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1.
Molecules ; 27(3)2022 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-35164224

RESUMO

The Celastraceae family comprises about 96 genera and more than 1.350 species, occurring mainly in tropical and subtropical regions of the world. The species of this family stand out as important plant sources of triterpenes, both in terms of abundance and structural diversity. Triterpenoids found in Celastraceae species display mainly lupane, ursane, oleanane, and friedelane skeletons, exhibiting a wide range of biological activities such as antiviral, antimicrobial, analgesic, anti-inflammatory, and cytotoxic against various tumor cell lines. This review aimed to document all triterpenes isolated from different botanical parts of species of the Celastraceae family covering 2001 to 2021. Furthermore, a compilation of their 13C-NMR data was carried out to help characterize compounds in future investigations. A total of 504 pentacyclic triterpenes were compiled and distinguished as 29 aromatic, 50 dimers, 103 friedelanes, 89 lupanes, 102 oleananes, 22 quinonemethides, 88 ursanes and 21 classified as others.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antineoplásicos/farmacologia , Celastraceae/química , Triterpenos Pentacíclicos/farmacologia , Animais , Humanos
2.
Nat Prod Res ; 36(22): 5904-5909, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34994265

RESUMO

The expression of virulence factors, such as biofilm formation, in association with the acquisition of resistance to multiple drugs, has evidenced the need for new and effective antimicrobial agents against Staphylococcus aureus. The evaluation of the pharmacological properties of plant-derived compounds is a promising alternative to the development of new antimicrobials. In this study, we aimed to evaluate the antibacterial, antibiofilm, and the synergistic and cytotoxic effects of netzahualcoyonol isolated from Salacia multiflora (Lam.) DC. roots. Netzahualcoyonol presented bacteriostatic (1.56-25.0 µg/mL) and bactericidal (25.0-400.0 µg/mL) effects against Gram-positive bacteria, disrupted the biofilm of S. aureus, and presented a synergistic effect after its combination with ß-lactams and aminoglycosides. The low cytotoxicity of netzahualcoyonol (Selectivity Index (SI) for S. aureus (2.56), S. saprophyticus (20.56), and Bacillus subtilis (1.28)) suggests a good security profile. Taken together, these results show that netzahualcoyonol is promising for the development of a new effective antibacterial agent.


Assuntos
Celastraceae , Salacia , Testes de Sensibilidade Microbiana , Staphylococcus aureus , Bactérias Gram-Positivas , Antibacterianos/farmacologia
3.
J Ethnopharmacol ; 289: 115009, 2022 May 10.
Artigo em Inglês | MEDLINE | ID: mdl-35077827

RESUMO

ETHNO-PHARMACOLOGICAL RELEVANCE: The bark of Semialarium mexicanum commonly known as 'Cancerina' is used as an infusion in Central America and Mexico to treat various wound infections, as well as skin and vaginal ulcers. AIM OF THE STUDY: This study aimed to determine the wound healing, anti-inflammatory and anti-melanogenic activities of the aqueous extract of Semialarium mexicanum and to identify the compounds related to these activities. MATERIALS AND METHODS: A bio-guided isolation of the active compounds of Semialarium mexicanum was carried out, selecting the sub-extracts and fractions depending on their wound healing, anti-inflammatory and anti-melanogenic activities in the RAW 264.7, NIH/3T3 and B16-F10 cells. RESULTS: Three compounds were obtained and characterised by nuclear magnetic resonance and mass spectrometry. These compounds are (3ß)-3-Hydroxy-urs-12-en-28-oic acid (1), (3ß)-Urs-12-ene-3,28-diol (2) and (2α, 19α)-2,19-Dihydroxy-3-oxo-urs-12-en-28-oic acid (3). Regarding the anti-inflammatory activity, the three compounds inhibited the production of NF-κB and NO, however, compound 3 was the most active with IC50 values of 8.15-8.19 µM and 8.94-9.14 µM, respectively, in all cell lines. The anti-melanogenic activity of these compounds was evaluated by the inhibition of tyrosinase and melanin in the B16-F10 cell line. The three compounds showed anti-melanogenic activity, however, compound 3 was the most active with an IC50 of 8.03 µM for the inhibition of tyrosinase production, and an IC50 of 8.53 µM for the inhibition of melanin production. Finally, concerning the wound healing activity, the three compounds presented proliferative activity in all the tested cell lines, however, compound 3 showed higher cell proliferation percentages than compounds 1 and 2 (88.89-89.60% compared to 64.92-65.71% and 71.53-71.99%, respectively). CONCLUSION: The wound healing, anti-inflammatory and anti-melanogenic activity of the aqueous extract of Semialarium mexicanum was tested and analysed in the present study, after having isolated three ursane-type triterpenes.


