Nanotechnology-based approaches applied to nutraceuticals.

Nutraceuticals and food industries are opening to a tremendously upcoming technology in the field of "Nano science". A new prospect has been defined by nanotechnology by conferring modified properties of nanomaterials and its application in the development of nanoformulations, nutritional supplements and food industry. Nanomaterials reveal exclusive properties because of their small size and high surface/volume ratio; thus, they have a complete application in nutraceuticals and food sector. In the existent review article, we obligate to present a comprehensive outline of the application of nanomaterials in development of advanced nano-based nutraceuticals with enhanced bioavailability, solubility, improved encapsulation efficiency, increased stability, sustained and targeted drug delivery, protection against degradation and microbial contamination and with improved pharmacological activity. It also highlights the importance of nanomaterials as nanosensors/nano-bio sensors for encapsulating peptides, antibodies, enzymes, etc. and in the food packaging industry and its future application. Thus, the review aims to focus on the benefits and new dimensions provided by nanomaterials and nanotechnology in health sectors by improving treatment strategies and quality of life.

Chemical constituents with antimicrobial and antioxidant activity from the aerial parts of Callistemon lanceolatus (Sm.) Sweet.

Callistemon lanceolatus (Sm.) Sweet grows all over the world and used to treat cough and bronchitis. The air-dried powder of the aerial parts was exhaustively extracted with methanol and the concentrated extract was adsorbed on silica gel for preparation of slurry. It was dried and subjected to silica gel column packed in petroleum ether. The column was eluted with organic solvents in order of increasing polarity to isolate 1-triacosanol (1), n-eicosanyl palmitate (2), n-heptadecanyl arachidate (3), n-tricosanyl palmitate, (4), 4-hydroxyphenethyl carbocerate (5), 4-hydroxyphenethyl gheddate (6), urs-12-en-3α-acetoxy-18ß-H-28-oic acid (7) and stigmast-5-en-3ß-ol-3ß-D-glucuronopyranoside (8). Among them, compound 5 and 6 were new fatty acid ester isolated from this plant. Compound 7 showed MIC 32 µg/mL against E. coli which was comparable to amoxicillin having same MIC 32 µg/mL. Compound 5 and 6 showed significant antioxidant activity by inhibiting DPPH due to the presence of phenolic groups.

Novel Piperine Derivatives with Antidiabetic Effect as PPAR-γ Agonists.

Piperine is an alkaloid responsible for the pungency of black pepper. In this study, piperine isolated from Piper nigrum L. was hydrolyzed under basic condition to obtain piperic acid and was used as precursor to carry out the synthesis of twenty piperine derivatives containing benzothiazole moiety. All the benzothiazole derivatives were evaluated for their antidiabetic potential by OGT test followed by assessment of active derivatives on STZ-induced diabetic model. It was observed that nine of twenty novel piperine analogues (5b, 6a-h), showed significantly higher antidiabetic activity in comparison with rosiglitazone (standard). Furthermore, these active derivatives were evaluated for their action as PPAR-γ agonists demonstrating their mechanism of action. The effects on body weight, lipid peroxidation, and hepatotoxicity after administration with active derivatives were also studied to further establish these derivatives as lead molecules for treatment of diabetes with lesser side-effects.

Ameliorative effects of Trichosanthes dioica Extract in suppressing inflammatory mediators and attenuating oxidative stress.

The present study aimed to investigate the anti-inflammatory activity of the ethanolic extract of the aerial parts of Trichosanthes dioica and its successive fractions. The effect on oxidative stress involved in the pathogenesis of inflammation was evaluated. The ethanolic extract and its successive fractions were administered at a dose of 150 and 300 mg/kg b. w. for testing their anti-inflammatory activity by a carrageenan-induced edema model. The results showed that the ethyl acetate fraction exhibited significant potency against inflammation. Pertaining to mechanistic insight, the anti-inflammatory effect might be attributed to the attenuation in tumor necrosis factor-α level (ELISA assay) and reduced expression of cyclooxygenase-2 and nuclear transcription factor-κB (immunohistochemistry). The alleviation in oxidative stress has been pertinent to the elevation in the activities of antioxidant enzymes (superoxide dismutase, catalase, and glutathione) by active fractions. Furthermore, the ulcerogenic effect was insignificant even at a three times higher dose. Finally, it was concluded that the ethyl acetate fraction which showed significant biological potential against inflammation and oxidative stress could be viewed as a source of effective treatment.

