Chalermpong Saenjum

Physicochemical and antioxidative properties of black, brown and red rice varieties of northern Thailand

Rice, the seed of Oryza species, is the major cereal crop in most of the developing countries. Nearly 95% of global rice production is done in Asian countries, and about half of the world’s population consumes it. Some speciality rices are not commonly consumed. Colored rice is one of such variety. In these varieties, high amounts of anthocyanin pigment are deposited in the rice coat to form its black (also known as purple), brown and red colors. Minimum studies are there to explain the properties of these rice varieties of Thailand. Thus, the current study was aimed to assess the physicochemical and antioxidative properties of three rice varieties (Chiang Mai Black rice, Mali Red rice and Suphanburi-1 Brown rice) of different cultivars of northern Thailand. Rice bran extracts of these three cultivars were prepared with different solvents (polar and non-polar) for the evaluation of total phytochemical content and anti-oxidant free-radical-scavenging properties. Chiang Mai Black rice contained higher concentration of phenolic acid, flavonoids, and anthocyanins (Cyanidin 3-glucoside, peonidin 3-glucoside, cyanidin chloride). Chiang Mai Black rice is richer in free-radical-scavenging compounds and activities than the other tested varieties. Polar extractions of rice bran are high in anti-oxidative compounds and activities than non-polar extractions.

The influence of extraction methods on composition and antioxidant properties of rice bran oil

The current study was employed to assess the influence of the different extraction methods on total tocols, γ-oryzanol content, and antioxidant properties of Chiang Mai Black rice, Mali Red rice, and Suphanburi-1 Brown rice bran oil. Rice bran oil (RBO) was extracted by Hexane, Hot pressed, Cold pressed, and Supercritical Fluid Extraction (SFe) methods. High yield of RBO was extracted by hexane and SFe methods. Total and subgroups of tocols, and γ-oryzanol content were determined by HPLC. The hexane extracted sample accounts for high content of γ-oryzanol and tocols. Besides, all of RBO extracts contain a significantly high amount of γ-tocotrienol. In vitro antioxidant assay results indicated that superior quality of oil was recovered by hexane extraction. The temperature in the extraction process also affects the value of the oil. Superior quality of oil was recovered by hexane extraction, in terms of phytochemical contents and antioxidant properties compared to other tested extraction methods. Further, thorough study of factors compromising the quality and quantity of RBO recovery is required for the development of enhanced functional foods and other related products.

A cost-effective assay for antioxidant using simple cotton thread combining paper based device with mobile phone detection

A cost-effective assay for antioxidant using simple cotton thread combining paper based device with mobile phone detection has been investigated. Standard and sample solutions flow along a bunch of cotton thread treated with sodium hydroxide via microfluidic behaviors without external pumping. The analyte solution reacts with the reagents that have been immobilized on the paper strip fixed at the end of the cotton bunch. The developed platforms were used for the assays of total phenolic content and antioxidant capacity by employing Folin-Ciocalteu and 2, 2-diphenyl-1-picryhydrazyl (DPPH) respectively. Simple detection can be made by employing a mobile phone camera (iPhone 4S) with Image J or Photoshop for image processing and evaluation. Gallic acid was used as a reference standard in this work, as its polyphenol structures can be found in many plants. The total phenolic content is expressed as gallic acid equivalents (GAE) (mg/g material). Inhibition capacity is calculated by the equation: % I = [(Io - Is)/ Io] × 100, where Is is the relative magenta intensity (CMYK mode) of sample, and Io the relative magenta intensity of DPPH•. IC50 inhibition can be estimated from the graph and can be used for the antioxidant capacity consideration. Applications to the assay green tea samples were demonstrated. The total phenolic contents in the green tea samples were found to be 48-105mg/g, with %RSD of less than 10 for that of higher 50 GAE mg/g and IC50 values of the samples studied were 25-50mg/L. The results obtained by the developed methods agree with that of the standard methods.

