20 research outputs found
Piperine-Loaded Sodium Caseinate Nanoglobules Delivered Transdermally Through Microneedle Patch for Improved Bioavailability at Adipose Tissue
No full textDespite being a well-known anti-obesity chemical, piperine has only found limited therapeutic use because of its poor bioavailability at the site of action. In order to test this hypothesis, we placed piperine sodium caseinate nanoglobules (PSN) in microneedle patches (MNPs), which may enhance piperine transdermal delivery and absorption. Clove oil, sodium caseinate to make nanoglobules, and PEG 400 as a stabilizer were used in a nanoglobules process to create the PSN. The polydispersity index (0.256) and particle size (134.4 nm) of the developed PSN were both smaller, while their zeta potential (−44.4 mV) and encapsulation efficiency (90%–95%) were both greater. Compared to native piperine, the PSN increased solubility, bioaccessibility (6.5 times), and bioavailability (2.8 fold). Moreover, the PSN-loaded MNPs were created using the micro-molding (poly-dimethylsiloxane (PDMS) mold) approach. In both PBS buffer and porcine skin, the PSN-loaded MNPs were rapidly hydrolyzed, with 50% piperine release in less than 5 min. Also, the produced MNPs demonstrated improved bioavailability of piperine in the plasma (180 ng/mL) and
adipose (425 ng/mL) tissue of C57BL6 mice. In conclusion, the work offered a theoretical foundation for utilizing new PSN-loaded MNPs as a viable piperine delivery method for treating obesity
Characterization of polyphenols profile, antioxidant, and in vitro activities of Nigella sativa L. (black cumin) seed oleoresin
No full textThe medicinal importance of Nigella sativa L. (black seeds) is portrayed by their traditional use against various ailments. The oleoresins obtained from spices are generally semi-solid concentrated whole extracts containing essential oil. This study deals with the extraction of oleoresins from black seeds by solvent extraction method using ethanol 70% (v/v), methanol & acetonitrile, and its characterization. Total polyphenols and flavonoids were estimated while DPPH and Fe2+ ion chelation assay was done to assess the antioxidant activity. Solvent extraction by 70% ethanol, methanol, and acetonitrile yielded 36.8, 34.9, and 22.1% oleoresin, respectively. High polyphenol and moderate flavonoid content were found in all three samples.
70% ethanolic oleoresin showed the highest polyphenol content 67.05 ± 1.48 µg GAE/mg and better antioxidant activity with the lowest IC50 of 0.86 ± 0.22 mg/ml for DPPH radical scavenging. The oleoresin was further characterized by HPLC and GC–MS techniques detecting the presence of various volatile compounds, thymoquinone showed well-resolved peaks with the highest percent area in the chromatograms. GC–MS chromatograms also showed that 40–45% of oleoresin consisted of essential fatty acids. In vitro enzyme inhibition assays against three digestive enzymes, pancreatic lipase (PL), α-amylase, and α-glucosidase were also done to check the anti-obese activity of the oleoresins. Results showed 50–60% inhibition of PL and α-amylase, while 20–30% inhibition of α-glucosidase activity. The study suggested that the oleoresins obtained from the spice N. sativa have nutraceutical properties and can be used as therapeutics for the prevention or treatment of various lifestyle disorders
Anti-adipogenic activity of oleoresin from Nigella sativa L. seeds via modulation of PPAR-γ and C/EBP-α expression in 3T3-L1 adipocytes
No full textThe in vitro antiadipogenic properties of oleoresin obtained from Nigella sativa L.(black cumin) seeds was evaluated in
this study using 3T3-L1 cells as model cell line. Despite containing beneficial compounds like polyphenols, thymoquinone,
flavonoids, and unsaturated fatty acids known for their antioxidant properties, its role in obesity management is not fully
understood. We hypothesized that black cumin seed oleoresin treatment would inhibit differentiation of 3T3-L1 preadipo-
cytes by regulating expression of transcription factors, peroxisome proliferator-activated receptor γ (PPAR-γ) and CCAAT
