In Vitro α-Glycosidase Inhibition and In Silico Studies of Flavonoids Isolated from Pistacia integerrima Stew ex Brandis.

The galls of Pistacia integerrima are used in folk medicine for curing diabetes. The main aim of this study was the purification of flavonoids from galls of P. integerrima. The methanolic extract was subjected to column chromatographic analysis which afforded six flavonoids, namely, 3,5,7,4'-tetrahydroxy-flavanone (1), naringenin (2), 3,5,4'-trihydroxy,7-methoxy-flavanone (3), sakuranetin (4), spinacetin (5), and patuletin (6). These isolated compounds (1-6) were tested against α-glycosidase. The maximum antagonistic effect was noted against compound 6 (97.65%) followed by compound 5 (90.42%) and compound 1 (90.01%) at the same concentration (0.2 µg). The inhibitory potential of all tested compounds was significant with a degree of variation from each other. Docking studies showed that all studied compounds interact with the active site residues via hydrogen bond interactions with hydroxyl groups, and thus, inhibition was enhanced. Hence, this finding would be the first screening of isolated flavonoids for α-glycosidase activity and with the mechanism of action. These flavonoids should be further investigated as candidate drugs for combating diabetes mellitus.

Nile crab Potamonautes niloticus shell extract: Chromatographic and molecular elucidation of potent antioxidant and anti-inflammatory capabilities.

Diseases emerging from oxidative stress and inflammatory imbalance are deeply threatening the modern world. Fisheries by-products are rich in bioactive metabolites. However, they are usually discarded, posing a real environmental burden. Herein we aimed to explore the bioactive compounds, anti-oxidant, and anti-inflammatory capabilities of the shell of the freshwater Nile crab Potamonautes niloticus. Methanolic extract of crab shell was subjected to GC/MS and HPLC analyses of total lipids, flavonoids, and phenolic acids. Also, zebrafish Danio rerio was subjected to inflammatory status using CuSO4, then treated with different doses of shell extract. Total antioxidant capacity and QPCR analyses for gene expression of different antioxidant enzymes, i.e. superoxide dismutase(sod), catalase (cat), and glutathione peroxidase (gpx) and pro-inflammatory cytokines, i.e. tumor necrosis factor alpha (tnf-α), nuclear factor kappa B (nf-κb), interleukin 1-Beta (il-1b) were assessed. The results showed the richness of crab shell extract with ω - 9 (32.78 %), ω - 7 (6.37 %), and ω - 6 (4 %) unsaturated fatty acids. Diverse phenolic acids and flavonoids were found, dominaed by Benzoic acid (11.24 µg mL-1), Syringic acid (11.4 µg mL-1), Ferulic acid (10.55 µg mL-1), Kampferol (9.47 µg mL-1), Quercetin (6.33 µg mL-1), and Naringin (4.16 µg mL-1). Crab extract also increased the total antioxidant capacity and oxidative stress enzymes mRNA levels by 1.3-2.15 folds. It down-regulated pro-inflammatory cytokines mRNA levels by 1.3-2 folds in comparison to positive control (CuSO4-induced) zebrafishes. The net results indicated that Nile crab shell extract is a rich source of anti-oxidant and anti-inflammatory compounds. Therefore, we recommend to continuously explore the bioactive capabilities of exoskeletons of different shellfish species. This can provide additive values for these products and reduce the environmental burden of their irresponsible discarding.

In Vivo Anti-Inflammatory, Analgesic, Muscle Relaxant, and Sedative Activities of Extracts from Syzygium cumini (L.) Skeels in Mice.

In the current study, the folklore medicine, Syzygium cumini, was experimentally evaluated for anti-inflammatory, analgesic, sedative, and muscle relaxant effects. The extract and fractions of S. cumini were found safe up to 1000 mg/kg with no mortality, except for slight sedation as a minor side effect. Both, the extract and various fractions of S. cumini demonstrated significant inhibition (86.34%) of carrageenan-induced inflammation in mice. Acetic acid induced writhes were attenuated (p < 0.001) by S. cumini in a dose-dependent manner, except for the n-hexane fraction. The maximum effect was observed at a dose of 500 mg/kg in mice. The maximum muscle relaxant effect of all tested samples was recorded at a dose of 500 mg/kg bodyweight, where the percent inhibition exhibited by dichloromethane fraction was 82.34%, followed by chloroform fractions (71.43%) and methanolic extract (70.91%). Our findings validate the folklore medicinal claims of S. cumini, as an analgesic and anti-inflammatory agent.

