hematoxilin and eosin.Levels of tumor necrosis factor-2(IL-2), IL-4, IL-10, transformαin(TNF-g growα), interleukinth factor-1(TGF-nd basic fibroblast growth factor(bFββ1) a-GF) were determined by real-time quantitative PCR.RESULTS: Compared with that of YNB group and APE gtoup, the skin of rats showed poor re-modeling and re-epithelization characterized by a significant decrease of neovascularization, epithelialization and fibroblast in the model group. In the APE group, levels of TNF-α-and IL-2 were significantly down-regulated and IL4 and IL-10 significantly upregulated in contrasted with that of model group.In addition, levels of TGF-roup were significantly iβ1 and bFGF in the APE gnduced compared with that of model group.CONCLUSION: The results suggest that the extracts from Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) promote wound healing in the rats, which is associated with enhancing antiinflammatory ability and inducing fibroblast formation.展开更多
Diterpenoid alkaloids have neroprotective activity.Herein,three napelline-type diterpenoid alkaloids 1-3,two aconitine-type diterpenoid alkaloids 4-5,and one isoquinline-type alkaloid 6,as well as one lignan glycoside...Diterpenoid alkaloids have neroprotective activity.Herein,three napelline-type diterpenoid alkaloids 1-3,two aconitine-type diterpenoid alkaloids 4-5,and one isoquinline-type alkaloid 6,as well as one lignan glycoside 7,have been isolated from the roots of Aconitum pendulum Busch.Compounds 1 and 7 were new compounds,and their chemical structures were determined on the basis of nuclear magnetic resonance(NMR)spectra and mass spectrometry analysis.A ThT assay revealed that compound 2 showed significant disaggregation potency on the Aβ_(1−42)aggregates.展开更多
Further phytochemical investigation of the unique C 18-norditerpenoid alkaloids from the roots ofAconitum delavayi Franch led to the isolation of two new norditerpenoid alkaloids, delavaconitine F 1 and delavaconitine...Further phytochemical investigation of the unique C 18-norditerpenoid alkaloids from the roots ofAconitum delavayi Franch led to the isolation of two new norditerpenoid alkaloids, delavaconitine F 1 and delavaconitine G 2. Their structures were determined from spectroscopic evidence.展开更多
基金supported by the National Natural Science Foundation of China (No.82274223)。
文摘Aconitum(Ranunculaceae)has a long-standing history in traditional Chinese medicine(TCM),where it has been widely used to treat conditions such as rheumatoid arthritis(RA),myocardial infarction,and heart failure.However,the potency of Aconitum alkaloids,the primary active components of Aconitum,also confers substantial toxicity.Therefore,assessing the efficacy and toxicity of these Aconitum alkaloids is crucial for ensuring clinical effectiveness and safety.Metabolomics,a quantitative method for analyzing low-molecular-weight metabolites involved in metabolic pathways,provides a comprehensive view of the metabolic state across multiple systems in vivo.This approach has become a vital investigative tool for facilitating the evaluation of their efficacy and toxicity,identifying potential sensitive biomarkers,and offering a promising avenue for elucidating the pharmacological and toxicological mechanisms underlying TCM.This review focuses on the applications of metabolomics in pharmacological and toxicological studies of Aconitum alkaloids in recent years and highlights the significant role of metabolomics in exploring compatibility detoxification and the mechanisms of TCM processing,aiming to identify more viable methods for characterizing toxic medicinal plants.
