Salvana Priscylla Manso Costa

Background/Objectives: Brazilian red propolis is a rich source of isoflavonoids with promising antioxidant and antileishmanial activities. However, its poor aqueous solubility and chemical instability limit its pharmaceutical application. This study aimed to develop microemulsion-based systems containing high concentrations of Brazilian red propolis extract (RPE) and evaluate their physicochemical properties, phytochemical composition, antioxidant capacity, and antileishmanial activity. Methods: Pseudoternary phase diagrams were constructed by water titration to select suitable microemulsion compositions. RPE was subsequently incorporated into the selected compositions to obtain RPE-loaded colloidal systems. The three selected RPE-free microemulsions and their corresponding RPE-loaded systems were characterized by pH, electrical conductivity, dynamic light scattering, rheological measurements, and polarized light microscopy (PLM). The RPE-loaded systems were further evaluated for phenolic marker content, antioxidant activity, and in vitro activity against Leishmania infantum. Results: Three RPE-loaded colloidal systems (F2-RPE12, F3-RPE30, and F4-RPE50) were developed. F2-RPE12 exhibited characteristics consistent with an oil-in-water microemulsion. Conductivity and PLM indicated physicochemical changes after RPE incorporation in F3-RPE30 and F4-RPE50, with localized birefringent features at higher RPE concentrations. Among the RPE-loaded systems, F4-RPE50 showed the highest phenolic and flavonoid contents and antioxidant activity. The RPE-loaded systems exhibited lower IC₅₀ values than RPE alone, with IC₅₀ values of 3.14, 2.28, and 0.56 µg·mL⁻¹ for F2-RPE12, F3-RPE30, and F4-RPE50, respectively, compared with 5.90 µg·mL⁻¹ for RPE. Conclusions: Overall, F4-RPE50 showed the most favorable phytochemical and biological performance, and the physicochemical and optical changes observed in the RPE-loaded systems open new avenues for investigating the relationship between structural organization and formulation performance.

Propolis is a natural product of honey bees whose chemical composition is influenced by different plant species and environmental factors, resulting in diverse biological activities. A new propolis type, the greenish-brown propolis (GBPUP), was identified in the northeast of Brazil. This study aimed to evaluate the influence of seasonal variation in the chemical composition of GBPUP extracts over a 12-month period. LC–ESI–Orbitrap–FTMS and UFLC–DAD–UV–Vis revealed a chemical composition with some differences to that of Brazilian green propolis, with pinocembrin as the major compound, followed by galangin, pinostrobin, chrysin, artepillin C, and pinobanksin. The extracts exhibited high levels of total phenolic, flavonoid, and flavanone contents and moderate to high antioxidant activity. Circos plot analysis showed that specific metabolites were responsible for the high activity against S. aureus (artepillin C, kaempferol, and ferulic acid) and C. albicans (galangin, pinobanksin, chrysin, and pinocembrin) and for moderate antibacterial activity against E. faecalis (rutin) and E. coli (luteolin, rutin, quercetin, and caffeic acid). ANOVA simultaneous component analysis (ASCA) showed a strong correlation between the metabolites (p-coumaric acid, artepillin C, luteolin) and leishmanicidal activity. Thus, seasonal evaluation allowed the identification of bioactive molecules, the months with greater bioactivity of the GBPUP extracts representing the first comprehensive study of the seasonality of this new and promising propolis variety.

Background/Objectives: Primary dysmenorrhea is a prevalent condition that causes severe uterine cramps in women worldwide. The objective of this work was to synthesize and characterize a novel immediate-release system using vitexin and ZIF-8, and to evaluate its pharmacological action in a model of primary dysmenorrhea. Methods: A 2² full factorial design guided the synthesis of the system. Physicochemical characterization was performed by FT-IR, TG, DSC, SEM, XRD, and in vitro release tests. Pharmacological activity was assessed in an oxytocin-induced dysmenorrhea model in mice. In addition, in silico molecular docking and molecular dynamics simulations were conducted to explore the potential mechanism of action of vitexin. Results: Optimal yield and loading capacity were achieved at the high levels of the factorial design. Characterization analyses confirmed the successful formation of the vitexin@ZIF-8 (VIT@ZIF-8) system. The release study demonstrated a markedly enhanced dissolution rate of vitexin. Both isolated vitexin and VIT@ZIF-8 reduced abdominal writhing when administered orally at 3 and 30 mg/kg, while intraperitoneal activity was observed only at 30 mg/kg. Computational analyses revealed favorable interactions of vitexin with aldose reductase (AKR1C3), suggesting this enzyme as a potential molecular target in dysmenorrhea. Conclusions: The VIT@ZIF-8 system represents a promising strategy to improve the dissolution profile of vitexin, although pharmacological activity in this model was not superior to the isolated compound. The combined in vivo and in silico evidence supports vitexin as a potential antidysmenorrheic agent, possibly through modulation of AKR1C3. These findings open avenues for future studies addressing the molecular pathways of vitexin and for the development of novel therapeutic approaches for primary dysmenorrhea.

