Search

Background: Natural products have been a cornerstone in the field of drug discovery for centuries, they have provided numerous therapeutic agents that have significantly impacted modern medicine. Centaurea alexanderina is a canescent herb that is native to Egypt and Libya and reported in Egyptian folk medicine as an anti-hyperglycemic, antioxidant, and antimicrobial herb. It is an understudied species, thusly, the target of this contribution was to perform a comparative study of the influence of plant part variation on its chemical and pharmacological characteristics. In this context, essential oil extracts from different parts of C. alexanderina (flowers, stems, leaves, and roots) have been analyzed chemically and tested for their antioxidant, antimicrobial, and anti-hyperglycemic activities. Methods: The essential oil extracts from different parts of C. alexanderina have been prepared and their chemical compositions have been analyzed using GC–MS technique. Antimicrobial activities of different essential oil extracts were evaluated via the agar cup diffusion method. DPPH radical scavenging and FRAP assays were used for determination of the antioxidant capacity. Anti-hyperglycemic activities of the four essential oil extracts under study were investigated via α-glucosidase inhibition assay. A computational study has been performed using molecular docking of the identified compounds in the most active essential oil extracts (leaves and roots) against α-glucosidase enzyme using PDB entry 5NN8. Results: A GC–MS analysis of the four essential oil extracts revealed high levels of non-terpenoid hydrocarbons in three essential oil extracts (flower, stems, and leaves) and alcohols in roots essential oil extract, followed by fatty acids in flowers, diterpenoids in stems, steroids in leaves, and fatty acid esters in roots. Roots and stems essential oil extracts exhibited selective activity against Pseudomonas aeruginosa (P. aeruginosa), whereas leaves essential oil extract showed activity against both Salmonella enterica (S. enterica) and Escherichia coli (E. coli). Essential oil extracts of different parts of the plant exhibited DPPH free radical scavenging activity with IC50 values of 128, 134, 152, and 163 μM for flowers, roots, stems, and leaves essential oil extracts; respectively, while in FRAP assay, the results showed different pattern; flowers revealed the highest activity followed by leaves, roots, and stems (107.50 ± 3.64, 125.80 ± 4.2, 139.4 ± 5.27, and 155.59 ± 5.27 ug/mL, respectively). In vitro evaluation of anti-hyperglycemic activity via inhibition of α-glucosidase enzyme assay unveiled leaves and roots essential oil extracts as the most inhibitors with IC50 values of 349 and 369 μg/mL; respectively. The molecular docking study of detected metabolites in the most active essential oil extracts against human α-glucosidase enzyme (PDB: 5NN8) revealed moderate to high binding affinities (-4.6 to -7.3 kcal/mol for leaves and -4.4 to -7.9 kcal/mol for roots essential oil metabolites). Conclusion: Current research demonstrated the variations in chemical composition and biological activities of essential oil extracts from different parts of Centaurea alexanderina and reported anti-hyperglycemic, antioxidant, and antimicrobial potentials of the different essential oil extracts. [ABSTRACT FROM AUTHOR] more...

Background: The Systemic Lupus Erythematosus Disease Activity-2000 Glucocorticoid Index (SLEDAI-2 KG) accounts for glucocorticoids and possibly promising. The Physician Global Assessment (PGA) is subjective and debatable. Objectives: Assessment of the validity of the SLEDAI-2 KG, its association with the PGA, and their potential association with the disease damage. Methods: A cross-sectional study included SLE patients managed at 2 tertiary centers in Egypt were conducted. The SLEDAI-2 K was the gold standard score for assessment the disease activity. The SLEDAI-2 KG incorporates glucocorticoids' dosage through an ordinal weight. The PGA (scale: 0–3) was categorized according to the PGA international standardization consensus in SLE study (PISCOS). Results: The study included 608 patients [546 (89.8%) females and [62 (10.2%) males; age at onset: 27.5 ± 8.5 years; age at assessment: 31.4 ± 9.4 years; disease duration: 6.1 ± 5.5 years for females]. The mean SLEDAI-2 K, SLEDAI-2 KG, and PGA was 11.9 ± 9.3, 16 ± 10.5, and 1.2 ± 0.8, respectively. The correlation between both the SLEDAI-2 KG (r: 0.96, p < 0.001) and PGA (r: 0.5, p < 0.001) and SLEDAI-2 K was statistically significant. The association's strength between both the SLEDAI-2 KG and PGA and SLEDAI-2 K declined among low activity-patients (SLEDAI-2 K < 6) [(r = 0,4; p < 0.001) (r = 0.2; p = 0.02), respectively], and the SLEDAI-2 KG and PGA were not associated in this subgroup (r: 0.07, p = 0.4). The agreement's strength between the SLEDAI-2 K and PISCOS-PGA was weak (kappa = 0.17, p < 0.001). The SLEDAI-2 K and SLEDAI-2 KG were comparable predictors for damage and the PGA was a weaker predictor. Conclusion: The SLEDAI-2 KG and PGA correlated significantly with the SLEDAI-2 K, yet the correlation's strength declined among low disease activity-patients. The SLEDAI-2 K and SLEDAI-2 KG were comparable predictors for damage. [ABSTRACT FROM AUTHOR] more...

