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1.
Xenobiotica ; 53(12): 634-643, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-38053346

RESUMO

C. officinalis Kuan is the dry root of Cyathula officinalis Kuan. Clinically, it is used for fall and flutter injury, rheumatism and arthralgia. Phytoecdysteroids have significant anti-inflammatory effects, and the phytoecdysteroids present in C. officinalis Kuan exhibit potential for treating rheumatoid arthritis.This study first developed a selective, accurate and efficient LC-MS/MS method for 12-day pharmacokinetic studies regarding the simultaneous determination of cyasterone, 25-epi-28-epi-cyasterone, precyasterone and capitasterone from C. officinalis Kuan phytoecdysteroids extract in normal and adjuvant arthritis rats.An Agilent Eclipse Plus C18 RRHD column (1.8 µm, 50mm × 2.1 mm) with a gradient mobile phase consisting of water (A) and acetonitrile (B) was used for analysis. The mass analysis was performed in an Agilent 6430 QQQ-MS mass spectrometer with positive mode multiple reaction monitoring (MRM).The results indicated that the AUC0-t and AUC0-∞ values of the four phytoecdysteroids in adjuvant arthritis rats were different from those in normal rats on the first day, which could provide a helpful reference for pharmacological and toxicological studies, as well as clinical applications of C. officinalis Kuan in the treatment of rheumatoid arthritis.


1. C. officinalis Kuan is the dry root of Cyathula officinalis Kuan which has been used for the treatment of flapping injury, rheumatism arthralgia, foot flaccidity, and tendon contracture thousands of years in China, and has been officially included in the Chinese Pharmacopoeia.2. A highly accurate, stable, and sensitive ultra-performance liquid chromatography with tandem mass spectrometry (UHPLC-MS/MS) method was first established and validated for simultaneously determination four phytoecdysteroids: cyasterone, 25-epi-28-epi-cyasterone, precyasterone and capitasterone in normal and adjuvant arthritis rats plasma samples 12 days of continuous gavage of C. officinalis Kuan phytoecdysteroids extract.3. The phytoecdysteroids is the important component of C. officinalis Kuan, which is difficult to separated. And there is no report for the pharmacokinetic study of phytoecdysteroids from C. officinalis Kuan. And the method provides a good reference for the follow-up studies clinical medication of the phytoecdysteroids from C. officinalis Kuan.


Assuntos
Artrite Experimental , Artrite Reumatoide , Medicamentos de Ervas Chinesas , Ratos , Animais , Cromatografia Líquida/métodos , Espectrometria de Massas em Tandem/métodos , Cromatografia Líquida de Alta Pressão/métodos , Espectrometria de Massa com Cromatografia Líquida , Artrite Experimental/tratamento farmacológico , Administração Oral , Artrite Reumatoide/tratamento farmacológico , Reprodutibilidade dos Testes
2.
J Ethnopharmacol ; 314: 116680, 2023 Oct 05.
Artigo em Inglês | MEDLINE | ID: mdl-37230282

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Pfaffia glomerata (Spreng.) Pedersen has traditionally been used as a tonic and a stimulant by the Brazilian population. It shows higher biomass accumulation and production of secondary compounds, such as the phytosterol 20-hydroxyecdysone. AIMS: The present study aimed to evaluate the effects of the hydroalcoholic extract of the root of tetraploid P. glomerata (BGEt) on testicular parenchyma, and its implications on fertility. MATERIAL AND METHODS: Adult Swiss mice were divided as: control (water) and sildenafil citrate (7 mg/kg), BGEt at 100, 200, and 400 mg/kg, and BGEtD 200 mg/kg (treated with BGE every three days). Males (n = 4/group) were mated with normal untreated adult females to assess fertility rates, while other animals (n = 6/group) were euthanized for testis, epididymis, and oxidative stress analyses. RESULTS: Increase in tubule diameter and epithelium height in the discontinuous group, in addition to an increase in the proportion of tubules with moderate pathologies was observed. The pre-implantation loss was lower in all treated groups. The post-implantation loss was significantly increased in all treated groups, except for the lowest BGEt dose. BGEt intake caused a decrease in daily sperm production, along with the number and quality of sperm in the epididymis. Changes were observed in protein carbonylation and hydrogen peroxide and nitric oxide levels, characterizing oxidative stress. CONCLUSIONS: The hydroalcoholic extract of P. glomerata tetraploid altered sperm and testicular parameters, compromising embryonic development after implantation.


