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Journal articles on the topic 'Lipoxygenase inhibitory activity'

Author: Grafiati

Published: 3 June 2025

Last updated: 31 July 2025

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1

CHEN, Ching-Jiunn, Hui-Sheng HUANG, Yu-Tsong LEE, Chia-Yi YANG, and Wen-Chang CHANG. "Characterization and purification of a lipoxygenase inhibitor in human epidermoid carcinoma A431 cells." Biochemical Journal 327, no. 1 (1997): 193–98. http://dx.doi.org/10.1042/bj3270193.

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A lipoxygenase inhibitor in the cytosolic fraction of human epidermoid carcinoma A431 cells was characterized and purified. The cytosolic inhibitor lost the inhibitory activity upon heating at 75 °C for 15 min or pretreating with 1 mg/ml trypsin at 37 °C for 60 min. Cytosol, after dialysis, lost the inhibitory activity but its inhibitory activity recovered when 1 mM GSH was added to the dialysate. The inhibitory activity of cytosol was also abolished by treatment either with 1 mM iodoacetate at 4 °C for 1 h or with 0.5 mM H2O2. The pI of the inhibitor was approx. 7.0. In addition to 12-lipoxyg

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2

Boudreau, Luc H., Grégoire Lassalle-Claux, Marc Cormier, et al. "New Hydroxycinnamic Acid Esters as Novel 5-Lipoxygenase Inhibitors That Affect Leukotriene Biosynthesis." Mediators of Inflammation 2017 (2017): 1–12. http://dx.doi.org/10.1155/2017/6904634.

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Leukotrienes are inflammatory mediators that actively participate in the inflammatory response and host defense against pathogens. However, leukotrienes also participate in chronic inflammatory diseases. 5-lipoxygenase is a key enzyme in the biosynthesis of leukotrienes and is thus a validated therapeutic target. As of today, zileuton remains the only clinically approved 5-lipoxygenase inhibitor; however, its use has been limited due to severe side effects in some patients. Hence, the search for a better 5-lipoxygenase inhibitor continues. In this study, we investigated structural analogues of

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3

Goodwin, J. S., and D. Atluru. "Mechanism of action of glucocorticoid-induced immunoglobulin production: role of lipoxygenase metabolites of arachidonic acid." Journal of Immunology 136, no. 9 (1986): 3455–60. http://dx.doi.org/10.4049/jimmunol.136.9.3455.

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Abstract Glucocorticoids stimulate polyclonal immunoglobulin (Ig) production in cultures of human peripheral blood lymphocytes. The mechanism of action of glucocorticoids in this system, and indeed in any physiologic system, is unknown. Because glucocorticoids stimulate the production of phospholipase A2-inhibitory glycoproteins, we investigated whether glucocorticoids stimulate polyclonal Ig production by inhibition of arachidonic acid metabolism. Nonspecific lipoxygenase/cyclooxygenase inhibitors stimulate polyclonal Ig production in a manner similar to the effect of glucocorticoids, whereas

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4

Hadjipavlou-Litina, D., S. E. Bariamis, M. Militsopoulou, C. M. Athanassopoulos, and D. Papaioannou. "Trioxsalen derivatives with lipoxygenase inhibitory activity." Journal of Enzyme Inhibition and Medicinal Chemistry 24, no. 6 (2009): 1351–56. http://dx.doi.org/10.3109/14756360902932776.

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5

Carter, G. W., P. R. Young, D. H. Albert, et al. "5-lipoxygenase inhibitory activity of zileuton." Journal of Pharmacology and Experimental Therapeutics 256, no. 3 (1990): 929–37. https://doi.org/10.1016/s0022-3565(25)23086-5.

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6

Ha, Tae Joung, Ken-ichi Nihei, and Isao Kubo. "Lipoxygenase Inhibitory Activity of Octyl Gallate." Journal of Agricultural and Food Chemistry 52, no. 10 (2004): 3177–81. http://dx.doi.org/10.1021/jf034925k.

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7

Ha, Tae Joung, and Isao Kubo. "Lipoxygenase Inhibitory Activity of Anacardic Acids." Journal of Agricultural and Food Chemistry 53, no. 11 (2005): 4350–54. http://dx.doi.org/10.1021/jf048184e.

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8

Ha, Tae Joung, Kuniyoshi Shimizu, and Isao Kubo. "Lipoxygenase inhibitory activity of alkyl protocatechuates." Food Chemistry 159 (September 2014): 471–76. http://dx.doi.org/10.1016/j.foodchem.2014.03.037.