enhancer binding protein α (C/EBP-α). Cells were cultured and differentiated for 8 days in Dulbecco modified Eagle media
(DMEM) containing 10% fetal bovine serum, both in the absence (control) and presence of 25, 50 and 100 μg/ml oleo-
resin. Oil red O staining after differentiation revealed a dose-dependent, substantial reduction in lipid droplet accumulation
in the differentiated adipocytes treated with oleoresin than differentiated control (DC) group. Molecular analysis revealed
downregulation in cellular induction of PPAR-γ, C/EBP-α and sterol regulatory element-binding protein 1 (SREBP1) tran-
scription factors. Furthermore, mRNA expression of particular target genes of these transcription factors— adiponectin,
adipocyte fatty acid binding protein (aP2), leptin and fatty acid synthase (FAS) was also dose dependently inhibited in
differentiated adipocytes by oleoresin treatment. The activation of adenosine monophosphate protein kinase (AMPK) and
phosphorylation of its substrate acetyl-CoA carboxylase (ACC) was detected by western blotting showing a significant
increase in their phosphorylated protein levels. Collectively, these findings suggest that black cumin seed oleoresin showed
anti-obesity effects by inhibiting lipid droplet formation and modulating molecular pathways involved in adipogenesis,
highlighting its potential as a natural therapeutic agent for obesity and related metabolic disorders
Boosting Curcumin Bioavailability: Unveiling the Potential of Sodium Caseinate Nanoparticle Microneedle Patches
No full textCurcumin is a well-known anti-obesity compound with limited clinical application due to its poor bioavailability at the target
site. Hence, we hypothesized that the curcumin sodium caseinate nanoparticles (CNC) loaded in microneedle patches (MNPs)
may improve curcumin bioavailability. The CNC were prepared with a microemulsion technique using clove oil, sodium casein-
ate to form nanoparticles and PEG 400 as a stabilizer and exhibited smaller particle size (100–250 nm) and polydispersity index
(0.201) with higher zeta potential (−45 mV) and entrapment efficiency (90%–95%). The CNC improved solubility, bioaccessibility
(7.2 fold) and bioavailability (2.6 fold) compared to native curcumin. Further, the CNC-loaded MNPs were developed by the
micro-molding and displayed a slow and controlled release of curcumin with superior bioavailability in the plasma (200 ng/mL)
and adipose (435 ng/mL) tissue of C57BL6 mice. Overall, the study advocates the novel CNC-loaded MNPs as a potential cur-
cumin delivery tool for treating obesity
Cassia auriculata Stem Bark Ameliorates the HFD+STZ-Induced Diabetes in both in vitro and in vivo Model
No full textBackground: The secondary metabolites from natural herbs are exploited to treat various human
ailments. The present study aimed to investigate the ameliorative effect of the methanolic extract
of Cassia auriculata (C. auriculata) stem-bark in both in vitro and in vivo mice model. Materials and
Methods: In vitro standard procedures were followed to determine the phytochemical profile.
High-fat-diet+STZ was administered to 6-weeks old mice to induce type-2-diabetes. Results: In
vitro study revealed that the highest total polyphenol and flavonoid contents with anti-oxidant
and anti-diabetic property was observed in the methanolic extract of C. auriculata stem-bark.
Type-2-diabetes rats showed significantly elevated fasting blood glucose levels with decreased
serum insulin level. Further, the oxidative stress in the serum and muscle as well as altered
activities of liver enzymes of carbohydrate metabolism in diabetic control mice compared to
normal control mice was observed. The histomorphology of liver and pancreas was deleteriously
altered in diabetic group mice. However, methanolic extract of C. auriculata stem-bark (200 mg/kg;
b.wt) and metformin (200 mg/kg; b.wt) treated diabetic mice did not show the above-mentioned
alterations suggesting its ameliorative effect in type-2-diabetes. Conclusion: The methanolic
extract of C. auriculata is potent enough to be employed as antidiabetic agent
Physicochemical characterization, polyphenols and flavonoids of different extracts from leaves of four varieties of tulsi (Ocimum sp.)
