fibroblasts

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.

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

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.

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.

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.

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

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.

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.

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.

Regaloside I is the monomeric component in lily. Regaloside I could be the main constituent in protecting human dermal fibroblasts from UVA-induced morphological changes [1].

Isosaponarin increases collagen synthesis in human fibroblasts, causes by up-regulated TbetaR-II and P4H production.

3′,4-O-Dimethylcedrusin can improve wound healing in vivo by stimulating the formation of fibroblasts and collagen.

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.

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

Glycozolidal (compound 12) is a carbazole alkaloid that exhibits antimicrobial activity against Porphyromonas gingivalis (P. gingivalis). In vitro studies have shown that Glycozolidal displays cytotoxic effects on human gingival fibroblasts (HGFs) and monocytic cells (U937), with IC50 values of 120.86 µg mL and 97.74 µg mL, respectively.

Tenuazonic Acid Copper Salt, a mycotoxin derived from Aspergillus, can inhibit protein synthesis in fibroblasts.

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

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).

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).

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].

Epidermal Growth Factor, murine submaxillary gland, is a bioactive polypeptide isolated from the submaxillary gland of mice. This growth factor acts as a mitogen, promoting the proliferation of epithelial cells, fibroblasts, and glial cells under a variety of experimental conditions.

Zymosan A, a polysaccharide from Saccharomyces cerevisiae (brewer's yeast), is a TLR2 agonist that promotes regeneration of ISCs from intestinal stem cells after radiation injury by up-regulating ASCL2 through the TLR2 signaling pathway and the Wnt signaling pathway.Zymosan A stimulates immune responses and induces inflammation , anorexia and elevated body temperature, and also inhibits the gap junction protein connexin 43 in human corneal fibroblasts and causes corneal stromal damage.

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.