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Cutibacterium acnes, Staphylococcus epidermidis, and Staphylococcus aureus proliferate within accumulated sebum and produce localised inflammation thereby inducing acne vulgaris. Essential oils are one of the leading natural products used for acne and are diluted in fixed oils to reduce irritation and toxicity. This study investigated the in vitro antimicrobial, anti-inflammatory, cytotoxicity, and skin retention properties of Rosa rubiginosa rosehip fixed oil in combination with essential oils having activity against acne vulgaris. The broth microdilution assay was used to determine the minimum inhibitory concentration (MIC), and the sum of the fractional inhibitory concentration index (ΣFIC) was calculated for the interactions. The lipopolysaccharide (LPS) induced inflammatory pathway in RAW 264.7 macrophages was used to assess anti-inflammatory activity. A dual-staining method in A549 epithelial cells was used to assess cytotoxicity. Qualitative Fourier Transform Infrared spectroscopy analysis was used for initial skin retention determination. Rosa rubiginosa oil combined with Cinnamomum zeylanicum essential oil displayed antimicrobial synergy (MIC = 0.42 mg/ mL; ΣFIC = 0.45) against three acne-inducing strains. Rosa rubiginosa fixed oil combined with Styrax benzoin essential oil suppressed LPS-induced nitrite production by 33.80%. Rosa rubiginosa oil combined with Melaleuca quinquenervia essential oil exhibited the lowest cytotoxicity (84.32% cell viability). Rosa rubiginosa oil combined with either C. zeylanicum, Eugenia caryophyllata, Rosa damascena or S. benzoin essential oil was retained within the porcine skin. Rosa rubiginosa fixed oil serves as an ideal carrier oil that can potentiate selected essential oils for the treatment of acne vulgaris. [ABSTRACT FROM AUTHOR]

Aims Antimicrobial resistance continues to be a growing concern, resulting in increased use of drug combinations. Antibiotic adjuvants are an emerging strategy that may potentiate an antibiotics efficacy. Ibuprofen's polypharmacological properties have been investigated for their antimicrobial and host-modulating potential. This study aimed to investigate the potential of a novel multidrug combination involving ibuprofen, essential oil compounds (EOCs), and conventional antimicrobials against skin pathogens. Methods and Results The minimum inhibitory concentrations of ibuprofen, conventional antimicrobials, and EOCs were determined and then combined and tested against 14 (reference and clinical) skin pathogens. The cytotoxicity was analysed using the MTT assay, whilst the anti-inflammatory effects were evaluated using lipopolysaccharide activated RAW264.7 murine macrophages. Four pairwise (Ibuprofen and antibiotic) (ΣFIC 0.33–0.50) and three triple (Ibuprofen and antibiotic with EOC) (ΣFIC 0.44–0.47) synergistic antimicrobial interactions were identified. These combinations demonstrated cell viability of 77.59%–100%. No combination significantly reduced nitric oxide production. Conclusion The results from this study provide insight into the potential of a multidrug combination involving ibuprofen with conventional antimicrobials and EOCs against common skin pathogens. [ABSTRACT FROM AUTHOR]

C24H18O8, monoclinic, P21 (no. 4), a = 7.9654(3) Å, b = 23.6910(8) Å, c = 21.2314(8) Å, β = 96.777(2)°, V = 3978.6(3) Å3, Z = 8, Rgt(F) = 0.0499, wRref(F2) = 0.1320, T = 200 K.

A promising strategy for combating bacterial infections involves the development of agents that disarm the virulence factors of pathogenic bacteria, thereby reducing their pathogenicity without inducing direct lethality. Sortase A, a crucial enzyme responsible for anchoring virulence factors to the cell surface of several pathogenic bacteria, has emerged as a possible target for antivirulence strategies. A series of hippocastanum species (Aesculus pavia, A. parviflora, Aesculus x carnea, and A. hippocastanum) were used to prepare ethanol- and water-based extracts for assessing their effect on Staphylococcus aureus sortase A. The extracts were characterized through HPLC analysis, and their polyphenols content was determined using the Folin–Ciocalteu method. The specific toxicity profile was evaluated in Daphnia magna using the median lethal concentration (LC50) and against the fibroblast MRHF cell line. The half maximal inhibitory concentration (IC50) values on sortase A, determined after 30 min of incubation, ranged from 82.70 to 304.31 µg/mL, with the A. pavia water extract exhibiting the highest inhibitory effect. The assessment of the A. pavia water extract on human fibroblasts revealed no significant signs of toxicity, even at a concentration of 500 µg/mL. This reduced toxicity was further validated through the Daphnia assay. These findings highlight the low toxicity and the potential of this extract as a promising source of future development of bacteria antivirulence solutions. [ABSTRACT FROM AUTHOR]