Assessment of Nevirapine Prophylactic and Therapeutic Dosing Regimens for Neonates

Background: Nevirapine (NVP) is a key component of antiretroviral prophylaxis and treatment for neonates. We evaluated current World Health Organization (WHO) weight-band NVP prophylactic dosing recommendations and investigated optimal therapeutic NVP dosing for neonates. Methods: The PHPT-5 study in Thailand assessed the efficacy of “Perinatal Antiretroviral Intensification” to prevent mother-to-child transmission of HIV in women with <8 weeks of antiretroviral treatment before delivery (NCT01511237). Infants received a 2-week course of zidovudine/lamivudine/NVP (NVP syrup/once daily: 2 mg/kg for 7 days; then 4 mg/kg for 7 days). Infant samples were assessed during the first 2 weeks of life. NVP population pharmacokinetics (PK) parameters were estimated using nonlinear mixed-effects models. Simulations were performed to estimate the probability of achieving target NVP trough concentrations for prophylaxis (>0.10 mg/L) and for therapeutic efficacy (>3.0 mg/L) using different infant dosing strategies. Results: Sixty infants (55% male) were included. At birth, median (range) weight was 2.9 (2.3–3.6) kg. NVP concentrations were best described by a 1-compartment PK model. Infant weight and postnatal age influenced NVP PK parameters. Based on simulations for a 3-kg infant, ≥92% would have an NVP trough >0.1 mg/L after 48 hours through 2 weeks using the PHPT-5 and WHO-dosing regimens. For NVP-based therapy, a 6-mg/kg twice daily dose produced a trough >3.0 mg/L in 87% of infants at 48 hours and 80% at 2 weeks. Conclusion: WHO weight-band prophylactic guidelines achieved target concentrations. Starting NVP 6 mg/kg twice daily from birth is expected to achieve therapeutic concentrations during the first 2 weeks of life.

Cell cycle arrest and apoptosis induction by methanolic leaves extracts of four Annonaceae plants

BackgroundUvaria longipes (Craib) L.L.Zhou, Y.C.F.Su & R.M.K.Saunders, Artabotrys burmanicus A.DC, Marsypopetalum modestum (Pierre) B.Xue & R.M.K.Saunders and Dasymaschalon sp. have been used for traditional medicine to treat cancer-like symptoms in some ethnic groups of Thailand and Laos.MethodsWe evaluated the anti-cancer activity of these Annonaceae plants against several human cancer cell lines. The apoptosis induction was detected by Annexin/propidium iodide (PI) staining. Phytochemical screening was tested by standard protocols and bioactive compounds were determined by HPLC.ResultsThe crude extracts from leaves of U. longipes, Dasymaschalon sp., A. burmanicus, and M. modestum showed particular effects that were found to vary depending on the cancer cell line, suggesting that the effect was in a cell-type specific manner. Interestingly, the induction of apoptotic cell death was prominent by the leaves-derived crude extract of M. modestum. This crude was, therefore, subjected to cell cycle analysis by PI staining. Results showed that this crude extract arrested cell cycle and increased the percentage of cells in the SubG1 phase in some cancer cell lines. The phytochemical screening tests indicated that all crude extracts contained tannins and flavonoids. HPLC of flavonoids using standards identified rutin as an active compound in U. longipes and Dasymaschalon sp., whereas quercetin was found in U. longipes and M. modestum.ConclusionsThese crude extracts provide a new source for rutin and quercetin, which might be capable of inducing cancer cell apoptotic death in a cell-type specific manner. This suggests, by analyzing the major bioactive compounds, the potential use of these crudes for chemotherapy in the future.

