• Title/Summary/Keyword: anti-solvent

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Skin Permeability of piroxicam Gel by Phonophoretic Transdermal Drug Delivery (음파영동 경피약물수송에 의한 Piroxicam Gel의 경피투과)

  • Choi Suk-Joo;Oh Myung-Hwa;Kim Tae-Youl
    • The Journal of Korean Physical Therapy
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    • v.14 no.4
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    • pp.147-162
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    • 2002
  • Transdermal permeation enhancer has been used to increased skin absorption. External control of drug release and skin absorption can also be achieved by iontophoresis or phonophoresis. However, because several problems with iontophoresis are that it has a risk to skin damage because of the change of pH and the increase of current density in applying it and that it can be applied only in the form of water solution, This study is to enhance drug permeation via skin following application of ultrasound. For this goal, in gel containing piroxicam, the degree of skin permeation in vitro and anti-inflammatory effect in in vivo were investigated. Permeation study using hairless mouse skin was performed at 37 $^{\circ}C$ using buffer saline as the receptor solution. The amount of piroxicam were quantified using a HPLC system consisting of solvent delivery system. Following adoption of ultrasound 1 MHZ, it showed relatively high permeation rate where it was compared with non treated by ultrasound. The influence of duty cycle having an effect on skin permeation rate was slight higher in the case of using pulsed mode. Skin permeation increase attended by intensity of ultrasound, the permeation of trice was accelerated at 2.0 W/$cm^{2}$ than 1.0 W/$cm^{2}$. The skin permeation of piroxicam was substantially influenced by ultrasound. Anti-inflammatory effects were determined using carrageenan-induced paw swelling method in SD rat. Paw swelling tests showed that pulsed phonophoresis group was more effective than control group and only gel application group. The conclusion of phonophoresis was found to improve significantly the skin permeation in vitro and the anti-inflammatory effect in vivo.

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Yijung-tang, a Traditional Herbal Formula, Exerts Anti-allergic Effect by Regulating Production of Th2-Type Chemokines and Cytokines (Th2 사이토카인 및 케모카인 분비 조절을 통한 이중탕의 항알러지 효능 연구)

  • Jeong, Soo-Jin;Seo, Chang-Seob;Lee, Mee-Young;Shin, Hyeun-Kyoo
    • Korean Journal of Pharmacognosy
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    • v.46 no.2
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    • pp.160-166
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    • 2015
  • Yijung-tang (YJT) is a traditional herbal formula comprising 4 medicinal herbs. In the present study, we performed the simultaneous analysis for three compounds of YJT and examined anti-allergic effects in vitro. The column for separation of three compounds was used Gemini C18 column and maintained at 40$^{\circ}C$. The mobile phase for gradient elution consisted of two solvent systems. To evaluate Th2 chemokines, YJT was treated into tumor necrosis factor (TNF)-${\alpha}$ and interferon (IFN)-${\gamma}$-stimulated HaCaT cells, and performed ELISA for thymus and activation regulated chemokine (TARC) and regulated on activation, normal T-cell expressed and secreted (RANTES). To measure Th2 cytokines, YJT was added into primary mouse splenocytes, and performed ELISA for interleukin (IL)-4, 5, 13. Calibration curves were acquired with r2 >0.9999. The contents of liquiritin, glycyrrhizin, and 6-gingerol in YJT were 4.50 mg/g, 11.10 mg/g, and 1.33 mg/g, respectively. YJT inhibited production of TARC and RANTES in TNF-${\alpha}$ and IFN-${\gamma}$-treated HaCaT cells. YJT also reduced production of IL-4, 5, and 13 in primary mouse splenocytes. In conclusion, our data will be a valuable information to improve quality control and anti-allergic effects of YJT.

