• Title/Summary/Keyword: Lipoxygenase inhibition

Search Result 76, Processing Time 0.034 seconds

Antioxidant and Tyrosinase Inhibitory Activities from Seed Coat of Brown Soybean

  • Lee, Jin-Hwan;Baek, In-Youl;Ko, Jong-Min;Kang, Nam-Suk;Shin, Seong-Hyu;Lim, Sea-Gyu;Oh, Ki-Won;Shin, Sang-Ouk;Park, Keum-Yong;Park, Ki-Hun;Ha, Tae-Joung
    • Food Science and Biotechnology
    • /
    • v.17 no.1
    • /
    • pp.1-7
    • /
    • 2008
  • Soybeans with brown, black, and yellow seed coats were compared to total phenolic contents and antioxidant activities including 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radicals. Also, 3 seed coats were examined for inhibitory activities on tyrosinase and lipoxygenase-1 on the basis of spectrophotometric and polarographic methods. Among seed coat extracts, 80% methanol extract of brown soybean seed coat showed the highest total phenolic contents ($68.9{\pm}3.29\;mg$ GAE/g) as well as exhibited potent scavenging effects on the DPPH ($IC_{50}=4.3\;{\mu}g/mL$) and ABTS ($IC_{50}=3.7\;{\mu}g/mL$) radicals. In a polarographic experiment, this extract was potentially inhibited the oxidation of L-tyrosine and L-3,4-dihydroxy-phenylalanin (L-DOPA) catalyzed by mushroom tyrosinase with $IC_{50}$ values of 12.4 and $63.7\;{\mu}g/mL$, respectively. It was also detected inhibition of the tyrosinase catalyzed oxidation of L-DOPA with an $IC_{50}$ value of 120.3 mg/mL in UV spectrophotometric experiment. In addition, this extract inhibited the linoleic acid peroxidation catalyzed by lipoxygenase-1 with an $IC_{50}$ value of $4.0\;{\mu}g/mL$. These results suggest that brown soybean may possess more beneficial effect on human health than black and yellow soybeans.

Inhibitory Effects of Phyto Extract Mixture (PEM381) on Type I Allergic Reaction (식물추출 복합물(PEM381)의 제I형 알레르기 반응 억제 효과)

  • Kim, Kyung-Bum;Lee, Eu-Gene;Chai, Ok-Hee;Song, Chang-Ho;Jeong, Jong-Moon
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.36 no.2
    • /
    • pp.155-162
    • /
    • 2007
  • The purpose of this study is to investigate the anti type I allergic effects and mechanisms of the phyto extract mixture (PEM381) which contains Camellia sinensis (leaf), Psidium guajava (leaf), and Rosa hybrida (flower). PEM381 was tested for its inhibitory effects on arachidonic acid cascade related enzymes (5-lipoxygenase and cyclooxygenase), the mast cell mediated allergic reaction and passive cutaneous anaphylaxis. $IC_{50}$ value of PEM381 against 5-lipoxygenase was $14.11{\pm}0.51ppm$ while that of positive control (nordihy-droguaiaretic acid) was $0.54{\pm}0.08ppm$. PEM381 also exhibited considerable selective inhibition of cyclooxygenase-2. PEM381 could inhibit both degranulation and histamine release in a dose dependent manner from rat peritoneal mast cells activated by compound 48/80. In addition, oral administration of PEM381 showed an inhibitory effect on passive cutaneous anaphylaxis reaction activated by anti-dinitrophenyl IgE antibody in mice. These results suggest that PEM381 may be useful for the prevention and treatment of type Ⅰ allergy related diseases.

