Five glutinous purple rice cultivars and non-glutinous purple rice cultivated in different altitudes in the north of Thailand were collected. The samples were extracted using ethanol and determined for anthocyanins using HPLC. The total phenolic content (TPC), total flavonoid content (TFC), and the antioxidant, anti-inflammatory, and antimicrobial activities against foodborne pathogens were investigated. The highland glutinous cultivar named Khao’ Gam Luem-Phua (KGLP) extract had significantly high levels of cyanidin 3-O-glucoside, peonidin 3-O-glucoside, delphinidin 3-O-glucoside, TPC, and TFC, as well as exerting a potent antioxidant activity through ABTS assay (524.26 ± 4.63 VCEAC, mg l-ascorbic-ascorbic/g extract), lipid peroxidation (IC₅₀ = 19.70 ± 0.31 µg/mL), superoxide anions (IC₅₀ = 11.20 ± 0.25 µg/mL), nitric oxide (IC₅₀ = 17.12 ± 0.56 µg/mL), a suppression effect on nitric oxide (IC₅₀ = 18.32 ± 0.82 µg/mL), and an inducible nitric oxide synthase production (IC₅₀ = 23.43 ± 1.21 µg/mL) in combined lipopolysaccharide-interferon-γ-activated RAW 264.7 murine macrophage cells. Additionally, KGLP also exhibited antimicrobial activity against foodborne pathogens, Staphylococcus aureus, Escherichia coli, Salmonella Enteritidis, and Vibrio parahaemolyticus. These results indicate that Thai glutinous purple rice cultivated on the highland could be a potent natural source of antioxidants, anti-inflammatories, and antimicrobial agents for use as a natural active pharmaceutical ingredient in functional food and nutraceutical products.

Background: Cissus quadrangularisLinn. (CQ) has been used in Indian and Thai traditional medicine for healing bone fractures because of numerous active ingredients in CQ. It is still unclear which compounds are the active ingredients for bone formation.Methods: The molecular docking technique, the ethanolic extraction along with hexane fractionation, and an in vitro experiment with a human osteoblast cell line (MG-63) were used to narrow down the active compounds, to prepare the CQ extract, and to test biological activities, respectively.Results: The molecular docking technique revealed that quercetin and β-sitosterol had highest and lowest potential to bind to estrogen receptors, respectively. Compared to the crude ethanol extract (P1), the ethanolic fraction (P2) was enriched with rutin and quercetin at 65.36 ± 0.75 and 1.06 ± 0.12 mg/g, respectively. Alkaline phosphatase (ALP) activity was significantly enhanced in osteoblasts exposed to the P2 in both tested concentrations. The amount of hydroxyproline was slightly increased in the P1 treatment, while osteocalcin was inhibited. Moreover, the P2 significantly activated osteoprotegerin (OPG) and inhibited receptor activator of nuclear factor κ ligand (RANKL) expression.Conclusions: Taken together, the enriched rutin and quercetin fraction of CQ triggered the molecules involved in bone formation and the molecules inhibiting bone resorption.

This is the first study to investigate the effect of ethanol concentrations on the phenolic content and biological activities of Sripanya Punica granatum peel extract. Various concentrations of ethanol, (20 to 80% v/v), were used in the maceration process. Extracts were investigated for total phenolic content by the Folin–Ciocalteu method, antioxidant activities by 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and anti-tyrosinase activity by a spectrophotometric method. The chemical composition was investigated using high-performance liquid chromatography. The irritation of the extracts was determined by Hen’s egg test–chorioallantoic membrane assay. The results demonstrated that E60, which was extracted using 60% v/v ethanol, had the highest yield (66.23 ± 0.38% w/w), the highest total phenolic content (490.42 ± 7.20 μg GAE/g), and the highest antioxidant and anti-tyrosinase activities. IC₅₀ values on DPPH^• and ABTS^•+ inhibition were 10.97 ± 0.97 and 6.48 ± 0.06 µg/mL, respectively. The 60% v/v ethanol extract (E60) possessed strong tyrosinase inhibition with an IC₅₀ value of 0.10 ± 0.13 µg/mL, which is more potent than kojic acid. The major constituents were punicalagin (4.05 ± 0.26% w/w) and ellagic acid (0.63 ± 0.04% w/w). E60 was safe for topical application since it did not induce irritation. Therefore, we suggest that E60 is a promising agent for further product development.

This study aimed to study the biotransformation of indigenous northern Thai purple rice using β-glucosidase-producing Lactobacillus (BGPL) to increase the content of bioactive anthocyanin for colorectal chemoprevention and immunization. BGPL, namely, Lactobacillus FR 332, was first isolated from Thai fermented foods. Indigenous northern Thai purple rice, namely, Khao’ Gam Leum-Phua (KGLP), was selected to study bioactive anthocyanin using biotransformation by L. plantarum FR332 according to the highest amounts of cyanidin-3-glucoside. The determination of anthocyanin quantities revealed that the highest cyanidin was detected after 12 h of biotransformation, corresponding to the highest β-glucosidase activity of L. plantarum FR332 and a decrease in cyanidin-3-glucoside. The anthocyanin extract, after 12 h of biotransformation, exhibited the most potent in vitro antioxidative activity. Additionally, it showed potent anti-inflammatory activity by inhibiting cyclooxygenase-2 (COX-2), nitric oxide, and inducible nitric oxide synthase (iNOS) production in interferon-γ-stimulated colon adenocarcinoma (HT-29) cells without exerting cytotoxicity. Moreover, it also showed a potent inhibitory effect on proinflammatory cytokine interleukin-6 (IL-6) secretion and an induction effect on anti-inflammatory cytokine IL-10 secretion. These documents highlight the potential to be used of the anthocyanin extract after 12 h of biotransformation by L. plantarum FR332 as a natural active pharmaceutical ingredient (NAPI) for colorectal chemoprevention and immunization.

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.

In this work, molecular docking, pharmacophore modeling and molecular dynamics (MD) simulation were rendered for the mouse P-glycoprotein (P-gp) (code: 4Q9H) and bioflavonoids; amorphigenin, chrysin, epigallocatechin, formononetin and rotenone including a positive control; verapamil to identify protein–ligand interaction features including binding affinities, interaction characteristics, hot-spot amino acid residues and complex stabilities. These flavonoids occupied the same binding site with high binding affinities and shared the same key residues for their binding interactions and the binding region of the flavonoids was revealed that overlapped the ATP binding region with hydrophobic and hydrophilic interactions suggesting a competitive inhibition mechanism of the compounds. Root mean square deviations (RMSDs) analysis of MD trajectories of the protein–ligand complexes and NBD2 residues, and ligands pointed out these residues were stable throughout the duration of MD simulations. Thus, the applied preliminary structure-based molecular modeling approach of interactions between NBD2 and flavonoids may be gainful to realize the intimate inhibition mechanism of P-gp at NBD2 level and on the basis of the obtained data, it can be concluded that these bioflavonoids have the potential to cause herb–drug interactions or be used as lead molecules for the inhibition of P-gp (as anti-multidrug resistance agents) via the NBD2 blocking mechanism in future.