• Title/Summary/Keyword: anti-solvent

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Anti-cancer Activity of Flavonoids from Aceriphyllum rossii (돌단풍(Aceriphyllum rossii)에서 분리한 플라보노이드의 항암활성)

  • Ahn, Eun-Mi;Han, Jae-Taek;Kwon, Byoung-Mog;Kim, Sung-Hoon;Baek, Nam-In
    • Applied Biological Chemistry
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    • v.51 no.4
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    • pp.309-315
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    • 2008
  • The methanol extract from the aerial parts of Aceriphyllum rossii was fractionated into ethyl acetate, n-BuOH and $H_2O$ layers through solvent fractionation. Repeated silica gel column chromatography of EtOAc and n-BuOH layers afforded five flavonol glycosides. They were identified as astragalin (1), kaempferol 3-O-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$6)-${\beta}$-D-glucopyranoside (2), rutin (3), kaempferol 3-O-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$4)-${\alpha}$-L-rhamnopyranosyl 1${\rightarrow}$6)-${\beta}$-D-glucopyranoside (4), and quercetin 3-O-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$4)-${\alpha}$-L-rhamnopyranosyl (1${\rightarrow}$6)-${\beta}$-D-glucopyranoside (5) on the basis of spectroscopic data. All of them showed an inhibition in farnesyl protein tranferase (FPTase) activity, and rutin (3) inhibited the growth of rat H-ras cell and the cell migration of human umbilical vein endothelial cells (HUVECs).

Nanopharmaceutical Approach for Enhanced Anti-cancer Activity of Betulinic Acid in Lung-cancer Treatment via Activation of PARP: Interaction with DNA as a Target -Anti-cancer Potential of Nano-betulinic Acid in Lung Cancer-

  • Das, Jayeeta;Samadder, Asmita;Das, Sreemanti;Paul, Avijit;Khuda-Bukhsh, Anisur Rahman
    • Journal of Pharmacopuncture
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    • v.19 no.1
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    • pp.37-44
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    • 2016
  • Objectives: This study examined the relative efficacies of a derivative of betulinic acid (dBA) and its poly (lactide-co-glycolide) (PLGA) nano-encapsulated form in A549 lung cancer cells in vivo and in co-mutagen [sodium arsenite (SA) + benzo[a]pyrene (BaP)]-induced lung cancer in mice in vivo. Methods: dBA was loaded with PLGA nanoparticles by using the standard solvent displacement method. The sizes and morphologies of nano-dBA (NdBA) were determined by using transmission electron microscopy (TEM), and their intracellular localization was verified by using confocal microscopy. The binding and interaction of NdBA with calf thymus deoxyribonucleic acid (CT-DNA) as a target were analyzed by using conventional circular dichroism (CD) and melting temperature (Tm) profile data. Apoptotic signalling cascades in vitro and in vivo were studied by using an enzyme-linked immunosorbent assay (ELISA); the ability of NdBA to cross the blood-brain barrier (BBB) was also examined. The stage of cell cycle arrest was confirmed by using a fluorescence-activated cell-sorting (FACS) data analysis. Results: The average size of the nanoparticles was ~ 110 nm. Confocal microscopy images confirmed the presence of NdBA in the cellular cytoplasm. The bio-physical properties of dBA and NdBA ascertained from the CD and the Tm profiles revealed that NdBA had greater interaction with the target DNA than dBA did. Both dBA and NdBA arrested cell proliferation at G0/G1, NdBA showing the greater effect. NdBA also induced a greater degree of cytotoxicity in A549 cells, but it had an insignificant cytotoxic effect in normal L6 cells. The results of flow cytometric, cytogenetial and histopathological studies in mice revealed that NdBA caused less nuclear condensation and DNA damage than dBA did. TEM images showed the presence of NdBA in brain samples of NdBA fed mice, indicating its ability to cross the BBB. Conclusion: Thus, compared to dBA, NdBA appears to have greater chemoprotective potential against lung cancer.