Khaya grandifoliola extracts have been conventionally found to be effective in the treatment of wounds and ulcers. This study assessed the phytochemical content of K. grandifoliola methanol and ethyl acetate extracts and used in vitro bioassays for bioactivity testing to confirm the ethnomedicinal uses. Phytochemical content and bioactivity of K. grandifoliola ethyl acetate and methanol extracts; (stem bark, root, leaf) were assessed using spectrophotometric analysis with standard calibration curves for respective phytochemicals and in vitro bioactivity assays including MTT, free radical scavenging activity, lipopolysaccharide-activated RAW 264.7 macrophages assay for cytotoxicity, anti-inflammatory antioxidant, and antimicrobial activities. The polyphenolic content of methanol extracts (37.49±1.40 -53.57±1.50 mg GAEQ/100 mg) was the highest phytochemical content measured. The methanol root extract had the highest terpenoid concentration (35.78±2.14 mg LIN EQ/100 mg). Methanol stem bark and root extracts exhibited anti-inflammation activity at 200 µg/mL, potent antioxidant activity (IC50; 38.68±5.09 µg/mL and 46.34±9.56µg/mL), and growth inhibition against Staphylococcus aureus (MIC; 1 and 2 mg/mg). Ethyl acetate root and leaf extracts inhibited the growth of Streptococcus pyogenes (MIC; 0.25 mg/mL). In conclusion, the high phenolic and terpenoid content of extracts which correlated positively with their biological activities could be the contributing factor to the biological effects such as wound healing of the extracts. [ABSTRACT FROM AUTHOR]

Flavonoids are a class of biologically active compounds with various proven nutraceutical benefits. In flavonoid C-glycosides, the aglycones are attached to sugar residues via cleavage-resistant C-C bonds which alter typical flavonoid pharmacokinetic properties. In these compounds, the combination of biological activities from the flavonoid moieties and sugar residues create unique and more diverse biological functions than those of O-glycosylated and unsubstituted flavonoids. Through a series of reverse phase chromatography techniques and various spectroscopic methods, the phytochemical investigation of Drimia altissima (L.F.) Ker Gawl., a specie from the Asparagaceae family, led to the isolation and chemical characterisation of a novel C-glucosylflavonoid, altissimin, with a unique apioglucoside arrangement to the apigenin aglycone. Altissimin was found to possess strong in vitro anti-proliferative activity against HeLa cervical cancer cells. [ABSTRACT FROM AUTHOR]

In South Africa, the number of people suffering from diabetes is believed to be rising steadily and the current antidiabetic therapies are frequently reported to have adverse side effects. Ethnomedicinal plant use has shown promise for the development of cheaper, cost-effective antidiabetic agents with fewer side effects. The aim of this study was to investigate the antidiabetic activity and mechanism of action of aqueous leaf extract prepared from Brachylaena elliptica. The potential of the extract for cytotoxicity was evaluated using MTT assay in HepG2 cells. The effects of the plant extract on glucose utilization in HepG2 cells and L6 myotubes, triglyceride accumulation in 3T3-L1, INS-1 proliferation, glucose metabolism in INS-1 cells, and NO production in RAW macrophages were also investigated using cell culture procedures. The inhibitory effects of the extract on the activities of different enzymes including alpha-amylase, alpha-glucosidase, pancreatic lipase, dipeptidyl peptidase IV (DPP-IV), collagenase, and CYP3A4 enzymes were evaluated. The extract also tested against protein glycation using standard published procedure. The plant extract displayed low level of toxicity, where both concentrations tested did not induce 50% cell death. The extract caused a significant increase in glucose uptake in HepG2 liver cells, with efficacy significantly higher than the positive control, berberine. The crude extract also displayed no significant effect on muscle glucose uptake, triglyceride accumulation in 3T3-L1, glucose metabolism in INS-1 cells, alpha-amylase, alpha-glucosidase, DPP-IV, lipase, protein glycation, and collagenase compared to the respective positive controls. The extract displayed a proliferative effect on INS-1 cells at 25 μg/ml when compared to the negative control. The plant also produced a concentration-dependent reduction in NO production in RAW macrophages and also demonstrated weak significant inhibition on CYP3A4 activity. The findings provide evidence that B. elliptica possess antidiabetic activity and appear to exact its hypoglycemic effect independent of insulin. [ABSTRACT FROM AUTHOR]

Context:Plants harbor endophytes with potential bioactivity.Markhamia tomentosa(Benth) K. Schum ex. Engl. (Bignoniaceae) is reported to possess antioxidant, anti-inflammatory and anticancer activities. Objective:The antifungal and antiproliferative properties of endophytic fungi extracts and fractions fromM. tomentosawere evaluated. Material and methods:Endophytic fungi were isolated from the leaves ofM. tomentosaand identified by ITS-rDNA sequence analysis. The antagonistic effect of the fungal strains was investigated against pathogenic fungi viz,Fusarium oxysporum, Sclerotinia sclerotiorium, Rhizoctonia solani,andBotrytis cinereausing the dual culture assay for 5–7 days. Antiproliferative effect of the fungal extracts and fractions (3.91–250 μg/mL) on HeLa cancer cell line was tested and IC50was calculated. Poisoning food assay and antifeedant activity against the pathogenic fungi andSpodoptera lituralarvae, for 7 days and 2 h, respectively, was also tested at concentrations of 250, 500 and 1000 μg/mL. Results:Fungal endophytesTrichoderma longibrachiatumandSyncephalastrum racemosumwere isolated from the leaves ofM. tomentosa. Isolated endophytic fungal strains and solvent extracts showed MIC value of 1000 μg/mL against tested pathogenic fungi in the dual culture and poisoning food assays. Methanol fraction ofS. racemosumisolate showed the most effective antiproliferative activity with IC50of 43.56 μg/mL. Minimal feeding deterrent activity againstS. lituralarvae was also observed. Discussion and conclusion:These findings showed that the leaves ofMarkhamia tomentosaharbor strains of endophytic fungi with promising health benefits, and suggest their antifungal and antiproliferative effects against pathogenic fungi and HeLa cancer cell line. [ABSTRACT FROM AUTHOR]