Background: The objective of this study was to make colloidal dispersions of the active compounds of radix of Angelica gigas Nakai that could be charaterized as nano-composites using hot melt extrusion (HME). Food grade hydrophilic polymer matrices were used to disperse these compound in aqueous media.
Methods and Results: Extrudate solid formulations (ESFs) mediated by various HPMCs (hydroxypropyl methylcelluloses) and Na-Alg polymers made from ultrafine powder of the radix of Angelica gigas Nakai were developed through a physical crosslink method (HME) using an ionization agent (treatment with acetic acid) and different food grade polymers [HPMCs, such as HP55, CN40H, AN6 and sodium alignate (Na-Alg)]. X-ray powder diffraction (XRD) analysis confirmed the amorphization of crystal compounds in the HP55-mediated extrudate solid formulation (HP55-ESF). Differential scanning calorimetry (DSC) analysis indicated a lower enthalpy (ΔH = 10.62 J/g) of glass transition temperature (Tg) in the HP55-ESF than in the other formulations. Infrared fourier transform spectroscopy (FT-IR) revealed that new functional groups were produced in the HP55-ESF. The content of phenolic compounds, flavonoid (including decursin and decursinol angelate) content, and antioxidant activity increased by 5, 10, and 2 times in the HP55-ESF, respectively. The production of water soluble (61.5%) nano-sized (323 ㎚) particles was achieved in the HP55-ESF.
Conclusions: Nano-composites were developed herein utilizing melt-extruded solid dispersion technology, including food grade polymer enhanced nano dispersion (< 500 ㎚) of active compounds from the radix of Angelica gigas Nakai with enhanced solubility and bioavailability. These nano-composites of the radix of Angelica gigas Nakai can be developed and marketed as products with high therapeutic performance.
Background : The Kenaf (Hibiscus cannabinus L.) is an annual plant rich in phenolics compound and antioxidant activity. Particle size has an enormous effect on extraction of plant bioactive compound. Therefore, to evaluate the optimum particle size on extraction of bioactive compound from Kenaf was investigated.
Methods and Results : Three kind of kenaf leaves; EF-1 and G-1 from Israel and Korea were collected in 2016 and the collected leaves were dried and pulverized are sorted by particle size. After adding 50 ㎖ of 100% ethanol per 0.5 ㎎ of the powder, the powder is extracted in an ultrasonic bath at 30℃ for 1 hour and then stirred for 1 hour at 250 rpm in the wise stirring. After extraction, the extract was filtered using filter paper. In the total polyphenol, flavonoid and antioxidant activity were higher in 100 to 200 ㎛ particle size of Gandae. On the other hand, phenolic compound, falvonoud and antioxidant were higher in 45 to 100 ㎛ particle size of EF-1 and G-1 Kenaf.
Conclusion : Based on the results, the Israel varieties showed the best results compared to the Kenaf varieties of Korea. Among them, EF-1 had a particle size of 45 – 100 ㎛ Showed the higher antioxidant activity. It is believed that the smaller the particle size, the larger the specific surface area, which leads to an increase in the extraction efficiency of kenaf.
Background : The Kenaf (Hibiscus cannabinus L.) is an annual plant of African and Indian origin. and there are a lot of flavonoids in the leaves. To determine the most suitable method for extracting of Kenaf cosmetic ingredients, the data of changes in polyphenol, flavonoid contents and DPPH radical scavenging activities were analyzed, based on concentration of Extraction Methods.
Methods and Results : 200 ㎖ of distilled water (100% ethanol in the case of ethanol extraction) was added to 20 g of the leaves of Kenaf; G-1 from Israel were collected in 2016 and the collected leaves were dried and pulverized, and five extraction methods were performed. The extraction method and conditions are as follows: pressurized high temperature extraction (AE: autoclave, 121 degrees, 15 minutes), ultrasonic extraction (UE: ultrasonic bath, 60 degree hot water, 1 hour), Hot water extraction (SE: spidulina mayina. 100 degrees 6 hours), Ethanol Extraction (EE: ethanol, spidulina mayina, 80 degrees 6 hours), room temperature stirring extraction (WSE: wise stirring, room temperature 250rpm 24 hours). After extraction, the mixture was filtered using a filter paper, and concentrated under reduced pressure at 40℃ for lyophilization. And diluted to 1,000 ppm with 80% ethanol.
