Category: 321673-30-7

Miyabe, Yoshishige published the artcileLTB₄ and BLT1 in inflammatory arthritis, Application of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Seminars in Immunology (2017), 52-57, database is CAplus and MEDLINE.

Inflammatory arthritis, including rheumatoid arthritis (RA), is characterized by infiltration of inflammatory cells into the joints. Biol. agents targeting TNF-α and IL-6 dramatically improve RA. However, some RA patients do not respond to current treatments and these broadly active upstream biol. agents increase the risk of severe infection. Therefore, there remains a need for other effective and safe treatments for RA. Many studies have implicated that blockade of leukotriene B4 (LTB₄) and its high affinity receptor BLT1 dramatically suppress arthritis in animal models. In addition, levels of LTB₄ in serum, synovial fluid and synovial tissue are increased in RA patients compared to healthy donors or osteoarthritis patients. These data suggest that LTB₄ and BLT1 likely contribute to the pathogenesis of human RA. However, several clin. trials inhibiting BLT1 in RA were not successful. Our recent data revealed that LTB₄ is a key mediator in a complement, lipid, cytokine and chemokine cascade that first initiates and then sustains neutrophilic inflammation in inflammatory arthritis. These new mechanistic studies suggest novel ways to target the LTB₄-BLT1 pathway for the treatment of RA and other inflammatory diseases.

Seminars in Immunology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Application of [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hirakata, Toshiaki published the artcileLeukotriene B₄ receptors as therapeutic targets for ophthalmic diseases, Safety of [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids (2020), 1865(9), 158756, database is CAplus and MEDLINE.

A review. Leukotriene B₄ (LTB₄) is an inflammatory lipid mediator produced from arachidonic acid by multiple reactions catalyzed by two enzymes 5-lipoxygenase (5-LOX) and LTA₄ hydrolase (LTA₄H). The two receptors for LTB₄ have been identified: a high-affinity receptor, BLT1, and a low-affinity receptor, BLT2. Our group identified 12(S)-hydroxy-5Z,8E,10E-heptadecatrienoic acid (12-HHT) as a high-affinity BLT2 ligand. Numerous studies have revealed critical roles for LTB₄ and its receptors in various systemic diseases. Recently, we also reported the roles of LTB₄, BLT1 and BLT2 in the murine ophthalmic disease models of mice including cornea wound, allergic conjunctivitis, and age-related macular degeneration. Moreover, other groups revealed the evidence of the ocular function of LTB₄. In the present review, we introduce the roles of LTB₄ and its receptors both in ophthalmic diseases and systemic inflammatory diseases. LTB₄ and its receptors are putative novel therapeutic targets for systemic and ophthalmic diseases.

Biochimica et Biophysica Acta, Molecular and Cell Biology of Lipids published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Safety of [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Goncalves, Aurelie published the artcileIntestinal Scavenger Receptors Are Involved in Vitamin K1 Absorption, Formula: C12H23N3S, the publication is Journal of Biological Chemistry (2014), 289(44), 30743-30752, database is CAplus and MEDLINE.

Vitamin K1 (phylloquinone) intestinal absorption is thought to be mediated by a carrier protein that still remains to be identified. Apical transport of vitamin K1 was examined using Caco-2 TC-7 cell monolayers as a model of human intestinal epithelium and in transfected HEK cells. Phylloquinone uptake was then measured ex vivo using mouse intestinal explants. Finally, vitamin K1 absorption was compared between wild-type mice and mice overexpressing scavenger receptor class B type I (SR-BI) in the intestine and mice deficient in cluster determinant 36 (CD36). Phylloquinone uptake by Caco-2 cells was saturable and was significantly impaired by co-incubation with α-tocopherol (and vice versa). Anti-human SR-BI antibodies and BLT1 (a chem. inhibitor of lipid transport via SR-BI) blocked up to 85% of vitamin K1 uptake. BLT1 also decreased phylloquinone apical efflux by ∼80%. Transfection of HEK cells with SR-BI and CD36 significantly enhanced vitamin K1 uptake, which was subsequently decreased by the addition of BLT1 or sulfo-N-succinimidyl oleate (CD36 inhibitor), resp. Similar results were obtained in mouse intestinal explants. In vivo, the phylloquinone postprandial response was significantly higher, and the proximal intestine mucosa phylloquinone content 4 h after gavage was increased in mice overexpressing SR-BI compared with controls. Phylloquinone postprandial response was also significantly increased in CD36-deficient mice compared with wild-type mice, but their vitamin K1 intestinal content remained unchanged. Overall, the present data demonstrate for the first time that intestinal scavenger receptors participate in the absorption of dietary phylloquinone.

