• Title/Summary/Keyword: Synthetic flavonoid

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Recent Advances in Anti-inflammatory Synthetic Flavonoids as Potential Drugs

  • Kim, Hyun-Pyo;Park, Hae-Il
    • Natural Product Sciences
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    • v.16 no.2
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    • pp.59-67
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    • 2010
  • Flavonoids are well-known anti-inflammatory agents that exert their effects via a variety of mechanisms including antioxidative action, inhibition of eicosanoid metabolizing enzymes and regulation of theexpression of proinflammatory molecules. In this review, synthetic approaches to obtain more useful flavonoid derivatives are summarized. Human clinical trials of flavonoid therapy are discussed. Through continual investigation to identify more potent and comparable flavonoids, new anti-inflammatory flavonoid therapy will be successfully launched, especially for the treatment of chronic inflammatory disorders.

Inhibition of Collagenase by Anti-inflammatory Synthetic Flavones

  • Park Hae-Il;Sin Bo-Young;Kim Hyun-Pyo
    • Biomolecules & Therapeutics
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    • v.14 no.1
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    • pp.36-39
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    • 2006
  • Some flavones/flavonols were previously found to inhibit collagenase. To establish a therapeutic potential for skin inflammation, twenty-three synthetic flavone derivatives were examined for their inhibitory potential against collagenase from Clostridium histolyticum. From the results, it was found that most of them having various hydroxyl, methoxyl, methylsulfuryl and/or chloro substitution(s) on A- and B-rings were not efficient collagenase inhibitors. Among the synthetic flavones tested, only two synthetic derivatives, 3',4'-dihydroxyflavone and 5-hydroxy-4'-methoxyflavone, weakly inhibited bacterial collagenase (13-29% inhibition at 50-100 ${\mu}M$).

Prenylated Flavonoids as Tyrosinase Inhibitors

  • Lee, Nan-Kyoung;Son, Kun-Ho;Chang, Hyeun-Wook;Kang, Sam-Sik;Park, Hae-Il;Heo, Moon-Young;Kim, Hyun-Pyo
    • Archives of Pharmacal Research
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    • v.27 no.11
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    • pp.1132-1135
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    • 2004
  • In order to find new tyrosinase inhibitors and the effects of prenyl residue on flavonoid molecules, eight prenylated and three synthetic vinylated flavonoids were examined on their inhibitory effect against tyrosinase activity. From the results, kuwanon C, papyriflavonol A, sanggenon D and sophoflavescenol were found to possess the considerable inhibitory activity. Especially, sanggenon D is revealed as a potent inhibitor ($IC_{50}$ =7.3$\mu$ M), compared to the reference compound, kojic acid ($IC_{50}$ =24.8 $\mu$M). However, the prenylation with isoprenyl group or the vinylation to flavonoid molecules did not enhance tyrosinase inhibitory activity.

Induction of ${\beta}$-Glucosidase and ${\alpha}$-Rhammosidase of Bacteroides JY-6 by Flavonoid Glycosides (플라보노이드배당체에 의한 Bacteroides JY-6의 ${\beta}$-글루코시다제 및 ${\alpha}$-람노시다제의 유도)

  • Jang, Il-Sung;Park, Jong-Baek;Kim, Dong-Hyun
    • YAKHAK HOEJI
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    • v.40 no.3
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    • pp.335-339
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    • 1996
  • Optimal medium for growth and glycosidases production of Bacteroides JY-6, an human intestinal bacterium, was general anaerobic medium or tryptic soy broth containing sod ium thioglycolate and ascorbic acid. By cocultivation of Staphylococcus R-48, Bacteroides JY-6 could be cultured in LB broth unable to culture JY-6. Heated Staphylococcus R-48 was also the inducer of the production of Bacteroides JY-6 glycosidases. These glycosidases were induced well by natural flavonoid glycosides, such as poncirin, naringin and rutin, but were not by synthetic substrates, p-nitrophenyl ${\beta$-D-glucopyranoside and p-nitrophenyl ${\alpha}$-L-rhanmopyranoside.

