Inclusion Complexes of β and HPβ-Cyclodextrin with α, β Amyrin and In Vitro Anti-Inflammatory Activity

Júnior, Walter Ferreira da Silva; Menezes, Danielle Lima Bezerra de; Oliveira, Luana Carvalho de; Koester, Letícia Scherer; Almeida, Patrícia Danielle Oliveira de; Lima, Émerson Silva; Azevedo, Eduardo Pereira de; Júnior, Valdir Florêncio da Veiga; Lima, Ádley Antonini Neves de

doi:10.3390/biom9060241

Cited by 28 publications

(27 citation statements)

References 47 publications

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“…Due to the progress of nanomaterials, the assessment of the biological activity of precursor compounds for OA and UA, i.e., α- and β- amyrines, could also be considered. Earlier research results indicated the possibility of introducing amyrins into nano emulsions [ 89 ] or β-cyclodextrins [ 90 ]. Their possible anticancer activity should be evaluated in novel nanoformulations.…”

Section: Discussionmentioning

confidence: 99%

Nanoformulations for Delivery of Pentacyclic Triterpenoids in Anticancer Therapies

2021

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The search for safe and effective anticancer therapies is one of the major challenges of the 21st century. The ineffective treatment of cancers, classified as civilization diseases, contributes to a decreased quality of life, health loss, and premature mortality in oncological patients. Many natural phytochemicals have anticancer potential. Pentacyclic triterpenoids, characterized by six- and five-membered ring structures, are one of the largest class of natural metabolites sourced from the plant kingdom. Among the known natural triterpenoids, we can distinguish lupane-, oleanane-, and ursane-types. Pentacyclic triterpenoids are known to have many biological activities, e.g., anti-inflammatory, antibacterial, hepatoprotective, immunomodulatory, antioxidant, and anticancer properties. Unfortunately, they are also characterized by poor water solubility and, hence, low bioavailability. These pharmacological properties may be improved by both introducing some modifications to their native structures and developing novel delivery systems based on the latest nanotechnological achievements. The development of nanocarrier-delivery systems is aimed at increasing the transport capacity of bioactive compounds by enhancing their solubility, bioavailability, stability in vivo and ensuring tumor-targeting while their toxicity and risk of side effects are significantly reduced. Nanocarriers may vary in sizes, constituents, shapes, and surface properties, all of which affect the ultimate efficacy and safety of a given anticancer therapy, as presented in this review. The presented results demonstrate the high antitumor potential of systems for delivery of pentacyclic triterpenoids.

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Section: Discussionmentioning

confidence: 99%

Nanoformulations for Delivery of Pentacyclic Triterpenoids in Anticancer Therapies

2021

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“…Despite indicating good intestinal absorption, high log P values indicate low water solubility, which can lead to low oral bioavailability. The pharmacokinetics of compounds 8 , 15 and 17 have already been studied and their oral bioavailability can be improved by formulations such as nanoemulsions, nanoparticles, liposomes, polymeric micelles and cyclodextrin complexes (Abriata et al, 2017; Cavazos‐Garduño et al, 2015; Da Silva Júnior et al, 2019; Kumar et al, 2018; Liu et al, 2016; Moura et al, 2020; Qiu et al, 2019; Rodrigues et al, 2013; Soica et al, 2014; Wang et al, 2019; Zhou et al, 2019).…”

Section: Resultsmentioning

confidence: 99%

In silico approach of secondary metabolites from Brazilian herbal medicines to search for potential drugs against SARS‐CoV‐2

Amparo

Seibert

Almeida

et al. 2021

Phytotherapy Research

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The new severe acute respiratory syndrome coronavirus (SARS‐CoV‐2) recently emerged as a worrying pandemic, with many confirmed cases and deaths globally. Therefore, there is a clear need for identifying effective therapeutic options and a review of secondary metabolites related to Brazilian herbal medicines was performed as a strategy for the discovery of new antiviral agents. To confirm this potential, an in silico screening of the identified compounds identified was also evaluated. The review was performed by the PubMed database and the selected natural compounds were subjected to in silico analysis such as QSAR, molecular docking and ADMET. 497 secondary metabolites were identified from 23 species. The in silico assays indicated 19 potential anti‐SARS‐CoV‐2 compounds, being triterpenes and phenolic compounds. The indicated compounds showed a high affinity with proteins considered as the main molecular targets against SARS‐CoV‐2 and parameters indicated low toxicity. In addition to Brazilian medicinal plants, these compounds can be found in other species and they can be a base for the synthesis of other anti‐COVID‐19 drugs. Therefore, this review is important to conduct researches that address the emerging need for drugs in COVID‐19 treatment.

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“…With γ CD, a significant reduction in the main ABAME reflection was also observed, in addition to secondary reflections distinct from those of the individual components; this occurred mainly with the IC prepared with γ CD at the 2:1 molar ratio by rotary evaporation (EVG2), which showed medium-to-low intensity reflections at 7°, 14°, 15°, and 16° different from the other systems. These results suggest that the three proposed systems have a crystalline phase distinct from the isolated components, which is, therefore, an indication of complexation [ 19 , 20 ].…”

Section: Resultsmentioning

confidence: 99%

In Silico Study, Physicochemical, and In Vitro Lipase Inhibitory Activity of α,β-Amyrenone Inclusion Complexes with Cyclodextrins

Oliveira

Menezes

Silva

et al. 2021

IJMS

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α,β-amyrenone (ABAME) is a triterpene derivative with many biological activities; however, its potential pharmacological use is hindered by its low solubility in water. In this context, the present work aimed to develop inclusion complexes (ICs) of ABAME with γ- and β-cyclodextrins (CD), which were systematically characterized through molecular modeling studies as well as FTIR, XRD, DSC, TGA, and SEM analyses. In vitro analyses of lipase activity were performed to evaluate possible anti-obesity properties. Molecular modeling studies indicated that the CD:ABAME ICs prepared at a 2:1 molar ratio would be more stable to the complexation process than those prepared at a 1:1 molar ratio. The physicochemical characterization showed strong evidence that corroborates with the in silico results, and the formation of ICs with CD was capable of inducing changes in ABAME physicochemical properties. ICs was shown to be a stronger inhibitor of lipase activity than Orlistat and to potentiate the inhibitory effects of ABAME on porcine pancreatic enzymes. In conclusion, a new pharmaceutical preparation with potentially improved physicochemical characteristics and inhibitory activity toward lipases was developed in this study, which could prove to be a promising ingredient for future formulations.

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Inclusion Complexes of β and HPβ-Cyclodextrin with α, β Amyrin and In Vitro Anti-Inflammatory Activity

Cited by 28 publications

References 47 publications

Nanoformulations for Delivery of Pentacyclic Triterpenoids in Anticancer Therapies

Nanoformulations for Delivery of Pentacyclic Triterpenoids in Anticancer Therapies

In silico approach of secondary metabolites from Brazilian herbal medicines to search for potential drugs against SARS‐CoV‐2

In Silico Study, Physicochemical, and In Vitro Lipase Inhibitory Activity of α,β-Amyrenone Inclusion Complexes with Cyclodextrins

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