Assuntos
Amaranthaceae , Tetraploidia , Masculino , Camundongos , Gravidez , Animais , Feminino , Testículo , Epididimo , Espermatozoides , Fertilidade , Desenvolvimento Fetal , Contagem de Espermatozoides , Sementes
3.
Phytochemistry ; 212: 113710, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37178942

RESUMO

Six undescribed C27-phytoecdysteroid derivatives, named superecdysones A-F, and ten known analogs were extracted from the whole plant of Dianthus superbus L. Their structures were identified by extensive spectroscopy, mass spectrometric methods, chemical transformations, chiral HPLC analysis, and the single-crystal X-ray diffraction analysis. Superecdysones A and B possess a tetrahydrofuran ring in the side chain and superecdysones C-E are rare phytoecdysones containing a (R)-lactic acid moiety, whereas superecdysone F is an uncommon B-ring-modified ecdysone. Notably, based on the variable temperature (from 333 K to 253 K) NMR experiments of superecdysone C, the missing carbon signals were visible at 253 K and assigned. The neuroinflammatory bioassay of all compounds were evaluated, and 22-acetyl-2-deoxyecdysone, 2-deoxy-20-hydroxyecdysone, 20-hydroxyecdysone, ecdysterone-22-O-benzoate, 20-hydroxyecdysone-20,22-O-R-ethylidene, and acetonide derivative 20-hydroxyecdysterone-20, 22-acetonide significantly suppressed the LPS-induced nitric oxide generation in microglia cells (BV-2), with IC50 values ranging from 6.9 to 23.0 µM. Structure-activity relationships were also discussed. Molecular docking simulations of the active compounds confirmed the possible mechanism of action against neuroinflammations. Furthermore, none compounds showed cytotoxicity against HepG2 and MCF-7. It is the first report about the occurrence and anti-neuroinflammatory activity of the phytoecdysteroids in the genus Dianthus. Our findings demonstrated that ecdysteroids may be used as potential anti-inflammatory drugs.


Assuntos
Dianthus , Dianthus/química , Ecdisterona/farmacologia , Simulação de Acoplamento Molecular , Doenças Neuroinflamatórias , Ecdisteroides/farmacologia
4.
Nutrients ; 15(5)2023 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-36904246

RESUMO

The genus Ajuga (Lamiaceae) is rich in medicinally important species with biological activities ranging from anti-inflammatory, antitumor, neuroprotective, and antidiabetic to antibacterial, antiviral, cytotoxic, and insecticidal effects. Every species contains a unique and complex mixture of bioactive metabolites-phytoecdysteroids (PEs), iridoid glycosides, withanolides, neo-clerodane terpenoids, flavonoids, phenolics, and other chemicals with high therapeutic potential. Phytoecdysteroids, the main compounds of interest, are natural anabolic and adaptogenic agents that are widely used as components of dietary supplements. Wild plants remain the main source of Ajuga bioactive metabolites, particularly PEs, which leads to frequent overexploitation of their natural resources. Cell culture biotechnologies offer a sustainable approach to the production of vegetative biomass and individual phytochemicals specific for Ajuga genus. Cell cultures developed from eight Ajuga taxa were capable of producing PEs, a variety of phenolics and flavonoids, anthocyanins, volatile compounds, phenyletanoid glycosides, iridoids, and fatty acids, and demonstrated antioxidant, antimicrobial, and anti-inflammatory activities. The most abundant PEs in the cell cultures was 20-hydroxyecdysone, followed by turkesterone and cyasterone. The PE content in the cell cultures was comparable or higher than in wild or greenhouse plants, in vitro-grown shoots, and root cultures. Elicitation with methyl jasmonate (50-125 µM) or mevalonate and induced mutagenesis were the most effective strategies that stimulated cell culture biosynthetic capacity. This review summarizes the current progress in cell culture application for the production of pharmacologically important Ajuga metabolites, discusses various approaches to improve the compound yield, and highlights the potential directions for future interventions.