Synthesis of 18F Labeled Clotrimazole Derivatives as a Potential PET Imaging Agent (18F을 표지 암 영상용 클로트리마졸 유도체의 합성)

  • Jung, Soon Jae;Kim, In Jong;Park, Jeong Hoon;Lee, Heung Nae;Kim, Sang Wook;Hur, Min Goo;Choi, Sang Moo;Yang, Seung Dae;Yu, Kook Hyun
    • Journal of Radiation Industry
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    • v.4 no.1
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    • pp.7-11
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    • 2010
  • Clotrimazole [1-{(2-chlorophenyl)-diphenylmethyl}-1H-imidazole, CLT] has been reported to inhibit the proliferation of vascular endothelial and act as an in vitro anti-VEGF drug. It is also shown to inhibit angiogenesis in an animal model. The radioisotope labeled clotrimazole derivative can be utilized to monitor the physiologic processes of cancer. In this study, we synthesized [$^{18}F$]fluoride labeled clotrimazole derivatives as a new tumor imaging agent for PET. The references were prepared by a refluxing with clotrimazole and an excess of fluoroalkyltosylate in acetonitrile for 36 h and clotrimazole reacted with ditosylalkane to give precursors. [$^{18}F$]Fluoride labeled reaction was performed with precursor in Kryptofix[2.2.2]/$K_2CO_3$ for 10 min at $80^{\circ}C$. The radiolabeling mixture was passed through a silica Sep-Pak cartridge to remove $^{18}F^-$. The [$^{18}F$]F-clotrimazole derivatives were synthesized with a 20~25% yield. In the radiofluorination step, we used acetonitrile and DMSO as a solvent and observed a higher yield at the acetonitrile (25%) reaction compared with the DMSO reaction (5%).

Antioxidant and Anti-inflammatory Activities of Different Parts of Ixeris dentata According to Extract Methods (씀바귀 부위별 용매추출 방법에 따른 항산화 활성 및 항염증 효과 비교)

  • Oh, Hee-Kyung
    • Journal of the Korean Applied Science and Technology
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    • v.37 no.6
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    • pp.1567-1574
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    • 2020
  • This study was to investigate the antioxidant and anti-inflammatory activity of leaf and stem of Ixeris dentate extract by hot water and 70% ethanol. The total flavonoid and polyphenol in 70% ethanol extract of leaf and stem of Ixeris dentate were significantly higher than those of hot water extracts. DPPH and ABTS free radical scavenging activity of 70% ethanol extract of leaf was higher than that of hot water extract of leaf. 70% ethanol extract of leaf was the highest on the DPPH and ABTS activity. Nitric oxide(NO) production of 70% ethanol extract was higher than that of hot water extract. According to this study, it was found that there was difference in physiological activity due to extraction solvents of each part of Ixeris dentate and it is believed that it can be used as an ingredient of functional foods using Ixeris dentate.

Evaluation of the anti-inflammatory effects of silkworm (Bombyx mori L.) pupal extracts against lipopolysaccharide-induced inflammation in the murine macrophage cell line RAW264.7

  • Kamidi, Rahul;HaeYong, Kweon;Hun-bok, Kim;Ji Hae, Lee
    • International Journal of Industrial Entomology and Biomaterials
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    • v.45 no.2
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    • pp.99-107
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    • 2022
  • Silkworm pupal extracts (SPE) were prepared in different solvents (water, 30%, 50%, 70%, and 100% ethanol) and their anti-inflammatory effects were evaluated in the RAW264.7 cell line. The SPE composition was initially evaluated by determining the protein content and performing Fourier transform infrared (FTIR) analysis. The protein content of the different SPE ranged from 6.75-130.93 mg/g of extract. FTIR analysis exhibited distinguishable absorption peaks among the extracts and indicated the presence of lipids, proteins, carbohydrates, and nucleic acid moieties. The levels of released nitric oxide (NO) and interleukin-6 (IL-6) expression in lipopolysaccharide (LPS)-induced RAW264.7 cells were only attenuated by 100% ethanolic SPE to 19.44% and 16.77%, respectively. The other solvent extracts were ineffective. Hence, further studies were conducted with 100% ethanolic SPE from three distinct stages of male and female silkworm pupae belonging to four silkworm varieties (Baegokjam; B, GoldenSilk; G, Juhwangjam; J, and YeonNokjam; Y). The best reduction in NO release and interleukin-1β (IL-1β) expression levels was achieved by the SPE of early female pupae belonging to the Baegokjam variety (32.72%) and those of early female pupae belonging to the Baegokjam and GoldenSilk (59.93%) varieties, respectively. The best reduction in IL-6 expression by 49.70% was achieved by SPE from female pupae of the mid-pupal stage belonging to the Baegokjam variety.