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Comparative Study of Antioxidant Activity of Apple and Pear Peel

  • Kim, Kyung Soon;Roh, Kwang Soo
    • Korean Journal of Plant Resources
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    • v.26 no.3
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    • pp.347-354
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    • 2013
  • Apple and pear are popular fruits consumed in Korea and are common fruit in daily diet. In order to compare the antioxidant activity of the apple and pear peels, total polyphenol contents, total flavonoid contents, $ABTS^+$ free radical scavenging activity, and DPPH free radical scavenging activity were measured from hot water, ethanol, and methanol extracts of the two fruit peels. The total polyphenol and flavonoid contents were highest in 95% methanol extracts of the apple peelsand 70% ethanol extract of the pear peels, respectively. Total polyphenol contents of the pear peels were higher than that of apple peels, and total flavonoid contents of the apple peels were higher than that of pear peels. The apple and pear peels had the highest $ABTS^{+{\cdot}}$ and DPPH free radical scavenging activity in 95% methanol extracts and 70% ethanol extracts, respectively. $ABTS^{+{\cdot}}$ and DPPH free radical scavenging activity of pear peels was higher than that of apple peels, and the DPPH free radical scavenging activity of apple and pear peels were detected in hot water, 95% methanol, and 70% ethanol extracts, respectively. Ascorbic acid, a synthetic antioxidant used as positive control, had significantly higher scavenging activity than the apple and pear peels. In conclusion, the apple and pear peelshave great potential as natural antioxidants. Therefore, above results should be considered to provide the possibility for the development of high functional antioxidants.

Evaluation of the Antioxidant Contents of Korean Wild Leaf Vegetables

  • Ahn, Hee-Jung;Cho, Mun-Jung;Cho, Youn-Ok
    • Nutritional Sciences
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    • v.3 no.2
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    • pp.98-102
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    • 2000
  • The purpose of this study was to evaluate the antioxidative potential of Korean wild leaf vegetables. Antixoidative activity of chamchwi (Aster scaber), nurucchwi (Pleurospermum kamtschaticum) sumssukbujengee (Aster glheni), moshidae (Adenophora remotiflora), spinach (Spinacia oleracea)k was evaluated as a reference for commonly used synthetic antioxidant, BHA. We compared the content of $\beta$-carotene, vitamin C and vitamin E as antioxidant vitamins, and total phenolic compound including flavonoid as non-vitamin compounds in Korean wild leaf vegetables and spinach. Thiobarbituric acid (TBA) value of Pleurospermum kamtschaticum, Aster scaber and Adenophora remotiflor was only 18-20% of control. TBA value of Aster glheni was 40% of control. On the basis of moles, the high level of vitamin C is the major contributor to the total antioxidant vitamin contents of Pleurospermum kamschaticum and Adenophora remotiflor. The amounts of flavonoid as well as total phenolic compound in Pleurospermum kamtschaticum and Adenophora remotiflor were also much higher than those of spinach. The amounts of flavonoid as well as total phenolic compound in Aster glheni were much higher than those of spinach while total amount of antioxidant vitamins was significantly lower than that of spinach. These results suggest that Pleurospermum kamtschaticum and Adenophora remotiflor could have antioxidative potency in food. Because of the higher content of antioxidant vitamins in Pleurospermum kamtschaticum and Adenophora remotiflor, these Korean wild leaf vegetables may have preventive effects on degenerative diseases, which have been associated with free radical mediated events.

