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This research explored the prebiotic potential of tamarind seed kernel powder (RTS), focusing on yield, nutritional composition, physicochemical properties using ATR-FTIR spectroscopy and colorimetric methods, effects on Bifidobacterium animalis in promoting the growth and biofilm formation compared to inulin using bacterial enumeration and crystal violet staining techniques, and the biofilm biomolecular composition characterization. The multi-nutrient composition RTS yielded 65.65 % ( w/w ), which significantly exhibited prebiotic activity in a dose-dependent manner with effective concentrations at 2.5 and 5 % RTS, stimulated B. animalis growth (rate 22 % • h -1 ) and enhanced biofilm formation (BFI = 256.71) exceeding the inulin. Moreover, ATR-FTIR spectroscopy and PCA analysis revealed the RTS-induced alteration of the biofilm's biomolecular composition, with a notable increase in amide A and a decrease in carboxylic hydroxyl groups. The study highlights RTS as a promising prebiotic agent with the potential for improving gut health, with further validation in the in vivo models being advisable., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2025 The Authors.)

Sesamolin possesses limited aqueous solubility, a drawback for biological activity study in cancer cell models. This study aimed to enhance sesamolin's ability to fight cancer, as it is a bioactive compound with low water solubility found in sesame. We developed different Pickering emulsion delivery systems and tested their anticancer effects on various cancer cell types. Sesamolin was incorporated into either sesame or olive oil and subsequently formulated as oil in water (o/w) Pickering emulsions stabilized by the carboxylated cellulose nanocrystal (cCNC). The anticancer activity was determined based on cell viability and the induction of cell death mechanisms. The results demonstrated a synergistic effect of the components in the emulsion, including sesamolin, sesame oil, and olive oil, and a decrease in HCT116 viability in a concentration-dependent manner and selectively on cancer cells compared to non-cancerous Vero cells. The primary mode of cell death was predominantly ROS-induced necrosis, with no change in caspase 3/7 activity, indicating the absence of apoptosis. This study first presents the necrotic cell death mechanism induced by sesamolin. The findings reveal that the cCNC emulsion delivery system is safe and appropriate for transporting lipophilic chemicals and can overcome solubility limitations., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Natthida Weerapreeyakul reports financial support was provided by the National Research Council of Thailand. Reny Rosalina reports financial support was provided by Khon Kaen University. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

Background: Skin commensal bacteria (Staphylococcus epidermidis) can help defend against skin infections, and they are increasingly being recognized for their role in benefiting skin health. This study aims to demonstrate the activities that Myristica fragrans Houtt. seed extracts, crude extract (CE) and essential oil (EO), have in terms of promoting the growth of the skin commensal bacterium S. epidermidis and providing metabolites under culture conditions to disrupt the biofilm formation of the common pathogen Staphylococcus aureus., Methods: The culture supernatant obtained from a co-culture of S. epidermidis with M. fragrans Houtt. seed extracts in either CE or EO forms were analyzed using gas chromatography-mass spectrometry (GC-MS) and liquid chromatography tandem mass spectrometry (LC-MS/MS), in silico investigations, and applied to assess the survival and biofilm formation of S. aureus., Results: The combination of commensal bacteria with M. fragrans Houtt. seed extract either CE or EO produced metabolic compounds such as short-chain fatty acids and antimicrobial peptides, contributing to the antimicrobial activity. This antimicrobial activity was related to downregulating key genes involved in bacterial adherence and biofilm development in S. aureus, including cna, agr, and fnbA., Conclusion: These findings suggest that using the culture supernatant of the commensal bacteria in combination with CE or EO may provide a potential approach to combat biofilm formation and control the bacterial proliferation of S. aureus. This may be a putative non-invasive therapeutic strategy for maintaining a healthy skin microbiota and preventing skin infections., (© 2024. The Author(s).)