Pancreatic Lipase Inhibitory and Antioxidant Activities of Polygonum aviculare Extract (마디풀 추출물의 Pancreatic Lipase 저해 및 항산화 활성 평가)

  • Kim, Tae-Hoon
    • Food Science and Preservation
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    • v.18 no.2
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    • pp.250-255
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    • 2011
  • As part of our continuing search for novel bioactive natural products, antioxidant and pancreatic lipase inhibitory activities of the aqueous ethanolic extract of Polygonum aviculare were investigated. In addition, the total phenolic content was quantified by a spectrophotometric method. The antioxidant properties of the extract were evaluated by radical scavenging assays such as DPPH and $ABTS^+$ radicals. The anti-obesity efficacy of P. aviculare extract was tested by porcine pancreatic lipase assay. All tested samples showed a dose-dependent pancreatic lipase inhibitory and radical scavenging activities. In terms of the $IC_{50}$ value, the ethyl acetate (EtOAc) soluble portion was most potent than other solvent soluble portions. The results suggested that P. aviculare could be considered as a new potential source of natural antioxidant and anti-obesity agent for food, nutraceutical, cosmetics industries.

Dietary Aloe Vera Gel Powder and Extract Inhibit Azoxymethane-induced Colorectal Aberrant Crypt Foci in Mice Fed a High-fat Diet

  • Chihara, Takeshi;Shimpo, Kan;Kaneko, Takaaki;Beppu, Hidehiko;Higashiguchi, Takashi;Sonoda, Shigeru;Tanaka, Miyuki;Yamada, Muneo;Abe, Fumiaki
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.2
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    • pp.683-687
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    • 2015
  • Aloe vera gel exhibits protective effects against insulin resistance as well as lipid-lowering and anti-diabetic effects. The anti-diabetic compounds in this gel were identified as Aloe-sterols. Aloe vera gel extract (AVGE) containing Aloe-sterols has recently been produced using a new procedure. We previously reported that AVGE reduced large-sized intestinal polyps in Apc-deficient Min mice fed a high fat diet (HFD), suggesting that Aloe vera gel may protect against colorectal cancer. In the present study, we examined the effects of Aloe vera gel powder (AVGP) and AVGE on azoxymethane-induced colorectal preneoplastic aberrant crypt foci (ACF) in mice fed a HFD. Male C57BL/6J mice were given a normal diet (ND), HFD, HFD containing 0.5% carboxymethyl cellulose solution, which was used as a solvent for AVGE (HFDC), HFD containing 3% or 1% AVGP, and HFDC containing 0.0125% (H-) or 0.00375% (L-) AVGE. The number of ACF was significantly lower in mice given 3% AVGP and H-AVGE than in those given HFD or HFDC alone. Moreover, 3% AVGP, H-AVGE and L-AVGE significantly decreased the mean Ki-67 labeling index, assessed as a measure of cell proliferation in the colonic mucosa. In addition, hepatic phase II enzyme glutathione S-transferase mRNA levels were higher in the H-AVGE group than in the HFDC group. These results suggest that both AVGP and AVGE may have chemopreventive effects on colorectal carcinogenesis under the HFD condition. Furthermore, the concentration of Aloe-sterols was similar between 3% AVGP and H-AVGE, suggesting that Aloe-sterols were the main active ingredients in this experiment.

The Protective Effects of an Ethyl Acetate Fraction of Raphiolepsis indica Against Oxidative Stress in HaCaT Keratinocytes (HaCaT 피부 각질세포의 산화적 스트레스에 대한 다정큼나무 에틸 아세테이트 분획물의 세포 보호 효과)

  • Yang, Eun Ju;Kim, Hye-Ran;Chang, Kyung-Soo;Chang, Jeong Hyun
    • Journal of Life Science
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    • v.30 no.8
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    • pp.688-694
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    • 2020
  • In a previous study, the total phenolic content in ethanol extracts of medicinal plants that naturally grow on Jeju Island were analyzed with the extracts of Raphiolepsis indica leaf found to have the highest. The current study was carried out to evaluate the total flavonoid content, radical-scavenging activity, and the protective effect of R. indica extracts and solvent fractions on oxidative stress in HaCaT keratinocytes. More specifically, total flavonoid content and 2-azino-bis 3-ethylbenzthiazoline-6-sulfonic acid (ABTS) radical-scavenging activity were measured to assess anti-oxidative activity, and protective effects against hydrogen peroxide (H2O2) were determined by 3-[4, 5-dimethylthiazol-2-yl]-2, 5-diphenyltetrazolium bromide assay on the HaCaT cells. Of the various fractions analyzed, the ethyl acetate extract of R. indica showed the highest total flavonoid content (149.13 mg/g extracts) and the lowest remaining ABTS. In addition, the ethyl acetate fraction was significantly more resistant against H2O2 than the negative control. Our results therefore suggest that an ethyl acetate fraction of R. indica protects HaCaT cells against oxidative stress and could prove useful for developing functional cosmetic materials.