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Antibacterial Activity and Synergism of the Hybrid Antimicrobial Peptide, CAMA-syn

  • Jeong, Ki-Woong;Shin, So-Young;Kim, Jin-Kyoung;Kim, Yang-Mee
    • Bulletin of the Korean Chemical Society
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    • v.30 no.8
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    • pp.1839-1844
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    • 2009
  • A 20-residue hybrid peptide CA(1-8)-MA(1-12) (CAMA) incorporating residues 1-8 of cecropin A (CA) and residues 1-12 of magainin 2 (MA) has high antimicrobial activity without toxicity. To investigate the effects of the total positive charges of CAMA on the antibacterial activity and toxicity, a hybrid peptide analogue (CAMA-syn) was designed with substitutions of $Ile^{10}\;and\;Ser^{16}$ with Lys. According to CD spectra, structure of CAMA-syn with increase of cationicity was very similar to that of CAMA in DPC micelle. CAMA-syn showed antimicrobial activity similar with CAMA while CAMA-syn has no hemolytic activity and much lower cytotoxicity against RAW 264.7 macrophage cells than CAMA. Also, CAMA and CAMA-syn significantly inhibited NO production by LPSstimulated RAW264.7 macrophage at 10.0∼20.0 $\mu$M. CAMA-syn displayed salt resistance on antimicrobial activity against Escherichia coli at the physiological concentrations of $CaCl_2\;and\;MgCl_2$. The combination studies of peptides and antibiotics showed that CAMA-syn has synergistic effects with synthetic compound and flavonoid against Enterococcus faecalis and VREF. CAMA-syn can be a good candidate for the development of new antibiotics with potent antibacterial and synergistic activity but without cytotoxicity.

Development and Verification of Make-up Base Containing Aloe

  • Min, Hyejo;Kim, MinJung;Kim, Jeonghee
    • Journal of Fashion Business
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    • v.19 no.3
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    • pp.121-129
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    • 2015
  • Aloe is a popular and effective agent used to cosmetic ingredient. It could replace artificial pigment on make-up base product and it is highly probable that might be useful as ingredients of multi-functional color cosmetic. In this study, we made a makeup base containing aloe extract and tested the effectiveness, safety and stability. Contents of polyphenol and flavonoid from the aloe extract were measured. To determine the antimicrobial effect from the aloe we used the paper disc diffusion method. We assessed the safety of make-up base containing aloe to cultured macrophage RAW 264.7 cells by MTT assay. Polyphenol contents of aloe extract and flavonoid respectively were 48 mg/g and 10 mg/g, in the 10 % concentration aloe extract. In case of aloe make-up base, the clear zone against Stapylococcus epidermidis was 9~11 mm and Stapylococcus aureus was also 9~11 mm. Growth activity of macrophage RAW 264.7 cells was over 80% in all concentration of make-up base containing aloe and general make base product. In conclusion aloe extract may be able to substitute the synthetic pigments and considered to be uses for ingredients multi-functional color cosmetic's ingredient.

Antioxidant Activities of Methanol Extracts from Root Parts of Korean Salad Plants

  • Chon, Sang-Uk;Kim, Tae-Soon;Shin, Ji-San;Boo, Hee-Ock
    • Korean Journal of Plant Resources
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    • v.21 no.6
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    • pp.413-419
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    • 2008
  • Phenolics level, total flavonoid content, and antioxidant were determined from the methanol extracts of the eight medicinal plants using roots. Total phenolics were found as the highest levels in the methanol extracts of Arctium lappa, and followed by Youngia sonchifolia and Cirsium japonicum. Total amount of the each phenol compounds were detected in C. japonicum extracts ($319.2\;mg\;kg^{-1}$) as the greatest component, and followed by A. lappa ($96.3\;mg\;kg^{-1}$) and Y. sonchifolia ($22.9\;mg\;kg^{-1}$). Total flavonoid content showed the highest amount in methanol extracts from A. lappa (68.1 mg $100\;g^{-1}$) and followed by Y. sonchifolia (11.2 mg $100\;g^{-1}$) Lycoris radiate extracts (87.2%) had the highest nitrite scavenging activity and followed by A. lappa (81.5%) and Y. sonchifolia (77.5%). Methanol extracts of A. lappa at 25 mg $100\;g^{-1}$ exhibited the highest DPPH radical scavenging activity by 90.8%, even though less activity than synthetic antioxidants Vitamin C or butylated hydroxytoluene (BHT). Level of polyphenols was highly correlated with anti oxidative activity ($r^2$ = 0.85). The results suggest that several medicinal plants selected had the potent biological activities, and that their activities were differential depending on plant species.