ABSTRACT
Botanical ingredients are widely used in food, dietary supplements, cosmetics, drugs, and other products. These ingredients may either be made as fresh material, dry and ground material, or as valorized sub-products obtained following more complex industrial process such as extraction, concentration, and purification. The plant sources of botanical ingredients are diverse. Roots, flowers, fruits, leaves, or seeds could be obtained from i) industrial crops (food and non-food); ii) wild plants (non-agroindustrial development); or iii) agroindustrial wastes (byproducts obtained during harvesting, post-harvesting, and industrial processing). Each of these sources is associated with specific challenges and advantages in the botanical ingredient industry. For example, industrial crops provide the most homogeneous raw material, but the degree of novelty and innovation in the development of these ingredients could be limited. Conversely, wild plants are the best source of novel ingredients; however, they require a lot of time and money to develop. These increased expenditures normally emerge from bioprospecting studies and legal procedures, given that the inclusion of a new ingredient is required. On the other hand, agroindustrial wastes are the most sustainable and environmentally friendly bioingredient sources; however their availability, homogeneity, and innocuousness are the most important challenges to solve.
Subject(s)
Humans , Botany , Pharmacists , Cosmetics , FoodABSTRACT
Objective: This study was designed to investigate the wound healing activity of aqueous extracts of Ullucus tuberosus (U. tuberosus) using in vitro models. Methods: Lyophilized pulp and acetone extracts of U. tuberosus were produced using ultrasound extraction. The capacity for collagenase activation was evaluated using fluo-rescence detection of the enzymatic activity. Then, the influence of U. tuberosus extracts on cell proliferation, cell migration and synthesis of the extracellular matrix (ECM) proteins, metalloproteinase (MMP-1) and pro-collagen was analyzed using human dermal fibroblasts in culture. Results: An increase in collagenase activity of 12%supports the utility of U. tuberosus as an agent for scar treatment. In addition, the extracts showed an increase in the pro-liferation and migration of human dermal fibroblasts and the production of pro-collagen and MMP-1 after treatment with U. tuberosus extracts. The increase in proliferation, migration and pro-collagen levels positively influenced the regeneration of scarless tissue during the proliferation phase, whereas the increase in MMP-1 may have favored the wound healing process during the remodeling and cellular differentiation phases. Conclusion: The results of this study show for first time that U. tuberosus is a promising candidate to support scarless tissue regeneration.
ABSTRACT
AbstractA new lycosinine derivative, 9-O-demethyllycosinine B, was isolated from the native Brazilian Hippeastrum breviflorumHerb., Amaryllidaceae, along with the well-known alkaloids lycosinine B and lycorine. The structure of the new compound was established by physical and spectroscopic methods. 9-O-demethyllycosinine B is the third lycosinine variant identified in the Amaryllidaceae family.
ABSTRACT
Taraxacum officinale F. H. Wigg, Asteraceae, is frequently misidentified or substituted with Hypochaeris radicata L., Asteraceae (false dandelion). To increase our knowledge of T. officinale and differentiate it from H. radicata, we investigated the two species using a combination of taxonomy, microscopy, and chromatographic studies via fingerprint profiles. Micromorphological characteristics were studied using scanning electron microscopy, while optic light microscopy was used for histochemical observations. Fingerprint profiles were constructed using HPTLC. T. officinale was found to have a morphologically distinct type of pluricellular trichomes that can be used to differentiate the two species, as these structures were not identified in H. radicata samples. Furthermore, two types of laticiferous vessels may also be distinctive characteristics of T. officinale at species level. In addition, the HPTLC data derived from methanolic extracts of H. radicata and T. officinale roots showed clearly different chemical profiles. Thus this study establishes the authenticity of T. officinale, and the observed parameters could help minimize drug substitutions in herbal medicines.
