Sisa puri pitaya merah bersama biji telah digunakan dalam penyediaan mufin yang dicampurkan dengan 10%, 15% dan 20% puri dalam formulasi bater. Ujian warna, kandungan jumlah polifenol, jumlah flavonoid, ujian antioksida; pemerangkapan radikal bebas 2,2-difenil-1-pikrilhidrazil (DPPH) dan ujian penurunan ferrik (FRAP) telah dijalankan. Warna bater 3 jenis mufin tersebut berwarna merah jambu violet. Warna merah jambu (nilai a) meningkat dengan signifikan (p<0.05) selaras peningkatan peratus kandungan puri manakala kecerahan (nilai L) menurun dengan peningkatan puri. Apabila dimasak, semua warna merah jambu daripada bater hilang. Permukaan mufin adalah lebih gelap (nilai L), dengan mufin 20% puri paling signifikan (p<0.05). Isi kesemua mufin berwarna kuning dan kecerahan (nilai L) didapati berkurang secara signifikan (p<0.05) dengan pertambahan peratus puri. Jumlah polifenol sampel mufin menunjukkan mufin 10% puri pitaya ekstrak air mengandungi jumlah polifenol yang paling tinggi (29.0 mg GAE/100 g sampel). Kandungan flavonoid menunjukkan mufin 20% puri pitaya mengandungi flavonoid yang paling signifikan (p<0.05) 15.3 mg katekin/100 g sampel berbanding mufin kawalan 11.0 mg katekin. Bagi ujian antioksida DPPH, semua mufin dengan puri pitaya menunjukkan peratus pemerangkapan yang lebih baik berbanding kawalan. Ujian FRAP menunjukkan pola yang serupa dengan keputusan mufin 10% (17.4), mufin 15% (15.4) dan mufin 20% (17.5 mg trolox/100 g sampel). Warna merah jambu bater mufin hilang semasa proses memasak namun nilai antioksida masih diperolehi dalam mufin masak.
As part of a search for novel inhibitors of HIV-1 reverse transcriptase, the acetone extract of the giant African snail, Achatina fulica, was shown to be active. Fractionation of the extract yielded inophyllums A, B, C, and E and calophyllolide (1a, 2a, 3a, 3b, and 6), previously isolated from Calophyllum inophyllum Linn., a known source of nutrition for A. fulica. From a methanol/methylene chloride extract of C. inophyllum, the same natural products in considerably greater yield were isolated in addition to a novel enantiomer of soulattrolide (4), inophyllum P (2b), and two other novel compounds, inophyllums G-1 (7) and G-2 (8). The absolute stereochemistry of inophyllum A (1a) was determined to be 10(R), 11(S), 12(S) from a single-crystal X-ray analysis of its 4-bromobenzoate derivative, and the relative stereochemistries of the other inophyllums isolated from C. inophyllum were established by a comparison of their 1H NMR NOE values and coupling constants to those of inophyllum A (1a). Inophyllums B and P (2a and 2b) inhibited HIV reverse transcriptase with IC50 values of 38 and 130 nM, respectively, and both were active against HIV-1 in cell culture (IC50 of 1.4 and 1.6 microM). Closely related inophyllums A, C, D, and E, including calophyllic acids, were significantly less active or totally inactive, indicating certain structural requirements in the chromanol ring. Altogether, 11 compounds of the inophyllum class were isolated from C. inophyllum and are described together with the SAR of these novel anti-HIV compounds.
