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1.
J Clin Transl Res ; 8(5): 434-444, 2022 Oct 31.
Article in English | MEDLINE | ID: mdl-36451797

ABSTRACT

Background and Aim: The brain is one of the most complex and crucial organs of our body. Its health is a matter of concern for all individuals as the number of aged people is increasing gradually in the world. Carica papaya is a ubiquitous plant, and its different parts possess neuroprotective effects against various neurodegenerative diseases. However, its brain anti-aging effects have remained uninvestigated. Therefore, this study has examined the brain anti-aging strength of C. papaya pulp and seeds extracts in D-galactose-induced aging rats. Methods: The rats were intraperitoneally injected with 150 mg/kg of D-galactose for 8 consecutive weeks to induce brain aging. In parallel, the rats of papaya pulp and papaya seed treated groups were injected with 150 mg/kg papaya pulp extract and 150 mg/kg papaya seed extract, respectively. The negative control group was only injected with 0.9% saline, whereas in the rats of the positive control group along with D-galactose 100 mg/kg VC was injected. After the treatment period, different neurobehavioral, neurochemical, and antioxidant analyses were performed to unmask the anti-aging strength of C. papaya pulp and seeds extracts. Results: C. papaya pulp and seed extracts significantly improved cognitive learning skills, memory, and muscular strength in aging rats while reducing stress and anxiety levels. Moreover, they enhanced neurotransmitters concentration and reduced oxidative stress. However, the anti-aging effects of C. papaya pulp were more significant than seeds. Conclusion: These results suggest that both C. papaya pulp and seed extracts possess neuroprotective effects against brain aging or age-related brain deteriorations but the age-protecting capability of C. papaya pulp is higher than C. papaya seeds. Therefore, it could be utilized as a component to design a novel brain anti-aging drug. Relevance for Patients: Brain aging is a natural process that every individual experiences in his life. The regular consumption of C. papaya can improve the quality of life by protecting neurons from age-related deteriorations.

2.
Pak J Pharm Sci ; 30(4(Suppl.)): 1431-1438, 2017 Jul.
Article in English | MEDLINE | ID: mdl-29043993

ABSTRACT

Obesity is an important risk factor for sleep disorders. This study aimed to evaluate the association of leptin, zinc and tryptophan (TRP) in obese subjects with sleep deficits [sleep apnea (SA), insomnia (IN)]. In this cross sectional case control, with the verbal and written consent 206, obese with sleep deficits and 30, non-obese/normal identified from various areas of Karachi, Pakistan. The socio-demographic data including; age, body mass index (BMI), education and residence, of participants was collected. After providing informed consent, fasting blood samples were taken and serum was collected. The serum concentration of leptin, zinc and TRP were analyzed by ELISA (Enzyme-linked immunosorbent assay), FAAS (Flame atomic absorption spectrophotometer) and HPLC (High performance liquid chromatography) respectively. A significant correlation was found between BMI (body mass index) and leptin, BMI and zinc, BMI and TRP. The correlation between leptin consecutively was significantly associated with zinc and TRP in obese patients. Sleep deficits elevated circulatory levels of leptin while lower zinc and TRP levels compared to levels seen in non-obese (Normal) subjects with no sleep deficits. Obese subjects exhibited significantly higher levels of leptin with sleep deficits compared with non-obese subjects with normal sleep pattern, while obese subjects with SA had significantly high levels of leptin than obese subjects with IN and IN+SA. Patients with sleep deficits had significantly lower levels of serum TRP and zinc than non-obese subjects with normal sleep pattern. Obese subjects with SA had significantly lower levels of zinc and elevated levels of TRP than obese subjects with IN. Obese patients with IN+SA had significantly lower levels of leptin and zinc than IN and SA , while TRP levels were significantly lower in subjects with IN than obese subjects with IN+SA and IN. These results suggest that elevated levels of leptin which are possibly by adiposity and lessened levels of zinc and TRP have a great impact on progression of obesity and their association can contribute to tempt sleep disorders.


