• Journal of the Korean Chemical Society
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• v.53 no.6
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• pp.693-703
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• 2009

The complex formation of anti-inflamatory drug piroxicam (PX, 4-hydroxy-2-methyl-N-2--pridyl-2H-1,2-benzothiazine-3-carboxadiamide-1,1-dioxide) with transition metal ions Co(II), Ni(II), Cu(II) and Zn(II) in methanol(MeOH)/water binary mixtures were studied by spectrophotometric method at 25$^{\circ}C$, constant pH = 5.0 and I = 0.1 M. The computer program SQUAD was used to extract the desired information from the spectral data. The outputs of the fitting processes were stability constants, standard deviations of the estimated stability constants, concentration distribution diagrams and spectral profiles of all species. The sequence of the stability constants of PX complexes with Co(II), Ni(II), Cu(II) and Zn(II) follow the Cu(II) > Co(II) > Ni(II) ${\approx}$ Zn(II) order. This may be due to different geometry tendencies of these metal ions. The acidity constants of the PX were also determined under above condition from its absorption spectra at different pH values. The computer program DATAN was used for determination of acidity constants of PX. The validity of the obtained acidity constants was checked by a well known computer program SPECFIT/32. The effects of the different parameters like solvent nature, cations characteristics on the stability and acidity constants were thoroughly discussed.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.44 no.2
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• pp.125-131
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• 2018

Ascorbic acid (Vitamin C) has been widely used in skin care formulations. Due to its remarkable effects on anti-oxidation, collagen biosynthesis and whitening, ascorbic acid is considered as an effectible anti-aging active ingredient. But, the instability problems of ascorbic acid in cosmetic formulation such as oxidation, browning and changes in smell is the difficult issue to be overcome for the application of high concentration of ascorbic acid. We tried to stabilize the ascorbic acid in non-aqueous liquid formulation that contains polyol solvent at first. The non-aqueous system was effectible to reduce oxidation. But, ascorbic acid was crystallized in the non-aqueous formulation at the low temperature below $5^{\circ}C$. We tried to develop way to stabilize the ascorbic acid in aqueous solutions to solve the crystallizing problem. In this study, we search the optimal ratio of antioxidant combination, such as zinc sulfate, glutathione and curcuma longa (turmeric) root extract. Formulations were stored at - $16^{\circ}C$, $5^{\circ}C$, $25^{\circ}C$, $40^{\circ}C$, $50^{\circ}C$ and cycle($5-40^{\circ}C$) (in incubator) for a period of eight weeks to investigate their stability. In the stability analysis, the test parameters consisted of color, scent, phase separation and sedimentation. Ascorbic acid stability was checked by HPLC analysis.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.36 no.2
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• pp.129-136
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• 2010

In order to evaluate anti-wrinkle activity of Carex humilis extract, free radical scavenging activity, elastase inhibitory activity and reduction of expression Matrix metalloproteinase-1 (MMP-1) mRNA and MMP-1 protein were investigated. The roots of Carex humilis were extracted with 95 % ethanol and successively partitioned with organic solvents with increasing polarity of the solvents. Each fraction of organic solvent were investigated by using free radical scavenging activity and elastase inhibitory activity test. Among them, EtOAc fraction showed antioxidant activity ($SC_{50}$=4.89 ${\mu}g/mL$) and elastase inhibitory activity ($IC_{50}$=23.5 ${\mu}g/mL$). EtOAc fraction was developed on silica gel by open-column chromatography and consecutively re-developed on C18 resin by prep-HPLC to give ${\alpha}$-viniferin as a major component, which was confirmed by spectrometric analysis. In the assay on expression of MMP-1 mRNA by RT-PCR and protein by western-blot, EtOAc layer (10 ~ 100 ${\mu}g/mL$) was reduced about 50 ~ 60 %, 50 ~ 65 % respectively and ${\alpha}$-viniferin (0.5 ~ 2 ${\mu}g/mL$) was inhibited about 60 ~ 75 %, 55 ~ 65 % respectively in human fibroblast. Therefore, our findings suggest that EtOAc layer of Carex humilis containing ${\alpha}$-viniferin can be useful as an active ingredient for cosmeceuticals of anti-wrinkle effects.

