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1.
Food Chem ; 317: 126377, 2020 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-32113137

RESUMO

Ligusticum chuanxiong extract-polylactic acid sustained-release microspheres (LCE-PLA) are fabricated in this study for enhancing both duration and hepatoprotective efficacy of the main bioactive ingredients. LCE-PLA in vitro release, cytotoxicity and in vivo hepatoprotective effect were discussed to evaluate its efficiency and functionality. Results demonstrated that the optimal drug-loading rate and encapsulation efficiency of tetramethylpyrazine (TMP, the main active ingredient) were 8.19%, 83.72%, respectively. The LCE-PLA in vitro release of TMP showed prolong 5-fold and in vitro cytotoxicity declined 25.00% compared with naked LCE. After 6 weeks of in vivo intervention in high fat diet mice, both liver aspartate aminotransferase and alanine aminotransferase levels were higher in LCE-PLA group than LCE group. The above results indicated that TMP had a higher bioavailability of hepatoprotection when encapsulation of LCE-PLA was applied. The current study has provided a promising novel way to enhance the efficacy of short half-life ingredients.


Assuntos
Ligusticum/química , Extratos Vegetais/química , Poliésteres/química , Pirazinas/administração & dosagem , Pirazinas/farmacocinética , Animais , Preparações de Ação Retardada , Meia-Vida , Células Hep G2 , Humanos , Fígado/efeitos dos fármacos , Masculino , Camundongos , Microesferas
2.
Sci Rep ; 10(1): 3689, 2020 02 28.
Artigo em Inglês | MEDLINE | ID: mdl-32111871

RESUMO

The root of Paeonia lactiflora Pall. (Chishao, CS) and Ligusticum chuanxiong Hort. (Chuanxiong, CX) were widely used as a drug pair in Chinese Medicine, and the combination of CS and CX showed a more significant inhibition on neuronal apoptosis in our previous study. In the present study, total paeony glycosides (TPGs) from CS and total ligustici phenolic acids (TLPAs) from CX were combined to evaluate the synergistic effects against focal cerebral ischemia both in vitro and in vivo. The combination of TPGs and TLPAs at 7:3 had the best anti-oxidative stress and anti-inflammatory effect on OGD-induced HUVEC. Additionally, the infarction area proportion and neuron apoptosis of rats by TPGs:TLPAs (7:3) was significantly lower than their alone in MCAO rats. Moreover, TPGs: TLPAs of 7:3 showed a more significant effect on decreasing the expression of MMP-2 and MMP-9, and increasing the protein expression or mRNA level of TIMP-1 than other combinations. The optimal ratio of TPGs and TLPAs at 7:3 could bring more remarkable protective effects against focal cerebral ischemia in MCAO rats by alleviating oxidative stress, inflammatory and neuronal apoptosis to protect the blood-brain barrier. Overall, the present study provided benefical evidence for clinical application of CS and CX as a "drug pair".


Assuntos
Isquemia Encefálica , Glicosídeos/farmacologia , Células Endoteliais da Veia Umbilical Humana/metabolismo , Hidroxibenzoatos/farmacologia , Ligusticum/química , Estresse Oxidativo/efeitos dos fármacos , Paeonia/química , Raízes de Plantas/química , Animais , Isquemia Encefálica/tratamento farmacológico , Isquemia Encefálica/metabolismo , Isquemia Encefálica/patologia , Glicosídeos/química , Células Endoteliais da Veia Umbilical Humana/patologia , Humanos , Hidroxibenzoatos/química , Masculino , Ratos , Ratos Sprague-Dawley
3.
Am J Chin Med ; 48(1): 1-16, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32054304

RESUMO

Pain is an unpleasant sensory and emotional experience in many diseases and is often caused by intense or damaging stimuli. Pain negatively affects the quality of life and increases high health expenditures. Drugs with analgesic properties are commonly used to relieve pain, but these Western medications could be overwhelmed by side effects including tolerance and addiction. Herbal medicines may provide alternative measures for pain management. In this review paper, after introduction of Chinese medicine theory and treatment modality, emphasis is placed on the application of Chinese herbs and herbal formulations in pain management. Three of the most commonly used herbs, i.e., Corydalis yanhusuo, Ligusticum chuanxiong, and Aconitum carmichaeli, are reviewed. Subsequently, using this ancient medical remedy, Chinese herbal formulation in treating common medical conditions associated with pain, such as headache/migraine, chest pain, abdominal pain, low back pain, neuropathic pain, osteoarthritis, and cancer pain, is presented. Chinese herbal medicines could be considered as a complementary and integrative approach in the modern armamentarium in combating pain.