Design and Synthesis of Butenolide-based Novel Benzyl Pyrrolones: Their TNF-α based Molecular Docking with In vivo and In vitro Anti-inflammatory Activity.

A focused library of novel benzyl pyrrolones has been synthesized and their in silico molecular docking studies carried out against TNF-α target. Among all the docked molecules, compound 3f showed best glide score of -6.89. All the synthesized compounds were evaluated for in vivo anti-inflammatory activity by carrageenan-induced paw edema model. Compounds showing significant anti-inflammatory activity were further tested for their in vitro TNF α expression. Compounds 3b and 2b were found to show significant inhibition of 76.22% and 71.47%, respectively after 5 h in comparison with standard drug indomethacin, which showed 80.98% inhibition of inflammation. Compounds 3b and 2b also suppressed TNF α level by 65.03% and 60.90% as compared indomethacin, which showed 68.84% of inhibition. Compound 3b showed significant analgesic activity of 60.04%, and its activity was comparable with indomethacin (64.04%). Compounds 3b and 2b were also tested for their effect on protein expression of COX-2 and NF-κB in the liver tissues. Compounds 3b and 2b were further evaluated for their gastric risk and lipid peroxidation action and showed superior GI safety along with reduction of LPO as compared to indomethacin. Hepatotoxicity study showed that these two compounds did not cause any damage to liver.

Attenuation of inflammatory mediators, oxidative stress and toxic risk evaluation of Aporosa lindleyana Baill bark extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditionally, Aporosa lindleyana Baill. has been used against various ailments viz. jaundice, fever, headache, seminal loss and insanity. The present study aims to evaluate the anti-inflammatory and anti-oxidant activity of the ethanolic extract of Aporosa lindleyana Baill. bark and its fractions. METHOD: The anti-inflammatory activity of ethanolic extract of Aporosa lindleyana Baill. bark and its various fractions at doses of 200mg/kg and 300mg/kg b.w. has been carried out by a carrageenan induced hind paw edema method. To establish the probable mechanism of action, TNF-α and NO levels have been estimated by an ELISA method and the effect of active fraction on COX-2 and NF-κB expressions has been evaluated. The effect on the levels of anti-oxidative enzymes (CAT, SOD & GPX) by the ethanolic extract and its fractions has also been investigated. Furthermore, peptic ulcer and hepatotoxic risk evaluation has also been carried out at three times higher dose than that used in inflammatory in vivo model. RESULTS: Among the extract and its various fractions tested for anti-inflammatory activity, the methanolic fraction at a dose of 300mg/kg showed significant inhibition in paw edema by 73% as compared to Indomethacin which showed 77% inhibition after 5h. The same dose of methanolic fraction also caused significant reduction in TNF-α (59.27%) and NO concentration (57.12%) while Indomethacin showed inhibition of 63.91% and 60.12%. The active methanolic fraction was also found to inhibit the expression of NF-κB and COX-2 induced by carrageenan. Histological studies showed that the ethanolic extract and its fractions did not cause any damage to the stomach as well as to liver. Moreover, the active fractions also decreased lipid peroxidation levels and increased the antioxidant enzyme activities (SOD, CAT, GPX). CONCLUSION: The results of present study demonstrated that significant anti-inflammatory activity of methanolic fraction of Aporosa lindleyana may be attributed to the modulation of pro-inflammatory mediators. Same fraction was also found to be effective against oxidative stress as it was found to elevate the levels of anti-oxidative enzymes. It can therefore be concluded that the methanolic fraction could be explored as a disease modifying agent against inflammation and oxidative stress.

Trapa natans L. root extract suppresses hyperglycemic and hepatotoxic effects in STZ-induced diabetic rat model.