This study presents the employment of Fourier transform infrared (FTIR) spectroscopy with attenuated total reflection and principal component analysis (PCA) to analyze the stability of a Pickering emulsion stabilized by carboxylated-cellulose nanocrystal (cCNC) comprising sesame oil phases with or without sesamolin. FTIR measurements identified an intermolecular hydrogen bond between the ester group of the triglyceride and the carboxyl group of the cCNC to create the emulsion droplet. The spectral bands from the hydroxyl group vibration (3700-3050 cm -1 ), carbonyl (1744 cm -1 ), CO groups of the ester triglyceride and cCNC (1160-998 cm -1 ) markedly discriminated between stabilized and destabilized emulsions. The PCA of FTIR spectra detected the change of molecular interaction during storage according to creaming, aggregation, and coalescence and changes in physicochemical parameters such as droplet size, refractive index, and zeta potential. Hence, PCA enabled the observation of the destabilization of emulsion in real-time., Competing Interests: Declaration of competing interest The authors declare the following financial interests/personal relationships which may be considered as potential competing interests: Natthida Weerapreeyakul reports financial support was provided by the National Research Council of Thailand. Reny Rosalina reports financial support was provided by Khon Kaen University. If there are other authors, they declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier Ltd. All rights reserved.)

Objectives: During the coronavirus disease-2019 pandemic, masks have become mandatory for protection against the virus transmitted by breathing. This study examined the impact of surgical masks used daily on civilian facial skin., Materials and Methods: Moisture, elasticity, pore, melanin, acne, wrinkle, and sensitivity parameters of 83 volunteers were measured numerically using an API-100 skin analyzer and camera recordings. Numerical values were compared following the device's algorithm calibrated according to age, gender, and race. Finally, the obtained data were statistically evaluated and compared with the averages., Results: Pore, melanin, acne, and wrinkle parameters were higher without gender discrimination, whereas moisture and elasticity parameters were low. While a significant increase was observed in women for sensitivity, the increase was not statistically significant in men., Conclusion: The negative effects of long-term daily wearing of surgical masks on facial skin were statistically significant. Therefore, taking outdoor breaks during mask use, washing the face intermittently, using moisturizing and purifying cosmetic products, and anti-wrinkle effects have been proposed to reduce the possible defects., Competing Interests: Conflict of Interest: The authors have no conflicts of interest to declare.

Dipterocarpus alatus has been used for the treatment of infectious skin diseases and ulcerative wounds in Thai traditional medicine. A major pathogen in human superficial skin infections is methicillin-resistant Staphylococcus aureus (MRSA). This study determined the wound healing, antibacterial, and anti-inflammatory activities of D. alatus twig emulgel against MRSA-infected mouse superficial skin wounds. Ethyl acetate-methanol crude extract of D. alatus twig was incorporated into emulgel at concentrations of 20 and 40 mg/g (D20 and D40) and its activity was compared to tetracycline emulgel (160 μg/g, Tetra). MRSA-infected superficial wounds demonstrated decreased skin barrier strength, increased transepidermal water loss (TEWL), and mast cell accumulation. Expression of toll-like receptor 2 (TLR-2), NF-κβ, TNFα, IL-1β, IL-6 and IL-10 genes were induced after MRSA infection. Daily application of 100 μL of D20 or D40 for 9 days restored skin barrier strength and TEWL while reducing mast cell and MRSA numbers compared to the non-treated group (MRSA-NT). The wounds treated with D20 and D40 were entirely healed on day 9. Expression of TLR-2 and cytokine-related genes NF-κβ, TNFα, IL-1β, IL-6 and IL-10 were normalized by treatment with either D20 or D40. Therefore, emulgel containing 20 to 40 mg/g ethyl acetate-methanol crude D. alatus twig extract is a good candidate for development as a topical formulation for MRSA-infected ulcerated wounds., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2023 The Authors.)

