• Journal of the Korean Chemical Society
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• v.67 no.2
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• pp.120-128
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• 2023

Osteoporosis is a disease that causes the weakening of bone by increasing porosity, which often results in fractures. Osteoporosis treatment measures include the use of Bisphosphonates and estrogen. However, these treatments cannot be used in the long term as these treatments have adverse side effects. Therefore, there is a need to identify better and safer treatment options. For this, 63 plant extracts were screened and among them, six extracts showed high anti-osteoclastic activity with low cytotoxicity. Of these six extracts, three extracts, Cudrania tricuspidata (P371), Ulmus davidiana var. japonica (P401), and Torilis japonica (P411), showed more than 50 percent osteoclast inhibition. While the remaining, Stewartia pseudocamellia extracts I and II (P370, P397) and Cuscuta chinensis (P418), showed moderate or between 40-50 percent osteoclast inhibition. Among all the extracts, Torilis japonica (P411) showed the highest inhibitory action against osteoclast development. Torilis japonica (P411) primary components include Kaempferol, Quercetin, and Luteolin, all proven to inhibit osteoclastogenesis. Stewartia pseudocamellia extracts I and II (P370 and P397) showed moderate or 44% osteoclast inhibition. Stewartia pseudocamellia extract II (P397) enhanced the growth of RAW 264.7 cells by 19%. Torilis japonica (P411) and Stewartia pseudocamellia extract II (P397) suppressed the expression of osteoclast-specific genes in RANKL-induced osteoclastogenesis in RAW 246.7 cells. Torilis japonica (P411) extracts even increased osteoblast-specific RUNX2 gene expression. This results provide that six extracts could be used as a potential treatment option for osteoporosis disease with the extracts of Torilis japonica (P411) and Stewartia pseudocamellia (P397) as an ideal candidates. However, the combination of the extract with higher osteoclastic inhibition and less toxic effects with further analysis should be recommended.

• Parasites, Hosts and Diseases
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• v.61 no.4
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• pp.449-454
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• 2023

Free-living amoebae (FLA) rarely cause human infections but can invoke fatal infections in the central nervous system (CNS). No consensus treatment has been established for FLA infections of the CNS, emphasizing the urgent need to discover or develop safe and effective drugs. Flavonoids, natural compounds from plants and plant-derived products, are known to have antiprotozoan activities against several pathogenic protozoa parasites. The anti-FLA activity of flavonoids has also been proposed, while their antiamoebic activity for FLA needs to be emperically determined. We herein evaluated the antiamoebic activities of 18 flavonoids against Naegleria fowleri and Acanthamoeba species which included A. castellanii and A. polyphaga. These flavonoids showed different profiles of antiamoebic activity against N. fowleri and Acanthamoeba species. Demethoxycurcumin, kaempferol, resveratrol, and silybin (A+B) showed in vitro antiamoebic activity against both N. fowleri and Acanthamoeba species. Apigenin, costunolide, (-)-epicatechin, (-)-epigallocatechin, rosmarinic acid, and (-)-trans-caryophyllene showed selective antiamoebic activity for Acanthamoeba species. Luteolin was more effective for N. fowleri. However, afzelin, berberine, (±)-catechin, chelerythrine, genistein, (+)-pinostrobin, and quercetin did not exhibit antiamoebic activity against the amoeba species. They neither showed selective antiamoebic activity with significant cytotoxicity to C6 glial cells. Our results provide a basis for the anti-FLA activity of flavonoids, which can be applied to develope alternative or supplemental therapeutic agents for FLA infections of the CNS.

• Journal of the Korean Society of Food Science and Nutrition
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• v.44 no.8
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• pp.1157-1164
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• 2015

The present investigation evaluated the antioxidant activities of water extracts from dandelion (Taraxacum officinale) aerial parts, roots, and mixed extracts. Mixed extract of T. officinale was a mixture of aerial parts and roots at 9:1 and 8:2 weight ratios. Extracts from aerial parts (DAE), roots (DRE), and mixture of aerial parts and roots (DME) were measured for cell viability and catalase activity in HepG2 cells, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, and lipid peroxidation inhibitory activity. Cell viabilities of HepG2 cells treated with DAE, DRE, DME 8:2, and DME 9:1 against $H_2O_2$-induced oxidative damage were 63.4%, 54.6%, 76.7% and 83.4% at a concentration of $400{\mu}g/mL$, respectively. Catalase activity was highest in DME 9:1 (12.2 mU/min/mg protein) compared with DAE (9.0 mU/min/mg protein) and DRE (9.7 mU/min/mg protein). DPPH radical scavenging activity of DME showed a significantly lower $EC_{50}$ value than DAE ($EC_{50}$ value of DME $9:1=163.3{\mu}g/mL$, DME $8:2=172.4{\mu}g/mL$, and $DAE=173.7{\mu}g/mL$). Lipid peroxidation inhibitory activity of DME showed a significantly lower $EC_{50}$ value than DAE [$EC_{50}$ values of DME $(9:1)=454.4{\mu}g/mL$, DME $(8:2)=426.6{\mu}g/mL$, and $DAE=654.7{\mu}g/mL$]. The results indicate that a small amount of T. officinale roots increased antioxidant activity of aerial parts. Especially, a 9:1 mixture was more valuable than 8:2 mixture for industry.