ABSTRACT
Introduction. Dihydrofolate reductase (DHFR) has been used successfully as a drug target in the area of anti-bacterial, anti-cancer and anti-malarial therapy. Although this bifunctional enzyme is also a potential drug target for treatment of leishmaniasis, there have been no reports on its efficacy against Leishmania ( Viannia ) species . Materials and methods. The gene encoding the bifunctional DHFR and thymidylate synthase (TS) of Le. (V.) braziliensis was isolated and expressed in E. coli. The enzyme was purified and characterized. The inhibitory effects of antifolates and four aporphine alkaloids on its activity were evaluated. Results. The full-length gene consists of a 1560-bp open reading frame encoding a 58 kDa translated peptide containing DHFR and TS domains linked together in a single polypeptide chain. The recombinant DHFR-TS enzyme revealed K m and V max values of 55.35 ± 4.02 µ M (mean ± SE) and 0.02 ± 5.34 x 10 -4 µ M/min respectively for dihydrofolic acid (H 2 F). The Le. braziliensis rDHFR-TS have Ki values for antimicrobial antifolates in the µM range. Methotrexate (MTX) was a more-potent inhibitor of enzymatic activity ( Ki = 22.0 µM) than trimethoprim ( Ki = 33 µM) and pyrimethamine ( Ki = 68 µM). These Ki values are significantly lower than those obtained for the aporphine alkaloids. Conclusion. The results of the study show the inhibitory effect of antifolate drugs on enzymatic activity, indicating that Le. braziliensis rDHFR-TS could be a model to studying antifolate compounds as potential antiprotozoal drugs.
Introducción. La dihidrofolato reductasa (DHFR) se ha utilizado como blanco molecular en tratamientos antibacterianos, anticancerígenos y antipalúdicos. También, actúa como blanco molecular en Leishmania ; sin embargo, no existen reportes de la enzima bifuncional en especies de Leishmania ( Viannia ). Materiales y métodos. Se ha aislado y expresado en Escherichia coli el gen que codifica para la enzima bifuncional DHFR y la timidilato-sintasa (TS) de Leishmania braziliensis . La enzima recombinante se purificó y caracterizó, y se evaluó el efecto inhibitorio de algunos antifolatos, así como de cuatro alcaloides aporfínicos. Resultados. El gen se compone de aproximadamente 1.560 pb y codifica un péptido de 58 kDa que contiene los dominios DHFR y TS ligados en una sola cadena polipeptídica. La enzima recombinante DHFR-TS, utilizando el dihidrofolato (H2F) como sustrato, presentó valores de K m y V max de 55,35 ± 4,02 (media ± el error estándar de la media) y de 0,02 ± 5,34 x 10 -4 , respectivamente. La enzima rDHFR-TS de L. braziliensis presentó valores de Ki para los antifolatos en el rango de micras. El metotrexato fue el inhibidor más potente de la actividad enzimática ( Ki =22,0 mM) en comparación del trimetoprim ( Ki =33 mM) y la pirimetamina ( Ki =68 mM). Estos valores de Ki son significativamente más bajos en comparación con los obtenidos para los alcaloides aporfínicos. Conclusión. Los resultados muestran el efecto inhibitorio de los antifolatos sobre la actividad enzimática, lo cual indica que la rDHFR-TS de L. braziliensis podría ser un modelo para estudiar moléculas antiprotozoarias potenciales.
Subject(s)
Folic Acid Antagonists/pharmacology , Leishmania/enzymology , Multienzyme Complexes/antagonists & inhibitors , Multienzyme Complexes/chemistry , Tetrahydrofolate Dehydrogenase/chemistry , Thymidylate Synthase/antagonists & inhibitors , Thymidylate Synthase/chemistryABSTRACT
Actualmente, los parásitos protozoarios son uno de los principales agentes causantes de morbilidad y mortalidad en el mundo, un problema complicado, además, por la aparición de resistencia a medicamentos en estos organismos. La resistencia a medicamentos observada en parásitos protozoarios se debe a diferentes mecanismos como la disminución de la entrada del medicamento a la célula por cambios en el transportador requerido, la pérdida de la activación del medicamento por parte del hospedero, las alteraciones en el blanco del medicamento y la expresión exagerada del transportador múltiple de medicamentos o glicoproteína P (Pgp). En esta revisión, nos centramos en: 1) el papel de las glicoproteínas P (Pgp) de la familia de proteínas ABC (ATP binding cassette) como los transportadores de múltiples medicamentos en la mediación de resistencia en protozoarios, especialmente en Leishmania, y en el desarrollo de resistencia cruzada para medicamentos estructural y funcionalmente no relacionados, y 2) en algunos conceptos relacionados con los mecanismos moduladores que podrían revertir la resistencia a medicamentos por fármacos y productos naturales. Numerosos moduladores o quimiosensibilizadores son conocidos por alterar la capacidad de las glicoproteínas P para mantener concentraciones intracelulares subtóxicas del medicamento; algunos ejemplos incluyen los bloqueadores de los canales de calcio como el verapamilo; sin embargo, se requieren altas concentraciones para una inhibición eficiente y duradera, las cuales producen efectos adversos indeseables. Por tanto, se necesitan más investigaciones relacionadas con los moduladores naturales para Pgp, los cuales podrían presentar menor toxicidad para el hospedero