Antioxidant and Cytotoxic Activity of a New Ferruginan A from Olea ferruginea: In Vitro and In Silico Studies.

Studies of the ethyl acetate extract bark extract of Olea ferruginea led to the isolation of one new compound Ferruginan A (1) in addition to two known compounds, Ferruginan (2) and cycloolivil (3). Structures of the isolated compounds were confirmed by mass spectrometry (MS) and NMR spectral data. The ethyl acetate fraction and compounds (1-3) were evaluated against breast cancer cell line (MCF-7) and as antioxidants using the free radical scavenging assay. Results revealed that compound 2 exhibits significant antioxidant activity with an IC50 value of 21.74 µg/mL. In addition, the ethyl acetate fraction showed good cytotoxic activity (79.31% inhibition at 250 µg/mL), whereas compounds 1-3 exerted mild cytotoxic activity (IC50 = 8.03-12.01 µg/mL) as compared to the standard (IC50 = 4.41 µg/mL) against MCF-7. Docking studies suggested that antioxidant activity is due to the chelation of compounds with copper present in the active site of tyrosinase. These results suggest that the extract exhibits considerable antioxidant activity, and the isolated compounds exert moderate anticancer activity.

Antidiabetic Activity of Ficusonolide, a Triterpene Lactone from Ficus foveolata (Wall. ex Miq.): In Vitro, In Vivo, and In Silico Approaches.

Diabetes is a chronic condition which is locally managed through the stem of Ficus foveolata. To find the exact chemical constituent responsible for this activity, a triterpene lactone (ficusonolide) isolated from F. foveolata was studied for antidiabetic potential through the in vitro antidiabetic paradigm employing L-6 cells and an in vivo antidiabetic assay against non-insulin-dependent rats. The results on glucose uptake in the L-6 cell line indicated that ficusonolide has enhanced the uptake of glucose by 53.27% over control at a dose of 100 µg/mL, while at doses of 50 and 25 µg/mL, the glucose uptake was enhanced by 22.42 and 14.34%, respectively. The extract of F. foveolata (100 mg/kg) and ficusonolide (50 mg/kg) demonstrated a significant (p < 0.001) decline in streptozotocin-induced hyperglycemia of diabetic rats. Ficusonolide displayed conspicuous inhibitory activity against the molecular docking studies with proteins such as dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase subjected to molecular targets. Detailed computational and structural insights affirmed promising interactions between target proteins and ficusonolide. In conclusion, the plant and its isolated compound have significant antidiabetic activity with a possible mechanism of interaction with DPP-IV, PTP-1B, α-glucosidase, and α-amylase.

Khat Chewing and Lipid Profile in Human and Experimental Animals.

BACKGROUND: Catha edulis, also known as khat or qat, is a plant that grows in East Africa and southern Arabia. Several millions of people chew the leaves and twigs of khat plant for their central stimulating amphetamine-like effects. Khat chewing is becoming more common in Europe and the United States, owing to worldwide migration. OBJECTIVE: This review examines the khat ingredients, global prevalence, and legal status as well as its effects on lipid profile. Methodology. A literature search was performed using PubMed, Scopus, and Google Scholar to collect information within articles published up to April 2021 with the goal of identifying relevant studies. The proposed mechanisms of cathinone effects on total cholesterol and triglyceride were also discussed. CONCLUSION: The khat chewing habit is considered as a serious economic and health issue that needs specialized programs to assist those people to quit or reducing this habit.

Augmented anticancer activity of curcumin loaded fungal chitosan nanoparticles.

