ear 3

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)

GM 1489 is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with Ki values of 0.002, 0.1, 0.5, 0.2, and 20 μM for MMP-1, MMP-8, MMP-2, MMP-9, and MMP-3, respectively. It reduces 5-aza-2'-deoxycytidine-induced increases in MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, and MMP-14 expression as well as cell invasion in AsPC-1, BxPC-3, Hs766T, MiaPaCa2, and PANC-1 cancer cells. Topical administration of GM 1489 (100 μg) inhibits increases in ear thickness and epidermal hyperplasia induced by phorbol 12-myristate 13-acetate and phorbol dibutyrate (PdiBu) in mice.

Ingenol-3-palmitate shows irritant and cocarcinogenic activity on mouse ear and on mice back skin.

Stigmastane-3 beta, 6 alpha-diol and stigmastane-3 beta, 6 beta-diol possess marked inhibitory activity against 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation in mice, the 50% inhibitory dose is 0.5--1.0 mg/ear.

Alpinone 3-acetate 具有抗炎作用，可抑制12-O-tetradecanophenol 13-acetate 所致小鼠耳部水肿模型的炎症反应。Alpinone 3-acetate 是Alpinone 衍生物 。Alpinone 是一种具有活性的天然化合物，来源于向日葵，具有免疫调节和抗病毒活性 。

IRBP1-20（1-20）是IRBP的一个十二肽片段，亦称视黄醇结合蛋白3，负责运输视锥细胞中的视黄醇和视黄醛至视网膜色素上皮，参与色素再生。在携带H-2b等位基因型的C57BL/6小鼠中，IRBP1-20用于诱导自身免疫性葡萄膜视网膜炎。IRBP1-20（3 µM）能增加初级小鼠脾淋巴细胞分泌IL-4、IL-5和IL-6的水平。用IRBP1-20免疫并再次挑战，可增加IFN-γ缺乏小鼠的耳部肿胀、眼部血管炎症、免疫细胞浸润和视锥细胞层损伤，以及视网膜脱落。