Conclusion : Based on the test results, EE method showed the highest results. In the case of using water as the solvent, the SE method showed the highest result. However, the results of the SE and AE methods are not significantly different from each other. Therefore, it is expected that if the extraction conditions of AE method are adjusted, the result of AE method will be higher than that of the SE method.
Background : The root of Angelica gigas Nakai is used as a traditional herbal medicine in Korea for the treatment of many diseases. Poor water solubility of the active compounds from A. gigas Nakai is a major obstacle to bioavailability.
Methods and Results : This work aimed to enhance the solubility of active compounds by a chemical (viz. surfactant) and physical (HME, hot melt extrusion) crosslinking method (CPC) in A. gigas Nakai. Infrared fourier transform spectroscopy (FT-IR) revealed multiple peaks in extrudate solids representing new functional groups including carboxylic acid, alkynes and benzene derivatives. Differential scanning calorimetry (DSC) analysis of the extrudate showed lower glass transition temperature (Tg) and lower enthalpy (ΔH) [Tg: 43℃; ΔH: <6 (J/g)] compared to the non-extrudate (Tg 68.5℃; ΔH: 123.2) formulations. X-ray powder diffraction (XRD) analysis revealed amorphization of crystal materials in extrudate solid. In addition, enhanced solubility (53%), nanonization (403 ㎚), and higher amount of extracted phenolic compounds were achieved in the extrudate solid compared to non extrudate (36%, 1499 ㎚, respectively). Among the different extrudates, acetic acid and span 80 mediated formulations showed superior extractions efficiency.
Conclusion : We conclude that the HME successfully enhanced the production of amorphous nano dispersions of phenolic compound including decursin from extrudate solid formulations. human dermal fibroblasts, which is, associated with the regulation of procollagen biosynthesis resulting from AMRP-induced TGF-β1 expression and the mitogenic activity in HDF cells, and therefore, is expected to reduce the age-dependent loss of extracellular matrix proteins.
Background: The root of Angelica gigas Nakai is used as a traditional herbal medicine in Korea for the treatment of many diseases. However, the poor water solubility of the active components in A. gigas Nakai is a major obstacle to its bioavailability.
Methods and Results: This work aimed at enhancing the solubility of the active compounds of A. gigas Nakai by a chemical (using a surfactant) and physical (hot melt extrusion, HME) crosslinking method. Fourier transform infrared spectroscopy revealed multiple peaks in the case of the extrudate solids, attributable to new functional groups including carboxylic acid, alkynes, and benzene derivatives. Differential scanning calorimetry analysis showed that the extrudate soilid had a lower glass transition temperature (Tg) and enthalpy (ΔH) (Tg : 43℃, ΔH : < 6 J/g) as compared to the non-extrudate (Tg : 68.5℃, ΔH : 123.2) formulations. X-ray powder diffraction analysis revealed the amorphization of crystalline materials in the extrudate solid. In addition, enhanced solubility (53%), nanonization (403 ㎚), and a higher amount of extracted phenolic compounds were achieved in the extrudate solid than in the non-extrudate (solubility : 36%, nanonization : 1,499 ㎚) formulation. Among the different extrudates, acetic acid and span 80 mediated formulations showed superior extractions efficiency.
Conclusions: HME successfully enhanced the production of amorphous nano dispersions of phenolic compound including decursin from extrudate solid formulations.
Background : Zinc (Zn) is one of dietary micronutrients and it is second highest trace element in the body. Over 95% of Zn is located in the cells, but its dominant storage site is absent in the body. Deficiency of Zn may result in anorexia, dysgeusia, dysosmia, skin rash, infection, alopecia, growth failure, and impaired wound healing. Therefore, adequate supplementation of Zn is very important to maintain normal physiological conditions.