Assuntos
Ajuga , Ajuga/química , Antocianinas , Flavonoides , Fenóis , Glicosídeos Iridoides , Anti-Inflamatórios , Técnicas de Cultura de Células
5.
Protoplasma ; 260(2): 467-482, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35788779

RESUMO

Plants adjust their complex molecular, biochemical, and metabolic processes to overcome salt stress. Here, we investigated the proteomic and epigenetic alterations involved in the morphophysiological responses of Pfaffia glomerata, a medicinal plant, to salt stress and the demethylating agent 5-azacytidine (5-azaC). Moreover, we investigated how these changes affected the biosynthesis of 20-hydroxyecdysone (20-E), a pharmacologically important specialized metabolite. Plants were cultivated in vitro for 40 days in Murashige and Skoog medium supplemented with NaCl (50 mM), 5-azaC (25 µM), and NaCl + 5-azaC. Compared with the control (medium only), the treatments reduced growth, photosynthetic rates, and photosynthetic pigment content, with increase in sucrose, total amino acids, and proline contents, but a reduction in starch and protein. Comparative proteomic analysis revealed 282 common differentially accumulated proteins involved in 87 metabolic pathways, most of them related to amino acid and carbohydrate metabolism, and specialized metabolism. 5-azaC and NaCl + 5-azaC lowered global DNA methylation levels and 20-E content, suggesting that 20-E biosynthesis may be regulated by epigenetic mechanisms. Moreover, downregulation of a key protein in jasmonate biosynthesis indicates the fundamental role of this hormone in the 20-E biosynthesis. Taken together, our results highlight possible regulatory proteins and epigenetic changes related to salt stress tolerance and 20-E biosynthesis in P. glomerata, paving the way for future studies of the mechanisms involved in this regulation.


Assuntos
Amaranthaceae , Proteômica , Azacitidina/farmacologia , Cloreto de Sódio/farmacologia , Tolerância ao Sal/genética , Epigênese Genética , Proteínas de Plantas/metabolismo , Estresse Fisiológico
6.
Chin J Nat Med ; 20(7): 551-560, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35907654

RESUMO

Achyranthes bidentata Blume is widely used as a traditional Chinese medicine with the effects of nourishing the liver and kidneys and strengthening muscles and bones. In this work, a rapid and simple strategy was developed for characterizing phytoecdysteroids by ultra-high-performance liquid chromatography coupled with liner ion trap-Orbitrap mass spectrometry using electrospray ionization in the negative mode. As a result, 47 phytoecdysteroids were unambiguously or tentatively characterized. Among them, seven known compounds were identified according to the reference standards along with molecular formula, retention time and fragmentation patterns, while others were mostly potential new compounds. Through targeted isolation, the structures of three new compounds were determined by NMR spectra, which were consistent with LC-MS characterization. The present study provides an efficient method to deeply characterize phytoecdysteroids.


Assuntos
Achyranthes , Achyranthes/química , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Gasosa-Espectrometria de Massas , Espectrometria de Massas , Medicina Tradicional Chinesa , Espectrometria de Massas por Ionização por Electrospray/métodos
7.
Artigo em Inglês | MEDLINE | ID: mdl-35526348