• Microbiology and Biotechnology Letters
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• v.46 no.1
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• pp.18-28
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• 2018

In this study, the antioxidant activities and cytoprotective effects against oxidative stress of Lonicera japonica Thunb. 50% ethanol extract and ethyl acetate fraction were investigated. Using the 1,1-diphenyl-2-picrylhydrazyl assay, the free radical scavenging activity (FSC50) of L. japonica Thunb. 50% ethanol extract and ethyl acetate fraction was determined as 152.00 and $77.25{\mu}g/ml$, respectively. To measure the reactive oxygen species (ROS) scavenging activity, the total antioxidant capacity (OSC50) was determined by using a luminol-dependent chemiluminescence assay. The antioxidant activity of the ethyl acetate fraction ($0.33{\mu}g/ml$) was approximately four times stronger than that of the 50% ethanol extract ($1.12{\mu}g/ml$). The protective effect against $^1O_2$-induced cellular damage of human erythrocytes (${\tau}_{50}$) was 46.0 min at $10{\mu}g/ml$ of the 50% ethanol extract and 52.3 min at $1{\mu}g/ml$ of the ethyl acetate fraction. We also investigated the cytoprotective effects against oxidative stress induced by $H_2O_2$ and the intracellular ROS scavenging activity in response to UVB irradiation and found that the extract and fraction protected human skin cells from damage and reduced ROS. These results confirmed that L. japonica Thunb. was a valuable plant-derived natural antioxidant with potential for development as an antioxidative functional ingredient.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.33 no.4
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• pp.263-267
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• 2007

Parabens are used in nearly all types of cosmetics and toiletries because they are formulated well and have broad spectrum of activity, interness, low costs and excellent chemical stability in relation to pH. 2-phenoxyethanol and chlorphenesin are common preservatives which are usually used in combination with parabens in cosmetics. Toxicity of parabens is generally low but application of parabens to damaged or broken skin has resulted in sensitization. Moreover, the possibility of their estrogenic potential, anesthetic effects and reproductive toxicity has been reported. Consequently there are some regulations in use of parabens. And the maximum permitted concentrations of chlorphenesin and 2-phenoxyethanol in cosmetic products are authorized by the same reasons. So it is important to control and estimate the amount of parabens in products. In this article, we proposed a valid method for the simultaneous determination of 8 preservatives including parabens in a short time using ultra performance liquid $chromatography^{TM}\;(UPLC^{TM})$. Separation of eight components was achieved in less than 10 min and resolutions were reasonable (USP resolution ${\geqq}\;2$). And limit of detection and quantification were evaluated. The method was suitably validated for specificity, linearity, precision (repeatability, intermediate precision) and accuracy for assay (recovery) based on International conference on harmonisation (ICH) guideline. The method was applicable to analysis of preservatives in cosmetic products.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.40 no.1
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• pp.11-20
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• 2014

In this work, the antioxidative effects and active component analysis of Gnaphalium affine D. DON. (G. affine) extracts were investigated. All experiments were performed with 70% ethanol extract, ethyl acetate fraction and aglycone fraction of the G. affine extract. The free radical (1,1-diphenyl-2-picrylhydrazyl, DPPH) scavenging activity ($FSC_{50}$) of ethyl acetate fraction ($6.15{\mu}g/mL$) of the G. affine was higher than that of (+)-${\alpha}$-tocopherol ($8.89{\mu}g/mL$), which is known as a reference control. Reactive oxygen species (ROS) scavenging activities ($OSC_{50}$) of the 70% ethanol extract ($1.60{\mu}g/mL$), ethyl acetate fraction ($0.075{\mu}g/mL$) and aglycone fraction ($2.28{\mu}g/mL$) of extract of G. affine on ROS generated in $Fe^{3+}$-EDTA/$H_2O_2$ system using the luminol-dependent chemiluminescence assay were much higher than that of L-ascorbic acid ($6.88{\mu}g/mL$). The cellular protective effects of 70% ethanol extract (${\tau}_{50}$ = 52.0 min) and aglycone fraction of the extract (${\tau}_{50}$ = 60.6 min) on the $^1O_2$-induced cellular damage of human erythrocytes were exhibited the higher protective effect than (+)-${\alpha}$-tocopherol (${\tau}_{50}$ = 38.0 min), known as a lipophilic antioxidant. TLC and HPLC were used to analyse active components in the aglycone fraction of the extract. Results showed that luteolin and apigenin were main components. These results suggest that the G. affine extract can be applied to an effective antioxidant in scavenging ROS including radicals.