Fungal chitosan (FCt) from Amylomyces rouxii, with 88.7% deacetylation degree and 112.4 kDa molecular weight, was utilized for nanoparticles (NPs) formation via ionic gelation. FCt-NPs were employed as carriers for curcumin (CUR) to augment its availability and anticancer bioactivity. The synthesis of CUR/FCt-NPs composite was succeeded as evidenced from their FTIR spectra. The scanning micrographs of synthesized CUR/FCt-NPs indicated their spherical shapes and well-distribution; they had average diameters of 115 ± 21 nm and positive zeta potentials of +33.8 mV. The NPs loading capacity for CUR was 21.6% and the encapsulation efficiency reached 83.8%. The CUR was vastly released in the beginning 5 h then gradually released up to 90 h, with higher release in pH 5.2 than in pH 7.0. The treatment of cancer cells, HCT-116 and A-549, with CUR/FCt NPs lead to time-dependent decrement of cells' viability; the dead cells were 67.6% from HCT-116 and 73.8% from A-546 after 96 h of exposure. Fluorescent imaging indicated that most cancer cells entered the apoptosis phase after treatment with 150 µM of CUR/FCt-NPs for 72 h. The efficiency of FCt-NPs was proved as carriers for loading CUR and augmenting its anticancer activity toward human cancer cells, using these natural and biosafe agents.

Augmented control of drug-resistant Candida spp. via fluconazole loading into fungal chitosan nanoparticles.

Fungal chitosan (ACT) extraction from Amylomyces rouxii, its transforming into nano-form, loading with fluconazole (Flu) and evaluation of synthesized nanoconjugates against drug-resistant (DR) Candida spp., were investigated. The produced ACT was characterized with 112.4 kDa molecular weight and 88.7% deacetylation degree. Synthesis of chitosan nanoparticles (NACT), and loading them with Flu were succeeded, using ionic gelation protocol, to generate stable Flu/NACT nanoconjugate' particles with mean size of 82 nm and zeta potential of +3.36 mV. The NACT entrapment efficiency was 78.7% and the drug loading capacity was 60.2%. Flu slowly released from NACT during the first 5 h, then release dramatically increased to the maximum (94.8%) after 12 h. The infra-red spectrum of Flu/NACT nanoconjugates confirmed the strong cross-linkage between their molecules. The antimycotic activity of NACT and Flu/NACT was proved against DR strains of C. albicans (2 strains), C. parapsilosis and C. glabrata, using qualitative and quantitative assays; Flu/NACT exhibited significant powerful activity, which was confirmed via observations with scanning microscopy. Finished cotton textiles with Flu/NACT had augmented potentiality for inhibiting challenged DR Candida spp., using in vitro assay. Accordingly, the synthesis and application of Flu/NACT nanoconjugates was astoundingly recommended for controlling DR Candida spp.

Prevalence of dyslipidemia among students of a Yemeni University.

OBJECTIVES: To estimate the prevalence of dyslipidemia and patterns of lipid profile and associated factors among Yemeni university students. METHODS: This cross-sectional study included 240 Yemeni students (116 males and 124 females) at Ibb University. The students were randomly selected from various faculties of the university. Demographic and clinical data were obtained from all participants. Fasting blood specimens were collected from all students for measurement of serum levels of total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C). The criteria of the National Cholesterol Education Program-Adult Treatment Panel III (NCEP-ATP III) were used. RESULTS: The mean age of the studied cohort was 19.8 ± 1.8 years; 48.3% were men and 51.7% were women. About 56.7% of the participants were from rural areas. Qat chewers and cigarette smokers comprised 63.3% and 6.7% of the cohort, respectively. No obese students were found in this study; however, 11.7% were overweight. The overall prevalence of dyslipidemia, hypercholesterolemia, hypertriglyceridemia, high LDL-C, and low HDL-C among the participating students were 86.7%, 21.7%, 23.8%, 31.7%, and 81.7%, respectively. Mixed hyperlipidemia was present in 8.8% of the students. The prevalence of isolated hypercholesterolemia, hypertriglyceridemia, and low HDL-C was 12.9%, 15%, and 70%, respectively. Dyslipidemia was significantly associated with male sex, increasing age, urban residence, and medical and natural science faculties. In contrast, smoking, qat chewing, physical activity, and the consumption of fast food, fruits and vegetables, and fish were not significantly associated with dyslipidemia. CONCLUSION: To our knowledge, this is the first human study conducted at Ibb University during wartime in Yemen. Dyslipidemia was highly prevalent among healthy Yemeni university students in Ibb city. Low HDL-C was the most prevalent type of dyslipidemia, followed by increased levels of LDL-C. Gender, age, residence, and type of faculty were also closely related to dyslipidemia. These results indicate the need for specialized programs to determine blood lipid levels and initiate intervention programs to reduce the prevalence and prevent the complications of dyslipidemia among Yemeni university students.