The Anti-Wrinkle and Whitening Effect of Extracts of Castanea crenata Inner Shell (밤부산물(율피)의 주름개선 및 미백 효과)

  • Jang, Min-Jung;Cheon, Soon-Ju;Kim, Hui-Yeong;Kwoen, Dae-Jun;Kim, Hak-Yoon;Kim, Sea-Hyun;Lee, Jin-Tae
    • Journal of Life Science
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    • v.21 no.5
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    • pp.734-738
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    • 2011
  • Aging in humans is inexorable and inescapable. The progressive decrease of physiological capacity and the reduction of the ability to cope with environmental stresses lead to increased susceptibility and vulnerability to human disease. Recently, in the cosmetic industry, many researchers have paid considerable attention to delaying or improving the symptoms of skin aging. Since the early 1990`s, there have been various challenges in developing cosmeceutical products which have strong anti-aging effects, and this has been an important issue in the cosmetic industry. Meanwhile, development of anti-aging cosmetics supported by biochemical activities in the skin has been researched. Castanea crenata inner Shell solvent extracts were investigated for anti-wrinkle and whitening effects, in order to apply it as a functional ingredient for cosmetic products. For anti-wrinkle effect, elastase inhibition activity of Castanea crenata inner shell acetone extract (CA) was 51.0% at a concentration of 100 ug/ml. The collagenase inhibition activity of CA and Castanea crenata inner shell ethanol extract (CE) was 96.4%, 94.3% at a concentration of 50 ug/ml. The tyrosinase inhibitory effect, which is related to skin-whitening, was 47.2% and 45.8% in CA and CE at a concentration of 500 ug/ml. All these results suggest that Castanea crenata inner shell can be effectively used as a cosmeceutical ingredient for the prevention of wrinkles.

Search for Plant-originated Antibacterial Compounds Against Pathogen (Acidovorax avenae subsp. citrulli) of Watermelon Bacterial Fruit Blotch (수박 과실썩음병 병원균(Acidovorax avenae subsp. citrulli)에 대한 식물유래 항균 활성물질 탐색)

  • Noh, Jin-Taek;Choi, Yong-Hwa
    • Korean Journal of Organic Agriculture
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    • v.23 no.1
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    • pp.77-89
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    • 2015
  • 133 Species of medicinal plants were used for the development of natural agrichemicals with anti-microbial activity against Acidovorax avenae subsp. citrulli, a pathogen of bacterial fruit blotch in watermelon. The MeOH-extracts of these medicinal plants were examined for anti-microbial activity by bioassay. The MeOH-extract of Citrus unshiu Markovich had the strongest antibacterial activity against Acidovorax avenae subsp. citrulli. To identify anti-microbial compounds from Citrus unshiu Markovich, solvent-fractionation was used. The fraction of hexane, which showing the highest value of anti-microbial activity, was analyzed by GC-MS. Each mass spectra, corresponding to each peak of chromatogram, was compared to mass database of Wiley library. As a result, d-Limonene, ${\gamma}$-terpinene, ${\beta}$-linalool, terpineol, palmitic acid, 9,12-octadecadienoic acid, Linolenic acid, and stigmasterol were identified. Among them, d-Limonene, ${\gamma}$-terpinene, ${\beta}$-linalool, and terpineol confirmed to be shown the anti-microbial activity by bioassay. Especially, d-Limonene and ${\gamma}$-terpinene found to have strong activity. In conclusion, we thought d-limonene and ${\gamma}$-terpinene from Citrus unshiu Markovich. Latin, had anti-microbial activity against Acidovorax avenae subsp. citrulli and could be candidates for the control agents for the control of bacterial fruit blotch in watermelon.

Biological Activities of Yellow Garlic Extract (황마늘 추출물의 생리활성)

