This research was to determine nutritional composition, essential and toxic elemental content, and major phenolic acid with antioxidant activity in Kadsura coccinea fruit. The results indicated that Kadsura coccinea fruit exhibited the high contents of total protein, total fat, ash and essential elements such as calcium (Ca), ferrum (Fe) and phosphorus (P). The levels of four common toxic elements, i.e. cadmium (Cd), mercury (Hg), arsenic (As) and lead (Pb), were lower than legal limits. By high-performance liquid chromatography (HPLC) analysis, gallic acid was identified as major phenolic acid in peel and pulp tissues. Its contents were no significant difference in both tissues. In comparison with two commercial antioxidants, the major phenolic acid extracted from Kadsura coccinea exhibited stronger 1,1-diphenyl-2-picrylhydrazyl radical-scavenging activity and reducing power. Kadsura coccinea fruit is a good source of nutrition and natural antioxidant. It is worthwhile to popularize this exotic fruit around the world.
The aim of this study is to determine the total phenolic content and primary antioxidant activity of methanolic and ethanolic extracts of four aromatic plants’ leaves namely knotweed (Polygonum minus), curry (Murraya koenigii), kaffir lime (Citrus hysrix) and fragrant screwpine (Pandanus odurus). Total phenolic content (TPC) assay using Folin-Ciocalteu method was used to assess the presence and level of phenolic compounds in each sample. The present study showed that both methanolic and ethanolic extracts of P. minus had the highest TPC and followed by M. koenigii, C. hystrix and P. odorus. Primary antioxidant activity in terms of free radical scavenging activities of both methanolic and ethanolic extracts was then measured by 2, 2, diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity assay. The lowest EC50 values based on the DPPH. radical scavenging activity were shown by P. minus extracts as compared to the other samples. For both ethanolic and methanolic extracts, the correlations between TPC and EC50 based on the DPPH. radical scavenging activity assay were negative and weak. Relatively, the present results suggest that of the four aromaticplants, P. minus and M. koenigii have shown potential as sources of natural antioxidants.
This study was undertaken to evaluate the potential of fruit waste materials as source of natural antioxidant. The fruit peels including mango, guava and papaya peel were used in this study. The total phenolic content (TPC) was determined by Folin-Ciocalteu assay while antioxidant activities were determined by using ferric reducing antioxidant power (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging, ferric thiocynate (FTC) and thiobarbituric acid (TBA) assays. These antioxidant activities were compared to synthetic antioxidants, BHA/BHT combination and ascorbic acid. The results demonstrated that TPC ranged from 3.23 to 15.84 g GAE/100 g extract. Mango peels extract exhibited highest TPC compared to guava peel and papaya peel extract. In the FRAP assay, mango peel extract at 200 ppm, guava peel extract at 400 ppm and papaya peel extract at 1200 ppm, exhibited reducing power comparable to the permissible amount of BHA/BHT at 200 ppm. At concentration of 250 μg/ml, the DPPH radical scavenging activity of extracts and standards decreased significantly in the order of mango peel extract > guava peel extract > BHA/BHT > ascorbic acid > papaya peel extract. For the FTC assay, the antioxidant activity of mango peel extract was significantly higher than ascorbic acid, guava peel and papaya peel extract but lower than BHA/BHT while in the TBA assay, percentage inhibition of BHA/BHT and ascorbic acid were found to be higher than fruit peel extracts. The quantitative analysis for flavonoids showed the presence of catechin, epicatechin and kaempferol in the peel extracts.
