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1.
Molecules ; 27(16)2022 Aug 12.
Article in English | MEDLINE | ID: mdl-36014395

ABSTRACT

Averrhoa carambola L. is reported for its anti-obese and anti-diabetic activities. The present study aimed to investigate its aqueous methanol leaf extract (CLL) in vivo anti-obese activity along with the isolation and identification of bioactive compounds and their in vitro α-glucosidase inhibition assessment. CLL improved all obesity complications and exhibited significant activity in an obese rat model. Fourteen compounds, including four flavone glycosides (1-4) and ten dihydrochalcone glycosides (5-12), were isolated and identified using spectroscopic techniques. New compounds identified in planta included (1) apigenin 6-C-(2-deoxy-ß-D-galactopyranoside)-7-O-ß-D-quinovopyranoside, (8) phloretin 3'-C-(2-O-(E)-cinnamoyl-3-O-ß-D-fucopyranosyl-4-O-acetyl)-ß-D-fucopyranosyl-6'-O-ß-D fucopyranosyl-(1/2)-α-L arabinofuranoside, (11a) phloretin3'-C-(2-O-(E)-p-coumaroyl-3-O-ß-D-fucosyl-4-O-acetyl)-ß-D-fucosyl-6'-O-(2-O-ß-D-fucosyl)-α-L-arabinofuranoside, (11b) phloretin3'-C-(2-O-(Z)-p-coumaroyl-3-O-ß-D-fucosyl-4-O-acetyl)-ß-D-fucosyl-6'-O-(2-O-ß-D-fucosyl)-α-L-arabinofuranoside. Carambolaside M (5), carambolaside Ia (6), carambolaside J (7), carambolaside I (9), carambolaside P (10a), carambolaside O (10b), and carambolaside Q (12), which are reported for the first time from A. carambola L. leaves, whereas luteolin 6-C-α-L-rhamnopyranosyl-(1-2)-ß-D-fucopyranoside (2), apigenin 6-C-ß-D-galactopyranoside (3), and apigenin 6-C-α-L-rhamnopyranosyl-(1-2)-ß-L-fucopyranoside (4) are isolated for the first time from Family. Oxalidaceae. In vitro α-glucosidase inhibitory activity revealed the potential efficacy of flavone glycosides, viz., 1, 2, 3, and 4 as antidiabetic agents. In contrast, dihydrochalcone glycosides (5-11) showed weak activity, except for compound 12, which showed relatively strong activity.


Subject(s)
Averrhoa , Leukemia, Lymphocytic, Chronic, B-Cell , Animals , Apigenin , Averrhoa/chemistry , Galactose , Glycoside Hydrolase Inhibitors/pharmacology , Glycosides/chemistry , Plant Leaves , Polyphenols/pharmacology , Rats , alpha-Glucosidases
2.
Molecules ; 25(10)2020 May 22.
Article in English | MEDLINE | ID: mdl-32455938

ABSTRACT

Averrhoa carambola L. is a tropical tree with edible fruit that grows at different climatic conditions. Despite its nutritive value and reported health benefits, it is a controversial fruit owing to its rich oxalate content. The present study aimed at investigating aroma and nutrient primary metabolites distribution in A. carambola fruits grown in Indonesia, Malaysia (its endemic origin) versus Egypt, and at different ripening stages. Two techniques were employed to assess volatile and non-volatile metabolites including headspace solid-phase micro-extraction (HS-SPME) joined with gas chromatography coupled with mass-spectrometry (GC-MS) and GC-MS post silylation, respectively. Twenty-four volatiles were detected, with esters amounting for the major class of volatiles in Egyptian fruit at ca. 66%, with methyl caproate as the major component, distinguishing it from other origins. In contrast, aldehydes predominated tropically grown fruits with the ether myristicin found exclusively in these. Primary metabolites profiling led to the identification of 117 metabolites viz. sugars, polyols and organic acids. Fructose (38-48%) and glucose (21-25%) predominated sugar compositions in ripe fruits, whereas sorbitol was the major sugar alcohol (2.4-10.5%) in ripe fruits as well. Oxalic acid, an anti-nutrient with potential health risks, was the major organic acid detected in all the studied fruits (1.7-2.7%), except the Malaysian one (0.07%). It increases upon fruit ripening, including considerable amounts of volatile oxalate esters detected via SPME, and which must not be omitted in total oxalate determinations for safety assessments.


