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1.
ACS Omega ; 9(5): 5319-5329, 2024 Feb 06.
Article in English | MEDLINE | ID: mdl-38343986

ABSTRACT

The instability of anthocyanins limits their application in food supplementation and in the food industry. Stabilities of strawberry anthocyanins (AN) were improved by complexation with both ß-CD and starch against heat, H2O2, light, and UV irradiation. The stability of AN against H2O2 (2.21 mM) dropped (<20%) in 6 h but was enhanced in ß-CD (49.32%) and starch (96.84%) complexes. Under light conditions, AN in the solid and solution (3.88 g/100 mL) forms degraded to 36.49 and 11.11%, while ß-CD and starch complexes displayed stabilities of 98.20 and 91.76%, respectively, after 60 days. Under UV irradiation, AN showed similar instability where both AN forms expressed stabilities of 36.75 and 66.18%, respectively, after 168 h, while ß-CD and starch complexes exhibited 51.13 and 40.10%, respectively. LC-MS-ESI showed that photoirradiation of both destroyed the full conjugation of the flavylium ring of the major components, pelargonidin and cyanidin hexoses; the mechanism was proposed. Docking binding models of major AN components in ß-CD were obtained.

2.
Ann Med ; 53(1): 1032-1040, 2021 12.
Article in English | MEDLINE | ID: mdl-34233552

ABSTRACT

BACKGROUND: Fibromyalgia (FM) is characterized by musculoskeletal pain, fatigue, sleep and memory disturbance. There is no definitive cure yet for FM-related health problems. Peroxisome proliferator-activated receptor's (PPAR's) activation is associated with insulin sensitisation and improved glucose metabolism. PPAR-γ was reported to alleviate FM allodynia. Limited data are discussing its effect on motor disorders. OBJECTIVE: To investigate the potential effect of PPAR-γ agonists (pioglitazone, as one member of thiazolidinediones (TZD)) on motor dysfunction in reserpine-induced FM in a rat model. MATERIALS AND METHODS: Thirty-six male Wistar rats were divided into negative control (n = 9) and reserpine-induced FM (n = 27) groups. The latter was subdivided into three equal subgroups (n = 9), positive control (untreated FM model), pioglitazone-treated and GW9662-treated. We evaluated muscle functions and activity of chloramphenicol acetyltransferase, superoxide dismutase, malondialdehyde, and serum levels of interleukin-8 and monocyte chemoattractant protein-1. RESULTS: Pioglitazone significantly relieved fatigue, improved muscle performance, reduced inflammatory cytokines and enhanced antioxidant's activity, while GW9662, a known PPAR-γ antagonist, aggravated the FM manifestations in the rat model. CONCLUSION: PPAR-γ agonists show a promising role against FM-associated motor dysfunctions.


Subject(s)
Fibromyalgia/drug therapy , Muscle, Skeletal/drug effects , Pioglitazone/therapeutic use , Reserpine/pharmacology , Thiazolidinediones/pharmacology , Animals , Fatigue , Fibromyalgia/chemically induced , Humans , Male , PPAR gamma , Rats , Rats, Wistar
3.
Bioorg Chem ; 94: 103458, 2020 01.
Article in English | MEDLINE | ID: mdl-31785854

ABSTRACT

A series of 2-phenyl-7-(aryl)pyrazolo[1,5-a]pyrimidine-3-carbonitriles 11a-j and 2-phenyl-7-(aryl)pyrazolo[1,5-a]pyrimidine-3,6-dicarbonitriles 16a-c was synthesized by the reaction of 5-amino-3-phenyl-1H-pyrazole-4-carbonitrile (5) with 3-(dimethylamino)-1-arylprop-2-en-1-ones 6a-j or 2-aryl-3-(dimethylamino)acrylonitriles 12a-c, respectively. In addition, 7-amino-5-oxo-2-phenyl-4,5-dihydropyrazolo[1,5-a]pyrimidine-3-carbonitrile (22) was prepared from the reaction of compound 5 with ethyl cyanoacetate. The anticancer activity of the newly synthesized compounds against Huh-7, HeLa, MCF-7 and MDA-MB231 cell lines showed moderate activity of compound 11f as anti-proliferative agent against Huh-7 cell line with IC50 = 6.3 µM when compared with doxorubicin (IC50 = 3.2 µM). On the other hand, compound 16b revealed potent anti-proliferative activity against HeLa cell line with IC50 = 7.8 µM when compared with doxorubicin (IC50 = 8.1 µM). Also compound 11i exhibited a promising anti-proliferative activity against MCF-7 cell line (IC50 = 3.0 µM) whereas IC50 of doxorubicin = 5.9 µM, finally compounds 11i and 16b have potent activity as anti-proliferative agents against MDA-MB231 cell line with IC50 = 4.32 and 5.74 µM, respectively when compared with doxorubicin (IC50 = 6.0 µM).


Subject(s)
Antineoplastic Agents/pharmacology , Pyrazoles/pharmacology , Pyrimidines/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Cell Cycle/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Molecular Structure , Pyrazoles/chemical synthesis , Pyrazoles/chemistry , Pyrimidines/chemical synthesis , Pyrimidines/chemistry , Structure-Activity Relationship
4.
Nutr Clin Pract ; 32(3): 378-384, 2017 Jun.
Article in English | MEDLINE | ID: mdl-28537519

ABSTRACT

BACKGROUND: Vitamin D deficiency is a prevalent condition among critically ill patients. Information about the relationship between vitamin D levels and outcomes in the intensive care unit (ICU) is sparse. PURPOSE: To evaluate vitamin D status among critically ill patients and its relevance to severity of illness, ICU stay period, and mortality. METHODS: This prospective multicenter study was conducted in the ICUs of Fayoum, Cairo, Alazhar, and Ain Shams university hospitals. All patients were subjected to interview questionnaire, laboratory investigation, vitamin D level assessment, and severity of illness evaluation using the Acute Physiologic Assessment and Chronic Health Evaluation II (APACHE II) score. RESULTS: In total, 250 patients were included in the study. The median age was 62 (40-73) years, and most patients were male (52%). The median serum level of vitamin D was 19 (7-40.6). Vitamin D was deficient in 197 patients (78.8%) on admission. While we grouped the ICU patients as vitamin D deficient, insufficient, and sufficient, vitamin D-deficient patients had more severe diseases (mean APACHE II score, 44 ± 15; P = .014). Prolonged ICU stay was observed among the deficient group but with no significant association. The overall mortality rate was 6.8%; of these, 70.5% were vitamin D-deficient patients. However, logistic regression analysis demonstrated that vitamin D deficiency was not an independent risk factor for mortality. CONCLUSION: Vitamin D insufficiency is common in critically ill patients (69%); it is associated with more severity of illness, but it is not an independent risk factor for longer ICU stay or mortality.


Subject(s)
Critical Illness/mortality , Vitamin D Deficiency/blood , Vitamin D Deficiency/epidemiology , Adult , Aged , Egypt/epidemiology , Female , Humans , Intensive Care Units , Logistic Models , Male , Middle Aged , Parathyroid Hormone/blood , Prevalence , Prospective Studies , Sample Size , Surveys and Questionnaires , Vitamin D/blood , Vitamin D Deficiency/diagnosis
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