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9

Lončarić, Melita, Ivica Strelec, Valentina Pavić, Domagoj Šubarić, Vesna Rastija, and Maja Molnar. "Lipoxygenase Inhibition Activity of Coumarin Derivatives—QSAR and Molecular Docking Study." Pharmaceuticals 13, no. 7 (2020): 154. http://dx.doi.org/10.3390/ph13070154.

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Lipoxygenases (LOXs) are a family of enzymes found in plants, mammals, and microorganisms. In animals and plants, the enzyme has the capability for the peroxidation of unsaturated fatty acids. Although LOXs participate in the plant defense system, the enzyme’s metabolites can have numerous negative effects on human health. Therefore, many types of research are searching for compounds that can inhibit LOXs. The best quantitative structure–activity relationship (QSAR) model was obtained using a Genetic Algorithm (GA). Molecular docking was performed with iGEMDOCK. The inhibition of lipoxygenase

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10

Handayani, Nadya Febri, Berna Elya, and Nuraini Puspitasari. "CYCLEA BARBATA LEAF EXTRACT: LIPOXYGENASE INHIBITORY ACTIVITY AND PHYTOCHEMICAL SCREENING." International Journal of Applied Pharmaceutics 10, no. 1 (2018): 106. http://dx.doi.org/10.22159/ijap.2018.v10s1.22.

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Objective: The aim of this study was to test the anti-inflammatory activity of methanol, ethyl acetate, and n-hexane Cyclea barbata Mier. leaf extractsusing a lipoxygenase inhibition method.Methods: Enzyme activity assay was performed using colorimetric method with lipoxygenase from soybean and linoleic acid as a substrate.Absorbance was measured at 234 nm. The total flavonoid content of the most active extract was determined using a colorimetric method with AlCl3and phytochemical screening.Results: The ethyl acetate extract had the highest lipoxygenase inhibiting activity, with an IC50 value

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11

Ménard, Luc, Michel Laviolette, and Pierre Borgeat. "Studies of the inhibitory activity of MK-0591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-yl-methoxy)-indol-2-yl]-2,2-dimethyl propanoic acid) on arachidonic acid metabolism in human phagocytes." Canadian Journal of Physiology and Pharmacology 70, no. 6 (1992): 808–13. http://dx.doi.org/10.1139/y92-108.

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We have investigated the inhibitory activity of compound MK-0591 (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-yl-methoxy)-indol-2-yl]-2,2-dimethyl propanoic acid) on 5-lipoxygenase (5-LO) product synthesis in various human phagocytes stimulated with either the ionophore A23187, opsonized zymosan (OPZ), platelet-activating factor (PAF), or forrnyl-methionyl-leucyl-phenylalanine (fMLP). The lipoxygenase products were analyzed by reversed-phase HPLC. MK-0591 inhibited the formation of 5-hydroxyeicosatetraenoic acid, leukotriene (LT) B4, its Ω-oxidation products, and 6-trans-isomers with I

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12

Pontiki, Eleni, and Dimitra Hadjipavlou-Litina. "Multi-Target Cinnamic Acids for Oxidative Stress and Inflammation: Design, Synthesis, Biological Evaluation and Modeling Studies." Molecules 24, no. 1 (2018): 12. http://dx.doi.org/10.3390/molecules24010012.

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Inflammation is a complex phenomenon that results as a healing response of organisms to different factors, exerting immune signaling, excessive free radical activity and tissue destruction. Lipoxygenases and their metabolites e.g., LTB4, are associated with allergy, cell differentiation and carcinogenesis. Lipoxygenase 12/15 has been characterized as a mucosal-specific inhibitor of IgA and a contributor to the development of allergic sensitization and airway inflammation. Development of drugs that interfere with the formation or effects of these metabolites would be important for the treatment

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13

Namngam, Chaianun, Praphan Pinsirodom, and Supakorn Boonyuen. "Fractionation, antioxidant and inhibitory activity of Thai mango seed kernel extracts." Czech Journal of Food Sciences 36, No. 1 (2018): 8–15. http://dx.doi.org/10.17221/225/2017-cjfs.

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Mango seed kernel extracts (MSKE) from Kaew and Choke-Anan mango cultivars were fractionated using Sephadex LH-20 column chromatography. Antioxidant activity and the inhibitory effects on tyrosinase, 5-lipoxygenase, hyaluronidase and α-glucosidase of MSKE fractions were evaluated. The key components of polyphenol, found in the most active fraction, were identified using LC-ESI-MS. Three major isolates were obtained from both cultivars of the MSKE with the absorbance being higher for Choke-Anan than Kaew. Fraction 3 of MSKE from both cultivars showed significantly (P ≤ 0.05) higher antioxidant

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14

Hadjipavlou-Litina, Dimitra, Thomas Garnelis, Constantinos M. Athanassopoulos, and Dionissios Papaioannou. "Kukoamine A analogs with lipoxygenase inhibitory activity." Journal of Enzyme Inhibition and Medicinal Chemistry 24, no. 5 (2009): 1188–93. http://dx.doi.org/10.1080/14756360902779193.

