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1.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4730-4735, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581082

RESUMO

The present study aimed to explore the mechanism of the sweating of Dipsacus asper on content changes of triterpene sa-ponins by detecting the total triterpene saponins and the index component asperosaponin Ⅵ in the crude and sweated D. asper, and analyzing the differentially expressed proteins by isobaric tags for relative and absolute quantification(iTRAQ) combined with LC-MS/MS. After sweating, the content of total triterpene saponins decreased manifestly, while that of asperosaponin Ⅵ increased significantly. As revealed by the iTRAQ-LC-MS/MS analysis, 140 proteins with significant differential expression were figured out, with 50 up-regulated and 90 down-regulated. GO analysis indicated a variety of hydrolases, oxido-reductases, and transferases in the differential proteins. The results of activity test on two differentially expressed oxido-reductases were consistent with those of the iTRAQ-LC-MS/MS analysis. As demonstrated by the analysis of enzymes related to the triterpene saponin biosynthesis pathway, two enzymes(from CYP450 and UGT families, respectively, which are involved in the structural modification of triterpene saponins) were significantly down-regulated after sweating. The findings suggested that sweating of D. asper presumedly regulated triterpene saponins by affecting the expression of downstream CYP450 s and UGTs in the biosynthesis pathway of triterpene saponins of D. asper.


Assuntos
Dipsacaceae , Saponinas , Triterpenos , Cromatografia Líquida , Humanos , Sudorese , Espectrometria de Massas em Tandem
2.
Sci Rep ; 11(1): 2600, 2021 01 28.
Artigo em Inglês | MEDLINE | ID: mdl-33510287

RESUMO

Scabiosa comosa and S. tschilliensis (SCST) are traditionally used for liver diseases in Mongolian medicine. However, their active ingredients and molecular mechanisms are unknown. The present study employed network pharmacology and experimental verification approaches to decipher the common pharmacological mechanisms of SCST on liver fibrosis, which is the key step in liver diseases. We predicted the targets of all available SCST ingredients with the SWISS and SuperPred servers and clustered the targets related to liver fibrosis from DrugBank, the OMIM database and the literature. We further evaluated the links between the herbal ingredients and pharmacological actions to explore the potential mechanism of action of SCST. We found that the PPARG signalling pathway could be regulated by SCST for liver fibrosis through enrichment analysis. The key targets included 8 co-targets, including HSP90AA1, PPARG, HSP90AB1, STAT1, etc., which play pivotal roles in the pathogenesis of liver fibrosis. Additionally, the top 15 key compounds included flavonoids and phenylpropanoids. Central to the pathogenesis of liver fibrosis is trans-differentiation or activation of hepatic stellate cells (HSCs). Therefore, LX2 cells, an immortalized human HSC line, were studied. Here, a total 37 components were isolated and identified from the inflorescences of SCST, including the new compound tschilliensisin, and the first separated components, ß-sitosterol and luteolin, and these compounds were assessed against anti-hepatic fibrosis. An MTT assay and quantitative real-time polymerase chain reaction (qRT-PCR) and Western blotting analyses demonstrated that the flavonoids of SCST revealed anti-hepatic fibrosis effects via anti-proliferation and increases in the Stat1, Pparg, Hsp90aa1 genes and STAT1 and PPARG proteins in LX-2 cells. In conclusion, these results indicate that SCST has multi-targeted and multi-component synergistic anti-hepatic fibrosis effects.


Assuntos
Dipsacaceae/química , Flavonoides/farmacologia , Cirrose Hepática/tratamento farmacológico , Terapia de Alvo Molecular , Extratos Vegetais/farmacologia , Actinas/metabolismo , Biomarcadores/metabolismo , Linhagem Celular , Proliferação de Células/efeitos dos fármacos , Humanos , Cirrose Hepática/metabolismo , Medicina Tradicional da Mongólia , Simulação de Acoplamento Molecular , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/uso terapêutico
3.
Microsc Res Tech ; 84(4): 682-694, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33105053