Methods and Results : Zinc sulfate monohydrate (ZnSO4)-loaded nanocomposites (NCs) were fabricated by using a hot-melt extruder (HME) system. Soluplus (SP) was adopted as an amphiphilic polymer matrix for HME processing. The micro-size of ZnSO4 dispersion was reduced to nano-size by HME processing with the use of SP. ZnSO4 could be homogeneously dispersed in SP through HME processing. ZnSO4/SP NCs with a 75 ㎚ mean diameter, a 0.1 polydispersity index, and a -1 mV zeta potential value were prepared. The physicochemical properties of ZnSO4/SP NCs and the existence of SP in ZnSO4/SP NCs were further investigated by solid-state studies. Nano-size range of ZnSO4/SP NC dispersion was maintained in the simulated gastrointestinal environments (pH 1.2 and 6.8 media). No severe toxicity in intestinal epithelium after oral administration of ZnSO4/SP NCs (at 100 ㎎/㎏ dose of ZnSO4, single dosing) was observed in rats.
Conclusion : These results imply that developed ZnSO4/SP NC can be used as a promising nano-sized zinc supplement formulation. In addition, developed HME technology can be widely applied to fabricate nano formulations of inorganic materials.
Background : The Kenaf (Hibiscus cannabinus L.) is an annual plant of African and Indian origin. and there are a lot of flavonoids in the leaves. To determine the most suitable method for extracting of Kenaf cosmetic ingredients, the data of changes in polyphenol, flavonoid contents and DPPH radical scavenging activities were analyzed, based on concentration of surfactants and Extraction Methods.
Methods and Results : The effect of autoclave extraction (AE) and ultrasonification extraction USE) with hydrophilic surfactant that is Brij35 diluted 15, 25 and 35 mM with water on antioxidant activity of Kenaf was investigated. The leaves of Kenaf; R from Israel were collected in 2016 and the collected leaves were dried and pulverized. The highest polyphenol content of Kenaf extracted was 47.54 ㎎/㎖ as Brij35 20 mM extract from AE after USE. The highest flavonoid content of Kenaf was 20.01 ㎎/㎖ as Brij35 25 mM extract from AE. The Brij35 20 mM extract from AE after USE showed higher DPPH radical scavenging activity than that of the other treatments.
Conclusion : Based on the test results, the extracts obtained by AE or AE after USE showed excellent antioxidant activity and effective component than extracts by USE. The results of the DPPH radical scavenging activity and total polyphenol content of the extracts obtained by AE after USE than AE were slightly improved, but there was no significant difference. Therefore, it is considered that the extract obtained by autoclave extraction most effective for use as a cosmetic ingredient.
The aim of this study was to determine the suitability of surfactant to extract higher phenolic compound, flavonoid and antioxidant activity from Tartary buckwheat and evaluate the potentiality of surfactant as a screening agent for breeding purpose. Primarily, we employed two types of surfactant (Hydrophilic: Tween 20 and Lipophilic: Span 80) to select the suitable surfactant agent for the extraction of optimum bioactive compounds. Between two surfactants, Tween 20 showed highest efficiency at 4 mM concentration to extract total phenolic content (TP), total flavonoid (TF) and antioxidant activity (AA). Tween 20 at 4 mM concentration was fixed for further analysis along with hot water (90℃) treatment as a control. In our findings, highest TP (118 ㎎/g), TF (38 ㎎/g) and AA (76%) was achieved in KW21 and KW22 among the fifteen accessions of Tartary buckwheat. In other way, TP, TF and AA was 200%, 120% and 110% higher in surfactant formulation compared with control treatment, respectively.