  • Kang, Jae Ran;Hwang, Cho Rong;Sim, Hye Jin;Kang, Min Jung;Kang, Sang Tae;Shin, Jung Hye
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.7
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    • pp.983-992
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    • 2015
  • This study investigated the quality characteristics and biological activities, such as antioxidant, whitening, anti-diabetes, and anti-inflammatory activities, of yellow garlic, by simplify processing time and manufacturing process compared with black garlic. Extracts were prepared various ratios of water and ethanol solvent [water : ethanol (v/v)=100:0, 70:30, 50:50, 30:70, 0:100] from yellow garlic. Alliin content of yellow garlic showed no difference compared with fresh garlic, whereas S-allyl cysteine content of yellow garlic was higher than that of fresh garlic. Alliin content of yellow garlic extracts increased in an ethanol concentration-dependent manner. Total phenol and flavonoid contents were highest in 100% ethanol extract. DPPH and ABTS radical scavenging abilities did not show significant differences among 0~70% ethanol extracts, whereas 100% ethanol extract showed the highest contents of 93.45% and 91.46%, respectively. Tyrosinase and ${\alpha}$-glucosidase inhibitory activities were also highest in 100% ethanol extract, but did not show significant differences among the extract solvents. Water and ethanol extracts from yellow garlic showed anti-inflammatory effects by modulating production of NO and cytokines at a concentration of $100{\mu}g/mL$. We suggest that yellow garlic has antioxidant, whitening, anti-diabetes, and anti-inflammatory activities and can be used as a functional material similar to black garlic.

Anti-oxidative Activities for the Flavonoids of the Syzygium aqueum Burm.f. Alston Branches from Jeju Island (제주 자생 물사과 가지 유래 Flavonoid 화합물의 항산화 활성)

  • Yeom, Hyun Sook;Lee, Nam Ho;Hyun, Ju Mi
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.44 no.2
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    • pp.151-159
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    • 2018
  • In this study, we investigated the anti-oxidative activities and cell protective effects of the constituents isolated from S. aqueum branches. DPPH and $ABTS^+$ radical scavenging activities were screened for the ethanol extract and solvent fractions, ethyl acetate (EtOAc) and butanol (BuOH) fractions showed potent activities. When HaCaT cells were treated with $H_2O_2$, the ethanol extract and EtOAc fractions ($20{\mu}g/mL$) protected the cells against oxidative damage. Two constituents were isolated from the EtOAc fraction of S. aqueum branches; pinocembrin (1), desmethoxymatteucinol (2). The chemical structures of the isolated compounds were elucidated based on the spectroscopic data including $^1H$ and $^{13}C$ NMR spectra, as well as comparison of the data to the literature values. Anti-oxidative activities and cell protective effects were studied for the isolated compounds. For the anti-oxidative activities, all of the compounds 1 and 2 showed DPPH and $ABTS^+$ radical scavenging activities. Also, from the cell protective effect test, the compounds 1 and 2 protected the cell against oxidative stress by $H_2O_2$. Based on these results, S. aqueum branches extract could be potentially applicable as anti-oxidant ingredients in cosmetic industries.

The Anti-Inflammatory Effects of Persicaria thunbergii Extracts on Lipopolysaccharide-Stimulated RAW264.7 Cells (Lipopolysaccharide로 처리 된 RAW264.7 세포에서 고마리 추출물의 항염증 효과)

  • Kim, Sang-Bo;Seong, Yeong-Ae;Jang, Hee-Jae;Kim, Gun-Do
    • Journal of Life Science
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    • v.21 no.12
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    • pp.1689-1697
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    • 2011
  • In this study, we investigated the anti-inflammation effect of Persicaria thunbergii (P. thunbergii) on RAW 264.7 murine macrophage cells. The anti-inflammatory activity of P. thunbergii was determined by measuring expression of the LPS-induced inflammatory proteins, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and nuclear factor-${\kappa}B$ (NF-${\kappa}B$), and the production of nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$). Methanol extract of P. thunbergii decreased the expression of iNOS, COX-2 and NF-${\kappa}B$, and increased the expression of HO-1 in LPS-stimulated RAW264.7 cells. Methanol extract was fractioned by n-butanol, hexane and ethyl acetate (EtOAc) and each fraction was tested for inhibitory effects on inflammation. Among the sequential solvent fractions, the EtOAc soluble fraction was investigated by the expression of prostaglandin $E_2$ ($PGE_2$), and showed decreasing form to the dose-dependent manner. EtOAc extract showed the most effective inhibitory activity of the expression of iNOS, COX-2 and NF-${\kappa}B$, and the production of NO. The study showed that P. thunbergii has anti-inflammatory activity through the decrease of NO and inhibition of iNOS, COX-2, $PGE_2$ and NF-${\kappa}B$ expression, and by the increase of HO-1 enzyme. This study needs for more investigation to find out the most effective single compound with anti-inflammatory activity.