RESUMO

Palynology gives the evidence for identification and elimination of taxonomically complex genera. Pollen morphology of nine species (three subg., three sect.) of the genus Cephalaria Schrad. was studied using light microscopy and scanning electron microscopy. Pollen grains of all investigated species are triporate, suboblate to subprolate (P/E = 0.75-1.28), and large-sized (P = 58.52 µm-114.38, E = 63.84-119.70 µm). The outline of pollen grains in equatorial view is circular or elliptic, in polar view circular, circular-triangular, or triangular. Pores are distinct, lolongate, elliptic, or circular, with an annulus, operculum, and distinct or indistinct, wide halo surrounding the aperture. Exine sculpture is echinate-microechinate or echinate-microechinate-nanoechinate. Additional diagnostic characters at the species level in Cephalaria Schrad. that can be used for the purposes of taxonomy are size of pollen grains and pores, the shape of pores, the width of the annulus, structure of the exine, dimension of echini and microechini, location of microechini, and presence/absence of nanoechini. Palynomorphological data are compared with the taxonomical classification system of investigated taxa. It is shown that pollen grains morphology of the genus Cephalaria Schrad. is similar to the pollen morphology of the genus Dipsacus L., which confirms their inclusion in the Dipsaceae tribe.


Assuntos
Caprifoliaceae , Dipsacaceae , Microscopia Eletrônica de Varredura , Pólen
5.
Molecules ; 25(21)2020 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-33138334

RESUMO

Scarce information about the phenolic composition of Scabiosa atropurpurea L. is available, and no carotenoid compounds have been reported thus far. In this study the phenolic and carotenoid composition of this plant was both investigated and associated bioactivities were evaluated. Aiming to obtain extracts and volatile fractions of known medicinal plants to valorize them in the pharmaceutical or food industries, two techniques of extraction and five solvents were used to determine the biologically active compounds. Gas chromatography coupled to flame ionization and mass spectrometry and liquid chromatography coupled to photodiode array and atmospheric pressure chemical ionization/electrospray ionization mass spectrometry highlighted the presence of 15 volatiles, 19 phenolic, and 24 natural pigments in Scabiosa atropurpurea L. stem samples; among them, the most abundant were 1,8-cineole, chlorogenic acid, cynaroside, and lutein. Bioactivity was assessed by a set of in vitro tests checking for antioxidant, antibacterial, antifungal, and allelopathic (against Brassica oleracea L. and Lens culinaris Medik) effects. Scabiosa atropurpurea L. stem extracts presented a considerable antioxidant, antibacterial, and allelopathic potential, with less antifungal effectiveness. These results indicate that the volatile fractions and extracts from S. atropurpurea L. stem could be considered as a good source of bioactive agents, with possible applications in food-related, agriculture, and pharmaceutical fields. Genetic investigations showed 97% of similarity with Scabiosa tschiliensis, also called Japanese Scabiosa.


Assuntos
Antibacterianos , Antifúngicos , Antioxidantes , Dipsacaceae/química , Extratos Vegetais/química , Caules de Planta/química , Antibacterianos/química , Antibacterianos/farmacologia , Antifúngicos/química , Antifúngicos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Dipsacaceae/crescimento & desenvolvimento , Cromatografia Gasosa-Espectrometria de Massas , Caules de Planta/crescimento & desenvolvimento , Tunísia
6.
Molecules ; 25(22)2020 Nov 12.
Artigo em Inglês | MEDLINE | ID: mdl-33198146

RESUMO

Colorectal cancer is a malignancy with a high incidence. Currently, the drugs used in chemotherapy are often accompanied by strong side effects. Natural secondary metabolites can interfere with chemotherapeutic drugs and intensify their cytotoxic effects. This study aimed to profile the secondary metabolites from the methanol extract of Scabiosa atropurpurea and investigate their in vitro activities, alone or in combination with the chemotherapeutic agent doxorubicin. MTT assay was used to determine the cytotoxic activities. Annexin-V/PI double-staining analysis was employed to evaluate the apoptotic concentration. Multicaspase assay, quantitative reverse transcription real-time PCR (RT-qPCR), and ABC transporter activities were also performed. LC-MS analysis revealed 31 compounds including phenolic acids, flavonoids, and saponins. S. atropurpurea extract intensified doxorubicin anti-proliferative effects against resistant tumor cells and enhanced the cytotoxic effects towards Caco-2 cells after 48 h. The mRNA expression levels of Bax, caspase-3, and p21 were increased significantly whereas Bcl-2 expression level was decreased. Furthermore, the methanol extract reversed P-glycoprotein or multidrug resistance-associated protein in Caco-2 cells. In conclusion, S. atropurpurea improved chemosensitivity and modulated multidrug resistance in Caco-2 cells which makes it a good candidate for further research in order to develop a new potential cancer treatment.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Neoplasias Colorretais/patologia , Dipsacaceae/química , Doxorrubicina/administração & dosagem , Doxorrubicina/farmacologia , Resistencia a Medicamentos Antineoplásicos , Extratos Vegetais/farmacologia , Subfamília B de Transportador de Cassetes de Ligação de ATP/metabolismo , Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia , Apoptose , Células CACO-2 , Caspases/metabolismo , Proliferação de Células , Neoplasias Colorretais/tratamento farmacológico , Combinação de Medicamentos , Resistência a Múltiplos Medicamentos , Humanos , Concentração Inibidora 50 , Metanol/química , Proteínas Associadas à Resistência a Múltiplos Medicamentos/metabolismo , Folhas de Planta/química , Polifenóis/química
7.
Phytochemistry ; 180: 112526, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33011562

