il-1 g

Balsalazide sodium hydrate (Balsalazide disodium) 可通过调节IL-6 STAT3通路起抑癌作用，可用于治疗炎症性肠病。

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

HCAR2 agonist 1 (Compound 9n) 是一种偏向Gi蛋白的变构调节剂，能够激活Gi蛋白相关的信号传导通路。该化合物展现了明显的抗炎效果，能够显著降低促炎细胞因子（TNF-α、IL-1β、IL-6 和 MCP-1）的mRNA表达水平，并在结肠炎小鼠模型中增强正位激动剂的抗炎作用。

Z21115 作为一种口服有效的磷酸二酯酶 4 (PDE4) 抑制剂，能特异性抑制 PDE4D7，其 IC50 值为 10.5 nM。它还能抑制 Lipopolysaccharide 诱导的 IL-6、TNF-α 和 iNOS 的表达。在 DSS 诱导的小鼠结肠炎模型中，Z21115 显示出了抗炎效果，并在剂量高达 1 g kg 时未观察到明显毒性。