基金Dalian Jiaotong University and Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine, Ministry of Science and Technology National Support Program (Grant No. 2012BAI29B01)
文摘Many herbal medicines have so far been utilized for the treatment of various ailments since the beginning of Chinese civilization. Aconitum is a botanical source for various pharmaceutically active components, which has been commonly used in traditional Chinese medicine for thousands of years. Increasing interest in Aconitum pharmaceutical resources has led to further discoveries of diterpenoid alkaloids, polysaccharides, fiavonoids and many other compounds in various Aconitum species, and to investigations on their chemotaxonomy, molecular phylogeny and pharmacology. In continuation with our studies on Aconitum pharmacophylogeny, here we review the phytochemistry, chemotaxonomy, molecular biology and phylogeny of Aconitum and their relevance to therapeutic efficacy and toxicity. An exhaustive literature survey is used to summarize the global scientific effort in the phytochemical and biological studies of Aconitum. More diterpenoid alkaloids have been found in various Aconitum species, among which the aconitine type （type III） is predominant. The versatile bioactivities of alkaloids and extracts, as well as the bioactivities of polysaccharides and other ingredients, are summarized and discussed in this review. The morphology-based 11-series classification of section Aconitum, subgenus Aconitum, is not supported by chemotaxonomy and molecular phylogeny. Molecular phylogeny based on nuclear and chloroplast DNA sequences divided the nine morphologically similar series into two clusters, which is bolstered by the chemotaxonomic data. It is essential to integrate the emerging technologies into Aconitum studies for both the sustainable utilization of Aconitum pharmaceutical resources and finding novel compounds with potential clinical utility and less toxicity. Systems biology and omics technologies will play an increasingly important role in booming pharmaceutical research involving bioactive compounds of Aconitum.
基金Supported by Scientific and Technological Projects of Ningxia Hui Autonomous Region(2008220)~~
文摘[ Objective] The paper was to study the contact toxicity and antifeedant activity of Aconitum flavum against cabbage worm. [ Method ] In- sect dipping method was adopted to determine the contact toxicity of the extracts of A. fiavum extracted from five polar solvents including ethanol, petroleum ether, ether, ethyl acetate, n-butanol and water; leaf dish method was adopted to determine the antifeedant activities of five solvent ex- tracts including ethanol, petroleum ether, ether, ethyl acetate, n-butanol and water against cabbage worm, [ Result] Extracts of A. flavum had high contact toxicity against cabbage worm. When the concentration was 100.00 mg/ml, the corrected mortality at 48 h roached 97.24%, and the insec- ticidal activities of five solvent extracts against cabbage worm in sequence were water 〉 n-butanol 〉 ethyl acetate 〉 ether 〉 petroleum ether, the cor- rected mortality of water extract at 48 h was 95.87% ; the antifeedant activities of five solvent extracts in sequence were water 〉 n-butanol 〉 ethyl ac- etate 〉 ether 〉 petroleum ether. [ Conclusion] Extracts of A. flavum had strong contact toxicity and antifeedant activity against cabbage worm, and the active ingredients with contact toxicity and antifeedant activity might be a kind of polar compound.
文摘Kiridine, a new C18-diterpenoid alkaloid, was isolated from the roots of Aconitum kirinense. Its structure was elucidated by MS, 1D- and 2D- NMR, and mono-crystal X-ray analysis. It is the first norditerpene alkaloid containing a 9,14-methylenedioxy group and the substituent at C-14 is (-configuration.
基金National Natural Science Foundation of China(Grant No.30471133).
文摘The composition and antimicrobial activities of the essential oil of Aconitum tanguticum from the southern part of Gansu Province of China were investigated. The essential oil of aerial parts was obtained by hydrodistillation with a 0.7% （v/w） yield. The chemical composition of the essential oil was analyzed by gas chromatography-mass spectrometry （GC-MS） method. Thirty-five compounds were characterized in the oil, which were mainly monoterpenoids （41.7%） and sequiterpenoids （12.7%）. The main compounds in the oil were （-）-tran-pinecarvyl acetate （15.6%）, heptane （14.88%）, cineole （6.82%）, 3-pinanone （3.64%）, pinocamphone （3.34%）, cadinol （2.93%）, and cubenol （2.33%）. These compounds are identified for the first time in Aconitum tanguticum. The antimicrobial activities of the oil were evaluated against 9 bacteria strains, 1 yeast strain and 3 fungi strains using agar diffusion and broth microdilution methods. It showed strong inhibition against Fusarium semitectum and methicillin-resistant Staphlococcus aureus, low activity against Escheriehia eoli, but no effect against Epidermophyton floccosum. Its MIC values ranged from 0.125 5.000 mg/mL. Thirty-five compounds are newly identified in Aconitum tanguticum.
