The rapid spread of bacterial infection caused by Staphylococcus aureus has become a problem to public health despite the presence of past trials devoted to controlling the infection. Thus, the current study aimed to explore the chemical composition of the extract of endophytic fungus Aspergillus fumigatus, isolated from Albizia lucidior leaves, and investigate the antimicrobial activity of isolated metabolites and their probable mode of actions. The chemical investigation of the fungal extract via UPLC/MS/MS led to the identification of at least forty-two metabolites, as well as the isolation and complete characterization of eight reported metabolites. The antibacterial activities of isolated metabolites were assessed against S. aureus using agar disc diffusion and microplate dilution methods. Compounds ergosterol, helvolic acid and monomethyl sulochrin-4-sulphate showed minimal inhibitory concentration (MIC) values of 15.63, 1.95 and 3.90 µg/mL, respectively, compared to ciprofloxacin. We also report the inhibitory activity of the fungal extract on DNA gyrase and topoisomerase IV, which led us to perform molecular docking using the three most active compounds isolated from the extract against both enzymes. These active compounds had the required structural features for S. aureus DNA gyrase and topoisomerase IV inhibition, evidenced via molecular docking.

Frankincense oil has gained increased popularity in skin care, yet its anti-aging effect remains unclear. The current study aimed to investigate the anti-photoaging effect of frankincense (Boswellia papyrifera (Del.) Hochst., Family Burseraceae) essential oil in an in vivo model. The oil was initially extracted by two methods: hydro-distillation (HD) and microwave-assisted hydro-distillation (MAHD). GC/MS analysis revealed the dominance of n-octyl acetate, along with other marker compounds of B. papyrifera including octanol and diterpene components (verticilla 4(20) 7, 11-triene and incensole acetate). Thereafter, preliminary investigation of the anti-collagenase and anti-elastase activities of the extracted oils revealed the superior anti-aging effect of HD-extracted oil (FO), comparable to epigallocatechin gallate. FO was subsequently formulated into solid lipid nanoparticles (FO-SLNs) via high shear homogenization to improve its solubility and skin penetration characteristics prior to in vivo testing. The optimimal formulation prepared with 0.5% FO, and 4% Tween^® 80, demonstrated nanosized spherical particles with high entrapment efficiency percentage and sustained release for 8 hours. The anti-photoaging effect of FO and FO-SLNs was then evaluated in UVB-irradiated hairless rats, compared to Vitamin A palmitate as a positive standard. FO and FO-SLNs restored the antioxidant capacity (SOD and CAT) and prohibited inflammatory markers (IL6, NFκB p65) in UVB-irradiated rats via downregulation of MAPK (pERK, pJNK, and pp38) and PI3K/AKT signaling pathways, alongside upregulating TGF-β expression. Subsequently, our treatments induced Procollagen I synthesis and downregulation of MMPs (MMP1, MMP9), where FO-SLNs exhibited superior anti-photoaging effect, compared to FO and Vitamin A, highlighting the use of SLNs as a promising nanocarrier for FO. In particular, FO-SLNs revealed normal epidermal and dermal histological structures, protected against UVβ-induced epidermal thickness and dermal collagen degradation. Our results indicated the potential use of FO-SLNs as a promising topical anti-aging therapy.

Alzheimer’s disease remains a global health challenge and an unmet need requiring innovative approaches to discover new drugs. The current study aimed to investigate the inhibitory activity of Albizia lucidior and Albizia procera leaves against acetylcholinesterase enzyme in vitro and explore their chemical compositions. Metabolic profiling of the bioactive plant, A. lucidior, via UHPLC/MS/MS-based Molecular Networking highlighted the richness of its ethanolic extract with budmunchiamine alkaloids, fourteen budmunchiamine alkaloids as well as four new putative ones were tentatively identified for the first time in A. lucidior. Pursuing these alkaloids in the fractions of A. lucidior extract via molecular networking revealed that alkaloids were mainly concentrated in the ethyl acetate fraction. In agreement, the alkaloid-rich fraction showed the most promising anticholinesterase activity (IC₅₀ 5.26 µg/mL) versus the ethanolic extract and ethyl acetate fraction of A. lucidior (IC₅₀ 24.89 and 6.90 µg/mL, respectively), compared to donepezil (IC₅₀ 3.90 µg/mL). Furthermore, deep in silico studies of tentatively identified alkaloids of A. lucidior were performed. Notably, normethyl budmunchiamine K revealed superior stability and receptor binding affinity compared to the two used references: donepezil and the co-crystallized inhibitor (MF2 700). This was concluded based on molecular docking, molecular dynamics simulations and molecular mechanics generalized born/solvent accessibility (MM–GBSA) calculations.

