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1.
Braz. J. Pharm. Sci. (Online) ; 59: e19334, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1439515

RESUMO

Abstract Present study analysed the therapeutic potential of traditionally acclaimed medicinal herb Nanorrhinum ramosissimum, using plant parts extracted with different solvents (10 mg/mL). Shoot extracts exhibited comparatively better antimicrobial properties, in comparison to root extracts. Total phenolic content was estimated, to ascertain its dependency on antioxidant properties of plant extracts. Antioxidant assay revealed promising results in comparison to IC50 value of standard ascorbic acid (52.2±0.07 µg/mL), for methanolic extracts of shoot (61.07±0.53 µg/mL and 64.33±0.33 µg/mL) and root (76.705±0.12 µg/mL and 89.73±0.28 µg/ mL) for in vivo and in vitro regenerants respectively. Correlation coefficient R2 values ranged between 0.90-0.95, indicating a positive correlation between phenolic contents and antioxidant activity. Plant extracts were also able to inhibit DNA oxidative damage again indicating their antioxidative potential. Antidiabetic potential was confirmed by alpha amylase inhibition assay where shoot methanolic extracts (invivo, in vitro) exhibited the best IC50 values (54.42±0.16 µg/mL, 66.09±0.12 µg/mL) in comparison to standard metformin (41.92±0.08 µg/mL). Ethanolic extracts of roots (in vitro, invivo) exhibited the relative IC50 values (88.97±0.32µg/mL,96.63±0.44 µg/mL) indicating that shoot parts had a better alpha amylase inhibition property; thus proving the herb's bioactive potential and its prospective therapeutic source for curing various ailments.


Assuntos
Plantas Medicinais/efeitos adversos , Extratos Vegetais/análise , Scrophulariaceae/classificação , Antioxidantes/farmacologia , Técnicas In Vitro/métodos , Hipoglicemiantes/agonistas
2.
Food Chem Toxicol ; 147: 111899, 2021 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-33279675

RESUMO

Pesticides are used to control and combat insects and pests in the agricultural sector, households, and public health programs. The frequent and disorderly use of these pesticides may lead to variety of undesired effects. Therefore, natural products have many advantages over to synthetic compounds to be used as insecticides. The goal of this study was to find natural products with insecticidal potential against Musca domestica and Mythimna separata. To achieve this goal, we developed predictive QSAR models using MuDRA, PLS, and RF approaches and performed virtual screening of 117 natural products. As a result of QSAR modeling, we formulated the recommendations regarding physico-chemical characteristics for promising compounds active against Musca domestica and Mythimna separata. Homology models were successfully built for both species and molecular docking of QSAR hits vs known insecticides allowed us to prioritize twenty-two compounds against Musca domestica and six against Mythimna separata. Our results suggest that pimarane diterpenes, abietanes diterpenes, dimeric diterpenes and scopadulane diterpenes obtained from aerial parts of species of the genus Calceolaria (Calceolariaceae: Scrophulariaceae) can be considered as potential insecticidal.


Assuntos
Dípteros/efeitos dos fármacos , Diterpenos/química , Diterpenos/farmacologia , Inseticidas/farmacologia , Animais , Desenho de Fármacos , Moscas Domésticas/efeitos dos fármacos , Modelos Biológicos , Estrutura Molecular , Relação Quantitativa Estrutura-Atividade , Scrophulariaceae/química , Sensibilidade e Especificidade
3.
Rev. cuba. plantas med ; 24(3): 1-10, 2019. tab, ilus
Artigo em Espanhol | MOSAICO - Saúde integrativa | ID: biblio-1247383

RESUMO

Introducción: la especie Capraria biflora L. perteneciente a la familia Scrophulariaceae, presenta una larga historia en la medicina tradicional por tener gran aplicación en varios tratamientos: cuyas causas podrían estar relacionados con infecciones antimicrobianas. Objetivo: Determinar la actividad antimicrobiana del extracto acuoso liofilizado de la especie Capraria biflora L. frente a una batería mínima de microorganismos de interés clínico. Métodos: la obtención del extracto se realizó por secado en horno, pulverización en un mortero, extracción por decocción y posterior liofilización. La actividad antibacteriana del extracto acuoso se evaluó in vitro, en dos concentraciones (10 y 50 mg/mL), mediante el sistema de ensayo de difusión en agar, con una batería mínima de cepas de microorganismos compuesta por cuatro bacterias Gram negativas: Klebsiella neumoneae (ATCC 10031), Salmonella tiphymurium (ATCC 14028), Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922), una bacteria Gram positiva: Staphylococcus aureus (ATCC 6538), y dos levaduras Cándida albicans (ATCC 10231) y Saccharomyces cerevisiae (BCTP 20/agosto/2008). Resultados: el extracto acuoso de las hojas de Capraria biflora L no presenta actividad antimicrobiana, a las concentraciones estudiadas, frente a las cepas de microorganismos de interés clínico utilizadas en el ensayo. Conclusiones: se reporta por primera vez la evaluación de la actividad antimicrobiana del extracto acuoso liofilizado de las hojas de Capraria biflora L. frente a cepas de bacterias y hongos de interés clínico a las concentraciones de 10 y 50 mg/mL. No se encontró un efecto inhibitorio y se recomienda realizar otros estudios de actividad antimicrobiana que inserten la temática de la virulencia microbiana, encaminados a evaluar el posible efecto bacteriostático que pueda presentar este extracto.


Introduction: the species Capraria biflora L., from the Scrophulariaceae family, has a long history of use in traditional medicine for the treatment of various disorders whose causes could be related to microbial infections. Objective: determine the antimicrobial activity of lyophilized aqueous extract from the species Capraria biflora L. against a minimum set of microorganisms of clinical interest. Methods: the extract was obtained by oven drying, pulverization in a mortar, decoction and lyophilization. In vitro antibacterial activity of the aqueous extract was evaluated at two concentrations (10 and 50 mg/ml) by the agar diffusion test with a minimum set of microorganism strains composed of four gram-negative bacteria: Klebsiella neumoneae (ATCC 10031), Salmonella tiphymurium (ATCC 14028), Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922), one gram-positive bacterium: Staphylococcus aureus (ATCC 6538), and two yeasts: Candida albicans (ATCC 10231) and Saccharomyces cerevisiae (BCTP 20/08/2008). Results: at the study concentrations, the aqueous extract of Capraria biflora L. leaves does not display antimicrobial activity against the strains of microorganisms of clinical interest evaluated in the assay. Conclusions: this is the first evaluation of the antimicrobial activity of lyophilized aqueous extract from leaves of Capraria biflora L. against strains of bacteria and fungi of clinical interest at concentrations of 10 and 50 mg/ml. No inhibitory effect was found. It is recommended to conduct further antimicrobial activity studies incorporating the topic of microbial virulence, aimed at evaluating the potential bacteriostatic effect of the study extract.


Assuntos
Scrophulariaceae , Anti-Infecciosos , Antibacterianos , Antifúngicos , Plantas Medicinais , Cuba , Liofilização , Medicina Tradicional
4.
Bioorg Med Chem Lett ; 26(2): 435-439, 2016 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-26684850

RESUMO

Biflorin 1 is a biologically active quinone, isolated from Capraria biflora. Five new biflorin-based nitrogen derivatives were synthesized, of which two were mixtures of (E)- and (Z)- isomers: (Z)-2a, (Z)-2b, (Z)-3a, (Z)- and (E)-3b, (Z)- and (E)-3c. The antibacterial activity was investigated using the microdilution method for determining the minimum inhibitory concentration (MIC) against six bacterial strains. Tests have shown that these derivatives have potential against all bacterial strains. The cytotoxic activity was also evaluated against three strains of cancer cells, but none of the derivatives showed activity.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Hidrazonas/farmacologia , Naftoquinonas/farmacologia , Oximas/farmacologia , Scrophulariaceae/química , Antibacterianos/síntese química , Antibacterianos/química , Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/química , Bactérias/efeitos dos fármacos , Infecções Bacterianas/tratamento farmacológico , Linhagem Celular Tumoral , Humanos , Hidrazonas/síntese química , Hidrazonas/química , Testes de Sensibilidade Microbiana , Naftoquinonas/síntese química , Naftoquinonas/química , Neoplasias/tratamento farmacológico , Oximas/síntese química , Oximas/química
5.
Ann Bot ; 116(5): 789-95, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-26199385

RESUMO

BACKGROUND AND AIMS: Studies that have evaluated the effects of heterospecific pollen (HP) receipt on plant reproductive success have generally overlooked the variability of the natural abiotic environment in which plants grow. Variability in abiotic conditions, such as light and water availability, has the potential to affect pollen-stigma interactions (i.e. conspecific pollen germination and performance), which will probably influence the effects of HP receipt. Thus, a more complete understanding of the extent, strength and consequences of plant-plant interactions via HP transfer requires better consideration of the range of abiotic conditions in which these interactions occur. This study addresses this issue by evaluating the effects of two HP donors (Tamonea curassavica and Angelonia angustifolia) on the reproductive success of Cuphea gaumeri, an endemic species of the Yucatan Peninsula. METHODS: Mixed (conspecific pollen and HP) and pure (conspecific pollen only) hand-pollinations were conducted under varying conditions of water and light availability in a full factorial design. Reproductive success was measured as the number of pollen tubes that reached the bottom of the style. KEY RESULTS: Only one of the two HP donors had a significant effect on C. gaumeri reproductive success, but this effect was dependent on water and light availability. Specifically, HP receipt caused a decrease in pollen tube growth, but only when the availability of water, light or both was low, and not when the availability of both resources was high. CONCLUSIONS: The results show that the outcome of interspecific post-pollination interactions via HP transfer can be context-dependent and vary with abiotic conditions, thus suggesting that abiotic effects in natural populations may be under-estimated. Such context-dependency could lead to spatial and temporal mosaics in the ecological and evolutionary consequences of post-pollination interactions.


Assuntos
Lythraceae/fisiologia , Tubo Polínico/crescimento & desenvolvimento , Pólen/fisiologia , Scrophulariaceae/fisiologia , Verbenaceae/fisiologia , Meio Ambiente , Luz , México , Reprodução , Especificidade da Espécie , Água/metabolismo
6.
Molecules ; 20(5): 8595-604, 2015 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-25985360

RESUMO

Capraria biflora L. is a shrub from the Scrophulariaceae family which produces in its roots a compound named biflorin, an o-naphthoquinone that shows activity against Gram-positive bacteria and fungi and also presents antitumor and antimetastatic activities. However, biflorin is hydrophobic and photosensitive. These properties make its application difficult. In this work we prepared biflorin micellar nanostructures looking for a more effective vehiculation and better preservation of the biological activity. Biflorin was obtained, purified and characterized by UV-Vis, infrared (IR) and 1H- and 13C-NMR. Micellar nanostructures of biflorin were then assembled with Tween 80®, Tween 20® and saline (0.9%) and characterized by UV-Vis spectroscopy and dynamic light scattering (DLS). The results showed that the micellar nanostructures were stable and presented an average size of 8.3 nm. Biflorin micellar nanostructures' photodegradation was evaluated in comparison with biflorin in ethanol. Results showed that the biflorin in micellar nanostructures was better protected from light than biflorin dissolved in ethanol, and also indicated that biflorin in micelles were efficient against Gram-positive bacteria and yeast species. In conclusion, the results showed that the micellar nanostructures could ensure the maintenance of the biological activity of biflorin, conferring photoprotection. Moreover, biflorin vehiculation in aqueous media was improved, favoring its applicability in biological systems.


Assuntos
Anti-Infecciosos/farmacologia , Candida/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Naftoquinonas/farmacologia , Anti-Infecciosos/química , Micelas , Testes de Sensibilidade Microbiana , Nanoestruturas/química , Naftoquinonas/química , Raízes de Plantas/química , Scrophulariaceae/química
7.
Genet Mol Res ; 14(4): 17472-81, 2015 Dec 21.
Artigo em Inglês | MEDLINE | ID: mdl-26782390

RESUMO

Biflorin is an o-naphthoquinone isolated from the roots of the plant Capraria biflora L. (Scrophulariaceae). In this study, the cytotoxic effects of biflorin were verified, and late apoptosis was detected in various cancer cell lines by in situ analysis. The cytotoxicity was further evaluated exclusively for 48 h of treatment in different tumor and non-tumor cell lines (Hep-2, HeLa, HT-29, A-375, and A-549, and HEK-293, respectively). The results indicated that biflorin induced selective cytotoxicity in tumor cells. HeLa cells were more susceptible to biflorin, followed by HT-29, A-549, A-375, and Hep-2 at all concentrations (range 5-50 µg/mL), and the highest half-maximal inhibitory concentration IC50 (56.01 ± 1.17 µg/mL) was observed in HEK-293 cells. Late apoptotic/necrotic events, observed by in situ immunostaining with Annexin V, varied with each cell line; an increase in late apoptotic events was observed corresponding to the increase in biflorin dosage. Hep-2 cells showed a greater percentage of late apoptotic events among the tumor cell lines when treated with higher concentrations of biflorin (69.63 ± 2.28%). The non-tumor HEK-293 line showed greater resistance to late apoptotic events, as well as a lower level of cytotoxicity (77.69 ± 6.68%) than the tested tumor lines. The data presented indicate that biflorin showed an important, possibly selective, cytotoxicity against tumor cell lines, thereby revealing a promising novel substance with potential anticancer activity for tumor therapy.


Assuntos
Antineoplásicos Fitogênicos/administração & dosagem , Naftoquinonas/administração & dosagem , Neoplasias/tratamento farmacológico , Antineoplásicos Fitogênicos/química , Apoptose/efeitos dos fármacos , Linhagem Celular Tumoral , Células HEK293 , Humanos , Naftoquinonas/química , Neoplasias/patologia , Scrophulariaceae/química
8.
Nat Prod Res ; 28(15): 1187-90, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-24735384

RESUMO

A new iridoid glucoside has been isolated from the Chilean native Alonsoa meridionalis (L.f.) Kuntze. Its structure has been assigned as 6'-O-ß-d-glucopyranosyl-8-O-acetylharpagide (1) by using spectroscopic methods. Harpagoside (2), laterioside (3) and verbascoside (4) were also identified.


