PAFR

Ginkgolide B (BN-52021) is a PAFR antagonist(IC50=3.6 μM) isolated from Ginkgo biloba.

48740 RP (RP 55779) is an antagonist of platelet-activating factor.

Tulopafant (RP 59227) is a potent platelet-activating factor (PAF) antagonist that increases capillary patency and prolongs allograft heart survival.

Ferulamide (4-Hydroxy-3-methoxycinnamide), a Ferulic acid derivative, shows potent inhibitory activity against arachidonic acid-induced platelet aggregation.

Scutellarein tetramethyl ether (4',5,6,7-Tetramethoxyflavone) is extracted from Siam weeds and exhibits anti-inflammatory activity through NF-κB pathway.

Futoquinol is an anti-platelet activating factor principle from the stem part of Piper futokadsura (Piperaceae), the Chinese drug haifengteng.

Hancinone C shows inhibitory activity against the platelet aggregation caused by PAF.

Pinusolide is a platelet activating factor ( PAF) antagonist, it may prove of therapeutic value in the treatment of hypotension, it has antileukemic potential, and could be used to treat neurodegenerative diseases. Pinusolide attenuates blockade of insulin signaling by enhancing IRS-1 tyrosine phosphorylation by the activating the AMPK pathway, indicates the targeting of AMPK represents a new therapeutic strategy for hyperglycemia-induced insulin resistance and type 2 diabetes.

Aristolactam AII has cytotoxic activity, it also shows platelet aggregation inhibitory activity.

(-)-Denudatin B (Denudatin B) is derived from Magnolia fargesii. (-)-Denudatin B has nonspecific antiplatelet action at high concentration by inhibiting phosphoinositides breakdown induced by collagen and thrombin.

Piperolactam C possesses anti-platelet aggregation activity in vitro. It can inhibit the growth of the fungi Cladosporium sphaerospermum and C. cladosporioides.

Cryptomeridiol is a potential skin-whitening agent, exhibits melanogenesis inhibitory activity on α-MSH-stimulated B16 melanoma cells. Cryptomeridiol has low activity against A. niger, T. mentagrophytes, and C. albicans. (-)-Cryptomeridiol also exhibits a significant and concentration-dependent inhibitory effect on PAF receptor binding, with inhibitory concentration (IC)(50) values of 17.5 uM.

Bisdethiobis(methylthio)gliotoxin is a platelet activating factor (PAF) antagonist.

Pregomisin shows platelet-activating factor (PAF) antagonistic activity and the IC 50 value is 4.8x10(-5) M.

Kadsurin A has anti-platelet activating factor activities.

Cyclocommunol exhibits cytotoxicity against hepatocellular carcinoma (SMMC-7721) and gastric carcinoma (BGC-823 and SGC-7901) cell lines. It also shows strong inhibition of arachidonic acid (AA)- and collagen-induced platelet aggregation.

(+)-Acuminatin exerts hepatoprotective activities, perhaps by serving as a potent antioxidant. (+)-trans-Acuminatin, and (+)-cis-acuminatin show weak activity against platelet aggregation with IC50 values of 108.5 and 90.02 uM, respectively. (+)-Acuminatin, and machilin G show dose-dependent potent inhibitory activities against PLCgamma1 in vitro with IC50 values ranging from 8.8 to 26.0 microM, the inhibition of PLCgamma1 may be an important mechanism for an antiproliferative effect on the human cancer cells, therefore, these inhibitors may be utilized as cancer chemotherapeutic and chemopreventive agents.

Myrianthic acid shows anticancer activity, it shows inhibitory activities on foam cell formation in human monocyte-derived macrophages induced by acetylated low-density lipoproteins at a 50 uM concentration. Myrianthic acid is equivalently inhibitive as acetylsalicylic acid (IC50: 57.0 microM) on epinephrine induced platelet aggregation.

