PDE

Theophylline (1,3-Dimethylxanthine) is a methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac, and central nervous system stimulant activities. It inhibits the 3', 5'-cyclic nucleotide phosphodiesterase that degrades cyclic AMP, thus potentiating the actions of agents that act through adenylyl cyclases and cyclic AMP.

Proxyphylline (7-(2-Hydroxypropyl)theophylline) is a dual of adenosine A1/A2a receptor inhibitor and phosphodiesterase (PDE) inhibitor. Proxyphylline acts as a cardiac stimulant, vasodilator and bronchodilator.

3-O-Methylquercetin is a selective and competitive PDE3/PDE4 inhibitor, and inhibits PDE3 than PDE4 with a low K(m) value; it inhibits total cAMP- and cGMP-phosphodiesterase (PDE) of guinea pig trachealis at low concentrations.

Moracin M, a phenolic compound found in the skin of Morus alba Linn., effectively inhibits phosphodiesterase-4 (PDE4), exhibiting IC50 values of 2.9 μM and 4.5 μM for PDE4D2 and PDE4B2, respectively, and showing significantly lesser activity on PDE5A1 and PDE9A2 with values over 40 μM and 100 μM, respectively. This compound demonstrates notable anti-inflammatory activity.

Robustine is a natural product, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro.

Norbraylin is a natural product from Toddalia asiatica.

Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

Acefylline (Theophylline-7-acetic acid), a stimulant drug of the xanthine chemical class, acts as an adenosine receptor antagonist. It is combined with diphenhydramine in the pharmaceutical preparation Etanautine to help offset its stimulant effects

Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432 73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.

Fraxin (Fraxoside) is a glucoside of fraxetin.

Glaucine has antitussive, antioxidative potential and antiviral activities, it may be an anti-arthritic agent, it can enhance LPS and zymosan-induced IL-10 production. Glaucine can inhibit the migration and invasion of human breast cancer cells by MMP-9 i

Butein is a cAMP-specific PDE inhibitor, protein tyrosine kinase inhibitor, and SIRT1 activator. It sensitizes HeLa cells to Cisplatin by targeting FoxO3a via the AKT and ERK/p38 MAPK pathways.

Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils.

Sophoflavescenol is a mixed inhibitor of PDE5 with a K(i) value of 0.005 microM. Sophoflavescenol has antioxidant, anti-inflammatory, and apoptotic effects , these effects might contribute to the antitumor activity without severe side effects. Sophoflaves

Nauclefine (Parvine) is a plant indole alkaloid natural product and induces apoptosis of diverse cancer cells via a PDE3A-SLFN12 dependent death pathway. Nauclefine binds PDE3A but does not inhibit the PDE3A's phosphodiesterase activity.

Reticulol is an isocoumarin derivative produced by certain species of Streptomyces. Reticulol inhibits cAMP phosphodiesterase (IC50 = 41 µM). Recticulol (M.W. 222.2) exhibits a potent in vitro cytotoxicity against the human lung tumor cell line A427 and the mouse melanoma cell line B16F10.

Theobromine (3,7-Dimethylxanthine), a xanthine alkaloid, is used as a bronchodilator and as a vasodilator.

Diphylline (Diprophylline) is a xanthine derivative. Diphylline exerts bronchodilator effects and to a lesser extent vasodilator and diuretic properties. Diphylline probably acts as a competitive inhibitor of phosphodiesterase which leads to an increase in intracellular cAMP. This results in relaxation of bronchial smooth muscle and other smooth muscles. Diphylline may also antagonize adenosinereceptors. Diphylline is used in the treatment of acute bronchial asthma, chronic bronchitis and emphysema.

Aminophylline (Phyllocontin) is a competitive nonselective phosphodiesterase inhibitor giving a bronchodilatory effect.

Ilexsaponin B2 is a natural product for research related to life sciences. The catalog number is TJS0502 and the CAS number is 108906-69-0.

Obscurolide A1 is a butenolide isolated from Streptomyces viridochromogenes cultures that shows weak inhibitory activity against Ca2+ CaM-dependent and non-Ca2+ CaM-dependent phosphodiesterases in cattle.

Ophiobolin A is a fungal metabolite and a phytotoxin and is an effective and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase (IC50: 9 μM). Ophiobolin A also has antimicrobial and anticancer activity.

Ginkgolide J (BN 52024) has neuroprotective activity, it can prevent A beta(1-42) induced inhibition of long-term potentiation in the CA1 region of mouse hippocampal slices.

Eurycomanone (Pasakbumin A) is cytotoxic on HepG2 cells by inducing apoptosis through the up-regulation of p53 and Bax, and down-regulation of Bcl-2.Eurycomanone has anti-cancer activity, inhibits A549 lung cancer cell proliferation in a dose-dependent manner at concentrations ranging from 5 to 20 μg/ml.