Monoterpenes are secondary metabolites of plants belonging to the terpenoid class of natural products. They are the most abundant components of essential oils that are generally considered to have various pharmacological properties. These compounds are reported to have antidiabetic effects in recent years. Due to natures complex biosynthetic machinery, they also exhibit a reasonable degree of structural complexity/diversity for further analysis in structure-activity studies. Therefore, monoterpenes as antidiabetic agents have been investigated by recent in vitro and in vivo studies extensively reported in the scientific literature and claimed by patent documents. The purpose of this survey is to provide a comprehensive and prospective review concerning the potential applications of monoterpenes in the treatment of diabetes. The data for this research were collected through the specialized databases PubMed, Scopus, Web of Science, and ScienceDirect between the years 2014 and 2022, as well as the patent databases EPO, WIPO, and USPTO. The research used 76 articles published in the leading journals in the field. The main effect observed was the antidiabetic activity of monoterpenes. This review showed that monoterpenes can be considered promising agents for prevention and/or treatment of diabetes as well as have a marked pharmaceutical potential for the development of bioproducts for therapeutics applications.

Solid Lipid Nanoparticles (SLNs) are drug delivery systems with important advantages over conventional nanosystems. Considering previously reported pharmacological and physicochemical properties of Platonia insignis seed butter (BBI), this work aimed at developing, characterizing and performing toxicological and antioxidant studies of SLNs produced from BBI. The GC-MS analysis identified palmitic and oleic acids as the major compounds. Three SLN prototypes were developed through high-shear homogenization followed by ultrasonication. During a 180-day stability evaluation, the formulation SLN/TW-1.5 presented greater stability since pH was around 6.0, as well as a lesser variation of the PdI (Polydispersity Index), particle size and Zeta Potential (ZP), confirmed with Raman Spectroscopy and Atomic Force Microscopy (AFM). The CC₅₀ in macrophages was around 249.4 µg∙mL⁻¹ for BBI, whereas the CC₅₀ value for SLN/TW-1.5 was 45.2 µg∙mL⁻¹. Electron Paramagnetic Resonance (EPR) showed a marked in vitro antioxidant activity for BBI and SLN/TW-1.5. After in vivo SLN/TW-1.5 administration in Zophobas morio larvae, assessment of reduced glutathione (GSH), nitrite (NO₂⁻) and myeloperoxidase (MPO) demonstrated antioxidant activity. Thus, the intrinsic physicochemical properties of BBI allowed the development of an optimized nanoformulation with high stability indexes, besides the great potential for antioxidant applications.

The high frequency of infectious diseases has spurred research into effective tactics to combat microorganisms that are resistant to several drugs. The overproduction of the transmembrane efflux pump protein NorA, which may export hydrophilic fluoroquinolones, is a common mechanism of resistance in S. aureus strains. This work evaluated the antimicrobial activity of the ethanolic extract from the leaves of Croton heliotropiifolius (EECH) against different bacterial and fungal strains, as well as investigating its modulating effect on the resistance to norfloxacin in a Staphylococcus aureus SA1199B overproducing the NorA efflux pump. Microdilution assays were used to assess the EECH’s antibacterial efficacy. The MIC of norfloxacin or ethidium bromide (EtBr) against the SA1199B strain was determined in the presence or absence of the EECH in order to assess the modifying influence on drug resistance. The EECH showed no activity against the Gram-positive and Gram-negative bacterial strains tested. The EECH also showed no antifungal activity against Candida albicans ATCC 10231. On the other hand, the extract reduced the MIC values for norfloxacin against SA1199B at subinhibitory concentrations. In addition, the EECH also reduced the MIC values of EtBr at subinhibitory concentrations, suggesting the occurrence of phytochemicals that inhibit efflux pumps. Molecular docking showed that retusin, a flavonoid found in the extract, could compete with norfloxacin at the orthosteric site of the NorA, indicating that it could be a potential efflux pump inhibitor. However, isolated retusin did not enhance the activity of norfloxacin or EtBr and it did not inhibit the EtBr efflux, showing that it is not a NorA inhibitor. Even though C. heliotropiifolius is a source of phytochemicals that function as adjuvants for norfloxacin, isolated retusin cannot be used in conjunction with norfloxacin to treat infections brought on by S. aureus that overproduces NorA.

