Sesquiterpenes (SS) are secondary metabolites formed by the bonding of 3 isoprene (C5) units. They play an important role in the defense and signaling of plants to adapt to the environment, face stress, and communicate with the outside world, and their evolutionary history is closely related to their physiological functions. This review considers their presence and extensively summarizes the 156 sesquiterpenes identified in Vitextaxa, emphasizing those with higher concentrations and frequency among species and correlating with the insecticidal activities and defensive responses reported in the literature. In addition, we classify the SS based on their chemical structures and addresses cyclization in biosynthetic origin. Most relevant sesquiterpenes of the Vitex genus are derived from the germacredienyl cation mainly via bicyclogermacrene and germacrene C, giving rise to aromadrendanes, a skeleton with the highest number of representative compounds in this genus, and 6,9-guaiadiene, respectively, indicating the production of 1.10-cyclizing sesquiterpene synthases. These enzymes can play an important role in the chemosystematics of the genus from their corresponding routes and cyclizations, constituting a new approach to chemotaxonomy. In conclusion, this review is a compilation of detailed information on the profile of sesquiterpene in the Vitex genus and, thus, points to new unexplored horizons for future research.

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.

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: 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.

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.