ABSTRACT
Alcalase hydrolyzates were prepared from the albumin (AH) and globulin (GH) fractions of eight chickpea (Cicer arietinum L.) genotypes from Mexico and 10 from other countries. Protein content, antioxidant activity (AA) (ABTS, DPPH), and degree of hydrolysis were evaluated and the best genotype was selected by principal component analysis. The hydrolyzates of the chosen genotype were analyzed for its antidiabetic potential measured as inhibition of α-amylase, α-glucosidase, and dipeptidyl peptidase-4 (DPP4). Peptide profiles were obtained by liquid chromatography-mass spectrometry (UPLC-DAD-MS), and the most active peptides were analyzed by molecular docking. The average antioxidant activity of albumin hydrolyzates was higher than that of globulin hydrolyzates. ICC3761 was the selected genotype and peptides purified from the albumin hydrolyzate showed the best antioxidant activity and antidiabetic potential (FEI, FEL, FIE, FKN, FGKG, and MEE). FEI, FEL, and FIE were in the same chromatographic peak and this mixture showed the best ABTS scavenging (78.25%) and DPP4 inhibition (IC50 = 4.20 µg/ml). MEE showed the best DPPH scavenging (47%). FGKG showed the best inhibition of α-amylase (54%) and α-glucosidase (56%) and may be a competitive inhibitor based on in silico-predicted interactions with catalytic amino acids in the active site of both enzymes. These peptides could be used as nutraceutical supplements against diseases related to oxidative stress and diabetes. PRACTICAL APPLICATION: This study showed that chickpea protein hydrolyzates are good sources of peptides with antidiabetic potential, showing high antioxidant activity and inhibition of enzymes related to carbohydrate metabolism and type 2 diabetes. These hydrolyzates could be formulated in functional foods for diabetes.
Subject(s)
Antioxidants/chemistry , Cicer/chemistry , Hypoglycemic Agents/chemistry , Peptides/chemistry , Plant Proteins/chemistry , Chromatography, Liquid , Cicer/genetics , Dipeptidyl Peptidase 4/chemistry , Dipeptidyl-Peptidase IV Inhibitors/chemistry , Genotype , Humans , Mass Spectrometry , Molecular Docking Simulation , Plant Extracts/chemistry , Protein Hydrolysates/chemistry , Seeds/chemistry , Seeds/genetics , alpha-Amylases/chemistry , alpha-Glucosidases/chemistryABSTRACT
Pithecellobium dulce is distributed in America and Asia where is widely used in traditional medicine. This study describes the bioguided fractionation of the methanol extract (ME) obtained from the P. dulce fruit that showed in vitro activity against Hymenolepis nana; Artemia salina assay was used to determine toxicity; and the purified compound was computationally analysed to obtain its absorption-distribution-metabolism-excretion-and-toxicity properties (ADMET). The ME and its fractions were more active than praziquantel (PZQ), and the purified compound was characterized as N-malonyl-(+)-tryptophan (NMT). Parasites treated with NMT showed shorter paralysis and death times (5 and 7 min) than those treated with PZQ (15 and 30 min), both used at 20 mg/mL. Toxicity and ADMET prediction results supported the slight-hazardousness and efficacy of the assayed fractions/compound. This is the first report of the antiparasitary activity of both the P. dulce ME and NMT, showing their potential to treat human H. nana infections.
Subject(s)
Fabaceae/chemistry , Fruit/chemistry , Hymenolepis nana/physiology , Tryptophan/isolation & purification , Tryptophan/pharmacology , Animals , Artemia/drug effects , Chemical Fractionation , Humans , Hymenolepis nana/drug effects , Plant Extracts/pharmacologyABSTRACT
BACKGROUND: Milk products fortified with vitamin D may constitute an alternative to pharmacological supplements for reaching the optimal levels of serum 25-hydroxyvitamin D [25(OH)D]. Our aim was to analyze the response of serum 25(OH)D and its predictive factors in postmenopausal healthy women after a dietary intervention with a milk fortified with vitamin D and calcium. METHODS: We designed a prospective study including 305 healthy postmenopausal women who consumed a fortified milk with calcium (900 mg/500 mL) and vitamin D3 (600 IU/500 mL) daily for 24 months. RESULTS: The 25(OH)D concentrations at 24 months were correlated to weight, to body mass index, to the percentage of fat, triglycerides and to baseline 25(OH)D levels. We found significant differences in the levels of 25(OH)D at 24 months according to baseline 25(OH)D levels (p < 0.001) and body mass index (p = 0.019) expressed at quartiles. Multivariate analysis showed an association between levels of 25(OH)D after the intervention and at baseline 25(OH)D (Beta = 0.47, p < 0.001) and percentage of body fat (Beta = -0.227, p = 0.049), regardless of the body mass index. CONCLUSIONS: In healthy postmenopausal women, the improvement in 25(OH)D after an intervention with a fortified milk for 24 months depends mainly on the baseline levels of serum 25(OH)D and on the percentage of body fat.