RESUMO

Phytochemical investigations of the roots of Scabiosa semipapposa Salzem ex D.C. have led to the isolation of 12 undescribed triterpenoid saponins named semipapposides A-L, one undescribed saponin semipapposide M obtained as an inseparable mixture, together with three known oleanolic acid glycosides. Their structures were elucidated by analysis of 1D and 2D-NMR (1H-1H COSY, TOCSY, HSQC-TOCSY, HSQC, ROESY or NOESY, and HMBC) spectroscopic data and mass spectrometry (HR-ESI-MS), and by comparison with those of related metabolites. All saponins possess a partial sequence rhamnopyranosyl-(1 â†’ 2)-xylopyranosyl or rhamnopyranosyl-(1 â†’ 2)-arabinopyranosyl- at C-3 of the aglycon and a gentiobiose unit at C-28. These results represent a contribution to the knowledge of the saponins of Scabiosa species and their chemotaxonomy.


Assuntos
Dipsacaceae , Ácido Oleanólico , Saponinas , Triterpenos , Estrutura Molecular , Raízes de Plantas
8.
Molecules ; 25(16)2020 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-32784367

RESUMO

Dipsacus asperoides is a kind of Chinese herbal medicine with beneficial health properties. To date, the quality of D. asperoides from different habitats has shown significant differences. However, the molecular differences in D. asperoides from different habitats are still unknown. The aim of this study was to investigate the differences in protein levels of D. asperoides from different habitats. Isobaric tags for relative and absolute quantification (iTRAQ) and 2DLC/MS/MS were used to detect statistically significant changes in D. asperoides from different habitats. Through proteomic analysis, a total of 2149 proteins were identified, of which 42 important differentially expressed proteins were screened. Through in-depth analysis of differential proteins, the protein metabolism energy and carbohydrate metabolism of D. asperoides from Hubei Province were strong, but their antioxidant capacity was weak. We found that three proteins, UTP-glucose-1-phosphate uridylyltransferase, allene oxide cyclase, and isopentyl diphosphate isomerase 2, may be the key proteins involved in dipsacus saponin VI synthesis. Eight proteins were found in D. asperoides in response to environmental stress from different habitats. Quantitative real-time PCR analysis confirmed the accuracy and authenticity of the proteomic analysis. The results of this study may provide the basic information for exploring the cause of differences in secondary metabolites in different habitats of D. asperoides and the protein mechanism governing differences in quality.


Assuntos
Dipsacaceae/metabolismo , Ecossistema , Raízes de Plantas/metabolismo , Proteômica , China , Dipsacaceae/genética , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Raízes de Plantas/genética , Transcriptoma
9.
Molecules ; 25(15)2020 Jul 22.
Artigo em Inglês | MEDLINE | ID: mdl-32707961

RESUMO

In previous studies, we isolated the known compound saponin XII from the roots of Dipsacus japonicus Miq. Here, we show that this compound reduced the number of acute myeloid leukemia OCI-AML3 cells as evaluated by a hemocytometer. Flow cytometry analyses demonstrated that the reported activity was associated with a significant increase of apoptosis and of cells in the G0/G1 phase of the cell cycle, with a decrease of cells in the S and G2/M phases. Thus, the inhibition of cell growth in OCI-AML3 cells was due to antiproliferative and pro-apoptotic effects. Interestingly, the bioactivity of saponin XII exerted its effect at a concentration as low as 1 µg/mL.