Journal of Biological Chemistry published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Cohen, Yifat published the artcileMechanisms of absorption of vitamin D₃ delivered in protein nanoparticles in the absence and presence of fat, Category: amides-buliding-blocks, the publication is Food & Function (2021), 12(11), 4935-4946, database is CAplus and MEDLINE.

Novel protein-based nanovehicles offer alternatives to fat for delivery of lipophilic bioactives (nutraceuticals and drugs), yet they raise important questions regarding the bioavailability and absorption mechanism of the bioactive without fat. To provide answers, we chose vitamin D₃ (VD3) as a model lipophilic-nutraceutical, re-assembled casein-micelles (rCM) as model protein-based nanovehicles, and non-fat yoghurt as a model food. We prepared three yoghurt formulations: 3% fat with D₃ dissolved in milk-fat, non-fat and 3% fat, both latter enriched with VD3 within rCM. Following in vitro digestion, D₃ retention and bioaccessibility were high (∼90% and ∼70%, resp.) in all formulations. VD3 uptake by Caco-2 cells was three-fold higher (p < 0.005) in the non-fat yoghurt enriched with VD₃ in rCM compared with enriched fat-containing yoghurts. SR-BI, CD36 and NPC1L1 transporters were involved in VD₃ absorption irresp. of the composition Thus, our findings demonstrate that protein nanovehicles may improve D₃ bioavailability, without altering its absorption mechanism compared to that from fat.

Food & Function published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Mancuso, Elettra published the artcileHDL (High-Density Lipoprotein) and ApoA-1 (Apolipoprotein A-1) Potentially Modulate Pancreatic α-Cell Glucagon Secretion, Related Products of amides-buliding-blocks, the publication is Arteriosclerosis, Thrombosis, and Vascular Biology (2020), 40(12), 2941-2952, database is CAplus and MEDLINE.

Subjects with low levels of HDL (high-d. lipoprotein) and ApoA-1 (apolipoprotein A-1) have increased risk to develop type 2 diabetes. HDL levels are an independent predictor of β-cell function and pos. modulate it. Type 2 diabetes is characterized by defects in both β and α-cell function, but the effect of HDL and ApoA1 on β-cell function is unknown. We observed a significant neg. correlation (r = -0.422, P<0.0001) between HDL levels and fasting glucagon in a cohort of 132 Italian subjects. In a multivariable regression anal. including potential confounders such as age, sex, BMI, triglycerides, total cholesterol, fasting and 2-h postload glucose, and fasting insulin, the association between HDL and fasting glucagon remained statistically significant (β = -0.318, P = 0.006). CD1 mice treated with HDL or ApoA-1 for 3 consecutive days showed a 32% (P<0.001) and 23% (P<0.05) reduction, resp., in glucagon levels following insulin-induced hypoglycemia, compared with controls. Treatment of pancreatic αTC1 clone 6 cells with HDL or ApoA-1 for 24 h resulted in a significant reduction of glucagon expression (P<0.04) and secretion (P<0.01) after an hypoglycemic stimulus and increased Akt (RAC-alpha serine/threonine-protein kinase) and FoxO1 (forkhead/winged helix box gene, group O-1) phosphorylation. Pretreatment with Akt inhibitor VIII, PI3K (phosphatidylinositol 3-kinase) inhibitor LY294002, and HDL receptor SCARB-1 (scavenger receptor class B type 1) inhibitor BLT-1 (block lipid transport-1) restored αTC1 cell response to low glucose levels. These results support the notion that HDL and ApoA-1 modulate glucagon expression and secretion by binding their cognate receptor SCARB-1, and activating the PI3K/Akt/FoxO1 signaling cascade in an in vitro α-cell model. Overall, these results raise the hypothesis that HDL and ApoA-1 may have a role in modulating glucagon secretion.