RESUMO

Reversed-phase high performance thin-layer chromatography (RP-HPTLC) on C18 bonded silica gel was combined with desorption electrospray ionization (DESI) and high resolution time of flight mass spectrometry (HRToFMS) to detect, characterize and image (MSI) phytoecdysteroids (plant-derived insect moulting hormones) in ethanolic extracts of members of the Silene plant family. As seen previously for silica gel, DESI provided a simple and convenient method for recovering polar polyhydoxysteroids from RP-HPTLC plates for the purposes of both the MS and MSI of extracts obtained from three species of the Silene family (Silene otites, S. nutans and S. viridiflora). Using RP-HPTLC/DESI/MSI/HRToFMS a number of ecdysteroids, including 20-hydroxyecdysone, polypodine-B, 2-deoxy-20-hydroxyecdysone and 2-deoxyecdysone were identified in these extracts. Differences were noted in the mass spectra obtained depending upon both the stationary phase on which they were separated, and the temperatures used in the heated transfer line used for introduction into the ion source. Ecdysteroids detected after chromatography on C18 bonded silica showed increased fragmentation due to water loss compared to those imaged from silica. In addition, the benefits of the additional resolution provided by 2-dimensional TLC for increasing spectral quality compared to a 1-dimensional separation are demonstrated.


Assuntos
Ecdisteroides , Espectrometria de Massas por Ionização por Electrospray , Cromatografia em Camada Fina/métodos , Ecdisterona , Extratos Vegetais/química , Sílica Gel , Espectrometria de Massas por Ionização por Electrospray/métodos
8.
Artigo em Inglês | WPRIM | ID: wpr-939920

RESUMO

Achyranthes bidentata Blume is widely used as a traditional Chinese medicine with the effects of nourishing the liver and kidneys and strengthening muscles and bones. In this work, a rapid and simple strategy was developed for characterizing phytoecdysteroids by ultra-high-performance liquid chromatography coupled with liner ion trap-Orbitrap mass spectrometry using electrospray ionization in the negative mode. As a result, 47 phytoecdysteroids were unambiguously or tentatively characterized. Among them, seven known compounds were identified according to the reference standards along with molecular formula, retention time and fragmentation patterns, while others were mostly potential new compounds. Through targeted isolation, the structures of three new compounds were determined by NMR spectra, which were consistent with LC-MS characterization. The present study provides an efficient method to deeply characterize phytoecdysteroids.


Assuntos
Achyranthes/química , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Gasosa-Espectrometria de Massas , Espectrometria de Massas , Medicina Tradicional Chinesa , Espectrometria de Massas por Ionização por Electrospray/métodos
9.
Int J Mol Sci ; 22(4)2021 Feb 19.
Artigo em Inglês | MEDLINE | ID: mdl-33669861

RESUMO

Microsorum species produce a high amount of phytoecdysteroids (PEs), which are widely used in traditional medicine in the Pacific islands. The PEs in two different Microsorum species, M. punctatum (MP) and M. scolopendria (MS), were examined using high-performance liquid chromatography (HPLC). In particular, MS produces a high amount of 20-hydroxyecdysone, which is the main active compound in PEs. To identify genes for PE biosynthesis, we generated reference transcriptomes from sterile frond tissues using the NovaSeq 6000 system. De novo transcriptome assembly after deleting contaminants resulted in 57,252 and 54,618 clean transcripts for MP and MS, respectively. The clean Microsorum transcripts for each species were annotated according to gene ontology terms, UniProt pathways, and the clusters of the orthologous group protein database using the MEGAN6 and Sma3s programs. In total, 1852 and 1980 transcription factors were identified for MP and MS, respectively. We obtained transcripts encoding for 38 and 32 enzymes for MP and MS, respectively, potentially involved in mevalonate and sterol biosynthetic pathways, which produce precursors for PE biosynthesis. Phylogenetic analyses revealed many redundant and unique enzymes between the two species. Overall, this study provides two Microsorum reference transcriptomes that might be useful for further studies regarding PE biosynthesis in Microsorum species.