Protective Effect on Oxidative DNA Damage and Antiproliferative Activity of Standardized γ-Oryzanol-Rich Extracts from Thai Purple Rice Bran

This study was carried out to investigate the protective effect of standardized γ-oryzanol-rich extracts on oxidative DNA damage induced by Fenton reaction and antiproliferative activity against human cancer cells. Six cultivars of Thai purple rice were collected in northern Thailand. Rice bran was extracted with hexane/ethyl acetate mixture and the extract was evaporated to obtain crude rice bran oil. Each rice bran oil was further purified by column chromatography to obtain the γ-oryzanol-rich extract. The extracts contained γ-oryzanol in the range of 1.17 – 7.54 % w/w, in which GAM THOR exhibited the highest γ-oryzanol content. The extr \acts containing more than 5.0 % w/w γ-oryzanol (GAM THOR, GAM DOI MUSUR and GAM SUKHOTHAI-2) were selected to be standardized with γ-oryzanol and then the protective effect on oxidative DNA damage and antiproliferative activity against four human cancer cell lines (HT-29, HCT 116, MDA-MB-468 and PC3) were investigated. The extracts (10 µg/ml) exhibited a protective effect on oxidative DNA damage induced by Fenton reaction as compared with standard quercetin (lower than 5 µg/ml). Furthermore, all of the extracts exerted antiproliferative activity against human cancer cell lines in a dose-dependent manner. GAM THOR exhibited the highest antiproliferative activity against HT-29, HCT 116, MDA-MB-468 and PC3 with an 50% inhibition concentration value of 52.18 ± 1.21, 40.58 ± 5.69, 48.59 ± 2.40 and 51.61 ± 1.30 µg/ml, respectively. From these findings, γ-oryzanolrich extracts from Thai purple rice bran show potential as chemopreventive supplements or in nutraceuticals.

Development of Colorectal-Targeted Dietary Supplement Tablets Containing Natural Purple Rice Bran Oil as a Colorectal Chemopreventive

Colorectal cancer occurs due to various factors. The important risks are dietary lifestyle and inflammatory bowel diseases, such as Crohn’s disease and ulcerative colitis. It has been found that the inhibitory enzyme cyclooxygenase-2 (COX-2) in the colorectal region can potentially reduce the risk of colorectal cancer. The present study investigated rice bran oil from natural purple rice bran, which exhibits antioxidant and anti-inflammatory activity. This study aimed to evaluate the bioactive compound content of natural purple rice bran oil (NPRBO) derived from native Thai purple rice and the anti-inflammatory activity of NPRBO in colorectal cancer cells, and to develop a colorectal delivery platform in the form of film-coated tablets. NPRBO from the rice bran of five different Thai purple rice cultivars, namely Khao’ Gam Leum-Phua (KGLP), Khao’ Gam Boung (KGB), Khao’ Gam Thor (KGT), Khao’ Gam Pah E-Kaw (KGPEK), and Khao’ Niaw Dam (KND), were extracted using the supercritical carbon dioxide extraction technique. The amount of γ-oryzanol (ORY), tocotrienols, and tocopherols present in NPRBOs and the in vitro anti-inflammatory activity of NPRBO were investigated. The highest anti-inflammatory NPRBO was transformed into a dry and free-flowing powder by liquisolid techniques. Then, it was compressed into core tablets and coated with Eudragit®L100 and Eudragit® NE30D. The in vitro release study of the film-coated NPRBO tablets was performed in three-phase simulated gastrointestinal media. The cultivar KGLP was superior to the other samples in terms of the ORY, tocotrienol and tocopherol contents and anti-inflammatory activity. Aerosil® was the most suitable absorbent for transforming NPRBO into a free-flowing powder and was used to prepare the NPRBO core tablets. The in vitro KGLP-NPRBO film-coated tablet release profile showed that no ORY was released at gastric pH while 85% of ORY was released at pH 7.4 after 6 h; this would be expected to occur in the colorectal area. Therefore, this study demonstrates the potential of KGLP-NPRBO to prevent colorectal cancer via a specific colorectal dietary supplement delivery system.