Subject(s)
Averrhoa/metabolism , Metabolome , Nutrients/metabolism , Volatile Organic Compounds/metabolism , Averrhoa/chemistry , Egypt , Esters/chemistry , Fruit/chemistry , Gas Chromatography-Mass Spectrometry , Humans , Malaysia , Nutrients/chemistry , Odorants/analysis , Volatile Organic Compounds/chemistry
3.
Pharm Dev Technol ; 24(6): 729-738, 2019 Jul.
Article in English | MEDLINE | ID: mdl-30775948

ABSTRACT

Fennel (Foeniculum vulgare Mill.) is a member of family Apiaceae. Trans-anethole, the major component of Fennel essential oil (FEO), possesses antioxidant and hepatoprotective effects. Transdermal nanoemulsions (NEs) are advanced colloidal systems for systemic and controlled drug delivery through the stratum corneum barrier. FEO NEs were prepared using the oil Lauroglycol™ 90, as it provides a larger NE existence zone than Captex® 300, in the constructed phase diagrams. Six systems were prepared using Tween20/propylene glycol (S/CoS) in the ratios 2:1 and 3:1 with oil to S/CoS mass ratios 1:9, 2:8 and 3:7. Physicochemical characterization revealed optimum properties regarding thermodynamic stability, droplet size and pH with a Newtonian flow pattern. In vitro permeation study in rat skin revealed the highest cumulative amount permeated (µg/cm2), flux and permeability coefficient values for F4 made up of 2% FEO, 4.67% Lauroglycol™ 90, 60% S/CoS in the ratio 3:1. Results of the in vivo hepatic dysfunction study in rats indicate promising significant amelioration of liver function reflected in ALT, AST, ALP, bilirubin, albumin, malondialdehyde and ammonia plasma levels. The results signify the promising approach of FEO NEs in achieving remedy of liver toxicity. The most promising effect is inherent to F4 which imparts a more positive effect than FEO.


Subject(s)
Delayed-Action Preparations/chemistry , Foeniculum/chemistry , Liver Diseases/drug therapy , Oils, Volatile/administration & dosage , Oils, Volatile/therapeutic use , Administration, Cutaneous , Animals , Emulsions/chemistry , Liver/drug effects , Liver/physiopathology , Liver Diseases/physiopathology , Male , Oils, Volatile/chemistry , Oils, Volatile/pharmacokinetics , Polysorbates/chemistry , Propylene Glycol/chemistry , Rats , Skin Absorption
4.
Pak J Biol Sci ; 22(11): 537-544, 2019 Jan.
Article in English | MEDLINE | ID: mdl-31930832

ABSTRACT

BACKGROUND AND OBJECTIVE: Hyperlipidemia (HLP) is a leading cause for cardiovascular disease and atherosclerosis. Insufficient physical activity and unhealthy diet plays an important role in the progression of HLP. The present study was conducted to investigate the protective effect of 2 unconventional edible oils (purslane and garden cress) on hyperlipidemia. MATERIALS AND METHODS: Diet high in fat and cholesterol was used as inducer of hyperlipidemia in rats for 5 weeks. Plasma and hepatic lipid profile were assessed. Plasma levels of malondialdehyde (MDA) as lipid peroxidation indicator was determined. Liver transaminases (AST and ALT) as liver function indicator and kidney function (creatinine and urea) were evaluated. RESULTS: Results clarified significant elevation in plasma and liver lipid profiles, MDA, liver enzymes (AST and ALT) and kidney function (creatinine and urea) in hyperlipidemic control compared to normal control. Supplementation with purslane and garden cress seeds oils either in diet or oral showed significant improvement in all the studied parameters. CONCLUSION: Purslane and garden cress oils investigated in the current study produced significant reduction and elevation in bad and good cholesterol, respectively in plasma. Also both oils reduced hepatic lipid accumulation effectively in hyperlipidemia model in rats. Oils administration reduced plasma malondialdehyde and improves liver and kidney functions.


Subject(s)
Dietary Fats, Unsaturated/isolation & purification , Hyperlipidemias/prevention & control , Plant Oils/isolation & purification , Animals , Diet, High-Fat , Dietary Fats, Unsaturated/administration & dosage , Dietary Supplements , Disease Models, Animal , Fats, Unsaturated/chemistry , Hyperlipidemias/blood , Hyperlipidemias/diet therapy , Hypolipidemic Agents/administration & dosage , Hypolipidemic Agents/chemistry , Hypolipidemic Agents/isolation & purification , Lepidium sativum/chemistry , Lipids/blood , Liver/drug effects , Liver/metabolism , Male , Plant Oils/administration & dosage , Plant Oils/chemistry , Portulaca/chemistry , Rats , Rats, Sprague-Dawley , Seeds/chemistry
5.
Pak J Biol Sci ; 22(12): 564-573, 2019 Jan.
Article in English | MEDLINE | ID: mdl-31930854

ABSTRACT

BACKGROUND AND OBJECTIVE: Anthocyanin is responsible for the red color of apple. Ultraviolet light plays a key role in activating the genes responsible for anthocyanin biosynthesis. However, the most important concern is using UV light irradiation on fruit to increase anthocyanins level and its nutritional quality. In this study, the accumulation of anthocyanin in green apple using UV-B and UV-C was investigated and its biological influence was evaluated in rats. MATERIAL AND METHOD: Green Golden delicious apples were irradiated with doses of UV-C and UV-B light for a period of 3 h/day each for 3 days. Two Groups of rats were fed on balanced diet or balanced diet supplemented with 10% apple exposure to UV (AP-UV) for a month. RESULTS: The HPTLC and spectrophotometric determination of anthocyanin revealed that color development was significantly increased by 90% in treated apple compared to the control apples. Histological difference was observed between the 2 groups. Plasma levels of uric acid, the activity of transaminases (ALT and AST) as well as malondialdehyde (MDA) were significantly elevated in AP-UV rats. Plasma total cholesterol, triglycerides and creatinine level did not differ among the 2 groups. Liver MDA and catalase levels were eminent in AP-UV rats compared to control. Gene expression of selected inflammatory cytokines (TNF-α, IL-6 and IL-1ß) was significantly up-regulated in liver of AP-UV rats in comparison to control rats. CONCLUSION: The result revealed that there is a health-hazard linked to feeding rats on diet containing irradiated-apple with UV-B and UV-C, which represented by body weight reduction, inflammation development, liver function and oxidative stress elevation.