A Study on the Azolla imbricata using as a Cosmetic Active Ingredient (물개구리밥(Azolla imbricata)을 이용한 주요 활성성분의 분리 및 화장품 소재 개발 연구)

  • Song, Min-Hyeon;Bae, Jun-Tae;Lee, Geun-Su;Zhang, Yong-He;Pyo, Hyeong-Bae
    • Journal of the Society of Cosmetic Scientists of Korea
    • /
    • v.36 no.1
    • /
    • pp.71-77
    • /
    • 2010
  • The water fern Azolla belongs to the Azollaceae and forms a symbiotic association with a $N_2$-fixing cyanobacterium, referred to as Anabaena azollae, and this association has currently been demonstrated to have potential as a nitrogen source for rice production. Because of that, Azolla fern has been used not only as organic manure in southern China and northern Vietnam for a long time but also as food for animate creatures in the underwater and decontaminant in the water. However, the phenolic compounds and active materials of Azolla have not been examined in detail in the past studies. In the present study, anti-oxidant ability test and experiment to find a particular active material of Azolla imbricata and Azolla imbricata fraction (AIF) were performed. In anti-oxidant test such as DPPH test and lipoxygenase inhibition test, the value of test represented high activities compared with authentic sample - green tea and NDGA (nordihydroguaiaretic acid). In MMP-1 test, related to collagen protection and elasticity of skin, its inhibitory effect was measured over 75 %, and the phenolic compounds of AIF related with this activity were confirmed luteolin derivatives by using FT-IR spectroscopy, element analyzer (EA) and Liquid chromatography-MASS spectroscopy.

The In Vitro and In Vivo Effect of Lipoxygenase Pathway Inhibitors Nordihydroguaiaretic Acid and Its Derivative Tetra-O-methyl Nordihydroguaiaretic Acid against Brucella abortus 544

  • Reyes, Alisha Wehdnesday Bernardo;Kim, Heejin;Huy, Tran Xuan Ngoc;Nguyen, Trang Thi;Min, Wongi;Lee, Dongho;Hur, Jin;Lee, John Hwa;Kim, Suk
    • Journal of Microbiology and Biotechnology
    • /
    • v.32 no.9
    • /
    • pp.1126-1133
    • /
    • 2022
  • This study investigated the contribution of lipoxygenase (LOX) inhibitors, nordihydroguaiaretic acid (NDGA), tetra-O-methyl nordihydroguaiaretic acid (M4N) and zileuton (ZIL), and thromboxane A2 (TXA2) inhibitor 4,5-diphenylimidazole (DPI) in the proliferation of Brucella abortus infection. None of the compounds affected the uptake of Brucella into the macrophages. We determined the effect of neutralizing leukotriene B4 (LTB4) receptor and showed that the uptake of the bacteria was inhibited at 30 min post-infection. M4N treatment attenuated intracellular survival of Brucella at 2 h post-incubation but it was not observed in the succeeding time points. DPI treatment showed reduced survival of Brucella at 24 h post-incubation while blocking LTB4 receptor was observed to have a lower intracellular growth at 48 h post-incubation suggesting different action of the inhibitors in the course of the survival of Brucella within the cells. Reduced proliferation of the bacteria in the spleens of mice was observed in animals treated with ZIL or DPI. Increased serum cytokine level of TNF-α and MCP-1 was observed in mice treated with M4N or ZIL while a lower IFN-γ level in ZIL-treated mice and a higher IL-12 serum level in DPI-treated mice were observed at 7 d post-infection. At 14 d post-infection, ZIL-treated mice displayed reduced serum level of IL-12 and IL-10. Overall, inhibition of 5-LOX or TXA2 or a combination therapy promises a potential alternative therapy against B. abortus infection. Furthermore, strong ligands for LTB4 receptor could also be a good candidate for the control of Brucella infection.

EFFECTS OF INHIBITORY DRUGS ON THE ARACHIDONIC ACID METABOLISM OF PERIODONTAL TISSUE (치은 Arachidonic acid 대사산물의 억제약물에 관한 실험적 연구)