ETHNOPHARMACOLOGICAL RELEVANCE: Trapa natans L. has a folkloric reputation as nutrient, appetizer and astringent. Its utility as antidiabetic, anticancer, diuretic, aphrodisiac, antidiarrhoeal and in many other maladies is well reported in the literature. Therefore, the present study has been carried out to study the antihyperglycemic effect of root extract of Trapa natans L. and its various fractions. Furthermore, hepatotoxic effects and lipid peroxidation risks have also been evaluated. METHODS: The ethanol extract and its successive fractions obtained from roots of Trapa natans have been administered in sucrose loaded and STZ- induced diabetic Wistar rats at doses of 50, 100 and 200mg/kg b.w. Glibenclamide was used as positive control. The evaluation of protective effects of extract as well as fractions against hepatotoxicity and lipid peroxidation at 600mg/kg b.w. has also been carried out. RESULTS: The methanol fraction emerged as the most potent antihyperglycemic fraction. It has also been found that the ethanolic extract as well as its fractions did not cause any lipid peroxidation and hepatotoxicity risks. CONCLUSION: It can be concluded that the intense investigations of the methanol fraction obtained from Trapa natans root extract can be done to provide an alternative natural therapy for hyperglycemia.

Anti-inflammatory and anti-nociceptive activities of two new triterpenoids from Adiantum capillus-veneris Linn.

Two new triterpenoids characterised as 30-normethyl fernen-22-one (capillirone, 1) and hopan-3ß-ol (capillirol B, 2), along with two known triterpenoids, 4-α-hydroxyfilican-3-one and 3-ß,4-α-dihydroxyfilicane, have been isolated from the ethanolic extract of the fronds of Adiantum capillus-veneris Linn. (Adiantaceae). Compounds 1 and 3 showed significant anti-inflammatory activity with 33.07% (p < 0.01) and 42.30% (p < 0.001) inhibition as compared to indomethacin that exhibited 60.00% (p < 0.001) inhibition after 3 h in the carrageenan-induced hind paw oedema method. Compound 3 showed potent anti-nociceptive activity with 42.37% inhibition as compared to indomethacin that showed 45.34% inhibition in the writhing test.

New flavones with antidiabetic activity from Callistemon lanceolatus DC.

Phytochemical investigation of the aerial parts of Callistemon lanceolatus DC (Myrtaceae) led to the isolation of two new flavones characterized as 5,7-dihydroxy-6,8-dimethyl- 4' -methoxy flavone (1) and 8-(2-hydroxypropan-2-yl)-5-hydroxy-7-methoxy-6-methyl-4'-methoxy flavone (2) along with the seven known phytoconstituents. The structures of new compounds have been established on the basis of chemical and spectral studies and known compounds were compared with the published literature data. The isolated flavones exhibited blood glucose lowering effect in streptozotocin induced diabetic rats.

Anti-inflammatory and anti-nociceptive activities of Platanus orientalis Linn. and its ulcerogenic risk evaluation.

ETHNOPHARMACOLOGICAL RELEVANCE: Leaves of Platanus orientalis Linn. are used in folk medicine as a wound-healer and ophthalmologic agent. Phytol derivatives from the leaves of plane-tree show anti-ulcer activity. Its analgesic and anti-inflammatory effects for knee pain were known to Persian scientists and hakims. MATERIALS AND METHODS: The ethanolic extract of Platanus orientalis Linn. and its various fractions were given at a dose of 100mg/kg po and 200mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 200mg/kg po. Gastric ulceration studies have been further carried out to study the ulcerogenic risk evaluation of the ethanolic extract and its various fractions at a dose of 600mg/kg body weight. RESULTS: Among the tested fractions, chloroform fraction exhibited better inhibition (68.33%) at 200mg/kg po dosage when compared to the standard drug Ibuprofen (66.66%) after 3h in the carrageenan induced hind paw edema. The ethanolic extract and all its fractions especially the chloroform (p<0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug i.e. Ibuprofen. The histopathological study of ethanolic extract and its fractions revealed that none of them cause ulcer. CONCLUSION: The present study indicates that Platanus orientalis Linn. has significant anti-inflammatory and analgesic effect.

Synthesis and biological evaluation of some novel sulfamoylphenyl-pyridazinone as anti-inflammatory agents (Part-II * ).