No full textLeaves from four varieties of tulsi (Camphor, Krishna, Lavanga and Vishnu) were collected, dried and extracts were prepared using different solvents such as acetone, water, dichloromethane, ethanol, hexane and methanol. The total solids content in dried leaf powder was highest in Lavanga and Camphor, while Krishna showed the least. The study revealed that various secondary metabolites such as polyphenols and flavonoids were present in tulsi leaf extracts. The HPLC profiling showed the presence of rosmarinic acid in all the extracts irrespective of the solvent extraction. The other polyphenols present in the tulsi leaf extracts were p-coumaric acid, isothymucin, proto-catechic acid and caffeic acid. The GC-MS analysis of the extracts revealed methyl eugenol in Krishna variety with all the solvents, Bornanone in Lavanga and Camphor varieties in all the solvent extracts and caryophyllene in Vishnu variety. The LC-MS/MS profile of Krishna variety of tulsi showed mallic acid, citric acid, rosmarinic acid and asiatic acid as major compounds. The LC-MS/MS profile of Camphor variety of tulsi showed major peaks of compounds like mallic acid, citric acid, gallic acid, chlorogenic acid and asiatic acid. The LC-MS/MS profile of Lavanga variety of tulsi showed mallic acid, citric acid, gallic acid, asiatic acid and sumaresinolic acid as major compounds. Similarly in case of Vishnu variety, mallic acid, citric acid, gallic acid, apigenin, and sumaresinolic acid were present in majority. These phytochemicals from natural plant sources are known to possess many health benefits and considered as safe. Hence, these bioactive compounds may be explored for possible application as nutraceuticals
The lasso peptide produced by Bacillus licheniformis MCC 2514 demonstrates efficacy in treating in-vivo Salmonella Typhimurium infection
No full textSalmonella, a significant pathogen transmitted through food, presents a substantial threat to public health. The
issue of antibiotic misuse is causing a quest for alternative replacements. An antimicrobial peptide, predicted as
lasso peptide 2514 (LP-2514), derived from the probiotic bacteria Bacillus licheniformis MCC 2514, has demon-
strated effectiveness against various foodborne pathogens including Salmonella. This study aims to assess the
efficacy of this peptide in vivo. Mice infected with Salmonella Typhimurium received daily oral administration of
LP-2514 (30 mg/kg/day) for 2 weeks until the symptoms subsided. After the treatment, biochemical and his-
topathological parameters were examined. LP-2514 treated mice demonstrated reduced infection, as evidenced
by a 5-fold decrease in aspartate aminotransferase concentration and a 10-fold decrease in alanine amino-
transferase concentration in plasma. Nitric oxide generation was decreased by 61.23 %, C-reactive protein by
75.9 %, and numerous antioxidant enzymes were elevated to suppress the infection. Increased expression of the
anti-inflammatory marker Interleukin-10 (IL-10) by 43-fold was observed in treated mice, while untreated mice
displayed elevated expression of pro-inflammatory cytokines indicating the severity of infection. Hence, LP-2514
successfully alleviated the disease symptoms caused by S. Typhimurium, thus exhibiting as a potential replace-
ment for antibiotics or food-grade preservatives
Oral bioavailability and amelioration of high fat diet induced obesity via AMPK/SIRT1 pathway using oleoresin from Nigella sativa L. seeds in C57BL/6 mice
No full textObjective: This study investigated the oral bioavailability and anti-obesity effects of oleoresin extracted from
seeds of Nigella sativa L. (NS), in high-fat-diet-fed C57BL/6 mice. NS is rich in polyphenols, flavonoids, and
unsaturated fatty acids; known for their anti-oxidant and anti-inflammatory activity. However, its role in
modulating lipid and energy metabolism remains unexplored.
Methods: Oleoresin was administered orally as well as intravenously (IV), and whole blood was collected at
predetermined time points. Thymoquinone (TQ) concentration in plasma was quantified using HPLC. For anti-
obesity assessment, 36 male C57BL/6 mice were divided into six groups, one normal diet and five HFD
groups. NS oleoresin was administered daily at doses 50, 100, and 200 mg/kg body weight (BW) for 8 weeks.