Assuntos
Ecdisteroides/metabolismo , Gleiquênias/enzimologia , Gleiquênias/genética , Transcriptoma/genética , Vias Biossintéticas/genética , Regulação da Expressão Gênica de Plantas , Biblioteca Gênica , Ontologia Genética , Ácido Mevalônico/metabolismo , Anotação de Sequência Molecular , Fenótipo , Filogenia , Folhas de Planta/genética , RNA Mensageiro/genética , RNA Mensageiro/metabolismo , Fatores de Transcrição/metabolismo
10.
Artigo em Inglês | MEDLINE | ID: mdl-32899750

RESUMO

Phytoecdysteroids are natural compounds with therapeutic benefits in both humans and animals. The effectiveness of natural products with health potential is based on the activities and potencies of their active ingredients. In this study, dominant ecdysteroids-ajugasterone C, 20-hydroxyecdysone and polypodine B-from the Serratula coronata (S. coronata) herb were separated by column chromatography, identified by spectroscopic data and quantified by high-performance liquid chromatography with a diode array detector (HPLC-DAD). The obtained concentration of ecdysteroids (approximately 23%) in the S. coronatae herb extract enhances the possibility of their use in pharmaceutical and cosmetic products with high levels of phytoecdysteroids. Moreover, this study has shown a positive effect of ecdysteroids-containing cream on changes in quality of life and a beneficial effect in reducing the symptoms of seborrheic dermatitis. It has been demonstrated that the application of the cream with phytoecdysteroids resulted in a statistically significant alleviation of symptoms (p < 0.05), especially in terms of itching, pain or burning sensations in the affected areas in comparison to previous symptoms.


Assuntos
Dermatite , Qualidade de Vida , Animais , Cromatografia Líquida de Alta Pressão/métodos , Humanos , Extratos Vegetais , Esteroides/química
11.
Vopr Pitan ; 89(2): 100-106, 2020.
Artigo em Russo | MEDLINE | ID: mdl-32459909

RESUMO

Formally, phytoadaptogens extracted mainly from medicinal plants are not food substances, and their use in preventive nutrition is significantly limited. However, screening studies can detect phytoadaptogens in food plants, however in much smaller quantities. For example, phytoecdysteroids are biologically active substances (BAS), used to relieve chronic fatigue syndrome, reduce nervous and muscle fatigue, improve memory and attention processes. Phytoecdysteroids can be isolated not only from various medicinal plants, but also from food plants like spinach (Spinacia oleracea) and quinoa (Chenopodium quinoa). Researchers show interest in possible synergies in the manifestation of a wide range of pharmacological effects, determined by a combination of phytoecdysteroids and other biologically active substances of these food plants. The aim of this research is a brief analytical review of publications characterizing the spectrum of minor biologically active substances of spinach and quinoa, as well as those devoted to the experimental assessment of their pharmacological activity in experiments on laboratory animals. Results. An analysis of the publications presented in the review indicates that spinach and its extracts are promising food sources of phytoadaptogens, carotenoids, phenolic compounds, in particular quercetin, kempferol, phenolic acids (p-coumaric, ferulic), as well as lignans metabolized into biologically active phytoestrogens (enterolactone and enterodiol). The possible prophylactic effect of spinach is being actively studied in vivo in laboratory animals when modeling diseases such as diabetes mellitus, cardiovascular and cancer diseases. Numerous adaptogenic effects and the neuroprotective effect of spinach and its extracts are shown, expressed in improving the memory and learning of animals. Publications of the last decade indicate an increased interest in such a promising food source of high-grade protein and a wide spectrum of biologically active substances, including phytoecdysteroids, as quinoa grains. More than 20 phenolic compounds in free or conjugated forms were found in quinoa grains; tannins, saponins, sterols, phytic acid, and ecdysteroids are present in small quantities. The consumptionof quinoa can have a beneficial effect on the organism, normalizing carbohydrate and lipid metabolism, reducing body weight and preventing excessive lipid peroxidation. The anti-inflammatory effects and antioxidant effects of quinoa are widely discussed. Conclusion. Spinach, quinoa and their extracts are promising food sources of biologically active substances, their pharmacological action is confirmed from the standpoint of evidence-based medicine by in vivo experimental studies. Accordingly, it is advisable to expand the use of these food plants for inclusion in biologically active dietary supplements, functional food ingredients and specialized food products for various purposes.