Seven novel 6-aryl-2-(p-sulfamoylphenyl)-4,5-dihydropyridazin-3(2H)-ones (2a-g) were synthesized by the condensation of appropriate aroylpropionic acid and 4-hydrazinobenzenesulfonamide hydrochloride in ethanol. Structure of all compounds have been elucidated by elemental analysis, IR, (1)H NMR, (13)C NMR, DEPT and MS spectrscopy. These compounds were tested for their anti-inflammatory activity in carrageenan-induced rat paw edema model. Compound 2b exhibited anti-inflammatory activity comparable to that of celecoxib (at 5 h). Two other compounds 2d and 2g showed promising anti-inflammatory activity (edema reduction more than 80% at 5 h). These compounds (2b, 2d and 2g) did not produce any ulceration in gastric region.

Anti-inflammatory and anti-nociceptive activities of ethanolic extract and its various fractions from Adiantum capillus veneris Linn.

AIM OF THE STUDY: To investigate the anti-inflammatory and anti-nociceptive activities of the crude ethanolic extract of Adiantum capillus veneris Linn. (Adiantaceae) and its various fractions. MATERIALS AND METHODS: The ethanolic extract and its fractions were given at a dose of 200 mg/kg po and 300 mg/kg po for testing their anti-inflammatory activity by carrageenan induced hind paw edema. The analgesic activity of the ethanolic extract and its fractions has been carried out by tail-flick method and writhing test at a dosage of 300 mg/kg po. Gastric ulceration studies have been further carried out to study the antiulcer effect of the ethanolic extract and its various fractions at dose of 900 mg/kg body weight. RESULTS: Amongst the tested fractions, the ethyl acetate fraction exhibited better inhibition (67.27%) at 300 mg/kg po dosage when compared to the standard drug Indomethacin (63.63%) after 3h in the carrageenan induced hind paw edema. The anti-inflammatory activity of the ethanolic extract and its various fractions appear to be related to the inhibition of NO release, and the decreasing TNF-α level. The ethanolic extract and all its fractions especially the ethyl acetate (p<0.01) showed significant analgesic activity with insignificant ulceration as compared to the standard drug, i.e. ibuprofen. The histopathological study of ethanolic extract and its fractions reveals that none of them cause ulcer. CONCLUSION: The present study indicates that Adiantum capillus veneris Linn. has significant anti-inflammatory and analgesic effect.

Antiinflammatory evaluation of alcoholic extract of galls of Quercus infectoria.

Galls of Quercus infectoria Olivier (Fagaceae) possess pleiotropic therapeutic activities, with particular efficacy against inflammatory diseases. The present study was undertaken to evaluate the effect of alcoholic extract of Q. infectoria galls on various in vivo and in vitro experimental models of inflammation. Oral administration of gall extract significantly inhibited carrageenan, histamine, serotonin and prostaglandin E2 (PGE2) induced paw oedemas, while topical application of gall extract inhibited phorbol-12-myristate-13-acetate (PMA) induced ear inflammation. The extract also inhibited various functions of macrophages and neutrophils relevant to the inflammatory response. In vitro exposure of rat peritoneal macrophages to gall extract ameliorated lipopolysaccharide (LPS) stimulated PGE2 and nitric oxide (NO) production and PMA stimulated superoxide (O2*-) production in a dose dependent manner. Gall extract also scavenged NO and O2*-. Probing into mechanism of NO inhibition in macrophages revealed gall extract to ameliorate the induction of inducible NO synthase (iNOS), respectively without any inhibitory effect on its catalytic activities even at higher concentrations. Gall extract also significantly inhibited formyl-Met-Leu-Phe (fMLP) stimulated degranulation in neutrophils. These results suggest that alcoholic extract of galls of Q. infectoria exerts in vivo antiinflammatory activity after oral or topical administration and also has the ability to prevent the production of some inflammatory mediators.

Terminoside A, a new triterpene glycoside from the bark of Terminalia arjuna inhibits nitric oxide production in murine macrophages.

Terminoside A (1), a new oleanane-type triterpene was isolated from the acetone fraction of the ethanolic extract of stem bark of Terminalia arjuna. The structure was established as olean-1alpha,3beta,22beta-triol-12-en-28-oic acid-3beta-D-glucopyranoside. On the basis of spectral data and chemical reactions, terminoside A, potently inhibited nitric oxide (NO) production and decreased inducible nitric oxide synthase (iNOS) levels in lipopolysaccharide-stimulated macrophages.