Anti-melanogenesis Effect of Phenolic Compounds Isolated from Gastrodia elata (천마(Gastrodia elate) 추출물로부터 분리된 페놀성 물질의 멜라닌 생성 억제작용)

  • 김경태;김진국;박선희;이정하;이수희;김기호;박수남
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.30 no.1
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    • pp.33-38
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    • 2004
  • Melanin pigmentation in human skin is a major defense mechanism against ultraviolet light of the sun, but abnormal pigmentation such as freckles, liver spot could be a serious aesthetic problem. Nearly all studies are mainly concentrated on searching for the materials that have inhibitory activities on tyrosinase. In this work, to isolate phenolic compounds from Gastrodia elata, we purified the extract through solvent fractionation, column chromatography, and recrystallization. They were identified as 4-hydroxybenzyl alcohol 1, bis(4-hydroxyphenyl)methane 2, gastrodin (4-${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 on the base of spectroscopic evidences. In order to investigate their depigmentation effect, inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in B16 melanoma cells were evaluated in vitro. We have found that 4-hydroxybenzyl alcohol 1 and gastrodin (4- ${\beta}$-D-glucopyranosyloxybenzyl alcohol) 3 have no tyrosinase inhibitory activity, but inhibit the melanin synthesis in B16 melanoma cells. Tyrosinase inhibitory activities of bis(4-hydroxyphenyl)methane 2 (IC$\_$50/ = 400 $\mu\textrm{g}$/mL) and butanol fraction (IC$\_$50/ = 46 $\mu\textrm{g}$/mL) were lower/higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL), but inhibitory activities of melanin synthesis in B16 melanoma cells were much higher than that of arbutin. Especially, tyrosinase inhibitory activities of isolated phenolic fraction (IC$\_$50/ = 2.37 $\mu\textrm{g}$/mL) from butanol fraction was very higher than that of arbutin (IC$\_$50/ = 114 $\mu\textrm{g}$/mL). Therefore, these results suggest that isolated phenolic compounds from Gastrodia elata have inhibitory activity against mushroom tyrosinase and inhibitory activity of melanin synthesis in 816 melanoma cells in vitro.

Antioxidant activities, production of reactive oxygen species, and cytotoxic properties of fractions from aerial parts of glasswort (Salicornia herbacea L.) (퉁퉁마디 지상부 분획의 산화방지 활성, 활성산소종 생성과 세포독성 조절작용)

  • Kang, Smee;Hong, Jungil
    • Korean Journal of Food Science and Technology
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    • v.48 no.6
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    • pp.574-581
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    • 2016
  • Glasswort (Salicornia herbacea L.) is an edible halophyte that grows in salt marshes. In the present study, anti- and pro-oxidant activities and cytotoxic properties of glasswort were investigated. Solvent fractions, including fractions of hexane, ethylether (Fr.E), ethylacetate (Fr.EA), butanol and water, were prepared from a 70% methanol extract of glasswort aerial parts. Fr.EA contained the highest levels of total polyphenols and flavonoids, showing the strongest scavenging activities against DPPH and ABTS radicals, and nitrite. In addition Fr.EA showed the most potent cytotoxic effects on HCT-116 colon cancer cells and INT-407 normal intestinal cells, followed by Fr.E. Most fractions also decreased the level of reactive oxygen species in the treated cells, but generated $H_2O_2$ in the medium. The cytotoxic activity of Fr.EA was more pronounced in the presence of ascorbic acid or N-acetylcysteine. These results indicate that the fractions from aerial parts of glasswort exhibit both anti- and pro-oxidant activities, and these activities modulate cytotoxic properties.

Functional Chemical Components and Their Biological Activities of Houttuynia cordata and Lespedeza cuneata (어성초와 야관문의 기능성 성분 분석과 항산화, 항고혈압, 및 항당뇨 활성)