Assuntos
Doenças Cardiovasculares/dietoterapia , Chenopodium quinoa , Diabetes Mellitus/dietoterapia , Análise de Alimentos , Neoplasias/dietoterapia , Spinacia oleracea , Animais , Antioxidantes/química , Antioxidantes/uso terapêutico , Doenças Cardiovasculares/metabolismo , Carotenoides/química , Carotenoides/uso terapêutico , Diabetes Mellitus/metabolismo , Modelos Animais de Doenças , Humanos , Neoplasias/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/uso terapêutico , Estudos Prospectivos
12.
Steroids ; 150: 108456, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31326452

RESUMO

The crude methanol extract of Sphenocentrum jollyanum root exhibited 98% and 80% antimicrobial activity against Aspergillus fumigatus Pinh and Vancomycin resistant enterococcus (VRE) at a concentration of 200 µg/mL, with IC50 11.45 and 12.95 µg/mL, respectively. The ethyl acetate fraction of methanol extract showed in-vitro antimicrobial activity against A. fumigatus Pinh at 83% with IC50 of <8 µg/mL. The phytochemical investigation of ethyl acetate fraction yielded six compounds, which were identified by their NMR, IR and MS spectral analyses as two new phytoecdysteroidal glycosides Sphenocentroside A (1), and Sphenocentroside B (2), and four known phytoecdysteroids: polypodoaurein (3), polypodine B (4), ecdysterone (5), and 20, 26-dihydroxyecdysone (6).


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Ecdisterona/farmacologia , Menispermaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antifúngicos/química , Antifúngicos/isolamento & purificação , Aspergillus fumigatus/efeitos dos fármacos , Relação Dose-Resposta a Droga , Ecdisterona/química , Ecdisterona/isolamento & purificação , Testes de Sensibilidade Microbiana , Conformação Molecular , Extratos Vegetais/isolamento & purificação , Estereoisomerismo , Relação Estrutura-Atividade , Enterococos Resistentes à Vancomicina/efeitos dos fármacos
13.
Adv Gerontol ; 32(1-2): 121-127, 2019.
Artigo em Russo | MEDLINE | ID: mdl-31228377

RESUMO

The course intake of the nutritional supplement «Kardisten¼ normalizes increased levels of cortisol in the blood, optimizes the activity of the vessels of the brain, improving the functional state and leading to an increase in the productivity of short-term and long-term memory, more pronounced in the group of persons up to 50. At initial organic changes in the brain vessels, «Kardisten¼ significantly reduces the level of cortisol, increases to a greater extent the productivity of memory than at atherosclerosis. «Kardisten¼ activates the natural mechanisms of increasing the functional capabilities of an organism, exerting a beneficial effect on the body of adults and the elderly people, and can be recommended for the correction of physical, mental health and preservation of active longevity.


Assuntos
Transtornos da Memória , Memória , Saúde Mental , Extratos Vegetais , Adulto , Idoso , Encéfalo/efeitos dos fármacos , Humanos , Hidrocortisona , Longevidade , Transtornos da Memória/tratamento farmacológico , Extratos Vegetais/uso terapêutico
14.
J Sep Sci ; 41(23): 4304-4314, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30303602

RESUMO

The review presents general principles for choosing optimal conditions for ecdysteroid separation, identification, and isolation using HPLC/TLC techniques in RP, NP-HILIC or NP modes. Analytics of ecdyteroids pose a still insufficiently resolved problem. Plant-derived ecdysteroids are a point of interest of pharmaceutical industry and sport medicine due to their postulated adaptogenic and anabolic properties. In insects, ecdysteroids regulate larval transformation. Maral root (Rhaponticum carthamoides, Leuzea carthamoides), traditional Siberian folk-medicine plant used as stimulant to boost overall health and fitness, is a particularly rich source of a wide variety of phytoecdysteroids. The similarity of molecular structures of ecdysteroids present in its extracts together with high content of unrelated compounds of similar chromatographic characteristics makes optimization of separation, identification and isolation of ecdysteroids a difficult analytical task. In that respect, two-dimensional separations, two-dimensional separations, 2D HPLC or 2D TLC, could be of use. For identification, the hyphenated techniques are particularly important. Thus, comprehensive overview of MS spectral parameters of ecdysteroids is provided. Described principles could easily be applied for separation of ecdysteroids in extracts from other sources. They are also useful for development of separation procedures for isolation of ecysteroids in preparative-scale applications.


