Coumarins

4-Methylumbelliferone is a hyaluronic acid biosynthesis inhibitor with antitumoral and antimetastatic effects.

Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H₁ receptor activity. Osthole also suppresses the secretion of HBV in cells.

Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC₅₀s of 0.37 and 19.42 μM, respectively.

Methoxsalen (8-Methoxypsoralen) is a furanocoumarin compound used in psoralen, used in studies of psoriasis, eczema, vitiligo and some sun-exposed cutaneous lymphomas, and is a P450 inhibitor.

Imperatorin is an effective of NO synthesis inhibitor (IC₅₀=9.2 μmol), which also is a BChE inhibitor (IC₅₀=31.4 μmol). Imperatorin is a weak agonist of TRPV1 with EC₅₀ of 12.6±3.2 μM.

(-)-Calanolide B is a non-nucleoside reverse transcriptase (NNRT) inhibitor with an IC₅₀ of 0.5 mM against HIV-1 RT. (-)-Calanolide B inhibits the replication of HIV-1 IIIb/LAV. (-)-Calanolide B is applicable to research related to HIV-1 infection.

3-(2-Hydroxypropyl)-8-hydroxy-3,4-dihydroisocoumarin is a 3,4-dihydroisocoumarin derivative found in some fungi and Catunaregam spinosa. 3-(2-Hydroxypropyl)-8-hydroxy-3,4-dihydroisocoumarin exhibits no significant monoamine oxidase or PI3Kα inhibitory activity.

Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.

Umbelliferone (7-Hydroxycoumarin), a natural orally active product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent. Umbelliferone induces cell cycle arrest, apoptosis and DNA fragmentation in HepG2 cells. Umbelliferone exhibits significant anticancer effects. Umbelliferone attenuates the alteration characteristics of allergic airway inflammation. Umbelliferone displays the neuroprotective effects and cross the blood-brain barrier. Umbelliferone exhibits anti-inflammatory and antioxidant effects in chronic alcohol-fed rats.

Psoralen (Ficusin) is a coumarin isolated from the seeds of Fructus Psoraleae. Psoralen exhibits a wide range of biological properties, including anti-cancer, antioxidant, antidepressant, anticancer, antibacterial, and antiviral, et al.

Esculin is a fluorescent coumarin glucoside, the active ingredient in ash bark. Esculin has antidiabetic effects, improves cognitive impairment in experimental diabetic nephropathy (DN) via the MAPK signaling pathway, and exerts antioxidant stress and anti-inflammatory effects. Esculin also has anticancer, antibacterial, antiviral, neuroprotective, antithrombotic, and therapeutic properties for eye diseases.

Coumarin is a potent and orally active anti-inflammatory agent. Coumarin shows an antinociceptive effect. Coumarin shows antibacterial, antifungal and anticancer activity.

Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities.

Bergamottin is a potent and competitive CYP1A1 inhibitor with a K_i of 10.703 nM.

Scopoletin is an inhibitor of acetylcholinesterase (AChE).

Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC₅₀ of 50 μM.

Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC₅₀s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1β, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.

Decursin ((+)-Decursin) is a potent anti-tumor agent. Decursin also is a cytotoxic agent and a potent protein kinase C activator. Decursin induces apoptosis and cell cycle arrest at G1 phase. Decursin decreases the expression of CDK2, CDK4, CDK6, cyclin D1 protein at 48 h. Decursin inhibits cell proliferation and migration. Decursin shows anti-tumor, anti-inflammatory and analgesic activities.

Angelicin is a furanocoumarin compound that functions as an inhibitor of NF-κB and MAPK signaling pathways, exhibiting anti-inflammatory, antiviral, and antitumor activities. It suppresses the lytic replication of γ-herpesviruses, such as MHV-68, early during viral infection, potentially inhibiting RTA gene expression (IC₅₀=28.95 μM). Angelicin also mitigates inflammation by inhibiting the phosphorylation and nuclear translocation of NF-κB, and the phosphorylation of p38 and JNK. Furthermore, it induces apoptosis in neuroblastoma cells by downregulating anti-apoptotic proteins like Bcl-2, Bcl-xL, and Mcl-1, while activating caspase-9 and caspase-3.