Key Engineering Materials Vol. 901

Abstract: Hepatocellular carcinoma (HCC) is a major public health problem and the leading cause of death of people around the world with a tendency to increase every year, leading to a large investigation on the development of HCC drugs. In this work, novel sorafenib derivatives containing 1,2,3-triazole moiety, M1-M5 were designed as potential HCC cancer inhibitors by targeting B-rapidly accelerated fibrosarcoma (B-RAF) and vascular endothelial growth factor receptor 2 (VEGFR-2). The bindings of M1-M5 in the cavity of B-RAF and VEGFR-2, which are kinases related to HCC cell growth, were investigated by molecular docking using iGEMDOCK v2.1 software. The results illustrated that M1-M5 bound in the binding site of B-RAF and VEGFR-2 in a similar manner to sorafenib. It was also found that the 1,2,3-triazole moiety of M1-M5 interacted well by hydrogen bonding with key amino acids in the binding site of B-RAF and VEGFR-2 which could inhibit the cancer cell growth. Although the binding energies of M1-M5 in B-RAF (-148.51 to -126.19 kcal/mol) were rather higher to that of sorafenib (-176.75 kcal/mol), the binding energies of M1-M5 in VEGFR-2 (-127.00 to -116.48 kcal/mol) were comparable to that of sorafenib (-127.03 kcal/mol). As a result, M1-M5 containing 1,2,3-triazole moiety were promising molecules to study in vitro on VEGFR-2 inhibitory assay and be leading compounds for the development as the anticancer drugs against HCC in the future.

Abstract: Palmyra (Borassus flabellifer Linn.) palm fruits are bright yellow and have a unique sweet scent. The ripe palm fruits are a rich source of carotenoids which are used as a non-toxic natural dye and have been recognized for their antioxidant benefits. This study aimed to explore the potential of palm fruit extract as a natural coloring agent. The ripe mesocarp of B. flabellifer was extracted using various organic solvents. The carotenoid content, polysaccharide composition, and antioxidant activity of the palm extracts were investigated. The ethanolic palm extract was selected for stability study in various conditions (pH, time, light, and temperature). Then, the extracted nanoemulsion loaded with B. flabellifer extract was formulated and evaluated. The ethanolic extract from the freeze-dried sample yielded high extractive content (42.9%) and showed the greatest antioxidant activity (IC₅₀ 2.4 mg/mL). The color intensity of the extract did not fade after exposure to a pH of more than 4. After the storage for 14 days, the color intensity significantly decreased. The light exposure did not influence the color intensity at 25°C. B. flabellifer ethanolic extracted nanoemulsions were successfully prepared by ultrasonication method with the oil to surfactant weight ratio of 1:9. The nanoemulsions loaded with ethanolic extract were stable. The nanoemulsion of the pulp extract could potentially be used as a natural dye.

Abstract: Phlogacanthus pulcherrimus T. Anderson (PPT) is an edible plant found in the northern and northeastern regions of Thailand. There is limited information about the anti-breast cancer activity of the ethanolic leaf extract of PPT. This study aimed to evaluate the effects of an ethanolic leaf extract of PPT on MCF-7 breast cancer cell lines. The biological effects, including cytotoxicity, cell apoptosis, colony formation, reactive oxygen species (ROS) formation and cell migration, were determined by a means of sulforhodamine B (SRB), acridine orange/ethidium bromide (AO/EB) staining, a clonogenic assay, flow cytometry and a scratch wound healing assay, respectively. The results demonstrated that the PPT extract showed cytotoxic on MCF-7 cells in a dose-dependent manner with 50% inhibitory concentration (IC₅₀) values of 119.9 ± 12.1 and 51.3 ± 4.7 μg/mL at 24 h and 48 h incubation, respectively. In addition, the extract exhibited cell apoptosis in a dose-dependent manner when used at a concentration of 50–100 μg/mL and inhibited colony formation with an IC₅₀ value of 26.0 ± 2.0 μg/mL when compared with the control group. The extract induced ROS formation in a dose-dependent manner when used at a concentration of 50–100 μg/mL. The extract suppressed MCF-7 cell migration, with significant effect at 25 μg/mL. These results indicate that PPT ethanolic leaf extract has an anticancer activity against MCF-7 breast cancer cells and may be useful for prevention and treatment of breast cancer.