Dihydroorotate dehydrogenase (DHODH) is the key enzyme in de novo biosynthesis of pyrimidine in both prokaryotes and eukaryotes. The de novo pathway of pyrimidine biosynthesis is essential in cancer cells proliferation. Leflunomide is an approved DHODH inhibitor that has been widely used for the treatment of arthritis. Similarly, brequinar sodium is another DHODH inhibitor that showed anti-tumour effect in MC38 colon carcinoma cells when used in combination with fluorouracil. Despite the potential role of DHODH inhibitors in cancer therapy, their mechanisms of action remain obscure and await further elucidation. Here, we evaluated the effect of DHODH inhibitors on the production of ATP and ROS in sensitive and non-sensitive breast cancer cells. Subsequently, the effects of DHODH inhibitors on cell cycle as well as on signalling molecules such as p53, p65 and STAT6 were evaluated in sensitive T-47D and non-sensitive MDAMB-436 cells. The correlations between DHODH protein expression, proliferation speed and sensitivity to DHODH inhibitors were also investigated in a panel of cancer cell lines. DHODH inhibitors-sensitive T-47D and MDAMB-231 cells appeared to preserve ROS production closely to endogenous ROS level whereas the opposite was observed in non-sensitive MDAMB-436 and W3.006 cells. In addition, we observed approximately 90% of intracellular ATP depletion in highly sensitive T-47D and MDAMB-231 cells compared to non-sensitive MDAMB-436 cells. There was significant over-expression of p53, p65 and STAT6 signalling molecules in sensitive cells which may be involved in mediating the S-phase arrest in cell cycle progression. The current study suggests that DHODH inhibitors are most effective in cells that express high levels of DHODH enzyme. The inhibition of cell proliferation by these inhibitors appears to be accompanied by ROS production as well as ATP depletion. The increase in expression of signalling molecules observed may be due to pyrimidine depletion which subsequently leads to cell cycle arrest at S-phase.
This study aims to determine the antioxidant capacities (AC) and antidiabetic properties of
phenolic extracts (free and bound) from white Tambun pomelo peels, kaffir lime peels, lime
peels and calamansi peels. AC, total phenolic content (TPC) and antidiabetic properties of
selected citrus peels extracts were determined spectrophotometrically using 2,2-Diphenyl-1-
picrylhydrazyl free radical (DPPH) scavenging, ferric-reducing antioxidant power (FRAP),
Folin-Ciocalteu (FC) and α-amylase and α-glucosidase inhibition assay, respectively. This
study found that the methanolic extract of kaffir lime showed the best AC with the lowest
IC50 value of DPPH radical (7.51 ± 0.50 mg/ml) and highest FRAP value [369.48 ± 20.15
mM Fe (II) E/g DW]. TPC of free phenolic extracts of all citrus peels were significantly (p<
0.05) higher compared to the bound phenolic extracts with extract of calamansi showed the
highest TPC. Free- and bound phenolic extract of calamansi also had the highest α-amylase
inhibition activity (61.79 ± 4.13%; 45.30 ± 5.35%) respectively. The highest inhibitory effect in
α-glucosidase inhibition assay of free- and bound phenolic extracts were white Tambun pomelo
(41.06 ± 10.94%) and calamansi (43.99 ± 22.03%) respectively. Hence, the citrus peels could
be furthered study for their potential in management and/or prevention of diabetes.
Propolis contains high concentrations of polyphenols, flavonoids, tannins, ascorbic acid, and reducing sugars and proteins. Malaysian Propolis (MP) has been reported to exhibit high 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity and ferric reducing antioxidant power (FRAP) values. Herein, we report the antioxidant properties and cardioprotective properties of MP in isoproterenol- (ISO-) induced myocardial infarction in rats. Male Wistar rats (n = 32) were pretreated orally with an ethanol extract of MP (100 mg/kg/day) for 30 consecutive days. Subcutaneous injection of ISO (85 mg/kg in saline) for two consecutive days caused a significant increase in serum cardiac marker enzymes and cardiac troponin I levels and altered serum lipid profiles. In addition significantly increased lipid peroxides and decreased activities of cellular antioxidant defense enzymes were observed in the myocardium. However, pretreatment of ischemic rats with MP ameliorated the biochemical parameters, indicating the protective effect of MP against ISO-induced ischemia in rats. Histopathological findings obtained for the myocardium further confirmed the biochemical findings. It is concluded that MP exhibits cardioprotective activity against ISO-induced oxidative stress through its direct cytotoxic radical-scavenging activities. It is also plausible that MP contributed to endogenous antioxidant enzyme activity via inhibition of lipid peroxidation.