Assuntos
Medicamentos de Ervas Chinesas/uso terapêutico , Manejo da Dor/métodos , Dor/tratamento farmacológico , Aconitum/química , Corydalis/química , Humanos , Ligusticum/química , Medicina Tradicional Chinesa , Estrutura Molecular , Qualidade de Vida
4.
J Ethnopharmacol ; 249: 112385, 2020 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-31730888

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cerebral ischemia, also known as stroke, can stimulate the proliferation and migration of endogenous neural stem cells (NSCS) in subventricular zone of the lateral ventricle and subgranularzone of the dentate gyrus in the adult hippocampus as a defense response to damage. However, the proliferation of endogenous NSCS is insufficient for central nervous system repair. Neurogenesis and anti-neuroinflammation are two important aspects for neuroprotection. Rhizome Ligusticum chuanxiong (LC), the dried rhizomes of Ligusticum striatum DC., has been widely used to treat stroke for over hundreds of years in Traditional Chinese Medicine. PURPOSE: of the study: Previous reports on pharmacological mechanism of LC mainly focus on the cerebral blood flow and thrombolysis. We aim to explore whether LC provides neuroprotective effect by increasing neurogenesis and inhibiting the IL-1ß, TNF-α and expressions of glial fibrillary acidic protein. MATERIALS AND METHODS: LC extract was delivered to microsphere-embolized (ME) cerebral ischemia Wister rats to examine its neuroprotection. Body weight, neurological scores, hematoxylin-eosin staining (HE), TUNEL assay were conducted for neurological damage. Neurogenesis was evaluated by assessing the expression of Doublecortin (DCX) and neurogenic differentiation1 (NeuroD1) through immunofluorescence staining. Western blot performed to measure the protein levels of growth associated protein-43(GAP-43), glial fibrillary acidic protein (GFAP). IL-1ß and TNF-α was detected by Elisa. RESULTS: LC alleviated pathomorphological change and apoptosis of neurons in the hippocampus caused by ME surgery. Furthermore, LC significantly increased the DCX in the DG of adult rat hippocampus at 14 days after surgery. A significant upregulation of GAP-43 compared to the ME after LC was administered. Besides, LC decreased pro-inflammatory cytokine (IL-1ß, TNF-α) and protein level of GFAP. CONCLUSION: The finding suggested that LC had the ability to protect neurons by promoting the endogenous proliferation of neuroblast and production of neural differentiation factor in rats after ischemia injury. Meanwhile, LC can anti-neuroinflammation, which is important for the treatment of neuron injury. Accordingly, LC perhaps a promising medicine for neuron damage therapy after cerebral ischemia.


Assuntos
Isquemia Encefálica/prevenção & controle , Ligusticum/química , Fármacos Neuroprotetores/farmacologia , Acidente Vascular Cerebral/prevenção & controle , Animais , Apoptose/efeitos dos fármacos , Modelos Animais de Doenças , Hipocampo/efeitos dos fármacos , Hipocampo/patologia , Inflamação/prevenção & controle , Masculino , Microesferas , Células-Tronco Neurais/metabolismo , Neurogênese/efeitos dos fármacos , Neurônios/efeitos dos fármacos , Neurônios/patologia , Ratos , Ratos Wistar
5.
J Chromatogr A ; 1616: 460755, 2020 Apr 12.
Artigo em Inglês | MEDLINE | ID: mdl-31812274

RESUMO

Ultra-performance convergence chromatography (UPC2), which combines the advantages of both reversed phase liquid chromatography (RPLC) and gas chromatograph (GC), is a novel, eco-friendly analytical method and could be a powerful supplement for RPLC and GC. Based on these characteristics, an UPC2 method was developed for the chemical analysis of Gaoben medicinal materials including six batches of Ligusticum sinense, six batches of Ligusticum jeholense and six batches of Conioselinum vaginatum and compared with the results by ultra-performance liquid chromatography (UPLC) method at the same time. Six compounds were determined by UPC2 method, and eight compounds were quantitatively analyzed by UPLC method. Hierarchical cluster analysis (HCA) and principle component analysis (PCA) methods were used to elucidate the resemblance relationship among these 18 samples. The results showed the samples from same species analyzed by UPC2 method were grouped together respectively. However, UPLC method could not distinguish these three kinds of Gaoben medicinal materials effectively. The compounds determined by UPC2 method showed the chemical taxonomic significance than those of UPLC method, and were more suitable for chemical quality evaluation of Gaoben medicinal materials from different regions. This showed good complementarity between UPC2 and UPLC methods. And the UPC2 method might provide a more efficient analytical method for the chemical quality evaluation of medicinal materials rich in volatile oils, which would be a powerful supplement to the current quality evaluation.