Doxorubicin (DOX) adalah salah satu ubat kemoterapi yang paling berkesan untuk merawat pelbagai neoplasma seperti leukemia, limfoma dan kanser payudara. Walau bagaimanapun, ia sering dikaitkan dengan kardiomiopati. Pada masa ini, tiada rawatan yang sesuai untuk mengurangkan kesan kardiomiopati tanpa kesan sampingan yang ketara. Oleh itu, kajian ini bertujuan untuk mengkaji kesan-kesan perlindungan potensi ekstrak benih padi (RSE) terhadap kesitotoksikan yang disebabkan oleh DOX menggunakan kajian kultur sel vitro. Keupayaan antioksidan RSE dinilai, dan hasilnya menunjukkan jumlah kandungan fenolik yang lebih rendah (TPC), tetapi jumlah kandungan flavonoid total (TFC) dan kapasiti antioksidan yang setara trolox (TEAC), dibandingkan dengan ekstrak benih wheatgrass. Satu siri eksperimen spektroskopi penyerapan dan pendarfluor menunjukkan bahawa RSE boleh menghalang pembentukan kompleks DOX-DNA pada kepekatan yang diuji. Tambahan pula, daya maju sel kardiomiosit sel, H9c2 (2-1), telah diuji selepas 24, 48 dan 72 jam rawatan DOX terhadap RSE menggunakan ujian proliferasi sel berdasarkan garam tetrazolium (MTS reagent). Hasilnya menunjukkan kesan perlindungan yang signifikan terhadap RSE terhadap kesitotoksikan yang disebabkan oleh DOX. Jalur sel karsinoma nasofarinks, HK1, digunakan sebagai kawalan untuk menentukan sama ada keberkesanan DOX terjejas oleh pentadbiran bersama RSE. Hasilnya tidak menunjukkan kesan negatif terhadap keberkesanan dadah. Pelbagai sifat berfaedah RSE menunjukkan potensi kuatnya untuk membangunkan agen kardioprotektif untuk melengkapi rawatan DOX dalam tetapan klinikal.
This study aimed to determine the total phenolics and antioxidant capacity of defatted dabai parts based on liquid extraction and optimized using response surface methodology (RSM). A two-level factorial design was applied to determine the effect of two independent variables (extraction time: X1 and % methanol: X2) on three response variables (total phenolic content: Y1, total flavonoid/anthocyanin content: Y2 and Trolox equivalent antioxidant capacity: Y3). The optimum conditions for extraction time and percent methanol were 36 min or 1 min and 62.25% or 53% for the defatted dabai pulp or peel, respectively. The RSM optimized extraction was compared with sonication-assisted extraction. Optimization results showed that defatted dabai parts had high total phenolic content and antioxidant capacity. Sonication-assisted extraction utilized the optimized extraction conditions had further increased the total phenolic content and antioxidant capacity of defatted dabai peel, but not in the pulp. Therefore, optimization of different extraction methods for the defatted fruit parts is recommended for future studies.
Svalbardines A and B (1 and 2) and annularin K (3) were isolated from cultures of Poaceicola sp. E1PB, an endophyte isolated from the petals of Papaver dahlianum from Svalbard, Norway. Svalbardine A (1) is a pyrano[3,2-c]chromen-4-one, a new analogue of citromycetin. Svalbardine B (2) displays an unprecedented carbon skeleton based on a 5'-benzyl-spiro[chroman-3,7'-isochromene]-4,8'-dione core. Annularin K (3) is a hydroxylated derivative of annularin D. The structure of these new polyketides, along with those of known compounds 4-6, was established by spectrometric analysis, including extensive ESI-CID-MS n processing in the case of svalbardine B (2).
A study was conducted to evaluate the bioavailability of alpha-, gamma- and delta-tocotrienols administered via oral, intravenous, intramuscular and intraperitoneal routes in rats. Three separate experiments, each conducted according to a two-way crossover design, were carried out to compare intravenous and oral, intramuscular and oral, and intraperitoneal and oral administration. Oral absorption of all three tocotrienols was found to be incomplete. Of the three tocotrienols, alpha-tocotrienol had the highest oral bioavailability, at about 27.7+/-9.2%, compared with gamma- and delta-tocotrienols, which had values of 9.1+/-2.4% and 8.5+/-3.5%, respectively. Such biodiscrimination was also observed in their total clearance rates (estimated from the intravenous data). alpha-Tocotrienol showed the lowest clearance rate at about 0.16 L kg(-1) h(-1), whereas that of delta- and gamma-tocotrienols was quite similar, with values of 0.24 and 0.23 L kg(-1) h(-1), respectively. Interestingly, all three tocotrienols were found to be negligibly absorbed when administered intraperitoneally and intramuscularly. Thus, these two routes of administration should be avoided when evaluating the biological activities of the tocotrienols in whole animal experiments.