基金Supported by Natural Science Foundation of Ningxia Hui Autonomous Region(NZ0932)National Key Technology R & D Program of China(20068AI06A15-11)~~
文摘[Objective] The purpose of this study was to clarify the structure,growth pattern and histochemical localization of alkaloids in root system of Aconitum flavum Hand.-Mazz.[Method] Paraffin sectioning and histochemistry were employed for performing the analysis in this study.[Result] The root system of Aconitum flavum Hand.-Mazz.consists of taproot,lateral root and adventitious root.The primary structure of root system is normal,but secondary structure shows abnormal.The cambium and the extra cambium of taproot form a ＂U＂-shaped secondary vascular bundle and tertiary bundle in abnormal secondary structure.The sieve tube group is made of little sieve tube group which is differentiated from primary phloem and cambium.Meanwhile,the secondary xylem in tuberous root also appears to be a ＂U＂ shape.Parenchyma cells of secondary phloem occupy most of the tuberous root.The sieve tube group of tuberous root is mainly differentiated from parenchyma cell of secondary phloem.[Conclusion] The difference in abnormal secondary structure of taproot and tuberous root are attributed to their varied cambium compose and activity pattern.Alkaloids are mainly accumulated in parenchyma cell of the inside cortex and between bundle in taproot,while parenchyma of secondary phloem and pith in tuberous root.
文摘wo diterpene alkaloids, lepenine and kirinine A were isolated for the first time from the roots of Aconitum kirinense Nakai. Their structures have been established by IR, HRMS, NMR analysis and chemical reactions, and kininine A was found to be a new C 20 diterpene alkaloid.
基金supported by the Sichuan Provincial Administration of Traditional Chinese Medicine Research Project(No.2018NQ008)
文摘According to folk usage of Aconitum carmichaelii Debx., the present study was designed to determine the feasibility of the stems and leaves of Aconitum carmichaelii Debx. as a new medicinal resource. Fourteen alkaloids in mother roots, fibrous roots, stems, and leaves of Aconitum carmichaelii Debx. were measured by HPLC-MS/MS. And multivariate analysis methods, such as clustering analysis and principal component analysis, were applied to analyze the difference among various parts. In addition, the acute toxicity, analgesia, and anti-inflammatory tests were carried out. The results suggested that the contents of alkaloids in mother roots and fibrous roots were approximate, but those of leaves and stems were different from mother roots and fibrous roots. The results of the acute toxicity testing demonstrated the toxicity of fibrous root was strongest, and mother roots were slightly less toxic than fibrous roots. The stems and leaves were far less toxic than mother and fibrous roots. In addition, the analgesia and inflammatory tests showed the effects of the various tissues had no difference each other. These results provided a basis for developing new complementary and alternative treatments for rheumatoid arthritis patients. Simultaneously, the approach may also turn wastes into treasure and promote the development of circular economy.
基金financially supported by the National Natural Science Foundation of China (81573396)Military Innovation Funding (16CXZ012)
文摘According to the Chinese Pharmacopoeia 2015, only processed Aconitum tubers can be clinically applied, and the effect of processing is unclear. This research aimed to explore the effect of processing on cardiac efficacy of alkaloids in Aconitum tubers. First, the chemical ingredients in unprocessed and processed Aconitum tubers were identified and compared by using high performance liquid chromatography time-of-flight mass spectrometry(HPLC-TOF/MS) and multivariate pattern recognition methods. Then the representative alkaloids in Aconitum tubers, aconitine, benzoylaconine, and aconine, which belong to diester-diterpenoid alkaloids,monoester-diterpenoid alkaloids, and amine-diterpenoid alkaloids, respectively, were selected for further validation of attenuated mechanism. Subsequent pharmacological experiments with aconitine, benzoylaconine,and aconine in SD rats were used to validate the effect of processing on cardiac functions. After processing the Aconitum tubers, it was found that the contents of diester-diterpenoid alkaloids were reduced, and those of monoester-diterpenoid alkaloids and amine-diterpenoid alkaloids were increased, suggesting that diesterditerpenoid alkaloids were transformed into monoester-diterpenoid alkaloids and amine-diterpenoid alkaloids.Through further decocting the aconitine in boiling water, it was confirmed that the three alkaloids could be progressively transformed. Pharmacological experiments with aconitine, benzoylaconine, and aconine in SD rats showed that aconitine at a dose of 0.01 mg/kg and aconine at a dose of 10 mg/kg enhanced the cardiac function, while benzoylaconine at a dose of 2 mg/kg weakened the cardiac function. The effect of processing is attributed to the transformation of the most toxic diester-diterpenoid alkaloids into less toxic monoesterditerpenoid alkaloids and amine-diterpenoid alkaloids.