Assuntos
Química Farmacêutica/métodos , Cromatografia Líquida de Alta Pressão/normas , Cromatografia Líquida/normas , Medicamentos de Ervas Chinesas , Química Farmacêutica/instrumentação , Análise por Conglomerados , Medicamentos de Ervas Chinesas/química , Ligusticum/química , Análise de Componente Principal
6.
J Pharm Biomed Anal ; 177: 112885, 2020 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-31563759

RESUMO

Tianma pills, a traditional formula made from Ligusticum chuanxiong and Gastrodia elata, are efficacious for the treatment of primary headache. Tetramethylpyrazine (TMP) and Ferulic acid (FA) are the bioactive ingredients of Ligusticum chuanxiong, while Gastrodin and Gastrodigenin are the bioactive ingredients of Gastrodia elata. Pharmacokinetic assessment of TMP, FA, gastrodin or gastrodigenin in blood or brain interstitial fluid (BIF) has been reported in healthy animals. However, the pharmacokinetic properties of TMP and FA have not been studied when they are co-administered in a blood-stasis migraine model. The present research investigated the pharmacokinetic behavior of TMP and FA after oral administration in the presence of different concentrations of gastrodin and gastrodigenin in a blood-stasis migraine model. Pharmacokinetic parameters were determined using blood-brain microdialysis in combination with the UHPLC-MS method. Compared to the control group, in which TMP and FA were administrated without gastrodin or gastrodigenin, the T1/2, MRT, Cmax and AUC0-∞ of TMP and FA were increased. These results indicate that varying concentrations of gastrodin and gastrodigenin play an important role in affecting the pharmacokinetics of TMP and FA. Low concentrations of gastrodin and gastrodigenin (similar to those found in Tianma pills) were more efficacious, validating the utility of the ancient formulation.


Assuntos
Barreira Hematoencefálica/metabolismo , Medicamentos de Ervas Chinesas/farmacocinética , Gastrodia/química , Ligusticum/química , Transtornos de Enxaqueca/tratamento farmacológico , Administração Oral , Animais , Álcoois Benzílicos/administração & dosagem , Álcoois Benzílicos/farmacocinética , Barreira Hematoencefálica/química , Barreira Hematoencefálica/citologia , Temperatura Baixa/efeitos adversos , Ácidos Cumáricos/administração & dosagem , Ácidos Cumáricos/farmacocinética , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Interações Medicamentosas , Medicamentos de Ervas Chinesas/administração & dosagem , Medicamentos de Ervas Chinesas/química , Líquido Extracelular/química , Glucosídeos/administração & dosagem , Glucosídeos/farmacocinética , Humanos , Masculino , Microdiálise , Transtornos de Enxaqueca/sangue , Transtornos de Enxaqueca/etiologia , Permeabilidade , Pirazinas/administração & dosagem , Pirazinas/farmacocinética , Ratos , Organismos Livres de Patógenos Específicos , Vasoconstrição/efeitos dos fármacos
7.
Zhongguo Zhong Yao Za Zhi ; 44(15): 3275-3280, 2019 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-31602883

RESUMO

The method of classifying the quality grade of traditional Chinese medicine slices with cross section model quality constant was applied to the grade evaluation of Ligusticum chuanxiong pieces,and a reasonable grade standard of L. chuanxiong pieces was established. The purpose is to classify the 15 batches of L. chuanxiong pieces by combining the advantages of traditional grading with modern quality control indicators. By measuring the natural morphological parameters,processing parameters and the intrinsic content of ferulic acid,an important active ingredient,of the 15 batches of L. chuanxiong pieces collected from different manufacturers and different batches of different medicinal materials markets,we can synthesize the results. The mass constants and percentage mass constants are calculated and analyzed based on the above data. The results showed that the quality constants of 15 batches of L. chuanxiong pieces collected ranged from 0.53-3.00; if the percentage mass constants were more than 80%,50%-80% was second-class pieces,and the rest were third-class pieces,the evaluation results were as follows: the quality constants of first-class L. chuanxiong pieces were more than 2.40,the quality constants of second-class L. chuanxiong pieces should be 1.70-2.40,and the quality constants of third-class L. chuanxiong pieces should be less than 1.70. In this paper,the method of dividing the quality constants of the top blade model into different grades is further applied and practiced,which proves that the method is scientific,reasonable and multi-adaptable. At the same time,it enriches the research data of the grade evaluation of L. chuanxiong pieces,provides a useful reference for the promotion of the grade evaluation of L. chuanxiong pieces,and lays an experimental foundation for the next research of the subject group.