  • Han, Se-Hee;Oh, Kwi-Ok;Kim, Hyung-Seop
    • Journal of Periodontal and Implant Science
    • /
    • v.23 no.2
    • /
    • pp.243-259
    • /
    • 1993
  • The bone resorbing activity of $PGE_2$ and elevated level of prostaglandins(PGs) and thromboxanes (TXs) in inflamed gingiva which are cyclooxygenase(C) metabolites have been well documented. Nonsteroidal anti-inflammatory drugs(NSAIDs) have been known to suppress gingival inflammation and bone resorption through the specific inhibitory action on the C pathway thereby decrease of various C metabolites. Recent studies provide unequivocal results that gingival tissue metabolizes arachidonic acid(AA) mainly through lipoxygenase(L) pathway. And the results of our previous experiments suggest that indomethacin may have inhibitory action on L as well as C. Thus we started this study to show the influences of several C inhibitors on the L activity at therapeutic and toxic dosage. Periodontal tissue samples were obtained from patients with advanced periodontitis and incubated with $^{14}C-AA(0.2{\mu}Ci)$ and various enzyme inhibitors. The tissue lipid extracts were separated by means of thin layer chromatography(TLC) and analyzed by means of autoradiography and TLC analyzer. Our results showed that aspirin inhibited C more selectively than L, however at higher concentration it also decreased HETEs production significantly. Indomethacin showed dose-dependent inhibition of L as well as C and all of the L metabolites were decreased to the same degree by high concentration of indomethacin. AA-861, which is an experimental tool of selective L inhibitor, showed inhibition of HETEs production but no effect on the production of $TXB_2$, PGs and $LTB_4$. Various propionic acid derivatives NSAIDs(ibuprofen, flurbiprofen, naproxen) showed the same patterns of effect on AA metabolism each other that was profound inhibition of PGs production, to the less degree HETEs and $TXB_2$ production, and of no effect on the $LTB_4$ production.

  • PDF

The Roles of Arachidonic Acid and Calcium in the Angiotensin II-induced Inhibition of $Na^+$ Uptake in Renal Proximal Tubule Cells

  • Park, Soo-Hyun;Koh, Hyun-Joo;Lee, Yeun-Hee;Son, Chang-Ho;Park, Min-Kyoung;Lee, Young-Jae;Han, Ho-Jae
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.3 no.1
    • /
    • pp.83-91
    • /
    • 1999
  • Angiotensin II (ANG II) has a biphasic effect on $Na^+$ transport in proximal tubule: low doses of ANG II increase the $Na^+$ transport, whereas high doses of ANG II inhibit it. However, the mechanisms of high dose ANG II-induced inhibition on $Na^+$ uptake are poorly understood. Thus the aim of the present study was to investigate signal transduction pathways involved in the ANG II-induced inhibition of $Na^+$ uptake in the primary cultured rabbit renal proximal tubule cells (PTCs) in hormonally defined serum-free medium. ANG II $(10^{-9}\;M)-induced$ inhibition of $Na^+$ uptake was blocked by losartan $(10^{-8}\;M,\;AT_1\;antagonist),$ but not by PD123319 $(10^{-8}\;M,\;AT_2\;antagonist)$ (P<0.05). ANG II-induced inhibition of $Na^+$ uptake was also completely abolished by neomycin $(10^{-4}\;M,$ PLC inhibitor), W-7 $(10^{-4}\;M,$ calmodulin antagonist), and $AACOCF_3\;(10^{-6}\;M,\;PLA_2\;inhibitor)$ (P<0.05). ANG II significantly increased $[^3H]arachidonic$ acid (AA) release compared to control. The ANG II-induced $[^3H]AA$ release was blocked by losartan, $AACOCF_3,$ neomycin, and W-7, but not by PD123319. ANG II-induced $[^3H]AA$ release in the presence of extracellular $Ca^{2+}$ was greater than in $Ca^{2+}-free$ medium, and it was partially blocked by TMB-8 $(10^{-4}\;M,$ intracelluar $Ca^{2+}$ mobilization blocker). However, in the absence of extracellular $Ca^{2+},$ it was completely blocked by TMB-8. In addition, econazole $(10^{-6}\;M,$ cytochrome P-450 monooxygenase inhibitor) and indomethacin $(10^{-6}\;M,$ cyclooxygenase inhibitor) blocked ANG II-induced inhibition of $Na^+$ uptake, but NGDA $(10^{-6}\;M,$ lipoxygenase inhibitor) did not affect it. In conclusion, $PLA_2-mediated$ AA release is involved in ANG II-induced inhibition of $Na^+$ uptake and is modulated by $[Ca^{2+}]_i$ in the PTCs.