Phytochemical investigation of Flacourtia rukam Zoll. & Mortizi (F. rukam) leaves and bark led to the isolation and characterization of seventeen compounds of which four phenolics were not previously described; 2-[(benzoyloxy)methyl]-phenyl-O-β-xylosyl-(1→2)-β-glucopyranoside (1), 2-[(benzoyloxy)methyl]-4-hydroxyphenyl-O-β-xylosyl-(1→2)-β-D-glucopyranoside (2), 2-hydroxy-5-(2-hydroxyphenoxy)phenoxy-β-glucopyranoside (3) and biphenyl-1,1′,2,2′-tetraol (5). Interestingly, the later compound is known as a synthetic but this is the first report for its isolation from nature. Chemical structures were established using extensive analysis of spectroscopic data (1 D and 2 D NMR and HRESIMS). Biphenyl-1,1,2,2′-tetrol (5) exhibited a good activity against Trypanosoma brucei trypomastigotes with IC50= 6.66 ug/mL. Compounds 2, 5, 9, 10, 11 and 12 showed a good in-vitro anti-inflammatory activity using proteinase inhibitory assay. On the contrary, all tested compounds were inactive as antileishmanial or antimalarial. [ABSTRACT FROM AUTHOR] more...

A triggering receptor expressed on myeloid cells-1 (TREM-1) is a member of the immunoglobulin superfamily with an established role in innate and adaptive immune response. We aimed to determine the plasma concentrations and clinical association of sTREM-1 in Systemic Lupus Erythematosus (SLE) patients. Plasma from 79 SLE patients and 35 normal healthy subjects were assayed for sTREM-1 and IL-6 levels using Enzyme Linked Immunosorbant Assay (ELISA). The clinical disease characteristics and serological data were prospectively assessed. Disease activity was scored using the SLE disease activity index. We detected significantly higher levels of sTREM-1 in plasma of SLE patients than the healthy control group. We also detected high sTREM-1 levels in subgroups of patients with neuropsychiatric manifestations (NPLE) and patients with the total high disease activity and NPLE activity. In addition, sTREM-l levels were significantly correlated with parameters of disease activity, i.e. SLEDAI score, IL-6, hypoalbuminemia. On the other hand, we did not find significant differences in sTREM-1 levels in relation to age, disease duration, medications, ESR, other organ system involvement, or the presence of anti-dsDNA. Our preliminary data indicated that sTREM-1 levels may be an additional useful marker of disease activity in SLE. It also highlights its importance in patients with NPLE. An additional prospective longitudinal study should be carried out to support these findings. [ABSTRACT FROM PUBLISHER] more...

