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。

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。

(E)-SIS3 (SIS3) 是 Smad3 抑制剂（(IC50=3 μM），具有选择性。(E)-SIS3 通过 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。

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。