Arteriosclerosis, Thrombosis, and Vascular Biology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Subramanian, Bhagawat C. published the artcileThe role of the LTB₄-BLT1 axis in chemotactic gradient sensing and directed leukocyte migration, Synthetic Route of 321673-30-7, the publication is Seminars in Immunology (2017), 16-29, database is CAplus and MEDLINE.

Directed leukocyte migration is a hallmark of inflammatory immune responses. Leukotrienes are derived from arachidonic acid and represent a class of potent lipid mediators of leukocyte migration. In this review, we summarize the essential steps leading to the production of LTB₄ in leukocytes. We discuss the recent findings on the exosomal packaging and transport of LTB₄ in the context of chemotactic gradients formation and regulation of leukocyte recruitment. We also discuss the dynamic roles of the LTB₄ receptors, BLT1 and BLT2, in mediating chemotactic signaling in leukocytes and contrast them to other structurally related leukotrienes that bind to distinct GPCRs. Finally, we highlight the specific roles of the LTB₄-BLT1 axis in mediating signal-relay between chemotaxing neutrophils and its potential contribution to a wide variety of inflammatory conditions including tumor progression and metastasis, where LTB₄ is emerging as a key signaling component.

Seminars in Immunology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C15H14O, Synthetic Route of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Kaithwas, Gaurav published the artcileEffect of L. usitatissimum (flaxseed/linseed) fixed oil against distinct phases of inflammation, Product Details of C12H23N3S, the publication is ISRN Inflammation (2013), 735158/1-735158/5, 5 pp., database is CAplus and MEDLINE.

The present investigation summarizes the effect of Linum usitatissimum fixed oil against different phases of acute inflammatory reaction, namely, protein exudation, peritoneal capillary permeability and leukocyte migration. The fixed oil exhibited dose-dependent inhibition of protein exudation vascular permeability, comparable to standard aspirin. The oil also inhibited the leukocyte migration in pleural exudates in a dose-dependent manner. Production of less vasodilatory (PGE3) and chemotactic (LTB5) eicosanoids through EPA (derived from linolenic acid) metabolism could account for the above observations.

ISRN Inflammation published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Product Details of C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wang, Min published the artcileApolipoprotein M induces inhibition of inflammatory responses via the S1PR1 and DHCR24 pathways, Related Products of amides-buliding-blocks, the publication is Molecular Medicine Reports (2019), 19(2), 1272-1283, database is CAplus and MEDLINE.

Apolipoprotein M (ApoM) is a type of apolipoprotein. It is well known that high-d. lipoprotein (HDL) decreases inflammatory responses via the apoM-sphingosine-1-phosphate (S1P) pathway. The present study further investigated the importance of ApoM in the inhibitory effects of HDL on inflammation. Furthermore, cell culture experiments were performed using a permanent human hybrid endothelial cell line (EA.hy926). In cell culture experiments, when cells were pre-cultured with rec-apoM or were engineered to overexpress apoM (apoMTg), they exhibited decreased expression levels of IL-1beta and MCP-1 following TNF-a treatment compared with in normal apoM-expressing cells (apoMTgN) Furthermore, the mRNA expression levels of IL-1beta and MCP-1 were significantly elevated following addition of the S1PR1 inhibitor W146, but not by the scavenger receptor class B type I inhibitor, block lipid transport-1 (BLT-1), in apoMTg cells prior to TNF-a treatment. Conversely, there were no differences in these inflammatory biomarkers under the same conditions in apoMTgN cells. The mRNA expression levels of DHCR24 were significantly reduced by the addition of BLT-1 prior to TNF-a treatment in apoMTg cells; however, there was no difference in the expression of this inflammatory biomarker in apoMTgN cells. In conclusion, ApoM displayed inhibitory effects against the inflammatory response in vivo and in vitro; these effects may be induced via the S1PR1 and DHCR24 pathways.

