dermal fibroblasts

Balicatib (AAE581) 是组织蛋白酶K 抑制剂，其对组织蛋白酶K 的抑制作用是组织蛋白酶B、L 和S 的抑制性的10到100倍。

alpha-L-Rhamnose (6-Deoxy-L-mannose) 是存在植物和细菌中的一种单糖。Rhamnose- 免疫原连接物能被用于免疫疗法。Rhamnose 能通过胞外途径穿过上皮细胞，能够作为肠吸收的标志。

(E)-SIS3 (SIS3) 是 Smad3 的选择性抑制剂，能够抑制 Smad3 磷酸化(IC50:3 μM)。它利用 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。

Capsorubin 是一种类胡萝卜素，具有多种生物活性。Capsorubin 在 167 μM 浓度下，对 2,2′-偶氮(2,4-二甲基戊腈)(AMVN) 诱导的脂质过氧化有抑制作用。capsorubin (1 μM) 可降低 uvb 诱导的人真皮成纤维细胞 DNA 链断裂和凋亡的形成。它还能抑制 Raji 细胞中由12-Carnosine 13-acetate 诱导的 eb 病毒早期抗原 (EBV-EA) 激活。

Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).

Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1 2 by MEK1 2. Nemorosone also inhibits growth of Capan-1, AsPC-1, and MIA-PaCa-2 pancreatic cancer cells (IC50s = 4.5-5.0 μM following a 72-hour treatment) but not human dermal and foreskin fibroblasts (IC50s = >35 μM).1 It induces apoptosis, abolishes the mitochondrial membrane potential, and increases cytosolic calcium concentration in pancreatic cancer cells in a dose-dependent manner. Nemorosone activates the caspase cascade in a dose-dependent manner and inhibits cell cycle progression, increasing the proportion of cells in the G0 G1 phase, in both neuroblastoma and pancreatic cancer cells.1,2 Nemorosone (50 mg kg, i.p., per day) also reduces tumor growth in an MIA-PaCa-2 mouse xenograft model.3References1. Holtrup, F., Bauer, A., Fellenberg, K., et al. Microarray analysis of nemorosone-induced cytotoxic effects on pancreatic cancer cells reveals activation of the unfolded protein response (UPR). Br. J. Pharmacol. 162(5), 1045-1059 (2011).2. Díaz-Carballo, D., Malak, S., Bardenheuer, W., et al. Cytotoxic activity of nemorosone in neuroblastoma cells. J. Cell. Mol. Med. 12(6B), 2598-2608 (2008).3. Wold, R.J., Hilger, R.A., Hoheisel, J.D., et al. In vivo activity and pharmacokinetics of nemorosone on pancreatic cancer xenografts. PLoS One 8(9), e74555 (2013). Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1 2 by MEK1 2. Nemorosone also inhibits growth of Capan-1, AsPC-1, and MIA-PaCa-2 pancreatic cancer cells (IC50s = 4.5-5.0 μM following a 72-hour treatment) but not human dermal and foreskin fibroblasts (IC50s = >35 μM).1 It induces apoptosis, abolishes the mitochondrial membrane potential, and increases cytosolic calcium concentration in pancreatic cancer cells in a dose-dependent manner. Nemorosone activates the caspase cascade in a dose-dependent manner and inhibits cell cycle progression, increasing the proportion of cells in the G0 G1 phase, in both neuroblastoma and pancreatic cancer cells.1,2 Nemorosone (50 mg kg, i.p., per day) also reduces tumor growth in an MIA-PaCa-2 mouse xenograft model.3 References1. Holtrup, F., Bauer, A., Fellenberg, K., et al. Microarray analysis of nemorosone-induced cytotoxic effects on pancreatic cancer cells reveals activation of the unfolded protein response (UPR). Br. J. Pharmacol. 162(5), 1045-1059 (2011).2. Díaz-Carballo, D., Malak, S., Bardenheuer, W., et al. Cytotoxic activity of nemorosone in neuroblastoma cells. J. Cell. Mol. Med. 12(6B), 2598-2608 (2008).3. Wold, R.J., Hilger, R.A., Hoheisel, J.D., et al. In vivo activity and pharmacokinetics of nemorosone on pancreatic cancer xenografts. PLoS One 8(9), e74555 (2013).

PF-03671148 is a potent ALK inhibitor. PF-03671148 inhibits the expression of fibrotic genes and protein markers both in vitro in human fibroblasts and in vivo in a rat wound repair model. Wound healing is not inhibited by the topical application of the ALK5 inhibitor to the wound. PF-03671148 may have potential utility for the prevention of dermal scarring.

Anticanceragent 136 (compound 22)，一种GDM C17-三唑类似物，对HDF表现出3.38 μM的IC50，与Hsp90有3.86 μM的Kd。本化合物功能为细胞凋亡诱导剂。

3,3′-Bisdemethylpinoresinol，一种木质素类的天然产物，具有抑制UVA照射下人真皮成纤维细胞中MMP-1的活性。该化合物可从Morinda citrifolia种子中分离提取。

H-Gly-Pro-Hyp-OH是一种有效和可口服的抗光老化胶原肽，能够减轻炎症，降低MMP-1和MMP-3含量；能够减轻H2O2诱导的真皮成纤维细胞老化；能够恢复皮质醇介导的I型胶原蛋白和GR激活的抑制和(TGF)-β信号等抑制；改善人体皮肤的水合性、弹性和抗皱性。

Tiger17是一种环状肽，属于tigerinin-RC1和tigerinin-RC2的衍生物，这两种化合物是在螃蟹吃蛙（F. cancrivora）皮肤分泌物中发现的抗微生物肽。在5至20µg/ml的浓度范围内使用时，Tiger17能增加HaCaT角质形成细胞和人类皮肤成纤维细胞的增殖，并且在20µg/ml的浓度下增加HaCaT细胞的迁移。此外，Tiger17还能增加RAW 264.7巨噬细胞的招募及其TGF-β1和IL-6的分泌。在全层皮肤创伤的小鼠模型中，局部应用20µg/ml的Tiger17能加速伤口闭合和重新上皮化的速度。

25-Hydroxytachysterol3 是 Vitamin D3 的一种代谢产物。它能够抑制表皮角质细胞和真皮成纤维细胞的增殖，并促进角质形成细胞的分化及抗氧化相关基因的表达。25-Hydroxytachysterol3 能够激活维生素 D 受体 (VDR)、芳烃受体 (AhR)、肝 X 受体 α β (LXRα β) 和过氧化物酶体增殖激活受体 γ (PPARγ)，并刺激 CYP24A1 的表达。

2-Isopropylmalic acid (α-Isopropylmalate) 抑制 PM2.5 处理的真皮成纤维细胞中过量活性氧的产生和应激激酶的激活，促进原代纤毛发生并恢复 PM2.5 诱导的真皮成纤维细胞中初级纤毛发育不全。

Regaloside I 是百合中的单体成分,可能是保护人类皮肤成纤维细胞免受 UVA 诱导的形态变化的主要成分。

Exserohilone ((-)-Exserohilone) 是硫代二酮哌嗪衍生物，能够抑制 TNF-α 诱导的ROS生成和MMP-1分泌，并促进人真皮成纤维细胞中 I 型前胶原 α1 的分泌。