Assuntos
Antineoplásicos/química , Dipsacaceae/química , Inibidores do Crescimento/química , Leucemia Mieloide Aguda/tratamento farmacológico , Extratos Vegetais/química , Saponinas/química , Antineoplásicos/farmacologia , Apoptose/efeitos dos fármacos , Divisão Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Descoberta de Drogas , Inibidores do Crescimento/farmacologia , Humanos , Extratos Vegetais/farmacologia , Saponinas/farmacologia
10.
Ann Palliat Med ; 9(2): 272-285, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-32233617

RESUMO

BACKGROUND: To explore the potential therapeutic effect of total flavonoids (TFs) extracted from Scabiosa comosa Fisch. ex Roem. et Schult on liver fibrosis in rat models and to identify the possible targets and pathways of TF in treating liver fibrosis by using a quantitative proteomics method. METHODS: Sixty Wistar rats were equally randomized into five groups: a blank control group, a model group, and high-, intermediate-, and low-dose TF treatment groups. Except for the blank control group, rats in the other four groups were intragastrically administered with CCL4 2 mL/kg to establish the liver fibrosis models. Furthermore, the high-, intermediate-, and low-dose TF groups were intragastrically given TF at a dose of 200, 100 and 50 mg/kg, respectively. After 10 weeks, the rats were sacrificed, and blood and liver samples were collected. Serum alanine transaminase (ALT), Aspartate aminotransferase (AST), and alkaline phosphatase (ALP) levels were measured, and hematoxylin and eosin (HE) staining and Masson's trichrome staining were used to observe the pathological changes in each group. The hydroxyproline content was also determined. Real-time polymerase chain reaction (PCR) and Western blotting (WB) were performed to detect the mRNA and protein expressions of α-smooth muscle actin (αSMA) and Collagen I. Mass spectrometry was performed for proteomic analysis. RESULTS: Compared with the blank control group, the model group had significantly higher ALT, AST, ALP, and hydroxyproline levels; also, HE and Masson staining showed fibrotic lesions and inflammatory cell infiltration in the model group. Compared with the model group, the high-, intermediate-, and lowdose TF groups had significantly decreased ALT, AST, and ALP levels (P<0.05), and a significantly lower hydroxyproline level (P<0.05), along with remarkably improved fibrotic lesions and inflammatory cell infiltration. Real-time PCR and WB showed that the model group had significantly higher expressions of αSMA and collagen I than those in the blank control group, whereas the TF groups had significantly lower expressions of αSMA and collagen I than those in the model group. A total of 5,014 proteins were detected by quantitative proteomics, among which 205 proteins were differentially expressed, 77 of which were upregulated and 128 of which were down-regulated. KEGG pathway analysis indicated that the peroxisome proliferator activated receptor (PPAR) and ECM-receptor interaction pathways were down-regulated in the TF groups compared with the model group. Among them, fatty-acid-binding protein (FABP) and von Willebrand factor (vWF) were the key proteins in the PPAR and extracellular matrix (ECM)-receptor interaction pathways. The proteomic results were validated by using WB, yielding consistent results. CONCLUSIONS: Our result demonstrated that the TF extract of Scabiosa comosa Fisch. ex Roem. et Schult has a good anti-liver fibrosis effect and may prevent liver fibrosis by reducing the content of α-SMA, CollagenⅠ in liver tissue. The anti-fibrosis mechanism of TF extract of Scabiosa comosa Fisch. ex Roem. et Schult may be the inhibition of key proteins FABP and vWF in PPAR, ECM RECEPTOR INTERACTION pathway.


Assuntos
Dipsacaceae/química , Relação Dose-Resposta a Droga , Flavonoides/farmacologia , Cirrose Hepática/tratamento farmacológico , Extratos Vegetais/farmacocinética , Substâncias Protetoras/farmacologia , Proteômica , Animais , Humanos , Masculino , Modelos Animais , Fitoterapia/métodos , Plantas Medicinais/química , Ratos , Ratos Wistar
11.
J Ethnopharmacol ; 258: 112912, 2020 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-32348843