Abstract: Dictyophora indusiata known as bamboo mushroom is an edible mushroom in Genus Dictyophora, Family Phallaceae that could produce highly viscous mucilage encased in the peridium. The viscous mucilage is clear-colorless hydrocolloid with high viscosity and high adhesive nature which made it possible to be developed into pharmaceutical excipients. This research work aimed at the application of the mucilage as a tablet binder. The mucilage was prepared as redispersible powder by lyphilization before used. The dried mucilage could be effectively used as a binder in paracetamol tablet formulations both as dry and wet binder. Increasing of the dried mucilage amount caused the stronger tablet with higher disintegration time. The optimum concentrations of the dried mucilage in tablet formulations were 2.0% w/w as dry binder and 1.0% w/w as wet binder. The obtained tablets revealed low friability and fast disintegration time. The drug dissolution was conformable to USP37 standard and comparable to that of commercial product. Accordingly, the Dictyophora indusiata mucilage could be functionally used as a tablet binder

Abstract: The objective of this research aimed to 1. formulate chewable toothpaste tablets containing mangosteen rind extract, 2. compare the suitable filler between lactose anhydrous and mannitol that adsorbs mangosteen rind extract by flowability and appearance indicators, 3. study the effect of type and amounts of foaming agents on stability of foam that leads to appropriate formulation, and 4. study market feasibility of chewable toothpaste tablets containing mangosteen rind extract. Survey method and self-administered questionnaire was used for data collection both before and after formulation in capital district of Nakhon Pathom. Thirty participants were selected and categorized into five groups which are tourists, dental patients, pharmacy students at Silpakorn University, office workers and dentists. After data collection is done, it was analyzed by using descriptive statistics. Results showed that mannitol is an appropriate adsorbent. It showed proper color and appearance as well as good flowability of extract. Cocamidopropyl betaine was selected as foaming agent. According to the survey, participants are interested in product. In addition, some dental specialists suggested to add fluoride. Overall, this product is interested and accepted among participants. Therefore, consumers are likely to buy chewable toothpaste tablet containing mangosteen rind extract.

Abstract: The amorphous solid dispersions (ASDs) containing amino methacrylate copolymer and surface-active agents were prepared to improve the nifedipine (NDP) dissolution. The different types of surface-active agent i.e., polysorbates 80, sodium lauryl sulfate (SLS) and polyethylene glycol (PEG) 400 were used. In order to evaluate the ASDs formulation,powder X-ray diffractometry and thermal analysis to characterize NDP crystallinity in ASDs and the dissolution study of NDP have been performed to compare the dissolution profiles. The ASDs were kept for 6 months to investigate the stability. In the X-ray diffraction pattern, no peak was observed in all samples of ASDs. No peak was found in sample of all ASDs from the thermograms. These results suggest that the drug may be molecularly dispersed in matrix of amino methacrylate copolymer. The drug dissolution at 120 min, from ASDs without surface-active agent and NDP powder were 58.31% and 17.95%, respectively. The dissolved NDP from ASDs composed of SLS, polysorbate 80 and PEG400 were 96.25%, 88.86% and 75.32%, respectively. These results may occur due to the reduction of surface tension, the addition of the low amount of high efficiency of surface-active agent e.g., SLS (compared with PEG400 and polysorbate 80) provided the higher NDP dissolution. The content analysis of NDP in selected ASDs was studied at the end of 3 and 6 months, the NDP content remained unchanged after storage.

Abstract: Mangiferin, a polyphenol of C-glycosylxanthone, exhibits various bioactivities with poor aqueous solubility. It is known as a potent antioxidant, which leads to remarkable UV protection and anti-aging properties. Mangiferin can be found in many plant species, among which the mango leaf is one of the primary sources. From our study, the extraction yield of mangifein obtained from the leaves of Mangifera indica L. variety Nam Doc Mai was 3.17% with 95.02% ± 0.064 purity (HPTLC analysis). The solubility of mangiferin in the studied pure solvents arranging in descending order were ethoxydiglycol, dimethyl isosorbide, polyethylene glycol 400, polyethylene glycol 600, propylene glycol, dipropylene glycol, glycerin, isopentyldiol, methanol, ethanol and water, whereas the addition of the solvent in water could increase the aqueous solubility of mangiferin. In several cases, the solubility was apparently higher than that dissolved in its pure solvent state. The log-linear solubility model for the cosolvent system was used to calculate the volume fractions of the selected solvents needed to solubilize mangiferin content at the twenty times of the IC₅₀ against DPPH radicals. In conclusion, the developed aqueous formulation contained 0.5% w/v of mangiferin and 20% w/v of polyethylene glycol 600 or dipropylene glycol as a solubilizer in water.

Abstract: “Mild” oral care products are needed by some groups of people, such as radiotherapy patients. This study developed oral cleansing products containing green tea (Camelia sinensis (L.) Kuntze) extracts with antibacterial activities and Centella asiatica (L.) Urb. extracts with a wound healing activity. We found that 3.13 mg/ml of green tea extract inhibited both Streptococcus mutans and Candida albicans, which can cause dental caries and oral candidiasis, respectively. Also, a 16 μg/ml C. asiatica extract promoted fibroblast migration in a wound healing study. The products were developed in 2 dosage forms, i.e. a solution and an impregnated gauze, which were isotonic, alcohol and volatile oil free formulations to prevent irritation and burning sensations. The products showed acceptable physical stability after testing under stressed conditions with post-test retention of antimicrobial activity.