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15

Alvarenga, Tavane A., Camila S. Bertanha, Pollyanna F. de Oliveira, et al. "Lipoxygenase inhibitory activity ofCuspidaria pulchraand isolated compounds." Natural Product Research 29, no. 11 (2014): 1083–86. http://dx.doi.org/10.1080/14786419.2014.981182.

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16

Saragatsis, Michail, and Eleni Pontiki. "Synthesis and Antioxidant Activities of Novel Pyrimidine Acrylamides as Inhibitors of Lipoxygenase: Molecular Modeling and In Silico Physicochemical Studies." Molecules 29, no. 6 (2024): 1189. http://dx.doi.org/10.3390/molecules29061189.

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The pyrimidine ring is present in various biomolecules such as DNA and RNA bases, aminoacids, vitamins, etc. Additionally, many clinically used drugs including methotrexate and risperidone contain the pyrimidine heterocyclic scaffold as well. Pyrimidine derivatives present diverse biological activities including antioxidant and anticancer activities and can be considered as privileged scaffolds in drug discovery for the treatment of various diseases. Piperidine pyrimidine amides have gained significant attention due to their enzymatic inhibitory activity. Based on our experience and ongoing in

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17

Chedea, Veronica Sanda, Adela Pintea, Andrea Bunea, Cornelia Braicu, Andreea Stanila, and Carmen Socaciu. "Physalis alkekengiCarotenoidic Extract Inhibitor of Soybean Lipoxygenase-1 Activity." BioMed Research International 2014 (2014): 1–7. http://dx.doi.org/10.1155/2014/589168.

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The aim of this study was to evaluate the effect of the carotenoidic saponified extract ofPhysalis alkekengisepals (PA) towards the lipoxygenase (LOX) oxidation of linoleic acid. Lipoxygenase activity in the presence of carotenoids, standard and from extract, was followed by its kinetic behaviour determining the changes in absorption at 234 nm. The standard carotenoids used wereβ-carotene (β-car), lutein (Lut), and zeaxanthin (Zea). The calculated enzymatic specific activity (ESA) after 600 s of reaction proves that PA carotenoidic extract has inhibitory effect on LOX oxidation of linoleic aci

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18

Shaikh, Zara, Uzma Ashiq, Rifat Ara Jamal, et al. "Synthesis, characterization, lipoxygenase, and tyrosinase inhibitory activities of non- cytotoxic titanium(III) and (IV) hydrazide complexes." Bulletin of the Chemical Society of Ethiopia 37, no. 2 (2022): 315–33. http://dx.doi.org/10.4314/bcse.v37i2.6.

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ABSTRACT. Ti(III) and (IV) hydrazide complexes were synthesized, characterized, and screened for their tyrosinase and lipoxygenase inhibitory and cytotoxic activities. The geometry of Ti(III) hydrazide complexes is tentatively assigned as octahedral. Magnetic moments were found around 1.7 B.M. and electronic spectral transition in the range of 495-518 nm. Evaluation of Ti(IV) and Ti(III) hydrazide complexes for tyrosinase and lipoxygenase inhibitory activities revealed varying inhibition potential. Hydrazide ligands were inactive against tyrosinase, while significant activity was observed agai

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19

Curini, Massimo, Francesco Epifano, Salvatore Genovese, et al. "Lipoxygenase Inhibitory Activity of Boropinic Acid, Active Principle of Boronia Pinnata." Natural Product Communications 1, no. 12 (2006): 1934578X0600101. http://dx.doi.org/10.1177/1934578x0600101214.

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Boropinic acid and other natural prenyloxycinnamic and benzoic acids were easily synthesized in high yield by a two-step sequence from the corresponding p-hydroxy aromatic acids and were assayed for radical scavenging activity using the DPPH test and for inhibition of enzymatic lipid peroxidation mediated by soybean 5-lipoxygenase. Compared to other acids and to known antioxidant compounds like BHT, Trolox and ascorbic acid, boropinic acid was far more active in the lipoxygenase test (IC50 = 7.6 ng/mL, p < 0.05). The recorded inhibition value suggested that boropinic acid acted as an enzyme

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20

Asma, Noor. "In-silico analysis of tenidap and its derivative as a novel 5-lipoxygenase inhibitor." International Journal of Pharmaceutical Sciences and Developmental Research 3, no. 1 (2018): 036–38. https://doi.org/10.17352/ijpsdr.000015.