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Dipsacus asper Wall. ex C.B. Clarke, a traditional Chinese herbal medicine, has long been used in China for the therapy of bone diseases (e.g. bone fracture, osteoporosis, rheumatic arthritis), traumatic hematoma, uterine bleeding and those caused by the deficiency of liver and kidney. AIM OF THE STUDY: This work aims to evaluate current research progress on chemical constituents, pharmacological activities, quality control, and pharmacokinetic of Dipsacus asper Wall. ex C.B. Clarke, pinpoint the shortcomings of existing studies, and provide meaningful guidelines for our future investigations. METHODS: Extensive database retrieval, such as PubMed, SciFinder and CNKI, was carried out by using keywords such as "Dipsacus asper", "Radix Dipsaci", and "Xuduan". Furthermore, relevant textbooks, patents, reviews, and digital documents were consulted to collate all available scientific literature and to provide a complete science-based survey of the topic. RESULTS: More than 100 compounds have been isolated and identified from Dipsacus asper Wall. ex C.B. Clarke, a substantial proportion of which were reported to be triterpenoids and iridoids. Biological effects such as protective effects against bone fracture, anti-osteoporosis, neuroprotective, cardioprotective, anti-aging and protection of reproductive system activities were also evaluated in vitro and in vivo. CONCLUSIONS: Diaphoretic processing resulted in the drop in the content of asperosaponin VI, which was highly associated with bone protective effect of DA. Therefore, diaphoretic processing was not a suitable processing method for DA. Although Dipsacus asper Wall. ex C.B. Clarke was traditionally used for therapy of osteoarthritis, the in-depth study of the underlying mechanism was very rare. Much endeavor had been made on the effect of DA on bone fracture. Notably, high-dose of Dipsacus asper administration may cause adverse impacts in maternal healthy and embryo-fetal development. It's not suitable for further development in those bioactivities, such as anti-inflammatory and free radical scavenging, which are shared in many other plant species. Pharmacological effects of individual component of DA is not equivalent to its traditional usage. Attention should be paid to the traditional effect of extract of DA.


Assuntos
Dipsacaceae/química , Medicamentos de Ervas Chinesas/farmacologia , Extratos Vegetais/farmacologia , Animais , Medicamentos de Ervas Chinesas/efeitos adversos , Humanos , Medicina Tradicional Chinesa , Extratos Vegetais/efeitos adversos , Controle de Qualidade
12.
Acta Biochim Pol ; 67(1): 41-47, 2020 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-32129972

RESUMO

The chemical composition of Succisa pratensis is not well known. The existing data indicate a substantial content of flavonoids, which include luteolin and apigenin 7-glucosides. The aim of this study was to elaborate the isolation protocol of these flavonoids from flowers and leaves of S. pratensis, to carry out their characterization, as well as evaluate the effect of S. pratensis extracts on activation of transcription factor NF-κB and α-amylase activity. The extraction protocol applied in this study allowed isolation and characterization of flavonoid fraction of S. pratensis. Their identity was confirmed by NMR spectra analysis, UV spectroscopy and electrospray ionization-tandem MS evaluation. Treatment of pancreatic α-amylase with S. pratensis extract inhibited this enzyme's activity to an extent comparable to that of isolated luteolin and apigenin 7-glucosides. Incubation of HepG2 cells for 24 h with S. pratensis extracts or isolated flavonoids resulted in moderate reduction in NF-κB transcription factor activation evaluated in terms of translocation of its active subunits from cytosol into nucleus and subsequently diminished expression of the COX-2 gene. Expression of NF-κB was also reduced. The most significantly diminished NF-κB activation and expression, as well as COX-2 expression, was found to result from treatment with isolated flavonoids and ethyl acetate extract of S. pratensis leaves. These results indicate that S. pratensis flavonoids may modulate the metabolic and signaling pathways whose deregulation is related to pathogenesis of liver cancer. Further studies are required to confirm these observations and assess the chemopreventive and/or therapeutic potential of the S. pratensis herb.


Assuntos
Apigenina/farmacologia , Glucosídeos/farmacologia , Neoplasias Hepáticas/metabolismo , Luteolina/farmacologia , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , alfa-Amilases/metabolismo , Inibidores de Ciclo-Oxigenase 2/farmacologia , Dipsacaceae/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Células Hep G2 , Humanos , Neoplasias Hepáticas/tratamento farmacológico , Neoplasias Hepáticas/etiologia , Extratos Vegetais/uso terapêutico , alfa-Amilases/antagonistas & inibidores
13.
Phytochemistry ; 174: 112350, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32208198

RESUMO

The genus Scabiosa (Caprifoliaceae) is represented by 80 species, widely used as medicinal plants for their positive effects on human diseases. On the basis of the interesting biological activity shown by Scabiosa spp., the phytochemical investigation of Scabiosa sicula L., never investigated before, was carried out. An initial LC-MS profile of the MeOH extract of S. sicula whole plant guided the isolation of 34 compounds, of which the structures were unambiguously elucidated by NMR analysis as phenolic compounds and triterpene saponins, among which eight undescribed compounds. Moreover, the total phenolic content of S. sicula methanol extract has been evaluated. On the basis of the pharmacological activities reported for Scabiosa species the antioxidant activity of the methanol extract was tested by TEAC and DPPH assays. Finally, the α-glucosidase inhibitory activity of the methanol extract was assayed, showing an IC50 value (49 µg/mL) comparable to that exerted by acarbose (90 µg/mL), used as positive control.