Subject(s)
Food Irradiation/adverse effects , Malus/radiation effects , Animals , Anthocyanins/metabolism , Color , Food Quality , Fruit/adverse effects , Fruit/metabolism , Fruit/radiation effects , Interleukin-1beta/genetics , Interleukin-6/genetics , Liver/metabolism , Liver/pathology , Male , Malus/adverse effects , Malus/metabolism , RNA, Messenger/genetics , RNA, Messenger/metabolism , Rats , Tumor Necrosis Factor-alpha/genetics , Ultraviolet Rays/adverse effects , Up-Regulation
6.
Drug Dev Ind Pharm ; 45(1): 32-42, 2019 Jan.
Article in English | MEDLINE | ID: mdl-30132727

ABSTRACT

Chronic renal failure (CRF) is among the major health problems that could lead to increased morbidity and mortality among population. 'Nutraceuticals' is an emerging field for natural agents from plant foods that could reduce the progression of such disease. Many newly developed drugs are having bioavailability problems owing to their water insolubility. Liquisolid technique is one of the promising technological approaches to increase solubility and hence, drug absorption. The aim of the present research is to prepare and evaluate the renoprotective effect of the walnut extracts liquisolid formulations in CRF rat model. Saturation solubility study claimed PEG 400 and Tween 20 as good solubilizers for walnut extracts, thus chosen for preparation. The angle of slide was determined for the carrier; microcrystalline cellulose and coating material; silicon dioxide and liquid load factor was evaluated. Eight liquisolid systems were prepared employing 25% and 50% of liquid medication. Their flow and compressibility parameters showed good properties. Dissolution study was more in favor of formulations prepared using PEG 400. Of these, formulation F8 comprising carrier/coat ratio (10:1) and 50% liquid medication, showing superior dissolution properties was selected to perform stability and in-vivo evaluations. Two CRF induced rat groups received F8 at two oral doses (50 and 100 mg/kg). Biochemical and nutritional parameters were compared with both normal and CRF control rats. Results showed improvement of renal function, oxidative stress, antioxidant and inflammatory biomarkers as well as increased appetite and body weight gain on administration of both doses of walnut liquisolid formulation, F8.


Subject(s)
Chemistry, Pharmaceutical/methods , Disease Models, Animal , Drug Carriers/administration & dosage , Juglans , Kidney Failure, Chronic/prevention & control , Plant Extracts/administration & dosage , Animals , Dose-Response Relationship, Drug , Drug Carriers/metabolism , Kidney Failure, Chronic/metabolism , Kidney Failure, Chronic/pathology , Male , Plant Extracts/isolation & purification , Plant Extracts/metabolism , Rats , Rats, Sprague-Dawley , Treatment Outcome
7.
Asian Pac J Trop Biomed ; 4(6): 456-62, 2014 Jun.
Article in English | MEDLINE | ID: mdl-25182947

ABSTRACT

OBJECTIVE: To study the antioxidant and anti-inflammatory activity of Butia capitata (B. capitata) leaf extracts along with phytochemical analysis of the proposed bioactive constituents. METHODS: Different successive extracts of B. capitata Becc. leaves were prepared with selective organic solvents and screened for their anti-inflammatory activities in tested animals and in-vitro antioxidant effect. An extensive phytochemical investigation of the bioactive extracts through paper chromatography, thin layer chromatography, column chromatography, gas-liquid chromatography (GLC), high pressure liquid chromatography and spectral analysis. GC-Mass, ultraviolet, hydrogen and carbon nuclear magnetic resonance, electron ionization-mass spectrometry, heteronuclear multiple bond correlation and heteronuclear multiple quantum correlation were carried out. RESULTS: Results showed that different extracts possess promising antioxidant effect and significant anti-inflammatory activity with variable degrees. The results of the phytochemical investigation of the bioactive extracts revealed the presence of volatile substances, lipoidal matter, α-tocopherol, free sugars, polysaccharides and flavonoidal compounds. CONCLUSIONS: B. capitata leaf extracts were shown to possess variable antioxidant effect, the most promising was methanol extract. Both polar and non polar extracts were proved to have anti-inflammatory activity, the non polar extract was superior in this respect. The bioactivity of the extracts was ascribed to the presence of flavonoids, sterols and α-tocopherol.

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