Background/objectives: Propolis, known for its medicinal properties, faces challenges in pharmaceutical applications due to its low aqueous solubility, attributed to its resinous and hydrophobic nature. This limits oral administration, reducing its bioavailability and pharmacological activities. To overcome these barriers, cyclodextrins (CDs), cyclic oligosaccharides, are widely studied as carrier systems that enhance the solubility and bioavailability of propolis and other nonpolar compounds. This study aimed to review patents that developed innovative therapeutic approaches to improve the physicochemical and biological properties of propolis through complexation with CDs. Methods: Active and application patents registered over the last 17 years were searched across multiple databases, resulting in the selection of eight inventions for detailed analysis. Results: These patents highlight therapeutic applications of propolis–CD systems for conditions such as diabetes and skin and gastrointestinal cancers, as well as antimicrobial, immunostimulant, and antioxidant effects. Additionally, novel extraction processes free of organic solvents, including nanometric-scale powder extracts, are described. Conclusions: Findings from scientific articles support the patent data, demonstrating that CD complexation significantly enhances the solubility and therapeutic efficacy of propolis. Thus, these patents present an innovative and promising strategy for developing propolis-based pharmaceutical products.

Genipa americana L., popularly known as “jenipapo”, is a species easily found, especially in northeastern Brazil. It is remarkable for having iridoids in its composition. Popular for its blue pigment which has been used to manufacture paints and dyes. Furthermore, this plant is utilized for medicinal purposes in addressing a variety of illnesses. This review provide a comprehensive picture of the phytochemical and biological activities characteristics of Genipa americana L. deal with its ethnomedicinal use and botany based on literature reports. These researches pointed out a range of secondary metabolites with iridoids being the most prevalent and abundant. Until now, the biological tests have shown important pharmacological activities, especially the antioxidant, insecticide and antibacterial activities. Besides presenting itself in a very promising way in other areas such as food and cosmetics industry, it is also used in popular medicine to treat several diseases having this potential use disseminated in its various parts. Finally, for a better analysis and validation of its health benefits and properties, extensive research is needed, including clinical trials. The information gathered and approached in this paper might support the planning and discussion of future studies on the topic.

Ayahuasca is a psychoactive decoction originally used in indigenous Amazonian culture. It consists of a dense brown liquid that most frequently results from the decoction of two plants native to the Amazon rainforest, Psychotria viridis (Rubiaceae) and Banisteriopsis caapi (Malpighiaceae). The composition of the decoction is variable, as several plant species can be used in its preparation. Its psychoactive effect occurs due to the presence of N,N-dimethyltryptamine (DMT), an agonist at serotonergic receptors (5-HT_1A/2A/2C) that is metabolized by the enzyme monoamine oxidase type A (MAO-A), and also the presence of β-carbolines, which are reversible MAO-A inhibitors. This joint interaction promotes a sequence of psychedelic neurochemical effects. Due to the current expansion of research on psychedelic substances and the growing public interest in the benefits of ayahuasca beyond its traditional use in the Amazon, academic research on its therapeutic capacity has been increasing. This study aimed to carry out a literature review on the scientific evidence for the therapeutic potential of ingesting ayahuasca. The review covered the period 2012-2022, and resulted in evidence on the therapeutic effects of ayahuasca on depression/anxiety, chemical dependency/alcoholism and Parkinson’s disease, as well as neuropsychological effects, and possible toxic effects on reproduction/embryonic development, among other adverse effects. The highest number of publications in the searched period dealt with the effects of ayahuasca on depression and anxiety. Further studies need to address the detailed mechanism of action of ayahuasca, as well as its potential toxicity, in order to demonstrate its safety.

Desde dezembro de 2019, quando foram noticiados os primeiros casos de infecção por SARS-CoV-2 (COVID-19) pesquisas têm sido conduzidas para testar opções terapêuticas para o tratamento desta doença. Dentre os vários agentes farmacológicos está a hidroxicloroquina, um medicamento antimalárico que não apresenta evidências de eficácia e segurança nos estudos em COVID-19. Mesmo mediante deste cenário, ocorreu um aumento pela procura e venda desse medicamento. Diante disso, considerando a diversificação dos medicamentos do mercado nacional, a qualidade desses produtos é objeto de perguntas e avaliações. Nesse sentido, o objetivo deste estudo foi analisar a qualidade física de comprimidos de referência, genéricos e similares dos comprimidos de hidroxicloroquina 400 mg comercializados em drogarias na cidade de Irecê-BA, avaliando os testes descritos na Farmacopeia Brasileira 6º edição, afim de avaliar a equivalência farmacêutica dos medicamentos. Trata-se de uma pesquisa experimental e exploratória, de natureza quantitativa, no qual avaliou quatro amostras de medicamentos de hidroxicloroquina de diferentes laboratórios (1 referência, 2 genéricos e 1 similar). Foram analisados: o aspecto visual, peso médio, dureza, friabilidade e desintegração. Todos os comprimidos das marcas analisadas apresentaram integridade, superfície homogênea, lisa e brilhante, coloração branca e visualmente não apresentavam nenhum defeito como falhas, fissuras e contaminação e foram caracterizados como oblongo e biconvexo, ou seja, não apresentaram irregularidade no aspecto visual. A determinação de peso médio mostrou que todas as amostras testadas dos comprimidos permaneceram dentro da variação máxima aceitável de 5%. Sendo assim, os lotes apresentaram uniformidade em seu peso e conteúdo. Para dureza, registrou-se valores unitários elevados para as amostras característico de comprimidos revestidos. Tal resultado não influenciou no processo de desintegração, uma vez que as amostras levaram poucos minutos para se desintegrarem, não ultrapassando também o tempo limite permitido menor que 30 minutos, para comprimidos revestidos por filme. Com relação ao teste de friabilidade, as amostras apresentaram uma pequena perda de massa, caracterizando-se como comprimidos de alta resistência a abrasão sem perda de integridade. No mais, todas as amostras atenderam as especificações da literatura descrita. Diante disso, entende-se que os medicamentos de hidroxicloroquina avaliados mostraram boa qualidade física podendo ser considerados equivalentes farmacêuticos.