Rice bran is a rich source of health-promoting nutrition and bioactive compounds; nevertheless, the properties of rice brans depend on cultivars, ages, and preparation methods, drawing the potential of raw materials for health benefits. Therefore, this research aimed to investigate the health-promoting properties of fermented rice bran extracts from cultivar black rice (H7F) and germinated brown rice (G13F), focusing on their prebiotic, antipathogenic bacteria activity and safety demonstrated in vitro and in vivo study models, respectively. Here, the screening of metabolites' change after rice bran fermentation by ATR-FTIR spectra revealed specific peaks corresponding to the composited components of protein, carbohydrate, and lipid. Then, in the in vitro study, the prebiotic capability of H7F and G13F extracts was demonstrated by a growth-promoting effect on Lactobacillus delbrueckii subsp. lactis under specific acidic conditions. Furthermore, antipathogenic bacterial activity against Escherichia coli and Staphylococcus aureus was presented at 25 mg/mL of MIC values and 50 mg/mL of MBC of both fermented rice bran extracts, eliminating the bacteria by interfering with the biofilm formation. For safety, an acute and chronic toxicity study using Wistar rats was conducted, in which changes in the body and organ weights, histopathology of organs, blood chemistry, and hematological parameters were observed after H7F and G13F treatment. Desirably, they showed no toxicity, with a significant reduction in blood cholesterol levels in the chronic treatment of H7F and G13F. Conclusively, the overall results evidenced the health benefits of H7F and G13F related to their prebiotic and antipathogenic bacteria properties and hypocholesterolemia potential with a high level of safety. Therefore, the fermented rice bran extracts were demonstrated as potential materials for the further development of functional ingredients and health products.

Skin hyperpigmentation is an aesthetic problem that leads to psychosocial issues. Thus, skin whitening agents from agro- and poultry-industrial co-products are considered high economic value ingredients of interest for sustainable application. Therefore, this study aimed to determine the cosmeceutical potential of anserine/carnosine-rich chicken extract (ACCE) from the Thai native chicken Pradu Hang Dam Mor Kor 55 (PD) meat. The chemical composition was identified and quantified using the HPLC-UV method. Then, the antioxidation potential of the extract was compared to that of L-anserine and L-carnosine, using 1,1-diphenyl-2-picrylhydrazyl assay and shikonin-induced production of reactive oxygen species in CCD-986Sk cell models, and the anti-melanogenesis effect in the MNT-1 melanoma cell line model was investigated. Furthermore, related mechanisms were identified using colorimetric tyrosinase assay and the Western blot technique. The ACCE was composed of L-anserine and L-carnosine as two major constituents. In a dose-dependent manner, ACCE, L-anserine, and L-carnosine manifested significant antioxidation potential and significant reduction of melanin production. Activation of the extracellular signal-regulated kinase (ERK) signaling pathway and inhibition of tyrosinase activity of ACCE were demonstrated as the mechanisms of the anti-melanogenesis effect. In conclusion, ACCE has been revealed as a potential cosmeceutical agent due to its antioxidation and anti-melanogenic activity in association with L-anserine and L-carnosine composition and biomolecular regulating ability. Therefore, further studies and development should be considered to support the utilization of anserine/carnosine-rich chicken extract in the cosmetic industry for economic value creation and sustainability.

Tamarindus indica L. or tamarind seed is an industrial by-product of interest to be investigated for its potential and value-added application. An ethanolic tamarind seed coat (TS) extract was prepared using the maceration technique and used to determine the phytochemical composition and bioactivities. The total phenolic and flavonoid contents were determined using colorimetric methods; moreover, chemical constituents were identified and quantified compared to the standard compounds using the HPLC-UV DAD technique. Bioactivities were investigated using various models: antioxidative activity in a DPPH assay model, anti-melanogenesis in B16 melanoma cells, anti-adipogenesis in 3T3-L1 adipocytes, and anti-microbial activity against S. aureus , P. aeruginosa , E. coli , and C. albican using agar disc diffusion and microdilution methods. The results manifested a high content of catechin as a chemical constituent and multiple beneficiary bioactivities of TS extract, including superior antioxidation to ascorbic acid and catechin, comparable anti-melanogenesis to deoxyarbutin, and significant anti-adipogenesis through inhibition of pre-adipocyte differentiation and reduction of lipid and triglyceride accumulation, and a broad spectral anti-microbial activity with a selectively high susceptibility to S. aureus when compared to 1% Parabens. Conclusively, TS extract has been revealed as a potential bioactive agent as well as an alternative preservative for application in food, cosmetic, and pharmaceutical product development.