Background : Cu ion is an essential mineral of animal feed. But rapid degradation of Cu ion in animal intestine causes poor immune activity and potential environment hazard. Therefore, to enhance immune system and control metal ion deliverly in intestine, we developed Cu ion nano suspension. In animal feed, > 127 ㎎/g of Cu ion are found but only 5 - 7 ㎎ are used out of them. Therefore, huge loss of Cu ion causes environment, economy and animal health problem. Methods and Results : Seven formulation were prepared to prepare nano suspension (particle size < 200 ㎚) of CuSO4. The particle diameter, polydispersity index, and zeta potential values of the samples were measured using dynamic light scattering (DLS) and laser Doppler methods (ELS-Z1000; Otsuka Electronics, Tokyo, Japan). Absorbance and Cu ion concentration was measured using UV-VIS Spectrophotometer. Cu ion nano particle (< 200 ㎚) was found in a formulation comprised of Cu ion : surfactant (lipophilic : hydrophilic) and PEG. In consistence with this result, total absorbance and concentration was found higher in the same formulation compared to control. Conclusion : From our experiment we may conclude that mixture of Cu ion : surfactant (lipophilic : hydrophilic) and PEG successfully prepared nano suspension which slow down the degradation of Cu ion in intestine with improving feed quality, animal health and prevent potential environment pollution.
Background : Kenaf (Hibiscus cannabinus L.) is a member of the malvaceae family and has been prescribed in traditional folk medicine in Africa and India. It showed broad biologicas activities such as hepatoprotective activity, antioxidative activity and haematinic activity. Kenaf leaves contain a lot of vegetable calcium, protein, iron and vitamins, so have high potential as functional food. Thus, the present study purposed to analyze useful substances contained in kenaf leaves and their activities and look for their possibilities as the materials of food and medicine. Methods and Results : We sowed the seeds of three varieties of kenaf, namely, Dowling, Everglade-41 and Tainung-2 at planting space of 20 × 20㎝ on the field and collected plants on the 98th , 127th and 141st days from sowing. The total polyphenol content was measured using a slightly modified Folin-Denis method, which uses the phenomenon that a phenolic substance turns blue by reaction with phosphomolybdate. Conclusion : We analyzed SOD enzyme activity related to the scavenging of superoxide anion radical (․O2-) through NBT reduction. As for the SOD activity of leaf extract by variety, the activity was 92.6%, 91.0% and 92.6%, respectively, in Tainung-2 on day 98, 127 and 141 from sowing, slightly higher than those in the other two varieties but not significantly different. The activity was slightly higher in the middle period of growth than in the harvest period, but not much different according to harvest time. As for the DPPH radical scavenging activity of leaf extract by variety, the activity was 80.87% and 80.71%, respectively, in Tainung-2 on day 98 (30th of October)and day127 (28th of September), slightly higher than the other two varieties.
Background : Buckwheat (Fagopyrum spp.) is an annual crop belonging to the polygonaceae family and cultivated in most of Asian and European countries. Nowadays, many people take interest in the utilization of buckwheat seed because of its high nutritional and pharmaceutical values. Especially, tartary buckwheat is drawing attention for its high rutin content, which is beneficial to health. Methods and Results : Tartary buckwheat sprout (TBS) was powdered and two grams of powder was mixed with 4 ㎖ H2O in a glass petri disc (100 x 20 ㎜) and exposed to far infrared irradiation (FIR) at different temperature (80, 100, 120, 140, 160℃) for an hour each. Further, the FIR treated powdered sprout samples were suspended in 200 ㎖ of 80% ethanol (v/v) and kept overnight in a shaker at room temperature. The extracts were filtered through Advantec 5B Tokyo Roshi Kaisha Ltd., Japan and dried using a vacuum rotatory evaporator (EYLA N-1000, Tokyo, Japan) in a 40℃ water bath. Dried samples were weighed and kept at 4℃ for further analysis. Conclusion : Total polyphenol was evaluated by Folin-Ciocalteau assay and total flavonoid by aluminum nitrate colorimetric assay, while antioxidant properties were evaluated based on DPPH free radical scavenging activity, metal chelating property and total antioxidant capacity. This study showed that FIR treatment to TBS caused a decrease in total antioxidant capacity and metal chelation property. However, there was a slight increase in total polyphenol and total flavonoid content from 80 to 120℃. Similarly, DPPH free radical scavenging activity also increased in the same way as TP and TF in TBS. The HPLC result revealed that quercetin production was directly proportional to temperature, and the production (average 14.87 ㎎/g dw) of quercetin was highest at 120℃ (an hour’s treatment), which was 13.54 times higher than the control in TBS.