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Tenidap is a derivative of Flavonoids which are actually plant derivatives, it shows inhibition activity of 5-lipoxygenase. Molecular models were directed to discover molecular docking mode, also to help explain molecular tool behind its inhibitory action. Molecular relations of tenidap with the catalytic trio (His523, His518, Ile875) inside active or dynamic position of 5-lipoxygenase through hydrogen bonding, appears to the major reason elaborate in its substantial 5-lipoxygenase activity of inhibition.

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21

Kubo, Isao, Kazuo Ha, Kazuo Tsujimoto, Felismino E. Tocoli, and Ivan R. Green. "Evaluation of Lipoxygenase Inhibitory Activity of Anacardic Acids." Zeitschrift für Naturforschung C 63, no. 7-8 (2008): 539–46. http://dx.doi.org/10.1515/znc-2008-7-812.

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6-Alkylsalicylic acids inhibit the linoleic acid peroxidation catalyzed by soybean lipoxygenase- 1 (EC 1.13.11.12, type 1) competitively and without pro-oxidant effects. This activity is largely dependent on the nature of their alkyl side chains. Inhibitory activities of anacardic acids, viz. 6-pentadec(en)ylsalicylic acids, isolated from the cashew Anacardium occidentale, were initially used for comparison because their aromatic head portions are the same. Consequently, the data should be interpreted to mean that changes in the hydrophobic side chain tail portions of the molecules evaluated c

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22

Ahmad, Viqar U., Farzana Kousar, Afsar Khan, et al. "Isolation of a New Lipoxygenase Active Saponin and a New Triterpenoid from the Leaves of Trachelospermum lucidum." Zeitschrift für Naturforschung B 60, no. 12 (2005): 1287–90. http://dx.doi.org/10.1515/znb-2005-1212.

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A new saponin trivially named leucioside (1) and a new triterpenoid along with two known lignans trachelosiaside (3) and matairesionol (4) C-glycosides, were isolated from the butanolic fraction of Trachelospermum lucidum. Compounds 1 and 4 showed potent inhibitory activity against lipoxygenase while compounds 2 and 3 showed moderate activity against lipoxygenase.

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23

Elya, Berna, Nuraini Puspitasari, and Annisa Chairani Sudarmin. "ANTIOXIDANT ACTIVITY AND INHIBITION OF LIPOXYGENASE ACTIVITY ETHANOL EXTRACT OF ENDOSPERM ARENGA PINNATA (WURMB) MERR." Asian Journal of Pharmaceutical and Clinical Research 10, no. 17 (2017): 76. http://dx.doi.org/10.22159/ajpcr.2017.v10s5.23102.

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Objective: The purpose of this study is to determine the antioxidant activity and the potential inhibition of lipoxygenase activity from sugar palm fruit.Methods: Antioxidant activity was evaluated by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ferric reducing antioxidant power (FRAP) methods. Inhibition of lipoxygenase activity was performed in vitro. Sugar palm fruit was macerated with 95% ethanol.Results: The results showed that sugar palm fruit ethanol extract has antioxidant activity when using DPPH method with EC50 of 141.3929 μg/mL and the FRAP method with EC50 of 60.2083 μg/mL. Inhibi

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24

YATABE, Takumi, Yoshio KAWAI, Teruo OKU, and Hirokazu TANAKA. "Studies on 5-Lipoxygenase Inhibitors. I. Synthesis and 5-Lipoxygenase-Inhibitory Activity of Novel Hydroxamic Acid Derivatives." CHEMICAL & PHARMACEUTICAL BULLETIN 46, no. 6 (1998): 966–72. http://dx.doi.org/10.1248/cpb.46.966.

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25

Avelia, Sismita, Marista Gilang Mauldina, and Berna Elya. "ANTIOXIDANT ACTIVITY AND LIPOXYGENASE INHIBITORY ASSAY WITH TOTAL FLAVONOID CONTENT OF GARCINIA LATERIFLORA BLUME LEAVES EXTRACT." Asian Journal of Pharmaceutical and Clinical Research 10, no. 17 (2017): 163. http://dx.doi.org/10.22159/ajpcr.2017.v10s5.23122.