  • Park, Seong Ik;Sohn, Ho-Yong;Lee, Chang Il;Hwang, Hee Young;Park, Seung Woo;Kim, Jong-Sik
    • Journal of Life Science
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    • v.30 no.2
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    • pp.169-177
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    • 2020
  • For this study, we prepared organic solvent fractions from methanol extracts of Houttuynia cordata and Lespedeza cuneate, and analyzed their chemical components and various biological functions such as anti-oxidation, angiotensin-converting enzyme (ACE) inhibition, and α-glucosidase inhibitory activities. We found that DPPH radical scavenging activity was highest in the ethyl acetate fractions of Houttuynia cordata (90.8%) and Lespedeza cuneata (91.2%), whereas ABTS radical scavenging activity was highest in the ethyl acetate fractions of Houttuynia cordata (86.1%) and the chloroform fractions of Lespedeza cuneata (95.6%). FRAP activity was highest in the ethyl acetate fraction of Houttuynia cordata (360.1 mg TE/g) and Lespedeza cuneata (239.2 mg TE/g). ACE inhibitory activity was highest in the chloroform fraction of Houttuynia cordata (13.2%) and Lespedeza cuneata (35.2%). And, α-glucosidase inhibitory activity was highest in the ethyl acetate fraction of Houttuynia cordata (56.3%), and the water residue of Lespedeza cuneata (93.6%). Finally, we investigated the DPPH radical scavenging activity of 20 types of pure compounds identified in Houttuynia cordata and Lespedeza cuneate. The results show that quercetin demonstrates the highest DPPH radical scavenging activity. Overall, these results help us to understand the functional chemical components of Houttuynia cordata and Lespedeza cuneate and the biological effects of these components.

A Study on the Classifying Quality Standard by Comparison with Physicochemical Characteristics of Virgin, Pure, Pomace Olive Oil (버진, 퓨어, 포마스 올리브유의 이화학적인 특성 비교를 통한 품질등급 구분에 관한 연구)

  • Cho, Eun-Ah;Lee, Young-Sang
    • The Korean Journal of Food And Nutrition
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    • v.27 no.3
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    • pp.339-347
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    • 2014
  • This study investigated the classification of olive oils that are mainly distributed in Korea via imports. The fatty acid contents, degree of color, pigments, anti-oxidants, and sterol contents are analyzed on the different types of olive oil as follows: 10 kinds of extra virgin olive oil, 5 kinds of pure olive oil, and 5 kinds of refined olive-pomace oil. As a result of fatty acid analysis, the majority of oleic acid ($C_{18:1}$) and palmitic acid ($C_{16:0}$), and minority of linoleic acid ($C_{18:2}$) and stearic acid ($C_{18:0}$) were detected without any significant differences between the grades of olive oils. The UV spectrum is related to the ${\Delta}K$, and it is a part of the analysis factor for the purity and degree of degradation of the oil. Extra virgin olive oil had ${\Delta}K$ of almost 0, pure olive oil had 0.07~0.12, and refined olive-pomace oil had 0.1~0.13. These differed from extra virgin oil, and the pure or pomace oil ${\Delta}K$ had a confirmed distinct difference. The color degrees of chlorophyll with a low $L^*$ value and $(-)a^*$ (green) and carotenoid with $(+)b^*$ (yellow) were confirmed to have correlation between extra virgin and other olive oils. To compare chlorophyll and carotenoid as natural pigment in olive oils, 417 nm and the ratio of the absorbance at 480 nm (417/480) was calculated at 1.62 of extra virgin, 1.85 of pure olive oil, and 3.32 of refined olive-pomace oil. Therefore, it will be possible to distinguish when the extra virgin or pure olive oil are mixed with olive-pomace oil. The total amount of tocopherol, an anti-oxidant, were 19.06 in extra virgin, 10.91 in pure olive oil, and 27.88 in refined olive-pomace oil. The high content of tocopherol in pomace oil caused recovery of solvent extraction from olive pulp. Thus, extra virgin oil and pure olive oil were distinguished by olive-pomace oil. Polyphenol compounds in extra virgin olive oil measured high only in ferulic acid with 0.543 mg/kg, caffeic acid with 0.393 mg/kg, and other vanillic acid, vanillin, and p-coumaric acid had similar amount of 0.3 mg/kg. All grade of olive oils had the highest ${\beta}$-sitosterol content. Af (Authenticity factor) value were estimated with campesterol and stigmasterol content ratio (%). Af value was 19.2 in extra virgin olive oil, 17.1 in pure olive oil, 16.9 in refined olive-pomace oil, which were distinctive from sunflower oil with 3.7, corn oil with 2.4, and soybean oil with 2.0. It can provide important indicator of olive oil adulteration with other cheap vegetable oils. The results of this study can be used as a database for the classification of olive oil grade and distinguishing between the different types of oils.

Spectrophotometric Study of Acidity and Complex Formation of Anti-Inflammatory Drug Piroxicam with Some Transition Metal Ions in Different Methanol/Water Mixtures by Chemometric Methods (Chemometric 방법에 의한 메탄올/물 계에서 전이 금속 이온과 소염제 Piroxicam의 산성도 및 착체 형성에 관한 분광광도법 연구)

  • Ghasemi, Jahan B.;Jalalvand, Alireza
    • 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.