The cassava root is an important global agro-industrial crop that yields cassava leaf as a left-over co-product of interest for further development as a sustainable resource of health and cosmeceutical active compounds. This work aimed to investigate the cosmeceutical potential and chemical composition of an ethanolic cassava leaf extract (BM). rutin, apigenin, and kaempferol were found to be major constituents via HPLC-DAD UV analysis. Interestingly, the multiple beneficial bioactivities of BM for cosmeceutical applications were manifested in a dose-dependent manner, including anti-oxidation in a 2,2-diphenyl-1-picrylhydrazyl assay, anti-melanogenesis in B16 melanoma cells, collagen synthesis enhancement in human fibroblasts, and anti-adipogenesis in 3T3-L1 adipocytes. Furthermore, the potential of the collagen synthesis enhancement of BM and rutin was significant when compared to ascorbic acid. Additionally, a UV filter property comparable to BEMT with characteristics of board spectral absorption and constant high absorptivity throughout all UV wavelength ranges was exhibited by UV-visible spectrophotometric analysis. In conclusion, the cassava leaf was found to be a potential natural cosmeceutical active agent with multiple cosmeceutical-related bioactivities with respect to a substantial composition of bioactive flavonols. These obtained data will support and encourage the further study and development of cassava leaves as potential economic and sustainable sources of bioactive agents for health and cosmeceutical applications.

Myristica fragrans Houtt. (Nutmeg) is a widely known folk medicine across several parts of Asia, particularly used in antimicrobial treatment. Bacterial resistance involves the expression of efflux pump systems (chromosomal nor A and mep A) in methicillin-resistant Staphylococcus aureus (MRSA). Crude extract (CE) and essential oil (EO) obtained from nutmeg were applied as efflux pump inhibitors (EPIs), thereby enhancing the antimicrobial activity of the drugs they were used in. The major substances in CE and EO, which function as EPIs, in a descending order of % peak area include elemicin, myristicin, methoxyeugenol, myristicin, and asarone. Here, we investigated whether the low amount of CE and EO used as EPIs was sufficient to sensitize MRSA killing using the antibiotic ciprofloxacin, which acts as an efflux system. Interestingly, synergy between ciprofloxacin and CE or EO revealed the most significant viability of MRSA, depending on nor A and mep A, the latter being responsible for EPI function of EO. Therefore, CE and EO obtained from nutmeg can act as EPIs in combination with substances that act as efflux systems, thereby ensuring that the MRSA strain is susceptible to antibiotic treatment.

Many studies have been conducted on the bioactive compounds of rice seeds, however, there is limited information on the bioactive compounds of rice sprouts. This study focused on the age effect on the phytochemical content of white and black glutinous rice sprouts harvested between 5 and 25 days old. We assessed yield, total phenolic content, total flavonoid content, total anthocyanin content, total chlorophyll content, and proximate analysis. HPLC results identified protocatechuic acid, vanillic acid, and rutin in the sprouts of both cultivars, ranging between 0.56-1.58, 0.65-7.69, and 0.47-1.68 mg/g extract, respectively. The amount of bioactive compounds and proximate compositions in black glutinous rice were generally higher than white glutinous rice in an age-dependent manner ( p < 0.05). At 5-7 days, black glutinous rice contained the highest total anthocyanin content, while white glutinous rice contained the highest total phenolic content and total flavonoid content ( p < 0.05). High total chlorophyll content was initially detected in white glutinous rice at a younger age than black glutinous rice ( p < 0.05), while total chlorophyll content in both cultivars was not significantly different. Our study confirms the presence of phytoconstituents in the rice sprouts of white and black glutinous rice and their potential as functional foods and for being further development as natural health products.