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Objective: Garcinia lateriflora Blume has been reported to have antioxidant activity using the 2,2-diphenyl-1-picrylhydrazyl method with methanol, ethyl acetate, and n-hexane leaves extract inhibitory concentration 50% (IC50) levels of 6.18, 8.03, and 156.8 μg/mL, respectively. Meanwhile, there has been no literature regarding G. lateriflora Blume’s lipoxygenase inhibition activity. The aim of this study was to determine the potential antioxidant activity and lipoxygenase inhibition activity of three leaf extracts of G. lateriflora Blume. Methods: These study test methods involved an assessmen

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Es-Saady, D., A. Najid, A. Simon, Y. Denizot, A. J. Chulia, and C. Delage. "Effects of Ursolic Acid and its Analogues on Soybean 15-Lipoxygenase Activity and the Proliferation Rate of A human Gastric Tumour Cell Line." Mediators of Inflammation 3, no. 3 (1994): 181–84. http://dx.doi.org/10.1155/s0962935194000244.

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The authors have previously isolated and purified ursolic acid from heather flowers (Calluna vulgarts). This terpene was found to inhibit HL-60 leukaemic cell proliferation and arachidonic acid oxidative metabolism in various cell species. The effects of ursolic acid and its analogues on soybean 15-lipoxygenase activity and on the proliferation of a human gastric tumour cell line (HGT), have been assessed. These triterpenes inhibited soybean 15-lipoxygenase at its optimal activity (pH 9). The proliferation ofHGT was decreased in a dose-dependent manner. At 20 μM the rank order is: ursolic acid

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27

Papaioannou, Paraskevi, Diamanto Lazari, Anastasia Karioti, et al. "Phenolic Compounds with Antioxidant Activity from Anthemis tinctoria L. (Asteraceae)." Zeitschrift für Naturforschung C 62, no. 5-6 (2007): 326–30. http://dx.doi.org/10.1515/znc-2007-5-603.

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From the aerial parts of Anthemis tinctoria L. subsp. tinctoria var. pallida DC. (Asteraceae), one new cyclitol glucoside, conduritol F-1-O-(6′-O-E-p-caffeoyl)-β-d-glucopyranoside (1), has been isolated together with four flavonoids, nicotiflorin (2), isoquercitrin (3), rutin (4) and patulitrin (5). The structures of the isolated compounds were established by means of NMR, MS, and UV spectral analyses. Methanolic extract and pure isolated compounds were examined for their free radical, scavenging activity, using the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free stable radical, and for their inhibi

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28

Saadullah, Malik, Muhammad Asif, Muhammad Uzair, et al. "Pharmacological evaluation of the hypoglycemic and anti- Alzheimer’s activities of aerial parts of Breynia distachia (Phyllanthaceae)." Tropical Journal of Pharmaceutical Research 21, no. 3 (2022): 579–87. http://dx.doi.org/10.4314/tjpr.v21i3.18.

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Purpose: To determine the cytotoxic, bronchorelaxant, spasmolytic, antidiabetic, α-glucosidase, acetylcholinesterase, butyrylcholinesterase, α-chymotrypsin and lipoxygenase inhibitory attributes of methanol and dichloromethane extracts of the aerial parts of Breynia distachia.Methods: The dichloromethane and methanol extracts of the aerial parts of the plant were prepared by maceration. Various ex vivo assays were employed, such as the brine shrimp lethality assay, lipoxygenase inhibitory activity assay, α-glucosidase inhibitory assay and α-chymotrypsin assay, as well as assays to assess the s

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29

Yahyavi, Hoda, Fatemeh Hosseinzadeh, Nastaran Karimi, et al. "Synthesis and biological evaluation of 1,3,4,5-tetrasubstituted pyrazole derivatives." Zeitschrift für Naturforschung B 71, no. 9 (2016): 973–77. http://dx.doi.org/10.1515/znb-2016-0092.

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AbstractWe report a solvent-free synthesis of novel 1,3,4,5-tetrasubstituted pyrazoles and investigate their inhibitory activity against soybean 15-lipoxygenase. It was revealed that all synthesized compounds exhibited good activity, and among them, 3-(furan-2-yl)-1,4,5-triphenyl-1H-pyrazole (5j) showed 10 times stronger inhibitory activity in comparison to the reference drug quercetin.

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30

Schneider, Isabella, and Franz Bucar. "Lipoxygenase inhibitors from natural plant sources. Part 1: Medicinal plants with inhibitory activity on arachidonate 5-lipoxygenase and 5-lipoxygenase[sol ]cyclooxygenase." Phytotherapy Research 19, no. 2 (2005): 81–102. http://dx.doi.org/10.1002/ptr.1603.

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31

YATABE, T., Y. KAWAI, T. OKU, and H. TANAKA. "ChemInform Abstract: 5-Lipoxygenase Inhibitors. Part 1. Synthesis and 5-Lipoxygenase-Inhibitory Activity of Novel Hydroxamic Acid Derivatives." ChemInform 29, no. 48 (2010): no. http://dx.doi.org/10.1002/chin.199848092.