Introduction: There are numerous studies on the therapeutic properties of Artocarpus heterophyllus. However, stud- ies on the aqueous extraction of A. heterophyllus leaves are limited. This present study was conducted to optimize the extraction conditions of A. heterophyllus leaves to yield the highest phenolic, flavonoids and antioxidant contents. Methods: Response surface methodology (RSM) was employed to obtain a higher phenolic extraction parameter(s) of A. heterophyllus leaves using Central Composite Design (CCD). The antioxidant activity was then determined via ABTS (2,29-azinobis (3 ethylbenzothiazoline-6-sulfonic acid)) and DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay and analysis of the individual phenolics was performed by high performance liquid chromatography (HPLC). Results: The optimum extraction conditions with higher phenolics content and antioxidant activity was achieved at 81°C, 100 min and 40 mL/g sample with a good desirability value of 0.87. Under these optimized parameters, total phenolics and flavonoids were 174.48 ± 4.05 mg GAE/g sample and 21.44 ± 0.05 mg RE/g sample, respectively. Meanwhile, antioxidant activity via ABTS and DPPH assays were 90.88% ± 0.09 and 87.22% ± 0.62, respectively. Finally, under optimal extraction conditions revealed 4 compounds identified as chlorogenic acid, quercetin, rutin and kaempferol. Conclusion: The optimisation are promising to improve phenolic yield and antioxidant activity in A. heterophyllus leaves. It also proved that A. heterophyllus leaves can be used as an alternative natural antioxidant especially in medicinal applications since all identified compound possess significant biological activities for human health.
The present work investigated the impact of several juice extraction methods (blender,
centrifugal juicer, and slow juicer) and thermal pasteurisation (72°C, 15 s) on the different
properties [physicochemical, polyphenol oxidase (PPO) activity, and functional] of
Clinacanthus nutans juice mix during storage (28 d, 4°C). Regardless of juicing technique, all
juices had similar colour and antioxidants [tested using 2,2-diphenyl-1-picrylhydrazyl
(DPPH) and ferric reducing antioxidant power (FRAP) methods]. The juices also had similar
PPO activity and sensory acceptance in terms of colour, aroma, flavour, mouthfeel, and
overall acceptability. The blender yielded juice with higher pH, soluble solids, and relative
viscosity than other methods. The slow juicer was the best at retaining ascorbic acid (39.33 ±
3.06 mg/100 mL), while the blender was best at retaining phenolic compounds (11.82 ± 0.12
mg gallic acid equivalents/100 mL) and chlorophyll (6.95 ± 0.31 μg/mL). Pasteurisation
negatively affected the colour, functional properties, and sensory characteristics (colour,
aroma, flavour, and mouthfeel) of the juice.
The growing demand for high value aromatic herb Polygonum minus-based products have increased in recent years, for its antioxidant, anticancer, antimicrobial, and anti-inflammatory potentials. Although few reports have indicated the chemical profiles and antioxidative effects of Polygonum minus, no study has been conducted to assess the benefits of micro-environmental manipulation (different shading levels) on the growth, leaf gas exchange and secondary metabolites in Polygonum minus. Therefore, two shading levels (50%:T2 and 70%:T3) and one absolute control (0%:T1) were studied under eight weeks and 16 weeks of exposures on Polygonum minus after two weeks. It was found that P. minus under T2 obtained the highest photosynthesis rate (14.892 µmol CO2 m-2 s-1), followed by T3 = T1. The increase in photosynthesis rate was contributed by the enhancement of the leaf pigments content (chlorophyll a and chlorophyll b). This was shown by the positive significant correlations observed between photosynthesis rate with chlorophyll a (r2 = 0.536; p ≤ 0.05) and chlorophyll b (r2 = 0.540; p ≤ 0.05). As the shading levels and time interval increased, the production of total anthocyanin content (TAC) and antioxidant properties of Ferric Reducing Antioxidant Power (FRAP) and 2,2-Diphenyl-1-picrylhydrazyl (DPPH) also increased. The total phenolic content (TPC) and total flavonoid content (TFC) were also significantly enhanced under T2 and T3. The current study suggested that P.minus induce the production of more leaf pigments and secondary metabolites as their special adaptation mechanism under low light condition. Although the biomass was affected under low light, the purpose of conducting the study to boost the bioactive properties in Polygonum minus has been fulfilled by 50% shading under 16 weeks' exposure.