To investigate the anti-obesity potential of Antidesma bunius L. (MM), a Thai local fruit which is named "Mao Luang," we have focused on the effects on pancreatic α-amylase and lipase enzyme activity and on adipocyte life cycle using the 3T3-L1 cell line as a model. In addition, the phytochemical composition and anti-oxidation potential were also analyzed using HPLC-PDA UV and colorimetric methods. The ethanolic extract of MM fruits prepared by a maceration method was used in the experiments. MM extract, yield 12.08% w / w , is composed primarily of phenolics and anthocyanins as the major phytochemicals, among which, gallic acid, catechin, anthocyanin-3-glucoside, and protocatechuic acid were initially identified. In addition, susceptibly inhibitory effects on oxidation in a DPPH assay; on lipase enzyme activity rather than amylase enzyme; and on adipocyte adipogenesis of MM were demonstrated. Interestingly, a concentration-dependent bi-modular manner of activity on adipocyte adipogenesis was discovered, whereby a significant anti-adipogenic effect was demonstrated at high concentration, whilst low concentrations of MM showed adipogenic induction. Lipolytic induction was manifested. Conclusively, the ethanolic MM extract was discovered to be a potential anti-obesity agent contributed by inhibitory effects on lipase enzyme and anti-differentiation and -adipogenesis in adipocytes which significantly correlated to the total phenolics content, as well as anti-oxidation as the mechanism of action. Nevertheless, to achieve effective application, further investigation in in vivo models should be considered.

The objective of this study was to develop oral disintegrating tablet (ODT) formulations of a heptapeptide, [Lys 5 ,MeLeu 9 ,Nle 10 ]-NKA(4-10), for the treatment of neurogenic bladder dysfunction. A design of experiment approach was applied to determine the optimal ratio of chosen excipients: gelatin (X 1 ), glycine (X 2 ), and sorbitol (X 3 ). These formulations were optimized for efficacy studies to produce ODTs exhibiting rapid disintegration times (Y 1 ) and appropriate structural integrity (Y 2 ) using JMP ® 12.0.1 software. Based on theoretically predicted values from 12 experimental runs, the optimal ODT formulation was determined to be 3% (w/v) gelatin, 2% (w/v) glycine, and 1% (w/v) sorbitol in deionized water. Using this formulation, blank and drug-loaded ODTs containing 1.5 mg or 5 mg of [Lys 5 ,MeLeu 9 ,Nle 10 ]-NKA(4-10) were manufactured by a lyophilization process. The peptide-loaded tablets disintegrated in less than 30 s and released 97% of the peptide within 15 min. The peptide was stable for 90 days under 25 °C/60% relative humidity (RH) and 40 °C/75% RH. In vivo efficacy of the peptide-loaded ODTs was confirmed in a rat acute spinal cord injury model under isovolumetric bladder pressure recording conditions, concluding that sublingual administration of peptide-containing ODTs evoke a rapid dose-related neurokinin 2-mediated increase in bladder pressure., (Copyright © 2017 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Corn silk or the stigma of Zea mays L. has traditionally been used in weight loss stimulation and treatment of cystitis, urinary infections and obesity. Purple corn silk, rich of polyphenolic substances, was reported on anti-diabetic and anti-obesity effect in animal studies. However, scientific evidence on mechanisms and targets of action of purple corn silk related to adipocyte life cycle has been limited., Aim of Study: To determine phytochemical compositions and investigate anti-obesity potential of the purple corn silk focusing on interruption of adipocyte life cycle; effect on pre-adipocyte proliferation, adipogenesis, adipocyte lipolysis, and apoptosis., Materials and Methods: The ethanolic purple corn silk extract (PCS) was prepared and investigated for phytochemical compositions by LC/MS/MS technique and anti-obesity potential using murine 3T3-L1 cell line. Using methyl thiazole tetrazolium (MTT) assay, the effects on pre-adipocytes and adipocyte viability and on pre-adipocytes proliferation at 24-, 48-, and 72-h incubation period were evaluated. In addition, anti-adipogenesis via inhibition on adipocyte differentiation and reduction of total lipid accumulation was evaluated using Oil Red O staining and spectrophotometric methods, respectively. The lipolysis effect was determined by measurement of glycerol released content using glycerol test kit after 48-h treatment of PCS to adipocytes. Apoptosis inductive effect was done by using 2-(4-Amidinophenyl)-6-indolecarbamidine dihydrochloride (DAPI) staining method., Results: The polyphenols including anthocyanins, quercetin and phenolic acids and derivatives were found as the major chemical compositions of the PCS. With multiple-stages interruption on the adipocyte life cycle, anti-obesity effect of PCS was interestingly demonstrated. When compared to the control, the PCS at concentration range between 250-1000 μg/mL showed anti-adipogenesis effect as expressing of significant inhibition on pre-adipocyte proliferation at all incubation period (43.52±5.28 - 75.51±9.09%) and significant decreasing of total lipid accumulation at concentration of 500μg/mL (80.22±6.58%) and 1000μg/mL (69.62±5.42%). Moreover, the PCS exhibited lipolysis and apoptosis inductive effect with dose dependent manner and significance at concentration of 1000μg/mL by increase of released glycerol content (173.88±6.13% of the control) and of nuclei condensing and apoptotic bodies (with relative apoptosis induction as 131.74±1.64% of the control)., Conclusion: Our data has evidenced the anti-obesity potential of PCS related interruption at multiple stages of adipocyte life cycle. Its potency was attributed to inhibition on adipocyte proliferation and adipogenesis as well as induction on lipolysis and apoptosis at high concentration. However, further in vivo investigation should be considered to insist the possibility in applications of PCS in prevention and treatment of obesity., (Copyright © 2017 Elsevier Ireland Ltd. All rights reserved.)