β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)

2-Hydroxy-3-methoxybenzoic acid glucose ester shows a potent antagonistic activity against platelet activating factor (PAF), it can prevent the mice from the PAF-induced death at a dose of 300 micrograms/mouse.

6-Acetyl-2,2-dimethylchroman-4-one and vanillin show anti-platelet aggregation activity induced by arachidonic acid in vitro.

Piperlotine C shows potent antiplatelet aggregation activity.

Kadsulignan L shows in vitro antiviral effects on hepatitis B virus. It also shows moderate platelet-activating factor (PAF) antagonistic activities with the IC50 value of 2.6 x 10(-5) M.

PAF-AN-1 is a novel potent platelet-activating factor receptor (PAF) antagonist involved in the study of anaphylactic death.

6-Deoxyjacareubin exhibits potent antioxidant and antifungal activities. 6-Deoxyjacareubin inhibits platelet activating factor (PAF) receptor with an IC50 of 29.0 microM and can be used in studies about natural PAF receptor antagonists.

1-Methoxyphaseollidin exhibits anti-Helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains. 1-Methoxyphaseollidin may show moderate cytotoxic activity against KB and L1210 cells. 1-Methoxyphaseollidin also shows inhibition of lysoPAF acetyltransferase activity.

Futoenone and a series of its derivatives have shown inhibitory activities against matrix metalloproteinases, the molecular modelings of these compounds indicate the preferred binding of the P2' site of the enzymes. Neolignan derivative compounds of the 2,4-diaryl-1,3-dithiolane and futoenone variety exhibit both platelet activating factor receptor(PAF)and 5-lipoxygenase antagonist activity.

Niranthin is a potent anti-leishmanial agent, inhibits the relaxation activity of heterodimeric type IB topoisomerase of L. donovani and acts as a non-competitive inhibitor interacting with both subunits of the enzyme. Niranthin also exhibits anti-hepatitis B virus, antiinflammatory and antiallodynic actions.

Rupatadine Fumarate (Rinialer) (UR-12592 Fumarate) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM.

Zingiberen newsaponin is a steroidal saponin from Dioscorea zingiberensis.

Epiyangambin is a phytotoxic lignan, it shows inhibition of seed germination of Agrostis stolonifera cv. penncross (Poaceae) and inhibition of development of Lactuca sativa L. (Asteraceae) seedlings in a microassay using 24-well plates. Epiyangambin exhibits significant inhibition of the transformation of murine epidermal JB6 cells, with the IC50 value of 0.15 microg/mL. (+)-Epiyangambin also has anti-platelet aggregation activity.

Spiradine F can significantly inhibit platelet-activating factor(PAF)-induced platelet aggregation in a concentration-dependent manner.

CV-6209 is a selective and potent platelet-activating factor (PAF) antagonist with antiproliferative effects, partial inhibition of acetylcholine-induced hypotension, and inhibition of Paf-induced PMN or platelet aggregation.CV-6209 has an antiplasmodial effect against Helicobacter pylori, and can inhibit PAF-induced hypotension in rats.

Pinusolidic acid shows a potent inhibitory effect on platelet activating factor (PAF) binding to rabbit platelets (IC50 = 2.3 x 10(-5) M, 7.48 +/- 2.11 micrograms/ml).

Piperlotine D shows potent antiplatelet aggregation activity.

Aristolactam BIII possesses anti-platelet aggregation activity in vitro, it also shows significant cytotoxic activity (IC50 values < 4 microg/mL) against P-388, HT-29 and A549 cell lines in vitro.

Yangambin is a selective antagonist of the cardiovascular effects of platelet activating factor (PAF); it has hypotensive effect, which is probably due to a peripheral vasodilatation that involves, at least, the inhibition the Ca2+ influx through voltage-gated Ca2+ channels. Yangambin also has central nervous system activity.

Piperenone is an insect antifeeding substance. It has anti-platelet-activating factor(PAF) activities, is a PAF-acether antagonist.