There are six tocol analogs present in palm oil, namely α-tocopherol (α-T), α-tocomonoenol (α-T₁), α-tocotrienol (α-T₃), γ-tocotrienol (γ-T₃), β-tocotrioenol (β-T₃) and δ-tocotrienol (δ-T₃). These analogs were difficult to separate chromatographically due to their similar structures, physical and chemical properties. This paper reports on the effect of pressure and injection solvent on the separation of the tocol analogs in palm oil. Supercritical CO₂ modified with ethanol was used as the mobile phase. Both total elution time and resolution of the tocol analogs decreased with increased pressure. Ethanol as an injection solvent resulted in peak broadening of the analogs within the entire pressure range studied. Solvents with an eluent strength of 3.4 or less were more suitable for use as injecting solvents.
This study used highly lipophilic agents with an aim to increase the oxidant inhibitory activity and enhance photothermal stability of a novel mixed soy lecithin (ML)-based liposome by changing the composition of formulation within the membrane. Specifically, the development and optimization of the liposome intended for improving Trolox equivalent antioxidant capacity (TEAC) value and %TEAC loss was carried out by incorporating a natural antioxidant, quercetin (QU). In this context, a focus was set on QU encapsulation in ML-based liposomes and the concentration-dependent solubility of QU was investigated and calculated as encapsulation efficiency (EE). To explore the combined effects of the incorporation of plant sterols on the integrity and entrapment capacity of mixed phospholipid vesicles, conjugation of two types of phytosterols (PSs), namely β-sitosterol (βS) and stigmasterol (ST), to mixed membranes at different ratios was also performed. The EE measurement revealed that QU could be efficiently encapsulated in the stable ML-based liposome using 0.15 and 0.1 g/100 mL of βS and ST, respectively. The aforementioned liposome complex exhibited a considerable TEAC (197.23%) and enhanced TEAC loss (30.81%) when exposed to ultraviolet (UV) light (280-320 nm) over a 6 h duration. It appeared that the presence and type of PSs affect the membrane-integration characteristics as well as photodamage transformation of the ML-based liposome. The association of QU with either βS or ST in the formulation was justified by their synergistic effects on the enhancement of the EE of liposomes. Parallel to this, it was demonstrated that synergistic PS effects could be in effect in the maintenance of membrane order of the ML-based liposome. The findings presented in this study provided useful information for the development and production of stable QU-loaded ML-based liposomes for food and nutraceutical applications and could serve as a potential mixed lipids-based delivery system in the disease management using antioxidant therapy.
The total phenolic contents (TPC) and antioxidant activities of five popular Malay raw salads or Ulam were investigated using DPPH radical scavenging and reducing ferric ion antioxidant power (FRAP) assays. The Ulam studied were the leaves of Cosmos caudatus (Ulam Raja), Oenanthe javanica (Selom), Murraya koenigii (Curry Leaf), Centella asiatica (Pegaga) and the seeds of Parkia speciosa (Petai). Ranking order of TPC (mg gallic acid equivalent per gram of plant on dry basis), TEACDPPH (µmol Trolox equivalent per gram of plant on dry basis) and TEACFRAP (µmol Trolox equivalent per gram of plant on dry basis) values were: Curry Leaf (33.18), Selom (31.8), Ulam Raja (31.3) > Pegaga (11.16) > Petai (6.45); Ulam Raja (212.8) > Selom (185.9) > Curry Leaf (82.1), Petai (67.62) > Pegaga (32.4); Selom (199.96) > Ulam Raja (183.11) > Curry Leaf (108.34) > Pegaga (65.99) > Petai (44.67), respectively. No significant correlation (p>0.05) was observed between antioxidant activities and TPC which could be due to steric hindrance or presence of other reducing agents. Interestingly, Selom showed antioxidant activities that are comparable to Ulam Raja.