Diosgenin encapsulated PCL-Pluronic nanoparticles (PCL-F68-D-NPs) were developed using the nanoprecipitation method to improve performance in brain cancer (glioblastoma) therapy. The nanoparticles were characterized by dynamic light scattering (DLS)/Zeta potential, Fourier-transform infrared (FTIR) spectra, X-ray diffraction (XRD), Field Emission Scanning Electron Microscopy (FESEM), and Transmission electron microscopy (TEM). The encapsulation efficiency, loading efficiency, and yield were calculated. The in vitro release rate was determined, and the kinetic model of diosgenin release was plotted and ascertained. The cytotoxicity was checked by MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl tetrazolium bromide)assay against U87-MG cells (glioblastoma cell lines). The obtained nanoparticles demonstrated good size distribution, stability, morphology, chemical, and mechanical properties. The nanoparticles also possessed high encapsulation efficiency, loading efficiency, and yield. The release rate of Diosgenin was shown in a sustained manner. The in vitro cytotoxicity of PCL-F68-D-NPs showed higher toxicity against U87-MG cells than free Diosgenin.
This study investigates the characteristics of an antioxidant cream made from the methanol extract of Piper sarmentosum leaves, which is locally known as the wild betel or pokok kadok in Malay. The secondary metabolites of the leaves were subjected to phytochemical tests to detect the presence of natural compounds. Antioxidant activity was described by its total phenolic content (TPC) and total flavonoid content (TFC), which was assessed by 2,2-Diphenyl-1-picrylhydrazyl (DPPH) assay. A phase diagram was constructed to find a possible region to formulate an antioxidant cream. In phytochemical screening, the methanolic extract showed positive presence of alkaloids, flavonoids, steroids, terpenoids and tannins. In quantitative analysis of antioxidative components, besides having significantly higher TFC content compared with quercetin (P
The antioxidant activity of two synthesized coumarins namely, N-(4,7-dioxo-2- phenyl-1,3-oxazepin-3(2H,4H,7H)-yl)-2-(2-oxo-2H-chromen-4-yloxy)acetamide 5 and N-(4-oxo-2-phenylthiazolidin-3-yl)-2-(2-oxo-2H-chromen-4-yloxy)acetamide 6 were studied with the DPPH, hydrogen peroxide and nitric oxide radical methods and compared with the known antioxidant ascorbic acid. Compounds 5 and 6 were synthesized in a good yield from the addition reaction of maleic anhydride or mercaptoacetic acid to compound 4, namely N'-benzylidene-2-(2-oxo-2H-chromen-4-yloxy)acetohydrazide. Compound 4 was synthesized by the condensation of compound 3, namely 2-(2-oxo-2H-chromen-4-yloxy) acetohydrazide, with benzaldehyde. Compound 3, however, was synthesized from the addition of hydrazine to compound 2, namely ethyl 2-(2-oxo-2H-chromen-4-yloxy)acetate, which was synthesized from the reaction of ethyl bromoacetate with 4-hydroxycoumarin 1. Structures for the synthesized coumarins 2-6 are proposed on the basis of spectroscopic evidence.