Molecular Medicine Reports published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C8H8O3, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Yu, Renchao published the artcileBaicalin promotes cholesterol efflux by regulating the expression of SR-BI in macrophages, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Experimental and Therapeutic Medicine (2016), 12(6), 4113-4120, database is CAplus and MEDLINE.

Intake of a high dosage of baicalin has previously been shown to attenuate hyperlipidemia induced by a high-fat diet. Baicalin functions as an activator of peroxisome proliferator-activated receptor-γ (PPAR-γ), which is the key regulator of reverse cholesterol transport (RCT). The present study aimed to test the hypothesis that baicalin could promote cholesterol efflux in macrophages through activating PPAR-γ. Phorbol 12-myristate 13-acetate-stimulated THP-1 cells were treated with oxidized low-d. lipoprotein and (3H)-cholesterol for 24 h, and the effects of baicalin on cholesterol efflux were evaluated in the presence of apolipoprotein A-1 (ApoA-1), or high-d. lipoprotein subfraction 2 (HDL2) or subfraction 3 (HDL3). The expression levels of scavenger receptor class B type I (SR-BI), PPAR-γ and liver X receptor-α (LXRα) were detected and specific inhibitors or activators of SR-BI, PPAR-γ and LXRα were applied to investigate the mechanism. Treatment of THP-1 macrophages with baicalin significantly accelerated HDL-mediated, but not ApoA-1-mediated cholesterol efflux. However, baicalin treatment increased the expression of SR-BI at the mRNA and protein levels in a dose- and time-dependent manner, and pre-treatment with the SR-BI inhibitor BLT-1 and SR-BI small interfering RNA significantly inhibited baicalin-induced cholesterol efflux. Furthermore, baicalin increased the expression of PPAR-γ and LXRα, and the application of specific agonists and inhibitors of PPAR-γ and LXRα changed the expression of SR-BI, as well as cholesterol efflux. It may be concluded that baicalin induced cholesterol efflux from THP-1 macrophages via the PPAR-γ/LXRα/SR-BI pathway.

Experimental and Therapeutic Medicine published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C20H21ClN4O4, Recommanded Product: [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Watanabe, Masaki published the artcileA turn on and a turn off: BLT1 and BLT2 mechanisms in the lung, Related Products of amides-buliding-blocks, the publication is Expert Review of Respiratory Medicine (2014), 8(4), 381-383, database is CAplus and MEDLINE.

A review. Leukotriene B₄ (LTB₄), a potent lipid mediator of inflammation derived from arachidonic acid through the action of 5-lipoxygenase, has been implicated in the pathophysiol. of several inflammatory diseases, including asthma and chronic obstructive pulmonary disease. A high-affinity LTB₄ receptor BLT1 has been shown to exert proinflammatory roles. A cyclooxygenase metabolite, 12(S)-hydroxyheptadeca-5Z, 8E, 10E-trienoic acid (12-HHT), is an endogenous ligand for BLT2, a low-affinity LTB₄ receptor. The recent study indicated that BLT2 has a protective role in allergic airway inflammation, suggesting different functions between BLT1 and BLT2 in the pathogenesis of asthma. Selective BLT1 antagonists may have a potential therapeutic application in patients with asthma, and BLT2 may represent a novel therapeutic target for lung diseases.

Expert Review of Respiratory Medicine published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C8H5F3N4, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics