Roots´ bark extract of Brosimum gaudichaudii Trécul (EBGT) is traditionally used for photochemotherapy of vitiligo due to the presence of furanocoumarins psoralen (PSO) and 5-methoxypsoralen (5-MOP) as major compounds. Though plant extracts may provide additional highly permeable psoralens-like substances which may act synergically on vitiligo's therapy. Thus, the aim of this work was to develop an LC-MS/MS method for screening new highly permeable furanocoumarins from B. gaudichaudii and to compare biomarkers permeability and solubility provided as single compounds or as crude extract, according to BCS. An optimized LC-MS/MS method showed twelve permeable and bioactive compounds, among which 9 furanocoumarins, 2 pyranocoumarins and 1 dihydrocinnamic acid derivative were detected in EBGT samples. Solubility of PSO and 5-MOP was found to be, respectively, six- and eleven-fold higher in crude extract than as pure compounds. Permeability (P) of PSO and 5-MOP in EBGT were higher than metoprolol, the low/high BCS permeability class boundary reference compound. Hence, both biomarkers were considered as highly permeable (BCS2) compounds. Their permeability were concentration-dependent displaying values from 30.26 ± 5.13-8.21 ± 2.16 × 10 cm/s and 10.72 ± 1.73-6.07 ± 1.27 × 10 cm/s, respectively, over a wide range (2.3-200.0 mg mL-1). Thus, a carrier-mediated absorption process is suggested as the main mechanism. Accordingly, all additional permeated coumarins, identified by LC-MS/MS, showed to be at comparable amount of biomarkers in the permeated samples inferring similar high permeability rate. Moreover, biomarkers and other highly absorbable and bioactive linear furanocoumarins from EBGT may be used for vitiligo´s photochemotherapy. Taken together, these findings bring additional evidences for using crude plant extract when aiming synergistic effects of bioactive compounds on melanogenic therapies.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.jpba.2020.113593 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Membranes of Polymer of Intrinsic Microporosity PIM-1 for Gas Separation: Modification Strategies and Meta-Analysis.
Nanomicro Lett
January 2025
Department of Chemical Engineering, Faculty of Science and Engineering, The University of Manchester, Manchester, M13 9PL, UK.
Polymers of intrinsic microporosity (PIMs) have received considerable attention for making high-performance membranes for carbon dioxide separation over the last two decades, owing to their highly permeable porous structures. However, challenges regarding its relatively low selectivity, physical aging, and plasticisation impede relevant industrial adoptions for gas separation. To address these issues, several strategies including chain modification, post-modification, blending with other polymers, and the addition of fillers, have been developed and explored.
View Article and Find Full Text PDFHuman keratinocytes grown at a gas-permeable interface in vitro stratify correctly to generate engineered human epidermis.
Cytotherapy
December 2024
School of Biological Sciences, University of Auckland, Auckland, New Zealand; Maurice Wilkins Centre, The University of Auckland, Auckland, New Zealand. Electronic address:
Background: One of the key functions of human skin is to provide a barrier, protecting the body from the surrounding environment and maintaining homeostasis of the internal environment. A mature, stratified epidermis is critical to achieve skin barrier function and is particularly important when producing skin grafts in vitro for wound treatment. For decades epidermal stratification has been achieved in vitro by culturing keratinocytes at an air-liquid interface, triggering proliferating basal keratinocytes to differentiate and form all epidermal layers.
View Article and Find Full Text PDFEnhancing Solubility of a BCS Class II Drug- Itraconazole by Developing and Optimizing Solid Lipid Nanoparticles using a Central Composite Design.
Pharm Nanotechnol
January 2025
Department of Pharmaceutical Sciences, Philadelphia College of Pharmacy, Saint Joseph University, Philadelphia, PA.
Background: Itraconazole (ICZ) has been approved by the FDA to treat many fungal infections including, blastomycosis, histoplasmosis, and aspergillosis. ICZ can be also used as prophylaxis in the population who are at high risk for developing systemic fungal infections, such as HIV patients, and chemotherapy patients.
Aim: However, since ICZ is a BCS Class II drug that has low solubility and high permeability, leads to low oral bioavailability.
Gut Microbiota Metabolites Sensed by Host GPR41/43 Protect Against Hypertension.
Circ Res
January 2025
Hypertension Research Laboratory, School of Biological Sciences (R.R.M., T.Z., E.D., L.X., A.B.-W., H.A.J., M.N., M.P., K.C.L., W.Q., J.A.O.D., F.Z.M.).
Background: Fermentation of dietary fiber by the gut microbiota leads to the production of metabolites called short-chain fatty acids, which lower blood pressure and exert cardioprotective effects. Short-chain fatty acids activate host signaling responses via the functionally redundant receptors GPR41 and GPR43, which are highly expressed by immune cells. Whether and how these receptors protect against hypertension or mediate the cardioprotective effects of dietary fiber remains unknown.
View Article and Find Full Text PDFInfluence of environmental settings, including vegetation, on speciation of the redox-sensitive elements in the sediments of monomictic Lake Kinneret.
Limnology (Tokyo)
July 2024
Department of Geological and Environmental Sciences, Faculty of Natural Sciences, Ben-Gurion University of the Negev, P.O. Box 653, 84105 Beer Sheva, Israel.
Unlabelled: The redox conditions in the littoral limnic sediments may be affected by the penetration of plant roots which provide channels for oxygen transport into the sediment while decomposition of the dead roots results in consumption of oxygen. The goal of this work was to study the impact of environmental parameters including penetration of roots of L. into the sediments on cycling of the redox-sensitive elements in Lake Kinneret.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!