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32

Feng, Jie, Xin Du, Hui Liu, et al. "Manganese-mefenamic acid complexes exhibit high lipoxygenase inhibitory activity." Dalton Trans. 43, no. 28 (2014): 10930–39. http://dx.doi.org/10.1039/c4dt01111b.

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33

VICAŞ, SIMONA IOANA, VERONICA SANDA CHEDEA, and CARMEN SOCACIU. "INHIBITORY EFFECTS OF ISOFLAVONES ON SOYBEAN LIPOXYGENASE-1 ACTIVITY." Journal of Food Biochemistry 35, no. 2 (2011): 613–27. http://dx.doi.org/10.1111/j.1745-4514.2010.00405.x.

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Ahmad, Ijaz, Abdul Malik, Nighat Afza, et al. "Enzymes Inhibitory Constituents From Buddleja Crispa." Zeitschrift für Naturforschung B 60, no. 3 (2005): 341–46. http://dx.doi.org/10.1515/znb-2005-0319.

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Steroidal galactoside 1 and aryl esters 2 and 3 have been isolated from Buddleja crispa, along with ginipin 4, gardiol 5, 1-heptacosanol 6, and methyl benzoate 7, isolated for the first time from this species. The structures of all of the compounds were determined by spectroscopic techniques and chemical studies. The steroidal galactoside 1 is an inhibitor of lipoxygenase. Compounds 1- 3 displayed inhibitory activity against butyrylcholinesterse, while compounds 2 and 3 further showed inhibition against acetylcholinesterase

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35

Kim, Ki H., Yvonne C. Martin, Dee W. Brooks, Richard D. Dyer, and George W. Carter. "Quantitative Structure-Activity Relationships of 5-Lipoxygenase Inhibitors. Inhibitory Potency of Pyridazinone Analogues." Journal of Pharmaceutical Sciences 83, no. 3 (1994): 433–38. http://dx.doi.org/10.1002/jps.2600830334.

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36

Salleh, Wan Mohd Nuzul Hakimi Wan, Muhammad Helmi Nadri, and Shamsul Khamis. "Chemical Composition and Lipoxygenase Inhibitory Activity of the Essential Oil of Alstonia Angustiloba." Chemistry Journal of Moldova 16, no. 2 (2021): 112–16. http://dx.doi.org/10.19261/cjm.2021.848.

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This study was aimed to investigate the chemica l compositions and lipoxygenase inhibitory activity of the essential oil from Alstonia angustiloba growing in Malaysia. The essential oils were obtained by hydrodistillation and fully characterized by gas chromatography and gas chromatography-mass spectrometry. Analysis of the A. angustiloba essential oil resulted in the identification of twenty-five chemical components, attributed 90.8% of the total oil. The most abundant components of A. angustiloba oil were linalool (21.2%), 1,8-cineole (16.8%), α-terpineol (9.5%), terpinene-4-ol (8.5%), β-car

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37

Schneider, Isabella, and Franz Bucar. "Lipoxygenase inhibitors from natural plant sources. Part 2: medicinal plants with inhibitory activity on arachidonate 12-lipoxygenase, 15-lipoxygenase and leukotriene receptor antagonists." Phytotherapy Research 19, no. 4 (2005): 263–72. http://dx.doi.org/10.1002/ptr.1604.

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38

Surapinit, Serm, Jirapast Sichaem, and Santi Tip-pyang. "Non-redox Lipoxygenase Inhibitors from Nauclea orientalis." Natural Product Communications 13, no. 1 (2018): 1934578X1801300. http://dx.doi.org/10.1177/1934578x1801300111.

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Eight alkaloids recently isolated from the roots of Nauclea orientalis (L.) L. were obtained to evaluate the lipoxygenase (LOX) inhibitory activity. According to the LOX inhibitory assay, the cis isomer 1 (IC50 39.2±1.1 μM) was more potent than the trans isomer 2 (IC50 52.1±1.5 μM) (P < 0.05). Compound 5 (IC5057.8±1.8 μM) was more potent than 6 (IC50 97.6±3.4 μM), 3 (IC50 112.1±2.6 μM) and 4 (inactive) (P <0.05), respectively. Alkaloid glycosides 7 and 8 were completely inactive in a screening assay. All active indole alkaloids were inactive in DPPH and 13-HPOD scavenging assays at the c

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39

Shindo, K., J. R. Baker, D. A. Munafo, and T. D. Bigby. "Captopril inhibits neutrophil synthesis of leukotriene B4 in vitro and in vivo." Journal of Immunology 153, no. 12 (1994): 5750–59. http://dx.doi.org/10.4049/jimmunol.153.12.5750.