Assuntos
Dipsacaceae , Antioxidantes , Cromatografia Líquida de Alta Pressão , Humanos , Compostos Fitoquímicos , Extratos Vegetais
14.
J Ethnopharmacol ; 254: 112710, 2020 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-32097699

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Dipsacus inermis Wall. is an edible Himalayan herb which is extensively used in traditional Ayurvedic system of medicine against various inflammation related disorders. AIM OF THE STUDY: This study was designed to evaluate the anti-inflammatory effects of Dipsacus inermis Wall. methanol extract (DIME) by using in vitro and in vivo models and to elucidate the underlying mechanism of action. MATERIALS AND METHODS: The in vitro anti-inflammatory potential of DIME was determined in LPS stimulated J774A.1 cells. The inhibitory effect of DIME on COX-2, PGE2 and inflammatory cytokines was determined by ELISA and RT-PCR. The suppression of ROS in response to DIME was determined by flow cytometry. Phosphorylation of NF-κBp65 and IκB degradation was determined by western blotting. RESULTS: Significant inhibition of NO, COX-2, PGE2 and pro-inflammatory cytokines including IL-1ß, TNF-α and IL-6 was found in response to DIME in LPS stimulated J774A.1 cells. The extract was found to down regulate the LPS induced expression of TNF-α, IL-6, iNOS and COX-2 along with inhibition of intracellular ROS. The in vivo studies carried on Wistar rats showed significant preventive effect of DIME against acetic acid induced increase in vascular permeability and carrageenan induced paw edema along with stabilization of histopathological alterations. CONCLUSION: The study demonstrated that DIME has significant in vitro and in vivo anti-inflammatory effect which is mediated by inhibiting the activation of NF-κB pathway. Our data opened a promising new pharmacological approach of designing anti-inflammatory drugs by studying individual fractions of the plant extract.


Assuntos
Anti-Inflamatórios/uso terapêutico , Dipsacaceae , Edema/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Permeabilidade Capilar/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Citocinas/genética , Citocinas/metabolismo , Dinoprostona/metabolismo , Edema/genética , Lipopolissacarídeos/farmacologia , Camundongos , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Extratos Vegetais/farmacologia , Folhas de Planta , Ratos Wistar , Espécies Reativas de Oxigênio/metabolismo
15.
J Sep Sci ; 43(7): 1265-1274, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31961066

RESUMO

The roots of Dipsacus asper Wall as a commonly used traditional Chinese medicine are used for tonifying liver and kidney and strengthening bones and muscles. However, an effective separation strategy for comprehensive and rapid separation of the main active compounds from the roots of D. asper is nonexistent. This investigation provided an effective separation method based on AB-8 macroporous resin column chromatography using different ratios of ethanol in water and two different modes of high-speed countercurrent chromatography with salt-containing solvent system for rapid enrichment and separation from the roots of D. asper. The macroporous resin column chromatography was performed on AB-8 resin using ethanol in water ratios of 10, 30, 40, 50, and 80% as the optimized enrichment conditions for iridoid glycosides and triterpenoid saponins with different polarities. For high-speed countercurrent chromatography separation, the conventional and recycling modes were combined together to develop a strategy for 12 compounds (1-12) from the enriched parts of 30, 40, and 80% ethanol, including six high-polarity iridoid glycosides (1-6) using inorganic salt-containing solvent system and six triterpenoid saponins (7-12). Recycling high-speed countercurrent chromatography separation was successfully applied to separate two isomers (9 and 10) after 11 cycles.