Acne is a highly prevalent skin disease with a great psychological impact on patients as self-perception, self-confidence, and depression. This work aimed to develop an anti-acne preparation from active anti-bacterial medicinal plants to circumvent the severe side effects and drug resistance commonly reported with topical erythromycin anti-acne preparations. Essential oils:Salvia officinalisL. (sage),Rosmarinus officinalisL. (rosemary),Commiphora myrrhaNees Engl. (myrrh),Origanum majoranaL. (marjoram),Pelargonium zonaleL. L’Hér. ex Aiton (geranium) andChrysanthemum morifoliumRamat. (chrysanthemum) were extracted by hydrodistillation and analyzed using gas chromatography/mass spectrometry (GC/MS). The anti-acne activities of the oils againstCutibacteriumacnes ATCC 6919 were evaluated by microdilution methods to determine the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The most active essential oils were loaded in a film-forming nanogel prepared with chitosan, pluronic F127 and glycerol in the ratio of 3:1:1, prior to investigation in a murine acne in vivo model. Marjoram and chrysanthemum oils showed the highest antimicrobial activity againstC. acnes(MIC = 0.156%v/vand 0.125%v/v, respectively). GC/MS of the actives showed that gamma-terpinene (26.46%) and terpinen-4-ol (22.24%) were the predominant constituents in marjoram, whereas chrysanthenone (32.79%) was the main component in chrysanthemum. The formulated essential oil-loaded film-forming nanogels of both oils exhibited significant anti-acne activity in mice via reducing the bacterial loads, activating the antioxidant nuclear factor erythroid 2–related factor 2 (Nrf2) pathway and inhibiting the inflammatory tumor necrosis factor-alpha (TNF-α) pathway. Further studies should be designed to evaluate the clinical evidence for the use of marjoram and chrysanthemum oil products in acne treatment.Graphical Abstract

Roots and aerial parts are the agricultural by-products of caraway (Carum carvi L.) fruit production. Hereto, the anti-obesity and hypolipidemic effects of caraway waste were assessed using different in vitro and in vivo tests performed on total ethanol extract (TEE), as well as its fractions. The ethyl acetate fraction (EtOAc fr.) exhibited the highest inhibitory activity on pancreatic lipase (PL), α-amylase and DPPH free radical. Accordingly, it showed the highest ameliorative activity against dyslipidaemia among other fractions and the total extract when tested on a high fat diet-fed mice model. It attenuated hepatic steatosis, reduced adipocyte size, ameliorated the lipid profile, and suppressed leptin concentrations as revealed by the histopathological and biochemical examinations. Umbelliferone, p-coumaric acid and isoquercitrin were isolated from the bioactive EtOAc fr. and quantified in both, the EtOAc fr. and TEE, using HPLC. Isoquercitrin displayed the highest inhibitory activity towards DPPH and PL (IC50: 10 ± 2.50 and 93.54± 2.62 µg/mL, respectively), whereas umbelliferone was the most active against α-amylase (IC50: 50.70 ± 2.83 µg/mL). Molecular docking was carried out to uncover the binding affinities to the enzymes’ active sites. Isoquercitrin demonstrated strong interaction in the binding site of lipase (-130.87 kcal·mol-1), via H-bonding with Asp79, Ile78, Arg256, Ser152 and Tyr114, whereas, umbelliferone formed H-bonding with Tyr59 and Leu142 and H-Pi interaction with Gln63 in the amylase enzyme’s active site (-65.99 kcal·mol-1). The current research highlights the great potential for caraway waste as a multitarget remedy against obesity, which incites further molecular and clinical studies.

There is strong evidence on the anticancer properties of secolariciresinol diglucoside (SDG), the predominant flaxseed lignan, especially for mammary and prostatic carcinomas. Although the effect of cultivar and location on flaxseed SDG level has been reported, much less is traced regarding the influence of agronomical treatments. The purpose of this study is to determine if agricultural management practices could enhance SDG accumulation in flaxseed. We studied the effect of irrigation frequencies (I), added nutrients (N, zinc and humic acid) and fertilization treatments (F) and their interactions on SDG level and seed yield of the Egyptian flax cultivar Giza 9. Samples were extracted and analyzed for SDG, after alkaline hydrolysis, using HPLC-UV method. The concentration of SDG and its yield varied between 415.55-845.95 mg/100 g whole seeds and 1.77-4.05 Kg/feddan on a dry weight basis, respectively according to different agricultural treatments. I, N and F factors and their interactions had a significant effect on SDG. I × N × F interaction contributed to the majority of SDG variation (31.81 %), followed by I factor (27.96 %), whereas seed yield was more affected by F factor (72.7 %). The I × F interaction was the only significant interaction on the seed yield contributing only for 0.43% of the variance. Moderate irrigation frequency with the humic acid foliar application and mineral nitrogen fertilizer was the best combination for achieving the highest SDG levels. Using optimum agronomic practice would benefit the nutraceutical industry by optimizing flaxseed lignan content and hence enhancing its anticancer, health-promoting effect.