Kuwait Journal of Science最新文献

This investigation is intended to demonstrate the synergistic, antibacterial, and antioxidant activity produced by the combination of essential oils (EOs) from Moroccan Clinopodium nepeta (CNEO), Ruta montana (RMEO), and Dittrichia viscosa (DVEO) EOs. The phytochemistry profile, the antibacterial effect and the antioxidant ability of EOs were assessed separately. Then, an augmented-simplex-centroid design was used to optimize the antibacterial activity of EOs formulations against Escherichia coli (E. coli) and Micrococcus luteus (M. luteus). The mixture design was also used to maximize the radical scavenging activity and the ferric reducing antioxidant power. The results of this study revealed that the optimal combination against E. coli conformed to 25% RMEO, 50% CNEO, and 25% DVEO, while the optimal mixture estimated against M. luteus was adjusted by the binary combination of 36% RMEO and 64% CNEO. Furthermore, the optimal association expected for DPPH inhibition is 37% RMEO, 40% CNEO, and 23% DVEO, while the formulation of 30% RMEO, 38% CNEO, and 32% DVEO presented the maximal mixture to obtain the highest ferric reducing power. These data showed the effectiveness of EOs mixtures against resistant bacteria and their promising employment as natural antioxidant agents in foods.

Novel derivatives of potential angiotensin converting enzyme (ACE-I) inhibitors (compounds 5a-e) were synthesized by reacting homophthalic anhydride with methyl esters of L-amino acids (L-isoleucine, L-phenylalanine, L-tyrosine, L-methionine, and L-serine). This reaction resulted in yields of 85% for compound 5a, 83% for compound 5b, 84% for compound 5c, 80% for compound 5d, and 85% for compound 5e. All the synthesized compounds were characterized by 1D and 2D NMR methods. In silico ADME properties of compounds 5a-e conform to Lipinski's drug rules. The in silico toxicological determination of the synthesized compounds suggest that compound 5a exhibits significant potential for adverse effects, such as causing hormonal imbalances. In comparison, the remaining compounds 5b-c demonstrate a lower risk profile. In silico biological activities of compounds 5a-e in the active site of ACE-I were determined by docking, which were then compared to the FDA approved antihypertensive drugs enalalapril and lisinopril. Docking studies revealed that compound 5b (ΔG^comp = −8.851 kcal/mol) possesses the greatest binding affinity in the Zn²⁺ binding site of ACE-I compared to those of lisinoprilat (ΔG^comp = −8.066 kcal/mol) and enalapril (ΔG^comp = −7.187 kcal/mol), strongly suggesting a great potential to be a lead candidate for novel antihypertensive drug development.

The present study employed microwave-assisted extraction (MAE) as a method to extract a crude extract high in polyphenols from the leaves of duku (Lansium domesticum Corr.), a medicinal plant indigenous to Indonesia. The study acquired data on the impact of various extraction parameters, such as ethanol concentration (X₁), microwave power (X₂), and extraction time (X₃), on the levels of total phenolics content (TPC), total flavonoids content (TFC), and antioxidant activity using 2,2-Diphenyl-1-picrylhydrazyl (DPPH) scavenging activity. The extraction process was optimized using a Box-Behnken design (BBD) and response surface methodology (RSM). The optimal conditions were achieved with an X₁ of 75%, an X₂ of 315 W, and an X₃ of 8.5 min. The aforementioned experimental settings yielded results of 86.176 mg GAE/g, 31.585 mg QE/g, and 75.850% for the TPC, TFC, and antioxidant activity, respectively. The extract included several significant active chemicals, including octadecanoic acid, undecane, 2-methyl-, 9-octadecenoic acid (Z)-hexyl ester, pentadecanoic acid, 9-hexadecanoic acid, phenolic and flavonoid compounds. The cytotoxic activity against MCF-7, T47D, and 4T1 cell lines was found to be slowed when exposed to crude extract doses ranging from 7.81 to 500.00 μg/mL. The present study's results suggest that MAE is a viable technique for extracting a polyphenol-rich crude extract from duku leaf. This extract shows promise as a natural antioxidant and has potential as an anti-breast cancer agent.