Background/Objectives: Chronic complications of diabetes mellitus are closely associated with increased oxidative stress and the formation of advanced glycation end products (AGEs). This study aimed to investigate the antioxidant and antiglycation potential of hesperetin-7-O-glucoside (HCD) and diosmetin-7-O-glucoside (DCD) formulations complexed with cyclodextrins, using in vitro and in silico experimental models to evaluate their efficacy in mitigating hyperglycemia-induced molecular damage. Methods: Antioxidant activity was assessed using chemical and erythrocyte-based oxidative stress models, whereas antiglycation activity was evaluated in BSA–fructose, BSA–methylglyoxal, and arginine–methylglyoxal models. Results: Both formulations showed measurable antioxidant effects, with concentration-dependent behavior observed in some of the evaluated assays. In the DPPH assay, HCD and DCD achieved maximum inhibition values of 30.71% and 26.61%, respectively. Furthermore, DCD exhibited higher total antioxidant capacity (102.80 µg vitamin C equivalents/mL) and nitric oxide scavenging activity (37.89%) than HCD. In a cellular model, both formulations (200 µg/mL) significantly reduced AAPH-induced hemolysis, with DCD providing superior protection (7.05% vs. 16.63% for HCD). Under oxidative stress induced by high glucose concentration in erythrocytes, HCD and DCD reduced non-protein thiol levels, and HCD significantly increased catalase enzyme activity. Regarding antiglycation activity, DCD demonstrated superior efficacy relative to HCD in the BSA-fructose system, achieving 43.23% inhibition. DCD also displayed concentration-dependent inhibition of fructosamine formation (up to 47.99%) and BSA glycation by methylglyoxal (up to 45.20%). Both formulations significantly reduced carbonylated protein levels and preserved free thiol groups. In the arginine–methylglyoxal model, DCD and HCD reached 44.03% and 48.82% inhibition, respectively. Molecular docking revealed high binding affinity of both flavonoids to the protein active site (−9.00 kcal/mol for hesperetin-7-O-glucoside and −9.04 kcal/mol for diosmetin-7-O-glucoside), suggesting a structural protective role. Conclusions: The HCD and DCD formulations demonstrated antioxidant and antiglycation activities that may contribute to attenuating molecular alterations associated with chronic hyperglycemia through complementary mechanisms, including antioxidant effects, protection against protein carbonylation, and inhibition of glycation. While these findings highlight the potential of the evaluated formulations, additional mechanistic and in vivo studies are required to establish their pharmacological applicability.

A inflamação é um mecanismo de proteção natural no qual o organismo designa atividades do sistema imunológico para combater infecções, eliminar moléculas tóxicas ou recuperar-se de lesões. No entanto, quando exacerbada, torna-se uma condição clínica na qual o sistema imune, através de citocinas e quimiocinas, contribui para a formação de espécies reativas de oxigênio que, por sua vez, agravam ou desencadeiam danos teciduais irreversíveis, contribuindo para o desenvolvimento de doenças crônicas como hipertensão e diabetes. Embora haja muitas medicações para o tratamento destas comorbidades, sendo grande parte sintéticas, estes fármacos geram diversas reações adversas, seja por sua biodisponibilidade, interações medicamentosas, metabolismo ou excreção. Nesse contexto, vem-se estudando cada vez mais a biodiversidade dos produtos naturais para a otimização do tratamento de condições clínicas. Com base neste princípio e devido à sua diversidade estrutural, diferentes tipos de flavonoides são continuamente estudados para avaliar propriedades farmacológicas como ações antioxidantes, atividades anti-inflamatórias, antidiabéticas e anti-hipertensivas. Pertencente à classe dos flavonoides, a naringenina se destaca por estas ações; no entanto, pouco se sabe sobre sua forma glicosilada e, devido à sua conformação estrutural, este flavonoide possui baixa biodisponibilidade no organismo. Assim, a complexação com β-ciclodextrinas é um dos métodos utilizados para melhorar a solubilidade da naringenina. Com o intuito de reunir informações sobre as propriedades farmacológicas supracitadas, este trabalho realizou uma revisão sobre a naringenina e seus efeitos na hipertensão e no diabetes.