Assuntos
Ecdisteroides/análise , Leuzea/química , Extratos Vegetais/análise , Raízes de Plantas/química , Cromatografia Líquida de Alta Pressão , Cromatografia em Camada Fina , Tamanho da Partícula , Propriedades de Superfície
15.
Nat Prod Res ; 31(5): 593-597, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27399832

RESUMO

A number of phytoecdysteroid compounds, such as ecdysterone, polipodin V, 2-deoxy-20-hydroxyecdysone, integristeron A and 2-deoxydizon were isolated from Stachys hissarica plant and their structures were confirmed by NMR, mass and IR spectroscopy. In addition, the biological activity of the S. hissarica plant's extract was tested on rats for wound healing activity. It was shown that the extract at repeated oral (per os) administration at a dose of 10 mg/kg speeds up the healing process of linear skin wounds in rats. The wound-healing activity of S. hissarica extract is confirmed to be effective and exceeds known drug methyluracil (2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine), especially in case of alloxan induced diabetic animals.


Assuntos
Ecdisteroides/farmacologia , Extratos Vegetais/farmacologia , Stachys/química , Cicatrização/efeitos dos fármacos , Aloxano , Animais , Diabetes Mellitus Experimental/fisiopatologia , Extratos Vegetais/análise , Ratos
16.
BMC Complement Altern Med ; 16(1): 375, 2016 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-27677846

RESUMO

BACKGROUND: Ajuga bracteosa has been extensively used traditionally for the treatment of a variety of diseases. The aim of the study was to scientifically validate the wide-scale exploitation of A. bracteosa in folk medicine various in vitro and in vivo assays. Moreover, these activities were related to the intrinsic biologically active phytoecdysteroids of A. bracteosa. METHODS: Aerial and root parts of A. bracteosa were first extracted separately with chloroform (AbCA and AbCR) and the residue was again extracted with methanol (AbMA and AbMR). Total flavonoid and phenolic contents were assayed as quercetin (QE) and gallic acid equivalents (GAE), respectively. These extracts were analyzed for in vitro antioxidant assessment including DPPH and H2O2 (% inhibition of free radicals), and reducing power and phosphomolybdenum methods (ascorbic acid equivalents AAE mg/g DW). Further, these extracts were assayed in vivo in separate groups of Sprague-Dawley rats for carrageenan induced rat paw edema inhibition, hotplate antinociception, forced swim antidepression and anticoagulation. Dose of each crude extract and standard drug given to rats was 200 mg/Kg- and 10 mg/10 mL/Kg body weight respectively. Plant extracts and standard drugs were administered orally, 60 min prior to the conduction of assays. Moreover, biologically active phytoecdysteroids were screened in A. bracteosa with the help of RP-HPLC. RESULTS: AbMA represented highest values of flavonoids (QE 1.98 % DW) and phenolic contents (GAE 5.94 % DW), significantly scavenged DPPH radicles (IC50 36.9) and reduced ferric ions with 718.4 mg ascorbic acid equivalent/g (AAE). Highest total antioxidant capacity was expressed by AbMR (927 mg AAE) with an IC50 value 19.1 µg/mL. The extracts which were found potent anti-oxidants, were also good at in vivo activities. AbMA significantly reduced edema in all the three hours of treatment (67.9, 70.3 and 74.3 %). AbMA also showed maximum nociceptor suppression in analgesic assay by delaying the time to start licking of paws in rats (57.7 ± 4.9 s). In addition, maximum anti-coagulation was also exhibited by AbMA (89.3 s), while all extracts were found strong antidepressants (≤15.66 s immobility time). Screening of biologically active phytoecdysteroids revealed the presence of 20-hydroxyecdysone (20-HE), makisterone (MKA), cyasterone (CYP) and ajujalactone (AJL). Total phytoecdysteroid content found in A. bracteosa was 1232.5 µg/g DW and 20-HE was most abundant (1232.5 µg/g DW) as compared to other phytoecdysteroids. CONCLUSION: Based on the tested in vitro and in vivo activities, AbMA was found to be a promising bioactive extract. These activities can be attributed to the intrinsic polyphenols and phytoecdysteroids contents of A. bracteosa.