• Journal of Life Science
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• v.24 no.6
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• pp.655-663
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• 2014

Woosul (Achyranthis radix), a widely used material in food and oriental medicinal industry, has different origins of plant species in Korea, Japan and China. In Korea, woosul is designated as the radix of Achyranthes japonica Nakai (AJN) and Achyranthes bidentata Blume (ABB) in the regulation of The Korean Pharmacopoeia. However, the comparative study of hot water (HW) extracts between AJN and ABB is still rudimentary. In this study, HW extracts and its subsequent organic solvent fractions of AJB and ABB were prepared, and their in-vitro antimicrobial, antioxidant and anti-diabetes activities were evaluated. The HW extract of ABB has higher sugars and polyphenol compounds, and higher lightness and lower yellowness compared than those of AJN. Analysis of biological activities showed that the ethylacetate (EA) fraction of AJN and n-hexane fraction of ABB have antibacterial activities, and the EA fractions of AJN and ABB has strong antioxidation activities determined by radical scavenging activity and reducing power. In anti-diabetes activity assay, the EA fractions of AJN and ABB showed ${\alpha}$-amylase inhibitory activities, while the butanol fractions of AJN and ABB showed ${\alpha}$-glucosidase inhibitory activities. Our results suggest that the HW extracts of AJB and ABB have different components and extraction yields, and their subsequent fractions have different biological activity. Therefore it was concluded that the EA fraction of AJN is appropriate to develop as natural medicine, and the HW extract of AJN is suitable to woosul-tea or woosul-sikhye production.

• Journal of Life Science
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• v.32 no.1
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• pp.44-50
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• 2022

The migration and proliferation of keratinocytes are key events in re-epithelization, itself a major phase in the wound healing process. Cuscuta japonica Choisy (CJC) is used as a traditional medicine to improve liver, heart, and intestinal function, and its extracts are reported to have various biological properties such as whitening, anti-oxidancy, and an anti-acne effect. However, it is not yet known in particular whether or not CJC essential oil (CJCEO) affects skin regeneration. In the present study, we isolated CJCEO by solvent extraction and tested its effect on wound healing responses using normal human keratinocytes, namely HaCaT cells. We found that CJCEO induced proliferation as well as migration in HaCaT cells in a dose-dependent manner. Compared with a control group, CJCEO treatment at 250 ㎍/ml increased proliferation by 239.98±5.51% in HaCaT cells in a dose and migration by 124.86±6.06%. Moreover, the oil induced sprout outgrowth and, at 250 ㎍/ml, increased collagen synthesis by 148.56±15.47% in HaCaT cells. These results demonstrate that CJCEO may promote skin regeneration and wound healing by increasing the migration, proliferation, and collagen synthesis of HaCaT cells. We therefore suggest that CJCEO could be used as a cosmetic material.

• Journal of the Korean Applied Science and Technology
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• v.40 no.5
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• pp.988-1000
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• 2023

Hesperetin(HT) is a potent antioxidant flavonoid aglycone derived from hesperidin(HD). The antioxidant, anti-inflammatory, and antimicrobial activities of HT and its cyclodextrin(CD) inclusion complexes were compared in vitro. HT was prepared by enzymatic hydrolysis of HD, and HT/CD complexes were prepared using 𝛽-cyclodextrin(𝛽-CD) and hydroxypropyl-𝛽-cyclodextrin(HP-𝛽-CD) by solvent co-evaporation method. The solubility of the HT/HP-𝛽-CD inclusion complex increased 93.5-fold compared to HT, and the solubility of HT/𝛽-CD increased 22.5-fold. The HT/HP-𝛽-CD inclusion complex showed a similar effect as HT on radical scavenging activity in antioxidant assays, whereas the HT/𝛽-CD inclusion complex showed slightly lower activity than HT. Cytotoxicity was low in the following order; HT/HP-𝛽-CD, HT/𝛽-CD, and HT in murine macrophage RAW264.7 cells. Treatment with HT and HT/CD inclusion complexes reduced the levels of inflammatory mediators such as nitric oxide(NO), tumor necrosis factor-𝛼(TNF-𝛼) and interleukin-6(IL-6) in the cells. HT and HT/HP-𝛽-CD inclusion complex were more effective than HT/𝛽-CD inclusion complex at relatively low concentrations. Inhibitory effects were tested on skin-pathogenic bacteria, Staphylococcus aureus and Pseudomonas aeruginosa, and they showed an antimicrobial effect on S. aureus in the order of HT = HT/HP-𝛽-CD > HT/𝛽-CD, but they did not show any significant inhibitory effect on P. aeruginosa. In conclusion, HT, the aglycone form of HD, and its CD inclusion complexes showed various biological activities. HT/HP-𝛽-CD inclusion complex, which is the highly soluble form of HT, showed relatively higher activity compared to HT/𝛽-CD inclusion complex.