Molecular modeling investigation of the potential mechanism for phytochemical-induced skin collagen biosynthesis by inhibition of the protein phosphatase 1 holoenzyme

The most prominent feature of UV-induced photoaged skin is decreased type 1 procollagen. Increase of the TGF-β/Smad signaling through inhibition of the TβRI dephosphorylation by the GADD34–PP1c phosphatase complex represents a promising strategy for the increase in type 1 collagen production and prevention of UV-induced skin photoaging. In this study, the molecular docking and dynamics simulations, and pharmacophore modeling method were run to investigate a possible binding site as well as binding modes between apigenin, daidzein, asiaticoside, obovatol, and astragaloside IV and PP1c. Through docking study, the possible binding site for these phytochemicals was predicted as the hydrophobic (PP1–substrate binding) groove. The result indicates that PP1 is the significant target of these compounds. Moreover, the 20,000-ps MD simulations present that the binding locations and modes predicted by the docking have been slightly changed considering that the MD simulations proffer more reliable details upon the protein–ligand recognition. The MM-GBSA binding free energy calculations and pharmacophore modeling rationally identify that the highly hydrophobic surfaces/pockets at close proximity of the catalytic core are the most favorable binding locations of the herbal compounds, and that some experimental facts upon a possible mechanism of increase in collagen biosynthesis can be explained. The present study theoretically offers the reliable binding target of the herbal compounds, and therefore helps to understanding the action mechanism for natural small molecules that enhance collagen production.

EPR and HPLC Investigation of Pigments in Thai Purple Rice

We investigated the pigments in Thai purple rice using electron paramagnetic resonance (EPR), X-band (9 GHz) EPR imaging (EPRI), and HPLC. The location and spatial distribution of the paramagnetic species in purple and white rice were determined by EPR and EPRI. EPR primarily detected three paramagnetic species in purple rice, which were identified as stable radicals, Mn2+, and Fe3+ based on the gvalues and hyperfine components of the EPR signals. Subsequent noninvasive two-dimensional (2D) EPRI revealed that these stable radicals are primarily located in the pigmented region of purple rice, while very few radicals were observed in the interior of the rice. HPLC revealed that the major compounds were cyanidin-3-O-glucoside and peonidin-3-O-glucoside. Scavenging activities, EPR, and EPR imaging results indicate that the stable radicals contain the radical state of anthocyanins and are mostly found within the pigmented embryo region of purple rice. They could be either associated with scavenging activities or could be one of the products of their oxidative decomposition.

Furanocoumarins from kaffir lime and their inhibitory effects on inflammatory mediator production

Abstract Two known furanocoumarins, namely, 6ˊ, 7ˊ-dihydroxybergamottin (1) and oxypeucedanin hydrate (2), were isolated from Kaffir lime (Citrus hystrix DC) fruit peel using an assay of nitric oxide scavenging effect-guided fractionation. The inhibitory activities of isolated coumarins on the production of nitric oxide (NO) and inducible nitric oxide synthase (iNOS) were studied in mouse macrophages RAW264.7 cells, whereas their inhibitory effect on cyclooxygenase-2 (COX-2) production was investigated using HT-29 and HCT116 cells. The results demonstrated that 1 inhibited lipopolysaccharide-interferon gamma-induced NO and iNOS production in RAW264.7 cells and COX-2 production in HT-29 and HCT116 cells with IC50 values of 16.16 ± 1.08, 18.63 ± 1.42, 18.19 ± 0.95 and 17.53 ± 0.88 µg/mL, respectively; 2 showed IC50 values of 18.23 ± 1.25, 22.54 ± 1.56, 22.27 ± 1.14 and 23.24 ± 1.05 µg/mL, respectively. Additionally, the positive control curcumin exhibited these activities with IC50 values of 12.52 ± 0.63, 15.55 ± 1.34, 14.29 ± 0.58 and 16.14 ± 0.65 µg/mL, respectively. The inhibitory effect of 1 on the production of iNOS and COX-2 was significantly stronger than that of 2. This study indicated that furanocoumarins from Kaffir lime fruit peels have potency for further development as an anti-inflammatory drug.