17.
Appl Physiol Nutr Metab ; 40(12): 1324-8, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26584207

RESUMO

Phytoecdysteroids such as 20-hydroxyecdysone (20HE) are nutritional supplements marketed as enhancers of lean body mass. In this study the impact of 20HE ingestion on protein kinase B/Akt-mechanistic target of rapamycin complex 1 signaling in the skeletal muscle and liver of male rats was found to be limited. Bioavailability of 20HE, whether consumed alone or with leucine, also remained low at all doses ingested. Additional work is necessary to clarify 20HE mechanism of action in vivo.


Assuntos
Suplementos Nutricionais , Ecdisterona/farmacologia , Fígado/efeitos dos fármacos , Complexos Multiproteicos/metabolismo , Músculo Esquelético/efeitos dos fármacos , Serina-Treonina Quinases TOR/metabolismo , Animais , Disponibilidade Biológica , Relação Dose-Resposta a Droga , Ecdisterona/farmacocinética , Leucina/farmacologia , Fígado/enzimologia , Masculino , Alvo Mecanístico do Complexo 1 de Rapamicina , Músculo Esquelético/enzimologia , Fosforilação , Proteínas Proto-Oncogênicas c-akt/metabolismo , Ratos Sprague-Dawley , Transdução de Sinais/efeitos dos fármacos
18.
Bol. latinoam. Caribe plantas med. aromát ; 11(6): 474-497, nov. 2012. ilus, tab
Artigo em Inglês | LILACS | ID: lil-723579

RESUMO

Silene is a genus of the Caryophyllaceae family, contains more than 700 species, which are widely distributed in Northern Hemisphere, but also in Africa, Asia and South American. Phytochemical investigations of Silene species have revealed that many components from this genus are highly bioactive. More than 400 compounds has been isolated, among them major are phytoecdysteroids. The paper reviews the biological (antitumour, antibacterial and antioxidant) activities and the phytoecdysteroids of genus Silene. We summarized the phytoecdysteroids content referring to 171 species from the genus Silene and list 93 phytoecdysteroids isolated over the past few decades. There are also reports on the mentioned folk and traditional effects of Silene plants.


Silene es un género de la familia Caryophyllaceae, conteniendo más de 70 especies, ampliamente distribuidas no solo en el hemisferio norte, sino que también en Africa, Asia y sud América. Investigaciones fotoquímicas de las especies de Silene han revelado que muchos componentes de este género son altamente bioactivos. Más de 400 compuestos han sido aislados, entre ellos los mayoritarios correspondientes a fitoecdiesteroides. El manuscrito revisa las actividades biológicas (antitumorales, antibacterianas y antioxidantes) y los fitoecdiesteroides del género Silene. Resumimos el contenido de fitoecdiesteroides en 171 especies del género Silene y listamos 93 fitoecdiesteroides aislados desde hace unas pocas décadas. Hay también reportes mencionados acerca de los efectos tradicionales y folclóricos de la plantas del género Silene.


Assuntos
Antibacterianos , Antineoplásicos Fitogênicos , Antioxidantes , Ecdisteroides , Plantas Medicinais/classificação , Silene , Etnofarmacologia , Medicina Tradicional , Especificidade da Espécie
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