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Abstract The aim of this investigation was to determine the effects of metalloproteinase inhibitors on leukotriene (LT) A4 hydrolase in human neutrophil cytosol and to examine the effects of captopril on intact neutrophils in vitro and in vivo. Cytosolic fractions were assayed for LTA4 hydrolase and 5-lipoxygenase activity in the presence or absence of inhibitors. Only bestatin, 1,10-O-phenanthroline, captopril and fosinoprilat demonstrated significant effects. The IC50 of captopril and fosinoprilat for LTA4 hydrolase activity were 500 microM and 1 mM, respectively. No inhibition of 5-lipoxyge

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Ng, Chean, Kamal Rullah, Faridah Abas, et al. "Hits-to-Lead Optimization of the Natural Compound 2,4,6-Trihydroxy-3-geranyl-acetophenone (tHGA) as a Potent LOX Inhibitor: Synthesis, Structure-Activity Relationship (SAR) Study, and Computational Assignment." Molecules 23, no. 10 (2018): 2509. http://dx.doi.org/10.3390/molecules23102509.

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A new series of 2,4,6-trihydroxy-3-geranyl-acetophenone (tHGA) analogues were synthesized and evaluated for their lipoxygenase (LOX) inhibitory activity. Prenylated analogues 4a–g (half maximal inhibitory concentration (IC50) values ranging from 35 μ M to 95 μ M) did not exhibit better inhibitory activity than tHGA (3a) (IC50 value: 23.6 μ M) due to the reduction in hydrophobic interaction when the alkyl chain length was reduced. One geranylated analogue, 3d, with an IC50 value of 15.3 μ M, exhibited better LOX inhibitory activity when compared to tHGA (3a), which was in agreement with our pre

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Venkateswarlu, Somepalli, Gandrotu Narasimha Murty, Meka Satyanarayana, and Vidavalur Siddaiah. "Design, Synthesis and Biological Activities of Dihydroaurones." Asian Journal of Chemistry 33, no. 6 (2021): 1396–402. http://dx.doi.org/10.14233/ajchem.2021.23139.

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To widen aurones applicability in achromatic food and cosmetic applications, a series of dihydroaurones were designed to mimic natural aurones as well as synthetic aurones. Dihydroaurones have been synthesized from the corresponding aurones by hydrogenation. These dihydroaurones and their corresponding aurones were screened for antioxidant, anti-inflammatory and tyrosinase enzyme inhibitory activity. Synthesized dihydroaurones (3b-f) displayed superior antioxidant activity in superoxide free radical scavenging assay than the standard gallic acid. Dihydroaurones (3b-f) also exhibited significan

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Conese, M., P. Montemurro, R. Fumarulo, et al. "Inhibitory Effect of Retinoids on the Generation of Procoagulant Activity by Blood Mononuclear Phagocytes." Thrombosis and Haemostasis 66, no. 06 (1991): 662–65. http://dx.doi.org/10.1055/s-0038-1646482.

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SummaryRetinoids are known to modulate several functions of mononuclear phagocytes. We have studied the effect of retinyl acetate (RAc) and retinoic acid (RA) on the production of procoagulant activity (PCA) by human peripheral blood mononuclear cells stimulated with endotoxin (1 εg/ml, 4 or 20 h at 37°C). Both compounds caused a dose-dependent reduction in the expression of cell-associated PCA (from 86 to <10% of control in the range of concentration comprised between 0.1 and 100 εM). This effect was also observed when the cells were exposed to retinoids for 10 min and washed before challe

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Kubo, Isao, Tae Joung Ha, and Kuniyoshi Shimizu. "Lipoxygenase Inhibitory Activity of 6-Pentadecanylsalicylic Acid without Prooxidant Effect." Natural Product Communications 5, no. 1 (2010): 1934578X1000500. http://dx.doi.org/10.1177/1934578x1000500121.

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6-Pentadecanylsalicylic acid, referred to as anacardic acid (C15:0), was found to inhibit the linoleic acid peroxidation competitively catalyzed by soybean lipoxygenase-1 (EC 1.13.11.12, Type 1) with an IC50 of 14.3 μM (4.88 μg/mL). This inhibition is a reversible reaction without pro-oxidant effects. The inhibition kinetics analyzed by Dixon plots indicates that anacardic acid (C15:0) is a competitive inhibitor and the inhibition constant, KI, was established as 6.4 μM. The hydrophilic head (salicylic acid) portion first chelates the iron in the active site and then the hydrophobic tail porti

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Lapenna, Domenico, Giuliano Ciofani, Sante Donato Pierdomenico, et al. "Inhibitory activity of salicylic acid on lipoxygenase-dependent lipid peroxidation." Biochimica et Biophysica Acta (BBA) - General Subjects 1790, no. 1 (2009): 25–30. http://dx.doi.org/10.1016/j.bbagen.2008.09.007.