Assuntos
Dipsacaceae/química , Glicosídeos Iridoides/isolamento & purificação , Saponinas/isolamento & purificação , Triterpenos/isolamento & purificação , Distribuição Contracorrente , Glicosídeos Iridoides/química , Medicina Tradicional Chinesa , Conformação Molecular , Raízes de Plantas/química , Sais/química , Saponinas/química , Estereoisomerismo , Triterpenos/química
16.
Zhongguo Zhong Yao Za Zhi ; 44(14): 2996-3001, 2019 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-31602845

RESUMO

Through the records of herbal and market investigations,the samples collected from different market and origin were analyzed,and the appearance character indexes were determined in order to revise the commodity specification and grade standard of Dipsaci Radix combined with production practice. This is also to analyze association of the appearance with quality different of intrinsic components. The investigation results indicated the root's long and thick was better,and atrovirens of fracture surface,there are most of the market is dominated by the ungraded goods. Through principal component analysis,variance analysis and cluster analysis,combining with the feasibility of actual operation and herbal record,the length,middle diameter and phloem color were filtrated and the specification was divided into 2 ranks: the selection and ungraded goods,and the grade was divided into 2 ranks for the selection goods: big,small selected goods. Moreover,there were no significant correlation between the appearance and the intrinsic quality index of Dipsaci Radix,the content of extractum were significantly positive correlation with the moisture,but had extremely negative correlation with the total ash. Multiple comparisons indicated that the content of the moisture,extractum and asperosaponin VI of the selected goods were higher than the ungraded goods,while the total ash content were lower,and they hasn't significant difference. The commodity specification and grade standard of Dipsaci Radix as a basis provide commodity specification and grade standard of communities and standardizing market trade order.


Assuntos
Dipsacaceae/química , Medicamentos de Ervas Chinesas/normas , Raízes de Plantas/química , Análise por Conglomerados , Plantas Medicinais/química , Análise de Componente Principal
17.
Life Sci ; 235: 116820, 2019 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-31476308

RESUMO

AIMS: Osteoporosis (OP) is a systemic metabolic bone disease characterized by bone mass decrease and microstructural degradation, which may increase the risk of bone fracture and leading to high morbidity. Dipsaci Radix (DR), one typical traditional Chinese medicine (TCM), which has been applied in the treatment of OP with good therapeutic effects and few side effects. However, the underlying molecular mechanisms of DR to treat OP have not been fully elucidated. In this study, we aim to dissect the molecular mechanism of DR in the treatment of OP. MATERIALS AND METHODS: A systems pharmacology approach was employed to comprehensively dissect the action mechanisms of DR for the treatment of OP. KEY FINDINGS: 10 compounds were screened out as the potential active ingredients with excellent biological activity based on in silico ADME (absorption, distribution, metabolism and excretion) prediction model. Then, 36 key protein targets of 6 compounds were identified by systems drug targeting model (SysDT) and they were involved in several biological processes, such as osteoclast differentiation, osteoblast differentiation and anti-inflammation. The target-pathway network indicated that targets are mainly mapped in multiple signaling pathways, i.e., MAPK, Tumor necrosis factor α (TNF-α), NF-κb and Toll-like receptor pathways. The in vitro results indicated that the compounds ursolic acid and beta-sitosterol effectively inhibited the osteoclast differentiation. SIGNIFICANCE: These results systematically dissected that DR exhibits the therapeutic effects of OP by the regulation of immune system-related pathways, which provide novel perspective to drug development of OP.


Assuntos
Bases de Dados de Produtos Farmacêuticos , Dipsacaceae/química , Medicamentos de Ervas Chinesas/farmacologia , Redes Reguladoras de Genes , Redes e Vias Metabólicas , Osteoporose/tratamento farmacológico , Biologia de Sistemas/métodos , Células CACO-2 , Humanos , Osteoporose/genética , Osteoporose/metabolismo , Transdução de Sinais
18.
J Ethnopharmacol ; 244: 112074, 2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31291608

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Osteoporosis is one of the most common bone diseases; it is characterized by bone loss and is a risk factor for hip fracture. Chinese herbal medicines (CHMs) and their related natural compounds have been used for treating many diseases, including bone diseases, since ancient times in China and are regarded as a cost-effective complementary therapy. AIM OF THE STUDY: The goal of this study was to investigate the osteoprotective mechanisms of these three Chinese herbs and their related natural compounds. The effects of CHMs and related natural compounds on RANKL-induced osteoclastogenesis in vitro were investigated. MATERIALS AND METHODS: A network pharmacology method was applied to study CHM-related natural compounds and their osteoporosis targets. In addition, their effect on RANKL-induced osteoclastogenesis in RAW264.7 cells was also investigated in vitro. RESULTS: Radix dipsaci, Eucommiae cortex, and Rhizoma drynariae exhibited protective effects against mortality in hip fracture patients. Furthermore, these three herbs inhibited RANKL-induced TRAP activities and reduced the expression of bone resorption-related genes in RAW264.7 cells. Network analysis of natural compound (ingredient)-target interactions identified 11 natural compounds. Signal pathway analyses suggested that these compounds may target cytokine-cytokine receptor interactions, including RANKL-induced osteoclastogenesis. Five novel natural compounds exhibited reduced RANKL-induced TRAP activities and bone resorption-related gene expression. CONCLUSION: The clinically used CHMs, Radix dipsaci, Eucommiae cortex, and Rhizoma drynariae, and natural compounds obtained from them may suppress RANKL-induced osteoclastogenesis in vitro.