Antioxidants in seaweeds have attracted increasing interest for its role in protecting human health. Therefore, the aim of this study was to assess the Total phenolic content (TPC) values and antioxidant activities in red seaweeds Kappaphycus alvarezii and Kappaphycus striatum of different solvent extracts. Total phenolic content (TPC) and antioxidant activities (DPPH scavenging assay and Trolox equivalent antioxidant capacity assay, TEAC) for both K. alvarezii and K. striatum extracts were determined using different solvents at different concentrations (ethanol: 50%, 70%, 100%; acetone: 50%, 70%, 100%; methanol: 50%, 70%, 100%). The TPC value was measured using the Folin-Ciocalteu’s method. The antioxidant activities were measured by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and Trolox Equivalent Antioxidant Capacity (TEAC) assay. The highest TPC value of K. alvarezii antioxidant extract was obtained by 50% ethanol extracts while for K. striatum obtained by 50% methanol extract. The highest percentage of DPPH free radical inhibition for K. alvarezii was shown by 50% acetone extract while K. striatum was shown using 50% methanol extract. The highest TEAC value for K. alvarezii was shown by 50% acetone while K. striatum extract was shown by 50% ethanol extract. The TPC values and antioxidant activities of all solvent extracts of K. striatum were significantly higher (p< 0.05) than K. alvarezii antioxidant extracts. The TPC values showed strong correlation (r = 0.797) with TEAC values for K. alvarezii antioxidant extract (p< 0.01). The TEAC values also showed strong correlation (r = 0.735) with percentage of DPPH free radical inhibition for K. alvarezii (p< 0.01). The TPC value, DPPH free radical scavenging assay and TEAC assay for K. striatum extracts showed strong correlation (r> 0.8) with each other (p< 0.01). In summary, K. striatum showed better antioxidant activity and higher TPC value than K. alvarezii.
This study aimed to compare the antioxidant content and antioxidant capacity of pulp and peel of two varieties of pomelo fruit (Tambun White and Tambun Pink). Antioxidants including total phenolic content, total flavonoid content and ascorbic acid content were determined using Folin-Ciocalteu reagent assay, aluminium chloride colorimetric assay and AOAC method, respectively. Antioxidant capacity of pomelo pulp and peel was measured using ferric reducing antioxidant potential and trolox equivalent antioxidant capacity assays. The peels of both pomelo fruits had higher antioxidant content and capacity than their pulps. Moreover, the white variety of pomelo had higher antioxidant content and capacity compared to the pink counterpart. Trolox equivalent antioxidant capacity of the samples was positively high correlated with total phenolic content (r = 0.978) and total flavonoid content (r = 0.959), except for ascorbic acid. Therefore, pomelo peel from white variety possessed higher antioxidant properties and it is potentially rich sources of natural antioxidants.
1. The effect of tocotrienol and tocopherol on glutathione S-transferase (GST) and gamma-glutamyl transpeptidase (GGT) activities in cultured rat hepatocytes were investigated. 2. Tocotrienol and tocopherol significantly decreased GGT activities at 5 days in culture but tocotrienol also significantly decreased GGT activities at 1-2 days. 3. Tocotrienol and tocopherol treatment significantly decreased GST activities at 3 days compared to the control but tocotrienol also decreased GST activities at 1-3 days. 4. Tocotrienol showed a more pronounced effect at a dosage of greater than 50 microM tocotrienol at 1-3 days in culture compared to the control.
We have investigated the pharmacokinetics and bioavailability of alpha-, gamma- and delta-tocotrienols under fed and fasted conditions in eight healthy volunteers. The volunteers were administered a single oral dose of mixed tocotrienols (300 mg) under fed or fasted conditions. The bioavailability of tocotrienols under the two conditions was compared using the parameters peak plasma concentration (Cmax), time to reach peak plasma concentration (Tmax) and total area under the plasma concentration-time curve (AUC(o-infinity)). A statistically significant difference was observed between the fed and fasted logarithmic transformed values of Cmax (P < 0.01) and AUC(0-infinity) (P < 0.01) for all three tocotrienols. In addition, the 90% confidence intervals for the ratio of the logarithmic transformed AUC(0-infinity) values of alpha-, gamma- and delta-tocotrienols under the fed state over those of the fasted state were found to lie between 2.24-3.40, 2.05-4.09 and 1.59-3.81, respectively, while those of the Cmax were between 2.28-4.39, 2.31-5.87 and 1.52-4.05, respectively. However, no statistically significant difference was observed between the fed and fasted Tmax values of the three homologues. The mean apparent elimination half-life (t(1/2)) of alpha-, gamma- and delta-tocotrienols was estimated to be 4.4, 4.3 and 2.3 h, respectively, being between 4.5- to 8.7-fold shorter than that reported for alpha-tocopherol. No statistically significant difference was observed between the fed and fasted t(1/2) values. The mean apparent volume of distribution (Vd/f) values under the fed state were significantly smaller than those of the fasted state, which could be attributed to increased absorption of the tocotrienols in the fed state.