• Journal of Food Hygiene and Safety
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• v.32 no.5
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• pp.371-380
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• 2017

In this study, 17 kinds of polyphenols and 5 kinds of anthocyanins were analyzed to compare the contents of polyphenols and anthocyanins in 76 colored agricultural products. A total of 17 polyphenols were analyzed simultaneously by 9 phenolic acids (gallic acid, protocatechuic acid, chlorogenic acid, vanillic acid, caffeic acid, syringic acid, p-coumaric acid, t-ferulic acid, t-cinnamic acid) and 8 flavonoids ((+)catechin, syringic aldehyde, rutin, epicatechin gallate, naringin, luteolin, naringenin, kaempferol) and 5 anthocyanins (delphinidin-3-glucoside, delphinidin-3-rutinoside, cyanidin-3-galactoside, cyanidin-3-glucoside, cyanidin-3-arabinoside) were simultaneously analyzed. The total content of 17 polyphenols was determined as seoritae $255.1{\pm}7.5{\mu}g/g$, seomoktae $275.8{\pm}5.3{\mu}g/g$, black rice $78.5{\pm}4.6{\mu}g/g$, black sesame $75.8{\pm}3.2{\mu}g/g$, blueberry $143.3{\pm}5.5{\mu}g/g$, aronia $195.2{\pm}4.9{\mu}g/g$ and blackcurrent $131.6{\pm}3.2{\mu}g/g$, the highest content was found in the order of seomoktae > seoritae > aronia > blueberry > blackcurrant > black rice > black sesame. The total content of 5 anthocyanins was determined as seoritae $82.4{\pm}17.2{\mu}g/g$, seomoktae $95.2{\pm}6.1{\mu}g/g$, black rice $74.1{\pm}9.7{\mu}g/g$, black sesame were not detected, blueberry $110.8{\pm}1.9{\mu}g/g$, aronia $218.9{\pm}6.1{\mu}g/g$ and blackcurrent $209.7{\pm}4.0{\mu}g/g$, the highest content was found in the order of aronia > blackcurrant > blueberry > seomoktae > seoritae > black rice. These results indicated that seomoktae and aronia possessed the high level of functional components and further study will be needed to develop high value-added foods based on the colored agricultural products.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.04a
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• pp.13-13
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• 2018