Association between qat chewing and dyslipidaemia among young males.

OBJECTIVES: This study investigated the association between qat chewing and prevalence and patterns of dyslipidaemia among young Yemeni males. METHODS: In this cross-sectional study, we used a multistage random cluster sampling method. Data were obtained using a questionnaire. Additionally, anthropometric measurements and fasting blood samples were collected. We used Program-Adult Treatment Panel III. The blood samples were analysed for lipid profile measurements including levels of total cholesterol, triglycerides, low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C). RESULTS: A total of 440 Yemeni male with mean age of 21.4 ± 3.6 years were enrolled. The students were divided into the following two groups-qat chewers (n = 283) and non-qat chewers (n = 77). The overall occurrence of dyslipidaemia was significantly higher in qat chewers than that in non-qat chewers (89.8% versus 80.5%) (P < 0.05). Hypercholesterolaemia, hypertriglyceridaemia, high LDL-C level, and mixed hyperlipidaemia were lower in qat chewers than in non-qat chewers (16.6%, 58.3%, 16.3%, and 10.6%, respectively, versus 20.8%, 64.9%, 18.2%, and 20.8%, respectively). Isolated hypertriglyceridaemia was slightly higher in qat chewers than in non-qat chewers (47.7% versus 44.2%). However, the incidence of low HDL-C level, isolated low HDL-C level, and isolated hypercholesterolaemia were generally higher in qat chewers than in non-qat chewers (83%, 25.1%, and 6%, respectively, versus 75.3%, 15.6%, and 0%, respectively). CONCLUSION: This study showed high prevalence of dyslipidaemia among Yemeni male qat chewers. Low HDL-C level was the main lipid variable, followed by hypertriglyceridaemia. Genetic factors, war conditions, physical inactivity, and low-fat traditional Yemeni diet were considered the determinants of the study findings.

Analysis of patients with end-stage renal disease on dialysis in Tabuk City, Saudi Arabia: A single-center, three-year retrospective study.

This study was performed to analyze various demographic data such as age, gender, nationality, status of the patients, and the causes of end-stage renal disease (ESRD) of 349 patients who were undergoing hemodialysis (HD) during the period from January 2013 to December 2015 at the Dialysis Center of King Khalid Hospital in Tabuk City. One hundred and fifty-two patients (43.6%) were on HD in 2015. Age of the patients ranged from 9 to 93 years and the mean age was 51.3 ± 17.6 years. Majority of the patients, i.e., 140 (40.1%) were in the age group of 40-59 years, followed by the age group of 60-79 years by 27.8% (97 patients). Saudis constituted 84.2% (294) and non-Saudis accounted 15.8% (55) of the patients over the years studied. There were 198 males (56.7%) and 151 females (43.3%). The death rate in 2014 was 6.2%, whereas it increased in 2015 to 10.5%. The high escape rate (10.3%) of patients was in 2014. Diabetic nephropathy was the most common cause of ESRD, accounting for 30.4% of all cases, followed by unknown etiologies accounting for 25.2%. Nearly 22.6% of all ESRD cases had hypertension. Primary glomerular disease was seen in 8.9% and obstructive uropathy in 3.7%. Other causes constituted 7.4% of the cases. The data of ERSD patients in Tabuk City are comparable with that of other regions of the Kingdom of Saudi Arabia. We conclude that analysis studies of HD centers help to understand the problems and the needs of the patients, find the solutions, and create a connection between the consumers and health-care providers.