Subject(s)
Leptin/blood , Obesity/blood , Sleep Apnea Syndromes/blood , Sleep Initiation and Maintenance Disorders/blood , Sleep , Tryptophan/blood , Zinc/blood , Adiposity , Adult , Biomarkers/blood , Body Mass Index , Case-Control Studies , Cross-Sectional Studies , Female , Humans , Male , Obesity/complications , Obesity/diagnosis , Prognosis , Sleep Apnea Syndromes/diagnosis , Sleep Apnea Syndromes/etiology , Sleep Apnea Syndromes/physiopathology , Sleep Initiation and Maintenance Disorders/diagnosis , Sleep Initiation and Maintenance Disorders/etiology , Sleep Initiation and Maintenance Disorders/physiopathology , Young Adult
3.
Pak J Pharm Sci ; 28(2): 521-3, 2015 Mar.
Article in English | MEDLINE | ID: mdl-25730784

ABSTRACT

Anti-glycation and α-glucosidase inhibition activities of microbial transformed compounds of dydrogesterone (1); 20R-hydroxy-9ß,10αa-pregna-4,6-diene-3-one (2), 17ß-hydroxy-9ß,10α-androsta-4,6-diene-3-one (3) and 9ß,10α-androsta-4,6-diene-3,17-dione (4) were evaluated. Compounds 1 and 4 showed potent α-glucosidase inhibitory activities, while 2 and 3 were found to be weak inhibitors, whereas anti-glycation activities of 1-4 were not observed.


Subject(s)
Dydrogesterone/pharmacology , Glycoside Hydrolase Inhibitors/pharmacology , Gibberella/metabolism , Glycosylation/drug effects , Rutin/pharmacology
4.
Pharm Biol ; 51(3): 383-90, 2013 Mar.
Article in English | MEDLINE | ID: mdl-23406359

ABSTRACT

CONTEXT: In the course of searching hepatoprotective agents from natural sources, the protective effect of chemical constituents of the marine brown alga Spatoglossum variabile Figaro et DE Notar (Dictyoaceae) against CCl4-induced liver damage in Wistar rats was investigated. The compounds were first investigated for in vitro radical scavenging potential and were also tested for ß-glucuronidase inhibition to further explore the relationship between hepatoprotection and antiradical potential. METHODS: The compounds cinnamic acid esters 1 and 2 and aurone derivatives 3 and 4 were first investigated for in vitro radical scavenging potential against 1,1-diphenyl-2-picrylhydrazyl radicals (DPPH), and superoxide anion radicals. In vivo hepatoprotective studies were performed in seven groups (n = 6) of Wistar rats. The test groups were pretreated with compounds (10 mg/kg body weight, po) orally for 30 min before the intraperitoneal administration of a dose of 20% CCl4 diluted with dietary cooking oil. Moreover, compounds were also tested for ß-glucuronidase inhibition to explore the relationship between hepatoprotection and radical scavenging potential. RESULTS: The test compounds 1-4 were found to exhibit antiradical activity against 1,1-diphenyl-2-picrylhydrazyl radicals with IC50 values ranging between 54 and 138 µM, whereas aurone derivatives 3 and 4 additionally exhibited superoxide anion scavenging effects with IC50 values of 95 and 87 µM, respectively. In addition, these compounds were found to be weak inhibitors of xanthine oxidase (IC50 ≥1000 µM). In animal model, pretreatment with compounds 2-4 significantly blocked the CCl4-induced increase in the levels of the serum biochemical markers. CONCLUSION: It appears that the hepatoprotection afforded by these compounds was mainly due to their radical scavenging activity that protected the cells from the free radicals generated by CCl4-induced hepatotoxicity.