  • PDF

Chemicals Constituents from Leaves of Diospyros iturensis (Gürke) Letouzey & F. White and their Biological Activities

  • Feusso, Hermann Marius Feumo;Dongmo, Jean de dieu;Djomkam, Hermine Laure Maza;Akak, Carine Mvot;Lateef, Mehreen;Ahmed, Ayaz;Azebaze, Anatole Guy Blaise;Waffo, Alain Francois Kamdem;Ali, Muhammad Shaiq;Vardamides, Juliette Catherine
    • Natural Product Sciences
    • /
    • v.26 no.4
    • /
    • pp.311-316
    • /
    • 2020
  • The chemical investigation of the methanolic crude extract of leaves of Diospyros iturensis gave us 15 known secondary metabolites identified as mixture of α-amyrenone (1) and β-amyrenone (2), β-amyrin (3), mixture of β-sitosterol (4) and stigmasterol (5), betulin (6), uvaol (7), betulinic acid (8), ursolic acid (9), corosolic acid (10), actinidic acid (11),11-O-p-hydroxybenzoylbergenin (12), bergenin (13) and mixture of stigmasterol glucoside (14) and β-sitosterol glucoside (15) respectively. The structures of secondary metabolites were elucidated with the help of NMR and mass spectral data and by comparison of their spectral data with literature. Among the fifteen isolated compounds, four compounds were identified for the first time in Diospyros genus. These included uvaol (7), corosolic acid (10), actinidic acid (11) and 11-O-p-hydroxybenzoylbergenin (12). Crude methanolic extract of leaves and four isolated compounds including betulin (6), betulinic acid (8), 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) were evaluated for their antiproliferative activity against two cancer cell lines CAL-27 and NCI-H460 by the MTT assay, antioxidant potential and inhibitory activity against the lipoxygenase and urease enzymes, respectively. The results indicated that the methanolic crude extract of leaves exhibited moderate antioxidant activity and was inactive against the two cancer cell lines. Betulin (6), 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) exhibited moderate antioxidant and lipoxygenase inhibition with IC50 = 65.8, 85.6, 82.5 μM and IC50 = 58.5, 95.2, 76.2 μM, respectively. Furthermore, 11-O-p-hydroxybenzoylbergenin (12) and bergenin (13) exhibited moderate urease inhibition activity with IC50 values of 45.6 μM and 49.8 μM, respectively.

Study on the anti-inflammatory effects of Cannabis sativa L. seed oil complex (햄프(Cannabis sativa L.)씨드오일 복합물의 항염증 효과에 관한 연구)

  • Chae-Hyun Kim;Se Gie Kim;Young-Ah Jang;Yong-Jin Kwon
    • Journal of the Korean Applied Science and Technology
    • /
    • v.41 no.2
    • /
    • pp.251-259
    • /
    • 2024
  • This study evaluated the potential of hemp seed oil (Cannabis sativa L. seed oil, CSO) and hemp seed oil complex (Cannabis sativa L. seed oil complex, CSOC) as an anti-inflammatory material through comparative analysis. Anti-inflammatory effects of CSO and CSOC were confirmed through lipopolysaccharide (LPS)-induced RAW264.7 model. As a result of confirming the inhibition of lipid oxidation through lipoxygenase inhibitory activity, CSO was not inhibited, but COSC was inhibited by more than 70%. As a result of confirming cytotoxicity through MTT analysis, CSO did not show cytotoxicity, but CSOC showed cytotoxicity at over 200 ㎍/ml. In LPS-induced RAW264.7, the expression of inducible nitric oxide synthase (iNOS) and the production of nitric oxide (NO) were significantly inhibited by CSOC compared to CSO. Additionally, CSOC significantly inhibited the expression of cyclooxygenase (COX)-2 and the production of prostaglandin E2 (PGE2). Through this study, we confirmed that CSOC has superior anti-inflammatory effects than CSO and has the potential to be used as an anti-inflammatory material.