The anti-inflammatory (INF) compounds (1-15) were isolated from Agrimonia pilosa Ledeb. (APL) by activity-guided isolation technique. The isolated compounds (1-15) were identified as quercetin-7-O-rhanmoside (1), apigenin-7-O-glycoside (2), kaempferol-7-O-glycoside (3), apigenin-7-O-[6"-(butyl)-glycoside] (4), querceitn (5), kaempferol (6), apigenin (7), apigenin-7-O-[6"-(pentyl)-glycoside] (8), agrimonolide (9), agrimonolide-6-O-glucoside (10), desmethylagrimonolide (11), desmethylagrimonolide-6-O-glucoside (12), luteolin (13), vitexin (14) and isovitexin (15). Flavonoids, compound 2, 3, 11, and 14-15 have been found in APL for the first time. Furthermore, two novel flavone derivatives, compound 4 and 8, have been isolated inceptively in plant. In the no cytotoxicity concentration ranges of $0-20{\mu}M$, nitric oxide (NO) production level of 1-15 was estimated in LPS-treated Raw 264.7 macrophage cells. The flavone aglycones, 7 (apigenin, $IC_{50}=3.69{\pm}0.34{\mu}M$), 13 (luteolin, $IC_{50}=4.62{\pm}0.43{\mu}M$), 6 (kaempferol, $IC_{50}=14.43{\pm}0.23{\mu}M$) and 5 (quercetin, $IC_{50}=19.50{\pm}1.71{\mu}M$), exhibited excellent NO inhibitory (NOI) activity in dose-dependent manner. In the structure activity relationship (SAR) study of apigenin-derivatives (APD), apigenin; Api, apigenin-7-O-glucoside; Api-G, apignenin-7-O-[6"-(butyl)-glycoside]; Api-BG and apignenin-7-O-[6"-(pentyl)-glycoside]; Api-P, from APL on INF activity was investigated. The INF mediators level such as NO, INF-cytokines, NF-KB proteins, iNOS and COX-2 were sharply increased in Raw 264.7 cells by LPS. When pretreatment with APD in INF induced macrophages, NOI activity of Api was most effective than other APD with $IC_{50}$ values of $3.69{\pm}0.77{\mu}M$. And the NOI activity was declined in the following order: Api-BG ($IC_{50}=8.91{\pm}1.18{\mu}M$), Api-PG ($IC_{50}=13.52{\pm}0.85{\mu}M$) and API-G ($IC_{50}=17.30{\pm}0.66{\mu}M$). The NOI activity of two novel compounds, Api-PG and Api-BG were lower than their aglycone; Api, but more effective than Api-G (NOI: Api-PG and Api-BG). And their suppression ability on INF cytokines such as $TNF-{\alpha}$, $IL-1{\beta}$ and IL-6 mRNA showed the similar tendency. Therefore, the anti-INF mechanism study of Api-PG and Api-BG on nuclear factor-kappa B ($NF-{\kappa}B$) pathway, representative INF mechanism, was investigated and Api was used as positive control. Api-BF was more effectively prevent the than phosphorylation of $pI{\kappa}B$ kinase (p-IKK) and p65 than Api-PG in Raw 264.7 cells. In contrast, Api-PG and Api-BG were not reduced the phosphorylation of inhibitor of kappa B alpha ($I{\kappa}B{\alpha}$). Moreover, pretreatment with Api-PG and Api-BG, dose-dependently inhibited LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) mRNAs and proteins in macrophage cells, and their expression were correlated with their NOI activity. Therefore, APL can be utilized to health promote agent associated with their AIN metabolites.

• Korean Journal of Food Science and Technology
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• v.37 no.2
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• pp.183-188
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• 2005

Effects of co-solvent polarity, citric acid, pressure, temperature, run time, and co-solvent ratio on extraction of major flavonoids from Lonicera Flos were investigated using supercritical fluid $CO_{2}(SF-CO_{2})$. HPLC analysis revealed addition of pure methanol resulted in low extraction yield of major flavonoids, luteoloin (Lu), Quercetin (Qu), Apigenin (Ap). Under same condition, as co-solvent polarity increased, yields of major flavonoids increased gradually, At optimum co-solvent extraction condirion of 60% aqueous methanol (10%, v/v), yields of Lu, Qu, and Ap were 42.09, 28.18, and 3.49 mg/100 g, respectively. Addition of citric acid to 60% aqueous methanol gave higher, with addition of 1% citrie acid resulting in highest yields of 63.2 (Lu), 39.35 (Qu), and 5.79 (Ap) mg/100 g. Optimum extraction conditions of major flavonoids were 200 bar, $50^{\circ}C$, 60 min, and $CO_{2}$-methanol-water(20: 1.8: 1.2).

• Journal of Life Science
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• v.24 no.9
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• pp.935-945
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• 2014

Persimmon leaves were commonly consumed as beverages, but were also used as popular folk medicine in Asia. The purpose of this work was to assess the biological activities of Diospyros Lotus L. extracts (DLLE). Various solvent extracts, including n-Hexnae, $CHCl_3$, EtOAc, and n-BuOH fractions, were obtained from the methanol extract of Diospyros Lotus L. leaves. The increasing interest in the powerful biological activity of plant phenolics and flavonoids outlined the necessity for determining their content in medicinal herbs. In this study, the total polyphenol and flavonoid contents (TPC and TFC) in the EA fraction were higher than those of other fractions. The biological activities of DLLE were tested using the 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS) radical scavenging activity assay, as well as superoxide dismutase (SOD) activity as an anti-oxidant effect and ${\alpha}$-glucosidase inhibitory activity as an anti-diabetic effect. The EA fraction with high TPC and TFC values showed the highest anti-oxidant effect and high ${\alpha}$-glucosidase inhibition. The EA fractions were further purified into eight fractions using open column chromatography. Higher anti-oxidant and anti-${\alpha}$-glucosidase activity were observed in polar fractions. The content of the flavonoids, including quercein-3-O-rutinoside, kaempferol-3-O-glucoside, myricetin, luteolin, and kaempferol, were analyzed in effective fractions using high-performance liquid chromatography (HPLC). The results suggest that DLLE have anti-oxidative and anti-diabetic effects and thus, have the potential as anti-diabetic materials and as a source for natural health products.