Aim and Background: A comparison between two Ficus species, cultivated in Egypt, was carried out in this study. Their DNA analysis revealed that they are not closely related. Materials and Methods: The pharmacopoeial constants of the leaves showed higher total ash and acid insoluble ash in F. lyrata than in F. platypoda. The other parameters were close in both species. Preliminary phytochemical screening revealed the presence of carbohydrate and/or glycosides, tannins, flavonoids, sterols, and triterpenes in their leaves and was detected in traces in their stems. Results: Saponification of n-hexane extract of the leaves yielded 46% and 74.8% for the unsaponifiable matters and 20% and 15% for the fatty acids for F. platypoda and F. lyrata, respectively. n-Docosane (21.69%) and n-heptacosane (33.77%) were the major hydrocarbons in F. platypoda and F. lyrata, respectively. b-Sitosterol was the main sterol, palmitic (22.07%) and carboceric (35.72%) acids were the major identified saturated fatty acids in both species, while linoleic acid was the main unsaturated fatty acid (18.66% and 16.7%) in both species, respectively. The acute toxicity study revealed that the two species were safe up to 2 g/kg. The antioxidant activity using 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay and pyrogallol as the standard was more significant for F. platypoda (232.6 μg/ml) than for F. lyrata, (790.9 μg/ml). The oral antihyperglycemic activity in diabetic rats using alloxan revealed that the 80% ethanolic extract of the leaves of F. platypoda was more active than that of the leaves of F. lyrata in decreasing the blood glucose level at 200 mg/kg/ day (107.9 ± 5.817, 127.2 ± 4.359) and 400 mg/kg/day (64.11 ± 4.358, 127.7 ± 6.889), respectively, when compared with the diabetic control gliclazide (172.3 ± 2.089). Conclusion: The results of this study provide evidence that the two Ficus species have antioxidant and antihyperglycemic activity, in the order F. platypoda and then F. lyrata. [ABSTRACT FROM AUTHOR] more...

Plantago is a large genus under family Plantaginaceae. Several Plantago species were noted for potent antioxidant, anti-inflammatory and wound healing activities. The current research investigated the potential bioactivities as well as the metabolic content of Plantago boisserei extract. Results highlighted the rich content of phenolics (450.93±7.4 mg GAE/g extract) and flavonoids (144.2±3.6 mg RE/g extract) in this species. HPLC analysis enabled the detection of 17 phenolic constituents among which ellagic acid was found in highest concentration (52.94 mg/g) followed by rutin (6.72 mg/g). Furthermore, P. boisserei extract exhibited a potent antioxidant activity evidenced by the IC 50 values in ABTS and H 2 O 2 assays (10.95 and 10.87 μg/mL, respectively) as well as in TAC assay (67.94 mg AAE/g). The anti-microbial activities of the extract revealed a moderate activity against Staphylococcus aureus and Proteus vulgaris. In vitro testing of the anti-inflammatory potential indicated a characteristic inhibition against COX-1 and COX-2 enzymes with IC 50 62.8 and 14.23 μg/mL, respectively, compared to ibuprofen (IC 50 8.07 and 6.58, respectively). Additionally, P. boisserei extract achieved a potent wound healing activity using in vivo rat model, this might be attributed to its high content of flavonoids together with other polyphenolic compounds that have a great free radical scavenging potential. In conclusion, P. boisserei is a promising candidate for more extensive phytochemical and biological exploration., (© 2024 Wiley-VHCA AG, Zurich, Switzerland.) more...

Purpose: To evaluate the albumin-fibrinogen ratio (AFR) and C-reactive protein-albumin ratio (CAR) as inflammatory markers in rheumatoid arthritis (RA) and to investigate their association with disease activity correlating with musculoskeletal ultrasonographic findings., Patients and Methods: A total of 125 cases of RA patients were consecutively enrolled in a multicenter cross-sectional study compared to 100 healthy controls, all subjects were investigated for fibrinogen, albumin, CRP, erythrocyte sedimentation rate, AFR, and CAR measurements. Patients' disease activity was assessed by disease activity score (DAS28-ESR), and they were subjected to high-frequency ultrasound both in greyscale and power Doppler., Results: RA patients had lower AFR and higher CAR than those in the control group (P < 0.001). A positive correlation was demonstrated between CAR and DAS score (r=0.589, P = 0.0001), whilst there was a precise negative correlation between AFR and DAS 28-ESR (r=-0.74, p<0.001). ROC curve analyses revealed fibrinogen showed the best sensitivity (92.1%) for the area under the curve of 0.928, at a criterion of 2.47, while AFR has an area under the curve of 0.826 with sensitivity and specificity (86.84% and 75%, respectively) at cut-off value 1.46. Actively diseased patients had elevated CAR than those in remission (P < 0.001). Patients with synovial thickening and bone erosions had lower AFR than those without, CAR was higher in patients with power doppler changes than those without (p=0.015)., Conclusion: Higher CAR and lower AFR were expressed in active RA than those in remission. CAR and AFR could be useful markers of ongoing inflammation and joint affection detected by musculoskeletal ultrasonography., Competing Interests: The authors declare no potential conflicts of interest concerning the research, authorship, and/or publication of this article., (© 2020 Afifi et al.) more...