In vitro Antioxidant, Anti-allergic and Anti-inflammatory Effects of Ethanol Extracts from Korean Sweet Potato Leaves and Stalks (한국산 고구마잎과 고구마줄기 에탄올 추출물의 in vitro 항산화, 항알레르기 및 항염증효과)

  • Kwak, Chung Shil;Lee, Kun Jong;Chang, Jin Hee;Park, June Hee;Cho, Ji Hyun;Park, Ji Ho;Kim, Kyung Me;Lee, Mee Sook
    • Journal of the Korean Society of Food Science and Nutrition
    • /
    • v.42 no.3
    • /
    • pp.369-377
    • /
    • 2013
  • In order to increase the utilization of sweet potato leaves and stalks as much as roots, it is necessary to study their beneficial potential. In this study, the antioxidant, antiallergic and anti-inflammatory effects of sweet potato leaves and stalks were evaluated by measuring total polyphenol and flavonoid contents, DPPH radical scavenging effects, the reducing power and inhibition effects on xanthine oxidase (XO), 5-lipoxygenase (LOX), and cyclo-oxygenase (COX)-2 activities. Blanched sweet potato leaves (SL), raw whole purple stalks (ST) and peeled stalks (PST) were freeze-dried and extracted with 95% ethanol. Total polyphenol content was highest in SL (11.03 mg/g), followed by ST (0.87 mg/g), and PST (0.37 mg/g). Total flavonoid content was highest for SL (9.01 mg/g), followed by ST (0.50 mg/g) and PST (0.25 mg/g). The $IC_{50}$ for DPPH radical scavenging effects was highest for SL ($43.6{\mu}g/mL$), followed by ST ($308.4{\mu}g/mL$) and PST ($1,631.3{\mu}g/mL$). The reducing power was highest for SL ($59.72{\mu}g$ ascorbic acid eq./mL), followed by ST ($12.56{\mu}g$ ascorbic acid eq./mL) and PST ($2.18{\mu}g$ ascorbic acid eq./mL) with $1,000{\mu}g/mL$ of ethanol extract. The inhibition rate on XO activity was highest for SL (13.06%), followed by ST (5.05%) and PST (0.0%) at $250{\mu}g/mL$ extract treatment. The inhibition rate on COX-2 activity was highest for SL (55.34%), followed by ST (2.18%) and PST (0.0%) at $250{\mu}g/mL$ extract treatment. The inhibition rate on 5-LOX activity was highest for SL (91.16%), followed by ST (33.38%) and PST (14.93%) at $50{\mu}g/mL$ treatment. Taken together, sweet potato leaves showed high antioxidative, anti-allergic and anti-inflammatory activities, especially with very strong inhibition effects on 5-LOX activity. These beneficial effects of sweet potato leaves might be mainly caused by the high content of polyphenols and flavonoids.

Study on Anti-thrombotic Activity, Superoxide Generation in Human Neutrophils and Platelet Aggregation in Human Blood of Hwao-tang

  • Park Won Hwan;Park Soo Young;Park Tae Woo;Kim Jong Gu;Kim Seog Ha;Kim Cherl Ho
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.18 no.5
    • /
    • pp.1494-1504
    • /
    • 2004
  • The present paper reports the effects of Hwaotang an atherosclerosis using a spontaneous experimental model, We have also investigated the pharmacological effect of Hwaotang on collagen- and ADP-induced blood platelet aggregation, thrombin-induced conversion of fibrinogen and fibrinolysis in in vitro experiments, and various effects on stimuli-induced superoxide generation in human neutrophils. Hwao-tang was shown to have inhibitory effect on collagen- and ADP-induced blood platelet aggregation, on thrombin-induced conversion of fibrinogen to fibrin and on the activity of plasminogen or plasmin. Hwao-tang also significantly inhibited fMLP-induced superoxide generation in a concentration-dependent manner, but not that induced by arachidonic acid. Hwao-tang inhibited neutrophil functions, including degranulation, superoxide generation, and leukotriene B4 production, without any effect on 5-lipoxygenase activity. In conclusion, the protection of extracts of Hwao-tang on the ischemic infarction induced artificially might be involved to their inhibition of thrombotic action. The results also indicate that Hwao-tang exerts the effects on superoxide generation related to the inhibition of neutrophil functions.