Subject(s)
Benzofurans/therapeutic use , Carbon Tetrachloride Poisoning/prevention & control , Cinnamates/therapeutic use , Free Radical Scavengers/therapeutic use , Liver/drug effects , Phaeophyceae/chemistry , Animals , Benzofurans/adverse effects , Benzofurans/chemistry , Benzofurans/pharmacology , Biomarkers/blood , Carbon Tetrachloride Poisoning/blood , Carbon Tetrachloride Poisoning/physiopathology , Cell Survival/drug effects , Cinnamates/adverse effects , Cinnamates/chemistry , Cinnamates/pharmacology , Drug Discovery , Enzyme Inhibitors/adverse effects , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Enzyme Inhibitors/therapeutic use , Escherichia coli Proteins/antagonists & inhibitors , Free Radical Scavengers/adverse effects , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology , Glucuronidase/antagonists & inhibitors , Humans , Liver/physiopathology , Male , Milk Proteins/antagonists & inhibitors , Neutrophils/drug effects , Rats , Rats, Wistar , Xanthine Oxidase/antagonists & inhibitors
5.
Life Sci ; 92(3): 187-92, 2013 Feb 27.
Article in English | MEDLINE | ID: mdl-23270944

ABSTRACT

AIMS: One of the aims of this research work is the isolation and identification of various constituents of two medicinally important plants (Iris loczyi and Iris unguicularis). Secondly, the prime aim is the biological evaluation of these natural products to discover new potential inhibitors of α-glucosidase enzyme and protein glycation. MAIN METHODS: Plants of the genus Iris contain a variety of secondary metabolites. Chromatographic techniques were applied for the isolation of different compounds from Iris loczyi and Iris unguicularis. All the isolated compounds were screened for their α-glucosidase enzyme inhibition and antiglycation potential. KEY FINDINGS: It is shown in the results that two compounds (Kaempferol and 8-Methoxyeriodictyol) isolated from plant Iris unguicularis and compounds (Arborinone and 5,7-dihydroxy-2',6-dimethoxyisoflavone) isolated from plant Iris loczyi possess promising activity against α-glucosidase enzyme as compare to acarbose which is used as a standard α-glucosidase inhibitor in this study. A flavanone (2',5-dihydroxy-6,7-methylenedioxy) isolated from Iris loczyi was explored as most active anti-glycating agent. SIGNIFICANCE: α-Glucosidase enzyme is a therapeutic target to treat carbohydrate mediated diseases. In this study various inhibitors of α-glucosidase are identified which might be important for the management of diabetes. Similarly, antiglycation agents may have application for the management of late diabetic complications.


Subject(s)
Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors , Iris Plant/chemistry , Animals , Carbohydrate Metabolism/drug effects , Cattle , Enzyme Inhibitors/therapeutic use , Glycosylation/drug effects , Metabolic Diseases/drug therapy , Metabolic Diseases/enzymology , alpha-Glucosidases/chemistry , alpha-Glucosidases/metabolism
6.
J Ethnopharmacol ; 144(1): 217-9, 2012 Oct 31.
Article in English | MEDLINE | ID: mdl-22954497

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Antidesma bunius Spreng. (Phyllantaceae), Averrhoa bilimbi L. (Oxalidaceae), Biophytum sensitivum (L.) DC. (Oxalidaceae), Ceriops tagal (Perr.) C.B. Rob. (Rhizophoraceae), Kyllinga monocephala Rottb. (Cyperaceae), and Rhizophora mucronata Lam. (Rhizophoraceae) are used as remedies to control diabetes. In the present study, these plants were screened for their potential α-glucosidase inhibitory activity. MATERIALS AND METHODS: The 80% aqueous ethanolic extracts were screened for their α-glucosidase enzyme inhibitory activity using yeast alpha glucosidase enzyme. RESULTS: Except for A. bilimbi with IC(50) at 519.86±3.07, all manifested a significant enzyme inhibitory activity. R. mucronata manifested the highest activity with IC(50) at 0.08±1.82 µg mL(-1), followed by C. tagal with IC(50) at 0.85±1.46 µg mL(-1) and B. sensitivum with IC(50) at 2.24±1.58 µg mL(-1). CONCLUSION: This is the first report on the α-glucosidase inhibitory effect of the six Philippine plants; thus, partly defining the mechanism on why these medicinal plants possess antidiabetic properties.


Subject(s)
Enzyme Inhibitors/pharmacology , Glycoside Hydrolase Inhibitors , Magnoliopsida , Plant Extracts/pharmacology , Diabetes Mellitus/drug therapy , Philippines , Plant Components, Aerial , Plant Roots , Plants, Medicinal
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