fibroblasts

Traumatic Acid (Dodec-2-Enedioic Acid) is a product of the hydroperoxide lyase pathway in plants. Potential as a wound healing agent that stimulates cell division near a wound site to form a protective callus.

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

Fumaric acid (2-Butenedioic acid) attenuates the eotaxin-1 expression in TNF-α-stimulated fibroblasts by suppressing p38 MAPK-dependent NF-κB signaling. Fumaric acid has recently been identified as an oncometabolite or an endogenous, cancer-causing metabolite. High levels of this organic acid can be found in tumors or biofluids surrounding tumors. Its oncogenic action appears due to its ability to inhibit prolyl hydroxylase-containing enzymes.

7-Dehydrocholesterol (Provitamin D3) down-regulates cholesterol biosynthesis in cultured Smith-Lemi-Opitz syndrome skin fibroblasts.

Addition of the Rhamnose (6-Deoxy-L-mannose)-rich polysaccharide, RROP-1, to normal human dermal fibroblasts (NHDFs) and human endothelial cells produced a dose-dependent stimulation of the calcium-signaling pathway, inducing fast and transient increases in Ca2 influx and intracellular free Ca2 level.

1-Hydroxyoctadecane (OctadecanolOctadecanol) is a fatty alcohol present in human and is normally incorporated into plasmalogen lipids. Sjogren-Larsson syndrome is defined by the triad of ichthyosis, mental retardation, and spasticity, and patients accumulate fatty alcohols such as Octadenol in the plasma and cultured fibroblasts.

DL-alpha-Tocopherol (Ephanyl) is a synthetic vitamin E that protects skin fibroblasts from the cytotoxic effects of UV light and has antioxidant properties.

Theaflavin-3-gallate (Theaflavine-3-Gallate) can play a role in decreased intestinal cholesterol absorption via inhibition of micelle formation. Theaflavin-3-gallate has anticancer and apoptotic effects in non-small cell lung carcinoma, it acts as prooxidants and induce oxidative stress, with carcinoma cells more sensitive than normal fibroblasts.

Cedrelone is a citrulline analog and a phenazine biosynthesis-like domain protein (PBLD) activator.Cedrelone induces apoptosis in cancer cells.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone has insecticidal activity, inhibiting the growth of arrowhead venom of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus). Cedrelone has insecticidal activity, inhibiting the growth of P. saucia and inhibiting moulting of the milkweed bug (Oncopeltus fasciatus).Cedrelone has antitumor effects and exhibits significant cytotoxicity against cancer cell lines such as -60, SMMC-7721, A-549, MCF-7, and SW480.Cedrelone is a very potent inducer of apoptosis, causing cell cycle arrest.Cedrelone is a very potent inducer of apoptosis, leading to cell cycle arrest.

Dieckol, a rhizomycin found in some brown algae species, has antimicrobial, anticancer, antioxidant, antiaging, antidiabetic, and neuroprotective effects, ameliorates acute hearing loss, and inhibits cell proliferation through cell cycle arrest in human tracheal fibroblasts via Hs680.Tr.

Dracorhodin perchlorate inhibits cell growth, and induces apoptosis in fibroblasts in a dose-and time-dependent manner, arresting cell cycle at G1 phase, may as a candidate for anti-breast cancer. Dracorhodin perchlorate can inhibit high glucose-induced serum and glucocorticoid induced protein kinase 1 (SGK1) and fibronectin(FN) expression in human mesangial cells, and this may be part of the mechanism of preventing and treating renal fibrosis of DN.

Capsorubin is a carotenoid with a variety of biological activities. capsorubin inhibited lipid peroxidation induced by 2,2′-azino(2,4-dimethylvaleronitrile) (AMVN) at a concentration of 167 μM. capsorubin (1 μM) reduced uvb-induced DNA strand breaks and apoptosis in human dermal fibroblasts. formation. It also inhibited the activation of ebvirus early antigen (EBV-EA) induced by 12-carnosine 13-acetate fobo in Raji cells.

Burnettramic acid A aglycone is a fungal metabolite and an aglycone form of burnettramic acid A, originally isolated from [A. burnettii], that exhibits anticancer activity. It is cytotoxic to NS-1 murine myeloma cells (IC50 = 8.4 μg ml) but not to neonatal foreskin fibroblasts (IC50 > 100 μg ml).

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).

Epifriedelanol (Epifriedelinol) suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can reduce cellular senescence in human primary cells, it may be used to develop dietary supplements or cosmetics that modulate tissue aging or aging-associated diseases.

Hygrolidin is a macrocyclic lactone originally isolated from S. hygroscopicus. It inhibits proliferation of a variety of cancer cell lines, including DLD-1 colon cancer, LNCaP prostate cancer, and K562 leukemia cells (IC50s = 2.9, 5.2, and 33 ng ml, respectively). Hygrolidin induces the expression and levels of p21 in DLD-1 cells, but not WI-38 fibroblasts, and leads to cell accumulation in the G1 and S phases without inducing apoptosis. It has antiparasitic activity against T. cruzi, L. donovani, and T. b. brucei but also induces cytotoxicity in HepG2 cells (IC50s = 1.1, 72.5, 77, and 24.5 nM, respectively).

Vaccarin is a major flavonoid glycoside in Vaccariae semen, its biotransformation pathways involves methylation, hydroxylation, glycosylation and deglycosylation.

Isosaponarin is a natural product with multiple activities. It inhibits the increase in Ca2+ levels induced by 4-aminopyridine in rat synaptosomes without affecting the membrane potential of synaptosomes, while reducing the phosphorylation of PKC, PKCα, SNAP-25, and MARCKS, thereby inhibiting the release of glutamate from vesicles in synaptosomes.

Theaflavin-3'-Gallate (Theaflavin 2B) usually comes from the leaves of Camellia sinensis (L.) O. Kuntze. Theaflavin-3'-gallate, act as prooxidants and induce oxidative stress, with carcinoma cells more sensitive than normal fibroblasts.

11-Dehydrocorticosterone is a metabolite of glucocorticoids, a sodium-retaining agent that increases SGK mRNA expression in cardiac fibroblasts and dose-dependently inhibits aldosterone.

Zymosan A, a polysaccharide derived from Saccharomyces cerevisiae, is a TLR2 agonist that can upregulate ASCL2 through the TLR2 and Wnt signaling pathways, promoting the regeneration of intestinal stem cells (ISCs) after radiation-induced injury. It exhibits significant radioprotective effects, helping to prevent and alleviate IR-induced intestinal damage. Additionally, Zymosan A can induce immune responses, inflammation, anorexia, and elevated body temperature, and is commonly used to establish peritonitis models.

Funiculosin, a neutral lipophilic antibiotic, demonstrates inhibitory effects against both DNA and RNA viruses, in addition to possessing antifungal properties. It effectively combats infections induced by pathogenic fungi within primary chicken embryo fibroblasts [1].

3,3′-Bisdemethylpinoresinol, a natural lignin derivative, exhibits MMP-1 inhibitory activity in UVA-irradiated human dermal fibroblasts and can be isolated from the seeds of Morinda citrifolia [1].