• Preventive Nutrition and Food Science
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• v.22 no.3
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• pp.184-190
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• 2017

Matrix metalloproteinases (MMPs) are endopeptidases that take significant roles in extracellular matrix degradation and therefore linked to several complications such as metastasis of cancer progression, oxidative stress, and hepatic fibrosis. Hizikia fusiformis, a brown algae, was reported to possess bioactivities, including but not limited to, antiviral, antimicrobial, and anti-inflammatory partly due to bioactive polysaccharide contents. In this study, the potential of H. fusiformis against cancer cell invasion was evaluated through the MMP inhibitory effect in HT1080 fibrosarcoma cells in vitro. H. fusiformis crude extract was fractionated with organic solvents, $H_2O$, n-BuOH, 85% aqueous MeOH, and n-hexane (n-Hex). The non-toxicity of the fractions was confirmed by MTT assay. All fractions inhibited the enzymatic activities of MMP-2 and MMP-9 according to the gelatin zymography assay. Cell migration was also significantly inhibited by the n-Hex fraction. In addition, both gene and protein expressions of MMP-2 and -9, and tissue inhibitor of MMPs (TIMPs) were evaluated by reverse transcription-polymerase chain reaction and Western blotting, respectively. The fractions suppressed the mRNA and protein levels of MMP-2, MMP-9 while elevating the TIMP-1 and TIMP-2, with the $H_2O$ fraction being the least effective while n-Hex fraction the most. Collectively, the n-Hex fraction from brown algae H. fusiformis could be a potential inhibitor of MMPs, suggesting the presence of various derivatives of polysaccharides in high amounts.

• Journal of Mushroom
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• v.12 no.4
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• pp.311-315
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• 2014

Oyster mushroom is one of the popular mushrooms for Korean people and it is thus one of the mushrooms that were mostly cultivated in Korea in addition to winter and king oyster mushrooms. This study was carried out to compare the medicinal effects of fruiting body of Pleurotus ostreatus extracts. We analyzed comparing antioxidant activity and polyphenol contents of fruiting body of Pleurotus ostreatus. Firstly, ASI 2099 showed the highest level in hot water. ASI 2122 showed the highest level in the 70% EtOH and MeOH extraction. Polyphenol contents was measured after extraction with different solvents. polyphenols contents is mostly 8~10 (mg/g) and there is no difference of polyphenols contents depending on the extract solvent.

• Korean Journal of Pharmacognosy
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• v.39 no.4
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• pp.347-351
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• 2008

The methanol (MeOH) extract of the rhizome of Alpinia officinarum Hance (Zingiberaceae) demonstrated a potent inhibition on the proliferation of cultured human tumor cell lines such as MES-SA (human uterine carcinoma cell line), MESSA/DX5 (multidrug resistant subline of MES-SA), HCT-15 (human colorectal adenocarcinoma cell line), HCT15/CL02 (multidrug resistant subline of HCT15). The MeOH extract was fractionated into four portions by serial solvent partition, ie., methylene chloride (CH2Cl2) soluble part, ethylacetate (EtOAc) soluble part, n-butanol (BuOH) soluble part and remaining water layer. Among them, the $CH_2Cl_2$ soluble part of the extract exhibited a most potent inhibition on the proliferation of tested tumor cell lines. Bioassay-guided fractionation of the $CH_2Cl_2$ soluble part led to the isolation of five diarylheptanoid and two flavonoid constituents, i. e., galangin (1), 7-(4"-hydroxy-3"-methoxyphenyl)-1-phenylhept-4-en-3-one (2), 1,7-diphenyl-5-hydroxy-3-heptanone (3), trans,trans-1-(3'-methoxy-4'-hydroxyphenyl)-7-phenyl-5-ol-4,6-dien-3-heptanone (4), 5-methoxy-7-(4"-hydroxy-3"-methoxyphenyl)-1-phenyl-3-heptanone (5), kaempferide (6), 5-hydroxy-7-(4"-hydroxy-3"-methoxyphenyl)-1-phenyl-3-heptanone (7). Structures of the isolated active components (1 - 7) were established by chemical and spectroscopic means.

• Journal of Pharmaceutical Investigation
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• v.36 no.6
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• pp.355-361
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• 2006

Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.