Assuntos
Anti-Inflamatórios/farmacologia , Celastraceae/química , Triterpenos/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Anti-Inflamatórios/isolamento & purificação , Linhagem Celular Tumoral , Concentração Inibidora 50 , Medicina Tradicional , Melaninas/metabolismo , Melanoma Experimental/metabolismo , Camundongos , Células NIH 3T3 , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Células RAW 264.7 , Triterpenos/química , Triterpenos/isolamento & purificação
4.
Nat Prod Res ; 36(15): 4026-4030, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-33729063

RESUMO

Bioactivity-guided isolation of the CHCl3-soluble fraction of the stems of Salacia chinensis L. (Celastraceae) was carried out to obtain a new 7',9-epoxylignan (1) and three 7,9':7',9-diepoxylignans (2-4). The absolute configuration of 1 was elucidated based on NMR and ECD spectroscopic data interpretation. All isolated lignans showed intermediate α-glucosidase inhibitory activity with the IC50 values ranging from 28.5 to 85.6 µM.


Assuntos
Celastraceae , Lignanas , Salacia , Lignanas/farmacologia , Espectroscopia de Ressonância Magnética , Extratos Vegetais/química , Salacia/química
5.
Bol. latinoam. Caribe plantas med. aromát ; 20(4): 386-393, jul. 2021. ilus
Artigo em Inglês | LILACS | ID: biblio-1352337

RESUMO

Leaves of Monteverdia ilicifolia ("espinheira-santa") are considered a medicinal tea by the Brazilian Sanitary Surveillance Agency (Anvisa), by their anti-dyspeptic, anti-acid and protective of the gastric mucosa properties. Their spiny margins are similar to those of other botanical species, which may lead to misidentifications. The aim of this work was to evaluate the authenticity of 32 samples of herbal drugs commercialized as "espinheira-santa" in the formal trade in Brazil, by macro and microscopic morphological studies of the leaves. The evaluation of the botanical authenticity was based on leaf venation patterns, shape and anatomy of the petiole and midrib region in cross section, vascular system arrangement and epidermal characters. Analysis of these characters compared to literature data suggests that 34% of the samples are M. ilicifolia and the remaining 66% are Sorocea bonplandii, a species with no clinical studies assuring its effective and safe use, representing thus a potential risk to public health.


Las hojas de Monteverdia ilicifolia ("espinheira-santa") son consideradas tés medicinales por la Agencia Nacional de Vigilancia Sanitaria (Anvisa), Brasil, por las indicaciones terapéuticas como antidispépticos, antiácidos y protectores de la mucosa gástrica. Sus márgenes foliares espinescentes se parecen a los de otras especies, conduciendo a identificaciones erróneas. El objetivo de este trabajo fue evaluar la autenticidad de 32 muestras de drogas vegetales vendidas como "espinheira-santa" en el comercio legal de Brasil, realizando un estudio morfológico de las hojas. Esta evaluación se ha basado en observar de la hoja, sus patrones de nerviación, su forma y anatomía (pecíolo y nervadura central en corte transversal), disposición del sistema vascular y caracteres epidérmicos. El análisis de la morfología, comparado con los datos de literatura, sugiere que el 34% de las muestras son M. ilicifoliay el 66% son Sorocea bonplandii, una especie que no cuenta con los estudios clínicos que garantizan su uso efectivo y seguro, representando un riesgo para la salud pública.


Assuntos
Plantas Medicinais , Maytenus/anatomia & histologia , Fraude , Controle de Qualidade , Brasil , Contaminação de Medicamentos , Folhas de Planta/anatomia & histologia , Celastraceae/anatomia & histologia
6.
Bol. latinoam. Caribe plantas med. aromát ; 20(4): 416-426, jul. 2021. tab, ilus
Artigo em Inglês | LILACS | ID: biblio-1369485

RESUMO

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitroas well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p<0.05) diminished the level of malondialdehyde, augmented catalase activities and elevated glutathione levels. However, SOD activities were significantly boosted in a dose-dependent manner by the crude extracts. Therefore, I. glomerataand S. kraussiipossess antioxidant properties, hence, can serve as a therapeutic modality in the treatment of oxidative stress-induced erectile dysfunction.


Las especies reactivas de oxígeno están implicadas en múltiples condiciones patológicas, incluyendo la disfunción eréctil. Este estudio evaluó el potencial antioxidante in vitro e in vivo de extractos metanólicos de Inula glomeratay Salacia kraussii. Los materiales vegetales fueron pulverizados y extraídos con metanol. A estos extractos crudos se les llevó a cabo el análisis fitoquímico junto con el contenido total de fenólicos y flavonoides, así como se les investigó la capacidad in vitro para atrapar radicales (ABTS, DPPH, NO.). Los potenciales antioxidantes in vivo de los extractos crudos (50/250 mg/kg de peso corporal) se determinaron en un modelo en ratas con disfunción eréctil. El análisis fitoquímico reveló que ambas plantas contuvieron flavonoides, taninos, terpenoides y alcaloides. Los extractos crudos con un grado variable de eficiencia, atraparon a los radicales ABTS y DPPH. Los extractos crudos a bajas concentraciones (50 mg/kg p.c) significativamente (p<0.05) disminuyeron el nivel de malondialdehído, aumentaron las actividades de catalasa y elevaron los niveles de glutatión. Sin embargo, las actividades de SOD por los extractos crudos fueron significativamente dosis-dependientes. Así, los extractos de I. glomeratay S. kraussii mostraron propiedades antioxidantes, y por lo tanto, podrían servir como una alternativa terapéutica en el tratamiento de disfunción eréctil inducida por estrés oxidativo.


Assuntos
Animais , Ratos , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Inula/química , Salacia/química , Antioxidantes/farmacologia , Antioxidantes/química , Ácidos Sulfônicos/metabolismo , Flavonoides/análise , Espécies Reativas de Oxigênio , Ratos Sprague-Dawley , Estresse Oxidativo/efeitos dos fármacos , Asteraceae/química , Celastraceae/química , Benzotiazóis/metabolismo , Compostos Fenólicos/análise , Compostos Fitoquímicos/análise , Óxido Nítrico/metabolismo
7.
Rev Soc Bras Med Trop ; 54: e0835, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33886820

RESUMO

INTRODUCTION: Bioprospection of plant products is used to discover new insecticides. METHODS: The larvicidal activity of ethanolic extract and triterpene (tingenone B) from the bark of Maytenus guianensis and their effect on pupation and emergence were evaluated against Aedes aegypti. RESULTS: Crude extract LC50 was 11.3 ppm and caused ejection of the larvae intestine; tingenone B LC50 was 14.8 ppm. Pupation was reduced by 20% and 10%, respectively; however, the emergence was not affected. CONCLUSIONS: The crude bark extract exhibited a higher larvicidal effect against the vector.


Assuntos
Aedes , Anopheles , Celastraceae , Inseticidas , Maytenus , Animais , Inseticidas/farmacologia , Larva , Mosquitos Vetores , Extratos Vegetais/farmacologia , Folhas de Planta
8.
Rev. Soc. Bras. Med. Trop ; 54: e08352020, 2021. graf
Artigo em Inglês | LILACS | ID: biblio-1288107

RESUMO

Abstract INTRODUCTION: Bioprospection of plant products is used to discover new insecticides. METHODS: The larvicidal activity of ethanolic extract and triterpene (tingenone B) from the bark of Maytenus guianensis and their effect on pupation and emergence were evaluated against Aedes aegypti. RESULTS: Crude extract LC50 was 11.3 ppm and caused ejection of the larvae intestine; tingenone B LC50 was 14.8 ppm. Pupation was reduced by 20% and 10%, respectively; however, the emergence was not affected. CONCLUSIONS: The crude bark extract exhibited a higher larvicidal effect against the vector.


Assuntos
Aedes , Celastraceae , Maytenus , Inseticidas/farmacologia , Anopheles , Extratos Vegetais/farmacologia , Folhas de Planta , Mosquitos Vetores , Larva
9.
Chem Biodivers ; 17(12): e2000773, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33108694

RESUMO

Cheiloclinium cognatum (Miers) A.C.Sm. is an endemic species of Brazilian Cerrado that belongs to Celastraceae family. The phytochemical study of C. cognatum branches led to the identification of ten triterpenoids (TPs), 3ß-acyloxyurs-12-ene (1), friedelin (2), ß-friedelinol (3), glut-5-en-3ß-ol (4), α-amyrin (5), ß-amyrin (6), ß-sitosterol (7), canophyllol (8), 29-hydroxyfriedelan-3-one (9) and friedelane-3ß,29-diol (10). TPs 4, 5 and 6 are described for the first Cheiloclinium genus and TPs 8 and 9 were isolated in expressive amounts. Their cytotoxic activities were evaluated against THP-1 and K562 leukemia cell lines. TPs 3 and 5 were the most active, exhibiting lower or similar IC50 against both cell lines when compared to the controls. Their mechanisms of action were investigated suggesting an intrinsic mitochondrial pathway of apoptosis evidenced by up-regulation of BAK mRNA expression. Chemometric studies indicated that their activities may be related to their molecular size and shape as well as electronic interactions of C-3 hydroxy group with molecular targets.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Celastraceae/química , Leucemia/patologia , Triterpenos/farmacologia , Antineoplásicos Fitogênicos/isolamento & purificação , Linhagem Celular Tumoral , Ensaios de Seleção de Medicamentos Antitumorais , Humanos , Triterpenos/isolamento & purificação
10.
Daru ; 28(1): 281-286, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32285314

RESUMO

BACKGROUND: Triterpenes are ubiquitous secondary metabolites present in plants. They can be found in both forms, as genins or conjugated as glycosides. Although distinct analytical methods to quantify these compounds in vegetal tissues are available in the literature, limitations like high cost, complexity on sample preparation, and selectivity are often challenging issues. This study aimed to develop and to validate a simple and rapid spectrophotometric method to detect and quantify total triterpenes in plant matrices. METHODS: The assay was conducted directly into glass tubes using vanillin, acetic acid, and sulphuric acid as reagents, and ß-sitosterol as reference standard. The samples were analyzed at 548 nm assessing the quality parameters of selectivity, linearity, precision, accuracy, limit of detection (LOD), limit of quantification (LOQ), and robustness. RESULTS: The method was selective, with precision and accuracy varying from 0.56% to 4.98% and 96.63% to 113.87%, respectively. The values of the limit of detection and quantification were 0.042 µg.mL-1 and 0.14 µg.mL-1, correspondingly. The correlation coefficient (r) at the concentration range of 3.08 µg.mL-1to 24.61 µg.mL-1 was 0.9998. The total of triterpenes found in of B. holophylla and M. ilicifolia leaves were 132.36 ± 20.36 mg EßS.g-1 of dry extract and 53.91 ± 2.6 mg EßS.g-1 of dry extract, respectively. CONCLUSION: The method was reliable to quantify total triterpenes extracted from Maytenus ilicifolia and Bauhinia holophylla. Graphical abstract.


Assuntos
Bauhinia , Celastraceae , Folhas de Planta/química , Espectrofotometria/métodos , Triterpenos/análise , Ácido Acético/química , Benzaldeídos/química , Limite de Detecção , Reprodutibilidade dos Testes , Ácidos Sulfúricos/química
11.
Phytochemistry ; 174: 112345, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-32200067

RESUMO

Ten poly-O-acylated ß-dihydroagarofuran sesquiterpenoids, siphonagarofurans A-J, were obtained from the fruits of Siphonodon celastrineus using chromatographic techniques. Their structures were elucidated by extensive use of 2-D NMR spectroscopic methods. The absolute configurations of siphonagarofurans A-J were assigned following analysis of calculated and experimental ECD spectra. The absolute configuration of siphonagarofuran A was also confirmed by X-ray crystallographic analysis. Selected compounds were evaluated for their cytotoxic activity against KB, Vero and Hela cell lines with siphonagarofuran J identified as the most active compound, with IC50 values ranging from 14 to 27 µM.


Assuntos
Celastraceae , Sesquiterpenos , Frutas , Células HeLa , Humanos
12.
Chem Biodivers ; 17(5): e2000107, 2020 May.
Artigo em Inglês | MEDLINE | ID: mdl-32222029

RESUMO

Extracts and compounds obtained from several species of Celastraceae family are reported as potential sources of drugs due to their diverse pharmacological properties. Nevertheless, essential oil composition from these species is still little known. This work aimed at the analysis of essential oils obtained from different Brazilian Celastraceae species. A total of seventeen oils were obtained using hydrodistillation process and analyzed by gas chromatography/mass spectrometry (GC/MS). Principal component analysis (PCA) allowed the identification of a chemical composition pattern among the analyzed essential oils. Some compounds were more frequent among Celastraceae species, such as cis- and trans-linalool oxide (14/17 oil samples), nerylacetone (13/17), linalool (11/17), ß-ionone (10/17), α-ionone (9/17), nerolidol (10/17), decanal (10/17), and dodecanoic acid (10/17). These results contribute to the chemophenetics of Celastraceae species.


Assuntos
Celastraceae/química , Óleos Voláteis/análise , Brasil , Cromatografia Gasosa-Espectrometria de Massas , Análise de Componente Principal , Especificidade da Espécie
13.
Nat Prod Res ; 34(6): 810-815, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30388899

RESUMO

Friedelan-3-one (1) and friedelane-3,16-dione (2) isolated from leaves and branches of Maytenus robusta Reissek were subjected to structural modifications via nucleophilic addition to the carbonyl group and Baeyer-Villiger oxidation in order to synthesize potential cytotoxic compounds. The oximes friedelane-3-hydroxyimino (3) and 3-hydroxyiminofriedelan-16-one (4) together with the lactones friedelane-3,4-lactone (5) and 3,4-lactonefriedelan-16-one (6) were characterized by IR and NMR spectroscopic analyses. Compounds 4 and 6 are reported for the first time. Cytotoxic screening via MTT assay in human leukemia cell lines (THP-1 and K562) demonstrated no significant improvement of compounds 3-6 when compared to the starting materials. Only compounds 3 and 5 demonstrated an improvement against K562 cells. However, the same assay on ovarian and breast cancer cell lines (TOV-21G and MDA-MB-231) showed a reduction in the IC50 for compounds 4-6, indicating that ring A modifications may enhance the biological potential.


Assuntos
Antineoplásicos/farmacologia , Celastraceae/química , Citotoxinas/isolamento & purificação , Iminas/química , Lactonas/química , Triterpenos/química , Antineoplásicos/síntese química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Citotoxinas/síntese química , Citotoxinas/farmacologia , Humanos , Iminas/síntese química , Lactonas/síntese química , Folhas de Planta/química , Relação Estrutura-Atividade , Triterpenos/isolamento & purificação
14.
J Chem Ecol ; 45(9): 789-797, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31422514

RESUMO

Peritassa campestris (Celastraceae) root bark accumulates potent antitumor quinonemethide triterpenes (QMTs). When grown in their natural habitat, plants of the family Celastraceae produce different QMTs such as celastrol (3) and pristimerin (4). However, when they are inserted in in vitro culture systems, they accumulate maytenin (1) as the main compound. Recently, Bacillus megaterium was detected as an endophytic microorganism (EM) living inside P. campestris roots cultured in vitro. We hypothesized that compound (1) controls EM growth more efficiently, and that the presence of EMs in the root culture causes compound (1) to accumulate. For the first time, this work has explored plant-microorganism interaction in a species of the family Celastraceae by co-culture with an EM. Live endophytic bacteria were used, and QMT accumulation in P. campestris adventitious roots was our main focus. The antimicrobial activity of the main QMTs against endophytic B. megaterium was also evaluated. Our results showed that compound (1) and maytenol (5) were more effective than their precursors QMTs (3) and (4) in controlling the EM. Co-culture of B. megaterium with roots significantly reduced bacterial growth whereas root development remained unaffected. Compound (1) production was 24 times higher after 48 hr in the presence of the highest B. megaterium concentration as compared to the control. Therefore, P. campestris adventitious roots affect the development of the endophyte B. megaterium through production of QMTs, which in turn can modulate production of compound (1).


Assuntos
Bacillus megaterium/metabolismo , Celastraceae/metabolismo , Extratos Vegetais/química , Raízes de Plantas/metabolismo , Triterpenos/química , Anti-Infecciosos/química , Antineoplásicos/química , Endófitos/metabolismo , Triterpenos Pentacíclicos , Fatores de Tempo
15.
Molecules ; 24(11)2019 Jun 04.
Artigo em Inglês | MEDLINE | ID: mdl-31167480

RESUMO

Lauridia tetragona (L.f) R.H. Archer is routinely used in traditional medicine; however, its hepatoprotective property is yet to be scientifically proven. To this effect, the hepatoprotective activity of the polyphenolic-rich fractions (PPRFs) was investigated against acetaminophen (APAP) injured HepG2 cells. The ability of the PPRF to scavenge free radicals was tested against 2,2-diphenyl-1-picrylhydrazyl (DPPH), and [2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonicacid)] (ABTS). The ferric ion reducing power (FRAP) was also evaluated as a cell-free antioxidant assay. The hepatoprotective activity was then investigated by observing the effect of PPRFs against APAP-induced reduction in cell viability of HepG2 cells. The concentrations of alanine aminotransferase (AST), aspartate aminotransferase (ALT) and lactate dehydrogenase (LDH) released into the medium were evaluated while the underlying mechanism was further explored through western blot analysis. Thereafter, the isolated PPRFs were identified using UHPLC-QToF-MS. All six fractions of the PPRFs isolated showed significant antioxidant properties that were evident by the effective scavenging of DPPH, ABTS, and higher FRAP. The results indicated that PPRF pretreatments ameliorated APAP-induced hepatocellular injury by significantly inhibiting the leakage of AST, ALT, and LDH into the medium. The most active fractions for hepatoprotection were PPRF4 and PPRF6 with IC50 of 50.243 ± 8.03 and 154.59 ± 1.9 µg/mL, respectively. PPRFs markedly increased activities of liver superoxide dismutase, total antioxidant capacity, and liver glutathione concentration. Both PPRF4 and PPRF6 significantly increased the expression of Nrf2 and translocation. The LC-MS analysis revealed the presence of a wide variety of polyphenolics such as coumarin, ferulic acid, and caffeine among the dominant constituents. In conclusion, this study demonstrates that the isolated PPRFs have potential hepatoprotective activity that may be due to the increased expression of antioxidative genes dependent on Nrf2.


Assuntos
Acetaminofen/efeitos adversos , Celastraceae/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Substâncias Protetoras/farmacologia , Alanina Transaminase/metabolismo , Antioxidantes/química , Antioxidantes/farmacologia , Aspartato Aminotransferases/metabolismo , Sobrevivência Celular/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas , Relação Dose-Resposta a Droga , Antagonismo de Drogas , Ativação Enzimática/efeitos dos fármacos , Glutationa/metabolismo , Células Hep G2 , Humanos , Concentração Inibidora 50 , Peroxidação de Lipídeos/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/química , Polifenóis/química , Substâncias Protetoras/química
16.
Phytochemistry ; 165: 112041, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31203103

RESUMO

Spiroterreusnoids A-F, six undescribed spiro-dioxolane-containing adducts bearing 3,5-dimethylorsellinic acid-based meroterpenoid and 2,3-butanediol moieties were isolated from the endophytic fungus Aspergillus terreus Thom from Tripterygium wilfordii Hook. f. (Celastraceae). The structures of these adducts were established by spectroscopy, single-crystal X-ray diffraction, and experimental electronic circular dichroism (ECD) measurements. Spiroterreusnoids A-F represent the first examples of adducts composed of 3,5-dimethylorsellinic acid-based meroterpenoids. It is noteworthy that spiroterreusnoids A-F possessing a spiro-dioxolane moiety exhibited potential abilities in inhibiting BACE1 (IC50 values ranging from 5.86 to 27.16 µM) and AchE (IC50 values ranging from 22.18 to 32.51 µM), while the other analogues without this fragment displayed no such activities. Taken together, spiroterreusnoids A-F represent the first multitargeted natural adducts that could inhibit BACE1 and AchE, and might provide a new template for the development of new anti-Alzheimer's disease drugs.


Assuntos
Acetilcolinesterase/metabolismo , Secretases da Proteína Precursora do Amiloide/antagonistas & inibidores , Ácido Aspártico Endopeptidases/antagonistas & inibidores , Dioxolanos/farmacologia , Inibidores Enzimáticos/farmacologia , Compostos de Espiro/farmacologia , Terpenos/farmacologia , Secretases da Proteína Precursora do Amiloide/metabolismo , Animais , Ácido Aspártico Endopeptidases/metabolismo , Aspergillus/química , Celastraceae/microbiologia , Dioxolanos/química , Dioxolanos/isolamento & purificação , Enguias , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Compostos de Espiro/química , Compostos de Espiro/isolamento & purificação , Terpenos/química , Terpenos/isolamento & purificação
17.
West Indian med. j ; 68(2): 129-135, 2019. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1341857

RESUMO

ABSTRACT Objective: Despite the presence of multitude of synthetic drugs against fever and inflammation, none has been proven entirely safe. In contrast, the accepted safety of plant derived natural products is inspiring the world. Based on this fact as well as in view of the diversified activities reported from the genus Gymnosporia, the present study was designed to evaluate the antipyretic and anti-inflammatory activity of Gymnosporia royleana (G royleana). Methods: The methanolic extract of the aerial parts of G royleana was screened for in-vivo antipyretic activity using the brewer's yeast-induced pyrexia mice model and for anti-inflammatory activity using the carrageenan-induced paw oedema and xylene-induced ear oedema mice model. Results: In the antipyretic assay, G royleana extract showed considerable antipyretic activity in a dose dependent fashion. Statistically significant antipyretic effects (p < 0.05) were observed at the end of the second hour of administration for all doses of extract and remained significant until the end of the experiment. The plant extract also displayed promising anti-inflammatory activity, in a dose dependent fashion, in both models of inflammation ie carrageenan- and xylene-induced oedema models, when compared to the controls. In the carrageenan-induced oedema model, significant effects (p < 0.01) were observed for 300 and 600 mg/kg doses after 60 minutes of xylene administration (ie 55.51% and 65.88% inhibition of oedema, respectively). Conclusion: The study provided evidence supporting the antipyretic and anti-inflammatory activity of the G royleana methanolic extract.


RESUMEN Objetivo: A pesar de la presencia de multitud de fármacos sintéticos en el arsenal contra la fiebre y la inflamación, ninguno ha dado pruebas de ser completamente seguro. En contraste con ello, la seguridad aceptada de los productos naturales derivados de las plantas inspira al mundo. Sobre la base de este hecho, así como en vista de las actividades diversificadas que se reportan con respecto al género Gymnosporia, el presente estudio se diseñó con el objeto de evaluar el potencial antipirético y antiinflamatorio de Gymnosporia royleana (G royleana). Métodos: El extracto de metanol de las partes aéreas de G royleana fue tamizado en busca de actividad antipirética in vivo, utilizando el modelo de pirexia inducida por levadura de cerveza en ratones, y de actividad antiinflamatoria utilizando modelos de ratones con oedema de las patas inducido mediante carragenina, y oedema de las orejas inducido mediante xileno. Resultados: En el ensayo antipirético, el extracto de G royleana mostró una actividad antipirética considerable en forma dependiente de la dosis. Se observó un efecto antipirético estadísticamente significativo (p < 0.05) en el transcurso de la segunda hora de administración para todas las dosis de extracto y se mantuvo significativo hasta el final del experimento. El extracto de la planta también mostró una actividad antiinflamatoria prometedora, de una manera dependiente de la dosis, en ambos modelos de inflamación, es decir, modelos de oedema inducido por carragenina y xileno, en comparación con el control. En el modelo de oedema inducido por carragenina, se observó un efecto significativo (p < 0.01) para dosis de 300 y 600 mg / kg después de 60 minutos de administración de xileno (es decir, 55.51% y 65.88% de inhibición del oedema, respectivamente). Conclusión: El estudio proporcionó pruebas suficientes sobre el potencial antipirético y antiinflamatorio del extracto de G royleana.


Assuntos
Animais , Camundongos , Extratos Vegetais/farmacologia , Celastraceae/química , Antipiréticos/farmacologia , Febre/tratamento farmacológico , Fitoterapia , Anti-Inflamatórios/farmacologia , Saccharomyces cerevisiae , Modelos Animais de Doenças , Febre/induzido quimicamente
18.
West Indian med. j ; 68(2): 136-141, 2019. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1341855

RESUMO

ABSTRACT Objective: In the present study, five new source compounds isolated from aerial parts of Gymnosporia royleana (G royleana) were screened for antibacterial and antifungal activities. Methods: Extraction from plant material was carried out using cold maceration technique. Isolation of pure compounds was accomplished through repeated column chromatography of different fractions obtained from crude extract and using silica gel as stationary phase. Their structures were established via advanced spectroscopic techniques along with the spectral data previously reported for these compounds. Dilution method was used for the evaluation of antimicrobial potential of the compounds against various microbial strains. Results: Among the tested compounds, Gymnosporin B displayed moderate antimicrobial activity against Escherichia Coli (E coli), Staphylococcus aureus (S aureus), Candida albicans (C albicans) and Aspergillus flavus (A flavus) [minimum inhibitory concentration (MIC) range; 32-64 μg/mL]. Similarly, Gymnosporin C also showed moderate activity against E coli and S aureus (MIC; 32 μg/mL each) as well as weak activity against C albicans and A flavus (MIC; 64 μg/mL each). However, Royaflavone showed moderate antibacterial activity against S aureus only (MIC; 32 μg/mL). Antimicrobial activity of the rest of the compounds was weak and negligible. Conclusion: The present study has provided fascinating results of antimicrobial activities of the isolated compounds. However, the broad antimicrobial spectrum of Gymnosporin B and Gymnosporin C demands for further exploration of these triterpenes, both on the basis of mechanism and quantitative structure-activity relationship.


RESUMEN Objetivo: En el presente estudio, cinco nuevos compuestos de origen aislados de partes aéreas de Gymnosporia royleana (G royleana) fueron tamizados en sus actividades antibacterianas y antifúngicas. Métodos: La extracción de material vegetal se realizó mediante la técnica de maceración en frío. El aislamiento de compuestos puros se logró a través de la cromatografía en columna repetida de diversas fracciones obtenidas del extracto crudo y usando gel de silicona como fase estacionaria. Sus estructuras fueron establecidas mediante técnicas espectroscópicas avanzadas junto con los datos espectrales previamente reportados para estos compuestos. El método de dilución fue usado para evaluar el potencial antimicrobiano de los compuestos contra diversas cepas microbianas. Resultados: Entre los compuestos sometidos a prueba, Gymnosporina B mostró una actividad antimicrobiana moderada contra Escherichia Coli (E coli), Staphylococcus aureus (S aureus), Candida Albicans (C albicans) y Aspergillus flavus (A flavus) [rango de concentración inhibitoria mínima (CIM); 32 - 64 μg/mL]. De manera similar, Gymnosporina C también mostró actividad moderada contra E coli y S aureus (CIM; 32 μg/mL cada uno) así como débil actividad frente a C albicans y A flavus (CIM; 64 μg/mL cada uno). Sin embargo, Royaflavone mostró actividad antibacteriana moderada sólo frente a S aureus (CIM; 32 μg/mL). La actividad antimicrobiana del resto de los compuestos fue débil e insignificante. Conclusión: El presente estudio ha proporcionado resultados interesantes acerca de las actividades antimicrobianas de los compuestos aislados. Sin embargo, el amplio espectro antimicrobiano de la Gymnosporina B y la Gymnosporina C exige una mayor exploración de estos triterpenos, tanto sobre la base del mecanismo como a partir de la relación cuantitativa estructura-actividad.


Assuntos
Extratos Vegetais/isolamento & purificação , Fitoterapia , Antibacterianos/farmacologia , Antifúngicos/farmacologia , Ascomicetos/efeitos dos fármacos , Aspergillus flavus/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Extratos Vegetais/farmacologia , Celastraceae/química , Bactérias Gram-Negativas , Bactérias Gram-Positivas/efeitos dos fármacos
19.
West Indian med. j ; 68(2): 121-128, 2019. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1341852

RESUMO

ABSTRACT Objective: Gymnosporia royleana (G royleana) Wall ex MA Lawson, locally known as (Sur Azghee), is traditionally used for the management of various diseases. In the current investigation, we made an effort to scientifically validate its traditional use in various pathological conditions, such as microbial infections and cancer, and to explore its additional pharmacological activities via random screening against locally accessible pharmacological methods, irrespective of its traditional uses like antidiabetic, haemagglutination and antioxidant assays. Methods: Extraction was carried out using a cold maceration methodology. Dilution method was used for antimicrobial susceptibility testing using different concentrations. Streptozocin (STZ) induced protocol was used to assess antidiabetic activity at a dose level of 200, 400 mg/ kg. Antioxidant activity, haemagglutination activity, and anticancer activities against HepG-2 and MCF-7 cell lines were determined as per established protocols. Similarly, the maximum amount of phenolic content (12.02 mg 100 g) was determined by using Folin Ciocalteu assay. Results: Promising antimicrobial activities in terms of minimum inhibitory concentration (MIC) were noted for crude extract (25-200 µg/mL), n-hexane (100-400 µg/mL), ethyl acetate (50-200 µg/mL) and aqueous (100-400 µg/mL). Antidiabetic potential was significant at a dose level of 200-400 mg/kg bodyweight by reducing the blood glucose level at days 10 and 15. The percentage of 2,2-diphenyl-1-picrylhydrazyl (DPPH) values increase by increasing the concentration of the plant extract (10-100 µg/mL). The methanol extract was found to possess high agglutination activity. Conclusion: It was concluded that this plant species possess significant antimicrobial, antidiabetic, antioxidant, anticancer and haemagglutination activities, which could be attributed to the phenolic content of the extract.


RESUMEN Objetivo: Gymnosporia royleana (G royleana) Wall ex MA Lawson, localmente conocida como "Sur Azghee", se utiliza tradicionalmente para el tratamiento de diversas enfermedades. En la investigación presente, tratamos de validar científicamente su uso tradicional en varias condiciones, tales como las infecciones microbianas y el cáncer, así como explorar sus actividades farmacológicas adicionales mediante el tamizado aleatorio frente a los métodos farmacológicos localmente accesibles, independientemente de sus usos tradicionales como ensayos antidiabéticos, hemaglutinantes, y antioxidantes. Métodos: La extracción se realizó mediante una metodología de maceración en frío. Un método de dilución se utilizó para la prueba de susceptibilidad antimicrobiana utilizando diferentes concentraciones. Se utilizó el protocolo inducido por estreptozotocina (STZ) para evaluar la actividad antidiabética a un nivel de dosis de 200, 400 mg/kg. La actividad antioxidante, la actividad de hemaglutinación, y las actividades anticancerígenas contra las líneas celulares HepG-2 y MCF-7, se determinaron según los protocolos establecidos. De modo similar. la cantidad máxima de contenido fenólico (12.02 mg 100 g) se determinó mediante el uso del ensayo Folin-Ciocalteu. Resultados: Se observaron actividades antimicrobianas prometedoras en términos de la concentración inhibitoria mínima (CIM) para el extracto crudo (25-200 μg/mL), el n-hexano (100-400 μg/mL), el acetato de etilo (50-200 μg/mL), y el extracto acuoso (100-400 μg/mL). El potencial antidiabético fue significativo a un nivel de dosis de 200-400 mg/kg de peso corporal mediante la reducción del nivel de glucosa en sangre a los 10 y 15 días. El porcentaje de los valores de 2,2-difenil-1-picrilhidracilo (DPPH) se incrementa al aumentar la concentración del extracto de la planta (10-100 μg/mL). Se halló que el extracto de metanol posee una alta actividad de aglutinación. Conclusión: Se concluyó que esta especie de planta posee importantes actividades antimicrobianas, antidiabéticas, antioxidantes, anticancerígenas y hemaglutinantes, que podrían atribuirse al contenido fenólico del extracto.


Assuntos
Animais , Camundongos , Extratos Vegetais/farmacologia , Celastraceae/química , Anti-Infecciosos/farmacologia , Antineoplásicos/farmacologia , Diabetes Mellitus/tratamento farmacológico , Modelos Animais de Doenças , Hemaglutinação , Hipoglicemiantes/farmacologia , Antioxidantes/farmacologia
20.
Molecules ; 24(5)2019 Feb 28.
Artigo em Inglês | MEDLINE | ID: mdl-30823439

RESUMO

An analytical method using UHPLC-MS was developed and applied to 16 crude CH2Cl2 extracts from Australian Celastraceae plants; the endemic plant materials were accessed from Griffith University's NatureBank resource and included bark, fruit, leaf, root, twig and mixed samples, all of which were collected from Queensland, Australia. The generated UHPLC-MS data were analysed and dereplicated using the scientific databases Dictionary of Natural Products and SciFinder Scholar in order to potentially identify new dihydro-ß-agarofurans from local Celastraceae plants. These investigations led to the large-scale extraction and isolation work on a prioritised fruit sample that belonged to the rainforest plant Denhamia celastroides. Chemical investigations resulted in the purification of four new natural products, denhaminols O⁻R (1⁻4), along with the related and known compound, denhaminol G (5). The structures of all the new compounds were determined via detailed analysis of NMR and MS data.


Assuntos
Celastraceae/química , Extratos Vegetais/química , Sesquiterpenos/análise , Sesquiterpenos/química , Austrália , Cromatografia Líquida de Alta Pressão , Espectrometria de Massas , Floresta Úmida
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