In the present study, in vitro antioxidant, free radical scavenging capacity, and hepatoprotective activity of methanol extracts from Polyalthia longifolia and Cassia spectabilis were evaluated using established in vitro models such as ferric-reducing antioxidant power (FRAP), 2,2-diphenyl-1-picryl-hydrazyl (DPPH(•)), hydroxyl radical (OH(•)), nitric oxide radical (NO(•)) scavenging, metal chelating, and antilipidperoxidation activities. Interestingly, all the extracts showed considerable in vitro antioxidant and free radical scavenging activities in a dose-dependent manner when compared to the standard antioxidant which verified the presence of strong antioxidant compound in leaf extracts tested. Phenolic and flavonoid content of these extracts is significantly correlated with antioxidant capacity. Since P. longifolia extract was exhibited better in vitro antioxidant activities, it was subjected for in vivo hepatoprotective activity in paracetamol-intoxicated mice. Therapy of P. longifolia showed the liver protective effect on biochemical and histopathological alterations. Moreover, histological studies also supported the biochemical finding, that is, the maximum improvement in the histoarchitecture of the liver. Results revealed that P. longifolia leaf extract could protect the liver against paracetamol-induced oxidative damage by possibly increasing the antioxidant protection mechanism in mice. Our findings indicated that P. longifolia and C. spectabilis have potential as good sources of natural antioxidant/antiaging compounds.
Water extract of Lentinus squarrosulus mycelia was analysed for nutritional content, antioxidant capacity, and antiulcer ability. The extract contains high protein (57.6 g/100 g) and low total fat (0.5 g/100 g) and is rich in magnesium (0.4 g/100 g), potassium (3.8 g/100 g), vitamins B(1) (1.42 mg/100 g), and B(3) (194.29 mg/100 g) with total phenolic content of 39.16 mg/100 g. The cupric reducing antioxidant capacity and 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity of the extract were A(450) of 0.20 ± 0.03 at 0.5 mg/ml and IC(50) of 14.29 mg/ml, respectively. Oral feeding of L. squarrosulus extract (250 mg/kg) offered significant gastric mucosal protection of Sprague-Dawley rats compared to cimetidine (50 mg/kg). The ulcer healing rate of ulcerated rats after 24, 48, and 72 hours of treatment was 82%, 90%, and 100%, respectively. The IL-1β level in the serum and the NF-κB level in the tissues indicate that the healing potential was associated with attenuation of proinflammatory cytokines.
Chitosan (beta-1, 4-D-glucosamine) is a deacetylated form of chitin with excellent biological properties in wound management. The natural properties of chitosan have the physical and chemical limitations to be widely used in biomedical fields. The improvement of the physical and chemical properties of chitosan with some additional chemicals will alter its biocompatibility. Therefore, the biological attribute of the modified chitosan must be evaluated. In this study, the cytotoxicity of oligo-chitosan (OC) and N, O- carboxymethyl-chitosan (NO-CMC) derivatives (O-C 1%, O-C 5%, NO-CMC 1% and NO-CMC 5%) was evaluated using primary normal human epidermal keratinocyte (pNHEK) cultures as an in vitro toxicology model at standardized cell passages (fourth passages). 3-[4, 5-dimethyl-2-thiazolyl]-2, 5-diphenyl tetrazolium bromide (MTT) was used as a cell viability assay. The O-C 1% is one of the most compatible chitosan derivatives because it steadily sustained >70% of viable cells until 72 hr post-treatment. This was followed by O-C 5%, NO-CMC 5% and NO-CMC 1%. Therefore, oligo-chitosan had the ideal properties of a biocompatible material compared to N, O- carboxymethyl-chitosan in this study.
The bark of Litsea costalis affords two new compounds named 4,4'-diallyl-5,5'-dimethoxy-[1,1'-biphennyl]-2,2'-diol, biseugenol A (1) and 2,2'-oxybis (4-allyl-1-methoxybenzene), biseugenol B (2) along with two known compounds (3-4), namely 5-methoxy-2-Hydroxy Benzaldehyde (3), and (E)-4-styrylphenol (4). The structures of 1 and 2 were determined using 1D and 2D NMR data. Also, the IR and NMR data were combined with quantum chemical calculations in the DFT approach using the hybrid B3LYP exchange-correlation function to confirm the structures of the compounds. Compounds showed fairly potent anticancer activity against cell lines and antioxidant (DPPH).