Background: Purple potato contain sufficient phenolic compound and flavonoid which has high antioxidant capacity. Due to poor water solubility of phenolic compounds and quick oxidation of anthocyanin, we could not get maximum health benefits from purple potato. Therefore, we developed surfactant based aqueous nano suspension to enhance the solubility of phenolic compounds and protect the oxidation of anthocyanin from purple potato. Methods and Results: Two types of surfactant were used in this experiment based on hydrophilic-lycophilic balance viz. Brij and Span. In our study, lycophilic surfactant showed highest efficiency in TP extraction compared to water and lipophilic surfactant below 10 mM concentration. On the other hand, lipophilic surfactant showed highest efficiency in extracting flavonoid content. Conclusion: It is concluded that hydrophilic surfactant was significantly increased phenolic compounds five times, and lipophilic surfactant increased flavonoid two times, and anthocyanin three times compared to control. Therefore, total antioxidant capacity was increases two times compared to control.
Background : Angelica gigas is a biennial or short lived perennial plant found in China, Japan, and Korea. The root of Angelica gigas has been used in oriental traditional medicine and is marketed as a functional food product in Europe and North America. Cham-Dang-Gui (Korean Angelica, the dried root of Angelica gigas Nakai (AGN)) has been principally cultivated in Korea and used as a Korean medicinal herb. It contains several chemicals, such as pyranocoumarins, essential oils, and polyacetylenes. Methods and Results : Fresh Angelica gigas Nakai was purchased from Pyeongchang (Korea). Standard samples of D, DA were obtained from Korea Promotion Institute for Traditional Medicine Industry (Gyeongsan, Korea). Soluplus was purchased from BASF (Ludwigshafen, Germany). AGN was dried in the oven at 55°C for 24 h and cooled at room temperature. The AGN sample was then stored at 4°C until milling. Oral solid formulations based on Angelica gigas Nakai and Soluplus were prepared by the hot melt extrusion (HME) method. AGN was pulverized into coarse and ultrafine particles, and their particle size and morphology were investigated. Ultrafine AGN particles were used in the HME process with high shear to produce AGN-based formulations. In simulated gastrointestinal fluids (pH 1.2 and pH 6.8) and water, significantly higher amounts of the major active components of AGN, decursin (D) and decursinol angelate (DA), were extracted from the HME-processed AGN/Soluplus group than the AGN EtOH extract group (p < 0.05). Based on an in vivo pharmacokinetic study in rats, the relative oral bioavailability of decursinol (DOH), a hepatic metabolite of D and DA, in administered mice was 8.75-fold higher than in AGN EtOH ext-treated group. Conclusion : Soluplus-included solid formulation prepared by HME can be a promising carrier for oral delivery of phytochemicals. These findings suggest that HME-processed AGN/Soluplus formulation could be a promising therapeutic candidate for oral bioavailability.
The aim of this investigation was to examine the influence of extrusion on dietary fiber profile and the contentof bioactive compounds, rutin and quercetin in young sprout, whole seed, and matured stem of Tartary buckwheat.WSI(water soluble index) is increased by a function of both screw profile and process temperature, compared to control indifferent parts of Buckwheat. Also, WSI of ME is increased more than 5.2 times in grain, compared to that of control. Theeffect of precooking by extrusion on the dietary fiber profile of buckwheat flour was evaluated. Precooking by extrusion sig-nificantly increased SDF in flour, although in most cases extrusion decrease in TDF a little. The thermo-mechanical treat-ment undergone by the buckwheat flour during extrusion led to redistribute part IDF fraction to SDF, leading to an increasein the latter. The content of rutin was increased about two fold in extruded flour of sprout, compared to in control. Thisincrease maybe why these compounds are released from cell wall by high shear processing under high temperature.