Assuntos
Dipsacaceae , Eucommiaceae , Osteoclastos/efeitos dos fármacos , Osteogênese/efeitos dos fármacos , Extratos Vegetais/farmacologia , Polypodiaceae , Animais , Humanos , Camundongos , Compostos Fitoquímicos/farmacologia , Raízes de Plantas , Ligante RANK , Células RAW 264.7 , Transdução de Sinais/efeitos dos fármacos
19.
Fitoterapia ; 135: 99-106, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31051193

RESUMO

Iridoid-monoterpenoid indole alkaloid hybrids (IMIAHs) represent a rare class of natural products reported from only several plants of Rubiaceae and Dipsacaceae families, while their structural assignments remain a very challenging work due to complexity and flexibility. In the current study, a new IMIAH (1) was isolated from the roots of Dipsacus asper and its structure with absolute configuration was unambiguously established by a combination of spectroscopic analyses, chemical degradation and ECD calculation. A new oleanane-type triterpenoid saponin (2) and 15 known co-metabolites were also obtained and structurally characterized. Our biological evaluations showed that compound 2 exhibited moderate inhibition against acetylcholine esterase (AChE) with an IC50 value of 15.8 ±â€¯0.56 µM, and compound 15 displayed potent cytotoxicity selectively against human A549 and H157 lung cancer cells with IC50 values of 6.94 ±â€¯0.24 and 9.06 ±â€¯0.12 µM, respectively.


Assuntos
Glucosídeos/farmacologia , Iridoides/farmacologia , Ácido Oleanólico/análogos & derivados , Alcaloides de Triptamina e Secologanina/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Dipsacaceae/química , Glucosídeos/química , Glucosídeos/isolamento & purificação , Humanos , Iridoides/química , Iridoides/isolamento & purificação , Estrutura Molecular , Ácido Oleanólico/química , Ácido Oleanólico/isolamento & purificação , Ácido Oleanólico/farmacologia , Raízes de Plantas/química , Alcaloides de Triptamina e Secologanina/química , Alcaloides de Triptamina e Secologanina/isolamento & purificação
20.
J Pharm Biomed Anal ; 173: 120-125, 2019 Sep 05.
Artigo em Inglês | MEDLINE | ID: mdl-31128424

RESUMO

Cephalaria species in Turkey known as "Pelemir" and they have many different biological activities due to their wide range of chemical content. The main goal of this study is determine the flavonoids and phenolic acids in Cephalaria species using high-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS). This method was developed for quantitation of reported compounds using reverse phase Fortis C18 (150 × 3 mm × 5 µm) column with a gradient of 0.1% formic acid solution (A) in water and (B) in methanol in ESI mode. The recoveries of developed method were obtained in the range of 90.4-109.4%. Limit of detection (LOD) and limit of quantification (LOQ) values were calculated in the range of 0.3-25.2 ppb and 3.0-102.3 ppb for the reported compounds. Uncertainty evaluations of all compounds were reported. Twenty-five flavonoids, five simple phenolics, two triterpenoids, one iridoid and vitamin C successfully identified and quantified for nineteen Cephalaria species. The main flavonoids in the studied species were determined as cyanidin-3-O-glucoside, luteolin-7-O-glucoside, kaempherol-3-O-glucoside, hyperoside, hesperidin, luteolin and quercetin while salicylic and caffeic acids were detected as major phenolic acids in the analyzed samples. This is the first full characterization study for nineteen Cephalaria species via HPLC-MS/MS.


Assuntos
Dipsacaceae/química , Flavonoides/análise , Fenóis/análise , Extratos Vegetais/análise , Cromatografia Líquida de Alta Pressão/métodos , Extratos Vegetais/química , Espectrometria de Massas em Tandem/métodos
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