基金supported by the National Natural Science Foundation of China(No.81673592).
文摘The tubers and roots of Aconitum(Ranunculaceae)are widely used as heart medicine or analgesic agents for the treatment of coronary heart disease,chronic heart failure,rheumatoid arthritis and neuropathic pain since ancient times.As a type of natural products mainly extracted from Aconitum plants,Aconitum alkaloids have complex chemical structures and exert remarkable biological activity,which are mainly responsible for significant effects of Aconitum plants.The present review is to summarize the progress of the pharmacological,toxicological,and pharmacokinetic studies of Aconitum alkaloids,so as to provide evidence for better clinical application.Research data concerning pharmacological,toxicological and pharmacokinetic studies of Aconitum alkaloids were collected from different scientific databases(PubMed,CNKI,Google Scholar,Baidu Scholar,and Web of Science)using the phrase Aconitum alkaloids,as well as generic synonyms.Aconitum alkaloids are both bioactive compounds and toxic ingredients in Aconitum plants.They produce a wide range of pharmacological activities,including protecting the cardiovascular system,nervous system,and immune system and anti-cancer effects.Notably,Aconitum alkaloids also exert strong cardiac toxicity,neurotoxicity and liver toxicity,which are supported by clinical studies.Finally,pharmacokinetic studies indicated that cytochrome P450 proteins(CYPs)and efflux transporters(ETs)are closely related to the low bioavailability of Aconitum alkaloids and play an important role in their metabolism and detoxification in vivo.
文摘Two new norditerpenoid alkaloids, spicatine A (1) and spicatine B (2) were isolated from the root of Aconitum spicatum. The new compounds were deduced on the basis of their spectral data (IR, HREIMS, EIMS, 1D, 2D-NMR). This is the first whole report on the isolation of diterpenoid alkaloids from the A.spicatum Stapf.
文摘In continuation of our studies on Aconitum hemsleyanum Pritz. var. pengzhouense, two new norditerpenoid alkaloids, pengshenines A (1) and B (2), have been isolated from the roots of the plants and their structures were elucidated by 1D- and 2D-NMR.
基金National Natural Science Foundation of China(Grant No.30973628)the National Science and Technology Major Project of China(Grant No.SQ2018ZX090301)
文摘In the present study,we aimed to investigate the chemical constituents and analgesic activity of Aconitum kusnezoffii Reichb. The isolation and purification of components were achieved by a series of chromatography, including silica gel, Sephadex LH-20 and HPLC. By using spectroscopic analysis, their structures were identified. Using PDE-4A as analgesic target, moleculardocking was conducted between isolated compounds by using Schrodinger software. Neoline is a typical non-ester diterpene alkaloid. It was studied by using the mouse torsion body method and hot plate method. A total of 12 diterpene alkaloids were obtainedand identified as Mesaconitine(1), Bewutine (2), Bewudine (3), Songoramine (4), Songorine (5), Neoline (6), Talasamine (7), isotalatizidine (8), Hokbusine A (9), Mesaconine (10), 8-OEt-14-benzoylmesaconine (11), 8-Methoxy-14-benzoyl-beiwutinine (12).Compounds 9 and 12 were isolated from Aconitum kusnezoffii Reichb. for the first time. Twelve diterpenealkaloids could act on the analgesic target. Neoline is a typical non-ester diterpene alkaloid. It had significant analgesic effect. Diterpene alkaloids were the main components of Aconitum kusnezoffiiReichb., and they had good analgesic activity.