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M. N. H. W. Salleh, W., N. A. Hashim, and S. Khamis. "Chemical constituents and lipoxygenase inhibitory activity of Piper stylosum Miq." Bulletin of the Chemical Society of Ethiopia 33, no. 3 (2019): 587. http://dx.doi.org/10.4314/bcse.v33i3.19.

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Lewis, Timothy A., Michelle A. Young, Mark P. Arrington, et al. "Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity." Bioorganic & Medicinal Chemistry Letters 14, no. 22 (2004): 5591–94. http://dx.doi.org/10.1016/j.bmcl.2004.08.060.

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Olufunmilayo., Olarenwaju, OLOGE Mary, Oyemitan Idris, et al. "Anti-inflammatory potentials, membrane stabilizing and xanthine oxidase inhibitory activities of Clerodendrum volibule ethanolic leaf extract on carragenaan- induced inflammation in rats." International Journal of Pharmacology and Toxicology 6, no. 1 (2018): 7. http://dx.doi.org/10.14419/ijpt.v6i1.8410.

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The folkloric use of Clerodendrum volubile P Beauv (Verbenaceae) for treatment of inflammatory conditions in the Southern part of Nigeria has been reported. The anti-inflammatory action of the ethanolic leaf extract on carrageenan-induced rat paw oedema, lipoxygenase and xanthine oxidase inhibitory effects, and membrane stabilizing potential were evaluated. The extract reduced carrageenan-induced rat paw oedema in a dose dependent manner compared to control group. C. volubile inhibited xanthine oxidase activity in a dose - dependent manner; at 0.5 mg/ml it exhibited maximum inhibitory activity

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Taddeo, Vito Alessandro, Francesco Epifano, Salvatore Genovese, and Serena Fiorito. "Inhibition of Soybean 15-Lipoxygenase by Naturally Occurring Acetophenones and Derricidin." Natural Product Communications 10, no. 4 (2015): 1934578X1501000. http://dx.doi.org/10.1177/1934578x1501000413.

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Three selected naturally occurring oxyprenylated secondary metabolites, namely 2-hydroxy4-isopentenyloxyacetophenone (1), 4-geranyloxy-2-hydroxyacetophenone (2), 4-farnesyloxyacetophenone (3), and derricidin (4) were synthesized and their inhibitory potency against soybean 15-lipoxygenase evaluated. Compounds 1 and 4 showed the most potent inhibitory activity with IC50 values of 2.5 μM and 0.6 μM.

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Mavridis, Evangelos, Eleftherios Bermperoglou, Eleni Pontiki, and Dimitra Hadjipavlou-Litina. "5-(4H)-Oxazolones and Their Benzamides as Potential Bioactive Small Molecules." Molecules 25, no. 14 (2020): 3173. http://dx.doi.org/10.3390/molecules25143173.

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The five membered heterocyclic oxazole group plays an important role in drug discovery. Oxazolones present a wide range of biological activities. In this article the synthesis of 4-substituted-2-phenyloxazol-5(4H)-ones from the appropriate substituted aldehydes via an Erlenmeyer–Plochl reaction is reported. Subsequently, the corresponding benzamides were produced via a nucleophilic attack of a secondary amine on the oxazolone ring applying microwave irradiation. The compounds are obtained in good yields up to 94% and their structures were confirmed using IR, 1H-NMR, 13C-NMR and LC/MS data. The

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Pruzanski, W., B. P. Kennedy, H. van den Bosch, E. Stefanski, M. Wloch, and P. Vadas. "Tenidap sodium inhibits secretory non-pancreatic phospholipase A2synthesis by foetal rat calvarial osteoblasts." Mediators of Inflammation 4, no. 1 (1995): 67–70. http://dx.doi.org/10.1155/s0962935195000123.

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Tenidap (TD) was initially defined as a dual inhibitor of cyclooxygenase and lipoxygenase. This study was designed to assess its inhibitory activity against proinflammatory phospholipase A2. This study shows that TD inhibits the synthesis of pro-inflammatory secretory non-pancreatic phospholipase A2(sPLA2). Concentrations as low as 0.25 μg/ml (0.725 μM) reduced the release of sPLA2by 40% from foetal rat calvarial osteoblasts stimulated with IL-1β and TNFα, whereas a concentration of 2.5 μg/ml (7.25 μM) reduced the release by over 80%. TD also markedly reduced the release of sPLA2from unstimula

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