Gamma-tocotrienol (GTT), an isomer of vitamin E and hydroxy-chavicol (HC), a major bioactive compound in Piper betle, has been reported to possess anti-carcinogenic properties by modulating different cellular signaling events. One possible strategy to overcome multi-drug resistance and high toxic doses of treatment is by applying combinational therapy especially using natural bioactives in cancer treatment.
Vitamin E is a fat-soluble compound and powerful antioxidant that have been shown to protect the cell membranes against damage caused by free radicals. Human vitamin E supplementation studies are usually limited to α-tocopherol but currently tocotrienols are also available. This study aims to compare the effects of tocotrienol rich fraction (TRF) with α-tocopherol (α-TF) supplementation on oxidative stress in healthy male and female older adults aged 50-55 years old. A total of 71 subjects both male and female aged between 50 and 55 years were divided into groups receiving placebo (n = 23), α-TF (n = 24) and TRF (n = 24) for six months. Blood was taken at baseline (month 0), 3 months and 6 months osf supplementation for determination of plasma malondialdehyde (MDA), protein carbonyl, total DNA damage, vitamin D concentration and vitamin E isomers. α-TF supplementation reduced plasma MDA and protein carbonyl in female subjects after 3 and 6 months. TRF supplementation reduced MDA levels in both males and females as early as 3 months while DNA damage was reduced in females only at 6 months. Supplementation with α-TF and TRF increased plasma vitamin D concentration in both males and females after 6 months, but vitamin D concentration in male subjects were significantly higher compared to female subjects in TRF group. Vitamin E isomer determination showed α-TF, α-tocotrienol and γ-tocotrienol were increased in both male and female subjects. In conclusion, TRF supplementation effects were different from α-TF in reducing oxidative stress markers and vitamin D levels with a more pronounced effect in female subjects.
This study investigated combination nanocarrier and microwave system for α-tocopherol and γ-tocotrienol delivery against dermatitis, without skin thinning effect of steroids. The vitamin E was formulated into water-rich/water-poor nanoemulsions, and had their droplet size, zeta potential, morphology, therapeutic content, encapsulation efficiency and release, in vitro skin therapeutics/nanoemulsion penetration, retention and permeation profiles, and in vivo pharmacodynamics characteristics examined, with skin pre-treated by precision microwave when applicable. The nanoemulsions had droplet sizes <150 nm and negative zeta potential values. The skin pre-treatment by microwave (1 mW/3985 MHz) promoted therapeutics accumulation in epidermis through enhancing nanoemulsion penetration into skin. The combination nano- and microwave technologies fluidized skin lipid and protein domains with epidermal microstructures being fluidized to a greater extent than dermis, allowing a relatively high epidermal-to-dermal nanoemulsion distribution. Microwave of lower or higher than 3985 MHz brought about lower skin therapeutics/nanoemulsion accumulation due to insufficient lipid/protein domain fluidization or microwave-skin interaction limiting at skin surfaces only. Using water-rich nanoemulsion with higher therapeutic release and skin pre-treatment with 3985 MHz microwave, dermatitis was alleviated in vivo without skin thinning of standard steroid. The use of combination microwave and nanotechnology promotes vitamin delivery and translates to positive dermatitis treatment outcome that warrants future investigation.