Extracts of Kaempferia parviflora (KP) were formulated in solid lipid nanoparticles (SLNs) in order to enhance their transdermal permeability. The KP extracts were entrapped within SLNs by adding them to a melted mixture of oils, surfactants and PEGylating agents and subsequently forming an oil-in-water microemulsion at an elevated temperature. Cooling of this microemulsion resulted in the formation of SLNs. The formulation with the optimum properties was composed of stearyl alcohol as the nanoparticle matrix and Tocopheryl Polyethylene Glycol Succinate (TPGS) as the surfactant. Particle sizes of 82-108 nm were obtained with entrapment efficiencies as high as 87%. The release of the flavonoids from the SLN matrix was measured after suspending them in a Phosphate Buffered Saline (PBS)/Tween 80 solution and demonstrated biphasic patterns. Permeability studies using a skin model composed of human-derived epidermal keratinocytes were conducted in which a topically applied KP extract-loaded SLN was compared to a KP-hydroxypropyl methylcellulose/Tween 80 gel formulation containing KP extract. The amount of total KP flavonoids in the SLNs and gel that had permeated through the skin after 25 hours (95.57 +/- 9.08 and 81.04 +/- 5.82 g, respectively) were found to be significantly different (P < 0.05). In addition, the flux values of three of the flavonoids were greater when incorporated in SLNs.

In this study, the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on multidrug resistance associated-proteins (MRP)-mediated transport in A549 cells were examined. The cells employed express MRP1 and MRP2, but not P-glycoprotein. The cellular accumulation of calcein, an MRP substrate, was significantly increased by various MRP inhibitors without being affected by verapamil, a typical P-glycoprotein inhibitor. Ethanol and aqueous extracts from K. parviflora rhizome increased the accumulation of calcein and doxorubicin in A549 cells in a concentration-dependent manner. The inhibitory potency of the ethanol extract for MRP function was greater than that of the aqueous extract. Among six flavone derivatives isolated from K. parviflora rhizome, 5,7-dimethoxyflavone exhibited a maximal stimulatory effect on the accumulation of doxorubicin in A549 cells. The accumulation of doxorubicin was increased by four flavone derivatives without 5-hydroxy group, but not by the other two flavone derivatives with 5-hydroxy group. In addition, 5,7-dimethoxyflavone and 3,5,7,3',4'-pentamethoxyflavone decreased resistance to doxorubicin in A549 cells. These findings indicate that extracts and flavone derivatives from the rhizome of K. parviflora suppress MRP function, and therefore may be useful as modulators of multidrug resistance in cancer cells.

