“…Important pharmacological effects were reported for red embaúba, such as anti-inflammatory, antioxidant, hepatoprotective, antiviral, , anti-acid secretion, hypoglycemic and vasorelaxant, and antihypertensive activities, which have been credited to the presence of catechins, procyanidins, flavonoids, and chlorogenic and caffeic acids …”
The use of medicinal plants concomitantly with conventional drugs can result in herb−drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb−drug interactions. Among CYP enzymes, CYP3A4 and CYP2D6 are the most relevant since they metabolize about 50% and 30% of the drugs on the market, respectively. Thus, the main goal of this study was to evaluate the occurrence of in vitro interactions between medicinal plant extracts and drug substrates of CYP3A4 and CYP2D6 enzymes. Standardized extracts from nine medicinal plants (Bauhinia forficata, Cecropia glaziovii, Cimicif uga racemosa, Cynara scolymus, Echinacea sp., Ginkgo biloba, Glycine max, Ilex paraguariensis, and Matricaria recutita) were evaluated for their potential interactions mediated by CYP3A4 and CYP2D6 enzymes. Among the extracts tested, C. glaziovii (red embauba) showed the most relevant inhibitory effects of CYP3A4 and CYP2D6 activity, while I. paraguariensis (yerba mate) inhibited CYP3A4 activity. Both extracts were chemically analyzed by UPLC-MS/MS, and these inhibitory effects could lead to clinically potential and relevant interactions with the drug substrates of these isoenzymes.
“…Important pharmacological effects were reported for red embaúba, such as anti-inflammatory, antioxidant, hepatoprotective, antiviral, , anti-acid secretion, hypoglycemic and vasorelaxant, and antihypertensive activities, which have been credited to the presence of catechins, procyanidins, flavonoids, and chlorogenic and caffeic acids …”
The use of medicinal plants concomitantly with conventional drugs can result in herb−drug interactions that cause fluctuations in drug bioavailability and consequent therapeutic failure and/or toxic effects. The CYP superfamily of enzymes plays an important role in herb−drug interactions. Among CYP enzymes, CYP3A4 and CYP2D6 are the most relevant since they metabolize about 50% and 30% of the drugs on the market, respectively. Thus, the main goal of this study was to evaluate the occurrence of in vitro interactions between medicinal plant extracts and drug substrates of CYP3A4 and CYP2D6 enzymes. Standardized extracts from nine medicinal plants (Bauhinia forficata, Cecropia glaziovii, Cimicif uga racemosa, Cynara scolymus, Echinacea sp., Ginkgo biloba, Glycine max, Ilex paraguariensis, and Matricaria recutita) were evaluated for their potential interactions mediated by CYP3A4 and CYP2D6 enzymes. Among the extracts tested, C. glaziovii (red embauba) showed the most relevant inhibitory effects of CYP3A4 and CYP2D6 activity, while I. paraguariensis (yerba mate) inhibited CYP3A4 activity. Both extracts were chemically analyzed by UPLC-MS/MS, and these inhibitory effects could lead to clinically potential and relevant interactions with the drug substrates of these isoenzymes.
“…Cecropia glaziovii freeze-dried extract was employed as model drug due to its high hygroscopicity, which leads to an increase in capillary forces acting on the particles loading it [ 14 ]. C. glaziovii is a highly bioactive vegetal species [ 15 – 19 ] and it has been studied before as a bioactive product for pharmaceutical purposes [ 20 , 21 ]. In the coating studies, two hydrophilic polymers (Kollidon® VA64 and Kollicoat® Protect) were assessed as coating materials to attach microspheres to the surface of carrier pellets.…”
Micro- and nanoparticles have been vastly studied due to their biopharmaceutical advantages. However, these particles generally display very weak packing and poor mechanical properties. Hereby, a new methodology is proposed to associate poorly flowing particles to macrostructures targeting the improvement of flowability and redispersibility of the particles. Cecropia glaziovii-loaded PLGA microspheres (4.59 ± 0.04 μm) were associated with carrier pellets by film coating in a top-spray fluid bed equipment. Optimal conditions were determined employing a IV-Optimal factorial design and RGB image analysis as 1% (w/v) Kollicoat® Protect as coating polymer (2:1 weight ratio of coating suspension to carrier pellets), containing 5 mg/mL microspheres (loading of 28.07 ± 1.01 mg/g). The method led to an improvement of the overall flowability. No relevant molecular interactions between PLGA microspheres and polymers were found. Microspheres detached rapidly from the surface of the pellets, without agglomeration, when exposed to hydrodynamic forces. In vitro release profiles, prior to and after fluid bed coating, showed no relevant changes in drug release rate and extent. The methodology developed is suitable for further applications when an improvement on the flow properties and redispersibility of the product is desired. We showed an easy-to-implement methodology that can be executed without significant increase in costs.
“…Furthermore, this flavonoid-containing fraction induced cardiac depression and inhibited adrenaline-induced contractions in aortic rings (Table 5S, Supporting Information) [90,91]. Similarly, a standardized hydroalcoholic extract of C. glaziovii caused ring aorta relaxation (Table 5S, Supporting Information) [71], as well as its butanol fraction. The latest fraction also blocked the peak Ca ++ current in chromaffin cells of a PC12 cell line [85].…”
Section: Cardiovascular Effectmentioning
confidence: 86%
“…Thus, a standardized hydroalcoholic extract of C. glaziovii showed antihyperglycemic activity and improved glucose tolerance in diabetic rats [71]; aqueous and butanol extracts of C. obtusifolia significantly reduced blood glucose levels in normal and pancreatectomized dogs [72], diabetic rats [73], diabetic mice [74], and hyperglycemic rabbits [75,76], and its methanol extract reduced plasma glucose in healthy mice [77] (Table 5S, Supporting Information). Interestingly, the hypoglycemia observed by the aqueous extract of C. obtusifolia was not accompanied by a rise in plasmatic insulin, suggesting that this effect was unrelated to beta-pancreatic cell stimuli [72].…”
Section: Hypoglycemic Effect and Anti-diabetic Potentialmentioning
This work covers a systematic review of literature about the genus Cecropia from 1978 to 2020, emphasizing the analysis of 10 of the most relevant species and their associated biological activities. Cecropia is a neotropical genus, which comprises about 61 native species in the American continent where it is known to be part of the traditional medicine of numerous countries. Secondary metabolites described for this genus showed an elevated structural and functional diversity, where polyphenols have been the most abundant. Based on this diversity, Cecropia phytochemicals represent an important source of potential therapeutic agents yet to be exploited. This review also highlights the effectiveness of combining chemometrics and ultra-performance liquid chromatography-tandem mass spectrometry as a novel approach to successfully single out Cecropia species phytochemicals. While the medicinal use of Cecropia species is officially recognized
in National Pharmacopoeias and Formularies of several Latin American countries, it is important to recognize that these phytomedicines are complex mixtures requiring a thorough understanding of their chemical composition and their correlation with biological activities to guarantee their quality, safety, and efficacy.
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