Subject(s)
Food, Fortified , Milk/chemistry , Postmenopause , Vitamin D/analogs & derivatives , Vitamin D/administration & dosage , Aged , Animals , Bone Density , Female , Humans , Middle Aged , Vitamin D/blood , Vitamin D/chemistryABSTRACT
OBJECTIVE: To determine the effect of the daily intake of calcium and vitamin D-enriched milk (with or without fructooligosaccharides [FOS]) on vitamin D, bone metabolism, and cardiovascular risk factors. MATERIALS AND METHODS: Two-year randomized controlled study, including 500 healthy postmenopausal women, assigned to 500 mL/day of skimmed milk to one of three groups: Low-dose (L): (120 mg/100 mL calcium, vitamin D3 30 UI/100 mL), group A: calcium and vitamin D (180 mg/100 mL and 120 UI/100 mL), and group B: calcium and vitamin D (180 mg/100 mL and 120 UI/100 mL) and FOS (5 g/L). We evaluated serum 25(OH)D, bone mineral density (BMD) by Dual Energy X-ray Absorptiometry, and biochemical data of glucose and lipid metabolism. RESULTS: After 24 months, vitamin D concentrations did not change in the control group, but increased in group A and group B, p < 0.001. We observed an increase in femoral neck BMD and an improvement in fasting plasma glucose, HbA1c, total cholesterol, low-density lipoprotein cholesterol, and apolipoprotein B 100. CONCLUSIONS: Daily intake of milk enriched with calcium and vitamin D in postmenopausal healthy women induces a significant improvement in vitamin D status, a significant increase in BMD at femoral neck, and also favorable effects on glucose and lipid profile.
Subject(s)
Bone Density/drug effects , Cardiovascular Diseases/blood , Milk , Osteoporosis, Postmenopausal/prevention & control , Postmenopause , Vitamin D/blood , Absorptiometry, Photon/methods , Aged , Animals , Anthropometry , Biomarkers/blood , Calcium, Dietary/administration & dosage , Calcium, Dietary/therapeutic use , Dose-Response Relationship, Drug , Double-Blind Method , Female , Food, Fortified , Humans , Middle Aged , Osteoporosis, Postmenopausal/drug therapy , Osteoporosis, Postmenopausal/physiopathology , Spain , Vitamin D/administration & dosageABSTRACT
CONTEXT: Helicteres vegae Cristóbal (Sterculiaceae) (Hv) and Heliopsis sinaloensis B.L. Turner (Asteraceae) (Hs) are endangered and poorly studied plant species; related plants have been used against chronic-degenerative and infectious diseases. Therefore, Hv and Hs could be sources of bioactive compounds against these illnesses. OBJECTIVE: To determine the chemical composition and biological activities (antioxidant, antimutagenic and antimicrobial) of Hv and Hs leaves (L) and stems (S). MATERIALS AND METHODS: Methanol extracts (ME) of each plant/tissue were evaluated for their phytochemicals; phenolics (HPLC-DAD-ESI-MS); antioxidant activity (AA) (0.125-4 mg/mL) (DPPH, ABTS, ORAC and ß-carotene discoloration); antimutagenicity (0.5 and 1 mg/plate) (Ames assay, tester strain Salmonella enterica serovar Typhimurium YG1024, 1-nitropyrene as mutagen); activity against human pathogens (1 mg/mL); and toxicity (0.01-2 mg/mL) (Artemia salina assay). RESULTS: All ME showed flavonoids and triterpenes/steroids. The ME-SHv had the highest content of total phenolics (TP) (2245.82 ± 21.45 mg GAE/100 g d.w.) and condensed tannins (603.71 ± 1.115 mg CE/100 g d.w.). The compounds identified were flavonoids (kaempferol 7-O-coumaroylhexoside, and two kaempferol 7-O-rhamnosylhexosides) and phenolics [rosmarinic acid, and 3'-O-(8â³-Z-caffeoyl) rosmarinic acid]. The ME-LHs showed the highest content of flavonoids (357.88 mg RE/g d.w.) and phenolic acids (238.58 mg CAE/g d.w.) by HPLC. The ME-SHv showed the highest AA. All ME were strong antimutagens (63.3-85.7%). Only the Hs extracts were toxic (ME-LHs, LC50 = 94.9 ± 1.7 µg/mL; ME-SHs, LC50 = 89.03 ± 4.42 µg/mL). DISCUSSION AND CONCLUSIONS: Both Hv and Hs are potential sources of preventive and therapeutic agents against chronic-degenerative diseases.
Subject(s)
Anti-Infective Agents/pharmacology , Antimutagenic Agents/pharmacology , Antioxidants/pharmacology , Asteraceae/chemistry , Malvaceae/chemistry , Plant Extracts/pharmacology , Animals , Anti-Infective Agents/chemistry , Anti-Infective Agents/isolation & purification , Anti-Infective Agents/toxicity , Antimutagenic Agents/chemistry , Antimutagenic Agents/isolation & purification , Antimutagenic Agents/toxicity , Antioxidants/chemistry , Antioxidants/isolation & purification , Antioxidants/toxicity , Artemia/drug effects , Bacteria/drug effects , Bacteria/growth & development , Benzothiazoles/chemistry , Biphenyl Compounds/chemistry , Chromatography, High Pressure Liquid , Giardia lamblia/drug effects , Giardia lamblia/growth & development , Methanol/chemistry , Microbial Sensitivity Tests , Mutagenicity Tests , Oxygen Radical Absorbance Capacity , Parasitic Sensitivity Tests , Phytotherapy , Picrates/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Plant Leaves/chemistry , Plant Stems/chemistry , Plants, Medicinal , Salmonella typhimurium/drug effects , Salmonella typhimurium/genetics , Solvents/chemistry , Spectrometry, Mass, Electrospray Ionization , Sulfonic Acids/chemistry , beta Carotene/chemistryABSTRACT
Las intoxicaciones por fósforo blanco, no han dejado de observarse en la actualidad (2). El fósforo blanco es un compuesto muy tóxico, que en el humano causa intoxicación aguda tras la ingesta por vía oral, que por lo general es en forma suicida, en mujeres jóvenes como son los casos que presentamos. El cuadro clínico es similar a los tres casos, caracterizado por dolor abdominal, vómito, ictericia y con un componente depresivo. Con el propósito de reducir su prevalencia las autoridades de salud deberían prohibir su fabricación y su venta.