pge2 production

Rebamipide (OPC12759) 是一种粘膜保护剂，可诱导COX-2表达，增加PGE2水平，并以 COX-2 依赖性方式增强胃粘膜防御。

Flavokawain B (Flavokavain B) 是从卡瓦醉椒的根提取物中，分离出的查尔酮。它是一种凋亡诱导剂，可抑制各种癌细胞株生长。它以极低的无毒浓度抑制人脑内皮细胞的迁移和血管形成，具有抗血管生成活性。

7-Demethylsuberosin (7-demethylsuberosin) 是一种分离自 Angelica gigasNakai 中的香豆素类化合物，具有抗炎作用。

2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂，mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。

Isofraxidin (Phytodolor) 是来自刺五加的香豆素成分，抑制MMP-7表达和人肝癌细胞侵袭。它作用于肝癌细胞，抑制ERK1 2磷酸化。它减弱iNOS 和COX-2表达，还抑制TLR4 髓样分化蛋白 2 复合物的形成。

Cafestol 是咖啡特有的一种二萜，可靶向 AP-1 抑制ERK，有化学预防、抗肿瘤、保肝、抗氧化和抗炎作用。它通过抑制NF-kB 活化途径强烈的抑制 PGE2的产生，还抑制 LGE 激活的 RAW264.7 细胞中的PGE2产生和环氧合酶(COX-2)的 mRNA 表达。

alpha-Cyperone (α-Cyperone) 与 IL-6, Cox-2, Cdc42, Nck-2, Rac1 的表达下调相关,从而能够抑制炎症反应。

Dehydroevodiamine (DHED) 是从吴茱萸中分离出的一种喹唑啉生物碱，可抑制 LPS 诱导的小鼠巨噬细胞中iNOS、COX-2、PGE2和NF-κB 的表达，对豚鼠心室肌细胞具有抗心律失常作用。

CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂，可抑制 NF-κB 信号通路。

TCS 2510 (CAY10598) 是一种选择性 PGE2 和 EP4 受体激动剂，可增强细胞内 cAMP 浓度和活性 β-caten 的丰度。TCS 2510 抑制TNF-α 产生，可用于研究代谢紊乱带来的疾病。

IKKβ-IN-1 是一种有效的、口服具有活力的 IkappaB(IKK-β) 抑制剂 (IC50: 0.20 μM)。IKKβ-IN-1 能够减少抑制小鼠巨噬细胞中 PGE2和 TNF-α的产生。IKKβ-IN-1 对小鼠具有保护作用，使其免受感染性休克诱导的死亡。

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as pyrrophenone inhibits the secretory type IB and IIA PLA2s with more than a hundred-fold less potency. Pyrrophenone has also been shown to inhibit calcium ionophore (A23187)-stimulated AA release from monocytic cells, interleukin-1-induced PGE2 synthesis in mesangial cells, and the production of PGE2, LTs, and platelet-activating factor by human neutrophils, always with maximal inhibition at concentrations below 1 μM.

ExcisaninA may be a potent inhibitor of AKT signaling pathway in tumor cells, it can inhibit invasion by suppressing MMP-2 and MMP-9 expression, it may be a potential anti-metastatic chemotherapeutic agent for the treatment of breast cancer. Excisanin A shows comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability.Excisanin A induces apoptosis in colon cancer cell line SW620 as determined by Annexin V staining, the cleavage of caspase-3 and the proteolytic degradation of poly (ADP-ribose) polymerase (PARP).

Luvangetin may have anti-inflammatory activity, it can inhibit NO and PGE2 production in LPS-stimulated BV2 cells. Luvangetin shows significant protection against pylorus-ligated and aspirin-induced gastric ulcers in rats and cold restraint stress-induced

U-51605, a stable analog of the endoperoxide prostaglandin H2 (PGH2), functions as an inhibitor with greater selectivity towards prostacyclin (PGI) synthase over thromboxane (TX) synthase. It also acts as a partial agonist at TP receptors. Studies show that at a concentration of 2.8 µM, U-51605 effectively inhibits PGI synthase in human foreskin fibroblasts, while a concentration of 5.6 µM is required to inhibit human platelet TX synthase. Furthermore, U-51605, at up to 1 µM, decreases the release of prostacyclin in SHR aorta triggered by the calcium ionophore A-23187 without impacting TXA2 production, and notably enhances the release of PGE2 and PGF2α.

Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂，相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH)，在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下，该抑制剂能抑制A549细胞中IL-1β诱导的PGE2生成以及在J774A.1巨噬细胞中，LPS诱导的IL-6和PGE2生成。同时，它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成，包括白三烯B4 (LTB4) 和5-H(p)ETE（IC50s分别为4.9和5.2 µM）。在体内，10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。

UT-11是一种有效且具有脑渗透性的mPGES-1抑制剂，能够降低人类(SK-N-AS)和小鼠(BV2)细胞内PGE2的生成，其IC50s分别是0.10 μM和2.00 μM。

Questinol exhibits significant anti-obesity activity. It shows anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, it can inhibit the production of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6 and inhibit NO an

CR6086 is a novel, potent EP4 antagonist showing favourable immunomodulatory properties, striking DMARD effects in rodents, and anti-inflammatory activity targeted to immune-mediated inflammatory diseases and distinct from the general effects of cyclooxygenase inhibitors. CR6086 showed selectivity and high affinity for the human EP4 receptor (Ki = 16.6 nM) and functioned as a pure antagonist (half-maximal inhibitory concentration, 22 nM) on PGE2-stimulated cAMP production.

COX-2-IN-10 是 COX-2 的有效抑制剂。COX-2-IN-10 对 IL-6、TNF-α 和 IL-1β 的产生表现出抑制作用。COX-2-IN-10 能够浓度依赖性地抑制 PGE2 的产生，其 IC50 值为 2.54 μM。COX-2-IN-10 在 mRNA 和蛋白水平上抑制 iNOS 和 COX-2 的表达。

2-Chloroadenosine-5'-O-diphosphate是一种腺苷5'二磷酸（ADP）的衍生物。它在浓度依赖性的方式下，促进了人类富含血小板的血浆中的聚集，并抑制了由前列腺素E2（PGE2）诱导的环磷酸腺苷（cAMP）的产生。2-Chloroadenosine-5'-O-diphosphate引起预收缩的孤立的豚鼠taenia coli条带放松（pD2 = 6.74），降低大鼠的动脉血压。此外，它还抑制了热休克蛋白70（Hsp70）家族成员mortalin的ATP酶活性（人类酶的表观Ki = 45.05 µM）。

Bavachromene 是可从补骨脂科 Fructus 提取得到的异戊二烯化查尔酮，具有雌激素活和抗菌活性，对脂多糖 （LPS） 激活的小胶质细胞中 NO 和 PGE2 的产生具有浓度依赖性抑制作用。

Prostaglandin E2 serinol amide 为 [3H]2-油酰甘油水解的弱抑制剂。该化合物无法通过水解产生 PGE2，因此不参与抑制白三烯 B4 的生物合成、超氧化物的生成、迁移以及抗菌肽的释放。

Arbaprostil, a synthetic analog of prostaglandin E2 (PGE2) known as 15(R)-15-methyl prostaglandin E2, was developed for its cytoprotective activity. In the commercial production of bulk arbaprostil, one potential impurity is 15(R)-15-methyl Prostaglandin A2 (15(R)-15-methyl PGA2). The pharmacology and EP receptor binding affinity of 15(R)-15-methyl PGA2 have not been reported.

YS121 是微粒体前列腺素 E2 合酶-1 (mPGES-1;IC50=3.4 μM) 和 5-脂氧合酶 (5-LOX;IC50=6.5 μM) 的双重抑制剂。在 IL-1β 刺激的 A549 细胞中，YS121以剂量依赖性地方式减少 PGE2 的产生，EC50为 12 μM。

Prostaglandin E2 Ethanolamide (PGE2-EA) 作为PGE2的类似物，通过COX-2催化内源性大麻素进行氧化而形成，具有可能调控人血以及人单核细胞中促炎细胞因子TNF-α产生的功能。

(R)-Vorbipiprant ((R)-CR6086) 作为口服前列腺素 E2 (EP4) 受体拮抗剂，绑定 EP4 受体的能力强，Ki 值为 16.6 nM。该化合物能有效抑制 PGE2 诱导的 cAMP 生成，IC50 值达 22 nM，显示出显著的免疫调节和抗血管生成特性，对小鼠胶原诱导性关节炎的改善效果显著。

iNOS/PGE2-IN-1 是一种 iNOS/PGE2 抑制剂，是一种有效的抗炎剂。iNOS/PGE2-IN-1 对 LPS 诱导的 NO 产生表现出抑制作用，具有低致溃疡倾向。

Manassantin A is a high potent HIF-1 inhibitor, it protects the gastric mucosa from ethanol-induced acute gastric injury, and suggest that these protective effects might be associated with COX/PGE2 stimulation, inhibition of iNOS production and NF-κB act

Saikogenin D possesses a dual effect: an inhibition of A23187-induced PGE2 production without a direct inhibition of cyclooxygenase activity; and an elevation of [Ca2+]i that is attributed to Ca2+ release from intracellular stores. Saikogenin D has immuno