Assuntos
Medicamentos de Ervas Chinesas/normas , Ligusticum/química , Medicina Tradicional Chinesa , Controle de Qualidade
8.
J Oleo Sci ; 68(9): 931-937, 2019 Sep 04.
Artigo em Inglês | MEDLINE | ID: mdl-31413242

RESUMO

The essential oil extracted from roots and rhizomes of Ligusticum jeholense Nakai et Kitagawa was investigated for its chemical composition by GC-MS analysis, and evaluated for its contact toxicity and repellency against Tribolium castaneum and Lasioderma serricorne, along with some of its individual components. The essential oil was rich in aromatics (65.34%) with low molecular weight. Major components included sedanolide (33.95%), 3-butylidenephthalide (18.76%), spathulenol (8.90%) and myristicin (6.76%). The results of bioassays indicated that the essential oil of L. jeholense and 3-butylidenephthalide possessed significant repellent activities against T. castaneum at 2 and 4 h post-exposure. Meanwhile, 3-butylidenephthalide had potent contact toxicity against L. serricorne (LD50 = 13.64 µg/adult). The minor component n-butylbenzene in the oil was highly toxic to T. castaneum (LD50 = 23.99 µg/adult) and L. serricorne (LD50 = 7.86 µg/adult) in contact assays, but failed to repel these beetles at all testing concentrations. Spathulenol and myristicin exerted good insecticidal and repellent effects on the two target insects. This work suggests that the essential oil of L. jeholense has promising potential for development as natural insecticide or repellent to control pest damage in warehouses.


Assuntos
Derivados de Benzeno/farmacologia , Repelentes de Insetos/farmacologia , Inseticidas/farmacologia , Óleos Voláteis/farmacologia , Anidridos Ftálicos/farmacologia , Tribolium/efeitos dos fármacos , Animais , Ligusticum/química , Óleos Voláteis/análise , Óleos Voláteis/toxicidade
9.
Zhongguo Zhong Yao Za Zhi ; 44(9): 1755-1759, 2019 May.
Artigo em Chinês | MEDLINE | ID: mdl-31342698

RESUMO

Quality constant is a kind of grading evaluation method of traditional Chinese medicine pieces based on the combination of traditional knowledge and modern quality control. This method has been successfully applied in the grading evaluation of Glycyrrizae Radix et Rhizome pieces and traditional Chinese medicine pieces,and with a positive influence in the industry. With Dachuanxiong Formula for example,different grades of Ligusticum chuanxiong and Gastrodia elata pieces formed high-quality,moderate and qualified Dachuanxiong Formula on the basis of the grading evaluation of the pieces,and the pharmacodynamics method was used to evaluate its efficacy. The results showed that the maximum vascular diastolic rates of Dachuanxiong Formula in the three grades were( 80. 3±5. 2) %,( 67. 0±6. 1) %and( 60. 3±6. 5) %,and the strength of pharmacodynamics was positively correlated with the grade of L. chuanxiong and G. elata pieces.The quality constant technique can objectively and quantitatively classify single decoctions,and has important correlations and prompts for the efficacy of traditional Chinese medicine prescriptions composed of these pieces,with important significance in promoting hierarchical management of the industry,implementing better price for high quality and defining high quality and superior effect.


Assuntos
Medicamentos de Ervas Chinesas/normas , Gastrodia/química , Glycyrrhiza/química , Ligusticum/química , Medicina Tradicional Chinesa , Raízes de Plantas/química , Controle de Qualidade , Rizoma/química
10.
Zhongguo Zhong Yao Za Zhi ; 44(9): 1793-1798, 2019 May.
Artigo em Chinês | MEDLINE | ID: mdl-31342704

RESUMO

Aiming at the phenomenon of heavy metal Cd exceeding the standard of Chuanxiong medicinal materials,the accumulation of 12 inorganic elements,including heavy metals,in Ligusticum chuanxiong was studied in this paper. It was found that the contents and distribution of most inorganic elements in the stems and leaves of L. chuanxiong were higher than those in the rhizomes at seedling and shooting stages. The content of most elements in rhizome reached the highest at harvest stage,and the distribution ratio of some elements in rhizome was higher than that in stem and leaf at harvest stage. But rhizome,stem and leaf of L. chuanxiong have relatively stable absorption capacity and enrichment effect on different elements,and are less affected by growth period and position. Rhizomes and stems and leaves of L. chuanxiong were enriched with Cd,and stems and leaves also accumulated Pb at seedling stage and stem stage. The absorption capacity of Pb in stems and leaves of L. chuanxiong was higher than that of rhizomes,and the ability of absorbing Cd was less than that of rhizomes at harvest time. The total uptake of Cd and Pb by L. chuanxiong decreased with the prolongation of growth time,but the proportion of Cd and Pb in rhizome increased,so that the content of Cd and Pb increased with the prolongation of growth time.


Assuntos
Cádmio/análise , Ligusticum/química , Metais Pesados/análise , Medicamentos de Ervas Chinesas/química , Folhas de Planta/química , Caules de Planta/química , Rizoma/química
11.
Int J Mol Med ; 44(2): 503-512, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31173163

RESUMO

Glaucoma is the leading cause of irreversible blindness worldwide; the apoptosis of the retinal ganglion cells (RGCs) is a hallmark of glaucoma. Tetramethylpyrazine (TMP) is the main active component of Ligusticum wallichii Franchat, and has been demonstrated to improve a variety of injuries through its antioxidative and antiapoptotic properties. However, these effects of TMP on glaucoma have not been studied. The present study aimed to investigate the potential role of TMP in glaucoma and to elucidate its possible mechanisms responsible for these effects. An in vitro model was generated, in which primary RGCs (PRGCs) were treated with H2O2. Our study revealed that TMP protected against H2O2­induced injury to PRGCs, as evidenced by enhanced cell viability, reduced caspase 3 activity and decreased cell apoptosis. We also reported that TMP treatment inhibited reactive oxygen species (ROS) production and malondialdehyde levels, but upregulated the antioxidative enzyme superoxide dismutase. In particular, TMP significantly increased the expression of microRNA­182­5p (miR­182) in H2O2­treated PRGCs, which was selected as the target miRNA for further research. In addition, our findings suggested that the protective effects of TMP on H2O2­induced injury were attenuated by knockdown of miR­182. The results of a luciferase reporter assay demonstrated that Bcl­2 interacting protein 3 (BNIP3), an effector of mitochondria­mediated apoptosis, was a direct target of miR­182. In addition, TMP treatment significantly decreased the expression of BNIP3, Bax, cleaved­caspase­3 and cleaved­poly(ADP­ribose)polymerase, but increased that of Bcl­2. Also, TMP treatment decreased the release of cytochrome c from mitochondria and improved mitochondrial membrane potential in H2O2­treated RGCs. Of note, the inhibitory effects of TMP on the mitochondrial apoptotic pathway were suggested to be reversed by knockdown of miR­182. Collectively, our findings provide novel evidence that TMP protects PRGCs against H2O2­induced damage through suppressing apoptosis and oxidative stress via the miR­182/mitochondrial apoptotic pathway.


Assuntos
Antioxidantes/farmacologia , MicroRNAs/genética , Estresse Oxidativo/efeitos dos fármacos , Pirazinas/farmacologia , Células Ganglionares da Retina/efeitos dos fármacos , Animais , Antioxidantes/química , Apoptose/efeitos dos fármacos , Células Cultivadas , Peróxido de Hidrogênio/metabolismo , Ligusticum/química , Masculino , Potencial da Membrana Mitocondrial/efeitos dos fármacos , Camundongos Endogâmicos BALB C , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/genética , Mitocôndrias/metabolismo , Pirazinas/química , Células Ganglionares da Retina/citologia , Células Ganglionares da Retina/metabolismo , Regulação para Cima/efeitos dos fármacos
12.
Carbohydr Polym ; 221: 73-83, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31227169

RESUMO

A protein-containing polysaccharide, LCP, showing strong antioxidant activity from the rhizome of Ligusticum chuanxiong Hort was fractionated and purified. Its physicochemical properties were characterised by gel permeation chromatography (GPC), gas chromatography-mass spectrometry (GC-MS), UV and IR analysis. The results showed that LCP was proteoglycan containing 85.7% total carbohydrate, 2.79% protein, 5.14% uronic acid, and four kinds of monosaccharides including xylose, glucose, mannose and galactose with molar ratios of 1.2: 7.8: 1: 2.1, respectively. The average molecular weight of LCP was 15.8 × 104 Da. In addition, the results indicated that LCP exhibited good radical scavenging abilities. Furthermore, LCP partially attenuated the incidence of mortalities and pericardial edema in zebrafish embryos exposed to hydrogen peroxide (H2O2). Moreover, LCP provided protection against H2O2-induced ROS generation and cell death in zebrafish embryo. These results indicated that LCP could be a potential approach for oxidative stress damage reversal.


Assuntos
Depuradores de Radicais Livres/farmacologia , Ligusticum/química , Polissacarídeos/farmacologia , Animais , Desenvolvimento Embrionário/efeitos dos fármacos , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/toxicidade , Peróxido de Hidrogênio/farmacologia , Peso Molecular , Estresse Oxidativo/efeitos dos fármacos , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/toxicidade , Espécies Reativas de Oxigênio/metabolismo , Rizoma/química , Peixe-Zebra/embriologia
13.
Fitoterapia ; 137: 104174, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31100437

RESUMO

Five new phthalide dimers, chaxiongnolides C-G (1-5), the two enantiomers of riligustilide (6a and 6b) and tokinolide B (7) were isolated from the aerial parts of Ligusticum sinense Oliv cv. Chaxiong. The structures of 1-5 were elucidated through extensive spectroscopic analysis, and the relative configurations of compounds 2 and 3 were further confirmed by an X-ray diffraction experiment. The absolute configurations of 1-3 were assigned by comparing calculated and experimental ECD spectra. The ECD exciton chirality method was used to confirm the absolute configurations of compounds 4, 5, 6a and 6b. Compounds 1-3 are the first dimeric phthalides to be reported that are comprising a sedanolide unit. The compounds were evaluated in vitro for their cytotoxic activity against select human cell lines.


Assuntos
Benzofuranos/química , Ligusticum/química , Benzofuranos/isolamento & purificação , Linhagem Celular , China , Humanos , Estrutura Molecular , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Componentes Aéreos da Planta/química , Estereoisomerismo , Difração de Raios X
14.
Drug Dev Res ; 80(5): 585-594, 2019 08.
Artigo em Inglês | MEDLINE | ID: mdl-30957263

RESUMO

The aims of the study were to evaluate the pharmacodynamic interaction between 3α-hydroxymasticadienonic acid and diligustilide (DLG), isolated from the plants Amphiptherygium adstringens and Ligusticum porteri, respectively, using the indomethacin-induced gastric injury model, as well as their individual gastroprotective efficacy in this model. Male Wistar rats were orally administered with 3α-hydroxymasticadienonic acid, DLG or the mixture of 3α-hydroxymasticadienonic acid-DLG (at a fixed-ratio combination of 1:1, 1:3, and 3:1). Thirty minutes later, the gastric damage was induced by a single oral dose of indomethacin (30 mg/kg). Three hours later, the gastric injury (mm2 ) was determined. 3α-hydroxymasticadienonic acid and DLG as individual compounds showed a gastroprotective effect against indomethacin-induced gastric damage (p < .05). The effective dose (ED50 ) values for each compound were 6.96 ± 1.25 mg/kg for 3α-hydroxymasticadienonic acid and 2.63 ± 0.37 mg/kg for DLG. The isobolographic analysis performed showed that the combination exhibited super-additive interaction as the experimental ED50 values (Zexp) were lower than theoretical additive dose values (Zadd; p < .05). Our results identify the super-additive (synergist) interaction between 3α-hydroxymasticadienonic acid and DLG and the gastric safety of both compounds in the indomethacin-induced gastric injury model, suggesting their potential in the future as a strategy to decrease the gastric damage associated to the chronic use of nonsteroidal anti-inflammatory drugs (NSAIDs).


Assuntos
Gastroenteropatias/tratamento farmacológico , Indometacina/efeitos adversos , Ligusticum/química , Extratos Vegetais/administração & dosagem , Triterpenos/administração & dosagem , Administração Oral , Animais , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Combinação de Medicamentos , Sinergismo Farmacológico , Mucosa Gástrica/efeitos dos fármacos , Mucosa Gástrica/lesões , Gastroenteropatias/induzido quimicamente , Gastroenteropatias/patologia , Masculino , Estrutura Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Triterpenos/farmacologia
15.
Bioorg Chem ; 84: 505-510, 2019 03.
Artigo em Inglês | MEDLINE | ID: mdl-30602133

RESUMO

Seven new butylphthalide derivatives, ligusticumolide A-G (1-7), together with two known butylphthalide derivatives (8-9) were isolated from an ethanol extract of Ligusticum chuanxiong Hort. The structures of these derivatives were elucidated from analysis of 1D/2D NMR, UV, IR and HRESIMS data. The absolute configurations of these derivatives were determined by electronic circular dichroism (ECD) calculations and Mosher's method. Ligusticumolide A (1) and ligusticumolide B (2) are enantiomers that were obtained by chiral separation. Ligusticumolide C (3) and ligusticumolide D (4) are diastereomers. All of the compounds were evaluated for their hepatoprotective activity against N-acetyl-p-aminophenol-induced HepG2 cell injury. Compounds 4, 5, and 7-9 showed more significant hepatoprotective activity than that of the positive control drug (bicyclol) at a concentration of 10 µM (p < 0.01).


Assuntos
Benzofuranos/química , Ligusticum/química , Substâncias Protetoras/química , Benzofuranos/isolamento & purificação , Benzofuranos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Dicroísmo Circular , Humanos , Ligusticum/metabolismo , Espectroscopia de Ressonância Magnética , Conformação Molecular , Raízes de Plantas/química , Raízes de Plantas/metabolismo , Substâncias Protetoras/isolamento & purificação , Substâncias Protetoras/farmacologia , Estereoisomerismo
16.
Nat Prod Res ; 33(10): 1399-1405, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-29262724

RESUMO

Two new (1-2) and six known (3-8) nucleoside alkaloids were isolated from the rhizomes of Ligusticum striatum DC. Compounds 1 and 2 (liguadenosines A and B) were unusual N-10 substituted adenosine derivatives. Their structures were elucidated by extensive spectroscopic analyses and ECD calculation. Most of them significantly inhibited the abnormal increase in platelet aggregation induced by ADP at concentrations of 50 and 100 µM. Particularly, the inhibitory effect of 3 was equivalent to aspirin.


Assuntos
Alcaloides/farmacologia , Ligusticum/química , Nucleosídeos/farmacologia , Inibidores da Agregação de Plaquetas/farmacologia , Rizoma/química , Alcaloides/isolamento & purificação , Aspirina/farmacologia , Humanos , Estrutura Molecular , Fator de Ativação de Plaquetas , Agregação Plaquetária/efeitos dos fármacos , Inibidores da Agregação de Plaquetas/química , Inibidores da Agregação de Plaquetas/isolamento & purificação
17.
Int J Mol Sci ; 19(12)2018 Dec 11.
Artigo em Inglês | MEDLINE | ID: mdl-30545008

RESUMO

The rhizoma of Ligusticum sinense, a Chinese medicinal plant, has long been used as a cosmetic for the whitening and hydrating of the skin in ancient China. In order to investigate the antimelanogenic components of the rhizoma of L. sinense, we performed an antimelanogenesis assay-guided purification using semi-preparative HPLC accompanied with spectroscopic analysis to determine the active components. Based on the bioassay-guided method, 24 compounds were isolated and identified from the ethyl acetate layer of methanolic extracts of L. sinense, and among these, 5-[3-(4-hydroxy-3-methoxyphenyl)allyl]ferulic acid (1) and cis-4-pentylcyclohex-3-ene-1,2-diol (2) were new compounds. All the pure isolates were subjected to antimelanogenesis assay using murine melanoma B16-F10 cells. Compound 1 and (3S,3aR)-neocnidilide (8) exhibited antimelanogenesis activities with IC50 values of 78.9 and 31.1 µM, respectively, without obvious cytotoxicity. Further investigation showed that compound 8 demonstrated significant anti-pigmentation activity on zebrafish embryos (10‒20 µM) compared to arbutin (20 µM), and without any cytotoxicity against normal human epidermal keratinocytes. These findings suggest that (3S,3aR)-neocnidilide (8) is a potent antimelanogenic and non-cytotoxic natural compound and may be developed potentially as a skin-whitening agent for cosmetic uses.


Assuntos
Ligusticum/química , Preparações Clareadoras de Pele/química , Animais , Arbutina , Humanos , Queratinócitos/efeitos dos fármacos , Melanoma Experimental , Camundongos , Extratos Vegetais/efeitos adversos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Rizoma/química , Preparações Clareadoras de Pele/efeitos adversos , Preparações Clareadoras de Pele/farmacologia , Peixe-Zebra
18.
Zhongguo Zhong Yao Za Zhi ; 43(19): 3893-3898, 2018 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-30453715

RESUMO

Ligustrazine is an important active ingredient of the traditional Chinese medicine Chuanxiong Rhizoma, but its content is a controversial topic. The endophytes of medicinal plants have the ability to produce the same active substances as the host, so this report focused on the endophytic Bacillus subtilis, to study the origin of ligustrazine in Chuanxiong Rhizoma preliminarily by inoculating the isolated endophytic B. subtilis to the Chuanxiong Rhizoma medium in vitro for solid state fermentation. Tissue grinding method was used to isolate the endogenetic B. subtilis. The morphological features, conventional physiological and biochemical reactions and 16S rRNA molecular techniques were combined to identify the endogenetic strains. Then, the strains that grew well in the medicinal matrix of Chuanxiong Rhizoma were screened out for further fermentation studies. The solid-state fermentation was performed at 37 °C for 30 d using Chuanxiong Rhizoma fermentation medium (40 g Chuanxiong Rhizoma powder, 100 mL sterile water, 121 °C, sterilization for 25 minutes). UPLC was used to detect the contents of ligustrazine, acetoin in the Chuanxiong Rhizoma fermentation medium and Chuanxiong Rhizoma. All the five strains were Gram-positive and had spores. Phylogenetic analysis of the 16S rRNA sequence showed that the endophytes were B. subtilis. The results of UPLC showed that ligustrazine was detected in the Chuanxiong Rhizoma fermentation medium inoculated with endogenetic B. subtilis LB3, LB3-2-1, LB4, LB5 and LB6-2, while not detected neither in blank Chuanxiong Rhizoma fermentation medium nor in Chuanxiong Rhizoma. This study showed that the endogenetic B. subtilis of Ligusticum chuanxiong Hort. can make use of Chuanxiong Rhizoma fermentation medium to produce ligustrazine. Endogenetic B. subtilis has a certain correlation with the accumulation of ligustrazine in Rhizoma Chuanxiong. We speculate that the ligustrazine may be derived from the catabolism of endogenetic B. subtilis in Ligusticum chuanxiong.


Assuntos
Bacillus subtilis , Ligusticum/química , Ligusticum/microbiologia , Pirazinas/análise , Endófitos , Fermentação , Filogenia , RNA Ribossômico 16S , Rizoma/química
19.
J Pharm Biomed Anal ; 160: 135-143, 2018 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-30086506

RESUMO

Cyperi Rhizoma (Xiangfu) combined with either Angelicae Sinensis Radix (Danggui) or Chuanxiong Rhizoma (Chuanxiong) are herb pairs that are commonly used in clinical settings. To illustrate the herb-herb interactions that occur when extracts from these herbs are obtained together, ultra-high-performance liquid chromatography coupled with triple quadrupole electrospray tandem mass spectrometry and response surface analysis were used. Volatile components, α-cyperone, nootkatone, ligustilide, senkyunolide A and senkyunolide I, were accurately identified with high precision. When Xiangfu was combined with Danggui at a 1:1 ratio, or with Chuanxiong at a 1:1 or 2:1 ratio, the dissolution rates of α-cyperone and nootkatone from the herbs were greatly increased, compared to those obtained from Xiangfu extract alone. The dissolution rates of ligustilide, senkyunolide A and senkyunolide I from Danggui or Chuanxiong changed proportionally to changes in the ratios of Xiangfu with either Danggui or Chuanxiong. Response surface analysis results presented polynomial regression equations between the dissolution of tested compounds and the corresponding input variables, including compatibility proportions and solvent dosage. Based on the predicted results from response surface analysis, a combination of Xiangfu with Chuanxiong at a ratio of near 1:1, or with Danggui at 1:2, resulted in the maximum dissolution of five volatile components. Our established method could be applied to herb-herb interaction research, and the results may provide a scientific basis for the development of Cyperi Rhizoma-Chuanxiong Rhizoma, or Cyperi Rhizoma-Angelicae Sinensis Radix-based formulas and products.


Assuntos
Angelica sinensis/química , Cyperus/química , Medicamentos de Ervas Chinesas/farmacologia , Ligusticum/química , Compostos Orgânicos Voláteis/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos de Ervas Chinesas/química , Medicina Tradicional Chinesa/métodos , Raízes de Plantas/química , Rizoma/química , Espectrometria de Massas em Tandem/métodos , Compostos Orgânicos Voláteis/química
20.
J Pharm Biomed Anal ; 154: 123-137, 2018 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-29571130

RESUMO

Ligustici Rhizoma et Radix (LR), known as Gaoben (GB) in Chinese, has been used in traditional Chinese medicine for more than 2000 years. However, the varieties of LR are not well characterized at present, and traditional recognition methods have encountered increasing difficulties. This research attempts to distinguish different varieties of LR and its adulterants based on their chemical composition. A total of 61 representative samples were collected, and their varieties were confirmed by combining expert opinion with DNA molecular technology. All of the samples were characterized by an UHPLC-Q/TOF-MS method. The marker components that may contribute to variety discrimination were discerned by a data mining method, and they were then hypothesized, analyzed, and identified. A cluster analysis was performed by partial least squares (PLS) based on their MS signals. Furthermore, a feature extraction to find out the characteristic components, and a correspondence analysis to illustrate the corresponding relationship between the varieties and their components, were developed. As a result, 71 components were identified, of which 27 components were unambiguously identified by comparison with standards. The cluster analysis shows that varieties of LR and its adulterant samples exhibited a certain classification trend, with butylphthalide, senkyunolide I, senkyunolide A, ferulic acid, (Z)-ligustilide, bergapten, levistilide A, vanillic acid, isochlorogenic acid C and isochlorogenic acid A as characteristic chemical components. The varieties and their components showed a modest correlation. In conclusion, our study verified the possibility of discriminating the varieties of LR according to their chemical compositions. This research provides a new reference for the recognition of LR and its adulterants.


Assuntos
Medicamentos Falsificados/análise , Medicamentos de Ervas Chinesas/análise , Ligusticum/química , Cromatografia Líquida de Alta Pressão/instrumentação , Cromatografia Líquida de Alta Pressão/métodos , Medicamentos Falsificados/química , Mineração de Dados , Contaminação de Medicamentos , Medicamentos de Ervas Chinesas/química , Raízes de Plantas/química , Rizoma/química , Espectrometria de Massas em Tandem/instrumentação , Espectrometria de Massas em Tandem/métodos
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