This study aimed to determine and compare antioxidant components and antioxidant capacity in different parts (skin, pulp, mace and seed) of nutmeg. Freeze dried samples were extracted using 80% methanol, while Folin-Ciocalteu assay was employed to determine total phenolic content, aluminium chloride assay was applied to determine total flavonoid content and ascorbic acid was assessed by titrimetric method. Antioxidant activities were evaluated by ferric reducing antioxidant power and trolox equivalent antioxidant capacity (TEAC) assays. Results revealed that nutmeg seed contained the highest TPC followed by mace, skin and pulp. Similar observation was also found for TFC. The highest ascorbic acid content was found in nutmeg mace, while the lowest was in its pulp. For antioxidant activity, nutmeg seed possessed the highest FRAP and TEAC values, while nutmeg pulp had the lowest as compared to other parts. Phenolic compounds in nutmeg samples have exhibited strong correlation with antioxidant capacity. Therefore, nutmeg is a potential functional food with high antioxidants, especially nutmeg seed. Phenolic compounds in nutmeg samples have exhibited strong correlation with antioxidant capacity. Therefore, nutmeg is a potential functional food with high antioxidants, especially nutmeg seed.
Gamma-tocotrienol (GTT) has been shown to exhibit significant antitumor activity in a variety of tumor cells. Previous findings have demonstrated that GTT had antiprolifera-tive effects on a liver cancer cell line (HepG2) with an IC50 value of 170μM. In this study, two dimensional gel electrophoresis (2DE) was used to determine changes in protein expression in HepG2 cell line following treatment with GTT. The ultimate aim is to identify the possible molecular mechanisms involved in GTT antitumor activity. This study is focused on obtaining a 2DE protein profile for HepG2 cell line with and without
GTT treatment. In the preliminary analysis of the resulting 2DE profiles, 18 protein spots were found to be differentially expressed in cells treated with GTT. This observa-tion is confirmed by extending the analysis to a larger sample size. By studying the effects of GTT treatment on differential protein expression in HepG2 cells the underly-ing mechanisms involved in the antitumor activity of GTT may be elucidated.
Oxidative stress and apoptosis can disrupt the bone formation activity of osteoblasts which can lead to osteoporosis. This study was conducted to investigate the effects of γ-tocotrienol on lipid peroxidation, antioxidant enzymes activities, and apoptosis of osteoblast exposed to hydrogen peroxide (H(2)O(2)). Osteoblasts were treated with 1, 10, and 100 μM of γ-tocotrienol for 24 hours before being exposed to 490 μM (IC(50)) H(2)O(2) for 2 hours. Results showed that γ-tocotrienol prevented the malondialdehyde (MDA) elevation induced by H(2)O(2) in a dose-dependent manner. As for the antioxidant enzymes assays, all doses of γ-tocotrienol were able to prevent the reduction in SOD and CAT activities, but only the dose of 1 μM of GTT was able to prevent the reduction in GPx. As for the apoptosis assays, γ-tocotrienol was able to reduce apoptosis at the dose of 1 and 10 μM. However, the dose of 100 μM of γ-tocotrienol induced an even higher apoptosis than H(2)O(2). In conclusion, low doses of γ-tocotrienol offered protection for osteoblasts against H(2)O(2) toxicity, but itself caused toxicity at the high doses.
The effect of γ -tocotrienol, a vitamin E isomer, in modulating gene expression in cellular aging of human diploid fibroblasts was studied. Senescent cells at passage 30 were incubated with 70 μ M of γ -tocotrienol for 24 h. Gene expression patterns were evaluated using Sentrix HumanRef-8 Expression BeadChip from Illumina, analysed using GeneSpring GX10 software, and validated using quantitative RT-PCR. A total of 100 genes were differentially expressed (P < 0.001) by at least 1.5 fold in response to γ -tocotrienol treatment. Amongst the genes were IRAK3, SelS, HSPA5, HERPUD1, DNAJB9, SEPR1, C18orf55, ARF4, RINT1, NXT1, CADPS2, COG6, and GLRX5. Significant gene list was further analysed by Gene Set Enrichment Analysis (GSEA), and the Normalized Enrichment Score (NES) showed that biological processes such as inflammation, protein transport, apoptosis, and cell redox homeostasis were modulated in senescent fibroblasts treated with γ -tocotrienol. These findings revealed that γ -tocotrienol may prevent cellular aging of human diploid fibroblasts by modulating gene expression.