文摘Two new norditerpenoid alkaloids were isolated from the roots of Aconitum nagarum.Their structures were elucidated as 13-hydroxyfranchetine 1 and 10-dehydroxyflavaconitine 2,respectively, by 1D and 2D NMR experiments.
基金financially supported by the Scientific Research Program Funded by Shaanxi Provincial Department(2010JK74909JK672)+1 种基金by the Special Research Fund for the Doctoral Program of Higher Education(20096118110008)the Natural Science Foundation of Shaanxi Province(SJ08B16)
文摘The chemical constituents from Aconitum richardsonianum var.pseudosessiliflorum were investigated.The roots of this plant were extracted three times with 90% EtOH at the room temperature.The ethanol extracts were combined and concentrated under reduced pressure to yield residue,which was suspended in water and successively partitioned with chloroform.The chloroform extraction was isolated and purified by silica gel and Sephadex LH-20 column chromatography.Six compounds were isolated and elucidated as delelatine（1）,isodelpheline（2）,3-acetylaconitine（3）,isoatisine（4）,nordhagenine A（5）and yunaconitine（6）.Compounds 1-5 were obtained from Aconitum Brunneum for the first time.Compound（1）showed significant cytotoxic activities（IC50=4.36 μM）against the human tumor cell line P388.
基金the Natural Science Foundation of Henan:Study of Combination Chuanwu(Aconitum Carmichaelii)and Banxia(Rhizoma Pinelliae)(No.18A330004)
文摘OBJEVTIVE: To investigate the effects of extracts from Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) on the excisional wound healing in a rat's model.METHODS: Rats were performed a surgical lesion with a 2.0 cm resected tissue in the dorsal fascia.Following, animals were randomly divided into model group, YNB group and APE group those were respectively treated with saline, 1 mg/mL of Yunnan Baiyao and 1 mg/mL of Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) extracts. Wound contractions in days 0, 3, 7, 14 and 21 were calculated by an image analyzer. Histological analysis was analyzed using hematoxilin and eosin.Levels of tumor necrosis factor-2(IL-2), IL-4, IL-10, transformαin(TNF-g growα), interleukinth factor-1(TGF-nd basic fibroblast growth factor(bFββ1) a-GF) were determined by real-time quantitative PCR.RESULTS: Compared with that of YNB group and APE gtoup, the skin of rats showed poor re-modeling and re-epithelization characterized by a significant decrease of neovascularization, epithelialization and fibroblast in the model group. In the APE group, levels of TNF-α-and IL-2 were significantly down-regulated and IL4 and IL-10 significantly upregulated in contrasted with that of model group.In addition, levels of TGF-roup were significantly iβ1 and bFGF in the APE gnduced compared with that of model group.CONCLUSION: The results suggest that the extracts from Chuanwu(Aconitum Carmichaelii) and Banxia(Rhizoma Pinelliae) promote wound healing in the rats, which is associated with enhancing antiinflammatory ability and inducing fibroblast formation.
基金This work was financially supported by National Natural Science Foundation of China(Nos.81673325 and 81711540311)the International Partnership Program of CAS(No.153631KYSB20160004)+1 种基金Gansu Province Key International S&T Cooperation Project(No.18YF1WA127)CAS Pioneer Hundred Talents Program.
文摘Diterpenoid alkaloids have neroprotective activity.Herein,three napelline-type diterpenoid alkaloids 1-3,two aconitine-type diterpenoid alkaloids 4-5,and one isoquinline-type alkaloid 6,as well as one lignan glycoside 7,have been isolated from the roots of Aconitum pendulum Busch.Compounds 1 and 7 were new compounds,and their chemical structures were determined on the basis of nuclear magnetic resonance(NMR)spectra and mass spectrometry analysis.A ThT assay revealed that compound 2 showed significant disaggregation potency on the Aβ_(1−42)aggregates.
基金the National Natural Science Foundation of China （No. 90409015）.
文摘Further phytochemical investigation of the unique C 18-norditerpenoid alkaloids from the roots ofAconitum delavayi Franch led to the isolation of two new norditerpenoid alkaloids, delavaconitine F 1 and delavaconitine G 2. Their structures were determined from spectroscopic evidence.