Results: Treatment groups showed significant reductions in body weight, blood glucose, LDL, triglycerides, total
cholesterol, and liver size, along with an increase in HDL levels. Gene expression analysis revealed that oleoresin
downregulated CCAAT/enhancer-binding protein alpha (C/EBPα) and peroxisome proliferator-activated recep-
tor gamma (PPARγ) expression, while slightly upregulating adenosine monophosphate-activated protein kinase
(AMPKα) gene in the higher dose group. Although the mitochondrial uncoupling protein (UCP1) was not
significantly altered, expression of sirtuin 1 and PGC-1, was enhanced indicating enhanced mitochondrial
biogenesis, insulin sensitivity and weight reduction. Histopathological examination showed reversal of hepatic
steatosis, as well as regular-sized adipocytes in dose-dependent treatment.
Conclusion: NS seed oleoresin supplementation may reduce the BW and lipid profile induced by HFD when given
in higher doses via activation of AMPK/SIRT1 pathway, potentially serving as a functional food therapeutic
against obesity and related complications
Nano-encapsulation of spice oleoresins using Hydroxypropyl β-cyclodextrin (HPBCD) and its bioavailability studies
No full textSpices are mostly used in traditional medicine since ancient times and they are used in the food for its flavour.
Oleoresins are the concentrated form of whole spices. There are many reports on the application of oleoresin, but
its consumption is limited due to its high pungency and insolubility. Thus, nano-encapsulation by Hydroxypropyl
beta-cyclodextrin (HPBCD) was attempted in this study to enhance the application of oleoresin into the food
system. HPBCD can form an inclusion complex with the spice oleoresin and helps in applying oleoresin in food
systems with improved solubility and bioavailability. In this study, the nano-encapsulation was done with
pepper, turmeric and chilli oleoresin, characterised for its physicochemical properties, and studied its in-vitro
drug release and in-vivo bioavailability. The particle size was found within 250 nm, and zeta potential was
shown above -30 mV, indicating stability. The encapsulation efficiency was shown above 85 % in all the
encapsulated oleoresin. The in-vitro drug release study showed that the highest percentage of the drug was
released in the intestine phase than stomach and colon. The percentage of the active component released in the
intestine was 92, 89 and 88 % by encapsulated pepper, turmeric and chilli oleoresin, respectively. The
bioavailability of these oleoresins was also improved upto 40–50 %. Therefore, the nano-encapsulated spice
oleoresin can be applicable in the food industry with its improvement in solubility and bioavailability
Evaluation of antioxidant properties, sensory profile of encapsulated spice oleoresins and molecular docking studies for the anti-depressive potential of their active components
No full textThis study aims to investigate the antioxidant potential, bioactive retention, and antidepressant effects of native
and encapsulated oleoresins from pepper, turmeric, and chili to enhance their therapeutic efficacy. The major
challenge in utilizing spice oleoresins is their low bioavailability and stability, which this study addresses
through nano-encapsulation using hydroxypropyl beta-cyclodextrin (HPBCD). The encapsulated oleoresins were
evaluated for their total polyphenol, flavonoid content, and antioxidant activity, revealing that turmeric oleo-
resin (TOR) demonstrated the highest antioxidant potential, followed by chili (COR) and pepper (POR). How-
ever, nano-encapsulation reduced antioxidant activity by 50–60 %, although it significantly improved the
stability and bioavailability of bioactives. Molecular docking studies further confirmed strong binding affinities
between bioactive compounds (piperine, curcumin, and capsaicin) and depression-related proteins, including
serotonin, Brain-Derived Neurotrophic Factor (BDNF), and Monoamine Oxidase (MAO), indicating potential
antidepressant effects. This study highlights the novelty of nano-encapsulation in enhancing the bioactivity and
therapeutic potential of spice oleoresins, offering promising insights for developing natural antidepressant formulations or functional foods to combat depression and neurodegenerative disorders