Assuntos
Glicosídeos Iridoides/isolamento & purificação , Scrophulariaceae/química , Chile , Glicosídeos , Glicosídeos Iridoides/química , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Piranos
9.
Mol Phylogenet Evol ; 76: 93-101, 2014 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-24636896

RESUMO

The taxa of the Leucophyllum pringlei clade were used to understand the influence of the Neogene orogenesis and the Quaternary climate cycles on the diversification of the flora of the xeric regions of North America. This clade includes the five southernmost species of the genus: L. ambiguum, L. flyrii, L. pruinosum and L. ultramonticola, which are distributed throughout the Chihuahuan Desert north of the Trans-Mexican Volcanic Belt, and L. pringlei in the region of Tehuacán-Cuicatlán south of this mountain range. Here we test whether these species diverged during the pluvial periods of the Pleistocene, and whether L. pringlei diverged earlier from the other species during the uplift of the Trans-Mexican Volcanic Belt. Using three plastid regions (psbA-trnH, psbK-psbI, trnL-F) and a nuclear (ITS) marker, phylogenetic analyses were carried out, along with a reconstruction of their ancestral area. Trees retrieved the five species in a monophyletic group with the most recent common ancestor distributed in the Sinaloan dry forest during the Late Miocene (8.08Ma), from where it dispersed to the Chihuahuan Desert during the Late Miocene (6.35Ma). The secondary uplift of the Sierra Madre Occidental during the Late Miocene to Early Pliocene influenced a vicariance event. Divergence between L. pringlei and the species from north of the Trans-Mexican Volcanic Belt occurred during the second volcanic episode in the Late Miocene (7.5-3Ma). The most recent common ancestor of L. ambiguum, L. pruinosum and L. ultramonticola was widely distributed in the southern part of the Chihuahuan Desert during the Early to Late Pliocene (3.50Ma). The diversification of these three species occurred in the Middle Pleistocene (0.9Ma) during the pluvial and inter-pluvial cycles.


Assuntos
Filogenia , Scrophulariaceae/classificação , Scrophulariaceae/genética , Clima Desértico , Marcadores Genéticos/genética , México , Plastídeos/genética , Análise Espaço-Temporal , Erupções Vulcânicas
10.
Ann Bot ; 113(2): 251-66, 2014 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24252281

RESUMO

BACKGROUND AND AIMS: The underlying evolutionary processes of pollinator-driven floral diversification are still poorly understood. According to the Grant-Stebbins model speciation begins with adaptive local differentiation in the response to spatial heterogeneity in pollinators. Although this crucial process links the micro- and macroevolution of floral adaptation, it has received little attention. In this study geographical phenotypic variation was investigated in Patagonian Calceolaria polyrhiza and its pollinators, two oil-collecting bee species that differ in body size and geographical distribution. METHODS: Patterns of phenotypic variation were examined together with their relationships with pollinators and abiotic factors. Six floral and seven vegetative traits were measured in 45 populations distributed across the entire species range. Climatic and edaphic parameters were determined for 25 selected sites, 2-16 bees per site of the most frequent pollinator species were captured, and a critical flower-bee mechanical fitting trait involved in effective pollination was measured. Geographical patterns of phenotypic and environmental variation were examined using uni- and multivariate analyses. Decoupled geographical variation between corolla area and floral traits related to the mechanical fit of pollinators was explored using a Mantel test. KEY RESULTS: The body length of pollinators and the floral traits related to mechanical fit were strongly correlated with each other. Geographical variation of the mechanical-fit-related traits was decoupled from variation in corolla size; the latter had a geographical pattern consistent with that of the vegetative traits and was mainly affected by climatic gradients. CONCLUSIONS: The results are consistent with pollinators playing a key role in shaping floral phenotype at a geographical scale and promoting the differentiation of two floral ecotypes. The relationship between the critical floral-fit-related trait and bee length remained significant even in models that included various environmental variables and an allometric predictor (corolla area). The abiotic environment also has an important role, mainly affecting floral size. Decoupled geographical variation between floral mechanical-fit-related traits and floral size would represent a strategy to maintain plant-pollinator phenotypic matching in this environmentally heterogeneous area.


Assuntos
Abelhas/fisiologia , Flores/anatomia & histologia , Geografia , Óleos de Plantas/metabolismo , Característica Quantitativa Herdável , Scrophulariaceae/anatomia & histologia , Scrophulariaceae/fisiologia , Animais , Argentina , Clima , Flores/fisiologia , Análise Multivariada , Fenótipo , Polinização , Análise de Regressão
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