The purpose of this study was to examine the effects of extracts and flavone derivatives from the rhizome of Kaempferia parviflora on P-glycoprotein (P-gp)-mediated transport in LLC-GA5-COL150, a transfectant cell line of a porcine kidney epithelial cell line LLC-PK1 with human MDR1 cDNA. Ethanol extract obtained from Kaempferia parviflora rhizome significantly increased the accumulation of rhodamine 123 and daunorubicin, P-gp substrates, in LLC-GA5-COL150 cells, but not in LLC-PK1 cells. The aqueous extract also increased the accumulation in LLC-GA5-COL150 cells with lower potency than the ethanol extract. The effects of flavone derivatives isolated from the rhizome of Kaempferia parviflora on P-gp function were examined. Among six flavones tested, 3,5,7,3',4'-pentamethoxyflavone most potently increased the accumulation of rhodamine 123 and daunorubicin in LLC-GA5-COL150 cells in a concentration-dependent manner. In addition, 5,7-dimethoxyflavone to lesser degree increased rhodamine 123 accumulation in LLC-GA5-COL150 cells. In contrast, the other four flavone derivatives had no significant effect on the accumulation of rhodamine 123 in LLC-GA5-COL150 cells in a concentration range tested. These results indicate that extracts and flavone derivatives from the rhizome of Kaempferia parviflora can inhibit P-gp function, which may be useful for overcoming P-gp-mediated multidrug resistance and improving the oral bioavailability of anticancer agents., ((c) 2006 Wiley-Liss, Inc. and the American Pharmacists Association.)

In this article, we use a nanotemplate engineering approach to prepare biodegradable nanoparticles composed of FDA-approved materials and possessing accessible gadolinium (Gd) atoms and demonstrate their potential as a Magnetic Resonance Imaging (MRI) contrast agent. Nanoparticles containing dimyristoyl phosphoethanolamine diethylene triamine penta acetate (PE-DTPA) were prepared using 3.5 mg of Brij 78, 2.0 mg of emulsifying wax and 0.5 mg of PE-DTPA/ml from a microemulsion precursor. After the addition of GdCl3, the presence of Gd on the surface of nanoparticles was characterized using inductively coupled plasma atomic emission spectroscopy and Scanning Transmission Electron Microscopy (STEM). The in vitro relaxivities of the PE-DTPA-Gd nanoparticles in different media were assessed at different field strengths. The conditional stability constant of Gd binding to the nanoparticles was determined using competitive spectrophotometric titration. Transmetallation kinetics of the gadolinium ion from PE-DTPA-Gd nanoparticles with zinc as the competing ionic was measured using the relaxivity evolution method. Nanoparticles with a diameter of approximately 130 nm possessing surface chelating functions were made from GRAS (Generally Regarded As Safe) materials. STEM demonstrated the uniform distribution of Gd3+ on the surface of the nanoparticles. The thermodynamic binding constant for Gd3+ to the nanoparticles was approximately 10(18) M(-1) and transmetallation studies with Zn2+ yielded kinetic constants K1 and K(-1) of 0.033 and 0.022 1/h, respectively, with an equilibrium constant of 1.5. A payload of approximately 10(5) Gd/nanoparticle was achieved; enhanced relaxivities were observed, including a pH dependence of the transverse relaxivity (r2). Nanoparticles composed of materials that have been demonstrated to be hemocompatible and enzymatically metabolized and possessing accessible Gd ions on their surface induce relaxivities in the bulk water signal that make them potentially useful as next-generation MRI tumor contrast enhancement agents.