The purpose of this study was to evaluate fermentation of milk in the presence of green tea (Camellia sinensis) with respect to changes in antioxidant activity, phenolic compounds and the growth of lactic acid bacteria. Pasteurized full fat cow's milk and starter culture were incubated at 41 °C in the presence of two different types of green tea extracts. The yogurts formed were refrigerated (4 °C) for further analysis. The total phenolic content was highest (p
Malignant melanoma continues to be a fatal disease for which novel and long-term curative breakthroughs are desired. One such innovative idea would be to assess combination therapeutic treatments - by way of combining two potentially effective and very different therapy. Previously, we have shown that DHODH inhibitors, A771726 and Brequinar sodium (BQR) induced cell growth impairment in melanoma cells. Similar results were seen with DHODH RNA interference (shRNA). In the present study, we showed that combination of BQR with doxorubicin resulted in synergistic and additive cell growth inhibition in these cells. In addition, in vivo studies with this combination of drugs demonstrated an almost 90% tumor regression in nude mice bearing melanoma tumors. Cell cycle regulatory proteins, cyclin B1 and its binding partner pcdc-2 and p21 were significantly downregulated and upregulated respectively following the combined treatment. Given that we have observed synergistic effects with BQR and doxorubicin, both in vitro and in vivo, these drugs potentially represent a new combination in the targeted therapy of melanoma.
Biphenyl-based compounds are clinically important for the treatments of hypertension and inflammatory, while many more are under development for pharmaceutical uses. In the present study, a series of 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl benzoates, 2(a-q), and 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl pyridinecarboxylate, 2(r-s) were synthesized by reacting 1-([1,1'-biphenyl]-4-yl)-2-bromoethan-1-one with various carboxylic acids using potassium carbonate in dimethylformamide at ambient temperature. Single-crystal X-ray diffraction studies revealed a more closely packed crystal structure can be produced by introduction of biphenyl moiety. Five of the compounds among the reported series exhibited significant anti-tyrosinase activities, in which 2p, 2r and 2s displayed good inhibitions which are comparable to standard inhibitor kojic acid at concentrations of 100 and 250 μg/mL. The inhibitory effects of these active compounds were further confirmed by computational molecular docking studies and the results revealed the primary binding site is active-site entrance instead of inner copper binding site which acted as the secondary binding site.
A new series of urea/thiourea derivatives have been efficiently synthesized from the reaction of L-3-hydroxytyrosine with selective isocyanates/isothiocyanates and characterized by Infra-red, proton & carbon-13 nuclear magnetic resonance spectral and mass spectrometry studies. All the synthesized compounds have been screened for their antioxidant activity by 1,1-diphenyl1-2-picrylhydrazyl radical assay, ferric reducing antioxidant power assay and also studied their molecular docking interaction profiles against 1N8Q and 3NRZ enzymatic proteins. The in vitro antioxidant activity has further supported by quantitative structure activity relationship, absorption, distribution, metabolism, and excretion & toxicity studies, bioactivity studies & enzyme inhibition assay and identified that they were potentially bound to ASP490 & ASP361 aminoacid residue in chain A of 1N8Q protein and GLN1194 aminoacid residue in chain L of 3NRZ protein and are responsible for potential antioxidant activity. It is proved that urea derivatives linked with 4-fluoro & 4-nitro and thiourea derivatives linked with 3-chloro & 4-fluoro have exhibited promising antioxidant activity. In eventual synthesized compounds have been identified as potential blood-brain barrier penetrable compounds and proficient central nervous system active neuro-protective antioxidant agents as they have envisaged as easily penetrable to blood-brain barrier thresholds, a neuroprotective property.